A series of new phthalimides 1(a-f) were synthesized via reaction phthalic anhydride with different amino acids under fusion conditions. Esterification of N-phthaloyl acid derivatives 1(a-f) with methanol in the presence of SOCl2 to producing the corresponding esters 2(a-f). Which on reaction with hydrazine hydrate in boiling n-butanol afforded the corresponding N-phthaloyl acid hydrazides 4(a-f) Reaction of compound (4a) with different aldehydes and ketones yielded the corresponding hydrazone derivatives 5(a-d). Some new phthalimides linked to hetero cyclic moieties such as benzimidazoles, benzoxazines and quinazolines were synthesized. The structure of the synthesized compounds was confirmed from their analytical and spectral data such as, IR spectra, 1H-NMR and mass spectra. Antimicrobial against two types of bacteria and anticancer activity for some of the synthesized imides were evaluated. The results showed that most of them have a good antimicrobial and anticancer activities.
Aims: This study was design to screen the stem bark extract of Pseudocedrela kotschyi for the presence of phytochemical constituents and evaluate the extract for antimicrobial activity on wide range of pathogenic bacteria and fungi species. Place and Duration of Study: Department of Pharmaceutical and Medicinal Chemistry, Usmanu Danfodiyo University Sokoto and Laboratory of Pharmaceutical Microbiology, Ahmadu Bello University Zaria, between April 2013 and Oct 2013. Methodology: Plant material was extracted with methanol and phytochemical screening carried out. Sequentially, the methanol extract was partitioned against chloroform, ethyl acetate and n-butanol to afford chloroform, ethyl acetate and n-butanol soluble fractions respectively. All fractions were evaluated against panel of pathogenic bacteria and fungi to include Methicillin Resistant Staphylococcus aureus (MRSA), Staphylococcus aureus, Streptococcus pyogenes, Corynebacterium ulcerans, Bacillus subtilis, Escherichia coli, Salmonella typhi, Shigella dysenteriae, Klebsiella pneumoniae, Neisseria gonorrhoeae, Pseudomonas aeruginosa, Candida albicans, Candida krusei and Candida tropicalis. Results: Phytochemical screening of the extracts revealed the presence of saponins, flavonoids, tannins, glycosides, anthraquinones, steroids/terpenes as well as alkaloids. The susceptibility test of the fractions at 30mg/ml have displayed activity against S. aureus, S. pyogenes, E. coli, S. dysenteriae, P. aeruginosa, C. albicans, C. krusei and C. tropicalis at zone of inhibition ranges between 20-28mm while the MIC and MBC/MFC results showed spectrum of antimicrobial activity ranges between 2.5-10mg/ml and 5-30 mg/ml respectively. Conclusion: The activity of the extracts against S. pyogenes, E. coli, S. dysenteriae, P. aeruginosa and C. albicans, justify the traditional use of stem bark of Pseudocedrela kotschyi in the treatment of diarrhoea, dysentery and oral infection which are diseases commonly caused by these organisms.
Aims: The present study was designed to evaluate the anti-diabetic as well as prophylactic activity of Jambadyarista and Bohumutrantak Ras in alloxan-induced diabetic rats. Study Design: Study the prophylactic and antiglycemic effects against diabetes of two Ayurvedic drugs ‘Jambadyarista’ and ‘Bohumutrantak Ras’ in normal as well as alloxan-induced diabetic rats using in vivo models. Place and Duration of Study: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka-1000, Bangladesh between December 2013 and March 2014. Methodology: To investigate the activity, 70 Long Evans rats divided into seven (A-G) groups were included in this study. Diabetes was induced by single intraperitoneal injection of alloxan (150mg/kg body weight) while the Ayurvedic drugs Jambadyarista and Bohumutrantak Ras were given orally at a dose of 200mg/kg of body weight. Group A was control group. Groups B and E were allowed to fast for 12 hours. Diabetes was induced by intraperitoneal injection of freshly prepared solution of alloxan (150mg/kg) in normal saline after base line glucose level determination. The alloxan-treated rats were allowed to food over night to overcome drug induced hyperglycemia. After 48 hours, blood glucose level was measured with an Accu-Chek glucometer using blood sample from the tail vein of each rat. Diabetes was established in animals when blood glucose level was raised to 11.1-32.6mmol/L. After the establishment of diabetes, the experiments were carried out. Groups D and G were allowed to induce diabetes by single intraperitoneal injection of alloxan (75mg/kg body weight) in normal saline every day for 5 days. Results: In case of alloxan-induced diabetic rats, Jambadyarista and Bohumutrantak Ras showed prophylactic activity against diabetes as well as also reduced blood glucose level. By statistical analysis of results, it was found that Jambadyarista and Bohumutrantak Ras have prophylactic activity against diabetes in normal and alloxan- induced diabetic rats. Conclusion: It can be inferred that the Ayurvedic drug “Jambadyarista and Bohumutrantak Ras” significantly possess prophylactic activity against diabetes. They also showed antidiabetic effect in alloxan-induced diabetic rats. Further comprehensive cellular and molecular investigations are required to characterize the exact mechanism responsible for its prophylactic and antidiabetic effects.
