白藜芦醇的有机合成方法

白藜芦醇是抗肿瘤剂和治疗心血管疾病的有效成份，可以广泛应用于医药、保健品、食品、化妆品等领域，白藜芦醇的制备、开发引起国内外医药、食品、材料等领域的关注。本文综述近年白藜芦醇的有机合成研究进展。     

The Role of Obesity and Diabetes in Dementia

Chronic conditions such as obesity, diabetes, and dementia are increasing in the United States (US) population. Knowledge of these chronic conditions, preventative measures, and proper management tactics is important and critical to preventing disease. The overlap between obesity, diabetes, and dementia is becoming further elucidated. These conditions share a similar origin through the components of increasing age, gender, genetic and epigenetic predispositions, depression, and a high-fat Western diet (WD) that all contribute to the inflammatory state associated with the development of obesity, diabetes, and dementia. This inflammatory state leads to the dysregulation of food intake and insulin resistance. Obesity is often the cornerstone that leads to the development of diabetes and, subsequently, in the case of type 2 diabetes mellitus (T2DM), progression to “type 3 diabetes mellitus (T3DM)”. Obesity and depression are closely associated with diabetes. However, dementia can be avoided with lifestyle modifications, by switching to a plant-based diet (e.g., a Mediterranean diet (MD)), and increasing physical activity. Diet and exercise are not the only treatment options. There are several surgical and pharmacological interventions available for prevention. Current and future research within each of these fields is warranted and offers the chance for new treatment options and a better understanding of the pathogenesis of each condition.     

Role of ANGPTL8 in NAFLD Improvement after Bariatric Surgery in Experimental and Human Obesity

Angiopoietin-like protein 8 (ANGPTL8) is an hepatokine altered in several metabolic conditions, such as obesity, type 2 diabetes, dyslipidemia and nonalcoholic fatty liver disease (NAFLD). We sought to explore whether ANGPTL8 is involved in NAFLD amelioration after bariatric surgery in experimental models and patients with severe obesity. Plasma ANGPTL8 was measured in 170 individuals before and 6 months after bariatric surgery. Hepatic ANGPTL8 expression was evaluated in liver biopsies of patients with severe obesity undergoing bariatric surgery with available liver pathology analysis (n = 75), as well as in male Wistar rats with diet-induced obesity subjected to sham operation, sleeve gastrectomy or Roux-en-Y gastric bypass (RYGB) (n = 65). The effect of ANGPTL8 on lipogenesis was assessed in human HepG2 hepatocytes under palmitate-induced lipotoxic conditions. Plasma concentrations and hepatic expression of ANGPTL8 were increased in patients with obesity-associated NAFLD in relation to the degree of hepatic steatosis. Sleeve gastrectomy and RYGB improved hepatosteatosis and reduced the hepatic ANGPTL8 expression in the preclinical model of NAFLD. Interestingly, ANGPTL8 inhibited steatosis and expression of lipogenic factors (PPARG2, SREBF1, MOGAT2 and DGAT1) in palmitate-treated human hepatocytes. Together, ANGPTL8 is involved in the resolution of NAFLD after bariatric surgery partially by the inhibition of lipogenesis in steatotic hepatocytes.     

Inhibition of Citrinin-Induced Apoptotic Biochemical Signaling in Human Hepatoma G2 Cells by Resveratrol

The mycotoxin citrinin (CTN), a natural contaminant in foodstuffs and animal feeds, exerts cytotoxic and genotoxic effects on various mammalian cells. CTN causes cell injury, including apoptosis, but its precise regulatory mechanisms of action are currently unclear. Resveratrol, a member of the phytoalexin family found in grapes and other dietary plants, possesses antioxidant and anti-tumor properties. In the present study, we examined the effects of resveratrol on apoptotic biochemical events in Hep G2 cells induced by CTN. Resveratrol inhibited CTN-induced ROS generation, activation of JNK, loss of mitochondrial membrane potential (MMP), as well as activation of caspase-9, caspase-3 and PAK2. Moreover, resveratrol and the ROS scavengers, NAC and α-tocopherol, abolished CTN-stimulated intracellular oxidative stress and apoptosis. Active JNK was required for CTN-induced mitochondria-dependent apoptotic biochemical changes, including loss of MMP, and activation of caspases and PAK2. Activation of PAK2 was essential for apoptosis triggered by CTN. These results collectively demonstrate that CTN stimulates ROS generation and JNK activation for mitochondria-dependent apoptotic signaling in Hep G2 cells, and these apoptotic biochemical events are blocked by pretreatment with resveratrol, which exerts antioxidant effects.     

