Understanding the relationship between the structural properties of lignin and their biological activities.

Due to the antioxidant properties of lignin, it has been demonstrated as an active substance for treating oxidation-related and inflammatory diseases. However, how the structural properties of lignin affect its biological activities is still ambiguous. In this study, Kraft lignin from wheat straw (KL-A) was used as the raw material to fractionate into three fractions (e.g., KL-B, KL-C, and KL-D) with different molecular weight by ultrafiltration, which possessed different physicochemical properties. The biocompatibility, in vivo and in vitro scavenging abilities for reactive oxygen species (ROS), and anti-apoptotic abilities of the lignin fractions were evaluated using SW1353 chondrocyte cell lines and were quantitatively fitted to their physicochemical properties. The results showed that lignin fractions with lower molecular weights, lower G/S ratios, and higher non-condensed phenolic OH contents endowed lignin with stronger ROS scavenging ability in vivo and in vitro, but was accompanied by increased cytotoxicity to cells. The half maximal inhibitory concentration (IC50) of KL-A, KL-B, KL-C, and KL-D were separately determined as 44.02, 33.43, 32.41, and 18.40 µg/mL. Furthermore, KL-D, with the lowest molecular weight and highest number of functional groups, showed the best antioxidant ability, while it performed poorly in inhibiting cellular apoptosis of chondrocytes. Compared to KL-D, KL-C with inverse structural properties, performed better in anti-apoptosis of SW1353 cells, which is the optimum lignin as promising active substances to be applied in the treatment of osteoarthritis in biomedical engineering.

Evaluating the bio-application of biomacromolecule of lignin-carbohydrate complexes (LCC) from wheat straw in bone metabolism via ROS scavenging.

Lignin-carbohydrate complexes (LCC) arebiomacromolecules that can be obtained from different biomass. Even some works have shown the LCC can efficiently scavenge the intracellular and endogenous reactive oxygen species (ROS), while little work has been carried out to investigate the potential application of LCC for ROS-related treatment in biological filed, especially for the treatment of periprosthetic osteolysis in vivo. In this work, Lignin-rich (LCC-A) and carbohydrate-rich (LCC-B) fractions in wheat straw are isolated and used as the ROS scavenger to promote osteoblast differentiation and inhibit osteoclast differentiation. The chemical composition and structures are characterized by high performance anion exchange chromatography (HPAEC) and nuclear magnetic resonance (NMR) technologies (quantitative 13C NMR and 2D-HSQC NMR), respectively. The results showed LCC-A possesses higher in vitro ROS-scavenging ability than LCC-B (89.8% vs 57.8%) and to inhibit osteoclast differentiation, whereas LCC-B more significantly activates cellular antioxidant activities via the KEAP1-NRF2-ARE pathway (218.5% vs 438.0% in the level of HO-1), thus promoting osteoblast differentiation in an inflammatory environment. Moreover, the therapeutic administration of LCC-A and LCC-B for Ti-particle-induced osteolytic murine calvariae showed both of them positively regulate and restore the bone metabolism, while preventing calvaria impairment. Hence, LCC from wheat straw exhibits efficient bone protective effects, suggesting it may be used as the promising ROS scavenger for clinical treatment of periprosthetic osteolysis.

Membrane active antimicrobial activity and molecular dynamics study of a novel cationic antimicrobial peptide polybia-MPI, from the venom of Polybia paulista.

As the frequent emergence of the resistant bacteria, the development of new agents with a new action mode attracts a great deal of interest. It is now widely accepted that antimicrobial peptides (AMPs) are promising alternatives to conventional antibiotics. In this study, antimicrobial peptide polybia-MPI and its analogs were synthesized and their antibacterial activity was studied. Our results revealed that polybia-MPI has potent antibacterial activity against both Gram-positive and Gram-negative bacteria. Its ability to make PI permeate into bacteria and lead to the leakage of calcein from model membrane LUVs, suggests a killing mechanism involving membrane perturbation. SEM and TEM microscopy experiments verified that the morphology of bacteria was changed greatly under the treatment of polybia-MPI. Compared with the conventional chemotherapy, polybia-MPI targets the cell membrane rather than entering into the cell to exert its antibacterial activity. Furthermore, molecular dynamics (MD) simulations were employed to investigate the mechanism of membrane perturbation. The results indicated that the α-helical conformation in the membrane is required for the exhibition of antibacterial activity and the membrane disturbance by polybia-MPI is a cooperative process. In conclusion, with the increasing resistance to conventional antibiotics, there is no doubt that polybia-MPI could offer a new strategy to defend the resistant bacteria.