Title |
In vitro studies on anti asthmatic, analgesic and anti convulsant activities of the medicinal plant Bryonia laciniosa.Linn |
| Int J Drug Discov Vol:2 Iss:2 (2010-12-21) : 1-10 |
Authors |
Vijay D., Jayarama Reddy, Gnanasekaran D., Ranganathan T.V. |
Published on |
21 Dec 2010 Pages : 1-10 Article Id : BIA0000175 Views : 1029 Downloads : 1033 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.2.1-10 |
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The study was carried out to ascertain anti asthmatic, analgesic and anti convulsant activities of
the medicinal plant Bryonia Laciniosa. The anti asthmatic activity was estimated by mesenteric mast cell
count by Atopic allergy method. Eddy's hot plate and Analgesiometer tests were used to assess the
analgesic activity of Bryonia Laciniosa. Anticonvulsant activity was evaluated by Maximum electroshockinduced
seizure test. The results indicated that 70% alcoholic extract of Bryonia laciniosa increased the
antiasmatic activity, analgestic activity and also anticonvulsant activity.
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Title |
Comparative modeling of CDP-diacylglycerol-serine O-phosphatidyltransferase in Clostridium botulinum: A potent target of Botulism |
| Int J Drug Discov Vol:2 Iss:2 (2010-12-21) : 11-16 |
Authors |
Koteswara Reddy G., Mohan Kalyan Reddy K., Nagamalleswara Rao K., Gyana R.Satpathy |
Published on |
21 Dec 2010 Pages : 11-16 Article Id : BIA0000176 Views : 1041 Downloads : 1166 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.2.11-16 |
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The bacteria Clostridium botulinum causing botulism. Botulism also known as botulinus
intoxication is a rare but serious paralytic illness caused by botulinum toxin, which is produced by the
bacterium Clostridium botulinum.CDP-diacylglycerol-serine O-phosphatidyltransferase is an enzyme
that catalyzes the CDP-diacylglycerol, L-serine and produce Cytidine monophosphate (CMP), (3-snphosphatidyl)-
L-serine in Clostridium botulinum. CMP is a nucleotide that is helpful in RNA synthesis in
Clostridium botulinum.The objective of enzyme inhibition needs structural characterization from its 3-D
structure in rational structure based drug design. Homology modeling can produce high-quality structural
models when the target and templates are closely related. MODELLER is the program used for
homology modeling which provides accurate and efficient models to build loops and side chains found
non-identical in sequence. It implements comparative protein structure modeling by satisfaction of
spatial restraints. The stereo chemical quality of a best model is validated by PROCHECK server with
86.2% residues under favored region from Ramachandran plot. The CASTp is used for locating,
delineating and measuring concave surface regions on three-dimensional structures of proteins. The
residues are identified in burial cavity of the best model as Leu (131,141,156), Ala (132), Ile (138,142),
Asn (145), Thr (149,153), and Gly (151) with hydrophobic nature. These include pocket located on
protein surfaces and voids buried in the interior of proteins that are frequently associated with binding
events. Thus present studies of modeling of CDP-diacylglycerol-serine O-phosphatidyltransferas
enzyme has brought future prospective to fight against botulism disease and provide better health
standaaards for community.
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Title |
Particulate vaccine for bacterial diseases |
| Int J Drug Discov Vol:2 Iss:2 (2010-12-21) : 17-19 |
Authors |
Hariprasad O., Gopinath V.P., Navya A., Yugandhar V.G., Sarma P.V.G.K |
Published on |
21 Dec 2010 Pages : 17-19 Article Id : BIA0000177 Views : 1044 Downloads : 948 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.2.17-19 |
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Particulate vaccines made a remarkable break through in the vaccines and drug
delivery systems. With their fine small structure they can pass through the cellular systems
and can trigger the type I and type II immune systems, which aid in the better immune
response. The sero conversation and the longevity of the particulate vaccines are found to be
better than the regular conventional vaccines. The development of recombinant vaccines and
sub unit vaccines having safer side in vaccination could not elicit stronger immune response,
because of their partial antigenicity. In such cases when coupled with nanoparticles triggers
better immune response. Recombinant Tetanus toxoid and Diphtheria toxoid when coupled
with nanoparticles showed significant TH1 and TH2 immune responses. Particulate vaccines
can be used in mucosal, nasal, ocular or transcutaneous modes for vaccination.
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Title |
Analog based pharmacophore strategy to identify novel leukotriene a4 hydrolase (LTA4H) inhibitors |
| Int J Drug Discov Vol:2 Iss:2 (2010-12-21) : 20-50 |
Authors |
Kranthi Raj K., Pathak L.P., Muttineni Ravikumar, Ramachandrana D. |
Published on |
21 Dec 2010 Pages : 20-50 Article Id : BIA0000178 Views : 1009 Downloads : 1047 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.2.20-50 |
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Leukotriene A4 hydrolase (LTA4H) is a hydrolase with a bifunctional zinc enzyme, which plays a
role in inflammation. LTA4H may also play an important role in carcinogenesis, especially chronic
inflammation-associated carcinogenesis. In this study, chemical feature based pharmacophore models
based on 22 currently available LTA4H inhibitors have been developed with the aid of HipHop and
HypoRefine modules within Catalyst program package. 3D pharmacophore model developed was,
characterized by distinct chemical features such as Hydrogen-bond acceptor (HA), Hydrogen-bond donor
(HD), Hydrophobic aliphatic (HPAli), Hydrophobic aromatic (HPAr) that are found to be responsible for the
activity of the LTA4H inhibitors. The correlation coefficient, root mean square deviation and cost difference
were 0.92, 1.0867 and 53.62 respectively, suggesting that a highly predictive pharmacophore model was
successfully obtained. The results of our study provide a valuable tool in designing new leads with desired
biological activity for virtual screening.
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Title |
Active site binding interactions of β-carboline derivative for HIV reverse transcriptase, protease and integrase |
| Int J Drug Discov Vol:2 Iss:2 (2010-12-21) : 51-55 |
Authors |
Prabha Garg, Rajender Kumar |
Published on |
21 Dec 2010 Pages : 51-55 Article Id : BIA0000179 Views : 1020 Downloads : 1042 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.2.51-55 |
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Abstract |
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Recently Anti-HIV activity of β-carboline derivatives is reported. The highly active compound
1-Formyl-beta-carboline-3-carboxylic acid methyl ester which has anti-HIV activity (IC50 = 2.9 μM) was
docked into the active sites of HIV reverse transcriptase (RT), integrase (IN) and protease (PR). The
compound was showing good binding energy score and binding interactions with RT as compared to PR
and IN after comparison of docking results. The compound showed two H bonding interactions with
Lys103 residue and good binding free energy score -8.63 Kcal/mol at temperature 298.15 K for HIV RT
protein.
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