Browsing by Author "Gudumac, Valentin"

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COORDINATION COMPOUND AS INHIBITOR OF SUPEROXID RADICAL
(2019) Garbuz, Olga; Pantea, Valeria; Usataia, Irina; Graur, Vasilii; Țapcov, Victor; Sardari, Veronica; Tagadiuc, Olga; Gudumac, Valentin; Gulea, Aurelian
A fost obținut un nou compus coordinativ biologic activ, nitratul de cupru [2 - ({2 [(ethylsulfanyl) (prop-2-en-1-yl) carbononoimidooyl] -hydrazinylidene} methyl) phenolate], care face parte din clasa isotiosemicarbazidelor metalelor de tranziție.S-a stabilit că acesta exercită proprietăți anti radicalice performante la acțiunea moleculei organice cu radicalul superoxidic. Datorită acestei poroprietăți compusul obținut poate avea o potențială aplicare in medicină in calitate de inhibitor al radicalilor superoxidici in corpul uman, care poate duce la prevenirea deteriorării tesutului cellular, aterosclerozii si carcinogenezei.Compusul coordinativ sintetizat extinde arsenalul inhibitorilor de radicali superoxidici cu activitate biologică importanta.
COORDINATION COMPOUND, DERIVATIVE OF ISOTHIOSEMICARBAZIDE OF TRANSITION METALS AS AN INHIBITOR OF SUPEROXIDE RADICALS
(2021) Pantea, Valeriana; Graur, Vasilii; Andronache, Lilia; Gulea, Aurelian; Tsapkov, Victor; Sardari, Veronica; Gamaniuc, Marina; Gudumac, Valentin
A new biologically active coordination compound, which belongs to the class of transition metal isotiosemicarbazides - bis (m2-acetate-o) -bis {[N-prop-2-en-1-yl-N'- (pyridin- 2-ylmethylidene) carbamo-hydrazonothioate] copper} dihydrate was obtained. It has established that this compound exhibits strong anti-radical properties to the action of the organic molecule with the superoxide radical. Due to this property, the obtained compound can have a wide application in medicine as an inhibitor of superoxide radicals in the human body, thus preventing damage to cells and tissues, atherosclerosis and carcinogenesis. The synthesized coordination compound expands the arsenal of superoxide radical inhibitors with high biological activity.
COORDINATION COMPOUNDS OF COBALT, NICKEL, AND COPPER OF SOME 1,3-DIPHENYLPYRAZOLE-4-CARBALDEHYDE THIOSEMICARBAZONES
(Academia de Ştiinţe a Moldovei, 2015) Gulea, Aurelian; Tsapkov, Victor I.; Cotovaia, Aliona; Garbuz, Olga; Graur, Vasilii О.; Nicolenco, Aliona; Guţu, Iacob; Gudumac, Valentin
COPPER (II) ACETATE COORDINATION COMPOUND WITH 2-FORMYLPYRIDINE 4-ALLYLTHIOSEMICARBAZONE MANIFESTS INHIBITORY ACTIVITY AGAINST SUPEROXIDE RADICALS
(Marina Sokolova Publishings, 2021) Pantea, Valeriana; Graur, Vasilii; Andronache, Lilia; Gulea, Aurelian; Tsapkov, Victor; Sardari, Veronica; Gamaniuc, Mariana; Gudumac, Valentin
A new biologically active coordination compound, which belongs to the class of transition metal isotiosemicarbazides - bis (2-acetate-o) -bis {[N-prop-2-en-1-yl-N'- (pyridin- 2-ylmethylidene) carbamo-hydrazonothioate] copper} dihydrate was obtained. It has established that this compound exhibits strong anti-radical properties to the action of the organic molecule with the superoxide radical. Due to this property, the obtained compound can have a wide application in medicine as an inhibitor of superoxide radicals in the human body, thus preventing damage to cells and tissues, atherosclerosis and carcinogenesis. The synthesized coordination compound expands the arsenal of superoxide radical inhibitors with high biological activity.
