Open Access Original Research Article

A Novel Catalytic Synthesis of Flavones under Autoclave Conditions and Comparative Study of Anti-cancer Activity

K. Rajeshbabu, S. Pushpalatha, B. Ramakrishna, V. Madhavarao

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/BJPR/2016/15884

Novel, less toxic, more effective catalysts were used to synthesize various flavones under auto clave conditions. Substituted o- hydroxyl acetophenones and benzaldehydes were reacted in-presence of 2, 4, 6-trimethylpyridine, a pinch of TiCl4 and yielded chalcones. Equimolar ratio of KIO3, KI, and H2SO4 was used as in situ catalytic source for I2 to convert chalcones to flavones. The progress of the reactions was monitored by TLC. Crude compounds were recrystallized from methyl alcohol. We obtained good yields of products within less time periods. We had gone through IR, HNMR, Elemental analysis and mass data to characterize the compounds. Selective compounds were screened for cytotoxic activity against A549 human tumour cell lines by MTT method and comparative study has been done. 

Open Access Original Research Article

In vitro Efficacies of Some Nigerian Medicinal Plant Extracts against Toxigenic Aspergillus flavus, A. parasiticus and A. ochraceus

Yemisi Adefunke Jeff-Agboola, Anthony Kayode Onifade

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/20390

The aim of this work was to find an alternative to chemical fungicides currently used in the control and prevention of activities of toxigenic Aspergillus flavus, A. parasiticus and A. ochraceus in food and feed. The antifungal activity of extracts of five medicinal plants used in native medicine in Nigeria is reported. All plant extracts were screened for their minimum inhibitory concentration (MIC) against toxigenic Aspergillus flavus, A. parasiticus and A. ochraceus. Antifungi efficacies of the medicinal Plant extracts showed that maximum antifungal activity was demonstrated by ethanolic, hot and cold water extracts of Borreria verticillata, Lactuca capenisi, Colocasia esculenta, Jatropha gossy and Ageratum conyzoide. Leaves part of the five medicinal plants were investigated for antifungal activities against toxigenic Aspergillus flavus using radial growth technique. The plant extracts of Borreria verticillata inhibited the growth of the test organisms. Borreria verticillata  appears to be more effective as an antifungal agent than other plant extracts. The ethanolic extracts were more effective than the cold and hot water extracts against the tested organism.

Open Access Original Research Article

Molecular Mechanisms of the Modulatory Effect of Vitamin E on Tacrolimus (FK506)-Induced Renal Injury in Rats

Hassan Afify, Abdel-Aziz H. Abdel-Aziz, Mahmoud Nour El-Din, Amany Balah, El-Sayed Akool

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/21684

Aim: This study was designed to evaluate the possible modulatory effect of vitamine E on tacrolimus (FK506)-induced renal injury in rats.

Methods: Twenty-four male Wistar rats (6 animals in each group) were used in this study. The first group (Control) received normal saline intraperitoneal (i.p.) daily for 21 days. The second group received FK506 (1 mg/kg/day i.p.) daily for 21 days. The third group was administered Vitamin E (250 mg/kg/day by oral gavage) 5 days before and concurrently during FK506 administration daily for 21 days. The fourth group received Vitamin E alone (as previously described in the third group).

Results: Administration of FK506 significantly increased blood urea nitrogen and serum creatinine levels. In addition, FK506 has also reduced the renal content of reduced glutathione, as well as the enzymatic activities of superoxide dismutase and catalase. Furthermore, these effects were associated with an increase in lipid peroxidation, inducible NO-synthase (iNOS), and NF-kB expression. Moreover, histopathological examinations showed severe damage of the renal tissues in animals treated with FK506. Interestingly, it was found that concomitant administration of vitamin E along with FK506 ameliorated all these parameters and improved renal function. Furthermore, the immunosuppressive effect of FK506 was not affected by vitamin E.

Conclusion: The findings of the present study suggest that concomitant use of vitamin E might be useful in reducing nephrotoxicity induced by FK506.

Open Access Original Research Article

Effects of Ethanol Extract of Unripe Annona muricata (l.) Fruits on the Haematological and Histopathological Parameters in Swiss Albino Rats Infected with Salmonella typhi

Olajide Sunday Faleye, Ebenezer Oluyemi Dada

Journal of Pharmaceutical Research International, Page 1-13
DOI: 10.9734/BJPR/2016/19971

Background: In addition to the problems of resistance to commonly used antibiotics, toxicity depicts the state of adverse effects caused by the interaction of toxicants with cells. Similarly, blood components are exposed to significant concentrations of toxic compounds as they form the medium for their transport.

Aims: To study the effects of ethanol extract of unripe Annona muricata fruits on the haematological and histopathological parameters in Swiss albino rats infected with Salmonella typhi.

Place and Duration of Study: Department of Microbiology Laboratory, Federal University of Technology, Akure, Ondo State, Nigeria, between June 2014 and December 2014.

Methodology: Matured unripe fruits of A. muricata were collected, dried, powdered and extracted using 70% ethanol. Eighteen rats of same age between 170-220 g in weight were selected and divided into six groups containing three each. The infectivity dose (ID) was determined using the clinical Salmonella typhi obtained from Don Bosco Catholic Hospital, Akure. The dose of the A. muricata fruit extract (400 mg/kg) used in this study was administered orally for 7 days. At the end of the treatment period, the rats were fasted overnight. Then blood samples were collected by cardiac puncture for haematological studies and there after sacrificed. Organs (liver, heart, kidney and spleen) were excised for relative organ weight analysis and histopathological studies.

