桃叶珊瑚苷的研究进展

综述了桃叶珊瑚苷在杜仲、车前草等植物中的分布,介绍了桃叶珊瑚苷的生物合成、理化性质及抗氧化、延缓衰老、抗病毒等生物活性,概括了冷浸提取法、醇提铅盐沉淀法、超声波提取法、大孔树脂吸附法等提取纯化方法,比较了硫酸铜-分光光度法、薄层色谱分离-分光光度法、对二甲氨基苯甲醛法、高效液相色谱法等测定方法,展望了桃叶珊瑚苷的应用前景,以期为桃叶珊瑚苷的研究和含桃叶珊瑚苷类药品的生产及开发提供参考。     

实时细胞电子分析技术用于水蛭、三七质量评价的初步研究

采用实时细胞电子分析技术测定水蛭、三七不同样本的时间剂量依赖性细胞反应曲线(TCRPs),对不同产地样本的TCRPs进行分析,并对生物活性强弱进行排序.同时,采用中国药典2010年版中的化学检测法和凝血酶滴定法分别对水蛭、三七各样本进行同步分析,比较不同检测方法得出结果的相关性.可见以实时细胞电子分析技术为基础的细胞生物活性测定结果与另两法所得结果基本一致.说明本技术能反映中药生物活性,有望为中药质量标准研究提供一种新方法.     

一株红树内生真菌Penicillium sp. JY246次级代谢产物及其活性研究

目的 研究一株红树角果木来源内生真菌Penicillium sp. JY246的次级代谢产物及其生物活性。方法 利用硅胶柱层析、Sephadex LH-20凝胶柱层析、半制备HPLC等方法,对该菌发酵产物的乙酸乙酯浸膏进行分离纯化;利用NMR、MS等波谱解析方法以及与文献数据对照,鉴定化合物的结构;通过抗菌和抗虫活性模型对化合物的生物活性进行评价。结果 从内生真菌Penicillium sp. JY246中分离得到12个化合物,分别为7-hydroxy-2-(2-hydroxypropyl)-5-methylchromone (1),(2′S)-2-(propan-2′-ol)-5-hydroxy-benzopyran-4-one (2),2, 3-dihydro-5-hydroxy-2(S)-methyl-4H-1-benzopyran-4-one (3),(11S)-diaprothin (4),questin (5),4-hydroxy-3-prenylbenzoic acid (6),4-methoxy-6-styryl-pyran-2-one (7),(R) 4-hydroxy-2-oxo-1-pyrrolidineacetamide (8),p-hydroxy-benzaldehyde (9),4-hydroxyacetophenone (10),apocynin (11)和1-(2,6-dihydroxyphenyl) ethan-1-one (12)。结论 从内生真菌Penicillium sp. JY246的次级代谢产物中分离得到12个单体化合物,并对所有化合物进行抗菌和抗虫活性测试。结果表明,化合物1, 2, 4和5显示抗细菌活性;化合物4, 5和8对棉铃虫幼虫显示了生长抑制活性。     

川芎及其中成药抗凝血作用测定方法的研究

目的以延长活化部分凝血活酶时间(APTT)为指标,建立定量测定川芎抗凝血作用的方法,评价川芎及其中成药的质量。方法川芎先后用乙醇和水定量提取,以总提取物为供试品,体外测定延长APTT值。家兔心脏取血,制备血浆,加入APTT试剂后,测定凝结时间。以APTT延长率为抗凝血活性的评价指标,用阿魏酸钠标定川芎的延长APTT活性。根据量反应平行线法(2.2)计算川芎的抗凝血活性。并测定了9份川芎药材、饮片及中成药的抗凝血活性。结果阿魏酸钠和川芎总提取物均具有显著的抗凝血活性,且可靠性检验结果成立。阿魏酸钠的给药质量浓度(1~5 mg/m L)与其APTT延长率呈良好的线性关系(r=0.995 5)。供试品重复测定抗凝血活性的RSD为9.34%(n=6),可信限率为15.98%(n=6)。不同川芎样品的抗凝血活性不同,5份川芎药材的抗凝血效价分别为5.431~7.620 U/g,川芎饮片及川芎酒炙饮片分别为5.910、3.017 U/g,通脉颗粒和血府逐瘀丸分别为14.516、29.035 U/g。结论建立的方法能准确测定川芎药材、饮片及其中成药的抗凝血活性并评价其质量。     

Mechanical and biological properties of photocurable oligolactide-HA composites investigated under accelerated degradation

The major concern related to biodegradable bone substitute materials is the loss of mechanical strength which can be undesirable when occurring too quickly before new bone formation. In this study, the multifunctional lactide oligomers having 2, 3, and 4 arms end capped with methacrylate groups were synthesized with the aim of improving the degradation properties. Their composites with hydroxyapatite (HA) were photopolymerized and subjected to accelerated degradation at 60 °C. The results showed that increasing number of arms significantly improved thermal and mechanical properties as well as biocompatibility of the composites. All composites although varying in number of arms had similar levels of bone-specific gene expression and calcification indicating their equal bioactivity in supporting bone formation. The high HA content in the composites was proposed to be responsible for enhanced osteoblast response, and this tended to suppress the effects of polymeric structure.     

