不同产地个青皮高效液相色谱指纹图谱研究

目的 研究不同产地个青皮的高效液相色谱(HPLC)法指纹图谱. 方法用Aichrom Bond AQ C₁₈色谱柱(250 mm×4.6 mm ,5 μm),乙腈和0.1%磷酸水为流动相,采用梯度洗脱,流速:1.0 mL•min^-1,柱温:30 ℃,检测波长:360 nm. 结果 建立HPLC指纹图谱共有模式,各产地个青皮药材质量有较好的相似性. 结论 该指纹图谱方法准确可靠,重复性好,可作为个青皮药材内在质量评价的依据.     

橙皮苷、柠檬烯及茶多酚清除自由基能力的对比研究

目的:研究橙皮苷、柠檬烯及茶多酚对1,1-二苯基-2-三硝基苯肼自由基( DPPH·) 和羟基自由基(·OH)的清除能力。方法:UV-Vis光谱分析方法测定3种天然产物对DPPH·和·OH自由基的清除作用。结果:3种天然产物在实验浓度范围内,对两种自由基均有清除作用,清除效果随浓度增大而增加。橙皮苷(IC₅₀=0.097,0.011)清除DPPH·和·OH的能力明显强于柠檬烯(IC₅₀=0.0024,0.0004)、茶多酚(IC₅₀=0.0144,0.009)。结论:橙皮苷比茶多酚、柠檬烯清除DPPH·和·OH的能力强。     

芙朴感冒颗粒中橙皮苷小肠吸收特征研究

目的 研究芙朴感冒颗粒中的橙皮苷跨膜吸收特征及其影响因素.方法 使用Caco-2细胞模型考察橙皮苷的小肠吸收,研究不同药物浓度、pH值、温度和抑制剂对橙皮苷在transwell细胞培养板中从顶膜(AP)到基底(BL)的双向渗透吸收的影响.采用药动学实验研究芙朴感冒颗粒在体内对橙皮苷吸收的影响.结果 橙皮苷以3种测试浓度...     

The potential of a niacinamide dominated cosmeceutical formulation on fibroblast activity and wound healing in vitro

Knowledge on the intrinsic mechanisms involved in wound healing provides opportunity for various therapeutic strategies. The manipulation of dermal fibroblast proliferation and differentiation might prove to beneficially augment wound healing. This study evaluated the combined effects of niacinamide, l ‐carnosine, hesperidin and Biofactor HSP® on fibroblast activity. The effects on fibroblast collagen production, cellular proliferation, migration and terminal differentiation were assessed. In addition, the authors determined the effects on in vitro wound healing. The optimal concentrations of actives were determined in vitro. Testing parameters included microscopic morphological cell analysis, cell viability and proliferation determination, calorimetric collagen detection and in vitro wound healing dynamics. Results show that 0·31 mg/ml niacinamide, 0·10 mg/ml l ‐carnosine, 0·05 mg/ml hesperidin and 5·18 µg/ml Biofactor HSP® proved optimal in vitro. The results show that fibroblast collagen synthesis was increased alongside with cellular migration and proliferation.     

Antioxidants and Collagen-Crosslinking: Benefit on Bond Strength and Clinical Applicability

Antioxidants are known for their potential of strengthening the collagen network when applied to dentin. They establish new intra-/intermolecular bonds in the collagen, rendering it less perceptive to enzymatic hydrolysis. The study evaluated the benefit on shear bond strength (SBS) of a resin–composite to dentin when antioxidants with different biomolecular mechanisms or a known inhibitor of enzymatic activity are introduced to the bonding process in a clinically inspired protocol. Specimens (900) were prepared consistent with the requirements for a macro SBS-test. Four agents (Epigallocatechingallate (EGCG), Chlorhexidindigluconate (CHX), Proanthocyanidin (PA), and Hesperidin (HPN)) were applied on dentin, either incorporated in the primer of a two-step self-etch adhesive or as an aqueous solution before applying the adhesive. Bonding protocol executed according to the manufacturer’s information served as control. Groups (n = 20) were tested after one week, one month, three months, six months, or one year immersion times (37 °C, distilled water). After six-month immersion, superior SBS were identified in PA compared to all other agents (p < 0.01) and a higher reliability in both primer and solution application when compared to control. After one year, both PA incorporated test groups demonstrated the most reliable outcome. SBS can benefit from the application of antioxidants. The use of PA in clinics might help extending the lifespan of resin-based restorations.     

Mangiferin and hesperidin metabolites are absorbed from the gastrointestinal tract of pigs after oral ingestion of a Cyclopia genistoides (honeybush tea) extract

Health-promoting properties such as antioxidative, anticarcinogenic, and cholesterol-lowering effects are described for mangiferin and hesperidin, the major phenolic compounds present in Cyclopia genistoides (honeybush). However, knowledge of their metabolic fate and their absorption from the gastrointestinal tract is very limited. The aim of this study was to determine the concentrations of mangiferin, hesperidin, and their metabolites in plasma, urine, and feces samples from pigs consuming an extract of Cyclopia genistoides. Pigs were administered up to 74 mg mangiferin per kilogram of body weight and 1 mg hesperidin per kilogram of body weight per day for 11 days. Plasma samples were collected at various time points on days 9 and 11 of the study and days 1 and 2 after termination of extract administration. Urine and feces were collected in fractions for 24 hours. In the plasma samples, the aglycone of mangiferin (norathyriol) was detected. Mean plasma concentrations ranged from 7.8 to 11.8 μmol/L. Six metabolites of mangiferin and hesperidin were detected in the urine, including methyl mangiferin, norathyriol, its monoglucuronide, hesperetin, hesperetin monoglucuronide, and eriodictyol monoglucuronide. Between 26.0% and 30.8% of the administered dose of hesperidin and only between 1.4% and 1.6% of mangiferin could be detected in the urine on days 9 and 11 of the study. Approximately 8.2% of the administered dose of mangiferin was determined in the feces. The main metabolite was norathyriol. Neither hesperidin nor metabolites ascribed to hesperidin intake were detected. The results suggest that formation of norathyriol from mangiferin occurs in vivo, and specific metabolites were identified in blood and excretion products in urine and feces. This study will aid in investigating the physiological functions of the parent compounds in vivo.     

