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Bakhshaee, Mehdi, Farahzad Jabbari, Saeed Hosseini, Reza Farid Hossaini, and Mohammad Hadi Sadeghian. "Additive Effect of Silymarine in Allergic Rhinitis Treatment." Otolaryngology–Head and Neck Surgery 143, no. 2_suppl (2010): P123. http://dx.doi.org/10.1016/j.otohns.2010.06.695.
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Amala, K., R. Ilavarasan, R. Arunadevi, and S. Amerjothy. "HEPATOPROTECTIVE EVALUATION OF EPALTES DIVARICATA (L.) CASS. WHOLE PLANT EXTRACTS AGAINST PARACETAMOL-INDUCED HEPATOTOXICITY IN RATS." International Journal of Pharmacy and Pharmaceutical Sciences 8, no. 12 (2016): 231. http://dx.doi.org/10.22159/ijpps.2016v8i12.14951.
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<p><strong>Objective: </strong>The plant of <strong><em>Epaltes</em></strong><strong> <em>divaricata </em>(L.) </strong>Cass.<strong> Traditionally used for jaundice. </strong>The present work aimed to investigate the hepatoprotective activity of alcohol and aqueous extract of the whole plant against paracetamol-induced hepatotoxicity in rats to substantiate its traditional use.</p><p><strong>Methods: </strong>The alcohol and aqueous (200 and 400 mg/kg) extract of <em>Epaltes divaricata</em> prepared by cold maceration were administered orally to the animals with hepatotoxicity induced by paracetamol (1000 mg/kg). Silymarine (40 mg/k) was given as reference standard. Hepatoprotective activity was assessed by estimating marker enzymes and by histopathological studies.</p><p><strong>Results: </strong>Both alcohol and aqueous (200 and 400 mg/kg) extract treatment significantly restored the paracetamol-induced elevations in levels of serum enzymes aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphate (ALP) and total bilirubin in a dose-dependent manner. Histopathological examination revealed that the treatment attenuated the paracetamol-induced damage to the liver. The hepatoprotective effect of both extracts was comparable to that of the standard hepatoprotective agent, silymarin.</p><p><strong>Conclusion: </strong>The alcohol and aqueous extract of <em>E. divaricata</em> exhibited hepatoprotective effect against paracetamol-induced liver damage in rats. This study also validated their traditional medicinal use in jaundice.</p>
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Boyer, Jean-Christophe, Francois Hernandez, Jacques Estorc, Jean-Emmanuel De La Coussaye, and Jean-Pierre Bali. "Management of Maternal Amanita phalloı̈des Poisoning during the First Trimester of Pregnancy: A Case Report and Review of the Literature." Clinical Chemistry 47, no. 5 (2001): 971–74. http://dx.doi.org/10.1093/clinchem/47.5.971.
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Abstract Background: Amanita phalloı̈des poisoning produces acute liver failure and often death. Maternal poisonings are rare, and medical decisions of abortion or liver transplantation in this critical situation frequently are based on laboratory data. We report here the case of a 22-year-old-woman in the 11th week of pregnancy, who ingested mushrooms. Case Report: The patient’s clinical symptoms (e.g., vomiting and diarrhea) and blood chemistry data (persistent increases of aspartate aminotransferase and alanine aminotransferase and severe decreases in prothrombin, factor V, factor II, factor VII, and factor X) indicated poisoning of medium severity. The management consisted of intravenous hydration, and administration of silymarine and N-acetylcysteine. No fetal damage was observed, and birth and development of the infant (now 2 years of age) proceeded without incident. Conclusion: Abortion is not necessarily indicated in maternal poisoning by A. phalloı̈des, even in the first trimester of pregnancy.
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Murukan, Greeshma, S. S. Sumayya, J. M. Aswathy, Bosco Lawarence, and K. Murugan. "VALIDATION OF HEPATOPROTECTIVE AND ANTIOXIDANT ACTIVITY OF FOLK LORE KNOWLEDGE OF PURIFIED ANTHOCYANIN FROM CELL SUSPENSION CULTURE OF CLERODENDRON INFORTUNATUM L.: A SEARCH." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 12 (2017): 37. http://dx.doi.org/10.22159/ijpps.2017v9i12.20042.
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ABSTRACT Objective: To validate the hepatoprotective and antioxidant activity of purified anthocyanin extracted from the cell suspension culture of Clerodendron infortunatum Linn. Methods: A protocol has been developed for the induction of callus proliferation from leaf and nodal explants of C. infortunatum. The explants were inoculated on MS medium supplemented with diverse combinations of 2,4-D and BAP for triggering callus formation. Subsequently, the green compact callus has been sub-cultured in the medium fortified with 2,4-D and Kinetin for anthocyanin synthesis. Cell suspension culture was also established and the elicitor, salicylic acid was used for triggering anthocyanin synthesis. Three different chromatographic columns (solid phase extraction by Sepharose C18 column, Oasis-MCX and Amberlite XAD 7 + Sephadex LH 120 sorbents) were employed to purify the in vitro synthesized anthocyanin from cell suspension cultures. For purity evaluation HPLC and molar absorptivity assay were used. Further, hepatoprotective and antioxidant activity was evaluated comparing with silymarine, as standard in rats. In vitro antioxidant scavenging activity was analysed by DPPH, FRAP and ORAC assay.Results: After 1 month, the leaf explants yielded remarkable green compact callus on MS medium containing 2.0 mg/l BAP and 0.5 mg/l 2,4-D. Salicylic acid enhanced anthocyanin synthesis. The mean purity values obtained by HPLC were 90.9% ± 1.9 and 80.60% ±2.3 for Oasis MCX, Amberlite XAD-7 + Sephadex LH-20 column respectively. However, the purity calculated by molar absorptivity was found to be less. The highest purity achieved using molar absorptivity analysis was with MCX cartidges i.e., 85.9 ± 3.8%. HPLC yielded 12 anthocyanin fractions. Remarkable antioxidant scavenging activity was noticed as revealed by DPPH, FRAP and ORAC assay. The hepatoprotection activity (25, 50, 100 mg/100g b.w) was compared with silymarine (25 mg/kg b.w) against CCl4 induced toxicity. Anthocyanin extract improved the AST, ALT and recovered the activity of kidney function by decreasing the urea and creatinine content. In addition, the administration of anthocyanin significantly inhibited the oxidative stress via its scavenging of the reactive oxygen species formed by CCl4 stress. Further, a decrease in the MDA, H2O2, NO accumulation and increase of GSH content were noticed. Similarly, improved lipid profiles, LDL and HDL levels were also observed suggesting that anthocyanin significantly suppress the toxicity via its activation of antioxidant enzymes (GST, CAT and SOD).Conclusion: The overall results showed that the purified anthocyanin of C. infortunatum function as an antioxidant and there by hepatoprotective protection against CCl4 inducedtoxicity in animal models.
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Shutov, D. V. "Heparprotective effect of Bergenia crassifolia extract and silymarinat experimental inhibition of β-oxidation of fatty acids causedby 4-pentenioc acid". Bulletin of Siberian Medicine 6, № 4 (2007): 64–70. http://dx.doi.org/10.20538/1682-0363-2007-4-64-70.
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The object of this research was to study rat liver bioenergetics at pathology caused by inhibition of β-oxidation of fatty acids against the background of 4-pentenoic acid injection and at silymarin and Bergenia crassifolia extract therapy. The experiment was conducted with 50 nonpedigreed male rats. The functional state of the energy production system was estimated by the polarogaphic method from the rate of oxygen consumption in different Chans metabolic states. At silymarin therapy, increase was observed in the oxidative phosphorylation coupling in all metabolic states. The Bergenia crassifolia extract favored normalization of energy production parameters in rat liver mitochondria more efficiently than silymarint did.
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Quaglia, M. G., E. Bossù, E. Donati, G. Mazzanti, and A. Brandt. "Determination of silymarine in the extract from the dried silybum marianum fruits by high performance liquid chromatography and capillary electrophoresis." Journal of Pharmaceutical and Biomedical Analysis 19, no. 3-4 (1999): 435–42. http://dx.doi.org/10.1016/s0731-7085(98)00231-3.
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El-Sheshtawy, Sahar M., Amal F. El-Zoghby, Nesreen A. Shawky, and Dalia H. Samak. "Aflatoxicosis in Pekin duckling and the effects of treatments with lycopene and silymarin." March-2021 14, no. 3 (2021): 788–93. http://dx.doi.org/10.14202/vetworld.2021.788-793.
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Background and Aim: Aflatoxins (AFs) are potent toxic metabolites produced from Aspergillus species. Whose existence in poultry ration leads to drastic economic losses, notably in duck, as the most susceptible poultry species. This study aimed to determine tissue residues of AFs, alterations in selected clinical chemistry variables in serum, mainly during the exposure period, and lycopene and silymarin's possible roles as herbal treatments against aflatoxicosis in Pekin duckling. Materials and Methods: The study used one hundred and twenty one-day-old Pekin ducklings and classified them into four groups comprising 30 ducklings in each group. The control group (G1) ducklings were fed a mycotoxin-free ration, and G2 received a naturally contaminated ration with 30 ppb of AFs. G3 and G4 consumed contaminated rations with AFs with 30 ppb for 2 weeks and were treated with lycopene 100 mg/kg or silymarin 600 mg/kg/food, respectively, for 10 days. Serum activities of alanine transaminase and alkaline phosphatase (ALP), glutamyl transferase, ALP, total protein and albumin creatinine and uric acid concentrations, oxidant/antioxidant parameters (malondialdehyde [MDA], total antioxidant capacity (TAC), glutathione S-transferase (GST), and catalase [CAT]), and hepatic AFs residue were determined. Lycopene and silymarin were used for the treatment of aflatoxicosis for another 10 days. Results: Hepatic and kidney parameters were elevated in the AFs intoxicated group and reduced in the lycopene- and silymarin-treated groups. They had elevated MDA and AFs residues with decreased antioxidant parameters (TAC, GST, and CAT) in the AFs group. At the same time, treatment with lycopene or silymarin had reversed the action of AFs on MDA, elevated the hepatic residue, and improved antioxidant activity. Conclusion: Lycopene and silymarin, with their potent antioxidant activity, can be used to reverse the harmful effects of AFs on hepatic and kidney tissue.
