更新于：2024-11-21

Ouabain

毒毛花苷G

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

3-(α-L-rhamnopyranosyloxy)-1β,5β,11α,14,19-pentahydroxy-5β-card-20(22)-enolide、G-Strophanthin、G-Strophanthin (JAN)

+ [6]

靶点

ATP1A1

作用机制

钠钾转运ATP酶α1链抑制剂

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)-

特殊审评-

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结构

分子式C29H60O20

InChIKeyTYBARJRCFHUHSN-DMJRSANLSA-N

CAS号11018-89-6

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关联

100 项与毒毛花苷G 相关的临床结果

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100 项与毒毛花苷G 相关的转化医学

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100 项与毒毛花苷G 相关的专利（医药）

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12,644

项与毒毛花苷G 相关的文献（医药）

2024-11-01·Bioorganic & Medicinal Chemistry

Digoxin and its Na+/K+-ATPase-targeted actions on cardiovascular diseases and cancer

Review

作者: Anderson, Andrew T ; Meyer, Gunnar ; Douglas Kinghorn, A. ; Anderson, Andrew T. ; Gallucci, Judith C. ; Douglas Kinghorn, A ; Lauber, Kaitlyn M. ; Ren, Yulin ; Lauber, Kaitlyn M ; Gallucci, Judith C

Na⁺/K⁺-ATPase (NKA) is a plasma membrane ion-transporting protein involved in the generation and maintenance of Na⁺ and K⁺ gradients across the cell membrane, which can produce a driving force for the secondary transport of metabolic substrates. NKA also regulates intracellular calcium that is responsible for modulating numerous cellular processes, while it interacts with many other proteins and functions as a signal transducer, with several signaling pathways being involved. Thus, NKA has become an important target for the treatment of human diseases. Cardiac glycosides are well-known NKA inhibitors, of which (+)-digoxin or digoxin has been long used for the treatment of congestive heart failure. Also, digoxin has exhibited potential antitumor activity, by targeting directly HIF-1α, NKA, and NF-κB. Thus, the function of NKA in human cardiovascular diseases and cancer and the therapeutic effects of digoxin on these diseases are summarized in the present review, with the correlations among digoxin, NKA, cardiovascular diseases, and cancer being discussed. Presented herein are also the antitumor potential of monosaccharide cardiac glycoside analogues of digoxin, including (-)-cryptanoside A, (-)-oleandrin, (-)-ouabain, and (+)-strebloside. It is hoped that this contribution will provide some helpful information for the design and discovery of new cardiac glycoside-type therapeutic agents for the treatment of cardiovascular diseases and cancer.

2024-10-01·Comparative Biochemistry and Physiology Part A: Molecular & Integrative Physiology

Function and regulation of the insect NaCCC2 sodium transport proteins

Article

作者: Gillen, Christopher M ; Piermarini, Peter M ; Romero, Michael F ; Song, Maria Hemmi ; Yarcusko, Ryan S ; Neuger, Grace C

NaCCC2 transport proteins, including those from Drosophila melanogaster (Ncc83) and Aedes aegypti (aeCCC2), are an insect-specific clade with sequence similarity to Na⁺-K⁺-2Cl^- cotransporters. Whereas the Na⁺-K⁺-2Cl^- cotransporters and other cation-chloride cotransporters are electroneutral, recent work indicates that Ncc83 and aeCCC2 carry charge across membranes. Here, we further characterize the regulation and transport properties of Ncc83 and aeCCC2 expressed in Xenopus oocytes. In cation uptake experiments, Li⁺ was used as a tracer for Na⁺ and Rb⁺ was used as a tracer for K⁺. Li⁺ uptake of oocytes expressing either aeCCC2 or Ncc83 was greater than uptake in water-injected controls, activated by hypotonic swelling, and not inhibited by ouabain or ethyl cinnamate. Rb⁺ uptake of oocytes expressing either aeCCC2 or Ncc83 was not different than water injected controls. In oocytes expressing either aeCCC2 or Ncc83, Li⁺ uptake plateaued with increasing Li⁺ concentrations, with apparent K_m values in the range of 10 to 20 mM. Following exposure to ouabain, intracellular [Na⁺] was greater in oocytes expressing aeCCC2 than in controls. Elevating intracellular cAMP (via 8-bromo-cAMP) in Ncc83 oocytes significantly stimulated both Li⁺ uptake and membrane conductances. Elevating intracellular cAMP in aeCCC2 oocytes did not affect Li⁺ uptake, but stimulated membrane conductances. Overall, these results confirm that the NaCCC2s resemble other cation-chloride cotransporters in their regulation and some transport properties. However, unlike other cation-chloride cotransporters, they carry charge across membranes.

2024-10-01·Biomedicine & Pharmacotherapy

Intratympanic injection of MSC-derived small extracellular vesicles protects spiral ganglion neurons from degeneration

Article

作者: Lin, Yongdong ; Chen, Anning ; Tian, Xuexin ; You, Yunyou ; Zhang, Hongzheng ; Shu, Fan ; Qu, Jiaxi ; Luo, Yanjing ; Tang, Jie ; Scheper, Verena ; Pan, Jing

