title: Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.
abstract: Allicin and derivatives thereof inhibit the CAC1 cysteine proteases falcipain 2, rhodesain, cathepsin B and L in the low micromolar range. The structure-activity relationship revealed that only derivatives with primary carbon atom in vicinity to the thiosulfinate sulfur atom attacked by the active-site Cys residue are active against the target enzymes. Some compounds also show potent antiparasitic activity against Plasmodium falciparum and Trypanosoma brucei brucei.
authors.affiliation: Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
authors.forename: Thilo
authors.initials: T
authors.lastname: Waag
authors.forename: Christoph
authors.initials: C
authors.lastname: Gelhaus
authors.forename: Jennifer
authors.initials: J
authors.lastname: Rath
authors.forename: August
authors.initials: A
authors.lastname: Stich
authors.forename: Matthias
authors.initials: M
authors.lastname: Leippe
authors.forename: Tanja
authors.initials: T
authors.lastname: Schirmeister
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents / Q000737:chemistry* / Q000494:pharmacology*; D003546:Cysteine Endopeptidases / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D004220:Disulfides; D005737:Garlic / Q000737:chemistry; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology*; D013441:Sulfinic Acids / Q000737:chemistry* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects / Q000201:enzymology*; D014353:Trypanosomiasis, African / Q000188:drug therapy
chemical_list: D000977:Antiparasitic Agents; D015853:Cysteine Proteinase Inhibitors; D004220:Disulfides; D013441:Sulfinic Acids; C006452:allicin; D003546:Cysteine Endopeptidases