海藻抗肿瘤抗细菌生物活性物质的研究

IOCAS-IR > 海洋环流与波动重点实验室

	海藻抗肿瘤抗细菌生物活性物质的研究
	徐年军
学位类型	博士
	2002
学位授予单位	中国科学院海洋研究所
学位授予地点	中国科学院海洋研究所
学位专业	海洋生物学
关键词	海藻细胞毒活性抗菌活性活性筛选先导化合物天然产物抗肿瘤药物松节藻
摘要	该文对近四年来海洋抗肿瘤药物的研究现状和大型海藻天然产物的研究现状进行了简要的综述.概述了近年来世界各国的海藻抗肿瘤筛选方面的工作进展;总结了近年来从蓝藻、甲藻、红藻、褐藻、绿藻中分离的活性化合物,其中包括已经进入临床研究阶段的Scytophycin、Halomon、Cryptophycin、Malyngamide、Tolytoxin等.综述了近四年来从大型海藻中分离的约100个天然化合物,其中大部分具有重要的生物活性.以采自山东沿海的39种海藻的96个样品为材料,进行了较系统的抗肿瘤生物活性的筛选,共发现了8种有选择性抗肿瘤活性的海藻.运用薄层层析方法对10种海藻提取物的抗金黄色葡萄球菌和大肠杆菌活性进行了研究,发现褐藻提取物的抗菌活性最高,红藻的抗菌活性较低,而绿藻门海藻几乎没有活性.红藻门的松节藻、鸭毛藻有一定的活性.褐藻门的酸藻和海黍子活性较高.酸藻和海黍子的3个强抗菌活性带对金黄色葡萄球菌的抑菌圈直径分别为33mm、17mm和17.5mm,酸藻水相的2个活性带还能抑制大肠杆菌,其抑菌圈直径分别为21mm和16mm.对山东沿海分布量较大的两种海藻进行了先导化合物的分离纯化和结构鉴定.对萱藻和松节藻中得到的纯化合物和其它粗提物进行了细胞毒活性的检验.
其他摘要	Tens of algae along Shandong coast were collected, and their cytoloxic and antibacterial activities were screened with high throughout screening methods (UTS). As a result, some algae with high activities against tumor cells or bacteria were (bund. The algae were Leoihesia dijformes, Polysiphonia urcedala, Scylosiphon lomeniariu.w (Jloiopeliisfurcalch Rhodomela confervoidcs etc. The work of isolating, purifying and identifying new leading compounds from Rhodomela confervoides and Scylosiphon lomcnlavius were completed. More than 30 compounds were isolated from them, among which-15 were identified by the combination of IR, MS, and ID. 2D NMR modern spectrum methods. There were 5 new compounds and I pure natural compound among the 15 compounds. Furthermore, the cytotoxic activities of these compounds were fulfilled by MTT method, and 9 of them were found to be with selective cytotoxic activities. The recent development of marine antitumor drugs and natural products from macroalgae were briefly reviewed. The studies of antitumor screening in recent years were covered. The bioactive substances in blue algae, dinoflagellate, red algae, brown algae and green algae were summarized, some of them had been applied to preclinic study, such as Scylophycin, Halomon, Cryplophycin. Malyngamide and Tolyloxin. About 100 natural products newly isolated from macroalgae in recent four years were also covered, almost all of which showed significant activities. The antitumor activity screening of 96 crude extracts of 39 species of algae was enclosed, fight species including Symphynchidiu laliiiscu/a, Rhodomela confervoides. Polysiphonia wvedala, Gloiopellis furcahu Lealhesia diffbnnes, Scylosiphon lomenuiriiis. Pimctaria lalifolia and Diclyopleris divaricata showed potent selectively iintineoplastic activities. The ethanol and chloroform extracts of Polysiphonia urccdala, the ethanol extracts of Scylosiphon lomcnlarius and the hexane extracts of Diclyopleris divaricala all showed powerful selectively cytoloxic activities, and their IC50 Were less than 4.40 ug/ml. The ethanol extracts of Scylosiphon tomentur'ws had also showed strong activities against HT-29 tumor cell, and the IC5() was 1.49 ug/ml. Thin layer chromatography (TLC) method was used to study the antibacterial activities against two kinds of bacteria, Escherichia coli and Staphylococcus aurcns. The activities of five seaweed extracts were detected, of which brown algae displayed the highest activities. Three bands from Desmarestia viridis and Sar^assuni kjclimanianum (Phaeophyta) exhibited powerful activities against Staphylococcus aurcns, the diameter of inhibition cycle was 33mm, 17mm and 17.5 mm. respectively. Two bands from Desmareslia viridis could inhibit the growth of Escherichia coli vigorously. The higher activity was detected in red algae. In comparision with browm and red algae, the activities of green algae were almost negligible. Two species of marine algae, Scylosiphon lomenlarius and Rhodomcla coufcrvoiilcs, were used to isolate and purify new leading compounds from them. More than ten compounds were isolated from Scylosiphon lomcntarius and identified as pigments, sterols, fatty acids and glycerides. Among them two were identified as (3R,3R')- β, β-carotene-3\3-diol and fucosterol, respectively. Seventeen compounds were isolated from Rhodomcla confervoidc and 14 were identified. Among them. 5 compounds, 3-bromo-4,5-bis(2J-dibromo-4.5-dihydroxybenzyl)K2-ben/.enedoil (XI.120), 3-bromo-4-[2,3-dibromo-4,5-dihydroxyphenyI] methyI-5-(hydroxymethyl) 1,2-benzenedoil (XU21), 2-methyl-3(2,3-dibromo-4,5-dihydroxy)-propylaldehyde (XU26). 2-methyl-3(2,3-dibromo-4,5-dihydroxy)-propnal methyl hemiacelal(XU28). 3-bix)mo-4-[2.3-dibromo-4,5-dihydroxyphenYl[inelhyl-5-(ethoxymethyl)-], 2-ben/ene -cloil (XU29), were all new. Another compound, 3-bromo-4.5-dihydroxy-ben/.oic acid methyl ester was isolated from natural resources for the first time. The cytoloxic results of all purified compounds and some crude extracts were reported. Two purified compounds D4-1 and BI-15 from Scylosiphon fomenioriiis were found lo be with strongly selective effects on three tumor cells. So were six compounds from Rhodomela confervoides. And some crude extracts were investigated lo have antitumor activities in the experiments.
页数	141
语种	中文
文献类型	学位论文
条目标识符	http://ir.qdio.ac.cn/handle/337002/1533
专题	海洋环流与波动重点实验室
推荐引用方式 GB/T 7714	徐年军. 海藻抗肿瘤抗细菌生物活性物质的研究[D]. 中国科学院海洋研究所. 中国科学院海洋研究所,2002.

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