Captopril (Synonyms: SA 333, SQ 14,225)

Captopril is an inhibitor of Angiotensin-I-converting enzyme (ACE) with IC50 value of 6nM [1].

Captopril is an old drug with antihypertensive efficacy commonly used in the control of blood pressure. Captopril is found to be an ACE inhibitor in all species studied. Administration of captopril inhibits the pressor response to intravenously administered angiotensin I but not that induced by angiotensin II both in normal human beings and in conscious normotensive rabbits. Captopril is proven to be a useful alternative to combination antihypertensive therapy in

the patients with resistant hypertension [2].

Captopril is also found to have anticancer activity. It can significantly reduce tumor growth without toxicity in athymic mice bearing LNM35 human lung cells xenografts. It is proven that captopril affects cell growth through inducing apoptosis [3].

References:
[1] FitzGerald RJ, Meisel H. Milk protein-derived peptide inhibitors of angiotensin-I-converting enzyme. Br J Nutr. 2000 Nov;84
[2] Bravo EL, Tarazi RC. Converting enzyme inhibition with an orally active compound in hypertensive man. Hypertension. 1979 Jan-Feb;1(1):39-46.
[3] Attoub S, Gaben AM, Al-Salam S, Al Sultan MA, John A, Nicholls MG, Mester J, Petroianu G. Captopril as a potential inhibitor of lung tumor growth and metastasis. Ann N Y Acad Sci. 2008 Sep;1138:65-72.