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Studies on The Low Toxic Antitumor Promoting Activities of Natural Products in Celastraceae Plants.

卫矛科植物天然产物低毒抗肿瘤促进活性的研究。

基本信息

批准号：
05453183
负责人：
TAKAISHI Yoshihisa
金额：
$ 4.61万
依托单位：
University of Tokushima
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (B)
财政年份：
1993
资助国家：
日本
起止时间：
1993 至 1995
项目状态：
已结题

项目摘要

Recently, studies on antitumor promoting activities have been reported detailing the inhibitory effects of several natural products on 12-O-tetradecanoylphorbol-13-acetate(TPA)induced Epstein-Barr virus early antigen(EBV-EA)activation. Tripterygium wilfordii Hook fil.has been used as an anticancer drug in China for hundreds of years. We have been studying the sesquiterpene constituents of some Celastraceae plants.We isolated about 50 new compounds from T.wilfordii Hook fil.var.regelii and Euonymus sieboldianus.To search for possible antitumor pormoters, we examined the inhibitory tendency of these compounds on EBV-EA activation. Some of these sesquiterpenes were observed to significantly inhibit the EBV-EA activation allow doses. Next, we attempted to test the cytotoxicity of these compounds, because it is important to develop a reagent for chemoprevention against cancer. Several compounds did not show any cytotoxicity. Above findings indicate that these compounds might be valuable antitumor promoters.Next, we tried to test in vivo two-stage carcinogenic test of mouse skin. Triptogelin A-1, one of the active compounds, exhibited remarkable inhibitory effects on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. Furthermore, triptogelin A-1 showed inhibitory effects in two stage carcinogenesis test in mouse lung.We evaluated sesquiterpenes for their antiviral activities, one of them, triptofordin C-2, was found to be active against herpes simplex virus type I and human cytomegalovirus. We suggest possible mechanisms of action of the compound.We also isolated new compounds from Celastraceae plants.These findings ndicated that data focus attention on possible exploitation of information for cancer preventive agent development.

近年来，一些天然产物对12-O-十四烷酰基佛波醇-13-乙酸酯（TPA）诱导的EB病毒早期抗原（EBV-EA）活化的抑制作用的研究已被报道。雷公藤作为抗癌药物在我国已有数百年的历史。本研究从卫矛科植物中分离得到了50个新化合物，并对这些化合物的抗EBV-EA活性进行了研究。观察到这些倍半萜中的一些显著抑制EBV-EA活化允许剂量。接下来，我们尝试测试这些化合物的细胞毒性，因为开发用于癌症化学预防的试剂是重要的。几种化合物未显示出任何细胞毒性。以上结果表明，这些化合物可能是有价值的抗肿瘤促进剂。活性化合物之一Triptogelin A-1在体内两阶段致癌试验中对小鼠皮肤肿瘤促进表现出显著的抑制作用。此外，triptogelin A-1在小鼠肺的两阶段致癌试验中显示出抑制作用。我们评价了倍半萜类化合物的抗病毒活性，其中triptofordin C-2被发现对单纯疱疹病毒I型和人巨细胞病毒具有活性。我们提出了该化合物可能的作用机制，并从卫矛科植物中分离出了新的化合物，这些发现表明，数据集中于可能开发癌症预防剂的信息。