Open Access Original Research Article

Comparative Studies of the Effect of Sphenocentrum jollyanum Pierre on High Fat and High Carbohydrate Diet Induced Obesity in Rats

Gabriel O. Anyanwu

Journal of Pharmaceutical Research International, Page 1416-1428
DOI: 10.9734/BJPR/2014/10463

Aim: The aim of this study was to compare the effect of ethanolic extract of Sphenocentrum jollyanum on high fat and high carbohydrate diet induced obesity in male wistar rats.
Methodology: 30 male wistar rats used for this study were divided into 5 groups of 6 rats each. Group 1 was fed the normal pellet diet (NPD), Group 2 and 3 were fed with high fat diet (HFD), Group 4 and 5 were with fed high carbohydrate diet (HCD) and all groups had free access to diets and water ad libitum for 18 weeks. Treatment with 500mg/kg b.w ethanolic extract of S. jollyanum for Group 3 and 5 started in the 14thweek, that is, at the end of obesity induction and lasted for another four weeks. The extract was suspended in normal saline and administered orally to the rats using a gavage tube. Thereafter, the food intake, body weight, total fat mass, adiposity index, total cholesterol, triglycerides, high density lipoprotein cholesterol, very low density lipoprotein cholesterol, low density lipoprotein cholesterol, creatine kinase, lactate dehydrogenase, glucose, insulin and leptin were measured.
Results: The results showed that feeding with HFD and HCD significantly increased (p<0.05) body weight, total fat mass, adiposity index, total cholesterol (TC), triglycerides (TG), very density low cholesterol (VDL-C), low density low cholesterol (LDL-C), creatine kinanse (CK) activity, lactate dehydrogenase (LDH), glucose, insulin and leptin levels. The ethanolic extract of S. jollyanum significantly decreased total fat mass, adiposity index, TC, TG, VDL-C, LDL-C, CK activity, LDH, glucose and leptin levels in the HFD group. While among the HCD group, S. jollyanum significantly decreased total fat mass, adiposity index and CK activity.
Conclusion: The high fat and high carbohydrate diet induced obesity in the wistar rats and the decrease in the lipid profile, heart biomarkers, glucose and leptin by ethanolic extract of S. jollyanum shows that the plant might possess anti-obesity effect.

Open Access Original Research Article

Effects of Aqueous Extract of Some Selected Vegetables on Halofantrine Hepato-cardiatoxicity in Rats

A. J. Alhassan, M. S. Sule, A. M. Wudil, U. Lawan

Journal of Pharmaceutical Research International, Page 1429-1438
DOI: 10.9734/BJPR/2014/7644

Aim: The protective effect of some selected vegetables {Moringa (Moringa oleifera), Cabbage (Brassica oleracea) and Tomato (Solanum lycopersicum)} against hepato- cardio toxicity of halofantrine (an antimalarial drug) was evaluated in 72 albino rats.
Study Design: The rats were grouped into eight of nine rats each. Three different doses; 7.1, 14.2 and 21.3mg/Kg of halofantrine were given to group II, III and IV respectively. Group V was co-administered with halofantrine and moringa extract 7.1 and 0.20mg/Kg respectively, Group VI co-administered with halofantrine and cabbage extract 7.1 and 0.10mg/Kg respectively, Group VII co-administered with halofantrine and Tomato extract 7.1 and 0.20mg/Kg respectively and Group VIII co-administered with halofantrine, moringa, cabbage and tomato extracts 7.1, 0.20, 0.10 and 0.20mg/Kg respectively). Group I was neither given the drug nor the vegetable extract serving as normal control.

Methodology: The liver and heart function indices were evaluated using standard methods.

Results: Serum liver enzymes, heart marker enzymes and concentration of malondialdehyde (MDA) were analyzed after 16, 96 and 192 hours of oral administration. Halofantrine administration caused significant increase (p<0.05) in the activities of all the enzymes with a peak at the 16th hour. Malondialdehyde had a peak at the 192 hours. The oral co-administration of vegetables extract showed a significant decrease (p<0.05) in the enzyme activities and concentration of malondialdehyde as compared sole administration of halofantrine. The result showed that Moringa, Cabbage and Tomato may have hepato and cardio protective effects against halofantrine toxicity. It may be concluded that consumption of vegetables may be beyond the nutritional needs but also for protective purposes.

