The metabolites and biotransformation pathways in vivo after oral administration of ocotillol,RT5, and PF11 |
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Authors: | Jihua Liu Huizhu Gan Ting Li Jia Wang Guangguang Du Yang An Xiaojing Yan Cong Geng |
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Institution: | 1. College of Pharmacy, Jilin University, Changchun, 130021 China;2. China-Japan Union Hospital, Jilin University, Changchun, 130021 China;3. College of Pharmacy, Jilin University, Changchun, 130021 China
Department of Pharmaceutics, Changzhi Medical College, Changzhi, 046000 China;4. Department of Clinical Laboratory, The Second Affiliated Hospital of Dalian Medical University, Dalian, 16023 China |
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Abstract: | Ocotillol, pseudo-ginsenoside RT5 (RT5), and pseudo-ginsenoside F11 (PF11) are ocotillol-type saponins that have the same aglycone structure but with different numbers of glucose at the C-6 position. In this study, the metabolites of ocotillol, RT5, and PF11 in rat plasma, stomach, intestine, urine, and feces after oral administration were investigated by ultra-performance liquid chromatography coupled with time-of-flight mass spectrometry. The results showed that RT5 was easily biotransformed into metabolites in vivo, whereas PF11 and RT5 were difficult to be biotransformed. Hydrogenation, dehydrogenation, dehydration, deglycosylation, deoxygenation, hydration, phosphorylation, deoxidation, glucuronidation, and reactions combining amino acid were speculated to be involved in the biotransformation of ocotillol, RT5, and PF11. Based on the structural analysis of metabolites, it was deduced that hydrogenation, dehydration, deoxidation, and reactions combining amino acid occurred on the aglycone structure, whereas deglycosylation, hydration, and phosphorylation occurred on the glycosyl chain. Further, metabolites in plasma, urine, feces, and tissues were different: First, glucuronidation products were found in urine, stomach, intestine, and feces, but not in plasma. Second, the ocotillol prototype was not identified in urine samples. Third, the RT5 prototype was found in stomach, intestine, feces, and urine, but not in plasma. |
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Keywords: | biotransformation metabolite ocotillol pseudo-ginsenoside F11 pseudo-ginsenoside RT5 |
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