排序方式: 共有14条查询结果,搜索用时 0 毫秒
11.
To investigate the antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo, six bromophenol derivatives 6-(2,3-dibromo-4,5-dihydroxybenzyl)-2,3-dibromo-4,5-dihydroxy benzyl methyl ether (1), (+)-3-(2,3-dibromo-4,5-dihydroxyphenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroisobenzofuran (2), 3-bromo-4-(2,3-dibromo-4,5-dihydroxybenzyl)-5-methoxymethyl-pyrocatechol (3), 2,2′,3,3′-tetrabromo-4,4′,5,5′-tetrahydroxy-diphenylmethane (4), bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (5), 2,2′,3-tribromo-3′,4,4′,5-tetrahydroxy-6′-ethyloxymethyldiphenylmethane (6) were isolated from brown alga Leathesia nana, and their cytotoxicity were tested by MTT assays in human cancer cell lines A549, BGC-823, MCF-7, B16-BL6, HT-1080, A2780,
Bel7402 and HCT-8. Their inhibitory activity against protein tyrosine kinase (PTK) with over-expression of c-kit was analyzed also by ELISA. The antitumor activity of ethanolic extraction of Leathesia nana (EELN) was evaluated on S180-bearing mice. All compounds showed very potent cytotoxicity against all of the eight cancer cell lines with IC50 below 10 μg/mL. In PTK inhibition study, all bromophenol derivatives showed moderate inhibitory activity and compounds 2,
5 and 6 showed significant bioactivity with the inhibition ratio of 77.5%, 80.1% and 71.4%, respectively. Pharmacological
studies reveal that EELN could inhibit the growth of Sarcoma 180 tumor and increase the indices of thymus and spleen to improve
the immune system remarkably in vivo. Results indicated that the bromophenol derivatives and EELN can be used as potent antitumor agents for PTK over-expression
of c-kit and considered in a new therapeutic strategy for treatment of cancer.
Supported by the National High Technology Research and Development Program of China (863 Program, No. 2007AA09Z410) and Knowledge
Innovation Program of Chinese Academy of Sciences (No. KZCX2-YW-209) 相似文献
12.
5种南海海藻醇提取物活性初步研究 总被引:1,自引:0,他引:1
海藻是海洋生物代谢产物的主要来源之一,能产生丰富多样的生物活性物质.为了更好地利用中国南海的海藻资源,分别对采自中国湛江硇洲岛的1种绿藻基根硬毛藻Chaetomorpha basiretorsa Setchell和4种红藻刺状鱼栖苔Acantophora spicififera (Vahl) Boerg、三列凹顶藻Laurencia tristicha Tseng, Chang et Xia、紫杉状海门冬Asparagopsis taxiformis (Delile) Trevisan、鸡毛菜Pterocladia tenuis Okam进行了生物活性研究,分别对细胞毒活性(KB、Bel-7402、PC-3M、Ketr3和MCF-7)、Na~+,K~+-ATPase抑制活性以及犬血管平滑肌细胞增殖抑制活性进行了筛选,部分海藻提取物表现出一定的生理活性. 相似文献
13.
14.
Thrombin, the ultimate proteinase of the coagulation cascade, is an attractive target for the treatment of a variety of cardiovascular diseases. A bromophenol derivative named (+)-3-(2,3-dibromo-4, 5-dihydroxy-phenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroiso-benzofuran 1, isolated from the brown alga Leathesia nana exhibited significant thrombin inhibitory activity. In this study, we investigated the inhibition of human thrombin in vitro with this bromophenol derivative, and its antithrombotic efficacy in vivo using the arteriovenous shunt model and the ferric chloride-induced arterial thrombosis model in rats. The results show that the bromophenol derivative is a potential inhibitor of thrombin (IC50=1.03 nmol/L). In antithrombotic experiments in vivo, the bromophenol derivative also shows good effect comparing with the control group. These data indicate that the bromophenol derivative is a potential drug for prophylaxis and the treatment of thrombotic diseases. 相似文献