RESUMO
Labdane diterpene andrographolide (1) is a major constituent of Andrographis paniculata and known to exhibit wide spectrum of biological activities. In this study, regioselective monoesters of (1) have been synthesized by using Amano lipase AK (Pseudomonas fluorescens) as a biocatalyst. Amano lipase AK was able to execute highly efficient esterification of hydroxyl group attached to C-14 carbon of (1) in presence of acyl donors. Among the various synthesized derivatives including two novel compounds such as andrographolide-14-propionate (3) and andrographolide-14-caproate (5) displayed antimicrobial activity against Staphylococcus aureus with low minimal inhibitory concentration (MIC) 4⯵g/mL and 16⯵g/mL respectively. Furthermore, they have shown low hemolysis activity at their respective MIC and increase in the permeability of the bacterial cell membrane as delineated by FITC uptake and SEM imaging studies.
Assuntos
Antibacterianos/farmacologia , Diterpenos/farmacologia , Lipase/metabolismo , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/biossíntese , Antibacterianos/química , Diterpenos/química , Diterpenos/metabolismo , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pseudomonas fluorescens/enzimologia , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
On 7 February 2021, Chamoli district (Uttarakhand, India) was devastated by a deadly rock-ice avalanche that led to a large causality of more than 200 people and a huge economic loss. We found noteworthy sequence of precursory signals of main failure/detachment preceded by a dynamic nucleation phase. The rock-ice avalanche appears to have been initiated by seismic precursors which were continuously active for 2:30 h prior to main detachment. The seismic amplitude, frequency characteristics and signal-to-noise ratio variation of detected tremors indicate static to dynamic changes in nucleation phase located at the source of detached wedge. The characteristics of seismic data distinguished debris flow and hitting obstacles from other seismic sources and allowed the estimations of debris flow speed. We analyzed and verified the seismic signals with field evidences to estimate the associated impacts and velocity of dynamic flow. The proximal high-quality seismic data allowed us to reconstruct the complete chronological sequence and evaluate impacts since the initiation of nucleation phase to its advancement. Furthermore, we suggest that real-time seismic monitoring with existing network and future deployment of integrated dense network can be used for forecasting of flow events and hazard mitigation in the downstream.
Assuntos
Desastres , Gelo , Humanos , ÍndiaRESUMO
In this data article we describe screening of various lipases for the regioselective acylation of Andrographolide. Each lipase was screened with seven acyl donors. Amano lipase AK from Pseudomonas fluorescens was used for the synthesis of two new acylated andrographolide derivatives. Two new compounds, andrographolide-14-propionate and andrographolide-14-caproate were characterized by various spectral studies. These two derivatives showed more antimicrobial activity than andrographolide.
RESUMO
Achieving selective and sensitive carbohydrate-protein interactions (CPIs) using nanotechnology is an intriguing area of research. Here we demonstrate that the different shapes of gold nanoparticles (AuNPs) functionalized with monosaccharides tune the bacterial aggregations. The mechanism of aggregation revealed that the large number of surface interactions of rod shaped mannose-AuNPs with E. coli ORN 178 compared with spherical and star-shaped AuNPs exhibited higher avidity and sensitivity. Moreover, such sensitive binding can be used for effective inhibition of bacterial infection of cells.
Assuntos
Escherichia coli/efeitos dos fármacos , Galactose , Ouro , Manose , Nanopartículas Metálicas , Aderência Bacteriana/efeitos dos fármacos , Escherichia coli/fisiologia , Infecções por Escherichia coli/prevenção & controle , Galactose/química , Galactose/farmacologia , Ouro/química , Ouro/farmacologia , Células HeLa , Humanos , Manose/química , Manose/farmacologia , Nanopartículas Metálicas/química , Nanopartículas Metálicas/ultraestrutura , Microscopia Eletroquímica de VarreduraRESUMO
We describe here the sugar functionalized ß-cyclodextrin-ferrocene glass slides as fully reversible bacterial biosensors under the influence of external adamantane carboxylic acid. The prototype d-mannose - E. coli ORN 178 and l-fucose - P. aeruginosa interactions serve as a model to illustrate the new approach.