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Information × Registration Number 2122U000982, Article popup.category Стаття Title popup.author popup.publication 01-01-2022 popup.source_user Інституційний репозитарій (електронний архів) Київського національного університету імені Тараса Шевченка popup.source https://ir.library.knu.ua/handle/15071834/5141 popup.publisher Elsevier BV Description An in vivo study of a photoswitchable cytotoxic peptide LMB040 has been undertaken on a chemically induced hepatocellular carcinoma model in immunocompetent rats. We analysed the pharmacokinetic profile of the less toxic photoform (“ring-closed” dithienylethene) of the compound in tumors, plasma, and healthy liver. Accordingly, the peptide can reach a tumor concentration sufficiently high to exert a cytotoxic effect upon photoconversion into the more active (“ring-open”) photoform. Tissue morphology, histology, redox state of the liver, and hepatic biochemical parameters in blood serum were analysed upon treatment with (i) the less active photoform, (ii) the in vivo light-activated alternative photoform, and (iii) compared with a reference chemotherapeutic 5-fluorouracil. We found that application of the less toxic form followed by a delayed in vivo photoconversion into the more toxic ring-open form of LMB040 led to a higher overall survival of the animals, and signs of enhanced immune response were observed compared to the untreated animals. popup.nrat_date 2024-12-09 Close