复方花刺参制剂抗凝血机制的实验研究

本研究旨在探讨复方花刺参制剂（Ｓｔｉｃｈｏｐｕｓ ｖａｒｉｅｇａｔｕｓ Ｃｏｍｐｏｕｄ ＳＴ复合剂）对大鼠血浆ＴＸＢ２、６－ｋｅｔｏ－ＰＧＦ１ａ、ＰＧＥ２、Ｆｇ及其对大鼠血小板聚集的影响。实验采用酶联免疫吸附法（ＥＬＩＳＡ法）测定各组大鼠血浆中ＴＸＢ２、６－Ｋｅ－ＰＧＦ１ａ、ＰＧＥ２的水平;另外,采用免疫比浊法测定两组大鼠血浆中纤维蛋白原（Ｆｇ）的含量,并同时观察各组大鼠３ｍｉｎ,１０ｍｉｎ内的血     

Inhibitory effects of copper-aspirin complex on platelet aggregation

目的：研究阿司匹林铜（ＣｕＡｓｐ）对血小板聚集性的影响及其机制．方法：用Ｂｏｒｎ氏法测定ＣｕＡｓｐ对兔血小板聚集性的影响．用荧光光度法和放射免疫法观察ＣｕＡｓｐ对兔血小板５羟色胺的释放和ＴＸＢ２的产生及血浆中ＴＸＢ２和６ｋｅｔｏＰＧＦ１α水平的影响．结果：ＣｕＡｓｐ体外呈浓度依赖性抑制花生四烯酸（ＡＡ）诱导的血小板聚集和５羟色胺的释放（ＩＣ５０分别为１７和１９μｍｏｌ·Ｌ－１，９５％可信限为９－３３和１０－３０μｍｏｌ·Ｌ－１），且抑制ＴＸＢ２的产生（Ｐ＜００５）．ＣｕＡｓｐ１０ｍｇ·ｋｇ－１灌胃选择性抑制ＡＡ诱导聚集．降低血浆ＴＸＢ２，同时升高６ｋｅｔｏＰＧＦ１α的水平（Ｐ＜００５）．结论：ＣｕＡｓｐ体内外均有比Ａｓｐ更强的抗血小板聚集作用．     

慢性支气管炎肺泡巨噬细胞释放6-酮-前列腺素F_(1α)和血栓素B_2的研究

１０例慢性支气管炎缓解期患者和１０例正常人的肺泡巨噬细胞（ＡＭ），加用ＬＰＳ体外培养。结果显示随着培养基中ＬＰＳ剂量增加，两组ＡＭ合成分泌的６－酮－前列腺素Ｆ１α（６－ｋｅｔｏ－ＰＧＦ１α）和血栓素Ｂ２（ＴＸＢ２）含量均逐渐增加。两组间存在显著差异性。表明慢性支气管炎缓解期患者ＡＭ更易活化释放这些炎性介质。对慢性支气管炎发生发展有重要影响     

阿斯匹林对冠心病患者血小板释放反应的影响

目的： 研究小剂量阿斯匹林（ＡＳＡ） 对冠心病患者血小板释放反应的影响及其机制。方法： 采用放免法（ＲＩＡ） 对４０ 例稳定期冠心病志愿者口服单剂４０ ｍｇ （２０ 例） 与３００ ｍｇ （２０ 例） ＡＳＡ 前后血浆β ＴＧ． ６ 酮 ＰＧＦ１α及ＴＸＢ２ 进行定量分析。结果： （１） 口服单剂４０ ｍｇ ＡＳＡ ２４ ｈ 血浆β ＴＧ 显著减少（ Ｐ＜ ０－０５） , 血浆ＴＸＢ２１２ ｈ 与２４ ｈ 均非常显著下降（ Ｐ＜ ０－０１） , 而血浆６ 酮 ＰＧＦ１α几乎不变（ Ｐ＞ ０－０５） ; （２） 口服单剂３００ ｍｇ ＡＳＡ 除了６ 酮 ＰＧＦ１α显著降低（ Ｐ＜ ０－０５） 外, 血浆β ＴＧ 及ＴＸＢ２ 变化态势同４０ ｍｇ 组。结论： 口服单剂４０ ｍｇ 与３００ ｍｇＡＳＡ 均能显著阻抑血小板释放反应, 此作用似与ＡＳＡ 降低机体ＴＸＡ２ 水平有关;３００ ｍｇＡＳＡ 可使体内ＰＧＩ２ 含量减少, 无法改善冠心病者ＰＧＩ２／ＴＸＡ２ 平衡。     