胆立宁软胶囊质量标准研究

[目的]建立胆立宁软胶囊质量控制标准。[方法]采用高效液相色谱法,对胶囊中芍药苷进行定量分析,采用薄层色谱法对方中枳壳药材进行定性鉴别。[结果]芍药苷进样量在0.287～5.74μg范围内,进样量与峰面积呈良好线性关系.A=1×106C＋127853,r=0.9995,平均回收率为96.4%,RSD为3.15%;TLC谱检出橙皮苷斑点。[结论]本实验确定的质量控制方法便捷,结果准确可靠、重复性好,可作为胆立宁软胶囊质量控制标准。     

HPLC法测定枳壳不同炮制品中柚皮苷、橙皮苷和新橙皮苷的含量

目的:用HPLC法对枳壳的江西炮制方法及其药典法炮制品中柚皮苷、橙皮苷和新橙皮苷含量进行测定。方法:色谱柱:E1823028 C18(250mm×4.6mm,5μm);流动相为乙腈-0.1%磷酸水(23:77),检测波长UV 285nm,流速1.0mL/min,柱温30℃。结果:柚皮苷在0.596-5.960μg范围内线性关系良好(r=0.9997),橙皮苷在0.106-1.060μg范围内线性关系良好(r=0.9996),新橙皮苷在0.470-4.700μg范围内线性关系良好(r=0.9999)。柚皮苷的平均回收率为101.17%(RSD=1.26%),新橙皮苷的平均回收率为101.28%(RSD=1.34%),橙皮苷的平均回收率为101.20%(RSD=0.895%)。结论:该方法简单、准确,可用于枳壳药材的质量控制;樟帮炮制法对枳壳的成分影响较大,并且有新的成分产生。     

Hesperidin induces antinociceptive effect in mice and its aglycone, hesperetin, binds to μ-opioid receptor and inhibits GIRK1/2 currents

This paper extended the evaluation of the depressant and antinociceptive activities of hesperidin in order to determine its effectiveness by the intraperitoneal and oral routes, its pharmacological interaction with diverse pathways of neurotransmission and the role of its aglycone, hesperetin. The capacity of hesperidin and hesperetin to bind to μ-opioid receptor and their actions on μ-opioid receptor co-expressed with GIRK1/GIRK2 channels (G protein-activated inwardly rectifying K⁺ channels) in Xenopus laevis oocytes were also determined.Hesperidin exhibited a depressant activity in the hole board and locomotor activity tests, antinociceptive activities in the abdominal writhing and hot plate tests and no motor incoordination in the inverted screen and rotarod assays, only by the intraperitoneal route. Hesperetin did not show any effects in vivo in mice in these models, but in vitro it displaced the [³H]DAMGO binding with low-affinity and inhibited inward currents through the expressed GIRK1/2 channels. Although hesperidin actions in vivo demonstrated to be mediated by an opioid mechanism of action, it failed to directly bind to and activate the μ-opioid receptor or produce any change on inward GIRK1/2 currents in vitro. However, it should be considered that hesperidin may be metabolized, possibly resulting in crucial changes in its biological activity.     

桔皮苷对糖尿病大鼠心电活动的影响

目的研究桔皮苷对糖尿病模型大鼠心电活动的影响。方法30只SD大鼠随机分为三组。糖尿病模型组（n=12）：一次性腹腔注射大剂量链脲佐菌素（STZ）诱导建立糖尿病模型;桔皮苷干预组（n=12）：建立糖尿病模型,每日10mg／kg桔皮苷灌胃;对照组（n=6）：不建模亦不干预。分组处理4周后,记录和比较三组大鼠在体、离体心电图及心室肌细胞动作电位特征。以1×10^-6mol／L和5×10^-6mol／L桔皮苷灌流糖尿病模型组大鼠心室乳头肌,连续记录动作电位变化。结果在体心电图分析显示,与对照组比较,糖尿病模型组和桔皮苷干预组大鼠心率均明显加快（P〈0．01,P〈0．05）;糖尿病模型组大鼠QT间期显著延长（P〈0．05）,桔皮苷干预组大鼠QT间期与对照组比较差异无统计学意义（P〉0．05）。离体心电图观察发现,糖尿病模型组快速型心律失常发生率为75．0％,明显高于桔皮苷干预组的16．7％（P〈0．05）。心室肌细胞动作电位各项参数比较显示,糖尿病模型组心肌细胞静息电位、动作电位幅度和0期最大除极速率均较对照组明显减小或下降,而动作电位时程延长;与糖尿病模型组比较,桔皮苷干预组动作电位各项参数则更接近对照组。两种浓度的桔皮苷灌流实验显示,与1×10^-6mol／L桔皮苷灌流比较,5×10^-6mol／L桔皮苷灌流对糖尿病大鼠心室乳头肌动作电位的恢复效应更为显著。结论桔皮苷可能通过逆转心电异常活动而降低糖尿病大鼠的心律失常发生率,且呈一定的浓度依赖效应。