Novel inhibitors of the (VIBVN) NAT protein identified through pharmacophore modeling.

Arylamine N-acetyltransferases (NATs, E.C. 2.

Inhibitory Effects of 3-Cyclopropylmethoxy-4-(difluoromethoxy) Benzoic Acid on TGF-β1-Induced Epithelial-Mesenchymal Transformation of In Vitro and Bleomycin-Induced Pulmonary Fibrosis In Vivo.

Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease characterized by lung inflammation and excessive deposition of extracellular matrix components. Transforming growth factor-β1 (TGF-β1) induced epithelial-mesenchymal transformation of type 2 lung epithelial cells leads to excessive extracellular matrix deposition, which plays an important role in fibrosis. Our objective was to evaluate the effects of 3-cyclopropylmethoxy-4-(difluoromethoxy) benzoic acid (DGM) on pulmonary fibrosis and aimed to determine whether EMT plays a key role in the pathogenesis of pulmonary fibrosis and whether EMT can be used as a therapeutic target for DGM therapy to reduce IPF.

Chitooligosaccharides Derivatives Protect ARPE-19 Cells against Acrolein-Induced Oxidative Injury.

Age-related macular degeneration (AMD) is the leading cause of vision loss among the elderly. The progression of AMD is closely related to oxidative stress in the retinal pigment epithelium (RPE). Here, a series of chitosan oligosaccharides (COSs) and -acetylated derivatives (NACOSs) were prepared, and their protective effects on an acrolein-induced oxidative stress model of ARPE-19 were explored using the MTT assay.

Leonurine attenuates OVA-induced asthma via p38 MAPK/NF-κB signaling pathway.

Leonurine (Leo) is a natural alkaloid extracted from Herba leonuri, which has many biological activities. However, whether leonurine has a protective effect on asthma remains unknown. The purpose of this study was to investigate the protective effect of leonurine on asthma.

Eupatilin inhibits keratinocyte proliferation and ameliorates imiquimod-induced psoriasis-like skin lesions in mice via the p38 MAPK/NF-κB signaling pathway.

Background: Psoriasis is a chronic inflammatory skin disease that is currently incurable and causes long-term distress to patients. Therefore, there is an urgent need to develop safe and effective psoriatic drugs. Eupatilin is a natural flavone, that has a variety of pharmacological effects.

Antidiabetic-activity sulfated polysaccharide from Chaetomorpha linum: Characteristics of its structure and effects on oxidative stress and mitochondrial function.

A water-soluble polysaccharide from the green alga Chaetomorpha linum, designated CHS2, was obtained by water extraction, preparative anion-exchange and size-exclusion chromatography. Results of chemical and spectroscopic analyses showed that CHS2 was a sulfated rhamnogalactoarabinan, and its backbone was mainly constituted by 4-linked and 3,4-linked β-l-arabinopyranose with sulfate groups at C-2/C-3 of 4-linked β-l-arabinopyranose. The branching contained 4-linked, 6-linked β-d-galactopyranose and terminal rhamnose residues.

Eupatilin Suppresses OVA-Induced Asthma by Inhibiting NF-κB and MAPK and Activating Nrf2 Signaling Pathways in Mice.

To investigate the effect of eupatilin in asthma treatment, we evaluated its therapeutic effect and related signal transduction in OVA-induced asthmatic mice and LPS-stimulated RAW264.7 cells. The BALF was tested for changes in lung inflammatory cells.

Anti-diabetic activity of a sulfated galactoarabinan with unique structural characteristics from Cladophora oligoclada (Chlorophyta).

The polysaccharide from green alga Cladophora oligoclada, OHSS2, was a sulfated galactoarabinan which was constituted by a backbone of (1 → 4)-β-l-arabinopyranose units with partial sulfate at C-3 of (1 → 4)-β-l-arabinopyranose units. The side chains containing (1 → 4)-β-l-arabinopyranose, (1 → 4)-β-d-galactopyranose and/or (1 → 4,6)-β-d-galactopyranose units were in C-2/C-3 of (1 → 4)-β-l-arabinopyranose units. OHSS2 had strong anti-diabetic activity in vitro assessed by inhibition of human islet amyloid polypeptide (hIAPP) aggregation.

