7-amino-3-arylazo-6-cyano-2-methylpyrazolo[5,1-c][1,2,4]triazines

In this study, 2-arylhydrazone-3-ketiminobutyronitriles were synthesised and reacted with hydrazine hydrate to afford 5-amino-4-arylazo-3-methyl-1H-pyrazoles. These compounds were then diazotised and coupled with malononitrile to give pyrazolylazomalononitriles. Thirteen novel pyrazolo[5,1-c][1,2,4]triazine dyes were synthesised by heating pyrazolylazomalononitriles in glacial acetic acid and characterised by elemental analysis and spectral methods. The effect of varying pH and solvent upon the absorption ability of the dyes substituted with electron-withdrawing and electron-donating groups at their o-, m- and p-position was examined in detail

A comparative study on the therapeutic effects of silymarin and silymarin-loaded solid lipid nanoparticles on D-GaIN/TNF-?-induced liver damage in Balb/c Mice

Nanostructure mediated drug delivery is known to have a potential to improve drug bioavailability, apart from fostering release deviation of drug molecules and enabling precision drug targeting. Solid lipid nanoparticles (SLNs) have drawn great deal of the attention of scientists in ?nding a solution to minimize pharmaceutic limitations of the drugs used. Silymarin(Sm)has so far been used for treating diverse liver and gall bladder disorders, such as cirrhosis, hepatitis, and jaundice, and for protecting the liver against poisoning from chemical and environmental toxins on account of its antihepatotoxic and antioxidative properties. The present study aims to develop a novel silymarin-loaded solid lipid nanoparticle (SmloadedSLN) system with enhanced bioavailability and with an ability to provide excellent hepatic protection for poorly water-soluble drugs. Based upon our investigation results with apoptotic markers, PCNA and light microscopic ?ndings, it can be concluded that Sm-loaded SLN signi?cantly reduced D-GaIN/TNF?-induced hepatotoxicity, which suggested improved bioactivity compared to Sm. In conclusion, Sm-loaded SLN could be a useful system for the delivery of poorly water-soluble Sm, apart from providing favourable hepatic protection

Evaluation of the efficacy of curcumin in experimentally induced acute sinusitis in rats

PubMed: 27929603We investigated the possible beneficial effects of curcumin (CMN) in the treatment of sinusitis. An experimentally induced sinusitis model was created in rats, and the results were evaluated histologically. Thirty-two healthy, female Sprague Dawley rats weighing 270 to 310 g each, were randomly divided into four groups. Group 1 was the control group. In Groups 2 to 4, experimentally induced acute sinusitis was developed, and the rats in those groups were given saline, sulbactam-ampicillin, and CMN, respectively, for 10 days. Then all rats were dissected, and samples of sinus mucosa were taken. Histologic examination was performed via light microscopy. In the sinusitis + antibiotic group, values of inflammation, vascular congestion, vascular dilatation, and subepithelial glandular atrophy were significantly higher; and values of mucosal damage and cilia loss, and hyperplasia of goblet cells, were not significantly different from those in the control group. In the sinusitis + CMN group, values of inflammation, vascular congestion, and vascular dilatation were significantly higher; and values of mucosal damage and cilia loss, hyperplasia of goblet cells, and subepithelial glandular atrophy were not significantly different from those of the control group. Histologic examination revealed that in the sinusitis + CMN group, a nearly normal appearance of the epithelial tissue and reduced cellular inflammation in connective tissue were observed. Minimal vascular congestion in connective tissue remained. The efficacy of CMN in acute sinusitis may be related to its potent anti-inflammatory effects on modulation of various inflammatory cytokines. When low side effects are taken into account, CMN therapy may be a promising option in the treatment of acute sinusitis. © 2016 Vendome Group, LLC All rights reserved

