Design, Synthesis, and Antifungal Evaluation of Neocryptolepine Derivatives against Phytopathogenic Fungi
作者:Jia-Kai Zhu、Jian-Mei Gao、Cheng-Jie Yang、Xiao-Fei Shang、Zhong-Min Zhao、Raymond Kobla Lawoe、Rui Zhou、Yu Sun、Xiao-Dan Yin、Ying-Qian Liu
DOI:10.1021/acs.jafc.9b06793
日期:2020.2.26
isolated from traditional African herbal medicine Cryptolepis sanguinolenta, and its broad spectrum of biological activities has been illuminated in past decades. In this study, neocryptolepine and its derivatives (1-49) were designed and synthesized from economical and readily available starting materials. Their structures were confirmed by proton nuclear magnetic resonance, carbon nuclear magnetic resonance
Neocryptolepine是一种从传统非洲草药Cryptolepis sanguinolenta中分离出来的生物碱,在过去的几十年中,其广泛的生物活性得到了阐明。在这项研究中,从经济且容易获得的原料中设计和合成了新隐油菜籽及其衍生物(1-49)。通过质子核磁共振,碳核磁共振和质谱法证实了它们的结构。筛选了合成的化合物对六种农业上重要的真菌茄根丝枯病菌,灰葡萄孢(B. cinerea),禾谷镰刀菌,冬瓜霉菌,菌核菌和稻瘟病菌的抗真菌特性。体外测定结果表明,化合物5、21、24、35、40、45,47和47对EC值低于1μg/ mL的真菌表现出显着的抗真菌活性。明显地,化合物24显示出对灰葡萄芽孢杆菌的最有效的抑制效力(EC 50 =0.07μg/ mL),并且来自体内实验的数据表明,化合物24表现出与阳性对照的鳞茎鳞茎相当的保护活性。初步的机理研究表明,化合物24显示出令人印象深刻的孢子