Notes

Time-dissociated Pharmacokinetic Pharmacodynamic Type of Cyclosporine between Malaysian Kidney Transplant Recipients.
In this work, we report a novel preparation of selenium nanorods (Se) doped cobalt oxide (Co3O4) nanoflowers encapsulated with graphene oxide (GO) nanocomposite (NC). Se nanorods were successfully decorated on Co3O4 nanoflowers and an increase in electrical conductivity was observed in Se-Co3O4@GO-NC. The as-prepared Se-Co3O4@GO-NC was utilized as an effective nanocomposite for the electrochemical detection of dimetridazole (DMZ) for the first time in the field of electrochemical sensors. Se-Co3O4@GO-NC modified glassy carbon electrode (GCE) which showed an excellent cathodic current response (17.6 μA) at the lower potential at -0.7314 V upon DMZ sensing. With the various optimized conditions, Se-Co3O4@GO-NC based electrochemical sensor displayed a lengthy linear range of 0.02-83.72 μM, limit of detection 3.4 nM and sensitivity of 1.898 μA.μM-1. cm-2 for DMZ detection. In addition, Se-Co3O4@GO-NC revealed fabulous catalytic reduction activity for DMZ, when compared to GO and Se-Co3O4 modified GCE. Additionally, Se-Co3O4@GO-NC is applied in real sample analysis of pigeon egg, milk and pigeon meat. The results illustrated that Se-Co3O4@GO-NC can be a promising nanocomposite for the electrocatalytic reduction of DMZ in clinical samples in biomedical field.Nanozyme, a kind of nanomaterials with enzymatic activity, has been developing vigorously over the past years owing to its advantages such as low-cost, easy storage, ease of use in harsh environments and so on, compared with natural enzymes. At present, as a typical two-dimensional nanomaterial, molybdenum disulfide (MoS2) and their hybrids with unexpected enzyme-like activities have caused wide attention. In this review, we mainly investigated the enzyme-like activities of MoS2 based nanomaterials, including peroxidase-like activity, catalase-like activity and superoxide dismutase-like activity. Furthermore, we systematically introduce recent research progress of MoS2 based nanomaterials in the fields of biological applications such as radiation protection, cancer therapy, antibacterial, and wound healing. Finally, the current challenges and perspectives of MoS2 based nanomaterials in the future are also discussed and proposed. We expect this review may be significant to understand the properties of MoS2 based nanomaterials and the development of two-dimensional nanomaterials with enzyme mimicking activities.Injectable thermosensitive hydrogel has been regarded as attractive drug delivery system, which displays a sol-gel phase transition upon injection in response to temperature. Recently, thermosensitive hydrogel has become a matter of importance in cancer therapy, providing high local drug concentration, sustained release characteristics, minimal invasiveness, and low systemic toxicities. Here, we review the extensive application of thermosensitive hydrogel in local cancer therapy, including chemotherapy, photothermal therapy, photodynamic therapy, gene therapy, chemo-photothermal combined therapy, and chemo-/immuno- combined therapy.Natural deep eutectic solvents (NaDESs) are promising green alternatives to conventional solvents widely applied in the extraction of natural products due to their physical and chemical superiorities. NHWD-870 In present study, 22 NaDESs consisted from food grade ingredients were screened in ultrasonic assisted extraction (UAE) of bioactive compounds from safflower. The oral bioavailabilities of hydroxysafflor yellow A (HSYA) and anhydrosafflor yellow B (ASYB) in the extracts were then investigated in SD rats with the help of HPLC-MS technique. The results revealed that l-proline-acetamide (l-Pro-Am) was an effective solvent with the yields of HSYA and ASYB at 32.83 and 8.80 mg/g. Pharmacokinetic studies revealed that the blood level of HSYA and ASYB were significantly higher after oral administration of l-Pro-Am extract than that of aqueous extract. Especially, the relative bioavailabilities (to aqueous extract) of HSYA and ASYB were calculated 183.5% and 429.8%.Lotus root (Nelumbo nucifera G.) is a high economic value crop in the world. In this study, the storage characteristics (color, sensory, texture, and fatty acids) of lotus root ("Elian No.5″) were evaluated at different harvest periods (September 2018, October 2018, November 2018, December 2018, and January 2019). Moreover, the storage characteristics were evaluated after the short- term and long-term storage of lotus root at 4 °C and 20 °C. The hardness of lotus root significantly decreased at both temperatures (4 °C and 20 °C) during the first 3 days of storage. In contrast, the decrease in hardness delayed at 4 °C (beyond 3 days of storage). Further, genes related to hardness at different storage temperatures were identified using the RNA-seq and qRT-PCR. The results of this study provide a reference for lotus root storage and a basis for the molecular breeding of longterm-storable lotus root.Protein modifications in liquid infant formula (IF) have been widely studied, but distinguishing between heat- and storage-induced structural changes remains challenging. A generic liquid IF was subjected to direct or indirect UHT treatment and stored at 40 °C up to 180 days. Colour and pH were monitored and structural changes were characterised by dynamic light scattering, SDS-PAGE and centrifugal field-flow fractionation (FFF) coupled with multi-angle light scattering (MALS) and UV detectors to evaluate whether heat-induced differences would level out during storage. Both direct- and indirect UHT treatment led to structural changes, where the higher heat load of the indirect UHT treatment caused more pronounced changes. Indications were that storage-induced changes in pH, browning and non-reducible cross-links were not dependent on UHT treatment. However, FFF-MALS-UV analysis allowed characterisation of complex aggregates, where structural changes continued to be most pronounced in indirect UHT treated samples, and