| 中文摘要 |
活血化瘀方劑具有通暢血行，祛除血瘀的作用，在臨床上除用於強身保健外，亦用於治療高血脂症、腦中風、心肌缺氧、冠心病及心絞痛等心血管疾病。在活血化瘀方劑中，人參、柴胡、蟾酥、三七及丹參等藥材常被廣泛地使用。經本研究團隊實驗證實這些藥材應該是透過似固醇化合物或丹參酚酸B鎂鹽等活性成分來達到部分的活血化瘀功效。因它們均具有抑制心肌細胞胞膜上的鈉鉀幫浦活性作用，導致細胞內的鈣離子濃度增高，引發心肌興奮收縮，加快血流的輸出和血流量，而達到促使血液循環及心肌收縮的效果；此作用機制與強心配醣體相似。並經電腦3D分子結構影像模擬分析顯示此似固醇化合物或丹參酚酸B鎂鹽均可與鈉鉀幫浦胞外區間產生鍵結；因鍵結的強弱而導致不同程度的抑制鈉鉀幫浦功效。此外，透過模擬腦中風動物試驗的藥物篩選平台，發現活血化瘀藥材中具有抑制鈉鉀幫浦的活性成分均能有效地保護腦神經，降低其受傷程度，未來在缺血性腦中風藥物開發上應當是頗具潛力。Traditional Chinese herbs for promoting blood circulation and eliminating stasis are constantly used to improve human health and to treat various cardiovascular diseases, such as hyperlipidemia, heart stroke, coronary heart disease, and myocardial infarction. Among these Chinese herbs, Ginseng, Chaihu, Chan-Su, Sanqi, and Danshen have been extensively used in diverse formulae of prescription. In our recent studies, we demonstrated that steroid-like compounds and magnesium lithospermate B in the above Chinese herbs are active ingredients responsible for the cardiac therapeutic effects. The pharmacologic mechanism of these active ingredients is similar to that of cardiac glycosides, i.e., via inhibition of Na+, K+-ATPase that causes accumulation of calcium in cells, increases inotropism, and enforces to increase blood volume and velocity. Molecular modeling analyses showed that steroid-like compounds and magnesium lithospermate B bind to the extracellular pocket of the Na+, K+-ATPase. According to the neuroprotective effects observed in a cortical brain slice-based assay model, effective inhibitors of Na+, K+-ATPase, such as steroid-like compounds and magnesium lithospermate B in Chinese herbs, are potential drugs for the treatment of ischemic stroke. |
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