基于DFT和UV-Vis的金丝桃苷印迹相互作用分析

为提高金丝桃苷(HYP)印迹效率,通过密度泛函理论(DFT)和紫外-可见光吸收光谱(UV-Vis)实验法对HYP、丙烯酰胺(AM)、衣康酸(IA)及其不同摩尔比例的HYP-AM和HYP-IA复合物进行理论计算和紫外光谱的测定,使用分子静电势(MEP)预测HYP、AM和IA的印迹活性位点,探讨HYP和AM(IA)分子间相互作用的印迹机理。结果表明:HYP中O11可与AM中H9(或H10)以及IA中H2(或H15)形成强氢键作用,而O12—H13、O15—H16、O25—H26、O27—H28、O41—H42、O44—H45、O47—H48、O52—H53可与AM中O7以及IA中O4(或O13)形成强氢键作用。HYP-AM和HYP-IA复合物系统的高摩尔比可以增加复合物的总相互作用能量。通过筛选不同功能单体可以增强活性位点之间的相互作用强度。HYP与AM(IA)之间发生的强氢键作用导致Ⅰ、Ⅱ、Ⅳ吸收峰发生红移,同时验证了DFT理论计算的准确性。HYP-AM和HYP-IA复合物的最优印迹比分别为n(HYP)∶n(AM)=1∶8和n(HYP)∶n(IA)=1∶7,且HYP-IA比HYP-AM的相互作用力更强,IA是更好的功能单体。     

高效液相色谱法测定山楂叶中金丝桃苷的含量

采用反相高效液相色谱法,使用Diamonsil C18柱(150 mm×4.6 mm,5 μm),以甲醇-水-冰醋酸(48∶52∶1)为流动相,检测波长为340 nm,对不同采收期的山楂叶金丝桃苷的含量进行了测定.结果表明,山楂叶中金丝桃苷的含量自6月份起呈上升趋势,到10月下旬含量最高.宜选用10月下旬采摘的山楂叶作为提取药材.     

Hyperoside Downregulates the Receptor for Advanced Glycation End Products (RAGE) and Promotes Proliferation in ECV304 Cells via the c-Jun N-Terminal Kinases (JNK) Pathway Following Stimulation by Advanced Glycation End-Products In Vitro

Hyperoside is a major active constituent in many medicinal plants which are traditionally used in Chinese medicines for their neuroprotective, anti-inflammatory and antioxidative effects. The molecular mechanisms underlying these effects are unknown. In this study, quiescent ECV304 cells were treated in vitro with advanced glycation end products (AGEs) in the presence or absence of hyperoside. The results demonstrated that AGEs induced c-Jun N-terminal kinases (JNK) activation and apoptosis in ECV304 cells. Hyperoside inhibited these effects and promoted ECV304 cell proliferation. Furthermore, hyperoside significantly inhibited RAGE expression in AGE-stimulated ECV304 cells, whereas knockdown of RAGE inhibited AGE-induced JNK activation. These results suggested that AGEs may promote JNK activation, leading to viability inhibition of ECV304 cells via the RAGE signaling pathway. These effects could be inhibited by hyperoside. Our findings suggest a novel role for hyperoside in the treatment and prevention of diabetes.     

Hyperoside nanocrystals for HBV treatment: process optimization,in vitro and in vivo evaluation

The aim of this study was to develop hyperoside (Hyp) nanocrystals to enhance its dissolution rate, oral bioavailability and anti-HBV activity. Hyp nanocrystals were prepared using high pressure homogenization technique followed by lyophilization. A Box–Behnken design approach was employed for process optimization. The physicochemical properties, pharmacokinetics and anti-HBV activity in vivo of Hyp nanocrystal prepared with the optimized formulation were systematically investigated. Hyp nanocrystals prepared with the optimized formulation was found to be rod shaped with particle size of 384?±?21?nm and PDI of 0.172?±?0.027. XRPD studies suggested slight crystalline change in drug. Dissolution rate obtained from Hyp nanocrystals were markedly higher than pure Hyp. The nanocrystals exhibited enhanced C_max (7.42?±?0.73 versus 3.80?±?0.66?mg/L) and AUC_0???t (193.61?±?16.30 versus 91.92?±?17.95?mg·h/L) with a 210.63% increase in relative bioavailability. Hyp nanocrystals exhibited significantly greater anti-HBV activity than Hyp. These results suggested that the developed nanocrystals formulation had a great potential as a viable approach to enhance the bioavailability of Hyp.     

高效液相色谱法同时测定云南白花木瓜不同部位中5个成分的含量

建立了一种采用高效液相色谱(HPLC)法同时测定白花木瓜中绿原酸、芦丁、金丝桃苷、齐墩果酸、熊果酸的质量浓度的方法,比较了果皮、果肉中绿原酸、芦丁、金丝桃苷、齐墩果酸、熊果酸质量浓度的差异.结果显示,在以A相(甲醇)和B相(体积分数为16％乙腈,体积分数为0.3％磷酸水溶液)为流动相的梯度洗脱条件下,绿原酸、芦丁、金丝...     

Extraction of hyperoside from Hypericum perforatum L. using CTAB reversed micelles

In this paper, the extraction of hyperosides from Hypericum perforatum L. using Cetyl‐trimethyl‐ammonium bromite (CTAB) reversed micelles was studied and the affecting factors, that is, pH value, CTAB concentration, and existence of anions in the system were comprehensively investigated. The result showed that extraction using CTAB reversed micelles is a very effective method to separate hyperoside from Hypericum perforatum L. This founding is very significant because it demonstrated that extraction using reversed micelles is a promising way to separate and purify materials of small molecules.     

HPLC法同时测定湘莲中芦丁、金丝桃苷及槲皮素含量

目的:建立高效液相色谱法同时测定湘莲中芦丁、金丝桃苷及槲皮素的含量。方法:采用Agilent ZORBAX SB-C₁₈色谱柱(4.6 mm×250 mm, 5μm),以甲醇—0.6%磷酸水溶液为流动相，梯度洗脱，流速1.0 mL/min,柱温30℃,检测波长255 nm。结果:20批湘莲样品中芦丁、金丝桃苷及槲皮素含量分别为1.32～2.06,1.36～2.43,1.41～3.26 mg/kg;芦丁、金丝桃苷和槲皮素检测质量浓度线性范围均为5～200μg/mL(R²=0.999 9),在相应的线性范围内，3种黄酮类物质线性关系好，灵敏度高，精密度、稳定性、重复性及回收率试验相对标准偏差(RSD)均小于4.0%;芦丁、金丝桃苷及槲皮素的平均加标回收率分别为96.6%,96.9%,97.4%。结论:该方法操作便捷且结果准确，可用于湘莲中黄酮类成分的含量测定和质量评价。