白藜芦醇的植物来源、药理活性及应用(英文)

在过去的数十年中,白藜芦醇作为一种广为人知的化合物,表现出多种生物活性。大量的研究表明,白藜芦醇作为一种天然产物,不仅具有潜在的应用价值,而且对多种人类疾病有治疗作用且副作用较小。本文综述了白藜芦醇的生物来源、药理作用及临床应用现状。     

桑中氧化白藜芦醇的研究进展

对近年来氧化白藜芦醇的研究进展进行总结。认为氧化白藜芦醇目前来源主要有天然植物提取、化学合成和生物转化3种途径,能快速被机体吸收且较低血药浓度就能发挥抗肿瘤、抑制酪氨酸活性,抗肥胖、神经保护等药理作用。     

白藜芦醇对M1/M2巨噬细胞极化的作用及其机制

目的研究白藜芦醇对M1/M2型巨噬细胞极化以及M1/M2型巨噬细胞能量代谢的影响。方法建立了骨髓来源巨噬细胞(BMDM)的体外培养模型。在BMDM以及Raw264.7细胞中加入白藜芦醇,应用RT-q PCR以及Western blot检测M1、M2型巨噬细胞的标志分子。应用细胞外流量测试仪检测白藜芦醇M1、M2型巨噬细胞能量代谢的影响。结果白藜芦醇可以促进M2型巨噬细胞极化,抑制M1型巨噬细胞极化。白藜芦醇促进M2型巨噬细胞标志蛋白arginase1的表达,同时也会促进抗炎细胞因子IL-10的表达。LPS具有促进M1型巨噬细胞糖酵解的功能,而白藜芦醇可以抑制LPS引起的巨噬细胞糖酵解增加。结论白藜芦醇作为天然产物之一,可通过抑制NO生成进而调控M1/M2型巨噬细胞的能量代谢,促进M2型巨噬细胞的极化。     

虎杖白藜芦醇及其脂质体剂型对帕金森病模型大鼠黑质细胞保护作用的研究

目的:氧化应激是帕金森病发病机制中的重要病理因素,是导致黑质多巴胺能神经元死亡的主要原因之一.白藜芦醇具有广泛的药理学作用和较强的抗氧化特性.本研究探讨从中药虎杖提取的白藜芦醇及其脂质体制剂对帕金森病模型大鼠黑质细胞的保护效应,为临床帕金森病治疗药物的开发提供实验依据.方法:实验用Wistar大鼠50只,随机分为正常组、假手术组、模型组、白藜芦醇干预组、白藜芦醇脂质体干预组,以6-羟基多巴胺单侧纹状体微量注射法制备帕金森病大鼠模型.白藜芦醇干预组及白藜芦醇脂质体干预组在造模成功后,以白藜芦醇、白藜芦醇脂质体灌胃,20 mg·kg-1,1次/d,连续14 d.观察各组大鼠的旋转行为学改变,采用HE染色、Nissl染色、酪氨酸羟化酶(TH)免疫组化方法统计黑质细胞总数、神经元总数、多巴胺能神经元数量,采用TUNEL法检测黑质细胞凋亡,以分光光度法检测黑质区总ROS活力和总抗氧化能力.结果:帕金森病模型大鼠在阿普吗啡诱导后,出现明显的行为学异常表现,黑质区细胞总数、神经元总数及多巴胺能神经元数量明显减少,凋亡细胞数量增加,组织总ROS活力显著增强,总抗氧化能力明显降低.白藜芦醇及白藜芦醇脂质体均能明显改善模型大鼠行为学异常,增加黑质区细胞总数、神经元总数、多巴胺能神经元数量,降低细胞凋亡率,提高组织总抗氧化能力,降低组织总ROS活力.在组织学指标的改善方面,白藜芦醇脂质体的效应较白藜芦醇单体更强.结论:中药虎杖来源的白藜芦醇及白藜芦醇脂质体对帕金森病模型大鼠黑质细胞具有明显的保护作用,这种保护作用可能与抗氧化活性有关.白藜芦醇脂质体较白藜芦醇单体在组织学指标改善上作用更强,可能与脂质体制剂提高了白藜芦醇的生物利用度有关.白藜芦醇脂质体可能是更有效的口服给药方式.     

