高效液相色谱-电化学检测法研究大蒜素对百草枯中毒小鼠脑组织中单胺类神经递质含量的影响

建立了单胺类神经递质的高效液相色谱-电化学检测方法,探讨了大蒜素对百草枯中毒小鼠脑组织内的单胺类神经递质及其代谢产物的影响。健康ICR小鼠随机分为4组:正常对照(Con)组、大蒜素(DAS)组、百草枯染毒(PQ)组和大蒜素治疗(PQ+DAS)组,每组6只。PQ组灌胃PQ 35 mg/kg建立中毒模型,Con组和DAS组灌服同体积生理盐水。DAS组和PQ+DAS组小鼠于造模2、26、50 h后腹腔内各注射1次DAS(25 mg/kg),PQ组和正常组小鼠腹腔内注射等量无菌生理盐水。造模12 h后处死小鼠。收集小鼠脑组织样品并称重,处理后进样。色谱分析采用Acclaim 120 C18(150 mm×2.1 mm,3μm)色谱柱,以离子对缓冲盐溶液-甲醇(93∶7,体积比)为流动相,流速为0.27 m L/min;电化学检测器检测,工作电压为450 m V。结果表明,与正常组和DAS组比较,PQ组部分神经递质水平降低;DAS治疗后能够改变上述生化指标的变化;与PQ组相比,PQ+DAS组神经递质含量增高,差异均具有统计学意义(P0.05)。脑组织样品中5-HT、DA、5-HIAA、DOPAC和HVA低、中、高3水平的加标回收率均为79.8%~112.1%,相对标准偏差(RSD)小于10%。实验表明,大蒜素对百草枯中毒后小鼠体内含量降低的神经递质有明显的上调作用。     

利用活体成像技术研究海茸β-1,3/1,6-葡聚糖在小鼠体内的分布

以海茸β-1,3/1,6-葡聚糖(DAG)为研究对象,首先经还原胺化反应在DAG还原端引入功能氨基,再将其与N-羟基丁二酰亚胺(NHS)活化的荧光染料(Cy7)偶联,获得Cy7标记的DAG分子;利用小动物活体成像技术研究了DAG在小鼠体内的分布.结果表明,DAG在小鼠体内主要分布于肺、肝和肾,具有靶向小鼠肺部和通过肾排泄的特点.该方法简便、数据可靠,为多糖和寡糖的体内分布与代谢研究提供了参考.     

药对青蒿-桂枝中挥发油成分的GC-MS分析与化学计量学解析

采用水蒸气蒸馏法从青蒿、桂枝及其药对中提取挥发油成分,利用气相色谱-质谱(GC-MS)联用技术进行分离检测,通过化学计量学解析法(CRM)对重叠色谱峰解析,并结合程序升温保留指数辅助定性.从药对及其单味药青蒿、桂枝中分别鉴定出69、66、68种挥发油;组成药对后,单味药成分减少,新成分增加,药对与单味药挥发油共存17种组分,它们是cis-细辛醚、丁子香烯、丁子香烯环氧化物等成分,占药对挥发油总含量的35.82%;而药对中挥发油的主要成分是(E)-桂皮醛(18.32%)和cis-细辛醚(10.20%)等,其含量并非单味药含量的简单相加,相关作用机理有待进一步研究.     

Effect of Sodium Fluoride on the Rate of Sperm Deformity in Male Mice

为探讨氟化钠对雄性小鼠精子畸形的影响,选取50只成年雄性小鼠随机分为5组:氟化钠染毒高剂量组(34 mg/kg)、中剂量组(17 mg/kg)、低剂量组(8.5 mg/kg)、环磷酰胺阳性对照组( 50 mg/kg)、生理盐水空白对照组,采用经口灌胃染毒,1次/d,连续5d,于首次染毒后的第35天颈椎脱臼将小鼠处死,取睾丸和附睾称质量,计算脏器系数；同时取附睾制片,观察精子形态,计数小鼠精子畸形率.结果表明,氟化钠染毒各组睾丸、附睾脏器系数与空白对照组比较,差别无统计学意义(P＞0.05),染毒各组精子畸形率普遍高于空白对照组,差别有统计学意义(P＜0.001),且随着染毒剂量的增加精子畸形率也有相应升高,呈现一定的剂量-反应关系(r=0.954,F=20.098,P＜0.05,R2=0.909).提示氟化钠能使雄性小鼠精子畸形率明显升高,具有一定的生殖毒性,能影响小鼠生殖功能,对小鼠生殖功能造成损害.     

