丹参酸 B 在大鼠体内静脉给药后的代谢产物的鉴定和药代动力学研究。
The identification and pharmacokinetic studies of metabolites of salvianolic acid B after intravenous administration in rats.
机构信息
State Key Laboratory of Natural Medicines, Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
State Key Laboratory of Natural Medicines, Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
出版信息
Chin J Nat Med. 2013 Sep;11(5):560-5. doi: 10.1016/S1875-5364(13)60101-6.
AIM
To identify and quantify the major metabolites of salvianolic acid B (SAB) after intravenous injection in rats.
METHODS
LC-IT/TOF-MS was used to identify the metabolites in rat bile, plasma, and urine; LC-MS/MS was used to quantify the two major metabolites.
RESULTS
In rat bile, plasma, and urine, nine metabolites were identified, including methylated metabolites of SAB, lithospermic acid (LSA), the decarboxylation and methylation metabolites of LSA, salvianolic acid S (SAS), and dehydrated-SAS. The t1/2 of monomethyl-SAB and LSA were both very short, and monomethyl-SAB had a larger AUC than LSA in rats.
CONCLUSION
Nine metabolites were found, the metabolic pathway was described, and the pharmacokinetic profiles of LSA and monomethyl-SAB were studied, thereby clarifying that methylation was the dominant metabolic pathway for SAB in rats.
目的
鉴定并定量分析丹参酸 B（SAB）在大鼠体内静脉注射后的主要代谢产物。
方法
采用 LC-IT/TOF-MS 鉴定大鼠胆汁、血浆和尿液中的代谢产物；采用 LC-MS/MS 定量分析两种主要代谢产物。
结果
在大鼠胆汁、血浆和尿液中鉴定出 9 种代谢产物，包括 SAB 的甲基化产物、丹酚酸 B（LSA）、LSA 的脱羧和甲基化产物、丹参酸 S（SAS）和脱水-SAS。单甲基-SAB 和 LSA 的 t1/2 均非常短，且单甲基-SAB 在大鼠体内的 AUC 大于 LSA。
结论
发现 9 种代谢产物，描述了代谢途径，并研究了 LSA 和单甲基-SAB 的药代动力学特征，从而阐明了在大鼠体内 SAB 的主要代谢途径为甲基化。
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