"The effects of a new chromenyl-methylenethiazolidine-2,4-dione in alleviating oxidative stress in a rat model of streptozotocin induced diabetes   "

Chis, Irina Camelia; Clichici, Andra; Simedrea, Ramona; Moldovan, Remus; Lazar, Viorica Leordean; Clichici, Simona; Oniga, Ovidiu; Nastasă, Cristina; Pharmacy, Victor Babeş street

doi:10.24193/subbchem.2018.4.08

Cited by 2 publications

(2 citation statements)

References 15 publications

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“…The study of TZD hybrids from the point of view of their in silico design, chemical synthesis, investigation of their antitumor, antidiabetic, antiinflammatory, antioxidant and antimicrobial activities, has enabled the discovery of very promising and druglike candidates. Considering the aspects presented above and our previous experience in the synthesis of hybrid thiazolidine-2,4-dione derivatives and in the investigation of their antimicrobial [30,36], anti-inflammatory [38], antioxidant [18,31] and antitumour [37] potential, our aim in this work was to obtain new symmetric bis-thiazolidine-2,4-diones and to evaluate, in silico, their capacity to inhibit Raf and Ras oncoproteins, as potential antitumor drug candidates.…”

Section: Introductionmentioning

confidence: 99%

SYNTHESIS AND IN SILICO APPROACHES OF NEW SYMMETRIC BIS-THIAZOLIDINE-2,4-DIONES AS Ras AND Raf ONCOPROTEINS INHIBITORS

Crisan¹

2023

FARMACIA

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Millions of people die of cancer every year, all around the world. Unfortunately, the conventional chemotherapy is associated with some pharmacotoxicological inconveniences. Due to this fact, the discovery of new anticancer agents is needed, with better activity and selectivity of action at the level of the tumour microenvironment. Thiazolidinediones, known mainly as antihyperglycemic substances, are more and more investigated for their antiproliferative properties. Prompted by our interest and experience in synthesizing new small molecules with biological potential, we present here the chemical synthesis of a new series of symmetric bis 5-arylidene-thiazolidine-2,4-diones. The molecular docking performed on K-Ras, N-Ras and B-Raf oncoproteins revealed a promising binding affinity to K-Ras, especially for the compounds 5b and 5h. A molecular dynamics simulation was made for the complexes of the two compounds with K-Ras oncoprotein, to predict the stability of the resulted complexes. RezumatMilioane de oameni mor anual din cauza cancerului, în întreaga lume. Din păcate, chimioterapia convențională este asociată cu unele inconveniente de ordin farmacotoxicologic. Din cauza acestui neajuns, este necesară descoperirea de noi agenți anticanceroși, cu activitate superioară și selectivitate de acțiune la nivelul micromediului tumoral. Tiazolidindionele, cunoscute în principal ca substanțe antihipergliceminate, sunt din ce în ce mai mult cercetate pentru proprietățile lor antiproliferative. Ca urmare a interesului și a experienței noastre în sinteza unor noi molecule mici cu potențial biologic, prezentăm aici sinteza chimică a unei noi serii de bis-5-ariliden-tiazolidin-2,4-dione. Andocarea moleculară realizată pe oncoproteinele K-Ras, N-Ras și B-Raf a arătat o afinitate de legare de K-Ras promițătoare, în special pentru compușii 5b și 5h. O simulare de dinamică moleculară a fost realizată pentru aceste două substanțe, pentru a prezice stabilitatea complecșilor formați cu oncoproteina K-Ras.

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Section: Introductionmentioning

confidence: 99%

SYNTHESIS AND IN SILICO APPROACHES OF NEW SYMMETRIC BIS-THIAZOLIDINE-2,4-DIONES AS Ras AND Raf ONCOPROTEINS INHIBITORS

Crisan¹

2023

FARMACIA

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“…The endothelial dysfunction (ED) that occurs in type 1 diabetes mellitus (T1DM) involves numerous and diverse pathogenetic mechanisms including inflammation, hyperglycaemia, production of reactive oxygen species (ROS) and of reactive nitrogen species (RNS), the decrease of nitric oxide (NO) availability or dyslipidemia [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 ]. Endothelial dysfunction is characterised by altered endothelial-dependent relaxation (EDR) produced by the decreased NO levels in the vessel wall [ 8 , 9 , 10 ], a process that leads to micro- and macrovascular complications, increasing significantly the morbidity and mortality in T1DM [ 1 ].…”

Section: Introductionmentioning

confidence: 99%

The Beneficial Effect of Swimming Training Associated with Quercetin Administration on the Endothelial Nitric Oxide-Dependent Relaxation in the Aorta of Rats with Experimentally Induced Type 1 Diabetes Mellitus

et al. 2023

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Type 1 diabetes mellitus is related to the vascular oxidative and nitrosative stress, the trigger for atherosclerosis and cardiovascular complications. The effects of moderate swimming training associated with quercetin oral administration were evaluated in aorta of rats with experimentally induced type 1 diabetes mellitus (T1DM), by analysing the nitric oxide-endothelial dependent relaxation (NO-EDR). T1DM rats received daily quercetin 30 mg/kg and followed the protocol of 5-weeks swimming exercise (30 min/day; 5 days/week). Aorta relaxation to acetylcholine (Ach) and sodium nitroprusside (SNP) were measured at the end of the experiment. Ach-induced endothelial dependent relaxation was significantly decreased in phenylephrine (PE) pre-contracted aorta of diabetic rats. Swimming exercise with quercetin administration preserved Ach-induced EDR but did not have any impact on SNP-induced endothelium-independent relaxation in the diabetic aorta. These findings suggest that quercetin administration associated with moderate swimming exercise could improve the endothelial NO-dependent relaxation in the aorta of rats with experimentally induced type 1 diabetes mellitus, showing that this therapeutical combination may improve and even prevent the vascular complications that occur in diabetic patients.

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"The effects of a new chromenyl-methylenethiazolidine-2,4-dione in alleviating oxidative stress in a rat model of streptozotocin induced diabetes "

Cited by 2 publications

References 15 publications

SYNTHESIS AND IN SILICO APPROACHES OF NEW SYMMETRIC BIS-THIAZOLIDINE-2,4-DIONES AS Ras AND Raf ONCOPROTEINS INHIBITORS

SYNTHESIS AND IN SILICO APPROACHES OF NEW SYMMETRIC BIS-THIAZOLIDINE-2,4-DIONES AS Ras AND Raf ONCOPROTEINS INHIBITORS

The Beneficial Effect of Swimming Training Associated with Quercetin Administration on the Endothelial Nitric Oxide-Dependent Relaxation in the Aorta of Rats with Experimentally Induced Type 1 Diabetes Mellitus

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