Open Access Short Research Article

In vitro Cytotoxicity of Scopoletin Derived from Eupatorium laevigatum Lam.

Ivana Grivicich, Rodrigo Noronha de Mello, Alexandre Quadros Ledel, Tatiana Moreira da Silva, Daiane Lopes da Silva Dieter, Felipe Umpierre Conter, Mariana Sagrillo Grossi, Alexandre Barros Falcão Ferraz

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/BJPR/2016/29662

Aims: Eupatorium laevigatum Lam. is commonly used as anti-inflammatory, antiseptic, anti-rheumatic, and in the treatment of colds and ulcers. The present study aimed to characterize the active fractions of the aerial parts of E. laevigatum, isolate its major constituents and to evaluate its cytotoxic effects against human tumor cells. 

Methodology: Phytochemical analysis of the aerial parts of E. laevigatum detected the presence of flavonoids, saponins and coumarins. Nuclear magnetic resonance with carbon and hydrogen determined that coumarin to be scopoletin. The human cancer cell lines HT-29, NCI-H460, MCF-7 and RXF-393 were used to evaluate cytotoxicity through the sulforodamine B assay as well the evaluation of oxidative damage through the thiobarbituric acid reactive species assay.

Results: Our study has shown that E. laevigatum crude extract and chloroform, ethyl acetate and butanol fractions are not cytotoxic in the concentrations used (up to 100 µg/mL), but the coumarin scopoletin isolated from the aerial parts of E. laevigatum presented a cytotoxic effect against NCI-H460 and RXF-393 cells (IC50 value of 19.1 and 23.3 µg/mL, respectively). Scopoletin did not show any oxidative effect.

Conclusion: The coumarin scopoletin can be found in E. laevigatum and this compound induces cytotoxicity in NCI-H460 and RXF-393 cell lines. Moreover, it is suggested that the cytotoxic effect of scopoletin is no related to oxidative damage.

Open Access Original Research Article

Pharmacological Study of Dopamine Receptors Agonist and Antagonist on Mouse Model of Myocardial Injury

Mohamed F. Shalaby, Alsayed A. Zaki

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/27706

Objective: The present study was designed to evaluate the potential protective effect of using mix of bromocriptine 7 mg/kg & metoclopromide 3 mg/kg on the inflammatory biomarkers AST, ALT and LDH1 against isoprotrenol-induced myocardial injury (MI) in mice model.

Methodology: Study the effect of dopamine, bromocriptine and metoclopramide on the blood pressure, myocardial inflammatory biomarkers and histological structure of the myocardial tissue. 35 adult male mice were divided into seven groups (5 mice each): group I, control group; group II, isoprotrenol treated group. Group III, Mice with MI were treated with dopamine (0.5/kg/day. IP) for 30 days. Group IV, Mice with MI were treated with bromocriptine (10 mg/kg/day, IP) for 30 days. Group V, Mice with MI were treated with metoclopromide (10 mg/kg. IP) for 30 days. Group VI, Mice with MI were treated with bromocriptine (3 mg/kg) & metoclopromide (7 mg/kg) for 30 days. Group VII, Mice with MI were treated with bromocriptine (7 mg/kg) & metoclopromide (3 mg/kg) for 30 days.

Results: Isoprotrenol induced MI was confirmed by disturbance in serum and heart tissue markers enzymes such lactate dehydrodenase, aspartate transaminase, alanin tranaminase and histopathological changes in the heart of Isoprotrenol administered mice. Mice with MI were treated with bromocriptine (7 mg/kg) & metoclopromide (3 mg/kg) for 30 days was found to ameliorate the effect of isoprotrenol induced histopathological changes, retained myocardial marker enzymes activities at near normal level.

Conclusion: The above results indicate the cardioprotective effect of mix of bromocriptine 7 mg/kg & metoclopromide 3 mg/kg aganist isoprotrenol-induced myocardial injury in mice.

Open Access Original Research Article

Knowledge and Practice of Prevention of Mother-To-Child-Transmission of HIV among Traditional Birth Attendants Practicing in Akwa Ibom, Nigeria

Unyime I. Eshiet, Polycarp G. Ekpe

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2016/28659

Background: Transmission of HIV from mother to child is by far the most common route of HIV infection in children. It is estimated that without effective interventions, between 67,500 and 125,000 infants will be infected with HIV annually in Nigeria. Traditional birth attendants assist in 60–80% of all deliveries and even more in the rural areas of developing countries including Nigeria.

