TY - JOUR
T1 - Inhibition of rat and human prolidases by captopril
AU - Ganapathy, Vadivel
AU - Pashley, Steven J.
AU - August Roesel, R.
AU - Pashley, David H.
AU - Leibach, Frederick H.
N1 - Funding Information:
Acknowledgements--This work was supported, in part, by Grant AM 28389 from the National Institutes of Health. We thank Mr. Paul Blankenship for his technical assistance and Mrs. Ida O. Thomas for her expert secretarial assistance. This is contribution number 0801 from the Department of Cell and Molecular Biology.
PY - 1985/4/15
Y1 - 1985/4/15
N2 - We examined the effects of captopril on prolidase activity of crude homogenates of various tissues in the rat and in the human. It was found that captopril caused significant inhibition of prolidases from liver, kidney, and intestine in both species, whereas it showed minimal inhibitory effect on erythrocyte prolidase. In the rat, Ki for the inhibition of kidney and liver prolidases was in the range of 25-35 μM while, in the human, the value was considerably higher. The nature of inhibition was found to be competitive both in the rat and in the human. Oral administration of captopril (daily dose, 40 mg/kg) for 7 days in the rat resulted in increased urinary excretion of peptide-bound 4-hydroxy-l-proline compared to controls, indicating in vivo inhibition of tissue prolidases by captopril.
AB - We examined the effects of captopril on prolidase activity of crude homogenates of various tissues in the rat and in the human. It was found that captopril caused significant inhibition of prolidases from liver, kidney, and intestine in both species, whereas it showed minimal inhibitory effect on erythrocyte prolidase. In the rat, Ki for the inhibition of kidney and liver prolidases was in the range of 25-35 μM while, in the human, the value was considerably higher. The nature of inhibition was found to be competitive both in the rat and in the human. Oral administration of captopril (daily dose, 40 mg/kg) for 7 days in the rat resulted in increased urinary excretion of peptide-bound 4-hydroxy-l-proline compared to controls, indicating in vivo inhibition of tissue prolidases by captopril.
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U2 - 10.1016/0006-2952(85)90507-6
DO - 10.1016/0006-2952(85)90507-6
M3 - Article
C2 - 3888225
AN - SCOPUS:0021813290
SN - 0006-2952
VL - 34
SP - 1287
EP - 1291
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 8
ER -