海藻抗肿瘤物质的筛选及其活性研究概况

SCREENING OF ANTITIMOR COMPOUNDS AND THE ACTIVITY SUBSTANCES FROM MARINE ALGAE

国际上海洋药物研究的热潮自20世纪60年代开始,20世纪70—80年代开展了大规模筛选,迄今为止发现具有抗肿瘤、抗病毒、抗心血管疾病、增强免疫系统等活性的海洋生物活性物质5000余种。海洋天然产物的药理活性侧重于抗肿瘤方面,从海藻中发现的抗肿瘤活性物质占有重要的地位,闪为海藻具有较好的生物多样性,而且其多变的生态环境和原始的进化地位使其拥有许多结构独特的活性物质。

The research of marine anti-tumor drugs develops rapidly, and marine algae are kinds of unique potentially pharmaceutic materials and some of them can be cultivated. It is very important for exploiting and utilizing the resource of marine algae before studying marine drugs. This paper reviews the works on screening of anti-tumor substances in marine algae and the compounds with antitumor activities.Different methods have been applied to evaluate the anti-neoplastic activities of marine algal extracts. Antitumor activities are determined by inhibiting KB human carcinoma cells, P388 lymphocytic leukemia or Ehrlich ascites tumor. They are also evaluated in a series of mechanismbased anticancer screens, including protein kinase C (PKC) , protein tryosine kinase (PTK) and inosine monophosphate dehydrogenase (IMPDH) .About 70 compounds with anti-tumor activities from marine algae have been reviewed in this paper. Many of them are important, such as Halomon, which isolated from marine red alga Portieria hornemanni. More than 10 halomon-related anti-tumor monoterpenes have been identified and are useful in clinical experiment. Malyngamide D is metabolites of Lyngbya majuscula, and it produces a highly cytotoxic profile against KB cells. Amphidinolid J is a cytotoxic macrolide from the marine dinoflagellate Amphiolinium sp. Other cytotoxci substances, such as okdaic acid, lyngbyatoxin A, debromoaplysiatoxin, hormothamnione, hormothamnin A, 15(28)-anhydrothysiferyl diacetate, 15-anhydrothysiferyl diacetate, magireol-A, magireol-B, magireol-C, 15 ( 28 )-anhydrothysiferyl diacetate, 15-anhydrothysiferyl diacetate, magireol-A, magireol-B, magireol-C, caulilide, dexylapachol, dilopholide and caulerpenyne are also introduced.