NGIWY-Amide: A Bioinspired Ultrashort Self-Assembled Peptide Gelator for Local Drug Delivery Applications

Fibrillar structures derived from plant or animal origin have long been a source of inspiration for the design of new biomaterials. The Asn-Gly-Ile-Trp-Tyr-NH2 (NGIWY-amide) pentapeptide, isolated from the sea cucumber Apostichopus japonicus, which spontaneously self-assembles in water to form hydrogel, pertains to this category. In this study, we evaluated this ultra-short cosmetic bioinspired peptide as vector for local drug delivery applications. Combining nuclear magnetic resonance, circular dichroism, infrared spectroscopy, X-ray diffraction, and rheological studies, the synthesized pentapeptide formed a stiff hydrogel with a high β-sheet content. Molecular dynamic simulations aligned well with scanning electron and atomic-force microscopy studies, revealing a highly filamentous structure with the fibers adopting a helical-twisted morphology. Model dye localization within the supramolecular hydrogel provided insights on the preferential distribution of hydrophobic and hydrophilic compounds in the hydrogel network. That was further depicted in the diffusion kinetics of drugs differing in their aqueous solubility and molecular weight, namely, doxorubicin hydrochloride, curcumin, and octreotide acetate, highlighting its versatility as a delivery vector of both hydrophobic and hydrophilic compounds of different molecular weight. Along with the observed cytocompatibility of the hydrogel, the NGIWY-amide pentapeptide may offer new approaches for cell growth, drug delivery, and 3D bioprinting tissue-engineering applications.

Olive-Leaf Extracts Modulate Inflammation and Oxidative Stress Associated with Human H. pylori Infection

Helicobacter pylori (H. pylori) is one of the major human pathogens and the main cause of pathological damages that can progress from chronic gastritis to gastric cancer. During the colonization of gastric mucosa, this bacterium provokes a strong inflammatory response and subsequent oxidative process, which are associated with tissue damage. Therefore, the objective of this research was to evaluate the ability of two olive-leaf extracts (E1 and E2) to modulate the inflammatory response and oxidative stress in H. pylori-infected human gastric AGS cells. The obtained results showed that both extracts significantly decreased interleukin-8 (IL-8) secretion and reactive oxygen species (ROS) production in human gastric AGS cells. Both extracts also showed antibacterial activity against different H. pylori strains. HPLC-PAD-MS characterization demonstrated that extract E1 was mainly composed of highly hydrophilic compounds, such as hydroxytyrosol (HT) and its glucosides, and it was the most effective extract as an antibacterial agent. In contrast, extract E2 was composed mostly of moderately hydrophilic compounds, such as oleuropein (OLE), and it was more effective than extract E1 as an anti-inflammatory agent. Both extracts exhibited similar potential to decrease ROS production. These results show the importance of standardizing the extract composition according to the bioactive properties that should be potentiated.

Characterization of the Permeation Properties of Membrane Filters and Sorption Properties of Sorbents Used for Polar Organic Chemical Integrative Samplers

<p>Polar organic chemical integrative samplers (POCIS) are promising devices for measuring time-weighted average concentrations of hydrophilic compounds in aquatic environments. However, the mechanism of POCIS uptake remains unclear. This study characterizes the permeation properties of polyethersulfone and polytetrafluoroethylene and the sorption properties of Oasis HLB (Waters), Envi-Carb (Supelco), and Oasis WAX (Waters) under identical conditions via calibration experiments of the POCIS. Plant protection products, neonicotinoid herbicides, and linear alkyl benzene sulfonates (LAS) were tested. The permeation experimental results suggested that the penetration rate constants (<i>k</i>_m) with high <i>K</i>_ow values (<i>K</i>_ow: octanol–water partition coefficient) were low, which indicated that the sorption of chemicals on the membrane may constitute a limiting factor for the permeation. The sorption experiments indicated that the sorption rate constants (<i>k</i>_s) depended on the type of sorbent instead of the <i>K</i>_ow values. Low <i>k</i>_s/<i>k</i>_m ratios were obtained for chemicals with low <i>K</i>_ow values, which implied that the POCIS uptake for highly hydrophilic compounds was controlled by both membrane and sorbent kinetics. The <i>k</i>_m and <i>k</i>_s values corresponded to the model and predicted the values of the sampling rates<i> </i>(<i>R</i>_s) for the LAS. These findings revealed the possibility of using <i>k</i>_s and <i>k</i>_m values to predict <i>R</i>_s values.</p>

Characterization of the Permeation Properties of Membrane Filters and Sorption Properties of Sorbents Used for Polar Organic Chemical Integrative Samplers

<p>Polar organic chemical integrative samplers (POCIS) are promising devices for measuring time-weighted average concentrations of hydrophilic compounds in aquatic environments. However, the mechanism of POCIS uptake remains unclear. This study characterizes the permeation properties of polyethersulfone and polytetrafluoroethylene and the sorption properties of Oasis HLB (Waters), Envi-Carb (Supelco), and Oasis WAX (Waters) under identical conditions via calibration experiments of the POCIS. Plant protection products, neonicotinoid herbicides, and linear alkyl benzene sulfonates (LAS) were tested. The permeation experimental results suggested that the penetration rate constants (<i>k</i>_m) with high <i>K</i>_ow values (<i>K</i>_ow: octanol–water partition coefficient) were low, which indicated that the sorption of chemicals on the membrane may constitute a limiting factor for the permeation. The sorption experiments indicated that the sorption rate constants (<i>k</i>_s) depended on the type of sorbent instead of the <i>K</i>_ow values. Low <i>k</i>_s/<i>k</i>_m ratios were obtained for chemicals with low <i>K</i>_ow values, which implied that the POCIS uptake for highly hydrophilic compounds was controlled by both membrane and sorbent kinetics. The <i>k</i>_m and <i>k</i>_s values corresponded to the model and predicted the values of the sampling rates<i> </i>(<i>R</i>_s) for the LAS. These findings revealed the possibility of using <i>k</i>_s and <i>k</i>_m values to predict <i>R</i>_s values.</p>

Profiles of Secondary Metabolites (Phenolic Acids, Carotenoids, Anthocyanins, and Galantamine) and Primary Metabolites (Carbohydrates, Amino Acids, and Organic Acids) during Flower Development in Lycoris radiata

This study aimed to elucidate the variations in primary and secondary metabolites during Lycorisradiata flower development using high performance liquid chromatography (HPLC) and gas chromatography time-of-flight mass spectrometry (GC-TOFMS). The result showed that seven carotenoids, seven phenolic acids, three anthocyanins, and galantamine were identified in the L. radiata flowers. Most secondary metabolite levels gradually decreased according to the flower developmental stages. A total of 51 metabolites, including amines, sugars, sugar intermediates, sugar alcohols, amino acids, organic acids, phenolic acids, and tricarboxylic acid (TCA) cycle intermediates, were identified and quantified using GC-TOFMS. Among the hydrophilic compounds, most amino acids increased during flower development; in contrast, TCA cycle intermediates and sugars decreased. In particular, glutamine, asparagine, glutamic acid, and aspartic acid, which represent the main inter- and intracellular nitrogen carriers, were positively correlated with the other amino acids and were negatively correlated with the TCA cycle intermediates. Furthermore, quantitation data of the 51 hydrophilic compounds were subjected to partial least-squares discriminant analyses (PLS-DA) to assess significant differences in the metabolites of L. radiata flowers from stages 1 to 4. Therefore, this study will serve as the foundation for a biochemical approach to understand both primary and secondary metabolism in L. radiata flower development.