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Journal articles on the topic 'Non-compound nucleus effects'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

H. Ali Alsafi, Mustafa, and Muthanna S. Farhan. "Synthesis, Characterization and Acute Anti-inflammatory Evaluation of New Mefenamic Acid Derivatives Having 4-Thiazolidinone Nucleus." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 28, no. 1 (2019): 138–46. http://dx.doi.org/10.31351/vol28iss1pp138-146.

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Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme.

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GUPTA, RAJ K., NIYTI, MONIKA MANHAS, SIGURD HOFMANN, and WALTER GREINER. "ROLE OF STATIC DEFORMATION AND COMPACT ORIENTATION OF TARGET NUCLEUS IN MEASURED FUSION, FUSION-FISSION AND CAPTURE CROSS-SECTIONS OF 244Pu+48Ca REACTION." International Journal of Modern Physics E 18, no. 03 (2009): 601–19. http://dx.doi.org/10.1142/s0218301309012744.

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The dynamical cluster-decay model (DCM), with deformations and orientation degrees of freedom of the incoming nuclei and of outging fragments included, is used to study the excitation functions of the "equatorial" compact hot fusion reaction 244 Pu +48 Ca →292114* (compact orientation angle θc=90° for 244 Pu ). Considering the higher multipole deformations up to hexadecapole deformation β4 and configurations with "compact" orientation θc, the model is shown to give a good description of the measured individual light-particle decay channels σxn, here x=3, 4 and 5, and other decay channels, the

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3

Zimdahl, Jack W., Kristin M. Barry, Jennifer Rodger, Chenae de Vis, Donald Robertson, and Wilhelmina Mulders. "Modulation of auditory processing by non-auditory brain areas: Effects of acoustic trauma." Journal of the Acoustical Society of America 154, no. 4_supplement (2023): A333. http://dx.doi.org/10.1121/10.0023713.

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Acoustic trauma (AT) induced hearing loss elicits plasticity in the form of altered spontaneous firing throughout the central auditory pathway, including at the level of the medial geniculate nucleus (MGN). Non-auditory areas such as the prefrontal cortex (PFC) and amygdala are thought to modulate auditory processing in the MGN, which may play a role in sensory gating. In our laboratory, we investigated the functionality of inputs from the PFC and amygdala on MGN activity in different animal models (rat and guinea pig) both without and with AT. The effects of AT on auditory thresholds were inv

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4

Mbaba, Mziyanda, Laura M. K. Dingle, Ayanda I. Zulu, et al. "Coumarin-Annulated Ferrocenyl 1,3-Oxazine Derivatives Possessing In Vitro Antimalarial and Antitrypanosomal Potency." Molecules 26, no. 5 (2021): 1333. http://dx.doi.org/10.3390/molecules26051333.

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A tailored series of coumarin-based ferrocenyl 1,3-oxazine hybrid compounds was synthesized and investigated for potential antiparasitic activity, drawing inspiration from the established biological efficacy of the constituent chemical motifs. The structural identity of the synthesized compounds was confirmed by common spectroscopic techniques: NMR, HRMS and IR. Biological evaluation studies reveal that the compounds exhibit higher in vitro antiparasitic potency against the chemosensitive malarial strain (3D7 P. falciparum) over the investigated trypanosomiasis causal agent (T. b. brucei 427)

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Heckmann, Gemot, Gerd Becker, Stephen Homer, Herbert Richard, Hans Kraft, and Peter Dvortsak. "Remarkably Large 15N, 13C and 18O Isotope NMR Shifts of the Mono-coordinate Phosphorus Atoms in the Compounds (Me3 Si)iPrNCP, K+[iPrNCP]-and KOCP · 2 DME (DME = 1,2-Dimethoxyethane)." Zeitschrift für Naturforschung B 56, no. 2 (2001): 146–51. http://dx.doi.org/10.1515/znb-2001-0206.

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The 31P and 13C NMR spectra of the heteroatom-substituted λ3-phosphaalkynes (Me3Si)- iPrNCP (1), K+ [iPrNCPl- (2) and KOCP · 2 DME (3) are described (Me = methyl; iPr = isopropyl). In addition,15N NMR data of 1 and 2 as well as further NMR results of all accessible nuclei of 1 to 3 are reported. The absolute values of the coupling constants 1J(31P13C) of 1, 2 and 3, 18.2, 45.7 and 57.2 Hz, respectively, are considerably different; the geminal coupling constants 2J( 31P15N) of the first two compounds show a decrease in the reverse order, 15.1 and 3.3 Hz. 13C, 29Si,15N, and 18O isotope effects o

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Shih, Chun-Ching, Chia-Yi Lee, Fung-Fuh Wong та Cheng-Hsiu Lin. "Protective Effects of One 2,4-Dihydro-3H-Pyrazol-3-one Derivative against Posterior Capsular Opacification by Regulation of TGF-β2/SMADs and Non-SMAD Signaling, Collagen I, and Fibronectin Proteins". Current Issues in Molecular Biology 44, № 10 (2022): 5048–66. http://dx.doi.org/10.3390/cimb44100343.

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Many elderly individuals frequently experience cataracts that interfere with vision. After cataract surgery, the left lens epithelial cell (LEC) exhibited fibrosis and posterior capsule opacification (PCO). Sometimes, there is a need for a second surgery; nevertheless, people try other methods, such as a good pharmacological agent, to treat PCO to reduce transforming growth factor-β2 (TGF-β2) amounts to avoid secondary surgery. The aim of the present study was to explore the potential anti-PCO activity of five 2,4-dihydro-3H-pyrazol-3-one (DHPO) derivatives in a TGF-β2-induced fibrogenesis SRA

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Salomon, Claudio J., Oreste A. Mascaretti, Charles E. Strouse та G. Punte. "Stereospecific synthesis, 1H and 13C NMR spectroscopy, and X-ray crystallographic studies of 6,6-dibromo-3α-cyano-2,2-dimethylpenam-(1R)-S-oxide". Canadian Journal of Chemistry 69, № 3 (1991): 578–83. http://dx.doi.org/10.1139/v91-087.

