4.4 Article

Identification and quantitative analysis of bioactive components from Potentilla kleiniana Wight et Arn with anti HIV-1 proteases activity

期刊

NATURAL PRODUCT RESEARCH
卷 -, 期 -, 页码 -

出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2022.2162513

关键词

Potentilla kleiniana; bioactive components; HIV-1 protease

资金

  1. Technology Planning Project of Guizhou Province [QianKe He Zhi Cheng [2020]4Y213, ZK[2022] general480]
  2. Innovation Group Project of Guizhou Province [QianKe He KY[2021]018]
  3. Association of Natural Science of Foundation of China [81760758]
  4. Research Center of Molecular Bioactivity from Traditional Chinese Medicine and Ethnomedicine [3411-4110000520364]
  5. Shenzhen Fund for Guangdong Provincial High-level Clinical Key Specialties [SZXK059]
  6. Bright Future Fund for Guangdong Provincial Hospital Pharmacology Research [2023A13]

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This study evaluated the antiviral activity of four Potentilla kleiniana extracts and seven compounds against HIV-1 protease, and found that they exhibited inhibitory effects on the enzyme.
Potentilla kleiniana Wight et Arn(PK, 'Wu Pi Feng' in Chinese? was recorded as Miao ethnic medicine for treatment of fever, cough, ulcer, and erysipelas for thousands years. This study aimed to evaluate the antiviral activity of four PK extracts and seven compounds by using HIV-1 protease (HIV-1 PR). In addition, Ultra-High Performance Liquid Chromatography and High Resolution Mass Spectrometry (UPLC-HRMS) was employed to identify the bioactive components. The toxicity assessment of the extracts was done before antiviral screening using a highly specific human aspartyl protease, renin protease by fluorimetric method. As a result, seven compounds and four extracts of PK inhibited HIV-1 PR with IC50 range from 0.009 to 0.36 mg/mL, and did not appreciably inhibit the general human protease renin. This study first demonstrated that four PK extracts, ellagic acid and ursolic acid potent inhibit HIV-1 protease, could be used as an efficacious drug candidate to treat SARS-CoV-2 infection.

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