抗肿瘤剂 LV:Genkwadaphnin 和 Yuanhuacine对P-388淋巴性白血病细胞核酸合成的影响

作者从芫花(Daphne genkwa)花的甲醇提取物分离得两个瑞香烷二萜酯的活性成份,分别为12-苯甲酰氧瑞香毒素(Genkwadaphnin,Ⅰ)和芫花酯甲(Yuanhuacine,Ⅱ)。根据Ⅱ的IR、~1H-NMR和~(13)C-NMR谱,作者认为,Ⅱ与后来报道的odoracin和gnidilatidin为同一化合物。     

三波长分光光度法测定芫花酯甲膜中芫花酯甲的含量

本文研究了应用三波长分光光度法测定芜花酯甲膜中芫花酯甲含量的方法。把三波长组合选择在基质溶液吸收ΔA值为零的组合波长λ_1(260um)、λ_2(232um)、λ_3(225um)处,直接测定了芫花酯甲的含量,回收率为100.3±0.32%。     

芫花的化学成分及药理作用研究进展

目的对芫花的化学成分及其药理作用的研究进展作一综述,提供有关芫花研究的相对较为全面的借鉴资料。方法查阅国内外公开发表的文献28篇,对从芫花中得到的多种化学成分及其药理作用进行论述。结果芫花中主要含有黄酮、香豆素等酚苷类成分及二萜原酸酯类、绿原酸类成分。在镇痛抗炎、抗白血病、抗肿瘤、妊娠中期引产、杀虫等方面有较好疗效。结论为芜花的进一步研究提供了依据。     

芫花酯乙与酯甲对579例中期妊娠引产的临床观察

<正> 芫花酯甲(yuanhuacine,下称甲素)及芫花酯乙(yuanhuadine,下称乙素)都是我国首先从瑞香科植物芫花(Daphnegenkwa Sieb.et Zucc.)根中分离得的新二萜类原酸酯化合物。最近,从芫花的花中又提出了乙素,得率高于根中3倍。甲素及乙素经药理实验证明可引起动物流产。甲素已用于临床作中期妊娠引产,在抗早孕方面已取得初步效果。鉴于乙素的生物活性可能强于甲素,我们对579例中期妊娠孕妇分别用甲素及乙素经羊膜腔注射     

几种有毒中药炮制前后微量元素变化

中药芫花、甘遂、商陆、红大戟攻下逐水,作用猛烈,有毒,须炮制后使用。狼毒破积杀虫,有大毒,内服须炮制。其炮制前后微量元素变化,尚未见到报道,我们对其炮制前后进行14种微量元素测定,现报告如下。1 实验材料:芫花一瑞香科植物芫花Daphne Genkwa Sieb.et zuce的干燥花蕾。醋芜花     

速效牙痛宁酊中芫花酯甲的限量测定

目的研究速效牙痛宁酊中芫花酯甲的限量测定方法。方法采用Agilent HC-C18柱(4.6 mm×250 mm,5μm),以乙腈:0.01%醋酸溶液为流动相,采用梯度洗脱,流速1.0 m L/min,柱温35℃,检测波长238 nm,芫花酯甲在7.50~150.0μg/m L浓度范围内有良好线性关系(r=0.9999),平均加样回收率为98.9%,RSD为1.09%。结果经HPLC测定其芫花酯甲的含量为5.02μg/m L对10批制剂进行检测其含量均<6.0μg/m L。结论本方法灵敏度高、准确、重复性好、专属性强,可用于测定速效牙痛宁酊中芫花酯甲的限量。     

芫花药材质量标准研究

目的:对17批芫花药材样品进行定性定量试验研究,提高芫花药材质量标准。方法:采用薄层色谱法鉴别芫花药材中芫花素成分;以高效液相色谱法测定其含量并制定限度要求,色谱柱为 Kromasil C_(18)(4.6 mm×250 mm,5 μm),流动相为甲醇-水-冰醋酸(65:35:0.5),流速为0.8 mL·min~(-1),柱温为40℃,检测波长为338 nm。结果:芫花药材中芫花素的薄层色谱鉴别特征明显,专属性强;芫花药材中芫花素的含量测定线性范围为0.086～0.432 μg(r=0.9998),平均回收率(n=5)为100.4%(RSD=2.4%),测得芫花药材中芫花素含量不低于0.2%。结论:本方法简单准确地对芫化药材的有效成分芜花素进行定性定量测定,为提高芫花药材的质控方法提供了实验数据,对于保证其质量和临床疗效具有重要的意义。     