The Inflammatory Profile of Obesity and the Role on Pulmonary Bacterial and Viral Infections

Obesity is a globally increasing health problem, entailing diverse comorbidities such as infectious diseases. An obese weight status has marked effects on lung function that can be attributed to mechanical dysfunctions. Moreover, the alterations of adipocyte-derived signal mediators strongly influence the regulation of inflammation, resulting in chronic low-grade inflammation. Our review summarizes the known effects regarding pulmonary bacterial and viral infections. For this, we discuss model systems that allow mechanistic investigation of the interplay between obesity and lung infections. Overall, obesity gives rise to a higher susceptibility to infectious pathogens, but the pathogenetic process is not clearly defined. Whereas, viral infections often show a more severe course in obese patients, the same patients seem to have a survival benefit during bacterial infections. In particular, we summarize the main mechanical impairments in the pulmonary tract caused by obesity. Moreover, we outline the main secretory changes within the expanded adipose tissue mass, resulting in chronic low-grade inflammation. Finally, we connect these altered host factors to the influence of obesity on the development of lung infection by summarizing observations from clinical and experimental data.     

The Multiple Mechanisms of Cell Death Triggered by Resveratrol in Lymphoma and Leukemia

Lymphoma and leukemia represent a serious threat to human health and life expectancy. Resveratrol is, among the natural-derived chemopreventive molecules, one of the most effective and better studied. In this paper the main mechanisms of cell death triggered by- or linked to- resveratrol are reviewed and discussed. The main focus is on lymphoma and leukemia experimental models where resveratrol has been tested and investigated at the cellular, molecular or physiological levels. The most relevant in vivo challenges involving resveratrol are also reported and analyzed in order to define the key features of this polyphenol and the potential for the treatment of hematologic tumors.     

高效液相色谱法测定葡萄酒和葡萄干中白藜芦醇的含量

采用Kromasil C18（250 mm×4.6 mm,5μm）色谱柱,乙腈-水（36∶64）体系流动相。用二级管阵列检测器在306 nm波长处检测,得白藜芦醇的保留时间约为7.3 min,检出限为0.020 3μg。测得红葡萄酒中白藜芦醇含量在1.21-3.44 mg/L,葡萄干中白藜芦醇含量在21.6-52.2μg/g。     

白藜芦醇及其类似化合物研发前景简

以白藜芦醇为先导化合物,通过结构修饰提高其生物活性,以及设计合理的药物传输系统以提高活性物质的生物利用度是当今的研究热点之一.文章对白藜芦醇的结构修饰及提高生物利用度的研究做了系统地评述.     

高效液相色谱法快速测定红酒中的白藜芦醇含量

文章建立了高效液相色谱法测定红酒中白藜芦醇的方法,色谱柱为Agilent ZORBAX Eclipse XDB C18(4.6 mm×250 mm,5μm),以乙腈-水(35∶65,水相中含0.1%冰乙酸)为流动相,流速1 mL/min,进样量20μL,室温,检测波长300 nm,外标法定量,该方法相对标准偏差为1.18%~1.99%,线性相关系数R2为0.999,检测限为2μg/mL。在上述条件下测定了随机抽取的部分市售红酒样品的白藜芦醇含量力。     

Sarcopenic Obesity in Liver Cirrhosis: Possible Mechanism and Clinical Impact

The picture of chronic liver diseases (CLDs) has changed considerably in recent years. One of them is the increase of non-alcoholic fatty liver disease. More and more CLD patients, even those with liver cirrhosis (LC), tend to be presenting with obesity these days. The annual rate of muscle loss increases with worsening liver reserve, and thus LC patients are more likely to complicate with sarcopenia. LC is also characterized by protein-energy malnutrition (PEM). Since the PEM in LC can be invariable, the patients probably present with sarcopenic obesity (Sa-O), which involves both sarcopenia and obesity. Currently, there is no mention of Sa-O in the guidelines; however, the rapidly increasing prevalence and poorer clinical consequences of Sa-O are recognized as an important public health problem, and the diagnostic value of Sa-O is expected to increase in the future. Sa-O involves a complex interplay of physiological mechanisms, including increased inflammatory cytokines, oxidative stress, insulin resistance, hormonal disorders, and decline of physical activity. The pathogenesis of Sa-O in LC is diverse, with a lot of perturbations in the muscle–liver–adipose tissue axis. Here, we overview the current knowledge of Sa-O, especially focusing on LC.     

