骨瓜提取物注射液的生物活性测定

目的采用生物活性测定法加强骨瓜提取物注射液的质量控制。方法建立巴豆油致小白鼠耳廓肿胀的实验模型来评价骨瓜提取物注射液消炎的功能。结果骨瓜提取物注射液能显著降低巴豆油所致小鼠耳廓肿胀度,其肿胀度明显低于模型对照组,表明骨瓜提取物注射液具有明显的抗炎作用。结论成功建立了测定骨瓜提取物注射液生物活性的动物模型,可用于骨瓜提取物注射液的生物活性测定。     

短指软珊瑚属次级代谢产物化学成分及其生物活性研究进展

短指软珊瑚属（Sinularia）分布十分广泛,富含结构新颖、生物活性显著的次级代谢产物,已成为国际上海洋天然产物的研究热点之一。该属软珊瑚中的次级代谢产物主要涉及倍半萜、二萜、倍半萜一二萜二聚体、二萜二聚体、降倍半萜、降二萜、降二萜二二聚体、杂萜、甾体及其糖苷、神经酰胺、长链烷基糖苷、亚精胺等结构类型,其中很多化合物具有抗肿瘤、抗菌、抗病毒和抗炎等生物活性。本文综述了1975年至2013年4月间报道的短指软珊瑚中的次级代谢产物及其生物活性的研究进展,以期为该领域海洋天然产物的后续研究与开发提供参考。     

Effect of additives on encapsulation efficiency,stability and bioactivity of entrapped lysozyme from biodegradable polymer particles

Low encapsulation efficiency, incomplete and erratic release profiles are the most common features of controlled released protein delivery systems employing biodegradable polymers. In the present study, lysozyme as a model protein was encapsulated in biodegradable microspheres using solvent evaporation method and the effect of amphiphilic stabilizer, a basic salt and a lyoprotectant on microparticle formulation was evaluated. Incorporation rat serum albumin (RSA) in the internal aqueous phase during emulsion increased the encapsulation efficiency of lysozyme and maintained the bioactivity. Use of NaHCO₃ improved the encapsulation efficiency of lysozyme from 15–94%, but at the cost of reduced in vitro release characteristics. Incorporation of both RSA and NaHCO₃ improved the bioactivity of lysozyme and decreased burst release of the protein from the polymer particle, but reduced the encapsulation efficiency from 90–70%. Addition of sucrose in the internal aqueous phase lowered the encapsulation efficiency which was restored by its addition in the external aqueous phase. Maintenance of internal aqueous phase pH close to the iso-electric point of the protein and osmotic balance between the internal aqueous phase and the external aqueous phase during solvent evaporation method helped in better encapsulation of the protein drug. In vitro release of the lysozyme correlated with the effect of different excipients on entrapment in polymer matrix. Entrapment efficiency as high as 76%, low burst effect and high bioactivity of the entrapped lysozyme was observed from the polymer particles. Use of RSA, sucrose and NaHCO₃ helped in a co-operative way towards the formulation of particles entrapping bioactive lysozyme.     

Insights into gastrointestinal microbiota-generated ginsenoside metabolites and their bioactivities

Abstract

The gastrointestinal microbiota and host co-evolve into a complex ‘super-organism,’ and this relationship plays a vital role in many physiological processes, such as drug metabolism. Ginseng is an important medicinal resource and the main ingredients are ginsenosides, which are less polar, difficult to absorb, and have low bioavailability. However, studies have shown that the biological activity of ginsenosides such as compound K (CK), ginsenoside Rg3 (Rg3), ginsenoside Rh2 (Rh2), 20(S)-protopanaxatriol (20(S)-PPT), and 20(S)-protopanaxadiol (20(S)-PPD) is closely related to the gastrointestinal microbiota. In this paper, the metabolic pathway of gastrointestinal microbiota-generated ginsenosides and the main pharmacological effects of these metabolites are discussed. Furthermore, our study provides a new insight into the discovery of novel drugs. Specifically, in new drug screening process, candidates with low biological activity and bioavailability should not be excluded. Because their metabolites may exhibit good pharmacological effects due to the involvement of the gastrointestinal microbiota. In addition, in further research studies to develop probiotics, a combination of agents could exert greater efficacy than single agents. Moreover, differences in lifestyle and diet lead to differences in the gastrointestinal microbiota in the human body. Therefore, administration of the same drug dose to different individuals could elicit different therapeutic effects, owing to the involvement of the gastrointestinal microbiota. Thus, treatment accuracy could be achieved by detecting the gastrointestinal microbiota before drug treatment.

• Highlights

• Gastrointestinal microbiota plays a decisive role in bioactivities of ginsenosides.

• The metabolic pathway and main pharmacological effects of ginsenoside metabolites are discussed.