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A stereospecific synthesis of 6,6-dibromo-3α-cyano-2,2-dimethylpenam-(1R)-S-oxide (2) is described. The X-ray single crystal investigation of this compound shows that it crystallizes in the monoclinic system, space group P21, with cell parameters a = 6.194(1), b = 9.363(1), c = 9.869(1) Å, β = 96.55(2)°, V = 568(1) Å3, and two molecules per unit cell. Thestructure was solved, from low temperature data, by direct methods, and refined, by least-squares procedures, to a final R = 3.17%, Rw = 3.38%, for 1221 observed independent reflections. The sulfoxide configuration is R. The thiazolidine prese

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Ávila-Román, Javier, Lirenny Quevedo-Tinoco, Antonio J. Oliveros-Ortiz, et al. "Synthesis and Bioevaluation of New Stable Derivatives of Chrysin-8-C-Glucoside That Modulate the Antioxidant Keap1/Nrf2/HO-1 Pathway in Human Macrophages." Pharmaceuticals 17, no. 10 (2024): 1388. http://dx.doi.org/10.3390/ph17101388.

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Background/Objectives: The beneficial effects of the flavonoid chrysin can be reduced by its poor oral bioavailability. It has been shown that chrysin-8-C-glucoside (1) has a better absorption capability. The aim of this study was to evaluate the antioxidant and anti-inflammatory activity of this glucoside, as well as the respective hexa-acetate derivative 1a and the hexa-ethyl carbonate derivative 1b since the inclusion of moieties in bioactive molecules may increase or modify their biological effects. Methods: THP-1 macrophages were used to determine the viability in the presence of chrysin

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Gao, Hong-Li, Yu Yang, Hua Tian, et al. "Puerarin Alleviates Blood Pressure via Inhibition of ROS/TLR4/NLRP3 Inflammasome Signaling Pathway in the Hypothalamic Paraventricular Nucleus of Salt-Induced Prehypertensive Rats." Nutrients 16, no. 16 (2024): 2580. http://dx.doi.org/10.3390/nu16162580.

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Background: Puerarin is an isoflavone compound isolated from the roots of a leguminous plant, the wild kudzu. Various functional activities of this compound in multiple diseases have been reported. However, the effect and mechanism of puerarin in improving blood pressure remain non-elucidated. Purpose: The current study was designed to assess the preventive effects of puerarin on the onset and progression of hypertension and to verify the hypothesis that puerarin alleviates blood pressure by inhibiting the ROS/TLR4/NLRP3 inflammasome signaling pathway in the hypothalamic paraventricular nucleu

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Campos, Alline Cristina, Fabricio Araújo Moreira, Felipe Villela Gomes, Elaine Aparecida Del Bel, and Francisco Silveira Guimarães. "Multiple mechanisms involved in the large-spectrum therapeutic potential of cannabidiol in psychiatric disorders." Philosophical Transactions of the Royal Society B: Biological Sciences 367, no. 1607 (2012): 3364–78. http://dx.doi.org/10.1098/rstb.2011.0389.

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Cannabidiol (CBD) is a major phytocannabinoid present in the Cannabis sativa plant. It lacks the psychotomimetic and other psychotropic effects that the main plant compound Δ 9 -tetrahydrocannabinol (THC) being able, on the contrary, to antagonize these effects. This property, together with its safety profile, was an initial stimulus for the investigation of CBD pharmacological properties. It is now clear that CBD has therapeutic potential over a wide range of non-psychiatric and psychiatric disorders such as anxiety, depression and psychosis. Although the pharmacological effects of CBD in dif

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KANWAR, SHEFALI, MANOJ K. SHARMA, BIRBIKRAM SINGH, RAJ K. GUPTA, and WALTER GREINER. "DECAY OF 202Pb* FORMED IN 48Ca+154Sm REACTION USING THE DYNAMICAL CLUSTER-DECAY MODEL." International Journal of Modern Physics E 18, no. 07 (2009): 1453–67. http://dx.doi.org/10.1142/s0218301309013725.

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The decay of compound nucleus 202 Pb *, formed in entrance channel reaction 48 Ca +154 Sm at different incident energies, is studied by using the dynamical cluster-decay model (DCM) where all decay products are calculated as emissions of preformed clusters through the interaction barriers. The calculated results show an excellent agreement with experimental data for the fusion-evaporation residue cross-section σ ER together with the fusion-fission cross-section σ FF (taken as a sum of the energetically favored symmetric [Formula: see text] and near symmetric A=65–75 plus complementary fragment

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Brashier, Dick, Sachin Maggo, Shaman Gill, Piyush Angrish, Anuj Singh, and Deepmala Rawat. "Lasmiditan: new drug for acute migraine." International Journal of Basic & Clinical Pharmacology 8, no. 2 (2019): 372. http://dx.doi.org/10.18203/2319-2003.ijbcp20190163.

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Migraine is ranked by the World Health Organization as the world’s second leading cause of disability. The current state of knowledge suggests that migraine is a neuronal process involving activation and sensitization of the trigeminal nociceptors and the trigeminocervical complex, as well as cortical spreading depression and abnormal brainstem activity. The present non vascular etiological basis has opened a new horizon in the treatment of acute migraine targeting the trigeminal pathways. Lasmiditan, a highly selective 5-HT1F receptor agonist, acts on the trigeminal system without causing vas

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Ye, Minsook, SunYoung Lee, Hyo Jeong Yu, et al. "Sedative-Hypnotic Effects of Glycine max Merr. Extract and Its Active Ingredient Genistein on Electric-Shock-Induced Sleep Disturbances in Rats." International Journal of Molecular Sciences 24, no. 8 (2023): 7043. http://dx.doi.org/10.3390/ijms24087043.

