Human liver spheroids in chemically defined conditions for studies of gene–drug, drug–drug and disease–drug interactions

2018 ◽  
Vol 19 (14) ◽  
pp. 1133-1138 ◽  
Author(s):  
Magnus Ingelman-Sundberg ◽  
Volker M Lauschke
Keyword(s):  
Drug Interactions ◽  
Human Liver

Human liver microsomal metabolism of paclitaxel and drug interactions

1998 ◽  
Vol 23 (3) ◽  
pp. 417-424 ◽  
Author(s):  
P. B. Desai ◽  
J. Z. Duan ◽  
Y -W. Zhu ◽  
S. Kouzi
Keyword(s):  
Drug Interactions ◽  
Human Liver ◽  
Microsomal Metabolism

scholarly journals Carbonyl Reduction of Flubendazole in the Human Liver: Strict Stereospecificity, Sex Difference, Low Risk of Drug Interactions

2019 ◽  
Vol 10 ◽  
Author(s):  
Vladimír Kubíček ◽  
Lenka Skálová ◽  
Adam Skarka ◽  
Věra Králová ◽  
Jana Holubová ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Sex Difference ◽  
Human Liver ◽  
Low Risk ◽  
Carbonyl Reduction

In-Vitro CYP3A4, CYP2E1 and UGT Activity in Human Liver Microsomes by Strobilanthes crispus Leaf Extracts

2020 ◽  
Vol 10 (2) ◽  
pp. 104-112
Author(s):  
Gabriel Akyirem Akowuah ◽  
Jin Han Chin ◽  
Siew Wei Yeong ◽  
Suk Yen Quah ◽  
Mariam Ahmad
Keyword(s):  
Drug Interactions ◽  
Human Liver ◽  
Liver Microsomes ◽  
Significant Inhibition ◽  
Human Liver Microsomes ◽  
Cyp3a4 Activity ◽  
Leaf Extracts ◽  
Strobilanthes Crispus ◽  
Glucuronosyl Transferase

Background: Strobilanthes crispus (L.) Bremek (Acanthaceae) leaves are used traditionally in Malaysia, Thailand, and Indonesia for anti-diabetic, anti-lytic, diuretic, and laxative purposes. Herb-drug interactions may potentiate or antagonize the absorption and metabolism of drugs which may result in potential toxicity. The aim of the present study was to investigate the effect of juice, hot aqueous, cold aqueous and methanol extracts of S. crispus leaves on phase I cytochrome 3A4 (CYP3A4) and Cytochrome 2E1 (CYP2E1) and phase II human liver enzyme UDP-Glucuronosyl Transferase (UGT). Methods: The herb-drug interactions of the leaf extracts and juice were determined by specific enzyme activity of CYP isoforms with specific probe substrate using spectrophotometry. CYP3A4 activity was measured for aminopyrine specific metabolite (formaldehyde) at 415 nm. CYP2E1 activity was determined using p-nitrophenol specific metabolite (p-nitrocatechol) at 535 nm. UGT activity was quantified through the consumption of p-nitrophenol by UGT at 405 nm. Results: All the S. crispus preparations showed significant inhibition of CYP3A4 activity. Only the methanolic extract showed a significant inhibition in CYP2E1. All the S. crispus extracts showed a significant effect on UGT activation at the higher concentration (1000 ng/ml). Only the cold aqueous extract and the juice showed UGT inhibition at lower concentration (1 ng/ml). Conclusion: S. crispus preparations showed in-vitro drug-herb interaction effects on human liver microsomes. Therefore, there is a possibility of drug-herb interaction could occur with S. crispus leaves through its effect on CYP3A4. Inhibition of the herb extracts on CYP2E1 could show anticarcinogenesis effects. The potency of drugs that metabolized via UGT pathway may be affected when co-administered with S. crispus leaf preparations.

Herb-Drug Interaction of 50 Chinese Herbal Medicines on CYP3A4 Activity in Vitro and in Vivo

2012 ◽  
Vol 40 (01) ◽  
pp. 57-73 ◽  
Author(s):  
Li-Heng Pao ◽  
Oliver Yoa-Pu Hu ◽  
Hsien-Yuan Fan ◽  
Chang-Ching Lin ◽  
Liang-Chun Liu ◽  
...  
Keyword(s):  
Enzymatic Activity ◽  
Drug Interactions ◽  
Human Liver ◽  
Liver Microsomes ◽  
Herbal Medicines ◽  
Human Liver Microsomes ◽  
Chinese Herbal Medicines ◽  
Chinese Herbal

The purpose of this study is to evaluate the effects of Chinese herbal medicines on the enzymatic activity of CYP3A4 and the possible metabolism-based herb-drug interactions in human liver microsomes and in rats. Fifty single-herbal preparations were screened for the activity of CYP3A4 using human liver microsomes for an in vitro probe reaction study. The enzymatic activity of CYP3A4 was estimated by determing the 6β-hydroxytestosterone metabolized from testosterone performed on a liquid chromatography-tandem mass spectrometry (LC-MS/MS). Huang Qin (Scutellaria baicalensis Geprgi), Mu Dan Pi (Paeonia suffruticosa Andr.), Ji Shiee Terng (Spatholobus suberectus Dunn.) and Huang Qi (Astragalus membranaceus [Fisch] Bge) have been demonstrated to have remarkable inhibiting effects on the metabolism of CYP3A4, whereas Xi Yi Hua (Magnolia biondii Pamp.) exhibited a moderate inhibition. These five single herbs were further investigated in an animal study using midazolam. Mu Dan Pi, Ji Shiee Terng and Huang Qi were observed to have greatly increased in the C max and AUC of midazolam. This study provides evidence of possible herb-drug interactions involved with certain single herbs.

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