番石榴叶中人白细胞弹性蛋白酶抑制剂的研究.doc

番石榴叶中人白细胞弹性蛋白酶抑制剂的研究
高月麒1,任风芝1,陈书红1,李丽红1,郑智慧1,何美莹2,张雪霞1
(1、华北制药集团新药研究开发有限责任公司,河北石家庄 050015;2、云南省热带作物科学研究所,云南景洪 666100)
摘要目的研究番石榴叶中的人白细胞弹性蛋白酶(HLE)抑制剂成分。方法通过溶剂提取、聚酰胺、硅胶柱色谱、Sephadex LH20柱色谱和HPLC制备等分离纯化,得到活性化合物,根据理化性质和光谱数据鉴定化学结构,应用白细胞弹性蛋白酶抑制剂高通量的筛选模型进行评价。结果从番石榴叶中分离到的活性成分为2α-羟基-3β-(反-桂皮酰基)-12-烯-28-羧基乌苏酸(I)和2α-羟基-3β-(顺-桂皮酰基)-12-烯-28-羧基乌苏酸(II)的混合物,对人白细胞弹性蛋白酶有较强的抑制活性,。结论化合物II为首次从该植物中发现,该混合物的HLE活性首次报道。
关键词:番石榴叶三萜白细胞弹性蛋白酶抑制剂
Study on human leukocyte elastase inhibitor from Psidium guajava L.
GAO Yue-qi1, REN Feng-zhi1,CHEN Shu-hong1,Ll Li-hong1,ZHENG Zhi-hui1,HE Mei-ying2,ZHANG Xue-xia1(1 、NCPC New Drug research and development CO.,Ltd., Shiiazhuang 050015; 2、Yun nan institute of tropical crops research, jinghong 666100 )
ABSTRACT: OBJECTIVE To study human leukocyte elastase(HLE) inhibitor constituents from Psidium guajava L. METHODS The pounds were isolated by solvent extraction and chromatography on PA、silica gel、Sephadex LH20 and structures were identified by physicochemical properties and spectral analysis. A high through-put screening method was used to explore the HLE inhibitor. RESULTS A mixture was isolated and identified as 2α-hydroxy-3β-(trans-p-coumaroyloxy)-urs-12-en-28-oic acid (I) and 2α-hydroxy-3β-(cis-p-coumaroyloxy)- urs-12-en-28-oic acid (II) , and this mixture showed s strong inhibitor activity against human leukocyte elastase with IC5