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Song, Im-Sook, So-Jeong Nam, Ji-Hyeon Jeon, Soo-Jin Park, and Min-Koo Choi. "Enhanced Bioavailability and Efficacy of Silymarin Solid Dispersion in Rats with Acetaminophen-Induced Hepatotoxicity." Pharmaceutics 13, no. 5 (2021): 628. http://dx.doi.org/10.3390/pharmaceutics13050628.
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We evaluated the bioavailability, liver distribution, and efficacy of silymarin-D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) solid dispersion (silymarin-SD) in rats with acetaminophen-induced hepatotoxicity (APAP) compared with silymarin alone. The solubility of silybin, the major and active component of silymarin, in the silymarin-SD group increased 23-fold compared with the silymarin group. The absorptive permeability of silybin increased by 4.6-fold and its efflux ratio decreased from 5.5 to 0.6 in the presence of TPGS. The results suggested that TPGS functioned as a solubilizing agent and permeation enhancer by inhibiting efflux pump. Thus, silybin concentrations in plasma and liver were increased in the silymarin-SD group and liver distribution increased 3.4-fold after repeated oral administration of silymarin-SD (20 mg/kg as silybin) for five consecutive days compared with that of silymarin alone (20 mg/kg as silybin). Based on higher liver silybin concentrations in the silymarin-SD group, the therapeutic effects of silymarin-SD in hepatotoxic rats were evaluated and compared with silymarin administration only. Elevated alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase levels were significantly decreased by silymarin-SD, silymarin, and TPGS treatments, but these decreases were much higher in silymarin-SD animals than in those treated with silymarin or TPGS. In conclusion, silymarin-SD (20 mg/kg as silybin, three times per day for 5 days) exhibited hepatoprotective properties toward hepatotoxic rats and these properties were superior to silymarin alone, which may be attributed to increased solubility, enhanced intestinal permeability, and increased liver distribution of the silymarin-SD formulation.
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Petrie, Michaela, Gerry McKay, and Miles Fisher. "Silymarin." Practical Diabetes 32, no. 4 (2015): 148–50. http://dx.doi.org/10.1002/pdi.1945.
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Ashraf, Aya, Passant A. Mahmoud, Haidy Reda, et al. "Silymarin and silymarin nanoparticles guard against chronic unpredictable mild stress induced depressive-like behavior in mice: involvement of neurogenesis and NLRP3 inflammasome." Journal of Psychopharmacology 33, no. 5 (2019): 615–31. http://dx.doi.org/10.1177/0269881119836221.
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Background: The neuropathology of depression is quite complex. Thus, treatment failures are frequent with current antidepressants, raising the need for more effective ones. Aims: This study aimed to investigate the influence of silymarin on depressive-like behavior induced by chronic unpredictable mild stress (CUMS) and explore the underlying mechanisms. Methods: Silymarin was formulated as nanostructured lipid carriers (a lipid-based type of nanoparticle with the advantages of physical stability, good release profile, and targeted delivery). Mice were subjected to CUMS paradigm during 14 days. During this period, mice received silymarin (200 mg/kg, p.o.) per se or in its nanoparticle form or fluoxetine (10 mg/kg, p.o.). On the 15th day behavioral and biochemical parameters were analyzed. Results: Oral administration of silymarin (200 mg/kg), particularly in its nanoparticulate form, exerted an antidepressant-like effect, comparable with fluoxetine in mice, as demonstrated in the behavioral despair tests. Silymarin also reversed prefrontal cortical and hippocampal CUMS-induced oxidative stress and neuroinflammation. Furthermore, silymarin augmented neurotransmitter levels, enhanced neurogenesis and inhibited nod-like receptor protein 3 inflammasome activation. Silymarin nanoparticles were superior to silymarin in certain parameters probably due to significantly higher brain silybinin (the major active component of silymarin) concentration by 12.46 fold in the group administered silymarin nanoparticles compared with the mice which were administered silymarin per se. Conclusions: The antidepressant-like effect of silymarin can be attributed to its antioxidant and anti-inflammatory effects as well as increased neurogenesis in the prefrontal cortex and hippocampus, which delineates silymarin, especially in nanoparticle form, as a promising strategy for treatment of depression.
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Yurtcu, E., ÖD İşeri, and FI Sahin. "Genotoxic and cytotoxic effects of doxorubicin and silymarin on human hepatocellular carcinoma cells." Human & Experimental Toxicology 33, no. 12 (2014): 1269–76. http://dx.doi.org/10.1177/0960327114529453.
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The aim of this study was to investigate genotoxic and cytotoxic effects of doxorubicin, silymarin, or in combination on HepG2 cells for 24 and 48 h. Both doxorubicin and silymarin caused dose-dependent inhibition of cell proliferation. After 48 h of treatment, doxorubicin application caused dramatically increased ratio of apoptotic cells. Both 24 and 48 h of silymarin and doxorubicin–silymarin combination caused significant increases in the rate of apoptotic cells. Applications of doxorubicin and silymarin separately for 24 h led to deoxyribonucleic acid (DNA) damages. After 48 h of incubation, doxorubicin-induced genotoxic damage was 2-fold higher than the silymarin-induced damage. After 24 and 48 h, DNA damage in response to combined applications of doxorubicin and silymarin was indifferent from silymarin- and doxorubicin-induced damage respectively. There was not any difference in genotoxicity levels between incubation periods in combined applications of doxorubicin and silymarin. Lipid peroxidation levels increased in all applications. Biopharmacotherapy with chemotherapeutic agents are of interest in the issue of adjuvant therapy. Here, we demonstrate in vitro potential genotoxic and cytotoxic antitumor effect of silymarin on HepG2 cells at achievable plasma level concentrations.
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Yang, Zongguo, Liping Zhuang, Yunfei Lu, Qingnian Xu, and Xiaorong Chen. "Effects and Tolerance of Silymarin (Milk Thistle) in Chronic Hepatitis C Virus Infection Patients: A Meta-Analysis of Randomized Controlled Trials." BioMed Research International 2014 (2014): 1–9. http://dx.doi.org/10.1155/2014/941085.
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Objective. This study aimed to evaluate the efficacy and safety of silymarin on chronic hepatitis C virus- (HCV-) infected patients.Methods. Randomized controlled trials (RCTs) of silymarin in chronic HCV-infected patients up to April 1, 2014 were systematically identified in PubMed, Ovid, Web of Science, and Cochrane Library databases.Results.A total of 222 and 167 patients in five RCTs were randomly treated with silymarin (or intravenous silibinin) and placebo, respectively. Serum HCV RNA relatively decreased in patients treated with silymarin compared with those administered with placebo, but no significance was found (P=0.09). Meta-analysis of patients orally treated with silymarin indicated that the changes of HCV RNA are similar in the two groups (P=0.19). The effect on alanine aminotransferase (ALT) of oral silymarin is not different from that of placebo (P=0.45). Improvements in quality-of-life (Short Form-36) in both silymarin and placebo recipients were impressive but relatively identical (P=0.09).Conclusion. Silymarin is well tolerated in chronic HCV-infected patients. However, no evidence of salutary effects of oral silymarin has yet been reported based on intermediate endpoints (ALT and HCV RNA) in this population. Moreover, intravenous administration of silymarin should be further studied.
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Won, Dong-Hoon, Lee-Han Kim, Boonsil Jang, et al. "In vitro and in vivo anti-cancer activity of silymarin on oral cancer." Tumor Biology 40, no. 5 (2018): 101042831877617. http://dx.doi.org/10.1177/1010428318776170.
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Silymarin, a standardized extract from milk thistle fruits has been found to exhibit anti-cancer effects against various cancers. Here, we explored the anti-cancer activity of silymarin and its molecular target in human oral cancer in vitro and in vivo. Silymarin dose-dependently inhibited the proliferation of HSC-4 oral cancer cells and promoted caspase-dependent apoptosis. A human apoptosis protein array kit showed that death receptor 5 may be involved in silymarin-induced apoptosis, which was also shown through western blotting, immunocytochemistry, and reverse transcription-polymerase chain reaction. Silymarin increased cleaved caspase-8 and truncated Bid, leading to accumulation of cytochrome c. In addition, silymarin activated death receptor 5/caspase-8 to induce apoptotic cell death in two other oral cancer cell lines (YD15 and Ca9.22). Silymarin also suppressed tumor growth and volume without any hepatic or renal toxicity in vivo. Taken together, these results provide in vitro and in vivo evidence supporting the anti-cancer effect of silymarin and death receptor 5, and caspase-8 may be essential players in silymarin-mediated apoptosis in oral cancer.
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Kim, Jung-Lye, Sin-Hye Park, Daewon Jeong, Ju-Suk Nam, and Young-Hee Kang. "Osteogenic activity of silymarin through enhancement of alkaline phosphatase and osteocalcin in osteoblasts and tibia-fractured mice." Experimental Biology and Medicine 237, no. 4 (2012): 417–28. http://dx.doi.org/10.1258/ebm.2011.011376.
