黄酮类化合物对动物实验性肝损伤保护作用的研究进展

各种黄酮类化合物如黄酮类、黄酮醇类、二氢黄酮类、异黄酮类、黄烷酮类等对化学性肝损伤、药物性肝损伤、免疫性肝损伤、酒精性肝损伤、缺血/再灌注性肝损伤等实验性肝损伤均有不同程度的保护作用。这种保护作用与黄酮化合物清除自由基、抗氧化、抗脂质过氧化反应、调节免疫功能等有关。研究各种黄酮类化合物对动物实验性肝损伤的作用对于开发防治肝脏疾病的药物有重要意义。该文就近年来黄酮类化合物对动物实验性肝损伤作用的研究进展作一综述。     

黄酮类化合物抗心脑血管缺血性疾病作用的研究进展

黄酮类化合物是一种广泛存在于传统中药中的次生代谢产物,拥有许多生物活性和药理作用。近年来,研究发现黄酮类化合物可以通过多种途径在缺血性脑卒中和缺血性心脏病的治疗中发挥有效的保护作用,同时对于其保护作用的机制也有了较为详细系统的阐释。比如黄酮类化合物可以在抗氧化、抑制炎症反应、细胞凋亡和自噬等病理生理机制中发挥有效作用。本文通过查阅国内外的相关文献,对黄酮类化合物抗心脑血管缺血性疾病的保护作用及其机制进行综述。旨在为抗心脑血管疾病药物的研究开发提供参考。     

黄酮类化合物抗肿瘤作用及其相关机制研究进展

黄酮类化合物种类繁多并广泛分布于自然界中,具有丰富的药理学活性。近年来,关于黄酮类化合物抗肿瘤作用的药理学研究日趋深入。大量研究结果表明,多种黄酮类化合物具有良好的体内外抗肿瘤活性,具有广阔的开发前景。该文综述了近年来国内外关于黄酮类化合物抗肿瘤作用及其相关机制的研究进展。     

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。     

黄酮类化合物抗肺动脉高压的研究进展

黄酮类化合物是一类多酚类化合物,根据其化学结构可分为黄酮醇、黄酮、黄烷酮、异黄酮、儿茶素、花青素和查耳酮。研究表明,黄酮类化合物具有抗氧化、抗炎、心血管保护、抗肿瘤、抗病毒、抗过敏等多种药理作用。该文查阅了近年来国内外研究文献,对黄酮类化合物抗肺动脉高压的作用及其机制进行综述,旨在为肺动脉高压的治疗提供新的候选药物及治疗途径。     

黄酮类化合物对三阴性乳腺癌肿瘤微环境的改善

目的 研究黄酮类化合物对三阴性乳腺癌(TNBC)肿瘤微环境(TME)的改善作用。方法 查阅国内外相关文献并归纳总结,综述黄酮类化合物通过影响TME对TNBC产生的作用。结果 黄酮类化合物通过不同机制,使TNBC细胞与TME相互作用,阻滞细胞周期、抑制癌细胞侵袭、转移、新血管生成和诱导细胞凋亡。结论 黄酮类化合物在TME中具有不同的抗TNBC活性,将TME作为治疗靶点的进一步研究具有重要意义。     

中药黄酮类化合物药理作用及作用机制研究进展

目的对黄酮类化合物的药理作用及其作用机制进行综述和分析。方法对近年来有关黄酮类化合物的药理作用及其作用机制的文献进行总结与分析。结果黄酮类化合物具有抗氧化、抗炎、镇痛、调节免疫、抗衰老、降血脂、抗肿瘤等药理作用,其作用机制可能与其抗自由基或抗氧化有关。结论黄酮类化合物是许多中草药的有效成分,具有广泛的生物活性,其产生生物活性的作用机制有待于进一步深入的研究。     

