An Antennae-Enriched Odorant-Binding Protein EonuOBP43 Mediate the Behavioral Response of the Tea Green Leafhopper, Empoasca onukii Matsuda to the Host and Nonhost Volatiles.

Olfaction is crucial for Empoasca onukii Matsuda to recognize odors from the host and nonhost plants, and it has been proposed that odorant binding proteins are directly required for odorant discrimination and represent potential targets of interest for pest control. Here, we cloned EonuOBP43 and expressed the recombinant EonuOBP43 protein. Furthermore, competitive fluorescence binding assays with 19 ligands indicated that terpenoids and alkanes showed a relatively higher than for other classes of chemicals. Additionally, ligand docking and site-directed mutagenesis results revealed that seven hydrophobic residues, including Val-86, Met-89, Phe-90, Ile-104, Ile-105, Leu-130, and Val-134, played a key role in the binding of EonuOBP43 to plant volatiles. In olfactometer tests, E. onukii were significantly attracted to α-farnesene and repelled to ß-caryophyllene, and dsOBP43 treated adult lost response to α-farnesene and ß-caryophyllene. In summary, our results demonstrated that EonuOBP43 may function as a carrier in the process of sensing plant compounds of E. onukii.

Actinidia chinensis Planch. root extract inhibits the proliferation, migration and invasion of breast cancer cells via the AKT/GSK-3ß signaling pathway.

INTRODUCTION: Actinidia chinensis Planch. root extract (acRoots), known as a traditional Chinese medicine (TCM), has shown antitumor efficacy in various types of human cancers. However, its role and underlying mechanisms in breast cancer (BCa) have not been elucidated. MATERIAL AND METHODS: In the present study, the effects of acRoots on cell viability, apoptosis, migration and invasion were analyzed by MTT assay, colony formation, flow cytometry, wound healing and Transwell assay in MDA-MB-231 and MDA-MB-453 breast cancer cell lines. The expression levels of relevant proteins were determined by Western blot assay. RESULTS: The results revealed that acRoots inhibited proliferation, migration, and invasion and promoted apoptosis of BCa cells. Moreover, acRoots decreased the expression of cyclin D1, survivin, Bcl-2, N-cadherin, and Snail and increased the expression of Bax and E-cadherin in MDA-MB-231 and MDA-MB-453 cells. AcRoots inhibited the AKT/GSK-3b pathway by decreasing the levels of phosphorylated AKT, phosphorylated GSK-3b and b-catenin. CONCLUSIONS: The described effects of acRoots on the cultured BCa cells suggest that they may be mediated by the inhibition of the AKT/GSK-3b signaling pathway. Thus, further studies are warranted to test the possibility that AcRoots may be used as a promising anticancer agent for breast cancer treatment.

Discovery and anti-diabetic effects of novel isoxazole based flavonoid derivatives.

3-O-[(E)-4-(4-cyanophenyl)-2-oxobut-3-en-1-yl] kaempferol is a novel lead compound to discover anti-diabetic and anti-obesity drugs. The present study reported the scaffold hopping of the lead compound to obtain a new isoxazole derivative, C45, which has improved glucose consumption at the nanomolar level (EC50 = 0.8 nM) in insulin resistant (IR) HepG2 cells. Western blotting showed that C45 markedly enhanced the phosphorylation of AMPK (AMP-activated protein kinase) and reduced the levels of the gluconeogenesis key enzymes PEPCK (phosphoenolpyruvate carboxykinase) and G6Pase (glucose 6-phosphatase) in HepG2 cells. The potential molecular mechanism of C45 may be activation of the AMPK/PEPCK/G6Pase pathways. We concluded that C45 might be a valuable candidate to discover anti-diabetic drugs.

Antidepressant-like effect of the saponins part of ethanol extract from SHF.

