Inhibition of lipid hydroperoxidation of low density lipoprotein by the Ca(2+)-channel and alpha 1-adrenoceptor antagonist monatepil maleate.
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| Abstract |
The antioxidative effect of monatepil maleate (CAS 103379-03-9, AJ-2615), a new antihypertensive agent, was investigated by measuring its ability to inhibit copper-induced lipid hydroperoxidation of low density lipoprotein (LDL) and was compared with those of diltiazem (Ca(2+)-channel antagonist), prazosin (alpha 1-adrenoceptor antagonist), and probucol. The concentration of AJ-2615 required to inhibit copper-induced lipid hydroperoxidation of LDL by 50% (IC50) was 28 mumol/l. The IC50 values for diltiazem, prazosin, and probucol were > 1 mmol/l, > 1 mmol/l, and 17 mumol/l, respectively. These results indicate that AJ-2615 has the same potent antioxidative effect as probucol and suggest that a previously reported ability of AJ-2615 to inhibit the progression of atherosclerosis may be due to this antioxidative property. In addition, the dihydrodibenzothiepine ring of AJ-2615 may have an antioxidative functions.
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| Authors | K Hayashi, Y Kuga, S Nomura, Y Okura, K Tanaka, Y Yasunobu, K Nomura, T Shingu, J Kuwashima, G Kajiyama |
| Journal | Arzneimittel-Forschung (Arzneimittelforschung) Vol. 46 Issue 4 Pg. 378-81 (Apr 1996) ISSN: 0004-4172 [Print] Germany |
| PMID | 8740082 (Publication Type: Journal Article) |
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