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与天冬酰胺和谷氨酰胺共轭的壳寡糖的体外抗HIV-1活性

In Vitro Anti-HIV-1 Activity of Chitosan Oligomers -Conjugated with Asparagine and Glutamine.

作者信息

Karadeniz Fatih

机构信息

Marine Biotechnology Center for Pharmaceuticals and Foods, College of Medical and Life Sciences, Silla University, Busan 46958, Republic of Korea.

出版信息

BioTech (Basel). 2023 Feb 8;12(1):18. doi: 10.3390/biotech12010018.

DOI:10.3390/biotech12010018
PMID:36810445
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9944945/
Abstract

Chitosan oligomers (COS) are polysaccharides obtained by the hydrolyzation of chitosan. They are water-soluble, biodegradable, and have a wide range of beneficial properties for human health. Studies have shown that COS and its derivatives possess antitumor, antibacterial, antifungal, and antiviral activities. The goal of the current study was to investigate the anti-human immunodeficiency virus-1 (HIV-1) potential of amino acid-conjugated COS compared to COS itself. The HIV-1 inhibitory effects of asparagine-conjugated (COS-N) and glutamine-conjugated (COS-Q) COS were evaluated by their ability to protect C8166 CD4+ human T cell lines from HIV-1 infection and infection-mediated death. The results show that the presence of COS-N and COS-Q was able to prevent cells from HIV-1-induced lysis. Additionally, p24 viral protein production was observed to be suppressed in COS conjugate-treated cells compared to COS-treated and untreated groups. However, the protective effect of COS conjugates diminished by delayed treatment indicated an early stage inhibitory effect. COS-N and COS-Q did not show any inhibitory effect on the activities of HIV-1 reverse transcriptase and protease enzyme. The results suggest that COS-N and COS-Q possess an HIV-1 entry inhibition activity compared to COS and further studies to develop different peptide and amino acid conjugates containing N and Q amino acids might yield more effective compounds to battle HIV-1 infection.

摘要

壳寡糖（COS）是通过壳聚糖水解获得的多糖。它们可溶于水、可生物降解，对人体健康具有广泛的有益特性。研究表明，COS及其衍生物具有抗肿瘤、抗菌、抗真菌和抗病毒活性。本研究的目的是比较氨基酸共轭COS与COS本身对人免疫缺陷病毒1型（HIV-1）的潜在抑制作用。通过评估天冬酰胺共轭（COS-N）和谷氨酰胺共轭（COS-Q）COS保护C8166 CD4+人T细胞系免受HIV-1感染和感染介导死亡的能力，来评价它们对HIV-1的抑制作用。结果表明，COS-N和COS-Q的存在能够防止细胞因HIV-1诱导而裂解。此外，与COS处理组和未处理组相比，在COS共轭物处理的细胞中观察到p24病毒蛋白的产生受到抑制。然而，延迟处理使COS共轭物的保护作用减弱，表明其具有早期抑制作用。COS-N和COS-Q对HIV-1逆转录酶和蛋白酶的活性没有显示出任何抑制作用。结果表明，与COS相比，COS-N和COS-Q具有HIV-1进入抑制活性，进一步研究开发含有N和Q氨基酸的不同肽和氨基酸共轭物可能会产生更有效的抗HIV-1感染化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/2ba52bb0acab/biotech-12-00018-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/6714b0bf7ef9/biotech-12-00018-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/83b498fcd46f/biotech-12-00018-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/6f7f8d308060/biotech-12-00018-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/2ba52bb0acab/biotech-12-00018-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/6714b0bf7ef9/biotech-12-00018-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/83b498fcd46f/biotech-12-00018-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/6f7f8d308060/biotech-12-00018-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d7e0/9944945/2ba52bb0acab/biotech-12-00018-g004.jpg

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