Pakistan Journal of Pharmaceutical Research

7

Authors: Mubashar Aziz1, Rakhshanda Baqai², Shahana Urooj Kazmi², Zulfiqar Ali Mirani3, Ahsan Sattar Sheikh4, Mazhar Ayaz1 ,Muhammad Hanif5, Najmul Hasan6

Bacterial biofilms are complex structured communities surrounded in a matrix of extra-cellular polymeric substances growing on rough surfaces. It is involved in multiple functions like trapping of nutrients, adherence, stability of biofilm structure and the penetration of many antibiotics.250Pus samples were collected from the depth of ulcers from each patient using Amies Transport Swabs. The specimens were inoculated on appropriate media. Biochemical characteristics of pathogens were observed by performing conventional biochemical tests and Quick Test Strips. Antibiotic resistance of isolates was checked by Kirby Bauer’s Disc Diffusion Method. Biofilm formation was initially detected by Congo Red Agar Method. Major biofilm forming isolates from different hospitals environment were Klebsiella spp., Corynebacterium spp., S. epidermidis while from hospital curtain’s samples, Shigella dysenteriae, Candida albicans and Aspergillus flavus were having capability of biofilm formation. S. aureus showed good biofilm forming ability in presence of 0.2% glucose, sucrose and lactose, P. aeruginosa showed enhancement in biofilm formation in presence of sucrose, glucose, and maltose while E. coli indicated increased biofilm formation in presence of lactose, sucrose and glucose. Most of the biofilm forming isolates were Multi drug resistant which indicate that extracellular material released by these pathogens cover the bacteria cell and hinder the antibiotic

10

Authors: Nor Hisam Zamakshshari1, Siau Hui Mah2, Gwendoline Cheng LianEe*1, Zalikha Ibrahim3, Soek Sin Teh4 and Irene See1

A series of xanthones isolated from Calophyllum depressinervosum and Calophyllum buxifolium were studied for their cytotoxicities. Ananixanthone (1), caloxanthone B (2), caloxanthone I (3), caloxanthone J (4), xanthochymone B (5), thwaitesixanthone (6),1,3,5,6-tetrahydroxyxanthone (7) and dombakinaxanthone (8) were successfully isolated from both Calophyllum species. These eight compoundsand a synthetically derived compound, thwaitesixanthone monoacetate (9) were tested for cytotoxicity activities against stomach cancer, SNU-1and LS-174T cell lines. Caloxanthone B (2) gave the highest cytotoxic activity against SNU-1 with anIC50 valueof 1.47μg/ml. Meanwhile, xanthochymone B (5) shows the highest cytotoxic activity against LS-174T cell with an IC50 value of 0.45μg/ml. The structure-activity relationship (SAR) studies predicted that the presence and arrangements of furano, pyrano and prenyl substituents in the xanthone skeleton are important towardsthe cytotoxic activity. A molecular docking simulation was performed tomodel the probable binding models of compound 2 into the HER-2(PDB ID: 3PP0) and compound 5 into β-catenin (PDB ID: 1JDH).

15

Authors: S. Ashutosh Kumar*1, Manidipa Debnath2, K. Anusha3, K. Manna1, JVLN Seshagiri Rao4, M. K. Singh1

The present investigation was undertaken to formulate and evaluate the losartan floating and bioadhesive drug delivery system using different polymers in different ratios. The main objective of the present work is to develop a novel osmotically controlled drug delivery system of losartan. It was aimed to prepare for prolonged residence in the stomach over conventional gastro retentive approaches. As the drug has short biological half-life (2 hours) hence it becomes necessary that it should be administered in 2 or 3 doses of 2.5 to 10 mg per day. Thus, the development of controlled-release dosage forms would clearly be advantageous. Formulated tablets gave satisfactory results for various evaluation parameters like tablet hardness, friability, weight variation, thickness, floating lag time, floating duration, content uniformity, ex vivo osmotically controlled strength and in vitro drug release. In all formulations Carbopol 974P is used to add osmotically controlled strength but the concentration of this polymer has significantly influenced the drug release due to its retarding property. Comparing the three different grades of Hydroxy propyl methyl cellulose (HPLC) (K4M, K15M and K100M), it was found that low-viscosity grades of HPMC K4M formulations released drug rapidly compared to K15M HPLC and K100M HPLC. Among all formulations K15M grade provided better controlled release characteristics with excellent drug release and in vitro buoyancy. From the above, it was also evident that at higher viscosity grades of polymer concentrations, the rate of drug release was retarded greatly.

