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首页> 美国卫生研究院文献>Molecules >Antifungal Activity of Chemical Constituents from Piper pesaresanum C. DC. and Derivatives against Phytopathogen Fungi of Cocoa
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Antifungal Activity of Chemical Constituents from Piper pesaresanum C. DC. and Derivatives against Phytopathogen Fungi of Cocoa

机译：吹笛性百乙酸乙酸乙酸乙烯化学成分的抗真菌活性。抗Cocoa植物病毒真菌的衍生物

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摘要

In this study, the antifungal potential of chemical constituents from Piper pesaresanum and some synthesized derivatives was determined against three phytopathogenic fungi associated with the cocoa crop. The methodology included the phytochemical study on the aerial part of P. pesaresanum, the synthesis of some derivatives and the evaluation of the antifungal activity against the fungi Moniliophthora roreri, Fusarium solani and Phytophthora sp. The chemical study allowed the isolation of three benzoic acid derivatives (1–3), one dihydrochalcone (4) and a mixture of sterols (5–7). Seven derivatives (8–14) were synthesized from the main constituents, of which compounds 9, 10, 12 and 14 are reported for the first time. Benzoic acid derivatives showed strong antifungal activity against M. roreri, of which 11 (3.0 ± 0.8 µM) was the most active compound with an IC50 lower compared with positive control Mancozeb® (4.9 ± 0.4 µM). Dihydrochalcones and acid derivatives were active against F. solani and Phytophthora sp., of which 3 (32.5 ± 3.3 µM) and 4 (26.7 ± 5.3 µM) were the most active compounds, respectively. The preliminary structure–activity relationship allowed us to establish that prenylated chains and the carboxyl group are important in the antifungal activity of benzoic acid derivatives. Likewise, a positive influence of the carbonyl group on the antifungal activity for dihydrochalcones was deduced.
机译：在该研究中，针对与可可作物相关的三种植物致病性真菌来确定来自吹笛者Pesaresanum和一些合成衍生物的化学成分的抗真菌潜力。该方法包括对P. Pesaresanum的空中部分的植物化学研究，一些衍生物的合成以及对真菌Monilioophthora Roreri，Fusarium solani和Phytophthora sp的抗真菌活性的评价。化学研究允许分离三种苯甲酸衍生物（1-3），一种二羟基酮（4）和甾醇的混合物（5-7）。从主要成分中合成了七种衍生物（8-14），其中第一次报告化合物9,10,12和14。苯甲酸衍生物对M. roreri表现出强烈的抗真菌活性，其中11（3.0±0.8μm）是具有IC50的最活性化合物，与阳性对照Mancozeb®（4.9±0.4μm）相比。二羟基酮和酸衍生物对F.Solani和Phytophthora SP有效。其中3（32.5±3.3μm）和4（26.7±5.3μm）分别是最活性化合物。初步结构 - 活性关系使我们建立戊酰化链和羧基在苯甲酸衍生物的抗真菌活性中是重要的。同样地，推导出羰基对二羟基酮抗真菌活性的阳性影响。

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