Development and Evaluation of Controlled Release Bilayer Tablets of Hydrochlorothiazide and Losartan Potassium – Pages 84-94

Development and Evaluation of Controlled Release Bilayer Tablets of Hydrochlorothiazide and Losartan Potassium
Pages 84-94
Manoj Kumar Mishra, Dubey Deepti and Upamanyu Neeraj
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.13
Published: 16 February 2015

Abstract: The aim of the present research work was to develop bilayer tablet dosage form containing combination of immediate and sustained matrix prepared from Hydrochlorothiazide (HTZ) and Losartan Potassium (LP) respectively for the treatment of hypertension and its associated complications. Immediate release HTZ was prepared using different superdisintegrants. LP sustained layer was prepared by compression technique. Both pre-compression and post-compression parameters were analyzed for all the tablets. In vitro release studies were carried out as per USP in pH (1.2) and phosphate buffer pH (6.8) using USP-XXI type II. Bilayer tablet (F6) formulated using higher concentration of HPMC K 15 exhibiting higher LP release rate (83.553± 0.22) for the period of 12 h. The In vitrorelease profile of drug from sustained matrix could be best expressed by First order as the plot showed highest linearity (R2 = 0.990) and diffusion was the dominating mechanism of drug release. The stability and FTIR studies are also indicating the absence of strong interaction between drug and polymer and compatibility among them.

Keywords: Hydrochlorothiazide, Losartan potassium, Bilayer tablets, kinetic models, controlled release.

Effect of Taro (Colocasia esculenta) Starch-Hydrocolloids Mixture on the Physical and Sensory Characteristics of Leavened Bread – Pages 77-83

Effect of Taro (Colocasia esculenta) Starch-Hydrocolloids Mixture on the Physical and Sensory Characteristics of Leavened Bread
Pages 77-83
Feroz Alam, Anjum Nawab, Tanveer Abbas, Mohib Kazimi and Abid Hasnain
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.12
Published: 16 February 2015

Abstract: During this study, different blends of taro starch-hydrocolloid were incorporated in yeast leavened bread and their effects were investigated. The specific volume, moisture content and slice shape of the bread were found to be improved by the addition of taro starch-guar gum blend. Taro starch-xanthan gum mixture was also found to be a good additive to improve specific volume, slice shape, crumb softness as well as sensory characteristics of bread. The study reveals taro starch-hydrocolloid blend can be utilized as a novel ingredient to improve the physical and sensory characteristics of leavened bread.

Keywords: Taro starch, Hydrocolloids, Bread, Physical Properties, Sensory Properties.

Inhibitory Effects of Chaga (Inonotus Obliquus) on Tumor Promotion in Two-Stage Mouse Skin Carcinogenesis – Pages 71-76

Inhibitory Effects of Chaga (Inonotus Obliquus) on Tumor Promotion in Two-Stage Mouse Skin Carcinogenesis
Pages 71-76
Ayako Akita, Yi Sun and Ken Yasukawa
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.11
Published: 16 February 2015

Abstract: The methanol extract of chaga (sclerotia of Inonotus obliquus) inhibited the promoting effect of 12-O-tetradecanoylphorbol-13-acatate (TPA) applied twice weekly on skin tumor formation in mice initiated with 7,12-dimethylbenz [a] anthracene. The methanol extract from chaga led to the isolation of eight triterpenoids (18). The anti-inflammatory activity of the isolated lanostane-type triterpenes was evaluated against TPA-induced inflammatory ear edema in mice. These compounds showed markedly anti-inflammatory effects, with a 50% inhibitory dose of 125-458 nmol/ear.

Keywords: Chaga, Inonotus obliquus, lanostane-type triterpene, antitumor promotion, anti-inflammation, two-stage carcinogenesis.