Objective: This study is aimed at assessing the knowledge and practice of Prevention of Mother-To-Child-Transmission of HIV among Traditional Birth Attendants practicing in Akwa Ibom, Nigeria.

Methods: A descriptive, cross-sectional survey using well structured, validated and pre-tested questionnaires to interview 600 TBAs from 21 randomly selected local government areas of Akwa Ibom State to assess their knowledge and practice of prevention of mother to child transmission (PMTCT) of HIV.

Results: 96.8% (581) of the study population were aware of the existence of HIV/AIDS, however only 194(32.3%) of these respondents who were aware of the existence HIV/AIDS were also aware of mother-to-child-transmission (MTCT) of HIV. Furthermore only 83 (42.8%) of the 194 respondents who were aware of MTCT of HIV were able to state correctly the various routes through which MTCT of HIV could occur. In addition 174(89.7%) of our respondents who were aware of MTCT of HIV also believed that MTCT of HIV could be prevented. However only 121(69.5%) of these 174 respondents knew that PMTCT can be achieved through proper medical interventions.

Conclusion: The knowledge and practice of PMTCT of HIV by the TBAs practicing in Akwa Ibom, Nigeria is less than adequate thus increasing the risk of vertical transmission of HIV. There’s an urgent need for the education and training of TBAs to improve their knowledge and enhance their practice.

Open Access Original Research Article

Determination of Minimum Inhibitory Concentrations of 4,4’-diacetyldiphenylselenide in Antibacterial Activity

Nadjah Belattar, Youcef Mechehoud, Samir Benayache, Kaddour Benlabed, Narimane Segueni, Fadila Benayache

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/27183

Aim: The present study was focused on evaluation of antibacterial activity of 4,4’-diacetyldiphenylselenide against some bacterial species.

Introduction: Many compounds containing selenium element, notably 4,4’-diacetyldiphenylselenide, have started getting a great pharmacological interest as bioactive molecules insofar as the -In vitro - antimicrobial tests were carried out on different bacterial strains.

Methodology: The 4,4’-diacetyldiphenylselenide was synthesized in our laboratory and reported for the first time in 2010. The studied bacterial strains were collected from different places, some ones are standard strains and the others were clinically isolated and identified by biochemical tests.

The antibacterial property was evaluated via determination of Minimum Inhibitory Concentrations (MIC) using dilution method in the same conditions.

Results and Discussion: The most effective MICs are achieved at 16 µg/ mL for Providencia rettgeri, 32 µg/ mL for Salmonella typhimurium, 88 ±11.31 µg/ mL for  Serratia  liquefaciens, 128 µg/ mL for Shigella  dysenteriae, 144 µg/ mL for Morganella morganii, 200 µg/ mL , 200 ± 11.31 µg/ mL for  Proteus mirabilis and Acinetobacter baumannii respectively.

Conclusion: This study showed that 4,4’-diacetyldiphenylselenide is a bacteriostatic agent at determined Minimum Inhibitory Concentrations (MIC)  against several pathogenic bacteria.

Open Access Original Research Article

Alpha-amylase Inhibitory Compounds from Musa cavendishii

Mohammed S. Abdel-Raziq, Fatma M. Abdel Bar, Ahmed A. Gohar

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2016/29280

Aims: To investigate the ethyl acetate fraction from the methanol extract of the leaves of Musa cavendishii and to evaluate the alpha-amylase inhibitory activity of its isolated phytochemicals and their value as potential anti-obesity products.

Study Design: Isolation and identification of phytochemicals from the ethyl acetate fraction and investigation of their alpha-amylase inhibitory activity through In vitro screening and docking study.

Place and Duration of Study: Faculty of Pharmacy, Mansoura University, between June 2013 and July 2016.

Methodology: Different phytochemicals were isolated and purified using different chromatographic techniques from the ethyl acetate fraction of the extract of dried powdered leaves of Musa cavendishii. Elucidation of the structures of the isolated compounds was performed using different spectroscopic methods (1H NMR, 13C NMR, NOESY, HSQC and HMBC). Alpha-amylase inhibition assay was used to evaluate the inhibitory activity of the isolated compounds. Furthermore, docking study was conducted to get an insight about the binding mode of the active compounds within the active site of the target enzyme.