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Glycine max Merr. (GM) is a functional food that provides many beneficial phytochemicals. However, scientific evidence of its antidepressive and sedative activities is scarce. The present study was designed to investigate the antidepressive and calmative effects of GM and its biologically active compound, genistein (GE), using electroencephalography (EEG) analysis in an electric foot shock (EFS)-stressed rat. The underlying neural mechanisms of their beneficial effects were determined by assessing corticotropin-releasing factor (CRF), serotonin (5-HT), and c-Fos immunoreactivity in the brain u

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Zhang, Kejie, Yuhan Chen, Yongli Zhang, Qin Yao, and Huiqin Zhuo. "Novel CRM1 Inhibitor Prevent the Nuclear Export of Beclin-1 Blocks Autophagy in Mantle Cell Lymphoma." Blood 124, no. 21 (2014): 3596. http://dx.doi.org/10.1182/blood.v124.21.3596.3596.

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Abstract Mantle cell lymphoma (MCL) is an aggressive histotype of B-cell non-Hodgkin’s lymphoma (NHL-B) with poor response to conventional chemotherapy and short survival which prompt the urgent need for novel therapeutic agents. Chromosomal Region Maintenance 1 (CRM1, Exportin 1, Xpo 1), the major mammalian export protein, plays a critical role in nuclear-cytosolic transport of multiple tumor suppressors which lose their normal function once they have exited the nucleus. We had found that CRM1 expression was higher in MCL cell lines and primary MCL cells than in normal B lymphocytes. Inhibiti

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Khamphikham, Pinyaphat, Adisak Tantiworawit та Songyot Anuchapreeda. "Pharmacologic Inhibition of XPO1 By Selinexor Improves Late-Stage Erythropoiesis in Severely Affected β 0-Thalassemia/Hemoglobin E". Blood 142, Supplement 1 (2023): 557. http://dx.doi.org/10.1182/blood-2023-178149.

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Ineffective erythropoiesis due to accumulation of excess α-globin chains profounds unwarranted consequences in β-thalassemia. In severe β-thalassemia, the excess α-globin chains trap HSP70-the guardian of GATA1-within the cytoplasm. Thus, in the nucleus, GATA1 is degraded and leads to late-stage erythropoiesis arrest. XPO1 is a nuclear exporter that exports HSP70 from the nucleus to the cytoplasm. Previous study showed that chemical downregulation of XPO1 in β-thalassemia major using an old generation of XPO1 inhibitor (KPT-251) could improve late-stage in vitro erythropoiesis. Moreover, XPO1

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Arroyo-Cruz, Luz V., Adriana Y. Aponte-Ramos, and Michelle M. Martínez-Montemayor. "Abstract P4-12-22: Ergosterol Peroxide affects the VCP/ANKZF1 complex spatial relationship and interaction in IBC cells." Clinical Cancer Research 31, no. 12_Supplement (2025): P4–12–22—P4–12–22. https://doi.org/10.1158/1557-3265.sabcs24-p4-12-22.

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Abstract Inflammatory breast cancer (IBC) is a highly aggressive and lethal type of breast cancer. Furthermore, patients with the triple-negative breast cancer subtype have tumors that lack the estrogen receptor, progesterone receptor, and HER2 expression. These tumors display greater invasiveness, and consequently, patients exhibit increased metastasis. Due to the lack of targeted therapies, IBC patients typically undergo multimodality therapy with cytotoxic chemotherapy like taxanes and anthracyclines, radiation, and surgery. There is an urgent need for selective therapies for IBC and natura

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Blasiak, Janusz, Jan Chojnacki, Elzbieta Pawlowska, Aleksandra Jablkowska, and Cezary Chojnacki. "Vitamin D May Protect against Breast Cancer through the Regulation of Long Noncoding RNAs by VDR Signaling." International Journal of Molecular Sciences 23, no. 6 (2022): 3189. http://dx.doi.org/10.3390/ijms23063189.

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Dietary vitamin D3 has attracted wide interest as a natural compound for breast cancer prevention and therapy, supported by in vitro and animal studies. The exact mechanism of such action of vitamin D3 is unknown and may include several independent or partly dependent pathways. The active metabolite of vitamin D3, 1α,25-dihydroxyvitamin D3 (1,25(OH)2D, calcitriol), binds to the vitamin D receptor (VDR) and induces its translocation to the nucleus, where it transactivates a myriad of genes. Vitamin D3 is involved in the maintenance of a normal epigenetic profile whose disturbance may contribute

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Ma, Ying-Qian, Ming Zhang, Zhen-Hua Sun, et al. "Identification of anti-gastric cancer effects and molecular mechanisms of resveratrol: From network pharmacology and bioinformatics to experimental validation." World Journal of Gastrointestinal Oncology 16, no. 2 (2024): 493–513. http://dx.doi.org/10.4251/wjgo.v16.i2.493.

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BACKGROUND Gastric cancer (GC) is one of the most aggressive malignancies with limited therapeutic options and a poor prognosis. Resveratrol, a non-flavonoid polyphenolic compound found in a variety of Chinese medicinal materials, has shown excellent anti-GC effect. However, its exact mechanisms of action in GC have not been clarified. AIM To identify the effects of resveratrol on GC progression and explore the related molecular mechanisms. METHODS Action targets of resveratrol and GC-related targets were screened from public databases. The overlapping targets between the two were confirmed us

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SLYVKA, Nataliia, Lesya SALIYEVA, Serhii HOLOTA, Ella KADYKALO, Larysa MARUSHKO та Mykhailo VOVK. "SYNTHESIS AND ANTIEXUDATIVE ACTIVITY OF N-ОXIDES 4-PYRIDINYLOXYSUBSTITUTED (BENZO)IMIDAZO[2,1-b][1,3]THIAZINES". Proceedings of the Shevchenko Scientific Society. Series Сhemical Sciences 2022, № 70 (2022): 102–9. http://dx.doi.org/10.37827/ntsh.chem.2022.70.102.