Open Access Original Research Article

Morphology, Functional and Pasting Properties of Ginger Starches Prepared by Four Different Drying Methods

Bamiro O. Adebowale, Bakre Lateef Gbenga, Faleye Yewande

Journal of Pharmaceutical Research International, Page 1439-1450
DOI: 10.9734/BJPR/2014/10499

Aim: This study aims at providing information on the morphology, physico-chemical and pasting properties of the ginger starches prepared by air drying, oven drying, freeze drying and microwave drying methods with a view to improving their utilization.
Place and Duration of Study: Department of Pharmaceutics and Pharmaceutical Technology, Olabisi Onabanjo University, Nigeria and Department of Pharmaceutics, University of Ibadan, Nigeria between March 2013 and February 2014
Methodology: Starch was isolated from the rhizomes of Zingiber officinale and dried by oven, freeze drying, air drying and microwave drying methods. They were studied for their composition, morphological, functional and pasting properties
Result: The residual protein content of the four starches was slightly different averaging 5.06%. The residual protein of air dried starch was the lowest and that freeze dried starch was the highest. There was no significant variation in the saponin and tannin contents of the dried samples. The amylose content of the ginger starches ranged between 20.7% and 22.1%.The rank order of the amylose content was microwave dried >freeze dried> air dried>oven dried. Drying methods had a significant effect (P<0.0001) on the solubility index and swelling capacity of the dried samples investigated. The rank order of the swelling capacity of the ginger starches was freeze dried<air dried<oven dried<microwave dried. A higher solubility index was observed among the oven-dried sample and the microwave sample compared to freeze dried and air dried samples. X-ray fluorimetric (XRF) analysis of the different starch powders showed the presence of iron, copper and zinc in trace amounts; and the absence of heavy metals like lead and mercury. All the four dried samples have fairly good flow. Significant differences were observed in individual pasting parameters of the ginger starches especially in peak viscosity, trough viscosity, final viscosity and setback viscosity. Peak viscosity was found to be lowest for freeze dried starch (300.42RVU) and highest for oven dried starch (324.25RVU). The rank order of the final viscosity was oven dried > microwave dried > air dried>freeze dried.
Conclusion: This study revealed that the physicochemical as well as the pasting properties of the ginger starches prepared by the four drying methods make them to be considered as excellent resource with possible applications in many food and pharmaceutical processing. The results also showed that difference in drying methods during processing has an effect on composition and pasting properties of ginger starch.

Open Access Original Research Article

Analgesic and Anti-inflammatory Activities of the Fruit Extract of Ampelocissus latifolia (Roxb) on Laboratory Animals

B. K. Das, U. K. Fatema, M. S. Hossain, R. Rahman, M. A. Akbar, F. Uddin

Journal of Pharmaceutical Research International, Page 1477-1485
DOI: 10.9734/BJPR/2014/8702