Aims: Lemon grass and mango bark serves as one of the medicinal plants used in Nigeria for the treatment of malaria by traditional herbalists. This study was designed to assess the effects of ethanolic extract of lemon grass and mango bark on the cerebral astrocytes of wistar rats. Place and Duration of Study: Department of Human Anatomy, Faculty of Basic Medical Sciences, University of Calabar, Calabar, Nigeria between December 2013 and May 2014. Methodology: Twenty (20) adult wistar rat were divided into four groups, each consisting of five rats. Group A served as the control that received distilled water, while the experimental groups B, C and D received 2000mg/kg ethanolic extract of lemon grass, 2000mg/kg ethanolic extract of mango bark, a combination of 1000mg/kg ethanolic extract of lemon grass and 1000mg/kg ethanolic extract of mango bark orally with the aid of orogastric tube respectively for two weeks and were sacrificed using chloroform. The brain of the rats were harvested and preserved using 10% formal saline. Histological processes were carried out and the tissues were stained using Hortegas. Results: Neurohistological studies carried out revealed hyperplasia of astrocytes in the treated groups B, C and D animals that received 2000mg/kg of ethanolic extract of lemon grass, 2000mg/kg of mango bark and combined 1000mg/kg of ethanolic extract of lemon grass and 1000mg/kg of ethanolic extract of mango bark. There was increased hyperplasia in group B animals that received 2000mg/kg of the lemon grass extract when compared with the control and the treated groups C and D. Conclusion: Thus, ethanolic extract of lemon grass, mango bark and combined extracts of mango bark and lemon grass has the potential to cause neuronal damage as seen in the hyperplasia of cerebral cortex astrocytes.
Aim: To investigate the dichloromethane fraction obtained from an aqueous methanol extract of green stems of Citrus jambhiri Lush. and evaluate the hepatoprotective effect of limonianin. Study Design: Isolation and identification of secondary metabolite and hepatoprotective activity of limonianin. Place and Duration of Study: Faculty of Pharmacy, Zagazig University and Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, between February 2012 and January 2014. Methodology: Psyllic acid, sinensetin, nobiletin, 6-demethoxytangeretin, limonianin, hesperetin, quercetin were isolated from the green stem of Citrus jambhiri. Their identity was unambiguously confirmed via different spectroscopic methods (UV, MS, 1H NMR, 13C NMR, H-COSY, HSQC and HMBC). The liver enzymes alanine aminotransferase (ALT), aspartate aminotransferase (AST), superoxide dismutase (SOD), malondialdehyde (MDA) and total antioxidant capacity (TAC) were used to evaluate the hepatoprotective effect of limonianin. Results: Limonianin exhibited an equal or even better hepatoprotective activity than the known and medicinally used flavonoid mixture silymarin on human hepatoma cells (HepG2) against D-galactosamine-induced hepatotoxicity. Limonianin at concentration 5 µM exhibited a reduction of ALT, AST and MDA with 46.50, 42.10 and 24.36%, respectively while SOD and TAC were elevated with 38.56 and 391.67%, respectively compared with D-galactosamine (D-GaIN) treated cells. At concentration of 10 µM, limonianin shows elevation of SOD and TAC with 74.56 and 791.67%, respectively compared with silymarin (63 and 766.67%, respectively). Conclusion: The findings of this study showed that limonianin could be used as ideal hepatoprotective agent.
