黄酮类化合物防治良性前列腺增生的作用机制研究进展

黄酮类化合物是一类母核为苯并吡喃酮的多酚化合物的总称,具有抗氧化、抗炎、抗肿瘤、心脑血管保护等多种生物活性。近年来研究显示,黄酮类化合物在防治良性前列腺增生中具有一定的作用。综述了黄酮类化合物防治良性前列腺增生作用机制的研究进展。     

柚皮苷对糖尿病及其并发症作用机制的研究进展

柚皮苷主要存在于芸香科柑橘属植物柚、葡萄柚、酸橙及其变种的果皮及果实中,属于双氢黄酮类化合物。研究表明柚皮苷具有抗1型及2型糖尿病的药理作用,作用机制为通过抑制糖尿病相关的氧化应激损伤、炎症、糖代谢酶异常等方面,同时在一定程度上延缓糖尿病并发症（包括糖尿病心肌病、糖尿病肾病、糖尿病视网膜病变及糖尿病神经病变）的发生与发展。探讨柚皮苷对糖尿病及其并发症作用机制的研究进展,旨在为抗糖尿病新药研发提供依据。     

棕矢车菊素的药理作用及其作用机制的研究进展

棕矢车菊素是主要存在于艾叶、野马追中的具有药理活性的黄酮类化合物,是一种多靶点的药物,具有抗氧化、抗癌、抗菌、抗炎、抗过敏等多种生物活性。对棕矢车菊素的抗肿瘤、抗炎、抗菌、降血糖、免疫抑制等多种药理活性及其作用机制进行综述,以期为其开发应用提供理论依据。     

牡荆素的神经保护作用及机制研究进展

牡荆素是一种天然黄酮类化合物,具有广泛的药理活性。近年来研究发现其对中枢系统和周围神经系统具有明显的保护作用,包括抗记忆损伤、抗癫痫、抗缺血缺氧性脑损伤、抗抑郁、镇痛等作用。这些神经保护作用可能是通过降低自由基水平、对抗神经凋亡、调节炎症因子及其通路、调节神经递质及相关受体等多途径,多靶点的机制实现的。该文就近年来牡荆素的神经保护作用及相关作用机制的研究进展作简要概述。     

黄酮类化合物抗肿瘤作用分子机制研究进展

天然黄酮类化合物(flavonoidscompounds)是植物体多酚类(polyphenolic compounds)的内信号分子及中间体或代谢物,具有多种药理活性。对黄酮类化合物的抗肿瘤作用研究已久,国内外文献报道较多,提出作用机制有:抑制肿瘤细胞增殖、促进肿瘤细胞凋亡、干扰细胞信号传导、调节抑癌基因和癌基因关系等。本文对黄酮类化合物抗肿瘤作用分子机制的研究进展进行了简要的概述。     

抗糖尿病及并发症黄酮类化合物的研究进展

黄酮类化合物为自然界中一类具有生物活性的天然产物.近年来发现槲皮素、芦丁、葛根素、原花青素和杨梅树皮素等黄酮类化合物对糖尿病及并发症有明显预防和治疗作用.作用机制研究表明黄酮类化合物对糖尿病性氧化损伤、炎症、糖代谢酶异常等方面均有较好治疗作用,同时一定程度延缓糖尿病并发症的发生和发展.文中按抗糖尿病作用机制对活性黄酮化合物进行分类和归纳,介绍其最新研究进展.     

水飞蓟宾保护胰岛β细胞的作用及机制

水飞蓟宾是从水飞蓟中提取的一种黄酮类天然化合物,已用于多种疾病的治疗.近年来研究显示,水飞蓟宾对胰岛β细胞具有抗氧化、抗炎、改善糖脂毒性、增加胰岛素敏感性,改善胰岛素抵抗的作用,有可能成为潜在的糖尿病防治药物.     

