3,269 research outputs found

    Anticonvulsant activity of some vanilloid receptor agonists

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    Background: Vanilloid receptors 1 (VR 1), a group of transient receptor potential channels family was cloned in 1997. They were found to be a potential target for treatment of different acute and chronic pain disorder. Recently these receptors were reported to be involved in several  pathological conditions.Objectives: The present study aimed to investigate the potential  anticonvulsant activity of five vanilloidal agonists (capsaicin, nonivamide, zingerone, dehydrozingerone and 6-gingerol).Methods: Experimental animal model of pentylenetetrazole (PTZ) induced seizure was used to investigate the potential anticonvulsant activity of capsaicin, nonivamide, zingerone, dehydrozingerone and 6-gingerol.Results: The data obtained showed that, all tested compounds (capsaicin, nonivamide, zingerone, dehydrozingerone and 6-gingerol) possess dose dependant anticonvulsant activity.Conclusion: The five vanilloidal agonists; capsaicin, nonivamide,  zingerone, dehydrozingerone and 6-gingerol exhibit anticonvulsant activity and may find clinical applications.Key words: Anticonvulsant, vanilloid receptor agonists and  pentylenetetrazol

    IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF METRONIDAZOLE, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITIONS

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    Objective: The aim of present study is to examine the in-vitro in-vivo correlation (IVIVC) of immediate release product. Metronidazole 500mg and its brands of immediate release dosage forms. Metronidazole is clearly classified into BCS class I, and could be evaluated under bio waiver conditions. Methods: The in vitro parameters employed were hardness, weight uniformity, friability, disintegration time, absolute drug content, dissolution rate (in 0.1 N Hydrochloric acid, phosphate buffer and acetate buffer at 37ºC), and dissolution efficiencies were also analyzed. The in-vitro dissolution study was performed on the brands, according to FDA,USP dissolution profile in three different PH (1.2), (4.5), and (6.8) at37ºC, using the USP apparatus II, then f1, f2 were determined for the time intervals of 10, 15, 30, 45 and 60 minutes, and dissolution efficiencies were calculated. MINITAB 14 statistical program used for in vitro in vivo correlation, level A was done for reference product. Results: A non linear relation was established which is typical for immediate release formulation, of class 1. There was significant relationship between in vitro and in vivo data of reference metronidazole product, Correlation and distribution of data with correlation coefficient (r=0.724, 0.837, 0.707), nonlinear relationship with p-value (>0.05) =(0.167, 0.098, 0.182), there is no out lines, no lake of fits at P-Values=0.0040, 006, 0.026.Conclusion: Study concluded that there is no linear correlation between percent of drug released and percent of drug absorbed ,this may be due to uncontrollable gastric emptying rate for class one Metronidazole.                          Peer Review History: Received 2 January 2020;   Revised 1 February; Accepted 3 March, Available online 15 March 2020 Academic Editor: Ahmad Najib, Universitas Muslim Indonesia,  Indonesia, [email protected] Received file:                Reviewer's Comments: Average Peer review marks at initial stage: 4.5/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Dr. Hayriye Eda Şatana Kara, Gazi University, Turkey, [email protected] Dr. Mohamed Ismail Nounou, Appalachian College of Pharmacy, Oakwood, Virginia, USA, [email protected] Similar Articles: IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF ATENOLOL, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITION

    Preliminary phytochemical evaluation and seed proximate analysis of Surib (Sesbanialeptocarpa DC.)

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    Background: Surib (Sessbanialeptocarpa) of the family Leguminosae is a wild plant widely spread in Gezira scheme and sometimes its seeds unavoidably get mixed with machinery-harvested crops especially wheat. Different parts of Surib have been used traditionally for various illnesses in Africa where the plant spread widely.Objectives: To evaluate the nutritional value of Surib.Methods: The preliminary phytochemical screening was performed using the conventional chemical tests using precipitation and color reagents as appropriate, while the standard methods of the Association of Official Analytical Chemists, 1980 were used for the determination of the proximate seed composition.Results: Preliminary phytochemical screening of different plant parts (seeds, leaves and roots) extracts showed the presence of alkaloids in seeds and roots. Seeds and leaves of the plants were found to contain saponins, flavanoids, anthraquinones and tannins while the roots are devoid of these constituents. Proximate analysis of the seed revealed that carbohydrates and crude fibers constitute about 80% while proteins and fats values were 5.25 and 6.13% respectively.Conclusion: The nutrient value of Surib seed is negligible for its low content of proteins and fatty substances and thus it is of no use as animal or human food. The qualitatively determined antinutrient phytoconstituents as tannins, alkaloids, saponins and flavanoids in the seed could be considered as another main limitation to effective utilization of Surib as an animal feed and/or human food.Keywords: Sesbania leptocarpa, proximate analysis, phytochemical screening

    IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF ATENOLOL, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITIONS

