槲皮素酯类衍生物研究进展

健康生活方式特别强调食物质量,多酚在这方面发挥了关键作用。槲皮素是一种天然多酚,是多种植物性食品中发现最丰富的类黄酮类化合物之一。槲皮素是天然的抗氧化剂,可以保护细胞免受自由基造成的损害。槲皮素是一种亲脂性化合物,能够穿过细胞膜,可调节众多与疾病进展、化学预防有关的细胞内和细胞外信号通路。槲皮素具有广泛的药理活性,抗炎、抗菌、抗癌和预防心脑血管疾病,但是它低溶解度和生物利用度限制了在临床上的应用。对槲皮素的结构进行优化修饰获得了溶解性能好、生物利用度高、活性明显改善、抗癌活性增强的槲皮素衍生物。综述了近年来槲皮素酯衍生物的研究进展,为槲皮素衍生物的进一步开发提供参考。     

木犀草素衍生物研究进展

木犀草素属于黄酮类化合物,主要以糖苷的形式存在于蔬菜、水果和中草药中。木犀草素属于天然抗氧化剂,具有丰富的生物活性,可调节众多与疾病进展有关的细胞内和细胞外信号通路,具有抗氧化、抗炎、抗糖尿病、抗癌等作用。越来越多的证据表明,摄入木犀草素可能有益于影响糖脂代谢紊乱,特别是胰岛素抵抗、糖尿病和肥胖。木犀草素低溶解度和较低的生物利用度限制了在临床上的应用。然而,木犀草素的低分子质量和易修饰的化学基团,使其具有药物开发的吸引力。因此,研究人员通过各种方法设计合成了木犀草素衍生物,以改善其不利因素,进而发挥预防和治疗疾病的作用。木犀草素衍生物溶解性能好、生物利用度高、活性明显改善、抗癌活性增强,本文综述了木犀草素衍生物的研究进展,为天然产物的研究、开发及利用提供参考。     

钒-药物分子配合物生物活性研究进展

无机钒化合物具有降血糖、抗癌、抗炎和抗菌等作用,但生物利用度低,且有一定的毒性,影响了其在药物领域的应用。选择药物分子作为钒的配体,不仅可提高钒化合物的生物利用度,而且可增强或改进药物分子的活性,同时可能降低钒的毒性,从而成为近年来钒化学领域一个新的研究方向。本文主要介绍钒与不同类型药物分子形成配合物的生物活性及相关工作。     

熊果酸的结构修饰与生物活性研究进展

熊果酸是从药用植物、水果和蔬菜中提取的具有多种药理活性的五环三萜类化合物.近年来,熊果酸的药理作用得到了广泛的研究,大量研究表明熊果酸具有多种药理活性,包括抗癌、抗炎、抗氧化、抗菌、抗糖尿病等.熊果酸虽然具有广泛的生物学活性,但其水溶性差、生物利用度低等限制了在临床上的应用.为了克服这些缺点,国内外研究人员通过对熊果酸母体骨架进行化学修饰,设计并开发了大量结构新颖、活性强的熊果酸衍生物.对近年来合成的有进一步研究价值的熊果酸衍生物及其生物活性研究进展进行总结,为以熊果酸为先导化合物的药物研究提供参考.     

槲皮素和芦丁的某些金属配合物的电喷雾质谱研究

槲皮素(quercetin)和芦丁(rutin)都是天然的黄酮类化合物,且槲皮素是芦丁的甙元,它们广泛存在于许多植物的花、叶、果实中,对其药理作用研究较多[1-3],但由于槲皮素和芦丁不溶于或难溶于水,不利于吸收[4],极大地限制了其生物利用度和体内给药途径.     

含1,3,4-噁二唑的葡萄糖苷衍生物的合成及抑菌活性

糖苷类化合物广泛存在于生物体内,并担负着重要生物功能,天然药物及中草药中的许多活性成分是糖苷化合物[1].糖苷类化合物的良好抗菌、抗癌活性激发了广大研究者的浓厚兴趣[2-3],启发人们通过糖苷化反应作为改变或增加生物活性的重要结构修饰方法[4],以增加化合物的水溶性和导向性,改进药理学性质.     

抗癌大环化合物的环合方法

大环化合物具有广泛的生物活性.一些具有抗癌活性的天然大环化合物已开发成上市药物或应用于临床研究.在抗癌大环化合物的合成中,环合步骤是整个合成过程中的关键,同时也是难点所在.目前已经发展出了一些方便实用的环合方法.文章以具有抗癌作用的大环化合物为例,简要介绍各种常用的大环环合方法及应用.     

