柚皮苷的人肠内菌生物转化(英文)

柚皮苷(1)是酸橙中含量最高的二氢黄酮苷类化合物, 将其与人肠内菌丛共温孵, 从温孵物中通过色谱方法得到原形化合物1和四个转化产物 (2-5), 根据谱学数据确定它们分别为柚皮苷-6"-乙酰物(2)、柚皮素(3)、根皮酸(4)和间苯三酚(5)。在1的糖苷链葡萄糖基6位能够特异性地发生乙酰化作用。1口服难以吸收。本文结果为阐明其生物利用度低提供了实验依据, 推测表现其生物活性的物质基础主要是其肠内菌生物转化产物3。肠内菌丛所致1的生物转化的继发结果,是它的转化产物吸收进入体循环发挥生物学作用, 此结果为进一步或再评价其体内过程、作用或毒性及其生物利用度提供了有用的信息。     

RP-HPLC法测定橘红痰咳液中柚皮苷含量

目的：建立反相高效液相色谱法测定主药化橘红中柚皮苷的含量。方法 ：采用ALLTIMA-C185MICRON柱,以甲醇-1%冰醋酸（40：60）为流动相,280nm为检测波长。结果：测得线性范围2.0-10.0ug/ml(r=0.9997),平均回收率为99.06%,RSD=1.16%。结论：方法准确、可靠,可作为质量控制的方法。     

负载柚皮苷AKE/GB30网箱在脊柱骨缺损模型修复中的作用及对BMPs-VEGF信号通路的影响

【摘要】 目的：观察负载柚皮苷的AKE/GB30网箱在脊柱骨缺损模型中的修复作用,并基于骨形成蛋白（BMPS）-血管内皮生长因子（VEGF）信号通路探讨该生物材料的作用机制。方法：用牙钻在30只新西兰雄兔L5与L6椎间制作一个7mm×5mm×4mm的缺损,建立脊柱骨缺损模型,制备AKE/GB30网箱。测试负载柚皮苷的AKE/GB30网箱生物力学性能,检测其体外释药行为。将造模成功的新西兰兔随机数字表法分为3组,即空白组、自体骨移植组、骨移植生物材料+柚皮苷联合组,除空白组外分别予以自体骨移植、负载柚皮苷的AKE/GB30网箱进行修复。术后6周、12周每组各取5只兔,微计算机断层扫描（Micro CT）检测骨修复情况[包括骨体积分数（BV/TV）、骨小梁厚度（Tb.Th）和骨小梁数目（Tb.N）];实时荧光定量聚合酶链反应（RT-PCR）检测骨形成蛋白2（BMP2）、VEGF、Runt相关转录因子2（RUNX2）、碱性磷酸酶（ALP）、骨钙素（OCN）信使核糖核酸（mRNA）表达;免疫印迹法（WB）检测骨组织BMP2、VEGF、RUNX2、ALP、OCN蛋白表达。结果：AKE/GB30网箱制作成功,且其特性检测结果符合脊柱骨缺损修复要求;负载柚皮苷的AKE/GB30网箱最大抗压强度为28MPa,最大抗压力为15N,6周时其累积释药率达（98.15±1.47）%;各组术后12周时BV/TV、Tb.Th和Tb.N,骨组织BMP2、VEGF、RUNX2、ALP、OCN的mRNA与蛋白表达均高于术后6周时（P＜0.05）,且自体骨移植组、骨移植生物材料+柚皮苷联合组上述指标均高于空白组（P＜0.05）,自体骨移植组、骨移植生物材料+柚皮苷联合组上述指标差异均无统计学意义（P＞0.05）。结论：负载柚皮苷的AKE/GB30网箱在脊柱骨缺损模型修复的效果等同于自体骨移植,可能是通过促进BMP2、VEGF、RUNX2、ALP、OCN表达实现的。     

Thermo-responsive injectable naringin-loaded hydrogel polymerised sodium alginate/bioglass delivery for articular cartilage