基于1H NMR代谢组学方法分析马兜铃酸I诱导的雌雄小鼠急性肾毒性

基于¹H NMR的代谢组学方法, 分析了C57BL/6J小鼠尿样的代谢特征, 揭示出马兜铃酸I(AAI)导致急性肾毒性的分子机理及其在雌性和雄性小鼠上差异的根源. 研究结果表明, AAI的急性肾毒性主要来自AAI给药后抑制了体内的三羧酸(TCA)循环和能量代谢, 破坏了体内肠道菌群的生态平衡, 改变了肾脏细胞内外的渗透压, 从而引起了肾小管的损伤. 代谢模式分析显示雄性小鼠对AAI的肾毒性比雌性小鼠更敏感, 可能源于雄性小鼠本身更低的能量代谢. 结果表明, 基于尿样¹H NMR代谢组学方法有可能为药物的毒性机制和毒性性别差异研究提供新思路.     

HMCM-22分子筛催化1,3-苯并二噁茂烷类化合物合成的研究

研究了HMCM-22分子筛催化邻苯二酚与环己酮、丁酮、丙酮、丙醛、丁醛、异丁醛、戊醛、异戊醛、正己醛、正辛醛、苯甲醛、二苯甲酮等十余种醛(酮)的缩合反应.考察了反应时间、酚与醛(酮)的配比、HMCM-22分子筛用量等因素对酚与醛(酮)反应的影响.结果表明,当酚与醛(酮)摩尔比为1∶1.4,催化剂用量为3.5 g/1mol醛(酮),反应5 h,选择性一般在97%以上,转化率也一般在70%以上,表明HMCM-22分子筛对邻苯二酚与醛(酮)的反应有较好的催化性能.     

117mSn-TTHMP的制备及生物性质研究

合成了具有亲骨性的氨基膦酸配体-TTHMP(三乙基四胺六甲撑膦酸),制备了117mSn(Ⅳ)-TTHMP,对配合物的稳定性、亲脂性作了研究,考察了它在大白兔体内显像及小鼠体内的分布。将其生物性质与已有文献报道的117mSn(Ⅳ)-HEDTMP作了比较。结果表明117mSn(Ⅳ)-TTHMP的制备简单,稳定性好,亲水,117mSn(Ⅳ)-TTHMP的靶向摄取率高于前两者,是一种极具潜力的新型放射性药物。     

磷酸基团在环丙沙星光敏损伤DNA中的作用

利用紫外-可见稳态吸收光谱, 稳态荧光发射光谱和激光光解瞬态光谱实验方法研究了磷酸基团在环丙沙星(CPX)光敏损伤DNA中的作用. 紫外-可见和稳态荧光光谱实验证实了磷酸根离子影响环丙沙星的稳态吸收和发射谱, 实验结果表明磷酸根是通过弱相互作用与环丙沙星结合. 我们还利用激光闪光光解实验分别研究了鸟苷(Gua), 脱氧鸟苷(dG)以及脱氧鸟苷酸(dGMP)对环丙沙星三线态(³CPX^*)的影响, 通过对比实验证实了在环丙沙星光敏损伤dGMP中, 由于磷酸基团的存在, 导致了环丙沙星三线态吸收峰的改变, 从而改变了光敏损伤反应的途径. 通过研究发现, 光敏损伤途径的改变是由于dGMP结构上磷酸基团通过氢键与环丙沙星结合所造成的. 最后, 根据实验结果并对比Gua, dG和dGMP的结构, 提出了一个合理的磷酸基团的作用机理.     

