吉产不同生长年限人参中8种主要人参皂苷与人参皂苷Rg_1比值的变化规律研究

目的:探讨吉产不同生产年限人参中8种主要人参皂苷与人参皂苷Rg_1的比值的变化规律,为其生长年限的鉴别提供参考。方法:收集吉林省不同生长年限(3～30年)的园参、林下参、野山参样品,采用高效液相色谱法(HPLC)测定人参中人参皂苷Rg_1、Re、Rf、Rb_1、Rc、Rb_2、Rb_3、Rd等8种成分的含量;计算各皂苷单体含量及8种人参皂苷总含量分别与人参皂苷Rg_1含量的比值,并探究该比值与生长年限的关系。结果:随人参生长年限的增长,园参中8种人参皂苷总含量与人参皂苷Rg_1的比值及人参皂苷Re、Rb_1、Rc、Rd单体含量与人参皂苷Rg_1的比值均逐渐减小(P<0.001),林下参中人参皂苷Re与人参皂苷Rg_1的比值呈先减小后增加趋势(P<0.001),野山参中8种人参皂苷总含量与人参皂苷Rg_1的比值及人参皂苷Re、Rb_1与人参皂苷Rg_1的比值均逐渐增加(P<0.001),而园参、林下参、野山参中人参皂苷Rf、Rb_3与人参皂苷Rg_1的比值则均无明显差异(P>0.05)。结论:园参、林下参、野山参均含有8种人参皂苷成分,可根据人参皂苷Rg_1含量和人参皂苷Re、Rb_1单体含量与人参皂苷Rg_1的比值初步推测其生长年限。     

RP-HPLC法同时测定西洋参含片中4种成分

目的建立同时测定西洋参含片中人参皂苷Rg_1、人参皂苷Re、人参皂苷Rb_1及拟人参皂苷F11含量的RP-HPLC方法。方法色谱柱为Agilent TC-C18(250 mm×4.6 mm,5μm);流动相为0.5 mL·L~(-1)磷酸溶液(A)-乙腈(B),梯度洗脱;流速:1.0mL·min~(-1);检测波长:203nm;柱温:30℃。结果人参皂苷Rg_1和人参皂苷Re及人参皂苷Rb_1在2.5~500μg·mL~(-1)、拟人参皂苷F11在5.0~1 000μg·mL~(-1)范围内线性关系良好(r≥0.999 4);平均加样回收率均大于95.0%。结论该方法简便、准确,重复性好,可作为西洋参含片的质量控制方法。     

NIRS结合PLS算法快速测定西洋参饮片中人参皂苷Rg_1、Re、Rb_1的总含量

目的:建立快速测定西洋参饮片中人参皂苷Rg_1、Re、Rb_1总含量的方法。方法:采用高效液相色谱法测定饮片中人参皂苷Rg_1、Re、Rb_1的总含量(作为参考值)。采用红外漫反射光谱技术(NIRS)结合偏最小二乘法(PLS)建立饮片中人参皂苷Rg_1、Re、Rb_1总定量模型:根据参考值采集62份饮片样品,以标准归一化法联合一阶导数法预处理光谱,饮片样品中人参皂苷Rg_1、Re、Rb_1总含量测定最佳波段为7 664.23~5 236.05 cm~(-1)。结果:饮片样品中人参皂苷Rg_1、Re、Rb_1总含量测定方法学验证符合要求。人参皂苷Rg_1、Re、Rb_1总定量模型的校正集相关系数为0.991 03,校正均方差为0.010 26。结论:该方法快速准确、简便无污染,可用于西洋参饮片中人参皂苷Rg_1、Re、Rb_1总含量的快速测定。     

人参质量控制的定性与定量方法研究

目的:建立中药人参的质量控制方法。方法:高效液相色谱法,Diamonsil~(TM)(钻石)C_(18)分析柱(150mm×4.6mm,5μm),流动相为乙腈-水(22:78),流速为1.0mL·min~(-1),检测波长为203nm,柱温40℃;抗疲劳药理试验以十全大补丸为阳性对照,小鼠灌胃给药(人参总皂苷)10d后观察其游泳持续时间的变化。结果:在本色谱条件下,11份不同人参商品完整药材中人参皂苷的HPLC图谱中可检出10个相对位置稳定的色谱峰,进而确定出7个人参皂苷的共有峰,作为其定性鉴别的指标峰;人参皂苷Rg_1、Re的回收率分别为98.6％和97.8％,RSD分别为0.15％和0.13％,人参皂苷Rg_1、Re的含量分别为0.091％～0.273％和0.033％～0.258％;人参皂苷可显著延长小鼠游泳的持续时间。结论:本文所建立的人参皂苷Rg_1;、Re含量测定及人参总皂苷的HPLC图谱鉴别方法,简便、准确,可用于人参的质量控制;药理实验研究表明人参总皂苷具有明显的抗疲劳作用,且量效关系显著。     

HPLC—ELSD测定红参中人参皂苷Rg1、Re、Rb1含量

目的:用 HPLC-ELSD 测定红参中人参皂苷 Rg_1、Re、Rb_1含量。方法:采用 Agilent XDB-C_(18)柱(4.6 mm×150 mm,5 μm),柱温30℃;流动相为乙腈-水,梯度洗脱[0～24 min:乙腈-水(19.5:80.5);24～39 min:乙腈-水(30:70)],流速1.0 mL·min~(-1);漂移管温度98.8℃,载气流速2.7 L·min~(-1)。结果:人参皂苷 Rg_1、Re、Rb_1分别在1.08～6.48 μg、0.678～4.068 μg、1.024～6.144 μg范围内呈良好的线性关系。3种人参皂苷的平均回收率(n=5)分别为99.2%(RSD=1.3%),99.3%(RSD=2.4%),99.9%(RSD=1.9%)。结论:本方法灵敏、简便、准确。     

