基于动物体内指标的枇杷果利尿活性物质部位及单体筛选研究  

Screening of Diuretic Fractions and Active Monomer from Loquat Fruit by Indices in vivo

作　　者：罗彭[1] 任赛赛[1] 梁宁[1] 陈攀[1] 廖彭莹[1] 潘为高[1] 

机构地区：[1]广西中医药大学,南宁530001

出　　处：《湖北农业科学》2015年第16期3986-3989,共4页Hubei Agricultural Sciences

基　　金：广西壮族自治区教育厅科研项目(2013YB125);广西高等学校高水平创新团队及卓越学者计划资助项目[桂教人(2014)7号];广西高校重点实验室资助项目[桂教科研(2014)6号]

摘　　要：为研究枇杷[Eriobotrya japonica(Thunb.)Lindl.]果的动物体内利尿作用,获得利尿活性物质部位和活性单体,阐述枇杷果利尿作用的物质基础,为开发和研制枇杷果植物药利尿剂奠定基础,通过试剂法提取、系统溶剂萃取制备枇杷果各极性物质部位。依据生物活性跟踪法,以小鼠体内利尿为活性指标,柱色谱等为分离纯化方法,筛选出利尿物质部位,并进一步追踪利尿单体。追踪过程中通过先小量摸索、后大量分离制备的策略,解决体内给药剂量过大的问题。通过波谱法鉴定单体结构。结果表明,枇杷果乙醇提取物的乙酸乙酯萃取段有较显著的体内利尿活性(P<0.05),利尿强度接近氢氯噻嗪而稍弱于呋噻米,利尿作用速度较缓和。从乙酸乙酯萃取段中分离纯化获得一个利尿活性物质,经鉴定为熊果酸,利尿作用显著(P<0.05),利尿强度接近氢氯噻嗪而稍弱于呋噻米,利尿作用速度较缓和。枇杷果药食两用,其乙酸乙酯萃取段可有望开发为长期使用的安全天然利尿药物。熊果酸是枇杷果利尿作用的物质基础,其含量可作为该药材利尿用途方面的质量控制指标。该研究是直接通过动物体内药理指标筛选活性单体成功的不多案例之一,具有方法学借鉴价值。The study was aimed at investigating the diuretic activity in vivo of loquat fruit extracts, obtaining diuretic fractions and active monomer, demonstrating the diuretic material foundation of loquat fruit,and finally providing a reference for plant diuretic medicine development. The fractions of different polarity were extracted by reagent and system solvent.The diuretic portion and active monomer were screened by column chromatography and bioassay-guided tracing method based the in vivo diuretic activity in mice.Before large scaled separation and purification,the screening was first through small-batch test.The monomer structure was identified by spectrometry.The results showed that ethyl acetate part of ethanol extracts from loquat fruit presented significant diuretic activity in vivo（P〈0.05）,and the diuretic intensity was similar to that of Hydrochlorothiazide and slightly inferior to that of Furosemide,the diuretic velocity was moderate.A diuretic activity monomer,which showed significant diuretic activity in vivo（P 0.05）,with medium diuretic activity intensity and moderate diuretic velocity）,was isolated from ethyl acetate extracts and identified as ursolic acid. It indicated that loquat fruit was a medicine-food fruit with high safety,its ethyl acetate extracts had the potential to be developed a safe natural diuretic for long-term use in clinic. Ursolic acid was the diuretic material foundation of loquat fruit, its content in loquat fruit could be used as the quality control index for diuretic usage.This study was one of few successful cases that directly screening the bio-activity monomer by pharmacological index in vivo,and might be a reference in methodology.

关 键 词：枇杷[Eriobotrya japonica(Thunb.)Lindl.]果 乙酸乙酯部位 熊果酸 利尿 体内 生物活性跟踪法 

分 类 号：S667.3[农业科学—果树学] R931.6[农业科学—园艺学]