摘要
小檗碱(berberine,BR)是以治疗肠道菌痢而著称的黄连素。近年来报道BR有正性肌力和抗心律失常作用,并伴有改善冠脉血流量、降低动脉压和扩张周围血管等作用,临床试用于治疗心衰和心律失常,取得了一定疗效。但BR为一季铵盐,极性大,胃肠道吸收差且不规则,剂量较大时对心肌产生抑制作用。又据报道四氢小檗碱型生物碱如四氢巴马汀(tetrahydropalmatine)和考雷明(coreximine)
It has been reported that berberine (BR) has positive inotropic and negative chronotropic effects. Recently, it has been tried in patients with arrhythmia and congestive heart failure. But BR, a quaternary ammonium salt, is absorbed poorly. We took BR as leading compound to synthesize its derivatives in order to find orally active agents. Compounds substituted by—OCH_3 in different positions of the D ring were synthesized. In the screening of inhibition of electrically induced contraction of isolated guinea pig left atria and spontaneous beating of its right atria, the synthesized compounds were found to possess activity of inhibiting spontaneous beating of isolated guinea pig right atria. Compound 14 was shown to be the most effective of the synthesized compounds with IC_(50) value of 4.34 (μ mol). The IC_(50) value of BR was 204 (μ mol).
出处
《药学学报》
CAS
CSCD
北大核心
1990年第10期780-784,共5页
Acta Pharmaceutica Sinica
关键词
小檗碱
肠道菌痢
心血管药物
Berberine
Positive inotropic effect
Arrhythmia