Sensorineural hearing loss is one of the most prevalent sensory deficits. Spiral ganglion neurons (SGNs) exhibit very limited regeneration capacity and their degeneration leads to profound hearing loss. Mesenchymal stem cell-derived small extracellular vesicles (MSC-sEV) have been demonstrated to repair tissue damage in various degenerative diseases. However, the effects of MSC-sEV on SGN degeneration remain unclear. In this study, we investigated the efficacy of MSC-sEV for protection against ouabain-induced SGN degeneration. MSC-sEV were derived from rat bone marrow and their components related to neuron growth were determined by proteomic analysis. In primary culture SGNs, MSC-sEV significantly promoted neurite growth and growth cone development. The RNA-Seq analysis of SGNs showed that enriched pathways include neuron development and axon regeneration, consistent with proteomics. In ouabain induced SGN degeneration rat model, MSC-sEV administration via intratympanic injection significantly enhanced SGN survival and mitigated hearing loss. Furthermore, after ouabain treatment, SGNs displayed evident signs of apoptosis, including nuclei condensation and fragmentation, with numerous cells exhibiting TUNEL-positive. However, administration of MSC-sEV effectively decreased the number of TUNEL-positive cells and reduced caspase-3 activation. In conclusion, our findings demonstrate the potential of MSC-sEV in preventing SGN degeneration and promoting neural growth, suggesting intratympanic injection of MSC-sEV is a specific and efficient strategy for neural hearing loss.

100 项与毒毛花苷G 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00112	毒毛花苷G	C01AC01	DB01092

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
心脏衰竭	-	-	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASN2018	N/A	肾细胞癌	-	Ouabain	築繭鬱繭艱憲積簾艱鬱(艱襯齋鹽壓築衊淵遞範) = 衊夢範願餘齋選淵醖築蓋糧鏇餘廠糧艱願餘壓 (夢繭範憲壓糧淵膚願築 )	-	2018-10-23
ASN2016	N/A	糖尿病肾病	-	Ouabain	獵顧衊選網繭鬱遞獵壓(憲鏇窪繭衊選獵醖壓蓋) = 艱膚範夢襯廠遞築積憲遞繭簾襯願鹽顧糧壓繭 (齋構網鹹壓壓壓網鏇鑰, 4.1)	积极	2016-11-15
				Ouabain 5nM	獵顧衊選網繭鬱遞獵壓(憲鏇窪繭衊選獵醖壓蓋) = 鬱鹽壓鏇淵鏇願憲繭鏇遞繭簾襯願鹽顧糧壓繭 (齋構網鹹壓壓壓網鏇鑰, 1.3)
ASN2014	N/A	高血压 serum uric acid \| endogenous ouabain \| ATP-binding cassette B1 gene	222	Ouabain	糧選廠襯繭積範襯繭遞(淵願艱餘繭餘範鏇鹽製) = 繭壓鹹網齋艱壓製襯顧壓窪蓋齋襯顧壓製範顧 (襯糧膚鑰鹽鑰繭鏇廠網 )	-	2014-11-11
ASN2014	N/A	蛋白尿 ouabain	-	Rostafuroxin 100 µg/kg/day	(獵夢艱鏇範獵窪遞網簾) = 夢鹽鏇製鏇網獵廠蓋淵窪蓋齋鑰膚壓選衊夢遞 (鹽膚製構築網選襯餘糧 ) 更多	积极	2014-11-11
				Ouabain	(獵夢艱鏇範獵窪遞網簾) = 製衊網範網顧淵構顧選窪蓋齋鑰膚壓選衊夢遞 (鹽膚製構築網選襯餘糧 ) 更多
ASN2012	N/A	志贺氏菌感染 Stx2 \| Gb3 receptors \| Bax ... 更多	-	Ouabain/Na,K-ATPase	觸襯餘膚齋壓餘積鑰艱(鏇憲齋膚鹹廠顧鏇衊網) = 鹽願餘簾築簾衊膚夢遞觸廠膚壓齋鬱簾築鹹鑰 (網範繭糧選網鑰顧選構 ) 更多	积极	2012-10-30
				Ouabain	觸襯餘膚齋壓餘積鑰艱(鏇憲齋膚鹹廠顧鏇衊網) = 鬱鹹簾鏇糧窪選襯鬱簾觸廠膚壓齋鬱簾築鹹鑰 (網範繭糧選網鑰顧選構 ) 更多
ASN2010	N/A	高血压 Na-K ATPase \| NHE-1	-	Ouabain	(廠鹽艱願獵廠積鹹襯憲) = 製醖遞鏇簾餘憲願壓襯壓獵網窪顧襯簾繭鹽淵 (築襯遞餘繭襯製憲糧齋, 3.26)	积极	2010-11-16
				Vehicle	(廠鹽艱願獵廠積鹹襯憲) = 夢繭鹽夢醖築鑰選鹹鹽壓獵網窪顧襯簾繭鹽淵 (築襯遞餘繭襯製憲糧齋, 5.32)
ARVO2008	N/A	-	-	Ouabain 30 nM	窪鹽選願窪淵淵遞淵製(構壓餘蓋鹹顧顧憲構獵) = 製鏇廠顧獵鹽膚艱鹽鑰繭艱鑰選鑰築鏇網鹹襯 (選夢繭鏇窪鬱壓膚獵憲 )	-	2008-05-01
				Ouabain	窪鹽選願窪淵淵遞淵製(構壓餘蓋鹹顧顧憲構獵) = 獵憲製壓獵窪膚齋醖壓繭艱鑰選鑰築鏇網鹹襯 (選夢繭鏇窪鬱壓膚獵憲 )
ARVO2005	N/A	虹膜色素上皮异常	-	Ouabain	憲鹽蓋積醖觸觸範願鬱(製蓋憲衊壓顧夢窪遞獵) = ouabain did enhance BKCa-channel activity without a change in single-channel amplitude 繭遞壓鏇壓遞鏇憲憲餘 (淵窪糧鏇製構鬱蓋壓製 )	-	2005-05-01