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Introduction and Aim: The green-synthesized Manganese nanoparticles (MnNPs) were produced rapidly by treating Manganese ions with an aqueous extract of Hopea ponga leaf. The reaction process was monitored using UV-visible spectroscopy. FTIR spectra of plant extract and MnNPs are illustrated. The aim of the present study is to evaluate in-vitro antioxidant and anticancer activity of aqueous leaf extract of H. ponga and its synthesized MnNPs. Materials and Methods: Herbal extraction was carried out by Soxhlet extraction method with water as a solvent. The antioxidant potential of plant extracts and MnNPs were evaluated by FRAP, H2O2, DPPH and PM assays. The effect of aqueous extract of H. ponga along with its synthesized MnNPs on the viability of non- small cell lung cancer (A549) cells was determined by MTT assay. Results: The synthesized MnNPs showed significant antioxidant activity in all performed assays. The aqueous extract from leaves of H. ponga has strong dose dependent anticancer activity against non-small cell lung cancer cells A549. Conclusion: The newly synthesized MnNPs showed significant antioxidant activity in all performed assays. Further, aqueous extract from leaves of H. ponga have a strong dose dependent anticancer activity against non- small cell lung cancer cells A549.

Objective To evaluate in vitro antioxidant and anti-inflammatory activity of Ximenia americana extracts. Methods Herbal extraction was done by Soxhlet extraction method with increasing polarity of solvents viz., chloroform, ethyl acetate, methanol, ethanol and water. Phytochemical analysis was done using different biochemical tests. Antioxidant potential of plant extracts were analyzed by ferric ion reducing antioxidant power, phosphomolybdenum and 2,2-diphenyl-1-picrylhydrazyl, and anti-inflammatory activity by using protein denaturation in vitro bioassay. Total phenolic content of each extract was also determined to assess their corresponding effect on antioxidant capacity of plant. Results Phytochemical analysis showed that each solvent extract contained broad spectrum of secondary metabolites, phenolic compounds, flavonoids, tannins and glycosides, whereas compared to other solvent extracts, chloroform extract showed negative result for phenolic compounds whereas aqueous extract exhibited the highest phenolic content and the significant antioxidant capacity based on the test performed. Out of all extracts, methanol extract showed high anti-inflammatory activity. Conclusions The present study revealed that different solvent extracts of Ximenia americana leaves contain broad spectrum of bioactive compounds. Results confirm that aqueous extract exhibited high antioxidant activity and methanol extract exhibited high anti-inflammatory activity. Further study requires purification, characterization and structural elucidation of phenolic compounds in both extracts that may help in the development of new phytopharmaceuticals.

Cellulose is the most abundant polymer in plants and the microbial conversion of cellulose is a subject of active research. Currently, cellulase is commonly used in many industrial applications, especially in animal feed, textile, waste water, brewing and wine making. A challenging strategy for the efficient utilization of this renewable resource is to use it as a base material for the production of desired metabolites. This chapter therefore focuses on exploring the cellulase producing bacteria and optimizing the parameters for the enzyme cellulase under varied conditions. Cellulolytic bacteria can be exploited for cellulase production which serves wide applications in industries, pharmaceuticals and further, use of these CDB as bio-inoculants can be incorporated to enhance organic matter decomposition in soil to increase soil fertility and to minimize the fertilizer application. It finds wide applications in reducing the environmental pollution and promote sustainable agriculture.