Results: The infectious dose (ID) of S. typhi on experimental rats in this study was 6.8x106 cfu/ml while the weights of liver, heart and spleen in all groups were not significantly different from the control. However, a significant increase in the heart was observed in group given the extract and antibiotics (ciprofloxacin). The Packed Cell Volume (PCV) and Haemoglobin (Hb) of rats treated with extract and ciprofloxacin increased significantly (p<0.05) compared to the control while a non-significant decrease was observed in the Red Blood Cell (RBC) of rats administered only extract and ciprofloxacin after treatment. White Blood Cells (WBC) of rats given the extract significantly reduced while there was no significant difference in the lymphocyte count of rat administered the extract of A. muricata and ciprofloxacin. Neutrophils of rats in all groups significantly increased (p<0.05). However, the monocyte and eosinophil level were not significantly different from the control. Minimal disruption and reduction in nuclear clumping were observed in the liver of rats infected/treated with the extract. Similarly, there were prominent improvements in the glomerula architecture as well as the white and red pulp of the spleen after treatment with the extract of A. muricata.

Conclusion: The extract stimulated blood production and possessed restorative effect on various organs examined. However, excessive use might be toxic to the heart.

Open Access Original Research Article

HPTLC Densitogram Profile of Aqueous Distillate (Arka) from Roots of Boerhaavia diffusa

Pooja ., V. K. Lal, A. Verma

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/19399

The aqueous distillate (arka) of Boerhaavia diffusa was prepared and investigated qualitatively for TLC. The following work constitutes the enrichment of constituents present in the aqueous distillate (arka) by partition technique using various solvents such as toluene and ethyl acetate in the ratio of (7:3), toluene:acetone:acetic acid (8.5:1:0.5) chloroform:methanol (9:1) Enrichment was determined by Thin Layer Chromatography and HPTLC. Hence it was concluded that aqueous distillate showed the better result for TLC in different solvent systems tried, but best solvent system selected for TLC was toluene: acetone: acetic acid in the ratio of (8: 0.5:1.5) using 5% methanol-sulphuric acid solution as detecting reagent.

Open Access Original Research Article

Evaluation of the Physicochemical and in vitro Dissolution Properties of Metformin Hydrochloride Tablet Brands Marketed in Five Cities in Ghana

Akwasi Sougi, Kwabena Ofori-Kwakye, Noble Kuntworbe, Samuel Lugrie Kipo, Mariam El Boakye-Gyasi

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/BJPR/2016/21862

Aim: A comparative evaluation of the physicochemical and in vitro dissolution properties of metformin hydrochloride tablet brands sampled in five cities in Ghana was undertaken to assess their pharmaceutical equivalence.

Place and Duration of Study: Department of Pharmaceutics, KNUST, Kumasi, Ghana, between August 2012 and December 2012

Methodology: Fourteen brands of metformin tablets plus the innovator brand, Glucophage, purchased from retail pharmacies were studied. The genuineness of the samples was determined using Fourier transform infra-red (FTIR) spectroscopy and thin layer chromatography (TLC). Pharmacopoeia tests such as uniformity of weight, hardness, friability, disintegration and assay were used to assess the physicochemical equivalence of the tablet brands. In vitro dissolution testing was conducted and the dissolution data subjected to analysis involving dissolution efficiency (DE), similarity factor (f2) and Biopharmaceutics classification system (BCS)-based biowaiver conditions, as a surrogate for bioequivalence studies.

Results: All the tablet brands complied with the official specifications for identification, uniformity of weight hardness and disintegration. Brand M9 failed the friability test while brands M5, M9 and M12 failed the assay test. Dissolution efficiency (DE) and similarity factor (f2) of the brands varied with pH of dissolution media with M4 (in 0.1 M HCl) having the highest DE and M9 (in phosphate buffer pH 6.8) the lowest.

Conclusion: Eleven of the fifteen tablet brands passed all the official tests and could be regarded as pharmaceutically equivalent but f2 analysis showed only six brands were similar to the reference brand (with f2 values ≥50 in the three dissolution media used). None of the metformin brands satisfied the criteria for BCS-based biowaiver for rapidly dissolving tablets. The study has shown that not all the metformin tablet brands sampled in five cities in Ghana are pharmaceutically equivalent.

Open Access Original Research Article

Study of Acid-base Indicator Property of Ethanolic Extract of Nerium indicum Flower

Khalid Da’u Khalid, Mustapha Balarabe Idris, Naziru Alhassan Muhammad, Ahmad Bala

Journal of Pharmaceutical Research International, Page 1-4
DOI: 10.9734/BJPR/2016/20556

A study has been done to investigate the indicator property of ethanolic extract of Nerium indicum. The commonly used synthetics indicators cause environmental pollution and pose hazardous effects in human body. Natural pigments in plants are highly coloured substance and may change with pH variation. The equivalence points of the titrations using flower extract is almost close or coincide with that of phenolphthalein (synthetic indicator). Therefore, use of ethanolic extract of Nerium indicum as an indicator for acid-base titration could be effectively employed as a substitute to the synthetic acid-base indicators.