阿司匹林铜的抗血小板聚集作用

目的：研究阿司匹林铜（ＣｕＡｓｐ）对血小板聚集性的影响及其机制，方法；用Ｂｏｒｎ氏法测定ＣｕＡｓｐ对兔血小板聚集性的影响，用荧光光度法和放射免疫法观察ＣｕＡｓｐ对兔血小板５－羟色胺的释放和ＴＸＢ２的产生及血浆中ＴＸＢ２和６－ｋｅｔｏ－ＰＧＦ１α水平的影响，结果：ＣｕＡｓｐ体外呈浓度依赖性抑制花生四烯酸（ＡＡ）诱导的血小板聚集和５－羟色胺的释放（ＩＣ５０分别为１７和１９μｍｏｌ．Ｌ＾－１，９５％可信     

阿斯匹林对冠心病患者血小板释放反应的影响

目的 研究小剂量阿斯匹林（ＡＳＡ）对冠心病患者血小板释放反应的影响及其机制。方法采用放免法（ＲＩＡ）对４０例稳定期冠心病志愿者口服单剂４０ｍｇ（２０例）与３００ｍｇ（２０例）ＡＳＡ前后血浆β－ＴＧ,６－酮－ＰＧＦ１α及ＴＸＢ２进行定量分析。结果：（１）口服单剂４０ｍｇＡＳＡ ２４ｈ血浆β－ＴＧ显著减少（Ｐ〈０．０５）,血浆ＴＸＢ２ １２ｈ与２４ｈ均非常显著下降（Ｐ〈０．０１）,而血浆６－酮－ＰＧＦ     

缩宫汤治疗子宫肌瘤月经异常（气虚血瘀型）初步研究

为了研究缩宫汤对子宫肌瘤月经异常（气虚血瘀型）患者的作用及其机制。观察４０例患者治疗前后经量、经期的变化,并测定血浆ＴＸＢ２、６－ｋｅＴｏ－ＰＧＦ１ａ浓度。结果缩宫汤止血有效率为８２．５％,除６－ｋｅＴｏ－ＰＧＦ１ａ外,ＴＸＢ２、Ｔ／Ｋ均显著高于正常对照组（Ｐ〈０．０１）。缩宫汤治疗后,除６－ｋｅＴｏ－ＰＧＦ１ａ皆有显著降低（Ｐ〈０．０１）,Ｔ／Ｋ趋于正常。提示调节血栓素Ａ２（ＴＸＡ２）、前列环素     

阿莫西林及其胶囊的氧瓶燃烧电位滴定

阿莫西林及其胶囊的氧瓶燃烧电位滴定韩学静，杨立新，唐之秀（河北省药品检验所，石家庄０５００１１；石家庄市新华制药厂，石家庄０５００９１）ＰＯＴＥＮＴＩＯＭＥＴＲＩＣＴＩＴＲＡＴＩＯＮＯＦＡＭＯＸＩＣＩＬＬＩＮＡＮＤＩＴＳＣＡＰＳＵＬＥＳＢＹＯＸＹＧＥ...     

绞股蓝总皂苷对内毒素、氧自由基介导血管内皮细胞表达c-sis基因和调节平滑肌细胞增殖的影响

目的　研究绞股蓝总皂苷（ Ｇｙｐ） 对血管平滑肌细胞增殖的调节与内皮细胞ｃ ｓｉｓ 基因表达和一氧化氮（ Ｎ Ｏ） 合成／ 释放的关系。方法　采用原位杂交法检测内皮细胞ｃ ｓｉｓｍ Ｒ Ｎ Ａ 表达,用 Ｇｒｉｅｓｓ 法测定内皮细胞 Ｎ Ｏ 释放量,用 Ｍ Ｔ Ｔ快速比色法检测平滑肌细胞（ Ｓ Ｍ Ｃ） 增殖。结果　内毒素（ Ｌ Ｐ Ｓ）１６ ｍｇ· Ｌ－ １ 促进牛主动脉内皮细胞ｃ ｓｉｓ 基因表达,明显降低内皮细胞培养液中一氧化氮含量,刺激 Ｓ Ｍ Ｃ 增殖;黄嘌呤－ 黄嘌呤氧化酶（ Ｘ Ｘ Ｏ） 系统产生的氧自由基（ Ｏ Ｆ Ｒ） 具有与 Ｌ Ｐ Ｓ 相似的作用。绞股蓝总皂苷对 Ｌ Ｐ Ｓ诱导的内皮细胞ｃ ｓｉｓ 基因表达具有明显抑制作用,并能对抗 Ｏ Ｆ Ｒ 诱导的 Ｅ Ｃ 损伤,保护内皮细胞释放 Ｎ Ｏ 的能力,抑制 Ｌ Ｐ Ｓ 和 Ｏ Ｆ Ｒ通过 Ｅ Ｃ 介导的 Ｓ Ｍ Ｃ 增殖。 Ｇｙｐ 的效应可被 Ｎ Ｏ 合成酶抑制剂硝基 左旋精氨酸部分取消。结论　绞股蓝总皂苷通过抑制内皮细胞ｃ ｓｉｓ 基因表达,促进内皮细胞合成（ 释放） Ｎ Ｏ抑制平滑肌细胞增殖     