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The imidazo[2,1-b][1,3]thiazine nucleus, as well as the pyridine-N-oxide fragment, are pharmacophore groups that have received much attention from researchers. That is why the combination of these scaffolds in the structure of a single molecule seems to be quite attractive from chemical and biological point of view. Synthetically available 4-pyridinyloxy-substituted (benzo)imidazo[2,1-b]thiazines were used as precursors to obtain previously unknown (benzo)imidazo[2,1-b][1,3]thiazin-6-yloxypyridine 1-oxides. It was found that the oxidation of the latter with m-chlorobenzoic acid under mild reac

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Ku, Hsiang-Ju, Yuan Chang, I.-Tsang Chiang, and Fei-Ting Hsu. "Abstract 5374: Amentoflavone induces apoptosis and promotes G1 phase cell cycle arrest through regulating p53 pathway in HT29 human colorectal cancer." Cancer Research 82, no. 12_Supplement (2022): 5374. http://dx.doi.org/10.1158/1538-7445.am2022-5374.

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Abstract Amentoflavone (AF) is a nature diflavonoid compound that could extract from Ginkgo biloba and Chamaecyparis obtusa. AF had been proven with many biological properties, including anti-oxidant activity, anti-inflammatory, and could also inhibit NF-κB mediating apoptosis to achieve anti-tumor effects in hepatocellular carcinoma. p53, a tumor suppressor gene that could inhibit cell division and proliferation through regulating with cell cycle and apoptosis related molecules. Patients with p53 gene mutation were often resistant to current standard treatment in clinic. Several studies also

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Ranganathan, Parvathi, Xueyan Yu, Jessica Hofstetter, et al. "Decitabine Priming Enhances The Antileukemic Effects Of The Selective Inhibitor Of Nuclear Export (SINE) CRM1/XPO1 Antagonist (Selinexor) In Acute Myeloid Leukemia (AML)." Blood 122, no. 21 (2013): 1453. http://dx.doi.org/10.1182/blood.v122.21.1453.1453.

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Abstract AML is a clonal hematopoietic disorder characterized by genetic and epigenetic alterations. The prognosis of AML is poor highlighting the urgent need for novel therapeutic approaches. Targeting aberrant DNA hypermethylation by using hypomethylating drugs such as decitabine has been recently investigated in AML. Our group reported a relatively effective (47% complete response) single agent decitabine treatment schedule for older AML patients. These results suggested the opportunity to capitalize on this relatively effective and non-toxic treatment by incorporating this compound into no

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Tsymbalyuk, Olga, Tetyana Veklich, Roman Rodik, et al. "Thapsigargin-resistant thiacalix[4]arene C-1087-sensitive component of the contractile activity in rat myometrium reflects the functioning of plasma membrane calcium pump." Studia Biologica 17, no. 3 (2023): 3–22. http://dx.doi.org/10.30970/sbi.1703.725.

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Background. According to existing knowledge, thiacalix[4]arene С-1087 is highly capable of inhibiting Са2+-pump (Са2+, Mg2+-АТРase) of the plasma membrane; at the same time it inhibits the functioning of Са2+-pump of the sarcoplasmic reticulum of uterine smooth muscles to some degree. The aim of this research was to study the effects of С-1087 on the concentration of Ca2+ ions and contractile activity of the rat myometrium cells using an inhibitor of Са2+-pump of the sarcoplasmic reticulum – thapsigargin. Materials and Methods. The experiments were conducted using outbred white non-pregnant ra

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Karpun, E. O., and V. V. Parchenko. "Synthesis, physicochemical properties and antigypoxic activity of some S-derivatives of 4-alkyl-5-(((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol." Farmatsevtychnyi zhurnal, no. 6 (December 9, 2020): 56–64. http://dx.doi.org/10.32352/0367-3057.6.20.06.

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Hypoxia is a discrepancy between the required energy of the cell in the mitochondrial oxidative phosphorylation system. The immediate cause of the deficiency is a decrease in the oxygen concentration in the mitochondria. Today there is a huge demand for the development of new anti-hypoxic drugs. t is known that 1,2,4-triazole compounds can have antimicrobial, anti-inflammatory, anti-hypoxic effects. Modification of the 1,2,4-triazole nucleus is a productive way to create original active molecules with a non-planar structure, for their binding to bio-target substrates. Derivatives of bis-1,2,4-

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Sahoo, Sushree Sangita, Caitlin Roake, Liliana Rindle, et al. "Functional Consequences of TCAB1 Mutations in Dyskeratosis Congenita." Blood 128, no. 22 (2016): 3890. http://dx.doi.org/10.1182/blood.v128.22.3890.3890.

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Abstract Dyskeratosis congenita (DC) is a rare telomere disease with pleiotropic manifestations and bone marrow failure (BMF) as a major cause of mortality. The genes involved in DC pathogenesis play a role in telomere maintenance but their function in other in biological systems has not been well characterized. Compound heterozygous missense mutations in TCAB1(WRAP53) were reported so far in two pedigrees with classic DC (Zhong et al, 2011). TCAB1 functions as a scaffold protein recruiting TERC to the sub-organelle Cajal bodies, thus contributing to the assembly of telomerase enzyme; among it

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Phong, Nguyen Viet, Byung Sun Min, Seo Young Yang та Jeong Ah Kim. "Inhibitory Effect of Coumarins and Isocoumarins Isolated from the Stems and Branches of Acer mono Maxim. against Escherichia coli β-Glucuronidase". Applied Sciences 12, № 20 (2022): 10685. http://dx.doi.org/10.3390/app122010685.