Aim of Study: This study was aimed to evaluate the possible analgesic and anti-inflammatory properties of the ethanol extract of fruit of Ampelocissus latifolia (Roxb).
Study Design: Assessment of analgesic and anti-inflammatory activities.
Place and Duration of Study: Department of Pharmacy, North South University, Dhaka, Bangladesh, between June 2012 and March 2013.
Methodology: The crude ethanol extract was investigated for the anti-inflammatory effect on Long Evans rats using carrageenan induced rat paw edema method. For anti-inflammatory study, 20 rats were divided into 4 different groups, each receiving either distilled water, standard drug or the extract at the doses of 250 and 500mg/kg body weight (BW). The analgesic activity was evaluated by hot plate and acetic acid induced writhing method in Swiss albino mice divided into 4 different groups (control, standard and extract at two different doses of 250 and 500 mg/kg BW).
Results: The results of preliminary phytochemical study revealed the presence of alkaloids, flavonoids, tannins, glycosides in significant amounts. The results of anti inflammatory activity study showed that the fruit extracts at a dose of 250 mg/kg and 500 mg/kg inhibited carrageenan-induced paw edema in Long- Evans rats. Both the extracts were able to show a dose dependent anti-inflammatory activity as compared to diclofenac sodium used as a standard drug. The extract elicited a highly significant (p<0.001) analgesic activity in a dose dependent manner on hot plate method, acetic acid-induced writhing test. In the hot plate method, the extract increased the reaction time of heat sensation to 94.71% and 82.7% at the doses of 250 and 500 mg/kg BW while that of the standard drug was 61.45% at the 3rd hour of study. In acetic acid induced writhing test, the percent inhibition of writhing response by the extract was 50.57% and 59.77% at 250 and 500 mg/kg doses respectively (p<0.001).
Conclusion: The anti-inflammatory and analgesic effect of the ethanol fruit extract of Ampelocissus latifolia (Roxb) may be due to the presence of various chemical constituents especially flavonoids, tannins, alkaloids or terpenoids. These experimental findings would further establish the scientific basis of the traditional uses of the plant in the management of inflammatory conditions as well as control of pain.

Open Access Original Research Article

Medicinal Potential of Phyllanthus emblica (Linn.) Fruits Extracts: Biological and Pharmacological Activities

S. M. Moazzem Hossen, Raihan Sarkar, Siam Mahmud, N. M. Abdul Aziz

Journal of Pharmaceutical Research International, Page 1486-1499
DOI: 10.9734/BJPR/2014/10307

Phyllanthus emblica (Linn.) is a common plant and fruits very popular in Bangladesh. It is a common ingredient of many traditional and herbal medicines. The intention of the present study was to explore the scientific relation with the traditional use of the fruit of Phyllanthus emblica (Linn.). Antimicrobial screening, analgesic activity, antidiarrheal activity and the brine shrimp lethality test for cytotoxic activity screening are the selected pharmacological activities. Phytochemical analysis of ethanolic fruits extract confirms that the fruit contain flavonoids, alkaloids, tannin, steroids, reducing sugar and gum. Experimental screening confirms that the fruit extract produced 19.07% and 38.67% writhing inhibition at the oral dose of 250 and 500mg/kg-body weights respectively. That means ethanol extract of the fruit of Phyllanthus emblica (Linn.) has an analgesic property. The ethanolic fruit extract of Phyllanthus emblica (Linn.) also significantly inhibited ear edema formation in xylene induced ear edema, considered as direct evidence that supporting the anti-inflammatory activity of ethanolic fruit extract of Phyllanthus emblica (Linn.) The fruit extract ha a remedy for a different bacterial disease is supported by the antibacterial screening tests. During the antidiarrheal activity screening at the dose of 500mg/kg-body weight, Phyllanthus emblica (Linn.) showed a moderate antidiarrheal activity in castor oil induced test in mice and caused an increase in latent period i.e. delayed the onset of diarrheal episode and decreased the frequency of defecation. T-test of these responses showed that the result is significant throughout the observation period. The ethanolic fruits extract have cytotoxic activity and test sample showed different mortality rate at different concentrations. The LC50 values were found to be 60µg/ml for the crude extract. The 90% mortality (LC90) values were 100µg/ml respectively. According to the results of the present investigation, we can conclude that the ethanolic fruits extract of Phyllanthus emblica (Linn.) has significant analgesic, anti-inflammatory, antimicrobial, anti-diarrheal and cytotoxic effects. This study also suggests us to isolate the active compound(s) responsible for those pharmacological properties.

