Novel Anthraquinone-based Derivatives as Potent Inhibitors for Receptor Tyrosine Kinases

The influence of new derivatives of 9,10-anthraquinone with benzoylthiourea, thiazole, triazole and amino acid fragments on the activity of membrane-associated tyrosine kinases was investigated. Inhibitors of protein tyrosine kinase activity of the membrane fraction, as promising agents to search for new potential anticancer agents among the studied compounds, were discovered.     

常润茶服用方法对蒽醌类物质溶出的影响及其通便作用的相关性研究

目的：以常润茶为例研究蒽醌类物质的加水量及浸泡次数等服用方法对有效成分溶出及通便作用的影响。方法：利用紫外分光光度法建立总蒽醌的含量测定方法,利用高效液相色谱法建立番泻苷A、番泻苷B、大黄酸的含量测定方法,考察不同浸泡次数、加水量下常润茶水浸液中有效物质的含量变化。利用洛哌丁胺复制便秘模型进行通便作用的验证并探究常润茶对肠动力及黏液分泌的影响,观察不同浸泡次数、加水量对小鼠小肠推进率、首粒排黑便时间、5 h黑便粒数、粪便含水量以及结肠胃动素(MTL)、促胃液素(GAS)、生长抑素(SS)、P物质(SP)的影响。结果：加水量与蒽醌类物质的溶出正相关,加水60～100倍蒽醌类物质溶出差异不大;浸泡1次可将大部分蒽醌类物质溶出,从第2次浸泡开始,总蒽醌、番泻苷A、番泻苷B、大黄酸的含量均明显减小。动物实验结果显示加水倍数为40倍、60倍、100倍时,常润茶均可有通便作用,未出现腹泻等不良反应,60倍、100倍水量通便作用显著。加水100倍,反复冲泡多次通便作用不优于浸泡1次。结论：本实验为产品的精准应用提供实验依据,对于规范蒽醌类产品具有积极意义。     

黄精根茎及须根中相关成分的分析

目的：黄精根茎与须根相关成分分析。方法：薄层层析法检测。结果：南京地区典精中含有多糖，几乎不含黄酮、蒽醌类化合物。结论：根茎与须根成分基本相同。     

影响大黄提取液中蒽醌含量的条件探讨

本文研究了不同溶媒十种提取方法对大黄提取液中蒽酯含量的影响，按所用溶媒不同分为醇提组和水提组，探讨了不同浓度，提取方法，煎煮时间等因素对提取的影响，结果表明，水提组中大黄后下１０分钟的提取液中蒽醌含量最高，醇提组中８０％提取液中蒽醌含最最高。     

小红参的化学成分研究

小红参的化学成分研究徐晓莹，周金云，方起程（中国医学科学院中国协和医科大学药物研究所，北京１０００５０）小红参（Ｒｕｂｉａｙｕｎｎａｎｅｎｓｉｓ（Ｆｒａｎｃｈ）Ｄｉｅｌｓ）是茜草科茜草属植物云南茜草的根（１）。民间根据小红参有温经通络、活血祛风、软坚...     

茜草总蒽醌的解热镇痛作用

目的　观察茜草总蒽醌的解热镇痛作用。方法　用热板法、电刺激法、扭体法测定茜草总蒽醌 (6 0mg·kg-1灌胃 )对小鼠痛阈值的影响及茜草总蒽醌对伤寒菌苗所致发热家兔的解热作用。结果　多种实验方法均显示茜草总蒽醌明显提高小鼠各时间组的痛阈值 ,并降低伤寒菌苗所致发热家兔的体温。结论　茜草总蒽醌有较强的解热镇痛作用。     

Ruthenium(II) anthraquinone complexes as two-photon luminescent probes for cycling hypoxia imaging in vivo

Recently, cycling hypoxia, with cycles of hypoxia followed by reoxygenation, was found to induce the up-regulation of HIF-1 activity in tumor cells and reduce the success rate of radiotherapy or chemotherapy. Thus, the ability to visualize cycling hypoxia in cells and in vivo is of great significance. To address this critical need, we have developed ruthenium(II) anthraquinone complexes as reversible two-photon luminescent probes; these probes are well suited for selectively and dynamically monitoring cycling hypoxia in live cells. Moreover, the probes can conveniently visualize inner hypoxia in 3D multicellular tumor spheroids and detect repeated cycles of hypoxia-reoxygenation in living zebrafish via two-photon luminescent imaging. The present study provides a powerful luminescent imaging tool for dynamically sensing of cycling hypoxia in vivo.     

肾安提取液对5／6肾切除大鼠肾功能的影响

目的探讨肾安提取液对5／6肾切除大鼠肾功能的影响。方法采用5／6肾切除法制作慢性肾衰竭（CRF）大鼠模型，随机分为7组：正常组、假手术组、模型组、肾安2g／kg组、肾安4g／kg组、肾安8g／kg组及阳性药物尿毒清3．6g／kg对照组，给药疗程2个月。大鼠存活率、体重、血尿素氮（BUN）、血肌酐（SCr）为观察指标。结果给药后2个月，肾安提取液三个剂量组BUN和SCr均明显降低；在降低BUN方面，肾安高剂量组明显优于尿毒清组。结论肾安提取液能降低5／6肾切除大鼠BUN、延缓肾功能。     

中药大黄的生化学研究ⅩⅫ蒽醌衍生物对兔肾髓质Na~+-K~+-ATP酶活性的抑制和利尿作用

家兔实验表明:大黄素、大黄酸以30 mg/kg的剂量灌胃给药,2～4h后尿量、排Na~+和K~+量达最高峰,比对照组明显增多。而芦荟大黄素和大黄酚的作用较弱。大黄素、大黄酸和芦荟大黄素对免肾髓质Na~+-K~+-ATP酶活性有较强的竞争性抑制作用。     

Cytotoxic efficacy of an anthraquinone linked platinum anticancer drug

Platinum complexes are widely used in cancer chemotherapy; however, they are associated with toxicity, high "non-specific" reactivity and relatively poor pharmacokinetic profiles. In particular, their low cellular uptake and rapid metabolic inactivation means that the amount of "active" drug reaching the nuclear compartment is low. Our strategy to facilitate nuclear accumulation was to introduce a hydrophobic anthraquinone (1C3) moiety to the Pt-complex. Anthraquinones are known to readily intercalate into DNA strands and hence, the Pt-1C3 complex may represent an effective system for the delivery of the platinum moiety to nuclear DNA. Efficacy of the complex was determined by measuring the extent and potency of cytotoxicity in comparison to cisplatin and an anthraquinone based anticancer drug, doxorubicin. The Pt-1C3 complex generated higher levels of cytotoxicity than cisplatin, with a potency of 19 +/- 4 microM in the DLD-1 cancer cell line. However, this potency was not significantly different to that of the 1C3 moiety alone. To examine the reason for the apparent lack of platinum related cytotoxicity, the cellular distribution was characterised. Confocal fluorescence microscopy indicated that the Pt-1C3 complex was rapidly sequestered into lysosomes, in contrast to the nuclear localisation of doxorubicin. In addition, there was negligible DNA associated Pt following administration of the novel complex. Thus, the addition of a 1C3 moiety generated sequestration of the complex to lysosomes, thereby preventing localisation to the nucleus.