| 摘要: |
| 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，因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，其研究始于巨大鞘丝藻的脂溶性提取物抗白血病活性的发现。20世纪80年代初美国和日本的科学家开始系统地筛选海藻的抗肿瘤活性物质，发现了许多新的化合物，如从松香藻中分离的Halomon，Scytophycin B目前已进入临床前药理评估阶段。
海洋药物的发展首先应着重可再生资源的开发和利用方面的研究，而海藻是一种取之不尽的药源物质，随着现代化生物技术的发展，特别是生物工程技术的发展和应用，基本上解决了药源藻类的养殖问题，为海藻抗肿瘤物质的研究提供了充足的材料和可行性，迄今海藻抗肿瘤生物活性物质的研究已取得了引人注目的成就。本文根据有关文献着重就海藻中抗肿瘤活性物质的筛选，以及相应的活性化合物作一综述。 |
| 关键词: 海洋药物 抗肿瘤 活性 |
| DOI： |
| 分类号: |
| 基金项目:中国科学院海洋研究所调查研究报告第4066号。国家自然科学基金资助项目，29932030号。 |
|
| SCREENING OF ANTITUMOR COMPOUNDS AND THE ACTIVITY SUBSTANCES FROM MARINE ALGAE |
|
Fan Xiao, Han Lijun, Xu Nianjun
|
|
Institute of Oceanology, Chinese Academy of Sciences
|
| Abstract: |
| 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 mechanism based anticancer screens, including protein kinase C (PKC), protein tyrosine 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. Malynganide 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 Amphiolonium sp. Other cytotoxic substances, such as okadaic acid, lyngbyatoxin A, debromoaplysiatoxin, hormothamnione, hormothamnin A, 15(28)-anhydrothysiferyl diacetate, 15-anhydrothysiferyl diacetate, magireol-A, magireol-B, magireol-C, caulilide, dexylapachol, dilopholide and caulerpenyne are also introduced. |
| Key words: marine drugs antitumor activities |
