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Mesua beccariana (Clusiaceae), A Source of Potential Anti-cancer Lead Compounds in Drug Discovery

机译:墨苏阿(Mesua beccariana),药物发现中潜在的抗癌先导化合物的来源

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An investigation on biologically active secondary metabolites from the stem bark of Mesua beccariana was carried out. A new cyclodione, mesuadione (1), along with several known constituents which are beccamarin (2), 2,5-dihydroxy-1,3,4-trimethoxy anthraquinone (3), 4-methoxy-1,3,5-trihydroxyanthraquinone (4), betulinic acid (5) and stigmasterol (6) were obtained from this ongoing research. Structures of these compounds were elucidated by extensive spectroscopic methods, including 1D and 2D-NMR, GC-MS, IR and UV techniques. Preliminary tests of the in vitro cytotoxic activities of all the isolated metabolites against a panel of human cancer cell lines Raji (lymphoma), SNU-1 (gastric carcinoma), K562 (erythroleukemia cells), LS-174T (colorectal adenocarcinoma), HeLa (cervical cells), SK-MEL-28 (malignant melanoma cells), NCI-H23 (lung adenocarcinoma), IMR-32 (neuroblastoma) and Hep-G2 (hepatocellular liver carcinoma) were carried out using an MTT assay. Mesuadione (1), beccamarin (2), betulinic acid (5) and stigmasterol (6) displayed strong inhibition of Raji cell proliferation, while the proliferation rate of SK-MEL-28 and HeLa were strongly inhibited by stigmasterol (6) and beccamarin (2), indicating these secondary metabolites could be anti-cancer lead compounds in drug discovery.
机译:进行了调查从墨角ua茎皮的生物活性次生代谢产物。一种新的环二酮,美甲adi酮(1),以及几种已知成分,例如苯卡马啉(2),2,5-二羟基-1,3,4-三甲氧基蒽醌(3),4-甲氧基-1,3,5-三羟基蒽醌(4),从这项正在进行的研究中获得了桦木酸(5)和豆甾醇(6)。通过广泛的光谱方法,包括1D和2D-NMR,GC-MS,IR和UV技术,阐明了这些化合物的结构。所有分离的代谢物对一组人类癌细胞系Raji(淋巴瘤),SNU-1(胃癌),K562(红白血病细胞),LS-174T(结肠直肠腺癌),HeLa的体外细胞毒性活性的初步测试宫颈细胞),SK-MEL-28(恶性黑色素瘤细胞),NCI-H23(肺腺癌),IMR-32(神经母细胞瘤)和Hep-G2(肝细胞性肝癌)进行了测定。美沙酮(1),贝卡马林(2),桦木酸(5)和豆甾醇(6)表现出对Raji细胞增殖的强烈抑制作用,而SK-MEL-28和HeLa的增殖速率被豆甾醇(6)和贝卡马林强烈抑制(2),表明这些次生代谢产物可能是药物发现中的抗癌先导化合物。

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    《Molecules》 |2012年第9期|共10页
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