ORIGINAL ARTICLES |
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3α-Hydroxybufadienolides in Bufo gallbladders: structural insights and biotransformation |
Li-Jun Ruan1,2, Zhi-Jun Song2, Ren-Wang Jiang1 |
1. State Key Laboratory of Bioactive Molecules and Draggability Assessment, College of Pharmacy, Jinan University, Guangzhou, 510632, China; 2. National Engineering Research Center for Southwest Endangered Medicinal Materials Resources Development, Guangxi Botanical Garden of Medicinal Plants, Nanning, 530023, China |
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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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Keywords
Bufadienolides
Bufo gargarizans
Toad bile
Self-defense
Biotransformation
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Fund:This work was financially supported by Guangxi Natural Science Foundation Program (Grant Number 2021GXNSFBA220068), National Natural Science Foundation of China (Grant Number 81872760 and 82204975), Natural Science Foundation of Guangdong province (Grant Number 2021A1515011251), Guangdong scientific scheme (Grant Number 2021A0505030032). |
Corresponding Authors:
Ren-Wang Jiang,E-mail:trwjiang@jnu.edu.cn
E-mail: trwjiang@jnu.edu.cn
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Issue Date: 16 May 2024
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