title: Study of the green tea polyphenols catechin-3-gallate (CG) and epicatechin-3-gallate (ECG) as proteasome inhibitors.
abstract: The green tea polyphenol catechin-3-gallate (CG) and epicatechin-3-gallate (ECG) were synthesized enantioselectively via a Sharpless hydroxylation reaction followed by a diastereoselective cyclization. Their potencies to inhibit the proteasome activity were measured. The unnatural enantiomers were found to be equally potent to the natural compounds.
authors.affiliation: Department of Applied Biology and Chemical Technology and the Open Laboratory of Chirotechnology, Institute of Molecular Technology for Drug Discovery and Synthesis, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, SAR, China.
authors.forename: Sheng Biao
authors.initials: SB
authors.lastname: Wan
authors.forename: Di
authors.initials: D
authors.lastname: Chen
authors.forename: Q Ping
authors.initials: QP
authors.lastname: Dou
authors.forename: Tak Hang
authors.initials: TH
authors.lastname: Chan
mesh_terms: D002392:Catechin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D019169:Jurkat Cells; D015394:Molecular Structure; D010636:Phenols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D059808:Polyphenols; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D061988:Proteasome Inhibitors; D013237:Stereoisomerism; D013662:Tea / Q000737:chemistry*
chemical_list: D015853:Cysteine Proteinase Inhibitors; D005419:Flavonoids; D010636:Phenols; D059808:Polyphenols; D061988:Proteasome Inhibitors; D013662:Tea; C417939:catechin gallate; D002392:Catechin; C062669:epicatechin gallate; D046988:Proteasome Endopeptidase Complex