Open Access Original Research Article

Availability of the Drugs for Malignant Diseases Treatment: Comparison between Developing and Developed Countries

Ankica Jelenković, Marija Ristić, Ivica Pejčić, Dušan Ristić, Bogdan Bošković

Journal of Pharmaceutical Research International, Page 1500-1520
DOI: 10.9734/BJPR/2014/9595

Aim: The financial burden of malignant diseases treatment has increased remarkably over the years. This is due to, among many reasons, the costs of drugs, especially those of the new classes. Thus, it is of interest to assess the availability and differential cost of anti-cancer drugs in developing countries compared to developed countries.
Study Design: The study was designed to determine the anti-cancer drugs availability in the world, in the United States of America (USA), the United Kingdom (UK) and the Republic of Serbia (RS), with the aim to get insights into the similarities and differences between developed and developing countries toward anti-cancer drugs availability, as well as the prices of these drugs. This analysis was based on three drug data bases for anti-cancer drugs that were available during 2011 and 2012 year in the world, USA, UK, and RS.
Results: About 37% of anti-cancer drugs that were present in the world market in 2011 year were also present in the RS (the drugs that were reimbursed by the state health insurance), compared to 74.8 and 67.4% that were available in the USA and the UK, respectively. Furthermore, out of all drugs registered in 2012 in the UK, 62.8% were present in the RS and almost all pharmacological groups were represented with some drugs, including very expensive ones like the biological agents. Most of the drugs in the RS were cheaper, regardless of whether they belonged to nonproprietary or brand-name drugs. These findings could be the result of the very low national gross domestic product in the RS and thus, the small funds earmarked for the health care.
Conclusion: The Republic of Serbia, which belongs to developing countries, face some difficulties in taking care of patients with malignant diseases where the prominent place have drugs for malignant diseases treatment, especially the newer classes, which are usually more expensive and generally do not provide the first-line treatment.

Open Access Original Research Article

Role of Magnesium Supplement on Hyperlipidemia and L-CAT Level in Patient on Atorvastatin Therapy

Sahar M. El-Haggar, Tarek M. Mostafa

Journal of Pharmaceutical Research International, Page 1521-1534
DOI: 10.9734/BJPR/2014/11145

Aim: This study aimed to evaluate the effect of magnesium supplement to atorvastatin on hyperlipidemic patients and to elucidate the possible ability of oral magnesium supplement to counteract or delay statins induced myalgia.
Study Design: Forty hyperlipidemic male and female patients were randomly divided into two groups: group one consisted of twenty patients, who received atorvastatin 10 mg once daily for 6 weeks then 20 mg once daily for another 6 weeks; group two consisted of twenty patients, who received the same dose of atorvastatin plus once daily oral low dose magnesium sulfate trihydrate 419.5 mg equivalent to 50 mg of magnesium.
Place and Duration of Study: The Laboratory of Pharmaceutical Research Center of Faculty of Pharmacy, Tanta University, Egypt, between July to December 2013.
Methodology: Two samples of venous blood (2 ml + 8 ml =10 ml total), were collected from all individuals, and were drawn from the antecubital vein before, 1.5 and 3 months after treatment. Sera and plasma were separated immediately for biochemical analyses of lecithin cholesterol acyltransferase (L-CAT) (ELISA), creatine kinase (CK), serum Ca+, Mg++, Na+, K+, lipid profile and aspartate transaminase (AST) (colorimetrically), and serum creatinine (S.Cr) spectrophotometrically.
Results: The statistical analysis revealed that, 3 months after treatment, both groups showed significant amelioration in lipid profiles and significant elevation in L-CAT level regarding to baseline data obtained before initiation of treatment. In addition, the patients received atorvastatin plus magnesium supplement showed significantly higher levels of serum magnesium, plasma L-CAT and HDL-cholesterol concentrations and significantly lower total cholesterol, LDL-cholesterol and triglycerides concentrations with non significant lower CK level as compared to the patients group received atorvastatin solely.
Conclusion: Mg++ supplement to atorvastatin improve all lipid profile and provide better control on dyslipidemia than atorvastatin alone. However, Mg++ supplement to atorvastatin doesn’t prevent elevation in CK; it may delay and provide some protection against statin induced myopathy that in turn may increase patient compliance.

