临床和实验室研究证明,循环血中去甲肾上腺素(NE)水平超过生理阈值可以造成心肌细胞能量生成障碍和储备耗竭,导致复杂的生化及随后组织结构变化,从可逆发展到不可逆,以至坏死。环境应激(stress)通过增加 NE 释放最后可能引起心肌坏死代谢改变,形成典型的。应激性心肌病”(Stress car-diomyopathy)。在儿茶酚胺性心肌病发生机制中,细胞钙超载起关键作用。本研究报告丹参制剂对 NE引起心脏损害的对抗作用及其膜保护机制。
An endogenous inhibitor of the sodium pump from the toad venom Chan′su was purified. The dry substance Chan′su was extracted with methanol. The dry residue was passed subsequently through membrane filters with the exclusion size of 10 000, 3 000 and 1 000 at 1 psi in a Filtron Pro Vario-3-System and applied to thin layer chromatography made of Silica 60 F 254+366 separated in CHCl 3∶MeOH∶H 2O. The R f 0.55 fractions inhibiting the sodium pump were purified on a HPLC-RP C18 using a linear H\-2O/methanol gradient at 220 nm and 250 nm on DAD detector. The bio-activity was measured by a specific enzyme-linked immunosorbent assay (ELISA) and 86 Rb-uptake into human red blood cells. In Chan′su there exists an inhibitor of the sodium pump which interacts with antibodies against ouabain and proscillaridin A, and inhibits the sodium pump activity in the red blood cells. The results show that a low molecular weight compound has been isolated from the toad venom Chan′su. It inhibits the sodium pump, interacts preferentially with antibodies against ouabain. It is water soluble and shows a maximum of absorbance at 250 nm. Several milligrams of the compounds from one kilogram were obtained in pure form. The inhibitor differs considerably in its chemical structure from ouabain, because ouabain shows an UV absorbance maximum at 220 nm while the new inhibitor at 250 nm.