COPPER(II) COORDINATION COMPOUNDS WITH THIOSEMICARBAZIDE DERIVATIVES AS INHIBITORS OF SUPEROXIDE RADICALS
(Marina Sokolova Publishings, 2022) Gulea, Aurelian; Tsapkov, Victor; Graur, Vasilii; Pantea, Valeriana; Andronache, Lilia; Shvets, I.; Matusovsky, V.; Lisii, D.; Botnaru, M.; Gudumac, Valentin
New biologically active coordination compounds of copper(II) based on substituted 3-(phenyl)-1-(pyridin-2-yl)prop-2-en- 1-one 4-allylthiosemicarbazones have been obtained. It was found that these compounds exhibit strong antiradical properties when interacting with a superoxide radical. Due to this property, the obtained compounds can find wide application in medicine as inhibitors of superoxide radicals in the human body, thus preventing damage of cells and tissues, multifactorial diseases, including carcinogenesis. The synthesized coordination compounds expand the arsenal of superoxide radical inhibitors with high biological activity. Their possible significance for the development of new treatment strategies for diseases associated with the overproduction of superoxide radicals discussed.
EXPRESIA ENZIMELOR GLUTATIONICE ÎN ŢESUTUL SPLENIC ESTE INFLUENȚATĂ DE DERIVAȚII TIOSEMICARBAZIDEI
(2021) Andronache, Lilia; Pantea, Valeriana; Gulea, Aurelian; Șveț, Ina; Ghindă, Sergiu; Privalova, Elena; Smeșnoi, Valentina; Gudumac, Valentin
Administrarea unor baze heterociclice Schiff noi și complexelor lor cu cuprul (II), derivați ai tiosemicarbazidei induce influenţe variate asupra activității enzimelor glutation-dependente în țesutul splenic. Este evidentă acţiunea selectivă a compușilor studiați asupra expresării enzimelor glutationice care se manifestă prin tendinţă de diminuare nesemnificativă a glutationreductazei (GR) și glutationperoxidazei (GPO), creșterea neimportantă a glutation-S-transferazei (GST) și depresia marcată a nivelului glutaredoxinei. Sporul leger al GST la acțiunea compușilor studiați poate fi considerată drept o reacție de protecție orientată să stagneze intensitatea proceselor peroxidice și să susțină activitatea ciclului glutationic, iar diminuarea enzimoactivității glutaredoxinei denotă efectul lor antiproliferativ, citostatic. Sunt necesare studii suplimentare pentru a evalua mecanismele de acțiune ale compușilor cercetați asupra activității enzimelor glutation-dependente în alte biosisteme și experimente pe animale pentru a aprecia importanța practică a rezultatelor obținute.
IN VITRO ANTIPROLIFERATIVE ACTIVITY AND ANTIOXIDANT CAPACITY OF NEW ORGANOMETALLIC COORDINATION COMPOUNDS, RESULTS CORRELATION ANALYSIS
(2016) Gulea, Aurelian; Gudumac, Valentin; Garbuz, Olga; Andronache, Lilia
A fost examinată și testată capacitatea inhibitorilor organometalici activi CMJ-33, CMSA-4, de a induce apoptoza în celulele epiteliale de carcinom de col uterin linia HeLa. Viabilitatea celulelor canceroase a fost determinată prin testul Alamar Blue fiind folosit un indicator redox – resazurin. S-a depistat activitate antitumorală mai mare a substanțelor testate decât la cea luată în calitate de etalon: - doxorubicina (DOXO). În scopul de a detecta eventuala prezenţă a efectelor adverse concomitente legate cu proprietățile pro-oxidante ale compușilor coordinativi, a fost folosită metoda cantitativă ORAC (Oxygen Radical Absorption Capacity). Rezultatele au demonstrat că substanțele testate CMT-67 şi CMSA-4 posedă activitate antioxidantă mai mare decât Trolox și DOXO. În această lucrare, noi constatăm prezența unei corelații pozitive semnificative (coeficient de corelație - 0,98) între efectele anti-proliferative și anti-oxidante pentru compuşii CMT-67, CMSA-4 și DOXO.
