牛膝菊中的萜类及甾醇类成分

 在细胞毒试验结果指导下,同步对牛膝菊(Galinsoga parviflora)全株的有效部位进行化学成分分离纯化,得到7个化合物,通过理化数据测定及波谱数据分析,鉴定了化学结构,分别是:对映-贝壳杉-16-烯-19-酸(1);对映-15-当归酰氧基-16-贝壳杉烯-19-酸(2);对映-15-当归酰氧基-16,17-环氧-19-贝壳杉烷酸(3);豆甾醇(4);α-菠甾醇(5);α-菠甾醇硬脂酸酯(6);β-谷甾醇(7).同时,细胞毒试验表明,牛膝菊的氯仿及乙酸乙酯提取物有一定细胞毒活性,其IC₅₀分别为8.5,10.5μg/mL.     

尖萼金丝桃中间苯三酚及黄酮类成分

 在细胞毒性试验结果指导下,对尖萼金丝桃(Hypericum acmosepaium N.Robson)全株的活性部位进行化学成分提取分离,得到6个单体,通过理化数据测定及波谱数据分析,鉴定了结构,分别是:Paglucinol(1);5-羟基-6-异丁酰基-2,2,8-三甲基-8-(3"-甲基-丁-2"-烯基)-2,8-二氢-1-苯并吡喃-7-酮(2);5-羟基-6-丙酰基-2,2,8-三甲基-8-(3"-甲基-丁-2"-烯基)-2,8-二氢-1-苯并吡喃-7-酮(3);7,8-(2",2"-二甲基吡喃)-5,3’,4’-三羟基-3-甲氧基黄酮(4);槲皮素(quercetin,5)及Ⅰ3,Ⅱ8-双芹菜甙元(Ⅰ3,Ⅱ8-biapigenin,6).同时,细胞毒性试验发现,尖萼金丝桃的二氯甲烷、乙酸乙酯萃取物及化合物(2),(5)具有细胞毒活性.     

In Vitro Cytotoxicity and Protein Drug Release Properties of Chitosan/Heparin Mlcrospheres

Chitosan/heparin microspheres were prepared using the water-in-oil emulsification solvent evaporation technique. The microsphere diameters were controlled by selecting the fabrication process parameters. Scanning electron micrographs showed that the chitosan/heparin microspheres were regular and the surface morphology was smooth. Fourier transform infrared showed that the chitosan amino groups reacted with heparin carboxylic groups to form acylamides in the microspheres. Analysis of the microsphere cytotoxicity showed that they had no cytotoxic effect and behaved very similar to the negative control （polystyrene）. To analyze the protein drug release profiles of the microspheres, bovine serum albumin was loaded as a model drug into the microspheres and released in vitro. Marked retardation was observed in the BSA release profiles. The results show that chitosan/heparin microspheres may provide a useful controlled release protein drug system for used in pharmaceutics.     

氧化石墨烯尺寸分级及细胞毒性研究进展

氧化石墨烯（graphene oxide, GO）是一种化学改性的石墨烯材料。作为化学法制备石墨烯的前驱产物,GO具有石墨烯固有的优异性能外,大量含氧官能团的存在还使其表现出两亲性,例如在诸多溶剂（尤其是水）中分散性能良好。不同尺寸的GO应用于不同领域。大尺寸GO因其结构完整,适用于于制备导电薄膜和整料。小尺寸GO因其优异的生物相容性和生物活性,常应用于生物医学领域。制备不同尺寸级别的GO,使其在不同领域中的应用发挥更好的作用很有必要。简单介绍了GO的制备方法及结构特性,重点总结了影响GO尺寸的因素、GO的尺寸分级方法以及GO细胞毒性的尺寸效应。     

丹参致大鼠肝细胞脂质过氧化损伤的实验研究

主要探讨了不同剂量(8,20和50mg／mL)丹参作用24h对大鼠肝细胞的脂质过氧化的影响．结果表明,随丹参浓度的增高,细胞培养液中丙氨酸氨基转换酶(ALT)、天门冬氨酸氨基转换酶(AST)活性逐渐增强,细胞中脂质过氧化产物——丙二醛(MDA)含量逐渐增高,细胞内超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH—PX)活性表现为先升高后下降的趋势．得出结论,一定剂量的丹参作用可导致大鼠肝细胞脂质过氧化损伤,可能为丹参对大鼠肝细胞毒性作用的机制之一。     

We find them here, we find them there: Functional bacterial amyloid

Protein amyloid is often deposited in connection with neurodegenerative diseases. Such deposits generally possess three principal drawbacks: cytotoxicity, lack of spatial control in their deposition and structural polymorphism. These are typical features of biologically non-optimized systems which have not been exposed to evolutionary pressure. Nevertheless, Nature uses the cross-beta self-organizing principle in many structural contexts where a strong but pliable material is needed. Functional amyloid is found in humans, invertebrates, fungi and, not least, bacteria, in which amyloid may be the rule rather than the exception. Detailed case studies reveal how directed nucleation can use tailor-made proteins optimized to assume a specific amyloid conformation, leading to remarkably robust assemblies. This makes it highly challenging to purify and analyze the products formed in vivo. We contrast pathogenic and in-vitro-formed amyloid with functional amyloid, paying particular reference to bacterial amyloid, and discuss challenges and perspectives in identifying and characterizing this class of protein.     

