Competitive/co-operative interactions in acid base sandwich: role of cation vs. substituents

Journal of Molecular Modeling - The glass transition temperature (T g) and density of poly-(phthalazinone ether sulfone ketone) (PPESK A) were estimated by molecular dynamic (MD) simulation. A...     

In vitro anti- biofilm and anti-bacterial activity of Sesbania grandiflora extract against Staphylococcus aureus

The main objective of this research is to investigate the anti-biofilm and anti-bacterial activity of Sesbania grandiflora (S. grandiflora) against Staphylococcus aureus. S. grandiflora extract were prepared and analyzed with UV –Vis spectroscopy, Fourier transform infrared spectroscopy, Dynamic light scattering. Biofilm forming pathogens were identified by congo-red assay. Quantification of Extracellular polymeric substance (EPS) particularly protein and carbohydrate were calculated. The efficacy of the herbal extract S. grandiflora and its inhibition against the pathogenic strain of S. aureus was also evaluated. The gradual decrease or disappearance of peaks reveals the reduction of protein and carbohydrate content in the EPS of S. aureus when treated with S. grandiflora. The antibacterial activity of S. grandiflora extract against the bacterial strain S. aureus showed that the extract were more active against the strain. To conclude, anti-biofilm and antibacterial efficacy of S. grandiflora plays a vital role over biofilm producing pathogens and act as a good source for controlling the microbial population.     

Aryloxy cyclohexyl imidazoles: A novel class of antileishmanial agents

Thirteen novel aryloxy cyclohexane-based mono and bis imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani and cytotoxicity assessed. These compounds were better than the existing drugs, sodium stibogluconate and pentamidine in respect to IC₅₀ and SI values. Promising compounds were tested further in vivo. Among all, the bis methylimidazole with 2-fluoro, 4-nitro aryloxy group (9) exhibited significant in vivo inhibition of 77.9%, thus providing new structural lead for antileishmanials.     

Identification of a Peptide-like Compound with Antimicrobial and Trypsin Inhibitory Activity from Seeds of Bottle Gourd (Lagenaria siceraria)

A low molecular mass peptide like compound with antimicrobial and trypsin inhibitory activity was isolated from the seeds of Lagenaria siceraria. It was purified by ion-exchange and reverse-phase chromatography. The molecular weight of the compound was 678.9 Dalton as determined by MALDI-MS. The infra-red absorbance at 1639 cm^?1, characteristic of an amide bond, by FTIR spectroscopic studies, and absorption at 214 nm on spectrophotometer indicates the peptidic nature of the compound. The compound exhibited antimicrobial activity when tested against Escherichia coli with minimum inhibitory concentration of 20 μM, and trypsin inhibitory activity inhibiting trypsin at a molar ratio of 1:2.     

Morphological,ecological and biological variations in the mustard aphid,Lipaphis pseudobrassicae (Kaltenbach) (Hemiptera: Aphididae) from different host plants

Genetic and morphological differentiation of insect populations in relation to the use of different host plants is an important phenomenon that leads to ecological specialization. In this study, we describe variations in morphology, and in ecological and biological parameters of Lipaphis pseudobrassicae (Kaltenbach) clones associated with three host species of Cruciferae, Brassica juncea (L.) var. rai sarson Czern and Cross (brown mustard), Brassica campestris L. var. sarson Prain (yellow mustard), and Rorippa indica (L.) Hiern (wild herb). This study was aimed at obtaining evidence regarding phenotypic differentiation induced by, or associated with, the use of distinct host species. Ten morphological characters, 4 growth parameters and 8 biological functions were investigated in wingless aphids collected from plants of the three host species. Aphids from B. campestris and B. juncea clones were bigger in size, heavier in weight and showed higher growth rates and fecundity than the clones from R. indica. Between the two crop plants, clones from B. juncea showed significantly higher growth rates than the clones from B. campestris. Transfer of L. pseudobrassicae populations from B. campestris to B. juncea and R. indica and vice versa resulted in poor performance. Results indicate that the average phenotype of L. pseudobrassicae individuals inhabiting different host plant species differs as a consequence of the contrasting feeding environments the host species provide.     

