In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) Benth
<i>Micromeria biflora</i>, a traditional medicinal plant, is extensively used for treating various painful conditions, such as nose bleeds, wounds, and sinusitis. A phytochemical investigation of the chloroform fraction of <i>Micromeria biflora</i> led to the isolation of sal...
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MDPI AG
2022-05-01
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| author | Abdullah S. M. Aljohani Fahad A. Alhumaydhi Abdur Rauf Essam M. Hamad Umer Rashid |
| author_facet | Abdullah S. M. Aljohani Fahad A. Alhumaydhi Abdur Rauf Essam M. Hamad Umer Rashid |
| author_sort | Abdullah S. M. Aljohani |
| collection | DOAJ |
| description | <i>Micromeria biflora</i>, a traditional medicinal plant, is extensively used for treating various painful conditions, such as nose bleeds, wounds, and sinusitis. A phytochemical investigation of the chloroform fraction of <i>Micromeria biflora</i> led to the isolation of salicylalazine. Salicylalazine was assessed in vivo for analgesia, muscle relaxation, sedative, and anti-inflammatory properties, as well as in vitro for COX-1/2 inhibition activities. It was assessed against a hot plate-induced model at different doses. The muscle relaxant potential of salicylalazine was evaluated in traction and inclined screening models, while sedative properties were determined using an open-field model. The anti-inflammatory potential of salicylalazine was assessed in histamine and carrageenan-induced paw edema screening models. Salicylalazine exhibited significant analgesic potential in a dose-dependent manner. In both screening models, an excellent time-dependent muscle-relaxation effect was observed. Salicylalazine demonstrated excellent sedation at high doses. Its anti-inflammatory activity was determined through the initial and late phases of edema. It exhibited anticancer potential against NCI-H226, HepG2, A498, and MDR2780AD cell lines. In vitro, salicylalazine showed preferential COX-2 inhibition (over COX-1) with an SI value of 4.85. It was less effective in the initial phase, while, in the later phase, it demonstrated significant effects at 15 and 20 mg/kg doses compared with the negative control. Salicylalazine did not exhibit cytotoxicity in the MTT assay, preliminarily indicating its safety. |
| first_indexed | 2024-03-10T01:05:50Z |
| format | Article |
| id | doaj.art-ccf9c851b1934358933ace566b76054f |
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| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T01:05:50Z |
| publishDate | 2022-05-01 |
| publisher | MDPI AG |
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| series | Molecules |
| spelling | doaj.art-ccf9c851b1934358933ace566b76054f2023-11-23T14:27:43ZengMDPI AGMolecules1420-30492022-05-012711337710.3390/molecules27113377In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) BenthAbdullah S. M. Aljohani0Fahad A. Alhumaydhi1Abdur Rauf2Essam M. Hamad3Umer Rashid4Department of Veterinary Medicine, College of Agriculture and Veterinary Medicine, Qassim University, Buraydah 52571, Saudi ArabiaDepartment of Medical Laboratories, College of Applied Medical Sciences, Qassim University, Buraydah 52571, Saudi ArabiaDepartment of Chemistry, University of Swabi, Anbar 23561, PakistanDepartment of Food Science and Human Nutrition, College of Agriculture and Veterinary Medicine, Qassim University, Buraydah 52571, Saudi ArabiaDepartment of Chemistry, COMSATS University Islamabad, Abbottabad 22060, Pakistan<i>Micromeria biflora</i>, a traditional medicinal plant, is extensively used for treating various painful conditions, such as nose bleeds, wounds, and sinusitis. A phytochemical investigation of the chloroform fraction of <i>Micromeria biflora</i> led to the isolation of salicylalazine. Salicylalazine was assessed in vivo for analgesia, muscle relaxation, sedative, and anti-inflammatory properties, as well as in vitro for COX-1/2 inhibition activities. It was assessed against a hot plate-induced model at different doses. The muscle relaxant potential of salicylalazine was evaluated in traction and inclined screening models, while sedative properties were determined using an open-field model. The anti-inflammatory potential of salicylalazine was assessed in histamine and carrageenan-induced paw edema screening models. Salicylalazine exhibited significant analgesic potential in a dose-dependent manner. In both screening models, an excellent time-dependent muscle-relaxation effect was observed. Salicylalazine demonstrated excellent sedation at high doses. Its anti-inflammatory activity was determined through the initial and late phases of edema. It exhibited anticancer potential against NCI-H226, HepG2, A498, and MDR2780AD cell lines. In vitro, salicylalazine showed preferential COX-2 inhibition (over COX-1) with an SI value of 4.85. It was less effective in the initial phase, while, in the later phase, it demonstrated significant effects at 15 and 20 mg/kg doses compared with the negative control. Salicylalazine did not exhibit cytotoxicity in the MTT assay, preliminarily indicating its safety.https://www.mdpi.com/1420-3049/27/11/3377<i>Micromeria biflora</i>anti-inflammatoryanalgesicmuscle relaxantsedativeanti-inflammatory |
| spellingShingle | Abdullah S. M. Aljohani Fahad A. Alhumaydhi Abdur Rauf Essam M. Hamad Umer Rashid In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) Benth Molecules <i>Micromeria biflora</i> anti-inflammatory analgesic muscle relaxant sedative anti-inflammatory |
| title | In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) Benth |
| title_full | In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) Benth |
| title_fullStr | In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) Benth |
| title_full_unstemmed | In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) Benth |
| title_short | In Vivo and In Vitro Biological Evaluation and Molecular Docking Studies of Compounds Isolated from <i>Micromeria biflora</i> (Buch. Ham. ex D.Don) Benth |
| title_sort | in vivo and in vitro biological evaluation and molecular docking studies of compounds isolated from i micromeria biflora i buch ham ex d don benth |
| topic | <i>Micromeria biflora</i> anti-inflammatory analgesic muscle relaxant sedative anti-inflammatory |
| url | https://www.mdpi.com/1420-3049/27/11/3377 |
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