ETHNOPHARMACOLOGICAL RELEVANCE: Suanzaorenhehuan Formula (SHF) has been used for treating depression-like disorders for many years in China. The saponins part of the SHF (SSHF) extract was the antidepressant effective component. AIM OF STUDY: To investigate the antidepressant-like effect of SSHF and its possible mechanisms. MATERIALS AND METHODS: Experimental approaches including the forced swim test (FST), the tail suspension test (TST) and unpredictable chronic mild stress (UCMS) were used to evaluate the effects of SSHF. The possible mechanisms were explored by measuring monoamine neurotransmitter in mice frontal cortex and hippocampus, testing monoamine oxidase enzyme (MAO) activities, antioxidant enzyme activities and free radicals levels in the brains of UCMS-exposed mice. RESULTS: The results showed that SSHF (10, 20, 40mg/kg) significantly decreased the immobility period in FST and TST in mice after two-week treatment. Whereas, SSHF had no significant effect on locomotor activity in mice. It was also found that the serotonin (5-HT) and noradrenaline (NE) levels in the hippocampus and frontal cortex were significantly increased only in 40mg/kg SSHF treated mice. In addition, SSHF (10, 20, 40mg/kg) significantly inhibited monoamine oxidase-A (MAO-A) and monoamine oxidase-B (MAO-B) after 21-day UCMS exposure. SSHF (10, 20, 40mg/kg) significantly decreased the nitrous oxide (NO) levels, and increased the activities of total antioxidant capability (T-AOC), glutathione peroxidase (GSH-PX), and catalase (CAT) in different degrees in the brains of UCMS-exposed mice. CONCLUSIONS: Our results suggested that SSHF may effectively produce an antidepressant-like effect, which appeared to involve the serotonergic, noradrenergic, monoamine oxidase enzyme and antioxidant systems.

Flavonoids from Tetrastigma obtectum enhancing glucose consumption in insulin-resistance HepG2 cells via activating AMPK.

Four new flavonoids including three C-glycosidic flavonoids, named tetrastigma A-D (1-4) and five known flavones (5-9) were isolated from the herbs of Tetrastigma obtectum (Wall.) Planch. The structures of 1-4 were elucidated by 1D- and 2D-NMR and HR mass spectrometric methods. Compound 1 caused significant enhancement in glucose consumption by insulin-resistant HepG2 cells compared with control cells. In addition, compound 1 stimulated phosphorylation of AMPK, which plays an important role in glycometabolism.

[A new flavanol glycoside from Phymatopteris hastata with effect on glucose metabolism].

By repeated column chromatography, including silica gel, macroporous resin, and preparative HPLC, a new compound (1) was isolated and purified. On the basis of spectroscopic methods, the structure of 1 was elucidated as ( - ) -epiafzelechin-3, 5-di-O-beta-D-apiofuranoside (1). In the bioassay screening experiments, glucose consumption assays in IR HepG2 cells and colorimetric assay of surface GLUT4myc translocation were used to assess the effects on glucose metabolism of compound 1. Both compound 1 and its derivatives--naringin could improve glucose consumption in IR HepG2 cells and enhance GLUT4 translocation in skeletal muscle cell L6myc in a dose-dependent manner, indicating that these two compouds showed potential anti-diabetic activities in vitro.

Alkaloids from Pachysandra terminalis inhibit breast cancer invasion and have potential for development as antimetastasis therapeutic agents.

The aim of the present study was to identify potentially useful natural compounds for the development of novel therapeutic agents to inhibit metastasis. A phytochemical investigation of Pachysandra terminalis resulted in the isolation of seven new pregnane alkaloids, terminamines A-G (1-7), and seven known alkaloids (8-14). The structures of 1-7 were elucidated by 1D- and 2D-NMR spectroscopic and mass spectrometric methods. Compounds 1-5 and 8-14 inhibited the migration of MB-MDA-231 breast cancer cells induced by the chemokine epithelial growth factor. In addition, compound 1 inhibited phosphorylation of integrin ß(1), which plays an important role in MB-MDA-231 cell adhesion and metastasis.

Synthesis and biological activity of novel tiliroside derivants.

A series of new tiliroside derivatives were synthesized and characterized by analytical (1)H NMR, (13)C NMR and mass spectrometry. All of the compounds were evaluated for anti-diabetic properties in vitro using HepG2 cells. Compounds 3c, 3d, and 3i-l caused significant enhancements in glucose consumption by insulin-resistant HepG2 cells compared with control cells and cells that were exposed to metformin (an anti-diabetic drug). Moreover, compound 3l significantly activated adenosine 5'-monophosphate-activated protein kinase activity and reduced acetyl-CoA carboxylase activity. Thus, the tiliroside derivative 3l offers potential to be developed as a new approach for treating type II diabetes.