Effects of Different Physical and Chemical Parameters on Phosphate Solubilization Activity of Plant Growth Promoting Bacteria Isolated from Indigenous Soil – Pages 64-70

Effects of Different Physical and Chemical Parameters on Phosphate Solubilization Activity of Plant Growth Promoting Bacteria Isolated from Indigenous Soil
Pages 64-70
Talat Yasmeen Mujahid, Syed Abdus Subhan, Abdul Wahab, Javeria Masnoon, Nuzhat Ahmed and Tanveer Abbas
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.10
Published: 16 February 2015

Abstract: he microorganisms play a vital role in fertility of soil and hence favors’ large group of plants. In present study we have successfully isolated certain bacteria from soil including both Gram positive and Gram negative bacteria and access their ability in phosphate solubilization. Effects of temperature, pH and different carbon sources, on phosphate solubilization, by these isolates were also determined. Low temperature 25 °C, pH between 5-7, and glucose as carbon source were found to be best for phosphate solubilization by most of the isolates. Present study highlights the importance of these plants growth promoting bacteria and their uses for agriculture purposes.

Keywords: Phosphate solubilization, Plant growth promoting bacteria, Indigenous Soil, Temperature, pH and Carbon sources.

Bioactive Metabolites from Indigenous Actinomycetes Isolated from Marine Water – Pages 57-63

Bioactive Metabolites from Indigenous Actinomycetes Isolated from Marine Water
Pages 57-63
Syed Abdus Subhan, Abdul Wahab, Talat Yasmeen Mujahid,Tanveer Abbas, Nayyar Mehmood and Iqra Ahmed
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.9
Published: 16 February 2015

Abstract: Microbial natural products have continued to play an important role in the discovery of novel chemicals for the development of important therapeutic agents. Actinomycetes form a potent reservoir of biologically active secondary metabolites and enzymes. The need for finding novel bioactive compounds for the development of new therapeutic agents is required due to the emergence of antibiotic resistance among pathogenic bacteria. Actinomycetes are considered as one of the best producers of variety of antagonistic compounds that could serve as potential chemotherapeutic agents. The present study was undertaken to find new antagonistic compounds from actinomycetes. Actinomycetes were successfully isolated from marine water samples collected at various locations of Karachi. Initially 39 isolates were collected out of which 23 were found to produce active metabolites against one or more test bacterial cultures. Actinomycetes strains IS26, IS33, and IS39 showed significant potential of having bioactive metabolites. Further, the spectrum of those strains was tested against gram positive and gram negative bacteria and results showed variable potential of actinomycetes to inhibit bacterial growth.

Keywords: Actinomycetes, Bioactive metabolites, Marine water, Antimicrobial, Human Pathogens.

Impact Evaluation of Calcium and Vitamin D Supplementation and Physical Activity on Bone Health Status of Elderly Population of Urban Vadodara – Pages 50-56

Impact Evaluation of Calcium and Vitamin D Supplementation and Physical Activity on Bone Health Status of Elderly Population of Urban Vadodara
Pages 50-56
Annapurna Maity, Komal Chauhan, Nishita Panwar and Pooja Mistry
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.8
Published: 16 February 2015

Abstract: Background: Osteoporosis is a global public health problem affecting the ageing population and influenced by poor nutrition, lack of physical activities, and absence of supplementation on time.

Objectives: To study the impact of Calcium and vitamin D supplementation along with weight bearing exercises on bone health status of elderly.

Methods:30 elderly males and 20 elderly females having poor BMD and poor serum vitamin D were supplemented with 1000 mg calcium and 500 IU vitamin D/ day along with weight bearing exercises for a period of 3 months, along with that 60000 IU vitamin D3/week for 2 months were given to 30 males only. Serum calcium, Vitamin D, BMD, dietary calcium intake, frequency of vitamin D rich food intake, anthropometry etc. were measured at the baseline as well as after the intervention.

