白藜芦醇及其类似物的合成及抗TPA促癌作用研究Studies on the synthesis of resveratrol and its analogs and their antipromotion of TPA
陈国良,单韦,徐颖,董金华,张宝凤,计志忠
CHEN Guo-liang1; SHAN Wei1; XU Ying2; DONG Jin-hua1; ZHANG Bao-feng2; JI Zhi-zhong1 (1.School of Pharmaceutical Engineering;
摘要(Abstract):
目的设计合成白藜芦醇类似物 ,并测试其抗佛波酯 (TPA)促癌作用。方法以 3,5 二羟基苯甲酸为原料经多步反应合成目标化合物 ,采用TPA致小鼠耳肿胀促癌法确定目标化合物抗TPA促癌作用。结果所有合成的目标化合物通过1H NMR确认其结构 ,大部分化合物具有明显的抗TPA促癌作用。结论白藜芦醇及其类似物具有较强抗TPA促癌作用。
Objective To design and synthesize resveratrol and its analogs,and to assay their activity of preventing the cancer induced by TPA.Methods The target compounds were synthesized from 3,5-dihydroxybenzoic acid.The activity of preventing the cancer induced by TPA was tested.Result The structures of all the target compounds synthesized were confirmed by 1H-NMR.Most target compounds had potent activity of preventing the cancer induced by TPA.Conclusions Resveratrol and its analogs show good antipromotion activity of TPA.
关键词(KeyWords):
制备;化学合成;白藜芦醇类似物;抗促癌;TPA
preparation; chemical synthesis; resveratrol analogs; antipromotion; TPA
基金项目(Foundation): 国家自然科学基金青年基金资助项目 (3980 0 185 )
作者(Authors):
陈国良,单韦,徐颖,董金华,张宝凤,计志忠
CHEN Guo-liang1; SHAN Wei1; XU Ying2; DONG Jin-hua1; ZHANG Bao-feng2; JI Zhi-zhong1 (1.School of Pharmaceutical Engineering;
参考文献(References):
- [1]JangM ,CaiL ,UdeaniGO ,etal.Cancerchemopreven tiveactivityofresveratrol,anaturalproductderivedfrom grapes[J].Science,1997,275:218-220.
- [2]MorenoMM ,PleixatsR .Dehydroaceticacidchemistry.Anewsynthesisofresveratrol,aphytoalexineofvitisvinifera[J].AnalesdeQuimica,1985,81:157-161.
- [3]ChenGL ,DongJH ,JiZZ .Animprovedsynthesisofresveratrol.AFMCInternationalMedicinalChemistrySymposium[C].Beijing,1999.
- [4]AdamsR ,MackenzieS ,LoeweS .Tetrahydocannabinolho mologswithdoublybranchedalkylgroupsinthe3- posi tion.ⅩⅧ[J].JAmChemSoc,1948,70:664-668.
- [5]韩锐.抗癌药物研究与实验技术[M ].北京:北京医科大学与中国协和医科大学联合出版社,1997.318.
- 陈国良
- 单韦
- 徐颖
- 董金华
- 张宝凤
- 计志忠
CHEN Guo-liang1 - SHAN Wei1
- XU Ying2
- DONG Jin-hua1
- ZHANG Bao-feng2
- JI Zhi-zhong1 (1.School of Pharmaceutical Engineering
- 陈国良
- 单韦
- 徐颖
- 董金华
- 张宝凤
- 计志忠
CHEN Guo-liang1 - SHAN Wei1
- XU Ying2
- DONG Jin-hua1
- ZHANG Bao-feng2
- JI Zhi-zhong1 (1.School of Pharmaceutical Engineering