Open Access Original Research Article

Anthelminthic Activity of Annona reticulata Seed Extracts

D. R. Yashwanth Kumar, A. B. Vedamurthy, H. Joy Hoskeri

Journal of Pharmaceutical Research International, Page 669-675
DOI: 10.9734/BJPR/2014/6055

Aims: To evaluate the anthelminthic activity of Annona reticulata seeds extracts against Pheretima posthuma.
Study Design: Helminth infections have tormented humans and animals for thousands of years. The indiscriminate uses of the anthelminthic drugs have lead to the emergence of resistant helminths against many anthelminthic agents. Thus the need for the treatment of helminthic infections and the prevention of the emergence of resistant strains has led to the screening medicinal plants for their anthelminthic activity.
Place and Duration of Study: Department of Biotechnology, The Oxford College of Science, Bangalore, Karnataka, India, between January 2012 and March 2012.
Methodology: The main aim of the present exploratory study is to evaluate the anthelminthic activity of A. reticulata seeds extracts. The in vitro studies revealed that the anthelminthic effects of crude chloroform and ethanolic extracts of A. reticulata on Pheretima posthuma was evident from induction of paralysis and mortality. Piperazine citrate was used as the standard reference drug and normal saline as a control group.
Results: Among all the concentrations of chloroform and ethanolic extracts tested, 12.5 mg/ml showed significant (p<0.01) anthelminthic activity. The results indicated that the ethanolic extract of A. reticulata is a more potent anthelminthic agent against Pheretima posthuma when compared with chloroform extract but less potent when compared with the standard drug.
Conclusions: The results of this investigation justifies the use of the seed extracts of A. reticulata in traditional medical practice for the treatment of helminth infections.

Open Access Original Research Article

Dynamic Changes in Antioxidant Activity during Floral Development of Couroupita guianensis

Saran Kumar Gupta, Mitali Ghosal, Dibakar Choudhury, Palash Mandal

Journal of Pharmaceutical Research International, Page 676-694
DOI: 10.9734/BJPR/2014/8106

Aims: To establish and optimize the in vitro antioxidant activity of methanolic extract of flower of C. guianensis at different developmental stages.
Place and Duration of Study: Plant Physiology and Pharmacognosy Research Laboratory, Department of Botany, University of North Bengal, Siliguri, between December 2010 and November 2011.
Methodology: The antioxidant activities of methanolic extracts of C. guianensis flower of different developmental stages were investigated spectrophotometrically against DPPH, ABTS, H2O2, NO, superoxide, hydroxyl radical and lipid peroxidation, along with ferric reducing power, metal chelating and β-carotene bleaching assay were performed. Total phenols, flavonoids and ortho-dihydric phenols were also determined by folin-ciocalteu, aluminium chloride and Arnow's reagent based standard methods respectively.
Results: The methanolic extract of floral stage-I was found to possess higher level of phenolic content, flavonoids as well as ortho-dihydric phenol content. The younger floral stages, stage-I and stage-II were observed with highly potential free radical scavenging activity, while stage-III showed highest degradation rate for β-carotene bleaching assay and stage-IV showed highest anti-lipid per oxidation activity against thiobarbituric acid.
Conclusion: The results demonstrated that the early floral stage showed the highest polyphenolic content and best antioxidant activity, therefore the early stages of this flower is suggested as the best harvest stage for medicinal purposes. Further studies are required for the isolation of active principles responsible for its antioxidant activity.

Open Access Original Research Article

Purification and Structure Elucidation of the Polyether Antibiotic Alborixin from Streptomyces pulcher CRF17

Imran Sajid, Khaled A. Shaaban, Shahida Hasnain

Journal of Pharmaceutical Research International, Page 695-704
DOI: 10.9734/BJPR/2014/5721