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We isolated eight known secondary metabolites, including two isocoumarins and six coumarins, from the stems and branches of Acer mono Maxim. Their structures were confirmed using nuclear magnetic resonance spectroscopy and by comparing the data to published reports. The inhibitory effects of all compounds (1−8) on Escherichia coli β-glucuronidase were evaluated for the first time using in vitro assays. 3-(3,4-Dihydroxyphenyl)-8-hydroxyisocoumarin (1) displayed an inhibitory effect against β-glucuronidase (IC50 = 58.83 ± 1.36 μM). According to the findings of kinetic studies, compound 1 could f

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Liu, Zheng, Ming Bian, Qian-Qian Ma, Zhuo Zhang, Huan-Huan Du та Cheng-Xi Wei. "Design and Synthesis of New Benzo[d]oxazole-Based Derivatives and Their Neuroprotective Effects on β-Amyloid-Induced PC12 Cells". Molecules 25, № 22 (2020): 5391. http://dx.doi.org/10.3390/molecules25225391.

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A series of novel synthetic substituted benzo[d]oxazole-based derivatives (5a–5v) exerted neuroprotective effects on β-amyloid (Aβ)-induced PC12 cells as a potential approach for the treatment of Alzheimer’s disease (AD). In vitro studies show that most of the synthesized compounds were potent in reducing the neurotoxicity of Aβ25-35-induced PC12 cells at 5 μg/mL. We found that compound 5c was non-neurotoxic at 30 μg/mL and significantly increased the viability of Aβ25-35-induced PC12 cells at 1.25, 2.5 and 5 μg/mL. Western blot analysis showed that compound 5c promoted the phosphorylation of

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Kosar Kirca, Basak, Gonca Ozdemir Tarı, Cıgdem Albayrak Kastas, Mustafa Odabasoglu, and Orhan Buyukgungor. "Crystal structure, spectral characterization, molecular modeling studies and structural effects of the proton transfer process for (E)-5-methoxy-2-[(3,4-dimethylphenylimino) methyl]phenol." Macedonian Journal of Chemistry and Chemical Engineering 36, no. 2 (2017): 265. http://dx.doi.org/10.20450/mjcce.2017.1295.

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The main purpose of this study is to characterize a new organic material, (E)-5-methoxy-2-[(3,4-dimethylphenylimino)methyl]phenol, which was synthesized and grown as a single crystal. The molecular structure and spectroscopic properties of the ortho-hydroxy Schiff base compound were determined by X-ray diffraction analysis, Fourier-transform infrared (FT-IR), ultraviolet-visible (UV-Vis) and nuclear magnetic resonance (NMR) spectroscopy techniques, experimentally and computationally with density functional theory (DFT) calculations. X-ray and UV-Vis studies show that the compound exists in an

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Tjaden, Amelie, Apirat Chaikuad, Eric Kowarz, et al. "Image-Based Annotation of Chemogenomic Libraries for Phenotypic Screening." Molecules 27, no. 4 (2022): 1439. http://dx.doi.org/10.3390/molecules27041439.

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Phenotypical screening is a widely used approach in drug discovery for the identification of small molecules with cellular activities. However, functional annotation of identified hits often poses a challenge. The development of small molecules with narrow or exclusive target selectivity such as chemical probes and chemogenomic (CG) libraries, greatly diminishes this challenge, but non-specific effects caused by compound toxicity or interference with basic cellular functions still pose a problem to associate phenotypic readouts with molecular targets. Hence, each compound should ideally be com

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Zhang, J., L. Shorr, M. Yoshiyama, et al. "Hyperperfusion and cardioplegia effects on myocardial high-energy phosphate distribution and energy expenditure." American Journal of Physiology-Heart and Circulatory Physiology 267, no. 3 (1994): H894—H904. http://dx.doi.org/10.1152/ajpheart.1994.267.3.h894.

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This study examines the hypothesis that high-energy phosphate (HEP) compound levels in unstimulated in vivo myocardium are defined by 1) the level of perfusion and 2) non-perfusion-dependent metabolic characteristics. This hypothesis was tested by determining 1) the effects of pharmacological hyperperfusion of functioning myocardium on transmural HEP compound distribution, contractile function, and myocardial oxygen consumption rate (MVO2) as well as 2) the effect of KCl cardioplegia on transmural myocardial HEP compound distribution. Creatine phosphate (CP) and ATP were measured across the an

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Ma, Xu-Chen, Shuo Dong, Shao-Yan Zhang, Ning Jia, and Song-Lei Ou. "Taraxerone triterpene inhibits cancer cell growth by inducing apoptosis in non-small cell lung cancer cells." Bangladesh Journal of Pharmacology 11, no. 2 (2016): 342. http://dx.doi.org/10.3329/bjp.v11i2.24338.

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<p class="Abstract">The objective of the present study was to evaluate the anti-cancer effects of taraxerone in non-small cell lung cancer cells (A-549). The effect of this compound on apoptosis and cellular morphology was also studied. MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay was used to evaluate the effect of the compound on cell viability. Cellular morphology after taraxerone treatment was demonstrated by fluorescence microscopy and transmission electron microscopy. The results revealed that taraxerone induced dose-dependent as well as time-dependent

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Lee, Dahae, Kem Ok Kim, Dongho Lee, and Ki Sung Kang. "Anti-Apoptotic and Antioxidant Effects of 3-Epi-Iso-Seco-Tanapartholide Isolated from Artemisia argyi against Iodixanol-Induced Kidney Epithelial Cell Death." Biomolecules 10, no. 6 (2020): 867. http://dx.doi.org/10.3390/biom10060867.

