Leafy vegetables are susceptible to drought stress. Amaranthus tricolor vegetables are resistant to abiotic stress, including drought, and are a source of ample natural phytochemicals of interest to the food industry due to their benefits to consumers’ health. Hence, the selected drought-resistant amaranth genotypes were evaluated for phytochemicals and antioxidant activity in an RCBD study with three replicates. The selected drought-resistant amaranth accessions contained ample carbohydrates, protein, moisture, and dietary fiber. We noticed many macroelements and microelements including iron, copper, manganese, zinc, sodium, molybdenum, boron, potassium, calcium, magnesium, phosphorus, and sulfur; adequate phytopigments, including betacyanins, betalains, betaxanthins, carotenoids, and chlorophylls; plentiful bioactive phytochemicals, including ascorbic acid, flavonoids, polyphenols, and beta-carotene; and antioxidant potential in the selected drought-resistant amaranth accessions. The drought-resistant amaranth accessions VA14 and VA16 were proven to have high ascorbic acid, beta-carotene, and polyphenol levels. The drought-resistant accessions VA12 and VA14 had high flavonoid levels. The drought-resistant accessions VA3, VA14, and VA16 had high AC both in regard to both DPPH and ABTS+. These drought-resistant accessions, VA3, VA14, and VA16, can be utilized as high-yielding varieties with antioxidant profiles for purposes of drinks. The correlation study revealed that bioactive phytopigments and phytochemicals of amaranth accessions had good free radical quenching capacity against 2,2′-azino-bis (3-ethylbenzothiazo-6-sulfonic acid) and diphenyl-1-picrylhydrazyl, equivalent to Trolox. It was revealed in the present study that these drought-resistant accessions contain plentiful proximate, nutraceuticals, phytopigments, bioactive phytochemicals, and antioxidant potentiality. Their drought resistance and quenching of ROS offer huge prospects for the promotion of health benefits and the feeding of communities in drought-prone semiarid and arid areas of the globe, especially those deficient in nutraceuticals, phytopigments, and antioxidants.

The development of green technology is creating great interest for researchers towards low-cost and environmentally friendly methods for the synthesis of nanoparticles. Copper oxide nanoparticles (CuO-NPs) attracted many researchers due to their electric, catalytic, optical, textile, photonic, monofluid, and pharmacological activities that depend on the shape and size of the nanoparticles. This investigation aims copper oxide nanoparticles synthesis using Aerva javanica plant leaf extract. Characterization of copper oxide nanoparticles synthesized by green route was performed by three different techniques: X-Ray Diffraction (XRD), Fourier Transform Infrared (FTIR) Spectroscopy, and Scanning Electron Microscopy (SEM). X-ray diffraction (XRD) reveals the crystalline morphology of CuO-NPs and the average crystal size obtained is 15 nm. SEM images showed the spherical nature of the particles and size is lying in the 15–23 nm range. FTIR analysis confirms the functional groups of active components present in the extract which are responsible for reducing and capping agents for the synthesis of CuO-NPs. The synthesized CuO-NPs were studied for their antimicrobial potential against different bacterial as well as fungal pathogens. The results indicated that CuO-NPs show maximum antimicrobial activities against all the selected bacterial and fungal pathogens. Antimicrobial activities of copper oxide nanoparticles were compared with standard drugs Norfloxacin and amphotericin B antibiotics. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of copper oxide nanoparticles were 128 μg/mL against all selected bacterial pathogens. MIC of fungus and minimum fungicidal concentration (MFC) of CuO-NPs were 160 μg/mL. Thus, CuO-NPs can be utilized as a broad-spectrum antimicrobial agent. The cytotoxic activity of the synthesized CuO-NPs suggested that toxicity was negligible at concentrations below 60 μg/mL.

