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抑制石蒜裂碱对细胞色素 P450 酶活性的影响。

inhibitory effect of lysionotin on the activity of cytochrome P450 enzymes.

机构信息

Department of Neurology, The Affiliated Hospital of Qingdao University, Qingdao, China.

Department of Neurology, Zibo No. 4 People's Hospital, Zibo, China.

出版信息

Pharm Biol. 2020 Dec;58(1):695-700. doi: 10.1080/13880209.2020.1787468.

DOI:10.1080/13880209.2020.1787468
PMID:32673137
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7470033/
Abstract

CONTEXT

Lysionotin, a major extraction of Maxim (Gesneriaceae), has a variety of pharmacological properties commonly used in the treatment of lung disease. A study of lysionotin on the activity of human liver cytochrome P450 (CYP) enzymes can provide guidance on the clinical application of lysionotin.

OBJECTIVE

This study investigated the interaction between lysionotin and CYPs.

MATERIAL AND METHOD

The effects of 100 μM lysionotin on eight human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19 and 2C8) were investigated using human liver microsomes (HLMs) with specific inhibitor as positive control and untreated HLMs as control. Meanwhile, the enzyme kinetic parameters were calculated. A time-dependent study was performed with a time interval of 5 min in 30 min.

RESULTS

Lysionotin was found to inhibit the activity of CYP3A4, 2C19, and 2C8, with IC values of 13.85, 24.95, and 30.05 μM, respectively. The inhibition of CYP3A4 was performed in a non-competitive manner with the value of 6.83 μM, while the inhibition of CYP2C19 and 2C8 was performed in a competitive manner with values of 12.41 and 14.51 μM. Moreover, it was found that the inhibition of CYP3A4 was time-dependent with / value of 6.618/0.048 min/μM. The inhibitory effect of lysionotin on the activity of CYP3A4, 2C19, and 2C8 indicated potential drug interactions between lysionotin and drugs metabolised by CYP3A4, 2C19, and 2C8. Further experiments are needed to assess the potential interactions.

摘要

背景

木蝴蝶属（Gesneriaceae）的主要提取物赖西诺汀具有多种药理学特性，常用于治疗肺部疾病。研究赖西诺汀对人肝细胞色素 P450（CYP）酶活性的影响，可以为赖西诺汀的临床应用提供指导。

目的

本研究旨在探讨赖西诺汀与 CYP 之间的相互作用。

材料和方法

采用人肝微粒体（HLMs）作为研究体系，以特异性抑制剂为阳性对照，未处理的 HLMs 为空白对照，研究 100μM 赖西诺汀对 8 种人肝 CYP 同工酶（即 1A2、3A4、2A6、2E1、2D6、2C9、2C19 和 2C8）的影响。同时，计算酶动力学参数。在 30 分钟内每隔 5 分钟进行一次时间依赖性研究。

结果

赖西诺汀对 CYP3A4、2C19 和 2C8 的活性有抑制作用，IC 分别为 13.85、24.95 和 30.05μM。CYP3A4 的抑制呈非竞争性， 值为 6.83μM，而 CYP2C19 和 2C8 的抑制呈竞争性， 值分别为 12.41 和 14.51μM。此外，研究发现 CYP3A4 的抑制具有时间依赖性， 值为 6.618/0.048min/μM。赖西诺汀对 CYP3A4、2C19 和 2C8 活性的抑制表明赖西诺汀与经 CYP3A4、2C19 和 2C8 代谢的药物之间可能存在药物相互作用。需要进一步的实验来评估潜在的相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/52d41e286b97/IPHB_A_1787468_F0008_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/b4d3051210f5/IPHB_A_1787468_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/bf15463a0ce7/IPHB_A_1787468_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/eb96c10ee2ce/IPHB_A_1787468_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/73f59e8fea45/IPHB_A_1787468_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/cfa16376d114/IPHB_A_1787468_F0005_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/215b872b8eed/IPHB_A_1787468_F0006_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/746b072f9782/IPHB_A_1787468_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/52d41e286b97/IPHB_A_1787468_F0008_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/b4d3051210f5/IPHB_A_1787468_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/bf15463a0ce7/IPHB_A_1787468_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/eb96c10ee2ce/IPHB_A_1787468_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/73f59e8fea45/IPHB_A_1787468_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/cfa16376d114/IPHB_A_1787468_F0005_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/215b872b8eed/IPHB_A_1787468_F0006_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/746b072f9782/IPHB_A_1787468_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47b9/7470033/52d41e286b97/IPHB_A_1787468_F0008_B.jpg

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3
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4
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5
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6
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5
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6
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