Effect of Santolina oblongifolia on ACII-immunized animals

The therapeutic effect of organic extracts of Santolina oblongifolia in adjuvant-carrageenan-induced inflammation (ACII) in Wistar rats was investigated. The present study concerns the effect of the extracts on serum copper (Cu) and zinc (Zn) levels, and on hindpaw swelling and ankle joint widths of arthritic animals. Compared with controls, the arthritic animals showed an increase in serum Cu levels, while serum Zn was decreased. The altered levels of trace elements in arthritic animals were significantly normalized in the chronic phase of the disease after treatment with most of the extracts of S. oblongifolia. Additionally, administration of the extracts significantly decreased the clinical signs of inflammation. The results of the present investigation indicated that these extracts could offer a partial protective action against changes induced by ACII in Wistar rats.     

Lipoxygenase inhibitory constituents fromIndigofera oblongifolia

Indigin, alkylated xanthene (1) and indigoferic acid (2) have been isolated from the chloroform soluble fraction of Indigofera oblongifolia, along with beta-sitosterol (3) and 3-hydroxybenzoic acid (4), which are reported for the first time from this species. Their structures were determined through spectroscopic techniques. Both the new compounds 1 and 2 showed significant activity against enzyme lipoxygenase, while 2 further showed moderate inhibition against BChE.     

丁基苯酞对原代培养的大鼠皮层神经细胞外液6-keto-PGF1α和TXB2及其比值的影响

目的旨在观察丁基苯酞(NBP)对神经细胞培养液中6-酮-PGF_1α和TXB₂含量及其比值的影响。用放射免疫方法,结果发现神经细胞在低糖低氧5h或低糖低氧5h/恢复糖氧3h条件下,d-,l-和dl-NBP(0.1～100μmol·L^-1)能够剂量依赖性升高细胞外液中的6-酮-PGF_1α含量,降低TXB₂水平,从而使6-酮-PGF_1α与TXB₂比值升高。而阿司匹林仅在小剂量(0.1,1μmol·L^-1)时能升高6-酮 PGF^1α与TXB^{2比值,大剂量(10,100μmol·L-1)时无影响。提示:NBP对6-酮-PGF_1α/TXB₂比值的升高可能与其增加局部脑血流和改善缺血性脑损伤有关。}     

Effects of antidepressants and antipsychotics on the 5HT2 receptor-mediated signal transducing system in human platelets

The IC₅₀ values of the antidepressants amoxapine, mianserin, desipramine, clomipramine and imipramine, and the antipsychotics spiroperidol, chlorpromazine, levomepromazine and haloperidol for³H-ketanserin binding, 5HT-induced intracellular Ca²⁺ increase, 5HT-induced shape change and³H-paroxetine binding in human plateletes were measured and the correlations of each parameter were examined. Results were as follows. Both the antidepressants and the antipsychotics had inhibitory effects on³H-ketanserin binding, 5HT-induced intracellular Ca²⁺ increase and 5HT-induced shape change and there were significant positive correlations between the IC₅₀ values of these three parameters. On the other hand, there were no significant correlations between the IC₅₀ values in³H-paroxetine binding and those in the other three parameters. These results suggest that³H-ketanserin binding, 5HT-induced intracellular Ca²⁺ increase and 5HT-induced shape change are useful and reliable tools for the assessment of the effects of the antidepressants and the antipsychotics on the 5HT₂ receptor-mediated signal transducing system in human platelets.     

半枝莲黄酮类化学成分分析

目的 分析半枝莲黄酮类化学成分。方法 采用硅胶、Sephadex LH-20等多种色谱方法,依据波谱数据对其结构进行分析和鉴定。结果 半枝莲中共分离了12个化合物,分别为圣草酚、野黄芩素、三裂鼠尾草素、黄芩苷、芹菜素、汉黄芩素、4''-羟基汉黄芩素、木犀草素、4'',5-二羟基-3'',5'',6,7-四甲氧基黄酮、柚皮素、7-羟基-5,8,2''-三甲氧基黄烷酮、大波斯菊苷。结论 分离得到的化合物类型均为黄酮苷元和苷类化合物,可为半枝莲的黄酮成分分析提供一定的科学依据。     

Effects of brazilin on the phospholipase A2 activity and changes of intracellular free calcium concentration in rat platelets

Brazilin {7,11 b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10(6H)-tetrol} inhibited thrombin-, collagen-and ADP-induced aggregation of washed rat platelets. Thrombin- and collagen-induced ATP release were also inhibited by brazilin in a concentration-dependent manner. Brazilin inhibited the formation of platelet thromboxane A₂ caused by thrombin, whereas it had no effect on the prostaglandin D₂ formation. Brazilin inhibited [³H]-arachidonic acid liberation from membrane phospholipids of thrombin-stimulated platelets. Brazilin inhibited the rise of intracellular free calcium caused by thrombin. These results indicate that the inhibition of phospholipase (PLA₂) activity and [Ca²⁺]_i elevation might be at least a part of antiplatelet mechanism of brazilin.     

