Sesquiterpenoids and bibenzyl derivative from Dendrobium hercoglossum.

Three new sesquiterpenoids, dendrohercoglin A - C (1-3), and one new bibenzyl derivative, dendronbiline D (4), together with nine known sesquiterpenoids (5-13) were isolated from Dendrobium hercoglossum. The structures of the new compounds were elucidated by extensive spectroscopic analysis as well as NMR and ECD calculations. All the compounds were evaluated for their neuroprotective and anti-inflammatory activities. Compounds 2 and 3 increased the H2O2-damaged SH-SY5Y cell viabilities from 43.3% to 58.6% and 68.4%, respectively. Compound 4 exhibited pronounced anti-inflammatory activity with IC50 value of 9.5 ± 0.45 µM which was superior to the reference compound quercetin (IC50: 15.7 ± 0.89 µM).

Anti-inflammatory and α-glucosidase inhibitory constituents from Dendrobium nobile Lindl.

Four new compounds ((±)-1-3), including one pair of enantiomers ((±)-1), along with 11 known bibenzyls (4-14) were isolated from Dendrobium nobile. The structures of the new compounds were elucidated by spectroscopic methods including 1D and 2D NMR as well as HRESIMS. The configurations of (±)-1 were established via the electronic circular dichroism (ECD) calculations. Compounds (+)-1 and 13 displayed pronounced α-glucosidase inhibitory activities with IC50 values of 16.7 ± 2.3 and 13.4 ± 0.2 µM, respectively, which were comparable to that of genistein (IC50, 8.54 ± 0.69 µM). Kinetic studies revealed that (+)-1 and 13 were non-competitive inhibitors against α-glucosidase and molecular docking simulations illuminated their interactions with α-glucosidase. All the isolates were also evaluated for their anti-inflammatory activities. Compounds 4, 5, and 11 exhibited superior inhibition activity with IC50 values ranging from 9.2 to 13.8 µM to that of quercetin (IC50, 16.3 ± 1.1 µM).

Lactose azocalixarene drug delivery system for the treatment of multidrug-resistant pseudomonas aeruginosa infected diabetic ulcer.

Diabetic wound is one of the most intractable chronic wounds that is prone to bacterial infection. Hypoxia is an important feature in its microenvironment. However, it is challenging for antimicrobial therapy to directly apply the existing hypoxia-responsive drug delivery systems due to the active targeting deficiency and the biofilm obstacle. Herein, we customizes a hypoxia-responsive carrier, lactose-modified azocalix[4]arene (LacAC4A) with the ability to actively target and inhibit biofilm. By loading ciprofloxacin (Cip), the resultant supramolecular nanoformulation Cip@LacAC4A demonstrates enhanced antibacterial efficacy resulting from both the increased drug accumulation and the controlled release at the site of infection. When applied on diabetic wounds together with multidrug-resistant Pseudomonas aeruginosa infection in vivo, Cip@LacAC4A induces definitely less inflammatory infiltration than free Cip, which translates into high wound healing performance. Importantly, such design principle provides a direction for developing antimicrobial drug delivery systems.

Structurally screening calixarenes as peptide transport activators.

Calixarenes are reportedly excellent activators that can remarkably improve the transport efficiencies of cell penetrating peptides. We employed eight calixarenes to systematically study the influence of structure on activation efficiency, which revealed that the scaffold, head group, and alkyl chain are all significant factors for activation efficiency by affecting affinities with the peptide and membrane.

Facile and label-free fluorescence strategy for evaluating the influence of bioactive ingredients on FMO3 activity via supramolecular host-guest reporter pair.

Screening inhibitors of flavin monooxygenase 3 (FMO3) is very important for treating trimethylamine N-oxide (TMAO) derived thrombotic diseases. Herein, focusing on Xuefu Zhuyu decoction (XFZYD) as a Chinese traditional medicine with antithrombotic efficacy, a facile and label-free fluorescence strategy was developed for evaluating the influence of the bioactive ingredients in XFZYD on FMO3 activity through indicator displacement assay. To this end, the optimized supramolecular host-guest (p-sulfonatocalix[4]arene-oxazine 1) reporter pair and FMO3 catalytic system were exploited to determine the influence of the bioactive compounds in XFZYD on the conversion from TMA to TMAO. From the nine compounds tested, naringin, paeoniflorin, ß-ecdysterone, 18ß-glycyrrhizic acid, amygdalin, albiflorin, and saikosaponin A downregulated FMO3 activity and reduced TMAO biosynthesis. Moreover, molecular docking was successfully applied to simulate the optimal conformation of a receptor-ligand complex between FMO3 and all tested compounds except for ß-ecdysterone. Therefore, this approach provides a novel and promising strategy for screening FMO3 inhibitors from Chinese traditional medicine by supramolecular sensing.

The effect of treatment stages on the coking wastewater hazardous compounds and their toxicity.

This study investigated the change of hazardous materials in coking wastewater at different treatment stages (anaerobic, anaerobic/aerobic, anaerobic/aerobic/photo degradation, anaerobic/aerobic/ozone oxidation treatment) and the effects of them on the development of maize embryos and the activity of amylase and protease in maize seeds. Moreover the interaction of refractory organic matters in the wastewater at different treatment stages with amylase and protease also were determined in vitro. The results show that the biodegradable and the refractory organic compounds in the wastewater both can affect maize embryo development (germination inhibition rate is 19.3% for biodegradable organic compounds). As the treatment stage preceding, the inhibition effect of coking wastewater on the development of the maize embryo (for germination inhibition rates change from 49.3% to 24.6%) and on enzymatic activity (inhibition rates change from 63.9% to 22.4% for amylase) decreases gradually, but the photo-degradation treatment to anaerobic/aerobic effluent can increase its toxicity. The changes in the ability of the refractory organic compounds to bind with enzyme proteins, combined with the analysis of the organic components by GC/MS, show that in the process of coking wastewater treatment no new toxic chemicals were produced.