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Open access

Mohammed M. Safhi, Mohammad Firoz Alam, Gulrana Khuwaja, Sohail Hussain, Mohammed Hakeem Siddiqui, Farah Islam, Ibrahim Khardali, Rashad Mohammed Al-Sanosi, Hassan A. Alhazmi, Andleeb Khan and Fakhrul Islam

Abstract

Cathinone, the active principle of khat (Catha edulis), stimulates, excites and produces euphoric feelings in khat users. Locomotor and rearing activities, either individual or in groups, of male Swiss albino mice were decreased significantly compared to the control. Motor coordination tests (rotarod, rope climb and grip tests) have shown decreased motor performance in the mice treated with cathinone compared to the control. The elevated plus maze test has shown significant anxiety in the mice compared to the control. Contents of dopamine and its metabolite, homovanillic acid, were increased in the limbic areas compared to the control group. In contrast, contents of 3,4-dihydroxyphenyl acetic acid were depleted significantly and dose dependently compared to the control group in the limbic areas of mice. In conclusion, natural cathinone has depleted motor coordination, accelerated anxiety in mice and altered the contents of dopamine and its metabolites.

Open access

Souad Hamimed, Nadji Boulebda, Hocine Laouer and Abdelmalik Belkhiri

Abstract

Introduction. The alcohol extract of Pellitory (Anacyclus pyrethrum) roots has been previously shown to exert anticancer activities on the Human Colorectal Cancer Cell Line (HCT) by targeting apoptosis, metastasis and cell cycle arrest. However, the nature of the cytotoxic molecules associated with this activity remains unexplored.

Aims. This study aims to reinvestigate Pellitory root extract as regard to its cytotoxic activity and to proceed to a bioguided fractionation to explore its active fraction and to give new insight in their phytochemical constituents.

Methods. Powdered roots were subjected to repeated extraction with Petroleum ether (Pe), Chloroform (Ch), Ethyl acetate (Ea) and Methanol (Me). Pellitory extracts were then screened for cytotoxic activity using the Brine Shrimp Lethality (BSL) bioassay.

Results. Ea extract exhibited a marked cytotoxic activity, with LC50 of 249.26 μg/mL in the BSL bioassay. The remaining extracts (Pe,Ch,Me) treated groups exhibited no or low mortality in the range of tested concentrations (1-1000 µg/mL). BSL assay-guided chromatographic fractionation of Ea active Extract revealed a highly cytotoxic fraction (F11) with LC50 of 42.5 µg/mL. Multistep purifications of the active F11 fraction afforded four alkamides, namely N-isobutyldeca-2,4-dienamide or Pellitorine (I), N-propyldodeca- -2,8-dienamide (II), N-isobutyltetradeca-2,4-dienamide (III) and N-propylnona-2,5- -dienamide (IV).

Conclusions. This study suggests that cytotoxic activity is localized mainly in the ethyl acetate extract (Ea) of pellitory roots. BSL assay fractionation of this active extract leads to the isolation of four alkamides, including pellitorine (I). While this isobutyl alkamide has previously shown strong cytotoxic activities against human cancer cell lines, the other compounds (II to IV) were not previously reported as cytotoxic. Subsequently, the isolated alkamides will be considered in future study as candidates for in depth in-vitro evaluation of their cytotoxicity against cancer and normal cell lines. Finally, through this study, BSL assay demonstrate again its usefulness as bench-top assay in exploring plant extracts for cytotoxic compounds.

Open access

Angeliki Moisidou

Abstract

A statistical analysis has been conducted with the aim to elucidate the effect of health care systems (HSs) on health inequalities assessed in terms of (a) differential access to health care services and (b) varying health outcomes among different models of HSs in EU-15 [(Beveridge: UK, IE, SE, FI, DK), (Bismarck: DE, FR, BE, LU, AT, NL), (Southern European model: GR, IT, ES, PT)]. In the effort to interpret the results of the empirical analysis, we have ascertained systematic differences among the HSs in EU-15. Specifically, it is concluded that countries with Beveridge HS can be characterized more efficient (than average) in the most examined correlations, showing particularly high performance in the health sector. Similarly, countries with Bismarck HS record fairly satisfactory performance, but simultaneously they display more structural weaknesses compared with the Beveridge model. In addition, our empirical analysis has shown that adopting Bismarck model requires higher economic cost, compared with the Beveridge model, which is directly financed by taxation. On the contrary, in the countries with Southern European HS, the lowest performances are generally identified, which can be attributed to the residual social protection that characterizes these countries. The paper concludes with a synthesis of the empirical findings of our research. It proposes some directions for further research and presents a set of implications for policymakers regarding the planning and implementation of appropriate policies in order to tackle health inequality within HSs.

