Academic literature on the topic 'IC50/EC50'
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Journal articles on the topic "IC50/EC50"
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Sebaugh, J. L. "Guidelines for accurate EC50/IC50 estimation." Pharmaceutical Statistics 10, no. 2 (March 2011): 128–34. http://dx.doi.org/10.1002/pst.426.
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Salazar, Carl, Ahmad M. El-Arabi, and Jacob J. Schmidt. "EC50 and IC50 Measurements of TRPM8 in Lipid Bilayers." Biophysical Journal 102, no. 3 (January 2012): 344a—345a. http://dx.doi.org/10.1016/j.bpj.2011.11.1887.
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Watcho, Pierre, Esther Ngadjui, Pepin Alango Nkeng-Efouet, Telesphore Benoît Nguelefack, and Albert Kamanyi. "Evaluation ofIn VitroUterotonic Activities of Fruit Extracts ofFicus asperifoliain Rats." Evidence-Based Complementary and Alternative Medicine 2011 (2011): 1–7. http://dx.doi.org/10.1093/ecam/nep221.
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The aim of the present study was to determine the uterotonic activities ofFicus asperifoliaand investigate its mechanism. The effects of aqueous and methanol extracts of the dried fruits ofF. asperifolia(0.05–1.60 mg mL−1) were evaluated on estrogenized isolated rat uterus in the presence and absence of atropine (1.73–55.27 nM), pyrilamine maleate (1.25 × 10−3to 40 × 10−3 M), indomethacin (0.06 × 10−5to 2.00 × 10−5 M) or hexamethonium (0.66 × 10−4to 21.43 × 10−4 M). Aqueous (EC50, 0.36 mg mL−1) and methanol (EC50, 0.22 mg mL−1) extracts as well as oxytocin (EC50, 0.02 nM), acetylcholine (EC50, 7.87 nM) and histamine (EC50, 0.76 nM) evoked concentration-dependent contractions of the uterus. Atropine, pyrilamine maleate and indomethacin concentration dependently blocked the response of the uterus to acetylcholine (IC50, 4.82 nM), histamine (IC50, 2.49 nM) and oxytocin (IC50, 0.07 nM), respectively, and to aqueous extract. Hexamethonium produced graded decreases in oxytocin-induced uterine contractions (IC50, 0.37 μM), but did not prevent the contractile effects of the aqueous extract (IC50, 9.88 μM). These results suggest thatF. asperifolia-induced uterotonic effect is related to the release of prostaglandins and contraction of the myometrial cells through muscarinic, oxytocic and H1histamine receptors. These data further give added value to the ethnic use ofF. asperifoliafor its abortificient and contraceptive properties.
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Umang Haribhai Gajjar, Niralee Kalpeshkumar Velhal, Hetvi Girdharbhai Parikh, Jayrajsinh Bhartbhai Parmar, Yash Bhut, and Viral Rupeshbhai Patel. "Evaluation of antioxidant activity of unpurified and purified datura seed." World Journal of Biology Pharmacy and Health Sciences 7, no. 1 (July 30, 2021): 030–35. http://dx.doi.org/10.30574/wjbphs.2021.7.1.0070.
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Aim: Evaluation of effect of shodhana process of datura seed (Datura stramonium) antioxidant activity. Methods: The datura was purified with two different processes viz. cow’s urine, and cow’s milk by Dolayantra method. Antioxidant activity was evaluated by in-vitro 1,1-Diphenyl-2-picryl hydrazyl (DPPH) radicals scavenging activity and Ferric reducing power ability (FRPA) assay. Result: cow urine purified datura (CUD) showed a significant effect in inhibiting DPPH, reaching up to 85.96% at concentration 1000 mcg/ml and its IC50 was 314.3 mcg/ml while Unpurified Datura Seed (UD) reaching up to 86.06% at concentration 1000 mcg/ml and its IC50 was 171.73 mcg/ml. The Cow Milk Purified Datura Seed (CMD) extract reach 69.72% at concentration 1000 mcg/ml and its IC50 value was 640. The IC50 value of Ascorbic acid was 23.35 mcg/ml. CUD showed a significant effect in reduction of ferric ion, reaching up to 85.59% reduction at concentration 1000 mcg/ml and its EC50 was 304.46 mcg/ml while UD reaching up to 86.11% at concentration 1000 mcg/ml and its EC50 was 280.28 mcg/ml. CMD extract reach 52.28% at concentration 1000 mcg/ml and its EC50 value was 1091.3mcg/ml.
