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

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.

Chitosan: A Potential Biopolymer in Drug Delivery and Biomedical Applications

“…To put it another way, COS-N and COS-Q were able to protect cells against the lysis caused by HIV-1. The synthesis of the viral protein p24 was also reduced in COS conjugate-treated cells relative to both the COS-treated and untreated groups [78].…”

“…Additionally, lowering the polymerization degree of low molecular weight chitosan increases their antiviral activity. Chitosan with a molecular weight below 10 kDa has been reported to display antiviral effects against several influenza virus subtypes, suggesting that molecular weight plays a role in antiviral activity [77,78].…”

Chitooligosaccharide and Its Derivatives: Potential Candidates as Food Additives and Bioactive Components

“…Furthermore, the potential of CHOS conjugated with asparagine (CHOS-N) and glutamine (CHOS-Q) to inhibit HIV-1 was explored. CHOS-N and CHOS-Q could protect human T cells from HIV-1 infection and cell death (Table 3) [133].…”

“…Increase IL-10 level Decrease NO and TNF-α levels [113] AE-CHOS and DEAE-CHOS Inhibit AGS gastric cancer cell growth via regulation of p53, p21, Bcl-2, and Bax proteins [126] Carboxymethyl-CHOS Suppress tumor growth in H22 tumor-bearing mice model [130] CHOS-asparagine and CHOS-glutamine Protect human T cells from HIV-1 infection [133] CHOS-epigallocatechin gallate 1. Antimicrobial activity against Listeria monocytogenes and Escherichia coli 2.…”

Isolation and Purification of Chitosan Oligosaccharides (Mw ≤ 1000) and Their Protective Effect on Acute Liver Injury Caused by CCl4

“…There are also studies using chitosan oligosaccharides as a drug carrier [ 8 , 9 ] or as a prebiotic to explore their influence on intestinal flora in different diseases [ 10 , 11 ]. It has also been revealed to have anti-diabetes [ 12 ], anti-obesity [ 13 ], anti-HIV-1 [ 14 ], and anti-Alzheimer’s disease [ 15 ] effects and promote calcium absorption [ 16 ].…”