首页|ALKALOIDS FROM THE TWIGS OF Catharanthus roseus
ALKALOIDS FROM THE TWIGS OF Catharanthus roseus
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Catharanthus roseus(L.)G.Don {Apocynaceae)is a famous plant used to treat numerous diseases,including diabetes,malaria,and cancer [1].The plant is rich in indole alkaloids.Among them,vinblastine and vincristine are typical compounds that have been used extensively for the clinical treatment of human cancers,such as testicular carcinoma,acute leukemia,rhabdomyosarcoma,and breast cancer [2-4],In order to find further bioactive alkaloids,we studied С roseus collected from Yunnan of China and isolated 19 alkaloids and an amide.The air-dried twigs of C.roseus(24.7 kg)were powdered and extracted with acetone(five times,each 40 L)at room temperature.After evaporation of the solvent,the acetone extract was acidified to pH 1-2 with 3% aq.tartaric acid and then partitioned with EtOAc.The acidic aqueous phase was basified to pH 10 with NH4OH and then extracted with CHCI3 to yield crude alkaloids(138 g),which was subjected to column chromatography(CC)over silica gel eluting with gradient CHCl3-MeOH(1:0→0:1)to yield four fractions(Frs.1-4).Fraction 1(43 g)was separated by silica gel CC with gradient petroleum ether-acetone(50:0→2:1)to give two subfractions.Subfraction la(13 g)was further isolated on Sephadex LH-20 CC(CHCI3:MeOH3:2)and then purified on a silica gel column with petroleum ether-EtOAc-diethylamine(20:1:1)to afford 2(5.1 mg),8(128.5 mg),9(6.0 mg),and 20(5.7 mg).Subfraction lb(21 g)was further separated on a RP-18 column eluting with 70% aq.MeOH,and Sephadex LH-20 CC(CHCl3-MeOH,3:2)and then purified on silica gel column with CHCl3-MeOH(50:1)to produce 1(9.9 mg),3(8.3 mg),10(10.5 mg),11(15.8 mg),12(20.1 mg),and 13(19.6 mg).Fraction 3(30 g)was separated by silica gel CC with gradient petroleum ether-acetone(50:0→2:1)to give three subfi-actions.Subfraction 3a(9.6 g)was separated by Sephadex LH-20 CC(CHClg-MeOH,3:2)and on a silica gel column with petroleum ether-EtOAc-diethylamine(10:1:1)and then purified on a silica gel column with СНС1з-МеОН(20:1)to obtain 4(25.6 mg),5(5.2 mg),6(10.1 mg),7(6.4 mg),and 14(24.0 mg).Subfraction 3b(1.2 g)was purified by Sephadex LH-20 CC(MeOH 100%)and then on a silica gel column with CHCl3-MeOH(15:1)to give 15(9.2 mg)and 16(8.5 mg).Subfi-action 3c(6 g)was isolated by Sephadex LH-20 CC(СНС1з-МеОН,3:2)and then on a silica gel column with CHCl3-acetone(8:1)to furnish 15(8.7 mg),16(7.4 mg),17(6.2 mg),18(10.5 mg),19(9.9 mg).
Zu-Liang He、Li Yang
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School of Chemistry and Chemical Engineering,Yunnan Normal University,650500,Kunming,P.R.China
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