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Hollande, F., J. P. Bali, and R. Magous. "Neurohormonal regulation of histamine synthesis in isolated rabbit fundic mucosal cells." American Journal of Physiology-Gastrointestinal and Liver Physiology 266, no. 3 (March 1, 1994): G395—G402. http://dx.doi.org/10.1152/ajpgi.1994.266.3.g395.
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In a population of rabbit fundic mucosal cells enriched in mucous and endocrine cells, gastrin and cholecystokinin octapeptide (CCK-8) were shown to increase dose-dependently histidine decarboxylase (HDC) activity with the same efficacy and high potencies [50% effective concentration (EC50) 0.389 +/- 0.041 and 0.275 +/- 0.011 nM, respectively], whereas pentagastrin was less potent (EC50 2.90 +/- 0.13 nM). L-365,260 and PD-135,666 inhibited gastrin- and CCK-8-stimulated HDC activity with a high potency [50% inhibitory concentration (IC50) 1.00 +/- 0.08 and 4.2 +/- 0.7 nM for gastrin-stimulated and 1.95 +/- 0.21 and 1.78 +/- 0.12 nM for CCK-8-stimulated HDC activity, respectively], whereas L-364,718 was 50 to 100 times less potent (EC50 100 +/- 2.5 and 91.2 +/- 3.1 nM, respectively on gastrin- and CCK-8-stimulated HDC activity). Carbachol also dose-dependently increased HDC activity (EC50 7.08 +/- 0.32 nM), and its effect was reversed by selective muscarinic-receptor antagonists with the following order of potency: pirenzepine (IC50 15.1 +/- 1.2 nM) > para-fluoro-hexahydro-siladifenidol (IC50 0.316 +/- 0.02 microM) > 11-2[(2-[(diethyl-amino)-methyl]-1-piperidinyl)acetyl]-5,11-dihydro-6H- pyrido[2,3-b][1,4]benzodiazepine-6-one (IC50 28.5 +/- 1.1 microM). Moreover, gastrin and carbachol were able to modify slightly but significantly both the Michaelis constant (Km) and the maximal velocity (Vmax) of HDC in the same way (18-20% reduction of the Km and 25-30% increase of the Vmax).(ABSTRACT TRUNCATED AT 250 WORDS)
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Zekovic, Zoran, Sasa Djurovic, and Branimir Pavlic. "Optimization of ultrasound-assisted extraction of polyphenolic compounds from coriander seeds using response surface methodology." Acta Periodica Technologica, no. 47 (2016): 249–63. http://dx.doi.org/10.2298/apt1647249z.
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Coriandrum sativum L. (coriander) seeds (CS) were used for preparation of extracts with high content of biologically active compounds. In order to optimize ultrasoundassisted extraction process, three levels and three variables of Box-Behnken experimental design (BBD) in combination with response surface methodology (RSM) were applied, yielding maximized total phenolics (TP) and flavonoids (TF) content and antioxidant activity (IC50 and EC50 values). Independent variables were temperature (40-80oC), extraction time (40-80 min) and ultrasonic power (96-216 W). Experimental results were fitted to a second-order polynomial model with multiple regression, while the analysis of variance (ANOVA) was employed to assess the model fitness and determine optimal conditions for TP (79.60oC, 49.20 min, 96.69 W), TF (79.40oC, 43.60 min, 216.00 W), IC50 (80.00oC, 60.40 min, 216.00 W) and EC50 (78.40oC, 68.60 min, 214.80 W). On the basis of the obtained mathematical models, three-dimensional surface plots were generated. The predicted values for TP, TF, IC50 and EC50 were: 382.68 mg GAE/100 g CS, 216 mg CE/100 g CS, 0.03764 mg/mL and 0.1425 mg/mL, respectively.
