抗疟药青蒿琥酯的研究

综述我国创制的抗疟新药青蒿琥酯的药理与临床应用进展,青蒿琥酯给药后在体内血浆中的浓度远大于体外对恶性疟原虫的最小抑制浓度,临床上清除疟原虫９５％所需时间仅为１６小时,临床应用数千例未见明显的毒副作用;可通过口服,静注,肌注及直肠等多种途径给药,青蒿琥酯的半衰期短,可能有利于延迟抗性的产生。该药已成为对恶性疟有快速治疗效果且耐受性好的抗疟药,现已在亚,非,拉等疟疾流行区被广泛用于治疗各种疟疾,是治疗     

复方蒿甲醚对Beagle犬的长期毒性

给Ｂｅａｇｌｅ犬ｐｏ复方蒿甲醚（蒿甲醚：本芴醇１：６,Ｗ／Ｗ）１１２,５５６,１０００ｍｇ．ｋｇ＾－１．ｋｇ＾－１,ｄ＾－１。第天１次, 取１４ｄ,给药结束后,各级一积少成多样２／３,留１／３继续观察２８ｄ,观测了临床症状和生理指标,血液学,血生化,尿,心电图,眼底及病理组织学,主要毒性反应为１０００ｍｇ．ｋｇ＾－１．ｄ＾－１组给药早期出现网织红细胞降低,心电图Ｑ－Ｔ间期延长,生化检查从中草转氨酶     

Ranbaxy／MMV——治疗疟疾的新希望

目前治疗疟疾最有效的药物青蒿素(artemisinin)(Ⅰ)是合成抗疟药如青蒿琥酯和蒿甲醚的基础，但由于其提取过程昂贵使得治疗费用很高。如果国际科学家小组能够成功开发出一种低廉的合成替代品，那么无疑会是疟疾治疗的突破性进展。     

复方蒿甲醚对Beagle犬的长期毒性

给 Beagle犬 po复方蒿甲醚 (蒿甲醚∶本芴醇 1∶ 6,W/W) 1 1 2 ,556,1 0 0 0 mg· kg-1· d-1,每天 1次 ,连服 1 4d.给药结束后 ,各组活杀 2 /3,留 1 /3继续观察 2 8d.观测了临床症状和生理指标 ,血液学 ,血生化 ,尿 ,心电图 ,眼底及病理组织学 .主要毒性反应为 1 0 0 0 mg·kg-1·d-1组给药早期出现网织红细胞降低 ,骨髓红系细胞的中幼红与早幼红比值降低 ,心电图 Q- T间期延长 ,生化检查谷草转氨酶 ,碱性磷酸酶轻度升高 .组织学检查可见肝 ,肾轻度损伤 .所有上述变化停药后均可恢复正常 . 556mg· kg-1· d-1及以下剂量组未见明显毒副作用 ,可视为基本安全剂量 .     

从青蒿素类抗疟药的开发历程谈创新新药的体会

回顾了青蒿素类抗疟药的开发历程，概括了此类药物的研究现状，畅谈了新药开发的若干体会。     

诺华公司生产的抗疟药安全有效

FDA于2008—12—01发布的文件中确认,诺华AG公司生产的复方抗疟药Coartem（蒿甲醚和本芴醇的复方制剂）有效,而且极少引起严重不良反应。     

蒿甲醚`蒿琥酯及其代谢产物双氢青蒿素在血浆中的薄层扫描定量法

报道了用薄层密度扫描定量法同时测定血浆中蒿甲醚(MDA)和双氢青蒿素(DHA)(A);蒿琥酯(AS)和DHA(B)以及单独测定DHA (C)的分析方法。线性范围除B法中AS为0.1至3.5μg外,余均为0.1至4.0μg(r均大于0.99,p<0.005)。检测限A法均为0.03μg;B、C法均为0.01μg。MDA和DHA平均回收率分别为82.8和92.2％;AS和DHA分别为95.5和89.2％;DHA为96％(c.v.均在6％以内)。并进行了大鼠DHA,MDA和DHA及AS和DHA的药物动力学研究,提供了各自的参数。     

青蒿研究的现状

本品为菊科植物黄花蒿(Artomisia annul L)的干燥地上部分。味苦,辛性寒,有清热解暑,除虱,截疟的功能。主治暑邪发热,阴虚发热,夜热早凉,骨蒸劳热,疟疾寒热和湿热黄疸。中药青蒿载于马王堆出土《五十二病方》,《神农本草经》。晋葛洪《时后备急方》治疟病方载有:“青蒿一握,以水二升渍,绞取汁尽服之。”此后,宋,元,明各作家医籍本草均有以复方“青蒿汤”,“截疟青蒿丸”,“青蒿散”制疟。李时珍亦称青蒿“制疟疾寒热”清代《瘟病条辨》用“青蒿鳖甲煎”“治少阳疟”。民间亦有流传使用。我国南省北诸省如广西,广     

