Protective and therapeutic effects of okra seed in acute nontraumatic brain injury.

AIM: The purpose of this study was to examine the protective and therapeutic effects of okra (Abelmoschus esculentus [AE]) seed extract, with its known antioxidant, immunomodulatory, and anti-inflammatory properties, in an acetaminophen (paracetamol, N-acetyl- para-aminophenol)-induced model of hepatotoxicity and subsequent acute non-traumatic brain damage. MATERIAL AND METHOD: Forty male Wistar rats were randomly divided into five equal groups, control, paracetamol (P), okra seed extract (AE), okra seed extract + paracetamol (P + AE), and okra seed extract + paracetamol + N-acetyl cysteine (NAC) (P + AE + N). AE was administered by oral gavage through a gastric tube at 600 mg/kg/day for seven days. On the eighth day of the procedure, a single 1 g/kg dose of paracetamol and 300 mg/kg NAC were injected via the intraperitoneal route 1.5 h after AE administration. Rat tissue specimens were subsequently subjected to biochemical and histopathological analyses. Levels of markers such as S100 calcium-binding protein B (S100B), neuron-specific enolase (NSE), and matrix membrane metalloproteinase-9 (MMP-9) were investigated from rat serum specimens. Malondialdehyde (MDA) and superoxide dismutase (SOD) were also measured to determine oxidant-antioxidant status. RESULTS: S100B, NSE, MMP-9, MDA levels, and SOD enzyme activities were examined using biochemical methods. MDA levels were significantly lower in the P + AE group and MMP-9 levels in the AE, P + AE, and P + AE + N groups compared to the P group. Histopathological examination results supported the biochemical findings. CONCLUSION: Okra seed extract exhibits a protective and therapeutic effect against non-traumatic brain damage resulting from acute paracetamol intoxication. We think that this benefit of AE derives from its antioxidant property.

Electrophysiologic and anti-inflammatorial effects of cyclooxygenase inhibition in epileptiform activity.

The aim of our study is to investigate the electrophysiological and anti-inflammatory effects of diclofenac potassium on epileptiform activity, which is the liquid form of diclofenac, and frequently used clinically for inflammatory process by inhibiting cyclooxygenase enzyme (COX). Wistar rats aged 2-4 months were divided into Epilepsy, Diazepam, Diclofenac potassium, and Diazepam+diclofenac potassium groups. Diazepam and diclofenac potassium were administered intraperitoneally 30 min after the epileptiform activity was created with penicillin injected intracortically under anesthesia. After the electrophysiological recording was taken in the cortex for 125 min, interleukin-1ß (IL-1ß), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) were evaluated by the ELISA in the serums. No change was observed between the groups in serum IL-1ß, IL-6, and TNF-α values. It was observed that the co-administration of diclofenac potassium and diazepam at 51-55, 56-60, 61-65, 111-115, and 116-120 min was more effective in reducing spike amplitude than diclofenac potassium alone (p < 0.05). Single-dose diclofenac potassium did not have an anti-inflammatory effect in epileptiform activity but both diazepam and diclofenac potassium reduced the epileptiform activity.

The antiinflammatory and electrophysiological effects of fingolimod on penicillin-induced rats.

BACKGROUND: The fact that inflammation triggers epileptic seizures brings to mind the antiepileptic properties of anti-inflammatory drugs. OBJECTIVE: To investigate the electrophysiological and anti-inflammatory effects of fingolimod on an experimental penicillin-induced acute epileptic seizure model in rats. METHODS: Thirty-two male Wistar rats were divided into four groups: control (penicillin), positive control (penicillin + diazepam [5 mg/kg]), drug (penicillin + fingolimod [0.3 mg/kg]) and synergy group (penicillin + diazepam + fingolimod). The animals were anesthetized with urethane, and epileptiform activity was induced by intracortical injection of penicillin (500,000 IU). After electrophysiological recording for 125 minutes, IL-1ß, TNF-α, and IL-6 were evaluated by ELISA in the serum of sacrificed animals. RESULTS: During the experiment, animal deaths occurred in the synergy group due to the synergistic negative chronotropic effect of diazepam and fingolimod. Although not statistically significant, fingolimod caused a slight decrease in spike-wave activity and spike amplitudes in the acute seizure model induced by penicillin (p > 0.05). Fingolimod decreased serum IL-1ß (p < 0.05); fingolimod and diazepam together reduced IL-6 (p < 0.05), but no change was observed in serum TNF-α values. CONCLUSION: Even in acute use, the spike-wave and amplitude values of fingolimod decrease with diazepam, anticonvulsant and anti-inflammatory effects of fingolimod will be more prominent in chronic applications and central tissue evaluations. In addition, concomitant use of fingolimod and diazepam is considered to be contraindicated due to the synergistic negative inotropic effect.