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Bone-remodeling imbalance induced by increased bone resorption and osteoclast formation is known to cause skeletal diseases such as osteoporosis. There has been growing interest in the anabolic natural agents that enhance bone formation. Silymarin is flavonolignans extracted from blessed milk thistle. Several studies suggest that silymarin possesses antihepatotoxic properties and anticancer effects against carcinoma cells. This study investigated promoting effects of silymarin on differentiation and mineralization of osteoblastic MC3T3-E1 mouse cells and on bone mineral density (BMD) by in vivo fracture experiments. Osteoblasts were treated with 1–20 μmol/L silymarin for 15 days in a differentiating medium. In addition, this study explored signaling pathways implicated in the osteoblastogenesis of silymarin. It was found that silymarin stimulated alkaline phosphatase (ALP) activity and calcium nodule formation in a dose-dependent manner with a substantial effect on osteoblast proliferation. Silymarin treatment enhanced collagen secretion, osteocalcin transcription and bone morphogenetic protein (BMP) expression. The BMP inhibitor noggin suppressed the silymarin-promoted ALP activity in differentiated osteoblasts, suggesting that its osteoblastogenic actions entail the BMP pathway. This was proved by increased SMAD1/5/8 phosphorylation and runt-related transcription factor 2 (Runx2) expression in the presence of silymarin. In 21-day fracture-healing experiments, fractured and silymarin (10 mg/kg)-treated C57BL/6 mice showed better bone healing than fractured mice. Silymarin supplementation improved tibial bone strength with elevated BMD and serum levels of osteogenic ALP and osteocalcin. Taken together, these results demonstrate, for the first time, that silymarin has a potential to enhance osteoblastogenesis through accelerating BMP/SMAD/Runx2 signal pathways and to improve fracture healing and bone strength in mouse tibiae.
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Jiang, Hui-Hui, Fa-Shun Yan, Liang Shen, and Hong-Fang Ji. "Silymarin versus Silibinin: Differential Antioxidant and Neuroprotective Effects against H2O2-induced Oxidative Stress in PC12 Cells." Natural Product Communications 11, no. 5 (2016): 1934578X1601100. http://dx.doi.org/10.1177/1934578x1601100520.
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The present study assessed comparatively the antioxidant activities of silymarin and its major active component silibinin and their neuroprotective effects against hydrogen peroxide (H2O2)-induced oxidative stress in rat pheochromocytoma PC12 cells. It was found that despite newly prepared silymarin and silibinin solution possessing comparable superoxide anion (O2.–)-scavenging activities, with time the activity of silymarin lowered slightly, but that of silibinin decreased dramatically. Both silymarin and silibinin suppressed H2O2-induced oxidative stress and apoptosis, and the neuroprotective effect of silymarin was overall relatively stronger than that of silibinin. The findings provided clues for future studies on therapeutic potentials of the whole silymarin or purified silibinin for neurodegenerative diseases.
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Maryana, Wina, Annisa Rahma, Diky Mudhakir, and Heni Rachmawati. "Phytosome Containing Silymarin for Oral Administration: Formulation and Physical Evaluation." Journal of Biomimetics, Biomaterials and Biomedical Engineering 25 (October 2015): 54–65. http://dx.doi.org/10.4028/www.scientific.net/jbbbe.25.54.
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Silymarin is a unique flavonoid complex isolated from milk thistle (Silybum marianum). It has been widely used as a hepatoprotective agent. Orally administered silymarin can be absorbed rapidly but only 20-50% of silymarin will be absorbed through gastrointestinal tract, resulting in low bioavailability. Those limitations are due to its low solubility, either in water and oil, and its low intestinal permeability. This study was aimed to develop silymarin-containing phytosome in order to improve the bioavailability of silymarin with sufficient safety and stability. This system consisted of silymarin-phospholipid complex prepared by solvent evaporation method, which was incorporated to form phytosome vesicles using thin layer method with various concentrations and molar ratios of silymarin and phospholipid. The vesicle size of phytosome was reduced with sonication. The results demonstrated that formula with 2% silymarin-phospholipid complex and molar ratio of silymarin to phospholipid of 1:5 showed the best phytosomal characteristics, with mean vesicle diameter of 133.534 ± 8.76 nm, polidispersity index of 0.339 ± 0.078, entrapment efficiency of 97.169 ± 2.412 %, and loading capacity of 12.18 ± 0.30 %. The preparation remained stable after freeze-thaw stability test. Analysis of Infrared spectroscopy and Differential Scanning Calorimetry confirmed the presence of physical and chemical interactions between silymarin and phospholipid within complex formation. Well formed and discrete vesicles were revealed by Transmission Electron Microscopy analysis, drug content measurement, and freeze-thaw stability test.
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Lalani, Salima, Malihe Masomian, and Chit Laa Poh. "Functional Insights into Silymarin as an Antiviral Agent against Enterovirus A71 (EV-A71)." International Journal of Molecular Sciences 22, no. 16 (2021): 8757. http://dx.doi.org/10.3390/ijms22168757.
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Enterovirus A71 (EV-A71) is a major neurovirulent agent capable of causing severe hand, foot and mouth disease (HFMD) associated with neurological complications and death. Currently, no FDA-approved antiviral is available for the treatment of EV-A71 infections. The flavonoid silymarin was shown to exert virucidal effects, but the binding site on the capsid was unknown. In this study, the ligand interacting site of silymarin was determined in silico and validated in vitro. Moreover, the potential of EV-A71 to develop resistance against silymarin was further evaluated. Molecular docking of silymarin with the capsid of EV-A71 indicated that silymarin binds to viral protein 1 (VP1) of EV-A71, specifically at the GH loop of VP1. The in vitro binding of silymarin with VP1 of EV-A71 was validated using recombinant VP1 through ELISA competitive binding assay. Continuous passaging of EV-A71 in the presence of silymarin resulted in the emergence of a mutant carrying a substitution of isoleucine by threonine (I97T) at position 97 of the BC loop of EV-A71. The mutation was speculated to overcome the inhibitory effects of silymarin. This study provides functional insights into the underlying mechanism of EV-A71 inhibition by silymarin, but warrants further in vivo evaluation before being developed as a potential therapeutic agent.
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Vecera, R., A. Zacharova, J. Orolin, N. Skottova, and P. Anzenbacher. " The effect of silymarin on expression of selected ABC transporters in the rat." Veterinární Medicína 56, No. 2 (2011): 59–62. http://dx.doi.org/10.17221/1579-vetmed.
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Silymarin (standardized extract from the seeds of the Silybum marianum) has been used in the supportive therapy of liver diseases and its cytoprotective activity is believed to be based on antioxidant properties. Our previous works showed hypolipidemic effects of silymarin. The ATP-binding cassette (ABC) transporters G5 and G8 play a major role in biliary cholesterol secretion. The ABCA1 transporter plays a significant role in movement of cellular cholesterol to high density lipoproteins. We investigated the possibility that silymarin affects the regulation of lipid metabolism via selected ABC transporters using rats fed a high-cholesterol diet with silymarin. The major finding in this study is that silymarin up-regulated mRNA of ABC transporters (G5, G8 and A1). This result suggests that silymarin positively affects the plasma lipoprotein profile via up-regulation of ABC transporters involved in lipid metabolism. Furthermore, this study shows for the first time that silymarin up-regulates the expression of these ABC transporters at the mRNA level.
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Lu, Suli, Jun Zhang, and Yue Wang. "Silymarin Inhibits Proliferation and Induces Apoptosis in Epstein-Barr Virus-Positive Lymphoma Cells by Suppressing Nuclear Factor-Kappa B�Pathway." Current Topics in Nutraceutical Research 18, no. 4 (2020): 348–53. http://dx.doi.org/10.37290/ctnr2641-452x.18:348-353.
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Epstein Barr virus-positive lymphoma results from the loss of homeostatic balance between Epstein Barr virus and immune cells. In this study, we investigated the mechanism underlying reduction in Epstein Barr virus-positive lymphoma cell proliferation and apoptosis by silymarin, an anti-inflammatory/antioxidant molecule extracted from Silybum�marianum (milk thistle). We examined the effect of silymarin on Raji cell proliferation, apoptosis, the expression of latent membrane protein�1, the proteins related to apoptosis, and the activation of nuclear factor kappa-B. Results showed that silymarin inhibited the proliferation and promoted apoptosis of Raji cells in a concentration-dependent manner. Also, silymarin reduced phosphorylated inhibitor of nuclear factor kappa-B and p65 levels. Silymarin treatment elevated latent membrane protein 1 expression and knockdown of this protein led to increased proliferation inhibition and apoptosis by silymarin. In conclusion, nuclear factor kappa-B and latent membrane protein 1 knockdown could work in concert with silymarin in suppressing Epstein Barr virus-positive lymphoma cell proliferation and inducing apoptosis.
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Gardouh, Ahmed, Sherif Shaker, Zainab Z. Ali, and Mamdouh Ghorab. "Silymarin Spray-Dried Proliposomes: Preparation, Characterization and Cytotoxic Evaluation." Drug Delivery Letters 10, no. 1 (2020): 14–23. http://dx.doi.org/10.2174/2210303109666190722114211.
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Background: Most liposomes problems are due to stability and consistency. Proliposomes is one of the solutions to overcome the disadvantage of liposomes. They are available in dry powder form, it is easy to distribute, transfer, measure and store. Objective: The aim of the present study was to find a novel method of preparing Silymarin proliposomes and study the effect of cholesterol concentrations and surfactant types on the physicochemical properties of silymarin proliposomes and its in-vitro release. Methods: Silymarin proliposomes were prepared by combining two simple methods ethanol injection method for liposomes preparation followed by the spray drying method to get a dry powder. The physicochemical properties including particle size, TEM, SEM, FTIR, encapsulation efficiency and dissolution studies were studied. Results: The particle size of silymarin liposomes were below 552.36 ± 17.63 nm but after reconstitution of silymarin proliposomes, the particle size was in the micro range due to the influence of the spray drying process. Cholesterol concentration was ranged from 50 to 150 mg per formula. Increasing Cholesterol concentration caused a significant increase in liposomes particle size and reduction in encapsulation efficiency. Three non-ionic surfactants were used to prepare silymarin proliposomes Tween 80, Cremophor RH 40 and Poloxamer 407. Formula F1 prepared with Phosal® 53 MCT (300 mg), Tween 80 (50 mg), cholesterol (50 mg) and Silymarin (140 mg) showed the smallest particle size (2066 ± 164.87 nm) upon reconstitution in water, highest encapsulation efficiency (89.51 ± 0.43%), and fastest in vitro release compared to other formulas. Cytotoxicity of Silymarin, formula F1 and formula F1/blank was assessed using an MTT assay on MCF-7, HepG2 and HBF-4 cells. The cytotoxic effect of silymarin was enhanced by loading it on proliposomes. Conclusion: Silymarin was successfully formulated into proliposomes combining ethanol injection and spray drying methods. The cytotoxicity of silymarin was improved when loaded on proliposomes owing to the formula.