In the human body, joint cartilage is of great importance. It has long been a big therapeutic problem to fix joint cartilage lesions as it appears due to different conditions. Recent stories have shown that the cartilage replacement process must delay the extracellular (ECM) cartilage deterioration and modulate the host''s inflammation response. For the reconstruction of the articular cartilage, drug-loaded injectable hydrogels were developed. This hydrogel could retain the chondrocyte phenotype, but the host''s inflammatory reaction could also be controlled. The bioglass (BG)/sodium alginate (SA) injectable hydrogels was combined with agarose (AG)/Naringin hydrogel in injectable thermal response for articular cartilage regeneration with a non-chargeable hydrogel that contains both Naringin and BG (Naringin–BG hydrogels). The Naringin–BG hydrogel has an adequate swelling ratio that encourages the fusion of tissue formed with host tissue and enables the gradual release of Naringin bioavailabilities enhanced in situ. The Naringin–BG hydrogel can upgrade the typical chondrocyte phenotype by upregulating aggrecan, SRY-box 9, and collagen type II alpha one chain. It may also stimulate the polarization of M2 macrophage, lower inflammations, and prevent ECM degradations through the decrease of the expressions of the indictable metalloproteinase-13 matrix, nitric oxide synthase, and metalloproteinase-1 matrix. The formed tissues were identical to normal tissues and firmly incorporated with the surrounding tissue after administering the Naringin–BG hydrogels into the rat model articular cartilage defects. Then the injectable Naringin–BG hydrogel increases the bioavailable content of Naringin and retains the chondrocyte phenotype.     

柚皮苷抗红细胞膜脂质过氧化作用研究

目的 研究柚皮苷在体外对氧自由基引发的红细胞膜脂质过氧化的影响.方法 采用黄嘌呤-黄嘌呤氧化酶(Xan-Xo)系统、紫外线(UV)照射及H2O2在体外诱导红细胞膜脂质过氧化,脂质过氧化物用硫代巴比妥酸比色法测定.结果 柚皮苷能抑制上述3种方法引起的红细胞膜硫代巴比妥酸反应物(TBARS)生成的增加,并呈剂量依赖性.结论 柚皮苷对氧自由基引起的细胞膜脂质过氧化损伤有保护作用.     

黄酮类化合物柚皮苷抑制HaCaT细胞RANTES产生的研究

目的：分析肿瘤坏死因子口（TNF-α）和γ干扰素（IFN-γ）是否诱导体外培养角质形成细胞株HaCaT产生趋化因子RANTES，了解柚皮苷是否影响TNF-α和IFN-γ／对合成RANTES的诱导作用。方法：TNF-α和IFN-γ刺激培养的HaCaT细胞，应用定量RT-PCR方法测定RANTES的mRNA表达，应用ELISA方法测定上清液中RANTES。结果：正常培养HaCaT细胞RANTES微弱表达，TNF-α和TFN-γ刺激使HaCaT细胞RANTES的mRNA表达与分泌量显著增加。柚皮苷0．5，0．25mmol·L^-1能抑制TNF-α和TFN-γ诱导的RANTES分泌。结论：柚皮苷可抑制TNF-α和TFN-γ引起的HaCaT细胞分泌RANTES。     

柚皮苷促进牙周韧带干细胞增殖和分化的研究

目的探讨不同浓度柚皮苷对牙周韧带干细胞增殖和分化的影响。方法分别在含有0.14 mg/mL(低浓度组)和1.4 mg/mL(高浓度组)柚皮苷的细胞培养基上对牙周韧带干细胞进行培养,并与不含柚皮苷的细胞培养基(空白对照组)培养情况进行对比。在培养1 d、4 d、7 d后对牙周韧带干细胞的增殖情况进行测定,在培养7 d、14 d后对牙周韧带干细胞的碱性磷酸酶活性及成骨相关基因[成骨特异性转录因子(Runx2)、骨钙素(OCN)、碱性磷酸酶(ALP)、Ⅰ型胶原(ColⅠ)]的表达进行测定。结果高浓度(1.4 mg/mL)的柚皮苷对牙周韧带干细胞的增殖具有促进作用(P0.05),对牙周韧带干细胞的成骨向分化也具有一定的促进作用,能够显著提高成骨相关基因(ColⅠ、ALP、OCN、Runx2)的表达。结论柚皮苷在一定的浓度和时间下,能促进牙周韧带干细胞的增殖与成骨向分化。     

