76 research outputs found
Evaluation of the Antimicrobial Potential of Punica Granatum Leaves Hydro-methanolic Extract against Selected Pathogens
For a long time, extracts of Punica granatumhave been used in alternative and complementary medicine. The object of the present study was to evaluate the activity of Punica granatumleaves hydro-methanolic extract against some Gram-positive, Gram-negative bacteria and Candida albicans using agar diffusion assay.The leaves yielded 34.7% of raw semisolid extract after maceration in hydro-methanol (50:50 v/v) andevaporation.After lyophilization, the dry powder was reconstituted in Muller-Hinton broth to get a concentration of 128 mg/mL; from which further 5lower concentrations have been prepared (64, 32, 16, 8, and 4 mg/mL in Muller-Hinton Broth).The extract exhibitedconcentration-dependent activity against some Gram-positive bacteria, namely,Listeria monocytogenes (20.67 ± 0.82), Clostridium perfringens (17.33 ± 0.52), Staphyllococcus aureus (10.5 ± 0.55), Bacillus cereus (8.83 ± 0.41), and Enterococcus fecalis (6.33 ± 0.52);and against three Gram-negative bacteria, namely, Shigellaflexneri (13.33 ± 0.8), Vibrio parahaemolyticus(12.17 ± 0.42) and Proteus vulgaris (8.5 ± 0.55);as well as against Candida albicans (15.8 ± 0.98); (the values are in mm after 128 mg/mL extract). However, the extract was without any visible activity againstEscherichia coli, Salmonella typhimuriumand Klebsiellaaerogenes.The minimum inhibitory concentrations (MICs) against susceptible organisms were1.06 mg/mL (Clostridium perfringens), 1.11 mg/mL (Vibrio parahaemolyticus), 2.08 mg/mL (Staphyllococcus aureus), 2.16 mg/mL (Bacillus cereus),2.76 mg/mL (Candida albicans), 3.07 mg/mL (Listeria monocytogenes), 3.80 (Shigella flexneri), 12.92 mg/mL (Proteus vulgaris) and 15.55 (Enterococcus faecalis).These data may indicate that Punica granatumleaves extract is active against some pathogenic bacterial strains and thus may be useful in treatment of disease conditionscaused by these bacteria at least as a complementary medicine
Department of Pharmacology, Faculty of Veterinary Medicine, Benha University, 13736 Moshtohor
Background: To shed some light on full characterization and utilization of non-steroidal anti-inflammatory drugs (NSAIDs) in veterinary medicine, this study, therefore, was designed to clarify the pharmacological effects of two NSAIDs (one selective, that is meloxicam, and the other is non-selective, that is piroxicam) on intestinal contractility of rabbit as a farm animal species.Methods: Rabbits were humanely slaughtered, and segments from different parts of intestinal tracts were dissected out and an intestinal segment of about 2 cm long was fixed in an organ bath containing warm oxygenated Tyrode’s solution at 37°C. The tissue was subjected to a resting tension of 2 g and allowed to equilibrate for 30 min and then the effects of graded increased concentrations of piroxicam and meloxicam were demonstrated on the normal rhythmic motility of the isolated intestinal segments. The sites of action of piroxicam and meloxicam were tried.Results: Piroxicam and meloxicam exhibited concentration-dependent relaxations of intestinal smooth muscle segments with minimal and maximal effects of more potency by prioxicam than meloxicam. Calculated inhibitory concentration 50% were 15.45 and 23.10 μg/ml bath for piroxicam and meloxicam, respectively. Effects of either piroxicam or meloxicam did not involve cholinergic, adrenergic, histaminergic, nitrergic, or purinergic pathways as the application of the corresponding agonists/antagonists did not affect the inhibitory response of piroxicam and meloxicam. It was assumed that the effects of the drugs were attributed to the direct effects of the drugs on the intestines in addition to inhibiting endogenous prostaglandin synthesis activity via their cyclo-oxygenase inhibiting properties.Conclusions: Data of the present study may indicate that piroxicam and meloxicam could be used effectively and safely in rabbits for their anti-inflammatory actions in small therapeutic doses. However, in large doses, they (particularly, piroxicam) may produce depressant effects on gastrointestinal tract motility that should be taken in consideration in the case of introducing these drugs in therapy with larger doses
Qualitative identification of the active principles in Citrullus colocynthis and evaluation of its teratogenic effects in albino rats
