Open Access Original Research Article

Aqueous Extract of Enantia chlorantha (Annonaceae) Prevents the Delay in Chronic Gastric Ulcer Healing Caused by Indomethacin in Rats

Kuissu Teukam Mimosette Mesmine, Enow-Orock Enonchong George, Mezui Christophe, Nkwengoua Zondengoumba Ernestine, Tan Vernyuy Paul, Nyasse Barthelemy

Journal of Pharmaceutical Research International, Page 1-13
DOI: 10.9734/BJPR/2015/19035

Aims: To investigate the ability of Enantia chlorantha aqueous extract to heal acetic acid-induced chronic gastric ulcers and to prevent the delay in chronic ulcer healing induced by indomethacin.

Study Design: Random allocation of male rats to groups of five rats each.

Place and Duration of Study: Department of Animal Biology and Physiology, Animal Physiology Laboratory (Gastroenterology Research Unit) University of Yaoundé 1 and Department of Biomedical Sciences (Pathology Unit), University of Buea between January and April 2015.

Methodology: Gastric ulcers were produced 5 days after submucosal injection of 30% acetic acid (0.05 ml) at the lesser curvature of rat stomachs corpus. The extract (250 and 500 mg/kg) was administered p.o. during 10 days. Ulcer healing was delayed by indomethacin administered s.c. at 1 mg/kg once daily for 2 weeks from 5 days after the acid injection. Extract or sucralfate were administered concomitantly. Mucus secretion and oxidative stress parameters (superoxide dismutase (SOD), malondialdehyde (MDA), reduced glutathione (GSH), catalase (CAT)) were measured, and macroscopic and histological assessment of ulcer healing was done.

Results: Ulcer healing rates were 82.7% and 88.6% for the 250 and 500 mg/kg doses of extract following 10 day treatment of acetic acid-induced ulcers vs 55.7% and 85.2% for spontaneous healing and Ranititine, respectively. Spontaneous healing (60.9%) was significantly (P<0.01) delayed by indomethacin (22.5% healing rate). Co-administration of extract (250-500 mg/kg) or sucralfate (100 mg/ kg) significantly (P<.001) inhibited the adverse effect of indomethacin, raising healing rates to 76.7%, 82.2% and 85.8%, respectively. Indomethacin significantly depressed gastric mucus production (39.79 mg) but extract and sucralfate restored values to 40.08-55.75 mg and 70.06 mg, respectively. Indomethacin raised MDA levels and decreased antioxidant enzyme levels. These effects were counteracted by E. chlorantha extract. Microscopy showed advanced re-epithelialisation with recovery of ulcer craters due to extract.

Conclusion: E. chlorantha accelerates the spontaneous healing of acetic acid-induced chronic gastric ulcers, and prevents the delay in chronic gastric ulcer healing caused by indomethacin. The healing-promoting effect of the extract could be due not only to stimulation of gastric mucus secretion but also to enhanced re-epithelialisation and inhibition of enhanced lipid peroxidation in the ulcerated gastric tissue.

Open Access Original Research Article

Synthesis and Evaluation of Novel Mannich Bases of N-methyl-3-phenyl-3-[4-trifluoromethyl) phenoxy] propan-1-amine (Fluoxetine)

Niaz Wali, G. A. Miana, Arif Hussain Shah

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/BJPR/2015/19068

Three new Mannich bases of Fluoxetine (FA-1, FA-2, and FA-3) were synthesized and screened for their antidepressant activity through forced swim test. These new Mannich bases were synthesized in reflux condenser. Although none of the new compounds showed extra activity compare to its parent compound, nonetheless, they maintained antidepressant activity. The Mannich Bases were synthesized by attaching formaldehyde and different ketones to the secondary amine of fluoxetine at position-7. Their chemical structures have been confirmed by means of 1H-NMR, 13C-NMR and MS data.

Open Access Original Research Article

Proliferative Effect of Malaysian Propolis on Stem Cells from Human Exfoliated Deciduous Teeth: An In vitro Study

Chew Shi Fung, Hafizah Mohamad, Siti Nurnasihah Md Hashim, Aung Thu Htun, Azlina Ahmad

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2015/19918

Aims: To investigate the effect of Propolis on viability of stem cells from human exfoliated deciduous teeth via 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay.

Study Design:  Cell based experimental study.

Place and Duration of Study: The Craniofacial Science Laboratory located at the School of Dental Sciences, University of Science, Malaysia (USM) Health Campus, between June 2014 and September 2014.

