Influence of the type and concentration of hydrocolloids on Ostwald ripening of emulsions stabilized with small molecular and non-ionic surfactants.

The effects of hydrocolloid gum, gum arabic, carrageenan, and xanthan on the Ostwald ripening of emulsions fabricated using Brij or Tween surfactants were examined. Emulsions prepared using pure n-decane exhibited low stability to Ostwald ripening, and modifying the oil composition by mixing corn oil improved the stability to Ostwald ripening. When gums were added to emulsions prepared using pure n-decane, the stability to Ostwald ripening decreased further, except for xanthan in emulsions stabilized using Tween surfactant. This could be because gums may affect interactions between water molecules and the hydrophilic head of the surfactant, increasing the water solubility of n-decane. However, gum addition (or viscosity increment) increased the stability of emulsions prepared using the modified oil composition (90% n-decane and 10% corn oil). In conclusion, emulsions unstable to Ostwald ripening may be negatively affected by gum addition, whereas emulsions relatively stable to Ostwald ripening may be positively affected.

The Effect of Korean Red Ginseng on Bisphenol A-Induced Fatty Acid Composition and Lipid Metabolism-Related Gene Expression Changes.

Bisphenol A (BPA), which is known to be an endocrine-disrupting chemical (EDC), is associated not only with estrogen activity and reproductive toxicity but also with a variety of metabolic disorders. BPA affects glucose tolerance, cholesterol biosynthesis, and fatty acid synthesis. Ginseng is a traditional medicinal plant that has been widely used in East Asia for more than 2000 years, and a number of health effects have been reported. Korean Red Ginseng (KRG) has also been shown to have effects on lipid metabolism and body weight reduction in vivo in obese mice. In this study, we administered BPA and KRG to ovariectomized (OVX) ICR mice. BPA (800 mg/kg/day) and KRG (1.2 g/kg/day) were orally administered to OVX mice for 3 days. KRG inhibited the increase in total fatty acid level by BPA as determined by lipid profiling in the liver of OVX mice. In addition, transcriptome analysis showed that KRG inhibited BPA-induced changes in lipid metabolic process-related genes. Our findings suggest that KRG can regulate BPA-induced changes in lipid metabolism.

Ginseng on Nuclear Hormone Receptors.

The first record of ginseng use dates back over two millennia, and ginseng is now popular in more than 35 countries. Ginsenosides are the pharmacological constituents responsible for the beneficial effects of ginseng. There is increasing evidence that ginseng and its bioactive ingredients are involved in the regulation of nuclear receptors, molecules that act in response to the specific binding of hormones, which link to a diverse array of signaling pathways, such as the ERK and PI3K/Akt pathways. Knowledge of the mechanism of how ginseng mediates these complexes is essential for the development of multi-target phytomedicine as possible therapy for different diseases. Here, we discuss the literature on the effects of ginseng and its constituents on estrogen, glucocorticoid, peroxisome proliferator-activated, and androgen nuclear hormone receptors, as well as how ginseng and its constituents exert their biological function in the treatment of cancer, obesity, and cardiovascular and neurological disorders. The accumulated results definitely show that the nuclear receptors are cellular targets of ginsenosides, but more rigorous data are required to establish and provide a scientific basis to confirm the suggested efficacy of ginseng or products with ginsenosides.

4,5-Di-O-Caffeoylquinic Acid from Ligularia fischeri Suppresses Inflammatory Responses Through TRPV1 Activation.

Ligularia fischeri (Ledeb.) Turcz., a perennial plant native to northeastern Asia, has long been used as folk remedies for the alleviation of inflammatory symptoms. We investigated whether the extract of L. fischeri (LFEx) and caffeoylquinic acid (CQA) derivatives, the pharmacologically active ingredients identified from L. fischeri, regulate inflammation via a transient receptor potential vanilloid 1 (TRPV1)-mediated pathway. Changes in intracellular Ca2+ levels to the LFEx and trans-5-O-CQA, 3,4-di-O-CQA, 3,5-di-O-CQA, and 4,5-di-O-CQA were monitored in TRPV1-expressing human embryonic kidney cell HEK 293T. LFEx and 4,5-di-O-CQA (EC50  = 69.34 ± 1.12 µM) activated TRPV1, and these activations were significantly inhibited by ruthenium red, a general blocker of TRP channels, and capsazepine, a specific antagonist of TRPV1. 4,5-Di-O-CQA has been determined having antiinflammatory effect under hypoxic conditions by detecting the expression of cyclooxygenase-2 (COX-2), a representative inflammatory marker, and cellular migration in human pulmonary epithelial A549 cells. 4,5-Di-O-CQA suppressed COX-2 expression and cell migration, and this inhibition was countered by co-treatment with capsazepine. This study provides evidence that L. fischeri is selective to inflammatory responses via a TRPV1-mediated pathway, and 4,5-di-O-CQA might play a key role to create these effects. Copyright © 2017 John Wiley & Sons, Ltd.