基于网络药理学与分子对接研究垂盆草治疗急性肝损伤的分子机制

目的 研究垂盆草中的黄酮类与氰苷类物质治疗急性肝损伤的分子机制。方法 通过数据库筛选出药物与疾病的共同靶点,用网络药理学构建相互作用网络,通过拓扑分析筛选核心靶点,构建PPI网络,通过GO与KEGG富集分析寻找与垂盆草中的黄酮类和氰苷类物质治疗急性肝损伤的相关信号通路,最后经由分子对接与MM-GBSA计算成分与核心靶点的结合自由能。结果 得到了72个潜在作用的急性肝损伤靶点和涉及120条信号通路(以KEGG为例),发现垂盆草潜在作用的关键基因靶点为MMP9、PARP1、MCL1。结论 初步验证了垂盆草主要活性成分中的黄酮类和氰苷类能与潜在作用靶标发生相互作用,揭示了垂盆草治疗急性肝损伤具有“多靶点-多通路”的作用机制,为后续深入验证其分子机制奠定了基础。     

天然黄酮类化合物防治糖尿病肾病的研究进展

糖尿病肾病（DN）是一种严重的糖尿病并发症,其发病机制复杂而多样。现代药理研究表明,天然黄酮类化合物具有多种潜在药用价值,对糖尿病肾病的防治作用就是其中之一。黄酮类化合物抗糖尿病肾病的作用机制是多方面药理活性的综合结果,包括通过抗氧化应激与清除自由基、抗炎、改善血糖血脂紊乱、抗凋亡、调节血管舒张及改善血流动力学异常等途径来实现。在查阅近年来国内外发表的相关文献后,对黄酮类化合物在糖尿病肾病防治中的多种作用及相关机制进行综述,以期为糖尿病肾病防治药物的研发提供参考。     

鱼腥草中黄酮类化合物的研究进展

鱼腥草为药食同源中药材,其自然资源丰富,含有许多的活性成分,其中黄酮类化合物含量多达三十多种。国内外有关鱼腥草黄酮类化合物的提取、纯化及生理活性和作用机制的总结报道文献较少,因此对提取、纯化及生理活性和其作用机制进行了总结,希望为今后的研究和应用提供参考。     

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...     

荔枝核活性成分提取及药理作用的研究进展

本文综述了近3年荔枝核提取工艺及其药理作用研究进展,提出虽然大量实验结果证实荔枝核主要的活性成分是荔枝核总皂苷和黄酮类化合物,且治疗肝病、糖尿病、乳腺增生、肿瘤等药理作用显著,但目前对荔枝核已知的主要药效物质研究仍停留在其粗提物上,有效部位的筛选与提纯缺乏系统及规范化,指出应尽快开展相关的如提取工艺优化及质量标准的制订等工作。     

Intestinal and hepatic glucuronidation of flavonoids

Flavonoids are polyphenolic phytochemicals present extensively in our daily diets, beverages, medicinal plants, and herbal remedies. The diverse biological effects of flavonoids have aroused great interest in scientists. In the past decade, various studies demonstrated extensive conjugate metabolisms, especially glucuronidation, of flavonoids in intestine and liver implying an important role of the glucuronidation in causing low oral bioavailability of flavonoids. The present article aims to review the up-to-date information on the studies of the first-pass metabolism, in particular glucuronidation, of flavonoids in the gastrointestinal tract and the liver, and also the isoformic enzymes involved in the metabolism and disposition of flavonoids. In addition, the role of efflux transporters, enterohepatic circulation, and enteric cycling in the disposition of flavonoid glucuronides has also been illustrated. Despite low oral bioavailabilities of the parent compounds, flavonoids and some of their bioactive phase II conjugates may accumulate adequate amount in the body to produce their pharmacological activities. Further investigation on the correlation between the accumulated concentrations of flavonoids and their pharmacological activities after their repeated oral administration is warranted.     

