HPLC法测定含化上清片中白花前胡甲素和白花前胡乙素的含量

目的建立含化上清片中白花前胡甲素和白花前胡乙素含量测定的高效液相色谱方法。方法色谱柱为Agilent C18(250mm×4.6mm,5μm);流动相为甲醇-水(75∶25);流速为1.0mL·min-1;检测波长为321nm;柱温为30℃。结果白花前胡甲素质量浓度在10.13~200.26μg·mL-1范围内呈良好的线性关系(r=0.999 2),加样回收率为98.9%,RSD为0.46%(n=6);白花前胡乙素质量浓度在10.36~200.72μg·mL-1范围内呈良好的线性关系(r=0.999 1),加样回收率为98.6%,RSD为0.55%(n=6)。结论该方法简单、准确、重复性好,可用于含化上清片中白花前胡甲素和白花前胡乙素的含量测定。     

HPLC法测定云南不同产地白花丹的不同部位中白花丹醌的含量

目的:建立白花丹药材中白花丹醌的反相高效液相色谱测定方法,以分别考察云南不同产地白花丹药材的不同部位中白花丹醌的含量。方法:色谱柱为 Kromasil C_(18)柱(250 mm×4.6 mm,5μm),流动相为甲醇-水(70:30),流速为1.0mL·min~(-1),检测波长为254 nm,柱温为25℃。结果:白花丹醌在25.3～253μg·mL~(-1)范围内,具有良好的线性关系,r=0.9998;平均回收率为99.0%,RSD=1.4%(n=6)。不同产地白花丹药材地上部分的白花丹醌含量分别为0.046%(嘎洒),0.079%(勐养),0.134%(嘎东),0.032%(曼东),0.047%(曼阁),0.057%(曼老);根部的白花丹醌含量分别为0.842%(嘎洒),1.04%(勐养),1.44%(嘎东),0.763%(曼东),0.639%(曼阁),1.97%(曼老)。结论:本法简便、准确,灵敏度高,重复性好,可用于控制白花丹药材质量。     

白花蒿素的结构

自菊科(Conpositae)植物白花蒿(Arlemisia factiflora Wall.)的花和叶中分离得到一种新的天然产物,命名为白花蒿素(lactiflorasyne)经光谱(UV,IR,MS,¹HNMR,²DNMR,¹³CNMR)分析以及X-光晶体衍射解析确定其结构如(Ⅰ)所示。     

复方白花龙胆中白花龙胆的鉴别和甘草酸的含量测定

目的建立复方白花龙胆的质量标准。方法采用TLC法定性,RP-HPLC法测定甘草中甘草酸的含量。用Krom asilC18色谱柱(250 mm×4.6 mm,5μm),以甲醇-0.2 mol.L-1醋酸铵-冰醋酸(67:33:1)为流动相,流速1.0 m l.m in-1,柱温25℃,检测波长250 nm。结果鉴别了复方中的白花龙胆;甘草酸铵进样量在0.402~2.010μg之间,进样量与峰面积呈很好的线性关系(r=0.9998),平均回收率为101.28%,RSD=1.71%(n=6)。3批样品中甘草酸的含量以甘草酸铵计,分别为4.042、4.006、4.062 mg.g-1(n=3)。结论所建方法简便、准确、重复性好,可用于复方白花龙胆的定性和定量分析。     

BP-HPLC测定白花前胡中Pd-Ia和Pd-Ⅱ的含量

目的:建立RP-HPLC测定白花前胡根中白花前胡丙素(Pd-Ia)和白花前胡丁素(Pd-Ⅱ)的含量.方法:采用Shim-Pack CLC-ODS柱,甲醇-水(79:21)为流动相,流速为1.0 ml@min-1,以Pd-Ia、Pd-Ⅱ为对照品,外标法峰面积定量,紫外检测(λ=323 nm).结果:Pd-Ia、Pd-Ⅱ线性范围分别为0.08～0.8 μg和0.064～0.28 μg,r=0.9999和r=0.9999,平均回收率分别为98.90%和98.91%.结论:方法准确,简便,灵敏度高,快速,重复性好.     