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M., Janakiraman. "PROTECTIVE EFFICACY OF SILVER NANOPARTICLES SYNTHESIZED FROM SILYMARIN ON CISPLATIN INDUCED RENAL OXIDATIVE STRESS IN ALBINO RAT." International Journal of Applied Pharmaceutics 10, no. 5 (2018): 110. http://dx.doi.org/10.22159/ijap.2018v10i5.28023.
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Objective: This present study was carried out to evaluate the protective efficacy of silver nanoparticles synthesized from silymarin on cisplatin-induced renal oxidative stress in the albino rat.Methods: Silver nanoparticles of silymarin was characterized by particle size, UV-Visible, FTIR and XRD analysis. Albino rats were divided randomly into six groups of six animals each. Group I Normal rats were treated with an oral dose of distilled water for 15 d. Group II rats were treated with single i. p. dose of cisplatin (16 mg/kg) on day 1. Group III rats were treated only with oral dose of silymarin (50 mg/kg/d) for 15 d. Group IV rats were treated only with oral dose of silver nanoparticles of silymarin (50 mg/kg/d) for 15 d. Group V rats were treated with an oral dose of silymarin for 14 d after single i. p. dose of cisplatin on day 1. Group VI rats were treated with oral dose of silver nanoparticles of silymarin for 14 d after single i. p. dose of cisplatin on day 1. Collected blood samples and kidney tissue samples were used for biochemical, enzymatic antioxidant and histopathological studies in all groups.Results: The formation of silver nanoparticles of silymarin were confirmed by particle size, UV-Visible analysis, crystalline nature was confirmed by X-ray diffraction analysis, and active principles were confirmed by FTIR analysis. Biochemical results of silver nanoparticles of silymarin-treated groups showed the significant (p˂0.05) decrease in the level of creatinine, urea, and uric acid as compared to cisplatin-induced rats and The enzymatic antioxidants of silver nanoparticles of silymarin-treated groups showed the significant (p˂0.05) increase in the level of glutathione reductase and significant decrease in MDA level as compared to cisplatin-induced rats. Additionally, histopathological results of silver nanoparticles of silymarin-treated groups also confirmed that the ameliorative effect of silymarin nanoparticle against cisplatin-induced rats.Conclusion: From this research work, we have concluded that silver nanoparticles of silymarin protected the kidney of albino rats from the adverse effects caused by cisplatin.
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Tao, Lina, Xiaoyu Qu, Yue Zhang, Yanqing Song, and Si-xi Zhang. "Prophylactic Therapy of Silymarin (Milk Thistle) on Antituberculosis Drug-Induced Liver Injury: A Meta-Analysis of Randomized Controlled Trials." Canadian Journal of Gastroenterology and Hepatology 2019 (January 10, 2019): 1–11. http://dx.doi.org/10.1155/2019/3192351.
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Background. Prophylactic therapy with silymarin to prevent the development of antituberculosis drug-induced liver injury (anti-TB DILI) has been under debate. We aimed to evaluate the effect of silymarin in the prevention of anti-TB DILI. Methods. We searched MEDLINE, PubMed, Embase, and Cochrane Central Register of Controlled Trials (CENTRAL) up to 30th November 2018. Randomized controlled trials (RCTs) that compared silymarin and placebo to prevent anti-TB DILI were included. All statistical analyses were conducted using STATA 12.0 software. Standardized mean difference (SMD) and risk ratio (RR) with 95% confidence intervals (CIs) were used to evaluate the effect of silymarin. The quality of included studies was assessed according to Cochrane handbook. Funnel plots and Egger’s tests were carried out to evaluate publication bias. Sensitivity analysis was conducted to assess the influence of each study. Results. A total of 1198 patients from five RCTs (585 with silymarin and 613 with placebo groups) were included. Overall, silymarin significantly reduced the occurrence of anti-TB DILI at week 4 [RR: 0.33, 95% CI (0.15, 0.75)]. In addition, silymarin exerted protective effect on liver function in patients undergoing anti-TB drugs [SMD = − 0.15, 95% CI (−0.24, −0.07), P < 0.001 (ALT); SMD =−0.14, 95% CI (−0.23, −0.06), P = 0.001(AST); SMD =−0.12, 95% CI (−0.20, −0.03), P = 0.008 (ALP)]. Silymarin led to similar AEs in placebo groups [OR: 1.09, 95% CI (0.86, 1.39), P = 0.47]. Conclusion. Prophylactic therapy of silymarin is contributed to a noticeably reduced risk of development of anti-TB DILI four weeks after the initiation. In addition, silymarin significantly improved the liver function in patients who are receiving anti-TB drugs.
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Petrásková, Káňová, Biedermann, Křen, and Valentová. "Simple and Rapid HPLC Separation and Quantification of Flavonoid, Flavonolignans, and 2,3-Dehydroflavonolignans in Silymarin." Foods 9, no. 2 (2020): 116. http://dx.doi.org/10.3390/foods9020116.
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Herbal preparations from Silybum marianum have been used since the fourth century BC in liver disease treatment and against numerous other pathologies. Consumption of silymarin containing drugs and food supplements continues to increase. Precise, fast, reliable, and complex determination of all components of silymarin preparations is paramount for assessing its pharmacological quality. We present here simple and fast HPLC-DAD and LC-MS analytical methods for the determination and quantification of all known silymarin components, including 2,3-dehydroflavonolignans that has not been achieved so far. The first method, using a common C18 column, allows baseline separation of previously inseparable silychristin A, B, isosilychristin, and silydianin. Moreover, this method allowed detection of three so far unknown silymarin components. In addition, the first analytical separation of enantiomers of 2,3-dehydrosilybin was achieved using a Lux 3μ Cellulose-4 chiral column, providing even more accurate description of silymarin composition. 2,3-Dehydroflavonolignans were isolated for the first time from silymarin using preparative chromatography on C18 and ASAHIPAK columns, and 2,3-dehydrosilychristin and 2,3-dehydrosilybin were for the first time conclusively confirmed by HPLC, MS, and NMR to be silymarin components. Using the optimized analytical methods, six various silymarin preparations were analyzed showing substantial differences in the composition.
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NASER, A. S., Y. ALBADRANY, and K. A. SHAABAN. "Isobolographic analysis of analgesic interactions of silymarin with ketamine in mice." Journal of the Hellenic Veterinary Medical Society 71, no. 2 (2020): 2171. http://dx.doi.org/10.12681/jhvms.23653.
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The present study was undertaken to explore the analgesic effect of silymarin and ketamine alone or in combination in mice. Analgesia was measured by using a hot plate and the writhing test. The up-and-down method was used to determine the median effective analgesic dosages (ED50s) of silymarin and ketamine administered intraperitoneally (ip) either alone or together. The ED50s of both drugs were analyzed isobolographically to determine the type of pharmacological interaction between them. The analgesic ED50s for silymarin and ketamine in mice were 57.22 and 1.96 mg/kg, ip, respectively. Concomitant administration of the silymarin and ketamine at fixed ration (0.5:0.5) of their individual ED50s was 38.4 mg/kg and 1.28 mg/kg, ip, respectively. Silymarin and ketamine at fixed ration (1:1) of their individual ED50s were 47.54 mg/kg and 1.58 mg/kg, ip, respectively . Depending on the isobolographic analysis and calculating Y value, the type of pharmacological interaction between silymarin and ketamine at a ratio of 0.5:0.5 and 1:1 of their analgesic ED50 values of each drug , was antagonistic .In the writhing test the concomitant administration of silymarin and ketamine at 120mg/kg and 4mg/kg , ip, respectively reduce significantly the numbers of writhing in compare with silymarin120 mg/kg,ip and ketamine 4mg/kg, ip separately. The results suggest that the co-administration of silymarin and ketamine was ineffective to reduce the central pain while the concomitant administration of silymarin and ketamine was effective to reduce the visceral pain.
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Matsuda, Takeru, Kevin Ferreri, Ivan Todorov та ін. "Silymarin Protects Pancreatic β-Cells against Cytokine-Mediated Toxicity: Implication of c-Jun NH2-Terminal Kinase and Janus Kinase/Signal Transducer and Activator of Transcription Pathways". Endocrinology 146, № 1 (2005): 175–85. http://dx.doi.org/10.1210/en.2004-0850.
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Silymarin is a polyphenolic flavonoid that has a strong antioxidant activity and exhibits anticarcinogenic, antiinflammatory, and cytoprotective effects. Although its hepatoprotective effect has been well documented, the effect of silymarin on pancreatic β-cells is largely unknown. In this study, the effect of silymarin on IL-1β and/or interferon (IFN)-γ-induced β-cell damage was investigated using RINm5F cells and human islets. IL-1β and/or IFN-γ induced cell death in a time-dependent manner in RINm5F cells. The time-dependent increase in cytokine-induced cell death appeared to correlate with the time-dependent nitric oxide (NO) production. Silymarin dose-dependently inhibited both cytokine-induced NO production and cell death in RINm5F cells. Treatment of human islets with a combination of IL-1β and IFN-γ (IL-1β+IFN-γ), for 48 h and 5 d, resulted in an increase of NO production and the impairment of glucose-stimulated insulin secretion, respectively. Silymarin prevented IL-1β+IFN-γ-induced NO production and β-cell dysfunction in human islets. These cytoprotective effects of silymarin appeared to be mediated through the suppression of c-Jun NH2-terminal kinase and Janus kinase/signal transducer and activator of transcription pathways. Our data show a direct cytoprotective effect of silymarin in pancreatic β-cells and suggest that silymarin may be therapeutically beneficial for type 1 diabetes.
