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

机译:墨索亚(Mesua beccariana)(药科)药物发现中潜在的抗癌先导化合物的来源

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摘要

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:进行了从墨角ua(Mesua beccariana)茎皮中的具有生物活性的次生代谢产物的研究。一种新的环二酮,美甲二酮(> 1 ),以及几种已知成分,例如贝卡马林(> 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 ),桦木酸(> 5 )和豆甾醇(> 6 )是从这项正在进行的研究中获得的。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(肝细胞肝癌)进行了测定。甲磺舒酮(> 1 ),贝卡马林(> 2 ),桦木酸(> 5 )和豆甾醇(> 6 )表现出强stigmasterol(> 6 )和beccamarin(> 2 )强烈抑制Raji细胞的增殖,而SK-MEL-28和HeLa的增殖速率受到强烈抑制,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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