@article{MTMT:34125145, title = {Pharmacological Evaluation of Newly Synthesized Cannabidiol Derivates on H9c2 Cells}, url = {https://m2.mtmt.hu/api/publication/34125145}, author = {Szőke, Kitti and Kajtár, Richárd and Gyöngyösi, Alexandra and Czompa, Attila and Fésüs, Adina and Lőrincz, Eszter Boglárka and Petróczi, Ferenc Dániel and Herczegh, Pál and Bak, István and Borbás, Anikó and Bakai-Bereczki, Ilona and Lekli, István}, doi = {10.3390/antiox12091714}, journal-iso = {ANTIOXIDANTS-BASEL}, journal = {ANTIOXIDANTS}, volume = {12}, unique-id = {34125145}, year = {2023}, eissn = {2076-3921}, orcid-numbers = {Fésüs, Adina/0000-0002-6351-7715; Borbás, Anikó/0000-0001-8462-4547; Bakai-Bereczki, Ilona/0000-0003-4601-7257} } @article{MTMT:32814186, title = {Beta-Carotene Affects the Effects of Heme Oxygenase-1 in Isolated, Ischemic/Reperfused Rat Hearts: Potential Role of the Iron}, url = {https://m2.mtmt.hu/api/publication/32814186}, author = {Csépányi, Evelin and Gyöngyösi, Alexandra and Lekli, István and Tósaki, Árpád and Bak, István}, doi = {10.3390/molecules27093039}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {27}, unique-id = {32814186}, issn = {1420-3049}, year = {2022}, eissn = {1420-3049} } @article{MTMT:32246883, title = {Preparation of Acyclovir-Containing Solid Foam by Ultrasonic Batch Technology}, url = {https://m2.mtmt.hu/api/publication/32246883}, author = {Haimhoffer, Ádám and Fenyvesi, Ferenc and Lekli, István and Béresová, Monika and Bak, István and Czagány, Máté and Vasvári, Gábor and Bácskay, Ildikó and Tóth, Judit and Budai, István}, doi = {10.3390/pharmaceutics13101571}, journal-iso = {PHARMACEUTICS}, journal = {PHARMACEUTICS}, volume = {13}, unique-id = {32246883}, issn = {1999-4923}, year = {2021}, eissn = {1999-4923}, orcid-numbers = {Béresová, Monika/0000-0001-8610-3788; Budai, István/0000-0002-8966-3817} } @article{MTMT:31841366, title = {Basic Pharmacological Characterization of EV-34, a New H2S-Releasing Ibuprofen Derivative.}, url = {https://m2.mtmt.hu/api/publication/31841366}, author = {Gyöngyösi, Alexandra and Vivien, Verner and Bakai-Bereczki, Ilona and Kiss, Attila and Rita, Zilinyi and Tósaki, Árpád and Bak, István and Borbás, Anikó and Herczegh, Pál and Lekli, István}, doi = {10.3390/molecules26030599}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {26}, unique-id = {31841366}, issn = {1420-3049}, abstract = {Cardioprotective effects of H2S are being suggested by numerous studies. Furthermore, H2S plays a role in relaxation of vascular smooth muscle, protects against oxidative stress, and modulates inflammation. Long-term high-dose use of NSAIDs, such as ibuprofen, have been associated with enhanced cardiovascular risk. The goal of the present work is the synthesis and basic pharmacological characterization of a newly designed H2S-releasing ibuprofen derivative.Following the synthesis of EV-34, a new H2S-releasing derivative of ibuprofen, oxidative stability assays were performed (Fenton and porphyrin assays). Furthermore, stability of the molecule was studied in rat serum and liver lysates. H2S-releasing ability of the EC-34 was studied with a hydrogen sulfide sensor. MTT (3-(4,5-dimethylthiazol 2-yl)-2,5-(diphenyltetrazolium bromide)) assay was carried out to monitor the possible cytotoxic effect of the compound. Cyclooxygenase (COX) inhibitory property of EV-34 was also evaluated. Carrageenan assay was carried out to compare the anti-inflammatory effect of EV-34 to ibuprofen in rat paws.The results revealed that the molecule is stable under oxidative condition of Fenton reaction. However, EV-34 undergoes biodegradation in rat serum and liver lysates. In cell culture medium H2S is being released from EV-34. No cytotoxic effect was observed at concentrations of 10, 100, 500 µM. The COX-1 and COX-2 inhibitory effects of the molecule are comparable to those of ibuprofen. Furthermore, based on the carrageenan assay, EV-34 exhibits the same anti-inflammatory effect to that of equimolar amount of ibuprofen (100 mg/bwkg).The results indicate that EV-34 is a safe H2S releasing ibuprofen derivative bearing anti-inflammatory properties.