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大蒜素与卡托普利的合成产物S-烯丙基巯基卡托普利对与代谢综合征相关的心血管危险因素的影响。

The effects of S-allylmercaptocaptopril, the synthetic product of allicin and captopril, on cardiovascular risk factors associated with the metabolic syndrome.

作者信息

Oron-Herman Mor, Rosenthal Talma, Mirelman David, Miron Talia, Rabinkov Aharon, Wilchek Meir, Sela Ben-Ami

机构信息

Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv, Israel.

出版信息

Atherosclerosis. 2005 Dec;183(2):238-43. doi: 10.1016/j.atherosclerosis.2005.03.009. Epub 2005 Apr 14.

Abstract

Pure allicin, prepared biosynthetically by reacting synthetic alliin with an immobilized alliinase enzyme, is known to possess cardioprotective effects. However, in its pure form, allicin is pharmacologically unstable. S-allylmercaptocaptopril (CPSSA) is a new stable synthetic compound produced by chemical reaction between allicin and the angiotensin converting enzyme inhibitor captopril. Using the fructose-induced metabolic syndrome rat model we studied the effects of short-term treatment with two doses of CPSSA on cardiovascular risk factors associated with the metabolic syndrome, in comparison to the effects of allicin and captopril separately. Allicin (8 mg/(kg day)) significantly reduced insulin, triglycerides, and homocysteine concentrations, and had a slight effect on SBP. Captopril (50mg/(kg day)) only improved blood pressure and homocysteine. Treatment with low dose of CPSSA (5mg/(kg day)) lowered SBP but did not improve any other measured parameter, while treatment with a higher dose (50mg/(kg day)) significantly decreased blood pressure, triglycerides, and homocysteine concentrations. We conclude that the combined molecule CPSSA integrates the anti-hypertensive, lipid-lowering, and homocysteine-reducing effects of both allicin and captopril, making it a potential cardiovascular protective agent.

摘要

通过使合成蒜氨酸与固定化蒜氨酸酶反应生物合成制备的纯大蒜素已知具有心脏保护作用。然而,大蒜素以其纯形式在药理学上不稳定。S-烯丙基巯基卡托普利(CPSSA)是一种通过大蒜素与血管紧张素转换酶抑制剂卡托普利之间的化学反应产生的新型稳定合成化合物。使用果糖诱导的代谢综合征大鼠模型,我们研究了与单独使用大蒜素和卡托普利的效果相比,两种剂量的CPSSA短期治疗对与代谢综合征相关的心血管危险因素的影响。大蒜素(8毫克/(千克·天))显著降低了胰岛素、甘油三酯和同型半胱氨酸浓度,并且对收缩压有轻微影响。卡托普利(50毫克/(千克·天))仅改善了血压和同型半胱氨酸。低剂量CPSSA(5毫克/(千克·天))治疗降低了收缩压,但未改善任何其他测量参数,而高剂量(50毫克/(千克·天))治疗显著降低了血压、甘油三酯和同型半胱氨酸浓度。我们得出结论,组合分子CPSSA整合了大蒜素和卡托普利的抗高血压、降血脂和降低同型半胱氨酸的作用,使其成为一种潜在的心血管保护剂。

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