孕鼠血浆一氧化氮减少与内皮素、血栓素、前列环素的关系

本文研究一氧化氮减少对孕鼠血浆内皮素（ＥＴ）、血栓素Ｂ２（ＴＸＢ２）、６－酮－前列腺素Ｆ１α（６－ｋｅｔｏ－ＰＧＦ１α）等血管活性因子的影响。结果显示妊娠大鼠血浆ＥＴ、ＴＸＢ２、６－ｋｅｔｏ－ＰＧＦ１α均升高，ＴＸＢ２／６－ｋｅｔｏ－ＰＧＦ１α比值降低，未妊娠大鼠血浆ＥＴ升高，６－ｋｅｔｏ－ＰＧＦ１α降低，ＴＸＢ２无显著变化，ＴＸＢ２／６－ｋｅｔｏ－ＰＧＦ１α比值升高。说明孕鼠体内一氧化氮减少时，ＥＴ及ＴＸＢ２上升，血管收缩，而作为代偿和保护机制，６－ｋｅｔｏ－ＰＧＦ１α升高，ＴＸＢ２比值降低。未妊娠大鼠无此代偿效应。     

高效液相色谱-串联质谱法同时测定地龙中4个黄曲霉毒素

目的:建立同时测定地龙中4个黄曲霉毒素含量的高效液相色谱串联质谱法。方法:样品经甲醇-水(80∶20,v/v)提取,通过免疫亲和柱净化后,采用高效液相色谱串联质谱法测定其中4个黄曲霉毒素的含量,以多反应监测(MRM)方式分别监测离子对m/z 313→241(黄曲霉毒素B1,CE 50 eV),m/z 315→259(黄曲霉毒素B2,CE 43 eV),m/z 329→243(黄曲霉毒素G1,CE 38 eV)和m/z 331→245(黄曲霉毒素G2,CE 40 eV)。结果:黄曲霉毒素B1、B2、G1、G2的检测限分别为0.03,0.02,0.03,0.02μg.kg-1,回收率在88.0%～100.3%范围内,RSD均低于6.1%。结论:该方法快速、灵敏,结果准确,适用于地龙中4个黄曲霉毒素的同时检测。     

HPLC法测定150种中药材中黄曲霉毒素G2、G1、B2、B1的含量

目的:建立了HPLC法测定150种中药材中的黄曲霉毒素G₂、G₁、B₂、B₁含量。方法:样品经70%甲醇提取、免疫亲和色谱柱净化后,用HPLC-柱后衍生-荧光检测器测定结果:黄曲霉毒素G₁、B₂在0.15～6.00 ng·ml^-1范围内,黄曲霉毒素C₁、B₁在0.5～20.00 ng·ml^-1范围内线性关系良好回收率为85.6%～92.0%结论:本法操作简便,结果准确、重复性好,可用于中药材中黄曲霉毒素G₂、G₁、B₂、B₁的测定     

Comparative cytotoxicity study of enniatins A, A1, A2, B, B1, B4 and J3 on Caco-2 cells, Hep-G2 and HT-29