丛柳珊瑚Euplexaura rhipidalis中细胞毒活性二萜成分分析

为了寻找结构新颖的海洋活性成分,对一种采自中国西沙海域丛柳珊瑚Euplexaura rhipidalis进行分离和纯化,并对获得的西松烷二菇化合物的抗肿瘤活性进行筛选,以探明该种丛柳珊瑚的活性组成成分.先利用正反相硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备HPLC等方法进行分离和纯化,再利用NMR、MS等波谱方法,并与文献对照确定了3个高氧化度的西松烷二萜类化合物,分别为eorulloidolide A（1）,（1R,3S,4S,7E,11E）-3,4-epoxycembra-7,11,15-triene（2）,（-）-corulloidolide E（3）;细胞毒活性模型评价结果发现,化合物3表现了较强的细胞毒活性,对5种癌细胞肝癌HepG2,Hep3B,乳腺癌阿霉素耐药株MCF-7/ADR,前列腺癌PC-3he,结肠癌HT-116的IC50值都低于10 μg/mL.表明西松烷二萜类化合物是该丛柳珊瑚E.rhipidalis的主要活性化合物类型之一.     

羊脆木的化学成分研究(Ⅰ)

在细胞毒试验结果指导下,采用萃取、柱层析、重结晶等方法,同步对羊脆木(Pittosporum kerrii Craib)枝叶粗提物的有效部位进行化学成分分离纯化得6个单体,通过波谱分析鉴定了结构,分别是α-菠甾醇(α-spinasterol,1),β-豆甾醇(β-stigmasterol,2),熊果醇(uvaol,3),α-菠甾醇-3-O-β-D-吡喃葡萄糖甙(α-spinasterol-3-O-β-D-glucopyranoside,4),β-豆甾醇-3-O-β-D-吡喃葡萄糖甙(β-stigmasterol-3-O-β-D-glucopyranoside,5),木犀草素(luteolin,6).化合物1～6均为首次从该植物中分离得到.细胞毒试验表明氯仿及乙酸乙酯提取物,以及从其中分离出来的化合物1、3、6具有细胞毒活性,对HL60细胞的IC50分别为6.5,5.0,10.0,9.5μg/mL和6.0μg/mL.     

碳酸钙材料对HL-7702细胞的体外毒性

以人正常肝细胞HL-7702为研究对象,探讨碳酸钙材料对细胞的体外毒性.将HL-7702细胞暴露于碳酸钙质量浓度为0、5、10、20、40、60、80、100 μg/mL的悬浮液中,通过CCK-8法检测暴露于碳酸钙材料悬浮液24 h后HL-7702细胞的存活率,并且检测HL-7702细胞内活性氧的含量.结果表明,该碳酸钙材料在实验剂量下对HL-7702无细胞毒性,能够引起人肝细胞内产生少量的活性氧(ROS).这些结果说明碳酸钙材料在一定剂量下对HL-7702细胞具有良好的体外细胞亲和性(毒性为0级或1级).     

Modulation of natural killer cell cytotoxicity and cytokine release by the drug glatiramer acetate

Glatiramer acetate (GA or Copaxone) is a drug used to treat experimental autoimmune encephalomyelitis in mice and multiple sclerosis in human. Here, we describe a new mechanism of action for this drug. GA enhanced the cytolysis of human NK cells against autologous and allogeneic immature and mature monocyte-derived dendritic cells (DCs). This drug reduced the percentages of mature DCs expressing CD80, CD83, HLA-DR or HLA-I. In contrast, it did not modulate the percentages of NK cells expressing NKG2D, NKp30, or NKp44. Nonetheless, anti-NKp30 or anti-CD86 inhibited GA-enhanced human NK cell lysis of immature DCs. Hence, CD86, and NKp30 are important for NK cell lysis of immature DCs, whereas CD80, CD83, HLA-DR and HLA-I are important for the lysis of mature DCs when GA is used as a stimulus. Further, GA inhibited the release of IFN-γ 24 h but increased the release of TNF-α 48 h after incubation with NK cells. Received 13 November 2008; received after revision 10 February 2009; accepted 18 February 2009