顶体反应抑制剂4'- 乙酰胺苯基4-胍基苯甲酸酯(AGB)具有阻断HIV-1进入细胞的作用

】目的: 研究4'- 乙酰胺苯基4- 胍基苯甲酸酯(AGB)抗 HIV-1 活性及作用靶点。方法: 通过 AGB对宿主细胞的毒性实验、合胞体抑制实验、融合阻断实验、对HIV-1感染细胞的保护作用实 验和对HIV-1急性感染细胞p24抗原产生的抑制作用等试验，观察AGB对HIV-1复制的影响和作 关键词: AGB; HIV-1; 病毒进入; 杀微生物剂; 杀精子活性 中图分类号: R967; 文献标识码: A 文章编号: 0253-357X(2005)11-0660-05 本研究为国家高技术研究发展计划(2003AA219142)、国 家科技攻关计划 (2004BA719A14)、中国科学院知识创新 工程重要方向(KSCX2-SW-216; KSCX12-SW-11)、云南 省科技攻关计划(2004NG12)和云南省生育调节与少数民 族优生研究重点实验室资助项目 通讯作者: 郑永唐; Tel: +86-871-5195684; Fax:+86-871-5191823; E-mail: zhengyt@mail.kiz.ac.cn 在我国, 人免疫缺陷病毒(human immunodeficiency virus, HIV)危害日趋严重，处在全国低流行 与局部地区及特定人群高流行并存的态势。卫生部 的数据显示，截止2005 年3 月底，全国累计报告 HIV 感染者114 703 例。专家估计我国实际HIV 感 染者超过100 万人。预计到2010 年, 全国HIV感染 者将突破千万。截止2004 年底, 云南省累计报告的 HIV 感染者已达28 391 人, 是全国流行最严重的地 区。艾滋病流行正由高危人群向一般人群传播。 新的证据显示近年来由性传播途径感染的比例有所 上升, 女性感染者的比例有较大幅度的上升, 迫切需 要发展一种女性可自主控制的方法 [1]。杀微生物剂 是可以局部用药于阴道和宫颈、能够杀灭或抑制 包括HIV等病毒性和细菌性病原体、人工合成或天 然的药物。具有避孕作用的杀微生物剂更是近年 来的研究热点，也具有广阔的应用前景[2,3]。 顶体酶是存在于精子顶体内的一种类胰蛋白 酶, 它是受精过程中的一种重要的蛋白水解酶, 此酶 能水解卵细胞的透明带, 使精子能够与卵细胞相融 合; 顶体酶还能促进生殖系统中激肽的释放, 后者能 够增强精子的活力和促进精子的运动, 顶体酶的失 活将导致不孕[4]。AGB(4'- 乙酰胺苯基 4- 胍基苯甲 酸酯)是顶体酶的抑制剂, 实验表明在多种动物中有 很好的杀精子作用[5-7]。Bourimbaiar等[8]曾报道AGB 还具有体外抗HIV-1的作用, 活性较N-9高, 且毒性 较小。在本实验中, 我们发现AGB 的体外抗HIV-1 活性主要是阻断HIV-1 进入细胞。 用机制。结果: AGB抑制HIV-1IIIB诱导C8166细胞形成合胞体, EC50为39.5 μg/ml; 抑制HIV-1感染 细胞上清中HIV-1 p24抗原的表达, EC50为33.36 μg/ml; 阻断HIV-1慢性感染H9细胞与正常C8166 细胞间融合的作用。结论: AGB具有阻断HIV-1 进入宿主细胞的作用，是一种有前景的具杀精子 作用的杀微生物剂。

Quakes in solid quark stars

A starquake mechanism for pulsar glitches is developed in the solid quark star model. It is found that the general glitch natures (i.e., the glitch amplitudes and the time intervals) could be reproduced if solid quark matter, with high baryon density but low temperature, has properties of shear modulus mu(c) = 10(30-34) erg/cm(3) and critical stress sigma(c) = 10(18similar to24) erg/cm(3). The post-glitch behavior may represent a kind of damped oscillations. (C) 2004 Elsevier B.V. All rights reserved.

Three-body force effect on P-3 F-2 neutron superfluidity in neutron matter, neutron star matter, and neutron stars

We investigate the effect of microscopic three-body forces on the P-3 F-2 neutron superfluidity in neutron matter, beta-stable neutron star matter, and neutron stars by using the BCS theory and the Brueckner-Hartree-Fock approach. We adopt the Argonne V18 potential supplemented with a microscopic three-body force as the realistic nucleon-nucleon interaction. We have concentrated on studying the three-body force effect on the P-3 F-2 neutron pairing gap. It is found that the three-body force effect considerably enhances the P-3 F-2 neutron superfluidity in neutron star matter and neutron stars.