The Parkinson’s disease kinase LRRK2 autophosphorylates its GTPase domain at multiple sites

Mutations in leucine-rich repeat kinase 2 (LRRK2) are a common cause of inherited Parkinson’s disease (PD). The protein is large and complex, but pathogenic mutations cluster in a region containing GTPase and kinase domains. LRRK2 can autophosphorylate in vitro within a dimer pair, although the significance of this reaction is unclear. Here, we mapped the sites of autophosphorylation within LRRK2 and found several potential phosphorylation sites within the GTPase domain. Using mass spectrometry, we found that Thr1343 is phosphorylated and, using kinase dead versions of LRRK2, show that this is an autophosphorylation site. However, we also find evidence for additional sites in the GTPase domain and in other regions of the protein suggesting that there may be multiple autophosphorylation sites within LRRK2. These data suggest that the kinase and GTPase activities of LRRK2 may exhibit complex autoregulatory interdependence.     

Understanding the molecular basis of plant growth promotional effect of Pseudomonas fluorescens on rice through protein profiling

Background  

Plant Growth Promoting Rhizobacteria (PGPR), Pseudomonas fluorescens strain KH-1 was found to exhibit plant growth promotional activity in rice under both in-vitro and in-vivo conditions. But the mechanism underlying such promotional activity of P. fluorescens is not yet understood clearly. In this study, efforts were made to elucidate the molecular responses of rice plants to P. fluorescens treatment through protein profiling. Two-dimensional polyacrylamide gel electrophoresis strategy was adopted to identify the PGPR responsive proteins and the differentially expressed proteins were analyzed by mass spectrometry.     

Synthesis and appetite suppressant activity of 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes as conformationally rigid analogues of fluoxetine

Several 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes (7-21) as conformationally rigid analogues of fluoxetine were synthesized and evaluated for their anorexigenic and antidepressant activities. For SAR studies the related acyclic analogues (22-27) were also prepared. Out of the 21 synthesized compounds, 10 compounds (9, 10, 11, 15, 16, 18, 21, 22, 23 and 27) exhibited significant anorexigenic activity (at 75 micromol/kg). Interestingly, all the compounds (7-20, 22-26) were devoid of antidepressant effect, except for compounds 21 and 27 in which the antidepressant activity was retained. Compound 16 emerged as the most active compound of the series with better anorexigenic activity (97.92%) compared to fluoxetine (76.25%) and even with a clinically used drug sibutramine, thus providing a new structural lead for appetite suppressants.     

Sarcomere lesion damage occurs mainly in slow fibers of reloaded rat adductor longus muscles

Sarcomerelesions were previously observed with reloading of rat adductor longusmuscles after spaceflight and hindlimb unloading (HU).Spaceflown rats displayed more lesioned fibers in the"slow-fiber" region, suggesting a damage-susceptible fiber type.Unloading induces fast myosin expression in some slow fibers,generating hybrid fibers. We examined whether lesion damage differedamong slow-, hybrid-, and fast-fiber types in HU-reloaded adductorlongus muscles. Temporal HU for 5, 8, 11, 14, and 17 days revealed that hybrid fiber percent, detected by antimyosin immunostaining, peaked at29 ± 12% by 14 days. A 14-day HU followed by 12-14 h ofvoluntary reloading was performed to induce lesions.² analysis showed that slowfibers were preferentially damaged, accounting for 92 ± 5% oflesioned fibers; hybrid and fast fibers accounted for 7 ± 4 and<0.5%, respectively. Atrophy did not explain differential lesiondamage across fiber types, as slow and hybrid fibers atrophied to asimilar extent. Because active myofiber contractions are requisite forlesion formation, selective recruitment of slow fibers most likelyexplains their damage susceptibility.