基于HPLC法及UPLC-MS法测定芫花饮片炮制前后7种成分的含量变化

目的：建立HPLC法及UPLC-MS法测定芫花中银椴苷、木犀草素、芹菜素、绿原酸、羟基芫花素、芫花素及芫花酯甲7种化学成分含量的方法,分析芫花炮制前后化学成分的变化。方法：采用HPLC法,测定银椴苷、木犀草素、芹菜素、绿原酸、羟基芫花素和芫花素6种成分的含量,色谱柱为AgilentEclipse Plus C18（250 mm×4.6 mm,5 μm）,流动相为乙腈（A）-0.1%甲酸（B）梯度洗脱,流速为1.0 mL·min^-1,进样量10 μL。同时采用UPLC-MS方法测定芫花酯甲的含量,色谱柱为ACQUITYUPLC HSS T3 C18 色谱柱（2.1 mm×100 mm,1.8 μm）,流动相为乙腈（A）-0.1%甲酸（B）梯度洗脱,流速0.3 mL·min^-1,柱温35 ℃,进样量1 μL。结果：7种成分的含量由高到低依次为芫花素＞绿原酸＞银椴苷＞芹菜素＞羟基芫花素＞木犀草素＞芫花酯甲。芫花炮制后7种成分的含量均发生一定程度的变化,其中绿原酸成分在炮制后含量有升高有降低,变化不明显;对于银椴苷和芹菜素成分,炮制后含量降低;对于木犀草素、羟基芫花素和芫花素3个成分,炮制后含量升高;对于芫花酯甲成分,炮制后含量降低。结论：该方法简便、灵敏、高效,为考察芫花饮片炮制前后的质量变化提供了技术支持。     

芫花萜引产药膜的研制及应用

芫花萜(又名芫花酯甲)系从瑞香料植物芫花根中分离出能终止中期妊娠的有效成份。用芫花萜注射液终止3～4个半月妊娠采用宫腔内注药法,操作麻烦、容易感染,成功率低,临床上较少采用。用手术流产方法终止3～4个半月妊娠比较困难,易引起子宫破裂、人流综合症、出血、羊水栓塞等。目前,临床上还没有比较理想的方     

不同产地芫花根皮药材中西瑞香素含量比较

目的采用高效液相色谱（HPLC）法测定不同产地芫花根皮中西瑞香素含量,确定何种产地芫花根皮中西瑞香素含量最高。方法采用Prodigy 5u 100A C18柱（250 mm×4.60 mm,5μm）,流动相为甲醇-0.2%磷酸水溶液（55∶45）,流速为1.0 m L/min,柱温30℃,紫外检测波长346 nm,进样量20μL。结果西瑞香素质量浓度在0.5-20μg/m L范围内与峰面积具有良好的线性关系（r=0.998 4）,平均回收率为98.62%,RSD=4.08%（n=6）。不同产地芫花根皮药材中西瑞香素含量差异较大。结论该法可准确地对芫花根皮药材中有效成分西瑞香素进行定量定性测定,对于保证其内在质量和临床疗效具有重要的意义。     

Comparison of 4 methods of midterm termination and their maternal influence (author's transl)]

This is a clinical study of water bag, rivanol, radix trichosanthis, and yuanhua in regard to their comparative rate of success as abortion techniques for midtrimester pregnancy. The average duration for accomplishing abortion, the condition of expulsion of the fetus, and the complications encountered were discussed. A comparison of the abortifacient effect of 3 yuanhua preparations (elixir of yuanhua flower, elixir of yuanhua root, and yuanhuacine) was made at the same time. The former 2 preparations showed no significant difference, and they had more merits than yuanhuacine. Radix trichosanthis, rivanol, and yuanhua exerted slight effects on the heart, liver, and kidneys in a minority of patients following abortion, but the effects were transient and reversible. Follow-up observation 1/2 year after abortion revealed a variable degree of changes with regard to menstruation, leukorrhea, libido, lumbar and abdominal pain, and psychogenic conditions. All were mild and reversible with no significant effects on subsequent pregnancy, parturition, and infant growth. Finally, the pros and cons of the 4 methods are summarized. The choice of preparations was emphasized. (author's modified)     

