丹参药材HPLC指纹图谱研究

目的：采用高效液相色谱法,建立丹参药材指纹图谱分析方法。方法：采用phenomenex Luna（4.6mm×250mm）色谱柱,0.5%冰醋酸水甲醇为流动相,梯度洗脱。结果：建立丹参药材HPLC指纹图谱,标定8个共有指纹峰。结论：该方法准确、可靠,为有效地评价丹参药材提供了重要依据。     

HPLC法同时测定复方丹参输卵管灌注液中丹参素和原儿茶醛的含量

目的:采用HPLC法同时测定复方丹参输卵管灌注液中丹参素和原儿茶醛的含量.方法:采用Inertsil C18(250 mm×4.6 mm,5μm)色谱柱;以甲醇-1%冰醋酸为流动相梯度洗脱;流速为1.0 ml·min-1;检测波长280 nm.结果:丹参素和原儿茶醛分别在9.8~78.2μg·ml-1(r=0.999 9)、2.0~19.9 μg·ml-1范围内线性关系良好(r=0.9996);加样回收率分别为98.59%和100.20%,RSD分别为0.25%和0.78%.结论:该方法简单可行、灵敏准确,可用于复方丹参输卵管灌注液的质量控制.     

高效液相色谱法测定复方丹参提取液中丹参素含量

目的采用高效液相色谱法测定复方丹参提取液中丹参素的含量。方法色谱柱:Agilent C18(250 mm×4.6 mm,5μm);流动相:甲醇-1%冰醋酸梯度洗脱;流速:1 mL.min-1;柱温为室温;检测波长:280 nm。结果线性方程为Y=11 981X 11.492(r=0.999 9),线性范围:20.8-145.6μg.mL-1,丹参素的平均含量为58.28μg.mL-1,RSD为0.77%,回收率100.03%,RSD为0.82%。结论该法操作简便,精确度高,可靠性强,可作为丹参和复方丹参制剂质量控制的标准。     

反相高效液相色谱法同时测定通脉口服液中丹参素和原儿茶醛的含量

目的建立同时测定通脉口服液中丹参素和原儿茶醛含量的方法。方法采用RP-HPLC对制剂中主要成分丹参素和原儿茶醛进行定量分析,色谱柱Suntek Krom asil C18(250 mm×4.6 mm,5μm),甲醇-0.5%冰醋酸溶液(16∶84)为流动相,检测波长281 nm。结果RP-HPLC结果稳定,精密度、重现性良好,丹参素和原儿茶醛分别在0.315 2~1.260 8μg和0.043 0~0.172 2μg范围内有较好的线性关系,加样回收率分别为101.81%和100.47%,RSD为2.13%和2.79%。结论可有效控制制剂质量。     

RP-HPLC法测定丹参不同部位中丹参素和原儿茶醛的含量

目的 采用RP-HPLC法测定丹参不同部位中丹参素和原儿茶醛的含量.方法 色谱柱为Kromasil C18柱(150 mm×4.6 mm,5 μm),流动相为甲醇-乙腈-1%冰醋酸(7:3:90),流速1.0 ml·min-1,检测波长280 nm,柱温为室温.结果 丹参素和原儿茶醛的线性范围分别为2.333～30.0...     

丹参药材中活性成分的测定及其聚类分析

目的 建立测定不同产地丹参药材中主要活性成分的方法,根据含量水平对丹参药材进行聚类分析.方法 采用HPLC指纹图谱法,分析柱为C18柱(150 mm×4.6 mm,10μm),用甲醇-1%四氢呋喃的1%甲酸水溶液进行梯度洗脱;测定波长286 nm,进行丹参活性成分的指纹图谱分析,以指纹图谱评价软件结合SPSS 13.0统计软件进行聚类分析.结果 定量分析了丹参药材的8个主要活性成分,所分析的丹参大致划分为两类.结论 所建方法分离度好、准确度高,适宜于丹参药材活性成分的测定;不同产地丹参药材之间活性成分的差异较大,其分布无明显的规律性;丹参药材在地理上的分布无明显的区域界限.     

高效液相色谱法同时测定复方丹参提取液中丹参素、原儿茶醛的含量

目的:建立高效液相色谱法(HPLC)同时测定复方丹参提取液中丹参素、原儿茶醛的含量。方法:Agilent C18柱(250 mm×4.6 mm,5μm),1%醋酸溶液-甲醇采用梯度洗脱,检测波长280 nm,流速1 mL·min-1。结果:复方丹参提取液中的杂质对丹参素、原儿茶醛的测定无干扰,各组分在各自的线性范围内均呈良好的线性关系(r>0.999),平均加样回收率、精密度、重现性和稳定性均符合有关规定。结论:本方法操作简便,结果准确,可以作为控制复方丹参内在质量的方法。     

高效液相色法谱测定舒冠胶囊中丹参素钠含量

目的：建立测定舒冠胶囊中丹参含量的测定方法。方法：采用HPLC测定丹参中丹参素钠的含量,色谱柱C18柱（4.6mm×250mm）,检测波长280nm,流速1.0mg·min-1,流动相为甲醇-水-冰醋酸-二甲基甲酰胺（5：90：5：2）。结果：丹参素钠在0.48μg～8.15μg浓度范围内与峰面积积分值呈良好线性关系,平均回收率99.91%,RSD为0.38%（n=5）。结论：该方法简便快速、重现性好,结果准确可靠、操作方便,可用于舒冠胶囊的质量控制。     

HPLC同时测定乐脉颗粒中的丹酚酸B和丹参素钠

目的建立同时测定乐脉颗粒中丹酚酸B和丹参素钠含量的方法。方法采用HPLC法,色谱柱为Shim-pack C18柱(150 mm×4.6 mm,5μm),流动相A为甲醇,B为5%冰醋酸溶液,梯度洗脱。流速1.0 ml.min-1;检测波长286 nm;柱温35℃。结果丹酚酸B和丹参素钠分别在0.1933~2.8995、0.0807~1.2105μg线性关系良好,r均为0.9999,丹酚酸B和丹参素钠的平均回收率分别为98.54%、98.36%,RSD分别为0.69%、0.57%(n=6)。结论所建方法操作简便、结果准确,重复性好,可用于该制剂的质量控制。     

HPLC法测定养血注射液中丹参素钠的含量

目的建立HPLC法测定养血注射液中丹参素钠含量的方法。方法采用Diamonsil C18色谱柱(200mm×4.6mm,5μm),以甲醇-0.5%冰醋酸=12∶88的水溶液系统为流动相,流速1m L·min-1,进样量20μL,柱温32℃,检测波长280nm。结果丹参素钠在10~200μg·m L-1线性关系良好(r=0.9997),平均加样回收率为99.68%,(RSD=3.0%)。结论本法简单易行,精确,可用于丹参素钠的质量控制。     

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.     

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.     

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.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

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.