4.6 Article

Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of Hypericum kouytchense

Journal

PHARMACEUTICALS
Volume 15, Issue 12, Pages -

Publisher

MDPI
DOI: 10.3390/ph15121499

Keywords

Hypericum kouytchense; active ingredient; UPLC-HRMS; HIV-1 protease; cathepsin L protease; molecular docking

Funding

  1. Innovation Group Project of Guizhou Province [Qian Jiao He KY (2021) 018]
  2. Guizhou Provincial Science and Technology Projects [Qian Ke He Zhi Cheng (2020) 4Y213, ZK (2022) general480]
  3. Research Center of Molecular Bioactivity from Traditional Chinese Medicine and Ethnomedicine [3411-4110000520364]
  4. Innovative and Entrepreneurial Project of Guizhou University of Traditional Chinese Medicine [2019(56)]
  5. Shenzhen Fund for Guangdong Provincial High-Level Clinical Key Specialties [SZXK059]
  6. Youth Science and Technology Talent Growth Project of Guizhou Province [Qian Jiao He KY (2022) 253]
  7. Project of Guizhou Provincial Health Commission [gzwkj2022-232, gzwkj2022-467]

Ask authors/readers for more resources

In this study, the antiviral activities of extracts from the insect gall of Hypericum kouytchense were evaluated. The active ingredients were identified and quantified, and their interactions with proteases were analyzed using molecular docking. The results suggest that these extracts and active ingredients have the potential to be developed for preventing and treating HIV or SARS-CoV-2 infections.
Hypericum kouytchense Levl is a semi-evergreen plant of the Hypericaceae family. Its roots and seeds have been used in a number of traditional remedies for antipyretic, detoxification, anti-inflammatory, antimicrobial and antiviral functions. However, to date, no bioactivity compounds have been characterized from the insect gall of H. kouytchens. In this study, we evaluated the antiviral activities of different extracts from the insect gall of H. kouytchen against cathepsin L, HIV-1 and renin proteases and identified the active ingredients using UPLC-HRMS. Four different polar extracts (HW, H30, H60 and H85) of the H. kouytchense insect gall exhibited antiviral activities with IC50 values of 10.0, 4.0, 3.2 and 17.0 mu g/mL against HIV-1 protease; 210.0, 34.0, 24.0 and 30.0 mu g/mL against cathepsin L protease; and 180.0, 65.0, 44.0 and 39.0 mu g/mL against human renin, respectively. Ten compounds were identified and quantified in the H. kouytchense insect gall extracts. Epicatechin, eriodictyol and naringenin chalcone were major ingredients in the extracts with contents ranging from 3.9 to 479.2 mu g/mg. For HIV-1 protease, seven compounds showed more than 65% inhibition at a concentration of 1000.0 mu g/mL, especially for hypericin and naringenin chalcone with IC50 values of 1.8 and 33.0 mu g/mL, respectively. However, only hypericin was active against cathepsin L protease with an IC50 value of 17100.0 mu g/mL, and its contents were from 0.99 to 11.65 mu g/mg. Furthermore, we attempted to pinpoint the interactions between the active compounds and the proteases using molecular docking analysis. Our current results imply that the extracts and active ingredients could be further formulated and/or developed for potential prevention and treatment of HIV or SARS-CoV-2 infections.

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