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红海海洋生物的细胞毒性和HIV-1酶抑制活性。

Cytotoxic and HIV-1 enzyme inhibitory activities of Red Sea marine organisms.

作者信息

Ellithey Mona S, Lall Namrita, Hussein Ahmed A, Meyer Debra

机构信息

Department of Biochemistry, University of Pretoria, Pretoria, 0002, South Africa.

出版信息

BMC Complement Altern Med. 2014 Feb 25;14:77. doi: 10.1186/1472-6882-14-77.

Abstract

BACKGROUND

Cancer and HIV/AIDS are two of the greatest public health and humanitarian challenges facing the world today. Infection with HIV not only weakens the immune system leading to AIDS and increasing the risk of opportunistic infections, but also increases the risk of several types of cancer. The enormous biodiversity of marine habitats is mirrored by the molecular diversity of secondary metabolites found in marine animals, plants and microbes which is why this work was designed to assess the anti-HIV and cytotoxic activities of some marine organisms of the Red Sea.

METHODS

The lipophilic fractions of methanolic extracts of thirteen marine organisms collected from the Red Sea (Egypt) were screened for cytotoxicity against two human cancer cell lines; leukaemia (U937) and cervical cancer (HeLa) cells. African green monkey kidney cells (Vero) were used as normal non-malignant control cells. The extracts were also tested for their inhibitory activity against HIV-1 enzymes, reverse transcriptase (RT) and protease (PR).

RESULTS

Cytotoxicity results showed strong activity of the Cnidarian Litophyton arboreum against U-937 (IC50; 6.5 μg/ml ±2.3) with a selectivity index (SI) of 6.45, while the Cnidarian Sarcophyton trochliophorum showed strong activity against HeLa cells (IC50; 5.2 μg/ml ±1.2) with an SI of 2.09. Other species showed moderate to weak cytotoxicity against both cell lines. Two extracts showed potent inhibitory activity against HIV-1 protease; these were the Cnidarian jelly fish Cassiopia andromeda (IC50; 0.84 μg/ml ±0.05) and the red algae Galaxura filamentosa (2.6 μg/ml ±1.29). It is interesting to note that the most active extracts against HIV-1 PR, C. andromeda and G. filamentosa showed no cytotoxicity in the three cell lines at the highest concentration tested (100 μg/ml).

CONCLUSION

The strong cytotoxicity of the soft corals L. arboreum and S. trochliophorum as well as the anti-PR activity of the jelly fish C. andromeda and the red algae G. filamentosa suggests the medicinal potential of crude extracts of these marine organisms.

摘要

背景

癌症和艾滋病毒/艾滋病是当今世界面临的两大重大公共卫生和人道主义挑战。感染艾滋病毒不仅会削弱免疫系统,导致艾滋病并增加机会性感染的风险,还会增加多种癌症的发病风险。海洋栖息地的巨大生物多样性反映在海洋动物、植物和微生物中发现的次生代谢产物的分子多样性上,这就是开展这项工作以评估红海一些海洋生物的抗艾滋病毒和细胞毒性活性的原因。

方法

对从红海(埃及)采集的13种海洋生物的甲醇提取物的亲脂性部分进行筛选,以检测其对两种人类癌细胞系的细胞毒性;白血病(U937)细胞和子宫颈癌细胞(HeLa)。非洲绿猴肾细胞(Vero)用作正常非恶性对照细胞。还测试了提取物对艾滋病毒-1酶、逆转录酶(RT)和蛋白酶(PR)的抑制活性。

结果

细胞毒性结果显示,刺胞动物树状软珊瑚对U-937具有较强活性(半数抑制浓度[IC50];6.5μg/ml±2.3),选择性指数(SI)为6.45,而刺胞动物曲纹肉芝软珊瑚对HeLa细胞显示出较强活性(IC50;5.2μg/ml±1.2),SI为2.09。其他物种对两种细胞系均表现出中度至弱的细胞毒性。两种提取物对艾滋病毒-1蛋白酶显示出强效抑制活性;它们是刺胞动物海月水母(IC50;0.84μg/ml±0.05)和红藻丝状乳节藻(2.6μg/ml±1.2)。有趣的是,对艾滋病毒-1蛋白酶活性最强的提取物,即海月水母和丝状乳节藻,在测试的最高浓度(100μg/ml)下对三种细胞系均无细胞毒性。

结论

树状软珊瑚和曲纹肉芝软珊瑚的强细胞毒性以及海月水母和丝状乳节藻的抗蛋白酶活性表明这些海洋生物粗提物具有药用潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/790e/3939812/26c23d6d52e0/1472-6882-14-77-1.jpg

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