Murine metabolism and absorption of lancemaside A, an active compound in the roots of Codonopsis lanceolata

Abstract

Lancemaside A, a triterpenoid saponin isolated from the roots of Codonopsis lanceolata, has been reported to ameliorate the reduction of blood testosterone levels induced by immobilization stress in mice. In the present study, we investigated the metabolism and absorption of lancemaside A in mice. After oral administration of lancemaside A at 100 mg/kg body weight, the unmetabolized compound appeared rapidly in plasma (t (max) = 0.5 h). Lancemaside A has a low bioavailability (1.1%) because of its metabolism by intestinal bacteria and its poor absorption in the gastrointestinal tract. Furthermore, we identified four metabolites from the cecum of mice after oral administration of lancemaside A: codonolaside II, echinocystic acid, echinocystic acid 28-O-beta-D: -xylopyranosyl-(1 --> 4)-alpha-L: -rhamnopyranosyl-(1 --> 2)-alpha-L: -arabinopyranosyl ester, and echinocystic acid 28-O-alpha-L: -rhamnopyranosyl-(1 --> 2)-alpha-L: -arabinopyranosyl ester. Among these metabolites, codonolaside II and echinocystic acid were detected in plasma, and their t (max) values were 4 and 8 h, respectively. These findings should be helpful for understanding the mechanism of the biological effect of lancemaside A.

Novel PI3K/Akt Inhibitors Screened by the Cytoprotective Function of Human Immunodeficiency Virus Type 1 Tat

“…Recently Lancemaside A has been reported to control blood testosterone level in mice [34], as well as inhibiting LPS-induced inflammation [35]. Compound K has previously been identified as a putative anti-cancer agent [25], [36].…”

Safety assessment of saponins extract in Dolichos falcatus Klein: Subchronic study in Sprague-Dawley rats

“…In most cases, the bioavailability of saponins is low when taken orally because of their poor oral absorption and gastrointestinal metabolism (Han et al, 2006;Liang et al, 2007). Some of saponins are 15 transformed to their deglycosylated compounds by intestinal bacteria before being absorbed into blood in the normal gastrointestinal environment (Takeda et al, 1996;Ha et al, 2010;Komoto et al, 2010;Wang et al, 2012). During the process of evaluating histopathology in this study, a slight injury of gastrointestinal tract was observed in the high-dose male rats with hemolytic anemia.…”

Gut microbiota: a new angle for traditional herbal medicine research

“…138 Codonolaside II, echinocystic acid 28-O-b-D- xylopyranosyl-(1,4)a-L-rhamnopyranosyl-(1,2)-a-L-arabinopyranosyl ester, and echinocystic acid 28-O-a-L-rhamnopyranosyl-(1,2)-a-L-arabinopyranosyl ester are other products that were produced by glycosidic bond hydrolysis. 139 In a previous study, it was shown that echinocystic acid potently inhibited acetylcholinesterase activity, and signicantly reversed scopolamine-induced memory and learning decits on passive avoidance tasks. Echinocystic acid more potently shortened the escape latencies prolonged by treatment with scopolamine when compared to lancemaside A in a Morris water maze task.…”