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The metabolites and biotransformation pathways in vivo after oral administrations of ocotillol, RT5 , and PF11.

Ocotillol, Pseudo-ginsenoside RT5 , and Pseudo-ginsenoside F11 are octilliol-type saponins, which have 0, 1, 2 of glucose at C-6 position with the same aglycone. In this paper, the metabolites of ocotilol, RT5 , and PF11 in rat plasma, stomach, intestine, urine, and feces after oral administrations were investigated with the method of ultra-performance liquid chromatography coupled with time of flight mass spectrometry (UPLC/QTOF-MS). The results showed that RT5 was easy to be transformed to metabolites in vivo. However, ocotillol was more difficult in biotransformation than PF11 and RT5 . The reactions of hydrogenation, dehydrogenation, dehydration, deglycosylation, deoxygenation, hydration, phosphorylation, deoxidation, glucuronidation, and combining amino acid were speculated to be involved in the transformation of ocotillol, RT5 and PF11 . Based on the structural analysis of metabolites, it was deduced that the transformation of hydrogenation, dehydration, deoxidation, and combining amino acid happened on aglycone, while deglycosylation, hydration, and phosphorylation occurred on glycosyl chain. It was found that the metabolites in plasma, urine, feces and tissues were different. Firstly, glucuronidation products were found in urine, stomach, intestine and feces, but not in plasma. Then, ocotillol prototype was not identified in urines. Eventually, RT5 prototype was found in stomach, intestine, feces and urine, but not in plasma.