毛姜花中的细胞毒活性二萜成分

Cytotoxic Labdane-type Diterpenes and Diterpene Derivative from Hedychium villosum

从毛姜花(Hedychium villosum Wall.)中分离得到1个新二萜(1)和1个已知二萜(3).新二萜命名为Villosumcoronarin,该化合物在氯仿或甲醇溶液中发生异构化,部分转化为其差向异构体1';其平面结构经质谱、红外光谱、氢谱、碳谱及无畸变极化转移增强技术(DEPT)、氢氢相关谱(1H-1H COSY)和异核多键相关谱(HMBC)等方法确证;其相对构型由氢谱、ROESY及量化计算确证.化合物3用琼斯试剂氧化后得到化合物4.生物活性筛选结果表明,化合物1对人白血病细胞株(HL-60)和肝癌细胞株(SMMC-7721)具有强的细胞毒活性,其活性超过阳性对照顺铂(DDP).化合物4对HL-60和SMMC-7721细胞具有显著的细胞毒活性.

Research on active components from rhizomes of Hedychium genus has led to isolation of some diterpenes with significant cytotoxic activities against Chinese hamster V-79 cells, KB cells, K562 ceils, A549 cells, etc.. Hedychium villosum Wall. is a perennial rhizomatous herb distributed in China and partially in Southeast Asia, which is used in the treatment of pain and inflammation. A new labdane-type diterpene （1）, methods. Compound 1 was identified as （ 11 S, 15R ） -11 -hydroxy-8 （ 17 ）, 12 （E） -labdadien-15,16-dial 11,15- hemiacetal. The known compound 3 was oxidized by Jones reagent to get diterpene derivative 4. Bioassays re- vealed that compound 1. had strong cytotoxic activity against HL-60 and SMMC-7721 cells with ICs0 values of 0. 74 and 4. 48 p, mol/L, respectively, the activities were stronger than the positive control, c/s-diaminedichlo- roplatinum（DDP）. Compound 4 also showed significant activities against HL-60 and SMMC-7721 ceils with ICs0 values of 3.15 and 9.57 mmol/L, respectively.