柚皮苷转化生成红花素及异红花素的研究

摘要：目的 利用一株日本曲霉，以柚皮苷为底物，转化生成红花素和异红花素并提高产物的发酵单位。方法 对 发酵培养基中氮源种类进行筛选并确定最适的添加浓度，考察微量元素对发酵的影响并确定最适添加浓度，降低溶解底 物的乙醇浓度并采用二次添加底物的方式等。结果 红花素发酵单位由66 μg/mL提高至389 μg/mL，异红花素发酵单位由 263 μg/mL提高至946 μg/mL。热豆粉是最佳氮源，添加浓度为0.3%；添加硫酸亚铁和氯化锰能够分别促进红花素和异红花素的 生成，其最适添加浓度分别为0.02%和0.01%；溶解底物的乙醇浓度由50%降低至26.6%，降低了乙醇对转化的不利影响；底物 添加次数由1次变为2次，有利于发酵单位的提高。结论 首次发现日本曲霉可直接转化柚皮苷生成红花素和异红花素，且柚皮 苷生物转化为红花素和异红花素的发酵单位较高。     

骨碎补提取工艺的实验研究

目的：优选骨碎补提取的最佳工艺条件。方法：以骨碎补中柚皮苷及骨碎补总黄酮的含量为指标,采用L^9（3^4）正交设计法对骨碎补的提取条件进行研究。结果：提取次数是骨碎补有效成分提取的关键因素,其次是溶媒用量,提取时间和乙醇浓度为最次要因素。结论：最佳提取工艺条件是14倍量55%乙醇回流提取3次,2h/次。     

Preventive effect of naringin on isoproterenol-induced cardiotoxicity in Wistar rats: an in vivo and in vitro study

This study was aimed to evaluate the preventive role of naringin on heart weight, blood glucose, total proteins, albumin/globulin (A/G) ratio, serum uric acid, serum iron, plasma iron binding capacity and membrane bound enzymes such as sodium potassium-dependent adenosine triphosphatase (Na(+)/K(+) ATPase), calcium-dependent adenosine triphosphatase (Ca(2+) ATPase) and magnesium-dependent adenosine triphosphatase (Mg(2+) ATPase) and glycoproteins such as hexose, hexosamine, fucose and sialic acid in isoproterenol (ISO)-induced myocardial infarction (MI) in rats and in vitro free radical scavenging assay. Male albino Wistar rats were pretreated with naringin (10, 20 and 40 mg/kg, respectively) for a period of 56 days. After the treatment period, ISO (85 mg/kg) was subcutaneously injected to rats at an interval of 24 h for 2 days. ISO-induced rats showed a significant (P<0.05) increase in the heart weight, blood glucose, serum uric acid, serum iron and a significant (P<0.05) decrease in the levels of total proteins, A/G ratio and iron binding capacity. A significant (P<0.05) decrease in the activity of Na(+)/K(+) ATPase and increase in the activities of Ca(2+) and Mg(2+) ATPase in the heart and a significant (P<0.05) increase in the levels of glycoproteins in serum and the heart were also observed in ISO-induced rats. Pretreatment with naringin for a period of 56 days exhibited a significant (P<0.05) effect and altered these biochemical parameters positively in ISO-induced rats. Naringin also scavenges 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis-(3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) and nitric oxide (NO) radicals in vitro. Thus, our study shows that naringin has cardioprotective role in ISO-induced MI in rats.