Efficacy of Curcumin in the healing of paracentesis in rats

WOS: 000330916100021PubMed: 24355767Objectives: The present study was designed to investigate the possible beneficial effect of Curcumin (CMN) in healing of paracentesis in terms of wound thickness, sclerosis and closure by histological evaluation. To evaluate the efficacy of CMN, paracentesis was performed experimentally in the rats; and the results were presented histologically. Methods: Sixteen, each 270-310 g weighted, healthy Sprague-Dawley female rats were included into the study. In both groups, paracentesis was performed into the eardrum bilaterally. In Group 1 (Paracentesis + Saline Group), saline drop was applied; and in Group 2 (Paracentesis + Curcumin group), Curcumin drop treatment was applied. Paracentesis area did not healed bilaterally in two rats (one in Group 1 and one in Group 2). Therefore, these two rats were excluded from the study. Histological examination performed in 14 rats and 28 temporal bones on the 15th day after the completion of drop treatment and closure of the paracentesis-area and wound healing were evaluated according to the histological examination criteria: Thickening of the tympanic membrane (ThicTM); and sclerosis. Results: Both tympanic membrane thickening and sclerosis values of Paracentesis + Curcumin Group (Group 2) were significantly lower than those of the Paracentesis + Saline Group's (median: 2.0) (p = 0.001). Histological examination by light microscopy showed that in Paracentesis + Curcumin Group (Group 2), the structure of the tympanic membrane is near to the normal and decreased sclerosis was observed in connective tissue. Whereas in Paracentesis + Saline Group (Group 1), tympanic membrane thickening and connective tissue sclerosis were observed. Conclusions: Curcumin improves wound healing process in paracentesis of TM. By using Curcumin drops, the closured paracentesis area was observed near to the normal eardrum; and thickness of the TM and sclerosis were less than the control, showing the improved healing at 15th day. The possible mechanisms may be anti-inflammatory effect, improving collagen deposition, and increasing fibroblast and vascular density in wounds thereby enhancing impaired wound healing. (C) 2013 Elsevier Ireland Ltd. All rights reserved.Continuous Education and Scientific Research AssociationExcept data collection, preparation of this paper including designing and planning was supported by Continuous Education and Scientific Research Association

The investigation of the prenatal and postnatal alcohol exposure-induced neurodegeneration in rat brain: protection by betaine and/or omega-3

We aim to study the effect of neurodegeneration on the brain of rat pups caused by prenatal and postnatal ethanol exposure with modified liquid diet to elucidate protective effects of betaine and omega-3 supplementation. When ethanol is consumed during prenatal and postnatal periods, it may result in fetal alcohol syndrome (FAS) in the offspring

Curcumin and LOXblock-1 ameliorate ischemia-reperfusion induced inflammation and acute kidney injury by suppressing the semaphorin-plexin pathway

Aims: Ischemia/reperfusion (I/R) is one of the most important causes of acute kidney injury (AKI), a clinical syndrome with kidney dysfunction and high mortality rates. New diagnostic biomarkers need to be defined to better illuminate the pathophysiology of AKI. For the first time, we aim to investigate the protective effects of Curcumin which is known for its antioxidant and anti-inflammatory properties and 12/15 lipoxygenase inhibitor LOXblock-1 on I/R induced AKI by modulating inflammatory processes, oxidative stress, apoptosis and semaphorin-plexin pathway. Main methods: The rats were divided into five groups, with eight animals per group: Sham, I/R, I/R + DMSO (1%, i.p.), I/R + Curcumin (100 mg/kg, i.p.), I/R + LOXblock-1 (2 mu g/kg, i.p.). Key findings: The renal function biomarkers (BUN, CREA and UA) in serum were significantly increased in the I/R group. The inflammatory (TNF-alpha, IL-6 and MCP-1), apoptotic (CYCS and CASP3) and oxidative stress parameters (MDA, MPO, TAS and TOS) measured by ELISA were significantly increased in the I/R group. In histopathological analysis, it was observed that I/R caused serious damage to kidney tissue. SEMA3A was found to increase both serum level and mRNA expression in I/R group. It was observed that curcumin and LOXblock-1 reduce inflammatory processes, oxidative stress and apoptosis via the semaphorin-plexin pathway by both measurements and histopathological analysis. Curcumin was proved more effective than LOXblock-1 with its antioxidant feature in I/R injury. Significance: The current study reveals the protective effects of Curcumin and LOXblock-1 on acute kidney injury by suppressing SEMA3A as a new biomarker.Commission of Scientific Research Projects of Eskisehir Osmangazi University, Eskisehir, Turkey [2019-2344, 2019-1915]This study was supported by the Commission of Scientific Research Projects of Eskisehir Osmangazi University, Eskisehir, Turkey with the grant numbers: 2019-2344 and 2019-1915.WOS:0005607654000092-s2.0-85087120412PubMed: 3260381

Evaluation of the Efficacy of Curcumin in Experimentally Induced Acute Otitis Media in Rats

WOS: 000335494400004PubMed: 24642584Objectives: We investigated the effect of curcumin (CMN) in the treatment of experimentally induced acute otitis media (AOM) in rats. Method: Thirty-two Sprague-Dawley female rats were used, yielding 64 temporal bones. Group 1 was the control group. For groups 2 to 4, AOM was induced experimentally, and saline, antibiotics (sulbactam-ampicillin), or CMN were administered for 14 days to groups 2, 3, and 4, respectively. During the histological examination, thickening of the tympanic membrane, damage to the epithelium, inflammation, and sclerosis were evaluated. Results: The AOM+antibiotic and AOM+CMN groups exhibited reduced histological damage compared with the AOM+saline group. No significant differences in thickening of the tympanic membrane or damage to the epithelium or inflammation were observed between the AOM+antibiotic and the AOM+CMN groups. However, the sclerosis values of the AOM+CMN group were significantly lower than those of the AOM+antibiotic group. Conclusion: CMN treatment resulted in similar effects on the experimentally induced AOM model as did the antibiotic treatment. The efficacy of this treatment may be related to its effects on the production of various inflammatory cytokines. In light of the worldwide increase in antibiotic resistance and the mild side effects of CMN, we suggest that CMN therapy may be a promising option in AOM treatment

