高效液相色谱法测定参芪五味子微丸中五味子甲素含量

目的建立参芪五味子微丸中五味子甲素的含量测定方法。方法采用高效液相色谱法,用十八烷基硅烷键合硅胶为固定相,以乙腈-水（12：88）为流动相,检测波长250nm,流速1mL／min。结果五味子甲素进样量在126．24～2524．8ng范围内与峰面积线性关系良好,r=1．0000（n=5）,平均加样回收率为99．93％,RSD=1．70％（n=9）。结论该方法适用于参芪五味子微丸中五味子甲素的含量测定。     

HPLC测定南五味子中的五味子酯甲和五味子甲素

目的 采用HPLC法测定南五味子中的五味子酯甲和五味子甲素.方法 采用Eclipse XDB-C18色谱柱(150 mm×4.6 mm,5 μm);乙腈-四氢呋喃-水(12∶17∶51)为流动相,流速1.0 mL·min-1,检测波长220 nm,柱温35 ℃.结果 五味子酯甲和五味子甲素的线性范围分别为0.047～0.282、0.049～0.291μg(r=0.9999);平均加样回收率分别为103.0%、103.5%,RSD分别为1.0%、1.2%.结论 所建方法简便、重复性好,可用于测定南五味子中的五味子酯甲和五味子甲素.     

七味都气丸中五味子醇甲的含量测定

目的:建立HPLC法七味都气丸中五味子醇甲含量的测定方法。方法:采用高效液相色谱法,色谱柱:钻石ODS柱(200 mm×4.6mm,5μm)。流动相:甲醇-水(64:36);流速为1.0ml·min~(-1);检测波长为250 nm;室温。结果:五味子醇甲的线性范围是0.12～1.48μg,r=0.999 9。平均加样回收率为98.2%,RSD=1.0%(n=9)。结论:该法可以用于测定七味都气丸中五味子醇甲的含量。     

反相高效液相色谱法测定参松养心胶囊中五味子甲素和五味子酯甲含量

目的建立高效液相色谱法测定参松养心胶囊中五味子甲素和五味子酯甲含量的方法。方法采用RP-HPLC法,色谱柱：Agilent Extend C18（250mm×4.6mm,5μm）;流动相：乙腈-水,梯度洗脱;流速：1.0mL.min-1;检测波长：230nm;柱温：35℃。结果五味子甲素进样量在0.020 2～0.161 7μg与峰面积线性关系良好,r=0.999 5,平均加样回收率为100.8%,RSD=0.3%;五味子酯甲进样量在0.021 0～0.168 0μg与峰面积线性关系良好,r=0.999 6,平均加样回收率为101.8%,RSD=0.3%。结论所建立的含量测定方法简便可行,结果准确可靠,可用于参松养心胶囊中五味子甲素和五味子酯甲的含量测定。     

HPLC法同时测定五酯微丸中五味子酯甲、五味子甲素和安五酯素

摘 要 目的：建立HPLC法同时测定五酯微丸中南五味子木脂素特征成分五味子酯甲、五味子甲素和安五酯素含量的方法。方法: 采用HPLC梯度洗脱同时测定五酯微丸中五味子酯甲、五味子甲素及安五酯素的含量,以月旭 Ultimate XB C18 (150 mm×4.6 mm, 3 μm)为色谱柱,四氢呋喃 水为流动相,梯度洗脱,检测波长为228 nm,柱温：35℃。结果: 五味子酯甲在0.040～0.805 μg的范围内,线性关系良好(r=0.999 9)。平均回收率为97.0%,RSD=1.67%。五味子甲素在0.092～1.846 μg的范围内,线性关系良好(r=0.999 9)。平均回收率为102.5%,RSD=1.49%。安五酯素在0.020 ～0.998 μg的范围内,线性关系良好(r=0.999 9)。平均回收率为95.0%,RSD=1.78%（n=6）。结论: 本方法简便、准确、重复性好,可提高五酯微丸的质量标准。     

HPLC法同时测定参芪五味子胶囊中五味子酯甲和五味子甲素的含量

目的:建立同时测定参芪五味子胶囊中五味子酯甲和五味子甲素含量的方法。方法:采用高效液相色谱法。色谱柱为Waters Xterra Ms C18,流动相为乙腈-四氢呋喃-水(18∶18∶64,V/V/V),流速为1.0 ml/min,检测波长为222 nm,柱温为25℃,进样量为10μl。结果:五味子酯甲和五味子甲素进样量分别在0.026 2⁰.418 4、0.024 90.418 4、0.024 9⁰.398 4μg范围内与各自峰面积积分值呈良好的线性关系(均r=0.999 9);精密度、稳定性、重复性试验的RSD≤1.7%;平均加样回收率分别为101.1%、100.8%,RSD分别为1.6%、1.5%(n=9)。结论:该方法重复性好、灵敏度高、结果准确可靠,可用于参芪五味子胶囊的质量控制。     

