姜黄素衍生物合成的研究进展

大量研究表明姜黄素具有抗肿瘤、抗炎、抗氧化、抗肝细胞毒性、抗菌等作用,在保健品及药物开发利用方面具有广泛的前景.近年来,以姜黄素为先导化合物,进行结构修饰合成其衍生物巳成为国内外研究的热点,国内外学者合成了大量的姜黄素衍生物.本文将对姜黄素衍生物合成的研究进展做简要的综述.     

姜黄素药理作用的研究进展

姜黄素是中药姜黄中提取的一种亲脂性多酚,具有抗炎、抗感染、抗氧化、抗肿瘤等多种药理作用.姜黄素在神经炎症疾病、风湿性疾病、感染性疾病、恶性肿瘤、动脉粥样硬化和心肌梗死中表现出较好的治疗潜力,已成为研究热点之一.现综述姜黄素药理研究的新进展.     

姜黄素的药理作用及临床应用

姜黄素是一种植物多酚,具有抗氧化、抗炎、抗肿瘤、肝保护等多种药理作用,且毒性低、安全性高,具有广阔的开发应用前景。本文通过综述姜黄素的药理作用,着重介绍近年来姜黄素对心脑血管疾病、消化系统疾病的实验研究和临床应用方面的进展。     

姜黄素研究进展

姜黄素(curcumin,Cur)是从姜科植物姜黄Curcuma longa L.中提取的一种酚类化合物,具有抗氧化、抗炎、抗肿瘤、抗HIV病毒、抗动脉粥样硬化、降血脂等作用。从姜黄素的理化性质、药理作用、体内代谢过程、新剂型研究进展、临床运用实验等方面进行归纳,探讨姜黄素开发成外用制剂的可行性。     

姜黄素的提取分离及其药理作用的研究近况

姜黄素是植物中天然成分,具有调节消化系统功能,以及保护心脑血管、抗微生物、清除自由基、抗癌、抗炎和抗氧化调节等功效。由于其提取分离工艺的不断发展,采用许多种方法从植物中获得姜黄素。综述姜黄素的提取分离方法及其在抗肿瘤和保护心脑血管等药理作用文献,并对其研究进展作了分析。     

具有抗肿瘤活性的姜黄素衍生物研究进展

姜黄素是一种具有抗肿瘤、抗阿尔茨海默病、抗氧化、抗炎、抗病毒等多种生物活性的天然多酚,但其存在生物利用度低、水溶性较差等缺点,使其临床应用受到限制。基于此．研究人员对姜黄素展开了大量的结构改造工作,以期能改善其生物活性及成药性。综述了具有抗肿瘤活性的姜黄素衍生物的研究进展,旨在为相关药物的研发提供参考。     

姜黄素生物利用度研究进展

姜黄素是姜黄的主要活性成分之一,在亚洲特别是印度和中国的药用历史悠久,还被广泛用于色素、食品添加剂及调味品。研究显示,姜黄素具有抗肿瘤、抗突变、抗增生、抗炎、抗氧化、抗人类免疫缺陷病毒、免疫调节、保护肝脏和肾脏及抗纤维化等药理作用。姜黄素所显现出来的生物化学特性使其成为有史以来最强大的化学预防剂和抗癌剂的代表之一。     

姜黄素调控非编码RNA抗肿瘤的研究进展

姜黄素是姜黄中一种小分子多酚化合物，是姜黄发挥生物活性的最主要成分，具有抗炎、抗氧化、抗病毒、抗肿瘤等广泛的药理作用。近年来，非编码RNA（ncRNA）作为姜黄素潜在的治疗靶点被广泛研究。姜黄素可通过ncRNA影响调控肿瘤细胞增殖、凋亡和迁移的关键信号通路或直接作用于相关蛋白进而发挥抗肿瘤作用。综述了姜黄素参与调控微小RNA（miRNA）、长链非编码RNA（LncRNA）和环状RNA（circRNA）发挥抗肿瘤作用的情况，希望对姜黄素的抗肿瘤研究提供参考依据。     

芒果苷及其衍生物的药理作用研究进展

芒果苷本身具有抗炎、抗氧化、抗肿瘤等多种药理作用,其衍生物更是改进了原料水溶性和脂溶性不佳的问题,使其发挥出更好的药效作用。本文主要就近5年来芒果苷及其衍生物的药理作用研究进行综述,以期为今后开展更深入的研究提供参考。     

提高姜黄素生物利用度方法的研究进展

摘 要 姜黄素是姜黄的主要活性成分之一,具有抗炎、抗氧化、抗肿瘤、抗血管粥样硬化、保护肝肾等多种药理作用,但生物利用度低限制了其在临床上的应用。本文参考大量文献,对提高姜黄素生物利用度的方法进行了综述。总结出姜黄素可通过不同的给药途径、制备成不同剂型等方法来提高其生物利用度,为新药的研发提供理论基础和研究思路。     

