IR@IIIM - Indian Institute of Integrative Medicine (CSIR)
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Quantitative structure activity relationship (QSAR) of piperine analogsfor bacterial NorA efflux pump inhibitors
No full textQuantitative structure activity relationship (QSAR) analysis of piperine analogs as inhibitors of efflux
pump NorA from Staphylococcus aureus has been performed in order to obtain a highly accurate model enabling prediction of inhibition of S. aureus NorA of new chemical entities from natural sources as well as synthetic ones. Algorithm based on genetic function approximation method of variable selection in Cerius2 was used to generate the model. Among several types of descriptors viz., topological, spatial,
thermodynamic, information content and E-state indices that were considered in generating the QSAR model, three descriptors such as partial negative surface area of the compounds, area of the molecular shadow in the XZ plane and heat of formation of the molecules resulted in a statistically significant model with r
Restoration of stress-induced altered T cell function and corresponding cytokines patterns by Withanolide A
No full textThis study was taken up to see the effect of Withanolide A (WS-1), a compound isolated from Withania somnifera root extract on chronic stress-induced alterations on T lymphocyte subset distribution and corresponding cytokine secretion patterns in experimental Swiss albino mice. Stress disturbs the homeostatic state of the organism and brings about behavioral, endocrine and immunological changes. The chronic suppression induced by stress depresses the immune functioning and increases susceptibility to diseases.Oral administration of WS-1 once daily at the graded doses of 0.25, 0.5, 1 and 2 mg/kg p.o. caused significant recovery of stress-induced depleted T cell population causing an increase in the expression of IL-2 and IFN-gamma (a signature cytokine of Th1 helper cells) and a decrease in the concentration of
corticosterone in stressed experimental animals. It also reversed the restraint stress-induced increase in
plasma alanine aminotransferase (ALT), aspartate aminotransferase(AST) and hepatic lipid peroxidation (LP)
levels and improved the restraint stress-induced decrease in hepatic glutathione (GSH), and glycogen levels,
thus showing the significant antistress potential of the test drug
Microwave-assisted synthesis of N-substituted cyclic imides and their evaluation for anticancer and anti-inflammatory activities
No full textA number of N-substituted cyclic imides 3a–e, 5a–e, 7a–d, and 9a–e have been synthesized in very high yields, by condensation of various diacids 2, 4, 6, and 8 with different amines under microwave irradiation.These compounds were screened for anticancer and anti-inflammatory activities, and compounds 3c, 3e, 5c, 9c, and 9d exhibited anticancer activity against colon (COLO 205) cancer better than 5-fluorouracil and mitomycin-C, and compound 9b exhibited anti-inflammatory activity better than standard drug phenyl butazone
Allyl tetrahydropyranyl ether: a versatile alcohol/thiol protecting reagent
No full textAllyl tetrahydropyranyl ether (ATHPE) can be used as a versatile protecting reagent. In combination with
NBS/I2, O-allyl group can easily be replaced by hydroxyls (including tertiary-OH) or thiols, in the molecules
comprising other reactive functional groups such as halogen, nitro, acetonide and alkene under mild reaction conditions (near neutral pH and ambient temperature)
Evaluation of the Antimicrobial, Antioxidant, and Anti-Inflammatory Activities of Hydroxychavicol for Its Potential Use as an Oral Care Agent
No full textHydroxychavicol isolated from the chloroform extraction of aqueous extract of Piper betle leaves showed inhibitory activity against oral cavity pathogens. It exhibited an inhibitory effect on all of the oral cavity pathogens tested (MICs of 62.5 to 500 �g/ml) with a minimal bactericidal concentration that was twofold greater than the inhibitory concentration. Hydroxychavicol exhibited concentration-dependent killing of Streptococcus
mutans ATCC 25175 up to 4� MIC and also prevented the formation of water-insoluble glucan. Interestingly, hydroxychavicol exhibited an extended postantibiotic effect of 6 to 7 h and prevented the emergence of mutants of S. mutans ATCC 25175 and Actinomyces viscosus ATCC 15987 at 2� MIC. Furthermore,it also inhibited the growth of biofilms generated by S. mutans and A. viscosus and reduced the preformed biofilms by these bacteria. Increased uptake of propidium iodide by hydroxychavicol-treated cells of S. mutans and A. viscosus indicated that hydroxychavicol probably works through the disruption of the permeability
barrier of microbial membrane structures. Hydroxychavicol also exhibited potent antioxidant and anti-inflammatory
