丹參為著名「活血去瘀」的傳統中藥,屬於唇形科多年生草本植物。丹參乾燥的根部常用於治療心血管疾病、活血去瘀、調經止痛、養血安神、涼血消炎等。依據文獻中記載,丹參甲醇萃取物大多為丹參酮化合物,丹參酮化合物具有許多的生物活性,例如抗腫瘤、抗氧化、抑制血小板凝集等作用。
先前實驗室從丹參之甲醇萃取物中分離與鑑定出一個微量的新化合物稱為新丹參內酯(neo-tanshinlactone),由於此化合物具有選擇性的抗乳癌活性,具有潛力能開發成為抗乳癌之新藥,其結構與活性相關性國內外亦尚未有進一步的探討,因此本論文是以neo-tanshinlactone為引導分子(lead compound),合成其類似物,並就其結構與活性相關性(structure-activity relationship)進行探討。
The dried roots of Salvia miltiorrhiza under the name Danshen has been used in traditional Chinese medicine for treatment of cardiovascular disease, hemorrhage, menstrual disorder, miscarriage, and swelling. According to literature reports, a lot of tanshinones were isolated and identified from S. miltiorrhiza and many of them have been also reported to exhibit diverse biological activities such as antitumor, antioxidant, and antiplatelet aggregation.
Recently, a new component, neo-tanshinlactone, was isolated from S. miltiorrhiza in our laboratory, and showed selective anti-breast cancer activity. Because this compound might be a useful lead for developing novel anti-breast cancer drug candidate, in this thesis we synthesized analogues of neo-tanshinlactone and studied the structure and anti-breast cancer activity relationship.