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Milić, Nataša, Nataša Milošević, Ljiljana Suvajdžić, Marija Žarkov, and Ludovico Abenavoli. "New Therapeutic Potentials of Milk Thistle (Silybum marianum)." Natural Product Communications 8, no. 12 (2013): 1934578X1300801. http://dx.doi.org/10.1177/1934578x1300801236.
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Silymarin is a bioflavonoid complex extract derived from dry seeds of Milk thistle [( Silybum marianum(L.) Gaernt. (Fam. Asteraceae/Compositaceae)] whose hepatoprotective effect has clinically been proved. Low toxicity, favorable pharmacokinetics, powerful antioxidant, detoxifying, preventive, protective and regenerative effects and side effects similar to placebo make silymarin extremely attractive and safe for therapeutic use. The medicinal properties of silymarin and its main component silibinin have been studied in the treatment of Alzheimer's disease, Parkinson's disease, sepsis, burns, osteoporosis, diabetes, cholestasis and hypercholesterolemia. Owing to its apoptotic effect, without cytotoxic effects, silymarin possesses potential applications in the treatment of various cancers. Silymarin is being examined as a neuro-, nephro- and cardio-protective in the damage of different etiologies due to its strong antioxidant potentials. Furthermore, it has fetoprotective (against the influence of alcohol) and prolactin effects and is safe to be used during pregnancy and lactation. Finally, the cosmetics industry is examining the antioxidant and UV-protective effects of silymarin. Further clinical studies and scientific evidence that silymarin and silibinin are effective in the therapy of various pathologies are indispensable in order to confirm their different flavonolignan pharmacological effects.
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Gad, Dina, Hamed El-Shora, Daniele Fraternale, Elisa Maricchiolo, Andrea Pompa, and Karl-Josef Dietz. "Bioconversion of Callus-Produced Precursors to Silymarin Derivatives in Silybum marianum Leaves for the Production of Bioactive Compounds." International Journal of Molecular Sciences 22, no. 4 (2021): 2149. http://dx.doi.org/10.3390/ijms22042149.
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The present study aimed to investigate the enzymatic potential of Silybum marianum leaves to bioconvert phenolic acids produced in S. marianum callus into silymarin derivatives as chemopreventive agent. Here we demonstrate that despite the fact that leaves of S. marianum did not accumulate silymarin themselves, expanding leaves had the full capacity to convert di-caffeoylquinic acid to silymarin complex. This was proven by HPLC separations coupled with electrospray ionization mass spectrometry (ESI-MS) analysis. Soaking the leaf discs with S. marianum callus extract for different times revealed that silymarin derivatives had been formed at high yield after 16 h. Bioconverted products displayed the same retention time and the same mass spectra (MS or MS/MS) as standard silymarin. Bioconversion was achieved only when using leaves of a specific age, as both very young and old leaves failed to produce silymarin from callus extract. Only medium leaves had the metabolic capacity to convert callus components into silymarin. The results revealed higher activities of enzymes of the phenylpropanoid pathway in medium leaves than in young and old leaves. It is concluded that cotyledon-derived callus efficiently produces compounds that can be bio-converted to flavonolignans in leaves tissue of S. marianum.
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Fidrus, Ujhelyi, Fehér, et al. "Silymarin: Friend or Foe of UV Exposed Keratinocytes?" Molecules 24, no. 9 (2019): 1652. http://dx.doi.org/10.3390/molecules24091652.
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The application of natural plant extracts in UV-protection is popular and intensively studied. Silymarin (from Silibum marianum), a naturally occurring polyphenol, has recently received attention due to its antioxidant, anti-inflammatory and anti-apoptotic effects. However, its role in the UV-mediated keratinocyte cell response is still controversial. In this study, we investigated the effects of Silibum marianum extracts with different origins and formulations on UVA-exposed HaCaT keratinocytes in vitro. Our results show, that silymarin treatment caused an inverse dose-dependent photosensitivity relationship (at higher doses, a decrease in cell viability and ROS production) after UVA exposure. The attenuation of the UVA-induced ROS generation after silymarin treatment was also observed. Moreover, silymarin pre-treatment increased the cyclobutane pyrimidine dimer photolesions in keratinocytes after UVA exposure. These results indicated the dual role of silymarin in UVA-exposed keratinocytes. It scavenges ROS but still induces phototoxicity. Based on our results dermatological applications of silymarin and related compounds should be considered very carefully.
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A. El-Marasy, Salma A., Reham M. Abd-Elsalam, and Omar A. Ahmed-Farid. "Ameliorative Effect of Silymarin on Scopolamine-induced Dementia in Rats." Open Access Macedonian Journal of Medical Sciences 6, no. 7 (2018): 1215–24. http://dx.doi.org/10.3889/oamjms.2018.257.
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AIM: This study aims to elucidate the possible ameliorative effect of silymarin on scopolamine-induced dementia using the object recognition test (ORT) in rats.METHODS: The study was extended to demonstrate the role of cholinergic activity, oxidative stress, neuroinflammation, brain neurotransmitters and histopathological changes in the anti-amnestic effect of silymarin in demented rats. Wistar rats were pre-treated with silymarin (200, 400, 800 mg/kg) or donepezil (10 mg/kg) orally for 14 consecutive days. Dementia was induced after the last drug administration by a single intraperitoneal dose of scopolamine (16 mg/kg). Then behavioural, biochemical, histopathological, and immunohistochemical analyses were then performed.RESULTS: Rats pre-treated with silymarin counteracted scopolamine-induced non-spatial working memory impairment in the ORT and decreased acetylcholinesterase (AChE) activity, reduced malondialdehyde (MDA), elevated reduced glutathione (GSH), restored gamma-aminobutyric acid (GABA) and dopamine (DA) contents in the cortical and hippocampal brain homogenates. Silymarin reversed scopolamine-induced histopathological changes. Immunohistochemical analysis showed that silymarin mitigated protein expression of the glial fibrillary acidic protein (GFAP) and nuclear factor kappa-B (NF-κB) in the brain cortex and hippocampus. All these effects of silymarin were similar to that of the standard anti-amnestic drug, donepezil.CONCLUSION: This study reveals that the ameliorative effect of silymarin on scopolamine-induced dementia in rats using the ORT maybe in part mediated by, enhancement of cholinergic activity, anti-oxidant and anti-inflammatory activities as well as mitigation in brain neurotransmitters and histopathological changes.
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Viktorova, Jitka, Milena Stranska-Zachariasova, Marie Fenclova, et al. "Complex Evaluation of Antioxidant Capacity of Milk Thistle Dietary Supplements." Antioxidants 8, no. 8 (2019): 317. http://dx.doi.org/10.3390/antiox8080317.
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Numerous in vitro assays are used to characterize the antioxidant properties of natural-based matrices. However, many of them generate contradictory and non-compliant results. In our study, we focused on the characterization of traditionally used biochemical (2,2′-azino-bis-(3-ethylbenzothiazoline-6 sulfonic acid) (ABTS), Oxygen Radical Absorption Capacity (ORAC), and 2,2-diphenyl-1-picrylhydrazyl (DPPH)) and cellular (CAA) antioxidant tests on a broad set of milk thistle dietary supplements containing silymarin. In addition to 26 commercially available preparations, also the natural silymarin extract available from Sigma Aldrich, St. Louis, MI, USA, and a model mixture of pure flavonoid/flavonolignans mimicking the silymarin composition were investigated as control samples. Significant differences in the antioxidant capacity of the supplements were observed. Unlike the DPPH, the results of the ABTS and ORAC methods correlated with the silymarin components determined by U-HPLC-HRMS/MS. The responses in CAA were considerably lower than in other assays. Silymarin exhibited a significantly higher antioxidant capacity than the artificially prepared flavonoid/flavonolignans mixture in all tests, indicating possible presence of other antioxidants of natural origin. The follow-up U-HPLC-HRMS/MS screening revealed the presence of tens of non-silymarin compounds with reported antioxidant activity (not only in the silymarin extract, but also in the milk thistle preparations). The sum of the total phenolics and the sum of the simple phenolics correlated with CAA results more than silymarin.
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Fitzpatrick, Leo, Ella Mokrushin, George Talbott, and Tibebe Woldermariam. "In Vitro and Ex Vivo Effects of Silymarin Derivatives on Proinflammatory Cytokine Secretion Using a Murine Colonic Strip Model." Planta Medica International Open 5, no. 02 (2018): e55-e60. http://dx.doi.org/10.1055/a-0733-3716.
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AbstractSilymarin has anti-inflammatory properties and documented anti-colitis activity. Our prior study determined that in vitro treatment with certain extracted fractions of silymarin inhibited stimulated proinflammatory cytokine secretion from cell lines relevant to colitis. In this study, colitis was induced in mice by giving dextran sulfate sodium drinking water for 6 days. The ex vivo effects of crude silymarin extract, two different silymarin fractions, as well as commercially derived silibinin and isosilibinin were examined by determining the secretion of MIP-2, TNF-α, and IL-17 in cell culture media from colonic strips. Further, the effects of silymarin-derived treatments on IL-8 and TNF-α secretion induced by the colitis supernatant was characterized with HT-29 colonic epithelial and RAW 264.7 macrophage cell lines. Prominent inhibition of MIP-2 and TNF-α secretion from colonic strips of mice with/without dextran sulfate sodium-induced colitis was observed with various silymarin treatments. Further, inhibition of dual (IL-23+IL-1β) cytokine-stimulated secretion of IL-17 from colonic strips of mice was found with certain silymarin treatments. Significant attenuation of TNF-α secretion from colitis supernatant-stimulated RAW 264.7 cells was observed for crude silymarin extract and isosilibinin treatments. Finally, inhibition of IL-8 secretion from the colitis supernatant-stimulated HT29 colonic epithelial cell line was found with isosilibinin. These results contribute to the identification of silymarin-derived flavonoligans with optimal anti-inflammatory properties for further testing in colitis models.
