Box-Behnken响应面法优化翻白草总黄酮的提取工艺

摘 要 目的：运用Box-Behnken响应面法优化翻白草中总黄酮的提取工艺。方法: 在单因素试验基础上,以提取时间、乙醇浓度以及料液比为考察因素,以翻白草总黄酮提取率为评价指标,利用 Box-Behnken 响应面法优化翻白草中总黄酮的提取工艺。结果: 提取的最佳工艺为：提取浓度为70%的乙醇,每次120 min,液料比为8∶1 ml·g^-1时,黄酮的提取率最高,总黄酮提取率预测值为3.86%,测定值为3.74%,其间相差0.12%。结论:使用Box-Behnken响应面法优化翻白草总黄酮的提取工艺科学可靠,可用于翻白草总黄酮的提取生产。     

Box-Behnken效应面法优化银线草中总黄酮的提取工艺

摘 要 目的： 通过Box Behnken效应面法优化银线草中总黄酮的提取工艺。方法: 以乙醇浓度(X¹)、液料比(X²)和提取时间(X³)为自变量,以银线草中总黄酮的提取量(Y)为因变量,利用Box Behnken效应面法优化银线草中总黄酮的提取工艺。结果: 银线草中总黄酮的最佳提取工艺参数为：乙醇浓度为54.8%,液料比为13.6,提取时间为2.0 h,通过3批验证提取工艺参数,银线草中总黄酮的提取量实测值与回归模型预测值的相对误差为-2.34%。结论:使用Box Behnken效应面法优化银线草中总黄酮的提取工艺,方法简便,精度更高。     

Box-Behnken设计响应面法优选水杨梅总黄酮提取工艺研究

摘 要 目的： 采用Box Behnken设计响应面法优化水杨梅的最佳提取工艺。方法: 以水杨梅中总黄酮含量为评价指标,通过单因素试验分别考察乙醇浓度、液料比、提取时间三个因素对总黄酮含量的影响,采用Box Behnken设计响应面法对水杨梅的提取工艺参数进行优化。结果: 水杨梅的最佳提取工艺：乙醇浓度为 50%,液料比为4.2倍,提取时间为80 min,在该条件下平均提取量12.590 0 mg·g^-1。结论:Box Behnken设计响应面法优化水杨梅总黄酮提取工艺合理,建立的数学模型和试验数据相符,具有较好的预测性。     

响应面设计优化抗癌散总黄酮提取工艺

摘 要 目的： 采用响应面分析法对复方抗癌散总黄酮热回流提取工艺进行优化。方法: 以单因素试验选择了提取时间、乙醇浓度、料液比3个因素为自变量,总黄酮提取率为响应值,通过3因素3水平的响应面分析,确定最佳提取工艺条件。结果: 最佳工艺条件为乙醇浓度64.56%,料液比为1∶26.97,提取时间为2.29 h,提取温度为85℃,总黄酮提取率可达45.94 mg·g^-1。结论: 采用响应面分析法对复方抗癌散总黄酮提取条件优化合理可行,可为其工业生产提供工艺参数依据。     

空心柴胡不同部位中柴胡皂苷a、d和总黄酮的含量比较

摘 要 目的：比较空心柴胡不同部位中柴胡皂苷a、d和总黄酮的含量,为临床合理使用药用部位提供参考。方法: 柴胡皂苷a、d含量测定采用HPLC法：色谱柱Inertsil C18柱（250 mm×4.6 mm,5 μm）;流动相：乙腈-水（40∶60）,流速：1.0 ml·min^-1;检测波长：210 nm,柱温：40 ℃,进样量：10 μl。总黄酮的测定采用比色法：检测波长为500 nm。结果: 柴胡皂苷a、柴胡皂苷d和柴胡总黄酮分别在0.21～1.26 mg·ml^-1(r=0.999 6)、0.25～1.51 mg·ml^-1(r=0.999 7)和4.00～25.00 μg·ml^-1(r=0.999 6)范围内与峰面积呈良好的线性关系;平均回收率分别为99.27%(RSD=2.15%,n=6)、99.4%(RSD=2.14%,n=6)和99.03%(RSD=1.34%,n=6）。空心柴胡根中柴胡皂苷a、d含量分别为0.31%、0.50%,其他部位含量较低;总黄酮在花中含量高达8.48%,在叶、茎、根中依次降低。结论:空心柴胡地上部分富含黄酮类化合物,根中柴胡皂苷含量较高,临床使用带根全草比较合理。     