A Novel PTP1B Inhibitor-Phosphate of Polymannuronic Acid Ameliorates Insulin Resistance by Regulating IRS-1/Akt Signaling.

Protein tyrosine phosphatase 1B (PTP1B) is a critical negative modulator of insulin signaling and has attracted considerable attention in treating type 2 diabetes mellitus (T2DM). Low-molecular-weight polymannuronic acid phosphate (LPMP) was found to be a selective PTP1B inhibitor with an IC of 1.02 ± 0.

Design, synthesis and lipid-lowering activities of penipyridone derivatives.

On the basis of our earlier discovered natural product penipyridone G with potential lipid-lowering utility, 35 penipyridone derivatives were designed, synthesized and characterized. Based on the oleic acid-induced HepG2 cell lipid accumulation model, compounds 12c, 14, 15f, 15k, 15o, 15p and 16f showed potent lipid-lowering activities among the synthetic compounds at 10 μM. In particular, compounds 4, 15k, 15o showed significant activities on inhibiting lipid accumulation in insulin resistant HepG2 cells, and these three compounds were safe and non-toxic within the concentration range of 400 μM.

Fucoidan from Suppresses Postprandial Hyperglycemia by Inhibiting Na/Glucose Cotransporter 1 Activity.

We previously demonstrated that fucoidan with a type II structure inhibited postprandial hyperglycemia by suppressing glucose uptake, but the mechanism remains elusive. Here, we aimed to assess whether the effect of glucose absorption inhibition was related to the basic structure of fucoidans and preliminarily clarified the underlying mechanism. Fucoidans with type II structure and type I structure were prepared from (AnF) or (LjF) and (KcF), respectively.

Photoprotective effect of Astragalus membranaceus polysaccharide on UVA-induced damage in HaCaT cells.

Background: The skin provides a predominant barrier against chemical, physical and microbial incursion. The intemperate exposure to ultraviolet A (UVA) radiation can cause excessive cellular oxidative stress, leading to skin damage, proteins damage and mitochondrial dysfunction. There is sufficient evidences supporting the proposal that mitochondria is highly implicated in skin photo-damage.

Oligomannuronate prevents mitochondrial dysfunction induced by IAPP in RINm5F islet cells by inhibition of JNK activation and cell apoptosis.

Background: Oligomannuronates (OM) are natural products from alginate that is frequently used as food supplement. The aim of this study was to investigate the in vitro protective effects of OM on RINm5F cells against human Islet amyloid polypeptide (IAPP) induced mitochondrial dysfunction, as well as the underlying mechanisms.

Methods: In the present study, we obtained several kinds of OM with different molecular masses, and then we used RINm5F cells as a model to elucidate the involvement of JNK signal pathway in hIAPP-induced mitochondrial dysfunction in pancreatic beta cells, and the protective effects of OM are associated with its ability to attenuate the mitochondrial dysfunction.

Protective effect of d-tetramannuronic acid tetrasodium salt on UVA-induced photo-aging in HaCaT cells.

UVA radiation from the sun is the main external stimulus in the pathogenesis of skin photo-aging. This process is associated with cellular oxidative stress. Here we aim at showing the protective effect of d-Tetramannuronic Acid Tetrasodium Salt (M4), a natural product, against UVA (30J/cm) irradiation-induced oxidative stress and photo-aging in HaCaT cells, and to reveal the molecular mechanism underlying the protective efficacy.

Protective Effect of L-Hexaguluroic Acid Hexasodium Salt on UVA-Induced Photo-Aging in HaCaT Cells.

This study aimed to show the α-L-Hexaguluroic acid hexasodium salt (G6) protective effect against UVA-induced photoaging of human keratinocyte cells. We found that G6 localized to the mitochondria and improved mitochondrial functions. G6 increased respiratory chain complex activities, which led to increased cellular ATP content and NAD/NADH ratio.

