不同采收月份和不同炮制方法对女贞子中红景天苷和酪醇含量的影响

目的探讨不同月份不同炮制方法对长沙地区女贞子中活性成分红景天苷及其苷元酪醇含量的影响。方法采收长沙岳麓山上8、10、12月份产女贞子,去杂质洗净。一部分直接晾干生制;另一部分晾干后用黄酒蒸制。用HPLC法测定不同月份红景天苷及酪醇的含量。色谱柱：Hydro-RP80A,C18（4.6×250mm,5μm）、流动相为甲醇-水（26∶74,V/V）;流速1mL·min-1;检测波长278nm;柱温20℃;进样量10μL。评价月份及炮制方法对女贞子的影响。结果 8、10、12月份生品与制品中红景天苷的含量分别为3.213±2.235mg·g-1、2.784±0.719mg·g-1、0.941±0.510mg·g-1和4.159±2.042mg·g-1、3.596±1.773mg·g-1、2.164±0.986mg·g-1。酪醇的含量分别为0.457±0.323mg·g-1、0.828±0.549mg·g-1、0.414±0.348mg·g-1和0.505±0.298mg·g-1、1.954±1.218mg·g-1、0.702±0.690mg·g-1。结论月份及炮制方法对女贞子活性成分含量有影响,故在实际应用时应根据不同需要适时采收并加以炮制。     

HPLC测定心脑欣滴丸中红景天苷和酪醇含量

目的建立HPLC同时测定心脑欣滴丸中红景天苷和酪醇含量的方法,为科学评价和有效控制心脑欣滴丸提供依据。方法采用WondasiL C18（4.6×250mm,5μm）色谱柱,以甲醇-水为流动相进行梯度洗脱,流速为1mL·min-1,检测波长275nm,柱温25℃。结果红景天苷、酪醇均能达到基线分离,线性范围分别为：25~400μg·mL-1（R2=1）,2.7~43.2μg·mL-1（R2=1）,平均回收率分别是99.82%（RSD=1.8%,n=6）,100.57%（RSD=2.5%,n=6）。结论该方法简单、准确度高、重复性好可用于测定心脑欣滴丸中红景天苷和酪醇的含量,可为该药的质量评价提供参考。     

女贞子饮片质量评价研究

目的研究建立女贞子饮片质量评价标准。方法以红景天苷和酪醇为对照品进行TLC鉴别,同时进行HPLC含量测定,采用Luna C18柱,流动相:乙腈-0.05%磷酸(3∶97),流速:1.0mL·min-1,检测波长:224nm。结果女贞子酒蒸后TLC图谱有显著差别,红景天苷和酪醇的含量显著增加。结论TLC方法简便、专属性强,HPLC方法测定精密度高、重复性好,为女贞子饮片的质量评价方法提供了试验依据。     

辅料对油橄榄叶提取物中橄榄苦苷与羟基酪醇稳定性的影响

目的 考察辅料种类、温度和时间对油橄榄叶中橄榄苦苷和羟基酪醇稳定性和均一性的影响。方法 橄榄苦苷与羟基酪醇的检测采用SinoChrom ODS-BP色谱柱(4.6 mm×250 mm,5 μm),以乙腈-水(25∶75)为流动相,流速1.0 mL·min^-1,检测波长232 nm。结果 以淀粉、羧甲基淀粉钠、微晶纤维素、低取代羟丙纤维素和滑石粉为辅料制得颗粒中的橄榄苦苷与羟基酪醇含量稳定。制颗粒过程中采用70 ℃烘干1 h即可。稠浸膏于4 ℃条件下,密闭遮光放置96?h后,其橄榄苦苷与羟基酪醇含量均一且稳定。结论 上述制剂辅料可用于油橄榄叶提取物的颗粒剂或片剂研究,且含量均一、稳定。     

HPLC法测定复方红景天口含片中红景天苷和酪醇的含量

目的:建立测定复方红景天口含片中红景天苷和酪醇含量的方法。方法:采用高效液相色谱法。色谱柱为AgilentTC-C18(250mm×4.6mm,5μm),流动相为乙腈-水(8.5∶91.5),流速为1.0mL·min-1,检测波长为275nm。结果:红景天苷、酪醇的进样量分别在0.642～5.136μg(r=0.9997)、3.600～36.000μg(r=0.9991)范围内与各自峰面积积分值呈良好的线性关系;平均回收率分别为100.29%、99.46%,RSD分别为1.69%、2.25%(n=9)。结论:本方法简便、快速、重复性好,可用于复方红景天口含片的质量控制。     

