Maytansine,15-(acetyloxy)-2'-de(acetylmethylamino)-2'-methyl-

Maytanbutacine

693.19

结晶(二氯甲烷-乙醚),熔点253～5°,[α]23/D-90°(C=0.055,乙醇)。UV λEtOHmax nm(ε):233(27200),253(24200),282(5050),290(5080)。IR λKBrmaxμ:5.73,5.82,6.00,6.32,8.16,9.17。MSm/e:631.2540,571.2331。NMR(CDCl3)δ:0.79(3H,s C-4CH3),1.20(3H,d,J=7,C-2'CH3),1.28(3H,d,J=7,C-2'CH3),1.28(3H,d,J=7,C-6CH3),1.67(3H,s,C-14CH3),2.23(3H,s,C-15 OCOCH3),2.43(1H,d,J2,2=14,J2,3=11,C-2H),2.47(1H,dd,J2,2=14,J2,3=3,C-2H),2.95(1H,d,J5,6=8.5,C-5H),3.16(3H,s,C-1NCH3),3.35(3H,s,C-10OCH3),3.51(1H,d,J10,11=9,C-10H),4.02(3H,s,C-20OCH3),4.26(1H,m,C-7H),4.79(1H,dd,J2,3=11,3,C-3H),5.60(1H,dd,J10,11=9,J11,12=14,C-11H),6.21(1H,s,C-15H),6.30(1H,dd,J12,13=10,C-12H),6.39(1H,s,C-9NH),6.44(1H,d,J12,13=10,C-13H),6.85(1H,d,J17,21=1.5,C-21H),7.09(1H,d,J17,21=1.5,C-17H),1.0～2.0(3H,C-6H,C-8H),2.0～2.6(1H,m C-2'H)。

有抗癌作用,对小鼠淋巴白血病和鼻咽癌KB细胞都有很强的活性。在最佳剂量12.5μg/kg时,对P388的生命延长率为79%;对KB细胞有细胞毒活性,ED50为0.0000015μg/ml。本品已进入临床研究阶段。

卫矛科植物齿叶美登木 Maytenus serrata(Hochst.ex Rich.)R.Wilczek 果实。

1.《植物药有效成分手册》人民卫生出版社1986

C34H45ClN2O11