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GnRH could markedly suppress progesterone secretion of cultured GCs with or without FSH and LH co-treatments. E〓 could invert the suppression of GnRH completely, also had the additive action on secreting progesterone with GnRH co-treatment. Mel partially released the suppression action of GnRH.

GnRH能强烈地抑制体外培养的颗粒细胞分泌孕酮,其抑制作用几乎不受FSH和LH影响;Mel仅表现部分地缓解了GnRH的抑制效应,但没有逆转。E〓不仅可以完全逆转GnRH的抑制作用,进而与GnRH叠加促进颗粒细胞分泌孕酮。

GnRH could mar Red I y suppress progesterone secretion of cultured GCs with or without FSH and LH co-treatments. E2 could invert the suppression of GnRH completely, also had the additive action on secreting progesterone with GnRH co-treatment. Mel partial ly released the suppression action of GnRH.

GnRH能强烈地抑制体外培养的颗粒细胞分泌孕酮,其抑制作用几乎不受FSH和LH影响;Mel仅表现部分地缓解了GnRH的抑制效应,但没有逆转。E_2不仅可以完全逆转GnRH的抑制作用,进而与GnRH叠加促进颗粒细胞分泌孕酮。

From the calculations, it can be found that the van der Waals interactions, the hydrophobic interactions, as well as the H-bonding interactions are crucial for the ligand binding. The 4-phenylamino group can produce strong van der Waals adn hydrophobic interactions with the nonpolar side chains of the residues deep in the binding cleft. The R^1 and R^2 substituents on the bicyclic chromophore can also produce strong van der Waals and hydrophobic interactions with the residues located at the exterior part of the binding pocket. Moreover, the two N atoms of the quinazoline can form H-bonds with EGFR, which will produce significant contribution to biological activities. The calculated nonbonded interactions between anilinoquinazolines and EGFR, as well as the information obtained from the predicted complexes, can interpret the structure-activities of the inhibitors well, which can afford us important information for structure-based drug design.

从模拟结果得到的抑制剂和靶酶之间的相互作用模式表明范德华相互作用、疏水相互作用以及氢键相互作用对抑制剂的活性都有重要的影响,抑制剂的苯胺部分位于活性口袋的底部,能够与受体残基的非极性侧链产生很强的范德华和疏水相互作用,抑制剂双环上的取代基团也能和活性口袋外部的部分残基形成一定的范德华和疏水性相互作用,而抑制剂喹唑啉环上的氮原子能和周围的残基形成较强的氢键相互作用,对抑制剂的活性有较大的影响,计算得到抑制剂和靶酶之间的非键相互作用能以及抑制剂和靶酶之间的相互作用信息能够很好地解释抑制剂活性和结构的关系,为全新抑制剂的设计提供了重要的结构信息。

It is the fluorosilicic ion that exsits in the slurry and plays an important role in flotation, fluorosilicic ion not only reacted with Fe〓 on the surface of aegirine to form ionic compound, but also formed stable Si-F bond in Si-O etching reaction. Only ionic compound was obtained when it was attached to hematite surface according to the theories of coordination chemistry, Compared with SiF〓, Fatty acid ion preferentially acts with Fe〓 on the minerals surface, therefore, SiF〓 Can't obstruct the adsorption of collector on the surface of hematite completly, but can reduce the flotation recovery of aegirine selectively.

运用FTIR、XPS等测试方法仔细研究了氟硅酸盐抑制剂对含铁硅酸盐钠辉石的选择性抑制作用机理,氟硅酸盐在弱酸性条件下对赤铁矿浮选的抑制作用很微弱,而对含铁硅酸盐钠辉石强烈抑制,从而扩大了两者之间的浮选差异;SiF〓是矿浆中起抑制作用的主要成分,SiF〓不仅与钠辉石表面的Fe〓形成离子型配合物,而且还与Si-O键形成稳定的Si-F共价键,而与赤铁矿表面只能形成离子型配合物,根据晶体配位场理论,与SiF〓相比较羧酸根离子将优先与矿物表面Fe〓发生配位作用,因此SiF〓的存在并不能完全阻碍捕收剂在赤铁矿表面的吸附作用,却能够选择性地抑制钠辉石的上浮。