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Fidrianny, Irda, Veliana Virna, and Muhamad Insanu. "ANTIOXIDANT POTENTIAL OF DIFFERENT PARTS OF BOGOR PINEAPPLE (ANANAS COMOSUS [L.] MERR. VAR. QUEEN) CULTIVATED IN WEST JAVA-INDONESIA." Asian Journal of Pharmaceutical and Clinical Research 11, no. 1 (January 1, 2018): 129. http://dx.doi.org/10.22159/ajpcr.2017.v11i1.22022.
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Objective: The aims of this research were to observe antioxidant activities from different parts of Bogor pineapple (Ananas comosus [L.] Merr. Var. Queen) using two antioxidant testing methods which were 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) and correlation of total phenolic and flavonoid contents with their inhibitory concentration 50% (IC50) of DPPH and exhibitory concentration 50% (EC50) of FRAP.Methods: Each sample was extracted by reflux using different polarity solvents. Antioxidant activities were determined using DPPH and FRAP assays, total phenolic content (TPC) using Folin–Ciocalteu reagent, flavonoid content by Chang’s method, and correlation with their IC50 DPPH and EC50 FRAP were analyzed by Pearson’s method.Results: IC50 DPPH of various extracts of different parts of Bogor pineapple ranged from 0.13 to 68.17μg/ml. The ethyl acetate peel extract of Bogor pineapple presented the highest TPC (7.84 g GAE/100 g) while the highest total flavonoid content (10.84 g QE/100 g) was shown by ethyl acetate bract extract of Bogor pineapple. TPC in peel extract of Bogor pineapple had negative and significant correlation with their EC50 FRAP. The IC50 DPPH and EC50 FRAP of peel extract of Bogor pineapple showed positive and significant correlation.Conclusion: All different part extracts of Bogor pineapple (except n-hexane flesh extract, peel extract, and bract extract) were categorized as a very strong antioxidant by DPPH method. Phenolic compounds in peel extract of Bogor pineapple were the major contributor in antioxidant activities by FRAP method. DPPH and FRAP methods gave linear results in antioxidant activities of Bogor pineapple peel extract.
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Fidrianny, Irda, Veliana Virna, and Muhamad Insanu. "ANTIOXIDANT POTENTIAL OF DIFFERENT PARTS OF BOGOR PINEAPPLE (ANANAS COMOSUS [L.] MERR. VAR. QUEEN) CULTIVATED IN WEST JAVA-INDONESIA." Asian Journal of Pharmaceutical and Clinical Research 11, no. 1 (January 1, 2018): 129. http://dx.doi.org/10.22159/ajpcr.2018.v11i1.22022.
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Objective: The aims of this research were to observe antioxidant activities from different parts of Bogor pineapple (Ananas comosus [L.] Merr. Var. Queen) using two antioxidant testing methods which were 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) and correlation of total phenolic and flavonoid contents with their inhibitory concentration 50% (IC50) of DPPH and exhibitory concentration 50% (EC50) of FRAP.Methods: Each sample was extracted by reflux using different polarity solvents. Antioxidant activities were determined using DPPH and FRAP assays, total phenolic content (TPC) using Folin–Ciocalteu reagent, flavonoid content by Chang’s method, and correlation with their IC50 DPPH and EC50 FRAP were analyzed by Pearson’s method.Results: IC50 DPPH of various extracts of different parts of Bogor pineapple ranged from 0.13 to 68.17μg/ml. The ethyl acetate peel extract of Bogor pineapple presented the highest TPC (7.84 g GAE/100 g) while the highest total flavonoid content (10.84 g QE/100 g) was shown by ethyl acetate bract extract of Bogor pineapple. TPC in peel extract of Bogor pineapple had negative and significant correlation with their EC50 FRAP. The IC50 DPPH and EC50 FRAP of peel extract of Bogor pineapple showed positive and significant correlation.Conclusion: All different part extracts of Bogor pineapple (except n-hexane flesh extract, peel extract, and bract extract) were categorized as a very strong antioxidant by DPPH method. Phenolic compounds in peel extract of Bogor pineapple were the major contributor in antioxidant activities by FRAP method. DPPH and FRAP methods gave linear results in antioxidant activities of Bogor pineapple peel extract.
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Huang, Ren-Qi, and Glenn H. Dillon. "Functional Characterization of GABAA Receptors in Neonatal Hypothalamic Brain Slice." Journal of Neurophysiology 88, no. 4 (October 1, 2002): 1655–63. http://dx.doi.org/10.1152/jn.2002.88.4.1655.