Objectives: The objective of the study is to evaluate the antioxidant, anti-inflammatory, and neuroprotective potential of Aegiceras corniculatum (L.) Blanco. Materials and Methods: Sequential Soxhlet extraction of titled plant material was carried out. Phytochemical analysis was performed using standard procedures. The total phenolic and flavonoid content was estimated along with in vitro antioxidant property of the extracts which was assessed by ferric ion-reducing power assay, phosphomolybdenum assay, 2,2-diphenyl-2-picrylhydrazyl assay, and hydrogen peroxide scavenging assay. Further, the extracts were assessed for anti-inflammatory property by in vitro protein denaturation assay, whereas neuroprotective activity was performed by pretreatment 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Results: Qualitative phytochemical analysis revealed the presence of alkaloids, phenols, flavonoids, tannins, anthraquinones, glycosides, lignins, and sterols. Quantitative phytochemical analysis revealed that the aqueous extract possessed high phenolic content and methanol extract possessed high flavonoid content when compared to other extracts. All the extracts showed antioxidant activity revealed through different assays. Among all the extracts, methanol extract showed significant anti-inflammatory activity with 85.32 ± 1.63 percentage inhibition of protein degradation. Methanol extract at the concentration of 5 μg showed comparatively significant neuroprotection against trimethyltin (TMT)-induced toxicity with 70.02% SK-S-NH cell survival against 56.30% cell survival TMT-intoxicated group. Conclusion: The leaf extracts of A. corniculatum possess antioxidant, anti-inflammatory, and neuroprotective properties.

This study was conducted to determine if constitutive levels of jasmonic acid (JA) and other octadecanoid compounds were elevated prior to herbivory in a maize genotype with documented resistance to fall armyworm (Spodoptera frugiperda) and other lepidopteran pests. The resistant inbred Mp708 had approximately 3-fold higher levels of jasmonic acid (JA) prior to herbivore feeding than the susceptible inbred Tx601. Constitutive levels of cis-12-oxo-phytodienoic acid (OPDA) also were higher in Mp708 than Tx601. In addition, the constitutive expression of JA-inducible genes, including those in the JA biosynthetic pathway, was higher in Mp708 than Tx601. In response to herbivory, Mp708 generated comparatively higher levels of hydrogen peroxide, and had a greater abundance of NADPH oxidase transcripts before and after caterpillar feeding. Before herbivore feeding, low levels of transcripts encoding the maize insect resistance cysteine protease (Mir1-CP) and the Mir1-CP protein were detected consistently. Thus, Mp708 appears to have a portion of its defense pathway primed, which results in constitutive defenses and the ability to mount a stronger defense when caterpillars attack. Although the molecular mechanisms that regulate the constitutive accumulation of JA in Mp708 are unknown, it might account for its enhanced resistance to lepidopteran pests. This genotype could be valuable in studying the signaling pathways that maize uses to response to insect herbivores.

New antimalarials are urgently needed. We have shown that tetrahydroquinoline (THQ) protein farnesyltransferase (PFT) inhibitors (PFTIs) are effective against the Plasmodium falciparum PFT and are effective at killing P. falciparum in vitro. Previously described THQ PFTIs had limitations of poor oral bioavailability and rapid clearance from the circulation of rodents. In this paper, we validate both the Caco-2 cell permeability model for predicting THQ intestinal absorption and the in vitro liver microsome model for predicting THQ clearance in vivo. Incremental improvements in efficacy, oral absorption, and clearance rate were monitored by in vitro tests; and these tests were followed up with in vivo absorption, distribution, metabolism, and excretion studies. One compound, PB-93, achieved cure when it was given orally to P. berghei- infected rats every 8 h for a total of 72 h. However, PB-93 was rapidly cleared, and dosing every 12 h failed to cure the rats. Thus, the in vivo results corroborate the in vitro pharmacodynamics and demonstrate that 72 h of continuous high-level exposure to PFTIs is necessary to kill plasmodia. The metabolism of PB-93 was demonstrated by a novel technique that relied on double labeling with a radiolabel and heavy isotopes combined with radiometric liquid chromatography and mass spectrometry. The major liver microsome metabolite of PB-93 has the PFT Zn-binding N -methyl-imidazole removed; this metabolite is inactive in blocking PFT function. By solving the X-ray crystal structure of PB-93 bound to rat PFT, a model of PB-93 bound to malarial PFT was constructed. This model suggests areas of the THQ PFTIs that can be modified to retain efficacy and protect the Zn-binding N -methyl-imidazole from dealkylation.

