Abstract
Human immunodeficiency virus type-1 (HIV-1) infection causes acquired immunodeficiency syndrome (AIDS). Currently, several anti-retroviral drugs are available, but adverse effects of these drugs have been reported. Herein, we focused on the anti-HIV-1 activity of Curcuma aeruginosa Roxb. (CA) extracted by hexane (CA-H), ethyl acetate (CA-EA), and methanol (CA-M). The in vitro HIV-1 protease (PR) and HIV-1 reverse transcriptase (RT) inhibitory activities of CA extracts were screened. CA-M potentially inhibited HIV-1 PR (82.44%) comparable to Pepstatin A (81.48%), followed by CA-EA (67.05%) and CA-H (47.6%), respectively. All extracts exhibited moderate inhibition of HIV-1 RT (64.97 to 76.93%). Besides, phytochemical constituents of CA extracts were identified by GC-MS and UPLC-HRMS. Fatty acids, amino acids, and terpenoids were the major compounds found in the extracts. Furthermore, drug-likeness parameters and the ability of CA-identified compounds on blocking of the HIV-1 PR and RT active sites were in silico investigated. Dihydroergocornine, 3β,6α,7α-trihydroxy-5β-cholan-24-oic acid, and 6β,11β,16α,17α,21-Pentahydroxypregna-1,4-diene-3,20-dione-16,17-acetonide showed strong binding affinities at the active residues of both HIV-1 PR and RT. Moreover, antioxidant activity of CA extracts was determined. CA-EA exhibited the highest antioxidant activity, which positively related to the amount of total phenolic content. This study provided beneficial data for anti-HIV-1 drug discovery from CA extracts.
Highlights
We found that Curcuma aeruginosa Roxb. (CA)-EA and CA-M were mainly composed of fatty acids, amino acids, and terpenoids (Supplementary data S2 and S3)
Our results indicated that these four candidate ligands found in CA-EA and CA-M extracts potentially inhibit Human immunodeficiency virus type-1 (HIV-1) reverse transcriptase (RT) at the RNase active site
Our current study demonstrated a novel biological activity of Curcuma aeruginosa Roxb
Summary
Acquired immunodeficiency syndrome (AIDS) is caused by the infection of the human immunodeficiency virus (HIV). Both HIV-1 and HIV-2 are found in HIV-infected patients, but HIV-1 infection shows more severe clinical pathology and progression of disease than. HIV-1 can infect the immune cells and, use the benefit of the host cells to replicate itself, and destroy the host cells. These processes cause immunocompromised hosts, leading to the infection of opportunistic pathogens such as Mycobacterium tuberculosis and death [2].
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