更新于：2024-11-21

Strophanthin K

毒毛花苷K

更新于：2024-11-21

概要

概要

基本信息

药物类型

小分子化药

别名-

靶点-

作用机制-

治疗领域

心血管疾病

在研适应症

心脏衰竭

非在研适应症-

原研机构-

在研机构-

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)批准上市

特殊审评-

登录后查看时间轴

关联

100 项与毒毛花苷K 相关的临床结果

登录后查看更多信息

100 项与毒毛花苷K 相关的转化医学

登录后查看更多信息

100 项与毒毛花苷K 相关的专利（医药）

登录后查看更多信息

927

项与毒毛花苷K 相关的文献（医药）

2022-11-04·ChemMedChem

Synthesis and Biological Evaluation of Cardiac Glycosides for Cancer Therapy by Targeting the DNA Damage Response

Article

作者: Zhang, Youwei ; Geng, Xinran ; Gavande, Navnath S. ; Ainembabazi, Diana ; Turchi, John J.

AbstractCardiac glycosides (CGs) are bioactive compounds originally used to treat heart diseases, but recent studies have demonstrated their anticancer activity. We previously demonstrated that Antiaris toxicaria 2 (AT2) possesses anticancer activity in KRAS mutated lung cancers via impinging on the DNA damage response (DDR) pathway. Toward developing this class of molecules for cancer therapy, herein we report a multistep synthetic route utilizing k‐strophanthidin as the initial building block for determination of structure–activity relationships (SARs). A systematic structural design approach was applied that included modifications of the sugar moiety, the glycoside linker, stereochemistry, and lactone ring substitutions to generate a library of O‐glycosides and MeON‐neoglycosides derivatives. These molecules were screened for their anticancer activities and their impact on DDR signaling in KRAS mutant lung cancer cells. These results demonstrate the ability to chemically synthesize CG derivatives and define the SARs to optimize AT2 as a cancer therapeutic.

2019-01-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Erythrofordins D and E, two new cassaine-type diterpenes from Erythrophleum suaveolens

4区 · 医学

Article

作者: Ahalt-Gottholm, Michelle ; O'Keefe, Barry R ; Guo, Liang ; Davis, Myrtle ; Evans, Jason R ; Grkovic, Tanja ; Newman, David J ; Jato, Johnson ; Grothaus, Paul G ; Collins, Jerry M ; Akee, Rhone K ; Hollingshead, Melinda

Two new cassaine-type diterpenoids, namely erythrofordins D (1) and E (2), sourced from a Cameroon collection of Erythrophleum suaveolens were isolated and assessed for anti-tumor activity. In the NCI-60 cancer cell assay, erythrofordins D (1) and E (2) were found to be cytotoxic in the low micro molar ranges with a mean GI₅₀ value of 2.45 and 0.71 µM, mean TGI value of 9.77 and 2.29 µM, and a mean LC₅₀ of 26.92 and 11.48 µM for 1 and 2 respectively. Using the COMPARE algorithm, the new compounds were found to have similar NCI-60 response profiles to the known cardiac glycosides hyrcanoside and strophanthin. In addition, in an assay examining the viability and contractile function in human cardiomyocytes derived from induced pluripotent stem-cells, erythrofordins showed cardiotoxicity effects at concentrations as low as 0.03 µg/mL.

2015-01-01·Angiologiia i sosudistaia khirurgiia = Angiology and vascular surgery

[At the origin of the development of russian angiology (dedicated to the 150 birthday of academician N.P. Kravkov)].

Article

作者: Uzbekova, D G

The article describes scientific activity of outstanding pharmacologist, Academician N.P. Kravkov (1865-1924) on studying dynamics of the vascular system in experiment: Using the method of isolated animal organs of animals, N.P. Kravkov discovered self-maintained periodic contractions of vessels independent of the central nervous system and not associated with cardiac contractions. On isolated animal organs (heart, kidneys, spleen, womb, pancreas and others) specialists of the laboratory of N.P. Kravkov studied vascular reactions and sensitivity of vascular zones to administration of pharmacological agents in normal conditions and on various experimental ''pathological" models. For studying physiology and pharmacology of coronary vessels irrespective of cardiac contractions masking change in their lumen N.P. Kravkov suggested his original method of cardiac arrest by means of administration of strophanthin followed by passing through vessels of the unfunctioning heart solutions of various pharmacological substances. N.P. Kravkov and !{is followers studied alterations in vascular tonicity on isolated organs of cadavers of people who had died of various diseases: tuberculosis, typhoid fever and epidemic typhus, scarlet fever, measles, diphtheria, pneumonia et cet. The scientist believed that studying the functional state of vessels on post-mortem material would make it possible to more precisely and accurately solve the problem of intravital alterations thereof N.P. Kravkov's works on physiology and pathology of'the vascular system served as the basis for the developing clinical discipline, i.e. angiology.

100 项与毒毛花苷K 相关的药物交易

登录后查看更多信息