虎杖野生植株及组织培养物中白藜芦醇和虎杖苷含量的比较

目的:比较白藜芦醇和虎杖苷在不同来源的虎杖材料中含量积累的差异,以期筛选出适宜的培养材料用于进一步的代谢调控研究。方法:采用反相高效液相色谱法对不同样品中白藜芦醇及虎杖苷的含量同时进行检测。结果:在多年生野生植株和室内人工栽培幼苗中,白藜芦醇和虎杖苷均在植物根及根茎部特异性累积,其含量要远远高于叶片和茎段。其中,以室内人工栽培3个月的幼苗中有效成分含量较高,虎杖苷的积累量为1.27%,是野生植株的1.25倍,白藜芦醇含量(0.401%)则接近野生植株水平。从虎杖的各种组织培养物中也可检测到白藜芦醇和虎杖苷的存在,但是二者含量的高低与培养物的生长速度、生理状况及发育时期密切相关。在几种培养物中,以毛状根的培养最具潜力,离体培养30 d后,其干重增长率为8.29,分别是自然根和悬浮细胞的8.4倍和192.8倍,而且还可积累一定量的虎杖苷(0.037%)和白藜芦醇(0.007%)。结论:所建立的分析检测方法,具有快速、简便和准确的特点,尤其适于大批量生物样品的同时测定。在几种不同来源的虎杖材料中,毛状根是适宜大规模培养并可持续收获有效成分的培养物。     

紫檀芪的研究进展

紫檀芪(Pterostilbene)作为反式二苯乙烯类化合物,是白藜芦醇的甲基化衍生物,具有抗氧化、抗肿瘤、降血脂和抑菌等多种生物活性,且生物利用度比白藜芦醇更高、更稳定。本文通过国内外文献的整理分析,对紫檀芪的天然来源、化学合成、生物合成、检测方法、代谢情况以及药理活性等方面的研究进行综述,探讨紫檀芪作为药物候选化合物的潜力,以期给研究者提供更多信息,同时也为紫檀芪的其他应用,如保健品、护肤品等研究提供文献依据。     

虎杖中白藜芦醇的超声提取及其抗氧化性研究

目的:探讨虎杖中白藜芦醇的超声波辅助浸提工艺及其抗氧化活性.方法:采用单因素和正交实验设计,研究了料液比、乙醇浓度、超声时间以及超声温度对白藜芦醇提取率的影响,并对白藜芦醇清除羟基自由基的抗氧化活性进行研究.结果:提取白藜芦醇的最佳工艺条件为:乙醇浓度80%,料液比1:25(g/mL),超声时间35 min,超声温度50℃.白藜芦醇具有清除羟基自由基的活性,且该活性与白藜芦醇浓度呈一定的量效关系.结论:获得了最佳提取工艺条件,该条件下白藜芦醇提取率为0.52%;白藜芦醇具有较强的抗氧化活性.     

基于理化性质 生物利用度和靶向递送的白藜芦醇现代药剂学研究进展

白藜芦醇是虎杖的主要活性成分,具有神经保护、抗肿瘤、抗菌等广泛的药理活性。然而白藜芦醇因水溶性差、生物利用度低、体内代谢迅速等缺点,限制了其在临床上的应用。基于白藜芦醇的理化性质和药理活性,探讨提高其生物利用度和改善白藜芦醇靶向递送的现代药剂学应用,为研究开发白藜芦醇新型给药系统提供理论依据。     

虎杖中白藜芦醇、白藜芦醇苷提取工艺的研究

目的 考察虎杖药材中白藜芦醇、白藜芦醇苷的最佳提取工艺.方法 采用HPLC法,以白藜芦醇、白藜芦醇苷为指标,通过单因素实验及正交试验确定从虎杖中提取白藜芦醇、白藜芦醇苷的最佳工艺.结果 虎杖药材的最佳提取工艺为:70％乙醇25倍量,加热时间为120min,辅助超声25 min.结论 该实验确定的最佳提取工艺稳定性好且简...     

白藜芦醇制备与制剂研究进展

白藜芦醇具有抗肿瘤、抗突变、抗炎、抗氧化、雌激素调节等多方面有益人类健康的生物药理活性。白藜芦醇作为来自种子植物中的抗毒素,对人类健康有着特殊保健功能,具有较高推广和综合利用价值,引起了生物医学界工作者高度重视。综述白藜芦醇在制备和制剂方面的研究进展,为开发与利用白藜芦醇提供依据。     

白藜芦醇对脑缺血损伤的保护作用及机制研究进展

脑缺血及其再灌注损伤是全球人口死亡和致残的主要原因之一,从天然植物或药物中提取单体开发神经保护剂已成为治疗脑缺血损伤的关键方法。白藜芦醇作为一种天然多酚类化合物,广泛存在于植物与食物中。大量研究表明白藜芦醇可通过保护血脑屏障、抑制炎症反应、抗氧化应激、抑制细胞凋亡、调节自噬等多种途径改善脑缺血损伤。在治疗及预防脑缺血损伤方面,白藜芦醇的有效性已被证实,但其具体的作用机制及分子靶点尚未完全阐明。因此,通过分析近10年国内外相关文献,对白藜芦醇治疗脑缺血损伤的作用靶点及机制研究、药动学、药物递送系统及安全性评价等进行综述,为白藜芦醇的开发和推广应用提供理论依据。     