高效液相色谱法同时测定五味护肝胶囊中五味子醇甲、五味子甲素和五味子乙素含量

目的 建立同时测定五味护肝胶囊中五味子醇甲、五味子甲素和五味子乙素含量的高效液相色谱法.方法 采用高效液相色谱法,色谱柱为Waters sunfire TMC18柱(150mm×4.6mm,5 μm);以乙腈-水(56:32)为流动相,流速为1.0mL/min,检测波长为250 nm.结果 五味子醇甲进样量的线性范围为0.087 04～0.696 32 μg,r=0.999 98,平均回收率为103.40%,RSD为1.42%(n:6);五味子甲素进样量线性范围为0.018 304～0.146 43μg,r=0.999 98,平均回收率为97.45%,RSD为0.88%(n=6);五味子乙素进样量的线性范围为0.040 80～0.326 4 μg,r=0.999 96,平均加样回收率为95.88%,RSD为0.76%(n=6).结论 该方法简便、快速、准确,重现性好,可作为该制剂的含量测定方法.     

HPLC切换波长法同时测定参芪五味子片中五味子酯甲和五味子甲素的含量

目的通过切换波长高效液相色谱法同时测定参芪五味子片中五味子酯甲和五味子甲素的含量。方法采用高效液相色谱法,使用Agilent Zorbax SB-C18(250 mm×416 mm,5μm)色谱柱,以甲醇-水(69∶31)为流动相,流速:1.0 mL.min-1,柱温:40℃,五味子酯甲检测波长为222 nm,五味子甲素检测波长为251 nm。结果五味子酯甲、五味子甲素分别在0.171~3.420μg(Y=24 107 309X+2.717 84×105,r=0.999 9),0.218~5.460μg(Y=2 069 343X+1.041 10×105,r=0.999 9)范围内与峰面积呈良好的线性关系。平均加样回收率分别为99.73%,99.21%,RSD(n=6)分别为1.3%,1.4%。结论本法灵敏、准确、简便、快速,可用于同时测定参芪五味子片中五味子酯甲和五味子甲素含量。     

HPLC法测定太太静心助眠口服液中五味子醇甲、五味子甲素和五味子乙素的含量

目的 采用HPLC法建立同时测定太太静心助眠口服液中五味子醇甲、五味子甲素和五味子乙素的方法.方法 色谱柱Waters C18柱(250 mm× 4.6 mm,5μm),流动相为甲醇-水(梯度洗脱),检测波长为254 nm.结果 五味子醇甲浓度在2.022～101.1 μg/mL范围内与峰面积呈良好的线性关系,r为0.999 9;五味子甲素浓度在2.004～100.2 μg/mL范围内与峰面积呈良好的线性关系,r为0.9999;五味子乙素浓度在2.030～101.5 μg/mL范围内与峰面积呈良好的线性关系,r为0.9999.五味子醇甲加样回收率的平均值为101.9％,RSD=1.9％;五味子甲素加样回收率的平均值为101.9％,RSD=1.2％;五味子乙素加样回收率的平均值为100.4％,RSD=1.0％.结论 本方法简便、准确可靠,适用于太太静心助眠口服液中五味子醇甲、五味子甲素和五味子乙素三个主要有效成分的测定.     

利肺片中五味子醇甲和五味子甲素含量测定方法研究

目的：建立同时测定利肺片中五味子醇甲和五味子甲素的反相高效液相色谱（RP-HPLC）方法。方法：样品用甲醇超声提取,过滤,取续滤液,用RP-HPLC直接测定,十八烷基硅烷键合硅胶色谱柱,流动相为甲醇∶水（梯度洗脱）,检测波长254nm。结果：五味子醇甲和五味子甲素分别为1.636～16.36μg（r=1.000）和1.636～16.36μg（r=0.9990）范围内线性关系良好。平均加样回收率（n=6）分别为97.6%～101.8%、98.9%～101.5%,RSD分别为1.6%、1.0%。结论：该方法快速简便,可以用于利肺片中五味子醇甲和五味子甲素的含量测定。     