微量硅掺杂改性羟基磷灰石的制备及对成骨细胞功能活性的影响

目的 研究以硅在天然骨中的含量为掺杂量制备的硅-羟基磷灰石(Si-HA)对成骨细胞活性的影响.方法 以水热法制备微量硅掺杂改性的Si-HA;通过X射线衍射(X-ray diffraction,XRD)及扫描电镜观察材料表面构相;MG63细胞在材料表面分别接种培养1、6、12 h及1、4、7、14 d,通过CCK8方法分别检测MG63细胞在材料表面的黏附、增殖情况;通过DAPI染色法验证CCK8检测细胞黏附数量;并对1、4、7、14 d成骨细胞碱性磷酸酶(ALP)活性进行检测;采用RT-PCR检测成骨细胞特异性基因ALP、Ⅰ型胶原(Col-Ⅰ)、骨钙素(OC)在1、4、7、14 d的表达.结果 Si的掺杂未改变HA表面结构及组成;MG63细胞在材料表面培养6、12 h,Si-HA表面细胞附着数量明显高于HA表面(P＜0.05);DAPI染色法与CCK8实验结果相同;细胞培养4、7d时,Si-HA较HA表面的增殖细胞数量增多(P＜0.05).细胞培养4、7d时,Si-HA材料表面ALP活性及基因表达高于HA表面(P＜0.05);4、7、14 d时Col-Ⅰ基因在Si-HA表面的表达量明显高于HA表面(P＜0.05).7、14 d时,OC基因在Si-HA表面的表达量明显高于HA表面(P＜0.05).结论 以硅在天然骨中的含量为掺杂量的Si-HA能够促进MG63成骨细胞黏附、增殖,上调成骨特异性基因的表达,提高了HA材料的生物学活性.     

Bioactivity guided fractionation of methanolic extract of Terminalia arjuna for its CYP3A and CYP2D inhibition in rat liver microsomes

Terminalia arjuna (T. arjuna) is an Indian medicinal plant belonging to the family Combretaceae and possesses numerous therapeutic activities including its immense cardioprotective activity. In the present work, a methanolic bark extract of T. arjuna was evaluated for CYP3A and CYP2D inhibition potential in rat liver microsomes (RLM). Further, the methanolic bark extract was fractionated successively using increasing polarity solvents starting with petroleum ether, chloroform, ethyl acetate and n‐butanol. The fractions so obtained were also evaluated for their CYP3A and CYP2D inhibition potential. Probe substrates testosterone and dextromethorphan were used for CYP3A and CYP2D respectively. The IC₅₀ values for the methanolic extract and the fractions were found to be less than 50 μg/ml in RLM for both CYP3A and CYP2D isoenzymes. The most potent n‐butanol fraction was further fractionated with column chromatography to isolate the highest active constituent responsible for the activity. Fraction 4 of the n‐butanol extract was the most potent fraction with IC₅₀ values of 5.64 ± 0.735 μg/ml and 16.63 ± 0.879 μg/ml for CYP3A and CYP2D in RLM, respectively. Therefore, in vitro data indicated that the Terminalia arjuna extract contains constituents that can potentially inhibit the CYP3A and CYP2D isoenzymes which may in turn lead to pharmacokinetic drug–herb interaction.     

一株西沙来源软珊瑚共附生真菌Penicillium citrinum（15XS112ZM-18）次级代谢产物及其活性研究

目的 研究1株中国西沙群岛永兴岛海域短指软珊瑚Sinularia cf. molesta共附生真菌Penicillium citrinum (15XS112ZM-18)的次级代谢产物及其生物活性。方法 利用TLC、硅胶柱层析、Sephadex LH-20凝胶柱层析、MPLC、半制备HPLC等方法,对菌株代谢物进行分离纯化;通过1H NMR及13C NMR等波谱学方法,结合相关文献数据,鉴定化合物结构;通过细胞毒活性模型评价化合物抗肿瘤活性。结果 从真菌P. citrinum (15XS112ZM-18)代谢产物中分离得到8个化合物,分别为：penicillenol A1 (1),penicillenol A2 (2),penicillenol B1 (3),penicillenol B2 (4),sorbicillin (5),2",3"-dihydrosorbicillin (6),ergosterol (7)和25–Hydroxyergosta-4,6,8(14),22-tetraen-3-one (8),其中化合物4在30 μmol L-1浓度下对HL-60细胞的抑制率达到100%,其IC50值为22.97 μmol L-1。     

多重靶向的4-取代苯胺喹唑啉类衍生物抗肿瘤活性研究进展

4-取代苯胺喹唑啉类化合物是喹唑啉类酪氨酸激酶抑制剂中活性较高的一类化合物,其对表皮生长因子受体、血管内皮生长因子受体、组蛋白去乙酰化酶等均有抑制作用,已成为抗肿瘤药物的研究热点。综述了近几年多重靶向的4-取代苯胺喹唑啉类化合物抗肿瘤活性的研究进展。     

Two new 12-membered macrolides from the endophytic fungal strain Cladosprium colocasiae A801 of Callistemon viminalis

Two new polyketide metabolites, the 12-membered macrolides 4-hydroxy-12-methyloxacyclododecane-2,5,6-trione (1) and 12-methyloxacyclododecane-2,5,6-trione (2), were isolated from the endophytic fungal strain Cladosprium colocasiae A801 of the plant Callistemon viminalis, together with five known derivatives. Their structures were fully characterized by means of detailed spectroscopic analysis for new structures, and in comparison with published data for known compounds. The antibacterial, cytotoxic, and α-glucosidase inhibitory activities of the new compounds 1 and 2 were evaluated.