姜黄素的临床研究进展

姜黄素具有广泛的药理活性,其作为治疗多种疾病的潜力药物的研究正越来越多的引起关注.多个临床Ⅰ期试验已证实,姜黄素口服安全且耐受性好:药动学表明,姜黄素口服不易吸收,生物利用度低.研究显示,姜黄素治疗乳腺癌、结肠癌、肠易激综合征、风湿性关节炎及动脉粥样硬化等有疗效.现总结了姜黄素临床研究的报道,以冀为姜黄素的应用研究提供参考.     

姜黄素剂型的研究概况

姜黄素是从姜科植物中提取的有效成分,具有多种药理活性,但水溶性差,口服吸收差。为增加其水溶性,便于临床用药,研究者对姜黄素的剂型进行了广泛研究。现将近年姜黄素的剂型研究概况作一综述。     

姜黄素剂型的研究概况

姜黄素是从姜科植物中提取的有效成分,具有多种药理活性,但水溶性差,口服吸收差。为增加其水溶性,便于临床用药,研究者对姜黄素的剂型进行了广泛研究。现将近年姜黄素的剂型研究概况作一综述。     

姜黄素剂型的研究概况

姜黄素是从姜科植物中提取的有效成分,具有多种药理活性,但水溶性差,口服吸收差.为增加其水溶性,便于临床用药,研究者对姜黄素的剂型进行了广泛研究.现将近年姜黄素的剂型研究概况作一综述.     

姜黄素体内吸收代谢及与肠道菌群互作研究进展

姜黄素是一种二苯基庚烷类化合物,因多样而显著的健康效应而被广泛关注。然而,姜黄素经口服消化吸收后生物利用度极低,其健康效应产生的物质基础和过程机制一直备受争议。本文综述姜黄素在机体内吸收转运及代谢过程的研究进展。姜黄素经由上消化道吸收并参与代谢时主要发生还原和结合反应,生成四氢姜黄素、六氢姜黄素、姜黄素葡萄糖苷酸、硫酸化姜黄素等特征代谢物。近年来,姜黄素在下消化道的代谢途径成为研究的热点。姜黄素不仅可被肠道菌群代谢为高活性代谢产物(如阿魏酸、四氢姜黄素、去甲氧基姜黄素、双去甲氧基姜黄素等),也可调节肠道菌群结构,维持菌群稳态。姜黄素的吸收和代谢过程及其与肠道菌群之间的相互作用,是揭示姜黄素健康效应和低生物利用度之间矛盾的关键。     

双去甲氧基姜黄素与姜黄素纳米乳药代动力学的比较研究

制备并考察双去甲氧基姜黄素纳米乳和单体姜黄素纳米乳的药代动力学特征。雄性SD大鼠口服灌胃分别给予双去甲氧基姜黄素纳米乳和单体姜黄素纳米乳后,于大鼠眼底静脉丛取血,采用HPLC法测定血浆中单体双去甲氧基姜黄素和姜黄素的浓度,DAS 2.1.1药动学软件计算药动学参数。得到双去甲氧基姜黄素纳米乳和单体姜黄素纳米乳主要药动学参数Tmax为1.50h和1.00 h;C_(max)为(85.87±2.53)和(85.60±2.30)μg/L;AUC0~72 h为(788.23±52.04)和(1 345.50±64.88)μg/L·h。表明姜黄素纳米乳的口服生物利用度比双去甲氧基姜黄素纳米乳更好。     

姜黄素生理活性、代谢以及生物利用度的研究进展

姜黄素是一种多酚类化合物,着色能力强,是世界上销量最大的七大天然食用色素之一,是被WHO和FDA公认的天然食品添加剂。除此之外,姜黄素因其具有分子中含有多个双键,同时还有酚羟基和羰基等活性基团,在抗肿瘤、抗炎、抗氧化、清除自由基、抗微生物以及对心血管系统、消化系统等多方面均有疗效,但其生物利用度低限制了在医药方面的应用,因此如何提高姜黄素的生物利用度成为国内外研究者共同关注的课题。该文从国内外研究现状出发,对姜黄素的生理活性及应用进行概括,并对姜黄素体内代谢途径进行综述,分析指出姜黄素生物利用度低的原因,并介绍研究姜黄素生物利用度的模型和提高其生物利用度的方法,为全面系统研究姜黄素生物利用度打下基础。     

姜黄素膜运载体系的构建及功能性应用研究进展

姜黄素因具有多种生物活性而获得广泛的研究关注,但由于其低水溶性和生理转运过程中的生化/结构降解,导致其生物利用度低下,制约其经济价值。因此,大量以姜黄素为基础的药物递送系统被引入,其中,将姜黄素纳入以生物聚合物为基础的膜运载体系被认为具有广阔的发展前景。多糖、蛋白质等都是经过广泛研究的聚合物载体,能够用于输送多种生物活性天然化合物。本文对姜黄素分子递送过程中存在的挑战以及构建姜黄素膜运载体系的研究进展进行概述,着重阐述姜黄素膜运载体系在食品抗氧化包装、新鲜度监测以及抗菌保鲜等方面的应用,旨在为姜黄素的进一步开发与应用提供理论参考。     

