Metodami luminol-dependentní chemiluminiscence byla sledována antioxidační aktivita N-(alkoxyfenyl)-2-(2-oxo-l-aza-l-cykloalkyl) acetamidů zkoumaných pro své potenciálně pozitivní působení na kognitivní funkce, stobadinu a jeho acylderivátů, které tvoří tzv. prodrug formu této látky se zvýšenou lipofilitou. V pokusech in vitro byl sledován vliv na produkci reaktivních kyslíkových metabolitů aktivovanými leukocyty. Dále byla stanovena celková antioxidační aktivita odpovídající schopnosti vychytávat peroxylový radikál a antioxidační aktivita vůči superoxidovému radikálu (generovaném v enzymatickém systému hypoxantin/xantinoxidasa) a hydroxylovému radikálu (generovanému Fentonovou reakcí). Antioxidační aktivita testovaných látek byla ve všech případech porovnána se stobadin dihydrochloridem. Antioxidační aktivita byla ve všech systémech ověřena u stobadinu a stanovena u jeho butyrylderivátu. Cinnamoylstobadin účinně snižoval pouze chemiluminiscenční aktivitu leukocytů. Potenciální zesilovače kognitivních funkcí byly antioxidačně neúčinné.
The luminol-enhanced chemiluminiscence method was used to investigate the antioxidative activity of N-(alkoxyphenyl)-2-(2-oxo-l-aza-l-cykloalkyl) acetamides studied as potential cognitive enhancers and stobadine acylderivatives which form prodrugs with increased lipophilicity. The effect on the production of reactive oxygen metabolites by activated leukocytes was studied in vitro. Furthermore, the total radical-trapping antioxidant parameter was evaluated as the peroxyl radical-trapping capacity and the scavenging effect on the superoxide anion radical (generated by the enzymatic system hypoxanthine/xanthine oxidase) and on the hydroxyl radical (produced in Fenton reaction) were studied. The antioxidative properties of the tested substances were compared with that of stobadine dihydrochloride. Only stobadine and its butyrylderivative have been demonstrated to possess free radical scavenging activity in all systems. Cinnamoylstobadine inhibited only the leukocyte chemiluminiscence activity. The potential cognitive enhancers did not show any antioxidant activity.
- Keywords
- STOBADIN,
- MeSH
- Acetamides MeSH
- Alkylation MeSH
- Antioxidants MeSH
- Indoles MeSH
- Luminescence MeSH
- Pyridinium Compounds MeSH
The purpose of investigation was to study the effect of pesticides from group of pyrethroids (e.g. decis) on the enzymatic function in the homogenate of the mucosal membrane of the proximal and distal segments of the small intestine. Determination of the degree of the activity of hydrolytic enzymes in the homogenates of some parts of the intestine allowed to show effect of pesticide decis on the gradient of distribution of enzymatic activity along the intestine. For characteristic of the enzymatic activity of the small intestine there was performed study of the activity of dipeptidase, amylase, invertase and alkaline phosphatase in the homogenate of the mucosal membrane from proximal and distal parts in multiple effects of pesticide decis in toxic dose (1/20 LD50 ) during 4 months. Changes of the enzymatic activity in acute poisoning were depended on the time of pesticide exposure and site of the bowel. The different digestive enzymes have different response to effect ofpesticidesof pyrethroid group (decis), there are differences in the reactions of proximal and distal part of the small intestine and there is correlation between changes of activity of the majority hydrolases and administered dose of pesticides.
