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冠状菌素 E 衍生物的制备及抗菌活性。

Preparation and antibacterial activity of coronarin E derivatives.

机构信息

School of Chinese Medicine, Yunnan University of Chinese Medicine, Kunming, Yunnan, P. R. China.

Department of Pharmacy, Qilu Hospital of Shandong University, Jinan, Shandong, P. R. China.

出版信息

Nat Prod Res. 2024 Jun;38(11):1898-1908. doi: 10.1080/14786419.2023.2228982. Epub 2023 Jun 28.

Abstract

Coronarin E is a main diterpene ever isolated from . With the aim to enlarge its potential application, four butenolide derivatives (compounds , , and ) were obtained from coronarin E synthetic method, and their antibacterial effects were also evaluated. It is noteworthy that compounds and exhibited stronger antibacterial activities against most of the tested bacterial strains than ampicillin and kanamycin, two first- and second-line antimicrobials in clinical. For example, minimum inhibitory concentration (MIC) of , , ampicillin and kanamycin against were 2, 1, 8 and 4 μg/mL, respectively, and MIC of the four compounds mentioned above against were 1, 0.5, 16 and 4 μg/mL, respectively. The current studies not only enrich the structural diversity of diterpenes derived from genus, but also provide potent candidates for the development of antibacterial medicines.

摘要

冠状菌素 E 是从. 中分离得到的主要二萜类化合物。为了扩大其潜在应用,采用冠状菌素 E 的合成方法得到了四个丁烯内酯衍生物(化合物 、 、 和 ),并对其抗菌活性进行了评价。值得注意的是,化合物 和 对大多数测试的细菌菌株的抗菌活性均强于氨苄西林和卡那霉素,这两种是临床一线和二线的抗菌药物。例如,化合物 、 、氨苄西林和卡那霉素对 的最小抑菌浓度(MIC)分别为 2、1、8 和 4μg/mL,而上述四种化合物对 的 MIC 分别为 1、0.5、16 和 4μg/mL。本研究不仅丰富了来源于. 属的二萜类化合物的结构多样性,而且为抗菌药物的开发提供了有潜力的候选药物。

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