叶酸和辛烯基琥珀酸酐双修饰菊粉胶束对姜黄素的荷载特性

叶酸修饰两亲性多糖是一种有效的疏水活性物质载体，能增加疏水活性物质的结肠靶向转运。以叶酸和辛烯基琥珀酸酐双修饰菊粉（folic acid octenylsuccinate inulin，FA-OS-菊粉）自聚集形成荷载姜黄素的胶束为研究对象，以胶束颗粒粒径、多分散性指数和姜黄素保留率为指标，探究了该胶束的热处理稳定性、冻融稳定性、贮藏稳定性及体外模拟胃肠液消化稳定性和释放特性。结果：荷载姜黄素FA-OS-菊粉胶束在热处理和贮藏过程中姜黄素保留率较高，但粒径和多分散性指数变化显著；消化结束时，FA-OS-菊粉胶束在模拟胃液中的姜黄素释放率小于2%，在模拟肠液中的姜黄素释放率小于10%，具有较好的控释效果。结论：荷载姜黄素FA-OS-菊粉胶束具有潜在的结肠靶向效果。     

姜黄素脂质体的研究进展

姜黄素具有多种药理活性,但其不稳定性、低水溶性以及较低的生物利用率极大限制了姜黄素的临床应用。为改善其理化特性和提高其生理功能,研究者对姜黄素剂型进行了广泛研究,其中姜黄素脂质体的研究已取得一定进展,本文综述了近年来姜黄素脂质体的制备技术、质量评价及其生理特性,为进一步开发利用姜黄素脂质体提供一定的参考。     

Curcumin in cancer management: recent results of analogue design and clinical studies and desirable future research

The ability of the curry constituent curcumin to delay the onset of cancer has been the topic of extensive research for many years. Abundant literature is devoted to mechanisms by which curcumin may mediate this activity. These insights have prompted investigations in which curcumin as lead molecule serves as a scaffold for synthetic chemical attempts to optimize pharmacological potency. Among the published analogues with notable efficacy are dimethylcurcumin, 1,5-bis(3-pyridyl)-1,4-pentadien-3-one and 3,5-bis-(2-fluorobenzylidene)-piperidinium-4-one acetate. Results of a small number of clinical pilot studies conducted with curcumin at doses of up to 12 g suggest tentatively that it is safe in humans. Prevention of adenoma recurrence constitutes a clinical paradigm worthy of further investigation for curcumin. Future clinical study should include measurement of mechanism-based pharmacodynamic parameters.     

Anticancer and carcinogenic properties of curcumin: considerations for its clinical development as a cancer chemopreventive and chemotherapeutic agent

A growing body of research suggests that curcumin, the major active constituent of the dietary spice turmeric, has potential for the prevention and therapy of cancer. Preclinical data have shown that curcumin can both inhibit the formation of tumors in animal models of carcinogenesis and act on a variety of molecular targets involved in cancer development. In vitro studies have demonstrated that curcumin is an efficient inducer of apoptosis and some degree of selectivity for cancer cells has been observed. Clinical trials have revealed that curcumin is well tolerated and may produce antitumor effects in people with precancerous lesions or who are at a high risk for developing cancer. This seems to indicate that curcumin is a pharmacologically safe agent that may be used in cancer chemoprevention and therapy. Both in vitro and in vivo studies have shown, however, that curcumin may produce toxic and carcinogenic effects under specific conditions. Curcumin may also alter the effectiveness of radiotherapy and chemotherapy. This review article analyzes the in vitro and in vivo cancer-related activities of curcumin and discusses that they are linked to its known antioxidant and pro-oxidant properties. Several considerations that may help develop curcumin as an anticancer agent are also discussed.     

Bidirectional interactions between dietary curcumin and gut microbiota

Abstract

Curcumin is a polyphenolic compound with a long history of use as an herbal remedy, dietary spice, and food-coloring agent. Despite curcumin possesses a wide range of biological and pharmacological activities, it exhibits extremely poor bioavailability, which makes its pharmacology intriguing and also hinders its clinical application. In recent years, there is ample evidence supporting the associations between the alteration of gut microbiota and many diseases. Interestingly, after oral administration, curcumin shows its preferential distribution and accumulation in the intestine. In view of the above aspects, we reviewed the updated knowledge regarding the bidirectional interactions between curcumin and gut microbiota from two perspectives: (1) gut microbiota regulation by curcumin and (2) curcumin biotransformation by digestive microbiota. Besides the study deals with 3 potential pharmacological implications: (1) identification of metabolites being more active and bioavaliable than parent curcumin; (2) assessment of contribution of gut microbiota regulation of curcumin to its pharmacological effects and (3) development of gut microbiota regulation-based disease prevention/treatment strategy for curcumin in view of its clinical safety. This review is important to deepen our understanding of the mechanisms of action of curcumin and to provide future directions about how to use this natural compound to combat human diseases.     