Open Access Original Research Article

Novel Tuberculostatic Agents Suitable for Treatment of Mycobacterium tuberculosis Infections of the Central Nervous System

Ronald Bartzatt, Preeti Sule, Suat L. G. Cirillo, Jeffrey D. Cirillo

Journal of Pharmaceutical Research International, Page 1535-1551
DOI: 10.9734/BJPR/2014/10353

Aims: To demonstrate the efficacy of five small molecule compounds for inhibiting the growth of Mycobacterium tuberculosis. To present evidence that these compounds will penetrate into the central nervous system.
Study Design: Five small molecule compounds bearing a hydrazide group were synthesized utilizing microwave excitation. These compounds were then placed into tissue culture with Mycobacterium tuberculosis at various concentrations for evaluation of bacterial growth inhibition.
Place and Duration of Study: The compounds to be tested were prepared at the University of Nebraska Chemistry Department August 2013. The evaluation of antibacterial activity was determined at the Texas A&M Health Science Center during October to December of 2013.
Methodology: Applying microwave excitation for generation of hydrazide groups within the structure of small molecule carboxylic acids, five agents were prepared for evaluation of bacterial growth inhibition. These agents were dissolved into tissue culture media at various concentrations. Having various levels of tuberculostatic agents, then tuberculosis bacteria were added to determine level of growth inhibition. Growth inhibition of the bacteria was achieved and measured by compound concentration for comparison and evaluation.
Results: Five compounds having a hydrazide functional group greatly inhibited the growth of Mycobacterium tuberculosis. All five agents had molecular weight less than 215 grams/mole and polar surface area of less than 70 Angstroms2. Values of Log P ranged from -0.226 to 0.998. Values of Log BB (Log [Cbrain/Cblood]) ranged from -0.711 to - 0.525, with a range in central nervous system penetration Cbrain/Cblood of 0.195 to 0.299. All compounds showed zero violations of the Rule of 5. Substantial inhibition of bacterial growth was observed at concentrations as low as 30 micrograms/mL, as measured by optical density and colony forming units.
Conclusion: These five hydrazide compounds substantially decreased the proliferation of tuberculosis bacteria at concentrations as low as 30 micrograms/mL. In addition, their physicochemical properties are shown to allow high levels of penetration into the central nervous system.

Open Access Original Research Article

Antimicrobial and Cytotoxic Activities and GC-MS Analysis of Phytocomponents of Methanolic Extract of Curculigo pilosa (Schum and Thonn) Engl. (Hypoxidaceae) Rhizomes

Elijah Y. Shaba, Abdullahi Mann, Jonathan Yisa

Journal of Pharmaceutical Research International, Page 1552-1567
DOI: 10.9734/BJPR/2014/10189