different storage-induced aggregation behaviour was observed.Nitrite, added to cured meat for its bacteriological and technological properties, is implicated in the formation of nitroso compounds (NOCs), such as nitrosylheme, nitrosamines and nitrosothiols, suspected to have a potential impact on human health. The mechanisms involved in NOC formation are studied in regard with the dose-response relationship of added nitrite and its interaction with ascorbate on NOC formation in a cured and cooked meat model. The impact of a second cooking stage on nitrosation was evaluated. The addition of nitrite in the cured and cooked model promoted heme iron nitrosylation and S-nitrosation but not N-nitrosation. Nitrite reduced lipid oxidation without an additional ascorbate effect. The second cooking sharply increased the nitrosamine content while the presence of ascorbate considerably lowered their levels and protected nitrosothiols from degradation. This study gives new insights on the chemical reactivity of NOCs in a cured meat model.Enzymatic browning is considered a critical factor that adversely decreases the quality of fresh-cut products. Although many individual physical or chemical methods have been explored to control browning, there are few approaches combining these technologies. In the present study, Sonchus oleraceus L. extract (SOLE) and ultrasound treatment efficiently controlled the activities of polyphenol oxidase, peroxidase, phenylalanine ammonia-lyase, lipoxygenase, soluble quinones, and intermediate and advanced products, and a lower malondialdehyde content and higher antioxidant capacity were observed in fresh-cut potato slices. More than 50 phenolics and flavonoids were identified in SOLE by liquid chromatography-tandem mass spectrometry. In conclusion, the combined SOLE and ultrasound treatment could serve as a promising method for attenuating enzymatic browning.In order to improve its aqueous solubility and emulsifying function, zein was partially hydrolyzed by trypsin and conjugated to chitosan oligosaccharide lactate by transglutaminase. Hydrolysis and covalent linkage to chitosan oligosaccharide was confirmed by free amine content, gel electrophoresis, and infrared spectroscopy. Enzymatic glycosylation was optimized at pH 6, 44 °C, and 4 h to bind approximately 95% of the free amines in the hydrolysates to chitosan oligosaccharide. Hydrolysis and conjugation increased solubility of zein by 47.60% and 72.93%. Hydrolysis and conjugation also decreased surface hydrophobicity by more than 20% and more than doubled emulsifying activity index, emulsion stability index, and foaming capacity. This enzymatic modification has potential to be applied to improve functional properties of other prolamins.P38α (which is also named MAPK14) plays a pivotal role in initiating different disease states such as inflammatory disorders, neurodegenerative diseases, cardiovascular cases, and cancer. Inhibitors of p38α can be utilized for treatment of these diseases. In this article, we reviewed the structural and biological characteristics of p38α, its relationship to the fore-mentioned disease states, as well as the recently reported inhibitors and classified them according to their chemical structures. We focused on the articles published in the literature during the last decade (2011-2020).Nitro based DprE1 inhibitors exemplified by benzothiazinones have been reported to elicit potent anti-tubercular activity. Poor PK properties associated with benzothiazinones have inspired the discovery of alternative nitro based DprE1 inhibitors. Quinolone based antibiotics on the other hand have good PK properties. The potent anti-tubercular activity of nitro compounds and the good PK properties of the quinolones have elicited an interest in us to construct a new class of nitro containing compounds around the quinolone scaffold with the aim of identifying novel DprE1 inhibitors with potent anti-tubercular activity. Thus, we report herein the anti-tubercular activity of novel 6-nitroquinolone-3-carboxamide derivatives achieved using less than five cheap synthetic transformations. Among the 23 target compounds evaluated for anti-tubercular activity, 12 were active against Mtb─ exhibiting activity in the range of less then 0.244-31.865 μM. Compound 25 having a molecular weight of 399 Da and ClogP value of 2.7 is the most active (MIC90 less then 0.244 μM) in this series. The SAR analyses suggest that anti-tubercular activity was influenced by substituents at position N-1 (R2) and C-3 (R3) of the quinolone ring. The activity data suggest that the nature of R3 has a stronger influence on the SAR compared to R2; with a fluorobenzyl and chlorobenzyl moiety at R2 being the most favoured when R3 is an aliphatic amine. Docking study confirms that compound 25 binds to the same hydrophobic pocket as does TCA1, and other nitro based DprE1 inhibitors, with its nitro group in close proximity with Cys387 residue.The widespread nature of several viruses is greatly credited to their rapidly altering RNA genomes that enable the infection to persist despite challenges presented by host cells. Within the RNA genome of infections is RNA-dependent RNA polymerase (RdRp), which is an essential enzyme that helps in RNA synthesis by catalysing the RNA template-dependent development of phosphodiester bonds. Therefore, RdRp is an important therapeutic target in RNA virus-caused diseases, including SARS-CoV-2. In this review, we describe the promising RdRp inhibitors that have been launched or are currently in clinical studies for the treatment of RNA virus infections. Structurally, nucleoside inhibitors (NIs) bind to the RdRp protein at the enzyme active site, and nonnucleoside inhibitors (NNIs) bind to the RdRp protein at allosteric sites. By reviewing these inhibitors, more precise guidelines for the development of more promising anti-RNA virus drugs should be set, and due to the current health emergency, they will eventually be used for COVID-19 treatment.
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