Naringin does not alter caffeine pharmacokinetics, energy expenditure, or cardiovascular haemodynamics in humans following caffeine consumption

1. Naringin, a grapefruit constituent interacts with many medications including caffeine, a popular weight loss supplement. The purpose of the current study was to identify changes in caffeine pharmacokinetics, resting energy expenditure (REE), oxygen consumption (VO(2)) and respiratory exchange ratio (RER) after an acute dosage of caffeine and naringin. 2. Using a double-blinded, counterbalanced design, REE, VO(2), and RER were measured before and systematically for 8 h after a single dosage of caffeine (CAF, 200 mg) with and without naringin (100 mg (CN100) or 200 mg (CN200)) in 10 apparently healthy individuals. A standardized meal was provided following 240-minute measurements (400 kcals; 35 g carbohydrate; 27 g protein; 7 g fat). 3. Caffeine, CN100, CN200 did not alter VO(2) or VO(2) area under the curve (137 301 +/- 8318, 139 729 +/- 9300, 134 297 +/- 8318, mL/480 min). Resting energy expenditure (k/cals) was 10.0 +/- 1.4% higher with CAF versus CN200 (6.0 +/- 1.4%) and CN100 (6 +/- 1.5%) at 240 min (P = 0.07) which was then negated following a standardized meal. Percent change in RER from pre to 240 min and pre to 480 min was not different between the CAF, CN100, or CN200 (-0.2 +/- 1.7%, 1.7 +/- 1.7%, -2.8 +/- 1.9%). 4. Although caffeine alone suggests a trend of increased REE, the results of the present study indicate that concurrent consumption of caffeine with naringin in acute dosages does not affect RER, VO(2), and prevents the increase of REE in adult humans. The results suggest that the interaction of grapefruit juice and caffeine may be due to constituents of grapefruit juice other than naringin or in addition to naringin.     

HPLC法测定通舒口爽胶囊中3种成分的含量

目的建立测定通舒口爽胶囊中柚皮苷,橙皮苷和新橙皮苷含量的HPLC方法。方法采用Diamonsil C18(200 mm×4.6 mm,5μm)色谱柱,流动相:甲醇-乙腈-体积分数为0.05%的磷酸水溶液(体积比为20∶10∶65),流速:1.0 mL.min-1,柱温:30℃,检测波长:280 nm。结果柚皮苷在8.88~88.8 mg.L-1内呈线性关系(r=0.999 7),平均回收率为100.5%;橙皮苷在7.60~76.0 mg.L-1内呈线性关系(r=0.999 6),平均回收率为100.5%;新橙皮苷在10.56~105.6 mg.L-1内呈线性关系(r=0.999 9),平均回收率为100.5%。结论本实验建立的方法可作为通舒口爽胶囊质量控制方法之一。     

RP-HPLC法测定复方百部止咳颗粒中5种黄酮类成分

目的 建立HPLC同时测定复方百部止咳颗粒中柚皮苷、橙皮苷、新橙皮苷、黄芩苷和黄芩素的方法。方法 Diamonsil C₁₈柱（200 mm×4.6 mm,5 mm）,流动相A为1%冰醋酸溶液,B为乙腈,线性梯度洗脱,检测波长283 nm,柱温30 ℃,体积流量1.0 mL/min,进样量10 μL。结果 柚皮苷、橙皮苷、新橙皮苷、黄芩苷和黄芩素分别在3.52～35.2 mg/mL（r＝0.999 8）,5.92～59.2 mg/mL（r＝0.999 9）,2.64～26.4 mg/mL（r＝0.999 7）,5.76～57.6 mg/mL（r＝0.999 7）,0.60～6.0 mg/mL（r＝0.999 8）线性关系良好;平均加样回收率依次为98.9%、99.8%、99.7%、99.8%、99.2%,RSD分别为0.6%、0.9%、1.0%、1.3%、1.3%。结论 该方法快速、简便,重现性好,适合于同时测定复方百部止咳颗粒中柚皮苷、橙皮苷、新橙皮苷、黄芩苷和黄芩素。     

