title: Anti-inflammatory and immunomodulatory flavones from Actinocarya tibetica Benth.
abstract: Herein, we report the isolation and immunomodulatory activity of 11 phytoconstituents, viz. 7 flavonoids, 3 pentacyclic triterpenes and 1 phytosterol of an unexplored plant Actinocarya tibetica Benth. Three flavones, 5-methoxy-6,7-methylenedioxyflavone (6), mosloflavone (7) and negletein (8), showed promising anti-inflammatory activity via inhibition of TNF-α and IL-1β with IC50 values of 0.22, 0.71, 16.4 μM and 10.8, 7.8, 6.4 μM, respectively. These flavones also showed dose-dependent inhibition of TNF-α, IL-1β and iNOS levels in the supernatant of mouse macrophage cell line J774A. Molecular modelling studies revealed orientation and interactions of flavones 6-8 in the active site of TNF-α. These flavones can be used as a starting point to discover lead structures for treatment of inflammatory and immunomodulatory diseases.
authors.affiliation: a Natural Product Chemistry Division, Indian Institute of Integrative Medicine (CSIR) , Canal Road, Jammu , 180001 , India.
authors.forename: Baljinder
authors.initials: B
authors.lastname: Singh
authors.forename: Tabasum
authors.initials: T
authors.lastname: Sidiq
authors.forename: Prashant
authors.initials: P
authors.lastname: Joshi
authors.forename: Shreyans K
authors.initials: SK
authors.lastname: Jain
authors.forename: Yogesh
authors.initials: Y
authors.lastname: Lawaniya
authors.forename: Surinder
authors.initials: S
authors.lastname: Kichlu
authors.forename: Anamika
authors.initials: A
authors.lastname: Khajuria
authors.forename: Ram A
authors.initials: RA
authors.lastname: Vishwakarma
authors.forename: Sandip B
authors.initials: SB
authors.lastname: Bharate
mesh_terms: D000276:Adjuvants, Immunologic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D028082:Boraginaceae / Q000737:chemistry*; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D053583:Interleukin-1beta / Q000037:antagonists & inhibitors; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors
chemical_list: D000276:Adjuvants, Immunologic; D000893:Anti-Inflammatory Agents; D053583:Interleukin-1beta; D014409:Tumor Necrosis Factor-alpha; D052247:Nitric Oxide Synthase Type II