血府逐瘀软胶囊中药材的鉴别及芍药苷的含量测定

目的建立血府逐瘀软胶囊的鉴别和含量测定方法。方法采用TLC法和HPLC法。结果TLC鉴别了样品中的赤芍、枳壳、牛膝、甘草等药材;HPLC测定了芍药苷的含量,芍药苷在0.1~0.9 mg范围内,线性关系良好(r=0.9999)。平均回收率为96.4%,RSD=1.4%。结论鉴别方法重复性好,专属性强;含量测定方法简便、准确。     

利胆片中药材的鉴别及大黄的含量测定

目的:提高利胆片的质量标准.方法:采用薄层色谱(TLC)法鉴别金银花、黄芩、知母及白芍,用高效液相色谱(HPLC)法测定方中大黄的含量.结果:TLC鉴别斑点明显.含量测定大黄素0.01064～0.3192 μg、大黄酚0.02586～0.7758 μg,进样量与峰面积线性关系良好.平均加样回收率大黄素为99.80%,RSD=0.78%(n=6);大黄酚为99.72%,RSD=1.18%(n=6).结论:建立的TLC鉴别和HPLC含量测定方法专属性强、重复性好,可用于利胆片的质量控制.     

酸枣仁合剂的薄层鉴别及酸枣仁皂苷A的含量测定

目的:建立酸枣仁合剂的鉴别和含量测定方法.方法:采用TLC法和HPLC法.结果:TLC法鉴别酸枣仁合剂中知母、茯苓和川芎等药材;HPLC测定酸枣仁皂苷A的含量,酸枣仁皂苷A在0.55～1.1 mg/mL范围内线形关系良好(r=0.9997),平均加样回收率为100.45%,RSD为1.30%.结论:鉴别重复性好、专属性强,含量测定方法简便,准确.     

三金分散片的鉴别及含量测定

目的 建立三金分散片鉴别和含量测定的方法.方法 采用TLC法及HPLC法.结果 TLC鉴别金樱根和积雪草药材,色谱清晰,分离度好.HPLC测定羟基积雪草苷,线性范围为1.206～12.064 μg(r=0.9991);平均回收率为99.69%(RSD=1.49%).结论 鉴别重复性好,专属性强;含量测定方法灵敏、准确.     

前列通瘀颗粒多指标成分薄层鉴别及含量测定研究

摘要：目的:基于多指标成分TLC鉴别及HPLC法含量测定全面控制前列通瘀颗粒质量。方法:对方中虎杖、黄芪、续断、赤芍进行TLC鉴别;同时对赤芍、虎杖、续断中的主要活性成分芍药苷、虎杖苷、川续断皂苷Ⅵ的含量进行测定。结果:TLC鉴别方法斑点清晰,专属性强;HPLC测定结果表明芍药苷、虎杖苷、川续断皂苷Ⅵ的线性范围分别为11.30～112.70μg·ml-1（r=0.999 8）、8.60～86.20μg·ml-1（r=0.999 7）、34.70～346.90μg·ml-1（r=0.999 7）;平均加样回收率分别为101.23%（RSD=0.86%）,100.43%（RSD=0.85%）,98.46%（RSD=0.59%）（n=6）。结论:研究结果表明多指标成分TLC鉴别及HPLC含量测定方法专属性好,准确度高,可作为前列通瘀颗粒的质量控制标准。     

参草宁心颗粒的薄层鉴别及含量测定研究

目的:建立参草宁心颗粒的薄层鉴别与含量测定方法。方法:鉴别采用薄层色谱(thin layer chromatography,TLC)法,含量测定采用高效液相色谱(high performance liquid chromatchromatography,HPLC)法。结果:实验建立了方中5味药丹参、苦参、炙甘草、地锦草和仙鹤草的薄层鉴别,所建立的方法均分离良好、斑点清晰、阴性无干扰;建立的含量测定方法同时评价了方中丹参、炙甘草、地锦草3味药中的活性成分丹酚酸B、甘草苷、没食子酸,3种成分分别在0.107~1.070,0.119~1.19,0.15~1.5μg范围内呈现良好的线性,回归方程分别为y=793 255x+133 630,y=489 205x+113 434,y=177 863x+69 444,相关系数r分别为0.999 6,0.999 1,0.999 4。精密度、稳定性、重复性实验的RSD值均<3%,加样回收率分别为99.47%,100.44%,100.04%,RSD分别为2.61%,2.34%,2.45%。结论:实验建立的TLC鉴别方法和HPLC含量测定方法均专属性强、重现性好,可用于参草宁心颗粒的质量控制。     

川黄颗粒的薄层鉴别及丹参素钠的含量测定

目的 建立川黄颗粒鉴别和含量测定的方法.方法 采用TLC法和HPLC法.结果 TLC鉴别川黄颗粒中的何首乌、黄芪、党参、枸杞子等药材;HPLC测定丹参素钠的含量,丹参素钠在0.26～1.84 mg的范围内,线性关系良好(r=0.9996).平均回收率为99.8%,RSD=1.4%.结论 鉴别重复性好、专属性强,含量测定方法简便、准确.     

金刚藤泡腾片的薄层鉴别及薯蓣皂苷元的含量测定

目的建立金刚藤泡腾片的质量标准。方法采用TLC法鉴别金刚藤泡腾片中的菝葜;HPLC法测定薯蓣皂苷元的含量。结果薯蓣皂苷元在1~32μg范围内,线性关系良好(r=0.9999),平均回收率为97.7%,RSD=2.0%。结论薄层鉴别重复性好,专属性强;含量测定方法专属、简便、准确。     

炙甘草合剂质量标准研究

目的 建立炙甘草合剂质量标准。方法 采用薄层色谱法(TLC)法对处方中的桂枝和甘草进行定性鉴别;采用高效液相色谱(HPLC)法对制剂中甘草酸进行含量测定;采用pH值测定法对制剂pH值进行检测。结果 桂枝、甘草的薄层鉴别斑点清晰,分离度好,专属性强;甘草酸进样量在0.20444～1.27775μg范围内与峰面积呈良好线性关系(r=1.0000,n=5);平均回收率为100.6%,RSD=1.47%(n=6)。结论 本文建立的TLC鉴别、含量测定方法和pH值范围,可用于炙甘草合剂的质量控制。     

小儿健脾口服液的质量标准

目的建立小儿健脾口服液的质量标准。方法采用TLC法鉴别白术、山楂,以HPLC测定橙皮苷的含量。结果TLC法可明显鉴别白术、山楂,橙皮苷在0.288～1.440μg内线性关系良好(r=0.9995),平均回收率为98.6%(RSD=1.03%,n=5)。结论方法简便、准确、稳定、重复性好,可用于该制剂的质量控制。     

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.     

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.