Comparative studies of organic contaminant removal in different calcium sulfite-enhanced oxidant/Fe(II) systems: Kinetics, mechanisms, and differentiated degradation pathways.

The application of S(IV) for the regeneration of Fe(II) has been widely investigated. As the common S(IV) sources, sodium sulfite (Na2SO3) and sodium bisulfite (NaHSO3) are soluble in the solution, resulting in excessive SO32- concentration and redundant radical scavenging problems. In this research, calcium sulfite (CaSO3) was applied as the substitution for the enhancement of different oxidant/Fe(II) systems. The advantages of CaSO3 could be summarized as follows: (1) it could sustainedly supplement SO32- for Fe(II) regeneration, preventing radical scavenging and unnecessary reagent waste; (2) the cost and toxicity of CaSO3 were extremely lower than that of other S(IV) sources; (3) the concentration of reactive species increased in the presence of CaSO3; and (4) after the reaction, SO42- would form CaSO4 precipitate, which would not increase the burden of SO42- in the solution. In the participation of CaSO3, the removal of trichloroethylene (TCE) and other organic contaminants were significantly promoted and different enhanced systems had high tolerance on complex solution conditions. The major reactive species in different systems were determined through qualitative and quantitative analyses. Eventually, the dechlorination and mineralization of TCE were measured and the differentiated degradation pathways in different CaSO3-enhanced oxidants/Fe(II) systems were elucidated.

Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy.

AIM: To develop an innovative 211At nanoplatform with high radiolabeling efficiency and low in vivo deastatination for future targeted alpha-particle therapy (TAT) to treat cancer. METHODS: Star-shaped gold nanoparticles, gold nanostars (GNS), were used as the platform for 211At radiolabeling. Radiolabeling efficiency under different reaction conditions was tested. Uptake in the thyroid and stomach after systemic administration was used to evaluate the in vivo stability of 211At-labeled GNS. A subcutaneous U87MG human glioma xenograft murine model was used to preliminarily evaluate the therapeutic efficacy of 211At-labeled GNS after intratumoral administration. RESULTS: The efficiency of labeling GNS with 211At was almost 100% using a simple and rapid synthesis process that was completed in only 1 min. In vitro stability test in serum showed that more than 99% of the 211At activity remained on the GNS after 24 h incubation at 37°C. In vivo biodistribution results showed low uptake in the thyroid (0.44-0.64%ID) and stomach (0.21-0.49%ID) between 0.5 and 21 h after intravenous injection, thus indicating excellent in vivo stability of 211At-labeled GNS. The preliminary therapeutic efficacy study demonstrated that 211At labeled GNS substantially reduced tumor growth (P < 0.001; two-way ANOVA) after intratumoral administration. CONCLUSION: The new 211At radiolabeling strategy based on GNS has the advantages of a simple process, high labeling efficiency, and minimal in vivo dissociation, making it an attractive potential platform for developing TAT agents that warrants further evaluation in future preclinical studies directed to evaluating prospects for clinical translation.

The anti-inflammatory components from the effective fraction of Syringae Folium (ESF) and its mechanism investigation based on network pharmacology.

The Syringae Folium (SF), noted in Chinese Pharmacopeia, has been used in herbal medicines to treat inflammatory diseases and its water extract of SF, Yanlixiao (YLX) which is commercial preparation traditional Chinese medicine has been widely used clinically against intestinal inflammations. To explore its therapeutic material basis of SF, an effective fraction from SF (ESF) was found out by bio-guided isolation and enrichment of active components. In this research, ESF was identified as the anti-inflammatory fraction by comparing the survival rate of LPS-induced inflammation mouse model. The in vivo anti-inflammation efficacy of ESF was further tested by mouse ear edema model. Fifteen main components of ESF were separated from ESF after identification by UPLC-TOF-MS, and their inhibition on lipopolysaccharide (LPS)-induced nitric oxide (NO) production was tested along with ESF in RAW 264.7 macrophages cell line. Aiming to search its anti-inflammation mechanisms, the network pharmacology study was performed based on the main active components. As results, ESF was found with better efficacy in inhibiting ear swelling (82.2 mg/kg, 43.7%) compared with YLX (293.3 mg/kg, 37.9%). Meanwhile, the main ESF components, luteolin and quercetin were found with significant efficacy in reducing NO production compared with aminoguanidine (positive control) (81.3%, 78.7% and 76.3%, respectively, 50 µg/ml). Analysis of network pharmacology also suggested that luteolin and quercetin could be the key components for the anti-inflammation activity of ESF, and NFKB1, RELA, AKT1, TNF and PIK3CG were identified as key targets and MAPK, NF-κB, TCR and TLRs signaling pathways could be involved in the anti-inflammation action of ESF. The results attained in this study indicated that ESF had the potential to be developed as an anti-inflammation agent applied in clinic.

The antibacterial activity of syringopicroside, its metabolites and natural analogues from Syringae Folium.

In the present study, the in vitro antibacterial activity of an effective fraction (ESF) from Syringae Folium (SF) on Methicillin-resistant Staphylococcus aureus (MRSA) was evaluated and then its in vivo activity was evaluated by using the MRSA-infected mouse peritonitis model. The ESF showed a significant in vitro and in vivo activity on decreasing the Minimum Inhibitory Concentrations (MICs) and increasing the survival rate of mouse from 42.8% to 100%. Six iridoid glucosides (IGs) of ESF were characterized by UPLC-TOF-MS method and also isolated by column chromatography. Most of them showed in vitro anti MRSA activity. Syringopicroside (Sy), the major compound of IGs, was found to increase the survival rate from 42.8% to 92.8% of the MRSA-infected mouse, which revealed Sy is also the main active components of ESF. In order to know why the effect of oral administration of SF is better than its injections in clinic and the metabolites of Sy, seven metabolites of Sy were isolated from rat urine and identified on the basis of NMR and MS spectra. Most of metabolites possessed stronger in vitro anti-MRSA activity than that of Sy, which furtherly proved the clinical result.

The antibacterial activity of phytochemically characterised fractions from Folium Syringae.

To identify the most active antimicrobial fraction of Folium Syringae, four common pathogens were used in an in vitro screening. The results indicated that the combination of the 30% and 60% ethanol fraction (FSC) obtained from the water extraction was the most active fraction with a minimal inhibitory concentration of 0.65 mg mL(-1). FSC was also found to be able to protect mice from a lethal infection of Staphylococcus aureus at clinical dosage (0.2 g kg(-1)) with a survival rate of 83.3%. The antibacterial activity of FSC was then tested using the serum pharmacology method which revealed that FSC exhibits a more long-lasting activity than the positive control (levofloxacin hydrochloride). The main components were confirmed to be iridoid glycosides and flavones by HPLC-MS analysis.