HPLC法同时测定注射用艾迪（冻干）中人参皂苷Rg1和人参皂苷Re的含量

目的:建立注射用艾迪(冻干)中人参皂苷Rg_1和人参皂苷Re的含量测定方法。方法:色谱柱为Hypersil C_(18)柱(250mm×4.6mm,5μm),流动相为乙腈-0.05%磷酸溶液(19∶81),流速为1.0mL·min~(-1),检测波长为203nm。结果:人参皂苷Rg_1浓度在20～200μg·mL~(-1),人参皂苷Re浓度在10～100μg·mL~(-1)范围内与峰面积呈良好的线性关系,相关系数分别为0.9997和0.9996;平均回收率分别为100.3%和97.6%(n=9)。结论:本法快速,准确,重复性好,可作为注射用艾迪(冻干)的质量控制方法。     

田七痛经胶囊检测方法的研究

目的:建立田匕痛经胶囊的质量控制方法。方法:采用 TLC 方法对田七痛经胶囊中的木香、川芎、延胡索进行定性鉴别;采用 HPLC 法,YWG C_(18)色谱柱(250 mm×4.6 mm,10μm),以乙腈-0.05%(v/v)磷酸溶液(100:400)为流动相,流速1 mL·min~(-1),检测波长203 nm,柱温为室温,进样量20μL,对田七痛经胶囊中的三七皂苷 R_1、人参皂苷 Rg_1和人参皂苷 Re 进行定性鉴别,并对人参皂苷 Rg_1进行含量测定。结果:木香、川芎、延胡索的薄层鉴别和三七皂苷 R_1、人参皂苷 Rg_1和人参皂苷Re 的 HPLC 鉴别专属性强,人参皂苷 Rg_1进样量在3.0～15.0μg范围内与峰面积呈良好的线性关系(r=1.000,n=5)。人参皂苷 Rg_1。平均回收率为99.1%,RSD=2.6%(n=5)。结论:本方法可准确地进行定性、定量,可用于控制田七痛经胶囊的质量。     

高效液相色谱-蒸发光散射测定三七中三七皂苷R1及人参皂苷Rg1、Re、Rb1的含量

目的:用 HPLC—ELSD 测定三七药材中三七皂苷 R_1及人参皂苷 Rg_1、Re、Rb_1的含量。方法:色谱柱为 Lichrospher NH_2柱(4.6 mm×250 mm,5μm),流动相为乙腈-水(80:20);漂移管温度为90℃,载气流速为2.1 L·min~(-1)。结果:三七皂苷 R_1及人参皂苷 Rg_1、Re、Rb_1分别在0.316～1.58μg、1.21～6.05μg、0.448～2.24μg及1.49～7.47μg呈良好线性关系;药材中4种成分的平均回收率(n=6)分别为102.2%(RSD=2.6%)、99.4%(RSD=2.2%)、101.8%(RSD=2.5%)及97.6%(RSD=2.4%)。结论:该方法简便、准确,分离效果好,无干扰,可用于三七药材的质量评价。     

胶束电动毛细管色谱法分离分析三七中的人参皂苷Rg1、人参皂苷Re和三七皂苷R1

目的:用胶束电动毛细管色谱法分离测定三七中人参皂苷 Rg_1、人参皂苷 Re 和三七皂苷 R_1 3种皂苷含量。方法:采用Beckman MDQ 电泳仪,40 cm×50 μm的熔融石英毛细管,有效柱长30 cm,缓冲液为20 mmol·L~(-1)SDS、40 mmol·L~(-1)胆酸钠、60 mmol·L~(-1)硼砂,检测波长200 nm。结果:人参皂苷 Rg_1低、中、高剂量的平均加样回收率分别为101.5%,100.6%,100.4%,RSD 分别为2.4%,2.2%,1.0%;人参皂苷 Re 低、中、高剂量的平均加样回收率分别为101.3%,99.23%,99.66%,RSD 分别为2.0%,1.3%,1.1%;三七皂苷 R_1低、中、高剂量的平均加样回收率分别为100.6%,100.5%,100.7%,RSD 分别为1.1%,1.1%,0.86%。结论:本方法能够将三七药材中人参皂苷 Rg_1、人参皂苷 Re 和三七皂苷 R_1完全分离,具有灵敏度高、快速、易于重现且所用试剂价格低廉的特点,因此适合于中药三七的测定,并对今后三七的鉴别和质量控制具有重要意义。     

HPLC-MS/MS法同时测定三七须根总皂苷中人参皂苷Rg_1和Re的含量

目的:建立以液-质联用法同时测定三七须根总皂苷中人参皂苷Rg1和Re含量的方法。方法:色谱柱为BDS HYPERSUL C18(150mm×2.1mm,5μm),流动相为乙腈-水(梯度洗脱),柱温为30℃;采用负离子多反应监测方法(MRM)测试。用于定量分析的对照品离子对分别为人参皂苷Rg1:m/z799.6→475.5;人参皂苷Re:m/z945.8→783.7;内标物紫杉醇m/z:852.5→525.3。结果:人参皂苷Rg1、人参皂苷Re标准曲线的线性范围分别为0.173～17.3μg·mL-1和0.156～39.1μg·mL-1,精密度和准确度等均符合样品分析的要求。结论:本方法准确、灵敏、特异性强,适用于三七须根总皂苷及其制剂中人参皂苷Rg1、Re含量的同时测定。     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.