Open Access Original Research Article

Antioxidant, Antimicrobial, Cytotoxic, Anticholinesterase, Antityrosinase Activities and Characterisation of Volatile Compounds of Verbascum oocarpum by SPME and GC-FID/MS

Seyda Kanbolat, Nuriye Korkmaz, Sıla O. Sener, Merve Badem, Nevin Ulas Colak, Mahmoud Abudayyak, Rezzan Aliyazicioglu, Ufuk Ozgen, Ali Kandemir, Sengul Alpay Karaoglu

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/JPRI/2018/45242

The objective of present study was to specify the antioxidant, antimicrobial, cytotoxic, anticholinesterase, and antityrosinase activities of Verbascum oocarpum Murb., together with its volatile components. The methanolic and aqueous extracts of aerial parts of V. oocarpum indicated substantial antioxidant activity derived from benzoic acid, sinapic acid, and quercetin compounds. The methanolic extract displayed moderate antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa, and Mycobacterium smegmatis. It also exhibited a higher IC50 value on tyrosinase than kojic acid, and lower acetylcholinesterase and butyrylcholinesterase inhibitor activities than galantamin. MTT analysis revealed that high concentrations of V. oocarpum extract can result in cytotoxicity, with an IC50 of 0.444 mg/mL. Common volatile components included pentadecane, hex-2(E)-enal, limonene, phenylacetaldehyde, isophorone, 1-methoxy-4-(2-propenyl)-benzene, 5,6,7,7a-tetrahydro-4,4,7a-trimethyl-2(4h)-benzofuranone and hexadecane. V. oocarpummay be of potential benefit to the food, cosmetical, and pharmaceutical sectors owing to its potent anticholinesterase, antioxidant, and antimicrobial activities, volatile components, and limited cytotoxicity.

Open Access Original Research Article

Study of Acute and Subacute Toxicities of Wakouba on Rats

Tiekpa Wawa Justine, Koutou Anatole, Bahi Calixte, Coulibaly Adama

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/JPRI/2018/36463

Aims: Wakouba is a salty substance used till medieval ages in traditional medical practices for the preventive treatment of hypertension. The current research focuses on the acute and sub-acute toxicity of this salt using laboratory Wistar rats.

Study Design: Wakouba prepared using rank 17 fronds from Elaeis guineensis plant’s crown: fronds harvested, dried, incinerated; then the ash dissolved into water and duly filtered. Then various Wakouba doses orally given to adult Wistar rats and acute and sub-acute toxicity parameters measured for 28-days.

Place and Duration of Study: Investigations performed at La Mé Research Station for Oil-Palm (National Agronomical Research Centre, CNRA) and Laboratory of Biochemical Pharmacodynamy (Felix Houphouët-Boigny University), between Mai 2014 and February 2015.

Methodology: For acute toxicity assessment, Wakouba given separately to rats at doses varying from 5,000 to 8,000 mg/kg body weight (BW) by oral route, and animals observed for behavioral changes or mortality. For sub-acute toxicity study, animals also orally administered with various Wakouba doses between 950 to 2,500 mg/kg BW, and then weekly examined, during 28 days, for toxicity symptoms dealing with hematological parameters (numbers of red blood cells, white blood cells, and hemoglobin; percentage of hematocrit, mean corpuscular volume, mean corpuscular rate, mean corpuscular hemoglobin, mean corpuscular hemoglobin concentration, lymphocytes, and platelet count), biochemical characteristics (urea, creatinine, aspartate aminotransferase, alanine aminotransferase, total cholesterol triglycerides, alkaline phosphatase, lactate dehydrogenase, and creatine phosphokinase), and histopathological traits (liver, heart, and kidney).

Results: Wakouba appeared a non-toxic substance because it revealed LD50 and MTD respective values of 6,308.57 and 5,000 mg/kg BW. Beyond the 28-days assessment, the rats were sacrificed for hematological, biochemical and histopathology concerns. Any significant variations in the overall hematological traits and some biochemical parameters (AST, ALP, CPK, LDL, and TP) were observed. However, at the rate of 2,500 mg/kg BW, Wakouba induced significant (P<0.001) increases in urea, creatinine, and HDL-cholesterol and decrease drop in the LDL-cholesterol from the treated animals. Histological examination of vital organs showed normal architecture suggesting no morphological trouble in the heart, kidney, and liver.

Conclusion: The oral administration of Wakouba did not produce any significant toxic effect from rats. Such observations are significant safety margin in the uses of Wakouba that could therefore be valorized in therapeutic approach through pharmaceutical formulations.

Open Access Original Research Article

Analysis of Prescribing Pattern among Cardiovascular Patients at National Institute of Cardiovascular Disease, Dhaka, Bangladesh

Imran Abdul Hai Sarker, Md. Siddiqul Islam, Lutfur Rahman, Abdullah Al Hasan

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/JPRI/2018/43122

Objective: The aim of this study was to comprehend the prescribing pattern among cardiovascular patients at the national institute of Cardiovascular Disease (NICVD), Dhaka, Bangladesh.

