Genistein Up-Regulates the Expression of EGF and E-Cadherin in the Treatment of Senile Vaginitis

Investigating the therapeutic effect of genistein (Gen) on postmenopausal senile vaginitis (SV) and its mechanism of action. Adult SPF female Wistar rats were selected to establish a bilateral ovariectomized animal model (OVX), which simulated senile vaginitis dominated by estrogen deficiency in ovarian dysfunction. After 14 days of continuous treatment, the morphology of vaginal epithelial tissue was observed and various types of epithelial cells were counted, and the body mass and uterine and vaginal index of rats were measured. the levels of vaginal tissue secretion, microorganism, hormone and glycogen in each group were measured and the reproductive health was evaluated clinically. The protein expression and mRNA expression of epidermal growth factor (EGF) and E-cadherin (E-cadherin) in vaginal tissues were detected by immunohistochemistry and RT-PCR, respectively. Result showed that Genistein lowered vaginal pH, increased vaginal index and vaginal health score, thickened epithelial layers and improved vaginal tissue atrophy after administration. Genistein also increased the contents of glycogen and Lactobacillus in vagina, and promoted the expression of EGF, E-cadherin protein and mRNA. To sum up, there is no significant change in serum E2 and FSH levels, indicating that genistein has no effect on hormone levels in rats. genistein promoted the proliferation of vaginal epithelial cells, thickened epithelial layers and the vaginal wall, which improved the resistance of vaginal epithelium, the recovery of self-cleaning ability and healed the vaginal wound and erosive surface to improve atrophy.     

In vivo effects of PCB-126 and genistein on vitellogenin expression in zebrafish

In this study, the vitellogenin (Vtg) modulation by genistein and polychlorinated biphenyl-126 (PCB-126) exposure in zebrafishes has been investigated. Both PCB-126 and genistein have been identified as aquatic pollutants and can further increase estrogenicity of waterways. Vtg is egg yolk precursor protein release by the hepatocytes during vitellogenesis. This process occurs normally in the hepatocytes in response to the activation with the estrogens such as 17-β-estradiol. Our immunohistochemical findings showed a Vtg expression that increases at 12 h and at 72 h in the liver of treated fishes with both PCB-126 and genistein, individually and in combination. Furthermore, for the first time, also hepatic stellate cells (HSC) in the liver parenchyma were strongly positive for vitellogenin.     

黄连素-染料木素有机盐水合物的制备、晶体结构及溶解性

合成了黄连素和染料木素的有机盐水合物[C₂₀H₁₈NO₄]⁺·[C₁₅H₉O₅]^-·2.5H₂O·0.5(C₂H₅OH),并测定了其晶体结构。 解析结果表明,该有机盐水合物属于单斜晶系,P2₁/c空间群。 染料木素7取代位的羟基失去了质子变成了染料木素阴离子。 羟基阴离子与4'取代位上的羟基形成了O—H••••O^-氢键,产生了一维的氢键链状结构。 两个水分子通过氢键作用形成了链状结构,并与染料木素阴离子形成二维的氢键结构。 加热失去水分子后,有机盐水合物变成无定型状态。 在乙醇水溶液中悬浮后,无定型可以转变成结晶的水合物结构。 形成黄连素-染料木素有机盐水合物后,染料木素在水中的溶解度略有增加。     