}, keywords = {HYDROGEN-SULFIDE; Gasotransmitter; anti-inflammatory property; H2S-releasing-ibuprofen; thiolacetic acid}, year = {2021}, eissn = {1420-3049}, orcid-numbers = {Bakai-Bereczki, Ilona/0000-0003-4601-7257; Kiss, Attila/0000-0003-3601-5143; Borbás, Anikó/0000-0001-8462-4547} } @article{MTMT:30345384, title = {Synthesis, in Vitro Biological Evaluation, and Oxidative Transformation of New Flavonol Derivatives. The Possible Role of the Phenyl-N,N-Dimethylamino Group.}, url = {https://m2.mtmt.hu/api/publication/30345384}, author = {Szabados-Fürjesi, Péter and Pajtás, Dávid and Barta, Aliz and Csépányi, Evelin and Kiss, Attila and Tósaki, Árpád and Bak, István}, doi = {10.3390/molecules23123161}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {23}, unique-id = {30345384}, issn = {1420-3049}, abstract = {Six new flavonols (6a⁻f) were synthesized with Claisen⁻Schmidt and Suzuki reactions and they were fully characterized by spectroscopic methods. In order to evaluate their antioxidant activities, their oxygen radical absorption capacity and ferric reducing antioxidant power were measured, along with their free radical scavenging activity against 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) and 2,2-diphenyl-1-picrylhydrazylradicals. In addition, their cytotoxicity on H9c2 cardiomyoblast cells was also assessed by a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Compounds bearing the phenyl-N,N-dimethylamino group (6a, 6c, and 6e) exhibited promising antioxidant potency and did not have any cytotoxic effect. After a consideration of these data, the oxidative transformation of the 6c compound was investigated in vitro with a chemical Fenton reaction and the identification of the formed oxidation products was performed by mass spectrometry. Two potential metabolites were detected. Based on these results, compound 6c can be a model compound for future developments. Overall, this work has proved the involvement of the phenyl-N,N-dimethylamino group in the antioxidant activity of flavonols.}, keywords = {CYTOTOXICITY; ANTIOXIDANT; flavonoid; Flavonol; Oxidative metabolism}, year = {2018}, eissn = {1420-3049}, orcid-numbers = {Kiss, Attila/0000-0003-3601-5143} } @article{MTMT:3365765, title = {Aged (Black) versus Raw Garlic against Ischemia/Reperfusion-Induced Cardiac Complications}, url = {https://m2.mtmt.hu/api/publication/3365765}, author = {Czompa, Attila and Szőke, Kitti and Prokisch, Jozsef and Gyöngyösi, Alexandra and Bak, István and Balla, György and Tósaki, Árpád and Lekli, István}, doi = {10.3390/ijms19041017}, journal-iso = {INT J MOL SCI}, journal = {INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES}, volume = {19}, unique-id = {3365765}, issn = {1661-6596}, year = {2018}, eissn = {1422-0067} } @article{MTMT:3360047, title = {The Effects of Long-Term, Low- and High-Dose Beta-Carotene Treatment in Zucker Diabetic Fatty Rats: The Role of HO-1}, url = {https://m2.mtmt.hu/api/publication/3360047}, author = {Csépányi, Evelin and Czompa, Attila and Szabados-Fürjesi, Péter and Lekli, István and Balla, József and Balla, György and Tósaki, Árpád and Bak, István}, doi = {10.3390/ijms19041132}, journal-iso = {INT J MOL SCI}, journal = {INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES}, volume = {19}, unique-id = {3360047}, issn = {1661-6596}, year = {2018}, eissn = {1422-0067} } @article{MTMT:3212037, title = {Effects of Momordica charantia (Bitter Melon) on Ischemic Diabetic Myocardium.