Open Access Minireview Article

How Nigella sativa Seeds Treat Diabetes and Ameliorates Diabetes Complications and Safety Studies: An Over View

Uzma Saleem, Shakila Sabir, Bashir Ahmad

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/30684

Nigella sativa is considered as a miracle drug. Although there is a list of diseases which can be treated by it but role of N.s seeds in treatment of diabetes is substantially important. There are multiple classes of antidiabetic agents which ameliorate the hyperglycemia by different ways. On the other hand, N.s as a single drug acts through multiple pathways to achieve normoglycemia. For instance, it enhances insulin production, glucose tolerance and beta cell proliferation. It reduces pancreatic inflammation, gluconeogenesis and glucose uptake from intestine. Interestingly, N.s not only improves the glycemic state but it also plays a significant role in the treatment of diabetes complications like neuropathy, nephropathy, cataract, dyslipidemia, cardiovascular disturbances, haematological abnormalities and atherosclerosis.

Open Access Original Research Article

Development and Evaluation of the Binding Properties of Raphia hookeri (Fam. Palmaceae) Gum in Pharmaceutical Tablet Formulations

Stephen O. Majekodunmi, Stanley Makper

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/28610

Aims: This study was aimed to evaluate the potential of using Raphia hookeri gum as a binder in tablet formulations.

Study Design: Extract of Raphia hookeri gum was investigated as a binding agent in paracetamol tablet formulation in comparison with gelatin BP as standard binder.

Place and Duration of Study: Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Uyo, Uyo, Nigeria.

Methodology: Different concentrations of 1, 2, 3, 4 and 5% w/w of Raphia hookeri gum and gelatin BP were used to formulate different batches of paracetamol tablets. The mechanical properties were assessed using crushing strength and friability tests while the drug release properties were assessed using disintegration time and dissolution time.

Results: The flow indices showed that granules formulated with Raphia hookeri gum did not possess good flow property whereas granules formulated with gelatin BP had a better flow property at all concentrations especially 5% w/w. The Carr’s Index and Hausner’s ratio fell within the acceptable limit of flow property. Tablets formulated with Raphia hookeri gum had better mechanical properties compared to those of gelatin BP. The crushing strength, disintegration and dissolution times increased with increased binder concentration while their friability decreased. Raphia hookeri gum produced tablets with stronger mechanical properties and longer disintegration and dissolution times than those containing gelatin BP.

Conclusion: This concludes/indicates that Raphia hookeri gum could be useful as a binding agent when high mechanical strength and slower release rates are desired as in controlled release formulations.

Open Access Original Research Article

Anti-angiogenic Potential of Mentha longifolia (Horse Mint): Chlorioallantoic Membrane Assay

Nazia Tabassum, Uzma Saleem, Bashir Ahmad

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/31083

Inhibition of angiogenesis is one of the mechanisms of action of anticancer drugs. The current study was designed to probe into anti-angiogenic effect of Mentha longifolia by employing Chorioallantoic membrane assay. White leghorn fertilized eggs were used in the study (n=10). On 6th day of incubation, aqueous solution of methanol extract (300-1000 µg/mL) of Mentha longifolia was applied to chicken embryos via CAM route. After 24 hours incubation, all eggs were opened carefully and CAM images were taken with camera. These images were loaded to SPIP software for quantification and assessment of structural changes in CAM. Blood vessels (primary, secondary and tertiary) diameters and CAM areas decreased in concentration dependent fashion in all treated groups as compared to values of control group. All embryos died at highest used concentration. It is concluded that methanol extract of Mentha longifolia possessed concentration dependent anti-angiogenic effect but toxic at 1000 µg/mL.

Open Access Original Research Article

Investigation of Enzymes Binding to “Voglibose- an Antidiabetic Drug” and the Choice of Enzyme to be Used for Biosensing

Shreedevi Kulkarni, Pramodkumar P. Gupta, Andhe Pallavi

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2016/30369

Aims: This paper mentions of the investigation of the enzymes binding to Voglibose and the choice of the enzyme which is suitable for drug enzyme interaction as used in biosensing. Voglibose is an antidiabetic drug which is reactive and hence used in very low concentrations. The existing methods of analysis of this drug are associated with certain disadvantages. Hence there is a need to establish alternative and simpler method of analysis which could be based on biosensing. The paper focuses on identification of the enzyme binding to the drug Voglibose.

