| Plant Euonymus alatus belonging to Celastraceae family, Euonymus genus, was fitst recorded in<Shen Nong’s Herbal Classic> and classified as middle product. Euonymus alatus distributes in north, middle, southwest and east of China and is rich in resources. Pharmacology studies have shown that it has anti-tumor, anti-oxidant, lipids regulating, hypoglycemic effect, retaeded atherosclerosis, and anti-feedant activities. In recent years, it was used for the treatment of diabetes, arteriosclerosis, hyperlipidemia, angina, rhus dermatitis, with the significant effectiveness. It was also used as the antit-umor drug in Korea and Janpan. Literatures scarcely showed system chemical constituents and thorough anti-tumor activity studies on this plant. Therefore, we took studies to this plant on separating and identifying its chemical compositions systematically, as well as cytotoxic activity screening in virto, aimed at discovering compounds with good anti-tumor activity, and laying the foundation for the development of anticancer drugs from natural products.The systematically phytochemical study on this plant, led to the isolation and identification of fifty-seven chemical constituents, including eight sesquiterpenoids, ten norsesquiterpenoids, two diterpenoids, eight triterpenoids, six sterides and cardiac glycosides, ten lignans, eight phenylpropanoids and five others. Among them,14-isovaleryloxy-neojunceol A (1),9β-furancarbonyloxy-6β,15a-dihydroxy-1a-(2)-methylbutanoyloxy-2a-propanoyloxy-dihydro-β-agarofuran (2) were two new sesquiterpenoids, compounds3-5,8-21,25-28,32-34,36-39,41,43-44,47-52,55-57were isolated from this plant for the first time.1.14-isovaleryloxy-neojunceol A2.6β,15a-dihydroxy-9β-furancarbonyloxy-4β-hydroxy-1a-2-methylbutanoyloxy-2a-propionyl-β-dihydroagarofuran3.6β,15a-diacetoxy-2a,9β-difurancarbonyloxy)-4β-hydroxy-1a-2-methylbutanoylo xy-β-dihydroagarofuran4.1a,2a,6β-triacetoxy-9β-furancarboxy-4β-hydroxy-15a-2-methylbutyroyloxy-β-dihydroagarofuran5.1a,2a,5β,8a,15a-pentaacetoxy-4β-hydroxy-3β-2-methylbutanoyl-12-nicotinoyl-8-oxo-β-dihydroagarofuran6. evonine 7. neoevonine8. madolin B9. annuionone D10.3β-hydroxy-5a,6a-epoxy-7-en-megastimen-9-one11.(3S,5R,6R,7E,9S)-3,5,6,9-tetrahydroxy-7-en-megastigmane12. grasshopper ketone13.8,9-dihydromegastigmatrienone14.9-epi-blumenol B15. corchoionol C16.(3S,5R,6R)-5-hydroxy-3,6-epoxy-β-ionol17.(3R,5S,6S,7E,9S)-7-ene-5-methoxy-3,6,9-trihydroxy-megastigmane18. loliolide19.6β-Hydroxyferruginol20. trans-phytol21. urs-12-ene-2β,3β,22a-triol22. epifriedelinol23. friedelin24. olean-12-ene-2β,3β,22a-triol25. taraxerone26. taraxerol27. primulagenin A28. maytenfolic acid29.β-sitosterol30.β-daucosterin31. acovenosigenin A3-O-a-L-rhamanopyranoside32. xysmalomonosid33. acovenosigenin A34. xysmalogenin35. secoisolariciresinol36. prinsepiol37. lariciresinol38. syringaresinol39. pinoresinol40. medioresinol 41. balanophonin42. isolariciresinol43. ficusesquilignan B44. hedyotol D45. coniferaldehyde46. ω-hydroxypropioguaiacone47.(1R,2R)-guaiacyl-glycerol48. C-veratroylglycol49. evofolin B50. feruloyl malate51. methyl feruloyl malate (14g)52. methyl feruloyl malate (14i)53.4-hydroxy-3-methoxybenzaldehyde54.4-hydroxy-3-methoxybenzoic acid55. ethylβ-D-glucopyranoside56.5,5-Diisobutoxy-2,2-bifuran57. corchorifatty acid ESome compounds were evaluated for cytotoxicity activities against four human cancer cell lines, A549, HCT116, SK-BR-3and HepG2by MTT assay. Compound1showed moderate activity against these cell lines with IC50values of24.98、12.79、11.34、11.33μg/mL. However, the other sesquiterpenoids did not show cytotoxicity. Nevertheless two cardiac glycosides (31,32) and there aglycones (33,34) showed well cytotoxicities. Compound31showed strong cytotoxicity against four cell lines with IC50values of0.001、0.00256、0.0749、0.001μg/mL, respectively. The influence of cardiac glycosides on the cell cycle of HCT116was also tested, and compounds31-34showed strong G2/M arret on it. Thus, their prohibition of proliferation on HCT116may correspond to the arrest of G2/M phase. |
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