抗HIV药物研究进展及发展趋势

本文分类总结了近年来抗HIV药物的研究进展以及以后的发展趋势,着重介绍了抗HIV的新的作用靶点和天然活性产物在抗HIV方面的应用。     

山茱萸多糖的分离纯化及活性研究

目的:山茱萸多糖的分离纯化及活性研究。方法:山茱萸经热水提取,去蛋白、超滤、醇沉、真空干燥得多糖粗品,经DEAE-32、SephacrylS-300HR柱层析得到精品多糖CSZP,并对CSZP进行免疫活性研究。结果:精品多糖CSZP均一,分子量为8．1×104,可明显增强细胞因子IL-2生物活性。结论:山茱萸多糖分离纯化工艺的建立及其免疫活性研究结果为以后进一步研究和开发山茱萸多糖提供了便利条件。     

817例儿童血红细胞SOD活性及血清LPO含量正常值研究

用邻苯三酚法及简易荧光法测定了817例儿童正常血红细胞内SOD活性及血清过氧化脂质含量。结果显示:(1)脐带血红细胞SOD活性显著低于各年龄组正常儿童(P<0.05),血清LPO含量显著高于(P<0.05)各年龄组正常儿童。(2)围产期血红细胞SOD活性明显低于新生儿围产期儿以后的各组儿童(P<0.05),血清LPO含量明显高于新生儿围产期儿以后的各组儿童(P<0.05)。(3)7天后新生儿血红细胞SOD活性明显低于其它各组儿童(P<0.05),血清LPO含量明显高于其它各组儿童(P<0.05)。(4)红细胞内SOD活性随年龄增长而逐渐升高。(5)7～14岁年龄组段内血清LPO含量女低于男(P<0.01)。(6)围产期新生儿组新生儿足跟血与静脉血红细胞内SOD活性、血清LPO含量无显著性差异(P>0.05)。     

猴头菌多糖的分离纯化及活性探讨

目的 :猴头菌多糖的分离纯化及活性探讨。方法 :人工栽培的猴头菌子实体经热水提取、去蛋白、超滤、醇化、真空干燥得多糖粗品 ,经 DEAE- 5 2、Sephacryl S- 4 0 0柱层析得到精品多糖 HEP,并对 HEP进行免疫活性研究。结果 :精品多糖HEP均一、分子量为 5 .5× 10 4 ,可明显增强细胞因子 IL- 2的生物活性。结论 :猴头菌多糖分离纯化工艺的建立及其免疫活性研究结果为以后进一步研究和开发猴头菌多糖提供了便利条件。     

挫伤大鼠坐骨神经后运动神经元酶组织化学的观察-SDH、ACP和AChE的改变

通过定位、定时、定量的方法压挫大鼠坐骨神经后,脊髓腰段伤侧前角运动神经元胞体的酶系发生一系列改变。从术后12小时到2周,SDH和AChE活性呈下降趋势,ACP活性呈上升趋势;以后三种酶活性逐渐恢复,SDH和AChE回升,ACP则降低,到术后4周时,三种酶活性均基本恢复正常。     

喹诺酮类抗菌素的临床应用与进展

自1962年第一个喹诺酮类药物萘啶酮酸(nalidixicacid/NegGram)上市以后,对喹诺酮类构效关系的研究推动了新药的开发。到目前为止,喹诺酮类药物已发展到第四代,并且对某些革兰氏阳性菌也有抗菌活性。据统计,目前已上市20多个喹诺酮类抗菌药,从第二代开始由于在其结构中引入氟基,其抗菌活性大大增强,80年代共上市6个品种其抗菌活性以环丙沙星最强,药代动力学性能以氧氟沙星最好。90年代共上市12个品种,其中以左氧氟沙星生物利用度最高,达99%,抗菌活性以加替沙星最强。第四代喹诺酮类抗菌素在抗菌活性和     