Effects of ginseng on two main sex steroid hormone receptors: estrogen and androgen receptors.

Ginseng has been used in China for at least two millennia and is now popular in over 35 countries. It is one of the world's popular herbs for complementary and alternative medicine and has been shown to have helpful effects on cognition and blood circulation, as well as anti-aging, anti-cancer, and anti-diabetic effects, among many others. The pharmacological activities of ginseng are dependent mainly on ginsenosides. Ginsenosides have a cholesterol-like four trans-ring steroid skeleton with a variety of sugar moieties. Nuclear receptors are one of the most important molecular targets of ginseng, and reports have shown that members of the nuclear receptor superfamily are regulated by a variety of ginsenosides. Here, we review the published literature on the effects of ginseng and its constituents on two main sex steroid hormone receptors: estrogen and androgen receptors. Furthermore, we discuss applications for sex steroid hormone receptor modulation and their therapeutic efficacy.

Methyl syringate, a TRPA1 agonist represses hypoxia-induced cyclooxygenase-2 in lung cancer cells.

BACKGROUND: We have previously found that methyl syringate is a specific and selective agonist of the human transient receptor potential channel ankyrin 1 (TRPA1) and suppresses food intake and gastric emptying in imprinting control region mice. Because TRPA1 has been implicated in inflammatory responses, and inflammation and tumorigenesis are stimulated by the cyclooxygenase-2 (COX-2)/prostaglandin E2 pathway in hypoxic cancer cells. PURPOSE: This study examined the effects of methyl syringate on hypoxia-induced COX-2 in human distal lung epithelial A549 cells. STUDY DESIGN: The effect of the methyl syringate on suppression of hypoxia-induced COX-2 in A549 cells were determined by Western blot and/or quantitative real-time polymerase chain reaction. The anti-invasive effect of methyl syringate was evaluated on A549 cells using matrigel invasion assay. RESULTS: Methyl syringate suppressed hypoxia-induced COX-2 protein and mRNA expression and promoter activity and reduced hypoxia-induced cell migration and invasion and secretion of vascular endothelial growth factor. These effects were antagonized by a TRPA1 antagonist, implying their mediation by the TRPA1 pathway. CONCLUSION: Together, these results indicate that methyl syringate inhibits the hypoxic induction of COX-2 expression and cell invasion through TRPA1 activation. These findings suggest that methyl syringate could be effective to suppress hypoxia-induced inflammation and indicate an additional functional effect of methyl syringate.

Estrogen receptor mediated effects of Cimicifuga extracts on human breast cancer cells.

Cimicifuga racemosa extracts have long been used to treat female reproductive disorders both in Asia and Europe. Here in this study, we examined the possible estrogen receptor (ER)alpha effects of Cimicifuga heracleifolia var. bifida ethanol extract (C-Ex), which has been used traditionally in Asia, in MCF-7 cells. The activity of C-Ex was characterized in a transient transfection system, using ERa and estrogen-responsive luciferase plasmids in HEK 293 cells and endogenous target genes were studied in MCF-7 cells. C-Ex failed to activate ERalpha and at a concentration of 0.005-0.5 mg/ml as examined by reporter activity. In addition, no statistically significant antiestrogenic activity was observed. However, to our interest, C-Ex enhanced expression of VEGF at 0.5 mg/ml concentration and repressed ERalpha both at the mRNA and protein levels in MCF-7 cells. These results suggested that C-Ex does not activate or inactivate ERalpha in a direct manner, but the extracts may affect factors in ER signal transduction pathway.

Activation of Estrogen Receptor by Bavachin from Psoralea corylifolia.

In this study, we examined the estrogenic activity of bavachin, a component of Psoralea corylifolia that has been used as a traditional medicine in Asia. Bavachin was purified from ethanolic extract of Psoralea corylifolia and characterized its estrogenic activity by ligand binding, reporter gene activation, and endogenous estrogen receptor (ER) target gene regulation. Bavachin showed ER ligand binding activity in competitive displacement of [(3)H] E2 from recombinant ER. The estrogenic activity of bavachin was characterized in a transient transfection system using ERα or ERß and estrogen-responsive luciferase plasmids in CV-1 cells with an EC50 of 320 nM and 680 nM, respectively. Bavachin increased the mRNA levels of estrogen-responsive genes such as pS2 and PR, and decreased the protein level of ERα by proteasomal pathway. However, bavachin failed to activate the androgen receptor in CV-1 cells transiently transfected with the corresponding receptor and hormone responsive reporter plasmid. These data indicate that bavachin acts as a weak phytoestrogen by binding and activating the ER.