Green tea polyphenols as inhibitors of ribonuclease A.
Ribonucleases (RNases), which are essential for cleavage of RNA, may be cytotoxic due to undesired cleavage of RNA in the cell. The quest for small molecule inhibitors of members of the ribonuclease superfamily has become indispensable with a growing number exhibiting unusual biological properties. Thus, inhibitors of RNases may serve as potential drug candidates. Green tea catechins (GTC), particularly its major constituent (-)-epigallocatechin-3-gallate (EGCG), have reported potential against cell proliferation and angiogenesis induced by several growth factors including angiogenin, a member of the RNase superfamily. This study reports the inhibition of bovine pancreatic ribonuclease A (RNase A) by EGCG and GTC. This has been checked qualitatively by an agarose gel based assay. Enzyme kinetic studies with cytidine 2',3' cyclic monophosphate as the substrate have also been conducted. Results indicate substantial inhibitory activity of a noncompetitive nature with an inhibition constant of approximately 80 microM for EGCG and approximately 100 microM for GTC measured in gallic acid equivalents.
Ghosh
Kalyan Sundar
KS
Department of Chemistry, Indian Institute of Technology, Kharagpur 721302, India.
Maiti
Tushar Kanti
TK
Dasgupta
Swagata
S
D004587:Electrophoresis, Agar Gel; D004789:Enzyme Activation; D004791:Enzyme Inhibitors / Q000737:chemistry; D005419:Flavonoids / Q000737:chemistry*; D007700:Kinetics; D010636:Phenols / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry*; D018515:Plant Leaves / Q000737:chemistry*; D059808:Polyphenols; D012259:Ribonuclease, Pancreatic / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013662:Tea / Q000737:chemistry*
D004791:Enzyme Inhibitors; D005419:Flavonoids; D010636:Phenols; D010936:Plant Extracts; D059808:Polyphenols; D013662:Tea; D012259:Ribonuclease, Pancreatic