亚慢性钐染毒对雄性小鼠精子质量的影响

为探讨稀土元素钐对雄性小鼠精子的毒性作用, 让5组小鼠自由饮用含硝酸钐0, 5, 50, 500, 2000 mg·L-1的溶液3个月后, 观察钐对小鼠精子活力、数量、畸形率及顶体完整率的影响. 结果表明: 各处理组精子活力、数量都有所降低, 其中2000 mg·L-1剂量组与对照组相比, 各指标值均有极显著差异(P《0.01); 50, 500, 2000 mg·L-1剂量组的精子畸形率与对照组相比也具有极显著差异(P《0.01), 且染毒剂量与精子总畸形率呈现出直线变化的剂量对数-效应关系. 因此精子畸形率可作为稀土元素钐作用于雄性生殖系统的标志指标; 各处理组的顶体完整率也均低于对照组. 说明亚慢性钐暴露对小鼠精子具有一定的毒性作用.     

葡萄糖转运蛋白显像剂6-18FDG的制备及在小鼠体内的分布

为了研究正电子核素18F标记的葡萄糖转运蛋白显像剂6-18氟-6-脱氧葡萄糖的制备及在小鼠体内的生物学分布, 以D-葡萄糖为起始原料, 经过丙酮和苯甲醛对1,2,3,5位羟基的定位保护, 然后用对甲苯磺酰氯和6位的羟基反应得到能被18F-进攻的离去基团, 最后用18F-离子通过亲核取代反应实现对葡萄糖6位的氟代标记; 反应中间体用NMR和MS表征, 最终产物用标准品6-19FDG在HPLC下对照确认, 测定放化纯度, 观察其在小鼠体内的生物学分布. 6-18氟-6-脱氧葡萄糖的放射性标记过程需35 min(从加速器轰击结束算起), 放化产率70%±5%(校正后, n=5), 放化纯度>95%. 小鼠体内的生物学分布表明, 各个器官在1.0 min达到峰值, 然后逐渐平衡. 初步研究结果表明, 6-18FDG是一种很有价值的葡萄糖转运蛋白显像剂, 为以后的体内外研究及活体显像奠定了基础.     

Determination of enrofloxacin and its metabolite ciprofloxacin in goat milk by high-performance liquid chromatography with diode-array detection. Optimization and validation

A high-performance liquid chromatography-diode array detection method (HPLC-DAD) combined with liquid chromatography-mass spectrometry was developed for the determination of enrofloxacin and its metabolite ciprofloxacin in goat milk. The HPLC-DAD method validation was compliant with the "DG SANCO 1805/2000" European regulation. The residues were extracted from milk with phosphate buffer, purified on a C18 Speedisk cartridge SPE (Baker) and then analysed using HPLC-DAD set at 277 nm. The decision limit (CCa) calculated by spiking samples at 100 microg/kg with both analytes, taking into account the maximum residue limit (MRL) of 100 microg/kg established by the European Union for the sum of enrofloxacin and its metabolite ciprofloxacin in milk, was 105.3 microg/kg for enrofloxacin and 105.5 microg/kg for ciprofloxacin. The detection capability (CCbeta) was 110.7 and 110.9 microg/kg for enrofloxacin and ciprofloxacin, respectively. The mean recoveries of the method, calculated by spiking samples at 50, 100 and 150 microg/kg were 84% for enrofloxacin and 88% for ciprofloxacin. The limit of quantification was 20 microg/kg for both analytes. The HPLC-DAD validated method was successfully applied for the first time in goats milk, and proved to be suitable for the sensitive and accurate quantification and confirmation analysis of enrofloxacin and ciprofloxacin for regulatory purposes.     

Toxicity and anticancer effects of an extract from Selaginella tamariscina on a mice model

The toxicity and antitumour effect of the ethanol extract of Selaginella tamariscina (STE), a plant widely used in folk medicine, were examined in a mice model. In the single-dose acute toxicity test, an oral administration of 10,000?mg?kg(-1) STE did not cause any lethality. The sub-acute toxicity study showed that the treatment by 250,?1000 and 3000?mg?kg(-1?)day(-1) for 30 continuous days did neither alter the body weights nor the haematological parameters in BALB/c mice. The anticancer effect of STE was evaluated in BALB/c mice inoculated with Lewis lung carcinoma cells. Oral administration of STE could not prevent the tumour formation but provided strong inhibition of tumour growth.     