Methodology: Different concentrations of Malaysian Propolis (groups 1, 2 and 3) diluted in culture media were used to treat on culture of stem cells from human exfoliated deciduous teeth. Pure culture media and culture media with Ethanol solvent were used as controls. MTT assay was done after 72 hours and the cell viability indices for Propolis-treated stem cells and respective controls were read via absorbance-rays 4 hours afterwards.

Results: Cell viability indices in Group-1 that has high Propolis concentrations showed significant reduction from control. In Group-2, stem cell viability in the lowest concentration of Propolis significantly increased. Cell viability in Group-3 all showed significant increase except for one concentration. One Way ANOVA was used for determination of significant difference in tested concentrations of Propolis. Differences were considered significant at (P = .05). The cell viability indices were significantly higher in culture media with lower concentrations of Propolis in comparison to control.

Conclusion: Propolis at low concentrations maintained and caused a significant increase in stem cell proliferation. Additional studies are necessary to investigate the optimal concentration of Propolis to enhance stem cell proliferation and its differentiation effect.

Open Access Original Research Article

The Protective Effect of Calcitriol on Diabetic Neuropathy in STZ-induced Diabetic Rats

Huda I. Abd Elhafiz, Maha M. El Batsh, Wael M. Y. Mohamed, Magda A. Mansour, Eman A. E. Badr, Abd Elrahman A. Yassin, Adel H. Omar

Journal of Pharmaceutical Research International, Page 1-15
DOI: 10.9734/BJPR/2015/19591

Diabetic peripheral neuropathy (DPN) is one of the diabetic complications that have a complex etiology and even with good glycemic control can have severe consequences. To date, there is no effective treatment for DPN. The current work aimed to investigate the possible protective effects of calcitriol on DPN by using streptozotocin-induced diabetic rats. Male rats were assigned into 5 equal groups: Normal control, diabetic untreated, diabetic treated with NPH Insulin, diabetic treated with calcitriol, diabetic received both insulin and calcitriol. Induction of diabetes mellitus was done by injection of a single dose of streptozotocin (30 mg/kg, intraperitonael). After 4 consecutive weeks, rats were subjected to tail flick latency test and blood samples were collected for biochemical assay of serum glucose, insulin, advanced glycation end products (AGEs). Sciatic nerves were dissected out for histopathological studies and estimation of tumor necrosis factor-α (TNF-α), superoxide dismutase (SOD) and malondialdhyde (MDA). Diabetes induced hyperalgesia, elevated levels of blood glucose, AGEs, TNF-α and MDA, decrease level of insulin and SOD together with marked structural changes in sciatic nerve. Minor to moderate improvement was recorded in either insulin- or calcitriol- treated diabetic subgroups. However, good amelioration was recorded in combination of insulin and calcitriol treatment. It is concluded that calcitriol improved the biochemical and histological changes induced by diabetes. Thus it may provide neural protection against DPN.

Open Access Original Research Article

A Study of the Antimicrobial Effectiveness of Diluted Antiseptics in Nigeria

Ezekiel Olugbenga Akinkunmi, Oluwatosin Ola Akinyemi, Olubunmi Ooreofe Olasehinde

Journal of Pharmaceutical Research International, Page 1-13
DOI: 10.9734/BJPR/2015/19241

Aim: The antimicrobial effectiveness of diluted antiseptics and the health risks that may be associated with any surviving pathogens were investigated.

Study Design: Experimental Study.

Place and Duration of Study: Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria, between March 2013 to December 2014.

Methodology: Six of the commonly used antiseptics selected for the study contain phenolics as main active agents while the seventh contains chlorhexidine gluconate and cetrimide. Dilutions of the antiseptics in Mueller Hinton Agar were done with water from the tap and with sterile distilled water inoculated with 108cfu/ml multidrug resistant Escherichia coli and Staphylococcus aureus clinical isolates. The identity, antibiotic resistance characteristics and production of Extended Spectrum β-lactamase (ESβL) by microbes that grew on antiseptics-agar plates at dilutions higher than manufacturers stated in-use concentrations were determined using morphological and biochemical characteristics as well as disc-diffusion methods.