Enniatins (ENs) are ionophoric, phytotoxic, antihelminthic, and antibiotic compounds of hexadepsipeptidic structure produced by several strains of Fusarium spp. The cytotoxicity effect of the ENs A, A₁, A₂, B, B₁, B₄ and J₃ was compared on three tumor cell lines, the human epithelial colorectal adenocarcinoma (Caco-2), the human colon carcinoma (HT-29), and the human liver carcinoma (Hep-G2). The endpoint evaluated was the mitochondrial integrity by using the MTT assays, after 24 and 48 h of incubation. The IC₅₀ value for EN A₂ on Caco-2 cells, after 24 h exposure, was 18.7 ± 4.5 μM and decrease to 2.6 ± 0.7 μM at 48 h of incubation. However, ENs A, A₁, B₁ and B₄ exert pronounced cytotoxic effects in all the cell lines tested by the MTT assay after 24 and 48 h of incubation. The EN A₁ demonstrated to be the most cytotoxic ENs tested. Moreover, no statistical differences were found between the IC₅₀ values obtained for EN A₁ on Caco-2, HT-29 and Hep-G2, with IC₅₀ values ranging from 9.1 ± 2.2 μM to 12.3 ± 4.3 μM at 24 h and decreasing in a range variable from 1.4 ± 0.7 μM to 2.7 ± 0.8 μM at 48 h. On the other hand, EN A, B₁ and B₄ showed lower cytotoxicity, but in a similar range as the IC₅₀ values reported on HT-29 (IC₅₀ values (24 h): 16.8 ± 4.3-26.2 ± 6.7 μM), Caco-2 (IC₅₀ values (24 h): 19.5 ± 4.1 μM) and Hep-G2 (IC₅₀ values (24 h): 23.4 ± 5.6-26.2 ± 7.6 μM) cells. Cytotoxic effect with a 48 h of incubation revealed also a significant toxicity of ENs A (IC₅₀ values ranged from 8.2 ± 1.8 to 11.4 ± 4.6 μM), B₁ (IC₅₀ values variables from 3.7 ± 0.7 to 11.5 ± 5.3 μM) and B₄ (IC₅₀ of 4.5 ± 2.9-15.0 ± 4.0 μM). In summary, this study demonstrated that ENs can exert toxic activity at low micromolar concentrations in mammalian cells.     

海藻酸盐敷料止血作用及生物相容性研究

摘要：目的 研究海藻酸盐敷料的止血性能,并初步探究其生物相容性。方法 采用凝血指数试验测定体外凝血性能。采用新西兰兔耳和背部创伤止血试验测定止血性能。采用溶血试验和细胞毒性试验进行初步安全性评价。结果海藻酸盐敷料、明胶海绵的凝血指数BCI分别为33.1±4.9、72.0±3.3,海藻酸盐敷料凝血效果优于明胶海绵。在背部创伤出血模型中,海藻酸盐敷料、明胶海绵、纱布的平均止血时间为（55.3±5.1）s、（80.2±7.4）s、（101±14.7）s,Hb光度吸收值分别为1.5±0.7、2.5±0.5、3.8±0.7。与明胶海绵比较,海藻酸盐敷料的平均止血时间缩短了31.05%,Hb光度吸收值降低了40.00%;与纱布比较,海藻酸盐敷料的平均止血时间缩短了45.25%,Hb光度吸收值降低了60.53%。在兔耳动脉止血实验中,海藻酸盐敷料、明胶海绵、纱布的出血量分别为（2.4±0.2）g、（3.0±0.2）g、（3.9±0.2）g,止血时间分别为（226.3±6.5）s、（332.3±14.2）s、（466.5±19.1）s。与明胶海绵组比较,海藻酸盐敷料的出血量降低了20.00%,止血时间分别为缩短了31.90%;与纱布比较,海藻酸盐敷料的出血量降低了38.46%,出血时间缩短了51.49%。海藻酸盐敷料的溶血率低于5%。细胞毒性实验中各浓度的海藻酸盐敷料浸提液为0级或1级,提示其对细胞无明显毒性。结论 海藻酸盐敷料具有良好的止血效果,溶血率符合国标要求,且对皮肤成纤维细胞无细胞毒性。     

A comparison of the vasodepressor effects of the cyclic endoperoxides PGG2 and PGH2 with those of PGD2 and PGE2 in hypertensive and normotensive rats

The vasodepressor actions of the cyclic endoperoxides PGG₂ and PGH₂ were compared with those of their products PGD₂ and PGE₂ using anaesthetised normotensive and genetically hypertensive rats. Given into the aortic arch of normotensives PGE₂ was approximately 6 times more potent than PGH₂ and 11 times more potent than PGG₂ and PGD₂. Hypertensive animals were 1.5–10 times more sensitive than normotensives to the depressor effects of PGG₂ and PGH₂, but their sensitivity to either PGD₂ or PGE₂ was similar. Thus in hypertensives the endoperoxides may be converted more readily to PGE₂ and other products.In both types of rat PGG₂ and PGH₂ given intravenously were as active or more active than after intra-arterial administration. Low but not high intravenous doses of PGE₂ were less effective than intra-arterial. Therefore PGG₂ and PGH₂ may be converted more readily to more active products during passage through the lungs but whereas small doses of PGE₂ are almost completely eliminated large doses may saturate pulmonary removal mechanisms.     

