玉竹中新高异黄酮类化合物及生物活性的研究.docVIP

玉竹中新高异黄酮类化合物及其生物活性研究 李丽红*，任风芝，陈书红，郑智慧，高月麒，张华，贺建功（华北制药集团新药研究开发有限责任公司天然药物室，河北 石家庄 050015） 摘要：目的 研究玉竹的生物活性成分。方法 利用各种柱色谱及高压液相色谱等方法进行分离和纯化，根据理化性质和光谱数据对化合物结构进行鉴定；并应用高通量筛选模型对化合物进行评价。结果 从玉竹中分离得到三个高异黄酮类化合物，确定结构分别为5，7-dihydroxy-6-methoxyl-8-methyl-3-(2′，4′-dihydroxybenzyl)chroman-4-one5，7- dihydroxy-6-methyl-3-(2′，4′-dihydroxybenzyl)- chroman-4-oneII）,5, 7-dihydroxy- 6-methoxyl-8-methyl-3-(4′-methoxybenzyl)chroman- 4-one（Ⅲ）, 三个化合物均显示了较强的抗肿瘤活性和抗炎活性。结论 化合物I～III为未见文献报道的新化合物，其抗肿瘤和抗炎活性为首次报道。 关键词：玉竹；高异黄酮；化学成分；抗肿瘤；抗炎；人白细胞弹性蛋白酶 Study on the new homoisoflavonoids and their bioactivity from Polygonatum odoratum (Mill.)Druce LI Li-hong*, REN Feng-zhi, CHEN Shu-hong, ZHENG Zhi-hui, GAO Yue-qi, ZHANG Hua, HE Jian-gong（Department of Natural Product Drug Discovery, Shijiazhuang 050015）ABSTRACT: OBJECTIVE To study the bioactive constituents of Polygonatum odoratum (Mill.)Druce. METHODS The compounds were separated by column chromatography and HPLC. On the basis of physicochemical properties and spectral data , their structures were confirmed. High through-put screening method was used to explore the activity of these compounds. RESULTS Three compounds were isolated and identified as 5，7-dihydroxy-6methoxyl-8-methyl-3-(2′，4′-dihydrox-ybenzyl)chroman-4-one5，7-dihydroxy-6-methyl-3-(2′，4′-dihydroxybenzyl)-chroman-4-oneII), 5, 7-dihydroxy-6-methoxyl-8- methyl-3-(4′-methoxybenzyl)chroman-4-one (Ⅲ). These compounds showed significant anti-tumor and anti-inflammatory effect CLUSION Compounds I～III were new homoisoflavonoids. Their anti-tumor and anti-inflammatory effects were reported for the first time. KEY WORDS: Polygonatum odoratum (Mill.)Druce; homoisoflavonoid; Chemical Constituents；anti-tumor; anti-inflammatory; human leukocyte elastase 玉竹为百合科(Liliaceae)黄精属(Polygonatum)植物玉竹(Polygonatum odoratum(Mill.)Druce)干燥根茎，为常用中药。最早以葳蕤之名始载于《神农本草经》，列为上品。玉竹味甘性平，能养阴润肺，益胃生津，用于燥热、伤阴、热伤和胃阴之症，有提高免疫力、强心、降血糖、降血脂等功效。主要含有多糖、皂苷、甾醇、黄酮类等成分1 仪器与材料 Volian INVOA 500型（TMS内标）核磁共振波仪，ZMD Micromass型质谱仪（Microm公司）；waters996型