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Lucie Navrátilová, Lenka Applová, Pavel Horký, Přemysl Mladěnka, Petr Pávek, František Trejtnar
Membrane organic anion-transporting polypeptides (OATPs) are responsible for the drug transmembrane transport within the human body. The function of OATP2B1 transporter can be inhibited by various natural compounds. Despite increased research interest in soya as a part of human diet, the effect of its active components to interact with hOATP2B1 has not been elucidated in a complex extent. This in vitro study examined the inhibitory effect of main soy isoflavones (daidzin, daidzein, genistin, genistein, glycitin, glycitein, biochanin A, formononetin) and their metabolites formed in vivo (S-equol, O-desmethylangolensin) towards human OATP2B1 transporter...
June 22, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Germán A Colareda, Alicia E Consolini
OBJECTIVES: Low-flow ischemia (LFI) is consequent to coronary disease and produces cardiac stunning during reperfusion (R). Energetic performance and mechanisms of Ca2+ handling during LFI/R are not known. Moreover, cardioprotection of the phytoestrogen genistein (Gen) remains to be demonstrated in LFI/R. The aim was to study the mechanisms of the stunning consequent to LFI/R and the effects of Gen on both sexes. METHODS: Rat ventricles were perfused inside a calorimeter to measure maximal pressure development (P) and total heat rate (Ht) before and during exposition to LFI/R...
June 21, 2018: Journal of Pharmacy and Pharmacology
Johanna Rienks, Janett Barbaresko, Kolade Oluwagbemigun, Matthias Schmid, Ute Nöthlings
Background: Type 2 diabetes is characterized by impaired glucose metabolism. Bioactive compounds in fruits and vegetables such as polyphenols have been suggested to influence glucose metabolism. Objective: The aim of the current study was to systematically review the literature and conduct dose-response meta-analyses to summarize evidence of polyphenol exposure in association with incident type 2 diabetes. Design: Prospective epidemiologic studies published before January 2018 were searched through 2 databases...
June 21, 2018: American Journal of Clinical Nutrition
H Hirata, Y Hinoda, V Shahryari, G Deng, Y Tanaka, Z L Tabatabai, R Dahiya
The authors report that there is a mistake in the representative picture of Fig. 4D (top row: PC3-miR1260b inh-0h) in the original version. The correct version of Fig. 4 with the original pictures for both PC3 miR-NC inh-0h and PC3-miR1260b inh-0h are provided below.
June 22, 2018: British Journal of Cancer
C F Ye, Y M Pan, H Zhou
The aim of this work was to study the mechanisms of vitamin D receptor (VDR) and Genistein (Gen) on the regulation of bone metabolism of phytoestrogens from cellular and epidemiological perspectives. MC3T3-E1 cells were treated with different concentrations of Gen, and the cell-proliferation rate was detected by an MTT colorimetric assay. The effect of the VDR receptor blocker ZK159222 on the Gen effect was then observed; after adding Gen to MC3T3-E1 cells, we detected the expression of VDR protein via Western blotting...
May 2018: Journal of Biological Regulators and Homeostatic Agents
Chantal Farmer
Milk yield is a crucial component of a sow operation because it is a limiting factor for piglet growth rate. Stimulating mammary development is one avenue that could be used to improve sow milk production. A number of studies have shown that nutrition of gilts or sows during the periods of rapid mammary accretion occurring during prepuberty, gestation, and lactation can affect mammary development. The present review provides an overview of all the information currently published on the subject and Table 1 summarizes the dietary treatments that enhance mammary development in pigs...
June 15, 2018: Journal of Animal Science
Qisheng Tang, Jianjun Ma, Jinbo Sun, Longfei Yang, Fan Yang, Wei Zhang, Ruixiao Li, Lei Wang, Yong Wang, He Wang
Radiosensitivity of prostate cancer (PCa) cells promotes the curative treatment for PCa. The present study was designed to investigate the synergistic effect of genistein and AG1024 on the radiosensitivity of PCa cells. The optimal X‑irradiation dose (4 Gy) and genistein concentration (30 µM) were selected by using the CCK‑8 assay. Before X‑irradiation (4 Gy), PC3 and DU145 cells were treated with genistein (30 µM), AG1024 (10 µM) and their combination. All treatments significantly reduced cell proliferation and enhanced cell apoptosis...
May 30, 2018: Oncology Reports
Bidisha Paul, Yuanyuan Li, Trygve O Tollefsbol
Dietary compounds that possess the properties of altering epigenetic processes are gaining popularity as targets for cancer prevention studies. These compounds when administered at optimal concentrations and especially in combination can have enhanced effects in cancer prevention or therapy. It is important to study the interaction of two or more compounds in order to assess their role in enhancing prevention. Genistein (GEN), found in soy, has been extensively studied for its role as an epigenetic modifier especially as a DNA methyltransferase (DNMT) inhibitor and sulforaphane (SFN), found in cruciferous vegetables, is known as a histone deacetylase (HDAC) inhibitor...
