title: Synthesis and antimicrobial evaluation of pogostone and its analogues.
abstract: Pogostone (PO) is one of the secondary metabolites from Pogostemon cablin (Blanco) Benth. (Lamiaceae), serving as the effective component of the antimicrobial activity. In this study, PO and a series of its analogues were synthesized by the reaction of dehydroacetate and aldehydes in tetrahydrofuran under a nitrogen atmosphere. Their activities against Candida albicans, Gram positive bacteria and Gram negative bacteria were evaluated. The antifungal results demonstrated that PO (MIC ranged from 12 to 97μg/mL against all strains, MFC ranged from 49 to 97μg/mL against all strains) and A3 (MIC ranged from 12 to 49, MFC over 195μg/mL) showed a strong activity against Candida albicans. While A1 (MIC ranged from 49 to 97μg/mL) and A2 (MIC ranged from 24 to 49μg/mL) have only shown effect against Guangzhou clinical isolates, the antibacterial results demonstrated that PO and its analogues showed no effects against the tested bacteria strains. This study suggests that pogostone analogues, with the appropriated structure modification, represented a kind of promising antifungal agents.
authors.affiliation: College of Chinese Medicines, Guangzhou University of Chinese Medicine, Guangzhou, PR China.
authors.forename: Yu-Yang
authors.initials: YY
authors.lastname: Yi
authors.forename: Jing-Jin
authors.initials: JJ
authors.lastname: He
authors.forename: Jun-Quan
authors.initials: JQ
authors.lastname: Su
authors.forename: Song-Zhi
authors.initials: SZ
authors.lastname: Kong
authors.forename: Ji-Yan
authors.initials: JY
authors.lastname: Su
authors.forename: Yu-Cui
authors.initials: YC
authors.lastname: Li
authors.forename: Si-Han
authors.initials: SH
authors.lastname: Huang
authors.forename: Chu-Wen
authors.initials: CW
authors.lastname: Li
authors.forename: Xiao-Ping
authors.initials: XP
authors.lastname: Lai
authors.forename: Zi-Ren
authors.initials: ZR
authors.lastname: Su
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D019686:Lamiaceae / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009822:Oils, Volatile / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D009822:Oils, Volatile; C483658:Pogostone