2007年1月3日:中科院上海营养科学研究所张瑞稳、王慧与沈阳药科大学教授赵余庆通过合作研究后发现:从人参果 和三七中提取到多种治疗癌症的有效成分-达玛烷苷元,接近于理想抗癌药物。目前,相关研究成果已分别发表于国际科学期刊《医用化学》和《癌症化疗与药理学》上。
作为中国传统中药的人参曾被用于多种中医验方。现代医学研究表明,人参皂苷作为人参中一类主要的有效成分,具有抗肿瘤活性,尤其是无糖化的达玛烷苷元,其抗癌活性大大增加,接近于常见的化疗药物,但其副作用却比化疗药小很多。非正式临床观测显示:人参对肿瘤的化疗具有减毒增效的作用,同时还可增强免疫系统的功能。
而上海科研人员不仅从人参果和三七中提取出了人参的主要有效成分人参达玛烷苷元,还运用专利技术进一步提纯,生产出多种有望治疗癌症的先导化 合物。据悉,这些物质在细胞实验中的表现比过去的人参提取物优异得多。如对前列腺癌的治疗,新化合物杀死癌细胞所需要的剂量,只有以往药物的1/25;而 对正常细胞无明显伤害。这意味着由这些先导化合物开发而成的新药,小剂量使用就能起到杀死癌细胞、却在与此同时保护健康细胞的作用。
In vitro anti-cancer activity and structure-activity relationships of natural products isolated from fruits of Panax ginseng. (人参果活性成分在体外的抗癌活性及其构效关系)
研究摘要:
PURPOSE(目的): Panax ginseng and its extracts have long been used for medical purposes; there is increasing interest in developing ginseng products as cancer preventive or therapeutic agents. The present study was designed to determine biological structure-activity relationships (SAR) for saponins present in Panax ginseng fruits.
METHODS(方法): Eleven saponins were extracted from P. ginseng fruits and purified by use of D(101) resin and ordinary and reverse-phase silica gel column chromatography. Their chemical structures were elucidated on the basis of physicochemical constants and NMR spectra. Compounds were then evaluated for SAR with their in vitro cytotoxicity against several human cancer cell lines.
RESULTS(结果): The 11 compounds were identified as 20(R)-dammarane-3beta,12beta,20,25-tetrol (25-OH-PPD, 1); 20(R)-dammarane-3beta,6alpha,12beta,20,25-pentol (25-OH-PPT, 2); 20(S)-protopanaxadiol (PPD, 3); daucosterine 4, 20(S)-ginsenoside-Rh(2) (Rh(2), 5); 20(S)-ginsenoside-Rg(3) (Rg(3,) 6); 20(S)-ginsenoside-Rg(2) (Rg(2), 7); 20(S)-ginsenoside-Rg(1) (Rg(1), 8); 20(S)-ginsenoside-Rd (Rd, 9); 20(S)-ginsenoside-Re (Re, 10); and 20(S)-ginsenoside-Rb(1) (Rb(1), 11). Among the eleven compounds, 1, 3 and 5 were the most effective inhibitors of cell growth and proliferation and inducers of apoptosis and cell cycle arrest. For 1, the IC(50) values for most cell lines were in the range of 10-60 microM, at least twofold lower than for any of the other compounds. Compounds 1 and 3 had significant, dose-dependent effects on apoptosis, proliferation, and cell cycle progression (化合物1【25-OH-PPD】和3【PPD】具有显著的、与剂量相关的抗癌活性,能够促进癌细胞凋亡、抑制癌细胞增殖和细胞周期进展).
CONCLUSIONS(结论): The results suggest that the type of dammarane, the number of sugar moieties, and differences in the substituent groups affect their anti-cancer activity. This information may be useful for evaluating the structure/function relationship of other ginsenosides and their aglycones and for development of novel anticancer agents.
发表于:Cancer Chemother Pharmacol. 2007 Apr;59(5):589-601