Antinociceptive activity and acute toxicity study of Flaveria trinervia whole plant extracts using mice

The antinociceptive activity of Flaveria trinervia extracts by tail-flicking and writhing methods was evaluated using mice. The abdominal writhing method was carried out by administering petroleum ether, chloroform and methanol extracts orally. After 1?h of incubation, 0.6% acetic acid (10?mL?kg(-1)) was administered intraperitoneally. After 5?min, each group of mice was observed for the amount of writhing for a duration of 20?min. Acetyl salicylic acid was used as the standard reference. The tail-flick method was carried out using a thermal model and the maximum possible analgesia was calculated. The LD?? values of petroleum ether, chloroform and methanol extracts were 700, 700 and 500?mg?kg?1, respectively. The methanol extract at 50?mg?kg?1 showed significant antinociceptive activity. The petroleum ether and chloroform extracts showed moderate antinociceptive activity at a dose of 70?mg?kg?1. The methanol extract showed more significant antinociceptive activity than the other extracts but was less effective than the standard. This investigation finds support for the ethnomedicinal claims of F. trinervia.     

Evaluation of the immunity activity of glycyrrhizin in AR mice

In this study, we evaluated effect of glycyrrhizin on immunity function in allergic rhinitis (AR) mice. The AR mice model were induced by dripping ovalbumin in physiological saline (2 mg mL?1, 10 μL) into the bilateral nasal cavities using a micropipette. After the AR model was induced, mice were randomly divided into six groups: the normal control, model, lycopene 20 mg kg?1 (as positive control drug) group, and glycyrrhizin 10, 20, 30 mg kg?1 groups. After the sensitization day 14, lycopene (20 mg/kg BW) and glycyrrhizin (10, 20 and 30 mg/kg BW) were given orally for 20 days once a day. Mice in the normal control and model groups were given saline orally once a day for 20 days. Results showed that glycyrrhizin treatment could dose-dependently significantly reduce blood immunoglobulin E (IgE), interleukin-4 (IL-4), interleukin-5 (IL-5), interleukin-6 (IL-6), nitrous oxide (NO), tumor necrosis factor-alpha (TNF-α) levels and nitrous oxide synthase (NOS) activity and enhance blood immunoglobulin A (IgA), immunoglobulin G (IgG), immunoglobulin M (IgM), interleukin-2 (IL-2) and interleukin-12 (IL-12) levels in AR mice. Furthermore, glycyrrhizin treatment could dose-dependently significantly enhance acetylcholinesterase (AchE) activity and reduce substance P (SP) level in peripheral blood and nasal mucosa of AR mice. We conclude that glycyrrhizin can improve immunity function in AR mice, suggesting a potential drug for the prevention and therapy of AR.     

Involvement of central noradrenaline, serotonin and dopamine system in the antidepressant activity of fruits of Solanum torvum (Solanaceae)

The methanolic extract (ME) of Solanum torvum seeds and its ethyl acetate fraction (EAF) were investigated for their antidepressant activity using behavioral (forced swim test, FST and tail suspension test, TST) and biochemical (monoamine oxidase, MAO reduced activity) tests. ME (10, 30 and 100?mg?kg(-1)) and EAF (10 and 30?mg?kg(-1)) dose dependently inhibited the immobility period, increased noradrenaline, serotonin and dopamine levels and inhibited the MAO enzymes in FST and TST using mice. Furthermore, we have observed antagonism between the threshold dose of ME (30 and 100?mg?kg(-1)) and EAF (10 and 30?mg?kg(-1)) with antagonists on behaviour mediated by neurotransmitters noradrenaline, serotonin and dopamine. MAO-A inhibition was more prominent as compared to MAO-B inhibition. The study provides evidence for antidepressant actions of S. torvum.     