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Delmas, Dominique, Jianbo Xiao, Anne Vejux, and Virginie Aires. "Silymarin and Cancer: A Dual Strategy in Both in Chemoprevention and Chemosensitivity." Molecules 25, no. 9 (2020): 2009. http://dx.doi.org/10.3390/molecules25092009.
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Silymarin extracted from milk thistle consisting of flavonolignan silybin has shown chemopreventive and chemosensitizing activity against various cancers. The present review summarizes the current knowledge on the potential targets of silymarin against various cancers. Silymarin may play on the system of xenobiotics, metabolizing enzymes (phase I and phase II) to protect normal cells against various toxic molecules or to protect against deleterious effects of chemotherapeutic agents on normal cells. Furthermore, silymarin and its main bioactive compounds inhibit organic anion transporters (OAT) and ATP-binding cassettes (ABC) transporters, thus contributing to counteracting potential chemoresistance. Silymarin and its derivatives play a double role, namely, limiting the progression of cancer cells through different phases of the cycle—thus forcing them to evolve towards a process of cell death—and accumulating cancer cells in a phase of the cell cycle—thus making it possible to target a greater number of tumor cells with a specific anticancer agent. Silymarin exerts a chemopreventive effect by inducing intrinsic and extrinsic pathways and reactivating cell death pathways by modulation of the ratio of proapoptotic/antiapoptotic proteins and synergizing with agonists of death domains receptors. In summary, we highlight how silymarin may act as a chemopreventive agent and a chemosensitizer through multiple pathways.
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Wu, Jia-Ping, Chin-Chuan Tsai, Yu-Lan Yeh, et al. "Silymarin Accelerates Liver Regeneration after Partial Hepatectomy." Evidence-Based Complementary and Alternative Medicine 2015 (2015): 1–14. http://dx.doi.org/10.1155/2015/603529.
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Partial hepatectomy (PHx) is a liver regeneration physiological response induced to maintain homeostasis. Liver regeneration evolved presumably to protect wild animals from catastrophic liver loss caused by toxins or tissue injury. Silymarin (Sm) ability to stimulate liver regeneration has been an object of curiosity for many years. Silymarin has been investigated for use as an antioxidant and anticarcinogen. However, its use as a supportive treatment for liver damage is elusive. In this study, we fed silymarin (Sm, 25 mg/kg) to male Sprague-Dawley rats for 7 weeks. Surgical 2/3 PHx was then conducted on the rats at 6 hrs, 24 hrs, and 72 hrs. Western blot and RT-PCR were conducted to detect the cell cycle activities and silymarin effects on hepatic regeneration. The results showed that silymarin enhanced liver regeneration by accelerating the cell cycle in PHx liver. Silymarin led to increased G1 phase (cyclin D1/pRb), S phase (cyclin E/E2F), G2 phase (cyclin B), and M phase (cyclin A) protein and mRNA at 6 hrs, 24 hrs, and 72 hrs PHx. HGF, TGFα, and TGFβ1 growth factor expressions were also enhanced. We suggest that silymarin plays a crucial role in accelerated liver regeneration after PHx.
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Rakelly de Oliveira, Dayanne, Saulo Relison Tintino, Maria Flaviana Bezerra Morais Braga, et al. "In VitroAntimicrobial and Modulatory Activity of the Natural Products Silymarin and Silibinin." BioMed Research International 2015 (2015): 1–7. http://dx.doi.org/10.1155/2015/292797.
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Silymarin is a standardized extract from the dried seeds of the milk thistle (Silybum marianumL. Gaertn.) clinically used as an antihepatotoxic agent. The aim of this study was to investigate the antibacterial and antifungal activity of silymarin and its major constituent (silibinin) against different microbial strains and their modulatory effect on drugs utilized in clinical practice. Silymarin demonstrated antimicrobial activity of little significance against the bacterial strains tested, with MIC (minimum inhibitory concentration) values of 512 µg/mL. Meanwhile, silibinin showed significant activity againstEscherichia coliwith a MIC of 64 µg/mL. The results for the antifungal activity of silymarin and silibinin demonstrated a MIC of 1024 µg/mL for all strains. Silymarin and silibinin appear to have promising potential, showing synergistic properties when combined with antibacterial drugs, which should prompt further studies along this line.
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Vargas-Mendoza, Nancy, Marcelo Angeles-Valencia, Ángel Morales-González, et al. "Effect of Silymarin Supplementation in Lung and Liver Histological Modifications during Exercise Training in a Rodent Model." Journal of Functional Morphology and Kinesiology 6, no. 3 (2021): 72. http://dx.doi.org/10.3390/jfmk6030072.
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Background: Exercise training induces adaptive physiological and morphological modifications in the entire organism; however, excessive loads of training may increase damage in tissues. The purpose of this study was to evaluate the effect of silymarin in lung and liver histological changes in rats subjected to exercise training (ET). Methods: Male Wistar rats were subjected to an 8-week ET treadmill program 5 days per week, 60 min/session, and were previously administered 100 mg ascorbic acid or 100 mg of silymarin. Results: Silymarin increased alveolar and bronchial muscle size, improve vascularization, and reduced tissue inflammation. In liver, silymarin promoted the reduction of lipid content. Conclusion: Silymarin supplementation may improve inflammation in pulmonary tissue after 8 weeks of the ET treadmill program, improve cell recovery, and reduce intrahepatic lipid content.
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Abdel-Salam, Omar M. E., Amany A. Sleem, and Fatma A. Morsy. "Effects of Biphenyldimethyl-dicarboxylate Administration Alone or Combined with Silymarin in the CCL4Model of Liver Fibrosis in Rats." Scientific World JOURNAL 7 (2007): 1242–55. http://dx.doi.org/10.1100/tsw.2007.193.
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The effect of biphenyldimethyldicarboxylate (DDB), a synthetic compound, in use for the treatment of chronic hepatitis was studied on hepatic injury caused in rats by administration of carbon tetrachloride (CCl4). Starting at time of administration of the first dose of CCl4, rats received DDB at four dose levels (3, 15, 75 or 375 mg/kg), silymarin (22 mg/kg), a combination of DDB (75 mg/kg) and silymarin (22 mg/kg) or saline (control) once orally daily for 30 days. The administration of DDB in CCl4-treated rats at 75 or 375 mg/kg resulted in 61.2-76.2% decrease in alanine aminotransferase (ALT) and 46.9-60.8% decrease in aspartate aminotransferase (AST), respectively compared with the CCl4control group. Silymarin treatment resulted in 34.6 and 30% decrease in ALT and AST, while DDB (75 mg/kg) combined with silymarin (22 mg/kg) resulted in 58.2 and 31% decrease in ALT and AST, respectively. Serum creatinine increased by 50% by DDB at 375 mg/kg. After treatment with DDB at 75 or 375 mg/kg or DDB combined with silymarin, the development of liver necrosis and fibrosis caused by CCl4was markedly reduced, while after DDB combined with silymarin no DNA aneuploid cells could be observed. The decrease in glycogen and protein contents in hepatocytes caused by CCl4was markedly prevented by co-treatment with DDB at 75 or 375 mg/kg or DDB combined with silymarin. It is concluded that in the model of hepatic injury caused by chronic administration of CCl4in rats, the synthetic compound DDB, limits hepatocellular injury and exerts antifibrotic effect. Better improvement in protein, DNA, mucopolysaccharide content was seen after both DDB and silymarin compared to DDB alone. It is suggested, therefore, that DDB alone or in combination with silymarin might prove of benefit in the therapy of chronic liver disease. Monitoring of kidney functions in patients taking DDB is warranted.
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Ghaznavi, Habib, Saeed Mehrzadi, Banafshe Dormanesh, et al. "Comparison of the Protective Effects of Melatonin and Silymarin Against Gentamicin-Induced Nephrotoxicity in Rats." Journal of Evidence-Based Complementary & Alternative Medicine 21, no. 4 (2016): NP49—NP55. http://dx.doi.org/10.1177/2156587215621672.
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This study compared the possible protective effects of silymarin and melatonin against gentamicin (GEN)-induced nephrotoxicity in rats. Rats were allocated to 6 groups: Group I, control group; Groups II and III, administered with silymarin or melatonin; Group IV, injected with GEN; and Groups V and VI, administered with silymarin or melatonin, and then injected with GEN. Compared with the rats in the control group, all rats injected with GEN significantly presented elevated levels of serum creatinine and urea that was accompanied by an increase in relative kidney weight, increase in renal reactive oxygen species (ROS) and malondialdehyde (MDA) levels, and reduction in renal glutathione (GSH) level and superoxide dismutase (SOD) activity. Silymarin and melatonin pretreatment significantly lowered the elevated serum urea and creatinine concentration, kidney weight, and renal ROS and MDA levels. In addition, silymarin and melatonin significantly enhanced renal GSH level and SOD activity. This study indicates that silymarin and melatonin can attenuate renal injury in rats treated with GEN possibly by reducing the ROS level.
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Khokhar, Aamna, Aisha Qayyum, and Momina Khokhar. "HEPATOTOXICITY;." Professional Medical Journal 24, no. 08 (2017): 1200–1205. http://dx.doi.org/10.29309/tpmj/2017.24.08.957.
