首页> 外国专利> ANTI-TUMOR ACTIVITY OF AECHL-1, NOVEL TRITERPENOID ISOLATED FROM AILANTHUS EXCELSA IN VITRO AND IN VIVO

ANTI-TUMOR ACTIVITY OF AECHL-1, NOVEL TRITERPENOID ISOLATED FROM AILANTHUS EXCELSA IN VITRO AND IN VIVO

机译:拟南芥AECHL-1,新三萜的体外和体内抗肿瘤活性

摘要

A novel chemical moiety triterpenoid AECHL-1 isolated from root bark of Ailanthus excelsa having anti-cancer properties exhibiting remarkable activity in treatment of various forms of tumors with specificity wherein it blocks the growth of four tumor cell lines with distinct origins and of different p53 status (B16F10 mouse melanoma, PC3 human prostate cancer, MCF-7 and MDA-MB-231 human breast cancer), having following characteristic IR, NMR and mass spectra IR (KBr): 3425, 3419 (hydroxyl group), 2972, 2966, 2923, 2873 (alkyl C—H stretch), 1733 (δ lactone), 1718 (Bi acetyl), 1680 (C═O conjugation with alkene), 1652 (—C═C stretching), 1600 (aromatic), 1492, 1454, 1394 (methyl stretching), 1222 (δ lactone), 1184, 1110, 1051, 1031 (acetals), 1018 nm (alkanes). 1H-NMR (DMSO, 400 Hz) δ: 0.95 (3H, t, 4′-CH3), δ:1.15 (3H, d, H-24), δ:1.235 (3H, d, 5′-CH3), δ: 1.5 (2H, ddd, 5′-CH2), δ: 1.73 (3H, ddd, H-21), δ: 1.83 (1H, s, H-9), δ: 1.87 (1H, s, H-14), δ: 1.9 (2H, s, H-18), δ: 2.16 (3H, s, H-18), δ: 2.3 (3H, d, H-19) δ: 2.71 (2H, s, H-20), δ: 3.45 (2H, dd, H-23), δ:3.65 (2H, d, H-22), δ: 3.95 (1H, t, H-12), δ: 4.05 (2H, s, H-22), δ: 5.30 (1H, s, H-15), δ: 5.46 (1H, s, OH-2), 6: 5.73 (1H, d,OH-2′), δ: 6.89 (1H, s, H-3), δ: 8.82 (1H, s, OH-11). Chemical shifts are given in ppm on the δ-scale, s=singlet, d=doublet, t=triplet. The mass spectra showing the following principal peaks: m/z: 1068 due to dimer formation. The actual [M+] was considered to be 543.8, 463.3 [M-C4H1O2], 461.4 [M-C4H2O2], 459.4 [M-C4H4O2], 361.2 [M-C9H11O4] is a solid mp. 248-250° C. possessed a molecular formula of C29H36O10 as indicated by EI and ES mass spectra.
机译:从臭椿的根皮中分离出的一种新型化学三萜类化合物AECHL-1具有抗癌特性,具有特异性地治疗各种形式的肿瘤的显着活性,其中它阻止了四种肿瘤细胞的生长。具有以下特征IR,NMR和质谱IR(KBr)的不同来源且具有不同的p53状态(B16F10小鼠黑素瘤,PC3人类前列腺癌,MCF-7和MDA-MB-231人类乳腺癌):3425、3419(羟基基团),2972,2966,2923,2873(烷基CH伸直),1733(δ内酯),1718(双乙酰基),1680(C═O与烯烃共轭),1652(-C═C伸张),1600 (芳族),1492、1454、1394(甲基拉伸),1222(δ内酯),1184、1110、1051、1031(缩醛),1018 nm(烷烃)。 1 H-NMR(DMSO,400 Hz)δ:0.95(3H,t,4'-CH 3 ),δ:1.15(3H,d,H-24 ),δ:1.235(3H,d,5′-CH 3 ),δ:1.5(2H,ddd,5′-CH 2 ),δ:1.73( 3H,ddd,H-21),δ:1.83(1H,s,H-9),δ:1.87(1H,s,H-14),δ:1.9(2H,s,H-18),δ: 2.16(3H,s,H-18),δ:2.3(3H,d,H-19)δ:2.71(2H,s,H-20),δ:3.45(2H,dd,H-23),δ :3.65(2H,d,H-22),δ:3.95(1H,t,H-12),δ:4.05(2H,s,H-22),δ:5.30(1H,s,H-15) ,δ:5.46(1H,s,OH-2),6:5.73(1H,d,OH-2'),δ:6.89(1H,s,H-3),δ:8.82(1H,s,OH) -11)。化学位移以ppm为单位在δ标度上给出,s =单峰,d =双峰,t =三重峰。质谱显示以下主要峰:m / z:由于形成二聚体,为1068。实际的[M + ]被认为是543.8,463.3 [MC 4 H 1 O 2 ], 461.4 [MC 4 H 2 O 2 ],459.4 [MC 4 H 4 O 2 ],361.2 [MC 9 H 11 O 4 ]是坚固的mp。 EI和ES质谱表明,在248-250℃下具有C 29 H 36 O 10 的分子式。

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