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Iodixanol is a non-ionic iso-osmolar contrast agent, but it is a risk factor for kidney damage and increases morbidity and mortality. In this study, we investigated the effect of 9 sesquiterpenes isolated from mugwort (Artemisia argyi) in contrast agent-induced cytotoxicity in LLC-PK1 cells. Cells were exposed to nine sesquiterpene compounds for 2 h, followed by incubation with iodixanol for 3 h. Cell viability was assessed using the Ez-Cytox assay. The level of reactive oxygen species was measured using 2′,7′-dichlorodihydrofluorescein diacetate staining. Apoptotic cell death was detected usi

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Sanches, Larissa Juliani, Poliana Camila Marinello, Carolina Panis, et al. "Cytotoxicity of citral against melanoma cells: The involvement of oxidative stress generation and cell growth protein reduction." Tumor Biology 39, no. 3 (2017): 101042831769591. http://dx.doi.org/10.1177/1010428317695914.

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Citral is a natural compound that has shown cytotoxic and antiproliferative effects on breast and hematopoietic cancer cells; however, there are few studies on melanoma cells. Oxidative stress is known to be involved in all stages of melanoma development and is able to modulate intracellular pathways related to cellular proliferation and death. In this study, we hypothesize that citral exerts its cytotoxic effect on melanoma cells by the modulation of cellular oxidative status and/or intracellular signaling. To test this hypothesis, we investigated the antiproliferative and cytotoxic effects o

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Han, Chun, Jiahong Ren, Feng Su, et al. "Hybrids of Quinoline and Anilinopyrimidine: Novel EGFRT790M Inhibitors with Antiproliferative Activity against Non-Small Cell Lung Cancer Cell Lines." Anti-Cancer Agents in Medicinal Chemistry 20, no. 6 (2020): 724–33. http://dx.doi.org/10.2174/1871520620666200302113206.

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Background: The third-generation irreversible Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors (TKIs) inhibit the T790M mutation while sparing EGFRWT. However, the C797S point mutation confers resistance to existing irreversible EGFRT790M inhibitors. Objective: Novel EGFRT790M inhibitors were designed through hybridization of quinoline and anilinopyrimidine, and biologically evaluated their antiproliferative activity against Non-Small Cell Lung Cancer (NSCLC) cell lines. Methods: The target compounds 11a-h were synthesized and structurally characterized with 1H, 13C Nuclear M

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Morgan, Ibrahim, Robert Rennert, Robert Berger, et al. "Identification and Characterization of Novel Inhibitors of Human Poly(ADP-Ribose) Polymerase-1." Molecules 30, no. 13 (2025): 2728. https://doi.org/10.3390/molecules30132728.

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Poly(ADP-ribose) polymerases (PARP) are a family of enzymes that were proven to play an essential role in the initiation and activation of DNA repair processes in the case of DNA single-strand breaks. The inhibition of PARP enzymes might be a promising option for the treatment of several challenging types of cancers, including triple-negative breast cancer (TNBC) and non-small cell lung carcinoma (NSCLC). This study utilizes several techniques to screen the compound collection of the Leibniz Institute of Plant Biochemistry (IPB) to identify novel hPARP-1 inhibitors. First, an in silico pharmac

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Mokady, Daphna, Jason Charish, Patrick Barretto-Burns, et al. "Small-Molecule-Directed Endogenous Regeneration of Visual Function in a Mammalian Retinal Degeneration Model." International Journal of Molecular Sciences 25, no. 3 (2024): 1521. http://dx.doi.org/10.3390/ijms25031521.

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Degenerative retinal diseases associated with photoreceptor loss are a leading cause of visual impairment worldwide, with limited treatment options. Phenotypic profiling coupled with medicinal chemistry were used to develop a small molecule with proliferative effects on retinal stem/progenitor cells, as assessed in vitro in a neurosphere assay and in vivo by measuring Msx1-positive ciliary body cell proliferation. The compound was identified as having kinase inhibitory activity and was subjected to cellular pathway analysis in non-retinal human primary cell systems. When tested in a disease-re

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Badalamenti, Natale, Maurizio Bruno, Roman Pavela та ін. "Acaricidal Activity of Bufadienolides Isolated from Drimia pancration against Tetranychus urticae, and Structural Elucidation of Arenobufagin-3-O-α-L-rhamnopyranoside". Plants 11, № 13 (2022): 1629. http://dx.doi.org/10.3390/plants11131629.

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Chemical characterization of the bulbs of Drimia pancration was conducted to isolate four steroidal saponins (1–4). Earlier, we focused on the structural elucidation of compounds 1–3. Herein, by means of 1H-NMR, 13C-NMR, Nuclear Overhauser Effects (NOE), and 2D-NMR spectra, the full stereochemical structure of 4 is reported, and all the 1H and 13C signals are assigned. Compounds 1–4 were tested for their acaricidal properties against the two-spotted spider mite Tetranychus urticae. Our results showed excellent activity of compound 1, with an LD50 (µg/cm2) of 0.29 and a LD90 (µg/cm2) of 0.96, w

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Satoh, Takumi, and Stuart Lipton. "Recent advances in understanding NRF2 as a druggable target: development of pro-electrophilic and non-covalent NRF2 activators to overcome systemic side effects of electrophilic drugs like dimethyl fumarate." F1000Research 6 (December 14, 2017): 2138. http://dx.doi.org/10.12688/f1000research.12111.1.

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Dimethyl fumarate (DMF) is an electrophilic compound previously called BG-12 and marketed under the name Tecfidera®. It was approved in 2013 by the US Food and Drug Administration and the European Medicines Agency for the treatment of relapsing multiple sclerosis. One mechanism of action of DMF is stimulation of the nuclear factor erythroid 2-related factor 2 (NRF2) transcriptional pathway that induces anti-oxidant and anti-inflammatory phase II enzymes to prevent chronic neurodegeneration. However, electrophiles such as DMF also produce severe systemic side effects, in part due to non-specifi

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Lee, Seoung Rak, Dahae Lee, Jae Sik Yu, et al. "Natalenamides A–C, Cyclic Tripeptides from the Termite-Associated Actinomadura sp. RB99." Molecules 23, no. 11 (2018): 3003. http://dx.doi.org/10.3390/molecules23113003.

