Study of the green tea polyphenols catechin-3-gallate (CG) and epicatechin-3-gallate (ECG) as proteasome inhibitors.
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.
Wan
Sheng Biao
SB
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.
Chen
Di
D
Dou
Q Ping
QP
Chan
Tak Hang
TH
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*
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