SCH 58261: A selective A2A adenosine receptor antagonists

The recent discovery of selective antagonists for the A_2A adenosine receptors has been of great help to further research in this field. One compound, SCH 58261, 5- amino-7-(β-phenylethyl)-2-(8-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine, is playing a key part in a variety of studies. This review describes its pharmacological characteristics as they are emerging in various laboratories. The compound has an affinity in the low nM range (Ki value of 1–2 nM) for A_2A receptors located on membranes from a variety of tissues and cell types, including rat and bovine brain striatum, human platelets, lymphocytes and neutrophils, porcine coronary arteries, and CHO cells transfected with the cloned human A_2A receptors. SCH 58261 has little or no affinity up to the μM range for adenosine A_2B, A₃, or other G protein-coupled receptors. Selectivity for A_2A vs. A₁ receptors varies from 53- to 750-fold, depending on membranes or type of assay. SCH 58261 blocks A_2A-receptor mediated increase of cyclic AMP formation with high potency (e.g., IC₅₀ values between 15 and 20 nM in human white blood cells). The tritiated form of SCH 58261 specifically labels A_2A receptors in discrete regions of the rat brain such as caudate-putamen, nucleus accumbens, and tuberculum olfactorium. In classic in vitro bioassays, such as A_2A-receptor-mediated vasodilation in coronary arteries, SCH 58261 displays competitive antagonistic properties (e.g., pA₂ value of 9.5 in porcine coronary arteries). In assays involving responses mediated by A₁ or A_2B receptors, SCH 58261 shows little or no activity up to concentrations about 100-fold higher than those affecting A_2A receptors (higher concentrations not being testable due to its poor water solubility). In the rat, SCH 58261 enhances locomotor activity (at 3.7 mg/kg ip), increases wakefulness (10 mg/kg ip) and slightly increases both blood pressure and heart rate (10 mg/kg ip). These activities appear to be specifically mediated by A_2A receptors since the drug counteracts the effect of A_2A receptor agonists in some experimental paradigms. In models mimicking CNS disorders, SCH 58261 potentiates the activity of L-DOPA or dopamine receptor agonists in the 6-hydroxydopamine-lesioned rat model. Moreover, the compound reduces brain infarct size in a rat model of cerebral ischemia. Altogether, SCH 58261 and its radiolabeled form have emerged as interesting tools for better understanding the function of A_2A receptors in physiological or altered conditions. Moreover, the neuroprotective properties of SCH 58261 indicate that drugs of this class have a potential for treatment of brain damage produced by Parkinson's disease or stroke. Drug Dev. Res. 42:63–70, 1997. © 1997 Wiley-Liss, Inc.     

治疗帕金森病新药:腺苷A_(2A)受体拮抗剂

腺苷A2A受体在基底神经节选择性表达并与运动行为有关。流行病学研究和实验室研究均表明阻断腺苷A2A受体能减轻多巴胺能神经元的退行性病变。腺苷A2A受体拮抗剂在改善PD症状的同时还能减缓疾病的进程。因此,腺苷A2A受体拮抗剂很可能成为治疗PD的新药物。     

真菌来源白细胞介素6受体拮抗剂2520A的研究

目的从真菌Torulomyces ovatus的代谢产物中分离白细胞介素6受体(IL-6R)拮抗剂。方法利用多种柱色谱进行分离纯化对IL-6R具拮抗活性的物质，根据理化性质、光谱数据确定其结构。结果从真菌Torulomyces ovatus的代谢产物中得到对IL-6R有拮抗活性的化合物2520A。结论2520A化合物为已知铁螯合物ferrichrome，首次报道该化合物具IL-6R拮抗活性，并确定其结构含有铁原子。     

Physiological regulation of acute inflammation by A2A adenosine receptor

The activation of Gs‐coupled A_2A adenosine receptor on the surface of immune cells increases levels of immunosuppressive cyclic AMP and leads to inhibition of secretion of proinflammatory cytokines, which, in turn, results in downregulation of acute inflammation. The role of A_2A receptors in the regulation of inflammation appears to be non‐redundant. Small doses of inflammatory stimulus induce high levels of proinflammatory cytokines and extensive tissue injury in A_2A receptor‐deficient (Adora2a^?/?) mice leading to death due to unregulated inflammatory damage. The gene‐dose effect of A_2A receptor expression in T cells suggests that there are no spare A_2A receptors and that the final outcome of immune cell activation may be dependent on the number of these receptors on the individual immune cells. Heterozygous (Adora2a^+/?) mice express decreased levels of A_2A receptor on the surface and adenosine‐induced cAMP‐accumulation of immune cells was lower than in wild‐type. Thus, the number of A_2A receptors determines cAMP response to adenosine and may pre‐determine the immunosuppressive role of adenosine. Drug Dev Res 64:172–177, 2005. © 2005 Wiley‐Liss, Inc.     

