光照条件对红花黄色素稳定性的影响

目的考察红花黄色素的光稳定性,为红花黄色素的提取纯化工艺提供参考依据。方法采用HPLC法,以羟基红花黄色素A的保留率为指标,考察红花黄色素在不同浓度乙醇及水中的光稳定性。结果光照条件下,羟基红花黄色素A的保留率水〉10%乙醇〉30%乙醇〉50%乙醇〉70%乙醇;影响羟基红花黄色素A稳定性因素大小顺序为：日光〉紫外〉白炽灯光〉避光。结论红花黄色素光不稳定,主要受光中紫外光影响;水中稳定性大于乙醇。     

注射用红花黄色素的质量控制及安全性研究

目的：探讨注射用红花黄色素的质量控制方法,建立其质量标准,并对安全性进行研究。方法：采用Wonda Sil C18高效液相色谱柱进行精密度、稳定性、重复性试验,建立指纹图谱。对红花黄色素的外观、pH、不溶性微粒、羟基红花黄色素A含量以及无菌情况及细菌内毒素进行检查。结果：方法学考察表明,检测方法精密度、稳定性、重复性均为良好;指纹图谱各色谱峰能有效分离;外观、pH检查稳定,不溶性微粒符合要求;羟基红花黄色素A的平均含量(n=6)为每瓶67.61 mg;无菌检查均显示无细菌生长,每1 mg红花黄色素中内毒素<0.12 EU,安全性好。结论：建立的方法操作简便、重复性好,质量控制准确可靠,可用于对注射用红花黄色素的质量控制和安全性评价。     

红花黄色素中主要成分的含量测定

目的 对药食两用天然色素红花黄色素进行质量控制。方法 采用紫外分光光度法和高效液相色谱法,以总黄色素和羟基红花黄色素A为指标,对红花黄色素中主要化学成分进行含量测定。结果 自制红花黄色素与市售红花黄色素(色价E=150)的总黄色素含量均＞99%,自制红花黄色素的羟基红花黄色素A含量最高,达20.21%,为市售红花黄色素的2~3倍。结论 市售红花黄色素的总黄色素含量随色价的增大而显著提高,不同的红花黄色素样品中羟基红花黄色素A的含量也存在较大差异,本研究为红花黄色素的质量分析控制奠定了基础。     

红花黄色素的药理学研究进展

红花为菊科植物红花的干燥管状花,一直备受人们关注。《本草纲目》称红花能"活血润燥,止痛散肿,通经"。红花含有多种化学成分,主要有色素、挥发油、脂肪酸、酚酸、黄酮类化合物等。从红花中分离得到的黄酮类化合物红花黄色素(SY)为主要有效成分。红花黄色素主要含有羟基红花黄色素A(HSYA)、红花黄色素B(SYB)、红花黄色素C(SYC)、山柰酚、山柰酚-3-葡萄糖苷、山柰酚-3-芸香糖苷、槲皮素、槲皮素-3-葡萄糖苷、红花     

红花药材黄色素类成分的HPLC指纹图谱研究

目的:建立红花药材黄色素类成分的高效液相色谱(HPLC)指纹图谱。方法:采用反相(RP)-HPLC法。色谱柱为Phenomenex C18(250mm×4.6mm,5μm),流动相为0.01%三氟乙酸水溶液-乙腈(梯度洗脱),流速为1.0mL·min-1,检测波长为403nm。结果:建立了红花药材黄色素类成分的HPLC指纹图谱,标定了8个共有指纹特征峰,方法学考察符合指纹图谱技术要求。结论:本方法稳定、可靠、精密度高、重复性好,可为红花药材质量标准的制定提供科学依据。     

红花中红花黄色素提取工艺优化的研究

目的:运用微波提取法优选从红花中提取红花黄色素的最佳工艺。方法:采用单因素实验法和正交设计法,考察固-液比、微波功率和微波提取时间等因素对红花黄色素提取转移率的影响,以及运用微波提取法优选红花黄色素提取的工艺,并与传统的温浸提取法作比较;用紫外分光光度计测定其含量。结果:用微波辅助提取红花黄色素的最佳工艺条件:浸泡30min,加20倍水,微波功率为600W,提取1min,提取两次。结论:该法与传统温浸法相比,用微波水提取红花黄色素缩短了提取时间,降低了提取成本,并具有较好的提取转移率,有推广价值。     

红花中羟基红花黄色素A的提取动力学研究

目的：确定羟基红花黄色素 A 的最佳提取工艺,并确立能够表征羟基红花黄色素 A 提取过程的动力学方程。方法以高效液相法测定不同温度、不同时间提取液中羟基红花黄色素 A 的含量,以 Fick 第一扩散定律为基础,建立浸提动力学方程,计算提取的速率常数、活化能等函数值。结果最佳提取工艺为加适量水,在90℃温浸提取60 min,拟合的动力学方程为lnk ＝－3263．3（1／T）＋6．5244,该模型能较好地描述红花中羟基红花黄色素 A 提取的动态过程,活化能为27．13 kJ·mol －1。结论红花中羟基红花黄色素 A 提取过程的动力学符合一级动力学方程特征。     

红花黄色素酶法提取工艺的正交试验研究

目的研究纤维素酶提取红花黄色素的工艺条件.方法以羟基红花黄色素A为指标,采用正交试验法和单因素试验法考察纤维素酶浓度、提取时间、提取温度、pH等因素对红花黄色素提取量的影响.结果最佳提取工艺为:溶媒pH为5.0、提取温度为60℃、纤维素酶浓度为0.15 mg爛mL-1,提取次数为2次,提取时间为60 min.结论此法稳定,可用于红花黄色素的提取.     

羟基红花黄色素A对体外培养人脐静脉内皮细胞增殖的抑制作用

红花具活血通经，散瘀止痛的功效，其主要水溶性组分为红花黄色素，红花黄色素的主要成分是羟基红花黄色素A。临床上红花多用于治疗冠心病、脑血栓、高血脂、肿瘤等。近年来人们对红花黄色素和羟基红花黄色素A的研究多集中在抗心肌缺血，抗血栓等心血管药理活性上，对它们在抗肿瘤方面的研究国内外鲜见报道。笔者通过建立非极性大孔树脂柱层析法，从红花中提取分离了羟基红花黄色素A，并观察到其能显著抑制鸡胚尿囊膜上新生血管的生成。     

红花黄色素治疗不稳定型心绞痛的临床观察

目的 观察注射用红花黄色素治疗不稳定型心绞痛的临床效果。方法 80例患者随机分为红花黄色素治疗组和对照组。对照组常规给予硝酸脂类、钙通道阻滞剂、β受体阻滞剂及阿司匹林治疗。治疗组在此基础上加用注射用红花黄色素100 mg加入0.9%氯化钠注射液250 mL中静滴,每日1次,14 d为一疗程。观察治疗前、后临床症状,每日心绞痛发作次数,持续时间,疼痛程度,心率、血压变化情况、硝酸甘油片的消耗量。结果 两组治疗后血脂情况都有所改善,但红花黄色素治疗组效果要优于对照组(P<0.01)。红花黄色素治疗组和对照组患者临床有效率分别为97.00%和86.00%,差异有统计学意义(P<0.05)。结论 红花黄色素治疗冠心痛心绞痛疗效确切。     

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.     

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.     

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.     

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.