细辛、杜仲及其合剂对D—半乳糖所致衰老小鼠NO、NOS和MDA的影响

研究了细辛、杜仲及其合剂对D－半乳糖所致衰老小鼠的抗衰老作用。观察小鼠脑组织一氧化氮合酶（NOS）、血浆一氧化氮（NO）、肝组织MDA的随龄变化,同时观察了细辛、杜仲及其合剂对上述指标的影响。结果表明：老龄小鼠血浆NO含量、脑组织NOS活性在中年期以前随龄上升,中年期以后随龄下降;肝组织MDA含量随龄增高;细辛、杜仲及其合剂能够增加NO、降低MDA含量,提高NOS活性。细辛、杜仲及其合剂具有一定的抗衰老作用。     

细辛、杜仲及其合剂对D-半乳糖所致衰老小鼠血液中过氧化氢酶活性的影响

本实验以Ｄ－半乳糖所致的衰老小鼠为研究对象,观察了过氧化氨酶（ＣＡＴ）随龄变化以及细辛、杜仲及其合剂在不同用药时间（１５、３０、４５天）对老龄小鼠上述的影响,初步探讨这几种不同中药抗衰老的作用机制．结果表明：小鼠的ＣＡＴ活性在中年期以前随龄上升,中年期以后随龄下降（Ｐ＜０．０１）;细辛、杜仲及其合剂能够提高老年小鼠ＣＡＴ活性;并在给药１５天时效果最显著．     

小麦阿拉伯木聚糖结构性质与生理功能研究进展

阿拉伯木聚糖（AX）是小麦细胞壁的主要结构多糖,具有高分子量、高粘度性、高持水性和氧化凝胶等理化特性,对于小麦及其面制品的加工品质具有重要影响。同时它还具有增强免疫力抗肿瘤、降血脂、降血糖、清除自由基抗氧化、减肥、润肠通便等生理活性。本文回顾了近年来AX研究成果,对以后小麦AX的研究提供了一定的参考依据。     

细辛、杜仲及其合剂对D-半乳糖所致衰老小鼠心、肝组织中谷胱甘肽过氧化物酶活性的影响

本实验以D-半乳糖所致的衰老小鼠为研究对象,观察了谷胱甘肽过氧化物酶（GSH-Px）随龄变化以及细辛、杜仲及其合剂在不同用药时间（15、30、45d）对老龄小鼠上述指标的影响,初步探讨这几种不同中药抗衰老的作用机制.结果表明：小鼠的GSH－Px活性在中年期以前随龄上升,中年期以后随龄下降（P＜0.01）;细辛、杜仲及其合剂能够提高老年小鼠GSH－Px活性;合剂和杜仲对上述指标发挥作用的时间早于细辛,为15d,纳辛为30d．     

生物活性因子修饰骨髓间充质干细胞的研究进展

骨髓间充质干细胞（BMSCs）是骨髓基质中存在的非造血系的具有多向分化潜能的成体干细胞,现已成为国内外医学研究的热点。生物活性因子分布在人体各个组织中,对骨髓间充质干细胞具有重要的调节作用。文章从BMSCs的含义、细胞特性、联合多种生物活性因子及对组织的治疗等方面进行详细的阐述。     

一种白僵菌代谢产物提取物抗实验性抑郁的研究

目的　研究一种白僵菌代谢产物提取物 (BCEF0 0 83)抗实验性抑郁的作用。方法　采用小鼠获得性绝望模型 (小鼠强迫游泳实验、小鼠悬尾实验 )及慢性不可预见性应激、孤养模型研究BCEF0 0 83抗实验性抑郁作用及可能的作用机制 ;采用紫外、荧光分光光度计法检测BCEF0 0 83对模型动物脑组织单胺氧化酶活性、单胺递质含量的影响。结果　在小鼠强迫游泳实验、小鼠悬尾实验中 ,BCEF0 0 832 5、5 0、10 0mg·kg-13个剂量组均可明显缩短小鼠的不动时间 ,且呈现一定的量效关系 ;BCEF0 0 832 5、5 0、10 0mg·kg-13个剂量组对慢性应激模型小鼠脑组织重线粒体MAO A ,B活性均有明显的抑制作用 ,且呈现一定的量效关系。BCEF0 0 832 5、5 0、10 0mg·kg-13个剂量组对慢性应激模型小鼠脑组织NE、5 HT、5 HIAA、DA的含量有不同程度的提高。结论　BCEF0 0 83具有一定的抗小鼠实验性抑郁作用 ,其机制可能与抑制动物脑组织单胺氧化酶活性、升高单胺递质含量有关。     

