Synthesis,Characterization, Molecular Docking,and Anticancer Evaluation of 4‐Thiazolidinone Analogues

Scaffolds containing one or more heteroatoms are ubiquitous in nature and are responsible for almost every biological processes in flora and fauna. The fact that heterocyclic cores have high propensity for biological targets, several nitrogen, oxygen, and sulfur‐containing heterocyclic compounds have been reported in the last few decades. One such intriguing class is 4‐thiazolidinone that exhibit diverse range of pharmacological activities. In the present study, we report synthesis, characterization, molecular docking, and anticancer evaluation of 10 new 4‐thiazolidinone analogues ( 5 – 14 ). One of the compounds ( 11 ) was structurally characterized using single crystal X structure. Anticancer evaluation against hepatocellular carcinoma cell line (HepG2) revealed that compound ( 7 ) was the most potent (IC₅₀ = 75 μM) while other showed moderate to low activity (85–530 μM). To underpin the druggability and possible modes of action, drug‐likeness was determined and docking studies were carried out against β‐carbonic anhydrase receptor (PDB ID: 3IA). Attempts have also been made to establish a structure–activity relationship of the reported compounds.     

Novel pressure and displacement sensors based on carbon nanotubes

We report newly designed pressure and displacement capacitive sensors based on a flexible paper–CNT structure.The carbon nanotube(CNT)powder was deposited on a thin paper substrate and was pressed at an elevated temperature.The sheet resistance of the paper–CNT films was in the range of 2–4 kΩ/cm2.The paper–CNT films were used to fabricate pressure and displacement sensors.The sensitivities of the pressure and the displacement sensors were found to be17.3 p F·m2/k N and 0.93 10-3p F/μm,respectively.The experimental results were compared with the simulated data and they found good agreement with each other.     

New ceramides from Platytaenia multicaule

Phytochemical investigation of Platytaenia multicaule resulted in the isolation of two new ceramides, N-triacontylpentadecanamide and 1,3,4-trihydroxy-2,dodecanoylamino-(24E)-unacotenene, along with two known compounds, beta-sitosterol and beta-sitosterol glycoside. The structure elucidation of the isolated compounds was based primarily on 1D and 2D NMR analyses, including COSY, NOESY, HMQC, and HMBC correlations.     

Effects of sludge retention time on membrane fouling and microbial community structure in a membrane bioreactor

In this study, the effect of sludge retention time (SRT) on membrane bio-fouling was investigated in a membrane bioreactor (MBR) equipped with a sequential anoxic/anaerobic reactor. Specific cake resistance (α), trans-membrane pressure (TMP), mixed liquor suspended solids (MLSS), particle sizes, extracellular polymer substances bound in sludge (bound-EPS) and their correlations with membrane bio-fouling were studied at different SRTs. As SRT decreased to 20 days, the bound-EPS per unit of biomass increased, and consequently, the value of α increased, which resulted in the rise of TMP. However, the reduction of the bound-EPS content was relatively small as compared to a significant decrease in the value of α at longer SRTs (above 60 days). These observations suggest that colloidal particles significantly contribute to membrane bio-fouling. In addition, the diversity of the microbial community structure of activated sludge in the MBRs was observed using the respiratory quinone profile. The ubiquinone species containing UQ-8, belonging to the class β-Proteobacteria type were the major constituents of the microbial community structure. The mole fraction of menaquinone MK-6, -7 and -8(H2) increased as SRT increased. Thus, the results of this study indicate that growth of microorganisms belonging to the δ- and ?-subclass of Proteobacteria as well as the members of the Cytophaga–Flavobacterium cluster increased at longer SRTs.     

Neuroprotective Effects of Green Tea Seed Isolated Saponin Due to the Amelioration of Tauopathy and Alleviation of Neuroinflammation: A Therapeutic Approach to Alzheimer’s Disease

Tauopathy is one of the major causes of neurodegenerative disorders and diseases such as Alzheimer’s disease (AD). Hyperphosphorylation of tau proteins by various kinases leads to the formation of PHF and NFT and eventually results in tauopathy and AD; similarly, neuroinflammation also exaggerates and accelerates neuropathy and neurodegeneration. Natural products with anti-tauopathy and anti-neuroinflammatory effects are highly recommended as safe and feasible ways of preventing and /or treating neurodegenerative diseases, including AD. In the present study, we isolated theasaponin E1 from ethanol extract of green tea seed and evaluated its therapeutic inhibitory effects on tau hyper-phosphorylation and neuroinflammation in neuroblastoma (SHY-5Y) and glioblastoma (HTB2) cells, respectively, to elucidate the mechanism of the inhibitory effects. The expression of tau-generating and phosphorylation-promoting genes under the effects of theasaponin E1 were determined and assessed by RT- PCR, ELISA, and western blotting. It was found that theasaponin E1 reduced hyperphosphorylation of tau and Aβ concentrations significantly, and dose-dependently, by suppressing the expression of GSK3 β, CDK5, CAMII, MAPK, EPOE4(E4), and PICALM, and enhanced the expression of PP1, PP2A, and TREM2. According to the ELISA and western blotting results, the levels of APP, Aβ, and p-tau were reduced by treatment with theasaponin E1. Moreover, theasaponin E1 reduced inflammation by suppressing the Nf-kB pathway and dose-dependently reducing the levels of inflammatory cytokines such as IL-1beta, IL-6, and TNF-alpha etc.     

Heat conduction in a semi-infinite solid when subjected to spatially decaying instantaneous laser source

A closed-form model for the computation of temperature and heat flux distribution in a semi-infinite solid when subjected to spatially decaying, instantaneous laser source is investigated. The appropriate dimensionless parameters are identified and the reduced temperature and heat flux as a function of these parameters are presented in the graphic form. Some special cases of practical interest are also discussed. It is demonstrated that the present analysis covers the classical case of no heat generation in the solid as well as some new solutions.

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Wärmeleitung in einem halbunendlichen Körper, der plötzlich durch eine mit zunehmender Eindringtiefe abklingende Laser-Wärmequelle beaufschlagt wird

Zusammenfassung Es wird ein geschlossenes Rechenmodell zur Ermittlung der Temperatur- und Wärmeflußverteilung in einem halbunendlichen Körper untersucht, der plötzlich durch eine mit der Eindringtiefe abklingende Laserquelle beaufschlagt wird. Die normierten Temperaturen und Wärmeflüsse sind als Funktionen relevanter Kenngrößen graphisch dargestellt. Spezialfälle von praktischem Interesse werden diskutiert. Die vorliegende Untersuchung liefert neben einigen neuen Lösungen auch das Ergebnis für den klassischen Fall, daß keine Wärmequellen wirksam sind.

     

Lipoxygenase inhibiting ethyl substituted glycoside from Symplocos racemosa

Phytochemical investigation of Symplocos racemosa resulted in the isolation of a new ethyl substituted glycoside, 1-ethyl brachiose-3'-acetate (1) along with four known compounds ketochaulmoogric acid (2), nonaeicosanol (3), triacontyl palmitate (4) and methyl triacontanoate (5). The substitution of ethyl group on 1 was natural because during the course of extraction and purification ethanol was not used. The structural elucidation of the isolated compounds was based primarily on 1D- and 2D-NMR analysis, including COSY, HMQC, and HMBC correlations. The glycoside 1 and triacontyl palmitate (4) displayed the inhibitory potential against lipoxygenase and urease enzyme, respectively.     

Large and high subgroup

It is proved that a high subgroup of a large subgroup is closed in a high subgroup of the group itself. Also a necessary and sufficient condition for a subgroup to be a pureabsolute summand is obtained.