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灯盏花素对六种人/大鼠细胞色素P450酶和P-糖蛋白的体外抑制作用。

In vitro inhibitory effects of scutellarin on six human/rat cytochrome P450 enzymes and P-glycoprotein.

作者信息

Han Yong-Long, Li Dan, Yang Quan-Jun, Zhou Zhi-Yong, Liu Li-Ya, Li Bin, Lu Jin, Guo Cheng

机构信息

Department of Pharmacy, Shanghai Jiao Tong University Affiliated Sixth People's Hospital, No. 600 Yishan Road, Shanghai 200233, China.

出版信息

Molecules. 2014 May 5;19(5):5748-60. doi: 10.3390/molecules19055748.

DOI:10.3390/molecules19055748
PMID:24802986
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6271944/
Abstract

Inhibition of cytochrome P450 (CYP) and P-glycoprotein (P-gp) are regarded as the most frequent and clinically important pharmacokinetic causes among the various possible factors for drug-drug interactions. Scutellarin is a flavonoid which is widely used for the treatment of cardiovascular diseases. In this study, the in vitro inhibitory effects of scutellarin on six major human CYPs (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six rat CYPs (CYP1A2, CYP2C7, CYP2C11, CYP2C79, CYP2D4, and CYP3A2) activities were examined by using liquid chromatography-tandem mass spectrometry. Meanwhile, the inhibitory effects of scutellarin on P-gp activity were examined on a human metastatic malignant melanoma cell line WM-266-4 by calcein-AM fluorometry screening assay. Results demonstrated that scutellarin showed negligible inhibitory effects on the six major CYP isoenzymes in human/rat liver microsomes with almost all of the IC50 values exceeding 100 μM, whereas it showed values of 63.8 μM for CYP2C19 in human liver microsomes, and 63.1 and 85.6 μM for CYP2C7 and CYP2C79 in rat liver microsomes, respectively. Scutellarin also showed weak inhibitory effect on P-gp. In conclusion, this study demonstrates that scutellarin is unlikely to cause any clinically significant herb-drug interactions in humans when co-administered with substrates of the six CYPs (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and P-gp.

摘要

细胞色素P450（CYP）和P-糖蛋白（P-gp）的抑制作用被认为是药物相互作用各种可能因素中最常见且具有临床重要性的药代动力学原因。灯盏花素是一种广泛用于治疗心血管疾病的黄酮类化合物。在本研究中，通过液相色谱-串联质谱法检测了灯盏花素对六种主要人源CYP（CYP1A2、CYP2C8、CYP2C9、CYP2C19、CYP2D6和CYP3A4）和六种大鼠CYP（CYP1A2、CYP2C7、CYP2C11、CYP2C79、CYP2D4和CYP3A2）活性的体外抑制作用。同时，通过钙黄绿素-AM荧光筛选试验在人转移性恶性黑色素瘤细胞系WM-266-4上检测了灯盏花素对P-gp活性的抑制作用。结果表明，灯盏花素对人/大鼠肝微粒体中的六种主要CYP同工酶显示出可忽略不计的抑制作用，几乎所有IC50值均超过100μM，而在人肝微粒体中对CYP2C19的IC50值为63.8μM，在大鼠肝微粒体中对CYP2C7和CYP2C79的IC50值分别为63.1和85.6μM。灯盏花素对P-gp也显示出较弱的抑制作用。总之，本研究表明，灯盏花素与六种CYP（CYP1A2、CYP2C8、CYP2C9、CYP2C19、CYP2D6和CYP3A4）和P-gp的底物合用时，不太可能在人体内引起任何具有临床意义的药草-药物相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/a0e39ae384d0/molecules-19-05748-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/b8e90c388c6c/molecules-19-05748-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/e99f8b01e6b1/molecules-19-05748-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/65b0a7a0b892/molecules-19-05748-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/a0e39ae384d0/molecules-19-05748-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/b8e90c388c6c/molecules-19-05748-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/e99f8b01e6b1/molecules-19-05748-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/65b0a7a0b892/molecules-19-05748-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c5fe/6271944/a0e39ae384d0/molecules-19-05748-g004.jpg

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