Chromone-3-aldehyde derivatives – sirtuin 2 inhibitors for correction of muscular dysfunction

Abstract The aim of the study was to evaluate experimentally, the myoprotective effect of new chromone-3-aldehyde derivatives in conditions of muscular dysfunction and to establish a potential mechanism of myoprotective activity – the blockade of the function of sirutin 2. Materials and methods. The effect of new chromone-3-aldehyde derivatives on the development of muscular dysfunction under the conditions of an electromiostimulation test, was studied. The degree of muscle fatigue was evaluated in the «grip-strength» and through test biochemical assays (determination of the activity of lactate dehydrogenase, creatine kinase, concentration of lactic and pyruvic acids, creatinine, myoglobin, and total protein) to determine the possible mechanism of action of the test compounds (5 new derivatives of chromone-3-aldehyde) and their effect on the function of sirtuin 2 was evaluated. Results. The study showed that chromone-3-aldehyde derivatives have a pronounced myoprotective effect associated with low toxicity (class 5 toxicity according to the GHS classification), which was confirmed by the results of the «grip-strength» test and biochemical tests data. Test compounds under the X3AC1, X3AOAC and X3AN codes evince sirtuin 2 inhibitory activity, which was reflected in a decrease in its concentration by 63.6% (p <0.05); 130.2% (p <0.05) and 218.8% (p <0.05). Conclusion. The study showed that chromone-3-aldehyde derivatives are promising subjects for further study with the goal of creating a drug with a high myoprotective effect and an optimal safety profile.

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The development of HPLC-DAD method for determination of active pharmaceutical ingredient in the potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)thio) acetate substance

Current Issues in Pharmacy and Medical Sciences ◽

10.2478/cipms-2019-0001 ◽

2019 ◽

Vol 32 (1) ◽

pp. 5-9

Author(s):

Roman Shcherbyna ◽

Volodymyr Parchenko ◽

Boris Varynskyi ◽

Andriy Kaplaushenko

Keyword(s):

High Performance ◽

Active Pharmaceutical Ingredient ◽

Diode Array ◽

Diode Array Detection ◽

Accuracy And Precision ◽

Array Detection ◽

Low Toxicity ◽

Derivatives Of

Abstract Derivatives of 1,2,4-triazole are actively researched by scientists and synthetic pharmacologists. The last studies have shown that potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)thio)acetate with low toxicity series exhibits antioxidant and hepatoprotective properties. Therefore, the purpose of this work was to develop a method for determining the API in the potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)thio)acetate substance using the method of high-performance liquid chromatography with diode array detection (HPLC-DAD). As a result of this work, it is shown that the developed method is specific and meets the requirements of linearity, accuracy and precision. The results of determining the contents of the API in real samples indicate that the method can be proposed to control the quality of the potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)thio)acetate substance.

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Features of phosphorus-calcium metabolism in children with neurogenic disorders of urination

Nephrology (Saint-Petersburg) ◽

10.36485/1561-6274-2020-24-1-45-50 ◽

2020 ◽

Vol 24 (1) ◽

pp. 45-50

Author(s):

Yu. F. Lobanov ◽

D. Y. Latyshev ◽

Ya. F. Zverev ◽

N. A. Tekuteva ◽

N. M. Mikheeva

Keyword(s):

Connective Tissue ◽

Calcium Metabolism ◽

Point System ◽

Industry Standards ◽

Muscular Dysfunction ◽

Connective Tissue Dysplasia ◽

Calcium And Phosphorus ◽

Comparison Of The Results ◽

Neurogenic Disorders

THE AIM: To study the characteristics of phosphorus-calcium metabolism in patients with neurogenic disorders of urination, taking into account the severity of the manifestations of connective tissue dysplasia. PATIENTS AND METHODS. The study included 90 children, including 60 children with neuro-muscular dysfunction of the bladder (NMDB) and 30 children with enuresis from the age of 5 to 15 years. The diagnosis was established based on a comprehensive examination and according to industry standards. Connective tissue dysplasia was diagnosed in children with the detection of 6 or more small external or visceral manifestations involving 3 or more organs from different systems. Assessment of the severity (severity) of connective tissue dysplasia was carried out according to the point system proposed by T.I. Kadurina et al. Each group was divided into subgroups depending on the severity of the manifestations of connective tissue dysplasia. The determination of the level of calcium and phosphorus in the blood and urine, as well as the calculation of the calcium-creatinine coefficient followed by a comparison of the results in these groups and subgroups. To assess the significance of differences, the Mann-Whitney test was calculated, p <0.05 was considered significant. RESULTS. he level of calcium and phosphorus in the urine was slightly higher in children with enuresis, especially in the morning portion of urine, where the concentration of calcium was 26% higher than in patients with NMDB. At the same time, the value of calcium /creatinine coefficient was significantly higher in the group of patients with enuresis and was 2 times higher than the normative indicators, which indicates the importance of hypercalciuria in the development of enuresis. СONCLUSION. According to the obtained data, the severity of calciuria, determined by the value of the calcium-creatinine coefficient, is significantly higher in patients with enuresis than with NMDB.