activities. This was evident from its concentration-dependent inhibition of lipid peroxidation and significant suppression of tumor necrosis factor alpha expression in human neutrophils. Its efficacy against adherent cells of S. mutans in water-insoluble glucan in the presence of sucrose suggests that hydroxychavicol would be a useful compound for the development of antibacterial agents against oral pathogens and that it has great potential for use in mouthwash for preventing and treating oral infections
Molecular characterization of bacterial population in the forest soil of Kashmir, India
No full textThe bacterial diversity in the forest soil of Kashmir, India was investigated by 16S rDNA-dependent molecular phylogeny. Small subunit rRNA (16S rDNA)from forest soil metagenome were amplified by polymerase chain reaction (PCR) using primers specific to the domain bacteria. 30 unique phylotypes were obtained by PCR based RFLP of 16S rRNA genes using endonucleases Hae 111 and Msp 1, which were most suitable to score the genetic diversity. The use of 16S rRNA analysis allowed identification of several bacterial populations in the soil belonging to the following phyla: Firmicutes (33.3%),Bacteroidetes (13.3%), Proteobacterium (6.6%), Planctomycete(3.3%), and Deferribacteraceae (3.3%) in addition to the others that were not classified, beyond Archaea domain, However, 36.6% of the retrieved bacterial sequences could not be grouped with any phylum/lineage.The large amount of unclassified clone sequence could imply that novel groups of bacteria were present in the forest soil
Structure–activity relationship (SAR) of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads
No full textAnalogues of parthenin were synthesized by substitutions at different reaction centres to establish a structure–activity relationship (SAR). Some of the molecules have displayed significant cytotoxicity in human cervical carcinoma (HeLa) and human myeloid leukemia (HL-60) cells. A few of the compounds also induced apoptosis in HL-60 cells measured in terms of sub-Go/G1 DNA fraction. Also one of the lead
molecules has been shown to be the inhibitor of both telomerase and topoisomerase-II
Synthesis, anticancer, and anti-inflammatory activity evaluation of methanesulfonamide and amidine derivatives of 3,4-diaryl-2-imino-4-thiazolines
No full textCondensation of 3,4-diaryl-2-imino-4-thiazolines 1a–j with methanesulfonyl chloride gavemethanesulfonamide derivatives 2a–j. Condensation of 2-cyanopyrazine,4-cyanopyridine, and 2-cyanopyridine with 3,4-diaryl-2-imino-4-thiazolines 1h–m in the presence of sodium methoxide afforded amidine derivatives 3a–j. Compounds 2a–j and 3a–j were screened against various human cancer cell lines(COLO-205, HEP-2, A-549, IMR-32) and their percentage growth inhibition profile determined at 1 × 10−5M. The antiinflammatory
activity of these compoundswas assessed using the carrageenan-induced paw edema model. Compound 2i exhibited 34.7% anti-inflammatory activity at 50 mg/kg p.o.,which is comparable to standard care drug phenyl butazone\ud
(37% activity at 50 mg/kg p.o.
A simple and reliable preparative high-performance liquid chromatographic technique for isolation of a bioactive flavone diglycoside from and extract of <i>Cuminum cyminum</i> seeds
No full textIn this paper we describe a sensitive and reproducible reversed-phase highperformance liquid chromatography (HPLC) method with photodiode-array detection for isolation and quantification of the bioactive hydrophilic constituent 7-(1-O-β-D-galacturonide-4′-(1-O-β-D-glucopyranosyl)-3′,4′,5,7-tetrahydroxyflavone, 1, from the seeds of Cuminum cyminum. Compound 1 was separated isocratically on a C18 preparative column, in high purity, after removal of solvents. The purity and identity of the compound were established by use of LC–mass spectrometry and by spectroscopic techniques(1H and 13C NMR). The purity of 1 was also confirmed by HPTLC
Arthrobacter sp. lipase immobilization on magnetic sol 13gel composite supports for enantioselectivity improvement
No full textA bacterial lipase from Arthrobacter sp. (ABL: IIIM Jammu, India strain, MTCC No. 5125) has been immobilized on non-magnetic (Type A) and magnetic (Type B) supports derived from copolymerization of 3-aminopropyltriethoxysilane and tetraethylorthosilicate.Immobilized ABLpresented 21 1334 mg/g protein binding providing 30 1375 units/g activity in Type A non-magnetic composites and 24 1345 mg/g protein
binding providing 35 1390 units/g activity with Type B supports containing magnetic particles. Immobilized
ABL preparations have shownenhanced stability at pH5 139 and temperature up to 70 8C whereas free ABL is
unstable under these conditions. Improved hydrolytic conversion as well as enantioselectivity were
observedwith acylfluoxetine intermediate (ethyl3-hydroxy-3-phenylpropanoate alkyl acylates) andchiral
auxiliaryacyl 1-phenyl ethanol usingimmobilized ABL derivatives (ee�99%; 3 134-fold increase in E-values)
as compared to ABL enzyme/cells (ee 93 1398%). Introduction of magnetic particles in these supports has led
to easier separation process with high product recovery yields