DCs acquired by our reformed methods express both CD83 and CD 14 molecules highly, and have a higher density than other domestic reports. The higher TNF in DCs culture medium of HC patient suggests DCs in patient still have antigen presenting ability and by optimization the culture medium would improve its presenting ability and have a potential value in design and application individual vaccine. Although antigens pulsed DCs have a decrescent antigen presenting ability but BCG HSP70 could induce its mature and improve its presenting ability. Suggests BCG HSP70 would be a useful mature inducer. Lymphocytes primed by DCs based HC vaccine have the specific cytotoxicity against HCC lines. The CTL after freezing and anabiotic could prophylaxis and therapy HC xenograft on nude mouse. The results also suggests that CD4〓 lymphocytes play a important role in HC with a good differentiation and would be useful in treatment this kind of HC. After being activated by Peptide LLNQHACAV of hAFP and apoptotic HCCs pulsed DCs respectively, the culture medium of activated lymphocytes both contains a high level Th1 cytokines IL-12 and TNF. Primed lymphocytes appeared a characteristic of NK cells. DCs not only inhibited the growth of human HCC and other cancer cells in vitro but also prevented the growth of HC xenograft on nude mouse in vivo. There are at least three kinds of mechanism playing important role in DC based vaccine ,there are inhibition of DCs, HC specific CTL and cytokines pathway.

诱导出的DC共同表达CD83和CD14分子,CD83分子表达明显高于国内报道;肝癌患者DC培养上清中TNF水平高于健康人,提示肝癌患者DC仍具一定的抗原呈递能力,适当调控可使其行使APC功能,以期在肝癌个体化疫苗中发挥作用;DC负载肝癌可溶性抗原后,抗原呈递能力降低,BCG HSP70可促进DC成熟,增加其抗原呈递能力,预示BCG HSP70有可能成为促进DC活化和成熟的另一重要分子;肝癌DC疫苗在体外诱导肝癌特异性淋巴细胞,活化的淋巴细胞在体外对肝癌细胞的杀伤以特异性CTL为主,同时分泌较高水平Th1型细胞因子IL-12和TNF,并抑制4种肝癌细胞生长;冷冻复苏后的肝癌特异性淋巴细胞可以预防和抑制人肝癌裸鼠皮下移植瘤,提示DC负载肝癌可溶性抗原后诱发的MHC-Ⅱ类限制性CD4〓T细胞有可能在分化程度高的肝癌治疗中发挥作用;用DC和HLA-A2〓DC分别负载凋亡肝癌细胞和hAFP218-226位LLNQHACAV HLA-A2限制性九肽,在体外诱导肝癌特异性淋巴细胞,活化后的CTL细胞分泌较高水平的Th1型细胞因子IL-12和TNF,并具较强杀伤活性,此CTL同时具备NK细胞特征;DC对肿瘤细胞的抑制作用可能是通过吞噬实现的,Fas-L在DC抑制中也起一定作用;DC对人肝癌裸鼠皮下移植瘤的抑制率为97%;在肝癌DC疫苗的作用中,至少联合3种以上机制,即通过DC的直接作用、肝癌特异性CTL和细胞因子途径直接或间接地杀伤和抑制肝癌细胞。

The results showed aqueous shoot extracts of Euphorbia maculata could inhibit seed germination speed in all the four species, reduce seed germination rate in Lycopersicon esculentum, Schizonepeta tenuifolia and Capsicum frutescents, and its effects increased with the increase of extracts concentration, while having no effects on seed germination of Edible umaranth.

结果表明,斑地锦浸提液可降低四种蔬菜种子的发芽速率,抑制番茄、辣椒和荆芥的发芽率,并且这种抑制作用随处理浓度的提高而加强,而对苋菜种子的发芽率无显著影响;0.4 g/ml的斑地锦浸提液强烈抑制了四种蔬菜根的生长,却不同程度地促进了辣椒、荆芥和苋菜茎的生长,对根/茎比的影响与对种子发芽率的影响类似。

The effect of genistein (0.8 mg/kg) was partially inhibited by L-NAME, or by sodium orthovanadate (50 μg/kg), a potent inhibitor of protein tyrosine phosphatase;(2) geni...

