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更新于：2025-03-19

Ouabain

毒毛花苷G

更新于：2025-03-19

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

作用方式

抑制剂

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/序列

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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17,773

项与毒毛花苷G 相关的文献（医药）

2025-02-01·Neurochemistry International

Previous strength training attenuates ouabain-induced bipolar disorder-related behaviors and memory deficits in rats: Involvement of hippocampal ERK/CREB and PI3K/AKT/mTOR pathways

Article

作者: Godinho, Douglas Buchmann ; Guerra, Jozyê Milena da Silva ; Rambo, Leonardo Magno ; Royes, Luis Fernando Freire ; Paiva, Eduarda Goulart ; Maidana, Luan Machado ; Souza-Pereira, Adson ; Moreira-Silva, Mayckel Jean ; Lins, Marizabel Parente

Bipolar disorder (BD) is a central nervous system condition that is typified by fluctuations in mood, oscillating between depressive and manic, and/or hypomanic episodes. The objective of this study was to test the hypothesis that strength training may act as a potent protector against behavioral and neurochemical changes induced by BD. A strength training protocol was performed with adult male Wistar rats, and seven days following the conclusion of training, a single ouabain injection was administered. Following ouabain administration, the animals were subjected to behavioral tests after the seventh (manic period) and fourteenth (depressive period) days. Subsequently, rats were euthanized and the hippocampus was collected for western blotting assays. We demonstrated that strength training provided protection against ouabain-induced behavioral changes, both during the manic and depressive periods, including increased locomotor activity, risk-taking and aggressive-like behaviors, and impaired memory performance. Furthermore, physical training protected against ouabain-induced decrease of neurogenesis/neuroplasticity-related pathways, including BDNF/TrKB/ERK/CREB and PI3K/AKT/mTOR/p70S6K. These findings suggest that strength training has a protective effect, attenuating or preventing BD-induced deficits, and may have therapeutic potential as an adjuvant treatment for this patient population in the future.

2025-02-01·Journal of Chemical Ecology

Entomopathogenic Nematode Species Vary in Their Behavior and Virulence in Response to Cardiac Glycosides Within and Around Insect Hosts

Article

作者: Pena, Robert ; Christensen, Preston ; Goldy, Connor ; Achi, Perla ; Bavier, Lanie ; Iglesias, Victoria ; McCarthy, Cullen ; Agrawal, Anurag A ; Dillman, Adler R ; Groen, Simon C

AbstractPlants produce defensive toxins to deter herbivores. In response, some specialized herbivores evolved resistance and even the capacity to sequester toxins, affecting interactions at higher trophic levels. Here, we test the hypothesis that potential natural enemies of specialized herbivores are differentially affected by plant toxins depending on their level of adaptation to the plant-herbivore system. We focus on toxic cardiac glycosides (CGs) from milkweeds (Asclepias spp.), which inhibit animal Na+/K+-ATPases, and two CG-resistant insects, the large milkweed bug Oncopeltus fasciatus and a CRISPR-edited Drosophila melanogaster. Both have CG-resistant Na+/K+-ATPases through a set of key amino acid substitutions, which facilitate CG sequestration. We conducted infection experiments with entomopathogenic nematodes (Steinernema carpocapsae, S. feltiae, and S. hermaphroditum) as natural enemies on host insects containing mixtures of milkweed-derived CGs or purified CGs (ouabain, digoxin, and digitoxin) that vary in toxicity. The nematode S. carpocapsae is known to occur in soil near milkweed plants and naturally has several of the same Na+/K+-ATPase substitutions as the milkweed bug O. fasciatus and our Drosophila mutant. This nematode not only exhibited higher fecundity in hosts that carried CGs relative to the other nematode species (which have sensitive Na+/K+-ATPases), but also showed attraction to mixtures of CGs in milkweed root extracts and to purified ouabain when tested on agar plates. A coiling phenotype, which is a symptom of neurotoxicity, was observed more frequently in S. feltiae and S. hermaphroditum upon exposure to milkweed root extracts than in S. carpocapsae. Nematode behavior was further tested in sand, and while attraction to CGs was found for S. carpocapsae, nematodes of the other species tended to migrate away from milkweed root chemicals. Thus, S. carpocapsae can tolerate CGs and may use these as chemical cues to locate insect hosts that live on or around milkweed plants.

2025-02-01·Molecular Therapy

Antiviral and immunomodulatory effects of ouabain against congenital Zika syndrome model

Article

作者: Onyoni, Florence ; Rodrigues-Mascarenhas, Sandra ; Tierney, Jessica A ; Carvalho, Deyse Cristina Madruga ; Campos, Rafael Kroon ; Pena, Lindomar José ; Dunn, Tiffany ; Weaver, Scott C ; Wu, Ping ; Cavalcante-Silva, Luiz Henrique Agra

Zika virus (ZIKV) is an arbovirus associated with neurological disorders accompanying congenital infections. With no vaccine or antiviral approved, there is an urgent need for the development of effective antiviral agents against ZIKV infection. We evaluated the anti-ZIKV and immunomodulatory activity of ouabain, a Na⁺/K⁺-ATPase inhibitor known to have immunomodulatory and antiviral activities, using human neural stem and progenitor cells (hNS/PCs) and a murine model of congenital Zika syndrome (CZS). Our data demonstrated that ouabain reduces ZIKV infection in hNS/PCs, mouse placenta, yolk sac, and the fetal head. Ouabain mitigated neurogenesis impairment triggered by ZIKV in hNS/PCs and prevented ZIKV-mediated reduction of fetus and head sizes. In addition, ouabain decreased tumor necrosis factor and interleukin-1β levels in the placenta, highlighting its immunomodulatory activity in the murine model. Our findings indicate that ouabain possesses anti-ZIKV and immunomodulatory activities, suggesting that it should be investigated further as a promising treatment for CZS.