HPLC同时测定参柏颗粒中甘草苷、柚皮苷、盐酸小檗碱

目的 建立参柏颗粒中甘草苷、柚皮苷和盐酸小檗碱的HPLC测定方法。方法 色谱柱为Diamonsil C₁₈柱（250 mm×4.6 mm,5 μm）,流动相为乙腈-0.1%磷酸溶液,梯度洗脱,体积流量1.0 mL/min,检测波长276 nm,柱温30 ℃。结果 甘草苷、柚皮苷、盐酸小檗碱的线性范围分别为0.164～0.820、0.480～2.400、0.048～0.240 μg,平均回收率分别为98.6%、98.4%、98.0%。结论 该方法简便快速、准确灵敏,为评价和控制参柏颗粒的质量提供了可靠的方法。     

Naringin suppresses the development of glioblastoma by inhibiting FAK activity

As the most common and lethal primary malignant brain cancer, glioblastoma is hard to timely diagnose and sensitive therapeutic monitoring. It is essential to develop new and effective drugs for glioblastoma multiform. Naringin belongs to citrus flavonoids and was found to display strong anti-inflammatory, antioxidant and antitumor activities. In this report, we found that naringin can specifically inhibit the kinase activity of FAK and suppress the FAK^p-Try397and its downstream pathway in glioblastoma cells. Our study showed out that naringin can inhibit cell proliferation by inhibiting FAK/cyclin D1 pathway, promote cell apoptosis through influencing FAK/bads pathway, at the same time, it can also inhibit cell invasion and metastasis by inhibiting the FAK/mmps pathway. All these showed that naringin exerts the anti-tumor effects in U87?MG by inhibiting the kinase activity of FAK.     

宣痹凝胶帖膏剂有效成分的透皮行为研究

目的:研究宣痹凝胶贴膏剂中有效成分龙胆苦苷、柚皮苷、原苏木素B的透皮吸收特性。方法:采用Franz扩散池法,以大鼠腹皮为体外模型,用HPLC测定接受液、皮中、膏中残留的龙胆苦苷、柚皮苷、原苏木素B 3种指标成分的含量。结果:宣痹凝胶贴膏剂中龙胆苦苷、柚皮苷、原苏木素B的透皮速率分别为3.47,1.59,2.13μg.cm-2.h-1;24 h的累积透过率分别为25.42%,11.73%,17.78%;在皮中的滞留量分别为0.231,0.593,0.568μg.cm-2,滞留率分别为0.027%,0.227%,0.475%;在膏中的残留量分别为2 179,674,278μg,残留率分别为81.36%,81.92%,73.83%。结论:宣痹凝胶贴膏剂中有效成分的体外透皮行为接近零级过程,皮中滞留率相比透过率和膏中残留率来说非常低。     

柚皮苷抑制高糖诱导的脐静脉内皮细胞与单核细胞的粘附作用

目的研究柚皮苷对高糖诱导的脐静脉内皮细胞(HUVECs)与单核细胞的粘附的抑制作用及机制。方法分离培养HUVECs后,采用不同剂量的柚皮苷预处理HUVECs,然后高糖诱导HUVECs;加入荧光染料标记单核细胞系THP-1细胞与HUVECs共同孵育,荧光显微镜下观察HUVECs与单核细胞的粘附作用并拍照,比较粘附密度;提取总蛋白后,Western blotting检测处理后HUVECs粘附分子的表达;荧光染料结合法检测处理后HUVECs活性氧的产生;提取处理的脐静脉内皮细胞核蛋白后,Western blotting检测核因子-κB在核内的量。结果高糖诱导HUVECs与单核细胞的粘附,柚皮苷可显著抑制高糖诱导的HUVECs与单核细胞的粘附。柚皮苷抑制高糖诱导的HUVECs细胞间粘附分子和血管内皮细胞粘附分子的表达,柚皮苷抑制高糖诱导的HUVECs活性氧产生,柚皮苷抑制高糖诱导的HUVECs核因子-κBp65活化。结论柚皮苷可能通过抑制高糖诱导的HUVECs活性氧产生,从而抑制核因子-κB的活化,进一步抑制细胞间粘附分子和血管内皮细胞粘附分子的表达,影响HUVECs与THP-1细胞的粘附,从而抑制高糖诱导的血管炎症...     