Ethanolic extract of Rubia peregrina L. (Rubiaceae) inhibits haloperidol-induced catalepsy and reserpine-induced orofacial dyskinesia

In the traditional Sardinian system of medicine, Rubia peregrina L. (Rubiaceae) is reported as an aphrodisiac herb. Since the aphrodisiacs may also have antioxidant and dopaminergic activities, the aim of this study was to study the effect of ethanolic extract of aerial parts of R. peregrina for the scavenging of free DPPH radicals and the inhibition of haloperidol-induced catalepsy in mice and reserpine-induced orofacial dyskinesia in rats. The extract exhibited significant antioxidant activity in a free radical DPPH assay with IC(50)?=?55.6?μg?mL(-1), which was very close to IC(50) of ascorbic acid. The extract of R. peregrina (100 and 200?mg?kg(-1) intraperitoneally, i.p.) significantly inhibited haloperidol (1?mg?kg(-1) i.p.) - induced catalepsy in mice (p?相似文献   

Determination of residues of enrofloxacin and its metabolite ciprofloxacin in chicken muscle by capillary electrophoresis using laser-induced fluorescence detection

A method for the residue analysis of the veterinary antimicrobial agent enrofloxacin and its active desethyl metabolite ciprofloxacin in chicken muscle tissue has been developed and validated. The detection of the analytes was performed by laser-induced fluorescence (LIF) detection using a HeCd laser (lambda(ex) = 325 nm) providing an enhancement in sensitivity and selectivity compared to conventional UV detection. The assay has been validated with satisfying results. The limits of quantification for enrofloxacin and ciprofloxacin were 5 microg/kg and 20 microg/kg, respectively, with a fivefold preconcentration yielded by a sample clean-up with a simple liquid-liquid extraction procedure. Calibration graphs were linear from 5 to 1000 microg/kg for enrofloxacin and from 20 to 1000 microg/kg for ciprofloxacin. The assay allows the detection of contaminated muscle samples at the required maximum residue limit of the European Union, which is 100 microg/kg for the sum of enrofloxacin and ciprofloxacin.     

Phytochemical investigation characterisation and anticonvulsant activity of Ricinus communis seeds in mice

The ethanol extract of the dried, powdered hull portion of Ricinus communis seeds indicated the presence of alkaloids, steroids, flavonoids, glycosides and phenolics, amongst others. Ricinine was isolated as an active constituent and characterised by various chemical and spectroscopic techniques. The anticonvulsant activity of the isolated compound was evaluated in mice using the maximal electroshock (MES) model. The isolated compound at a dose of 60?mg?kg?1 body weight, orally, significantly (p?相似文献   

Determination of Fluoroquinolones in Animal Feed by Ion Pair High-performance Liquid Chromatography with Fluorescence Detection

A sensitive and simple method is described for the determination of fluoroquinolones by high-performance liquid chromatography (HPLC) using a C18 column and fluorescence detection. The mobile phase was acetonitrile and 0.025M phosphate acid with 0.0025M sodium 1-heptanesulfonate monohydrate in water with a gradient program. The chromatographic conditions were optimized for the determination of ciprofloxacin, enrofloxacin, sarafloxacin, and flumequine in animal feed. The samples were extracted by a hydrochloric acid and acetonitrile followed by dilution in 0.01M oxalic acid at pH 4.0 and purified by solid-phase extraction. The procedure was validated by fortifying feed at 200, 1000, and 2000?µg/kg. The limits of detection and quantification were from 28.5 to 74.7 and 31.7 to 94.6?µg/kg, respectively. The average recoveries for fluoroquinolones were from 89.7 to 100.3%. The method was validated and shown to be efficient and precise for quantification of fluoroquinolones in animal feed. The results demonstrate the feasibility of the method for routine use to monitor these substances in feed.     

Trichosanthes dioica root possesses stimulant laxative activity in mice

Trichosanthes dioica Roxb. (Cucurbitaceae), named 'pointed gourd' in English, is a dioecious climber grown in India. This study was aimed at evaluating the laxative activity of the aqueous extract of T. dioica root (TDA) in Swiss albino mice. The laxative activity of TDA (100 and 200?mg?kg(-1) body weight per os) was evaluated by assessing the excretory bowel activities in naive (non-constipated) and in drug (loperamide)-induced constipation in mice. Further, the gastrointestinal transit was measured in both naive and in constipated mice. Castor oil (0.5?mL/mouse per os) was used as the reference. TDA significantly and dose-dependently increased all the excretory bowel activities and gastrointestinal transit in both naive and constipated mice. TDA at 200?mg?kg(-1) body weight was found to be the most active, causing diarrhoea in mice. Thus, T. dioica root demonstrated stimulant laxative activity in Swiss mice, validating its traditional usage in India.