• It provides new insights into novel drug discovery and further research to find probiotic, combinations to exert greater efficacy.

• Differences in lifestyle and diet, varies the gastrointestinal microbiota in the human body. However, the same dose of a drug producing different therapeutic effects may involve gastrointestinal microbiota.

     

应用凝血酶偶联磁微粒技术对水蛭类药材中抗凝血酶活性的检测

水蛭是传统中药,它的主要药效功能之一是具有抗凝血酶活性组分。而在中药材及其制剂中能否检测出具有抗凝血酶活性,除与药材制取方法和制剂制备的工艺有关外,还可能与所含有的伪水蛭素含量有关。本文报道应用凝血酶偶联带有氨基末端的磁性微粒,从两种水蛭干品浸出液中分离纯化水蛭素,通过对抗凝血酶活性的检测,以求取对药材质量的评价,本法工艺简单、快速,亦可用于批量生产的初步纯化,为进一步精制提供基础。     

单抗工作参考品的活性赋值研究

利用一级参考品对工作参考品的多次标定,对工作参考品进行生物学活性的赋值。本文先理论计算应标定次数,若工作参考品多次标定的均值位于预设相对效价水平内时,则定义工作参考品的效价为100%。结果显示:在活性方法的总中间精密度为11.66%、预设效价水平为95%105%、置信水平为95%时,应进行至少21次标定。实际22次标定的均值为101.96%,故定义工作参考品与一级参考品效价一致即100%。结果提示采用先计算应标定次数后进行标定的方式,通过判断均值是否位于预设效价水平对工作参考品进行活性赋值,该策略对于生物制药企业具有一定的参考意义。     

天然产物抗菌作用的研究进展

感染性疾病不断进化并对现有药物产生抗药性,而天然产物为抵抗细菌性和真菌性疾病提供了新药研究的先导化合物。概述近年来抗细菌和抗真菌的天然产物及其生物活性的研究进展,为该类药物的深入研究和开发利用提供数据支撑和参考。     

In vivo evaluation of the trabecular bone behavior to porous electrostatic spray deposition-derived calcium phosphate coatings

OBJECTIVES: Electrostatic spray deposition (ESD) is a new technique to deposit calcium phosphate (CaP) coatings. The aim of the present study was to evaluate the bone behavior of ESD CaP-coated implants with various degrees of crystallinities in the trabecular bone of the femoral condyle of goats. MATERIAL AND METHODS: Using the ESD technique, thin porous CaP coatings were deposited on tapered, conical, screw-shaped titanium implants. Three different heat-treatments were applied, resulting in amorphous CaP (400 degrees C, ESD1), crystalline carbonate apatite (500 degrees C, ESD2), and crystalline carbonated hydroxyapatite (700 degrees C, ESD3). Implants were inserted into the trabecular bone of the femoral condyles of goats for 12 weeks, and titanium (Ti) implants served as controls. RESULTS: The results showed that ESD-derived coatings are osteocompatible. Histomorphometrical analysis showed that the application of a CaP coating resulted in more bone contact along the press-fit area of the implant compared with the Ti implants. Moreover, the percentage bone contact of the ESD3-coated implants was increased, compared with the Ti control group. Regarding the other coatings, no differences were found compared with the control group. CONCLUSION: Crystalline carbonated hydroxyapatite ESD-coated implants positively influenced the biological performance compared with Ti control implants.     

含镧羟基磷灰石的合成和性能研究

目的：研究湿法合成含镧式磷灰石的可行性及其体外生物活性。方法：采用湿法合成羟基磷磷石和两种不同的含羟基磷灰石粉,在３００℃、６００℃、９００℃热处理。红外光谱及Ｘ线衍射分析粉的成分。将９００℃热处理的两种含羟基磷灰石及羟基磷灰石的压片在模拟体液内浸泡,采用扫描电镜及溶液钙离子浓度测定法观察其体外生物活性,结果：通过热处理可去除含镧羟基磷灰石及羟基磷灰石内的杂质成分,获得的羟基磷灰石。含镧羟基磷灰石     

双分子取代苯酚氨羧酸螯合剂对放射性钍促排活性的构效关系

目的对已合成的１５个双分子取代苯酚氨羧酸螯合剂经动物实验观察对２３４Ｔｈ的促排活性,以探讨化学结构与促排活性的构效关系。方法以大鼠尿、粪中２３４Ｔｈ排出量的增高,组织（肝、骨）中蓄积量的降低与对照组比较作为评价指标。结果１５个螯合剂中除４个外均显示不同程度的促排活性,其中有３个其尿、粪中２３４Ｔｈ的排出量达６０％～７０％,肝、骨中２３４Ｔｈ的蓄积量明显降低。结论取代基中邻苯二酚类的促排活性为最好,为本实验之冠,间苯二酚的活性最差,对苯二酚居中。