白藜芦醇诱导肿瘤细胞凋亡研究进展

白藜芦醇是一种具有抗氧化、抗肿瘤、诱导细胞凋亡等生物活性的天然多酚类化合物。本文对近年来白藜芦醇诱导人宫颈癌HeLa细胞、白血病细胞、肝癌细胞和胃癌细胞等细胞凋亡方面的研究进展进行了分析和总结,并重点探讨了白藜芦醇诱导肿瘤细胞凋亡的分子机制,总结了白藜芦醇通过阻滞细胞周期、调节相关基因及蛋白表达和线粒体诱导细胞凋亡途径的研究现状,以及白藜芦醇作为肿瘤药物在临床研究中的潜在应用前景。     

白藜芦醇纳米乳的制备及大鼠体内的药动学研究

目的制备白藜芦醇纳米乳并探讨其在大鼠体内的药动学行为。方法以油酸乙酯作为油相,聚氧乙烯氢化蓖麻油RH40为乳化剂,无水乙醇为助乳化剂,采用滴定法绘制伪三元相图以优化纳米乳处方,对所制备的白藜芦醇纳米乳进行粒径、透射电镜及红外光谱测定等理化性质的表征。大鼠ig给药后,采用HPLC测定其血药浓度,计算其药动学参数,利用DAS软件分析其药动学特征。结果白藜芦醇纳米乳处方为药物-油相-混合乳化剂-水的质量比为1∶10∶24∶65,所制备纳米乳的粒径为40 nm左右,电镜观察其形态为圆形球状结构,红外光谱结果表明白藜芦醇以活性的反式结构存在于纳米乳的油相中。与白藜芦醇混悬剂相比,白藜芦醇纳米乳在大鼠体内的血药浓度时间曲线下面积(78.89 h·μg/mL)为混悬剂(54.42h·μg/mL)的1.45倍,达峰浓度(3.29μg/mL)是混悬剂(1.70μg/mL)的1.93倍,可以提高白藜芦醇口服给药的生物利用度。结论所制备的纳米乳制剂有希望为白藜芦醇的有效递送提供新的给药途径。     

白藜芦醇脂质体对C6胶质瘤细胞的抑制作用分析

目的:制备白藜芦醇脂质体并对其体外抗肿瘤作用进行评价。方法:通过薄膜分散-硫酸铵梯度法制备白藜芦醇脂质体,使用粒度仪对脂质体进行表征;确定C6胶质瘤细胞对数生长期;通过磺酰罗丹明B蛋白(SRB)法评价游离白藜芦醇及其脂质体对C6胶质瘤细胞的抗增殖作用,利用流式法考察白藜芦醇及其脂质体对C6胶质瘤的凋亡作用,以及C6胶质瘤细胞对白藜芦醇和其脂质体的摄取作用。结果:白藜芦醇脂质体的平均粒径(139.97±0.64)nm,Zeta电位(-7.00±0.74)m V;游离白藜芦醇和白藜芦醇脂质体对C6胶质瘤细胞的抑制率最高分别可达(73.30±0.56)%和(91.70±0.60)%,差异有统计学意义(P0.05);游离白藜芦醇和白藜芦醇脂质体对C6胶质瘤细胞的诱导凋亡率分别为(20.03±0.85)%和(27.18±0.96)%,差异有统计学意义(P0.05);C6胶质瘤细胞对游离白藜芦醇和白藜芦醇脂质体的摄取率分别为(67.79±1.19)%和(77.61±1.67)%。结论:相比于游离的白藜芦醇,白藜芦醇脂质体对C6胶质瘤细胞的抗增殖作用更明显,具有更强的诱导C6胶质瘤细胞凋亡作用。白藜芦醇脂质体可以更多地被C6胶质瘤细胞摄取,这在一定程度上促进了其对C6胶质瘤细胞的抗增殖作用和诱导凋亡能力。说明白藜芦醇脂质体具有较强的体外抗C6胶质瘤作用。     

Resveratrol inhibits mucin gene expression, production and secretion from airway epithelial cells

The study investigated whether resveratrol significantly affects mucin gene expression, production and secretion from airway epithelial cells. Confluent NCI‐H292 cells were pretreated with resveratrol for 30 min and then stimulated with EGF (epidermal growth factor), PMA (phorbol 12‐myristate 13‐acetate) and TNF‐α (tumor necrosis factor‐α) for 24 h, respectively. The MUC5AC gene expression and mucin protein production were measured by RT‐PCR and ELISA. The effect of resveratrol on TNF‐α‐ or PMA‐induced activation of NF‐κB p65 was also examined. Confluent primary rat tracheal surface epithelial (RTSE) cells were pretreated with adenosine triphosphate (ATP) for 5 min and then treated for 30 min in the presence of resveratrol to assess the effect on mucin secretion using ELISA. The results were as follows: (1) resveratrol inhibited the expression of MUC5AC gene induced by EGF or PMA or TNF‐α from NCI‐H292 cells; (2) resveratrol also inhibited the production of MUC5AC mucin protein induced by the same inducers from NCI‐H292 cells; (3) resveratrol inhibited the activation of NF‐κB p65 by TNF‐α or PMA in NCI‐H292 cells; (4) resveratrol significantly decreased ATP‐induced mucin secretion from cultured RTSE cells. This result suggests that resveratrol can regulate mucin gene expression, production and secretion, by directly acting on airway epithelial cells. Copyright © 2011 John Wiley & Sons, Ltd.     