Substituted tetrahydroquinolines (THQs) have been previously identified as inhibitors of mammalian protein farnesyltransferase (PFT). Previously we showed that blocking PFT in the malaria parasite led to cell death and that THQ-based inhibitors are the most potent among several structural classes of PFT inhibitors (PFTIs). We have prepared 266 THQ-based PFTIs and discovered several compounds that inhibit the malarial enzyme in the sub- to low-nanomolar range and that block the growth of the parasite (P. falciparum) in the low-nanomolar range. This body of structure–activity data can be rationalized in most cases by consideration of the X-ray structure of one of the THQs bound to mammalian PFT together with a homology structural model of the malarial enzyme. The results of this study provide the basis for selection of antimalarial PFTIs for further evaluation in preclinical drug discovery assays.

A simple one-pot procedure has been developed for the selective etherification of aryl silyl ethers in aryl, alkyl bis-silyl ethers to generate alkyl tert-butyldimethylsilyl-protected aryl alkyl ethers and biaryl ethers in good to excellent yields.

We have developed a high-throughput assay for screening chemical libraries for compounds that affect cell sheet migration during wound closure in epithelial cell monolayers. By using this assay, we have discovered a new inhibitor of cell sheet migration. This compound (UIC-1005) is a 3,4-disubstituted oxazolidinone that bears an electrophilic alpha,beta-unsaturated N-acyl group required for activity. UIC-1005 also inhibits growth in an epithelial cell proliferation assay. The molecule does not display general toxicity at concentrations at which it potently inhibits cell sheet migration and growth. Unlike certain 3,5-disubstituted oxazolidinones, it exhibits no antibacterial activity. UIC-1005 therefore represents a new class of bioactive oxazolidinone derivative that may prove useful as a probe for signaling pathways leading to cell motility.

A pair of complementary methods was developed using CeCl 3 ·7H 2 O/CH 3 CN and LiOH/DMF to selectively deprotect alkyl and aryl silyl ethers, respectively, from the corresponding bis-silyl ethers in excellent yields.

Objective: Evaluating antidiabetic property of Hopea ponga and Vitex leucoxylon extracts by using in vitro assays.Methods: The exhaustive serial extraction was carried out with a series of solvents: chloroform, ethyl acetate, methanol, ethanol and water with increasing polarity using Soxhlet apparatus. The concentrated and dried extracts were evaluated for antidiabetic activity by employing standard in vitro techniques (α-amylase and glucose uptake assay using yeast model in which the effects of extracts on α-amylase and glucose uptake was tested by considering the percentage of inhibition of α-amylase and increase in glucose uptake in yeast cells).Results: In vitro antidiabetic studies show that in case of Hopea ponga methanol extract showed comparable antidiabetic activity with percentage of α-amylase inhibition 51.7925±0.92794 % and with IC50 value 96.53 µg and it was less on comparison with standard i.e. 71.0907±0.67796% with IC50 value 70.33 µg and in case of glucose uptake assay aqueous extract showed higher activity over all remaining extracts with percentage of inhibition 49.8100±0.62476% and with IC50 value 250.95 µg. whereas in case of Vitex leucoxylon aqueous extract exhibited significant activity in both performed assays i. e α-amylase inhibition and glucose uptake assay with percentage 54.6147±0.46397% and 57.1337±0.44201% respectively when compared to other solvent extracts.Conclusion: Results confirm that aqueous extract of Vitex leucoxylon exhibited highest antidiabetic activity among all extracts. Additional studies are needed for purification, characterization and structural elucidation of bioactive compounds from aqueous extract and also confirm its antidiabetic property by in vivo studies. The present study provides scientific evidence that the leaves of Hopea ponga and Vitex leucoxylon possess anti-diabetic efficacy. Thus, considering its relative antidiabetic potency, these extracts are the useful therapeutic agents for treating and management of diabetes.