高效液相色谱-荧光检测法测定沉香中黄曲霉毒素B1、B2、G1、G2

目的建立高效液相色谱–光化学衍生–荧光检测法测定沉香药材中黄曲霉毒素B1、B2、G1、G2。方法采用高效液相色谱法,通过免疫亲和柱提取和净化,荧光检测器检测。Agilent Zorbax Ecilpse Plus C18色谱柱(250 mm×4.6 mm,5μm);流动相:甲醇–水(45∶55);体积流量:0.8 m L/min;柱温:30℃;进样盘温度:4℃;荧光激发波长为360 nm,发射波长为450 nm。结果黄曲霉毒素B1、B2、G1、G2分别在9.3~74.4、3.0~24.0、9.3~74.4、3.5~28.0 pg线性关系良好,r均大于0.998 0;检测限分别为1.86、0.60、1.86、0.70 pg,定量限分别为7.44、2.40、7.44、2.80 pg。平均回收率分别为78%、92%、82%、99%,RSD值分别为4.4%、3.0%、4.3%、2.8%。结论所建立的方法结果准确、重复性、稳定性均良好,可用于沉香药材中黄曲霉毒素的质量控制。     

Antipsychotic regulation of dopamine D1, D2 and D3 receptor mRNA

A range of antipsychotic drugs, both “typical” and “atypical”, was administered to rats over a time course and at several different dosages. The mRNA levels of dopamine D₁ , D₂ and D₃ receptor were measured in either whole brain or dissected brain regions. D₃ receptor mRNA was up-regulated in whole brain by clozapine (10 and 30 but not 3 mg/kg/day), sulphide (50 and 100 but not 20 mg/kg/day), haloperidol (3 but not 1 or 0.3 mg/kg/day), flupenthixol (3 but not 1 or 0.3 mg/kg/day), pimozide (4.5 but not 1.5 or 0.5 mg/kg/day) and loxapine (1.2 and 4 mg/kg/day but not 0.4 mg/kg/day). Sulphide (100 mg/kg/day), clozapine (30 mg/kg/ day) and haloperidol (3 mg/kg/day) all up-regulated the D₃ receptor mRNA in nucleus accumbens and olfactory tubercles but not striatum. D₁ and D₂ receptor mRNA was up-regulated in whole brain by haloperidol and loxapine only, and in the case of haloperidol this was localized to striatum and prefrontal cortex. Haloperidol, clozapine and sulphide all down-regulated D₁ mRNA in hippocampus and additionally haloperidol and sulpiride down-regulated it in the cerebellum. This work shows that all the drugs tested upregulated D₃ receptor, but effects on D₁ and D₂ receptors were less general.     

Compression characteristics of basic tricalcium phosphate (Ca3(PO4) 2, Ca(OH)2)

It is shown that tricalcium phosphate obeys the Heckel equation only if a particle density of 1.92 g/cm³ (rather than the true density of 3.1 g/cm³) is used to determine the relative density of compacts. It is shown by comparing mercury intrusion porosimetry data with nitrogen adsorption data, that a large portion of the solid has pores of diameters of less than 60 Å. It would appear that this part of the pore space is not compressible in conventional pressure ranges, and that it should not be considered part of the Heckel pore space. It is shown by hysteresis loops that (in as much as simple interpretations are permissible) there is a substantial amount of ink-bottle pores, and that both neck and cavity volumes decrease in a logical fashion with increased applied pressure.     

高效液相色谱-光化学衍生法测定湖南产莲子中黄曲霉毒素G1、G2、B1、B2

目的对不同来源的湖南产莲子中黄曲霉毒素G_1、G_2、B_2、B_1进行高效液相色谱-光化学衍生法测定。方法采用高效液相色谱–光化学衍生法,采用岛津GL Inertsil ODS-3色谱柱(250 mm×4.6 mm,5μm),流动相为甲醇–乙腈–水(35∶13∶52),柱温35℃;光化学衍生器(254 nm)激发波长λ_(ex)=360 nm,发射波长λ_(ex)=450 nm。结果黄曲霉毒素G_1、G_2、B_2、B_1分别在6.7～33.3、11.4～56.8、10.3～51.5、4.1～20.3 pg线性关系良好;平均回收率分别为98.07%、97.72%、96.11%、99.52%,RSD值分别为1.69%、1.40%、2.72%、1.34%(n=6)。9批莲子样品中,有6批未检出黄曲霉毒素,来自于农贸市场农户自存的2批次检出黄曲霉毒素B_1,实验室塑料袋包装储存1年的1批检出黄曲霉毒素B_1、B_2,但质量分数均低于法定标准限量。结论不同来源湖南产莲子中黄曲霉毒素质量分数均低于《中国药典》2020年版规定限量。该法测定结果准确、重复性良好,可为完善莲子安全性控制和质量标准提升提供实验依据。