INFLUENCE OF COPPER COORDINATION COMPOUNDS AND CYANOBACTERIAN REMEDY BIOR ON BONE COLLAGEN AND HYDROXYPROLINE CONCENTRATIONS (ONTOGENETIC VIEW)
(Elan-Poligraf, 2011-07-07) Tagadiuc, Olga; Gulea, Aurelian; Rudic, Valeriu; Gudumac, Valentin
The aim of our research was to assess the influence of copper coordination compounds CMT-28 and CMT-67 and cyanobacterian remedy BioR on bone collagen and hydroxyproline (HYP) concentrations at different stages of postnatal ontogenesis in normal physiological conditions and experimental osteopathy (EO). The survey was conducted on a sample of 301 white laboratory rats of both sexes, which were divided depending on their stage of postnatal ontogenetic development and experimental model: control; animal with experimental osteopathy (EO); animals with EO+CMT-28 1 mg/kg body weight; animals with EO+CMT-67 1 mg/kg body weight; animals with EO+BioR 1mg/kg body weight; animals with EO+BioR 2 mg/kg body weight; animals with EO+CMT-28+BioR (1 mg/kg body weight each); animals with EO+BioR+CMT-67 (1 mg/kg body weight each). In physiological conditions the ontogenetic modifications of the bone collagen and HYP content are statistically conclusive and of the same orientation, the maximum concentration was identified in adult animals and the minimum at advanced stages of postnatal ontogenesis regardless of sex. Experimental osteopathy is characterized by age and sex dependent changes of the collagen and hydroxyproline concentrations in bone, the most significant changes being revealed in young females. Copper coordination compounds, BioR and their combinations increase the turnover of the collagen in bone in EO that is accompanied by decrease of collagen and increase of the HYP concentration that is probably a compensatory mechanism oriented to the replacement of the damaged collagen and the restoration of its normal nanostructure with the recovery of the bone.
METODĂ NOUĂ DE APRECIERE A TOXICITĂŢII SUBSTANŢELOR CHIMICE
(Imprimt Plus, 2018-09-21) Toderaș, Ion; Gulea, Aurelian; Gudumac, Valentin; Roșcov, Elena; Garbuz, Olga
We developed a new invention that relates to method for assessing the toxicity of chemical substances.The method of the invention includes the preparation of the culture of Paramecium caudatum, adding to the samples investigated to test chemicals in various concentrations, incubating the sample to be studied and control the addition of colourant 3-amino-7-dimethylamino-2-methylphenazine hydrochloride, incubation with subsequent addition of solution of formalin, centrifuging the sample, removing the supernatant, adding the solution of hydroxide of sodium, determine the absorbance using a spectrophotometer, followed by calculating the percentage of paramecii viability and determine the lethal concentration (LC50) at the same time as the value of the concentration LC50 is small, the toxicity of the tested substance is higher.
