title: Activity-guided investigation of Carissa carandas (L.) roots for anti-inflammatory constituents.
abstract: The present study was structured to investigate the anti-inflammatory potential of the extracts, fractions and compounds isolated from Carissa carandas (L.) roots. Bioassay guided fractionation of methanol extract based on inhibitory potential towards proinflammatory mediators (TNF-α, IL-1β and nitric oxide (NO)) led to the identification of stigmasterol (1), lupeol (2), oleanolic acid (3), carissone (4) and scopoletin (5) as potential anti-inflammatory agents. Carissone (4) (IC50 = 20.1 ± 2.69 μg/mL) and scopoletin (5) (IC50 = 24.6 ± 1.36 μg/mL) exhibited significant inhibition of NO production comparable to specific NO inhibitor (L-NAME; IC50 = 19.82 ± 1.64 μg/mL) without affecting the cell viability. Also, 4 and 5 at a concentration of 30 μM were found to inhibit 41.88-53.44% of TNF-α and IL-1β. To the best of our knowledge, this is the first report displaying the anti-inflammatory effects of C. carandas (L.) roots, partially mediated by inhibition of TNF-α, IL-1β and NO.
authors.affiliation: a Department of Natural Products , National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S.A.S. Nagar, Mohali 160062 , Punjab , India.
authors.forename: Sindhuja
authors.initials: S
authors.lastname: Galipalli
authors.forename: Neeraj K
authors.initials: NK
authors.lastname: Patel
authors.forename: K
authors.initials: K
authors.lastname: Prasanna
authors.forename: Kamlesh K
authors.initials: KK
authors.lastname: Bhutani
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D029062:Apocynaceae / Q000737:chemistry*; D002460:Cell Line; D006801:Humans; D053583:Interleukin-1beta / Q000037:antagonists & inhibitors; D009569:Nitric Oxide / Q000096:biosynthesis; D009828:Oleanolic Acid / Q000494:pharmacology; D053978:Pentacyclic Triterpenes / Q000494:pharmacology; D010936:Plant Extracts / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry*; D012603:Scopoletin / Q000494:pharmacology; D045787:Sesquiterpenes, Eudesmane / Q000494:pharmacology; D013265:Stigmasterol / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors; D000094042:Lupanes
chemical_list: D000893:Anti-Inflammatory Agents; D053583:Interleukin-1beta; D009569:Nitric Oxide; D009828:Oleanolic Acid; D053978:Pentacyclic Triterpenes; D010936:Plant Extracts; D012603:Scopoletin; D045787:Sesquiterpenes, Eudesmane; D013265:Stigmasterol; D014409:Tumor Necrosis Factor-alpha; C538844:carissone; C010480:lupeol; D000094042:Lupanes
keywords: Carissa carandas; carissone; interleukin-1β; nitric oxide; scopoletin; tumour necrosis factor-α