Aims: This study was aimed at comparing the physicochemical and bioavailability profiles of some brands of Levofloxacin 500mg tablets that are registered in Nigeria by her regulatory authority and to examine the feasibility of interchangeability of the brands. Methodology: The physicochemical equivalence of ten brands of Levofloxacin 500 mg tablets (LEV-1 to LEV-10) were evaluated using both official and unofficial standards including weight variation, hardness, friability test, chemical assay, disintegration, dissolution rate and drug content. Five of the brands were also evaluated for bioavailability profiles using a single dose randomized two period cross–over designs measuring the concentration of drugs in the urine. Urinary samples before dosing and at various appropriate time intervals up to 12 hours were analyzed by validated Double Beam U. V. Spectrophotometer method with 99.8% extraction recovery. Pharmacokinetic parameters for bioequivalence evaluation Cmax, Tmax and AUC were determined. Results: The resultsshowed that 60% of the levofloxacin brands (LEV-2, LEV-4, LEV-5, LEV-7, LEV-8 and LEV-9) failed in at least one of the tested physicochemical parameters. The statistical comparison of the physicochemical parameters showed no difference between the innovator brand (LEV-1) and three of the tested generic brands (LEV-3, LEV-6 and LEV-10). Unlike LEV-5, the results obtained from the reference ratios of the parameters from bioavailability studies for the physicochemical equivalent brands were found to be within bioequivalence acceptable range with the reference brand indicating that they are bioequivalent in terms of Cmax and AUC to the innovator brand. Conclusion: The study indicates that 60% of the brands may not be used interchangeably with the innovator brand; consequently, the therapeutic substitution of these brands is not advisable. The formulation and/or the manufacturing process affect the weight uniformity, content uniformity, dissolution and thus the bioavailability of the drug products.
Anekécia Lauro da Silva, Sheilla Andrade de Oliveira, Jamerson Ferreira de Oliveira, Edna de Farias Santiago, Antônio Sérgio Alves de Almeida Júnior, Íris Trindade Tenório Jacobi, Christina Alves Peixoto, Vinícius Pinto Costa Rocha, Milena Botelho Pereira Soares, Ivan da Rocha Pitta, Maria do Carmo Alves de Lima
Aims: Verify the potential of the schistosomicidal imidazolidine derivative (5Z)-3-(4-bromo-benzyl)-5-(4-chloro-benzylidene)-4-thioxo-imidazolidin-2-one. Study Design: In this study, we tested the imidazolidinic derivative 3 through in vitro evaluations, cytotoxicity assay and analysis of Scanning Electron Microscopy to verify its therapeutic potential in the treatment of schistosomiasis. Place and Duration of Study: Departamento de Antibióticos, Universidade Federal de Pernambuco (UFPE), Fundação Oswaldo Cruz (FIOCRUZ)/PE and (FIOCRUZ)/BA between January 2013 and march 2014. Methodology: This study was approved by the Ethics Committee on Animal Use Research Center Aggeu Magalhães/Oswaldo Cruz Fundação (CPqAM/FIOCRUZ) authorized by the license No. 21/2011. Male albino Swiss mice were used Mus musculus 25 days old weighing 50 grams. Compound 3 was assayed for its cytotoxicity through cell J774 macrophage lineage. The amount of inhibitory concentration (LC50) was determined by nonlinear regression using the Graph Pad Prism version 5.01. Then the compound was evaluated against adult worms of S. mansoni by performing the activity in vitro at doses 100-20µg/mL and ultrastructural investigation by Scanning Electron Microscopy (SEM) at doses of 100 and 60μg/ml. The PZQ was the positive control of the experiment. Results: The derivative 3 showed LC50 of 29.7±3.9mM. Compound 3 was able to have decreased motility of S. mansoni culminating with a mortality rate of 100% at doses of 60 and 100µg/mL on the fourth day of observation of the experiment. In the SEM, the compound caused various soft tissue changes of S. mansoni parasites such as blistering, destruction of the integument with loss of spines and tubercles, body contraction and windy. Conclusion: The derivative imidazolidine 3 showed a promising schistosomicidal activity in vitro. However, conducting further studies with the completion of work in front of the live schistosomiasis is required.
Aims: To assess dentist’s knowledge and practice in relation antibiotic prescription and to investigate if they follow the current international guidelines. Methodology: In this cross sectional study a structured and pretested questionnaire was sent to 202 licensed dental practitioners in UAE, Iran and Jordan took place in period between December 2011 and January 2012 by e-mail and physical delivery. Results: Of 160 responding dentists 93.1% would prescribe antibiotics for dentofacial infections with systemic signs but many prescribe antibiotics for conditions where antibiotic therapy is not required according to good practice. Amoxicillin was the most frequently prescribed antibiotics. The non-clinical factor that may affect decision of the majority of dentists to prescribe antibiotics was perception of the effectiveness of those antibiotics in previous cases they treated with same agent (61.25%). Most of the respondents (84%) prescribe prophylactic antibiotics for patients at risk of infective endocarditis. Conclusion: This study reveals that antibiotics were still being prescribed by dental practitioners where recent guidelines suggest there is no indication.