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Objectives: To evaluate the protective role of silymarin against methotrexate(MTX) induced hepatotoxicity in mice. Study design: Randomized controlled trial on animalmodel. Period: 06 months from March 2016 to August 2016. Settings: Department ofPharmacology and Therapeutics, Army Medical College, Rawalpindi. Material and Methods:Thirty male BALB/c mice were randomly divided into five groups (n=6). Group A received 0.2 mlnormal saline intraperitoneally served as control for MTX. Group B received 0.2 ml distilled waterorally for 7 days served as control for oral silymarin. Group C received single intraperitonealinjection of MTX 20 mg/kg. Group D received silymarin 25 mg/kg orally for seven days. GroupE received silymarin 25 mg/kg orally for 7 days with MTX 20 mg/kg intraperitoneally at day 4.Blood samples for measuring serum ALT (Alanine Transaminase), AST (Aspartate transaminase)and ALP (Alkaline Phosphatase) along with liver samples for hepatic histological examinationwere taken after 24 hours of last dose. Results: Silymarin show hepatoprotective effect againstMTX induced hepatotoxicity. Conclusion: Silymarin has hepatoprotective potential whenadministered along with MTX.
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Kheiripour, Nejat, Jamshid Karimi, Iraj Khodadadi, Heidar Tavilani, Mohammad Taghi Goodarzi, and Mohammad Hashemnia. "Silymarin prevents lipid accumulation in the liver of rats with type 2 diabetes via sirtuin1 and SREBP-1c." Journal of Basic and Clinical Physiology and Pharmacology 29, no. 3 (2018): 301–8. http://dx.doi.org/10.1515/jbcpp-2017-0122.
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Abstract Background: In this study, we have investigated whether silymarin intake influences lipid and glycogen content in conjunction with sirtuin1 (SIRT1) and sterol regulatory element-binding protein 1c (SREBP-1c) expressions in liver of type 2 diabetic rat. Methods: Thirty-six male Wistar rats were randomly divided into six groups: control groups (C) and diabetic groups (D); the control groups received 60 or 120 mg/kg silymarin (C+S60 or C+S120), and the diabetic groups received 60 or 120 mg/kg silymarin (D+S60 or D+S120) daily for 8 weeks. Serum biochemical parameters, as well as glycogen, lipid and oxidative stress biomarkers, in the liver tissue were measured by spectrophotometric methods. Additionally, SIRT1 and SREBP-1c messenger RNA (mRNA) expressions were evaluated by quantitative polymerase chain reaction. Results: Diabetes caused a significantly increased fasting blood sugar, homeostasis model assessment for insulin resistance, liver total cholesterol and triglyceride (TG) content, which were attenuated after the administration of silymarin. Dietary silymarin caused the improvement of lipid content in the liver of diabetic rats. Moreover, silymarin administration promoted SIRT1, suppressed SREBP-1c mRNA expression, reduced liver nitric oxide and protein carbonyl content, and increased liver glycogen, catalase and glutathione peroxidase activity. Furthermore, histopathological changes were improved in the treated groups. Conclusions: Silymarin administration considerably restored hepatic changes induced by streptozotocin and nicotinamide. The upregulation of SIRT1 mRNA expression by silymarin may be associated with decreased lipid, increased glycogen content and downregulation of the SREBP-1c gene in the liver.
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Lu, Cheng-Wei, Tzu-Yu Lin, Kuan-Ming Chiu, Ming-Yi Lee, Jih-Hsin Huang, and Su-Jane Wang. "Silymarin Inhibits Glutamate Release and Prevents against Kainic Acid-Induced Excitotoxic Injury in Rats." Biomedicines 8, no. 11 (2020): 486. http://dx.doi.org/10.3390/biomedicines8110486.
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Silymarin, a polyphenoic flavonoid derived from the seeds of milk thistle (Silybum marianum), exhibits neuroprotective effects. In this study, we used a model of rat cerebrocortical synaptosomes to investigate whether silymarin affects the release of glutamate, an essential neurotransmitter involved in excitotoxicity. Its possible neuroprotective effect on a rat model of kainic acid (KA)-induced excitotoxicity was also investigated. In rat cortical synaptosomes, silymarin reduced glutamate release and calcium elevation evoked by the K+ channel blocker 4-aminopyridine but did not affect glutamate release caused by the Na+ channel activator veratridine or the synaptosomal membrane potential. Decreased glutamate release by silymarin was prevented by removal of extracellular calcium and blocking of N- and P/Q-type Ca2+ channel or extracellular signal-regulated kinase 1/2 (ERK1/2) but not by blocking of intracellular Ca2+ release. Immunoblotting assay results revealed that silymarin reduced 4-aminopyridine-induced phosphorylation of ERK1/2. Moreover, systemic treatment of rats with silymarin (50 or 100 mg/kg) 30 min before systemic KA (15 mg/kg) administration attenuated KA-induced seizures, glutamate concentration elevation, neuronal damage, glial activation, and heat shock protein 70 expression as well as upregulated KA-induced decrease in Akt phosphorylation in the rat hippocampus. Taken together, the present study demonstrated that silymarin depressed synaptosomal glutamate release by suppressing voltage-dependent Ca2+ entry and ERK1/2 activity and effectively prevented KA-induced in vivo excitotoxicity.
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Dionisie, Vlad, Simona Clichici, Rodica M. Ion, et al. "In vivosilymarin’s antioxidant and anti-apoptotic effects on photodynamic therapy’s responsiveness." Journal of Porphyrins and Phthalocyanines 21, no. 03 (2017): 189–97. http://dx.doi.org/10.1142/s1088424617500304.
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Several studies have shown that some anti-oxidant natural compounds in combination with photodynamic therapy (PDT) can enhance the effectiveness of treatment. The aim of this study is to evaluate the effect of silymarin (SIL) in combination with 5,10,15,20-tetra-sulphonato-phenyl-porphyrin (TSPP) based photodynamic therapy, on experimental tumors. 30 Wistar rats with Walker carcinosarcoma, were divided into 6 groups: group 0 (control) — control, untreated group; group 1 (TSPP) — one dose of TSPP; group 2 (SIL) — silymarin; group 3 (PDT) — TSPP and irradiation 24 h after; group 4 (SIL[Formula: see text]PDT) — silymarin, TSPP and irradiation 24 h after; group 5 (SIL[Formula: see text]IR) and group 6 (IR) — irradiation and in addition, group 5 received SIL. Silymarin administered before photodynamic therapy decreased the lipid peroxidation ([Formula: see text] < 0.05) and modulated the antioxidant defense in tumor treated with PDT and silymarin suggesting that silymarin administration along with photodynamic therapy has an anti-oxidant effect. The caspase — 8 level and -3 activity increased in PDT and PDT [Formula: see text] SIL groups compared to the control; between the two groups there was a significant difference in term of apoptosis in favor to PDT. In conclusion, silymarin administration inhibited the reactive oxygen species generation and reduced the tumoral cells’ apoptosis, suggesting that natural compound administered before photodynamic therapy did not improve the therapy’s effect.
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El-Elimat, Tamam, Karem Alzoubi, Mahmoud AbuAlSamen, Zeinab Al Subeh, Tyler Graf, and Nicholas Oberlies. "Silymarin Prevents Memory Impairments, Anxiety, and Depressive-Like Symptoms in a Rat Model of Post-Traumatic Stress Disorder." Planta Medica 85, no. 01 (2018): 32–40. http://dx.doi.org/10.1055/a-0710-5673.
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AbstractPost-traumatic stress disorder (PTSD) is a debilitating psychopathological disease that is triggered by exposure to traumatic events. It is usually associated with substantial comorbidities, such as cognitive impairment, anxiety, and depression. Silymarin has been recently reported to exert neuroprotective activities against neurodegenerative diseases such as Alzheimerʼs and Parkinsonʼs diseases. Herein, the beneficial effects of silymarin in ameliorating PTSD-like symptoms such as memory impairments, anxiety, and depression were evaluated using a single-prolonged stress (SPS) rat model of PTSD. Male Wistar rats were randomly assigned into four groups: control, silymarin, SPS, or SPS + silymarin. Rats were administrated silymarin, 100 mg/kg i. p. for 4 wk. Rats in all groups were tested for short- and long-term memory in the radial arm water maze (RAWM), for anxiety-like behaviors using the open field test (OFT) and elevated plus maze (EPM) test, and for depression-like symptoms using the tail suspension test (TST). Conventional analyses of the RAWM, EPM, OFT, and TST were conducted using analysis of variance. Additionally, the anxiety-related behavior parameters of the EPM and OFT were entered to principal component analysis. Regression scores based on the first two extracted components, which accounted for 61% of the variance, were indicative of the anxiolytic activity of silymarin. Collectively, the results suggest that silymarin treatment prevents SPS-induced long-term memory impairments, anxiety, and depressive-like symptoms in rat models.
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Alcaraz-Contreras, Y., RP Mendoza-Lozano, ER Martínez-Alcaraz, et al. "Silymarin and dimercaptosuccinic acid ameliorate lead-induced nephrotoxicity and genotoxicity in rats." Human & Experimental Toxicology 35, no. 4 (2015): 398–403. http://dx.doi.org/10.1177/0960327115591373.
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We studied the effect of silymarin and dimercaptosuccinic acid (DMSA), a chelating agent that was administered individually or in combination against lead (Pb) toxicity in rats. Wistar rats (200 ± 20) were randomly divided into five groups. Group A served as a control. Groups B–E were exposed to 2000 ppm of lead acetate in drinking water for 8 weeks. Group B served as a positive control. Group C received silymarin (100 mg kg−1 orally) for 8 weeks. Group D received DMSA (75 mg kg−1 orally) once daily for the last 5 days of treatment. Group E received DMSA and silymarin as groups C and D, respectively. The effect of Pb was evaluated and accordingly the treatments on blood lead levels (BLLs), renal system, and genotoxic effects were calculated using comet assay. The BLLs were significantly increased following the exposition of lead acetate. The administration of silymarin and DMSA provided reduction in BLLs. Silymarin and DMSA provided significant protection on the genotoxic effect of Pb. The toxic effect of Pb on kidneys was also studied. Our data suggest that silymarin and DMSA improve the renal histopathological lesions.