MICROMOLECULAR INHIBITORS OF SUPEROXIDE RADICALS
(2021) Andronache, Lilia; Pantea, Valeriana; Gulea, Aurelian; Șveț, Inna; Graur, Vasilii; Matcovschi, Valerii; Gamaniuc, Marina; Gudumac, Valentin
Background: Currently, there is a growing interest in new copper (Cu2+) heterocyclic coordination compounds (CC), isothiosemicarbazide derivates, which demonstrated multiple beneficial properties, but their effect on reactions with free radicals such as the superoxide radical has not been investigated. Material and methods: The action of new micromolecular complexes of copper (Cu2+) chloride and bromide with methyl n- (prop-2-en-1-yl) -2- (pyridin2-ylmethylidene) hydrazine carbimidothioate on capturing activity of the superoxide radical was determined by the spectrophotometric method in vitro experiments. Results: It was established that the micromolecular complexes of copper (II) chloride and bromide with methyl n-(prop-2-en-1-yl)-2-(pyridin-2ylmethylidene) hydrazine carbimidothioate have been found to possess strong superoxide radical inhibitor properties when interacting with a superoxide radical. In addition to this, the IC50 of the studied compounds depends on the nature of the acid-ligand in the internal sphere of the complex and increases in the following sequence: Cl-–Br-. Conclusions: The established property of mentioned compounds is new, because their use as micromolecular inhibitors of superoxide radicals has not been described so far. The synthesized CC expand the arsenal of superoxide radical inhibitors with high biological activity. Their possible significance for the development of new treatment strategies for diseases associated with the overproduction of superoxide radicals is discussed.
MODIFICĂRILE SISTEMULUI GLUTATIONIC ERITROCITAR ÎN NORMĂ ŞI ASTM BRONŞIC ASOCIAT SUB ACŢIUNEA UNOR COMPUŞI BIOLOGICI ACTIVI AUTOHTONI
(2016) Pantea, Valeriana; Tagadiuc, Olga; Procopișin, Larisa; Andronache, Lilia; Gulea, Aurelian; Gudumac, Valentin
S-a studiat infl uenţa compuşilor biologic activi (CBA) autohtoni - CMD-4, CMD-8, CMJ-33 şi CMJ-23 asupra indicilor sistemului glutationic eritrocitar (GSH, GR, GPO, GST, G-6-PDH) in vitro în condiţii normale şi în astmul bronşic (AB) de severitate diferită. S-a stabilit că CBA autohtoni exercită efecte modulatoare relevante asupra pricipalelor enzime ale metabolismului GSH, preponderent stimulatoare, fapt ce ar putea fi apreciat ca un răspuns pozitiv ce poate proteja celulele de efectele toxice ale stresului oxidativ specifi c pentru AB. Indicii studiați pot fi folosiți ca biomarcheri informativi pentru monitorizarea procesului patologic și aprecierea efi cienţei preparatelor noi la restabilirea biochimică şi funcţională a sistemelor de protecție celulare în AB și diverse leziuni pulmonare.
NEW INHIBITORS OF GLYCATION AND OF THE FORMATION OF ADVANCED GLYCATION END PRODUCTS
(Academia de Ştiinţe a Moldovei, 2015) Andronache, Lilia; Gudumac, Valentin; Gulea, Aurelian; Tagadiuc, Olga; Garbuz, Olga; Pantea, Valeriana
NEW INORGANIC AND ORGANIC MOLECULAR INHIBITORS OF CANCER CELLS PROLIFERATION, THE MECHANISMS OF ACTION
(2021) Garbuz, Olga; Gulea, Aurelian; Gudumac, Valentin
The aim of the thesis: elucidation of the effect of the new molecular inhibitors based on organic and complex compounds on the proliferation of human cancer cell lines in comparison with such anticancer drugs as doxorubicin and cis-dichlorodiammineplatinum; determination of the inhibitors action mechanism.
NICKEL(II) COMPLEXES WITH PENTANE-2,4-DIONE BIS(4-ALLYLTHIOSEMICARBAZONE)
(2020) Gulea, Aurelian; Graur, Vasilii; Ciumacov, Iurie; Petrenko, Peter; Garbuz, Olga; Țapcov, Victor; Gudumac, Valentin
Reaction of pentane-2,4-dione with N-(prop-2-en-1-yl)hydrazinecarbothioamide at a 1: 2 molar ratio in ethanol resulted in the formation of a pyrazole derivative. The latter reacted with nickel perchlorate at a 1: 1 molar ratio to form the nickel complex with pentane-2,4-dione bis(4-allylthiosemicarbazone). The same type of nickel complex was obtained as a result of N-(prop-2-en-1-yl)hydrazinecarbothioamide reaction with pentane-2,4-dione and nickel nitrate at a 2: 1: 1 molar ratio. Antimicrobial, antifungal, antioxidant, and anticancer activities of the obtained compounds were studied.