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    Objective: The aim of present study is to examine the in vitro-in vivo correlation (IVIVC) of immediate release product. Atenolol 100mg and its brands of immediate release dosage forms. Atenolol is clearly classified into BCS class III, and could be evaluated under bio waiver conditions. Methods: The in vitro parameters employed were hardness, weight uniformity, friability, disintegration time, absolute drug content, dissolution rate (in 0.1 N Hydrochloric acid, phosphate buffer and acetate buffer at 37ºC), and dissolution efficiencies were also analyzed. The in-vitro dissolution study was performed on the brands, according to FDA, USP  dissolution profile in three different PH (1.2), (4.5), and (6.8) at 37ºC, using the USP apparatus II. A non linear relation was established which is typical for immediate release formulation, of class III. Results: All Atenolol brands released about 90% drug in PH (6.8), where about 87% in PH (4.5), reference drug released about 91% and test drug released about 87% in pH (1.2). Dissolution efficiency of  the entire brands differed by less than 10% from the innovator brand. According to MINITAM 14 statistical program, there was significant relationship between in vitro and in vivo data of reference Atenolol product. Conclusion: By applying level A in vitro-in vivo correlation, study concluded that there is no linear correlation between percent of drug released and percent of drug absorbed, this may be due to uncontrollable permeability rate for class three Atenolol.                    Peer Review History: Received 20 September 2019;   Revised 16 December; Accepted 7 January, Available online 15 January 2020 Academic Editor: Dr. Amany Mohamed Alboghdadly, Princess Nourah bint abdulrahman university, Riyadh, [email protected] UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file:                Reviewer's Comments: Average Peer review marks at initial stage: 3.0/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Dr. Hayriye Eda Şatana Kara, Gazi University, Turkey, [email protected] Dr. Nicola Micale, University of Messina, Italy, [email protected] Similar Articles: FAST DISSOLVING DRUG DELIVERY SYSTEMS: FORMULATION, PREPARATION TECHNIQUES AND EVALUATION FAST DISSOLVING TABLETS: A PROMISING APPROACH FOR DRUG DELIVERY DEVELOPMENT AND EVALUATION OF FAST DISSOLVING THIN FILMS OF ARIPIPRAZOLE TABLET GRANULATION: CURRENT SCENARIO AND RECENT ADVANCE

    Anticonvulsant Activity of Capsicum Annum (Red Pepper) Fruit Extract using Pentylentetrazole and Maximum Electroshock Induced Seizure Tests in Rats

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    Background: Epilepsy is a disorder of brain function characterized by periodic and unpredictable occurrence of seizures that refers to as a transient alteration of behavior due to disordered, synchronous and rhythmic firing of populations of brain neurons. Modern drug therapy of epilepsy is complicated by side effects and inability to control seizures in some patients.Objectives: The present study was conducted to test the anticonvulsant activity of Capsicum annum fruit extract in rat models.Materials and Methods: The methanolic extract of Capsicum annum fruit was tested for its potential anticonvulsant activity using pentylentetrazole (PTZ) and maximum electroshock (MES) induced seizure models in rats. The simple activity meter was used to determine the sedative activity of Capsicum annum fruit extract. Thereafter, the protective index was calculated.Results: Results obtained showed that the extract at concentrations of 5, 9, 10, 20 and 40 mg/kg produced dose dependent anticonvulsant activity. Capsicum annum (40 mg/kg, i.p.) caused 100% protection from seizure induced by PTZ and sedation in 50% of rats (TD50). Fifty percent anticonvulsant activity was produced by 9mg/kg Capsicum annum. Moreover, the protective index was calculated to be more than four. When tested on seizure induced by MES, Capsicum annum extract at doses of 10, 20 and 40 mg\kg showed no seizure protection.Conclusion: It could be concluded that Capsicum annum fruit could be a source for potential antiepileptic agent(s). Further studies are needed to determine the active constituents responsible for the anticonvulsant activity as well as to elucidate their mechanism(s) of action.Key words: Epilepsy, Pentylenetetrazole, electroshock, Capsicum annum, Sudan

    Clinical hypoglycemic effects of allium cepa (Red Onion) in Type 1 Diabetic patients

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    Background: Type 1 diabetes mellitus is an autoimmune disease caused by destruction of pancreatic islet beta cells and characterized by defect in insulin secretion.Objectives: The present study was carried out to investigate the hypoglycemic effects of Allium cepa in patients with type 1 diabetic patients.Results: In the assessment of the hypoglycaemic activity of Allium cepa in type 1 diabetic patients (n=21), crude Allium cepa (100g) caused a  considerably lowered value in the fasting blood glucose levels by about 89 mg/dl in relation to insulin (145 mg/dl) after 4 hours. Also the ingestion of crude Allium cepa by type 1 diabetic patients produced a significant reduction in the induced hyperglycemia (GTT) by about 120 mg/dl in relation to water (77 mg/dl) and the standard drug insulin (153 mg/dl).Conclusion: Crude Allium cepa produced hypoglycemic effects, thus it could be used as a dietary supplement in management of diabetes. Key words: Allium cepa, hypoglycemia, type 1 diabetes