}, url = {https://m2.mtmt.hu/api/publication/3212037}, author = {Czompa, Attila and Gyöngyösi, Alexandra and Szőke, Kitti and Bak, István and Csépányi, Evelin and Haines, DD and Tósaki, Árpád and Lekli, István}, doi = {10.3390/molecules22030488}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {22}, unique-id = {3212037}, issn = {1420-3049}, abstract = {Objective: A rat model is here used to test a hypothesis that Momordica charantia (Bitter melon (BM)) extract favorably alters processes in cardiovascular tissue and is systemically relevant to the pathophysiology of type 2 diabetes (T2DM) and related cardiovascular disease. Methods: Male Lean and Zucker Obese (ZO) rats were gavage-treated for six weeks with 400 mg/kg body weight bitter melon (BM) extract suspended in mucin-water vehicle, or with vehicle (Control). Animals were segregated into four treatment groups, 10 animals in each group, according to strain (Lean or ZO) and treatment (Control or BM). Following six-week treatment periods, peripheral blood was collected from selected animals, followed by sacrifice, thoracotomy and mounting of isolated working heart setup. Results: Body mass of both Lean and ZO rats was unaffected by treatment, likewise, peripheral blood fasting glucose levels showed no significant treatment-related effects. However, some BM treatment-related improvement was noted in postischemic cardiac functions when Lean, BM-treated animals were compared to vehicle treated Lean control rats. Treatment of Lean, but not ZO, rats significantly reduced the magnitude of infarcted zone in isolated hearts subjected to 30 min of ischemia followed by 2 h of working mode reperfusion. Immunohistochemical demonstration of caspase-3 expression by isolated heart tissues subjected to 30 min of ischemia followed by 2 h of reperfusion, revealed significant correlation between BM treatment and reduced expression of this enzyme in hearts obtained from both Lean and ZO animals. The hierarchy and order of caspase-3 expression from highest to lowest was as follows: ZO rats receiving vehicle > ZO rats receiving BM extract > Lean rats treated receiving vehicle > Lean rats administered BM extract. Outcomes of analyses of peripheral blood content of cardiac-related analytics: with particular relevance to clinical application was a significant elevation in blood of ZO and ZO BM-treated, versus Lean rats of total cholesterol (high density lipoprotein HDL-c + low density lipoprotein LDL-c), with an inferred increase in HDL-c/LDL-c ratio-an outcome associated with decreased risk of atherosclerotic disease. Conclusions: BM extract failed to positively affect T2DM- and cardiovascular-related outcomes at a level suggesting use as a standalone treatment. Nevertheless, the encouraging effects of BM in enhancement of cardiac function, suppression of post-ischemic/reperfused infarct size extent and capacity to modulate serum cholesterol, will likely make it useful as an adjuvant therapy for the management of T2DM and related cardiovascular diseases.}, year = {2017}, eissn = {1420-3049} } @article{MTMT:3212029, title = {Antioxidant Properties and Oxidative Transformation of Different Chromone Derivatives.}, url = {https://m2.mtmt.hu/api/publication/3212029}, author = {Csépányi, Evelin and Szabados-Fürjesi, Péter and Kiss, Attila and Frensemeier, LM and Karst, U and Lekli, István and Haines, DD and Tósaki, Árpád and Bak, István}, doi = {10.3390/molecules22040588}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {22}, unique-id = {3212029}, issn = {1420-3049}, abstract = {Nowadays, there is an increase in the application of natural products for the prevention of different disorders or adjuvant substances next to pharmacological treatment. Phytochemicals include different chromone derivatives, which possess a wide spectrum of biological activity. The aim of the present study was the investigation of the