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Published on: November 27, 2016
3α-Hydroxybufadienolides in Bufo gallbladders: structural insights and biotransformation
Li-Jun Ruan1,2, Zhi-Jun Song2, Ren-Wang Jiang3
1State Key Laboratory of Bioactive Molecules and Draggability Assessment, College of Pharmacy, Jinan University, Guangzhou, 510632, China.
Abstract:
Bufadienolides, naturally occurring steroids primarily found in toads, have garnered attention for their pharmacological properties and ecological significance. In this study, we isolated and identified 21 bufadienolides from the gallbladders of Bufo gargarizans, comprising four new compounds and 17 known ones. Notably, the predominance of 15 bufadienolides with a 3α-OH configuration in toad bile differs significantly from the 3β-OH bufadienolides found in venom secreted by toad glands. Moreover, our investigation into the biotransformation of 3β-OH and 3α-OH bufadienolides in the liver and kidney tissues of toads revealed an irreversible conversion from 3β-OH to 3α-OH bufadienolides, suggesting a crucial role in toad self-detoxification. These findings provide valuable insights into the structural diversity of bufadienolides and advance our understanding of their medical and ecological significance.
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