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本文研究原儿茶酸的三类衍生物,(1)原儿茶酸的四甲基吡嗪盐,(2)原儿茶酸与β-阻断剂有效基团相结合的衍生物,(3)原儿茶酸的同分异构物。利用测定猫冠状窦流量、心肌耗氧量、动静脉氧差、血压、心率等指标以及大、小鼠整体耐缺氧以探讨改变原儿茶酸的化学结构与药理作用间的关系。适量的吡嗪原儿茶酸在轻度增加冠脉流量的同时能较明显降低心肌耗氧量,而同剂量的四甲基吡嗪则明显增加心肌耗氧量,吡嗪原儿茶酸降低心肌耗氧量的程度较单用原儿茶酸约强14倍。四甲基吡嗪增强了原儿茶酸降低心肌耗氧量的作用。而原儿茶酸又能使四甲基吡嗪从增加心肌耗氧量反转为降低心肌耗氧量。 原儿茶酸与β-阻断剂有效基团相结合合成的7704(异)、7704(叔)的作用基本上与β-阻断剂相似,但作用强度较心得宁弱。 原儿茶酸同分异构物2,5-二羟基苯甲酸与2,6-二羟基苯甲酸虽能明显延长整体动物耐缺氧,但对猫心肌耗氧量则无明显作用。
This article studies three derivatives of protocatechuic acid, (1) tetramethylpyrazine salts of protocatechuate, (2) derivatives of protocatechuic acid and β-blocker active groups, ( 3) Protocatechuic acid isomers. The relationship between the chemical structure of protocatechuic acid and its pharmacological effects was explored by measuring the coronary flow, the myocardial oxygen consumption, arterial venous oxygen difference, blood pressure, heart rate and other indicators, as well as the overall hypoxia tolerance in mice and large mice. Appropriate amount of pyrazine protocatechuic acid can significantly reduce myocardial oxygen consumption while mildly increasing coronary flow, while the same dosage of tetramethylpyrazine significantly increased myocardial oxygen consumption, pyrazine protocatechuic acid decreased Myocardial oxygen consumption than the degree of protoporphyrin about 14 times stronger. Tetramethylpyrazine enhances the role of protocatechuic acid in reducing myocardial oxygen consumption. Protocatechuic acid and tetramethylpyrazine can reverse the increase in myocardial oxygen consumption to reduce myocardial oxygen consumption. The combination of protocatechuic acid and β-blocker effective groups synthesized 7704 (iso), 7704 (tert) was essentially similar to β-blocker, but had a weaker acting strength. Protocatechuic acid isomers 2,5- dihydroxybenzoic acid and 2,6-dihydroxybenzoic acid can significantly prolong the overall animal hypoxia, but the myocardial oxygen consumption of cats had no significant effect.