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In recent years, investigations into the biochemistry of insect-associated bacteria have increased. When combined with analytical dereplication processes, these studies provide a powerful strategy to identify structurally and/or biologically novel compounds. Non-ribosomally synthesized cyclic peptides have a broad bioactivity spectrum with high medicinal potential. Here, we report the discovery of three new cyclic tripeptides: natalenamides A–C (compounds 1–3). These compounds were identified from the culture broth of the fungus-growing termite-associated Actinomadura sp. RB99 using a liquid c

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Lourenço-Lopes, Catarina, Paula Garcia-Oliveira, Maria Carpena, et al. "Scientific Approaches on Extraction, Purification and Stability for the Commercialization of Fucoxanthin Recovered from Brown Algae." Foods 9, no. 8 (2020): 1113. http://dx.doi.org/10.3390/foods9081113.

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The scientific community has corroborated the numerous beneficial activities of fucoxanthin, such as its antioxidant, anti-inflammatory, anticancer or neuroprotective effects, among others. These properties have attracted the attention of nutraceutical, cosmetic and pharmacological industries, giving rise to various possible applications. Fucoxanthin may be chemically produced, but the extraction from natural sources is considered more cost-effective, efficient and eco-friendly. Thus, identifying suitable sources of this compound and giving a general overview of efficient extraction, quantific

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Silvestro, Serena, Giovanni Schepici, Placido Bramanti, and Emanuela Mazzon. "Molecular Targets of Cannabidiol in Experimental Models of Neurological Disease." Molecules 25, no. 21 (2020): 5186. http://dx.doi.org/10.3390/molecules25215186.

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Cannabidiol (CBD) is a non-psychoactive phytocannabinoid known for its beneficial effects including antioxidant and anti-inflammatory properties. Moreover, CBD is a compound with antidepressant, anxiolytic, anticonvulsant and antipsychotic effects. Thanks to all these properties, the interest of the scientific community for it has grown. Indeed, CBD is a great candidate for the management of neurological diseases. The purpose of our review is to summarize the in vitro and in vivo studies published in the last 15 years that describe the biochemical and molecular mechanisms underlying the effect

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Banasiak, Anna, Nicolò Zuin Fantoni, Andrew Kellett, and John Colleran. "Mapping the DNA Damaging Effects of Polypyridyl Copper Complexes with DNA Electrochemical Biosensors." Molecules 27, no. 3 (2022): 645. http://dx.doi.org/10.3390/molecules27030645.

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Several classes of copper complexes are known to induce oxidative DNA damage that mediates cell death. These compounds are potentially useful anticancer agents and detailed investigation can reveal the mode of DNA interaction, binding strength, and type of oxidative lesion formed. We recently reported the development of a DNA electrochemical biosensor employed to quantify the DNA cleavage activity of the well-studied [Cu(phen)2]2+ chemical nuclease. However, to validate the broader compatibility of this sensor for use with more diverse—and biologically compatible—copper complexes, and to probe

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Heo, Gwangbeom, Yuju Kim, Eun-La Kim та ін. "Atractylodin Ameliorates Colitis via PPARα Agonism". International Journal of Molecular Sciences 24, № 1 (2023): 802. http://dx.doi.org/10.3390/ijms24010802.

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Atractylodin is a major compound in the rhizome of Atractylodes lancea, an oriental herbal medicine used for the treatment of gastrointestinal diseases, including dyspepsia, nausea, and diarrhea. Recent studies have shown that atractylodin exerts anti-inflammatory effects in various inflammatory diseases. Herein, we investigated the anti-colitis effects of atractylodin and its molecular targets. We determined the non-cytotoxic concentration of atractylodin (50 μM) using a cell proliferation assay in colonic epithelial cells. We found that pretreatment with atractylodin significantly inhibits t

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Barth, Marie-Christin, Norman Häfner, Ingo B. Runnebaum, and Wolfgang Weigand. "Synthesis, Characterization and Biological Investigation of the Platinum(IV) Tolfenamato Prodrug–Resolving Cisplatin-Resistance in Ovarian Carcinoma Cell Lines." International Journal of Molecular Sciences 24, no. 6 (2023): 5718. http://dx.doi.org/10.3390/ijms24065718.

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The research on the anticancer potential of platinum(IV) complexes represents one strategy to circumvent the deficits of approved platinum(II) drugs. Regarding the role of inflammation during carcinogenesis, the effects of non-steroidal anti-inflammatory drug (NSAID) ligands on the cytotoxicity of platinum(IV) complexes is of special interest. The synthesis of cisplatin- and oxaliplatin-based platinum(IV) complexes with four different NSAID ligands is presented in this work. Nine platinum(IV) complexes were synthesized and characterized by use of nuclear magnetic resonance (NMR) spectroscopy (

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Chen, Rui, Lini Huo, Yogini Jaiswal, et al. "Synthesis and Evaluation of Anticancer Activity of New 4-Acyloxy Derivatives of Robustic Acid." International Journal of Molecular Sciences 20, no. 21 (2019): 5336. http://dx.doi.org/10.3390/ijms20215336.

