Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i>
<i>Hypericum kouytchense</i> Lévl 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 compo...
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| Format: | Article |
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MDPI AG
2022-11-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/12/1499 |
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| author | Bo Wen Pan Jun Wei Xiao Su Mei Li Xin Yang Xia Zhou Qing Wen Sun Mei Chen Shou Xia Xie Meena Kishore Sakharkar Jian Yang Ying Zhou Ying Wei |
| author_facet | Bo Wen Pan Jun Wei Xiao Su Mei Li Xin Yang Xia Zhou Qing Wen Sun Mei Chen Shou Xia Xie Meena Kishore Sakharkar Jian Yang Ying Zhou Ying Wei |
| author_sort | Bo Wen Pan |
| collection | DOAJ |
| description | <i>Hypericum kouytchense</i> Lévl 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 <i>H. kouytchens</i>. In this study, we evaluated the antiviral activities of different extracts from the insect gall of <i>H. kouytchen</i> 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 <i>H. kouytchense</i> insect gall exhibited antiviral activities with IC<sub>50</sub> values of 10.0, 4.0, 3.2 and 17.0 µg/mL against HIV-1 protease; 210.0, 34.0, 24.0 and 30.0 µg/mL against cathepsin L protease; and 180.0, 65.0, 44.0 and 39.0 µg/mL against human renin, respectively. Ten compounds were identified and quantified in the <i>H. kouytchense</i> insect gall extracts. Epicatechin, eriodictyol and naringenin chalcone were major ingredients in the extracts with contents ranging from 3.9 to 479.2 µg/mg. For HIV-1 protease, seven compounds showed more than 65% inhibition at a concentration of 1000.0 µg/mL, especially for hypericin and naringenin chalcone with IC<sub>50</sub> values of 1.8 and 33.0 µg/mL, respectively. However, only hypericin was active against cathepsin L protease with an IC<sub>50</sub> value of 17100.0 µg/mL, and its contents were from 0.99 to 11.65 µg/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. |
| first_indexed | 2024-03-09T15:58:57Z |
| format | Article |
| id | doaj.art-036898305f604fb2a95f3387916ef39b |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T15:58:57Z |
| publishDate | 2022-11-01 |
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| series | Pharmaceuticals |
| spelling | doaj.art-036898305f604fb2a95f3387916ef39b2023-11-24T17:16:14ZengMDPI AGPharmaceuticals1424-82472022-11-011512149910.3390/ph15121499Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i>Bo Wen Pan0Jun Wei Xiao1Su Mei Li2Xin Yang3Xia Zhou4Qing Wen Sun5Mei Chen6Shou Xia Xie7Meena Kishore Sakharkar8Jian Yang9Ying Zhou10Ying Wei11College of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, ChinaCollege of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, ChinaDepartment of Pharmacology, Shenzhen People’s Hospital (The Second Clinical Medical College, Jinan University, The First Affiliated Hospital, Southern University of Science and Technology), Shenzhen 518020, ChinaCollege of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, ChinaCollege of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, ChinaCollege of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, ChinaCollege of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, ChinaDepartment of Pharmacology, Shenzhen People’s Hospital (The Second Clinical Medical College, Jinan University, The First Affiliated Hospital, Southern University of Science and Technology), Shenzhen 518020, ChinaCollege of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, SK S7N 5E5, CanadaCollege of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, SK S7N 5E5, CanadaCollege of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, ChinaCollege of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, China<i>Hypericum kouytchense</i> Lévl 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 <i>H. kouytchens</i>. In this study, we evaluated the antiviral activities of different extracts from the insect gall of <i>H. kouytchen</i> 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 <i>H. kouytchense</i> insect gall exhibited antiviral activities with IC<sub>50</sub> values of 10.0, 4.0, 3.2 and 17.0 µg/mL against HIV-1 protease; 210.0, 34.0, 24.0 and 30.0 µg/mL against cathepsin L protease; and 180.0, 65.0, 44.0 and 39.0 µg/mL against human renin, respectively. Ten compounds were identified and quantified in the <i>H. kouytchense</i> insect gall extracts. Epicatechin, eriodictyol and naringenin chalcone were major ingredients in the extracts with contents ranging from 3.9 to 479.2 µg/mg. For HIV-1 protease, seven compounds showed more than 65% inhibition at a concentration of 1000.0 µg/mL, especially for hypericin and naringenin chalcone with IC<sub>50</sub> values of 1.8 and 33.0 µg/mL, respectively. However, only hypericin was active against cathepsin L protease with an IC<sub>50</sub> value of 17100.0 µg/mL, and its contents were from 0.99 to 11.65 µg/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.https://www.mdpi.com/1424-8247/15/12/1499<i>Hypericum kouytchense</i>active ingredientUPLC–HRMSHIV-1 proteasecathepsin L proteasemolecular docking |
| spellingShingle | Bo Wen Pan Jun Wei Xiao Su Mei Li Xin Yang Xia Zhou Qing Wen Sun Mei Chen Shou Xia Xie Meena Kishore Sakharkar Jian Yang Ying Zhou Ying Wei Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i> Pharmaceuticals <i>Hypericum kouytchense</i> active ingredient UPLC–HRMS HIV-1 protease cathepsin L protease molecular docking |
| title | Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i> |
| title_full | Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i> |
| title_fullStr | Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i> |
| title_full_unstemmed | Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i> |
| title_short | Inhibitors of HIV-1 and Cathepsin L Proteases Identified from the Insect Gall of <i>Hypericum kouytchense</i> |
| title_sort | inhibitors of hiv 1 and cathepsin l proteases identified from the insect gall of i hypericum kouytchense i |
| topic | <i>Hypericum kouytchense</i> active ingredient UPLC–HRMS HIV-1 protease cathepsin L protease molecular docking |
| url | https://www.mdpi.com/1424-8247/15/12/1499 |
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