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In this study, the dynamic stability of soil slopes was analysed using the finite element method (FEM). The analysis was performed using the Plaxis 2D software, which is a popular FEM software package. The study aimed to investigate the behaviour of soil slopes under dynamic loading conditions and to evaluate the accuracy and effectiveness of the FEM approach for predicting slope stability. A 2D slope model was created using Plaxis 2D, and dynamic analyses were performed under different loading conditions. A Shake Table was used for simulating the loading conditions at different frequencies and amplitude. The results of the analysis showed that the slope stability was highly dependent on the dynamic loading conditions and the soil properties. Under earthquake like ground motions which were simulated with the help of shake table under controlled environment, the slope experienced significant deformations and displacements. The deformations were calculated in the form of crest settlement and toe settlement. The study also evaluated the accuracy of the FEM approach by comparing the simulation results with the experimental data. The comparison showed that the FEM approach provided a good prediction of the slope behaviour under dynamic loading conditions and could be used as a reliable tool for analysing slope stability. Overall, the study demonstrated the effectiveness of the FEM approach for analysing the dynamic stability of soil slopes and highlighted the importance of considering dynamic loading conditions in slope stability analysis. The study also provided insights into the behaviour of soil slopes under different loading conditions and could be useful for designing safer and more stable slopes in practice.

Intracellular trafficking is essential to maintain the plasma membrane-cell wall interface, a site where environmental stimuli such as limited water availability can be perceived. However, the identity of plant trafficking regulators, and their relationship to drought resistance, is unclear. An amino acid substitution in the Non-Phototrophic Hypocotyl3 (NPH3) domain of NPH3/RPT2-Like5 (NRL5)/Naked Pins in Yucca8 (NPY8) causes extreme drought sensitivity due to mis-regulated proline metabolism. This NPH3-domain mutation inhibits NRL5 GTPase activity, disrupts interaction with RAB small GTPases and the SNARE proteins VAMP721/722, and diminishes NRL5 polar localization. Our finding that the NPH3 domain is plant specific type of GTPase participating in intracellular trafficking provides a basis to understand NPH3-domain function in diverse processes including abiotic stress resistance, hormone signaling and maintenance of cellular polarity.One-Sentence SummaryGTP association and trafficking interaction of the NPH3 domain is essential for NRL5 function in drought resistance.

In this study, a comparative efficacy of Cananga odorata EO (CoEO) and its nanoencapsulated formulation into chitosan nanoemulsion (CoEO-CsNe) against a toxigenic strain of Aspergillus flavus (AF-M-K5) were investigated for the first time in order to determine its efficacy in preservation of stored food from fungal, aflatoxin B1 (AFB1) contamination and lipid peroxidation. GC and GC–MS analysis of CoEO revealed the presence of linalool (24.56%) and benzyl acetate (22.43%) as the major components. CoEO was encapsulated into chitosan nanoemulsion (CsNe) through ionic-gelation technique and characterized by High Resolution-Scanning Electron Microscopy (HR-SEM), Fourier Transform Infrared spectroscopy (FTIR), and X-Ray Diffraction (XRD) analysis. The CoEO-CsNe during in vitro investigation against A. flavus completely inhibited the growth and AFB1 production at 1.0 μL/mL and 0.75 μL/mL, respectively. Additionally, CoEO-CsNe showed improved antioxidant activity against DPPH• and ABTS•+ with IC50 value 0.93 and 0.72 μL/mL, respectively. Further, CoEO-CsNe suppressed fungal growth, AFB1 secretion and lipid peroxidation in Arachis hypogea L. during in situ investigation without causing any adverse effect on seed germination. Overall results demonstrated that the CoEO-CsNe has potential of being utilized as a suitable plant based antifungal agent to improve the shelf-life of stored food against AFB1 and lipid peroxidation mediated biodeterioration.