ANTECEDENTES: O fato de a inflamação desencadear crises epilépticas traz à mente as propriedades antiepilépticas dos anti-inflamatórios. OBJETIVO: Investigar os efeitos eletrofisiológicos e anti-inflamatórios do fingolimode em um modelo experimental de crise epiléptica aguda induzida por penicilina em ratos. MéTODOS: Trinta e dois ratos Wistar machos foram divididos em quatro grupos: controle (penicilina), controle positivo (penicilina + diazepam [5 mg/kg]), droga (penicilina + fingolimode [0,3 mg/kg]) e grupo sinergia (penicilina + diazepam + fingolimode). Os animais foram anestesiados com uretano, e a atividade epileptiforme foi induzida por injeção intracortical de penicilina (500.000 UI). Após registro eletrofisiológico por 125 minutos, IL-1ß, TNF-α e IL-6 foram avaliados por ELISA no soro dos animais sacrificados. RESULTADOS: Durante o experimento, ocorreram mortes de animais no grupo sinérgico devido ao efeito cronotrópico negativo sinérgico do diazepam e do fingolimode. Embora não seja estatisticamente significativo, o fingolimode causou uma ligeira diminuição na atividade pico-onda e nas amplitudes pico no modelo de convulsão aguda induzida pela penicilina (p > 0,05). O fingolimode diminuiu a IL-1ß sérica (p < 0,05); fingolimode e diazepam juntos reduziram a IL-6 (p < 0,05), mas não foi observada alteração nos valores séricos de TNF-α. CONCLUSãO: Pensa-se que o efeito anticonvulsivante leve de uma dose única de fingolimode será mais proeminente em aplicações crônicas e em avaliações de tecidos centrais. Além disso, o uso concomitante de fingolimode e diazepam é considerado contraindicado devido ao efeito inotrópico negativo sinérgico.

Anti-inflammatory potential of liraglutide, a glucagon-like peptide-1 receptor agonist, in rats with peripheral acute inflammation.

The present study aimed to explore the possible anti-inflammatory actions of liraglutide (LRG), a glucagon-like peptide-1 (GLP-1) receptor agonist, and to compare with tramadol (TR) or LRG, and TR combination treatment by investigating the inflammatory signs such as pain hypersensitivity, edema, and fever in carrageenan (CG)-induced acute peripheral inflammation model in rats. The levels of several biomarkers for inflammatory status, angiogenesis, and oxidative stress were also measured in inflamed tissues. CG induced inflammation in the paws of rats identified by hypersensitivities, redness, edema and fever. LRG, significantly improved the hypersensitivity to mechanical (from 4 to 35.5 g) or cold (from 5 to 44.2 s) stimuli, reduced the edema (paw mass, from 2.54 to 1.85 g), and fever (paw temperature, from 33.6 to 27.3 °C). LRG dramatically suppressed the inflammatory signs when compared to those of TR. In addition, co-administration of TR and LRG resulted in further reduction of sensitivity to mechanical and cold stimuli. Anti-inflammatory potential of LRG altered depending on their inhibitory effects in the biomarkers of inflamed paws. Consequently, the suppressive actions of LRG in the inflammation induced hypersensitivities, edema, and fever, indicating that these drugs have significant anti-inflammatory potential with anti-hypersensitivities, anti-edema, and anti-pyretic effects. LRG with anti-inflammatory actions may be a highly promising therapeutic option for the management of inflammatory conditions or inflammatory-related various diseases.

Synthesis and biological evaluation of novel N,N'-diaryl cyanoguanidines acting as potent and selective carbonic anhydrase II inhibitors.

A series of novel N,N''-diaryl cyanoguanidines were synthesized by reacting diphenyl N-cyanocarbonimidate with sulfanilamide followed by treatment of the obtained cyano-O-phenylisourea with substituted aromatic amines. The newly prepared N,N''-diaryl cyanoguanidines showed a very interesting inhibition profile against four selected human carbonic anhydrase (CA, EC 4.2.1.1) isoforms, hCA I and hCA II (cytosolic), hCA IV (membrane-bound), and hCA IX (transmembrane). All these compounds showed a potent inhibition against isoform hCA II,with inhibition constants in the low nanomolar range, as well as a high selectivity for hCA II over hCA I, IV and IX. Since hCA II is an important drug target for antiglaucoma agents, these isoform-selective inhibitors may be considered of interest for further medicinal/pharmacologic studies.