Two different fucosylated chondroitin sulfates: Structural elucidation, stimulating hematopoiesis and immune-enhancing effects.

Two fucosylated chondroitin sulfates FCS and FCS were isolated from the sea cucumber Holothuria polii and Holothuria tubulosa, respectively. The NMR spectroscopy and HILIC-FTMS methods were applied for their detailed structural characterization. Chemical analysis indicated that the two FCSs all contained a chondroitin sulfate backbone chondroitin sulfate-like core and fucosyl branches of α-L-Fuc2,4S, α-L-Fuc4S or α-L-Fuc3,4S linked to O-3 of glucuronic acid residues.

Anti-diabetic activities of agaropectin-derived oligosaccharides from Gloiopeltis furcata via regulation of mitochondrial function.

The aim of the present study was to investigate whether agaropectin-derived oligosaccharides from Gloiopeltis furcata (SAOs) exert an anti-diabetic effect in sodium palmitate (PA)-induced insulin resistant HepG2 cells. We found that SAOs were co-localized with mitochondria and regulated mitochondrial function. SAOs reduced respiratory chain activities, which led to reduced respiratory oxygen consumption and increased the cellular ADP/ATP ratio in a certain degree of dose-dependent manner.

Purification, structural characterization, and immunomodulatory activity of the polysaccharides from Ganoderma lucidum.

A preliminary relationship was illustrated between the structural characteristics and corresponding immunomodulatory activities of G. lucidum polysaccharides. Two polysaccharides (GLP-1 and GLP-2) were purified from Ganoderma lucidum extracts by gradient ethanol precipitation and a Q-Sepharose Fast Flow (QFF) strong anion-exchange column.

Anti-Metabolic Syndrome Effects of Fucoidan from via Reactive Oxygen Species-Mediated Regulation of JNK, Akt, and AMPK Signaling.

Recent studies have reported that dietary fiber improved metabolic syndrome (MetS). However, the effects of fucoidans on MetS were still not clear. In this study, we evaluated the activity of fucoidan from (FvF) on attenuating MetS and first elucidated the underlying mechanism.

Alkaline Extraction, Structural Characterization, and Bioactivities of (1→6)-β-d-Glucan from .

The purpose of this study is to develop a robust approach to obtain β glucans from and to characterize their structural and biological properties for sustainable utilization. The alkali extraction was optimized with an orthogonal experimental design, and a concise process for obtaining specific targeting polysaccharides from was developed in this study. After purification with a Q-Sepharose Fast Flow strong anion-exchange column, the monosaccharide composition, a methylation analysis, and NMR spectroscopy were employed for their structural characterizations.

Profiling and Structural Characterization of High Neu5Gc or Sulfate-containing O-glycans from Hyla Rabbit Intestinal Mucin.

Intestinal mucins constitute the major component of the mucus covering the epithelium of the gastrointestinal tract, thereby forming a barrier against microbial colonization. Rabbits are bred in large numbers worldwide, with little known about intestinal O-glycosylation despite this insight being crucial to the understanding of host-pathogen interactions. In the present study, a major mucin-type glycopeptide (RIF6) of hyla rabbit intestine was isolated and the O-glycans were extensively characterized based on liquid chromatography-tandem mass spectrometry (LC-MS/MS) combined with bioinformatics approaches.

Structural characterization and anti-thrombotic properties of fucoidan from Nemacystus decipiens.

The sulfated polysaccharide NP2 was isolated and purified from Nemacystus decipiens, the structure and antithrombotic activity of NP2 was further studied. NP2 was composed of fucose, glucuronic acid, galactose and xylose at molar ratios of 76.3:20.

Structural Characteristics and Anticoagulant Property In Vitro and In Vivo of a Seaweed Sulfated Rhamnan.

Great diversity and metabolite complexity of seaweeds offer a unique and exclusive source of renewable drug molecules. Polysaccharide from seaweed has potential as a promising candidate for marine drug development. In the present study, seaweed polysaccharide (SPm) was isolated from , the polymeric repeat units and anticoagulant property in vitro and in vivo of SPm were investigated.