单羰基姜黄素类似物的结构改造及药理作用研究进展

姜黄素是中药姜黄的主要活性成分,具有抗肿瘤、抗炎、抗氧化等多种药理活性。临床前研究发现,姜黄素具有体内代谢速度快、溶解度不高、生物利用度低等缺陷,因此,其临床应用受到了限制。近年来国内外科学家以姜黄素为先导化合物,设计合成了大量的单羰基姜黄素类似物,并对其药理活性进行了评价,以解决姜黄素存在的缺陷。本文从单羰基姜黄素类似物连接链的角度进行分类,分别对1,4-戊二烯-3-酮类、环酮类和查尔酮类姜黄素类似物的设计合成、活性测试和构效关系等方面进行综述,并对未来姜黄素类似物的设计合成进行展望,为开发更为高效的姜黄素类新药提供参考。     

姜黄素单羰基类似物的研究进展

目的总结近几年来姜黄素单羰基类似物在合成、稳定性及药理活性方面的研究进展。方法通过检索查找相关文献。结果合成的姜黄素单羰基类似物不仅稳定性有所提高,且其药理活性也有所提高。结论姜黄素单羰基类似物具有进一步的研究价值和良好的应用前景。     

姜黄素衍生物的合成方法研究进展

姜黄素是姜科和天南星科植物中广泛存在的一种色素,具有抗肿瘤、抗炎、抗氧化等活性,毒性低,但其临床应用因稳定性差、生物利用度低而受到限制。近年来,对姜黄素衍生物的合成方法主要分为两类,一是改变姜黄素的哥二酮结构或苯环结构,设计合成其类似物;二是在姜黄素结构中引入其他活性小分子。通过以上结构改造,能够有效改善姜黄素的稳定性、溶解度及生物活性,为其临床应用创造了良好的前景。     

姜黄素纳米凝胶的制备及其应用研究进展

姜黄素是从姜黄根茎中提取分离得到的黄色多酚类化合物,具有抗肿瘤、抗炎、抗菌、抗氧化等广泛的药理活性。但由于其稳定性、水溶性差,生物利用度低等缺点严重地限制了姜黄素的治疗应用。纳米凝胶在改善姜黄素的溶解度、生物相容性、稳定性、靶向性和治疗效果方面均表现出良好的潜力。本文对姜黄素纳米凝胶的制备方法及其在肿瘤防治、创面治愈、炎症治疗和眼部给药等领域的应用进行综述,为姜黄素的进一步临床研究和应用开发提供文献参考。     

Antidepressant and anti-stress effects of curcumin inmice

Curcumin (diferuloylmethane), a yellow colouring agent contained in the rhizome of Curcuma Longa (turmeric), has a wide array of pharmacological and biological activities, such as antioxidant, anti-inflammatory, immunomodulating and anticarcinogenic effects. In this study, curcumin was examined for the antidepressant and anti-stress effects in forced swimming,     

Suppression of pro-inflammatory and proliferative pathways by diferuloylmethane (curcumin) and its analogues dibenzoylmethane, dibenzoylpropane, and dibenzylideneacetone: role of Michael acceptors and Michael donors

Curcumin, a diferuloylmethane, has been shown to exhibit anti-inflammatory and anti-proliferative activities. Whereas curcumin has both a Michael acceptor and a Michael donor units, its analogues dibenzoylmethane (DBM, a component of licorice) and dibenzoylpropane (DBP) have a Michael donor but not a Michael acceptor unit, and the analogue dibenzylideneacetone (DBA) has a Michael acceptor unit. In the current report, we investigated the potency of DBM, DBP, and DBA in relation to curcumin for their ability to suppress TNF-induced NF-κB activation, NF-κB-regulated gene products, and cell proliferation. We found that all four agents were active in suppressing NF-κB activation; curcumin was most active and DBM was least active. When examined for its ability to inhibit the direct DNA binding activity of p65, a subunit of NF-κB, only DBP inhibited the binding. For inhibition of TNF-induced IKK activation, DBA was most active. For suppression of TNF-induced expression of NF-κB-regulated gene products such as COX-2 (inflammation marker), cyclin D1 (proliferation marker), and VEGF (angiogenesis marker), DBA and curcumin were more active than DBM. Similarly for suppression of proliferation of leukemia (KBM-5), T cell leukemia (Jurkat), prostate (DU145), and breast (MDA-MB-231) cancer cells, curcumin and DBA were most active and DBP was least active. Overall, our results indicate that although curcumin and its analogues exhibit activities to suppress inflammatory pathways and cellular proliferation, a lack of Michael acceptor units in DBM and DBP can reduce their activities.     