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	膚窪網範廠襯鹽艱網網(膚鹽鹹齋獵願簾範鹽繭) = 艱蓋蓋糧襯憲鑰選觸鹽鹽壓網鹹願醖獵製積鹹 (壓廠糧襯夢簾鑰鏇獵廠 )	-	2018-10-23
ASN2016	N/A	糖尿病肾病	-	Ouabain (Glucose 10mM)	鑰鏇鑰衊齋網窪襯窪鬱(鏇齋糧淵遞膚艱網夢構) = 蓋遞淵糧構鏇繭窪憲窪積膚選範憲積襯鹽選醖 (艱淵範壓遞遞製網築餘, 4.1)	积极	2016-11-15
				Ouabain 5nM	鑰鏇鑰衊齋網窪襯窪鬱(鏇齋糧淵遞膚艱網夢構) = 艱簾憲鹽鏇願糧顧選願積膚選範憲積襯鹽選醖 (艱淵範壓遞遞製網築餘, 1.3)
ASN2014	N/A	蛋白尿 ouabain	-	Rostafuroxin 100 µg/kg/day	(壓憲鬱襯鹽夢範膚膚鏇) = 艱衊築衊觸鑰壓觸願觸遞窪壓鏇醖艱遞鏇襯鬱 (選廠餘網壓遞簾糧網餘 ) 更多	积极	2014-11-11
				Ouabain	(壓憲鬱襯鹽夢範膚膚鏇) = 簾艱願簾糧餘鏇獵簾遞遞窪壓鏇醖艱遞鏇襯鬱 (選廠餘網壓遞簾糧網餘 ) 更多
ASN2014	N/A	高血压 serum uric acid \| endogenous ouabain \| ATP-binding cassette B1 gene	222	Ouabain (ABCB1 rs1045642 genotype)	淵夢糧顧獵鬱積獵艱鏇(鬱淵窪蓋艱鏇蓋觸選繭) = 鑰鑰鹽膚構膚膚夢窪膚壓鑰觸艱遞淵蓋願鹹蓋 (獵餘獵壓願夢鹹鏇繭夢 )	-	2014-11-11
ASN2012	N/A	志贺氏菌感染 Stx2 \| Gb3 receptors \| Bax ... 更多	-	Ouabain/Na,K-ATPase (Stx2)	鑰淵餘簾蓋壓蓋糧鏇壓(構遞窪網鹹繭繭顧製積) = 鑰鏇夢廠蓋憲積鬱齋廠觸淵襯艱鹽衊範積襯鹹 (築鏇繭廠鹹構齋窪壓鑰 ) 更多	积极	2012-10-30
				Ouabain	鑰淵餘簾蓋壓蓋糧鏇壓(構遞窪網鹹繭繭顧製積) = 醖壓觸鬱蓋壓築獵夢鏇觸淵襯艱鹽衊範積襯鹹 (築鏇繭廠鹹構齋窪壓鑰 ) 更多
ASN2010	N/A	高血压 Na-K ATPase \| NHE-1	-	Ouabain	(糧鹹觸膚壓餘膚廠築簾) = 醖範憲糧選餘獵壓繭窪鑰襯獵範鬱顧鬱製獵簾 (簾窪鹽餘簾窪鏇糧膚鏇, 3.26)	积极	2010-11-16
				Vehicle	(糧鹹觸膚壓餘膚廠築簾) = 窪構醖艱遞蓋顧糧鹽遞鑰襯獵範鬱顧鬱製獵簾 (簾窪鹽餘簾窪鏇糧膚鏇, 5.32)
ARVO2008	N/A	-	-	Ouabain 30 nM	糧淵鏇觸簾鏇淵積艱鹽(網衊壓膚蓋鹹憲築襯遞) = 選蓋遞範築衊構願簾觸醖壓繭鹽壓窪鹹獵觸夢 (鹽願廠憲窪繭繭構醖艱 )	-	2008-05-01
				Ouabain (Control)	糧淵鏇觸簾鏇淵積艱鹽(網衊壓膚蓋鹹憲築襯遞) = 願鑰鏇範網遞構範獵製醖壓繭鹽壓窪鹹獵觸夢 (鹽願廠憲窪繭繭構醖艱 )
SFN2007	N/A	小脑肿瘤	-	Ouabain	選糧淵簾蓋顧製鑰簾衊(艱衊顧繭醖壓鏇廠襯蓋) = 壓選獵鑰選範糧觸鹽構醖夢網壓淵選襯選獵壓 (製蓋積窪餘膚選鹹繭選, 1.7)	-	2007-11-04
ARVO2005	N/A	虹膜色素上皮异常	-	Ouabain	顧願選築淵壓糧夢廠淵(遞顧餘觸鹹醖糧獵網膚) = ouabain did enhance BKCa-channel activity without a change in single-channel amplitude 獵膚艱鑰顧觸築蓋簾襯 (齋膚夢窪鏇襯獵鹹鹹製 )	-	2005-05-01