香鳞毛蕨中的新间苯三酚及其体外抗菌活性  

A new phloroglucinol from Dryopteris fragrans and its antibacterial activity in vitro

作　　者：郑诗倩 宋国强 殷川平 陈艳芬 王帅帅 沈志滨 ZHENG Shi-qian;SONG Guo-qiang;YIN Chuan-ping;CHEN Yan-fen;WANG Shuai-shuai;SHEN Zhi-bin(School of Traditional Chinese Medicine,Guangdong Pharmaceutical Uniersity,Guangzhou 511400,China;Guangzhou Hipover Pharmaceutical R&D Co.,Ltd.,Guangzhou 510620,China;Guangdong Prorincial Engineering Technology Research Center of Localied Precision Drug Delivery Prepuration,Guangzhou 510006,China;Cosmetics Engineering Technology Research Center of Guangdong Prorince,Guangshou 510006,China)

机构地区：[1]广东药科大学中药学院,广东广州511400 [2]广州海博特医药科技有限公司,广东广州510620 [3]广东省局部精准药物递药制剂工程技术研究中心,广东广州510006 [4]广东省化妆品工程技术研究中心,广东广州510006

出　　处：《中国中药杂志》2022年第9期2474-2479,共6页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81202885);国家重点研发计划“中医药现代化”重点专项(2018YFC1707100)。

摘　　要：采用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、TLC薄层色谱和半制备液相色谱等方法,从香鳞毛蕨Dryopteris fragrans 50%乙醇提取物中分离得到1个新的间苯三酚类化合物。通过MS、^(1)H-NMR、^(13)C-NMR等波谱学方法并结合文献确定其化学结构为2,5-cyclohexadien-1-one, 2-{[2,6-dihydroxy-4-methoxy-3-methyl-5-(1-isobutyl)phenyl]methyl}-3,5-dihydroxy-4,4-dimethyl-6-(1-oxobutyl)(1),命名为异绵马素BB(disaspidin BB)。对该化合物进行体外抗菌活性筛选,实验结果显示,与常用的外用药红霉素或莫匹罗星相比,异绵马素BB对表皮葡萄球菌Staphylococcus epidermidis(SEP)、溶血葡萄球菌S.haemolyticus(SHA)和耐甲氧西林金黄色葡萄球菌methicillin-resistant S.aureus(MRSA)均具有显著抗菌活性(P<0.05);异绵马素BB对耐头孢他啶的表皮葡萄球菌SEP1~SEP4、溶血葡萄球菌SHA5~SHA7、耐甲氧西林金黄色葡萄球菌MRSA8和MRSA9均敏感;异绵马素BB对表皮葡萄球菌和溶血葡萄球菌的MIC分别为1.67~2.71、10.00~33.33μg·mL^(-1)。结果表明异绵马素BB具有较好的抗菌活性以及开发成外用抗感染新药的价值。A new phloroglucinol was isolated from 50% ethanol extract of Dryopteris fragrans by silica gel column chromatography, Sephadex LH-20 gel column chromatography, thin-layer chromatography(TLC), and preparative liquid column chromatography. On the basis of MS, ^(1)H-NMR,^(13)C-NMR, and reference materials, compound 1 was identified as 2,5-cyclohexadien-1-one, 2-{[2,6-dihydroxy-4-methoxy-3-methyl-5-(1-isobutyl)phenyl]methyl}-3,5-dihydroxy-4,4-dimethyl-6-(1-oxobutyl)(1), and named disaspidin BB. Compound 1 was evaluated for its antibacterial activity. The experimental results showed that compared with the commonly used topical antibiotics erythromycin or mupirocin, disaspidin BB exhibited significant antibacterial activities against Staphylococcus epidermidis(SEP), S. haemolyticus(SHA), and methicillin-resistant S. aureus(MRSA)(P<0.05). Additionally, disaspidin BB was sensitive to ceftazidime-resistant SEP1-SEP4, SHA5-SHA7, MRSA8, and MRSA9. The MIC values of disaspidin BB against SEP and SHA were 1.67-2.71 μg·mL^(-1) and 10.00-33.33 μg·mL^(-1) respectively. Disaspidin BB has good antibacterial activities and deserves development as a new anti-infective drug for external use.

关 键 词：香鳞毛蕨 间苯三酚衍生物 异绵马素BB 抗菌活性 

分 类 号：R284.1[医药卫生—中药学]