应用代谢组学探讨芫花酯甲对人肝细胞L02的毒性作用

目的 采用代谢组学分析芫花酯甲抑制人肝细胞L02增殖的差异代谢物,并揭示其毒性机制。方法 芫花酯甲0, 2.5, 5和10 μmol·L^-1加入L02细胞孵育48 h后,采用超高效液相色谱串联四级杆飞行时间质谱(UPLC-QTOF/MS)分析细胞代谢物;运用偏最小方差判别分析模型区别对照组和芫花酯甲2.5,5和 10 μmol·L^-1作用L02后细胞代谢物的总体差异;计算各组细胞代谢物归一化后的峰面积与细胞毒性强度的相关系数,从而发现并鉴定芫花酯甲损伤L02细胞的差异标志物;采用DAVID数据库分析差异代谢标志物相关基因的信号通路。结果 正常对照组及芫花酯甲2.5,5和 10 μmol·L^-1组间的L02细胞代谢物存在明显差异,共鉴定出5个细胞代谢物峰面积显著下调,与细胞毒性强度的相关系数为-0.53~-0.96;5个代谢物峰面积显著上调,与细胞毒性强度的相关系数为0.72~0.99。代谢物包括磷脂类和脂肪酸类等,主要涉及甘油磷脂代谢、鞘脂代谢、脂肪酸氧化、花生四烯酸代谢和有丝分裂原激活蛋白激酶细胞凋亡等相关信号通路。结论 代谢组学方法能够鉴定芫花酯甲诱导人肝细胞L02损伤的差异标志物及其信号通路。     

New 6(17)-epoxylathyrane diterpene: aellinane from Euphorbia aellenii induces apoptosis via mitochondrial pathway in ovarian cancer cell line

Euphorbia species have been used in traditional medicine in many countries for the treatment of cancer. This article aims to evaluate the capability of a new lathyrane diterpene isolated from Euphorbia aellenii to induce apoptosis in the Caov-4 cell line to determine the underlying mechanism of its anticancer effects. A new 6(17)-epoxylathyrane diterpenes: aellinane from Euphorbia aellenii was evaluated for viability of Caov-4 cells by MTT method. Apoptosis induction by lathyrane diterpene was confirmed by annexin V-FITC/PI staining, and caspase-6 activation. The Bcl2 and Bax protein content were detected by Western blot analysis. Finally, we employed the fluorescent ROS detection kit and fluorochrome JC-1 to determine ROS levels and loss of mitochondria membrane potential (ΔΨm) in Caov-4 cells, respectively. The results show that lathyrane diterpene has significant cytotoxic effect against Caov-4 cells. The IC50 value was 45?μM. Annexin V/propidium iodide (PI) staining and caspase-6 activity assay confirmed that lathyrane diterpene is able to induce apoptosis in Caov-4 cells. The results also demonstrate that lathyrane diterpene up-regulated Bax and down-regulated Bcl-2 proteins. Moreover, apoptotic effect of lathyrane diterpene was also related to ROS production and loss of mitochondrial membrane potential (ΔΨm). This study demonstrated that lathyrane diterpene has profound activity against Caov-4 cells. Analysis of apoptosis-related proteins revealed that lathyrane diterpene triggered the mitochondrion-mediated apoptosis pathway, which led to the loss of mitochondrial membrane potential (ΔΨm) and activation of caspase-6. Therefore, we believe that lathyrane diterpene might be a promising natural compound in ovarian cancer therapy.     

注射用青霉素钠品质参数的近红外漫反射光谱法测定

建立近红外漫反射光谱法测定注射用青霉素钠含量、水分和pH等品质参数的方法。结果表明，校正方程的各项指标均较优，3项指标的平均回收率分别为99．7％、99．8％、99．6％，RSD分别为1．5％、0．9％、1．3％。     

注射用奥美拉唑钠水分含量的近红外漫反射光谱法测定

采用近红外漫反射光谱法对注射用奥美拉唑钠的水分含量进行定量分析.采集62份样品的近红外光谱,采用偏最小二乘法建立数学模型.50个样品经内部交叉验证建立预测模型,内部交叉验证均方差为0.136%;12个样品进行外部验证,外部验证预测均方差为0.074%,预测值与对照值的相关系数为0.9966.平均回收率为99.4%,RSD为3.2%.     