Hepatoprotective and anti-inflammatory activities of Plantago major L.

OBJECTIVE: The aim of this study was to investigate anti-inflammatory and hepatoprotective activities of Plantago major L. (PM). MATERIALS AND METHODS: Anti-inflammatory activity: Control and reference groups were administered isotonic saline solution (ISS) and indomethacin, respectively. Plantago major groups were injected PM in doses of 5 mg/kg (PM-I), 10 mg/kg (PM-II), 20 mg/kg (PM-III) and 25 mg/kg (PM-IV). Before and three hours after the injections, the volume of right hind-paw of rats was measured using a plethysmometer. HEPATOPROTECTIVE ACTIVITY: The hepatotoxicity was induced by carbon tetrachloride (CCl4) administration. Control, CCl4 and reference groups received isotonic saline solution, CCl4 and silibinin, respectively. Plantago major groups received CCl4 (0.8 ml/kg) and PM in doses of 10, 20 and 25 mg/kg, respectively for seven days. Blood samples and liver were collected on the 8th day after the animals were killed. RESULTS: Plantago major had an anti-inflammatory effect matching to that of control group at doses of 20 and 25 mg/kg. It was found that reduction in the inflammation was 90.01% with indomethacin, 3.10% with PM-I, 41.56% with PM-II, 45.87% with PM-III and 49.76% with PM-IV. Median effective dose (ED50) value of PM was found to be 7.507 mg/kg. Plantago major (25 mg/kg) significantly reduced the serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels when compared to the CCl4 group. The histopathological findings showed a significant difference between the PM (25 mg/kg) and CCl4 groups. CONCLUSION: The results showed that PM had a considerable anti-inflammatory and hepatoprotective activities.

Evaluation of the anthelmentic activity of garlic (Allium sativum) in mice naturally infected with Aspiculuris tetraptera.

This study was performed to investigate the anthelmentic (nematodes) effect of garlic in Swiss albino mice naturally infected with Aspiculuris tetraptera. Natural infection was determined by the use of cellophane tape method on the perianal region and by the technique of centrifugal flotation of stool samples. The infected mice were divided into three groups; namely, Group 1: garlic treatment groups (n: 18), Group 2: positive control (treated with ivermectin, n: 19) and Group 3: untreated control group (n: 19). The mice in Group 1 were given orally freshly crushed garlic homogenates every day for 7 days. The animals in Group 2 were treated with ivermectin intramuscular at a dose of 0.2 mg/kg body weight. The mice in Group 3 received only serum physiologic orally. After 8 days of administrations, all mice were killed humanely using inhalation anaesthesia and then the parasites in the intestine were counted. It was observed that garlic and ivermectin were 91.24 % and 78.03 % effective against A. tetraptera in naturally infected mice, respectively. Results obtained from this study were compared statistically and differences were found to be significant (p<0.001). It was found that garlic was efficient along the duration of the treatment in mice. Garlic may be useful as an alternative treatment against nematode parasites in animals and human. This article includes a new research using Allium sativum anthelmentic effect on mouse and has been patented.

Comparison of the effects of local and uncontrolled levamisole preparations on mice naturally infected with Aspiculuris tetraptera.

This study was performed to compare effectiveness of two levamisole preparations prepared in two different countries (Iran and Turkey) in mice naturally infected with Aspiculuris tetraptera. For this purpose, natural infection was diagnosed using the cellophane tape method on the perianal region and centrifugal flotation technique on the feces of mice obtained from the experimental Animal Unit of the Faculty of Medicine, University of Yüzüncü Yil, Van. Mice naturally infected with A. tetraptera were then divided in three groups. Animals in Group 1 (8 animals) received levamisole prepared in Iran, animals in Group 2 (8 animals) received levamisole prepared in Turkey and animals in Group 3 (6 animals) were used as untreated controls. Both levamisole preparations were used in a 10 mg/kg dose. After drug administrations, stool samples of the animals in all groups were examined for seven days. On the eighth day, the animals were humanely destroyed using inhalation anesthesia. After euthanasia, parasites in the intestine were also counted. As a result; levamisole coming through uncontrolled border trade from Iran was 69.3% effective against A. tetraptera and the levamisole prepared in Turkey was 91.7% effective in naturally infected mice. Results obtained from this study compared statistically and the differences were found to be significant (p < 0.001).