    Phytochemical and Antibacterial Evaluation of Parinari curatetellifolia Planch Ex Benth (Chrysobalanaceae)

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    Parinari curatellifolia Planch ex Benth (Chrysobalanaceae) is used in traditional medicine for the treatment of pneumonia, wound infections, dressing of fractures and dislocation. P.curatellifolia stem bark extracts in methanol, ethylacetate and n-butanol were evaluated for antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus subtilis using cup plate method. The extracts were used at 50mg/ml concentration. The extracts were also screened for the presence of some secondary metabolites. The result of the antibacterial screening produced zones of inhibition ranging from 12-21mm for the methanolic extract while the ethylacetate and n-butanol fractions showed inhibition zones of 16-24mm respectively. The aqueous extract showed inhibition zones ranging from 12-20mm. Ampicillin (0.01mg/ml) used aspositive control, showed zones of inhibition ranging from 14-34mm. Ethylacetate fraction was the most active of the extracts on the test bacterial species. Water was used as negative control. The extracts inmost cases compared favorably with the ampicillin. The activity of the extracts was more on the gram positive bacteria than on the gram negative ones. The minimum inhibitory concentrations (MICs) of theethylacetate fraction for B. subtilis, P. aeruginosa were 1.56mg/ml each, for E.coli and S. aureus were 3.13 mg/ml and 0.78mg/ml respectively. The minimum bactericidal concentrations (MBCs) of the ethylacetate fraction for B.subtilis and S. aureus were 6.25mg/ml each, for P. aeruginosa and E.coliwere 12.50mg/ml each. The phytochemical screening revealed the  presence of anthraquinones, tannins, saponins, flavonoids,  cardiacglycosides, terpenoids, and carbohydrates. The antibacterial activity of the extracts may be attributable to the presence of these compounds in the extracts. The findings of this work lend support to the ethnomedical use of the plant.Key Words: Antibacterial; Phytochemistry; MIC; MBC; Parinari curatellifoli

    The immune enhancer, thymoquinone, and the hope of utilizing the immune system of Aedes caspius against disease agents

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    Insects have developed an efficient defence system against  microorganisms, which involves both humoral and cellular mechanisms. Recent studies on insect defence system are aimed at utilizing it inthe battle against mosquito-borne diseases. However, mounting immune responses of insects has proved to impose fitness costs. The current study was conducted to test the costs of enhancing the immune responses of Aedes caspius by oral administration of thymoquinone, the active ingredient of the black seed oil, Nigella sativa L. (Ranunculaceae). The obtained results showed an effective humoral activity against Micrococcus luteus (NCTC 2665, Sigma-Aldrich, UK) and Bacillus cereus when mosquitoes were injected with lipopolysaccharide (LPS), Bacillus thuringiensis or B. cereus. However, this activity showed no effect against B. thuringiensis. Furthermore, oral administration of thymoquinone enhanced the humoral activity against B. cereus but not against B. thuringiensis. On the other hand, thymoquinone-enhanced immunity imposed reproductive costs in terms of higher percentages of follicular apoptosis and resorption. This observation has been confirmed by the semiquantitative reverse transcriptase polymerase chain reaction (RT-PCR) analysis, which showed a relatively higher expression of selected caspases genes, namely: CASP 18, CASP 19 and CASP 20, but not CASP 21, transcripts in immune enhanced mosquitoes compared to non-enhanced ones. Based on these results, this study suggests that enhancing the humoral activity by thymoquinone proved to be costly in terms of triggering follicular apoptosis and resorption. Thus, as part of the scenario ofimmunity-reproduction conflict, it was concluded that the impact of immune stimulation and/or enhancement on the vector reproduction constitutes a limiting factor to the utilization of thymoquinone in the immuno-control strategy against mosquito-borne diseases

    Detection of Optimum pH of Momordica balsamina Seeds Lectin

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    Background: Lectins are carbohydrate binding proteins of non-immune origin that reversibly and non-enzymatically bind carbohydrates with high specificity for the chemical structure of the glycan array without changing their structure.Objectives: The present study aimed to detect the optimum pH of Momordica balsamina seeds lectin (MbSL).Materials and Methods:A season fresh of Momordica balsamina fruit seeds were brought from urban areas of Sudan (Gadarif and north Kurdofan states), then the lectin was isolated from saline extract by affinity chromatography on alpha agarose lactose matrix then the purified lectin activity was evaluated in different buffers to detect the optimum pH.Results: The activity of the lectin remained stable in the pH range 2-12.Conclusion: A lactose-binding lectin from seeds of Momordica balsamina medicinal plant shares a high degree of similarity with other Cucurbitaceae family lectins in term of their physicochemical features including sugar specificity, effect of pH on lectin stability.Keywords: Momordica balsamina; lectin; seeds; plant lectin; pH; protein
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