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Two series of dimethoxyindanone imbedded novel fluorinated spiropyrrolidine heterocyclic hybrids were synthesized employing two different less explored azomethine ylides and were measured for their efficiency as inhibitors for Alzheimer's disease. Among the spiropyrrolidine heterocyclic hybrids, the indole based fluorinated compound with a methoxy substituent at the meta- position of the aryl ring exhibited the utmost potent AChE and BChE inhibitory activities with an IC 50 of 1.97 ± 0.19 µM and 7.08 ± 0.20 µM respectively. The plausible mechanism of inhibition on ChE receptors was unveiled via molecular docking studies. [ABSTRACT FROM AUTHOR]

A small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sensitive towards compound 1g and it showed dose dependent cytotoxic effect at 48 hrs of incubation. The IC 50 values of compound 1g against HCT116 and JURKAT cell lines are 12.14 ± 1.53 and 10.68 ± 0.68 µM, respectively. Further studies on the determination of mechanism of action of compound 1g discovered that it brought the cell death by inducing Caspase 3 dependent apoptosis and also by arresting the cell cycle at S phase. These studies revealed that compound 1g can be recommended as a potential anti-cancer agent. [ABSTRACT FROM AUTHOR]

Pseudomonas aeruginosa MTCC 4997 capable of degrading phenol was isolated and its immobilization potential in calcium alginate, polyurethane foam, k-carrageenan, polyacrylamid, agarose and hen egg white was investigated. All the immobilized matrices showed faster degradation than free cells in a packed bed reactor. Comparatively polyurethane foam immobilized cells retained 100% phenol degradation recorded up to150 mL/h flow rate followed by 50 mL/h flow rate from alginate and k-carrageenan, respectively. Furthermore, polyurethane foam immobilized cells capable of degrading phenol up to the concentration of 1500 mg/L with in 750 min. Polyurethane foam immobilized non-regenerated and regenerated cells were tested for their phenol degradability up to 150 days. Non-regenerated cells showed 100% efficiency of phenol degradation up to 90 days, while regenerated cells showed significant100% efficiency up to 135 days. [ABSTRACT FROM AUTHOR]

The aim of the current study was to isolate and characterize a strain which could utilize catechol as sole source of carbon and energy. The strain Achromobacter xylosoxidans 15DKVB was isolated from paper and pulp industrial effluent contaminated site of Harihar. In the present study 38 bacterial strains isolated were investigated for their ability to degrade catechol in MBM at different concentrations ranging from 100 mg/L to 2000 mg/L. The taxonomic position of strain 15DKVB was studied by sequencing of 16SrRNA gene with a GenBank accession number HQ448950. The maximum-likelihood algorithm showed that, strain 15DKVB formed a coherent cluster with the clade that comprised type strains of Achromobacter genus. The optimal temperature and pH for biodegradation of catechol by strain 15DKVB were 37 °C and pH 7.5 respectively. Among the carbon and nitrogen sources tested, glucose (83.4%) and yeast extract (99.6%) showed highest catechol degradation. Interestingly the strain 15DKVB was able to degrade catechol completely up to 1600 mg/L within 198 h. Immobilization experiment demonstrated that freely suspended cells could degrade 500 mg/L catechol within 60 h of incubation, whereas, the same cell population in alginate-immobilized flask, amended with 500 mg/L catechol was degraded in 42 h. Our results evidently depict that physicochemical parameters of Harihar industrial effluents does not comply with national standards set by ISI to discharge the effluents into irrigation waters. The isolated strain 15DKVB could be a good alternative for the bioremediation of catechol contaminated paper and pulp industrial effluent water and soil. These findings may open new bioremediation applications for the degradation of catechol. [ABSTRACT FROM AUTHOR]

Abstract: Oxidative stress is believed to contribute to neuronal damage induced by cerebral ischemia/reperfusion (I/R) injury. The present study was undertaken to evaluate the possible cerebroprotective and antioxidant effect of hydroalcoholic extract of Eclipta alba against global cerebral ischemia in the rat. Adult Wistar albino rats were treated with extract of Eclipta alba (250 and 500mg/kg/day, p.o.) for 10 days. The global cerebral ischemia–reperfusion injury was induced by occluding bilateral common carotid arteries (BCCA) for 30min, followed by 4h reperfusion. Quercetin (20mg/kg, i.p.) was used for the reference compound. After that, animals were sacrificed by decapitation, brain was removed, various biochemical estimations, cerebral edema, assessment of cerebral infarct size, and histopathological examinations were carried out. BCCA caused significant depletion in superoxide dismutase (SOD), glutathione peroxidase (GPx), reduced glutathione (GSH), catalase (CAT), glutahione-S-transferase (GST), glutathione ruductase (GR) and significant increase in malondialdehyde (MDA) in brain. Pretreatment with hydroalcoholic extract of Eclipta alba significantly reversed the levels of biochemical parameters and significantly reduced the edema and cerebral infarct size as compared to the ischemic control group. Eclipta alba at higher dose markedly reduced ischemia-induced neuronal loss of the brain. Reduction of cerebral edema, an early symptom of ischemia, is one of the most important remedies for reducing subsequent chronic neural damage in stroke. The results of the study show that Eclipta alba pretreatment ameliorates cerebral ischemia/reperfusion injury and enhances the antioxidant defense against BCCA occlusion induced I/R in rats; so it exhibits cerebroprotective property. HPLC fingerprint of hydroalcoholic extract of Eclipta alba was performed for conforming the coumestan present in the plant extract. [Copyright &y& Elsevier]

