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某些细胞松弛素及其衍生物对疫霉属物种的抗真菌活性。

Fungitoxic activity of some cytochalasins and their derivatives on Phytophthora species.

作者信息

Evidente A, Cristinzio G, Capasso R, Andolfi A

机构信息

Dipartimento di Scienze Chimico-Agrarie, Università di Napoli Federico II, Portici, Italy.

出版信息

Nat Toxins. 1997;5(6):228-33. doi: 10.1002/(sici)1522-7189(1997)5:6<228::aid-nt2>3.0.co;2-m.

Abstract

The activity of cytochalasin B was tested on 8 Phytophthora species, while the same toxin, some of its derivatives and natural analogues, namely cytochalasin F and deoxaphomin, were assayed at 2 x 10(-5) - 2 x 10(-4) M on the most sensitive species, P. cactorum. A significant inhibitory activity on P. cactorum was shown by cytochalasin B, its 7-monoacetyl derivative, and deoxaphomin. The hydroxy group at C-20 and the conformational freedom of the macrocyclic ring proved to be important structural features for this activity. The 7-hydroxy group at C-7 appeared to have no influence on this toxicity, while a size reduction associated with the carbocyclic nature of the macrocycle seems to lightly increase the activity. The 7-O-acetylcytochalasin B showed selective toxic activity on P. cactorum at the tested concentration, thus suggesting a possible use as a fungicide for this compound.

摘要

在8种疫霉属物种上测试了细胞松弛素B的活性,而对于最敏感的物种恶疫霉,在2×10⁻⁵ - 2×10⁻⁴ M浓度下测定了相同毒素、其一些衍生物和天然类似物,即细胞松弛素F和脱氧腐壳菌素的活性。细胞松弛素B、其7-单乙酰衍生物和脱氧腐壳菌素对恶疫霉表现出显著的抑制活性。C-20位的羟基和大环的构象自由度被证明是该活性的重要结构特征。C-7位的7-羟基似乎对这种毒性没有影响,而与大环的碳环性质相关的尺寸减小似乎会轻微增加活性。7-O-乙酰基细胞松弛素B在测试浓度下对恶疫霉表现出选择性毒性活性,因此表明该化合物可能用作杀真菌剂。

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