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The hypothalamus influences a number of autonomic functions. The activity of hypothalamic neurons is modulated in part by release of the inhibitory neurotransmitter GABA onto these neurons. GABAA receptors are formed from a number of distinct subunits, designated α, β, γ, δ, ε, and θ, many of which have multiple isoforms. Little data exist, however, on the functional characteristics of the GABAA receptors present on hypothalamic neurons. To gain insight into which GABAA receptor subunits are functionally expressed in the hypothalamus, we used an array of pharmacologic assessments. Whole cell recordings were made from thin hypothalamic slices obtained from 1- to 14-day-old rats. GABAA receptor-mediated currents were detected in all neurons tested and had an average EC50 of 20 ± 1.6 μM. Hypothalamic GABAA receptors were modulated by diazepam (EC50 = 0.060 μM), zolpidem (EC50 = 0.19 μM), loreclezole (EC50 = 4.4 μM), methyl-6,7-dimethoxy-4-ethyl-β-carboline (EC50= 7.7 μM), and 5α-pregnan-3α-hydroxy-20-one (3α-OH-DHP). Conversely, these receptors were inhibited by Zn2+ (IC50 = 70.5 μM), dehydroepiandrosterone sulfate (IC50 = 16.7 μM), and picrotoxin (IC50 = 2.6 μM). The α4/6-selective antagonist furosemide (10–1,000 μM) was ineffective in all hypothalamic neurons tested. The results of our pharmacological analysis suggest that hypothalamic neurons express functional GABAA receptor subtypes that incorporate α1 and/or α2 subunits, β2 and/or β3 subunits, and the γ2 subunit. Our results suggest receptors expressing α3–α6, β1, γ1, and δ, if present, represent a minor component of functional hypothalamic GABAA receptors.
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Luyao, Harmie, Hendrik Luesch, and Mylene Uy. "GPCR Pharmacological Profiling of Aaptamine from the Philippine Sponge Stylissa sp. Extends Its Therapeutic Potential for Noncommunicable Diseases." Molecules 26, no. 18 (September 16, 2021): 5618. http://dx.doi.org/10.3390/molecules26185618.
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We report the first isolation of the alkaloid aaptamine from the Philippine marine sponge Stylissa sp. Aaptamine possessed weak antiproliferative activity against HCT116 colon cancer cells and inhibited the proteasome in vitro at 50 µM. These activities may be functionally linked. Due to its known, more potent activity on certain G-protein coupled receptors (GPCRs), including α-adrenergic and δ-opioid receptors, the compound was profiled more broadly at sub-growth inhibitory concentrations against a panel of 168 GPCRs to potentially reveal additional targets and therapeutic opportunities. GPCRs represent the largest class of drug targets. The primary screen at 20 µM using the β-arrestin functional assay identified the antagonist, agonist, and potentiators of agonist activity of aaptamine. Dose-response analysis validated the α-adrenoreceptor antagonist activity of aaptamine (ADRA2C, IC50 11.9 µM) and revealed the even more potent antagonism of the β-adrenoreceptor (ADRB2, IC50 0.20 µM) and dopamine receptor D4 (DRD4, IC50 6.9 µM). Additionally, aaptamine showed agonist activity on selected chemokine receptors, by itself (CXCR7, EC50 6.2 µM; CCR1, EC50 11.8 µM) or as a potentiator of agonist activity (CXCR3, EC50 31.8 µM; CCR3, EC50 16.2 µM). These GPCRs play a critical role in the treatment of cardiovascular disease, diabetes, cancer, and neurological disorders. The results of this study may thus provide novel preventive and therapeutic strategies for noncommunicable diseases (NCDs).
Dissertations / Theses on the topic "IC50/EC50"
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Mavundza, Edison Johannes. "Antioxidant and antibacterial activities of ethanol extract and flavonoids isolated from Athrixia phylicoides." Diss., University of Pretoria, 2010. http://hdl.handle.net/2263/25977.