Objectives: To investigate the antimicrobial and cytotoxic activities of crude methanol extract of Curculigo pilosa (Schum and Thonn) Engl. (Hypoxidaceae) rhizomes and its solvent soluble fractions and to analyze the most active fraction by Gas Chromatography Mass Spectrometry (GC-MS) technique.
Place and Duration of Study: Department of Chemistry and Department of Microbiology, School of Natural and Applied Sciences, Federal University of Technology, Minna, Nigeria in June, 2012.
Methodology: Shade air-dried powder of Curculigo pilosa rhizomes was extracted with methanol by Soxhlet extraction. Crude methanol extract of Curculigo pilosa root (CCPM) and the solvent soluble fractions namely: n-hexane (CPH), chloroform (CPC), ethylacetate (CPE), n-butanol (CPB) and residue (CPM) were obtained. Phytochemical constituents of the most active fraction (methanol residue) of Curculigo pilosarhizomes were determined using GC-MS technique.
Results: The antimicrobial activity of some solvent fractions tested except n-hexane fraction appears to be promising with Minimum Inhibitory Concentration (MIC) ranging from 0.09–6.25 mg/mL. However, ethyl acetate and n-butanol fractions showed antibacterial activity against highest number of bacterial strains. The results revealed that methanolic residue was more potent than derived fractions. Cytotoxicity assay results indicated weak cytotoxic activity of the crude C. pilosa methanol root extract as displayed by its LC50(764.07μg/mL). The qualitative phytochemical evaluation indicates the presence of chemical constituents such as flavonoids, terpenoid, saponins, tannins, alkaloids, cardiac glycosides, steroid and anthraquinone. The quantitative analysis of its metabolites depicts alkaloids (12.80±0.49), saponins (54.49±0.33), flavonoids (44.88±0.36), tannins (69.49±0.65), phenols (50.40±0.34), oxalates (10.95±0.63), cyanides (44.87±0.70) and phytate (15.00±0.05). The major phytocomponents identified by GC-MS analysis in the combined fractions of C. pilosa methanolic residue indicated that there were different types of high and low molecular weight compounds. In particular, it revealed the presence of 3-eicosyne (8.98%), pentadecanoic acid (2.41%) hexadecanoic acid (31.18%), octadecanoic acid (1.52%) 9-octadecenoic acid (24.42%), linoleic acid ethyl ester(3.93%), androstan-3-one (5.90%), 1-phenanthrenenmethanol (5.78%), 1,2-benzenedicarboxylic acid (4.59%), hexanedioc acid (13.38%), 8,11-octadecadienoic acid (9.02%), nonadecane (3.52%), ethanol-2, 2-oxybis (20.75%), propane-1-(1-methylethoxy) (8.05%) and 2, 6,10-dodecatriene-1-ol (5.14%).
Conclusion: In this study, some of the phytocompounds identified are biologically important and may have contributed to the observed antimicrobial activity, hence their therapeutic significance which may support the ethnomedicinal uses of C. pilosa in the treatment of venereal diseases in humans.

Open Access Review Article

Herbal Drug Development from Traditional Formulations: Refocusing Pharmaceutics and Posology for Accelerated Validation

Sunday J. Ameh, Barnabas K. Toge, Benjamin U. Ebeshi, Aminu A. Ambi, Magaji Garba, John Alfa, Karniyus S. Gamaniel

Journal of Pharmaceutical Research International, Page 1451-1476
DOI: 10.9734/BJPR/2014/10617

Background: The World Health Organization (WHO) recommended that the toxicity data of a traditional medicine (TM) product that has been in use for 20 years or more without untoward effects should be determined, as the first step in its research and development (R&D). Such data in conjunction with efficacy data would be used to develop an appropriate dosage form of the product. A key objective in researching such a product is to validate the basis of the therapy, including the formula. Such validation, and any attempt to modernize the product, should be guided by an understanding of the traditional know-how. The Nigerian National Institute for Pharmaceutical Research and Development (NIPRD) utilized this approach in developing Niprisan, an antisickling drug, based on a TM product used since antiquity in Yoruba Medicine.
Aim: This article aimed to advocate the continuance and improvement of the WHO model of herbal drug research and regulation (HDRR) as the most logical approach for adoption by researchers and regulators.
Methodology: NIPRD’s adoption of the WHO model since 1989 was reviewed in parallel with trends in herbal drug research worldwide; and within the contexts of regulatory practices by Nigeria’s National Agency for Food and Drug Administration and Control (NAFDAC) and the European Medicines Evaluation Agency (EMEA), with a view to identifying more effective strategies within the WHO paradigm for HDRR.
Conclusion: Drug regulatory agencies (DRAs) like NAFDAC require effective laws, policies and quality management systems (QMS) to execute their mandates effectively. On the other hand, NIPRD’s output depends upon proper actions by a seasoned and responsive DRA. Therefore, noting that NIPRD and NAFDAC were both created by military decrees in 1989 and 1992 respectively, rather than by parliament acts, it is recommended that in addition to instituting more effective laws and policies to regulate NAFDAC, both NIPRD and NAFDAC need to adopt and implement suitable QMS for self-regulation, eg: ISO 9001 for whole organizations; and ISO/IEC 17250 for the laboratories.