Biochemical properties of peptides encrypted in bovine milk proteins

Milk proteins are precursors of many different biologically active peptides. These peptides are inactive within the protein sequence, requiring enzymatic proteolysis for release of the bioactive fragment from the proteins precursor. It is evident that activated peptides originating from milk proteins should be taken into account as potential modulators of various regulatory processes in the body. Activated peptides are potential modulators of various regulatory processes in the living system: immuno-modulatory peptides stimulate the activities of cells of the immune system and several cytomodulatory peptides inhibit cancer cell growth, antimicrobial peptides kill sensitive microorganisms, angiotensin-I-converting enzyme (ACE)-inhibitory peptides exert an hypotensive effect, opioid peptides are opioid receptor ligands which can modulate absorption processes in the intestinal tract, mineral binding peptides may function as carriers for different minerals, especially calcium, antithrombotic peptides inhibit fibrinogen binding to a specific receptor region on the platelet surface and inhibit aggregation of platelets. Moreover, many milk-derived peptides reveal multifunctional properties, i.e. specific peptide sequences having two or more different biological activities have been reported. Bioactive peptides can interact with target sites (e.g. receptors, enzymes) at the luminal side of the intestinal tract, or they could be absorbed and reach any potential site of action in the system to elicit physiological effects. Bioactive peptides encrypted in bovine milk proteins can be produced on an industrial-scale and are claimed to be health enhancing components for functional foods, nutraceuticals and pharmaceutical preparations that are used to reduce risk of disease or to enhance certain physiological functions.     

Bioactive peptide-modified biomaterials for bone regeneration

Bioactive biomaterials are desirable as tissue engineering scaffolds by virtue of their capability to mimic the natural environment of the extracellular matrix. Bioactive biomaterials have been achieved by incorporating synthetic short peptide sequences into suitable materials either by surface modification or by bulk incorporation. The goal is to enhance cell attachment and other basic functions. Bioactive peptides can be obtained from biological or chemically synthesized sources, increasing their specific cellular responses for tissue growth and development. Compared to using an entire growth factor in regenerative therapy, these peptides demonstrate potential advantages such as overcoming possible immunogenicity, being less susceptible to degradation, and producing fewer tumor-related side effects. Biomaterial scaffolds modified with peptides can provide biological ligands for cell-scaffold interactions that promote cell attachment, proliferation, and differentiation. Peptide-based biomaterial scaffolds can be fabricated to form two- and three-dimensional structures. This review discusses cell-binding, biominerailization inducing peptides, and receptor-binding peptides for bone regeneration. This review also addresses issues related to peptide immobilization as well as potential complications that may develop as a result of using these versatile bioactive peptides. The development of self-assembled peptide amphiphiles with the goal of generating new three-dimensional scaffolds for tissue engineering is also summarized.     

Study on the volume flows through polymeric membranous dressing with silver ions

The volume flows through double-layer polymeric membranous dressing, formed by three types of theromoplastic polymeric fibers called Textus Bioactive were studied. The first layer contains two types of fibers: the polymeric fibers containing hydrophobic core and hydrophilic surfaces with silver zeolite and hydrophilic super absorbing polymers (SAP). The second layer of membrane contains third type of polymeric fibers, arranged parallel to surface's skin, creating a net, which prevents membranous dressing from sticking to treated wound. The pressure characteristics of the volume flux were determined and it was stated that the value of this flux is dependent on the value of hydrostatic pressure difference (deltaP) and the concentration difference (deltaC) of solutions separated by membrane. Experimental results show that the membranous dressing Textus Bioactive posses the rectifying properties with reference to volume flows. These properties occurs above a threshold value of deltaC. Using the Kedem-Katchalsky equations, the model of the volume flows through membranous dressing Textus Bioactive was made.     

