IRJP-VOLUME 01 ISSUE 01 SEPTEMBER 2011


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International Research Journal of Pharmaceuticals      ISSN 2048-4143 
Volume 01 No.01 September 2011 (Pages 1-41)      


Title

01) Electrochemical, Spectroscopic and Molecular Docking Studies of Anticancer Organogermalactones (pp. 1-8).

Author (s)


Fouzia Perveen, Rumana Qureshi, Afzal Shah, Safeer Ahmed, Farzana Latif Ansari, Saima Kalsoom and Sumera Mehboob 

Abstract

Cyclic voltammetry, UV-Vis spectroscopic and molecular docking methods have been used to predict the effect of biologically potent compounds on the DNA proliferation under physiological conditions (pH 7.4 and 4.7). The interaction of organogermanium compounds namely β-o-flourophenyl-γ-bis (8-quinolinoxy) germa-γ-lactone (GLf) and β-methyl-γ-bis (8-quinolinoxy) germa-γ-lactone (GLm) with DNA was investigated at human body temperature. The diffusion coefficients and heterogeneous electron transfer rate constants have been calculated and discussed. The comparison of the voltammetric signals of GLfand GLm revealed that the reduction potential of the reducing moiety, lactone can be modulated by changing the electronic properties of the attached substituents. For the investigation of the DNA binding affinity of germa-γ-lactones, the formation constants were calculated from the decrease in peak current and increase in absorbance. The experimental results were supported by molecular docking study. The current study is expected to provide useful insights into the design of anticancer drugs and understanding the mechanism by which such drugs interact with DNA and exert their biochemical action. 


Title

02) In-Vitro Antibacterial Activity of Two Medicinal Plants Neem (Azadirachta indica) and Peppermint (pp. 9-14).

Author (s)

 

Dr. Saba Irshad, Muneeba Butt and Hira Younus 

Abstract

The use of medicinal plants is a universal phenomenon. Every culture on earth has relied on the huge variety of natural chemistry found in healing plants for their therapeutic properties. All drugs of the past were substances with a particular therapeutic action and they were extracted from plants. Thus, medicinal plants may define as any plant that may have medicinal use. The objective of the present study was to evaluate the antibacterial activity of Neem (Azadirachta indica) and Peppermint (Mentha piperita) by using agar diffusion assay and gel filtration chromatography. The bacterial strains used in this research work were Escherichia coli, Bacillus subtilius, Salmonella typhi, Pseudomonas, Staphylococcus aureus, Klebsiella pneumoniae, Staphylococcus epidermitis. The Neem leaves (Azadirachta indica) were macerated in different organic solvents including pure, ethanol, acetone and methanol whereas Peppermint leaves (Mentha piperita) were macerated in acetone, methanol and ethanol. Then, by using agar diffusion assay antibacterial activity of these medicinal plants was estimated. The zones of inhibition were measured by scaling and represented by tables and graphs. The Neem extract of Acetone and Peppermint Oil showed the maximum antibacterial activity as compared to other solvent extracts. Then, distilled water macerated form of Neem and Peppermintwere used for gel filtration chromatography technique in order to determine the fraction containing the active components. Fraction 8 of both Neem and Peppermint showed maximum antibacterial activity against all above mentioned bacterial strains. Furthermore, this study recommended for the isolation and separation of bioactive compounds responsible for the antibacterial activity which would be done by using thin layer chromatography (TLC) and High-performance liquid chromatography (HPLC).


Title

03) Formulation and Evaluation of Polyherbal Gel for Wound Healing (pp. 15-20).

Author (s)

Nikunjana A Patel, Megha Patel and Rakesh P Patel

 

Abstract

Terminalia arjuna, Centella asiatica and Curcuma longa are reported to possess wound healing, anti-inflammatory, antioxidant and anti-bacterial activities. The carbopol 934 gel formulations containing different concentrations of extract of the above mentioned herbs were formulated and their wound healing activity was studied on experimentally induced open wounds in albino rats. The individual herbs were evaluated for their standard specification according to the Herbal Pharmacopoeia of India. Extracts were obtained by established procedures. HPTLC analysis for the extracts was carried out for identification of some known active constituents present in these herbs. Formulations containing 1% and 2% herbal extracts were prepared and applied topically three times a day to open wounds for 24 days post-operatively and compared with base control.  The treated wounds showed a faster rate of wound contraction compared with controls. The wound contraction studies revealed that the wound contractions increase with an increase in the herbal extract concentration.


Title

04) Formulation of Floating Mixed Matrix Tablets Using Low Density Copolymer (pp.27-32.

Author (s)

J. A. Raval, J. K. Patel and Nai-Hong Li


Abstract

Drugs with a narrow absorption window in the gastrointestinal tract have poor absorption. Therefore, gastroretentive drug delivery systems (GRDDS) have been developed, which prolong the gastric emptying time. Several techniques such as floating drug delivery system, low density systems, raft systems, mucoadhesive systems, high density systems, superporous hydrogels and magnetic systems, have been employed. Floating drug delivery systems have a bulk density less than gastric fluids and so, remain buoyant in the stomach for a prolonged period of time, releasing the drug slowly at the desired rate from the system. Dosage forms available as gastric floating systems include tablets, capsules, granules and microspheres. This research attempt is to investigate formulation of mixed matrix controlled drug delivery system with all the possible mechanisms used to achieve gastric retention. The tablets were prepared by direct compression technique, using hydrophilic matrixing polymers chitosan and carbopol with or without low density copolymer (used to get bouyancy). Tablets were physically characterized and evaluated for in vitro release characteristics for 8 hours in 0.1N HCl at 37oC. The effect of low density copolymer addition and drug release pattern was also studied. The release rate was modified by varying the concentration of matrix-forming polymers, and the addition of water-soluble or water-insoluble diluents. Variation on the floating lag time was checked with different concentrations of low-density copolymer. In vitro release mechanism was evaluated by kinetic modeling. Similarity factor, floating lag time, and drug release were taken as parameters for the selection of the best batch. The highly porous copolymer provided low density and, thus, excellent in vitro floating behavior of the tablets in the concentration of 17 %w/w. It was concluded that it was possible to formulate a low-density drug delivery system giving prolongation of the drug release patterns.


Title

05) Docking Modes of Pfz3 and its Analogues into the Lipoamide Binding Site on PDHK2 (pp. 33-41).

Author (s)

 Pragya Gahlot and Rita Kakkar


Abstract

Inhibitors based on the PDHK2 synthetic inhibitor Pfz3 have been docked into the lipoamide binding site of PDHK2. It is found that all analogues bind at the same site, and most of the proposed structural modifications lead to better binding. This suggests that homologous inhibitors have similar binding patterns in and modes of interaction with PDHK2, and have a similar inhibitory mechanism. In particular, replacement of the isopropyl group docking in the hydrophobic region by its fluoro analogue leads to better docking. Another potential improvement can be brought out by replacement of chlorine by bromine. Replacement of the carbonyl oxygen by sulphur, however, has a deleterious effect, as it reduces the hydrogen bond energy. Most of the considered modifications improve the score, and all but one of the new compounds score higher than Pfz3 itself. Further, ADME screening provided a peer analysis for the final selection of potential candidates from the compound library generated. This approach promises to suggest future leads for rational drug design.