Open Access Original Research Article

Synthesis, Characterization and Evaluation of Biological Properties of Pyrazolo- and Oxazolo-pyridocarbazoles and Pyridoazacarbazoles as Potent Anti-microbial Agents

Taruna Yadav, D. Kishore, Bhawani Singh

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2015/19615

Aims: Fused carbazoles, azacarbazoles and quinolines are endowed with a wide array of pharmacological properties. Keeping these properties in the mind, the study was undertaken to seek structural modifications to generate novel synthetic analogues of carbazoles, azacarbazoles and quinolines and to examine their biological properties.

Methodology: Pyrazole and isoxazole condensed pyridocarbazoles and pyridoazacarbazoles were synthesized by the cyclo-condensation reactions of corresponding enol ethers, chalcones, oxoketenedithio acetals and dimethyl aminomethylene ketones with hydroxylamine hydrochloride and hydrazine hydrate respectively.

Results: Pyrazoles and isoxazoles were synthesized. The structures of all the compounds have been established on the basis of their elemental analysis and spectral (IR, 1H NMR and MS) data. Formation of the compounds were also confirmed by the spectral data.

Conclusion: Compound 8-methyl-4,5-dihydroisoxazolo[4,3-i]pyrido[2,3-a]carbazol-10-ol (12b) and 5-N-benzyl-8-methyl-3-methylthio-4H-pyrrazolo[4,3-i]pyrido[2,3-a]azacarbazol-10-ol (14a) were screened for the anti-bacterial (against E. coli and B. cereus) and anti-fungal (against M. phaseolina and F. solani) activities. Both the compounds showed moderate activities as compared to standards (Ciprofloxacin for anti-bacterial and Fluconazole for anti-fungal activity) used.

Open Access Original Research Article

Efficacy Appraisal of Some Antidiabetic Herbal Preparations Available in Bangladesh

Md Ranzu Ahmed, Begum Rokeya, A. K. Azad Khan, Md Rausan Zamir, M. Abu Sayeed, M. Mosihuzzaman

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2015/19870

Antidiabetic Herbal Preparations (ADHP) are being used for the management of diabetes mellitus (DM) but their efficacy in controlling hyperglycemia is not scientifically evaluated. This study was undertaken to evaluate the antihyperglycemic potency of some selected antidiabetic HPs (herbal preparations) manufactured locally and readily available in Bangladesh. Six ADHPs were collected from herbal medicine shops in Dhaka city produced by five different local herbal pharmaceuticals companies. Acute and chronic responses of the selected ADHPs on glycemic status were determined by feeding test on streptozotocin induced type 2 diabetic model rats. Plasma glucose concentrations were measured at baseline and after oral administration of ADHPs. Acute responses were investigated after 30 and 60 minutes of oral glucose load when ADHPs were administered simultaneously or 30 minutes before oral glucose load. Chronic responses were investigated at 14 and 28 days after ADHPs administration in two different doses. Data were expressed as mean±SD. Statistical analysis within groups was done using paired‘t’- test. Comparison between groups was done using one-way ANOVA with post Hoc Bonferroni test. Among the six ADHPs tested, only ADHP-3 showed significant reduction of plasma glucose levels compared to control. It was effective at 30 (p<0.05) and 75 (p<0.01) minutes when ADHPs were administered simultaneously with oral glucose load. ADHP-3 was also effective at 60 and 105 minutes (p<0.01 at both time points) when ADHPs were administered 30 minutes before oral glucose load. In case of chronic responses evaluation, ADHP-3 at a dose of 200 mg/kg/day insignificantly reduced blood glucose levels compared to baseline (p=0.342) at 28 days but at a dose of 400 mg/kg/day significantly reduced blood glucose levels (p=0.040).

Open Access Original Research Article

Anthelmintic Effects of Different Extracts of Hopea odorata Leaves on Tubifex tubifex Worm Using In vitro Method and their Condensed Tannin Content

Mohammed Munawar Hossain, Mohammad Shah Hafez Kabir, Tanvir Ahmad Chowdhury, Abul Hasanat, Nishan Chakrabarty

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/BJPR/2015/19064

Objective: To investigate the therapeutic effects of different extracts of Hopea odorata leaves in anthelmintic (In vitro) and to determine their total condensed tannin (proanthocyanidin) content.

Methods: Leaves of Hopea odorata was extracted with pure methanol (MEHO), ethanol (EEHO) and water (AEHO), which are tested for anthelmintic activity on aquarium worm Tubifex tubifex by using four concentrations viz., 2.5, 5, 10 and 20 mg/ml of each. Total condensed tannin content determined based on the previous procedure of Oyedemi et al. [1].

Result: Among the all extracts, MEHO exhibited strong anthelmintic activity In vitro. Where it paralyzed (4.05±0.35 min; P<0.05) and produced death (7.5±0.38 min; P<0.001) of the Tubifex tubifex at highest 20 mg/ml dose close to the value of the standard, Levamisole (3.3±0.38 min and 6.5±0.76 min) at 1 mg/ml. The content of condensed tannin excellent at all extracts, but MEHO (96.99±0.34 mg catechin/g) contained maximum among them. For both of experiment, activity found as follows, MEHO > EEHO > AEHO.

Conclusion: These findings suggest that the plant may be a potential source for the development of new anthelmintic and condensed tannin is a type of phytochemical which may exhibit anthelmintic activity.