In anticancer drug discovery, multi-targeting compounds have been beneficial due to their advantages over single-targeting compounds. For instance, VEGFR-2 has a crucial role in angiogenesis and cancer management, whereas HDACs are well-known regulators of epigenetics and have been known to contribute significantly to angiogenesis and carcinogenesis. Herein, we have reported nineteen novel VEGFR-2 and HDAC dual-targeting analogs containing diaryl-pyrazoline thiazolidinediones and their in vitro and in vivo biological evaluation. In particular, the most promising compound 14c has emerged as a dual inhibitor of VEGFR-2 and HDAC. It demonstrated anti-angiogenic activity by inhibiting in vitro HUVEC proliferation, migration, and tube formation. Moreover, an in vivo CAM assay showed that 14c repressed new capillary formation in CAMs. In particular, 14c exhibited cytotoxicity potential on different cancer cell lines such as MCF-7, K562, A549, and HT-29. Additionally, 14c demonstrated significant potency and selectivity against HDAC4 in the sub-micromolar range. To materialize the hypothesis, we also performed molecular docking on the crystal structures of both VEGFR-2 (PDB ID: 1YWN) and HDAC4 (PDB-ID: 4CBY), which corroborated the designing and biological activity. The results indicated that compound 14c could be a potential lead to develop more optimized multi-target analogs with enhanced potency and selectivity.

Fibromyxoma is a benign, painless, and locally destructive tumor is quite a rare finding of oral cavity. The etiology of tumor is unknown, but mandible has been found to be more commonly involved than maxilla. Moreover, its limited occurrence to the teeth bearing areas and occasional presence of odontogenic epithelial fragments within the tumor is suggestive of odontogenic origin. It’s histological and radiological features makes a fibromyxoma difficult to differentiate from other odontogenic tumor leading to its misinterpretation as malignant lesion and therefore we here present a rare case of fibromyxoma of maxilla describing its clinical and radiological aspects with its post-operative follow up.

Thiazolidinedione (TZD), being a privileged scaffold, has been known as a significant structural moiety of antidiabetic drugs. TZD has been known to improve glycaemic control in type 2 diabetes mellitus (T2DM) by increasing insulin sensitivity in the body. A novel series of 5-benzylidene 2,4-thiazolidinedione derivatives were designed, synthesized (V1-V28), and structurally confirmed by different spectroscopic techniques such as FTIR

Nitric oxide (NO) is an essential redox-signaling molecule free radical, contributes a significant role in a diverse range of physiological processes. Photo-triggered NO donors have significant potential compared to other NO donors because it releases NO in the presence of light. Hence, an efficient visible light-triggered NO donor is designed and synthesized by coupling 2,6-dimethyl nitrobenzene moiety at the peri-position of 1, 8-naphthalimide. The NO-releasing ability is validated using various spectroscopic techniques, the photoproduct is characterized, and finally, the NO generation quantum yield is also determined. Furthermore, the photo-generated NO has been employed to Arabidopsis thaliana as a model plant to examine the effect of photoreceptor-mediated NO uptake on plant root growth regulation molecule.

The present study reports the formulation of Apium graveolens essential oil (AGEO) with its major components linalyl acetate (LA) and geranyl acetate (GA) (1:1:1) as a novel green preservative for protection of postharvest food commodities from fungal infestations, aflatoxin B1 (AFB1) secretion, free radical generation and lipid peroxidation. The essential oil based novel formulation displayed considerable inhibitory action against fourteen food borne molds responsible for deterioration of stored food commodities, in addition to the most toxigenic strain of Aspergillus flavus (AFLHPR14) isolated from fungal and aflatoxin contaminated rice seeds. The observed higher efficacy of designed formulation was due to the synergistic action of essential oil and its major components. Fungal plasma membrane was recorded as the possible target site of antifungal action of the formulation as revealed through reduction in membrane ergosterol content, increased intracellular propidium iodide (PI) fluorescence and enhanced leakage of cellular ions (sodium, potassium, calcium) and 260, 280 nm absorbing materials. Further, inhibition of methylglyoxal (an aflatoxin inducer) confirmed the aflatoxin inhibitory potential of novel formulation based on essential oil and its major components. High antioxidant potential as observed through DPPH and ABTS·+ radical scavenging assay, improved phenolic content, considerable inhibition of lipid peroxidation in stored rice seeds, in situ efficacy on AFB1 inhibition in food system under storage container system, acceptable sensorial characteristics and favorable safety profile during animal trials suggest the recommendation of the designed formulation for large scale application as green preservative by food and agriculture based industries against fungal and aflatoxin contamination of stored commodities.