4

Authors: Sana Riaz, Muhammad Aadil, , Sohail Anjum, Ghulam Mustafa and Tariq Javed

Finger print patterns are extensively used for the study of individuality as most legitimate evidence against criminals. Due to the massive potential of fingerprints as a definite method of identification they can be useful to analyze their correlation with gender. In present study, total 166 Pakistani subjects with (70.83%) of males and (29.1%) of females were selected for this study. Whorls were the most frequent fingerprint pattern (48.21%), while arches were the least common (10.11%). There high frequency of whorls (35.4%) and females have higher incidence of loops (14.2%).The ridge density can also predict the gender as the female had higher ridge density (13±1) than males (12±1).Whorls were predominant in blood group O, A, B and AB in both Rh negative and Rh positive individuals.

5

Authors: Ardas Masood, Sania Ahmad, Asma Noor, Jawaria Khan, Sibtain Haider, Muhammad Imran Qadir

HIV–1 (human immunodeficiency virus type–1) is the disease causing agent for AIDS. It is pathogenic retrovirus which joined in a long polypeptide chain when viral RNA is translated into a polypeptide sequence. It contains different proteins like reverse transcriptase, protease, integrase, etc. These proteins have to be altered from polypeptide chain before these enzymes become to start function. Reverse transcriptase is inhibited by. We applied existing system by virtual screening analysis of HIV-RT from PDB database versus chemical compounds from ZINC database using “Autodockvina” and “cornia sketch tool”. Different hypothetical ligands were deliberate on cornia sketch tool and their structures were docked with (HIV-RT) PDB file. The structure with best recording was selected and the database of zinc was separated for similar structures and consequences in 18 hits.

6

Authors: Jean Carlo González-Guevara, German L Madrigal Redondo, Rolando Vargas Zúñiga, Santiago Rodríguez Sibaja

Introduction: Ginger is a medicinal plant native to India. Has been reported their potential use in cosmetics, medicines and natural products, however depending on crop conditions the medicinal components of the different parts of the plant not only changes in concentration but in its composition, this modifies its medicinal action. The aim of this study was to characterize by physicochemical methods the chemical composition of essential oil obtained from rhizomes of Zingiber officinale grown in the area of San Carlos, Costa Rica in order to standardize future hydroponic cultivations of the plant and validate their subsequent pharmacological or cosmetic effects. Materials and methods: the rhizomes of the plant were used, the active principles were extracted by ethanolic extraction with Soxleth and distillation by entrainment with vapor, analysis was performed by using a qualitative phytochemical profile for the ethanolic extract, and the composition of the essential oil was studied by gas chromatography coupled to mass spectrometry detector (GC-MS).Results and Conclusions. The presence of flavonoids, alkaloids, saponins, tannins and triterpenes in the ethanolic extract was qualitatively determined. In characterizing the essential oil by GC-MS were identified as lead compounds the geranialdehyde (27.42%), nerol (20.11%), 1.8-cineole (13.35%), camphene (4.65%) and E-geraniol (3.92%). The composition obtained was compared with the composition reported in the literature, obtaining a clear difference with those reported in other studies, allowing predicting an antimicrobial behavior unlike most traditional essential oils of the rhizomes.

11

Authors: Muhammad Saleem, Amna Batool, Umme Habib a Hasan, UmerMaqsood, Farha Abid

Various pathophysiologic facets contribute to the pathogenesis of hypertension and are root causes of cardiovascular diseases with end-organ damage. Seeing that, reninangiotensin pathway along with sympathetic nervous system are predominantly involved in HTN development and recently targeted with conventional antihypertensive therapies including diuretics, b-blockers, and calcium channel blockers, renin–angiotenin–aldosterone system antagonists with erratic results. Although current therapeutic modalities target these contributory factors but still not effectual in the apt management of blood pressure in many populations thus pointing towards the inevitability of newer pharmacological as well as non-pharmacological approaches to not only manage but cure this perplexing disorder. Aldosterone synthase inhibitor, selective aldosterone receptor antagonist, prorenin inhibitor and vasopeptidase inhibitor in company with other complementary alternatives consisting of vaccine based strategies, gene based therapeutics (targeting both vasodilatory genes along with vasoconstrictor genes), fine-tuning of endothelium-mediated responses and device base interventions including baroreflex sensitization and renal sympathetic denervation may lead to more effective , curative or preventive employment against CVS diseases. Hence, these narrative approaches in HTN therapeutics are although slow in progress but intriguing area which in future might be more beneficial in the treatment and management of hypertension in majority of populace with minimum risks.