Background: This study was designed to identify the active contents of Citrullus colocynthis plant and to examine their teratogenicity in rats. The fruit pulp of the poisonous plant was collected randomly from Suq-Alkhamis district, Tripoli, Libya. Methods: The glucoside colocynthin was isolated by lead acetate method while the alkaloids and saponins were isolated by maceration method. These active principles were then identified by chemical tests, color reactions and thin layer chromatography. Possible teratogenic effects of the fruit pulp extract was investigated by its administration to twelve pregnant rats on the 7th day of gestation at a dose of 40.6 mg/kg body weight that is equivalent to one fourth of the LD50 of the extract.Results: Gross anatomical observation on the 20th day of gestation revealed a high percentage of resorbed fetuses, smaller size and weight fetuses as well as absence of coccygeal vertebrae, metacarpal and metatarsal bones, and carpal and tarsal bones.Conclusions: It could be concluded that the extract of fruit pulp of Citrullus colocynthis, obtained from Libya, contain glucosidal as well as other principles that may cause teratogenic effects if given during at the early stage of pregnancy
Effects of amoxicillin repeated administration on the hemogram and biogram of sheep
Background: The object of the present study was to investigate the possible alterations in hematological and biochemical parameters of sheep that may occur following intramuscular injection of amoxicillin.Methods: Amoxicillin was injected to 10 sheep at a dosage regimen of 7Â mg/kg of body weight for 5 successive days. Two types of blood samples (with and without ethylenediaminetetraacetic acid as an anticoagulant) were collected from the jugular vein before and after the antibiotic course.Results: Amoxicillin significantly (p<0.001) increased total leukocyte count and (p<0.05) absolute eosinophilic count when compared with those of the control samples. Aspartate aminotransferase, alkaline phosphatase and cholesterol, were significantly (p<0.05) higher than the corresponding control values. In addition, amoxicillin significantly (p<0.05) increased blood urea nitrogen and creatinine but decreased phosphorus level when compared with those of prior-administration samples.Conclusions: These data may suggest that although the side changes caused by amoxicillin are minor in sheep, yet the liver and kidney functions should be monitored during its usage in therapy and it should be used with care for treatment of sheep with renal and/or hepatic impairments; its dosage regimen should be adjusted to avoid its hepatotoxic and nephrotoxic effects
Anti-inflammatory potential of Agaricus in carrageenan-induced model of local inflammation in rats
Background: The concept of effects of Agaricus on inflammatory responses is still controversial. This study, therefore, was designed to assess the potential of the anti-inflammatory effect of Agaricus 100% extract on acute inflammation using the model of carrageenan-induced paw edema in rats.Methods: Four groups among five (six rats each) have been injected with carrageenan (0.1Â mL of 3% solution), intra-plantar in the right hind paw; the first group was injected with saline instead in the same manner and kept as control. An hour earlier, rats received different treatments, either saline (inflamed control), or diclofenac (inflamed, standard-treated), or Agaricus extract (5Â mL/kg as small dose or 10Â mL/kg as a large dose). The volume of the developed paw edema has been measured at an hour interval fashion (1~6 hrs) and at 24 hrs.Results: Agaricus extract showed inhibitory effects on the carrageenan-induced edema in time-Â and dose-dependent manner, at the late phase (2~ hrs) of the inflammatory response (small dose) and at both early (~2 hrs) and late phases (large dose). The effects were comparable to those of diclofenac being 11.74, 08.46, 08.99, 09.72 and 09.89% at 2-6 hrs (small dose); 14.04, 23.91, 21.92, 17.99, 15.63 and 16.96% at 1-6 hrs (large dose); 16.85, 31.30, 35.38, 35.97, 34.72 and 34.63% (diclofenac). The anti-inflammatory effect of Agaricus could be attributed to its phytochemical content which may inhibit the inducible inflammatory mediators (as prostaglandins and nitric oxide) in the late phase (small dose) and/or inhibiting both early (histamine and oxygen free radicals) and late mediators (large dose).Conclusions: These data may indicate that Agaricus extract has the potential of anti-inflammatory activity that could be applied in acute inflammatory disorders
SYNTHESIS OF NEW PYRIMIDINE DERIVATIVES AND EVALUATION OF THEIR ANTICANCER AND ANTIMICROBIAL ACTIVITIES