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Xie, Zhang, Zhang, and Yuan. "Metabolism, Transport and Drug–Drug Interactions of Silymarin." Molecules 24, no. 20 (2019): 3693. http://dx.doi.org/10.3390/molecules24203693.
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Silymarin, the extract of milk thistle, and its major active flavonolignan silybin, are common products widely used in the phytotherapy of liver diseases. They also have promising effects in protecting the pancreas, kidney, myocardium, and the central nervous system. However, inconsistent results are noted in the different clinical studies due to the low bioavailability of silymarin. Extensive studies were conducted to explore the metabolism and transport of silymarin/silybin as well as the impact of its consumption on the pharmacokinetics of other clinical drugs. Here, we aimed to summarize and highlight the current knowledge of the metabolism and transport of silymarin. It was concluded that the major efflux transporters of silybin are multidrug resistance-associated protein (MRP2) and breast cancer resistance protein (BCRP) based on results from the transporter-overexpressing cell lines and MRP2-deficient (TR-) rats. Nevertheless, compounds that inhibit the efflux transporters MRP2 and BCRP can enhance the absorption and activity of silybin. Although silymarin does inhibit certain drug-metabolizing enzymes and drug transporters, such effects are unlikely to manifest in clinical settings. Overall, silymarin is a safe and well-tolerated phytomedicine.
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Ghobadi Pour, Mozhgan, Naser Mirazi, Hojjatollah Alaei, Shirin Moradkhani, Ziba Rajaei, and Alireza Monsef Esfahani. "Effects of lactulose and silymarin on liver enzymes in cirrhotic rats." Canadian Journal of Physiology and Pharmacology 95, no. 5 (2017): 522–29. http://dx.doi.org/10.1139/cjpp-2016-0454.
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Silymarin, a mixture of antihepatotoxic flavonolignans used in the treatment of liver diseases, and lactulose, a nonabsorbable synthetic disaccharide, were investigated to analyze their probable synergic and healing effects in a hepatic cirrhotic rat model. Liver damage was induced by the administration and subsequent withdrawal of thioacetamide. The significant decrease in liver enzymes and malondialdehyde levels confirmed the curative effects of silymarin and lactulose. In the silymarin + lactulose group, liver enzyme and malondialdehyde levels were significantly reduced compared with those in the thioacetamide group. All treatments led to liver regeneration and triggered enhanced regeneration. Silymarin and lactulose alone or in combination have potent curative effects and reduce thioacetamide-induced liver damage.
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Ramezannezhad, Pantea, Ali Nouri, and Esfandiar Heidarian. "Silymarin mitigates diclofenac-induced liver toxicity through inhibition of inflammation and oxidative stress in male rats." Journal of Herbmed Pharmacology 8, no. 3 (2019): 231–37. http://dx.doi.org/10.15171/jhp.2019.34.
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Introduction: Diclofenac (DIC) is one of the compounds derived from acetic acid which isknown for its anti-inflammatory and analgesic attributes. Silymarin is a flavonoid compoundwhich is derivate from Silybum marianum seeds. This research was done to assess the protectiverole of silymarin against liver toxicity induced by DIC in male rats.Methods: Randomly, 40 male Wistar rats were assigned into five groups as follows: Group 1:control group, Group 2: DIC-only treated (50 mg/kg, i.p), Group 3: silymarin-only treated (200mg/kg, p.o); Groups 4 and 5: DIC (50 mg/kg, i.p) plus silymarin (100 mg/kg and 200 mg/kg, p.o,respectively) treated. Various biochemical, molecular, and histological parameters were evaluatedin serum and tissue.Results: In the DIC-only treated group, the levels of liver glutathione peroxidase (GPx), superoxidedismutase (SOD), intracellular glutathione (GSH) and catalase (CAT) significantly diminished andthe levels of total bilirubin, alkaline phosphatase (ALP), nitrite, alanine aminotransferase (ALT),malondialdehyde (MDA), serum tumor necrosis factor-α (TNF-α), aspartate aminotransferase(AST), and TNF-α gene expression were remarkably elevated relative to control animals. In otherhands, treatment with silymarin caused a noticeable elevation in GPx, SOD, GSH, CAT and aremarkable reduction in levels of total bilirubin, ALP, nitrite content, ALT, MDA, serum TNF-α,AST and TNF-α gene expression relative to DIC-only treated group. Histopathological injurieswere also improved by silymarin administration.Conclusion: The results confirm that silymarin has an ameliorative effect on liver toxicity inducedby DIC and oxidative stress in male rats.
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Jee, Seung-Cheol, Min Kim, and Jung-Suk Sung. "Modulatory Effects of Silymarin on Benzo[a]pyrene-Induced Hepatotoxicity." International Journal of Molecular Sciences 21, no. 7 (2020): 2369. http://dx.doi.org/10.3390/ijms21072369.
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Benzo[a]pyrene (B[a]P), a polycyclic aromatic hydrocarbon, is a group 1 carcinogen that introduces mutagenic DNA adducts into the genome. In this study, we investigated the molecular mechanisms underlying the involvement of silymarin in the reduction of DNA adduct formation by B[a]P-7,8-dihydrodiol-9,10-epoxide (BPDE), induced by B[a]P. B[a]P exhibited toxicity in HepG2 cells, whereas co-treatment of the cells with B[a]P and silymarin reduced the formation of BPDE-DNA adducts, thereby increasing cell viability. Determination of the level of major B[a]P metabolites in the treated cells showed that BPDE levels were reduced by silymarin. Nuclear factor erythroid 2-related factor 2 (Nrf2) and pregnane X receptor (PXR) were found to be involved in the activation of detoxifying genes against B[a]P-mediated toxicity. Silymarin did not increase the expression of these major transcription factors, but greatly facilitated their nuclear translocation. In this manner, treatment of HepG2 cells with silymarin modulated detoxification enzymes through NRF2 and PXR to eliminate B[a]P metabolites. Knockdown of Nrf2 abolished the preventive effect of silymarin on BPDE-DNA adduct formation, indicating that activation of the Nrf2 pathway plays a key role in preventing B[a]P-induced genotoxicity. Our results suggest that silymarin has anti-genotoxic effects, as it prevents BPDE-DNA adduct formation by modulating the Nrf2 and PXR signaling pathways.
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Sutsko, I. P., A. G. Shlyahtun, A. V. Titko, et al. "Evaluation of silymarin and berberine efficiencies in the self-emulsifying drug delivery systemin paracetamol-induced experimental toxic liver injury." Doklady of the National Academy of Sciences of Belarus 64, no. 6 (2020): 713–22. http://dx.doi.org/10.29235/1561-8323-2020-64-6-713-722.
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The hepatoprotective properties of the silymarin and the plant alkaloid berberine combinationin experimental paracetamol-inducedliver damage were studied. Silymarin was obtained from milk thistle seeds. The conditions for extraction of flavonolignans (silymarin) were optimized. 70 % ethyl alcohol, ethyl acetate and water were used as extractants. It was shown that the optimal conditions for the extraction of flavonolignans in order to obtain the maximum yield of flavonolignans were alcohol extraction in a Soxhlet apparatus. The experiment showed that the combined of silymarin and berberine was greater than their individual actions, which most effectively permitted stabilization of hepatocyte membranes and prevented altering their integrity in paracetamol-induced toxic liver damage. The self-emulsifying system with silymarin and berberine to a greater extent a significant extent prevented dystrophic changes in hepatocytes and necrosis in liver tissue, reduced hyperfermentemia in rat blood serum, prevented disturbance in the activity of thioredoxin reductase and enzymes of the glutathione antioxidant system and there by more effectively prevented hepatocyte functional impairment.
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Sonali, Dalwadi, Soni Tejal, Thakkar Vaishali, and Gandhi Tejal. "Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution." Acta Pharmaceutica 60, no. 4 (2010): 427–43. http://dx.doi.org/10.2478/v10007-010-0038-3.
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Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution The influence of preparation methodology of silymarin solid dispersions using a hydrophilic polymer on the dissolution performance of silymarin was investigated. Silymarin solid dispersions were prepared using HPMC E 15LV by kneading, spray drying and co-precipitation methods and characterized by FTIR, DSC, XRPD and SEM. Dissolution profiles were compared by statistical and model independent methods. The FTIR and DSC studies revealed weak hydrogen bond formation between the drug and polymer, while XRPD and SEM confirmed the amorphous nature of the drug in co-precipitated solid dispersion. Enhanced dissolution compared to pure drug was found in the following order: co-precipitation > spray drying > kneading methodology (p < 0.05). All preparation methods enhanced silymarin dissolution from solid dispersions of different characteristics. The co-precipitation method proved to be best and provided a stable amorphous solid dispersion with 2.5 improved dissolution compared to the pure drug.
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Guo, Hong, Hui Cao, Xiaowei Cui, et al. "Silymarin’s Inhibition and Treatment Effects for Alzheimer’s Disease." Molecules 24, no. 9 (2019): 1748. http://dx.doi.org/10.3390/molecules24091748.
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As a longstanding problem, Alzheimer’s disease (AD) has stymied researchers in the medical field with its increasing incidence and enormous treatment difficulty. Silymarin has always been valued by researchers for its good efficacy and safety in treating liver disease. Recent studies have shown that silymarin also has good pharmacological activity in the nervous system, especially for the treatment of AD. Silymarin can control the production of Aβ by inhibiting the precursor substance of Aβ (β-amyloid precursor protein), and it can inhibit the polymerization of Aβ. Silymarin can also increase the acetylcholine content in the nervous system by inhibiting cholinesterase activity. At the same time, it also has the effect of resisting oxidative stress and the inflammatory response of the nervous system. These pharmacological activities contribute to the inhibition of the onset of AD. The good efficacy of silymarin on AD and its high safety and availability give it huge potential for the treatment of AD.