Effects of dietary wheat germ deprivation on the immune system in Wistar rats: a pilot study

Bioactive molecules that can gain access to body tissues through the gastrointestinal tract may interact with immune regulatory circuits and effector functions. Among these are plant lectins, such as wheat germ (WG) agglutinin, which constitute common components of the human diet and target the immune system on a daily basis. Dietary bioactive molecules might be considered as immunomodulatory signals. To investigate the possible effects on the immune system of the long-term absence of such signals, two groups of rats were fed on a diet containing or deprived of WG. The WG-deprived diet induced a state of functional unresponsiveness in lymphocytes from primary and secondary lymphoid organs, as evaluated by in vitro stimulation with T cell mitogen phytohemoagglutinin (PHA) and B cell mitogen lypopolysaccarides (LPS). The unresponsive state of the immune cells could be reversed by injection of antigen emulsified in oil with inactivated mycobacteria (complete Freund's adjuvant, CFA) Dietary signals can thus interact with the immune system possibly influencing its shaping during ontogenesis.     

Differential antagonism of denzimol to various components of metrazol-induced seizures in rats and mice

The antagonism of various components of maximal metrazol-seizures and the induction of ataxia have been studied in mice and rats by comparing Denzimol to 10 standard antiepileptic drugs. The data were analyzed by Cluster and Principal Components Analysis. Denzimol, phenytoin, carbamazepine and AD-810 showed an antagonistic effect on tonic but not on clonic seizures regardless of the animal species. Barbiturates, benzodiazepines and valproic acid, on the other hand, antagonized the whole pattern of metrazol-seizures. The selective activity of Denzimol and phenytoin against tonic seizures was also confirmed from literature data, which reported the activity of these compounds against bicuculline, thiosemicarbazide or picrotoxin induced convulsions.     

一种白僵菌代谢产物提取物抗抑郁作用的研究

目的研究一种白僵菌代谢产物提取物(BCEF)的抗抑郁作用。方法采用未预知的慢性应激实验、育亨宾毒性实验、5羟色胺酸诱导甩头实验等多种模型研究BCEF抗实验性抑郁作用及可能的作用机制。结果慢性刺激d10、d21后BCEF50mg·kg-1可使慢性应激大鼠水平得分与垂直得分显著增加;BCEF(100mg·kg-1,ig,qd×14d)可升高育亨宾给药后24h的小鼠死亡率;BCEF50、100mg·kg-1可明显增加5羟色胺酸诱导甩头小鼠的甩头次数。结论BCEF在多种抑郁模型上具有一定的抗抑郁作用,可能与增强NE、5HT能神经系统有关。     

猪脾细胞干扰素安全性的研究(五)围产期毒性试验

受孕的母鼠在妊娠期完成、即将分娩的妊娠后期,连续4d注射大剂量PSIFN,在母鼠泌乳期再对其进行3d加强注射。观察母鼠的仔胎起始数目、畸胎和死胎数目、仔胎的发育状况及生殖能力、母鼠的生长及能否再次受孕能力。结果表明PSIFN对受孕母鼠生殖、生活状况、对子代小鼠的生长发育、生殖能力均没有影响。     

Minimum information about a bioactive entity (MIABE)

Bioactive molecules such as drugs, pesticides and food additives are produced in large numbers by many commercial and academic groups around the world. Enormous quantities of data are generated on the biological properties and quality of these molecules. Access to such data - both on licensed and commercially available compounds, and also on those that fail during development - is crucial for understanding how improved molecules could be developed. For example, computational analysis of aggregated data on molecules that are investigated in drug discovery programmes has led to a greater understanding of the properties of successful drugs. However, the information required to perform these analyses is rarely published, and when it is made available it is often missing crucial data or is in a format that is inappropriate for efficient data-mining. Here, we propose a solution: the definition of reporting guidelines for bioactive entities - the Minimum Information About a Bioactive Entity (MIABE) - which has been developed by representatives of pharmaceutical companies, data resource providers and academic groups.