3味山姜属中药的性效与活性成分相关性研究

To study on the relation between warming properties and cold dispelling, total flavonoids extracted by ethanol from 3 kinds of Chinese drugs of Alpinia Roxib, including Gaoliangjiang, Dagaoliangjiang, Hongdoukou were study. The model was made by rats with cold syndrome originated from gastric ulcer. To achieve this goal , the whole body functions on rats were tested. This index including the content of SOD, MDA, MOT, GAS, the activity of H+-K+-ATP, SS, bFGF, PDGF, 6-keto-PGF1α in gastric, as well as activity of Na+-K+-ATP and Ca2+-Mg2+-ATP, SDH and hepatic glycogen content in liver. Other index including astric juice quantity, total acidity and protease activity of gastric juice, the contents of NEFA, LPL, HL, COR, PAF, TXB2, ET, NO in the serum. To find out the material basic of this drug oriented Alpinia, further study was made with total flavonoids isolated and purified from ethyl acetate part of the materials, by Silica gel column chromatography and HPLC method. Besides, NMR and LC-MS/MS are used to identify and determine active constituents. To analysis the effective constituents of flavonoids transitional components and metabolite in rats' serum were studied. Through the study, we struggled to explore the correlation between genetic relationship, chemical composition, the properties of pungent and warm, and the effects of warming the middle-jiao and dispersing cold, to understand scientific value of the theory of TCDE，to provide ideas and methods for interpreting the scientific connotation of drug properties theory and effect, and finally to have significance of revealing the essence of traditional Chinese medicine between nature and function.

以高良姜、大高良姜、红豆蔻3味山姜属中药为研究对象，采用乙醇回流提取法提取3味中药总黄酮类成分，用大鼠复制胃溃疡寒证模型，分别对3味中药总黄酮类成分进行辛温药性与温中散寒功效研究，测定大鼠全身机能指标，胃组织SOD、MDA、MOT、GAS、H+-K+-ATP酶、SS、bFGF、PDGF、6-keto-PGF1α的含量，胃液量，胃液总酸度，胃蛋白酶活性，肝脏中Na+-K+-ATP酶、Ca2+-Mg2+-ATP酶、SDH活性和肝糖原含量，血清中NEF、LPL、HL、COR、PAF、TXB2、ET、NO的含量。对3味中药总黄酮进行分离纯化，HPLC分析、NMR和LC-MS/MS鉴定成分。最后，对分离的黄酮类活性成分进行入血成分分析，研究其体内血清移行成分。探讨“亲缘关系-药性-效用-物质基础”之间的内在关联，为解读中药药性理论与功效的科学内涵提供思路和方法，揭示中药性效的科学本质。

本项目在中医药理论指导下，以药用植物亲缘关系为切入点，选择高良姜、大高良姜、红豆蔻3味山姜属中药为研究对象，采用乙醇回流提取法提取3味中药的黄酮类成分，采用灌服冰知母水煎液和冰乙酸溶液的方法复制大鼠胃溃疡寒证模型，选取干姜姜辣素为阳性对照药，对 3 味山姜属中药的黄酮类成分进行性效研究。药性研究观察了黄酮类成分对胃溃疡寒证大鼠全身机能（体温、体重、进食、饮水、毛发及精神状态）、能量代谢（肝组织Na+- K+-ATP 酶、Ca2+-Mg2+-ATP 酶、SDH、肝糖原）、脂代谢（血清NEFA、LP、HL）相关指标的影响；药效研究检测了胃液、胃酸及胃蛋白酶、血清（PAF、TXB 2 、COR、NO、ET）及胃组织（MDA、SOD、MOT、GAS、MTL、SS、H＋-K＋-ATP 酶、bFGF、PDGF、6-keto-PGF1α）相关指标，并观察了胃黏膜的形态学、组织病理学变化。同时，对黄酮类成分进行了体外化学成分和体内入血成分研究。结果显示：3 味山姜属中药黄酮类成分具有温热药性；其药性与物质基础之间存在关联，黄酮类成分可能是其温热药性共有的物质基础。3味山姜属中药黄酮类成分对胃溃疡寒证大鼠具有温中散寒药效，有减少胃液量，降低胃蛋白酶活力，升高胃酸pH值，促进溃疡面愈合等作用。3味山姜属中药共有的黄酮类成分为高良姜素；高良姜与红豆蔻共有的黄酮类成分为芹菜素；高良姜与大高良姜共有的黄酮类成分为山奈素。3味山姜属中药黄酮类成分在胃溃疡寒证大鼠体内均为原型成分入血，这些成分可能分别是3味中药抗胃溃疡寒证的药效物质基础。本研究说明：具有亲缘关系的中药，其化学成分存在相关性。通过探讨“亲缘关系-药性-效用-物质基础”之间的内在关联，为解读中药药性理论与功效的科学内涵提供了思路和方法，在一定程度上揭示了中药性效的科学本质，对推动中药性效的学术发展具有积极意义。