Potential Effects of Soy Isoflavones on the Prevention of Metabolic Syndrome

Isoflavones are polyphenols primarily contained in soybean. As phytoestrogens, isoflavones exert beneficial effects on various chronic diseases. Metabolic syndrome increases the risk of death due to arteriosclerosis in individuals with various pathological conditions, including obesity, hypertension, hyperglycemia, and dyslipidemia. Although the health benefits of soybean-derived isoflavones are widely known, their beneficial effects on the pathogenesis of metabolic syndrome are incompletely understood. This review aims to describe the association between soybean-derived isoflavone intake and the risk of metabolic syndrome development. We reviewed studies on soy isoflavones, particularly daidzein and genistein, and metabolic syndrome, using PubMed, ScienceDirect, and Web of Science. We describe the pathological characteristics of metabolic syndrome, including those contributing to multiple pathological conditions. Furthermore, we summarize the effects of soybean-derived daidzein and genistein on metabolic syndrome reported in human epidemiological studies and experiments using in vitro and in vivo models. In particular, we emphasize the role of soy isoflavones in metabolic syndrome-induced cardiovascular diseases. In conclusion, this review focuses on the potential of soy isoflavones to prevent metabolic syndrome by influencing the onset of hypertension, hyperglycemia, dyslipidemia, and arteriosclerosis and discusses the anti-inflammatory effects of isoflavones.     

Health Effects of Soy Isoflavones and Green Tea Catechins on Cancer and Cardiovascular Diseases Based on Urinary Biomarker Levels

Plant polyphenols have various health effects. Genistein, which is abundant in soybeans, and epigallocatechin-3-gallate, which is abundant in green tea, are major flavonoids, a subclass group of polyphenols. Several epidemiological studies have shown that these flavonoids have beneficial effects against cancer and cardiovascular diseases. However, other studies did not show such effects. Several confounding factors, including recall bias, are related to these inconsistent findings, and the determination of metabolites in the urine may be useful in reducing the number of confounding factors. Equipment, which can be used by research participants to collect samples from a portion of voided urine within 24 h without the help of medical workers, has been developed for epidemiological investigations. Previous studies, in which flavonoid metabolites in these urine samples were measured, revealed that soy intake was correlated with a reduced risk of certain types of cancer and cardiovascular diseases worldwide. Although soybeans and green tea consumption may have protective effects against cancer and cardiovascular diseases, further clinical studies that consider different confounding factors are required to provide evidence for the actual impact of dietary flavonoids on human diseases, including cancer and cardiovascular diseases. One possible mechanism involved is discussed in relation to the downregulation of reactive oxygen species and the upregulation of 5′-adenosine monophosphate-activated protein kinase elicited by these flavonoids.     

Development of Genistein Drug Delivery Systems Based on Bacterial Nanocellulose for Potential Colorectal Cancer Chemoprevention: Effect of Nanocellulose Surface Modification on Genistein Adsorption

Genistein is an isoflavone with antioxidant, anti-inflammatory, and anticancer properties. That said, its use in the industry is limited by its low solubility in aqueous systems. In this work, bacterial nanocellulose (BNC) and BNC modified with cetyltrimethylammonium (BNC-CTAB) were evaluated as genistein-encapsulating materials for their controlled release in cancer chemoprevention. Thin films were obtained and characterized by contact angle, AFM, TEM, UV–Vis spectroscopy FTIR, and TGA techniques to verify surface modification and genistein encapsulation. The results show a decrease in hydrophilization degree and an increase in diameter after BNC modification. Furthermore, the affinity of genistein with the encapsulating materials was determined in the context of monolayer and multilayer isotherms, thermodynamic parameters and adsorption kinetics. Spontaneous, endothermic and reversible adsorption processes were found for BNC-GEN and BNC-CTAB-GEN. After two hours, the maximum adsorption capacity corresponded to 4.59 mg GEN∙g⁻¹ BNC and 6.10 mg GEN∙g⁻¹ BNC-CTAB; the latter was a more stable system. Additionally, in vitro release assays performed with simulated gastrointestinal fluids indicated controlled and continuous desorption in gastric and colon fluids, with a release of around 5% and 85%, respectively, for either system. Finally, the IC50 tests made it possible to determine the amounts of films required to achieve therapeutic concentrations for SW480 and SW620 cell lines.     

Synthesis and Crystal Structure of a Genistein-derived Compound

A genistein derivative, 5-hydroxy-3-（4-hydroxyphenyl）-7-（2-（piperidin- 1-yl）ethoxy）- 4H-chromen-4-one 3, was designed, prepared and structurally characterized by single-crystal X-ray diffraction. X-ray structure analysis reveals that 3 crystallizes in the orthorhombic system, space group Pbca, with a = 16.238（3）, b = 10.308（2）, c = 22.987（5）A, V = 3847.6（13）A3, Z = 8,μ= 0.093 mm^-1, Dc = 1.317 g/cm^3, F（000） = 1616, R = 0.0789 and wR = 0.1554 for 1463 observed reflections with I 〉 2σ（I）.     