中药白花前胡根中香豆素白花前胡素(E)的分离鉴定

从白花前胡(Peucedanum praeruptorum Dunn)根的醚提取物中除分得已知香豆素白花前胡丙素和另一种结晶外,还分得一种具有生理活性的香豆素单体,命名为(+)白花前胡素(E)[(+)praeruptorin E]。经元素分析、紫外、红外、质谱、核磁、气相及水解产物的鉴定,证明白花前胡素(E)为(+)3′-当归酰基-4′-异戊酰基-顺式-凯林酮(+)3′-angeloyl-4′-isovalerylcis-khellactone,此香豆素对小白鼠具有耐缺氧作用。关于其他成分,将另有报告。     

基于UPLC法快速测定前胡配方颗粒中指标性成分

目的 建立超高效液相法(UPLC)对前胡配方颗粒中白花前胡甲素、白花前胡乙素和白花前胡素E同时快速定量分析的方法。方法 采用Acquity UPLC BEH C₁₈色谱柱(50 mm×2.1 mm, 1.7μm),以甲醇-水为流动相,梯度洗脱,体积流量0.4 mL·min^-1,在321 nm波长处进行检测,柱温25℃,进样量2.0μL。结果 前胡配方颗粒中3种有效成分在考察线性范围内线性关系良好,白花前胡甲素、白花前胡乙素、白花前胡素E的线性范围分别为1.870～18.70μg·mL^-1(r=0.9998)、0.2075～2.075μg·mL^-1(r=0.9998)、0.2220～2.220μg·mL^-1(r=0.9997),加样回收率均在98.85%～99.76%,RSD均小于2.0%。结论 该方法简便,准确,快速,重复性好,可用于前胡配方颗粒的快速质量控制,并为将来该配方颗粒的质量标准提升提供参考。     

白花丹炮制前后对大鼠四氯化碳慢性肝损伤模型的影响

目的比较白花丹炮制前后对大鼠慢性肝损伤模型的影响。方法选用体重180~220 g SD大鼠,随机分为正常对照组,模型对照组,秋水仙碱组(1×10-4 g·kg-1),白花丹生品高、低剂量(10、5 g·kg-1)组,白花丹炮制品高、低剂量(10、5 g·kg-1)组。除正常对照组外,其余各组大鼠皮下注射40%四氯化碳花生油溶液,按0.6 m L/l00 g体重给予,每周2次,连续8周,造模2周后连续给药6周,实验结束后腹主动脉取血,检测血清中AST、ALT、ALB、TP及HA含量,另取适量肝组织检测Hyp、SOD、MDA含量。结果白花丹生品组出现毒性反应,有动物死亡,其余各组均无动物死亡现象。白花丹炮制品组实验后动物体重显著增长,而白花丹生品组这一现象不明显。白花丹生品组和炮制品组对大鼠慢性肝损伤模型血清AST、ALT、ALB、TP含量均有不同程度的降低作用,炮制品组降低AST、ALT作用与白花丹生品组相比显著增强。白花丹生品及炮制品对HA及Hyp含量均有不同程度的降低作用,均可提高肝损伤大鼠肝组织SOD活性,降低MDA含量,且呈剂量依赖性,炮制品效果更好。结论白花丹生品及炮制品对大鼠慢性肝损伤均具有一定的保护作用,白花丹炮制后能达到一定的减毒增效作用。     

白花丹不同提取部位体外抗肿瘤及急毒研究

白花丹为蓝雪科植物白花丹Plumbago zeylanicaL.的干燥根、根茎和全草。为东南亚许多国家及中国多民族常用药材[1]。在民间有良好地治疗某些恶性疾病(癌症)的临床应用基础,本文拟对白花丹不同溶媒提取物进行体外抗肿瘤活性筛选,以期为进一步开发利用提供科学依据。1材料与方法1.1材料1.1.1供试品白花丹石油醚部位(A)、三氯甲烷(B)、乙酸乙酯(C)、水饱和的正丁醇(D)、水部位(E)均自备。1.1.2试剂RPMI1640、DMEM(低糖),购自Gibco;小牛血清,购自成都哈里;胰蛋白酶,购自Gibco;MTT、DMSO,购自Sigma公司。1.1.3癌细胞株乳腺癌细胞株(mda…     

白花前胡中白花前胡甙和Pd-C-I的分离和鉴定

从白花前胡(Peucedanum,praeruptorum)根中分得7个化合物,经化学方法和光谱分析分别鉴定为Pd-C-I(I),白花前胡甙(II),香草酸(III),没食子酸(IV),nodakenin(V),rutarin(VI)和isorutarin(VII)。II为新化合物,其化学结构为4-O-β-D-吡喃葡萄糖基-3-甲氧基苯丙酮,命名为白花前胡甙。I为首次从白花前胡中分得的线型二氢吡喃香豆素类化合物,这对前胡属植物化学分类学有一定意义。还利用2DNMR纠正了文献中关于化合物I和VII的个别碳信号归属的错误。     

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.     

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.     

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.     

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.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.