Isolation, structural characteristics and cytotoxicity of the constitutes from L.

Seventeen compounds were isolated from the aerial parts of L., including 1 previously undescribed xanthone and 6 firstly isolated compounds. The structures of compounds were identified by Mass spectrometry and NMR spectroscopy.

Synthesis and Fungicidal Activities of Coumarin Derivatives as Succinate Dehydrogenase Inhibitors.

Succinate dehydrogenase inhibitors (SDHIs) have been developed to the fastest growing family of fungicides. To develop novel succinate dehydrogenase (SDH) inhibitors, 27 novel non-amides coumarin derivatives were designed, synthesized, and characterized. The bioassay revealed that most of the target compounds exhibited significant antifungal activity against Botrytis cinerea in vitro.

Novel Aminocoumarin Derivatives against Phytopathogenic Fungi: Design, Synthesis and Structure-Activity Relationships.

Phytopathogenic fungi is the most devastating reason for the decrease of the agricultural production and food safety. To develop new fungicidal agents for resistance concerning, a novel series of aminocoumarin derivatives were synthesized and their fungicidal activity were investigated both in vitro and in vivo. Transmission electron microscope (TEM), scanning electron microscope (SEM), RNA-Seq, 3D-QSAR and molecular docking were applied to reveal the underlying anti-fungal mechanisms.

Trimethylamine N-Oxide (TMAO) Inducing Endothelial Injury: UPLC-MS/MS-Based Quantification and the Activation of Cathepsin B-Mediated NLRP3 Inflammasome.

TMAO is a new risk biomarker for cardiovascular disease. With trimethylammonium as its main chemical skeleton, TMAO is structurally similar to many endogenous metabolites, such as acetylcholine, carnitine, phosphorylcholine, etc. The mechanism of TMAO on the pathological process of CVD is still unclear.

Xanthanolides in L.: Structures, Synthesis and Bioactivity.

Xanthanolides were particularly characteristic of the genus , which exhibited broad biological effects and have drawn much attention in pharmacological application. The review surveyed the structures and bioactivities of the xanthanolides in the genus , and summarized the synthesis tactics of xanthanolides. The results indicated that over 30 naturally occurring xanthanolides have been isolated from the genus in monomeric, dimeric and trimeric forms.

Iron metabolism disorder regulated by BMP signaling in hypoxic pulmonary hypertension.

Backgrounds And Aims: Unexplained iron deficiency is associated with poorer survival in patients with pulmonary hypertension (PH). Bone morphogenetic protein (BMP) signaling and BMP protein type II receptor (BMPR2) expression are important in the pathogenesis of PH. BMP6 in hepatocytes is a central transcriptional regulator of the iron hormone hepcidin that controls systemic iron balance.

Hypoxia-elicited cardiac microvascular endothelial cell-derived exosomal miR-210-3p alleviate hypoxia/reoxygenation-induced myocardial cell injury through inhibiting transferrin receptor 1-mediated ferroptosis.

Objective: Ferroptosis is a novel mode of non-apoptotic cell death induced by build-up of toxic lipid peroxides (lipid-ROS) in an iron dependent manner, which is a key event in ischemia/reperfusion (I/R)-induced cardiomyocytes damages. Studies indicated that ischemic preconditioning with cardiac microvascular endothelial cells (CMECs) protected against I/R-induced cardiomyocytes damages. However, the role of hypoxia-conditioned CMECs-derived Exo (H-exo) in I/R cardiomyocytes damages remains largely unclear.

UHPLC-QTOF-MS/MS based characterization of anti-tumor constituents in L. and identification of EGFR-TK inhibitors by virtual screening.

The constituents of L., as a traditional anticancer medicine of Kazakh, were firstly profiled with UHPLC-QTOF-MS/MS. The potential compounds against EGFR-TK were virtually screened.

Dual-Responsive Alginate Hydrogel Constructed by Sulfhdryl Dendrimer as an Intelligent System for Drug Delivery.

Intelligent stimulus-triggered release and high drug-loading capacity are crucial requirements for drug delivery systems in cancer treatment. Based on the excessive intracellular GSH expression and pH conditions in tumor cells, a novel glutathione (GSH) and pH dual-responsive hydrogel was designed and synthesized by conjugates of glutamic acid-cysteine dendrimer with alginate () through click reaction, and then cross-linked with polyethylene glycol (PEG) through hydrogen bonds to form a 3D-net structure. The hydrogel, self-assembled by the inner disulfide bonds of the dendrimer, is designed to respond to the GSH heterogeneity in tumors, with a remarkably high drug loading capacity.

Structured oral examination as an effective assessment tool in lab-based physiology learning sessions.

Traditional oral examination (TOE) is criticized for the shortage of objectivity, standardization, and reliability. These perceived limitations can be mitigated by the introduction of structured oral examination (SOE). There is little evidence of the implementation of SOE in physiology laboratory courses.

subsp: bioassay-guided isolation and its chemical basis of antitumor cytotoxicity.

Inspired by the allelopathetic effects of subsp, bioassay-guided isolation was employed to identify its antitumor constituents and clarify the chemical basis of its multitarget activity. Among four fractions of extraction, TCM-fr and PE-fr were discovered to exhibit significant cytotoxicity aganist HepG two and A549 cells, which were further isolated by chromatographic methods to yield 16 compounds, including six active ones: xanthatin (), xanthinosin (), lupeol (), oleanolic acid (), betulinic acid () and emodin () with IC of 10 ∼ 120μM. The systematically study of antitumor constituents has firstly provided a chemical basis for the multitarget and synergistic anticancer activity of the genus .

Ellagic acid promotes browning of white adipose tissues in high-fat diet-induced obesity in rats through suppressing white adipocyte maintaining genes.

Promoting brown adipose tissue (BAT) formation and function reduces obesity. Ellagic Acid (EA), located abundantly in plant extracts and fruits, has been shown to modulate formation and differentiation of adipocytes, although its role in the process of browning of white adipose tissue (WAT) has not been elucidated. In this study, fifty-six five-week old SD rats were randomly assigned to receive normal diet (ND, 10% lipids) or high-fat diet (HFD, 60% lipid) with or without various dosages of EA for 24 weeks.

Promising Fungicides from Allelochemicals: Synthesis of Umbelliferone Derivatives and Their Structure⁻Activity Relationships.

Umbelliferone was discovered to be an important allelochemical in our previous study, but the contribution of its activity and structure has not yet been revealed. In this study, a series of analogues were synthesized to determine the skeleton of umbelliferone and examine its fungicidal activity. Furthermore, targeted modifications were conducted with three plant parasitic fungi to examine the lead compounds.

Endoplasmic Reticulum Stress Related Molecular Mechanisms in Nonalcoholic Fatty Liver Disease (NAFLD).

Non-alcoholic fatty liver disease (NAFLD) is a common public health issue and is considered a main drive for liver diseases. However, the basic mechanisms that trigger the development of NAFLD still remain somewhat elusive. Endoplasmic reticulum (ER) stress facilitates the unfolded protein response (UPR) and contributes to the etiology of steatosis, nonalcoholic steatohepatitis and ultimately hepatocarcinoma.

Low shear stress upregulates the expression of fractalkine through the activation of mitogen-activated protein kinases in endothelial cells.

: Fractalkine (FKN) is a cytokine which plays an important role in atherosclerosis and other inflammatory diseases. Studies have shown that FKN induces integrin-independent leukocyte adhesion to primary endothelial cells under physiological flow conditions. Further, increased expression of FKN has been demonstrated in atherosclerotic lesions induced by low shear stress.