Open access

Katayoon Karimzadeh

Abstract

Large amounts of valuable waste are produced during sea food processing. This has a great potential for conversion to biologically active proteins and polysaccharides. Among these compounds, sulfated polysaccharides have been considered due to their many biological properties.

The present work was conducted to study anticoagulant activities and angiotensin-I converting enzyme (ACE) inhibitory effects of glycosaminoglycans (GAGs) extracted from the cartilage of sturgeon (Acipenser persicus). The enzymatic extraction of sturgeon cartilage was performed in the presence of cetylpyridinium chloride salt. The structure was characterized via electron microscope and Fourier transform infrared spectroscopy (FTIR) analysis. Herein, ACE inhibitory and anticoagulant properties of extracted GAGs were determined.

The amount of GAGs was 6.8±1.3% of cartilage dry weight. GAGs showed good activity in ACE inhibitory – with a highest level of 85.7%. The derived anticoagulant activity indexes, APPT (activated partial thromboplastin time) and TT (Thrombin time) of the extracted polysaccharide showed a prolonging of clotting time, compare to control.

The results of this study revealed that the cartilage extracted GAGs possess promising ACE inhibitory properties and anticoagulant effects. Thus, the product can be substituted for blood reducing drugs and antithrombotic agents at least in laboratory conditions.

Open access

Olajumoke A. Oyebode, Ochuko L. Erukainure, Neil A. Koorbanally and Md. Shahidul Islam

Abstract

In this study, we identified bioactive compounds from the ethanolic extracts of the leaves, stem bark and root bark of Acalypha wilkesiana through GC-MS analysis and investigated the effects of these extracts on some of the enzymes linked to type 2 diabetes. Plant parts were extracted sequentially with ethyl acetate, ethanol and water. GC-MS analysis revealed the presence of long-chain alkyl acids, esters, ketones and alcohols including phytol and phytol acetate along with some secondary metabolites such as xanthone, vitamin E and various types of sterols including stigmasterol, campesterol and sitosterol. Ethanolic extracts of all the parts showed a dose- -dependent inhibition of α-glucosidase and α-amylase activity. The extracts also demonstrated anti-lipase activity. The ethanolic extract of root bark showed the highest inhibition of enzymes compared to other extracts. The EC50 values (concentrations for 50 % inhibition) of α-glucosidase, α-amylase and lipase inhibition were 35.75 ± 1.95, 6.25 ± 1.05 and 101.33 ± 5.21 μg mL-1, resp. The study suggests that A. wilkesiana ethanolic extracts have the ability to inhibit the activity of enzymes linked to type 2 diabetes. Further studies are needed to confirm the responsible bioactive compounds in this regard.

Open access

J. Veteskova, M. Obsivan, Z. Kmecova, M. Radik, J. Srankova, E. Malikova, J. Klimas and P. Krenek

Abstract

Aim: Chemokine stromal cell derived factor-1 (SDF-1) plays an important role in many processes such as apoptosis, proliferation, migration and angiogenesis, and these effects are mediated mostly by the receptor CXCR4. The aim of this study was to determine the expression of SDF-1 and CXCR4 in the ventricles of rats with monocrotaline-induced pulmonary hypertension.

Methods: 10–12 weeks old male Wistar rats were injected with monocrotaline (s. c., 60mg/kg; MON) or vehicle (CON). Rats were sacrificed 1 week (1W-MON, 1W-CON), 2 weeks (2W-MON, 2W-CON) and 4 weeks after monocrotaline administration (4W-MON, 4W-CON). Gene expression of SDF-1 and CXCR4 was determined by qRT-PCR.

Results: We observed a decrease in the SDF-1 expression on mRNA level in the right ventricle in 2W-MON and 4W-MON rats without any changes in the left ventricles and a decrease in CXCR4 expression in 1W-MON in both ventricles with an increase of CXCR4 expression in 4W-MON in the left ventricle (*P ˂ 0.05).

Conclusion: SDF-1/CXCR4 axis is affected in both ventricles of rats with monocrotaline model of pulmonary hypertension.

Open access

M. Kocmálová, J. Ľupták, J. Barboríková, I. Kazimierová, M. Grendár and J. Šutovský

Abstract

Background: This study specified the role of several significant ion channels regulating the metabolism of calcium ions in contraction and relaxation of human detrusor muscle in order to identify possible target for future drugs that are capable of treating diseases resulting from impaired detrusor activity, e.g. overactive bladder. Although this disease can be successfully treated with muscarinic receptor antagonists or β3 agonist, many patients may not be suitable for chronic therapy, especially due to the relatively high side effects of the treatment.

Material and Methods: The study used the isolated detrusor tissue samples, which were obtained from the macroscopic healthy tissue of urinary bladder from 19 patients undergoing a total prostatectomy because of localized prostate cancer. Each biological sample was prepared into 8 strips. We used oxybutynin and mirabegron as control drugs and several blockers of specific subtypes calcium and potassium ion channels as tested substances. The contractility of bladder was investigated by an organ tissue bath method in vitro and contraction was induced by carbachol.