Results: Mean BMD T-scores (-1.1 to -2.5: osteopenia; >-2.5: osteoporosis) of the elderly males and females were significantly (p≤0.001) decreased after the intervention depicting improvement (baseline:-2.34±0.50, final:-1.86±0.61). 26.7% reduction in osteoporotic cases among males and 50 % among women was achieved. Mean serum calcium (baseline: 9.38±0.63, final: 9.46±0.61) and vitamin D level (baseline: 23.76±13.17, final: 35.48±14.84) was increased significantly (p≤0.05). 60% males and 70% females achieved vitamin D sufficiency level after the intervention. Mean physical endurance (Grip strength, standing balance, walking speed and rise from chair) scores were significantly increased in both males and females. Locomotor problems were reduced among 6.7% males and 40% females after regular weight bearing exercise and supplementation.

Conclusion:Calcium and vitamin D supplementation with daily weight bearing exercise has a preventive and curative effect on BMD and it maintains the serum calcium and vitamin D levels. Long term and high dose supplementation needs further investigation.

Keywords: Elderly, BMD, Calcium, Vitamin D, Physical Activity.

In Silico Design & Development of Some Selected Flavonols Against Beta–Glucuronidase Inhibitory Activity – Pages 43-49

In Silico Design & Development of Some Selected Flavonols Against Beta–Glucuronidase Inhibitory Activity
Pages 43-49
Sovan Pattanaik, Sudam Chandra Si, Sudhanshu Sekhar Rout, Anindya Bose and Siva Shankar Nayak
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.7
Published: 16 February 2015

Abstract: Drug discovery process develops faster due to more advances in computational techniques. The protein ligand interaction well predicted due to the in-silico approach study. The present investigation focused towards the development of lead structure for treatment of hepatic disorders. An increase in serum acid hydrolase, including β-glucuronidase has been reported in numbers of pathological conditions such as arthritis, renal diseases and epilepsies. Enhancement of this enzyme β–glucuronidase in blood has been found to correlate significantly with liver damage. β-glucuronidase inhibitor is a novel approach which is different from the available hepatoprotective drug therapies.

Method: The current study is based on in-silico ligand screening and in-vitro estimation of the three flavonols [Naringenin, Quercetin and 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one] compounds with enzyme β-glucuronidase. Molecular docking software Py Rex and Py Mol was used to dock the selected ligand in the binding site of the crystal structure of protein.

Results: Docking results are based on the least binding energy of the selected flavonols compounds. Further attempt has been made towards in-vitro estimation of this enzyme with those selected compounds. The binding affinity with existence of hydrogen bonds leads to find out the mechanism which was well correlated with the findings of in-vitroinhibitory activity.

Conclusion: The result outcome of the binding orientation of 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one linked with the active amino acid residue of the protein and the binding affinity leads to find out the mechanism for its potential in-vitro inhibitory activity.

Keywords: Protein ligand, β-glucuronidase, serum acid, Chromen, binding affinity.

In Vitro Activity of Cocoa Powder Extracts on Some Biomarkers Implicated in P. falciparum Malaria Pathogenesis – Pages 38-42

In Vitro Activity of Cocoa Powder Extracts on Some Biomarkers Implicated in P. falciparum Malaria Pathogenesis
Pages 38-42
Seth Kwabena Amponsah and Nana Nim Dwumfour
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.6
Published: 16 February 2015

Abstract: Malaria is a public health concern in many developing countries, including Ghana, and efforts are being made to eradicate it. Extracts from natural products have been used in several malaria endemic areas for malaria prophylaxis and treatment. Natural cocoa powder has been reported to possess in vitro direct inhibitory on P. falciparum. This study investigated the effect of natural cocoa powder on inducible nitric oxide, TNF-α and IL-10, biomarkers that play different roles in malaria pathogenesis. Chloroform and ethylacetate fractions of cocoa powder were cultured together with phytohemagglutinin-stimulated peripheral blood mononuclear cells (PBMCs) for 24 hours at 37°C with 5% CO2. Cell free supernatants were harvested and assayed for iNO, TNF-α and IL-10. Inducible NO was determined by diazotization reaction developed by Griess. TNF-α and IL-10 were determined by ELISA. This study showed that TNF-α and iNO in phytohemagglutinin-stimulated PBMCs were significantly reduced by cocoa fractions (p < 0.05), but IL-10 levels did not change significantly (p > 0.05), although TNF-α is known to up-regulate IL-10.Apart from the documented direct inhibitory effect of cocoa powder on P. falciparum, it can be hypothesized that the antiplasmodial activity of unsweetened cocoa powder could also be due to its ability to significantly inhibit iNO and TNF-α, inflammatory substances implicated in severe malaria pathogenesis.