白藜芦醇的制备及其检测方法研究进展

白藜芦醇是一种植物抗毒素,广泛存在于葡萄、花生、虎杖等植物中,具有抗癌、抗菌、抗氧化等重要的生物功效。首先,综述了白藜芦醇从天然植物中直接提取、化学合成、利用生物技术制备的方法;其次,对白藜芦醇检测方法的研究近况作了综述,包括高效液相色谱法、薄层色谱法、毛细管电泳法、色谱联用技术等。     

白藜芦醇美白功效的初步研究

研究了白藜芦醇对B16黑色素细胞的增殖、细胞内酪氨酸酶活性及黑色素合成的影响。结果表明,白藜芦醇可抑制细胞增殖,对细胞内酪氨酸酶活性有明显抑制作用,能明显减少细胞内黑色素的含量,从而起到美白的作用。与熊果苷和乙基Vc相比较,白藜芦醇在0.5μg/mL的较低浓度下即可达到前二者在50μg/mL浓度下的抑制效果。     

The Role of Molecular and Hormonal Factors in Obesity and the Effects of Physical Activity in Children

Obesity and overweight are defined as abnormal fat accumulations. Adipose tissue consists of more than merely adipocytes; each adipocyte is closely coupled with the extracellular matrix. Adipose tissue stores excess energy through expansion. Obesity is caused by the abnormal expansion of adipose tissue as a result of adipocyte hypertrophy and hyperplasia. The process of obesity is controlled by several molecules, such as integrins, kindlins, or matrix metalloproteinases. In children with obesity, metabolomics studies have provided insight into the existence of unique metabolic profiles. As a result of low-grade inflammation in the system, abnormalities were observed in several metabolites associated with lipid, carbohydrate, and amino acid pathways. In addition, obesity and related hormones, such as leptin, play an instrumental role in regulating food intake and contributing to childhood obesity. The World Health Organization states that physical activity benefits the heart, the body, and the mind. Several noncommunicable diseases, such as cardiovascular disease, cancer, and diabetes, can be prevented and managed through physical activity. In this work, we reviewed pediatric studies that examined the molecular and hormonal control of obesity and the influence of physical activity on children with obesity or overweight. The purpose of this review was to examine some orchestrators involved in this disease and how they are related to pediatric populations. A larger number of randomized clinical trials with larger sample sizes and long-term studies could lead to the discovery of new key molecules as well as the detection of significant factors in the coming years. In order to improve the health of the pediatric population, omics analyses and machine learning techniques can be combined in order to improve treatment decisions.     

白藜芦醇化学合成研究进展

白藜芦醇是一种植物抗毒素,近几年来大量的研究发现白藜芦醇具有多种生物活性和药理作用．可以广泛应用于医药、保健品、食品、化妆品等领域。白藜芦醇的制备、开发引起国内外医药、食品、材料等领域的关注。笔者综述了近年白藜芦醇的化学合成研究进展。     

Oxidative Stress in Obesity: A Critical Component in Human Diseases

Obesity, a social problem worldwide, is characterized by an increase in body weight that results in excessive fat accumulation. Obesity is a major cause of morbidity and mortality and leads to several diseases, including metabolic syndrome, diabetes mellitus, cardiovascular, fatty liver diseases, and cancer. Growing evidence allows us to understand the critical role of adipose tissue in controlling the physic-pathological mechanisms of obesity and related comorbidities. Recently, adipose tissue, especially in the visceral compartment, has been considered not only as a simple energy depository tissue, but also as an active endocrine organ releasing a variety of biologically active molecules known as adipocytokines or adipokines. Based on the complex interplay between adipokines, obesity is also characterized by chronic low grade inflammation with permanently increased oxidative stress (OS). Over-expression of oxidative stress damages cellular structures together with under-production of anti-oxidant mechanisms, leading to the development of obesity-related complications. The aim of this review is to summarize what is known in the relationship between OS in obesity and obesity-related diseases.     