Open Access Original Research Article

Modulatory Effect of Ethanolic Leaf Extract of Annona muricata Pre-treatment on Liver Damage Induced by Dimethylnitrosamine (DMN) in Rats

Usunobun Usunomena, Okolie P. Ngozi, Eze G. Ikechi

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2015/19841

Aim: This study aim to evaluate the modulatory effect of ethanolic leaf extract of Annona muricata against dimethylnitrosamine (DMN)-induced hepatic toxicity in rats.

Methodology: Twenty-four (24) male albino rats divided into four (4) groups of six (6) rats each were used for the study. Group 1 served as control and was untreated, group 2 and 3 were pre-treated with 400 mg/kg Annona muricata for one week while group 3 and 4 each received a single oral dose of 20 mg/kg DMN after one week. The rats were sacrificed 48 hrs after DMN administration.

Place and Duration of Study: University of Benin and Benson Idahosa University, Benin city, between January and April, 2015.

Results: In rats administered 20 mg/kg DMN, Annona muricata pre-treatment at 400 mg/kg body weight significantly reduced the levels of alanine aminotransferase (ALT), aspartate amino-transferase (AST), alkaline phosphatase (ALP), gamma-glutamyltransferase (GGT), total cholesterol (TC), triglyceride (TG) and malondialdehyde (MDA) as well as significantly increased reduced glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT) compared to DMN-alone administered rats which showed the opposite. Histopathological study in corroborating biochemical analysis also showed significant reduction of liver damage in the rats.

Conclusion: Annona muricata significantly restored the antioxidant levels in the liver, counteracted oxidative hepatic dysfunction and exhibited significant protective effect against DMN-induced liver toxicity, which can be mainly attributed to the antioxidant property of Annona muricata.

Open Access Original Research Article

CP-MLR Directed QSAR Rationales for the 1-aryl Sulfonyl Tryptamines as 5-HT6 Receptor Ligands

Manju Choudhary, Shreekant Deshpande, Brij Kishore Sharma

Journal of Pharmaceutical Research International, Page 1-17
DOI: 10.9734/BJPR/2015/18732

A QSAR study has been carried out to rationalize the 5-HT6 receptor binding affinities of the 1-aryl sulfonyl tryptamine derivatives using Dragon descriptors. A higher value of molecular symmetry and topology accounting Randic shape index descriptor PW4 (path/walk 4) would be favorable to improve the binding affinity. Presence of more number of bromine atoms (descriptor nBR) and presence of such structural fragment in which a hydrogen atom attached to sp3 hybridized carbon with no hetero atom rather than one hetero atom attached to next carbon atom (descriptors H-046 and H-052) will be supportive to the activity. The prevalence of atomic properties to explain the binding affinity is evident from the associations of polarizability to the path length 7 of Moran autocorrelation (MATS7p), masses to eigenvalues n.2 and 7 of Burden m atrix (BELm2 and BEHm7), Sanderson electronegativity to highest eigenvalue n.2 Burden matrix (BEHe2) and van der Waals volume to path length 8 of Geary autocorrelation (GATS8v) and charge content in terms of topological and mean topological charge indices (GGI3 and JGI2). The dominance of the information content of the descriptors, emerged in CP-MLR models, has also confirmed by the PLS analysis.

The derived QSAR models and descriptors shared in these models revealed that the substituents of tryptamine moiety have sufficient scope for further modification.

Open Access Review Article

Antibiotic Resistance: Challenges and Prospect for Therapy in Developing Countries

M. Y. Tula, O. Iyoha, F. O. Iruolaje

Journal of Pharmaceutical Research International, Page 1-16
DOI: 10.9734/BJPR/2015/19061

The hope raised by the discovery of antibiotics has been marred by the emergence of antibiotic resistance. The major reason for this is the inappropriate use of antibiotics due to a lack of uniform policy and disregard to hospital infection control practices. Bacterial infections increase the morbidity and mortality, increase the cost of treatment, and prolong hospital stay adding to the economical burden on the nation. The problem is further compounded by the lack of education and “over the counter” availability of antibiotics in developing countries where no one really has a good idea of the extent of antibiotic resistance, because it hasn’t been monitored in a coordinated fashion and there is no good national system to test for antibiotic resistance. This menace can be managed by a lot of concerted efforts with only a few prescribed in this review study.

Open Access Review Article

Screening of Pharmacognostical, Phytochemical Profile and Traditional Application of Ficus benghalensis

Sattya Narayan Talukdar, Md. Bokhtiar Rahman, Sudip Paul

Journal of Pharmaceutical Research International, Page 1-17
DOI: 10.9734/BJPR/2015/20130

Ficus benghalensis belonging to Moraceae family is mostly familiar as “Banyan tree” or “Indian fig” with several vernacular names. Gigantic in appearance, as a colossal evergreen tree, it is extended by spreading branches through the substantiation of aerial roots. As an indigenous plant of South Asia, it is considered as a sacred plant in certain regions because of its numerous roles in its history, culture, heritage, religion as well as inhabitant’s life style from ancient time. Its legendary remedial potency is also bolstered by enormous phytotherapeutical features recommended by local practitioner for long years and verified by epic ayurvedic classic “Charak Samhita”. Extensive presence of certain potent secondary metabolites including flavonoids, alkaloids, glycosides, phenolic compounds etc. has been screened out from its several portions including bark, root, leaf, fruit and latex. Current pharmacognostical evaluations unravel its effective functions as antioxidant, anti-diabetic, analgesic, anti-diarrheal agent and role in relieving several skin diseases. This review based on Ficus benghalensis is a compendium of its recent advancements in the field of phytopharmacognosy along with its ethnobotanically established therapeutical roles.