کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5850507 | 1561776 | 2014 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Evaluation of the in vitro/in vivo drug interaction potential of BST204, a purified dry extract of ginseng, and its four bioactive ginsenosides through cytochrome P450 inhibition/induction and UDP-glucuronosyltransferase inhibition
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کلمات کلیدی
tmax20(R)-ginsenoside Rg320(S)-ginsenoside Rg3the 50% inhibitory concentrationAUC0–tUGTIC50CyPCmaxLC–MS/MS - LC-MS / MSNADP+ - NADP +UDP-glucuronosyltransferase - UDP-گلوکورونوسیل ترانسفرازβ-nicotinamide adenine dinucleotide phosphate - β-نیکوتین آمید آدنین دینکلوتید فسفاتtime to reach Cmax - زمان برای رسیدن به CmaxCytochrome P450 - سیتوکروم پی۴۵۰Peak plasma concentration - غلظت پلاسما در قلهliquid chromatography–tandem mass spectrometry - کروماتوگرافی مایع و اسپکترومتری توده دو طرفه
موضوعات مرتبط
علوم زیستی و بیوفناوری
علوم کشاورزی و بیولوژیک
دانش تغذیه
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We evaluated the potential of BST204, a purified dry extract of ginseng, to inhibit or induce human liver cytochrome P450 enzymes (CYPs) and UDP-glucuronosyltransferases (UGTs) in vitro to assess its safety. In vitro drug interactions of four bioactive ginsenosides of BST204, S-Rg3, R-Rg3, S-Rh2, and R-Rh2, were also evaluated. We demonstrated that BST204 slightly inhibited CYP2C8, CYP2D6, CYP2C9, and CYP2B6 activities with IC50 values of 17.4, 26.8, 31.5, and 49.7 μg/mL, respectively. BST204 also weakly inhibited UGT1A1, UGT1A9, and UGT2B7 activities with IC50 values of 14.5, 26.6, and 31.5 μg/mL, respectively. The potential inhibition by BST204 of the three UGT activities might be attributable to S-Rg3, at least in part, as its inhibitory pattern was similar to that of BST204. However, BST204 showed no time-dependent inactivation of the nine CYPs studied. In addition, BST204 did not induce CYP1A2, 2B6, or 3A4/5. On the basis of an in vivo interaction studies, our data strongly suggest that BST204 is unlikely to cause clinically significant drug-drug interactions mediated via inhibition or induction of most CYPs or UGTs involved in drug metabolism in vivo. Our findings offer a clearer understanding and possibility to predict drug-drug interactions for the safe use of BST204 in clinical practice.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Food and Chemical Toxicology - Volume 68, June 2014, Pages 117-127
Journal: Food and Chemical Toxicology - Volume 68, June 2014, Pages 117-127
نویسندگان
Yu Fen Zheng, Soo Hyeon Bae, Eu Jin Choi, Jung Bae Park, Sun Ok Kim, Min Jung Jang, Gyu Hwan Park, Wan Gyoon Shin, Euichaul Oh, Soo Kyung Bae,