Aims: To screen Streptomyces sp. from saline soil in Pakistan, for its antimicrobial activity and to purify and identify the active metabolites produced by mass spectrometry and NMR spectroscopy. Strain identification by morphological, biochemical, physiological characterization and by 16S rRNA gene sequencing.
Study Design: Cultivation in lab fermenter, solvent extraction and purification of the compounds by column chromatography, identification of the compounds by mass spectrometry and NMR spectroscopy, determination of the antimicrobial activity and cytotoxicity.
Place and Duration of Study: Department of Microbiology and Molecular Genetics, University of the Punjab, Lahore, Pakistan and Institute of Organic and Bio molecular Chemistry, University of Göttingen, Germany, between February, 2007 and April, 2009.
Methodology: The strain was cultivated in a 20 liter fermenter (working volume 10 liters) and the culture broth was extracted with ethyl acetate, acetone and methanol. The resultant crude extract was fractionated on silica gel and the components were purified by column chromatography (silica gel, sephadex column and preparative TLC). The pure component was identified by mass spectrometry (ESI and HRESI-MS), NMR analysis (1H and 13C NMR) and by comparison with reference data, the antimicrobial activity and cytotoxicity was determined by disc diffusion assay and by micro well cytotoxicity assay against Artimia salina.
Results: The morphological, biochemical and physiological characterization suggested that isolate CRF17 belongs to the genus Streptomyces. Further NCBI BLAST of the partial 16S rDNA gene sequence 1420 bp (gene bank accession number: EU294134) from the isolate CRF17 showed 99% identity and 98% query coverage towards Streptomyces pulcher. The scale up fermentation of the isolate CRF17 yielded active compound and was identified as alborixin (1).
Conclusion: The isolate Streptomyces pulcher CRF17 is a potent producer of the antibiotic alborexin and can be exploited for its commercial production.

Open Access Original Research Article

Antiplasmodial Activity of Leaf Extracts of Zanthoxylum chalybeum Engl.

Godfrey S. Bbosa, Norah Mwebaza, Aloysius Lubega, Nathan Musisi, David B. Kyegombe, Muhammad Ntale

Journal of Pharmaceutical Research International, Page 705-713
DOI: 10.9734/BJPR/2014/6528

Background: Medicinal herbs have long been used in the treatment of malaria in the endemic tropical and subtropical regions of the world, especially in sub-Saharan Africa where malaria has remained as a top killer disease to children under five years and expectant mothers. Among the herbs commonly used in Uganda to treat malaria is Zanthoxylum chalybeum (ZC) root-bark and to a lesser extent its leaves. However, the continued use of the root-bark has led to plant extinction due to the destructive method of harvesting the herb as opposed to the leaves.
Aim: The study investigated the antiplasmodial activity of the crude ether and methanol leaf extracts of ZC with chloroquine diphosphate as a positive control.
Materials and Methods: The in vitro Micro-Test (MARK III) kit was used to determine the antiplasmodial activity of Z. chalybeum Engl. ether and methanol extracts. The effective concentration that caused a 50% P. falciparum schizonts suppression (EC50) values were determined. The antiplasmodial activities of the ether and methanol extracts were expressed as 50% effective concentration (EC50) that was determined from dose-response curve by non-linear regression analysis (curve-fit) using GraphPad Prism (version 6) software at 95% confidence intervals.
Results: The results showed that ether extract of ZC had EC50 value of 13.39 (95% CI: 10.82 – 16.59) µg/ml and methanol extract had EC50 value of 8.10 (95% CI: 5.89 – 11.12) µg/ml. The chloroquine diphosphate, standard had EC50 value of 25.33 (95% CI: 17.07 – 37.60) µg/ml.
Conclusion: The ether and methanol extracts of Z. chalybeum Engl. contains compounds that caused Plasmodium falciparum schizonts suppression at a lower concentration, hence the continued use of the herb by the traditional herbalist and local communities in Uganda, in the treatment of malaria.

Open Access Original Research Article

Adverse Drug Reaction Reports in an Antiretroviral Treatment Centre in Jos, North Central Nigeria

L. O. Ogwuche, V. B. Ojeh, I. A. London, N. Naima, C. Dady, A. I. Finangwai, I. O. Abah, K. D. Falang, P. Agaba, O. A. Agbaji

Journal of Pharmaceutical Research International, Page 714-721
DOI: 10.9734/BJPR/2014/6520