虎杖中白藜芦醇的提取方法比较和优化研究

提取了虎杖中的活性成分白藜芦醇,用高效液相色谱法检测白藜芦醇的含量。通过对5种不同提取工艺的比较,用正交设计选取最佳工艺,实验结果表明:弱碱性条件下超声波法提取效果最好,用10倍量pH=8的80%乙醇、超声波提取4次,每次15m in,白藜芦醇提取含量可达到0.373%。     

Role of Cannabidiol for Improvement of the Quality of Life in Cancer Patients: Potential and Challenges

There is currently a growing interest in the use of cannabidiol (CBD) to alleviate the symptoms caused by cancer, including pain, sleep disruption, and anxiety. CBD is often self-administered as an over-the-counter supplement, and patients have reported benefits from its use. However, despite the progress made, the mechanisms underlying CBD’s anti-cancer activity remain divergent and unclear. Herein, we provide a comprehensive review of molecular mechanisms to determine convergent anti-cancer actions of CBD from pre-clinical and clinical studies. In vitro studies have begun to elucidate the molecular targets of CBD and provide evidence of CBD’s anti-tumor properties in cell and mouse models of cancer. Furthermore, several clinical trials have been completed testing CBD’s efficacy in treating cancer-related pain. However, most use a mixture of CBD and the psychoactive, tetrahydrocannabinol (THC), and/or use variable dosing that is not consistent between individual patients. Despite these limitations, significant reductions in pain and opioid use have been reported in cancer patients using CBD or CBD+THC. Additionally, significant improvements in quality-of-life measures and patients’ overall satisfaction with their treatment have been reported. Thus, there is growing evidence suggesting that CBD might be useful to improve the overall quality of life of cancer patients by both alleviating cancer symptoms and by synergizing with cancer therapies to improve their efficacy. However, many questions remain unanswered regarding the use of CBD in cancer treatment, including the optimal dose, effective combinations with other drugs, and which biomarkers/clinical presentation of symptoms may guide its use.     

白藜芦醇在化妆品中的应用与检测展望

白藜芦醇具有良好的抗氧化性和消除自由基的能力,在化妆品方面具有良好的应用价值,其已被列入《国际化妆品原料标准目录》(INCI)中,市场上已有厂家推出含白藜芦醇的产品。介绍了白藜芦醇的理化性质、在化妆品中的应用以及现有检测技术和方法。同时比较了目前常用的白藜芦醇检测方法的差异和优劣,为建立化妆品中白藜芦醇的检测方法提供参考。最后提出了白藜芦醇在化妆品中的应用前景和推荐检测方法。     

The Role of Sarcopenic Obesity in Cancer and Cardiovascular Disease: A Synthesis of the Evidence on Pathophysiological Aspects and Clinical Implications

Obesity is globally a serious public health concern and is associated with a high risk of cardiovascular disease (CVD) and various types of cancers. It is important to evaluate various types of obesity, such as visceral and sarcopenic obesity. The evidence on the associated risk of CVD, cancer and sarcopenic obesity, including pathophysiological aspects, occurrence, clinical implications and survival, needs further investigation. Sarcopenic obesity is a relatively new term. It is a clinical condition that primarily affects older adults. There are several endocrine-hormonal, metabolic and lifestyle aspects involved in the occurrence of sarcopenic obesity that affect pathophysiological aspects that, in turn, contribute to CVD and neoplasms. However, there is no available evidence on the role of sarcopenic obesity in the occurrence of CVD and cancer and its pathophysiological interplay. Therefore, this review aims to describe the pathophysiological aspects and the clinical and epidemiological evidence on the role of sarcopenic obesity related to the occurrence and mortality risk of various types of cancer and cardiovascular disease. This literature review highlights the need for further research on sarcopenic obesity to demonstrate the interrelation of these various associations.     

水溶性白藜芦醇衍生物的制备及其性质研究

为了增强白藜芦醇(1)的水溶性和抗肿瘤的靶向性,通过DCC/DMAP偶联法,分别将葡萄糖和1引入两端均羧基化的聚乙二醇两端构建葡萄糖-聚乙二醇支载白藜芦醇衍生物,其结构经1H-NMR和IR表征;采用UV法测定产物中白藜芦醇的含量及水溶性。结果表明,由PEG4000支载的葡萄糖-聚乙二醇-白藜芦醇的水溶性最好。