HPLC法同时测定复方瘤清合剂中莪术二酮、莪术醇、牻牛儿酮含量

目的 建立一种同时测定复方瘤清合剂中莪术二酮、莪术醇、牻牛儿酮含量的方法。方法 采用C₁₈色谱柱(4.6 mm × 150mm,5μm),以乙腈 – 水( 34 : 66 )为流动相,检测波长为203 nm,进样量10 μm,流速1 ml?min_-1,柱温30℃。结果 莪术二酮在0.1398 – 1.3980 mg?mL_-1浓度范围内进样量与峰面积线性关系良好( r = 0.9998, n = 6 ),平均回收率为99.75%,RSD为0.76%;莪术醇在0.0304 - 0.3040 mg?mL_-1浓度范围线性关系良好( r = 0.9998, n = 6 ),平均回收率为99.52%,RSD为1.04%;牻牛儿酮在0.0968 – 0.9680 mg?mL_-1浓度范围线性关系良好( r = 0.9998, n = 6 ),平均回收率为99.67%,RSD为0.63%。结论 该方法可以同时测定莪术中三种有效成分含量,并且准确、方便、专属性强,可以很好地控制制剂的质量。     

莪术油葡萄糖注射液中莪术醇及牻牛儿酮的含量测定

目的建立测定莪术油葡萄糖注射液中莪术醇及牻牛儿酮含量的高效液相色谱法。方法以十八烷基硅烷键合硅胶为填充剂,流动相为乙腈-0.5%冰醋酸水溶液(65∶35),流速为1mL/min,检测波长为210nm。结果莪术醇及牛儿酮的线性范围分别为25.61～2.561μg/mL和25.42～2.542μg/mL,r分别为0.9997和0.9999(n=6),平均回收率分别为99.43%和99.50%,RSD分别为0.38%和0.40%(n=9)。结论该法简便、准确,能同时测定莪术油葡萄糖注射液中莪术醇及牻牛儿酮的含量,可用于其质量控制。     

UV-Vis法测定莪术酮胶束中莪术酮的含量

目的:建立以紫外-可见分光光度法测定莪术酮胶束中莪术酮含量的方法。方法:以香草醛硫酸溶液显色,在500nm波长处测定吸收度。结果:莪术酮检测浓度在0.050～0.400mg.mL-1范围内与吸收度呈良好线性关系(r=0.9993);平均回收率为99.14%,RSD=1.23%(n=9)。结论:本方法简便、准确,可用于本品的质量控制。     

GC法测定不同品种莪术药材中3种成分的含量

目的建立莪术药材中β-榄香烯、=牛儿酮和莪术二酮的GC含量测定方法 ,并比较不同品种莪术药材中3种成分的含量。方法采用DB-225毛细管柱,FID检测器。结果β-榄香烯、=牛儿酮和莪术二酮的线性范围分别为：1.019-5.095mg.mL-1（r=1.0000）;1.0609-10.609mg.mL-1（r=0.9999）;2.218-4.436mg.mL-1（r=0.9999）。平均回收率分别为：β-榄香烯100.6%,RSD=1.95%（n=9）;=牛儿酮100.6%,RSD=1.85%（n=9）;莪术二酮99.6%,RSD=2.13%（n=9）。结论不同品种莪术药材挥发油中莪术二酮的含量存在显著性的差异。该法准确、可靠,可用于莪术药材的质量控制。     

温莪术和温郁金中牛儿酮的含量测定

目的建立温莪术和温郁金药材中牛儿酮的含量测定方法。方法采用高效液相色谱（HPLC）法，色谱柱为Hypersil CN(4.6 mm×250 mm，5 μm)；乙腈 水（40∶60）为流动相；流速为1.0 mL·min 1，检测波长为210 nm。结果牛儿酮的线性范围为1.9～22.8 μg·mL 1(r＝0.999 9)，平均回收率为96.95 %，RSD为1.12 %。结论该测定方法简便易行，结果准确，可作为温莪术、温郁金药材的质量控制方法。     