蜂蜜炼制前后黄酮类成分种类和含量变化分析

目的研究中药辅料蜂蜜炼制前后黄酮类成分变化。方法参考《中药药剂学》,对不同来源的6种蜂蜜进行炼制。供试品经固相萃取法富集黄酮类成分。采用高效液相色谱-三重四级杆串联质谱(HPLC-TQ-MS)法测定,Thermo Accucore RP-MS色谱柱(100 mm×2.1 mm,2.6μm),以0.1%甲酸水溶液-甲醇为流动相进行梯度洗脱,体积流量0.3 m L/min,柱温30℃。质谱条件:采用电喷雾离子源(ESI),正离子检测模式,多反应监测模式(MRM)扫描分析。结果蜂蜜中共检测到12种黄酮类成分,包括黄酮苷元、二氢黄酮苷元和异黄酮苷元。黄酮苷元有8种:槲皮素、桑黄素、木犀草素、山柰酚、芹菜素、汉黄芩素、高良姜素和白杨素;二氢黄酮苷元有3种:短叶松素、柚皮素和乔松素;异黄酮苷元染料木素。不同蜜源蜂蜜所含黄酮类成分种类和含量存在明显差异。6个蜂蜜样品炼制后,都发现了蜂蜜中没有报道过的芦丁和芸香柚皮苷,12种检测到的蜂蜜黄酮类成分在炼制后其量都有不同程度的变化,椴树蜜的槲皮素、桑黄素、木犀草素、山柰酚、芹菜素、汉黄芩素、乔松素和白杨素量均有增加,短叶松素、柚皮素和高良姜素量没增加反而还有下降的;洋槐蜜中除芹菜素量增加不明显外,其余均有所增加,尤其是槲皮素和桑黄素增加的较为明显;百花蜜和枣花蜜12种黄酮类成分量均显著增加。结论炼制可造成蜂蜜中黄酮类成分的种类和含量发生改变。     

HPLC法测定通林片中柚皮苷的含量

目的建立通林片的中柚皮苷的含量测定方法。方法在L ichrospher5-C184.6 mm×25 cm柱上,甲醇-0.4%磷酸溶液(40∶60)为流动相,检测波长为波长为283 nm,流速为1.0 m l.m in-1。结果柚皮苷的量在0.3~1.5μg范围内呈良好的线性关系(r=0.999 5),回归方程为A=2295380C-66402。精密度试验RSD为0.71%,该方法平均回收率为98.43%,RSD=1.63%。结论该方法简单、快速、准确。     

舒通胶囊柚皮苷含量测定及制备工艺改进

目的建立舒通胶囊中柚皮苷含量测定方法,改进中药提取、纯化工艺。方法采用HPLC法测定柚皮苷含 量,以脱水浸膏得率和枳壳活性成分柚皮苷含量为判断指标,考察提取时间和纯化方法对指标成分的影响。结果柚皮苷在 50 -1500 ng范围内线性良好,平均加样回收率为99. 90 %,RSD为1. 71% ;中药提取以药材-水（1： 10）连续提取2次,每次 0.5 h制备,经纯化柚皮苷含量与固体比值最大,处方得率较为满意。结论以中药浸誉固体得率和有效成分含量测定方法综 合评价,改进舒通胶囊的制备工艺,试验设计科学合理’含量测定操作简便、结果准确,适用于本品工艺考察及质量控制。