(PF2)-P-3 neutron superfluidity in neutron stars and three-body force effect

We investigate the (PF2)-P-3 neutron superfluidity in beta-stable neutron star matter and neutron stars by using the BCS theory and the Brueckner-Hartree-Fock approach. We adopt the Argonne V-18 potential supplemented with a microscopic three-body force as the realistic nucleon-nucleon interaction. We have concentrated on studying the three-body force effect on the (PF2)-P-3 neutron pairing gap. It is found that the three-body force effect is to enhance remarkably the (PF2)-P-3 neutron superfluidity in neutron star matter and neutron stars.

Antikaon condensation and in-medium kaon and antikaon production in protoneutron stars

Antikaon condensation and kaon and antikaon production in protoneutron stars are investigated in a chiral hadronic model (also referred to as the FST model in this paper). The effects of neutrino trapping on protoneutron stars are analyzed systematically. It is shown that neutrino trapping makes the critical density of K- condensation delay to higher density and (K) over bar (0) condensation not occur. The equation of state (EOS) of (proto)neutron star matter with neutrino trapping is stiffer than that without neutrino trapping, As a result, the maximum masses of (proto)neutron stars with neutrino trapping are larger than those without neutrino trapping. If hyperons are taken into account, antikaon does not form a condensate in (Proto)neutron stars. Meanwhile, the corresponding EOS becomes much softer, and the maximum masses of (proto)neutron stars are smaller than those without hyprons. Finally, our results illustrate that the Q values for K+ and K- production in (proto)neutron stars are not sensitive to neutrino trapping and inclusion of hyperons.

Antikaon condensation and deconfinement phase transition in neutron stars

Antikaon condensation and deconfinement phase transition in neutron stars are investigated in a chiral hadronic model (also referred as to the FST model) for the hadronic phase and in the MIT bag model for the deconfined quark matter phase. It is shown that the existence of quark matter phase makes antikaon condensation impossible in neutron stars. The properties of neutron stars are sensitive to the bag constant. For the small values of the bag constant, the pure quark matter core appears and hyperons are strongly suppressed in neutron stars, whereas for the large bag constant, the hadron-quark mixed phase exists in the center of neutron stars. The maximum masses of neutron stars with the quark matter phase are lower than those without the quark matter phase; meanwhile, the maximum masses of neutron stars with the quark matter phase increase with the bag constant.

Transport parameters in neutron stars from in-medium N N cross sections

We present a numerical study of shear viscosity and thermal conductivity of symmetric nuclear matter, pure neutron matter, and beta-stable nuclear matter, in the framework of the Brueckner theory. The calculation of in-medium cross sections and nucleon effective masses is performed with a consistent two- and three-body interaction. The investigation covers a wide baryon density range as needed in the applications to neutron stars. The results for the transport coefficients in beta-stable nuclear matter are used to make preliminary predictions on the damping time scales of nonradial modes in neutron stars.

Clemaps: Multiple Alignment Of Protein Structures Based On Conformational Letters

CLEMAPS is a tool for multiple alignment of protein structures. It distinguishes itself from other existing algorithms for multiple structure alignment by the use of conformational letters, which are discretized states of 3D segmental structural states. A letter corresponds to a cluster of combinations of three angles formed by C-alpha pseudobonds of four contiguous residues. A substitution matrix called CLESUM is available to measure the similarity between any two such letters. The input 3D structures are first converted to sequences of conformational letters. Each string of a fixed length is then taken as the center seed to search other sequences for neighbors of the seed, which are strings similar to the seed. A seed and its neighbors form a center-star, which corresponds to a fragment set of local structural similarity shared by many proteins. The detection of center-stars using CLESUM is extremely efficient. Local similarity is a necessary, but insufficient, condition for structural alignment. Once center-stars are found, the spatial consistency between any two stars are examined to find consistent star duads using atomic coordinates. Consistent duads are later joined to create a core for multiple alignment, which is further polished to produce the final alignment. The utility of CLEMAPS is tested on various protein structure ensembles.

The giant zooxanthellae-bearing ciliate Maristentor dinoferus (Heterotrichea) is closely related to folliculinidae

The small subunit rDNA sequence of Maristentor dinoferus (Lobban, Schefter, Simpson, Pochon, Pawlowski, and Foissner, 2002) was determined and compared with sequences from other Heterotrichea and Karyorelictea. Maristentor resembles Stentor in basic morphology and had been provisionally assigned to Stentoridae. However, our phylogenetic analyses show that Maristentor is more closely related to Folliculinidae. Our results support the creation of a separate family for Maristentor, Maristentoridae n. fam., and also confirm the phylogenetic grouping of Folliculindae, Stentoridae, Blepharismidae, and Maristentoridae, which we informally call 'stentorids'. Maristentor, rather than Stentor itself, appears to be most significant in understanding the origins of folliculinids from their aloricate ancestors. Our analyses suggest continued uncertainty in the exact placement of the root of heterotrichs with this phylogenetic marker.