An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone

An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone

Kurarinone is a major component found in the dried roots of Sophora flavescens Ait. that participates in vital pharmacological activities. Recombinant CYP450 supersomes and liver microsomes were used to study the metabolic profiles of kurarinone and its inhibitory actions against cytochrome P450 (CY...

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Main Authors: Youfa Qin, Yongkun Zhu, Xiaoyan Xue, Guanghui Zhou, Huibo Li, Jian Wang
Format: Article
Language:English
Published: Hindawi Limited 2020-01-01
Series:Evidence-Based Complementary and Alternative Medicine
Online Access:http://dx.doi.org/10.1155/2020/5267684
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spelling doaj-5e90900e42c540c995dfd63f4354575e2020-11-25T02:50:04ZengHindawi LimitedEvidence-Based Complementary and Alternative Medicine1741-427X1741-42882020-01-01202010.1155/2020/52676845267684An In Vitro Study for Evaluating Permeability and Metabolism of KurarinoneYoufa Qin0Yongkun Zhu1Xiaoyan Xue2Guanghui Zhou3Huibo Li4Jian Wang5Department of Clinical Pharmacy, SSL Central Hospital of Dongguan City, Dongguan, ChinaDepartment of Clinical Pharmacy, SSL Central Hospital of Dongguan City, Dongguan, ChinaDepartment of Clinical Pharmacy, SSL Central Hospital of Dongguan City, Dongguan, ChinaRehabilitation Department of Traditional Chinese Medicine, Dongguan Third People’s Hospital, Dongguan, ChinaDepartment of Pharmacy, Peking University Third Hospital, Beijing, ChinaSchool of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, ChinaKurarinone is a major component found in the dried roots of Sophora flavescens Ait. that participates in vital pharmacological activities. Recombinant CYP450 supersomes and liver microsomes were used to study the metabolic profiles of kurarinone and its inhibitory actions against cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes. 100 μM of kurarinone strongly inhibited more than 90% of UGT1A1, UGT1A6, CYP1A2, and CYP2C9. CYP1A2 and CYP2D6 played important roles in catalyzing the biotransformation of kurarinone. Moreover, metabolism of kurarinone considerably differs among species, and metabolic characteristics were similar between monkey and human. Kurarinone demonstrated moderate permeability at values of pH 4.0 and 7.4. Our findings offer a clearer idea to understand the pharmacological and toxicological mechanisms of kurarinone.http://dx.doi.org/10.1155/2020/5267684
collection DOAJ
language English
format Article
sources DOAJ
author Youfa Qin
Yongkun Zhu
Xiaoyan Xue
Guanghui Zhou
Huibo Li
Jian Wang
spellingShingle Youfa Qin
Yongkun Zhu
Xiaoyan Xue
Guanghui Zhou
Huibo Li
Jian Wang
An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone
Evidence-Based Complementary and Alternative Medicine
author_facet Youfa Qin
Yongkun Zhu
Xiaoyan Xue
Guanghui Zhou
Huibo Li
Jian Wang
author_sort Youfa Qin
title An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone
title_short An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone
title_full An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone
title_fullStr An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone
title_full_unstemmed An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone
title_sort in vitro study for evaluating permeability and metabolism of kurarinone
publisher Hindawi Limited
series Evidence-Based Complementary and Alternative Medicine
issn 1741-427X
1741-4288
publishDate 2020-01-01
description Kurarinone is a major component found in the dried roots of Sophora flavescens Ait. that participates in vital pharmacological activities. Recombinant CYP450 supersomes and liver microsomes were used to study the metabolic profiles of kurarinone and its inhibitory actions against cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes. 100 μM of kurarinone strongly inhibited more than 90% of UGT1A1, UGT1A6, CYP1A2, and CYP2C9. CYP1A2 and CYP2D6 played important roles in catalyzing the biotransformation of kurarinone. Moreover, metabolism of kurarinone considerably differs among species, and metabolic characteristics were similar between monkey and human. Kurarinone demonstrated moderate permeability at values of pH 4.0 and 7.4. Our findings offer a clearer idea to understand the pharmacological and toxicological mechanisms of kurarinone.
url http://dx.doi.org/10.1155/2020/5267684
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