水飞蓟素防治实验性肝病的作用及相关临床应用的研究进展

水飞蓟素是一种黄酮类化合物，具有清除活性氧、抗脂质过氧化、抗炎、抗肿瘤等多种药理作用。笔者通过查阅大量相关文献，发现水飞蓟素对各种肝病均具有较好的防治作用。随着基础研究的深入，发现水飞蓟素还可以促进肝细胞的修复与再生，与抗病毒药物及其他护肝药物联用时能更显著地降低血清转氨酶水平及改善肝纤维化，具有安全性高及耐受性好的优点。本文主要对水飞蓟素对不同肝病的防治作用、作用机制及其临床应用现状进行综述，以期为水飞蓟素在防治肝病方面的深入研究、药物开发和临床应用等方面提供参考。     

白藜芦醇抗肿瘤药理作用机制研究进展

白藜芦醇是一种天然单体化合物,属于非黄酮类的多酚化合物,存在于多种植物中。现代药理研究发现,白藜芦醇具有抗炎、抗氧化、抗肿瘤、调节代谢与机体免疫等药理活性。白藜芦醇对结肠癌、胰腺癌、卵巢癌、乳腺癌等多种肿瘤细胞均有抑制作用,其抗肿瘤作用逐渐成为研究热点。白藜芦醇可以通过抑制肿瘤细胞的增殖、诱导肿瘤细胞凋亡、抑制肿瘤细胞侵袭和转移、调节机体免疫功能、直接作用于相关靶点等发挥抗肿瘤活性。就白藜芦醇在不同肿瘤细胞中发挥的抗肿瘤作用及其机制进行综述,以期为抗肿瘤新药的研发提供参考依据。     

小分子药物治疗糖尿病肾病的药理作用研究进展

糖尿病肾脏病是糖尿病常见微血管并发症，起病隐匿，是以蛋白尿为显著特征的进行性肾功能衰退疾病，是导致终末期肾病、诱发心血管疾病和早发死亡的重要危险因素。小分子药物是化学合成的活性物质，通常相对分子质量小于1 000，其发挥作用的实质是药物与靶蛋白之间的相互作用。小分子药物可通过改善血流动力学、抗炎、抗氧化、抗肾间质纤维化等多种途径发挥防治糖尿病肾脏病的作用。综述了多种小分子药物防治糖尿病肾病的药理作用及其机制，旨在为早期干预或延缓糖尿病肾病进展的治疗和联合用药提供思路。     

中药总黄酮抗肿瘤活性及机制的研究现状

中药有效部位总黄酮是一大类天然产物,具有多种生物活性。研究表明,总黄酮对肝癌、肺癌、乳腺癌、胃癌、白血病等多种癌症均有一定的防治作用,但其机制研究仍不够全面与深入。本文旨在归纳近年来中药总黄酮防治肿瘤的实验研究,从抑制肿瘤细胞生长、增殖及侵袭转移、诱导细胞凋亡、改善免疫功能、抑制相关酶的表达、调节氨基酸等代谢途径、逆转耐药等方面探讨总黄酮的抗肿瘤机制,为今后高效、安全利用中药资源,寻找新型抗肿瘤药物,以期为临床协助治疗提供理论依据。     