New mechanisms and therapeutic potential of curcumin for colorectal cancer

Curcumin is a polyphenol derived from Curcuma longa. Over the last few years, a number of studies have provided evidence of its main pharmacological properties including chemosensitizing, radiosensitizing, wound healing activities, antimicrobial, antiviral, antifungical, immunomodulatory, antioxidant and anti-inflammatory. More recent data provide interesting insights into the effect of this compound on cancer chemoprevention and chemotherapy. In fact, preclinical studies have shown its ability to inhibit carcinogenesis in various types of cancer including colorectal cancer (CRC). Curcumin has the capacity of interact with multiple molecular targets affecting the multistep process of carcinogenesis. Also, curcumin is able to arrest the cell cycle, to inhibit the inflammatory response and the oxidative stress and to induce apoptosis in cancer cells. Likewise, it has been shown to possess marked antiangiogenic properties. Furthermore, curcumin potentiates the growth inhibitory effect of cyclo-oxygenase (COX)-2 inhibitors and traditional chemotherapy agents implicating another promising therapy regimen in the future treatment of CRC. However, its clinical advance has been hindered by its short biological half-life and low bioavailability after oral administration. This review is intended to provide the reader an update of the bioavailability and pharmacokinetics of curcumin and describes the recently identified molecular pathways responsible of its anticancer potential in CRC.     

生姜现代药理学特性研究进展

生姜是一种常见且广泛使用的中国传统中草药,它富含多种化学成分,包括酚类化合物、萜烯类、纤维素、糖类等,而生姜益于健康的主要原因在于其存在的姜辣素、姜黄素、姜精油等多种生物活性成分。许多年来,不少研究者挖掘了生姜的现代药理学特性,无论是对人体的抗癌、抗炎、增强免疫力、降脂降糖,还是作为化学物质的抑菌、抗氧化等,都表明生姜具有重要的营养价值和医药功效。本文针对姜中姜辣素、姜黄素、姜精油、姜多糖的抗肿瘤、降脂降糖、抗氧化、抑菌等现代药理学特性的研究进展进行了梳理和总结,并讨论了相关的作用机制,明确了生姜作为一种药食两用植物的主要功效成分和研究热点,以期为生姜产品的深入研发和疾病预防的潜力挖掘提供必要的理论知识基础。     

花青素与姜黄素在食品包装领域的应用

花青素和姜黄素对于活性包装至关重要,探讨其内在机理,可为花青素、姜黄素智能包装膜的相关研究提供理论参考。本文综述了花青素、姜黄素的结构和性质、提取方法、抗氧化活性、花青素和姜黄素在食品包装上的应用以及两种色素混合在食品包装上的应用。花青素和姜黄素由于其自身结构特点,在不同的pH下有不同的颜色,花青素作为颜色指示剂变色范围广,但性质不稳定,易受到外界因素影响。姜黄素稳定性高于花青素,但变色范围窄。此外,两者均具有很好的抗氧化活性,可作为颜色指示剂与抗氧化剂应用在食品包装中。花青素和姜黄素的变色特点、稳定性以及功能活性对食品新鲜度指示包装的性能具有显著的影响,将两种色素混合作为指示剂添加到食品包装中,有助于提高花青素的稳定性,从而获得更好的指示效果。     

姜黄素的生理功能及其在方便面中的应用

本文介绍了姜黄素的防癌、抗癌功能及其作用机理,同时介绍了姜黄素产品在方便面中的应用。     

姜黄素的抗氧化机制及以其为先导物的抗氧化化合物研究进展

姜黄素具有抗氧化、抗肿瘤、抑菌等多种药理活性。近年来为开发姜黄素类抗氧化剂,国内外研究者设计和合成了大量姜黄素衍生物。本文介绍了姜黄素及其衍生物的抗氧化机制,重点概述基于抗氧化的姜黄素抗氧化衍生物的研究进展。     

Emerging importance of dietary phytochemicals in fight against cancer: Role in targeting cancer stem cells

Recent years have seen an unpretending increase in research using dietary phytochemicals for targeting cancer and cancer stem cells (CSCs) due to the limited efficacy of conventional chemotherapy and radiotherapy and numerous associated side effects. A large number of dietary phytochemicals using traditional recommendation and experimental approaches have been demonstrated to have anti-proliferative, anti-metastatic, reactive oxygen species (ROS) inducing, anti-angiogenic, pro-apoptotic effects and efficacy in targeting cellular molecules and pathways implicated in malignancy. Researchers have shown the knack of phytochemicals in interfering with the CSCs self-renewal process. Thus, dietary phytochemicals can play a significant role in the cancer therapy owing to the plethora of targets without toxicity. In this review, we have discussed about the basic knowledge of CSCs, their identification, characterization, mechanism of self-renewal pathways (Wnt/β-catenin, Hedgehog, and Notch), features that help in the survival of CSCs and use of phytochemicals to replace chemotherapy. Applications of phytochemicals including curcumin, epigallocatechin-3-gallate (EGCG), resveratrol, lycopene, and sulforaphane for their effect on targeting cancer and in particular CSCs along with their molecular mechanisms responsible for pharmacological action are also discussed.