As sessile organisms, plants constantly monitor environmental cues and respond appropriately to modulate their growth and development. Membrane transporters act as gatekeepers of the cell regulating both the inflow of useful materials as well as exudation of harmful substances. Members of the multidrug and toxic compound extrusion (MATE) family of transporters are ubiquitously present in almost all forms of life including prokaryotes and eukaryotes. In bacteria, MATE proteins were originally characterized as efflux transporters conferring drug resistance. There are 58 MATE transporters in Arabidopsis thaliana, which are also known as DETOXIFICATION (DTX) proteins. In plants, these integral membrane proteins are involved in a diverse array of functions, encompassing secondary metabolite transport, xenobiotic detoxification, aluminium tolerance, and disease resistance. MATE proteins also regulate overall plant development by controlling phytohormone transport, tip growth processes, and senescence. While most of the functional characterizations of MATE proteins have been reported in Arabidopsis, recent reports suggest that their diverse roles extend to numerous other plant species. The wide array of functions exhibited by MATE proteins highlight their multitasking ability. In this review, we integrate information related to structure and functions of MATE transporters in plants. Since these transporters are central to mechanisms that allow plants to adapt to abiotic and biotic stresses, their study can potentially contribute to improving stress tolerance under changing climatic conditions.

Microbes are the biggest shareholder for the quantitative and qualitative deterioration of food commodities at different stages of production, transportation, and storage, along with the secretion of toxic secondary metabolites. Indiscriminate application of synthetic preservatives may develop resistance in microbial strains and associated complications in human health with broad-spectrum environmental non-sustainability. The application of essential oils (EOs) as a natural antimicrobial and their efficacy for the preservation of foods has been of present interest and growing consumer demand in the current generation. However, the loss in bioactivity of EOs from fluctuating environmental conditions is a major limitation during their practical application, which could be overcome by encapsulating them in a suitable biodegradable and biocompatible polymer matrix with enhancement to their efficacy and stability. Among different nanoencapsulated systems, nanoemulsions effectively contribute to the practical applications of EOs by expanding their dispersibility and foster their controlled delivery in food systems. In line with the above background, this review aims to present the practical application of nanoemulsions (a) by addressing their direct and indirect (EO nanoemulsion coating leading to active packaging) consistent support in a real food system, (b) biochemical actions related to antimicrobial mechanisms, (c) effectiveness of nanoemulsion as bio-nanosensor with large scale practical applicability, (d) critical evaluation of toxicity, safety, and regulatory issues, and (e) market demand of nanoemulsion in pharmaceuticals and nutraceuticals along with the current challenges and future opportunities.

Monotargeting anticancer agents suffer from resistance and target nonspecificity concerns, which can be tackled with a multitargeting approach. The combined treatment with HDAC inhibitors and PPARγ agonists has displayed potential antitumor effects. Based on these observations, this work involves design and synthesis of molecules that can simultaneously target PPARγ and HDAC. Several out of 25 compounds inhibited HDAC4, and six compounds acted as dual-targeting agents. Compound

Present study deals with the efficacy of nanoencapsulated Homalomena aromatica essential oil (HAEO) as a potent green preservative against toxigenic Aspergillus flavus strain (AF-LHP-NS 7), AFB1 and free radical mediated deterioration of stored spices. GC-MS analysis revealed linalool (68.51%) as the major component of HAEO. HAEO was encapsulated into chitosan nanomatrix (CS-HAEO-Ne) and characterized through SEM, FTIR and XRD. CS-HAEO-Ne completely inhibited A. flavus growth and AFB1 biosynthesis at 1.25 µL/mL and 1.0 µL/mL, respectively in comparison to unencapsulated HAEO (1.75 µL/mL and 1.25 µL/mL respectively). CS-HAEO-Ne exhibited superior antioxidant efficacy (IC50 (DPPH) = 4.5 µL/mL) over unencapsulated HAEO (IC50 (DPPH) = 15.9 µL/mL). Further, CS-HAEO-Ne caused significant reduction in ergosterol content in treated A. flavus and provoked leakage of cellular ions (Ca+ 2, Mg+ 2 and K+) as well as 260 nm and 280 nm absorbing materials. Depletion of methylglyoxal level in treated A. flavus cells deals with the novel antiaflatoxigenic efficacy of CS-HAEO-Ne. CS-HAEO-Ne depicted excellent in situ efficacy by inhibiting mold attack and AFB1 contamination, mineral preservation and acceptable sensorial profile. Moreover, broad safety paradigm (LD50 value = 8006.84 µL/kg) of CS-HAEO-Ne also suggest it as novel green preservative to enhance shelf life of stored spices.