Flavonoids as anticancer agents: structure-activity relationship study

The protection against some forms of cancer provided by many common foods has been observed in multiple epidemiological studies. Non-nutritive dietary compounds, such as flavonoids, have been considered as the responsible agents for such observations and since then, much research activity has been done about their potential anticancer effect. As a result, these compounds have been shown to regulate proliferation and cell death pathways leading to cancer. Thus, flavonoids such as the synthetic flavone, flavopiridol; the soy isoflavonoid, genistein; the tea catechin epigallocatechin gallate; or the common dietary flavonol, quercetin, are emerging as prospective anticancer drug candidates and some of them have already entered in clinical trials. In view of the therapeutic potential of flavonoids, many researchers have tried to elucidate possible structure-activity relationships that might lead to new drug discovery. However, and possibly due to the information being very scattered, there is very little understanding about a possible relationship between the flavonoid structure and their anticancer activity. Besides their therapeutic potential, since lots of flavonoids are present in our diet, a greater understanding of their anticancer properties might also modify our dietary habits in order to attack cancer with an effective weapon, prevention. This paper seeks to show, in a brief but comprehensive way, the anticancer properties of flavonoids. Through an understanding of the cancer process and its treatment, flavonoids are studied as possible useful compounds in cancer prevention and cancer therapy. Furthermore, this review attempts to compile and discuss the literature studying structure-activity relationships, in order to show structural requirements implicated in the anticancer activity of flavonoids, which might help to rationalize their development as antitumor agents.     

Therapeutic potential of traditional Chinese medicine for the treatment of NAFLD: A promising drug Potentilla discolor Bunge

Nonalcoholic fatty liver disease (NAFLD) is characterized by excessive accumulation of hepatic lipids and metabolic stress-induced liver injury. There are currently no approved effective pharmacological treatments for NAFLD. Traditional Chinese medicine (TCM) has been used for centuries to treat patients with chronic liver diseases without clear disease types and mechanisms. More recently, TCM has been shown to have unique advantages in the treatment of NAFLD. We performed a systematic review of the medical literature published over the last two decades and found that many TCM formulas have been reported to be beneficial for the treatment of metabolic dysfunctions, including Potentilla discolor Bunge (PDB). PDB has a variety of active compounds, including flavonoids, terpenoids, organic acids, steroids and tannins. Many compounds have been shown to exhibit a series of beneficial effects for the treatment of NAFLD, including anti-oxidative and anti-inflammatory functions, improvement of lipid metabolism and reversal of insulin resistance. In this review, we summarize potential therapeutic effects of TCM formulas for the treatment of NAFLD, focusing on the medicinal properties of natural active compounds from PDB and their underlying mechanisms. We point out that PDB can be classified as a novel candidate for the treatment and prevention of NAFLD.     

Protective effects of Astragalus saponin I on early stage of diabetic nephropathy in rats

Diabetic nephropathy (DN) has become the leading cause of end stage failure, but no renoprotective treatment has been very available for use in DN. Astragalus saponin I (AS I), a component extracted from Astragalus membranaceus BUNGE, was studied in experimental DN induced by administration of streptozotocin in male rats. The early DN rats were treated with 3 doses of AS I for 8 weeks to analyze its efficacy with different parameters. By comparison with vehicle-treated DN rats, the renal hypertrophy, the oxidative stress intensity, and the blood glucose level of DN rats were ameliorated by AS I. Also, the microalbuminuria level, advanced glycated end-products either in serum or in kidney cortex, and the aldose reductase activity were significantly reduced. Furthermore, the expression of transforming growth factor beta1 mRNA in kidney cortex by RT-PCR analysis was markedly declined. Both the relative grade of mesangium hyperplasia by microscopical observation and the thickness of glomerular base membrane by electron microscope measurement were decreased significantly. Therefore, the results suggest that AS I has therapeutic effects on several pharmacological targets in the progress of DN and is a potential drug for prevention of early stage DN.     

Effects of heat treatment of mandarin peel on flavonoid profiles and lipid accumulation in 3T3-L1 adipocytes

Citrus peel, a primary byproduct of citrus fruits, contains a variety of flavonoids. Heat treatment is a favorable food processing for solid peel to release bioactive compounds from tissues and intensify nutritional effects. In this study, we explored alterations of flavonoids by thermal treatment of mandarin peel and their effects on lipid accumulation and intracellular levels during differentiation of 3T3-L1 cells to adipocytes. The heat-treated sample showed stronger inhibition on the formation of lipid droplets than the non-treated sample, along with enhanced intracellular levels of flavonoids. Overall flavonoids, especially flavonoid aglycones showing better efficacy, were found to increase in the peel after heat-treatment. Our findings indicate thermal processing could help release flavonoids from citrus peel and convert them into aglycone forms, leading to efficient cellular uptake and suppression of lipid accumulation in 3T3-L1 cells. This study provides useful information of heat-treated citrus peel as potential dietary supplements with anti-obesity-related effects.     