ABSTRACTObjectives: The objective of this work is to synthesize new pyrimidine derivatives starting from ethyl 2,4-dioxo-4-(thiophen-2-yl)butanoate.Several oxadiazole, triazole, and thiadiazole moieties were incorporated into the pyrimidine backbone. The structure of the novel compounds wascharacterized by elemental analysis and spectroscopic methods.Methods: Synthesis of the target compounds was materialized starting from 2-oxo-6-(thiophen-2-yl)-2,3-dihydropyrimidine-4-carbohydrazide (4)which was prepared from the appropriate ethyl 2-oxo-6-(thiophen-2-yl)-2,3 dihydropyrimidine-4-carboxylate (2). Several synthetic pathways wereused for the preparation of the targets. Some of the newly synthesized compounds were subjected to in vitro cytotoxic screening against breastcarcinoma and colon carcinoma cell lines. On the other hand, the antimicrobial activity evaluation of some newly prepared compounds was performedusing cup plate diffusion method.Results: It was observed that the oxadiazole derivative 7b was the most potent compound against breast carcinoma cell line (IC=7.6 μg/ml). However,pyrimidine carrying substituted 1,2,4-triazole-2-thione moiety at position 6, 11 showed the highest cytotoxic activity against colon carcinoma cellline (IC50=4.7 μg/ml). On the other hand, compound 5c was the most active broad spectrum antimicrobial agent against the chosen microbial strains.Conclusion: From the observed results, further investigations recommended for the synthesis of heterocycles incorporated to pyrimidine backboneas cytotoxic as well as broad spectrum antimicrobial agents.Keywords: Pyrimidine, Oxadiazole, Triazole, Thiadiazole, In vitro anticancer study, Antimicrobial study.5
Lipid profile improving effect of Coriandrum sativum seed extract in rats
Background: Hyperlipidaemia is a common disease in middle-aged and elderly people. It has received attention, as it indirectly affects the normal metabolism, blood viscosity and vital organ functions. It is a risk factor for cardiovascular and cerebrovascular diseases. Therefore, the aim of the present study was to evaluate the possible antihyperlipidemic effect of Coriander sativum seed extract (CSSE) in rats fed on high-fat diet.Methods: A parallel study design was adopted on 42 albino rats, divided randomly into 7 groups with different treatments. After a 6 week-experimental course, blood samples were collected and analysed for lipid and organ function parameters. Phytochemical analysis was conducted on the used seed extract to detect the active principles underlying its effects.Results: CSSE (150 and 300 mg/kg, orally, once daily) along with a high-fat (1.5% cholesterol+1.5% coconut oil, in diet) diet resulted in a significant (p≤0.05) improvement in plasma lipid parameters, including, total cholesterol, triacyglycerols and lipoproteins, compared to the high-fat group. group. The extract significantly (p≤0.05) improved hepatic (total proteins, albumin, globulins, total conjugated and unconjugated bilirubins, AST, ALT, GGT), cardiac (CK-MB and troponin-I) and renal (urea, creatinine & uric acid) biomarkers. Phytoanalysis of CSSE revealed presence of phlobatannin and flavonoids. The protection % produced by small and large doses of CSSE were dose-dependent and parallel to those of the standard antihyperlipidemic rosuvastatin (2 mg/dl orally, daily).Conclusions: These data indicate that CSSE has a marked antihyperlipidemic effect and could be a source for a promising nutraceutical antihyperlipidemic drug depending on its high phenolic and flavonoid content
Ciprofloxacin and levofloxacin adversely affect male infertility indicated by pharmacological, andrological and pathological evidence
Background: Drug-induced reproductive organs toxicities is an important aetiology in investigation of male infertility. The aim is to study levofloxacin effect on male reproductive system in comparison to ciprofloxacin.Methods: Twenty-five male wister rats weighted 230±20 gm and aged 8 weeks were randomly divided into five groups of five. The first group received ciprofloxacin with dose 78.23 mg/kg/day in 2 doses (therapeutic dose). The second group received the double dose of the first group ciprofloxacin. The third group received levofloxacin with dose 39.11 mg/kg/day once daily (OD) (therapeutic dose). The Fourth group received the double dose of the third group levofloxacin. However, the fifth group served as a control and received normal saline with carboxymethylcellulose OD. All treatments were administered orally for 14 days. On the 15th day, blood samples and reproductive organs were obtained from all rats. Testicular tissues were prepared for genetic testing and chemical and microscopical examination.Results: Ciprofloxacin and