NOVEL 2-FORMYLPYRIDINE 4-ALLYL-S- METHYLISOTHIOSEMICARBAZONE AND ZN(II), CU(II), NI(II) AND CO(III) COMPLEXES: SYNTHESIS, CHARACTERIZATION, CRYSTAL STRUCTURE, ANTIOXIDANT, ANTIMICROBIAL AND ANTIPROLIFERATIVE ACTIVITY
(2019) Balan, Greta; Usataia, Irina; Graur, Vasilii; Ciumacov, Iurie; Petrenko, Peter; Gudumac, Valentin; Gulea, Aurelian; Pahonțu, Elena; Burduniuc, Olga
New zinc (II), copper (II), nickel (II) and cobalt (III) complexes, [Zn (HL)2]I2 (1), [Cu (HL)Cl2] (2), [Cu (HL)Br2] (3), [Cu (HL)(H2O)2](ClO4)2 (4), [Ni (HL)2]I2·H2O (5), [Co(L)2]Cl (6), [Co(L)2]NO3 (7), [Co(L)2]I·[Co(L)2](I3) (8) were obtained with 2-formylpyridine 4-allyl-S-methylisothiosemicarbazone (HL). The isothiosemicarbazone ligand was characterized by NMR (1H and 13C), IR spectroscopy and X-ray diffraction. All the complexes were characterized by elemental analysis, IR, UV–Vis, ESI-MS spectroscopy, molar conductivity, magnetic susceptibility measurements. X-ray diffraction analysis on the monocrystal and powder elucidated the structure of the complexes 1, 5, 7 and 8. The ligand and the complexes were tested for their antioxidant and antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Candida albicans. Also, the antiproliferative properties of these compounds on human leukemia HL-60, human cervical epithelial HeLa, human epithelial pancreatic adenocarcinoma BxPC-3, human muscle rhabdomyosarcoma spindle, large multinucleated RD cells and normal MDCK cells have been investigated. The nickel complex 5 and cobalt complexes 6, 7 showed promising antiproliferative activity and low toxicity.
NOVEL 2-FORMYLPYRIDINE 4-ALLYL-S-METHYLISOTHIOSEMICARBAZONE AND ZN(II), CU(II), NI(II) AND CO(III) COMPLEXES: SYNTHESIS, CHARACTERIZATION, CRYSTAL STRUCTURE, ANTIOXIDANT, ANTIMICROBIAL AND ANTIPROLIFERATIVE ACTIVITY
(John Wiley & Sons Ltd, 2020) Balan, Greta; Burduniuc, Olga; Usataia, Irina; Graur, Vasilii; Chumakov, Yurii; Petrenko, Peter; Gudumac, Valentin; Gulea, Aurelian; Pahontu, Elena
New zinc (II), copper (II), nickel (II) and cobalt (III) complexes, [Zn (HL) 2 ]I 2 (1), [Cu (HL)Cl 2 ](2), [Cu (HL)Br 2 ](3), [Cu (HL)(H 2 O) 2 ](ClO 4 ) 2 (4), [Ni (HL) 2 ]I 2 H 2 O(5), [Co(L) 2 ]Cl (6), [Co(L) 2 ]NO 3 (7), [Co(L) 2 ]I[Co(L) 2 ](I 3 ) (8) were obtained with 2-formylpyridine 4-allyl-S-methylisothiosemicarbazone (HL). The isothiosemicarbazone ligand was characterized by NMR ( 1 H and 13 C), IR spectroscopy and X-ray diffraction. All the complexes were character- ized by elemental analysis, IR, UV–Vis, ESI-MS spectroscopy, molar conductiv- ity, magnetic susceptibility measurements. X-ray diffraction analysis on the monocrystal and powder elucidated the structure of the complexes 1,5, 7and 8. The ligand and the complexes were tested for their antioxidant and antimi- crobial activity against Staphylococcus aureus,Escherichia coli,Klebsiella pneumoniae and Candida albicans. Also, the antiproliferative properties of these compounds on human leukemia HL-60, human cervical epithelial HeLa, human epithelial pancreatic adenocarcinoma BxPC-3, human muscle rhabdomyosarcoma spindle, large multinucleated RD cells and normal MDCK cells have been investigated. The nickel complex 5and cobalt complexes 6,7showed promising antiproliferative activity and low toxicity