高效液相色谱法测定清新胶囊中红景天苷和酪醇的含量

目的:建立用高效液相色谱法测定清新胶囊中红景天苷和酪醇含量的方法。方法:色谱柱:安捷仑ZORBAX Stable Bound(50mm×4．6mm,1．8μm);流动相:甲醇-乙腈-水(6．5:3．5:90),流速0．8 ml·min-1,检测波长275 nm,柱温30℃。结果:红景天苷在0．11～1．59μg,酪醇在0．03～0．39μg范围内呈现良好的线性关系,相关系数分别为r1=0．999 9和r2= 0.999 9。平均回收率为红景天苷101．0％,酪醇99.6％,RSD分别为1．2％,2．0％。结论:谈方法简便,快速,结果准确可靠,可用于该制剂质量控制。     

红景天提取物的特征图谱及主要成分含量研究

摘要：目的:测定红景天提取物中红景天苷和酪醇的含量,并建立HPLC特征图谱,为红景天提取物的质量评价提供依据,并对其原料红景天的基源鉴定提供参考。方法:色谱柱：Thermo Hypersil Gold C18（250 mm×4.6 mm, 5μm）;流动相：乙腈-0.3%冰醋酸溶液,梯度洗脱;流速：1.0 ml·min-1;检测波长：275 nm;柱温：30℃。结果:红景天苷和酪醇分别在8.928～446.400,9.505～475.250μg·ml-1范围内线性关系良好,平均加样回收率分别为101.3%,99.5%,RSD分别为1.26%,1.28%（n=9）。特征图谱研究中,以红景天苷为参照峰共确定6个特征峰,并对其进行了归属。结论:该方法简便高效,稳定可靠,可用于红景天提取物的质量控制及其原料红景天的基源鉴定。     

RP-HPLC法同时测定红景天口服液中红景天苷和酪醇的含量

目的建立反相高效液相色谱法同时测定红景天口服液中红景天苷和酪醇的含量。方法采用Kromasil C18柱(250 mm×4.6 mm,5μm);甲醇-水(体积比为20∶80)为流动相;柱温:30℃;检测波长:275 nm;流速:1.0 mL.min-1。结果红景天苷和酪醇分别在0.048~0.960 g.L-1(r=0.999 9,n=6)和0.013~0.390 g.L-1(r=1.000 0,n=6)内线性关系良好;平均回收率(n=9)分别为95.5%(RSD=1.3%)和95.2%(RSD=1.6%)。结论本方法可用于红景天口服液的质量控制。     

红景天苷及其苷元酪醇的抗炎、抗肿瘤和免疫调节作用

红景天苷及其苷元酪醇是存在于红景天属、越桔属、杜鹃花属、女贞属等植物中的天然抗氧化剂,通过提高细胞的抗氧化能力,清除活性氧,调控炎性细胞因子表达和抑制炎症介质合成,从而产生抗炎作用和防止癌变的发生。红景天苷能上调几种细胞周期蛋白依赖激酶抑制因子表达,减少细胞周期蛋白依赖激酶Cdc2和细胞周期蛋白B1表达,使癌细胞周期滞留在G2期,抑制癌细胞生长。红景天苷对非特异性免疫、体液免疫和细胞免疫均有提高作用,也能对抗免疫抑制剂对骨髓造血功能的抑制。女贞子中的红景天苷和酪醇含量亦很高,因此应加强来源植物女贞子的化学、药理和药效研究。     

RP-HPLC法测定复方酪萨维口腔速崩片中酪萨维和红景天苷的含量

目的:建立测定复方酪萨维口腔速崩片中酪萨维和红景天苷含量的方法。方法:采用反相高效液相色谱法。色谱柱为Agilent TC-C18(250mm×4.6mm,5μm),流动相分别为0.2%磷酸溶液-乙腈=86∶14(酪萨维)、甲醇-水=15∶85(红景天苷),柱温为35℃,流速为1.0mL·min-1,检测波长分别为254nm(酪萨维)、275nm(红景天苷)。结果:酪萨维和红景天苷进样量的线性范围分别为0.08～1.60μg(r=0.9998)、0.80～8.00μg(r=0.9993);平均加样回收率分别为100.22%(RSD=1.58%,n=6)、99.37%(RSD=1.35%,n=6)。结论:本方法操作简便、结果准确、专属性强、重复性好,可用于复方酪萨维口腔速崩片的质量控制。     

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.     

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.     

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.     

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.