June 13, 2018: International Journal of Molecular Sciences
Roberta Ettari, Santo Previti, Santina Maiorana, Alessandro Allegra, Tanja Schirmeister, Silvana Grasso, Maria Zappalà
Curcumin and genistein are two natural products obtained from Curcuma longa L. and soybeans, endowed with many biological properties. Within the last years they were shown to possess also a promising antitrypanosomal activity. In the present paper, we investigated the activity of both curcumin and genistein against rhodesain, the main cysteine protease of Trypanosoma brucei rhodesiense; drug combination studies, according to Chou and Talalay method, allowed us to demonstrate a potent synergistic effect for the combination curcumin-genistein...
June 13, 2018: Natural Product Research
Alisa A Suen, Wendy N Jefferson, Carmen J Williams, Charles E Wood
Developmental exposure to estrogenic chemicals is an established risk factor for cancer of the female reproductive tract. This increase in risk has been associated with disruption of normal patterns of cellular differentiation during critical stages of morphogenesis. The goal of this study was to document uterine epithelial phenotypes over time following neonatal treatment with the synthetic estrogen diethylstilbestrol (DES) or the soy phytoestrogen genistein (GEN) in female CD-1 mice. Both DES and GEN induced three distinct populations of abnormal endometrial epithelial cells: luminal (SIX1+/P63-/CK14-/CK18+), basal (SIX1+/P63+/CK14+/CK18-), and mixed/bipotential (SIX1+/P63-/CK14+/CK18+), which were all established by early adulthood...
January 1, 2018: Toxicologic Pathology
Ming Zhang, Yujun Wu, Mengmeng Wang, Ying Wang, Raza Tausif, Ying Yang
Pulmonary vascular remodeling is an important pathological feature of pulmonary arterial hypertension (PAH), which is characterized by thickening of the medial smooth muscle layer. Hypertrophy of pulmonary artery smooth muscle cells (PASMCs) participates in the development of medial thickening. Genistein can attenuate PAH and inhibit medial thickening of pulmonary arteries. Since hypoxia is one of the main causes of pulmonary hypertension, this study aims to investigate the mechanism of genistein in inhibiting hypertrophic responses in PASMCs induced by hypoxia...
May 1, 2018: Journal of Nutritional Biochemistry
Jing Luo, Aihua Wang, Wei Zhen, Yao Wang, Hongwei Si, Zhenquan Jia, Hana Alkhalidy, Zhiyong Cheng, Elizabeth Gilbert, Bin Xu, Dongmin Liu
We previously discovered that phytonutrient genistein rapidly activates cAMP signaling in β-cells and improves islet mass in diabetic mice. However, the mechanism underlying these actions of genistein is still unclear. Here, we show that pharmacological or molecular inhibition of Gαs blocked genistein-stimulated adenylate cyclase activity in plasma membrane and intracellular cAMP production in INS1 cells and islets. Further, genistein stimulation of cAMP generation was abolished in islets exposed to a specific GPR30 inhibitor G15 or islets from GPR30 deficient (GPR30-/-) mice...
May 12, 2018: Journal of Nutritional Biochemistry
Yu-Zhen Zhang, Jiawei Zhang, Ling Tan, Zhining Xia, Chong-Zhi Wang, Lian-Di Zhou, Qihui Zhang, Chun-Su Yuan
Thermo-responsive magnetic molecularly imprinted polymers were prepared by simple surface molecular imprinting polymerization for the selective adsorption and enrichment of formononetin from Trifolium pretense by temperature regulation. Using formononetin as a template, N-isopropylacrylamide as the thermo-responsive functional monomer, and methacrylic acid as an assistant functional monomer, the polymers were synthesized on the surface of the magnetic substrate. The results show that imprinted polymers attained controlled adsorption of formononetin in response to the temperature change, with large adsorption capacity (16...
June 7, 2018: Journal of Separation Science
Carmen Sarasquete, María Úbeda-Manzanaro, Juan B Ortiz-Delgado
Based on the assumed oestrogenic and apoptotic properties of soya isoflavones (genistein, daidzein), and following the current OECD test-guidelines and principle of 3Rs, we have studied the potential toxicity of phytochemicals on the zebrafish embryos test (ZFET). For this purpose, zebrafish embryos at 2-3 h post-fertilisation (hpf) were exposed to both soya isoflavones (from 1.25 mg/L to 20 mg/L) and assayed until 96 hpf. Lethal and sub-lethal endpoints (mortality, hatching rates and malformations) were estimated in the ZFET, which was expanded to potential gene expression markers, determining the lowest observed effect (and transcriptional) concentrations (LOEC, LOTEC), and the no-observable effect (and transcriptional) concentrations (NOEC, NOTEC)...