Methodology: The current study was carried out in a national institute of Cardiovascular Disease (NICVD), Dhaka, Bangladesh from 13th February, 2017 to 2nd December, 2017. Cross-sectional types of descriptive research were performed in the cardiac outpatient department through the period of study. A total of 1,000 patients meeting the inclusion and exclusion criteria, were interviewed with the structured questionnaire. The questionnaire includes the demographic details of the patients, prescribing trend and the written permission was also taken from administrative offices as well as patients in this hospital.

Results: The findings of this study suggest that out of 1,000 patients, only 13.1% of patients were used monotherapy, whereas 86.9% of patients were taken combination therapy for the treatment of CVD. Among the combination therapy, penta therapy was the most popular.

Conclusions: Drug prescription pattern in our study observed that combination therapy was more commonly prescribed than monotherapy.

Open Access Original Research Article

Toxicological Investigations of Ethanolic Leaves Extract of Dissothis thollonii (Melastomataceae)

Donald Sédric Tala, Siméon Pierre Chegaing Fodouop, David Ngoudjou Tsafack, Norbert Kodjio, Charles Fokunang, Donatien Gatsing

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/JPRI/2018/39412

Dissotis thollonii is widely used in Cameroon for the treatment of typhoid fever, gastrointestinal disorders, inflammation, kidney diseases, pregnancy control and sinusitis. However there is lack of experimental data on its possible toxicity.

The aim was to investigate acute and subchronic toxicity of the ethanol leaf extract of Dissotis thollonii in healthy Wistar rats.

In acute toxicity tests, a single administration of the ethanolic leaf extract (5000 mg/kg) of Dissotis thollonii was given orally to 4 female rats. The general behavior, adverse effects, and mortality were recorded for up to 14 days post-treatment. On the 15th day, the rats were weighed and euthanized for necropsy. In sub-chronic toxicity tests, the extract (18.28; 62.50; 250 and 1000 mg/kg/day) was given orally to both male and female rats for 28 days. General behavior, adverse effects, and mortality were observed throughout the experimental period. Food intake, body weight, organ weight, hematological parameters, biochemical parameters and histopathological changes were evaluated.

Dissotis thollonii leaf extract did not cause any death or any hazardous symptoms during acute toxicity, and the LD50 of his was higher than 5000 mg/kg. Sub-chronic administration of Dissotis thollonii leaf extract showed significant (p > 0.05) variations in some biochemical parameters (serum urea, urinary urea, ALT, AST, and ALP) in the experimental groups at the dose of 250 mg/kg and 1000 mg/kg for both male and female rats. No major morphological changes were observed in the histopathological analysis of liver and kidney. However, a congestion on liver sections at a dose of 1000 mg/kg for females and at 250; 1000 mg/kg for males was observed.

These findings showed that acute or subchronic oral administration of the ethanolic leaf extract of Dissotis thollonii may be considered as relatively free of toxicity. However, prolonged use of high doses of the extract orally should be exercised with caution to avoid a possible liver injury.

Open Access Review Article

Appraisal of Bioenhancers in Improving Oral Bioavailability: Applications to Herbal Medicinal Products

Francis A. Oladimeji, Adebanjo J. Adegbola, Cyprian O. Onyeji

Journal of Pharmaceutical Research International, Page 1-23
DOI: 10.9734/JPRI/2018/45330

The oral route of administration is associated with some challenges such as poor aqueous solubility and low intestinal permeability of many active pharmaceutical ingredients resulting in decreased drug absorption and subsequent poor bioavailability. In recent years, research on bioenhancers has started receiving increased attention and this approach can complement the traditional methods of solubility enhancement. Bioenhancers boost the bioavailability of drugs when co-administered at low doses with the drug. A large variety of compounds have been clearly demonstrated to possess significant bioenhancing activity with different mechanisms of action. Some compounds considered as bioenhancers isolated from plants include piperine, gallic acid, niaziridine, sinomenine, genistein, and lysergol. There are several reports of herbal medicinal products (HMPs) that require large doses to be therapeutically effective and some studies have identified that the active compounds in such products have poor bioavailability. Thus, there is every need to optimise dosage formulations of HMPs. The application of the concept of bio-enhancement and knowledge of their mechanism of action can lead to the selective use of suitable bioenhancers resulting in reduction in therapeutic dose of the HMP, thus reducing the possibilities of toxicity. This review was aimed at updating knowledge on different natural bioenhancers and also provides an overview of currently marketed HMPs containing bioenhancers. The article highlights different strategies that can be employed to improve the bioavailability of HMPs. The bioactive constituents of the HMP were identified and facts on their physicochemical properties, metabolic fate, as well as factors that impact on their gastrointestinal absorption, were examined with a view to providing information to serve as a guide in developing suitable bioavailability enhancement strategies for other HMPs.