A serine protease inhibitor from hemolymph of green mussel, Perna viridis.
Bioactivity guided fractions of cell-free hemolymph of bacterially challenged marine mussel, Perna viridis led to the isolation of a novel quaternary alkaloid 1, which was identified by its spectral data. The isolated molecule 1 has been found to be a potent serine protease inhibitor (SPI) showing IC(50) and K(i) values of 102.5 and 97.1-104.68 microM, respectively. The E(t)/K(i) value of SPI is 6.3, whereas E(t)/K(m) value is 1.04. The Van't Hoff analysis showed that the value of K(i) decreases with increase in temperature, and the binding of the inhibitor is entropically driven.
Khan
M S
MS
Division of Biochemical Science, National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411 008, India.
Goswami
U
U
Rojatkar
S R
SR
Khan
M I
MI
D000470:Alkaloids / Q000737:chemistry; D000818:Animals; D001682:Biological Availability; D002474:Cell-Free System; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006458:Hemolymph / Q000378:metabolism*; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D049883:Perna; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013696:Temperature; D013816:Thermodynamics; D014357:Trypsin / Q000737:chemistry
D000470:Alkaloids; D015842:Serine Proteinase Inhibitors; D014357:Trypsin