亚硝胺化合物对人源肝癌细胞HepG2的DNA损伤风险评价

目的 使用人肝癌HepG2细胞筛选亚硝胺的体外彗星试验的S9 mix配方，并对17种常见的亚硝胺化合物开展彗星试验，研究其DNA亲和力和碱基嵌入风险。方法 在非S9活化和S9活化条件下对HepG2细胞进行N-二甲基亚硝胺（NDMA）、N-二乙基亚硝胺（NDEA）、N-亚硝基二丁胺（NDBA）、N-亚硝基二异丙胺（NDIPA）、N-亚硝基-N-甲基-4-氨基丁酸（NMBA）、N-亚硝基甲乙胺（NMEA）、N-亚硝基-N-乙基异丙胺（NEIPA）、N-亚硝基二丙胺（NDPA）、N-甲基-N-亚硝基苯胺（NMPA）、亚硝基二苯胺（NDPh）、二乙醇亚硝胺（NDELA）、亚硝基吗啉（NMOR）、亚硝基-N-甲基-N-（2-苯基）乙胺（NMPEA）、亚硝基吡咯烷（NPYR）、亚硝基哌啶（NPIP）、4-甲基亚硝胺基-1-3-吡啶基-1-丁酮（NNK）、N-亚硝基降烟碱（NNN）给药处理，2种条件均设置溶媒对照（0.5% DMSO）、3个浓度梯度的给药组和阳性对照组，在非S9活化条件下以甲基磺酸甲酯（MMS）为阳性对照，S9活化条件下以环磷酰胺（CP）为阳性对照。以NDMA和NDEA为例比较3种S9 mix配方对亚硝胺化合物体外DNA亲和力和DNA损伤风险，选择效果最优者开展剩余化合物在S9条件下的彗星试验，计算各组尾DNA含量百分率（% tail DNA）的平均值和中位数。结果 在非S9代谢活化条件下17种常见亚硝胺化合物均未导致HepG2细胞核DNA明显损伤。S9 mix配方C中S9体积分数仅为3.36%，但对亚硝胺化合物的代谢活化效果最佳。在该条件下，除NDPh外，其余亚硝胺化合物均对HepG2细胞存在DNA的损伤作用。烷基类亚硝胺化合物对DNA损伤作用强弱顺序依次为NDMA>NEIPA>NDPA>NMEA>NDEA>NDBA>NDIPA，与化合物α氢的数目基本呈正相关。含苯基的亚硝胺化合物对DNA损伤作用强弱顺序依次为NMPEA>NMPA>NDPh，而环状亚硝胺化合物对DNA损伤作用强弱顺序为NMOR>NPIP≈NPYR。结论 提供最新的亚硝胺化合物体外DNA损伤风险数据，并提出适宜亚硝胺化合物的体外彗星试验S9 mix配方，为亚硝胺化合物的毒性评价提供手段。     

MN-9202对兔血小板聚集、5-HT释放、TXB_2合成及Ca~(2 )转运的影响(英文)

目的:研究新二氢吡啶类钙拮抗剂MN-9202对兔血小板激活的影响,并探讨其作用机制。方法:以Fu-ra-2 AM为荧光探针,采用时间扫描方式记录血小板内Ca~(2 )的变化;分别用HPLC/ECD和放射免疫测定法检测5-HT及TXB_2。结果:MN-9202剂量依赖地抑制ADP或凝血酶诱导的血小板聚集,抑制TXA_2的释放并且能有效阻滞激活血小板胞内Ca~(2 )水平的增加。MN-9202 1μmol·L~(-1)能抑制胶原15mg·L~(-1)诱导的5-HT释放反应,但对胶原45mg·L~(-1)诱导的反应无抑制作用。结论:MN-9202阻滞血小板Ca~(2 )内流并抑制血小板花生四烯酸代谢及激活反应。     

Polyphenolic compounds isolated from the leaves of Myrtus communis

Four hydrolyzable tannins [oenothein B (1), eugeniflorin D₂ (2), and tellimagrandins I (3) and II (4)], two related polyphenolic compounds [gallic acid (5) and quinic acid 3,5-di-O-gallate (6)], and four myricetin glycosides [myricetins 3-O-β-d-xyloside (7), 3-O-β-d-galactoside (8), 3-O-β-d-galactoside 6″-O-gallate (9), and 3-O-α-l-rhamnoside (10)] were isolated from the leaves of Myrtus communis. Antioxidant activities of the isolated compounds were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay.     