A small library of new class of dispiropyrrolidinyl-piperidone tethered indono[1,2- b ]quinoxaline heterocyclic hybrids 7 a – j were synthesized employing multicomponent 1,3-dipolar cycloaddition strategy in [bmim]Br. The azomethine ylide employed is first of its kind and generated in situ from indenoquinoxalinone and l -tryptophan, a combination that has not been employed previously for the in situ generation of azomethine ylides. The synthesized heterocyclic hybrids 7a – j were evaluated for their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, therein compounds 7h and 7j displayed more potent AChE and BChE enzyme inhibition than the standard drug with IC 50 values of 3.22, 2.01, 12.40 and 10.45 mM, respectively. Molecular docking studies have also been investigated for most active compounds that disclosed interesting binding templates to the active site channel of cholinesterase enzyme. [ABSTRACT FROM AUTHOR]

A small library of spirooxindole-pyrrolidine hybrids have been synthesized for the first time in an ionic liquid, [bmim]Br in good to excellent yields employing a new class of non-stabilized azomethine ylides derived from isatin and tyrosine, a combination that has been rarely employed for the in situ generation of azomethine ylides using [3+2] cycloaddition strategy. Following the synthesis and characterization of the spirooxindole-pyrrolidine heterocyclic hybrids, they were tested for their anticancer activity as against the changes in the concentrations and time periods with different in vitro cell cultures containing cancer and non-cancer cells, where the results revealed for a potential therapeutic activity. Further analysis for the mechanism of cell death by the cancer cells indicated for the caspase-dependent apoptotic pathway, specifically mediated by caspase-3. Based on these results, it can be demonstrated that the synthesized spirooxindole-pyrrolidine hybrids may serve as one of the better therapeutic agents used for the treatment of malignant tumors. [ABSTRACT FROM AUTHOR]

Stroke is a major cause of death and disability worldwide. The resulting burden on the society continues to grow, with increase in the incidence of stroke. Oxidative stress has been involved in the pathogenesis of several neurological diseases including acute stroke.Focal and global cerebral ischemia represents diseases that are common in the human population.In recent years much attention is being paid towards the exploration of herbal preparation, antioxidant agents and combination therapies including COX-2 inhibitors in experimental model of stroke.Possible effect of a hydroalcoholic leaf extract of Clerodendron glandulosum Coleb ( C. glandulosum )on oxidant-antioxidant status in ischemia-hypoperfusion injury in the rat forebrain has been investigated.Healthy adult male Wistar albino rats were divided into five groups ( n = 8). Group I was served as Sham control (normal saline 1 ml/kg, orally), group II was served hypoperfusion control (normal saline 1 ml/kg, orally), group III, group IV were served as hydroalcoholic extract treated (200 and 400 mg/kg, orally) and group V was treated with Quercetin (10 mg/kg, orally) for 14 days to assess preventive and curative effects of C. glandulosum . Flavonoid and phenolic compounds exhibit a broad spectrum of biological activity, including antioxidant. C. glandulosum extract (200 and 400 mg/kg, p.o) was administered orally, once daily for a period of 2 weeks after the occlusion of BCCA. After 14th days rats were subjected to behavioral studies. After behavioral studies animals were sacrificed and brain was removed and homogenized. Estimation of Lipid peroxidation (LPO) Myeloperoxidase (MPO), estimation of protein levels and the activities of Superoxide dismutase (SOD), Catalase (CAT), were performed. Infarct size and histopathological changes were observed in treated groups. [ABSTRACT FROM AUTHOR]

Active site of h AChE showing the docked compounds, (6f) and (6i) in the binding pocket of enzyme. A small library of structurally fascinating spiropyrrolidine tethered imidazole heterocylic hybrids has been synthesized regioselectively in good yields employing [bmim]Br mediated 1,3-diplar cycloaddition strategy. The new class of azomethine ylide generated in situ from l -histidine and 11 H -indeno[1,2- b ]quinoxalin-11-one reacts with various substituted β -nitrostyrenes affording the spiropyrrolidine tethered imidazole heterocylic hybrids. Compounds thus synthesized were assessed for their in vitro cholinesterase (ChEs) inhibitory activities, among them compounds possessing 4-methyl and 4-methoxy substituents on the aryl ring showed potent activities with IC 50 values of 2.02 ± 0.05 and 2.05 ± 0.06 μM against AChE and 12.40 ± 0.14 and 11.45 ± 0.28 μM against BChE enzyme, respectively. In addition, the most active compounds were performed for their molecular docking simulation and the results revealed interesting binding templates to the active site channel of cholinesterase enzymes. [ABSTRACT FROM AUTHOR]