Potential protective effect of resveratrol on acoustic trauma: electron microscopy study

WOS: 000384168600022PubMed: 27608909OBJECTIVE: To investigate the potential preventive effect of resveratrol in rats exposed to acoustic trauma (AT). MATERIALS AND METHODS: In this experimental study, Wistar albino rats were divided into three groups: Group 1 (Control, n = 6), Group 2 (AT, n = 6), and Group 3 (resveratrol + AT). The rats in Group 2 were exposed to AT. The rats in Group 3 received resveratrol (300 mg/kg/day) via gavage for 7 days. On day 7, the rats were exposed to AT 10 min following resveratrol treatment. Histological sections of the cochleae were examined using light microscopy, transmission (TEM), and scanning electron microscopy (SEM). RESULTS: The cochlear hair cells, stereocilia, and Deiters' cells of the control group appeared normal in all microscopic evaluations. In Group 2, light microscopy revealed predominantly inner hair cell loss, although the outer hair cells were affected. TEM and SEM examination showed severe loss of stereocilia and SEM revealed stereocilia arranged in an asymmetric array. The cochlear structure in Group 3 appeared well preserved under the light microscope, and although TEM and SEM revealed stereocilia loss, the hair cells and stereocilia appeared near normal compared with those of Group 2. CONCLUSIONS: Resveratrol may have a protective effect against AT damage in the cochlea, most likely through its antioxidant activity. Our results may be useful for studies in humans exposed to AT and noise-induced hearing loss related to chronic exposure to occupational noise.Continuous Education and Scientific Research Association"With the exception of data collection, the preparation of this paper, including design and planning, was supported by the Continuous Education and Scientific Research Association." Only scientific support was provided; no grant or funding was received

Protective effect of betaine against skeleton muscle apoptosis in rats induced by chronic alcohol and statin consumption

AIM: The aim of the present study was to investigate the effect of apoptosis on rat skeletal muscle caused by chronic alcohol and statin consumption with modified liquid diet and to elucidate protective effects of betaine supplementation

The Potential Protective Effects of 2-aminoethyl Diphenylborinate against Inner Ear Acoustic Trauma: Experimental Study Using Transmission and Scanning Electron Microscopy

Shojaolsadati, Paria/0000-0001-8311-5425WOS: 000357533000002PubMed: 26223709OBJECTIVE: In this prospective experimental study, we investigated the preventive effects of 2-aminoethyl diphenylborinate (2-APB) in rats exposed to acoustic trauma (AT). Light microscopic, transmission electron microscopic (TEM), and scanning electron microscopic (SEM) examinations were performed. MATERIALS and METHODS: Eighteen healthy Wistar albino rats were divided into the following three groups: groups 1 (control), 2 (AT), and 3 (AT+APB). The rats in groups 2 and 3 were exposed to AT; in group 3 rats, 2-APB at 2 mg/kg was also administered, initially transperitoneally, after 10 min. RESULTS: During the light microscopic, TEM, and SEM examinations, the structures of the cochlear hair cells, stereocilia, and Deiter's cells were normal in the control group. In the AT group, the organ of Corti and proximate structures were damaged according to the light microscopic examination. During the TEM examination, intense cellular damage and stereocilia loss were detected, while during the SEM examination, extensive damage and stereocilia loss were observed. Decreased damage with preserved cochlear structure was detected during the light microscopic examination in the AT+APB group than in the AT group. During the TEM and SEM examinations, although stereocilia loss occurred in the AT+APB group, near-normal cell, cilia, and tectorial membrane structures were also observed in the AT+APB group compared with the AT group. CONCLUSION: 2-APB may have protective effects against AT damage of the cochlea. The main mechanism underlying this effect is the inhibition of the vasoconstriction of the cochlear spiral modiolar artery, thereby improving cochlear blood flow. We conclude that 2-APB may also be effective if used immediately following AT.Continuous Education and Scientific Research AssociationWith the exception of data collection, the preparation of this paper, including design and planning, was supported by the Continuous Education and Scientific Research Association. Only scientific support was provided; no grant or funding was received