Filczewski M, Kosmala M, Oledzka K
Institute of Pharmaceutical Industry, Department of Pharmacology, Warszawa, Poland.
Pol J Pharmacol Pharm. 1988 May-Jun;40(3):233-9.
The circulatory effects of oleanoic acid sodium hydrogen succinate (OSS), an analogue of the anti-ulcer drug, carbenoxolone, were investigated. As carbenoxolone produces such adverse effects as sodium retention and a subsequent elevation of the arterial blood pressure in man, the present study was aimed at determining whether OSS is similar or different from it in this respect. Carbenoxolone, (43,3 mg/kg po) and OSS (66,6 mg/kg po) were given to rats twice daily for 4 weeks. The systolic blood pressure was elevated already after the first week of treatment. The hypertension was accompanied by bradycardia, which increased with the time of treatment. In the blood an increase in the creatinine level, a decrease in the urea level, and a slight elevation in sodium concentration were found after the treatment, while the potassium concentration during the whole treatment period (4 weeks) remained unchanged. Although the principal aldosterone-like effects of carbenoxolone were attributed to the oxygen presence in position 11 of the glycyrrhetinic acid ring, [8], the absence of an oxygen at that position in OSS did not cause the loss of the adverse circulatory effect.
研究了抗溃疡药物甘珀酸的类似物琥珀酸氢齐墩果酸(OSS)的循环系统作用。由于甘珀酸会产生诸如钠潴留以及随后人体动脉血压升高等不良反应,本研究旨在确定OSS在这方面与甘珀酸是相似还是不同。给大鼠每日两次口服甘珀酸(43.3毫克/千克)和OSS(66.6毫克/千克),持续4周。治疗第一周后收缩压就已升高。高血压伴有心动过缓,且心动过缓随治疗时间延长而加重。治疗后血液中肌酐水平升高、尿素水平降低、钠浓度略有升高,而整个治疗期间(4周)钾浓度保持不变。尽管甘珀酸的主要醛固酮样作用归因于甘草次酸环11位上的氧的存在,[8],但OSS在该位置没有氧并不会导致不良循环作用的丧失。