Simultaneous estimation of genistein and daidzein in Pueraria tuberosa (Willd.) DC by validated high-performance thin-layer chromatography (HPTLC) densitometry method

The present study was performed to estimate the concentration of genistein and daidzein in ethanol extract of tubers of Pueraria tuberosa (Indian kudzu or Vidarikanda) and its various fractions (n-hexane, ethyl acetate, n-butanol, and aqueous) by high-performance thin-layer chromatography (HPTLC). The separation of bioactive compounds was performed using mobile phase, toluene:ethyl acetate:acetone:formic acid (20.0:4.0:2.0:1.0) and detected at wavelength 269?nm. The method was validated for linearity, accuracy, precision, limit of detection (LOD), limit of quantification (LOQ), etc. by International Conference on Harmonization guidelines. The calibration range was found to be 100–600?ng/band for both the bioactive compounds. Daidzein was separated with an R_f value of 0.39?±?0.02 and genistein with an R_f value of 0.54?±?0.02. Average recovery was 99.96 and 99.90% for genistein and daidzein, respectively. The LOD and LOQ were 14.786 and 44.805?ng, respectively, for genistein, and 9.607 and 29.114?ng, respectively, for daidzein. Both the phytoconstituents were found in ethanol extract and its ethyl acetate fraction only. The developed HPTLC method was simple, precise, robust, specific, rapid, and cost effective and could be used for quality control analysis and quantification of genistein and daidzein in different herbal formulations containing the plant species.     

Genistein: A Potential Natural Lead Molecule for New Drug Design and Development for Treating Memory Impairment

Genistein is a naturally occurring polyphenolic molecule in the isoflavones group which is well known for its neuroprotection. In this review, we summarize the efficacy of genistein in attenuating the effects of memory impairment (MI) in animals. Scopus, PubMed, and Web of Science databases were used to find the relevant articles and discuss the effects of genistein in the brain, including its pharmacokinetics, bioavailability, behavioral effects, and some of the potential mechanisms of action on memory in several animal models. The results of the preclinical studies highly suggested that genistein is highly effective in enhancing the cognitive performance of the MI animal models, specifically in the memory domain, including spatial, recognition, retention, and reference memories, through its ability to reduce oxidative stress and attenuate neuroinflammation. This review also highlighted challenges and opportunities to improve the drug delivery of genistein for treating MI. Along with that, the possible structural modifications and derivatives of genistein to improve its physicochemical and drug-likeness properties are also discussed. The outcomes of the review proved that genistein can enhance the cognitive performance and ameliorate MI in different preclinical studies, thus indicating its potential as a natural lead for the design and development of a novel neuroprotective drug.     

Separation and determination of isoflavones in red clover by micellar electrokinetic capillary chromatography

A micellar electrokinetic capillary chromatography (MECC) method has been developed for the determination of the four isoflavones, i.e. biochanin A, formononetin, genstein and daidzein in red clover (Trifolium Pratense L.). The effect of running buffer pH and concentration were investigated. An electrolyte composed of 30 mm borate, 20 mm sodium dodecyl sulfate (SDS) and 4 mg/mL HP-beta-CD containing 5% (v/v) ethanol at pH 10.1 provides a satisfactory separation for all the analytes. The applied voltage was 25 kV, and the capillary temperature was kept constant at 25 degrees C with a UV detection at 254 nm. The relative standard deviations (RSD) of the migration time and peak area were less than 1.73 and 3.94% (intra-day), and 2.29 and 4.38% (inter-day), respectively, under the optimized separation conditions. Regression equations revealed a good linear relationship between the peak area of each compound and its concentration. The contents of the four compounds in red clover were successfully determined with satisfactory repeatability and recovery.