UV spectrometric and DC polarographic studies on apigenin and luteolin

Remarks on polyphenolic compounds has been arisen since past few years. The flavonoids appears to be the important groups of compounds with their capability to inhibit DNA damage, lipid peroxidation, to quench free radicals and, at least, anticarcinogenic and antiproliferative effects. On the other hand, their mechanism of action is still unexplained. Apigenin and luteolin are the most wide-spread flavones and they exhibited to be useful in chemoprevention. UV spectrometric and DC polarographic studies on these two compounds have been carried out with regard to changing pH. The most significant changes were observed at basic pH. These results could aid to elucidation of their mechanism of action as pH is one of the important factors for bioprocesses passing in living organisms.     

水飞蓟素在慢性疾病中的抗氧化作用研究概述

水飞蓟素(silymarin)作为护肝药物被广泛应用于各类肝病,其护肝作用与水飞蓟素强大的抗氧化、抗炎和抗脂质沉积等作用有关。越来越多研究表明水飞蓟素在氧化应激引发的如心血管疾病、代谢综合征、神经退行性疾病、癌症和并发症等慢性疾病都具有良好治疗效果。本篇列举了近五年水飞蓟素治疗慢性病的通路研究,重点阐述慢性疾病与氧化应激的损伤机制和水飞蓟素的抗氧化能力在其中发挥的关键作用,以期为水飞蓟素的临床使用提供用药思路。     

Hypouricemic action of selected flavonoids in mice: structure-activity relationships

Hyperuricemia and gout appear to be rapidly increasing worldwide and frequently cause symptoms of metabolic syndrome. Dietary flavonoids have their potential beneficial effects on human health. In the present study, 15 flavonoids (quercetin, morin, myricetin, kaempferol, icariin, apigenin, luteolin, baicalin, silibinin, naringenin, formonoetin, genistein, puerarin, daidzin and naringin dihydrochalcone) were selected to investigate for their hypouricemic action in mice. Oral administration of quercetin, morin, myricetin, kaempferol, apigenin and puerarin at 50 and 100 mg/kg for 3 d was able to elicit hypouricemic actions in hyperuricemic mice induced by potassium oxonate. Luteolin, formonoetin and naringenin showed the significant effects only at 100 mg/kg. Quercetin, puerarin, myricetin, morin and kaempferol significantly reduced liver uric acid level in hyperuricemic animals. In addition, quercetin, morin, myricetin, kaempferol and puerarin exhibited significant inhibition on the liver xanthine oxidase (XOD) activities. It seems to be likely that these flavonoids reduce serum urate levels by mainly inhibiting XOD activity. However, the hypouricemic effect of apigenin observed seemed not to parallel with the changes in liver uric acid level and liver XOD activity, implying that apigenin might act via other mechanisms apart from inhibiting enzyme activity simply. Analysis of the chemical structure showed that a planar structure with the hydroxyl groups played a crucial role in hypouricemic activity of flavonoids. The exact mechanism of the hypouricemic action of flavonoids in vivo should be investigated in the future.     

赶黄草总黄酮缓解体力疲劳的作用研究

目的： 研究赶黄草总黄酮缓解小鼠体力疲劳的作用及机制。方法： 将小鼠随机分为空白对照组、阳性对照谷胱甘肽（GSH）组和赶黄草总黄酮三个剂量组（100,200,400 mg·kg^-1）,连续灌胃14 d,进行小鼠负重游泳试验,检测小鼠血清尿素氮、肝糖原、游泳前后全血乳酸及肝SOD,MDA和MAO含量,采用Western blot检测骨骼肌组织PGC-1α蛋白的表达。结果： 赶黄草总黄酮明显延长小鼠力竭游泳时间,降低血清尿素氮和运动后血乳酸浓度,升高肝糖原含量;赶黄草总黄酮升高疲劳小鼠肝组织中SOD水平,降低MDA,MAO含量;赶黄草总黄酮明显促进骨骼肌组织中PGC-1α的蛋白表达,与空白对照组比较,差异有显著性（P<0.05）。结论： 赶黄草总黄酮具有明显的缓解体力疲劳作用,其机制可能与促进PGC-1α蛋白表达和抗氧化作用有关。     

Effects of flavonoids on immune and inflammatory cell functions.

