Synthesis and bioevaluation of water-soluble -cyclodextrin-diterpene acid conjugates.

A series of -cyclodextrin (-CD)-conjugates were prepared by combining three abietane-type diterpene acids with two azide-functionalized -CDs via click chemistry, and the antiviral activity against wild-type and omicron SARS-CoV-2 spike pseudovirus as well as the antibacterial activity against were investigated. All the synthesised conjugates exhibited no significant cytotoxicity to BHK-21-hACE2 cells with cell viability over 80% at concentration of 15 M. Among the conjugates, the heptavalent -CD-dehydroabietic acid conjugate exhibited higher anti-SARS-CoV-2 activity against the omicron variant compared to the other conjugates.

Oleanolic acid derivative alleviates cardiac fibrosis through inhibiting PTP1B activity and regulating AMPK/TGF-β/Smads pathway.

Cardiac fibrosis (CF) in response to persistent exogenous stimuli or myocardial injury results in cardiovascular diseases (CVDs). Protein tyrosine phosphatase 1B (PTP1B) can promote collagen deposition through regulating AMPK/TGF-β/Smads signaling pathway, and PTP1B knockout improves cardiac dysfunction against overload-induced heart failure. Oleanolic acid (OA) has been proven to be an inhibitor of PTP1B, and its anti-cardiac remodeling effects have been validated in different mouse models.

Novel mono- and multivalent N-acetylneuraminic acid glycoclusters as potential broad-spectrum entry inhibitors for influenza and coronavirus infection.

N-acetylneuraminic acid (Neu5Ac) is a glycan receptor of viruses spread in many eukaryotic cells. The present work aimed to design, synthesis and biological evaluation of a panel of Neu5Ac derivatives based on a cyclodextrin (CD) scaffold for targeting influenza and coronavirus membrane proteins. The multivalent Neu5Ac glycoclusters efficiently inhibited chicken erythrocyte agglutination induced by intact influenza virus in a Neu5Ac density-dependent fashion.

Discovery of Pentacyclic Triterpenoid PROTACs as a Class of Effective Hemagglutinin Protein Degraders.

Influenza hemagglutinin that drives viral entry into cells via the membrane fusion process is an up-and-coming antiviral drug target. Herein, we described for the first time the design, synthesis, and biological characteristics of a new class of pentacyclic triterpenoid-based proteolysis targeting chimeras (PROTACs) to enhance the degradation of hemagglutinin target. Among these PROTACs, showed the best degradation effect on the hemagglutinin with a median degradation concentration of 1.

Novel -Cyclodextrin-Based Heptavalent Glycyrrhetinic Acid Conjugates: Synthesis, Characterization, and Anti-Influenza Activity.

In our continuing efforts toward the design of novel pentacyclic triterpene derivatives as potential anti-influenza virus entry inhibitors, a series of homogeneous heptavalent glycyrrhetinic acid derivatives based on -cyclodextrin scaffold were designed and synthesized by click chemistry. The structure was unambiguously characterized by NMR, IR, and MALDI-TOF-MS measurements. Seven conjugates showed sufficient inhibitory activity against influenza virus infection based on the cytopathic effect reduction assay with IC values in the micromolar range.

Low Molecular Weight Fucoidan Inhibits Pulmonary Fibrosis In Vivo and In Vitro via Antioxidant Activity.

In this study, sulfated polysaccharides extracted from were degraded by free radicals to obtain low molecular weight fucoidan (LMWF). The and effects of LMWF on bleomycin-treated pulmonary fibrosis mice and TGF-treated A549 cells, respectively, were evaluated, and the role of antioxidant activity was assessed. H&E, Masson's trichrome, and Sirius red staining results showed that bleomycin induced obvious pathological changes and collagen deposition in the lung tissue of mice.

Dispersible MoS micro-sheets induced a proinflammatory response and apoptosis in the gills and liver of adult zebrafish.

Molybdenum disulfide (MoS), one of the next-generation two-dimensional materials (2DMs), has attracted increasing attention due to its unique physicochemical properties. However, the aquatic toxicity of dispersible MoS is still unknown. Herein, we synthesized chitosan functionalized MoS (CS-MoS) micro-sheets with a satisfying water-dispersible performance.

Effect of Bulk MoS₂ on the Metabolic Profile of Yeast.

MoS2, a kind of two-dimensional material with unique performances, has been widely used in many fields. However, an in-depth understanding of its toxicity is still needed, let alone its effects on the environmental microorganism. Herein, we used different methods, including metabolomics technology, to investigate the influence of bulk MoS2 (BMS) on yeast cells.

Effects of dispersible MoS nanosheets and Nano-silver coexistence on the metabolome of yeast.

As a new rising star in the post-graphene two-dimensional materials (2DMs), molybdenum disulfide (MoS) attracts increasing attentions and is widely applied. However, the chemical and toxicological interaction between MoS and other co-contaminants is still poorly understood. Nano-silver (N-Ag) is the most commonly used nanomaterial in commercial products and distributed widely in the environment.

Dispersible MoS Nanosheets Activated TGF-β/Smad Pathway and Perturbed the Metabolome of Human Dermal Fibroblasts.

In postgraphene two-dimensional materials (2DMs), MoS has attracted increasing attention in the biomedical field due to its excellent physicochemical properties. However, the toxicity and biocompatibility evaluation of MoS is not fully addressed. Herein, chitosan functionalized MoS (CS-MoS) nanosheets, which showed perfect dispersibility and stability performances, were synthesized and characterized.