title: Quantitatively metabolic profiles of salvianolic acids in rats after gastric-administration of Salvia miltiorrhiza extract.
abstract: Salvianolic acids, the well-known active components in Salvia miltiorrhiza, have been shown to possess markedly pharmacological activities. However, due to the complex in vivo course after administration, the pharmacologically active forms are still poorly understood. In present study, we evaluated the stability of eight major salvianolic acids from Danshen extract under different chemical and physiological conditions. We also quantitatively explained the absorption, metabolism and excretion of these salvianolic acids in rats after gastric-administration, which was carried out by simultaneously determining the amounts of salvianolic acids and their metabolites in the rat gastrointestinal contents, gastrointestinal mucosa, plasma, bile and urine. We found that: 1) protocatechuic aldehyde (PAL) was much stable whether in acidic environment (pH4.0) or in alkaline environment (pH8.0), while other salvianolic acids were stable in acidic environment and instable in alkaline environment; 2) PAL, salvianoli acid A (SAA) and salvianolic acid B (SAB) were instable whether in rat stomach or in small intestine, while other salvianolic acids were stable in rat stomach and instable in small intestine; 3) after gastric-administration, except PAL and Danshensu (DSS), other phenolic acids would be metabolized into DSS and caffeic acid (CA) in the rat gastrointestinal tract before absorption, and only free and glucuronidated PAL, CA and DSS were detected in rat plasma, bile and urine. In conclusion, it was the free and glucuronidated PAL, CA and DSS rather than the prototypes of other salvianolic acids that were present in plasma with considerable concentrations after gastric-administration.
authors.affiliation: Department of Pediatrics, Hangzhou First People's Hospital (Hangzhou Hospital affiliated Nanjing Medical University), Hangzhou 310006, China.
authors.forename: Zhanli
authors.initials: Z
authors.lastname: Liu
authors.affiliation: Department of Pediatrics, Hangzhou First People's Hospital (Hangzhou Hospital affiliated Nanjing Medical University), Hangzhou 310006, China.
authors.forename: Xunyang
authors.initials: X
authors.lastname: Zheng
authors.affiliation: Chongqing Academy of Chinese Materia Medica, No.34, Nanshan Road, Nan'an District, Chongqing 400065, China.
authors.forename: Yanlei
authors.initials: Y
authors.lastname: Guo
authors.affiliation: Chongqing Academy of Chinese Materia Medica, No.34, Nanshan Road, Nan'an District, Chongqing 400065, China.
authors.forename: Weihan
authors.initials: W
authors.lastname: Qin
authors.affiliation: Chongqing Academy of Chinese Materia Medica, No.34, Nanshan Road, Nan'an District, Chongqing 400065, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Hua
authors.affiliation: Chongqing Academy of Chinese Materia Medica, No.34, Nanshan Road, Nan'an District, Chongqing 400065, China. Electronic address: yangychem@126.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Yang
mesh_terms: D000475:Alkenes / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D001547:Benzaldehydes / Q000737:chemistry / Q000493:pharmacokinetics; D002109:Caffeic Acids / Q000737:chemistry / Q000493:pharmacokinetics; D002396:Catechols / Q000737:chemistry / Q000493:pharmacokinetics; D004355:Drug Stability; D004365:Drugs, Chinese Herbal / Q000493:pharmacokinetics*; D062385:Hydroxybenzoates / Q000737:chemistry / Q000493:pharmacokinetics; D007773:Lactates / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D055442:Metabolome; D015394:Molecular Structure; D059808:Polyphenols / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D027561:Salvia miltiorrhiza / Q000737:chemistry
chemical_list: D000475:Alkenes; D001547:Benzaldehydes; D002109:Caffeic Acids; D002396:Catechols; D004365:Drugs, Chinese Herbal; D062385:Hydroxybenzoates; D007773:Lactates; D059808:Polyphenols; C568740:salvianolic acid; C028972:dan-shen root extract; C035055:3,4-dihydroxyphenyllactic acid; C005581:protocatechualdehyde; C017616:phenolic acid; C040048:caffeic acid
keywords: Glucuronidation; Metabolism; Protocatechuic acid; Protocatechuic aldehyde; Salvianolic acid; Stability