The activity of compounds extracted from feverfew on histamine release from rat mast cells

An extract of the plant feverfew (Tanacetum parthenium) produces a dose-dependent inhibition of histamine release from rat peritoneal mast cells stimulated with anti-IgE or the calcium ionophore A23187. Greater inhibition of anti-IgE-induced histamine release was achieved with feverfew compared with the inhibition of A23187-induced release. Inhibition of anti-IgE-induced histamine release by feverfew extract was observed when the drug was added simultaneously with anti-IgE and the inhibitory activity increased only slightly when the drug was preincubated with the cells for 5 min before anti-IgE stimulation. In this respect feverfew differs from cromoglycate and quercetin. Feverfew extract inhibited anti-IgE-induced histamine release to the same extent in the absence and presence of extracellular glucose. It is concluded that feverfew extract contains a novel type of mast cell inhibitor.     

Immunomodulatory activity of protein-bound polysaccharide extracted from chelidonium majus

In the course of searching immunomodulators from natural sources, the protein-bound polysaccharide, CM-Ala, has been isolated from the water extract of Chelidonium majus L. (Papaveraceae). The immunostimulatory characteristics have been investigated in several experiments such as generation of activated killer (AK) cells, proliferation of splenocytes, activation of macrophages and granulocyte macrophage-colony forming cell (GM-CFC) assay. Of the fractions obtained using Sephacryl S200 column chromatography, CM-Ala was the most effective fraction that augmented the cytotoxicity against Yac-1 tumor cells from 0.88% to 34.18% by culturing with splenocytes for 5 days. CM-Ala also enhanced nitric oxide production by two fold in peritoneal macrophages and exhibited antitumor activity. It showed mitogenic activity on both spleen cells and bone marrow cells. CM-Ala induced proliferation of splenocytes by 84 fold and increased GM-CFC numbers by 1.48 fold over than the non-treated. On the contrary, CM-Ala had cytotoxic activity to a diverse group of tumor cells. From the above results, we proposed that CM-Ala has a possibility of an effective antitumor immunostimulator.     

The effect of polysaccharide extracted from the marine alga Capsosiphon fulvescens on ethanol administration

Seaweed extracts have recently been found to have antioxidant and antitumor activities. Capsosiphon fulvescens (Cf) is a green alga and nutrient-dense food source. In a previous study, we extracted polysaccharide from Cf (Cf-PS) and demonstrated its antitumor effect in gastric cancer cells. In this report, we describe the protective effect of Cf-PS against alcohol-induced gastric injury in rats and adenocarcinoma (AGS) cells. In vivo assay revealed stomach damage in rats treated with alcohol alone; however, the stomach condition of rats co-treated with Cf-PS and alcohol matched that of the control group. Cf-PS also inhibited alcohol-induced cell death in AGS cells. Compared with alcohol treatment alone, Cf-PS and alcohol co-treatment increased phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2) and Akt but inhibited poly-ADP-ribose polymerase (PARP) cleavage. Thus, ERK1/2 and Akt activation are instrumental in the protective effect of Cf-PS against alcohol-induced cell death in AGS cells. Moreover, Cf-PS treatment reduced the expressions of cyclooxygenase-2 (COX-2) and the inducible form of nitric oxide (iNOS), proteins related to ulcers. These results suggest that Cf-PS could help protect against alcohol-induced peptic ulcers.     

The suppressant effect of GEA3162 on spontaneous serotonin release from human colonic mucosa in vitro

The effect of a lipophilic nitric oxide (NO)-releasing compound 5-amino-3-(3,4-dichlorophenyl) 1,2,3,4-oxatriazolium (GEA3162) on the spontaneous release of 5-hydroxytryptamine (5-HT) from human colonic mucosa was investigated in vitro. In the presence of tetrodotoxin, spontaneous outflow of 5-HT from the human colonic mucosa was measured by high-performance liquid chromatography with electrochemical detection. GEA3162 concentration-dependently suppressed the 5-HT outflow, but neither the NO-activated soluble guanylate cyclase inhibitor 1H-[1,2,4]-oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) nor peroxynitrite scavenger ebselen affected the suppressant effect of GEA3162. Moreover, neither the L-type calcium channel blocker nicardipine, NO synthase inhibitor l-N(G)-nitroarginine methyl ester nor guanylate cyclase activator guanylin affected the spontaneous 5-HT outflow. These results indicate that human colonic mucosa is capable of eliciting tetrodotoxin-resistant and nicardipine-insensitive 5-HT release, and that GEA3162 can suppress the 5-HT release via an action on colonic mucosa through mechanism independent of ODQ-sensitive cyclic GMP system or peroxynitrite generation.     