Present study deals with the efficacy of nanoencapsulated Homalomena aromatica essential oil (HAEO) as a potent green preservative against toxigenic Aspergillus flavus strain (AF-LHP-NS 7), storage fungi, AFB

Twinning is referred to the development of two separate teeth that arose from the complete separation of one tooth bud. The present paper discusses twinning in detail and attempts to differentiate twinning from gemination, fusion and concrescence.

The present investigation reports antifungal and antiaflatoxigenic efficacy of Salvia sclarea essential oil (SSEO) and its combination with Linalyl acetate (LA) (1:1) against herbal drug deteriorating molds and aflatoxin B1 contamination. GC-MS analysis of SSEO showed Linalyl Acetate (LA) (61.33%) and Linalool (LL) (17.59%) as major components. The SSEO and LA combination displayed better antifungal and antiaflatoxigenic activity as compared to SSEO and LA used individually. SSEO and LA combination was effective in reduction of ergosterol and enhanced leakage of vital ions and UV-absorbing materials in a dose dependent manner. The combination caused significant reduction in cellular methylglyoxal content, an aflatoxin inducer suggesting its future application for development of aflatoxin resistant herbal drug varieties through green transgenics. The combination also showed pronounced antioxidant activity as compared to SSEO and LA used separately. Interestingly, the combination showed significant in situ protection of Picrorhiza kurroa rhizomes against mould infestation.

Herbal raw materials get contaminated with different microbes during collection and postharvest processing, causing both quantitative and qualitative damage leading to degradation of active principles. Currently, a wide range of plant products including essential oils have been found efficacious against fungal and mycotoxin contamination of raw materials and have been recommended as green preservatives for postharvest protection of herbal raw materials. Extracts of different higher plants and bioactive constituents, viz., carvone (from Carum carvi), azadirachtin (from Azadirachta indica), and isothiocyanate (from horseradish and brassicaceous plants) have exhibited promising efficacy against microbial contamination. Currently, nanotechnological approach has enhanced the bio-efficacy of phytochemicals through controlled release, site specific delivery, and enhanced stability. The present article throws light on different plant products recommended in postharvest preservation of herbal raw materials and also explains the future technological advancements in their better utilization as preservative of herbal raw materials. Such documentation of pharmacological efficacy of traditionally used plant products would also be helpful in bioprospection of plant diversity against biopiracy.

Monotargeting anticancer agents suffer from resistance and target nonspecificity concerns, which can be tackled with a multitargeting approach. The combined treatment with HDAC inhibitors and PPARγ agonists has displayed potential antitumor effects. Based on these observations, this work involves design and synthesis of molecules that can simultaneously target PPARγ and HDAC. Several out of 25 compounds inhibited HDAC4, and six compounds acted as dual-targeting agents. Compound 7i was the most potent, with activity toward PPARγ EC50 = 0.245 μM and HDAC4 IC50 = 1.1 μM. Additionally, compounds 7c and 7i were cytotoxic to CCRF-CEM cells (CC50 = 2.8 and 9.6 μM, respectively), induced apoptosis, and caused DNA fragmentation. Furthermore, compound 7c modulated the expression of c-Myc, cleaved caspase-3, and caused in vivo tumor regression in CCRF-CEM tumor xenografts. Thus, this study provides a basis for the rational design of dual/multitargeting agents that could be developed further as anticancer therapeutics.

Prostate cancer is a common malignancy in men worldwide. In the initial treatment, ADT has been used as the cornerstone, but unfortunately, mainstream patients transition to the refractory state of prostate cancer, i.e., CRPC. Thus, newer therapeutics are required for the treatment of patients un or less responsive to ADT. Epigenetic aberrations, namely, DNA methylation and histone modifications are the ultimate chauffeurs of prostate cancer with an emerging role to erase the roadmaps to this disease. However, more robust clinical evidence would be indispensable to put forward reliable therapeutics with the scope to effectively combat this disease. In this review, we have described the present status of epigenetic biomarkers and their clinical impacts on prostate cancer. We have also comprehensively deliberated the role of different epigenetic master regulators involved in the management of disease, appropriate treatment landscape, and the recent preclinical and ongoing clinical evaluations in prostate adenocarcinoma.

