A negative impact of radicals on human’s health is responsible for growing research interest in antioxidant properties of substances, which protect organisms from the damaging influence of these reactive species. Angiotensin-converting enzyme inhibitors (ACE-I) are the most popular drugs used in cardiovascular diseases. There are a lot of clinical reports that ACE-I have antioxidant properties, due to the fact, that prolonged use improves conditions of patients with neurodegenerative disorders and slow inflammatory processes. The paper shows the antioxidant properties of a selected ACE-I: cilazapril, ramipril, imidapril, lisinopril, perindopril, and quinapril. Among numerous methods for antioxidant activity estimation, DPPH reduction is the most popular and commonly used one due to its ease, speed, sensitivity and the usage of stable radicals. UV-Vis spectrophotometry was used to examine interactions of chosen ACE-I with model-free radicals. Absorption of UV-Vis spectra of DPPH (reference), and DPPH interacting with the tested ACE-I were compared. For all tested ACE-I kinetics of their interaction with DPPH, up to 30 minutes, were obtained. The strongest interaction with DPPH was observed for imidapril and cilazapril and the lowest interaction for lisinopril. Studies have shown usefulness UV-Vis spectrophotometry for obtaining information on interactions of ACE-I with model-free radicals.
Salicylic acid heated at different temperatures and times was examined by an X-band (9.3 GHz) EPR spectroscopy, UV-Vis spectrophotometry, TGA and colorimetry test to optimize its thermal sterilization process. Free radical formation (~1018 spin/g) during thermal sterilization of salicylic acid according to the pharmaceutical norms at temperature 120oC and time of 120 minutes was compared with those for heating at the new tested temperatures and times: 130oC and 60 minutes, and 140oC and 30 minutes. It was obtained that the relatively lower free radical concentrations characterized salicylic acid heated at temperatures (times): 120oC (120 minutes), and 130oC (60 minutes), than at temperature (time) 140oC (30 minutes). So treatment at temperature 120oC during 120 minutes, and temperature 130oC during 60 minutes, were recommended as the optimal for thermal sterilization of salicylic acid. Salicylic acid should not be sterilized at temperature 140oC during 30 minutes, because of the highest free radical formation. Free radical systems of thermally treated salicylic acid revealed complex character. Fast spin-lattice relaxation processes existed in heated salicylic acid. Strong dipolar interactions characterized all the heated salicylic acid samples. EPR spectroscopy, UV-Vis spectrophotometry, thermogravimetry, and color measurement may be helpful besides microbiological analysis to optimize thermal sterilization conditions of salicylic acid.
INTRODUCTION: Fungal lesions are accompanied by inflammation, during which large amounts of free radicals are formed. Antifungal drugs, which have an additional antioxidant effect, could contribute to a faster recovery. An important role in ensuring effective and safe pharmacotherapy of fungal lesions is played by proper drug storage and appro-priate patient actions during treatment. Ultraviolet radiation can generate free radicals in a drug due to photolysis. A drug containing free radicals may cause toxic effects in the body. The aim of the study was to research the antioxidant properties of selected antifungal drugs of azole derivatives. Addi-tionally, the impact of UVC radiation on the tested drugs and their interaction with the DPPH free radical was studied. MATERIAL AND METHODS: The tested azole samples were exposed to 24-hour UVC radiation. The interaction of drug samples with a model DPPH free radical, before and after exposure to UV radiation, was studied. UV-Vis spectroscopy and colourimetry in the CIE Lab colour analysis system were used as the research techniques. RESULTS: Among the initial samples of the tested drugs only ketoconazole interacted with the DPPH free radical, causing its extinction. Exposure to UVC radiation increased the antioxidant properties in ketoconazole and miconazole. The CIE Lab parameters, UV spectra and interaction kinetics of those two drugs with DPPH were different after UVC exposure, which may indicate changes in ketoconazole and miconazole. The highest stability to ultraviolet radiation was shown by fluconazole, whose CIE Lab parameters, UV spectra and interaction with DPPH did not change after exposure of the sample to light radiation. CONCLUSIONS: The research using UV-Vis spectrophotometry and colourimetry enabled the impact of UVC radiation on selected antifungal drugs to be evaluated, including evaluation of their interaction with the model DPPH free radical. It is recommended to protect ketoconazole and miconazole from exposure to light. It is also advisable to protect patients from the sun during pharmacotherapy with these drugs.
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WSTĘP: Zmianom grzybiczym towarzyszy stan zapalny, w trakcie którego wytwarzane są duże ilości wolnych rodników. Leki działające przeciwgrzybiczo, wykazujące dodatkowo działanie antyoksydacyjne, mogłyby się przyczynić do szybszego powrotu do zdrowia. Ważną rolę w zapewnieniu skutecznej i bezpiecznej farmakoterapii zmian grzybiczych odgrywają prawidłowe przechowywanie leku oraz odpowiednie postępowanie pacjenta w trakcie leczenia. Promieniowanie ultrafioletowe może generować wolne rodniki w leku w procesie fotolizy. Lek zawierający wolne rodniki może powodować efekty toksyczne w organizmie. Celem pracy było zbadanie właściwości antyoksydacyjnych wybranych leków przeciwgrzybiczych pochodnych azoli. Dodatkowo sprawdzono wpływ promieniowania UVC (ultraviolet C) na badane leki oraz ich oddziaływanie z modelowym wolnym rodnikiem DPPH (2,2-Diphenyl-1-picrylhydrazyl). MATERIAŁ I METODY: Badane próbki azoli poddano 24-godzinnej ekspozycji na promieniowanie UVC. Zbadano oddziaływanie próbek leków z modelowym wolnym rodnikiem DPPH przed i po naświetlaniu ich promieniowaniem ultrafioletowym. Jako techniki badawcze zastosowano spektroskopię UV-Vis (ultraviolet-visible) oraz kolorymetrię w układzie analizy barwy CIE Lab. WYNIKI: Spośród wyjściowych próbek badanych leków tylko ketokonazol oddziaływał z wolnym rodnikiem DPPH, powodując jego wygaszenie. Ekspozycja na promieniowanie UVC powodowała wzrost właściwości antyoksydacyjnych w ketokonazolu oraz w mikonazolu. Parametry CIE Lab, widma UV oraz kinetyka oddziaływania z DPPH obu leków były odmienne po naświetlaniu promieniowaniem UVC, co może wskazywać na zmiany zachodzące w ketokonazolu i mikonazolu. Największą stabilność na promieniowanie ultrafioletowe wykazywał flukonazol, którego parametry CIE Lab, widma UV oraz oddziaływanie z DPPH nie zmieniły się po naświetlaniu próbki. WNIOSKI: Badania z zastosowaniem spektrofotometrii UV-Vis oraz kolorymetrii pozwoliły na ocenę wpływu promieniowania UVC na wybrane leki przeciwgrzybicze, w tym na ocenę ich oddziaływania z modelowym wolnym rodnikiem DPPH. Zaleca się ochronę ketokonazolu i mikonazolu przed światłem. Wskazana jest również ochrona przed słońcem pacjentów w trakcie farmakoterapii tymi lekami.
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