ArticlePloS one2014
Resibufogenin and cinobufagin activate central neurons through an ouabain-like action.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 48 citations in OpenAlex.
- Resibufogenin promotes angiogenesis via the VAV3-mediated ITGA5-VEGF signaling axis in macrophages to alleviate myocardial infarction.Acta pharmacologica Sinica · 2026Article
- Central toxic effects of an antitumoral bufadienolide: In silico targets and in vivo findings.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Synthesis and Biological Evaluation of RBG Derivatives as Nrf2 Activators for the Treatment of Parkinson's Disease.International journal of molecular sciences · 2026Article
- Cinobufagin as a Potential Intervention Against Liver Cancer-A Comprehensive Review.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Exploring the pharmacological mechanisms of resibufogenin in castration-resistant prostate cancer via network pharmacology and experimental validation.Frontiers in oncology · 2026Article
- Insights into the Therapeutic Use ofPharmaceuticals (Basel, Switzerland) · 2025Review
- Cinobufagin: Unveiling the hidden bufadienolide's promise in combating alimentary canal cancer development and progression - a comprehensive review.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Article
- Resibufogenin: An Emerging Therapeutic Compound with Multifaceted Pharmacological Effects - A Comprehensive Review.Medical science monitor : international medical journal of experimental and clinical research · 2024Review
- Article
- Identification of resibufogenin, a component of toad venom, as a novel senolytic compound in vitro and for potential skin rejuvenation in male mice.Biogerontology · 2023Article
- Toad venom-derived bufadienolides and their therapeutic application in prostate cancers: Current status and future directions.Frontiers in chemistry · 2023Review
- Enhancement of Dissolving Capacity and Reducing Gastric Mucosa Irritation by Complex Formation of Resibufogenin with β-Cyclodextrin or 2-Hydroxypropyl-β-cyclodextrin.Molecules (Basel, Switzerland) · 2022Article
- Resibufogenin Targets the ATP1A1 Signaling Cascade to Induce G2/M Phase Arrest and Inhibit Invasion in Glioma.Frontiers in pharmacology · 2022Article
- Aitongxiao improves pain symptoms of rats with cancer pain by reducing IL-1, TNF-α, and PGE2.International journal of clinical and experimental pathology · 2021Article
- The spinal microglial IL-10/β-endorphin pathway accounts for cinobufagin-induced mechanical antiallodynia in bone cancer pain following activation of α7-nicotinic acetylcholine receptors.Journal of neuroinflammation · 2020Article
- Article
- Cinobufacini promotes apoptosis of bladder cancer cells by influencing the expression of autophagy-related genes.Oncology letters · 2018Article
- Promising galactose-decorated biodegradable poloxamer 188-PLGA diblock copolymer nanoparticles of resibufogenin for enhancing liver cancer therapy.Drug delivery · 2017Article
- Arginine derivatives of dicarboxylic acids from the parotid gland secretions of common toad Bufo bufo-New agonists of ionotropic γ-aminobutyric acid receptors.Doklady. Biochemistry and biophysics · 2017Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Cinobufagin and resibufogenin are two major effective bufadienolides of Chan su (toad venom), which is a Chinese medicine obtained from the skin venom gland of toads and is used as a cardiotonic and central nervous system (CNS) respiratory agent, an analgesic and anesthetic, and as a remedy for ulcers. Many clinical cases showed that Chan su has severe side-effects on the CNS, causing shortness of breath, breathlessness, seizure, coma and cardiac arrhythmia. We used whole-cell recordings from brain slices to determine the effects of bufadienolides on excitability of a principal neuron in main olfactory bulb (MOB), mitral cells (MCs), and the cellular mechanism underlying the excitation. At higher concentrations, cinobufagin and resibufogenin induced irreversible over-excitation of MCs indicating a toxic effect. At lower concentrations, they concentration-dependently increased spontaneous firing rate, depolarized the membrane potential of MCs, and elicited inward currents. The excitatory effects were due to a direct action on MCs rather than an indirect phasic action. Bufadienolides and ouabain had similar effects on firing of MCs which suggested that bufadienolides activated neuron through a ouabain-like effect, most likely by inhibiting Na+/K+-ATPase. The direct action of bufadienolide on brain Na+ channels was tested by recordings from stably Nav1.2-transfected cells. Bufadienolides failed to make significant changes of the main properties of Nav1.2 channels in current amplitude, current-voltage (I-V) relationships, activation and inactivation. Our results suggest that inhibition of Na+/K+-ATPase may be involved in both the pharmacological and toxic effects of bufadienolide-evoked CNS excitation.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.