异鸟苷掺入的富鸟嘌呤寡核苷酸的合成

目的改进异鸟苷单体的合成路线,合成异鸟苷掺入的富鸟嘌呤的寡核苷酸.方法以6-O-苄基鸟嘌呤为原料,经环氧开环、催化氢化、水解还原制备异鸟苷,经多步反应后得到异鸟苷亚磷酰化产物,采用固相合成方法合成异鸟苷掺入的富含鸟嘌呤的寡核苷酸.结果与结论经环氧开环能够区域选择性地得到N9取代的单一产物,收率提高到40%,并成功地合成了异鸟苷掺入的富含嘌呤十六聚寡核苷酸.本合成路线具有区域选择性强、路线简单、易操作、收率高等优点.     

许树化学成分研究

目的研究许树Clerodendrum inerme的化学成分。方法利用硅胶柱色谱进行分离和纯化,通过光谱分析鉴定结构。结果分离到8个化合物,鉴定为木栓酮(friedelin,Ⅰ)、豆甾醇(stigmasterol,Ⅱ)、白桦酸(betulinicacid,Ⅲ)、金合欢素(acacetin,Ⅲ)、丁香酸(syringicacid,Ⅳ)、对甲氧基苯甲酸(Ⅴ)、芹菜素(apigenin,Ⅵ)和胡萝卜苷(daucosterol,Ⅶ)。结论化合物Ⅱ、Ⅲ、Ⅳ、Ⅳ、Ⅶ为首次从该植物中分离得到。     

Epitopes of human brain acetylcholinesterase

The main purpose of the present work was to identify B-cell epitopes on human brain acetylcholinesterase (AChE) by the synthetic peptide approach. Five hundred and seventy-four decapeptides comprising amino acids No. n to n+9 (where n denotes the residue number of the 583 amino acids in the primary structure of human brain AChE and is an integer in the range 1-574) were synthesized, using the multipin combinatorial chemical synthesis technique, and biotinylated. Epitopes of human brain AChE were detected by enzyme-linked immunosorbent assay (ELISA) and compared with the predicted epitopes of human AChE by 'Goldkey' software. Among 574 synthetic decapeptides, 47 decapeptides at 11 antigenic regions showed immunoreactivity with mouse anti-human brain AChE polyclonal antibodies. The minimum sequence of epitope was defined at every antigenic region explored. The locations and sequences of the former ten continuous epitopes at the 11 antigenic regions of the human brain AChE had been identified as follows: TPVLVWIY (112-119), RTVLVSMNY (143-151), LLDQRLALQW (173-182), RRATQLAH (246-253), VFRFSFVPV (294 approximately 302), KDEGSYFLVY (332-341), RVYA (424-427), LMRY (476-479), KAPQWPPY (496-503), GLRAQACAFW (523-532). The rate of hits of the predicted epitopes from the software came out at 33%. In our work, the epitopes of human AChE have been mapped by purified polyclonal antibody at eleven distinct sites in the primary structure.     

曲靖市某磷酸盐厂"三废"中的氟对周围人群健康的影响

目的了解曲靖市某磷酸盐厂排出“三废”中的氟对周围人群影响情况。方法当地疾病控制与监督部门于1998年对该厂周围的虹桥、耿屯、望城、螃蟹坡4个村人群进行随机抽样调查。结果尿氟>3 mg/L检出率分别为1.72%、23.44%、33.33%,16.13%。发现低年龄组患氟斑牙比较严重,4个村检出率分别为45.16%、64.52%、72.73%、81.25%,而高年龄组患氟骨症比较明显。结论有关部门必须加强对该厂废气排放的管理。     

基于UHPLC-QqQ-MS的四逆散水提液中16种主要化学成分的定量研究

目的 建立同时测定四逆散水提液中16种化学成分含量的方法。方法 应用UHPLC-QqQ-MS技术,采用负离子模式进行扫描,以MRM配对离子方式进行定量。结果 柴胡皂苷A、柴胡皂苷B₂、柴胡皂苷C、柴胡皂苷D、橙皮素、儿茶素、甘草苷、甘草酸、甘草素、绿原酸、没食子酸、芍药苷、芍药内酯苷、异甘草素、异绿原酸A、橙皮苷在负离子模式下响应良好。结论 本实验所建立的同时测定四逆散水提液中16种化学成分含量的分析方法专属性强、快速、灵敏且准确可靠,在完成含量测定的同时又可以准确给出化合物质量数信息,从而达到成分鉴别的效果,该方法可以为四逆散水提液的全面质量控制提供技术支持。      

