7 research outputs found

    Hyperglycemia is associated with lower levels of urokinase-type plasminogen activator and urokinase-type plasminogen activator receptor in wound fluid

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    Aims: Wounds in patients with hyperglycemia show impaired healing. Plasminogen activation is crucial in several overlapping phases of wound healing process. In this study, we aimed i) to compare acute wound fluid in patients with hyperglycemia and normoglycemia, ii) to focus on the elements of plasminogen activation in the wound fluid, and iii) to determine if the acute wound fluid characteristics are associated with surgical site infections

    Investigation of Gold Nanoparticle Naproxen-Derived Conjugations in Ovarian Cancer

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    Ovarian cancer, which is one of the most diagnosed cancertypesamong women, maintains its significance as a global health problem.Several drug candidates have been investigated for the potential treatmentof ovarian cancer. Nonsteroidal anti-inflammatory drugs (NSAIDs) demonstratedanti-cancer activity through the inhibition of cyclooxygenase 2 (COX-2)and by inhibiting COX-2-dependent prostaglandin (PG) production. Naproxenis one of the most used NSAIDs and Naproxen-derived compounds (NDCs)may show potential treatment effects on cancer as chemotherapeuticdrugs. Although there are successful drug development studies, thelack of solubility of these drug candidates in aqueous media resultsin limited bioavailability and high variability of patient responsesduring treatment. Low aqueous solubility is one of the main problemsin the pharmaceutical industry in terms of drug development. Nanotechnology-basedstrategies provide solutions to hydrophobic drug limitations by increasingdispersion and improving internalization. In this study, two differentNDCs (NDC-1 and NDC-2) bearing a thiosemicarbazide/1,2,4-triazolemoiety were synthesized and tested for chemotherapeutic effects onovarian cancer cells, which have a high COX-2 expression. To overcomethe limited dispersion of these hydrophobic drugs, the drug moleculeswere conjugated to the surface of 13 nm AuNPs. Conjugation of drugsto AuNPs increased the distribution of drugs in aqueous media, andNDC@AuNP conjugates exhibited excellent colloidal stability for upto 8 weeks. The proposed system demonstrated an increased chemotherapeuticeffect than the free drug counterparts with at least 5 times lowerIC50 values. NDC@AuNP nanosystems induced higher apoptosis rates,which established a simple and novel way to investigate activity ofprospective drugs in drug discovery research

    Design, synthesis, molecular docking and biological evaluation of 1,2,4-triazole derivatives possessing a hydrazone moiety as anti-breast cancer agents

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    Compounds containing 1,2,4-triazoles and hydrazone structural frameworks have been widely studied and demonstrated to exhibit a wide range of pharmacological properties. In this work, a descriptive series of new hybrid compounds with a 1,2,4-triazole ring and a hydrazone moiety were designed and synthesized by oxidative cyclization of thiourea derivatives using molecular iodine under mild conditions. The structure of synthesized compounds was characterized by employing different spectral techniques including FTIR, 1H NMR, 13C NMR, HRMS, and X-ray analysis. Furthermore, the proposed structure of BIH2 was resolved using single-crystal X-ray analysis. The compounds were evaluated for their in vitro anti-breast cancer activity and the most promising compound BIH4 with a methyl group substituted to a benzene ring exhibited significant dose-dependent cytotoxicity with selectivity to MDA-MB-231 cells in a Resazurin assay. The investigation of cell cycle progression analysis of the most active compound using a flow cytometer displayed a cell cycle arrest in the sub G1 phase. Furthermore, molecular modeling studies for the synthesized compounds were performed to predict their binding affinities toward the active site of BCL-2. The findings of the molecular modeling investigations were highly consistent with those of the cytotoxicity results
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