GST的这一效应可被L 硝基精氨酸甲酯部分阻断,预先注射蛋白酪氨酸磷酸酶抑制剂正钒酸钠( 5 0 μg/kg),可部分抑制GST( 0 8mg/kg)引起的效应;( 2 )向肾血管灌注环路中直接注射GST也可剂量依赖性地降低肾动脉的灌流压,预先注射正钒酸钠可完全抑制GST引起的效应,而L NAME对此效应没有影响;( 3 )肠系膜血管灌流环路中注射GST可剂量依赖性地降低其灌流压,这一效应可被正钒酸钠部分抑制,而L NAME对此无影响。

The effect of genistein (0.8 mg/kg) was partially inhibited by L-NAME, or by sodium orthovanadate (50 μg/kg), a potent inhibitor of protein tyrosine phosphatase;(2) genistein also decreased the PP of renal vascular bed in a dose-dependent manner and the effect of genistein was completely inhibited by pretreatment with sodium orthovanadate, but unaffected by L-NAME; and (3) genistein decreased the PP of mesenteric vascular bed in a dose-dependent manner, an effect which was partially inhibited by sodium orthovanadate, but unaffected by L-NAME.

GST的这一效应可被L-硝基精氨酸甲酯部分阻断,预先注射蛋白酪氨酸磷酸酶抑制剂正钒酸钠(50 μg/kg),可部分抑制GST (0.8 mg/kg)引起的效应;(2)向肾血管灌注环路中直接注射 GST 也可剂量依赖性地降低肾动脉的灌流压,预先注射正钒酸钠可完全抑制GST引起的效应,而L-NAME对此效应没有影响;(3)肠系膜血管灌流环路中注射GST可剂量依赖性地降低其灌流压,这一效应可被正钒酸钠部分抑制,而L-NAME对此无影响。

The effect of genistein (0.8 mg/kg) was partially inhibited by L-NAME, or by sodium orthovanadate (50 μg/kg), a potent inhibitor of protein tyrosine phosphatase;(2) Genistein also decreased the PP of renal vascular bed in a dose-dependent manner. The effect of genistein was completely inhibited by pretreatment with sodium orthovanadate, but unaffected by L-NAME;(3) Genistein decreased the PP of mesenteric vascular bed in a dose-dependent manner, an effect which was partially inhibited by sodium orthovanadate, but unaffected by L-NAME.

GST的这一效应可被L-硝基精氨酸甲酯部分阻断,预先注射蛋白酪氨酸磷酸酶抑制剂正钒酸钠(50 μg/kg),可部分抑制GST (0.8 mg/kg)引起的效应;(2)向肾血管灌注环路中直接注射 GST 也可剂量依赖性地降低肾动脉的灌流压,预先注射正钒酸钠可完全抑制GST引起的效应,而L-NAME对此效应没有影响;(3)肠系膜血管灌流环路中注射GST可剂量依赖性地降低其灌流压,这一效应可被正钒酸钠部分抑制,而L-NAME对此无影响。

RESULTS:(1) ET-1 could increase total protein production, surface area, ERKs activity and [Ca2+]i in cultured cardiomyocyte in dose-dependent manner at concentrations ranging from 10-9 to 10-7 mol/L. And this effect could be abolished by BQ123, an antagonist of ETA receptor, partly inhibited by PTX, but not by BQ788, an antagonist of ETB receptor.(2)The activation of ERKs and the increase of [Ca2+]i induced by ET-1 were obviously inhibited by PD98059, a selective ERKs kinase inhibitor, and nifedipine, a calcium channel blocker, respectively. Both antagonists partially inhibited ET-1-stimulated cardiomyocyte hypertrophic response.(3) Staurosporine, a selective PKC inhibitor, could inhibit ET-1-stimulated cardiomyocyte hypertrophic response and increase of [Ca2+]i, but not affect the activation of ERKs.

结果: ①ET-1浓度依赖性增加新生大鼠心肌细胞蛋白质含量和心肌细胞表面积、ERKs活性及[Ca2+]i浓度,以上作用可被ETA受体拮抗剂BQ123所完全抑制,被百日咳毒素部分抑制,而ETB受体拮抗剂BQ788则无效;②ERKs激酶特异性抑制剂PD98059可完全抑制ET-1激活ERKs的作用,钙通道拮抗剂硝苯地平可明显抑制ET-1介导的[Ca2+]i浓度增加,但二者皆仅部分抑制ET-1介导的心肌细胞肥大反应;③蛋白激酶C选择性抑制剂staurosporine并不能明显抑制ET-1介导的ERKs激活,但可抑制ET-1介导的的[Ca2+]i浓度增加及心肌细胞肥大反应。

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