温郁金醋制前后5种成分含量变化考察

摘要：目的:比较温郁金醋制前后5种成分含量变化。方法:采用HPLC法对温郁金和醋温郁金中的莪术二酮、吉马酮、莪术醇、β-榄香烯、姜黄素5种成分进行定量分析。结果:莪术二酮、吉马酮、莪术醇、β-榄香烯、姜黄素5种成分能够良好分离,线性范围分别为2.506～20.050μg·ml-1（r=0.999 5）、0.919～7.355μg·ml-1（r=0.999 6）、0.964～7.714μg·ml-1（r=0.999 7）、0.927～7.416μg·ml-1（r=0.999 4）、1.123～8.982μg·ml-1（r=0.999 3）;平均加样回收率分别为99.59%（RSD=0.95%）,98.84%（RSD=0.91%）,99.41%（RSD=1.19%）,98.72%（RSD=0.79%）,98.94%（RSD=1.06%）（n=6）。温郁金经醋制后莪术二酮及吉马酮的含量显著降低（P<0.05）,莪术醇和β-榄香烯的含量则有所增加,而姜黄素含量无明显变化,5-羟甲基糠醛为炮制后新增加的成分。结论:基于HPLC法对温郁金和醋温郁金中5种成分进行定量分析,为进一步对温郁金炮制前后的质量变化和药效物质基础提供参考依据。     

HPLC法测定椒莪合剂中5种成分的含量

摘要：目的:建立HPLC法测定椒莪合剂中莪术二酮、莪术醇、牻牛儿酮、呋喃二烯和α-亚麻酸的含量。方法:采用Diamonsil Plus C18色谱柱（250 mm×4. 6 mm,5μm）,流动相为乙腈-水,梯度洗脱测定椒莪合剂中莪术二酮、莪术醇、牻牛儿酮、呋喃二烯的含量,检测波长为216 nm,流速:1. 0 ml·min-1,柱温:30℃,进样量:10μl。以乙腈-1%醋酸溶液（85∶15）为流动相,检测波长为205 nm,柱温:25℃,进样量:10μl,检测α-亚麻酸的含量。结果:莪术二酮、莪术醇、牻牛儿酮、呋喃二烯、α-亚麻酸在4. 49～71. 84μg·ml-1,5. 60～73. 52μg·ml-1,2. 67～42. 64μg·ml-1,1. 84～21. 44μg·ml-1,20. 00～428. 48μg·ml-1范围内线性关系良好,r≥0. 999 6;平均加样回收率分别为97. 83%,96. 41%,98. 31%,98. 31%,97. 83%,RSD分别为2. 9%,2. 9%,2. 5%,2. 9%,1. 8%（n=6）。结论:该方法操作简单、数据准确、重复性好,能够对椒莪合剂中的5种成分进行含量测定,为提高椒莪合剂的质量标准提供了有效的方法。     

温莪术药材中的牛儿酮含量测定

目的建立温莪术药材的牛儿酮含量测定方法。方法采用HPLC法,色谱柱为HypersilCN(4.6mm×250mm,5μm);乙腈-水(40∶60)为流动相;流速为1.0mL/min,检测波长为210nm。结果牛儿酮的线性范围为1.9～22.8μg/mL(r=0.9999),平均回收率为96.95%,RSD为1.12%。结论该测定方法简便易行,结果准确,可作为温莪术药材的质量控制方法。     

高效液相色谱法测定莪术中吉马酮的含量

目的 :建立以高效液相色谱法测定莪术中吉马酮含量的方法。方法 :色谱柱为C18,流动相为乙腈 -水 (梯度洗脱 ) ,流速为1 .0ml/min ,检测波长为214nm。结果 :吉马酮检测浓度在0. 95～285μg/ml范围内线性关系良好 (r=0 .9999) ,平均回收率为97.89 % (RSD=2.52 % ,n=5)。结论 :本方法简便、可靠 ,可用于莪术药材的含量测定和质量控制。     

黔产莪术和种子中提取挥发油的具体成分异同比较

目的研究黔产莪术和莪术种子中挥发油质控成分的检定方法与含量范围。方法建立高效液相色谱法(HPLC)同时测定黔产莪术与莪术种子中吉马酮和呋喃二烯含量方法:色谱柱为C18(4.6 mm×250 mm,5μm),流动相为乙腈(A)-水(B),梯度洗脱(0~20 min,60%A~95%A;20~35 min,95%A),流速为1 ml/min,检测波长为216 nm,柱温35℃,进样量10μl。结果吉马酮和呋喃二烯的检测浓度分别在4.18~83.6μg/m L(r=0.9999),10.21~204.2μg/ml(r=1.0000)范围呈现良好的线性关系;吉马酮和呋喃二烯的平均回收率(n=6)分别103.2%(RSD=1.44%,102.2%(RSD=1.28%),重复性实验(n=6)RSD分别为0.90%,2.10%。结论黔产莪术与莪术种子中提取的挥发油的质量,可以用挥发油中所含吉马酮和呋喃二烯含量进行控制。控制范围是:黔产莪术挥发油中吉马酮,呋喃二烯含量依次是85.87%~100.10%,59.07%~78.92%;黔产莪术种子挥发油中吉马酮,呋喃二烯含量依次是65.69%~80.47%,59.94%~68.41%。     

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.     

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.     

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.