藤茶中双氢黄酮醇的分离、结构鉴定及其药理活性

Isolation,structuredeterminationandpharmacologicalactivityofflavanonolfromAmpelopsisgrosedentata

目的：分离和鉴定藤茶（Ａｍｐｅｌｏｐｓｉｓｇｒｏｓｓｅｄｅｎｔａｔａ））中一种双氢黄酮醇成分，研究其药理活性。方法：用溶剂和柱层析对藤茶的一种双氢黄酮醇进行分离；用理化常数测试和光谱法（ＵＶ，ＩＲ，ＥＩ－ＭＳ，１ＨＮＭＲ，１ＨＮＭＲ＋Ｄ２Ｏ，１３ＣＮＭＲ）对其进行结构鉴定；用兔胸主动脉条实验，观察其对去甲肾上腺素（ＮＡ）和高Ｋ＋所致主动脉条收缩的影响。结果：分离得到一种双氢黄酮醇成分，鉴定为３，３′，４′，５，５′，７－六羟基－２，３－双氢黄酮醇，即双氢杨梅树皮素（ｄｉｈｙｄｒｏｍｙｒｉｃｅｔｉｎ）。双氢杨梅树皮素能使ＮＡ的量效反应曲线右移，最大反应降低，使高Ｋ＋所致的收缩幅度下降。小鼠ｉｇ最大耐受量为５ｇ／ｋｇ，小鼠腹腔注射ＬＤ５０及其可信限为１．４１±０．１３ｇ／ｋｇ（Ｐ＝０．９５）。结论：双氢杨梅树皮素在本种植物中为首次报道。它能明显拮抗ＮＡ和高Ｋ＋所致的兔胸主动脉条收缩反应，毒性低。

OBJECTIVE:ToisolateanddetermineflavanonolfromAmpelopsisgrosedentataandtostudyitspharmacologicalactivity.METHOD:TheflavanonolwasisolatedfromAmpelopsisgrosedentatabyusingsolventandcolumnchromatographyanditsstructurewasdeterminedbyusingphysicochemicalpropertiesandspectradata(UV,IR,EI-MS,1HNMR,1HNMR+D2O,13CNMR).Theeffectsofdihyromyricetinwerenotedonthecontractionofrabbitaorticstripscausedbynoradrenaline(NA)andhighK+solution.RESULTS:FlavanonolwasisolatedfromtheleavesofAmpelopsisgrosedentataandidentifiedas3,3′,4′,5,5′,7-hexahydroxy-2,3-dihydroflavanonol(dihy-dromyricetin),whichcanshiftthedose-effectrelationshipcurvesofNAtorightanddecreasethemaximalre-sponse.AlsoitcaninhibitthecontractionevokedbyhighK+solution.Mice:igLD505g/kg,miceipLD501.41±0.13g/kg(P=0.95).CONCLUSION:Dihydromyricetinwithlesstoxicitywasfoundfirstlyinthisspecies,andcaninhibitthecontractionsofrabbitaorticstripsevokedbyNAandhighK+solution.