汉中地区虎杖中白藜芦醇苷及苷元含量的测定

目的 测定汉中地区虎杖中白藜芦醇苷及苷元的含量。方法 采用HPLC法直接测定，色谱柱为EclipseXDBC8柱，流动相为乙腈－水，流速为1mL/min，检测波长为303nm。结果 虎杖中白藜芦苷的含量为2．5％，白藜芦醇的含量为0．43％。结论 汉中地区虎杖中白藜芦醇的含量为首次报道，白藜芦醇苷的含量高于文献报道的结果。     

Therapeutic Potential of Resveratrol in Type I Gaucher Disease

Resveratrol is a natural polyphenol that possesses various beneficial properties, such as anti‐inflammatory, anti‐oxidant, and neuroprotective effects. This study evaluated the potential therapeutic effects of resveratrol on primary fibroblasts derived from a patient with Gaucher disease. 3‐(4,5‐Dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assays were carried out to determine whether resveratrol affects cell survival. Changes in the expression levels of apoptosis‐inducing factor (AIF), Bax, cleaved caspase‐3, acetyl‐coenzyme A acetyltransferase 1 (ACAT1), E3‐binding protein (E3BP), and citrate synthase (CS) were determined by western immunoblot to characterize the effect of resveratrol treatment on Gaucher disease cells. Intracellular glucosylceramide levels in resveratrol‐treated patient cells were determined by thin‐layer chromatography (TLC). Resveratrol significantly increased the viability of patient cells in comparison with that of control cells. After exposure to resveratrol, expression levels of the apoptotic factors AIF, Bax, and cleaved caspase‐3 dose‐dependently decreased, while those of ACAT1, E3BP, and CS dose‐dependently increased. TLC showed a significant decrease in glucosylceramide levels in patient cells treated with resveratrol. These findings demonstrate that resveratrol can reduce apoptotic events and glucosylceramide levels in Gaucher disease cells, and that it merits further research as a possible therapeutic compound. Copyright © 2015 John Wiley & Sons, Ltd.     

The effect of resveratrol supplementation on biomarkers of liver health: A systematic review and meta-analysis of randomized controlled trials

This study aimed to evaluate the effect of resveratrol on liver biomarkers in adult participants, using systematic review and meta-analysis of randomized controlled trials. PubMed, Scopus, Web of Science and Cochran Library was searched, up to October 2021. The pooled effects were calculated using a random-effects model and expressed as weighted mean difference and 95% confidence interval. The methodological quality of studies as well as certainty of evidence were assessed by standard tools. Thirty-seven relevant trials were found. Although overall analysis found no significant change, subgroup analysis showed a significant improvement in alanine aminotransferase (ALT; −7.79 U/L) and glutamyl transferase (−6.0 U/L) in patients with liver disorders, and ALT (−2.22 U/L) in younger adults; however, high-dose supplementation (>1,000 mg/day) appeared to increase alkaline phosphatase concentration (+5.07 U/L). ALT also increased in older adults (+2.33 U/L) following resveratrol supplementation. We found resveratrol did not have a significant effect on liver health in the general population. However, resveratrol could be effective in patients with liver disorders. Our findings also suggest that high-dose resveratrol administration and supplementation in older adults should be performed with caution. Further high-quality clinical trials are also needed to firmly establish the clinical efficacy of resveratrol.     

Dimerization of resveratrol by the grapevine pathogen Botrytis cinerea

Resveratrol (trans-3,4',5-trihydroxystilbene) is produced by grapes (Vitis spp.) in response to microbial attack by the fungal grapevine pathogen Botrytis cinerea. Several reports indicate that pathogenic B.cinerea strains are capable of biotransforming resveratrol into an assortment of unidentified oxidized metabolites as a means of reducing the antifungal effects of resveratrol and facilitating Botrytis invasion into host-plant tissues. Studies utilizing growing incubations of Botrytis cinerea ATCC 11542 with resveratrol resulted in the production of three new (restrytisols A-C) (1-3) and three known (resveratrol trans-dehydrodimer, leachinol F, and pallidol) oxidized resveratrol dimers. All of the metabolites were evaluated for their anti-HIV-1, cytotoxic, and cyclooxygenase (COX) I and COX II inhibitory activities.