正交函数光谱法测定复方普鲁卡因注射液的含量

目的：测定复方普鲁卡因注射液中普鲁卡因的含量。方法：使用正交函数分光光度法。结果：盐酸普鲁卡因的平均回收率为１００．０４％,ＲＳＤ为０．１５％（ｎ＝６）。结论：样品不经分离直接测定,结果准确,可用于普鲁卡因制剂的快速质量检验。     

Variation in growth and diterpene lactones among field-cultivated <Emphasis Type="Italic">Andrographis paniculata</Emphasis>

Seed-raised Andrographis paniculata (Acanthaceae) from 28 accessions were grown in a randomized complete block design to determine morphological characteristics and diterpene contents. The average amount of dried leaves per individual was between 2.13 and 8.23 g. The average andrographolide content varied from 12.44 to 33.52 mg/g dried leaves and 14-deoxy-11,12-didehydroandrographolide content varied from 0.23 to 2.08 mg/g dried leaves. The differences in phytomass and diterpene contents among the plants from different accessions were statistically significant. Furthermore, we isolated the elite individual plants containing high amounts of andrographolide and 14-deoxy-11,12-didehydroandrographolide (up to 52.57 and 3.46 mg/g dried leaves, respectively). The results indicated those populations are potentially important sources for breeding and improvement of cultivars.     

UV—Vis法测定猕猴桃根提取物多糖的含量

目的建立从猕猴桃根中提取多糖,并测定多糖含量的方法。方法以UV-Vis法为检测手段．应用苯酚．硫酸法测定称猴桃根提取物多糖的含量。结果在10．02-60．12μg·mL-1范围内呈良好的线性关系,回归方程为：A=0．0159C＋0．028（r=0．9997）,猕猴桃根多糖平均回收率为100．41％,RSD为1．10％．样品含量为56．74％,RSD为1．21％。结论本方法可靠、简便、准确,可用于称猴桃根中多糖的含量测定。     

Evaluation of poly(d,l-lactide-co-glycolide) microspheres for the lung-targeting of yuanhuacine,a novel DNA topoisomerase I inhibitor

The present study was intended to develop poly(d,l-lactide-co-glycolide) (PLGA; 50:50, 0.15 dL/g) microspheres (MS) loaded with yuanhuacine (YHC) for passive targeting in lung as well as providing a simple evaluation method for the targeting efficiency of MS. A kind of photochromic spiropyran dye was applied to label MS to clearly demonstrate the in vivo distribution characteristics through intravenous injection into mice and rabbits. Sections of 10-μm thickness from different organs were cut using a microtome, and fluorescent microscopy was used to determine the biodistribution of the MS. The average particle size of MS was 9.0 μm, and the glass transition temperature was 37–40°C. In vitro, the cumulative release achieved 50.8% in 24 h. Histological sections from different organs indicated that the amount of MS in lung achieved maximum in 6 h, as about 8 times as in liver and 70 times higher than the average concentration of other organs. In vivo, MS were gradually swelled and drug concentration remained just 10% in 12 h, which would not result in long time embolization in the lung. This evaluation method supplies a simple and visualized channel in focus for the targeting efficiency of PLGA MS.     

近红外光谱法快速分析注射用盐酸头孢甲肟及其水分的含量

目的建立近红外通用性模型,对注射用盐酸头孢甲肟及其水分进行无损、快速定量分析。方法以不同企业生产的注射用盐酸头孢甲肟为分析对象,用光纤测定近红外漫反射光谱,并通过聚类分析方法确定校正集和预测集,考察不同预处理方法、谱段的影响,选择建立最佳的注射用盐酸头孢甲肟及其水分的定量模型。结果注射用盐酸头孢甲肟定量分析模型由36个校正集样品建立校正模型,17个样品用于外部验证,验证集相关系数为96.33%,校正集均方差为1.19%,验证集均方差为1.66%。注射用盐酸头孢甲肟水分定量分析模型由34个样品校正集样品建立校正模型,19个样品用于外部验证,验证集相关系数为96.39%,校正集均方差为0.22%,验证集均方差为0.26%。结论 2个模型结合可以对注射用盐酸头孢甲肟含量和水分进行快速测定,方法简便,结果准确可靠,适合大量重复性样品的分析测定。