Suppression of systemic inflammation and signs of acute and chronic cholangitis by multi-kinase inhibitor 1-(4-Cl-benzyl)-3-chloro-4-(CF3-phenylamino)-1H-pyrrole-2,5-dione

Kuznietsova, Halyna; Byelinska, І.V.; Dziubenko, Natalia; Lynchak, Oksana; Milokhov, Demyd S.; Khilya, O. V.; Finiuk, Nataliya; Klyuchivska, Olga; Stoika, Rostyslav; Rybal’chenko, V. K.

doi:10.1007/s11010-021-04144-y

Cited by 5 publications

(4 citation statements)

References 53 publications

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“…[ 18,19 ] We evaluated the cytotoxicity of LevNPs and DMSO (control) against fibroblasts as reported previously. [ 20–22 ] As shown in Figure S3B, Supporting Information, 0.1% DMSO showed no cytotoxicity with over 90% cell viability and LevNPs with 0.06% residual DMSO also did not exhibit toxicity toward cells.…”

Section: Resultsmentioning

confidence: 99%

Fructose‐Derived Levan Nanoparticles Protect Against Osteoarthritis by Directly Blocking CD44 Activation

Cho

Lee

et al. 2022

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Although the development of several inflammatory diseases can be initiated in response to CD44 receptor signaling dysregulation, anti‐CD44 antibody therapy has been discontinued in clinical trials owing to its severe adverse effects. Moreover, biocompatible materials that block CD44 are unknown. Here, self‐assembled levan nanoparticles (LevNPs) through simple nanoprecipitation without chemical conjugation of biocompatible levan are developed. LevNPs are prepared through a simple nanoprecipitation without chemical conjugation; this results in particles with a consistently dispersed hydrodynamic diameter of approximately 230 nm. The physicochemical properties of LevNP are well‐maintained even after long‐term storage in a physiological buffer, suggesting that LevNPs are stable and useful for various biomedical applications. A protein array and an in silico LevNP‐CD44 interaction assay reveal that LevNPs specifically bind to CD44. Importantly, CD44 is highly expressed in the cartilage of patients with osteoarthritis (OA). LevNPs showed no cytotoxicity and reduced catabolic factor expression in an OA mimic in vitro. Furthermore, intra‐articular injection of LevNPs exhibited long‐term retention ability in the knee joint and protection against posttraumatic OA cartilage destruction in mice with medial meniscus destabilization–induced OA. These results show that LevNPs are biocompatible and exhibit potential as a nanotherapeutic for protecting against OA pathogenesis by directly blocking CD44.

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Section: Resultsmentioning

confidence: 99%

Fructose‐Derived Levan Nanoparticles Protect Against Osteoarthritis by Directly Blocking CD44 Activation

Cho

Lee

et al. 2022

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“…We studied the effect of different variants of gel composition (GC) Benzidaflaziverdine on the viability of pseudonormal human keratinocytes of the HaCaT line, as well as mouse fibroblasts of BALB-3T3 line and mouse macrophages of J774.2 line. Various methods of cell survival assessment were used: MTT-assay [26][27][28], staining of cells with fluorescent dyes Hoechst 33342 and Propidium iodide (PI) [29,30], as well as a test for the genotoxic effects on cells (DNA comet assay) [30,31]. The antioxidant properties of the developed GC variants were evaluated using DPPH (1,1-diphenyl-2-picrylhydrazyl) reagent, Merck (Dam-stadt, Germany) [32][33][34] and DCFDA-H2 (2',7'dichlorodihydrofluorescein diacetate), Molecular Probes™ produced for the Thermo Fisher [29,32].…”

Section: Methodsmentioning

confidence: 99%

“…Cell culturing was carried out in the Dulbecco-modified Eagle's medium (DMEM) (Sigma Chem Co., USA) in the presence of the decomplemented fetal bovine serum (Sigma Chem Co., USA) and 50 μg/ml gentamicin (Sigma, Chem Co., USA) in a thermostat with 5% CO2 content at 37°C and 100% humidity. Cells were subcultured every 2-3 days at 0.5-1 million cells per 1 ml of culture medium [26,27]. The number of living cells was determined with the MTT assay, using the manufacturer's recommendations (Sigma, Chem Co., USA) [28].…”

Section: Cholisalmentioning

confidence: 99%

Study of Cytocompatibility of Different Supplements in Gel Compositions Used for the Treatment of Periodontal Diseases in Orthodontic Patients via Exploration of Mechanisms of Their Cytopathic and Cytoprotective Effects in Cultured Human and Mouse Cells

