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从中国千里光中提取的抗口腔常见病原菌的炔酸类化合物

Anti-oral common pathogenic bacterial active acetylenic acids from Thesium chinense Turcz.

机构信息

The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.

Department of Periodontology, Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.

出版信息

J Nat Med. 2018 Mar;72(2):433-438. doi: 10.1007/s11418-018-1180-3. Epub 2018 Feb 12.

Abstract

Discovery of agents for oral infectious diseases is always encouraged in natural products chemistry. A bioassay-guided isolation led to the isolation of two new acetylenic acids (1, 2) along with seven known ones (3-9) from the ethanol extract of Thesium chinense Turcz, a commonly used oral anti-bacterial and anti-inflammatory herb. Their structures were elucidated on the basis of spectroscopic and chemical evidence. Exocarpic acid (3) demonstrated the most promising activity against three tested oral pathogenic bacterial strains, Porphyromonas gingivalis, Fusobacterium nucleatum, and Streptococcus mutans, with minimum inhibitory concentration values of 0.86, 3.43, and 13.70 μg/mL, respectively. Compounds 1, 2, 4, 5 and 7 also showed potential activities against periodontal bacteria (P. gingivalis, F. nucleatum).

摘要

在天然产物化学中,一直鼓励发现用于口腔传染病的药物。基于生物测定指导的分离方法,从常用的口腔抗菌和抗炎草药中华兔耳风(Thesium chinense Turcz)的乙醇提取物中分离得到了两个新的炔酸(1、2)和七个已知的炔酸(3-9)。根据光谱和化学证据确定了它们的结构。外果皮酸(3)对三种测试的口腔致病菌(牙龈卟啉单胞菌、核梭杆菌和变形链球菌)表现出最有希望的活性,最小抑菌浓度值分别为 0.86、3.43 和 13.70 μg/mL。化合物 1、2、4、5 和 7 也表现出对牙周细菌(牙龈卟啉单胞菌、核梭杆菌)的潜在活性。

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