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刺芒柄花素渗透性与代谢的体外评价研究

An In Vitro Study for Evaluating Permeability and Metabolism of Kurarinone.

作者信息

Qin Youfa, Zhu Yongkun, Xue Xiaoyan, Zhou Guanghui, Li Huibo, Wang Jian

机构信息

Department of Clinical Pharmacy, SSL Central Hospital of Dongguan City, Dongguan, China.

Rehabilitation Department of Traditional Chinese Medicine, Dongguan Third People's Hospital, Dongguan, China.

出版信息

Evid Based Complement Alternat Med. 2020 Sep 13;2020:5267684. doi: 10.1155/2020/5267684. eCollection 2020.

DOI:10.1155/2020/5267684
PMID:33005200
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7509555/
Abstract

Kurarinone is a major component found in the dried roots of 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 M 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.

摘要

苦参酮是从朝鲜槐干燥根中发现的一种主要成分，具有重要的药理活性。使用重组CYP450超微粒体和肝微粒体研究苦参酮的代谢谱及其对细胞色素P450（CYP）和尿苷二磷酸葡萄糖醛酸基转移酶（UGT）的抑制作用。100μM的苦参酮强烈抑制超过90%的UGT1A1、UGT1A6、CYP1A2和CYP2C9。CYP1A2和CYP2D6在催化苦参酮的生物转化中起重要作用。此外，苦参酮的代谢在不同物种之间有很大差异，猴子和人类之间的代谢特征相似。苦参酮在pH值为4.0和7.4时表现出中等通透性。我们的研究结果为理解苦参酮的药理和毒理机制提供了更清晰的认识。

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Sophoraflavanone G from Sophora flavescens induces apoptosis in triple-negative breast cancer cells.
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Inhibition of Cytochrome P450 Activities by Extract and Its Prenylated Flavonoids in Human Liver Microsomes.提取物及其异戊烯基黄酮对人肝微粒体细胞色素P450活性的抑制作用。
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