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科學家成功從人參中發現理想抗癌藥物-達瑪烷苷元

達瑪烷苷元PPD抑制紫外線誘導的MMP表達
MMP-1 is an enzyme which is able to digest collagen in the skin, and overe-exposure to UV will excessively activate MMP-1, thus leads to collagen loss in the skin, acceleartes the skin aging process. New findings in this article suggest dammarane sap...
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2007年1月3日:中科院上海營養科學研究所張瑞穩、王慧與瀋陽藥科大學教授趙餘慶通過合作研究後發現:從人參果和三七中提取到多種治療癌症的有效成分- 達瑪烷苷元,接近於理想抗癌藥物。目前,相關研究成果已分別發表於國際科學期刊《醫用化學》和《癌症化療與藥理學》上。

作為中國傳統中藥的人參曾被用於多種中醫驗方。現代醫學研究表明,人參皂苷作為人參中一類主要的有效成分,具有抗腫瘤活性,尤其是無糖化的達瑪烷苷元,其抗癌活性大大增加,接近於常見的化療藥物,但其副作用卻比化療藥小很多。非正式臨床觀測顯示:人參對腫瘤的化療具有減毒增效的作用,同時還可增強免疫系統的功能。

而上海科研人員不僅從人參果和三七中提取出了人參的主要有效成分人參達瑪烷苷元,還運用專利技術進一步提純,生產出多種有望治療癌症的先導化合物。據悉,這些物質在細胞實驗中的表現比過去的人參提取物優異得多。如對前列腺癌的治療,新化合物殺死癌細胞所需要的劑量,只有以往藥物的1/25;而對正常細胞無明顯傷害。這意味著由這些先導化合物開發而成的新藥,小劑量使用就能起到殺死癌細胞、卻在與此同時保護健康細胞的作用。
In vitro anti-cancer activity and structure-activity relationships of natural products isolated from fruits of Panax ginseng. (人參果活性成分在體外的抗癌活性及其構效關係)

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(結果): 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】具有顯著的、與劑量相關的抗癌活性,能夠促進癌細胞凋亡、抑制癌細胞增殖和細胞週期進展) . CONCLUSIONS(結論): 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.

發表於:Cancer Chemother Pharmacol. 2007 Apr;59(5):589-601

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