Results: The amplitude of contraction was successfully decreased by positive control drugs and, from tested agents, the comparable effect had the substance capable of influencing IP3 receptors and Orai-STIM channels and combination consisting of drugs possessing an inhibitory effect on IP3 receptors, L- and T-type voltage-gated calcium channels and Orai-STIM channels.

Conclusion: The present work represents a new finding about handling Ca2+ in urinary bladder contraction and pointed to a dominant role of IP3 receptor-mediated pathway in the regulation of Ca2+ metabolism, which may represent a future strategy in pharmacotherapy of impaired detrusor activity.

Open access

Z. Kmecova, E. Malikova, B. Zsigmondova, M. Radik, J. Veteskova, M. Marusakova, P. Krenek and J. Klimas

Abstract

Aim: Nitric oxide signalling pathway showed to be one of the crucial factors in the treatment and pathogenesis of pulmonary arterial hypertension. The aim of this study was to determine the effect of administration of inorganic nitrate, NaNO3, on the expression of caveolin-1 and its phosphorylated isoform (pTyr14Cav-1) in lungs in the experimental model of monocrotaline induced pulmonary hypertension.

Methods: 10 weeks old male Wistar rats were subcutaneously injected with 60 mg/kg dose of monocrotaline (MCT) or vehicle (CON). Twelve days after the injection, part of the MCT group was receiving 0.3 mM NaNO3 (MCT+N0.3) daily in the drinking water and rest was receiving 0.08% NaCl solution. Four weeks after MCT administration, the rats were sacrificed in CO2. Protein expression in lungs was determined by western blot.

Results: We observed a significant decrease in the caveolin-1 expression and a significant shift towards the expression of pTyr14Cav-1 in the group treated with nitrate (p < 0.05).

Conclusion: NaNO3 administration affected the expression of caveolin-1 and the ratio of its active (phosphorylated) isoform increased.

Open access

M. Sasváriová, B. Tyukos-Kaprinay, L. Salvaras, K. Belovičová, E. Bögi, V. Knezl, M. Barteková, T. Stankovičová and M. Dubovický

Abstract

A number of pregnant women all over the world suffer from depression and are treated during gestation with antidepressants, mostly with selective serotonin reuptake inhibitors or selective serotonin and norepinephrine reuptake inhibitors. Exposure to prenatal stress is also a great risk factor for a developing fetus and could be responsible for altered fetal development or various neurobehavioral disturbances of a child. Administration of selective serotonin and norepinephrine reuptake inhibitor venlafaxine is associated with various cardiovascular adverse effects, such as tachycardia, increased blood pressure, arrhythmias and hypertensive crisis. The aim of this study was to focus on the effect of pre-gestational chronic mild unpredictable stress and/or administration of antidepressant venlafaxine (10 mg/kg/day, p. o.) on specific parameters, determining the function of the cardiovascular system of male and female rat offspring. Blood pressure and standard ECG were recorded in the offspring. Exposure to pre-gestational stress did not cause significant changes in the systolic, diastolic blood pressure and pulse frequency either in males or in females, compared to the unexposed control animals. Pre-gestational stress caused the shortening of QT interval and prolongation of QRS complex duration in males. On the other hand, in females, the effects of pre-gestational stress were potentiated by the administration of venlafaxine and resulted in elevated systolic and diastolic blood pressure, prolonged QT interval and shortened QRS complex duration, compared to the control. In conclusion, the female rat offspring are more sensitive to exposure to pre-gestational, to chronic mild unpredictable stress and venlafaxine.

Open access

D. Micháliková, B. Tyukos Kaprinay, B. Lipták, K. Švík, L. Slovák, R. Sotníková, Š. Bezek and Z. Gáspárová

Abstract

The aim of this study was to determine pharmacological possibilities of influencing the risk factors of metabolic syndrome (MetS). Hypertriacylglycerolemic (HTG) rats fed with high-fat-fructose diet (HFFD) were used as a model of the MetS. Wistar rats fed with standard diet were used as negative control group. HTG rats fed with HFFD for 8 weeks were used as positive control group. The effects of atorvastatin and SMe1EC2 were tested. The compounds were administered to the HTG rats after 5 weeks of HFFD, once a day for 3 weeks. After 8 weeks, the blood serum lipid profile and electrophysiology of neurotransmission in hippocampal sections were evaluated in vitro. SMe1EC2 and atorvastatin had a significant effect on total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-cholesterol) and atorvastatin had a significant effect on triacylglycerols (TGs). SMe1EC2 improved the long-term potentiation (LTP) course in the hippocampus.