Recent evidences highlight the usefulness of small molecule (Histone deacetylase 4) HDAC4 inhibitors in the several preclinical paradigms. Major toxicity and mutagenicity issues associated with hydroxamate HDAC inhibitors, stimulated us to develop potent non-hydroxamate inhibitors. In the present work a novel series of thiazolidinedione (TZD) derivatives with pyridine as cyclic linker and TZD ring as zinc binding group was designed and screened in a panel of isoenzymes of HDACs, wherein the most potent compounds exhibiting HDAC4 IC50-values

Thiazolidinedione (TZD) has been an interesting scaffold due to its proven antidiabetic activity and encouraging findings in anticancer drug discovery. We synthesised benzylidene thiazolidinedione derivatives which exhibited excellent antiproliferative effects in chronic myeloid leukemic cells K562 and the most active compounds 3t and 3x had GI50 value of 0.9 and 0.23 µM respectively. Both the compound was found to arrest the growth of K562 cells in G0/G1 phase in a time and dose dependent manner. Further, western blot analysis revealed that 3t and 3x could also inhibit the expression of cell proliferation markers, PCNA and Cyclin D1 and compound 3x up-regulated apoptosis markers, cleaved PARP1 and activated caspase 3, which could be a possible mechanism for the excellent antiproliferative effects exhibited by these compounds. In vitro combination studies of 3t and 3x with Imatinib found to potentiate the antitumor effects of Imatinib. Further in vivo efficacy in K562 xenografts, of 3t and 3x alone and in combination with Imatinib was found to be promising and far better than control group and combination treatment was found to be more effective as compared to only Imatinib treated or test compound treated animals. Thus, our findings suggest that these compounds are promising antitumor agents and could help to enhance the anticancer effects of Imatinib and other tyrosine kinase inhibitors, when used in combination.

Cancer cells increase their glucose uptake and glycolytic activity to meet the high energy requirements of proliferation. Glucose transporters (GLUTs), which facilitate the transport of glucose and related hexoses across the cell membrane, play a vital role in tumor cell survival and are overexpressed in various cancers. GLUT1, the most overexpressed GLUT in many cancers, is emerging as a promising anti-cancer target. To develop GLUT1 inhibitors, we rationally designed, synthesized, structurally characterized, and biologically evaluated in-vitro and in-vivo a novel series of furyl-2-methylene thiazolidinediones (TZDs). Among 25 TZDs tested, F18 and F19 inhibited GLUT1 most potently (IC50 11.4 and 14.7 μM, respectively). F18 was equally selective for GLUT4 (IC50 6.8 μM), while F19 was specific for GLUT1 (IC50 152 μM in GLUT4). In-silico ligand docking studies showed that F18 interacted with conserved residues in GLUT1 and GLUT4, while F19 had slightly different interactions with the transporters. In in-vitro antiproliferative screening of leukemic/lymphoid cells, F18 was most lethal to CEM cells (CC50 of 1.7 μM). Flow cytometry analysis indicated that F18 arrested cell cycle growth in the subG0-G1 phase and lead to cell death due to necrosis and apoptosis. Western blot analysis exhibited alterations in cell signaling proteins, consistent with cell growth arrest and death. In-vivo xenograft study in a CEM model showed that F18 impaired tumor growth significantly.

The study reports efficacy of Melissa officinalis L. essential oil (MOEO) as a safe plant-based insecticide against Tribolium castaneum Herbst (TC) by induction of oxidative stress. MOEO nanoencapsulation in chitosan matrix was performed to enhance its bioefficacy. GC–MS analysis of MOEO depicted geranial (31.54%), neral (31.08%), and β-caryophyllene (12.42%) as the major components. MOEO showed excellent insecticidal potential in contact (100% mortality at 0.157 μL/cm2) and fumigant bioassays (LC50 = 0.071 μL/mL air) and 100% repellency at concentration ≤ 0.028 μL/cm2. Increased reactive oxygen species (ROS), superoxide dismutase (SOD), catalase (CAT), and decreased ratio of reduced glutathione (GSH) to oxidized glutathione (GSSG) at the LC50 dose suggested significant oxidative stress on TC in MOEO treatment sets. The encapsulated MOEO exhibited enhanced activity as fumigant (LC50 = 0.048 μL/mL air) and showed significant antifeedant activity in situ (EC50 = 0.043 μL/mL). High LD50 value (13,956.87 μL/kg body weight of mice) confirmed favorable toxicological profile for non-target mammals. The findings depict potential of nanoencapsulated MOEO as an eco-friendly green pesticide against infestation of stored food by TC.