7,10—二芳基—六氢（四氢）苯并[C]吖啶—8—酮的合成

吖啶及吖啶酮类化合物具有广泛的药理活性,其中许多化合物具有明显的杀菌、抗炎、增强记忆、镇痛和抗癌等活性。如早年开发的抗癌药物山柚柑碱(Acronycine)就具有显著的抗癌作用,且抗瘤谱较广。近年来抗癌新药安吖啶(Amsacrime)在临床上用于治疗急性白血病收到疗效后,对吖啶及吖啶酮衍生物的合成及抗癌活性研究日渐增多。已测定了一些化合物     

基于天然产物的抗肿瘤缀合物的研究进展

由于肿瘤疾病发病机制的复杂性及靶向药物的耐药性问题,单靶点药物已经不能很好地治疗癌症.利用拼合原理将两个或多个不同的药物或药效基团适当连接得到的缀合物,其相对于拼接前的单一药物,可能具有抑制多个肿瘤靶点的能力,或者发挥协同抗癌作用.许多天然产物被证明具有抗癌活性,但由于各种缺点,如生物利用率低,毒副作用大等,不能应用于...     

HPLC法测定人体尿液中的4'-羟基和6-甲氧基黄烷酮

黄烷酮(Flavanone)属于黄酮类化合物(Flavonoids),具有2-苯基色原酮化学结构.黄烷酮类化合物广泛存在自然界,其衍生物大多从天然植物中提取而得,取代基多为羟基、甲氧基、苄氧基、异戊烯基、香叶基等,是多种药用植物有效成分之一.据有关文献报道,许多黄烷酮类化合物具有抗菌、消炎、抗肿瘤、抗HIV病毒、抗诱变、抗氧化、抗癌活性等诸多生物活性~([1]).由于其显著的生物、药理活性及独特的可靼性结构,引起了化学和医药工作者浓厚的研究兴趣.     

Medicinal plants with anti-inflammatory activities

Medicinal plants have been the main remedy to treat various ailments for a long time and nowadays, many drugs have been developed from traditional medicine. This paper reviews some medicinal plants and their main constituents which possess anti-inflammatory activities useful for curing joint inflammation, inflammatory skin disorders, cardiovascular inflammation and other inflammatory diseases. Here, we provide a brief overview of quick and easy reading on the role of medicinal plants and their main constituents in these inflammatory diseases. We hope that this overview will shed some light on the function of these natural anti-inflammatory compounds and attract the interest of investigators aiming at the design of novel therapeutic approaches for the treatment of various inflammatory conditions.     

Determination of Rutin in Amaranthus spinosus Linn. Whole Plant Powder by HPTLC

A simple, precise and accurate high-performance thin-layer chromatographic method has been established for the determination of rutin in the whole plant powder of Amaranthus spinosus Linn. Rutin has been reported to have anti-diabetic, anti-thrombotic, anti-inflammatory and anti-carcinogenic activity. A methanol extract of the whole plant powder was used for the experimental work. The concentration of rutin in the whole plant powder was found to be 0.15%. Separation was performed on silica gel 60 F₂₅₄ HPTLC plates with ethyl acetate:formic acid:methanol:distilled water in the proportion 10:0.9:1.1:1.7 (v/v), as mobile phase. The determination was carried out using the densitometric absorbance mode at 363 nm. Rutin response was linear over the range 10–60 μg mL^?1. The HPTLC method was evaluated in terms of sensitivity, accuracy, precision and reproducibility.     

Resveratrol Promotes Angiogenesis in a FoxO1-Dependent Manner in Hind Limb Ischemia in Mice

Critical limb ischemia (CLI) is a severe form of peripheral artery diseases (PAD) and seriously endangers the health of people. Therapeutic angiogenesis represents an important treatment strategy for CLI; various methods have been applied to enhance collateral circulation. However, the current development drug therapy to promote angiogenesis is limited. Resveratrol (RSV), a polyphenol compound extracted from plants, has various properties such as anti-oxidative, anti-inflammatory and anti-cancer effects. Whether RSV exerts protective effects on CLI remains elusive. In the current study, we demonstrated that oral intake of RSV significantly improved hind limb ischemia in mice, and increased the expression of phosphorylated Forkhead box class-O1 (FoxO1). RSV treatment in human umbilical vein endothelial cells (HUVECs) could increase the phosphorylation of FoxO1 and its cytoplasmic re-localization to promote angiogenesis. Then we manipulated FoxO1 in HUVECs to further verify that the effect of RSV on angiogenesis is in a FoxO1-dependent manner. Furthermore, we performed metabolomics to screen the metabolic pathways altered upon RSV intervention. We found that the pathways of pyrimidine metabolism, purine metabolism, as well as alanine, aspartate and glutamate metabolism, were highly correlated with the beneficial effects of RSV on the ischemic muscle. This study provides a novel direction for the medical therapy to CLI.     

