ABSTRACT
A thermogravimetric analysis is used to analyze the thermal kinetics and investigate the synergistic effects between Alternanthera philoxeroides (AP) and waste tires (WTS) in a temperature range of 50-900 °C under three heating rates (15, 25, and 35 °C/min). Two model-free methods (FWO and KAS) and a model-fitting method (CR) were applied to calculate the activation energy. Results revealed that heating rates had no significant effect on the pyrolysis operation. The addition of WTS improved the thermal degradation of the samples as the samples had more than one stage during the main reaction period. A promoting synergistic effect was found in the blend 75A25WT and obtained the lowest activation energy among all the blends without a catalyst, while the blend 50A50WT exhibited an inhibiting effect. On the other hand, the addition of HZSM-5 accelerated the reaction time and obtained the lowest activation energy among all the blends without a catalyst. Furthermore, ΔW of 75A25WT+C was the lowest, indicating that the blend with a catalyst exhibited the strongest synergistic effect. This research confirmed that the addition of WTS improved the thermal parameters of the samples and clarified the capacity of HZSM-5 to reduce the activation energy.
Subject(s)
Heating , Pyrolysis , Biomass , Catalysis , Kinetics , Physics , ThermogravimetryABSTRACT
Two novel alkaloids compounds together with fifteen know metabolites were identified from Aspergillus ochraceus. The stereochemistry features of the new molecules were determined via HRESIMS, NMR, ECD, and XRD analyses. Amongst these, compounds two compounds exhibited potential efficacy as anti-Parkinson's disease with the EC50 values of 2.30 and 2.45â µM, respectively. ADMET prediction showed that these compounds owned favorable drug-like characteristics and safe toxicity scores towards CNS drugs. Virtual screening analyses manifested that the compounds exhibited not only robust and reliable interactions to adenosine receptors A2A , but also higher binding selectivity to A2A receptors than to A1 and A3 receptors. Molecular dynamics simulation demonstrated the reliability of molecular docking results and the stability of the complexes obtained with the novel compounds and A2A receptors in natural environments. It is the first time that anti-PD lead compounds have been identified from Aspergillus ochraceus and targeting adenosine A2A receptors.
Subject(s)
Adenosine A2 Receptor Antagonists/pharmacology , Antiparkinson Agents/pharmacology , Aspergillus ochraceus/chemistry , Receptor, Adenosine A2A/metabolism , Adenosine A2 Receptor Antagonists/chemistry , Adenosine A2 Receptor Antagonists/metabolism , Adenosine A2 Receptor Antagonists/pharmacokinetics , Animals , Antiparkinson Agents/chemistry , Antiparkinson Agents/metabolism , Antiparkinson Agents/pharmacokinetics , Cell Line, Tumor , Drug Evaluation, Preclinical , Female , Humans , Male , Mice , Molecular Docking Simulation , Molecular Dynamics Simulation , Neuroprotective Agents/chemistry , Neuroprotective Agents/metabolism , Neuroprotective Agents/pharmacokinetics , Neuroprotective Agents/pharmacology , Rats , StereoisomerismABSTRACT
Hyperjaponol H (1), a new filicinic acid-based meroterpenoid, with a 6/6/10 ring system trans-fused by hetero-Diels-Alder cycloaddition between a germacrane sesquiterpenoid and a filicinic acid moiety, was isolated from aerial parts of Hypericum japonicum. The elucidation of its structure and absolute configuration were accomplished by the analyses of extensive spectroscopic data and the comparison of Cotton effects of electron circular dichroism (ECD) with previously reported ones. The bioactivity assay showed that hyperjaponol H exhibited a moderate inhibitory efficacy on lytic Epstein-Barr virus (EBV) DNA replication in B95-8 cells.
Subject(s)
Butyrophenones/pharmacology , Cyclohexenes/pharmacology , Hypericum/chemistry , Sesquiterpenes, Germacrane/pharmacology , Terpenes/pharmacology , Animals , Antiviral Agents/pharmacology , Butyrophenones/chemistry , Carbon-13 Magnetic Resonance Spectroscopy , Cell Line , Cell Survival/drug effects , Circular Dichroism , Cyclohexenes/chemistry , Ganciclovir/pharmacology , Herpesvirus 4, Human/drug effects , Humans , Proton Magnetic Resonance Spectroscopy , Sesquiterpenes, Germacrane/chemistry , Terpenes/chemistry , Virus Replication/drug effectsABSTRACT
Present study aimed to investigate the eff ect of curcumin-pretreatment on intestinal I/R injury and on intestinal mucosa barrier. Thirty Wistar rats were randomly divided into: sham, I/R, and curcumin groups (n=10). Animals in curcumin group were pretreated with curcumin by gastric gavage (200 mg/kg) for 2 days before I/R. Small intestine tissues were prepared for Haematoxylin & Eosin (H&E) staining. Serum diamine oxidase (DAO) and tumor necrosis factor (TNF)-α levels were measured. Expression of intestinal TNF-α and tight junction protein (ZO-1) proteins was detected by Western blot and/or immunohistochemistry. Serum DAO level and serum and intestinal TNF-α leves were signifi cantly increased after I/R, and the values were markedly reduced by curcumin pretreatment although still higher than that of sham group (p<0.05 or p<0.001). H&E staining showed the significant injury to intestinal mucosa following I/R, and curcumin pretreatment signifi cantly improved the histological structure of intestinal mucosa. I/R insult also induced significantly down-regulated expression of ZO-1, and the eff ect was dramatically attenuated by curcumin-pretreatment. Curcumin may protect the intestine from I/R injury through restoration of the epithelial structure, promotion of the recovery of intestinal permeability, as well as enhancement of ZO-1 protein expression, and this eff ect may be partly attributed to the TNF-α related pathway.