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Simultaneous determination of eight derivatives of propranolol in cornea perfusate in vitro by high performance liquid chromatography

Chinese Journal of Chromatography ◽

10.3724/sp.j.1123.2012.06039 ◽

2013 ◽

Vol 30 (11) ◽

pp. 1183-1187

Author(s):

Haitao WU ◽

Chuanbing CHEN ◽

Ningsheng WANG ◽

Suiqing MI ◽

Nanying LIAO

Keyword(s):

High Performance Liquid Chromatography ◽

Liquid Chromatography ◽

Simultaneous Determination ◽

High Performance ◽

Derivatives Of

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Spectrophotometric study of the complexation equilibria of cadmium ions with 5-bromo and 5-chloro derivatives of 2-(2-pyridylazo)-5-diethylaminophenol (BrPADAP, ClPADAP)

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19830052 ◽

1983 ◽

Vol 48 (1) ◽

pp. 52-59 ◽

Cited By ~ 4

Author(s):

Vlastimil Kubáň ◽

Miroslav Macka

Keyword(s):

Equilibrium Constants ◽

Spectrophotometric Study ◽

Graphical Analysis ◽

Optimal Conditions ◽

Cadmium Ions ◽

Brij 35 ◽

Ethanol Medium ◽

Triton X ◽

Derivatives Of

The composition, optical characteristics, molar absorption coefficients and equilibrium constants of the reactions of formation of the ML and ML2 complexes of both reagents with cadmium(II) ions were determined by graphical analysis and numerical interpretation of the absorbance-pH curves by the modified SQUAD-G program. Optimal conditions were proposed for the spectrophotometric determination of Cd in 10% v/v ethanol medium in the presence of 0.1% w/v Triton X-100 or 1% w/v Brij 35. BrPADAP and ClPADAP are the most sensitive spectrophotometric reagents for the determination of cadmium(II) ions (ε = 1.28-1.44 . 105 mmol-1 cm2 at 560 nm and pH 8.0-9.5) with a high colour contrast in the reaction (Δλmax ~117 nm) and a selectivity similar to that of other N-heterocyclic azodyes (PAR, PAN, etc.).

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Spectrophotometric study of the acid-base and optical properties of the 5-bromo and 5-chloro derivatives of 2-(2-pyridylazo)-5-(diethylamino)phenol (BrPADAP, ClPADAP) and their complexation equilibria with zinc(II) ions

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19822676 ◽

1982 ◽

Vol 47 (10) ◽

pp. 2676-2691 ◽

Cited By ~ 6

Author(s):

Miroslav Macka ◽

Vlastimil Kubáň

Keyword(s):

Equilibrium Constants ◽

Spectrophotometric Study ◽

Graphical Analysis ◽

Alkaline Media ◽

Acid Base ◽

Ethanol Medium ◽

Triton X ◽

Mixed Water ◽

Derivatives Of

The optical and acid-base characteristics of BrPADAP and ClPADAP were studied in mixed water-ethanol and water-DMF media and in 10% ethanol medium in the presence of cationic, anionic and nonionic tensides. The composition, optical characteristics, molar absorption coefficients and equilibrium constants of the ML and ML2 complexes with zinc(II) ions were found by graphical analysis and numerical interpretation of the absorbance curves by the modified SQUAD-G program. Optimal conditions were found for the spectrophotometric determination of Zn(II) in the presence of 0.1% Triton X-100 or 1% Brij 35 in alkaline media with pH = 6.5-10. BrPADAP and ClPADAP are the most sensitive reagents (ε = 1.3-1.6 . 105 mmol-1 cm2 at 557 and 560 nm, respectively) for the determination of zinc with high colour contrast of the reaction (Δλ = 104 nm) and selectivity similar to that for the other N-heterocyclic azodyes (PAN, PAR, etc.).

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SYNTHESIS AND DETERMINATION OF LYCOMARASMIN ACTIVITY OF SOME DERIVATIVES OF ASPARTIC ACID

Journal of Biological Chemistry ◽

10.1016/s0021-9258(18)57142-8 ◽

1948 ◽

Vol 176 (3) ◽

pp. 1299-1308 ◽

Cited By ~ 1

Author(s):

D.W. Woolley

Keyword(s):

Aspartic Acid ◽

Derivatives Of

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Roquefortine C Occurrence in Blue Cheese

Journal of Food Protection ◽

10.4315/0362-028x-64.2.246 ◽

2001 ◽

Vol 64 (2) ◽

pp. 246-251 ◽

Cited By ~ 41

Author(s):

CARLO FINOLI ◽

ANGELA VECCHIO ◽

ANTONIETTA GALLI ◽

IVAN DRAGONI

Keyword(s):

Yeast Extract ◽

Culture Media ◽

Penicillium Roqueforti ◽

Blue Cheese ◽

Penicillium Crustosum ◽

Sucrose Medium ◽

Low Toxicity ◽

Yeast Extract Sucrose ◽

Roquefortine C

Several strains of Penicillium are used for the production of mold-ripened cheeses, and some of them are able to produce mycotoxins. The aims of the research were the determination of roquefortine C and PR toxin in domestic and imported blue cheeses, the identification of the penicillia used as starter, and the investigation of their capacity for producing toxins in culture media. Roquefortine C was always found in the cheeses at levels ranging from 0.05 to 1.47 mg/kg, whereas the PR toxin was never found. The identification of the fungal strains present in the domestic cheeses included Penicillium glabrum, Penicillium roqueforti, and Penicillium cyclopium in the Gorgonzola “dolce” and Penicillium roqueforti in the Gorgonzola “naturale”; in one case, the presence of Penicillium crustosum was observed. The strains isolated from the foreign cheeses belonged to P. roqueforti. The strains were able to produce between 0.18 and 8.44 mg/liter of roquefortine in yeast extract sucrose medium and between 0.06 and 3.08 mg/liter and less than 0.05 mg/liter when inoculated in milk at 20°C for 14 days and 4°C for 24 days, respectively. Linear relations between production of roquefortine in culture media and cheeses did not emerge. PR toxin ranged from less than 0.05 to 60.30 mg/liter in yeast extract sucrose medium and was produced in milk at 20°C from only one strain. The low levels and the relatively low toxicity of roquefortine make the consumption of blue cheese safe for the consumer.

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