氟喹诺酮类药物研究的新进展

氟喹诺酮类药物是最近十多年迅猛发展的一类全合成抗感染药物，本综述介绍了上海医药工业研究院在这方面的研究与开发以及国际上的新进展。     

我国喹诺酮类抗感染药物的研究进展

对我国近几年喹诺酮类药物研究开发概况、新合成路线与工艺改进、结构改造与构效关系研究进行了简要的述评。     

Artemisinin drugs: novel antimalarial agents

Artemisinin and its derivatives, artesunate and artemether, represent a new class of antimicrobial drug with potent activity against Plasmodium falciparum. Although they show excellent efficacy in both severe and uncomplicated malaria, dosage regimens still need to be optimised and pharmacokinetic profiles defined. In the treatment of uncomplicated malaria, the artemisinin drugs should be used in combination with a long acting antimalarial to protect both drugs against the emergence of resistance. In the treatment of severe malaria, parenteral artemether is at least as effective as quinine and is simpler to use. The use of rectal preparations of artesunate and artemisinin at the rural health level will facilitate early initiation of the treatment of falciparum malaria and this may reduce the proportion of patients progressing to severe disease. All of the artemisinin drugs have comparable efficacy; the choice of derivative should be based upon availability, cost and quality of the preparation. Artemisinin, artesunate and artemether are well-tolerated in both adults and children, with no evidence to date of serious clinical toxicity.     

双膦酸类药物研究进展

综述双膦酸类药物的化学（合成、含水不同的晶型、分类和构效关系）、药理（药效特点、作用机制、药物动力学和毒理）及其治疗骨吸收性疾病（包括变形性骨炎、高钙血症、溶骨性骨转移和骨质疏松症）的进展     

中国千金藤属（Stephania）植物中生物碱类化学成分的研究进展

综述了近年来中国千金藤属植物中生物碱类化学成分的研究成果，为本属植物的深入研究提供有用的资料。     

甲壳素／壳聚糖水解酶的研究进展

甲壳素／壳聚糖水解酶包括甲壳素酶、壳聚糖酶、溶菌酶以及一些非专一性水解酶。本文主要介绍了这些酶的分离纯化、结构鉴定、作用模式、动力学研究、固定化和基因改进等方面的研究现状和最新进展。     

我国喹诺酮类抗感染药物的研究开发进展

对我国喹诺酮类药物已开发产品的概况、新合成路线与工艺改进、结构改造与构效关系研究以及环丙氟啶酸的临床前研究作了较系统的述评。     

RECENT ADVANCES IN RESEARCH ON RADIOFREQUENCY FIELDS AND HEALTH

Since the Royal Society of Canada report on potential health risks of radiofrequency (RF) fields from wireless telecommunications in the spring of 1999, there have been several newly published reports on risks associated with the use of mobile phones. This article provides a summary of scientific research on the potential health effects of radiofrequency fields that has been reported since the original Royal Society report was published. This update also discusses several earlier results not included in the original report.     

mRNA expression profiles for the response of human tumor cell lines to the antimalarial drugs artesunate,arteether, and artemether

The antimalarial artemisinin derivatives artesunate (ART), arteether (ARE), and artemether (ARM) reveal remarkable antineoplastic activity. In the present investigation, we identified mRNA expression profiles associated with the response of tumor cells to ART, ARE, and ARM. We performed correlation and hierarchical cluster analyses of inhibition concentration 50% (IC(50)) values and basal mRNA expression levels of 464 genes deposited in the database of the National Cancer Institute, USA. Correlating IC(50) values of ART, ARE, and ARM and of 16 established antineoplastic drugs revealed that the artemisinin derivatives could not be assigned with a known class of drugs with defined mode(s) of action. The basal mRNA expression of 208 out of 464 genes (45%) correlated significantly with IC(50) values of at least one artemisinin derivative. These genes were from different classes (drug resistance genes, DNA damage and repair genes, apoptosis-regulating genes, proliferation-associated genes, oncogenes, tumor suppressor genes and cytokines). We identified two different gene clusters by hierarchical cluster analysis. One cluster contained predominately genes significantly correlated to all three artemisinin derivatives. This overlapping set of genes points to common molecular mechanisms of tumor inhibition by all three drugs in which genes affecting cellular proliferation may play an important role. The second cluster contained genes differentially associated with the response of artemisinin derivatives to cancer cells. The number of correlating drug resistance genes in this cluster increased in the order ART相似文献