Mitochondrial dysfunction and synaptic damage are important features of Alzheimer's disease (AD) associated with amyloid β (Aβ) and tau. We reported previously that the scaffolding protein RanBP9, which is overall increased in brains of patients with AD and in mutant APP transgenic mice, simultaneously promotes Aβ generation and focal adhesion disruption by accelerating the endocytosis of APP and β1-integrin, respectively. Moreover, RanBP9 induces neurodegeneration in vitro and in vivo and mediates Aβ-induced neurotoxicity. Here we show in primary hippocampal neurons that RanBP9 potentiates Aβ-induced reactive oxygen species (ROS) overproduction, apoptosis, and calcium deregulation. Analyses of calcium-handling measures demonstrate that RanBP9 selectively delays the clearance of cytosolic Ca2+ mediated by the mitochondrial calcium uniporter through a process involving the translocation of cofilin into mitochondria and oxidative mechanisms. Further, RanBP9 retards the anterograde axonal transport of mitochondria in primary neurons and decreases synaptic mitochondrial activity in brain. These data indicate that RanBP9, cofilin, and Aβ mimic and potentiate each other to produce mitochondrial dysfunction, ROS overproduction, and calcium deregulation, which leads to neurodegenerative changes reminiscent of those seen in AD.—Roh. S.-E., Woo, J. A., Lakshmana, M. K., Uhlar, C., Ankala, V., Boggess, T., Liu, T., Hong, Y.-H., Mook-Jung, I., Kim, S. J., Kang, D. E. Mitochondrial dysfunction and calcium deregulation by the RanBP9-cofilin pathway.

Many studies have documented the induction of belowground defenses in plants in response to aboveground herbivory and vice versa, but the genes and signaling molecules mediating systemic induction are not well understood. We performed comparative microarray analysis on maize whorl and root tissues from the insect resistant inbred Mp708 in response to foliar feeding by fall armyworm (Spodoptera frugiperda) caterpillars. Although Mp708 has elevated jasmonic acid (JA) levels prior to herbivory, genes involved in JA biosynthesis were up-regulated in whorls in response to fall armyworm feeding. Alternatively, genes possibly involved in regulating ethylene (ET) perception and signaling were up-regulated in roots following foliar herbivory. Transcript levels of genes encoding proteins involved in direct defenses against herbivores were enhanced both in roots and leaves, but transcriptional factors and genes involved in various biosynthetic pathways were selectively down-regulated in the whorl. The results indicate that foliar herbivory by fall armyworm changes root gene expression pathways suggesting profound long distance signaling. Tissue specific induction and suppression of JA and ET signaling pathway genes provides a clue to their possible roles in signaling between the two distant tissue types that eventually triggers defense responses in the roots in response to foliar herbivory.

A pair of complementary methods was developed using CeCl 3 ·7H 2 O/CH 3 CN and LiOH/DMF to selectively deprotect alkyl and aryl silyl ethers, respectively, from the corresponding bis-silyl ethers in excellent yields.

In plants, ethylene and jasmonate control the defense responses to multiple stressors, including insect predation. Among the defense proteins known to be regulated by ethylene is maize insect resistance 1-cysteine protease (Mir1-CP). This protein is constitutively expressed in the insect-resistant maize (Zea mays) genotype Mp708; however, its abundance significantly increases during fall armyworm (Spodoptera frugiperda) herbivory. Within 1 h of herbivory by fall armyworm, Mir1-CP accumulates at the feeding site and continues to increase in abundance until 24 h without any increase in its transcript (mir1) levels. To resolve this discrepancy and elucidate the role of ethylene and jasmonate in the signaling of Mir1-CP expression, the effects of phytohormone biosynthesis and perception inhibitors on Mir1-CP expression were tested. Immunoblot analysis of Mir1-CP accumulation and quantitative reverse-transcriptase polymerase chain reaction examination of mir1 levels in these treated plants demonstrate that Mir1-CP accumulation is regulated by both transcript abundance and protein expression levels. The results also suggest that jasmonate functions upstream of ethylene in the Mir1-CP expression pathway, allowing for both low-level constitutive expression and a two-stage defensive response, an immediate response involving Mir1-CP accumulation and a delayed response inducing mir1 transcript expression.

A simple one-pot procedure has been developed for the selective etherification of aryl silyl ethers in aryl, alkyl bis-silyl ethers to generate alkyl tert-butyldimethylsilyl-protected aryl alkyl ethers and biaryl ethers in good to excellent yields.