antioxidant activity, cytotoxicity and oxidative transformation of nine chromone derivatives. First, we investigated the radical scavenging activity (ABTS), the oxygen radical absorption capacity (ORAC) and the ferric reducing antioxidant power (FRAP) of the investigated molecules. The cytotoxic effects of the compounds were tested on H9c2 cell cultures by the MTT assay. Each compound showed a significant ORAC value compared to the reference. However, the compound 865 possess significantly higher FRAP and ABTS activity in comparison with the reference and other tested molecules, respectively. Based on these assays, the compound 865 was selected for further analysis. In these experiments, we investigated the oxidative metabolism of the compound in vitro. The molecule was oxidized by the Fenton reaction, artificial porphyrin and electrochemistry; then, the formed products were identified by mass spectrometry. Four possible metabolites were detected. The results revealed the compound 865 to possess good antioxidant properties and to be stable metabolically; hence, it is worth investigating its effects in vivo.}, keywords = {antioxidants; CYTOTOXICITY; Flavonoids; CHROMONE; Oxidative metabolism}, year = {2017}, eissn = {1420-3049}, orcid-numbers = {Kiss, Attila/0000-0003-3601-5143} } @article{MTMT:2935306, title = {Cardiovascular effects of low versus high-dose beta-carotene in a rat model}, url = {https://m2.mtmt.hu/api/publication/2935306}, author = {Csépányi, Evelin and Czompa, Attila and Haines, David and Lekli, István and Bakondi, Edina and Balla, György and Tósaki, Árpád and Bak, István}, doi = {10.1016/j.phrs.2015.07.021}, journal-iso = {PHARMACOL RES}, journal = {PHARMACOLOGICAL RESEARCH}, volume = {100}, unique-id = {2935306}, issn = {1043-6618}, abstract = {beta-carotene (BC), a lipid-soluble tetraterpene precursor to vitamin A, widely distributed in plants, including many used in human diet, has well-known health-enhancing properties, including reducing risk of and treatment for certain diseases. Nevertheless, BC may also act to promote disease through the activity of BC derivatives that form in the presence of external toxicants such as cigarette smoke and endogenously-produced reactive oxygen species. The present investigation evaluates the dose-dependent cardioprotective and possibly harmful properties of BC in a rat model. Adult male rats were gavage-fed BC for 4 weeks, at dosages of either 0, 30 or 150mg/kg/day. Then, hearts excised from the animals were mounted in a "working heart" apparatus and subjected to 30min of global ischemia, followed by 120min of reperfusion. A panel of cardiac functional evaluations was conducted on each heart. Infarct size and total antioxidant capacity of the myocardium were assessed. Heart tissue content of heme oxygenase-1 (HO-1) by Western blot analysis; and potential direct cytotoxic effects of BC by MTT assay were evaluated. Hearts taken from rats receiving 30mg/kg/day BC exhibited significantly improved heart function at lower reperfusion times, but lost this protection at higher BC dosage and longer reperfusion times. Myocardial HO-1 content was significantly elevated dose-responsively to both BC dosage. Finally, in vitro evaluation of BC on H9c2 cells showed that the agent significantly improved vitality of these cells in a dose range of 2.5-10muM. Although data presented here do not allow for a comprehensive mechanistic explanation for reduced cardioprotection at high dose BC, it is speculated that since Fe2+ produced as a metabolite of HO-1 activity, may determine whether BC acts as an antioxidant or prooxidant agent, the strong induction of this enzyme in response to ischemia/reperfusion-induced oxidative stress may account for the high-dose BC loss of cardioprotection.}, year = {2015}, eissn = {1096-1186}, pages = {148-156} }