Structural Study of Sulfur-Added Carbon Nanohorns

In the past few decades, nanostructured carbons (NCs) have been investigated for their interesting properties, which are attractive for a wide range of applications in electronic devices, energy systems, sensors, and support materials. One approach to improving the properties of NCs is to dope them with various heteroatoms. This work describes the synthesis and study of sulfur-added carbon nanohorns (S-CNH). Synthesis of S-CNH was carried out by modified chemical vapor deposition (m-CVD) using toluene and thiophene as carbon and sulfur sources, respectively. Some parameters such as the temperature of synthesis and carrier gas flow rates were modified to determine their effect on the properties of S-CNH. High-resolution scanning and transmission electron microscopy analysis showed the presence of hollow horn-type carbon nanostructures with lengths between 1 to 3 µm and, diameters that are in the range of 50 to 200 nm. Two types of carbon layers were observed, with rough outer layers and smooth inner layers. The surface textural properties are attributed to the defects induced by the sulfur intercalated into the lattice or bonded with the carbon. The XRD patterns and X-ray microanalysis studies show that iron serves as the seed for carbon nanohorn growth and iron sulfide is formed during synthesis.     

虎杖提取工艺初探

对乙肝康君虎杖进行单方水提、复方水提及７０％醇提工艺比较，结果７０％醇提，总蒽酯提取率为９６．７％，大黄素提取率为９６．１％，但经回收酒精，浓缩，干燥后，总蒽酯保留率为６８．９％，大黄素保留率为６５．６％。     

Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre

As the so-called “next frontier” in global economic terms, Africa’s disease burden continues to choke and cripple economic growth across the continent. The highest burden is attributable to malaria and tuberculosis (TB), which also remain among the deadliest infectious diseases affecting mankind the world over (Malaria, 627,000 deaths; TB, 1.5 million deaths, in 2020). In achieving self-determination with respect to the health needs of all who live on the continent, Africa must align with global north efforts and be a source of health innovation. This will in part require the creation of an ecosystem of innovative pharmaceutical R&D and expanding it across the continent by scaling up through sustained performance and excellence. To this end, the Holistic Drug Discovery and Development (H3D) Centre at University of Cape Town in South Africa has risen to this challenge. Here, we highlight the innovation experiences gained at H3D, covering the advances made in our quest to contribute to a global pipeline of therapeutic interventions against malaria and TB. We discuss selected chemical series starting from their identification, structure–activity relationships, mode of action, safety, proof-of-concept studies, and lessons learned.     

春根藤化学成分的研究(Ⅱ)

目的 :探讨春根藤的化学成分。方法 :柱色谱分离 ,波谱及单晶X衍射分析鉴定结构。结果 :分离鉴定了8个化合物 ,为bauerenyl acetate(18) ,东莨菪素(19) ,liriodendrin(20) ,松脂醇 2-氧-β-D-葡萄糖苷(21) ,胡萝卜苷 (22) ,白瑞素 (23) ,七叶素(24)和七叶苷(25)。结论 :8个化合物均系首次从该植物中分得 ,化合物 20 ,21,23～25系首次从该属植物中分得 ,bauerenyl acetate为新的天然产物。     

淡黄香茶菜地下部位化学成分

目的: 研究淡黄香茶菜Isodon flavida地下部分的主要化学成分. 方法: 采用硅胶、葡聚糖凝胶Sephadex LH-20,MCI 树脂等多种柱色谱技术进行分离纯化,运用理化性质和现代波谱技术鉴定结构. 结果: 从淡黄香茶菜地下部分的70%丙酮提取物的乙酸乙酯部位分离鉴定11个化合物,分别为角鲨烯(1),豆甾-4-烯-3-酮(2),豆甾-4-烯-3,6-二酮(3),8(17),13-ent-labdadien-15→16-lactone-19-oic acid(4),1-油酸单甘油酯(5),2α-羟基-乌索酸(6),山楂酸(7),2α,3α,23-三羟基乌苏-12,20(30)-二烯-28-酸(8),豆甾醇(9),7α-羟基谷甾醇(10),β-谷甾醇(11). 结论: 除化合物7外均为首次从该植物中分离得到.本研究对于深入了解认识香茶菜属植物地下部分的化学品质具有一定的帮助.