Influence of tetrahydrocurcumin on hepatic and renal functional markers and protein levels in experimental type 2 diabetic rats

Curcumin is the most active component of turmeric. It is believed that curcumin is a potent antioxidant and anti-inflammatory agent. Tetrahydrocurcumin is one of the major metabolites of curcumin that exhibits many of the same physiologic and pharmacological activities as curcumin and in some systems may exert greater antioxidant activity than curcumin. Oral administration of tetrahydrocurcumin at 80 mg/kg body weight to diabetic rats for 45 days resulted in a significant reduction in blood glucose and significant increase in plasma insulin levels. In addition, the diabetic rats had decreased levels of plasma total protein, albumin, globulin and albumin/globulin ratio as compared to control rats. After treatment with tetrahydrocurcumin and curcumin total protein, albumin, globulin and albumin/globulin ratio were brought back to near normal. The activities of hepatic and renal markers were significantly elevated in diabetic rats as compared to control rats, and treatment with tetrahydrocurcumin and curcumin has reversed these parameters to near normal levels. In diabetic rats, the decreased levels of urea, uric acid and creatinine with increased levels of albumin and urine volume was observed, and treatment with tetrahydrocurcumin and curcumin reversed these parameters to near normal. Tetrahydrocurcumin appeared to have a better protective effect when compared to curcumin.     

Bioavailability of curcumin: problems and promises

Curcumin, a polyphenolic compound derived from dietary spice turmeric, possesses diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Phase I clinical trials have shown that curcumin is safe even at high doses (12 g/day) in humans but exhibit poor bioavailability. Major reasons contributing to the low plasma and tissue levels of curcumin appear to be due to poor absorption, rapid metabolism, and rapid systemic elimination. To improve the bioavailability of curcumin, numerous approaches have been undertaken. These approaches involve, first, the use of adjuvant like piperine that interferes with glucuronidation; second, the use of liposomal curcumin; third, curcumin nanoparticles; fourth, the use of curcumin phospholipid complex; and fifth, the use of structural analogues of curcumin (e.g., EF-24). The latter has been reported to have a rapid absorption with a peak plasma half-life. Despite the lower bioavailability, therapeutic efficacy of curcumin against various human diseases, including cancer, cardiovascular diseases, diabetes, arthritis, neurological diseases and Crohn's disease, has been documented. Enhanced bioavailability of curcumin in the near future is likely to bring this promising natural product to the forefront of therapeutic agents for treatment of human disease.     

Liposomal delivery system enhances anti-inflammatory properties of curcumin

Curcumin is a well-established natural antioxidant and anti-inflammatory agent. Up till now its potential in treatment of vaginal inflammation has not been evaluated. We are aiming at developing liposomal delivery system for curcumin targeting vaginal administration. Liposomes as nanosized phospholipid-based vesicles are expected to solubilize curcumin and enhance its activity, thus serving as an advanced topical formulation in the treatment of vaginal inflammation. Curcumin and curcuminoids were analyzed by the high-performance liquid chromatography method. Liposomes containing curcumin/curcuminoids of various sizes were prepared and characterized. Antioxidant activities of curcumin and liposomal curcumin were compared based on 1,1-diphenyl-2-picrylhydrazyl radical scavenging and superoxide dismutase activities. The anti-inflammatory activities were determined by measuring the inhibition of lipopolysaccharide -induced nitric oxide, interleukin-1β, and tumor necrosis factor-α production in macrophage RAW 264.7 cells. Curcumin/curcuminoids were encapsulated in phosphatidylcholine vesicles with high yields. Vesicles in the size range around 200 nm were selected for stability and cell experiments. Liposomal curcumin were found to be twofold to sixfold more potent than corresponding curcuminoids. Moreover, the mixture of curcuminoids was found to be more potent than pure curcumin in regard to the antioxidant and anti-inflammatory activities. Liposomal delivery systems for curcumin are promising formulations for the treatment of vaginal inflammation.     

Curcumin entrapped hyaluronan containing niosomes: preparation,characterisation and in vitro/in vivo evaluation

Curcumin, a natural polyphenolic compound, has numerous pharmacological activities; while it faces several bioavailability problems, due to its poor solubility and stability. So, many nanostructures have been designed to overcome these drawbacks. The aim of this study was to prepare a polymeric niosomal structure by incorporating hyaluronan to improve curcumin efficiencies. Hyaluronan containing niosomes were prepared by thin film hydration medium with slight modifications. In the formulation of hyaluronan containing niosomes size and zeta potential studies, Atomic Force Microscopy (AFM), Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), in-vitro release test, DPPH antioxidant assay and in-vivo anti-inflammatory test were investigated. The results showed that hyaluronan containing niosomes were 249.83?±?6.38?nm and the entrapment of curcumin was 98.28?±?0.278% (w/w). In addition, the shape of the hyaluronan containing niosomes was spherical. 500?µl of the prepared formulation with 4.002?×?10^?7 moles of curcumin showed 100% antioxidant effect. Moreover, the anti-inflammatory effect of the hyaluronan containing niosomes was higher than the anti-inflammatory effect of the simple suspension of curcumin.