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目的:探讨盐炙益智仁石油醚部位缩尿的有效成分,并进行药效学验证,拟阐明盐炙益智仁的缩尿药效物质基础以及作用机制。方法:采用硅胶和HPLC等色谱手段进行化学成分的分离纯化,根据理化性质和1H-NMR,13C-NMR波谱数据鉴定化合物结构;通过BL-420S型生物机能实验系统测定膀胱逼尿肌张力的变化,采用分别加4种兴奋剂Ba Cl2,磷酸组胺、多巴胺、乙酰胆碱累计加药物的方法,观察化合物对豚鼠膀胱逼尿肌肌条的收缩张力活动影响。结果:盐炙益智仁石油醚部位成分分离并鉴定出9个化合物[圆柚酮,11-hydroxy-valenc-1(10)-en-2-one,香科酮(teucrenone),7-表-香科酮(7-epiteucrenone B),12-羟基圆柚酮(12-hydroxynootkatone),杨芽黄素,β-谷甾醇,胡萝卜苷,棕榈酸],通过药效学验证7-epiteucrenone B与温肾缩尿密切相关。结论:7-epi-teucrenone B可能是通过拮抗磷酸组胺的H1受体释放从而抑制豚鼠膀胱逼尿肌收缩张力。推测盐炙益智仁石油醚部位中的7-epi-teucrenone B可能为盐炙益智仁缩尿主要有效成分。
OBJECTIVE: To investigate the effective components of the petechia oil of Sunburn Yizhen and its pharmacodynamic validation, and to elucidate the substance basis and mechanism of the urine-digesting effect of Yanzhuo Yi Zhi Ren. Methods: The constituents were separated and purified by silica gel and HPLC. The structures of compounds were identified by 1H-NMR and 13C-NMR spectra. The changes of bladder detrusor tension were determined by BL-420S bio-functional system , Respectively, plus four kinds of stimulants Ba Cl2, histamine phosphate, dopamine, acetylcholine cumulative plus drug method to observe the compound on the guinea pig bladder detrusor muscle contraction of tension activity. Results: Nine compounds [pomelanone, 11-hydroxy-valenc-1 (10) -en-2-one, teucrenone, - 7-epiteucrenone B, 12-hydroxynootkatone, tabuchimentin, β-sitosterol, daucosterol, palmitic acid] Wenshen Shenju are closely related. Conclusion: 7-epi-teucrenone B may inhibit the contractile tension of guinea-pig bladder detrusor muscle by antagonizing the release of histamine H1 receptor. It is inferred that 7-epi-teucrenone B in the salt sunburn Yizhen petroleum ether site may be the main active ingredient of salt sunburn Yizhuo diuretic.