Urease and serine protease inhibitory alkaloids from Isatis tinctoria.
Phytochemical investigations on the alkaloidal fraction of the whole plant of the Isatis tinctoria led to the isolation of the alkaloids 1-6., 3'-Hydroxyepiglucoisatisin (3), Epiglucoisatisin (2) were found to be potent urease inhibitors in a concentration-dependent manner with IC(50) values 25.63 +/- 0.74, 37.01 +/- 0.41 and 31.72 +/- 0.93, 47.33 +/- 0.31 microM against Bacillus pasteurii & Jack bean urease, respectively. Compounds 3 and 2 also showed potent inhibitory potential against alpha-chymotrypsin with IC(50) values of 23.40 +/- 0.21 and 27.45 +/- 0.23 microM, respectively.
Ahmad
Ijaz
I
Departemnt of Chemistry, Kohat University of Science and Technology, Kohat, N.W.F.P, , Pakistan. drijaz_chem@yahoo.com
Fatima
Itrat
I
Afza
Nighat
N
Malik
Abdul
A
Lodhi
Muhammad Arif
MA
Choudhary
Muhammad Iqbal
MI
D000470:Alkaloids / Q000737:chemistry* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D031219:Isatis / Q000737:chemistry*; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D012697:Serine Endopeptidases / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014510:Urease / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000470:Alkaloids; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D012697:Serine Endopeptidases; D014510:Urease