A systematic investigation on flavonoids,catechin, β-sitosterol and lignin glycosides from Saraca asoca (ashoka) having anti-cancer & antioxidant properties with no side effect

Saraca asoca is an IUCN red-listed tree species that extensively famous in the Ayurvedic medicine field. Saraca asoca (Roxb.) de Wilde belongs to the family Fabaceae, has been used to treat various gynecological disorders, bacterial infections, worm infestations, haemmorhagic dysentery, uterine pain, skin diseases, cancer, circulatory, cardiovascular disorders, and many others. All parts of the Saraca asoca have medicinal values. Numerous antioxidant compounds like flavonoids, catechin, beta-sitosterol, lignin glycosides are present in the bark, leaf, and flower of Saraca asoca plant, which help to stabilize free radicals molecules that are associated with the development of cancer conditions. Currently in the cancer research study field new and more effective modes of natural therapies are recently being analyzed. Traditional medicines have been used for their preventative role against various diseases in the human population. Plant based therapy for cancer prevention is becoming more demanding due to its various unique properties such as natural chemical composition, less expensiveness, naturally available., easily orally administrable, significant chemo-protective activities, nontoxic to normal cells in the body, less side effects compared to other synthetic chemotherapeutic drugs. The chemotherapeutic drugs will be harmful to both cancer and normal cells. Additionally, some common side effects or health consequences like vomiting, nausea, bleeding, hair fall, alopecia, hyperuricemia, thrombocytopenia, bone marrow depression, mucositis are very common after chemotherapeutic drug treatment in cancer. This review paper summarizes the evidences which agree with the fact that flavonoids and other phenolic compounds in Saraca asoca plant possess significant antioxidant activity and an efficient chemopreventive characteristic against different types of cancer. This paper reviews the anticancer activities of Saraca asoca bark and flower and discusses the potential preventive roles of phenolic and flavonoids compounds, present in bark and flower of Saraca asoca in the cancer treatment process.     

Neuroprotective Effects of Quercetin in Pediatric Neurological Diseases

Oxidative stress is a crucial event underlying several pediatric neurological diseases, such as the central nervous system (CNS) tumors, autism spectrum disorder (ASD) and attention-deficit/hyperactivity disorder (ADHD). Neuroprotective therapy with natural compounds used as antioxidants has the potential to delay, ameliorate or prevent several pediatric neurological diseases. The present review provides an overview of the most recent research outcomes following quercetin treatment for CNS tumors, ASD and ADHD as well as describes the potential in vitro and in vivo ameliorative effect on oxidative stress of bioactive natural compounds, which seems like a promising future therapy for these diseases. The neuroprotective effects of quercetin against oxidative stress can also be applied in the management of several neurodegenerative disorders with effects such as anti-cancer, anti-inflammatory, anti-viral, anti-obesity and anti-microbial. Therefore, quercetin appears to be a suitable adjuvant for therapy against pediatric neurological diseases.     

A Novel Approach to Unraveling the Apoptotic Potential of Rutin (Bioflavonoid) via Targeting Jab1 in Cervical Cancer Cells

Rutin has been well recognized for possessing numerous pharmacological and biological activities in several human cancer cells. This research has addressed the inhibitory potential of rutin against the Jab1 oncogene in SiHa cancer cells, which is known to inactivate various tumor suppressor proteins including p53 and p27. Further, the inhibitory efficacy of rutin via Jab1 expression modulation in cervical cancer has not been yet elucidated. Hence, we hypothesized that rutin could exhibit strong inhibitory efficacy against Jab1 and, thereby, induce significant growth arrest in SiHa cancer cells in a dose-dependent manner. In our study, the cytotoxic efficacy of rutin on the proliferation of a cervical cancer cell line (SiHa) was exhibited using MTT and LDH assays. The correlation between rutin and Jab1 mRNA expression was assessed by RT-PCR analysis and the associated events (a mechanism) with this downregulation were then explored via performing ROS assay, DAPI analysis, and expression analysis of apoptosis-associated signaling molecules such as Bax, Bcl-2, and Caspase-3 and -9 using qRT-PCR analysis. Results exhibit that rutin produces anticancer effects via inducing modulation in the expression of oncogenes as well as tumor suppressor genes. Further apoptosis induction, caspase activation, and ROS generation in rutin-treated SiHa cancer cells explain the cascade of events associated with Jab1 downregulation in SiHa cancer cells. Additionally, apoptosis induction was further confirmed by the FITC-Annexin V/PI double staining method. Altogether, our research supports the feasibility of developing rutin as one of the potent drug candidates in cervical cancer management via targeting one such crucial oncogene associated with cervical cancer progression.