研究动态
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Cladoic Acid,一种来自枝孢菌属的抗克氏锥虫聚酮化合物。 TP-F2020。

Cladoic Acid, an Anti-Trypanosoma cruzi Polyketide from Cladosporium sp. TP-F2020.

发表日期:2024 Aug 05
作者: Md Masud Rana, Shiyang Lu, Tatiana Ascencio Menjívar, Keisuke Fukaya, Junko Nakajima-Shimada, Daisuke Urabe, Yasuhiro Igarashi
来源: JOURNAL OF NATURAL PRODUCTS

摘要:

从枝孢属真菌中分离出一种新的聚酮化合物——枝酸。通过广泛的光谱分析阐明了具有全E三烯侧链的高度氧化的反式十氢化萘环的结构。计算机辅助构象分析证明了反十氢萘核心独特的椅/扭船构象和B环的灵活性。枝酸对克氏锥虫有活性,并抑制无鞭毛体和上鞭毛体的增殖,IC50 值分别为 27 和 46 μM,但它对 P388 鼠白血病细胞、细菌或真菌没有表现出任何明显的活性,表明它是一种潜在的药物。抗恰加斯病药物开发的候选者。
A new polyketide, cladoic acid, was isolated from a fungus of the genus Cladosporium. The structure of the highly oxygenated trans-decalin ring with an all-E triene side chain was elucidated by extensive spectroscopic analysis. The unique chair/twist-boat conformation of the trans-decalin core and the flexibility of the B-ring were demonstrated by computer-aided conformational analysis. Cladoic acid was active against Trypanosoma cruzi and inhibited the proliferation of amastigotes and epimastigotes with IC50 values of 27 and 46 μM, respectively, but it did not show any appreciable activity against P388 murine leukemia cells, bacteria, or fungi, indicating it is a potential candidate for drug development against Chagas disease.