Han Shu-Xian, You Yun
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
Key Laboratory of Chinese Internal Medicine, Beijing University of Chinese Medicine, Beijing 100700, China.
Zhongguo Zhong Yao Za Zhi. 2016 Mar;41(5):818-822. doi: 10.4268/cjcmm20160510.
PNS (total saponins of Panax notognseng, PNS) has a clear effect and wide application prospect for cardiovascular diseases. At the same time, saponins have hemolytic properties, which are related to its molecular structure type and dosage. On one hand, this article summarizes the research progress of PNS in heart cerebrovascular pharmacology pharmacological in recent five years, a number of studies both in vitro and in vivo for overall body, organs, cells and molecules, show that PNS could improve myocardial and cerebral ischemia injury, and it has effects in resisting thrombosis, inflammation, oxidation, atherosclerosis, and modulating vascular endothelial cells function and improving the cerebral ischemia injury etc. On the other hand, the hemolysis effect of PNS is closely related to its molecular structure type and administrating dosage. Different structures bring about different hemolysis activities. Structure-activity relationship suggests that the length of sugar side chains attached to C-20 and the disaccharide connection mode on C-3 may influence the hemolysis activity of PNS. Within the dose range from 2.5 to 250 mg•L⁻¹, PNS has no hemolysis activity. However, PNS exhibits hemolytic properties at high concentrations(≥500 mg•L⁻¹). Based on the hemolytic or anti-hemolysis characteristics of saponins, and dose-response relationship, the rational clinical application of PNS can be guaranteed by controlling the ratio of hemolytic monosaponins in PNS and improving the hemolytic test method.
三七总皂苷(PNS)对心血管疾病有确切疗效且应用前景广阔。同时,皂苷具有溶血特性,这与其分子结构类型和剂量有关。一方面,本文综述了近五年PNS在心脑血管药理学方面的研究进展,多项体内外研究从整体、器官、细胞和分子水平表明,PNS可改善心肌和脑缺血损伤,具有抗血栓形成、抗炎、抗氧化、抗动脉粥样硬化作用,还能调节血管内皮细胞功能及改善脑缺血损伤等。另一方面,PNS的溶血作用与其分子结构类型和给药剂量密切相关。不同结构具有不同的溶血活性。构效关系表明,连接在C-20位的糖侧链长度及C-3位的二糖连接方式可能影响PNS的溶血活性。在2.5至250mg•L⁻¹剂量范围内,PNS无溶血活性。然而,PNS在高浓度(≥500mg•L⁻¹)时表现出溶血特性。基于皂苷的溶血或抗溶血特性以及剂量反应关系,通过控制PNS中溶血单皂苷的比例并改进溶血试验方法,可保证PNS临床合理应用。