Background: Cancer being a complex disease, single targeting agents remain unsuccessful. This calls for “multiple targeting”, wherein a single drug is so designed that it will modulate the activity of multiple protein targets. Topoisomerase 2 (Top2) helps in removing DNA tangles and super-coiling during cellular replication, Casein Kinase 2 (CK2) is involved in the phosphorylation of a multitude of protein targets. Thus, in the present work, we have tried to develop dual inhibitors of Top2 and CK2. Objective: With this view, in the present work, 2 human proteins, Top2 and CK2 have been targeted to achieve the anti-proliferative effects. Methods: Novel 1-acetylamidoanthraquinone (3a-3y) derivatives were designed, synthesized and their structures were elucidated by analytical and spectral characterization techniques (FTIR, 1H NMR, 13C NMR and Mass Spectroscopy). The synthesized compounds were then subjected to evaluation of cytotoxic potential by the Sulforhodamine B (SRB) protein assay, using HL60 and K562 cell lines. Ten compounds were analyzed for Top2, CK2 enzyme inhibitory potential. Further, top three compounds were subjected to cell cycle analysis. Results: The compounds 3a to 3c, 3e, 3f, 3i to 3p, 3t and 3x showed excellent cytotoxic activity to HL-60 cell line indicating their high anti-proliferative potential in AML. The compounds 3a to 3c, 3e, 3f, 3i to 3p and 3y have shown good to moderate activity on K-562 cell line. Compounds 3e, 3f, 3i, 3x and 3y were found more cytotoxic than standard doxorubicin. In cell cycle analysis, the cells (79-85%) were found to arrest in the G0/G1 phase. Conclusion: We have successfully designed, synthesized, purified and structurally characterized 1- acetylamidoanthraquinone derivatives. Even though our compounds need design optimization to further increase enzyme inhibition, their overall anti-proliferative effects were found to be encouraging.

Masticatories are prone to fungal and mycotoxin contamination during postharvest processing. The plant based preservatives may be recommended as safe alternatives of synthetic chemicals for their proper storage to protect them from fungal and mycotoxins contamination. This review presents an overview on mycoflora and mycotoxins associated with plant masticatories and prospectives of essential oils and their nanoencapsulated formulations as safe plant based preservatives.

The study explores the potential of Cistus ladanifer essential oil (CLEO) as plant based preservative against fungal and aflatoxin B1 contamination of stored oil seeds. Aspergillus flavus AF-M-K5 was identified as the most aflatoxigenic isolate during mycoflora analysis of selected oil seeds. Chemical characterization of CLEO through GC-MS revealed α-asarone (78.841%) as the major component. The minimum inhibitory concentration and minimum aflatoxin inhibitory concentration of CLEO against A. flavus AF-M-K5 were recorded to be 0.6, and 0.5 μL/mL, respectively. Significant reduction in ergosterol content and enhancement of leakage of Ca2+, K+ and Mg2+ ions from treated fungal cells emphasized fungal plasma membrane as the site for antifungal action of CLEO. The CLEO caused reduction of methylglyoxal, the aflatoxin inducing substrate. This is the first report on an essential oil as methylglyoxal inhibitor suggesting a novel mode of action in reduction of AFB1 biosynthesis. The IC50 values for CLEO as determined by DPPH• and ABTS•+ assay were 7.3 μL/mL and 1.13 μL/mL respectively, depicting remarkable antioxidant activity. CLEO caused considerable protection of stored oil seeds from contamination of A. flavus (90.6%) and from storage molds (78.03%) without affecting seed germination.

The present communication is on a rediscovery of an endemic moth Gurna indica (Moore, 1879) from India. This species is rediscovered from India after more than 125 years. Till this study, the literature published on this species is based on the type species housed in museum or based on the catalogues. The genus Gurna is a monotypic and endemic to India.

Thiazolidinedione (TZD) containing derivatives have been proved to be promising anticancer agents in preclinical and clinical evaluation phases. Hybrid molecules not just offer the benefits such as enhanced therapeutic effects and improved specificity, but in addition could beat drug resistance, so hybridization of thiazolidinedione scaffold with other anticancer pharmacophoric scaffolds may constitute a hopeful strategy to develop newer and more efficacious anticancer agents. Based on this approach, in past decade, several such hybrids containing TZD scaffold have been reported and evaluated for their antitumor activity, and some of them revealed excellent in vitro potency, indicating their potential as presumed anticancer drugs. This review summarizes the recent advances of TZD hybrids as potential anticancer agents, highlighting their antitumor activity and possible mechanism of action. Structure‐activity relationship (SAR) studies will also be discussed to direct the rational molecular hybridization of TZD scaffolds to design more effective candidates.

