香茶菜属贝壳杉烷型二萜抗菌活性三维定量构效关系研究

项目名称： 香茶菜属贝壳杉烷型二萜抗菌活性三维定量构效关系研究

项目编号： No.30800835

项目类型： 青年科学基金项目

立项/批准年度： 2009

项目学科： 金属学与金属工艺

项目作者： 王大成

作者单位： 吉林大学

项目金额： 23万元

中文摘要： 通过Sephadex LH-20、MCI-gel CHP-20P、RP-HPLC等方法，从蓝萼香茶菜等植物中共分离到45个单体化合物。通过1D NMR、2D NMR和HRMS等各种谱学研究方法及理化性质，鉴定出42个化合物的结构。其中5个为未见文献报道的新化合物，6个为从该属植物中首次分离到，8个为从该种植物中首次分离到的化合物。 采用微量稀释法物进行体外抑菌活性的研究。结果表明，在2.0～1000 μmL浓度范围内，化合物对大肠杆菌均没有抑制作用，无最小抑菌浓度 (MIC) 测定值。化合物对金黄色葡萄球菌的MIC为16～500 μmL，具有相对较强的抑制金黄色葡萄球菌活性。对其抗菌机制进一步研究表明，二萜类化合物glaucocalyxin A具有抑制金黄色葡萄球菌引起的血小板凝聚作用。构效关系研究表明，具有α#20057;烯基环戊酮结构的化合物均具有抗菌活性，该结构是抗菌活性必须基团。另外具有6βH的化合物抗菌活性较强，推测活性的增强是由于6βH与C-15的羰基形成氢键的结果。 在本课题的资助下培养了3名研究生（两人已经毕业，一人在读）已发表论文6篇（SCI收录2篇）。

中文关键词： 香茶菜；活性成分；抗菌作用；构效关系

英文摘要： Through thin-layer chromatography, silica gel column chromatography, Sephadex LH-20 column chromatography, MCI polystyrene reversed phase resin column chromatography, RP-18 open column chromatography, semi-preparative HPLC (ODS), TLC and other chromatographic separation techniques and methods, 45 compounds were isolated from the ethanol extract of the roots and the aqueous extract of the aerial parts of R. japonica var. glaucocalyx and other medicinal plants. With the spectral methods of Co-TLC, 1D NMR, 2D NMR, MS, and physico-chemical properties, 42 compounds were identified Five new compounds haven't been reported in any literature; six compounds were obtained from this genus; eight compounds were isolated from this species for the first time. The anti-bacterial activities in vitro of five isolated compounds were evaluated using micro-broth dilution method by NCCLS under the concentration range of 2.0?1000 μmL. Experimental results showed that all of them had no inhibition on Escherichia coil and no MIC measurements. The MIC of compounds against Staphyloccocus aureus was range from 16 to 125 μmL, which indicated the relatively strong inhibitory activity of S. aureus. The results suggest that the structural feature of amethylenecyclopentanone system was an essential active centre for the antimicrobial activity. Further study indicate that compounds with 6βH have more strong pottential against microbial. It was proposed that the enhanced activity of such components was attributed to hydrogen-bonding between 6βH and ketone group at C-15. Under the support of this found two master have been praduate and one will get her master dgree in this year. Six papers have been published with the assigment of support of the found.

英文关键词： Rabdosia; bioactive components; anti-bacterial activity; structure activity relationship