Background: Reports of adverse drug reactions (ADR) in the era of increasing uptake of antiretroviral drugs particularly in Sub Saharan Africa and especially in Nigeria have been on the rise.
Aim: We set out to collate and characterize the pattern of adverse drug reactions in patients on antiretroviral drugs in our treatment centre.
Study Design: Retrospective Cross sectional study
Place and Duration of Study: The study was carried out at the APIN Centre, Jos University Teaching Hospital, Plateau State, North Central Nigeria from July 2010 to December 2012.
Methodology: We reviewed the case files and data base entries of 215 patients attending our treatment centre. These are patients who had reported cases of adverse drug reactions. We took note of demographic profiles of the patients, the medical history as well as the different types of antiretroviral drugs the patients were taking. The types of adverse drug reactions and offending drugs were noted and categorized using descriptive statistics.
Results: Out of 215 case files and databases of patients in which there were reports of adverse drug reactions, 80 (37.2%) were male and 135 (62.8%) were female. Almost thirty two percent (31.6%) of the patients were on Zidovudine/Lamivudine/Nevirapine (AZT/3TC/NVP), 14.9%on Zidovudine/Lamivudine/Tenofovir/Lopinavir/ritonavir (AZT/3TC/TDF/LPV/r), 13.5% on Stavudine/Lamivudine/Nevirapine (D4T/3TC/NVP). Anemia was the most common ADR representing 23.4% of all ADRs and 29.3% of all ADRs were associated with Zidovudine.
Conclusion: Our study shows that in antiretroviral treatment centre such as our own, healthcare providers/practitioners should take particular note of troubling adverse drug reactions such as anaemia. Healthcare providers/practitioners should particularly have in place alternative treatment regimens as these adverse drug reactions may be potential cause of medication non adherence which in the long run lead to treatment failure.

Open Access Original Research Article

Development and Validation of First Derivative Spectrophotometric Method for Quantification of Darunavir in Tablets

Josilene Chaves Ruela Corrêa, Cristina Helena dos Reis Serra, Hérida Regina Nunes Salgado

Journal of Pharmaceutical Research International, Page 722-730
DOI: 10.9734/BJPR/2014/6326

Aims: Darunavir is widely used in HIV/AIDS therapy. It is a HIV protease inhibitor that has excellent efficacy against the virus. The aim of this study is to develop and validate an analytical method fast and free of interferences for determination of darunavir ethanolate as raw material and tablet dosage form.
Methodology: As the formulation excipients show high interference in darunavir determination by a direct UV absorption measurement a derivative spectrophotometry was applied. A selective, easy and fast method was achieved employing simple and cheap instrumentation by using first-order derivative spectrophotometry.
Results: The first-derivation of spectrum of the drug measured between 200 and 400 nm allowed identification of the analyte and showed absence of placebo interference. The assay was based on the absorbance at 276nm. The linear concentration range was established from 11 to 21 μg/mL. The intra-day and inter-day precision expressed as RSD was 0.06% and 3.75% respectively with mean recovery of 99.84%.
Conclusion: The proposed analytical method is able to quantify darunavir as raw material and tablets and can be used routinely by any laboratory applying a spectrophotometer with a derivative accessory. The great difference of the method proposed here is that it proves to be free of placebo interferences as well as simple, fast and low cost.

Open Access Original Research Article

A Study of Serum Levels of Select Heavy Metals and Histology of Brain, Lung, Heart and Ileum of Rats Chronically Exposed to Kerosene

Ayobola A. Iyanda

Journal of Pharmaceutical Research International, Page 731-738
DOI: 10.9734/BJPR/2014/2983

In rural Africa, a number of alternative treatment options are explored because of poverty and unawareness. Kerosene is one such agent used for the treatment of a myriad of diseases. The aim of the study was to investigate the effects of trace amounts of kerosene on lung, heart, brain and intestine in rats. Eighteen rats were used consisting of 6 rats per group. The first and second groups were administered kerosene (0.4 ml of kerosene/kg body weight) through oral and dermal route respectively. Six other rats served as the control. Results showed significant damage to all the tissues examined; with pathologic presentation comprising of pulmonary congestion, severely stunted villi, congestion of coronary vessels, and diffuse spongiosis of the cerebral cortex in kerosene administered group while control group featured no visible lesion. Although As, Al and Cd were not significantly different in kerosene exposed groups compared with control, Si was significantly lower (oral), and significantly increased (dermal) (p<0.05) compared with control. Results of this study suggest that exposure to even small quantities of kerosene may damage a variety of organs/tissues in the body and its exposure to human subjects for whatever reason should be discouraged.