Effects of d-amphetamine on human aggressive behavior

Male research subjects were administered placebo and three doses of d-amphetamine (5, 10 and 20 mg/70 kg) in a laboratory situation which provided both aggressive and non-aggressive response options. The non-aggressive response was button pressing maintained by presentation of points exchangeable for money at the end of the session. The aggressive response was button pressing on a separate manipulanda which ostensibly subtracted points from a fictitious partner. Aggressive responding was elicited by subtracting points from the research subjects which was attributed to the fictitious partner. d-Amphetamine increased both aggressive and non-aggressive responding, particularly at 5 and 10 mg/70 kg. At the highest dose (20 mg/70 kg), aggressive responding decreased to levels similar to those observed during placebo sessions, while monetary reinforced responding remained elevated.     

抗胆碱药α-环戊基苯甲氧基烃胺类化合物的合成

本文报道了一系列α-环戊基苯甲氧基烃胺类抗胆碱化合物的合成。所用的原料。α-环戊基苯甲醇系由澳代环戊烷和苯甲腈进行格氏反应,得到的环戊基苯基酮,再以四氢铝锂还原成相应的醇。此法制备的较文献方法的产率高,且为纯品。以α-环戊基苯甲醇和氯代烃胺在氢化钠存在下缩合或以。α-环戊基-α-氯代苯甲烷与氮杂环烷醇缩合制得目的物。药理筛选结果显示,所合成的化合物都有不同程度的抗胆碱作用。     

Flavonoids from the whole plants ofOrostachys japonicus

From the whole plants ofOrostachys japonicus, kaempferol, quercetin, astragalin, quercitrin, isoquercitrin, cynaroside, afzelin, 3-O-α-L-rhamnosyl-7-O-β-D-glucosyl kaempferol, and 3,7-di-O-β-D-glucosyl kaempferol were isolated and characterized by spectral data.     

Anti-platelet effects of flavonoids and flavonoid-glycosides from Sophora japonica

A methanol extract of Sophora japonica was subjected to anti-platelet activity guided fractionation affording the isolation of four flavonoids and six flavonoid-glycosides: biochanin A (1), irisolidone (2), genistein (3), sissotrin (4), sophorabioside (5), genistin (6), tectoridin (7), apigenin (8), quercitrin (9), and rutin (10). The structure of each compound was determined by a variety of spectroscopic methods. Among the compounds, 1, 3, and 7 showed approximately 2.5-6.5 fold greater inhibitory effects on arachidonic acid (AA) and U46619 induced platelet aggregation (IC50: 19.9 and 99.8 microM; 20.3 and 53.8 microM; 25.9 and 123.4 microM, respectively) than acetylsalicylic acid (ASA, IC50: 63.0 and 350.0 microM). Compound 2 was an approximately 22-40 fold stronger inhibitor than ASA on AA and U46619 induced aggregation (IC50: 1.6 and 15.6 microM, respectively).     

艾叶制炭对人主动脉内皮细胞TFPI、vWF、NO和活化血小板JNK1表达的影响

目的 研究艾叶制炭前后对人主动脉内皮细胞组织因子途径抑制物（TFPI）、内皮细胞血管性假血友病因子（vWF）、NO含量的影响,以及对大鼠血小板氨基末端激酶-1（JNK1）表达水平的影响,阐明艾叶炭止血机制。方法 将体外培养的人主动脉内皮细胞（HEAC）随机分组,分别给予不同极性（石油醚、二氯甲烷、醋酸乙酯、正丁醇、水、水提物、鞣质、总黄酮）部位的艾叶生、炭品,终质量浓度为200、100、50 μg/mL,培养48 h后,取细胞培养液试剂盒法测定TFPI、vWF、NO含量;采用免疫蛋白印迹方法检测艾叶制炭前后各部位对大鼠血小板JNK1磷酸化水平的影响。结果 与对照组及相应生品组比较,艾叶炭品二氯甲烷和鞣质部位TFPI、NO含量显著降低,vWF含量显著升高（P<0.01）;大鼠血小板JNK1磷酸化水平显著升高（P<0.01）。与对照组比较,艾叶鞣质部位TFPI、NO含量显著降低,vWF含量显著升高（P<0.01）;大鼠血小板JNK1磷酸化水平显著升高（P<0.01）。结论 二氯甲烷和鞣质部位是艾叶炭的主要止血作用部位,其止血机制为降低TFPI、NO含量、增加vWF的含量;明显提高血小板JNK1的磷酸化水平。