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In the present study, a series of 4-acyloxy robustic acid derivatives were synthesized and characterized for evaluation of their anti-cancer activity. The structures of these derivatives were elucidated by mass spectra (MS) nuclear magnetic resonance spectra (NMR). The single-crystal X-ray diffraction structure of one of these compounds was obtained, for further validation of the target compound structures. The anticancer activities of the target products were evaluated against human leukemic cells HL-60, human non-small cell lung carcinoma cells A-549, human hepatic carcinoma cells SMMC-7721,

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Al-Hussan, Rasha, Nawal A. Albadr, Ghedeir M. Alshammari, Soheir A. Almasri, Farah Fayez Alfayez та Mohammed Abdo Yahya. "Phloretamide Protects against Diabetic Kidney Damage and Dysfunction in Diabetic Rats by Attenuating Hyperglycemia and Hyperlipidemia, Suppressing NF-κβ, and Upregulating Nrf2". Pharmaceutics 16, № 4 (2024): 505. http://dx.doi.org/10.3390/pharmaceutics16040505.

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Potent hypoglycemic and antioxidant effects were recently reported for the apple-derived phenolic compound phloretamide (PLTM). The renoprotective effects of this compound are yet to be shown. This study aimed to examine the potential of PLTM to prevent diabetic nephropathy in streptozotocin-induced diabetic rats and to examine the possible mechanisms of protection. Non-diabetic and STZ-diabetic male rats were treated orally by gavage with either the vehicle or with PTLM (200 mg/kg; twice/week) for 12 weeks. PTLM significantly increased urine volume and prevented glomerular and tubular damage

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Amawi, Haneen, Noor Hussein, Sai H. S. Boddu та ін. "Novel Thienopyrimidine Derivative, RP-010, Induces β-Catenin Fragmentation and Is Efficacious against Prostate Cancer Cells". Cancers 11, № 5 (2019): 711. http://dx.doi.org/10.3390/cancers11050711.

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Thienopyrimidines containing a thiophene ring fused to pyrimidine are reported to have a wide-spectrum of anticancer efficacy in vitro. Here, we report for the first time that thieno[3,2-d]pyrimidine-based compounds, also known as the RP series, have efficacy in prostate cancer cells. The compound RP-010 was efficacious against both PC-3 and DU145 prostate cancer (PC) cells (IC50 < 1 µM). The cytotoxicity of RP-010 was significantly lower in non-PC, CHO, and CRL-1459 cell lines. RP-010 (0.5, 1, 2, and 4 µM) arrested prostate cancer cells in G2 phase of the cell cycle, and induced mitotic ca

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Lasch, Alexandra, Philip Marx-Stoelting, Albert Braeuning, and Dajana Lichtenstein. "More than additive effects on liver triglyceride accumulation by combinations of steatotic and non-steatotic pesticides in HepaRG cells." Archives of Toxicology 95, no. 4 (2021): 1397–411. http://dx.doi.org/10.1007/s00204-021-02997-2.

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AbstractThe liver is constantly exposed to mixtures of hepatotoxic compounds, such as food contaminants and pesticides. Dose addition is regularly assumed for mixtures in risk assessment, which however might not be sufficiently protective in case of synergistic effects. Especially the prediction of combination effects of substances which do not share a common adverse outcome (AO) might be problematic. In this study, the focus was on the endpoint liver triglyceride accumulation in vitro, an indicator of hepatic fatty acid changes. The hepatotoxic compounds difenoconazole, propiconazole and tebu

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Feng, Jingwen, Songlin Li, Bing Zhang та ін. "FGFC1 Exhibits Anti-Cancer Activity via Inhibiting NF-κB Signaling Pathway in EGFR-Mutant NSCLC Cells". Marine Drugs 20, № 1 (2022): 76. http://dx.doi.org/10.3390/md20010076.

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FGFC1, an active compound isolated from the culture of marine fungi Stachybotrys longispora FG216, elicits fibrinolytic, anti-oxidative, and anti-inflammatory activity. We have previously reported that FGFC1 inhibited the proliferation, migration, and invasion of the non-small cell lung cancer (NSCLC) cells in vitro. However, the precise mechanisms of FGFC1 on NSCLC and its anti-cancer activity in vivo remains unclear. Hence, this study was focused to investigate the effects and regulatory mechanisms of FGFC1 on two NSCLC cell lines, EGFR-mutant PC9 (ex19del) and EGFR wild-type H1299. Results

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Predes, Danilo, Luiz F. S. Oliveira, Laís S. S. Ferreira та ін. "The Chalcone Lonchocarpin Inhibits Wnt/β-Catenin Signaling and Suppresses Colorectal Cancer Proliferation". Cancers 11, № 12 (2019): 1968. http://dx.doi.org/10.3390/cancers11121968.

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The deregulation of the Wnt/β-catenin signaling pathway is a central event in colorectal cancer progression, thus a promising target for drug development. Many natural compounds, such as flavonoids, have been described as Wnt/β-catenin inhibitors and consequently modulate important biological processes like inflammation, redox balance, cancer promotion and progress, as well as cancer cell death. In this context, we identified the chalcone lonchocarpin isolated from Lonchocarpus sericeus as a Wnt/β-catenin pathway inhibitor, both in vitro and in vivo. Lonchocarpin impairs β-catenin nuclear loca

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Bacelar Sacramento de Araújo, Taís, Leonardo de Oliveira Siquara da Rocha, Manuela Torres Andion Vidal, et al. "GANT61 Reduces Hedgehog Molecule (GLI1) Expression and Promotes Apoptosis in Metastatic Oral Squamous Cell Carcinoma Cells." International Journal of Molecular Sciences 21, no. 17 (2020): 6076. http://dx.doi.org/10.3390/ijms21176076.

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Due to its importance in the pathogenesis of oral squamous cell carcinoma (OSCC), the Hedgehog (HH) pathway is considered a potential therapeutic target. We investigated the effects of GANT61, a GLI inhibitor, on HH gene expression, as well as on metastatic OSCC cell proliferation and death. Following culture in DMEM medium, cytotoxicity of GANT61 against different tumor and non-tumor cell types was assessed by alamarBlue assays. Cytotoxicity analysis revealed that the metastatic HSC3 cell line was the most sensitive (IC50: 36 µM) to the tested compound. The compound’s effects on the expressio

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