Dietary phenols are antioxidants with diverse physiological functions that are beneficial for human health. The objective of this research work was to investigate antioxidant activity of p-coumaric acid (p-CA) using four in vitro methods, the protective effects against oxidative stress in PC12 cells, and hypolipidemic effects on High fat-diet (HFD) mice model. The p-CA exhibited moderate antioxidant activity in the selected in vitro assay. The highest chelating activity of p-CA at 50 μg/mL was found to be 52.22%. Pretreatment with p-CA significantly enhanced cell viability of PC12 cell and suppressed AAPH-induced intracellular ROS generation and AAPH-induced LDH release. The hypolipidemic effects of p-CA (100 mg/kg BW) was directly linked to the increased expression of nuclear factor erythroid 2-related factor (Nrf2) by 2.0-fold, Glutathione peroxidase (Gpx) by 3.8-fold, Superoxide dismutase (SOD-1) by 1.6-fold, Heme oxygenase (HO-1) by 1.72-fold and NAD(P)H Quinone Dehydrogenase 1 (NQO-1) by 1.5-fold compared with HFD group. In addition to these effects, p-CA decreased total cholesterol and atherosclerosis index levels, and increased catalase (CAT) level in serum, total antioxidant capacity (T-AOC) and glutathione peroxidase (GSH-Px) levels in liver as compared HFD group. Administration of p-CA also promoted the recovery of hyperlipidemia steatohepatitis in mice by ameliorating lipid peroxidation. These results suggested that p-CA is a potent antioxidant with potential therapeutic efficacy for treating hyperlipidemia symptoms.
In recent decades, infections caused by the opportunistic fungus Candida albicans have increased, especially in patients with immunodeficiency. In this study, we investigated the mechanism of action of sanguinarine (SAN) against C. albicans both in vitro and in vivo. SAN exhibited antifungal activity against C. albicans clinical isolates, with MICs in the range of 112.8–150.5 μM. Furthermore, scanning electron and transmission electron microscopy showed that SAN induced morphological changes as well as structure disruption in C. albicans cells, including masses of cellular debris, ruptured cell walls, and membrane deformation. Flow cytometry revealed that SAN could lead to cell membrane damage, and ergosterol content analysis indicated that SAN could cause ergosterol content reduction exceeding 90%. Further, we validated the efficacy of SAN against candidiasis caused by C. albicans in a murine model, and SAN significantly improved survival and reduced weight loss compared to vehicle. The treatment of 1.5 and 2.5 mg/kg/d SAN obviously reduced the fungal burden in the kidney. In addition, histopathological examination indicated that no fungal cells were observed in lung and kidney tissues after SAN treatment. Hence, this study suggests that SAN is a promising plant-derived compound for the development of an effective anticandidal agent.
In this paper, a new amphiphilic mono-6-β-cyclodextrin octadecylimine (6-β-CD-N-ODMA) copolymer was synthesized based on β-cyclodextrin and octadecylamine, which can self-assemble to form polymeric micelles. Drug-loaded micelles (a new drug carrier) were obtained using 6-β-CD-N-ODMA and paclitaxel (PTX) by the dialysis method. Orthogonal experiments were used to optimize the preparation method of the drug-loaded micelles. The drug-loading content of the carrier prepared by the optimized method was 1.97%. The physicochemical properties of blank micelles and drug-loaded micelles were evaluated by the fluorescence probe method, infrared spectra, dynamic light scattering, and scanning electron microscopy. The release properties of the carrier were investigated. The carrier has good pH sensitivity and the cumulative release rate after 96 h was 88% in PBS (pH = 5.0). The Ritger–Peppas equation is the optimal model for PTX released at pH 5.0, implying that the hydrolysis effect of 6-β-CD-N-ODMA is the main reason for PTX release. The results indicate that the developed carrier can increase the solubility of PTX and possess potential for increased clinical efficacy of PTX.
17 January 2022 in Applied Organometallic Chemistry
Three transition metal complexes (M = Fe III , Co III , Cu II ) were synthesized by hydrothermal method from bis(2-hydroxy-1-naphthalene-formaldehyde) 3,4-diaminobenzoic acid (H 3 L). They were characterized by infrared spectroscopy, elemental analysis, mass spectrometry. Artificial enzymes were constructed by hybridizing bovine serum albumin (BSA) with the metal complexes and characterized by UV-Vis and MALDI-TOF-MS. The binding of metal complexes with BSA was studied by UV-Vis spectroscopy, Raman spectroscopy, fluorescence spectroscopy, and circular dichroism spectroscopy. The secondary structure changes of BSA caused by the binding of metal complexes were investigated. All the three metal complexes can cause the intrinsic fluorescence quenching of BSA, which is mainly static quenching. The addition of metal complexes changed the conformation of BSA and decreased the content of α–helix structure. The activity of SOD was measured by xanthine oxidase-NBT method. Antioxidant activity tests showed that all metal complexes exhibited certain SOD activity, which increased after the formation of hybrid proteins. Asymmetric oxidation of thioether catalyzed by artificial enzymes was studied. The optimum reaction conditions were obtained by optimizing the reaction conditions. Substrate universality experiments were carried out under the optimum reaction conditions, showing good activity and enantioselectivity, with enantioselectivity up to 81%.