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Selected Botanicals and Plant Products That Lower Blood Glucose (Continued)
Published in Robert Fried, Richard M. Carlton, Type 2 Diabetes, 2018
Robert Fried, Richard M. Carlton
The extracts and organic fractions of L. chinensis tested yielded a methanol extract and an ethyl acetate fraction found to be potent inhibitors of rat lens aldose reductase (RLAR) in vitro, their IC50 values being 3.6 and 0.3 μg/mL, respectively. The IC50 is the concentration of an inhibitor where the response (or binding) is reduced by half.
Inhibitory effect of proteinase K against dermatophyte biofilms: an alternative for increasing the antifungal effects of terbinafine and griseofulvin
Published in Biofouling, 2022
Raimunda Sâmia Nogueira Brilhante, Raissa Geovanna Pereira Lopes, Lara de Aguiar, Jonathas Sales de Oliveira, Géssica dos Santos Araújo, Germana Costa Paixão, Waldemiro de Aquino Pereira-Neto, Rosemayre Souza Freire, João Victor Serra Nunes, Renan Pereira de Lima, Flávia Almeida Santos, José Júlio Costa Sidrim, Marcos Fábio Gadelha Rocha
Proteinase K cytotoxicity against J744A.1 macrophages significantly reduced the cell viability from 8 µg ml−1 to 128 µg ml−1. These data suggest that the use at lower concentrations could be safe. In this study, 4 µg ml−1 of proteinase K alone significantly reduced the metabolic activity of biofilms in vitro. The absence of cytotoxicity at this concentration indicates the possibility of systemic delivery. On the other hand, systemic use of proteinase K–antifungal combinations would not be the best method due to IC50 of 17.99 ± 1.25 µg ml−1. A possible strategy to solve this issue is the topical use of proteinase K through locoregional drug delivery (such as with a drug-impregnated adhesive), which could improve proteinase K effectiveness whilst limiting toxicity and other side effects (Di Prima et al. 2019; Laffleur et al. 2021). In this context, concentrations higher than IC50 could be used. The drug-impregnated adhesive for local distribution promotes local accumulation up to 10-fold higher than those obtained following administration of solution form (Di Prima et al. 2019).
Molecular docking and dynamics study to explore phytochemical ligand molecules against the main protease of SARS-CoV-2 from extensive phytochemical datasets
Published in Expert Review of Clinical Pharmacology, 2021
Shafi Mahmud, Mohasana Akter Mita, Suvro Biswas, Gobindo Kumar Paul, Maria Meha Promi, Shamima Afrose, Robiul Hasan, Sharmin Sultana Shimu, Shahriar Zaman, Salah Uddin, Trina Ekawati Tallei, Talha Bin Emran, Abu Saleh
We have performed the half-maximal inhibitory concentration (IC50) value prediction to understand the plausible experimental antiviral study of the currently studied molecules. The IC50 value is a powerful parameter for quantifying a compound’s ability to inhibit a biological process by half and is widely used to represent the inhibitory effects of compounds. The theoretical IC50 for felmichin, delta-oleanolic acid, emodin 1-O-beta-D-glucoside, and control was 8.0, 0.105, 268.61, 322.42 µM respectively (Table S5). The greater the value, the greater the dose required to achieve the inhibitory effects and consequently, the greater the possibility of off-target drug binding effects and, thus potential toxicity. Thus these results indicate that all compounds; specially delta-oleanolic acid showed better inhibition constant than the control.
Effect of hypoxia on proliferation and glucocorticoid resistance of T-cell acute lymphoblastic leukaemia
Published in Hematology, 2021
All cells were treated with increasing concentrations of Dex for 48 h, followed by assessment of cell viability by MTT assay, which was performed as described previously [18]. IC50 (concentration that inhibits 50%) values calculated by a decrease of 50% in cell viability rate compared to that of the control cell. The coefficient of drug interaction (CDI) was used to analyze the effects of treatment combinations. The CDI is calculated as follows: CDI = AB/ (A×B). According to the absorbance of each group, AB is the ratio of the combination groups to control group; A or B is the ratio of the single treatment group to control group. Thus, a CDI value <1, = 1 or >1 indicates that the drugs are synergistic, additive or antagonistic, respectively. CDI >1.25 indicates that the drugs are significantly antagonistic.