The article presents the potential of essential oils (EOs) as plant based pesticides against Tribolium castaneum (Herbst) (red flour beetle), a cosmopolitan secondary insect pest of stored ...

Staphylococcus aureus is closely associated with food poisoning incidences, more, because of intoxication due to contamination of food with its enterotoxins. Staphylococcus enterotoxin A (SEA) is highly resistant to heat and other food processing conditions and has been implicated in food borne diseases from dairy products. Here we describe a rapid, gold nanoparticle based lateral flow immunoassay (LFIA) for detecting SEA in milk. Assay is in sandwich format and uses two specific monoclonal antibodies against SEA, one of which is labeled with gold nanoparticles and other is immobilized at control line. We also demonstrate the effect of using a combination of additives in capture antibody in order to enhance assay sensitivity. The developed LFIA is specific and has a lower detection limit of 0.5 μg/ml. LFIA is tested both on spiked buffer and milk samples and display good reproducibility. The assembled strips stable for a month at 4 °C. The method may be suitable for testing SEA in milk samples as it is quick, easy to perform and reproducible.

In the present study, two novel series of compounds incorporating naphthyl and pyridyl linker were synthesized and biological assays revealed 5-((6-(2-(5-(2-chlorophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy) naphthalene-2-yl)methylene)thiazolidine-2,4-dione (14b) as the most potent dual inhibitors of vascular endothelial growth factors receptor-2 (VEGFR-2) and histone deacetylase 4 (HDAC4). Compounds 13b, 14b, 17f, and 21f were found to stabilize HDAC4; where, pyridyl linker swords were endowed with higher stabilization effects than naphthyl linker. Also, 13b and 14b showed best inhibitory activity on VEGFR-2 as compared to others. Compound 14b was most potent as evident by in-vitro and in-vivo biological assessments. It displayed anti-angiogenic potential by inhibiting endothelial cell proliferation, migration, tube formation and also suppressed new capillary formation in the growing chick chorioallantoic membranes (CAMs). It showed selectivity and potency towards HDAC4 as compared to other HDAC isoforms. Compound 14b (25 mg/kg, i.p.) also indicated exceptional antitumor efficacy on in-vivo animal xenograft model of human colorectal adenocarcinoma (HT-29). The mechanism of action of 14b was also confirmed by western blot.

Biotechnology embraces various physical and chemical phenomena toward advancement of health diagnostics. Toward such advancement, detection of toxins plays an important role. Toxins produce severe health impacts on consumption with high mortality associated in acute cases. The most prominent route of infection and intoxication is through food matrices. Therefore, rapid detection of toxins at low concentrations is the need of modern diagnostics. Lateral flow immunoassays are one of the emergent and popularly used rapid detection technology developed for detecting various kinds of analytes. This review thus focuses on recent advancements in lateral flow immunoassays for detecting different toxins in agricultural food. Appropriate emphasis was given on how the labels, recognition elements, or detection strategy has laid an impact on improvement in immunochromatographic assays for toxins. The paper also discusses the gradual change in sensitivities and specificities of assays in accordance with the method of food processing used. The review concludes with the major challenges faced by this technology and provides an outlook and insight of ideas to improve it in the future.

Tuberculosis (TB) ranks second, next to AIDS making it most formidable disease in the present age. One of the crucial enzymes involved in cell wall synthesis of Mycobacterium tuberculosis, InhA (enoyl acyl carrier protein reductase), one of the crucial enzymes involved in cell wall synthesis of Mycobacterium tuberculosis, has been authenticated as an effective target for anti-mycobacterial drug development. In the current work, novel derivatives of 1,2,4-triazole-5-thione rationally designed, synthesized and spectrally characterized as promising InhA inhibitors. Anti-mycobacterial potential was determined by resazurin microtiter assay using Mtb H37Rv strain. The mechanism of action of these compounds was confirmed by InhA enzyme inhibition studies. 6b, the most active compound of the series displayed MIC of 0.19 µM in resazurin microtiter assay and InhA inhibition with IC50 of 90 nM.