高效毛细管电泳法测定白术中白术内酯Ⅰ的含量

摘 要 目的： 建立高效毛细管电泳( HPCE) 测定白术中白术内酯Ⅰ（Atractylenolide-1）含量的方法。方法: 运用高效毛细管电泳方法,熔融石英毛细管(75μmID ×50 cm) ,缓冲液为50 mmol·L^-1硼砂缓冲液,检测波长:210 nm ,分离电压:20 kV,柱温25℃,用0.45 μm微孔滤膜过滤后进样,压力进样:50 mbar×5 sec。结果: 方法最低检测浓度为0.5 μg·mL^-1,线性范围2～100 μg·mL^-1,r=0.996,线性关系良好。日内RSD为1.3% ,日间RSD为2.5%,平均回收率分别为97.1%。结论:本法简单、灵敏经济,可作为白术中白术内酯Ⅰ的含量的测定。     

不同炮制方法对麦麸中化学成分的影响

摘 要 目的：分别用高效液相色谱法和紫外可见分光光度法测定湖北麦麸及其炒制品中阿魏酸和总黄酮的含量,探讨不同炮制方法对麦麸中阿魏酸和总黄酮含量的影响。方法: 采用SHIMADZU C18色谱柱（250 mm×4.6 mm,5 μm）,流动相为乙腈 0.1%磷酸水溶液（16∶84）等度洗脱,流速1.0 ml·min^-1,检测波长320 nm,柱温35℃;采用紫外可见分光光度法,在（258±2）nm处对不同炮制品中总黄酮含量进行测定。结果: 麦麸的生品、炒黄品、炒焦品、过焦品、蜜炙品中阿魏酸的含量分别为2.07,2.33,1.68,1.11,0.83 μg·g-1,总黄酮含量分别为5.96,7.15,9.73,13.61,9.42 mg·g-1。结论: 根据麦麸炒制程度的加大,阿魏酸含量呈下降趋势,总黄酮含量呈增加趋势。     

ASE-HPLC法快速测定决明子中大黄酚和橙黄决明素

摘 要 目的：建立快速溶剂萃取（ASE）及HPLC测定决明子中大黄酚和橙黄决明素的分析方法。方法: 利用正交试验对ASE350快速溶剂萃取系统进行提取方法的研究,采用HPLC法同时测定决明子中大黄酚和橙黄决明素的含量。色谱柱为ACE Excel C18 PFP柱(75 mm×2.1 mm,2.5 μm),流动相为乙腈 0.1%磷酸溶液梯度洗脱,流速为0.4 ml·min^-1,检测波长为284 nm,柱温为40℃。结果: 采用甲醇为萃取溶剂、萃取温度为120℃、静态萃取时间为5 min以及循环萃取3次的方法最优,可以很好地提取决明子中大黄酚和橙黄决明素,耗时仅为药典提取方法的1/9。大黄酚和橙黄决明素线性范围为0.73~58.57 μg·ml^-1(r=0.999 7)和1.09~87.29 μg·ml^-1（r=0.999 6),平均回收率分别为102.7%（RSD=0.8%）和98.2%（RSD=1.5%）。 结论:该方法能简便、快速、准确的测定决明子中的大黄酚和橙黄决明素。     

枫蓼肠胃康胶囊中7种黄酮类成分的含量测定及总黄酮提取工艺的优化

摘 要 目的：建立高效液相色谱法同时测定枫蓼肠胃康胶囊中7种黄酮类成分的含量,并对总黄酮提取工艺进行优化。方法: 采用正交试验法优化总黄酮的提取工艺。含量测定色谱条件：色谱柱：Waters RPl8 (250 mm×4.6 mm,5 μm);流动相A：甲醇-水（80∶20）,流动相B：甲醇-0.2%甲酸(17∶83),梯度洗脱;流速：1.0 ml·min^-1;柱温：35℃;可变检测波长(0～27 min,λ1 = 260 nm;27～60 min,λ2 = 360 nm)。结果: 7种黄酮成分在60 min内达到基线分离,线性相关系数均≥0.990 0,平均加标回收率在95.95%～97.84%之间,RSD在0.81%～1.33%之间。总黄酮提取的最佳工艺条件为溶媒倍量1∶15,大孔吸附树脂极性为弱极性（AB-8）,超声提取时间30 min,乙醇体积分数60%。结论:所建立的方法操作简单,精密度高,重复性好,对枫蓼肠胃康胶囊的质量控制和检测都有一定指导意义。     

粉防己碱醇质体含量及包封率测定

摘 要 目的: 建立粉防己碱醇质体中药物含量及包封率的测定方法。方法: 采用低温超速离心法分离游离药物和醇质体,采用HPLC法检测醇质体中游离药物含量和总药量,并计算包封率。结果:粉防己碱在2 ～ 100 μg·ml^-1范围内线性关系良好（ r=0. 999 7）;平均回收率为100.2%（RSD=1.00%, n=9）。用此方法测定3批粉防己碱醇质体的主药含量和包封率,结果分别在97.2%～101.5％及78.4%～81.3%之间。结论:该方法操作简便,结果准确,适合于粉防己碱醇质体的含量和包封率测定。     

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.     

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.

     

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.     

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.