Study Design: In this work there are two enzyme namely alpha amylase and alpha glucosidase which are considered as the potential targets for drug enzyme interaction for the drug Voglibose. The study is based on two approaches. The first one is molecular docking process done to verify the inhibition activity of the enzyme by the drug and the next method is chemical analysis to confirm the results obtained in molecular docking.

Place and Duration of Study: This experiment was carried out as a part of the project under Indian Nanotechnology User Program (INUP) at IITB, Mumbai.

Methodology: Molecular docking is a simulation procedure which is used to confirm the inhibition activity of alpha amylase and alpha glucosidase by Voglibose and compare their inhibition activities so as to choose the suitable enzyme for further applications. Chemical analysis is done to re-confirm the same and chose the target enzyme for biosensing applications.

Results: The docking experiments are done to show that Voglibose inhibits both alpha amylase and alpha glucosidase but a more stable complex is formed with alpha amylase and hence alpha amylase is used for the chemical analysis to reconfirm its inhibition by Voglibose. Thus, alpha amylase can be used as the target enzyme for drug enzyme interactions with Voglibose for further applications in biosensing.

Conclusion: The present In-silico and In-vitro swot analysis indicates that alpha glucosidase and alpha amylase binds to Voglibose. The interaction outcome from molecular docking and chemical analysis suggests that in future one can consider alpha amylase as a choice of target enzyme in applications of biosensing.

Open Access Original Research Article

Comparative Evaluation of Poly Herbal Formulation from Traditionally Used Eritrean Medicinal Plants against Pathogenic Microorganisms

Jeevan J. Kaushik, Nuredin Mohammedkassm, Dawit Mebrahtu, Atul Kaushik, Merhawi Kidane, Meron Solomon, Michael Teklemariam, Salih Mohammedbrhan

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/30059

Aim: The present study was taken to investigate the in vitro anti-microbial activity of Poly herbal formulation (PHF) of Schinus molle, Rhamnus prinoides, Grewia ferruginea, Achyranthes aspera against different human pathogenic strains.

Methods: Leaves of selected plants were extracted by using Ethanol-Aqueous solution (70:30). The antimicrobial activities of different plants singly as well as various combined formulations were screened using agar well diffusion assay.

Results and Discussion: All Poly herbal formulation showed zone of inhibition ranged from 23-40 mm against S. aureus as well as it was found to be susceptible to all the selected plant extracts when tested as single plant extract. In antifungal screening, the combined extract of Schinus molle and Grewia ferruginea showed significant zone of inhibition against tested fungi when these two extracts were combined in the ratio of 1:1. C. albicans also showed susceptibility when all the four plant extracts were combined in equal ratio. While E. coli was found resistant to all the single and combined forms of the selected plant extracts.

Conclusion: Based on comparison aspect of antimicrobial activity of the plant extracts it can be concluded that combined plant extracts overcome the problem of resistance towards antimicrobial effect of a single plant extract or purified drug. Results also conclude that the diseases or infections caused by S. aureus and C. albicans can be treated by preparing drugs from these combinations of plants.

Open Access Original Research Article

Artemisia annua L.- Vernonia amygdalina Del: A Potential Herbal Artemisinin Combination Treatment against Malaria

Nambejja Cissy, Ogwang Patrick Engeu, Onegi Berna, Anyama Norbert, Matu Esther

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/BJPR/2016/29555

Aim of Study: The aim of the study was to determine the potential of Vernonia amygdalina - Artemisia annua combination as a possible herbal artemisinin combination treatment of malaria.

Place and Duration of Study: Study was conducted at Natural Chemotherapeutics Research Institute, Ministry of Health, Kampala Uganda and at the Centre for Traditional Medicine and Drug Research, Kenya Medical Research Institute, Nairobi Kenya, from March 2013 to January 2014.

