Qsar studies of side chain modified DI and TRI-peptides in mimicking the Bio-potency of anti-nociceptive action of enkephalin

QSAR Studies of smaller chain peptides has been proposed for predicting enkephalin mimic anti-nociceptive activity using a lipophilic parameter partition coefficient. C Log P Program was developed basically based on the fragmentation approach, has been written in Fortran IV. The test compounds, Ile-Val, Phe-Gly, Asn-Cys, Gly-Cys-Val and Ile-Val-Glu were encoded as topological representation of molecular structures using alpha numeric language smiles notation. Log P values obtained for the smaller chain dipeptides and tri-peptides were -0.481 [Ile-Val]; -1.757 [Phe-Gly]; -4,159 [Asn-Cys]; -2.318 [Gly-Cys-Val] and -1.627 [Ile-Val-Glu]. Substitution of glycyl or L-amino acid residues by D-amino acids at appropriate sites of some bioactive peptides may cause a considerable rise in potency. The effect is most dramatic at the Gly-position of enkephalin. Drugs which are to be targeted for the CNS should have log P value of approximately 2. Hence it was concluded that Phe-Gly and Gly-Cys-Val are selected as potential targets for enkephalin like anti-nociceptive activity

Evaluation studies of antimicrobial activity on the leaf extracts of Achyranthes aspera Linn

Disc diffusion method was employed to determine the effect of methanol, acetone and chloroform extracts of the dried leaves of Achyranthes aspera against Staphylococcus aureus, Streptococcus fecalis, Klebsiella pneumoniae, Proteus vulgaris, Escherichia coli, Pseudomonas aeruginosa and Candida albicans. The chloroform extract shown to exhibit maximum potency against E. coli and Pseudomonas aeruginosa. Methanol extract showed moderate potency against E. coli and Candida species. Acetone extract was less effective against most of the species used except Streptococcus fecalis. Among all the extracts tested, none of the extract was found to be effective against gram positive S. aureus and gram negative Proteus vulgaris

Antimicrobial activity of extracts and isolates of the leaves of Plumeria alba Linn.

Disc diffusion method was employed to determine the effect of methanol, chloroform and acetone extracts of the dried leaves of Plumeria alba Linn. [Apocyitaceac] against fungi [Candida albicans] and bacteria [Bacillus subtilis, Proteus vulgaris Staphylococcus aureus. Pseudomonas aeruginosa, Streptococcus fecalis, Escherichio coil, Staphylococcus albus and Klebsiella pneumoniae]. The methanol and acetone extracts exhibited a prominent antimicrobial activity. The methanolic and acetone extracts were further fractionated by column chromatography to yield 2 pure isolates. The methanol pure component-2 [MPC[2]-50% Ethyl acetate:Methanol] and Acetone pure component-2 [APC[2]-70% Acetone:Ethyl acetate] have shown significant activity against all organisms used except Klebsiella

Anti-microbial activity of extracts and isolates of leaves of acalypha canescana linn

The in vitro antibacterial activity of the extracts and isolates of Acalypha canescana [leaves] have been studied against bacteria [Bacillus subtilis, Staphlylococcus aureus, Proteus vulgaris, Pseudomonas aeruginosa] and fungi [Candida albicans]. The total acetone extract, total methanol extract, total chloroform extract, total benzene extract and the fractionated two isolates of acetone extract and benzene extract have shown significant activity against the organisms used, almost comparable with the standard drugs Ciprofloxacin and Clotrimazolc. This in vitro testing also resulted in activity guided isolation of four antibacterial and antifungal principles from the leaves

In vivo anti-tumour activity of Wrightia tomentosa in Ehrlich ascites carcinoma bearing mice

Anti-tumour activity of ethanolic extracts of leaf and bark of Wrightia tomentosa [Fam: Apocynaceae] in the mice transplanted with Ehrlich ascites carcinoma [EAC] were investigated. The EAC mice receiving 100 and 200 mg/kg ethanolic leaf and bark extract showed a dose dependent elevation in tumour-free survival and a highest number of survivors were observed at 200 mg/kg for leaf extract of ethanol. which was considered as an optimum dose for its neoplastic action. The Median survival time [MST] for this dose was approximately 44 days when compared with 23 days of non-drug treated controls. Statistical analysis also indicates that the leaf extract showed highly significant anti-tumour potency [p<0.00l] when compared with control

Hepatoprotective effect of ethanol extract from leaves of Phyllanthus emblica in rats

In this study, phytochemical extraction was carried out on the leaves of Phyllanthus emblica using ethanol as the organic solvent. The antioxidant activity of ethanol extract from Phyllanthus emblica was evaluated by various biochemical marker parameters, including super oxide dismutase [SOD - anion radical scavenging], catalase [CAT - hydrogen peroxide scavenging], glutathione peroxidase [GPX], glutathione reductase [GRD - reducing power], glutathione transferase [GTS] and thio-barbituric acid reactive substances [TBARS] measurement. Hepato cellular damage was induced by intraperitoneal administration of CCl[4] in male albino Sprague-Dawley strain rats. The reduced levels of SOD, CAT, GPX and GRD with CCl[4] treated animals attain normal level, after administration of ethanolic extract of Phyllanthus emblica. However, the activity of GTS was significantly higher in CCl[4] treated animals, which were brought down towards normal level in herb treated rats. The increased concentration of TBARS with CCl[4] treated rats attains normal level after administration of ethanolic extract of the same plant. An antioxidant property appears to be predominantly responsible for this hepato-protective action of the drug

Pharmacological evaluation of smaller chain di- and tri-peptides in alloxan-induced rabbits

Amino acids and smaller chain peptides form an integral part of body's inventory of drugs which maintain the various functions, vital to human life and health. Test drugs such as Ile-Val, Ile-Val-Glu and Gly-Phe showed significant anti-diabetic activity, with Ile-Val being most effective amongst all using insulin as a standard drug. Statistical analysis showed that test drug possessed significant antidiabetic activity [t-value at P<0.01=4.02]. The smaller chain peptide combinations are showing significant anti-diabetic activity due to better physical and chemical stability in comparison with the long chain peptide combinations of the standard insulin

Toward a pharmacophore for anti-tumor based tubulin inhibitors: insight from a catalyst hypogen mapping of cryptophycin analogues

The invention of a new class of anti-tumour tubulin inhibitors based on a pharmacophore hypothesis for small molecule analogues of cryptophycin is discussed. A training set of 20 compounds was selected from 45 crypiophycin inhibitors [1C 50 value ranges from 0.022 nm to 1860 nm] of Periyar Bio in-house data bases to generate hypogen model. All structures were built and minimized within the CATALYST and conformational analysis was implemented using the pooling algorithm. The maximum number of conformers generated was 250 and a range of 10 kcal/mol was chosen. Training set consists of 20 compounds tested against human tubulin was used to develop pharmacophore hypothesis. Among the generated 10 hypotheses, the best pharmacophore model [Hypothesis 1] feature one hydrogen bond acceptor, one hydrogen bond donor, one hydrophobic aliphatic and one ring aromatic with the correlation coefficient of 0.948, RMS deviation of 0.774, and a cost difference of 57.71. The obtained pharmacophore models were validated on 18 test molecules. The mapping of hypothesis 1 models on to a highly active compound 6S [1C 50 = 0.58 nm] and the mapping of hypothesis 1 model on to a highly inactive compound 7a [1C 50 = 2000 nm], was successfully designed using CATALYST Hypogen. For the test set, the accuracy in predicting active compounds was greater than 95%, while 8% and 1% representing both false positive and negative, respectively