Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its Compounds
<i>Phyllanthus amarus</i> Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of <i>P. amarus</i> extract and its compounds. The antialler...
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MDPI AG
2021-01-01
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| Online Access: | https://www.mdpi.com/1420-3049/26/3/695 |
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| author | Nur Zahirah Abd Rani Kok Wai Lam Juriyati Jalil Hazni Falina Mohamad Mohd Shukri Mat Ali Khairana Husain |
| author_facet | Nur Zahirah Abd Rani Kok Wai Lam Juriyati Jalil Hazni Falina Mohamad Mohd Shukri Mat Ali Khairana Husain |
| author_sort | Nur Zahirah Abd Rani |
| collection | DOAJ |
| description | <i>Phyllanthus amarus</i> Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of <i>P. amarus</i> extract and its compounds. The antiallergic activity was determined by measuring the concentration of allergy markers release from rat basophilic leukemia (RBL-2H3) cells with ketotifen fumarate as the positive control. As a result, <i>P. amarus</i> did not stabilize mast cell degranulation but exhibited antihistamine activity. The antihistamine activity was evaluated by conducting a competition radioligand binding assay on the histamine 1 receptor (H1R). Four compounds were identified from the high performance liquid chromatography (HPLC) analysis which were phyllanthin (<b>1</b>), hypophyllanthin (<b>2</b>), niranthin (<b>3</b>), and corilagin (<b>4</b>). To gain insights into the binding interactions of the most active compound hypophyllanthin (<b>2</b>), molecular docking was conducted and found that hypophyllanthin (<b>2</b>) exhibited favorable binding in the H1R binding site. In conclusion, <i>P. amarus</i> and hypophyllanthin (<b>2</b>) could potentially exhibit antiallergic activity by preventing the activation of the H1 receptor. |
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| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T03:21:19Z |
| publishDate | 2021-01-01 |
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| series | Molecules |
| spelling | doaj.art-4b9bf5b0e8df40c3a27d5c6daab32b2c2023-12-03T15:08:44ZengMDPI AGMolecules1420-30492021-01-0126369510.3390/molecules26030695Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its CompoundsNur Zahirah Abd Rani0Kok Wai Lam1Juriyati Jalil2Hazni Falina Mohamad3Mohd Shukri Mat Ali4Khairana Husain5Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, MalaysiaDrug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, MalaysiaDrug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, MalaysiaDrug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, MalaysiaHorticulture Research Centre, Malaysian Agricultural Research and Development Institute (MARDI), P.O. Box 12301, Kuala Lumpur 50774, MalaysiaDrug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, Malaysia<i>Phyllanthus amarus</i> Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of <i>P. amarus</i> extract and its compounds. The antiallergic activity was determined by measuring the concentration of allergy markers release from rat basophilic leukemia (RBL-2H3) cells with ketotifen fumarate as the positive control. As a result, <i>P. amarus</i> did not stabilize mast cell degranulation but exhibited antihistamine activity. The antihistamine activity was evaluated by conducting a competition radioligand binding assay on the histamine 1 receptor (H1R). Four compounds were identified from the high performance liquid chromatography (HPLC) analysis which were phyllanthin (<b>1</b>), hypophyllanthin (<b>2</b>), niranthin (<b>3</b>), and corilagin (<b>4</b>). To gain insights into the binding interactions of the most active compound hypophyllanthin (<b>2</b>), molecular docking was conducted and found that hypophyllanthin (<b>2</b>) exhibited favorable binding in the H1R binding site. In conclusion, <i>P. amarus</i> and hypophyllanthin (<b>2</b>) could potentially exhibit antiallergic activity by preventing the activation of the H1 receptor.https://www.mdpi.com/1420-3049/26/3/695<i>Phyllantus amarus</i>antiallergicRBL-2H3beta-hexosaminidasehistamineradioligand |
| spellingShingle | Nur Zahirah Abd Rani Kok Wai Lam Juriyati Jalil Hazni Falina Mohamad Mohd Shukri Mat Ali Khairana Husain Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its Compounds Molecules <i>Phyllantus amarus</i> antiallergic RBL-2H3 beta-hexosaminidase histamine radioligand |
| title | Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its Compounds |
| title_full | Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its Compounds |
| title_fullStr | Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its Compounds |
| title_full_unstemmed | Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its Compounds |
| title_short | Mechanistic Studies of the Antiallergic Activity of <i>Phyllanthus amarus</i> Schum. & Thonn. and Its Compounds |
| title_sort | mechanistic studies of the antiallergic activity of i phyllanthus amarus i schum thonn and its compounds |
| topic | <i>Phyllantus amarus</i> antiallergic RBL-2H3 beta-hexosaminidase histamine radioligand |
| url | https://www.mdpi.com/1420-3049/26/3/695 |
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