title: Inhibition of NO production by highly-oxygenated diterpenes of Orthosiphon stamineus and their structure-activity relationship.
abstract: Nitric oxide (NO) has been implemented in various pathological processes. In the present study, 47 highly-oxygenated isopimarane-type and novel carbon framework staminane-type diterpenes isolated from Orthosiphon stamineus of Indonesia, Okinawa, Myanmar and Vietnam were evaluated for their inhibitory activity in NO production by lipopolysaccharide (LPS)-activated macrophage-like J774.1 cells. All the isolated diterpenes showed concentration-dependent inhibition of NO production in LPS-activated macrophage-like J774.1 cells, and based on the results, their structure-activity relationship were established.
authors.affiliation: Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Japan.
authors.forename: Suresh
authors.initials: S
authors.lastname: Awale
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Tezuka
authors.forename: Arjun H
authors.initials: AH
authors.lastname: Banskota
authors.forename: Shigetoshi
authors.initials: S
authors.lastname: Kadota
mesh_terms: D000818:Animals; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis*; D031342:Orthosiphon; D010100:Oxygen / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004224:Diterpenes; D009569:Nitric Oxide; D010100:Oxygen