Methodology: After authentication of the plants, mature healthy Artemisia annua and Vernonia amygdalinaleaves were collected and shade dried over 2 weeks. The dry materials were then each separately extracted by maceration using Petroleum ether and methanol. The filtrates obtained were first concentrated by fanning and then oven dried at 50°C to constant weight of dry extract.  Eight groups of Plasmodium bergheiANKA infected mice were treated once daily for 4 days from the day of inoculation as follows; group I, 200 mg/kg bwt of A. annua methanol extract; group II, 125 mg/kg of V. amygdalina methanol extract; group III,  200 mg/kg of A. annua pet ether extract; group IV, 125 mg/kg of V. amgydalina  pet ether extract; group V, 125 mg/kg of V. amygdalina + 200 mg/kg of A. annua methanol extracts group; VI, 125 mg/kg of V. amygdalina + 200 mg/kg of A. annua pet ether extracts; group VII (positive control), 15 mg/kg of artemisinin+ 3 mg/kg of naphthoquine  and group VIII (negative control),  0.2 ml 10% Tween 80.

Parasitaemia in each mice was determined by microscopy on day 5 while survival times were recorded over 30 day period. The means of percent parasitaemia and survival times for each treatment group were determined and differences tested for significances using One-way analysis of variance followed by Student's t-test at P=0.05 using STATA version 13.0 statistical program.

Results: The petroleum ether extracts combination produced 100% parasite clearance by day 5 just like the Artemisinin-Napthoquine. The survival times for the herbal combination were however poor and significantly less i.e 10.67±1.09 days compared to more than 30.0 ± 0.0 days for the ACT, P=0.000.

Conclusion: The V. amygdalina-A. annua petroleum ether extract combination shows promise for use as a herbal artemisinin combination against malaria however the survival times need improvement to match that of the ACT.

Open Access Original Research Article

Bioactive Constituents from Apium leptophyllum Fruits

Iman E. Helal, Amal A. Galala, Hassan-Elrady A. Saad, Ahmed F. Halim

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/30289

Aims: This study was undertaken to characterize the bioactive constituents of Apium leptophyllum fruits and to evaluate their cytotoxicity, anti-inflammatory and alpha-amylase inhibitory effects.

Study Design: Isolation and identification of the phytochemicals from the petroleum ether and methanol extracts and investigation of the cytotoxicity, anti-inflammatory and α-amylase inhibitory activities.

Place and Duration of Study: Faculty of Pharmacy, Mansoura University, Egypt and College of Pharmacy, University of Louisiana at Monroe, USA, between June 2013 and January 2016.

Methodology: In the course of our study on Apium leptophyllum fruits, six compounds were isolated and purified using different chromatographic techniques and their structures were determined on the basis of their spectroscopic data (IR, NMR, MS). The cytotoxic, anti-inflammatory and α-amylase inhibitory activities of the prepared fruit essential oil as well as the isolated compounds were performed.

Results: Pentacosanol, 1-nonadecanol and 7α-hydroxy stigmasterol are reported for the first time from family Apiaceae, corosolic acid from genus Apium and β-sitosterol from Apium leptophyllum fruits along with the previously reported compound 8-hydroxy cuminic acid. The essential oil and 8-hydroxy cuminic acid exhibited the highest cytotoxic activity against cell lines of human hepatocellular carcinoma (HePG-2) with IC50 = 28.3 and 29.0 μg/mL and human breast carcinoma (MCF-7) with IC50 = 10.4 and 12.6 μg/mL, respectively. They also revealed a remarkable anti-inflammatory activity with 49.54% and 34.83% inhibition, respectively. The essential oil activity on tested cell lines of other types of human breast carcinoma alongside with that of an immortalized, non-tumorigenic human mammary epithelial (MCF10A) suggests a highly selective cytotoxic effect against MCF-7 cell line. Moreover, 8-hydroxy cuminic acid showed a good α-amylase inhibitory activity with 54.21% inhibition (IC50 = 43.75 µg/mL).

Conclusion: A new scientific evidence for the ethnopharmacological use of the herb in inflammatory conditions and describe, for the first time, the selective cytotoxic activity of the fruit essential oil.