levofloxacin negatively altered reproductive organ weights, sperm parameters and serum follicle stimulating hormone (FSH) and luteinizing hormone (LH) level (p<0.05). Additionally, serum testosterone level was significantly deceased in ciprofloxacin-treated group (the double dose) (p<0.05) relative to control. The difference between ciprofloxacin and levofloxacin was significant in seminal vesicle weight and serum LH and FSH level (p<0.05). Testicular histopathological changes were also found with the two drugs with different degrees. Effects of levofloxacin and ciprofloxacin were dose-dependent.Conclusions: Both ciprofloxacin and levofloxacin adversely affect andrological function that should be monitored and controlled during application of these drugs
Gentamicin and amikacin adversely affect male infertility indicated by pharmacological, andrological and pathological evidence
Background: Many drugs are implicated in male infertility and screening for medication history is an important for diagnosis and treatment of the problem. The aim is to study amikacin effect on male reproductive system in comparison to gentamicin.Methods: Twenty-five male wister rats weighted 220±20 gm and aged 8 weeks were randomly divided into five groups of five. The first group received gentamicin in dose 18.25 mg/kg/day once daily (OD) (therapeutic dose). The second group received gentamicin with double dose of the first group. The third group received amikacin in dose 54.75 mg/kg/day OD (therapeutic dose). The Fourth group received amikacin with double dose of the third group. However, the fifth group served as a control and received normal saline (NS) OD. All treatments were administered intraperitoneally (IP) for 14 days. On the 15th day, blood samples and reproductive organs were obtained from all animals. Testicular tissues were prepared for genetic testing and chemical and microscopical examination.Results: Amikacin and gentamicin negatively affected reproductive organs weights, sperm parameters, serum follicle stimulating hormone and luteinizing hormone (LH) level relative to control (p<0.05). However, serum testosterone level was only affected with gentamicin (p<0.05). A significant difference between gentamicin and amikacin was found in sperm count, testis and epididymis weights and serum testosterone and LH level (p<0.05). Testicular histopathological changes were also found with the two drugs with different degrees. Effects of both gentamicin and amikacin were dose-dependent.Conclusions: Both gentamicin and amikacin adversely affect andrological function that should be monitored and controlled during application of these drugs
Randomised clinical trial: a leucine-metformin-sildenafil combination (NS-0200) vs placebo in patients with non-alcoholic fatty liver disease
BACKGROUND:
Sirtuin 1 (Sirt1) is suppressed in non-alcoholic fatty liver disease (NAFLD), while its' stimulation or overexpression results in reduced disease severity in pre-clinical NAFLD models. Leucine allosterically activates Sirt1 and synergise with other Sirt/AMPK/NO pathway activators. We developed a triple combination of leucine, metformin and sildenafil (NS-0200), which was effective in a mouse model of non-alcoholic steatohepatitis (NASH).
AIM:
To report the results from a Phase 2, randomised clinical trial of of NS-0200 in 91 subjects with NAFLD (liver fat ≥15% by magnetic resonance imaging-proton-density fat fraction (MRI-PDFF)).
METHODS:
Subjects were randomised to placebo, low-dose (1.1 g leucine/0.5 g metformin/0.5 mg sildenafil) or high-dose NS-0200 (1.1 g leucine/0.5 g metformin/1.0 mg sildenafil) b.d. for 16 weeks; change in hepatic fat was assessed via MRI-PDFF, and lipid metabolism was assessed via changes in the lipidomic signature. Seventy subjects completed the trial and met a priori compliance criteria. Analyses were conducted on the full cohort and on those with alanine aminotransferase (ALT) values above median (50 U/L; n = 35).
RESULTS:
In the full cohort, active treatments did not separate from placebo. High dose NS-0200 reduced hepatic fat by 15.7% (relative change from baseline) in the high ALT group (P < 0.005) while low dose NS-0200 and placebo did not significantly change hepatic fat. Lipidomic analysis showed dose-responsive treatment effects in both overall and high ALT cohorts, with significant decreases in metabolically active lipids and up-regulation of fatty acid oxidation.
CONCLUSION:
These data support further evaluation of high-dose NS-0200 for treating NASH, especially in those with elevated ALT (NCT 02546609)
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