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从蟾蜍毒液中筛选蟾蜍毒内酯,鉴定出 γ- 蟾蜍毒它灵是一种有潜力的抗炎剂。

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

机构信息

Third Level Research Laboratory of State Administration of Traditional Chinese Medicine, School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, P. R. China.

Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Guangzhou, P. R. China.

出版信息

Planta Med. 2022 Jan;88(1):43-52. doi: 10.1055/a-1248-2626. Epub 2020 Oct 13.

DOI:10.1055/a-1248-2626
PMID:33049786
Abstract

Toad venom () 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-, CuSO-, 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.

摘要

蟾蜍毒液 () 在中国和东亚/东南亚国家被用于治疗感染和炎症性疾病。然而,蟾蜍毒液的抗炎成分尚未得到系统评估和明确界定。为了研究蟾蜍毒液的抗炎作用并鉴定新的抗炎成分,我们使用斑马鱼作为替代药物筛选模型,评估了之前从蟾蜍毒液中分离得到的 14 种蟾蜍甾烯类化合物的抗炎作用。结果发现,大多数蟾蜍甾烯类化合物对脂多糖、CuSO 或尾部横断引起的斑马鱼炎症模型具有显著的抗炎作用。此外,γ-蟾蜍毒它灵( 6: )通过抑制髓样分化初级反应 88/核因子-κB 和 STAT3 信号通路抑制脂多糖诱导的炎症。本研究证实了斑马鱼在药物筛选中的潜力,阐明了蟾蜍毒液中蟾蜍甾烯类化合物的抗炎作用,并表明 γ-蟾蜍毒它灵将来可能被开发为治疗炎症性疾病的新型治疗剂。

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