Coriandrum sativum L. seeds are traditionally used to treat diabetes and its complications (inflammation and formation of reactive oxygen species) around the world. The present study investigates the antidiabetic, anti-inflammatory, and antioxidant effects of the polyphenol fraction of Coriandrum sativum seeds (PCS). Diabetic mice were orally administered with PCS (25 and 50 mg/kg b.w.) for 28 days. Oral glucose tolerance (OGTT) was also evaluated along with the anti-inflammatory effect, assessed by measuring paw edema development induced with carrageenan in Wistar rat and the antioxidant activity assessed using two tests (β-carotene discoloration and DPPH). Treatment of diabetic mice with PCS for four weeks managed their high fasting blood glucose levels, improved their overall health, also revealed an excellent antihyperlipidemic activity. The OGTT result showed a potent antihyperglycemic activity, and following the anti-inflammatory and antioxidant effects, the PCS exhibited a perfect activity. LC-MS/MS result revealed the presence of 9 polyphenols. This modest work indicates that the PCS have an important antidiabetic, antihyperglycemic, antihyperlipidemic, anti-inflammatory, and antioxidant effect that can be well established treatment of diabetes and its complications.

Forty-four bicyclo ((aryl) methyl) benzamides, acting as glycine transporter type 1 (GlyT1) inhibitors, are developed using molecular modeling techniques. QSAR models generated by multiple linear and non-linear regressions affirm that the biological inhibitory activity against the schizophrenia disease is strongly and significantly correlated with physicochemical, geometrical and topological descriptors, in particular: Hydrogen bond donor, polarizability, surface tension, stretch and torsion energies and topological diameter. According to in silico ADMET properties, the most active ligands (L6, L9, L30, L31 and L37) are the molecules having the highest probability of penetrating the central nervous system (CNS), but the molecule 32 has the highest probability of being absorbed by the gastrointestinal tract. Molecular docking results indicate that Tyr124, Phe43, Phe325, Asp46, Phe319 and Val120 amino acids are the active sites of the dopamine transporter (DAT) membrane protein, in which the most active ligands can inhibit the glycine transporter type 1 (GlyT1). The results of molecular dynamics (MD) simulation revealed that all five inhibitors remained stable in the active sites of the DAT protein during 100 ns, demonstrating their promising role as candidate drugs for the treatment of schizophrenia.

Tankyrase is part of poly (ADP-ribose) polymerase superfamily required for numerous cellular and molecular processes. Tankyrase inhibition negatively regulates Wnt pathway. Thus, Tankyrase inhibitors have been extensively investigated for the treatment of clinical conditions associated with activated Wnt signaling such as cancer and fibrotic diseases. Moreover, Tankyrase inhibition has been recently reported to upregulate osteogenesis through the accumulation of SH3 domain-binding protein 2, an adaptor protein required for bone metabolism. In this study, we investigated the effect of Tankyrase inhibition in osteoblast differentiation of human skeletal (mesenchymal) stem cells (hMSCs). A Tankyrase inhibitor, XAV-939, identified during a functional library screening of small molecules. Alkaline phosphatase activity and Alizarin red staining were employed as markers for osteoblastic differentiation and in vitro mineralized matrix formation, respectively. Global gene expression profiling was performed using the Agilent microarray platform. XAV-939, a Tankyrase inhibitor, enhanced osteoblast differentiation of hBMSCs as evidenced by increased ALP activity, in vitro mineralized matrix formation, and upregulation of osteoblast-related gene expression. Global gene expression profiling of XAV-939-treated cells identified 847 upregulated and 614 downregulated mRNA transcripts, compared to vehicle-treated control cells. It also points towards possible changes in multiple signaling pathways, including TGFβ, insulin signaling, focal adhesion, estrogen metabolism, oxidative stress, RANK-RANKL (receptor activator of nuclear factor κB ligand) signaling, Vitamin D synthesis, IL6, and cytokines and inflammatory responses. Further bioinformatic analysis, employing Ingenuity Pathway Analysis identified significant enrichment in XAV-939-treated cells of functional categories and networks involved in TNF, NFκB, and STAT signaling. We identified a Tankyrase inhibitor (XAV-939) as a powerful enhancer of osteoblastic differentiation of hBMSC that may be useful as a therapeutic option for treating conditions associated with low bone formation.