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19-羟基蟾毒它灵,一种从中美洲特有蟾蜍 Rhinella centralis(蟾蜍科)的腮腺分泌物中分离得到的主要蟾毒内酯,可抑制克氏锥虫的生长。

19-Hydroxy-bufalin, a major bufadienolide isolated from the parotoid gland secretions of the Panamanian endemic toad Rhinella centralis (Bufonidae), inhibits the growth of Trypanosoma cruzi.

机构信息

Centro de Biodiversidad y Descubrimiento de Drogas, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT AIP), Panama; Department of Biotechnology, Acharya Nagarjuna University, India; Departamento de Bioquímica, Facultad de Ciencias Naturales, Exactas y Tecnología, Universidad de Panamá, Panama.

Smithsonian Tropical Research Institute (STRI), Panama; Departamento de Zoología, Facultad de Ciencias Naturales, Exactas y Tecnología, Universidad de Panamá, Panama.

出版信息

Toxicon. 2020 Apr 15;177:89-92. doi: 10.1016/j.toxicon.2020.02.009. Epub 2020 Feb 13.

DOI:10.1016/j.toxicon.2020.02.009
PMID:32061723
Abstract

American trypanosomiasis is a parasitic neglected disease, responsible for the death of approximately 10,000 people every year. Amphibians are recognized for producing in their cutaneous glands substances with pharmacological potential against a variety of pathologies. Here we investigated the antiprotozoal activity against Trypanosoma cruzi of bufadienolides isolated from the parotoid glands secretions of the toad Rhinella centralis from Panama. NMR and mass spectrometry analysis led to the identification of the active compound 19-hydroxy-bufalin, for which its antitrypanosomal activity and occurrence in the genus Rhinella are reported for the first time. This compound showed low cytotoxicity and significant selectivity which confers to it a potential role for the treatment of Chagas disease.

摘要

美洲锥虫病是一种寄生虫性被忽视疾病,每年导致约 10000 人死亡。两栖动物因其皮肤腺产生具有多种病理治疗潜力的物质而被认可。在这里,我们研究了来自巴拿马中央蟾蜍的腮腺分泌物中分离出的蟾蜍内酯对克氏锥虫的抗原生动物活性。NMR 和质谱分析导致了活性化合物 19-羟基-蟾蜍精的鉴定,这是首次报道其抗锥虫活性和在 Rhinella 属中的存在。该化合物显示出低细胞毒性和显著的选择性,这使其有可能用于治疗恰加斯病。

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引用本文的文献

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Antimicrobial Secretions of Toads (Anura, Bufonidae): Bioactive Extracts and Isolated Compounds against Human Pathogens.
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