Inhibitory effects of Korean plants on HIV-1 activities

Area of Science:

• Natural Product Chemistry
• Virology
• Pharmacology

Background:

• The human immunodeficiency virus type 1 (HIV-1) remains a significant global health challenge, necessitating the continuous search for novel antiviral agents.
• Natural sources are a rich reservoir for discovering compounds with potential therapeutic applications, including anti-HIV-1 activity.

Purpose of the Study:

• To screen methanol extracts of 49 Korean plants for inhibitory effects against key HIV-1 enzymes: reverse transcriptase (RT) and protease.
• To evaluate the anti-HIV-1 activity of these plant extracts.

Main Methods:

• Methanol extracts of 49 Korean plants were prepared and screened.
• Inhibition assays were performed for HIV-1 reverse transcriptase (RNA-dependent DNA polymerase and ribonuclease H activities) and HIV-1 protease.
• Anti-HIV-1 activity was assessed using relevant efficacy and selectivity indices.

Main Results:

• Agrimonia pilosa, Cornus kousa, Limonium tetragonum, and Mallotus japonicus exhibited significant inhibition of HIV-1 reverse transcriptase activity (IC50 values ranging from 6.3 to 11.9 µg/mL).
• Agrimonia pilosa also showed activity against ribonuclease H activity (IC50 = 98.4 µg/mL).
• Agrimonia pilosa, Atractylodes japonica, Clematis heracleifolia, and Syneilesis palmata demonstrated activity against HIV-1 protease.
• Crinum asiaticum var. japonicum displayed significant anti-HIV-1 activity (ED50 = 12.5 µg/mL) with a favorable selectivity index (SI) of 16.

Conclusions:

• Several Korean plant species possess compounds with potent inhibitory activity against critical HIV-1 enzymes.
• These findings highlight the potential of Korean flora as a source for developing novel anti-HIV-1 therapeutic agents.