Semotiadil, a new calcium antagonist, is a very potent inhibitor of LDL-oxidation.
The influence of semotiadil, a novel benzothiazine calcium antagonist on in-vitro copper-, 2,2àzo-bis-(2,4 dimethylvaleronitrile)[AMVN]-, and 2,2àzo-bis-(2-amidinopropane) [AAPH]-induced low-density lipoprotein (LDL) oxidation was assessed. The following parameters were measured: lag-time of oxidation, maximal rate of oxidation, dienes formed through continuous monitoring of developing conjugated dienes, thiobarbituric acid reactive substances, isoprostane(8-iso-PGF2alpha)-generation and relative electrophoretic mobility. The effect was compared with nifedipine, amlodipine and diltiazem. Besides the influence on isoprostane (8-iso-PGF2alpha)-generation where nifedipine was equipotent with semotiadil at 10(-3) M, semotiadil demonstrated a strong and significant effect in attenuating the indicated indices of LDL-oxidation, in particular, dose-dependently (10(-3) M to 10(-7) M). These results indicate that semotiadil may have the strongest antioxidant activity on LDL among the calcium antagonists examined.
Kritz
H
H
Rehabilitation Center Engelsbad, Baden.
Oguogho
A
A
Aghajanian
A A
AA
Sinzinger
H
H
D000328:Adult; D000578:Amidines / Q000378:metabolism; D001391:Azo Compounds / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D003300:Copper / Q000378:metabolism; D015237:Dinoprost / Q000031:analogs & derivatives / Q000096:biosynthesis; D028441:F2-Isoprostanes; D006801:Humans; D008077:Lipoproteins, LDL / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D009570:Nitriles / Q000378:metabolism; D016877:Oxidants / Q000378:metabolism; D010084:Oxidation-Reduction; D013844:Thiazoles / Q000494:pharmacology*; D017392:Thiobarbituric Acid Reactive Substances / Q000378:metabolism
D000578:Amidines; D001391:Azo Compounds; D002121:Calcium Channel Blockers; D028441:F2-Isoprostanes; D008077:Lipoproteins, LDL; D009570:Nitriles; D016877:Oxidants; D013844:Thiazoles; D017392:Thiobarbituric Acid Reactive Substances; C099252:oxidized low density lipoprotein; C055792:2,2'-azobis(2,4-dimethylvaleronitrile); C075750:8-epi-prostaglandin F2alpha; C046728:2,2'-azobis(2-amidinopropane); D003300:Copper; D015237:Dinoprost; C064356:sesamodil