Results: (6S,9S)-roseoside 1-A was reported form the titled plant for the first time along with six reported compounds viz., (6S,9R)-roseoside 1-B, kaempferol-3-O-rutinoside 6, p-hydroxybenzoic acid 2, rutoside 7, catechuic acid 5, quercetin 4 and kaempferol 3. The diglucosides, kaempferol-3-O-rutinoside and rutoside exhibited better alpha-amylase inhibitory activity (80.45 and 98.0% inhibition, respectively) than the positive standard alph-amylase inhibitor (acarbose) used (57.0%) at a concentration of 50 µg/mL. In an agreement with the results of alpha-amylase inhibition assay, the docking results indicated that these two diglucosides 6 and 7, showed the highest binding scores (-8.16 and -7.68 kcal/mol) compared to positive standard acarbose (-5.40 kcal/mol).

Conclusion: This study showed that flavonoid diglucosides e.g. kaempferol-3-O-rutinoside and quercetin-3-O-rutinoside (rutoside) could be potential inhibitors for alpha-amylase and could be used as anti-obesity phytochemicals.

Open Access Original Research Article

Antiplasmodial Activity of Lantana camara in Mice Infected with Plasmodium berghei­

Vishavas L. Ranpariya, Sachin K. Parmar, Navin R. Sheth

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/27408

Aims: To investigate the antiplasmodial activity of Lantana camara L. (Verbenaceae) in mice infected with Plasmodium berghei­.

Study Design:  The plant extract was evaluated for its antiplasmodial activity in P. berghei infected mice model.

Place and Duration of Study: Department of Pharmaceutical Sciences, Saurashtra University, Rajkot, Gujarat, India, during June 2010 to August 2013.

Methodology: The schizonticidal potential of L. camara methanolic extract (LCME, 250 and 500 mg/kg, orally) was evaluated during the early stage (suppressive model), established infections (curative model) as well as the prophylactic model in Swiss albino mice. Chloroquine (CQ, 5 mg/kg) and pyrimethamine (PM, 1.2 mg/kg) were used as a reference standard drugs. The parasitemia levels were measured from thin smears made from tail blood of each mouse employed in the study. The curative activity of LCME was assessed from the mean survival time (MST). Rectal temperature measurement was used as a supportive parameter. Oxidant generation potential of the LCME was also evaluated to elucidate the probable mechanism of action.

Results: LCME exhibited significant antiplasmodial activity in both suppressive and prophylactic models. The effect was well-comparable to CQ and PM, respectively. The MST was found much longer in LCME-treated animals than the control ones. The rectal temperature was remained near to normal in these groups. The glutathione level was significantly lowered in LCME-treated groups.

Conclusion: In our study, the LCME exhibited a significant antiplasmodial activity in all three models (viz. suppressive, prophylactic and curative).

Open Access Original Research Article

Antimicrobial Activity of Camel’s Urine and Its Effect on Multidrug Resistant Clinical Bacterial and Fungal Isolates

Marwa Salah Mostafa, Reham Ali Dwedar

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/29342

Aims: The aim of this work is to study the In vitro antimicrobial effect of camel’s urine on a variety of multi-drug resistant bacterial and fungal isolates.

Methodology: Agar dilution method was used to determine the effect of different concentrations of camel’s urine (10%, 7.5%, 5% and 2.5%) on 50 clinical bacterial isolates including: 10 methicillin-resistant Staphylococcus aureus (MRSA), 10 multi-drug resistant coagulase negative staphylococci (CoNS), 10 multi-drug resistant Enterococcus spp., 10 extended spectrum β-lactamase (ESBL)–producing Gram-negative bacilli and 10 carbapenemase-producing Gram-negative bacilli. In addition, the antifungal effect of camel’s urine on four Candida albicans and one candida non albicans was also assessed.

Results: All used concentrations of camel’s urine produced complete inhibition of the growth of the four Candida albicans, Candida non albicans and the 10 CoNS isolates. The growth of MRSA, Enterococcus spp., ESBL-producing and carbapenemase-producing Gram-negative bacilli was completely inhibited by camel’s urine at concentrations 10%, 7.5% and 5%. However, these bacterial isolates showed significant growth at 2.5% camel’s urine concentration.

Conclusion: The present study provides clear evidence that camel’s urine has a strong antifungal and antibacterial effect against multi-drug resistant bacteria.