Hodovanyi

Чухрай

Hodovana

et al. 2023

Proc Shevchenko Sci Soc Med Sci

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Introduction. A search continues for effective means which may reduce the overload of harmful factors, eliminate the inflammatory process, and reduce stress on the periodontal tissues during the active period of orthodontic treatment. We developed and patented the gel composition (GC) Benzidaflaziverdine prepared based on Proteflazid® (flavonoids) and benzydamine hydrochloride (BH) T-Sept® for the local treatment of the periodontal tissues in the form of a periodontal dressing in the orthodontic patients. The aim of this study was to evaluate the cytocompatibility of different combinations of components in gel composition based on flavonoid complex and benzydamine hydrochloride (Benzidaflaziverdine) used for the treatment of periodontal diseases in orthodontic patients. For this, mechanisms of their cytopathic and cytoprotective effects will be explored using cultured human and mouse cells. Methods. We studied the effect of different supplements used in GC Benzidaflaziverdine on the viability of pseudonormal human keratinocytes of the HaCaT line and mouse fibroblasts of the BALB-3T3 line, and mouse macrophages of the J774.2 line. Various methods of cell survival assessment were used: MTT-assay, staining of cells with fluorescent dyes Hoechst 33342 and Propidium iodide (PI), as well as a test for the genotoxic effects on cells (DNA comet assay). The antioxidant properties of the developed GC variants were evaluated using DPPH (1,1-diphenyl-2-picrylhydrazyl), Merck (Dam-stadt, Germany), and DCFDA-H2 (2’,7’-dichlorodihydrofluorescein diacetate). Results. We demonstrated that the Sample containing gel base and BH in the form of a solution (Tantum Verde®) possessed weak prooxidant properties. While the Sample contained gel base, powdered BH (T-Sept®) and Sample containing gel base and powdered BH (T-Sept® and Proteflazid®) possessed pronounced antioxidant properties. Conclusions. Tests with DPPH and DCFDA dyes were used to confirm the hypothesis regarding the cytoprotective effect of the patented gel composition Benzidaflaziverdine for local application in the form of a periodontal bandage due to the antioxidant activity of the flavonoid complex, which reaches the maximum level at the 2nd hour of exposure. This gel composition can be recommended for use in clinical periodontology for medical support of orthodontic patients before and during the active phase of orthodontic treatment.

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“…The study protocol with human lymphocytes isolated from healthy adult human peripheral blood was approved by the Ethics Committee of the Institute of Cell Biology of National Academy of Sciences of Ukraine (protocol #2 dated by January 27, 2019). Lymphocytes of human peripheral blood were isolated from blood consisting of anti-coagulant sodium heparin solution 10 U/ml (B. BRAUN MEDICAL, S.A., Spain) on density gradient of Gradisol G (Polfa, Poland), as described [27]. The blood: Gradisol G mixture (1:1) was centrifuged at 400×g at room temperature for 30 min.…”

Section: Cells Culture and Cytotoxicity Mtt Assaymentioning

confidence: 99%

Synthesis of the novel cage amides and imides and evaluation of their antibacterial and antifungal activity

Palchykov¹,

Gaponov²,

Manko³

et al. 2022

Ukr.Biochem.J.

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Cage amides and imides bearing bicyclo[2.2.1]- and bicyclo[2.2.2]-subunits were synthesized and evaluated both for antimicrobial activity toward five key ESKAPE pathogenic bacteria: one Gram‐positive bacteria methicillin‐resistant Staphylococcus aureus (ATCC 43300), four Gram‐negative bacteria Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 700603), Acinetobacter baumannii (ATCC 19606) and Pseudomonas aeruginosa (ATCC 27853) and for antifungal activity towards pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (H99; ATCC 208821). Compound VP-4539 with bicyclo[2.2.2]octene motif demonstrated the highest cytotoxic activity towards C. neoformans, while human keratinocytes of HaCaT line, murine fibroblasts of Balb/c 3T3 line and mitogen-activated lymphocytes of peripheral human blood were found to be tolerant to its action. VP-4539 compound did not intercalate into salmon sperm DNA indicating that its cytotoxicity is not related to intercalation into nucleic acid. Keywords: antifungal, antimicrobial, bicyclo[2.2.1]heptane, bicyclo[2.2.2]octene, cytotoxicity, DNA intercalation, human keratinocytes, lymphocytes, сage compounds

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Suppression of systemic inflammation and signs of acute and chronic cholangitis by multi-kinase inhibitor 1-(4-Cl-benzyl)-3-chloro-4-(CF3-phenylamino)-1H-pyrrole-2,5-dione

Cited by 5 publications

References 53 publications

Fructose‐Derived Levan Nanoparticles Protect Against Osteoarthritis by Directly Blocking CD44 Activation

Fructose‐Derived Levan Nanoparticles Protect Against Osteoarthritis by Directly Blocking CD44 Activation

Study of Cytocompatibility of Different Supplements in Gel Compositions Used for the Treatment of Periodontal Diseases in Orthodontic Patients via Exploration of Mechanisms of Their Cytopathic and Cytoprotective Effects in Cultured Human and Mouse Cells

Synthesis of the novel cage amides and imides and evaluation of their antibacterial and antifungal activity

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