title: [Study on in vitro metabolic rate and metabolites or 9-dehydro-17-dehydro-andrographolide].
abstract: To investigate the metabolic rate and metabolites of 9-dehydro-17-dehydro-andrographolide, which is the main active ingredient in Xiyanping injection, by using the in vitro rat liver microsome incubation system. 9-dehydro-17-dehydro-andrographolide was incubated together with liver microsome mixed with NADPH. Its metabolic rate was studied by determining its residual concentrations with the UHPLC-MS/MS method; Its metabolites were identified by the UPLC-TOF-MS(E) method. The results showed that 9-dehydro-17-dehydro-andrographolide was metabolized faster than rat liver microsomes mixed with coenzymes, with t½ and CL of (19.7 ± 0.5) min and (35.1 ± 0.8) mL x min(-1) x g(-1) (protein), respectively. Based on the high resolution mass spectrum data and information from literatures, altogether nine metabolites of 9-dehydro-17-dehydro-andrographolide were identified in the incubation system, particularly hydroxylated and dehydrogenized products. The results of identification would provide a basis for screening out more active andrographolide derivatives.
authors.forename: Jun
authors.initials: J
authors.lastname: Shao
authors.forename: Wei-kang
authors.initials: WK
authors.lastname: Chen
authors.forename: Dong-kun
authors.initials: DK
authors.lastname: Zheng
authors.forename: Shuang-cheng
authors.initials: SC
authors.lastname: Ma
authors.forename: Yue-hua
authors.initials: YH
authors.lastname: Luo
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004224:Diterpenes / Q000737:chemistry* / Q000378:metabolism*; D004365:Drugs, Chinese Herbal / Q000737:chemistry* / Q000378:metabolism*; D008862:Microsomes, Liver / Q000737:chemistry / Q000378:metabolism; D015394:Molecular Structure; D051381:Rats; D053719:Tandem Mass Spectrometry
chemical_list: D004224:Diterpenes; D004365:Drugs, Chinese Herbal; C030419:andrographolide