STUDY OF MAGNETIC AND ANTIOXIDATIVE PROPERTIES OF SOME BIOMETAL COORDINATION COMPOUNDS OF o-VANILLIN ISONICOTINOYLHYDRAZONE
(Academia de Ştiinţe a Moldovei, 2015) Gulea, Aurelian; Tsapkov, Victor I.; Bîrcă, Maria; Cotovaia, Aliona; Gudumac, Valentin; Garbuz, Olga; Petcenco, I.; Malic, Elena
SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-FORMYLPYRIDINE N(4)-ALLYL-3-SELENO-SEMICARBAZONE AND ITS COPPER COORDINATION COMPOUND
(2015) Graur, Vasilii; Garbuz, Olga; Zariciuc, Elena; Gudumac, Valentin; Gulea, Aurelian
The paper presents the synthesis of the 2-formylpyridine N(4)-allyl-3-seleno-semicarbazone that was studied using NMR spectroscopy. This ligand was used for the synthesis of a copper(II) chloride coordination compound. The study of antimicrobial and antifungal activities showed that these substances possess bacteriostatic and bactericidal activities towards a series of gram-positive and gram-negative bacteria and fungi in the range of concentration 0.7-500μg/mL. The activity of the copper(II) coordination compound towards gram-negative microorganisms significantly exceeds the activity of the ligand. The antioxidant activity of the synthesized selenosemicarbazones exceeds the activity of the coordination compound. These substances inhibit proliferation of MeW-164, HL-60 and HeLa tumor cells. 16 references, 1 table, 7 schemes
SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-FORMYLPYRIDINE N(4)-ALLYL-3-SELENO-SEMICARBAZONE AND ITS COPPER COORDINATION COMPOUND
(2015) Graur, Vasilii; Garbuz, Olga; Zariciuc, Elena; Gudumac, Valentin; Gulea, Aurelian
The paper presents the synthesis of the 2-formylpyridine N(4)-allyl-3-seleno-semicarbazone that was studied using NMR spectroscopy. This ligand was used for the synthesis of a copper(II) chloride coordination compound. The study of antimicrobial and antifungal activities showed that these substances possess bacteriostatic and bactericidal activities towards a series of gram-positive and gram-negative bacteria and fungi in the range of concentration 0.7-500μg/mL. The activity of the copper(II) coordination compound towards gram-negative microorganisms significantly exceeds the activity of the ligand. The antioxidant activity of the synthesized selenosemicarbazones exceeds the activity of the coordination compound. These substances inhibit proliferation of MeW-164, HL-60 and HeLa tumor cells. 16 references, 1 table, 7 schemes
SYNTHESIS AND BIOLOGICAL ACTIVITY OF COPPER, NICKEL, AND COBALT COORDINATION COMPOUNDS OF CONDENSATION PRODUCTS OF SOME CHALCONES WITH 4-PHENYLTHIOSEMICARBAZIDE
(Academia de Ştiinţe a Moldovei, 2015) Tsapkov, Victor I.; Boeva, Maria; Botnaru, Maria; Garbuz, Olga; Gulea, Aurelian; Gudumac, Valentin