June 2, 2018: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
Ming-Xian Ho, Christina C-W Poon, Ka-Chun Wong, Zuo-Cheng Qiu, Man-Sau Wong
Genistein and icariin are flavonoid compounds that exhibit estrogen-like properties in inducing bone formation and reducing bone loss associated with estrogen deficiency in both preclinical and clinical studies. However, the mechanisms that are involved in mediating their estrogenic actions in bone cells are far from clear. The present study aimed to study the signaling pathways that mediate the estrogenic actions of genistein and icariin in osteoblastic cells. The effects of genistein and icariin on the activation of estrogen receptor (ER) and the downstream mitogen-activated protein kinase (MAPK) and phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathway in murine osteoblastic MC3T3-E1 cells and rat osteoblastic UMR-106 cells were studied...
2018: Frontiers in Pharmacology
Wided Kouidhi, Raymond Bergès, Gaetan Drouin, Catherine Desmetz, Jacques Auger, Michèle El May, Marie Chantal Canivenc-Lavier
OBJECTIVES: We previously reported that maternal exposure to genistein, vinclozolin, ingested alone or in combination, affects submandibular salivary glands of rats' offspring's. Here, we investigated the responsiveness of submandibular gland when such xenohormone exposure occurs later in life. MATERIALS AND METHODS: Chemicals were given orally to male and female Wistar rats (1mg/kg body weight per day), from weaning to adulthood. Submandibular glands and plasma were collected at postnatal day 100 for histological and molecular analysis...
June 4, 2018: Oral Diseases
Xiaocong Pang, Weiqi Fu, Jinhua Wang, De Kang, Lvjie Xu, Ying Zhao, Ai-Lin Liu, Guan-Hua Du
Estrogen receptor α (ER α ) is a successful target for ER-positive breast cancer and also reported to be relevant in many other diseases. Selective estrogen receptor modulators (SERMs) make a good therapeutic effect in clinic. Because of the drug resistance and side effects of current SERMs, the discovery of new SERMs is given more and more attention. Virtual screening is a validated method to high effectively to identify novel bioactive small molecules. Ligand-based machine learning methods and structure-based molecular docking were first performed for identification of ER α antagonist from in-house natural product library...
2018: Oxidative Medicine and Cellular Longevity
Yan Zhang, Li-Ping Zhou, Xiao-Li Li, Yong-Jian Zhao, Ming-Xian Ho, Zuo-Cheng Qiu, Dong-Feng Zhao, Daniel Kam-Wah Mok, Qi Shi, Yong-Jun Wang, Man-Sau Wong
Our previous study reported that the in vitro osteogenic effects of 8-prenylgenistein (8PG) were more potent than its parent compound genistein. This study aimed to evaluate the osteoprotective effects of 8PG in ovariectomized (OVX) mice as well as to characterize its estrogenic effects in uterus. Mature OVX mice were treated with phytoestrogen-free diet containing 8PG or genistein. Trabecular bone mass and most of the micro-structural parameters were ameliorated at the distal femoral metaphysis in OVX mice upon treatment with genistein and both doses of 8PG...
May 11, 2018: Oncotarget
Yu-Si Liang, Wen-Tao Qi, Weiqun Guo, Chun-Ling Wang, Ze-Bin Hu, Ai-Ke Li
Aim: The purpose of this study was to investigate the possible mechanisms of genistein (GEN) and daidzein (DAI) in inducing apoptosis of colon cancer cells by inhibition of lipid droplets (LDs) accumulation. Methods: HT-29 cells were used and treated by GEN or DAI in this paper. LDs accumulation was induced and inhibited by oleic acid (OA) and C75, respectively. The expression changes of LDs-related markers were confirmed by semiquantitative real time-PCR (RT-PCR), Western blotting, and immunofluorescence staining...
2018: Food & Nutrition Research
Hongxue Shen, Dandan He, Shuxia Wang, Pinggang Ding, Jianan Wang, Jianming Ju
Genistein (GEN) is a natural dietary isoflavone, has been reported to show anticancer activities. However, its poor aqueous solubility and oral bioavailability limit its clinical application. We designed a novel genistein-loaded mixed micelles (GEN-M) system composed of Soluplus® and Vitamin E d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) were prepared by organic solvent evaporation aimed to overcome the challenges of GEN's poor solubility and then further improve its oral bioavailability. The optimized, spherical-shaped GEN-M was obtained at a ratio of 10:1 (Soluplus® :TPGS)...
May 31, 2018: Drug Development and Industrial Pharmacy
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