Screening of Bufadienolides from Toad Venom Identifies Gammabufotalin as a Potential Anti-inflammatory Agent

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Abstract
Toad venom (Chansu) is used in the treatment of infectious and inflammatory diseases in China and East/Southeast Asian countries. However, the anti-inflammatory components of toad venom have not yet been systematically evaluated and clearly defined. To investigate the anti-inflammatory effects of toad venom and identify new anti-inflammatory ingredients, we used zebrafish, an alternative drug screening model, to evaluate the anti-inflammatory effects of 14 bufadienolides previously isolated from toad venom. Most of the bufadienolides were found to exert significant anti-inflammatory effects on lipopolysaccharide-, CuSO4-, or tail transection-induced zebrafish inflammatory models. Moreover, gammabufotalin ( 6) inhibits lipopolysaccharide-induced inflammation by suppressing the myeloid differentiation primary response 88/nuclear factor-kappa B and STAT3 signal pathways. This study confirms the potential of zebrafish in drug screening, clarifies the anti-inflammatory effects of bufadienolides from toad venom, and indicates that gammabufotalin may be developed as a novel therapeutic agent for inflammatory diseases in the future. Received: 01 February 2020 Accepted after revision: 23 August 2020 Publication Date: 13 October 2020 (online) © 2020. Thieme. All rights reserved. Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany
Funding Information
  • the Guangzhou Education Bureau University Scientific Research project (201831845)
  • The Guangdong Province Universities and Colleges Pearl River Scholar Funded Scheme (GDHVPS2018)
  • the Applied Basic Research Programs of Yunnan Province for Youths (No.2017FD110)
  • the National Science Foundation of China (81730110, 81903886, 81973544)
  • the National Science Foundation of China (81730110, 81903886, 81973544)
  • the National Science Foundation of China (81730110, 81903886, 81973544)
  • Young Elite Scientists Sponsorship Program by CACM (2019-QNRC2-C14)

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