Molecular crosstalk between TRAIL and natural antioxidants in the treatment of cancer

The endogenous protein, tumour necrosis factor receptor apoptosis-inducing ligand (TRAIL), induces apoptosis in a wide variety of transformed and cancer cells but has little or no effect on normal cells. Therefore, TRAIL is considered to be a tumour-selective, apoptosis-inducing cytokine and a promising new candidate for cancer prevention and treatment. Some cancer cells are however resistant to TRAIL-induced apoptosis, but treatment in combination with conventional chemotherapeutic drugs or radiation generally restores TRAIL sensitivity in those cells. A novel class of molecules exhibiting synergy with TRAIL but devoid of major side effects are emerging as alternative approaches to treat resistant cancer cells, including natural antioxidants such as sulphoraphane or the flavonoids curcumin, quercetin, resveratrol, baicalein and wogonin. In this issue of the BJP, Lee et al. demonstrate that treatment of TRAIL-resistant cancer cells with wogonin restores TRAIL-induced cell death in a reactive oxygen species-dependent manner through up-regulation of p53 and Puma.     

黄酮类化合物改善胰岛素抵抗的研究进展

黄酮类化合物为自然界中一类具有生物活性的天然产物.近年研究发现槲皮素、芦丁、葛根素和杨梅黄酮等黄酮类化合物对胰岛素抵抗、糖尿病、高血脂等相关症状有明显预防和治疗作用.本文就黄酮类化合物改善胰岛素抵抗最新研究进展作一介绍.     

2型糖尿病肾病相关生化指标检测及临床意义

目的分析糖尿病肾病与各相关因素的关系以指导临床及早期防治。方法对56例2型糖尿病患者及健康对照组相关指标进行统计分析。结果 CAU组、MAU组及NAU组HbA1c、UA均高于NC组(P<0.05);4组HCY、ADPN呈递增趋势;hs-CRP水平随病变程度而增加。结论多种因素影响DN的发生,积极地控制各种危险因素对预防和延缓DN的发生与发展有重要的意义。     

The anti-cancer charm of flavonoids: a cup-of-tea will do!

Hormone-dependent cancers of the breast, prostate and colon have, in the past decade, become the leading causes of morbidity and mortality. Billions of dollars have been, and still are being spent to study cancers like these, and, in the past three decades, thanks to work by thousands of dedicated scientists, tremendous advancements in the understanding and treatment of cancer have been made. Nevertheless, as there is no sure-fire cure for a variety of cancers to date, natural protection against cancer has been receiving a great deal of attention lately not only from cancer patients but, surprisingly, from physicians as well. Phytoestrogens, plant-derived secondary metabolites, are diphenolic substances with structural similarity to naturally-occurring human steroid hormones. Phytoestrogens are normally divided into three main classes: flavonoids, coumestans and lignans. Flavonoids are found in almost all plant families in the leaves, stems, roots, flowers and seeds of plants and are among the most popular anti-cancer candidates. Flavonoidic derivatives have a wide range of biological actions such as antibacterial, antiviral, anti-inflammatory, anticancer, and antiallergic activities. Some of these benefits are explained by the potent antioxidant effects of flavonoids, which include metal chelation and free-radical scavenging activities. Patent applications regarding flavonoids range from protocols for extraction and purification from natural resources and the establishment of various biological activities for these extracts to novel methods for the production and isolation of flavonoids with known biological activities. This review will bring the reader up to date on the current knowledge and research available in the field of flavonoids and hormone-dependent cancers, and many of the submitted patents that exploit flavonoids.