title: Tyrosinase inhibition studies of cycloartane and cucurbitane glycosides and their structure-activity relationships.
abstract: In the present paper, tyrosinase inhibition studies and structure-activity relationship of eight cycloartane glycosides and one cucurbitane glycoside and its genin, which were isolated from Astragalus (Leguminoseae) and Bryonia (Cucurbitaceae) plants, have been discussed. The activities are compared with two reference tyrosinase inhibitors, kojic acid and l-mimosine. These studies and the SAR showed that the askendoside B which exhibited highly potent (IC50 =13.95 microM) tyrosinase inhibition could be a possible lead molecule for the development of new medications of several skin diseases related with the over-expression of the enzyme tyrosinase, like hyperpigmentation. The molecule also may be interesting for the cosmetic industries as a skin whitening agent.
authors.affiliation: Pharmacology Research Laboratory, Faculty of Pharmaceutical Sciences, University of Science and Technology, Chittagong, Bangladesh. mahmud.khan@fagme.duit.no
authors.forename: Mahmud Tareq Hassan
authors.initials: MT
authors.lastname: Khan
authors.forename: M Iqbal
authors.initials: MI
authors.lastname: Choudhary
authors.lastname: Atta-ur-Rahman
authors.forename: Reyhan P
authors.initials: RP
authors.lastname: Mamedova
authors.forename: Manzura A
authors.initials: MA
authors.lastname: Agzamova
authors.forename: Mukhlis N
authors.initials: MN
authors.lastname: Sultankhodzhaev
authors.forename: Mahamed I
authors.initials: MI
authors.lastname: Isaev
mesh_terms: D027883:Astragalus Plant / Q000737:chemistry; D019662:Cucurbitaceae / Q000737:chemistry; D006027:Glycosides / Q000737:chemistry* / Q000378:metabolism; D008898:Mimosine / Q000737:chemistry / Q000378:metabolism; D015394:Molecular Structure; D014442:Monophenol Monooxygenase / Q000378:metabolism*; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism; D011753:Pyrones / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D006027:Glycosides; D010455:Peptides; D011753:Pyrones; D014315:Triterpenes; C514277:cucurbitane; D008898:Mimosine; C085352:cycloartane; C011890:kojic acid; D014442:Monophenol Monooxygenase