Results: The tap water samples were found to contain heterotrophic bacteria, coliforms and staphylococci as contaminants. Four of the antiseptic product samples could not inhibit growth at dilutions higher than the in-use concentration while the effects of dilutions on the remaining were inconclusive since the concentrations after dilution could not be determined in all cases from the instruction given by the manufacturer. Nineteen (70.4%) of the 27 surviving organisms on the diluted antiseptics were Klebsiella pneumonia strains. Other isolates were 3 Streptococcus spp; 2 Pseudomonas aeruginosa; 2 S. aureus and 1 S. epidermidis strain. All the isolates were multidrug resistant and four of the K. pneumonia isolates produced ESβL. There was no growth in the antiseptics diluted with sterile distilled water.

Conclusion: It is concluded that instructions for dilutions of antiseptics should consider the effects of dilutions on the antimicrobial activities of the antiseptics in order to prevent failure of antisepsis which might have been happening all along with these commonly used antiseptics.

Open Access Original Research Article

Anti-oxidant and Anti-inflammatory Activity of Cassia auriculata (Flowers)

N. Muruganantham, S. Solomon, M. M. Senthamilselvi

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2015/18059

Aim: To analyze the antioxidants and anti-inflammatory potential of ethanolic crude extract of Cassia auriculata flowers.

Study Design: 2 kg of fresh flowers were soaked with 90% ethanol at room temperature (25ºC-30ºC). After 72 hrs the ethanolic extract was filtered. This extract was distilled and finally the crude was obtained. This ethanolic crude to get required concentrations and were used for screening antioxidants and anti-inflammatory activities.

Place and Duration of Study: PG & Research Department of Chemistry, Periyar E.V.R. College (Autonomous), Trichy, Tamilnadu, India. During the month of August and September 2014.

Methodology: Fresh flowers of Cassia auriculata were extracted with ethanol and evaluated for antioxidant activities by 2,2-Diphenyl 1-picryl hydrazyl solution (DPPH), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sul- phonic acid (ABTS) assay and anti inflammatory activites by humen blood cell (HRBC) membrane stabilization method and Inhibition of albumin denaturation method.

Results: The results obtained showed that the ethanolic crude extract of Cassia auriculata flowers can be considered as good sources of anti-oxidants, anti-inflammatory and can be incorporated into the drug formulations.

Conclusion: This study justifies the anti-oxidants, anti-inflammatory activity of ethanolic crude extract of Cassia auriculata Flowers. Further detailed analysis of this sample is required to identify the presence of bioactive compounds responsible for anti-oxidants, anti-inflammatory activities. Studies are highly needed for future drug development.

Open Access Original Research Article

Spasmogenic Activity of the Aqueous Methanolic Extract of Unripe Carica papaya Fruit in Isolated Uterine Muscle of the Rat

Ebere O. Odirichukwu, Nneka V. S. Uchechukwu, Edmund C. Mbegbu, Chukwuka N. Uchendu, David Ogwu

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2015/19248

Aims: This study investigated the effect of the aqueous methanolic extract of unripe Carica papaya (AMEUCP) on uterine contractility and its possible mechanism(s) of action.

Place and Duration of the Study: The study was carried out in the Department of Veterinary Surgery and Theriogenology, Michael Okpara University of Agriculture, Umudike, Nigeria and the Department of Veterinary Physiology and Pharmacology, University of Nigeria, Nsukka, Nigeria between February and June 2013.

Methods: Fresh mature unripe pawpaw fruits were obtained from Nsukka and extracted by cold maceration with 80% methanol for 48 hours and then concentrated to dryness. Estrogenised uterine muscle strips were harvested from sexually mature non-gravid female rats (200-250 g). In each experiment, a strip of about 1cm was mounted in a 50ml organ bath containing Krebs’ physiological salt solution, connected to an isometric electronic force displacement transducer and an oscillograph. The following drugs were used as receptor agonists or antagonist:  Salbutamol (0.2 µM), Isoprenaline (0.1 µM), Prazosin (10 nM), Propranolol (0.2 µM), cholinergic receptor antagonist; Atropine (240 nM). The extract and the standard drugs were applied at concentrations corresponding to the final bath concentration.

Results: The extract elicited forceful contraction of the uterus in a dose dependent manner and the mechanism of this contraction has been shown to involve the stimulation of myometrial cholinergic and alpha adrenoceptors, mobilization of calcium ion from the extracellular fluid and partly by release of calcium ions from the sarcoplasm.

Conclusion: These findings justify the traditional use of the plant for its uterotonic properties while deciphering its possible mechanisms of action may serve as a focal point for development of new uterotonics or oxytocics.