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The ethanol extract of A. phylicoides was investigated for its antioxidant activity using the DPPH scavenging method. The extract showed good antioxidant results with a EC50 value of 10.64 ± 0.0842 µ/ml. The extract was also tested for antibacterial activity against microorganisms (Staphylococcus aureus, Enterococus faecalis, Bacillus cereus, Bacillus subtilis, Bacillus pumilus, Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumonia) commonly known to pose a threat in the wellbeing of man. All tested microorganisms were significantly inhibited by the extract with the MIC values ranging from 3.13 µg/ml to 6.25 µg/ml. Folin-Ciocalteu’s reagent method was used to determine total phenolic content of dried and freshly prepared crude extract of A. phylicoides. Higher total phenolic content (28.28 ± 0.019 mg GAC/100g) and antioxidant activity (EC50, 10.64 ± 0.084 µg/ml) was observed in the dried extract compared to the fresh extract with a TPC value of 23.04 ± 0.003 mg GAC/100g and EC50 of 13.97 ± 0.066 µg/ml. Bioassay-guided fractionation of ethanolic extract from aerial parts of Athrixia phylicoides using silica and sephadex column chromatography led to the isolation of four known flavanoids, 5-hydroxy-6,7,8,3’,4’,5’-hexamethoxyflavon-3-ol (1), 3-0- demethyldigicitrin (2), 5,6,7,8,3’,4’-hexamethoxyflavone (3) and Quecertin (4). Due to the low yield, no further tests were done on compound 3. A DPPH-scavenging assay was performed to evaluate the antioxidant activity of the isolated compounds. All the tested compounds showed potent antioxidant activity with EC50 values ranging from 1.27 to 3.41 µg/ml. Compound 4 showed a higher antioxidant activity (EC50, 1.27 µg/ml) than vitamin C (EC50, 2.66 µg/ml) used as a control. The MIC values of the isolated compounds against tested microorganisms varied from 20 to more than 40 µg/ml. All the tested compounds showed no activity against S. aureus, B. pumilus, K. pneumonia and P. aeruginosa at the highest concentration tested (40 µg/ml). These compounds together with the extract were further analyzed by XTT assay on Vero cells. The extract showed a low toxicity effect on the cells at lower concentrations exhibiting EC50 value of 107.8 ± 0.129 µg/ml. Compound 4 showed minimal toxicity effect on the cells with a EC50 value of 81.38±0.331 µg/ml, compared to Compound 1 and 2 which exhibited EC50 values of 27.91 ± 0.181 µg/ml and 28.92 ± 0.118 µg/ml respectively. The results obtained from this study provide a clear rationale for the medicinal uses of Athrixia phylicoides.Dissertation (MSc)--University of Pretoria, 2011.
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Abrahams, Beynon. "The effects of various combinations of different classes of anticancer drugs and tyrosine kinase inhibitors on the human MCF-7 breast carcinoma cell line." Thesis, University of the Western Cape, 2014. http://hdl.handle.net/11394/3846.
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Magister Scientiae (Medical Bioscience) - MSc(MBS)This study investigated the effects of TKIs on the growth and proliferation of MCF-7 breast carcinoma cells in culture. MCF-7 cells were exposed to different concentrations of TKIs alone and in combination with each other. Inhibition of cell growth by TKIs used individually occurred in a dose- and time-dependent manner. When EGFR Inhibitor I, EGFR Inhibitor II/BIBX1382 and the multi-specific EGFR/ErbB-2/ErB-4 Inhibitor were used in combination with each other at equimolar log dose concentrations, the combined effects on cell growth was significantly different to inhibitors used individually as reflected in a decreased EC50 (IC50) during combination treatments. Generally, for the combinations with DOX, CPL and the TKIs, synergistic as well as antagonistic effects were observed at isoeffective concentrations with resultant decreases in dose reduction indices (DRIs) implying greater efficacies with the respective combinations. In this study, conventional PCR was used to detect and illustrate the presence of the EGFR gene in the samples, while RT-qPCR was used to determine the mRNA expression levels of this gene in MCF-7 breast carcinoma cells
Book chapters on the topic "IC50/EC50"
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MarÉchal, Eric. "Measuring Bioactivity: KI, IC50 and EC50." In Chemogenomics and Chemical Genetics, 55–65. Berlin, Heidelberg: Springer Berlin Heidelberg, 2011. http://dx.doi.org/10.1007/978-3-642-19615-7_5.
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