Keywords: Antiplasmodial activity, Cytokines, fractions, Peripheral blood mononuclear cells, Supernatants.

Fungi Isolated from Traditional and Exotic Apple Varieties from Portugal and Patulin Production – Pages 30-37

Fungi Isolated from Traditional and Exotic Apple Varieties from Portugal and Patulin Production
Pages 30-37
C.M.M. Almeidaand M.M. Lopes
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.5
Published: 28 January 2015

Abstract: The objective of our study was to examine the effects of cultivar type on developed fungi species and evaluate the potential for patulin production by fungi. In addition, patulin diffusion was also investigated. The experiments were carried out in traditional (Bravo de Esmolfe) and exotic apples (Golden, Starking, Fuji, Reineta Parda and Gala Galaxy) varieties from Portugal. High-performance liquid chromatography with solid phase extraction and UV detection (SPE-HPLC-UV) was validated and used to analyze patulin in the apple. The most prevalent fungal population was Penicillium spp and 27% of rotten fruits had patulin. Fungi of the genera Cladosporium spp., Alternaria spp., Fusarium sppand Aspergillus spp. were also found even in apples without patulin production. The variety with the highest production of patulin was Bravo Esmolfe, however this variety showed the lowest prevalence of Penicillium spp. compared to other varieties of apples where was detected patulin.

Patulin was not detected in any apples of Fuji and Gala varieties, despite having been identified fungi usually associated with the production of patulin. Thus, these two varieties are presented as the most suitable for the production of the apple based-foods.

Keywords: Patulin, Mycotoxins, Apples, Toxigenic fungi, HPLC, SPE.

Effect of Topical Application of Hydro-Ethanolic Extract of Acacia nilotica Pods on Second-Degree Cutaneous Infected Burns – Pages 24-29

Effect of Topical Application of Hydro-Ethanolic Extract of Acacia nilotica Pods on Second-Degree Cutaneous Infected Burns
Pages 24-29
Kossi Metowogo, Tchin Darré, François Daubeuf, Povi Lawson-Evi, Kwashi Eklu-Gadegbeku, Kodjo A. Aklikokou, Gado Napo-Koura, Nelly Frossard and Messanvi Gbeassor
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.4
Published: 28 January 2015

Abstract: Acacia nilotica is a medicinal plant used traditionally in Togo to treat various diseases including burn wounds. The aim of this study was to evaluate experimentally Acacia nilotica burn wound healing effect.

Cutaneous burn wounds were symmetrically caused on depilated areas of rat skin through contact with an aluminum bar (r = 10 mm), preheated at 80°C for 30 sec. Five groups of animal were constituted and each group contained 8 mice. Four groups of animal’s burn wounds were infected by Staphylococcus aureus. One group burn wound is uninfected and serves as negative control. Burn wounds were assessed by planimetry and histological parameters of healing. Twelve days after burn wound induction, wound contraction in the uninfected groups (negative control) was 19.9% for topical application against -2.43% for infected control. In the infected groups treated with extract, wound contraction was generally stimulates. Histological examination showed granulated tissue developing over the wounds treated with the extract of A. nilotica at 2.5% and 5% where the proliferation of fibroblasts and neo-blood vessels was very marked.

In conclusion, A. nilotica pod contents tannin, flavonoids, alkaloids and protein reduces DPPH solution and significantly accelerates wound healing of burns, and this is the case even if wounds are infected with 109CFU/mL of S. aureus.

Keywords: Burns wound, A. nilotica, histology, wound infection, wound healing.