Open Access Original Research Article

Comparative Phytochemical Screening and In vitro Evaluation of Biological Activities between Aqueous and Ethanolic Extract of Momordica charantia L. Fruits

Abhijit Das, Palash Karmakar, Md. Golam Kibria, Pankaj Chandra Debnath, Mohammad Safiqul Islam, Mohammad Mafruhi Sattar

Journal of Pharmaceutical Research International, Page 739-750
DOI: 10.9734/BJPR/2014/7364

Aims: The study was conducted to compare the presence of different phytochemicals and biological activities like cytotoxicity, anthelmintic activity, antioxidant and free radical scavenging activities between aqueous and ethanolic extract of Momordica charantia L. Fruits.
Methodology: The cytotoxic assay was undertaken using brine shrimp lethality test (BSLT) while the anthelmintic activity was carried out with the determination of time of paralysis and death of earthworm (Pheritima posthuma) at five different concentrations. Antioxidant and free radical scavenging activities were measured by 1,1-diphenyl-2-picryl-hydrazyl (DPPH) method and determining the total phenolic contents.
Results: Study revealed that several phytochemicals were found common for both of the extracts, though proteins and amino acids were only found in ethanolic extract. Both the extracts showed mild cytotoxic activity where the ethanolic extract showed better potency (LC50=24.245 µg/ml) than aqueous extract (LC50=24.515 µg/ml). In case of anthelmintic activity, ethanolic extract was also found significantly potent than aqueous extract at five different concentrations. IC50 values for the total antioxidant activity were 304.41±0.903 µg/ml and 479.05±1.393 µg/ml for ethanolic and aqueous extract, respectively. Ethanolic extract contained a significantly higher concentration of total phenols (71.08 ± 0.380 mg of GAE/g of extract) in comparison to aqueous extract (57.33±0.520 mg of GAE/g of extract).
Conclusion: Therefore, in all aspects of the study, ethanolic extract was found more potent than aqueous extract. It can be concluded that M. charantia fruits are abundant of various phytochemicals and possess versatile biological activities.

Open Access Original Research Article

In vitro and In vivo Antitrypanosomal Effects of Petroleum Ether, Chloroform and Methanol Extracts of Artemisia maritima Linn

A. C. Ene, S. E. Atawodi, Y. E. O. Apeh

Journal of Pharmaceutical Research International, Page 751-758
DOI: 10.9734/BJPR/2014/7631

Petroleum ether, chloroform and methanol extracts of the whole plant of Artemisia maritima Linn were studied in vitro and in vivo for antitrypanosomal activity against Trypanosoma brucei brucei in Swiss albino mice. The extracts were also screened for phytochemicals/secondary metabolites. All the extracts showed trypanocidal activity against T. brucei brucei in vitro with the petroleum ether extract showing the highest activity. The in vivo study revealed that only the chloroform extract A. maritima exhibited antitrypanosomal activity. This extract at a dose of 100mg/kg body weight significantly (p<0.05) reduced the parasitemia in T. brucei brucei infected mice when compared with the other treatment groups. The chloroform extract of A. maritima at this dose reduced the level of parasitemia to 26%. This reduction in the level of parasitemia is statistically significant (p<0.05) compared to the other treatment groups and the untreated control group. The result of the phytochemical analysis revealed that the extracts contain secondary metabolites like flavonoids, terpenoids, steroids, anthraquinones and alkaloids. The presence of these secondary metabolites in this plant might be responsible for the antitrypanosomal activity exhibited by its extracts.

Open Access Original Research Article

Comparative Study of Anticonvulsant Property among Different Fluoro Substituted Synthesized Benzothiazole Derivatives

I. Shanmukha, A. M. Madhusudhana, E. Jayachandran, M. Vijay Kumar, B. Prakash

Journal of Pharmaceutical Research International, Page 759-769
DOI: 10.9734/BJPR/2014/6876

Objective: The present study is to evaluate antiepileptic activity of some fluoro benzothiazolo oxadiazolo quinazoline and sulfonamido quinazoline derivatives.
Background of the Study: Epilepsy is a chronic disorder of the brain, characterized by the periodic and unpredictable occurrence of seizures. Epilepsies affect around 1–2% of the world population including the fact that the convulsions of approximately 25% of epileptics are inadequately controlled by medication.
Materials and Methods: Albino mice (weighing 20-25g) of either sex were used in this study. MES seizures were induced in mice by delivering electroshock of 60ma for 0.2 seconds by means of an electro- convulsiometer transauricularly through a pair of ear clip electrodes. Both test animals and standard group received diazepam (5mg/kg) p.o strychnine nitrate (1 mg/kg) was administered.
Results and Discussion: MES induced convulsion the mentioned dose was administered one hour prior to MES elicitation. It was observed that all SSBDs except ap-7, bz-10 and s-5 shown significant anticonvulsant effect. The results are compiled in the Table 1 and graphically depicted in Figs 1 and 2 respectively.
Conclusion: The present investigation revealed that the SSBDS ap-3, ap-6 and bz-9 were shown significant anticonvulsant activity against both MES and strychnine induced models.