中药止咳橘红颗粒对CYP3A4和CYP1A2抑制作用的研究

目的：在人体内研究止咳橘红对CYP3A4和CYP1A2的抑制作用，以预测止咳橘红与常用临床药物的相互作用。方法：咪哒唑仑和咖啡因分别作为CYP3A4和A2的探针药物，采取交叉设计，10名受试者在服用3d止咳橘红的前后均服用7.5mg咪哒唑仑和100mg咖啡因，服药后采血测定两者及代谢产物的代谢动力学参数，探讨针药物及代谢物的浓度用HPLC-MS法测定，Cmax,tmax从药时曲线中直接读出，AUC用梯形法计算，Ke用3P87程序进行拟合计算，分析服药前后CYP3A4和CYP1A2被抑制的情况，结果 服用止咳橘红后，咪哒唑仑的代谢受到了轻微的抑制，它的血药浓度，达峰时间和药时曲线下面积都有了升高趋势，但无显著差异。而咖啡因的代谢未受到影响。结论 止咳橘红对CYP3A4的活性有较弱的抑制作用，能够导致CYP3A4底物咪哒唑仑代谢的轻微抑制，而对CYP1A2的活性没有影响。止咳橘红长期使用或超过治疗剂量使用时是否会对CYP3A4产生显著性影响。尚需进一步的研究证明。     

Towards selective phosphodiesterase 2A (PDE2A) inhibitors: a patent review (2010 - present)

Introduction: The cyclic nucleotides cAMP and cGMP are ubiquitous intracellular second messengers regulating a large variety of biological processes. The intracellular concentration of these biologically relevant molecules is modulated by the activity of phosphodiesterases (PDEs), a class of enzymes that is grouped in 11 families. The expression of PDEs is tissue- and cell-specific allowing spatiotemporal integration of multiple signaling cascades. PDE2A is a dual substrate enzyme and is expressed in both the periphery and in the central nervous system, however its expression is highest in the brain, where it is mainly localized in the cortex, hippocampus, and striatum. This suggests that this enzyme may regulate intraneuronal cGMP and cAMP levels in brain areas involved in emotion, perception, concentration, learning and memory.

Areas covered: This review covers the patent applications published between January 2010 and February 2016 on phosphodiesterase 2A inhibitors.

Expert opinion: Recent publications in the literature and in filed patent applications demonstrate the interest of pharmaceutical companies for PDE2A. This has increased the insights of its possible therapeutic role but the few clinical trials were terminated. Based on the ongoing interest in the field it is likely that new clinical trials can be expected and will unravel the therapeutic potential of PDE2A inhibition.     

A.A., Constructivism,and Reflecting Teams

Numerous studies and clinical anecdotes reveal a relationship between attendance at A.A. meetings and/or degree of involvement in A.A. and maintenance of sobriety. Hypotheses as to how A.A. and/or the A.A. meeting is helpful to its members have ranged from a focus on factors common to all therapy groups, to aspects of A.A. “treatment” which are behavioral in nature. Presented here is another way of understanding A.A.'s effectiveness within the frame of more recent, constructivistic approaches to family therapy. In particular, the A.A. topic meeting is compared to the reflecting team concept of Tom Anderson.     

五味子甲素对大鼠肝微粒体CYP3A活性的影响

目的：通过体外药物代谢实验探讨五味子甲素对CYP3A活性的影响。方法：以大鼠肝微粒体为载体,选取咪达唑仑（MDZ）作为药物“探针”,建立高效液相色谱（HPLC）检测方法,体外给药测定五味子甲素对MDZ的IC50值以及相关酶动力学参数。结果：孵育体系内源性物质不干扰测定,方法快捷、稳定、灵敏度高。在肝微粒中,五味子甲素对MDZ的IC50浓度为6．26μmol／mL,相关酶动力学参数：Km=15．77μmol／L,Ki=5．50μmol／mL。结论：五味子甲素对大鼠肝微粒体CYP3A活性具有抑制作用,其抑制作用为混合型,即：非竞争与反竞争抑制。     

伊贝碱甙A的分离和鉴定

伊贝母Fritillaria pallidiflora Schreb系百合科贝母属伊贝母的干燥鳞茎,是药用贝母之一,已列入中华人民共和国1985年版药典。主产于新疆,具有产量高、生物碱含量高和抗病虫害能力强等优点。中国农科院左家特产研究所于1985年在吉林省引种栽培伊贝母获得成功。为阐明吉林省栽培的伊贝母的有效成分,以便扩大栽培和应用,我们研究了伊贝母的生物碱成分,曾分离到西贝素、西贝素-3β-D-葡萄糖甙和贝母辛。在继续研究中,又