No doubt can remain that the flavonoids have profound effects on the function of immune and inflammatory cells as determined by a large number and variety of in vitro and some in vivo observations. That these ubiquitous dietary chemicals may have significant in vivo effects on homeostasis within the immune system and on the behavior of secondary cell systems comprising the inflammatory response seems highly likely but more work is required to strengthen this hypothesis. Ample evidence indicates that selected flavonoids, depending on structure, can affect (usually inhibit) secretory processes, mitogenesis, and cell-cell interactions including possible effects on adhesion molecule expression and function. The possible action of flavonoids on the function of cytoskeletal elements is suggested by their effects on secretory processes. Moreover, evidence indicates that certain flavonoids may affect gene expression and the elaboration and effects of cytokines and cytokine receptors. How all of these effects are mediated is not yet clear but one important mechanism may be the capacity of flavonoids to stimulate or inhibit protein phosphorylation and thereby regulate cell function. Perhaps the counterbalancing effect of cellular protein tyrosine phosphatases will also be found to be affected by flavonoids. Some flavonoid effects can certainly be attributed to their recognized antioxidant and radical scavenging properties. A potential mechanism of action that requires scrutiny, particularly in relation to enzyme inhibition, is the redox activity of appropriately configured flavonoids. Finally, in a number of cell systems it seems that resting cells are not affected significantly by flavonoids but once a cell becomes activated by a physiological stimulus a flavonoid-sensitive substance is generated and interaction of flavonoids with that substance dramatically alters the outcome of the activation process.     

甘草提取物及有效成分抗代谢相关脂肪性肝病的药理作用及机制研究进展

甘草是最常用的药用植物,广泛应用于食品及制药行业。甘草的化学成分主要有三萜皂苷类、黄酮类和多糖类等,具有抗氧化、免疫调节、抗病毒及抗炎保肝等多种药理作用。现代研究发现甘草提取物及有效成分（甘草酸、甘草次酸、甘草查尔酮A、甘草总黄酮等）能通过调节糖脂代谢、减轻氧化应激、改变肠道菌群、保护肠道屏障等机制达到改善及治疗代谢相关脂肪性肝病（MAFLD）的目的。综述近年来甘草提取物及有效成分抗MAFLD的药理作用及机制研究进展,旨在为该类药物的临床合理应用及新药研发提供理论依据。     

Inhibitory effect of flavonoids on sulfo- and glucurono-conjugation of acetaminophen in rat cultured hepatocytes and liver subcellular preparations

A large group of flavonoids was investigated for inhibitory effects on sulfo- and glucurono-conjugation of acetaminophen when added to rat cultured hepatocytes and liver subcellular preparations. The flavonoids inhibited the production of both sulfate and glucuronide conjugates in the cultured cells, with potencies that depended on the specific flavonoid. Among the flavonols, quercetin, kaempferol and galangin were much more effective than myricetin and morin. Flavones including luteolin, apigenin and chrysin were as effective as the corresponding three flavonols above. The inhibition of conjugation by other simple flavones such as 3-, 5-, 7- and 3',4'-OH flavones, and by catechins such as epicatechin and epigallocatechin, was very weak. These data suggest that the presence of both C5 and 7 hydroxyl substitutions on the A-ring in the flavone structure is required for effective inhibitory activity. The effect of flavonoids on sulfo- and glucurono-conjugation was also examined by incubating acetaminophen with isolated liver cytosolic and microsomal preparations, respectively. The active flavonoids in the cells remarkably inhibited the sulfation, but not glucuronidation, in cell-free enzymatic preparations in vitro. The mechanism of inhibition of conjugation by flavonoids in cultured hepatocytes is not likely to depend on the direct inhibition of sulfo- and glucurono-transferase activity by flavonoids.