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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，一些研究详细报道了几种天然产物对12- o - tetradecanoylphorol -13-acetate（TPA）诱导的eb病毒早期抗原（EBV-EA）活化的抑制作用。雷公藤。在中国被用作抗癌药物已有数百年的历史。我们一直在研究一些Celastraceae植物的倍半萜成分。从威氏弓形虫、钩蝇、变种、雷氏和希波氏卫矛中分离到约50个新化合物。为了寻找可能的抗肿瘤启动子，我们检测了这些化合物对EBV-EA活化的抑制倾向。其中一些倍半萜被观察到显著抑制EBV-EA激活允许剂量。接下来，我们试图测试这些化合物的细胞毒性，因为开发化学预防癌症的试剂很重要。一些化合物没有表现出任何细胞毒性。上述结果表明，这些化合物可能是有价值的抗肿瘤促进剂。接下来，我们尝试进行小鼠皮肤的体内两阶段致癌试验。其中一种活性化合物雷公藤gelin A-1在体内两期癌变试验中显示出显著的抑制小鼠皮肤肿瘤促进作用。雷公藤gelin A-1在小鼠肺两期癌变试验中显示抑制作用。我们评估了倍半萜的抗病毒活性，其中一种，雷公藤福丁C-2，被发现对单纯疱疹病毒I型和人巨细胞病毒有活性。我们提出了该化合物可能的作用机制。我们还从Celastraceae植物中分离到了新的化合物。这些发现表明，数据将注意力集中在可能利用信息开发癌症预防剂上。