ArticleBritish journal of pharmacology2011
Kukoamine B, a novel dual inhibitor of LPS and CpG DNA, is a potential candidate for sepsis treatment.
Article in British journal of pharmacology, 2011. 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, 50 citations in OpenAlex.
- Safety, Tolerability, and Pharmacokinetics of Kukoamine B in Healthy Volunteers: A Randomized, Double-Blind, Placebo-Controlled, Multiple-Dose Phase I Study.Advances in therapy · 2023Trial
- Article
- Pharmacological properties, safety, pharmacokinetic and clinical trials of kukoamine A and B.Inflammopharmacology · 2026Review
- Advances in anti-inflammatory treatment of sepsis-associated acute respiratory distress syndrome.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2025Review
- The Effect of the Root Bark ofAntioxidants (Basel, Switzerland) · 2024Article
- First-in-Human Safety, Tolerability, and Pharmacokinetics of Single-Dose Kukoamine B Mesylate in Healthy Subjects: A Randomized, Double-Blind, Placebo-Controlled Phase I Study.Infectious diseases and therapy · 2024Article
- Mechanism and therapeutic potential of traditional Chinese medicine extracts in sepsis.Frontiers in pharmacology · 2024Review
- Research Progress on Natural Small-Molecule Compounds for the Prevention and Treatment of Sepsis.International journal of molecular sciences · 2023Review
- Quality Control ofMolecules (Basel, Switzerland) · 2022Article
- Signaling pathways and intervention therapies in sepsis.Signal transduction and targeted therapy · 2021Review
- Exposure-Response Modeling to Support Dosing Selection for Phase IIb Development of Kukoamine B in Sepsis Patients.Frontiers in pharmacology · 2021Article
- The Central Role and Possible Mechanisms of Bacterial DNAs in Sepsis Development.Mediators of inflammation · 2020Review
- Anti-Osteoporotic Effects of Kukoamine B Isolated fromInternational journal of molecular sciences · 2019Article
- A Metabolomics Approach to Investigate Kukoamine B-A Potent Natural Product With Anti-diabetic Properties.Frontiers in pharmacology · 2018Article
- Kukoamine B promotes TLR4-independent lipopolysaccharide uptake in murine hepatocytes.Oncotarget · 2016Article
- Modulation of Toll-like receptor signaling in innate immunity by natural products.International immunopharmacology · 2016Review
- Synthetic Human TLR9-LRR11 Peptide Attenuates TLR9 Signaling by Binding to and thus Decreasing Internalization of CpG Oligodeoxynucleotides.International journal of molecular sciences · 2016Article
- A novel role of kukoamine B: Inhibition of the inflammatory response in the livers of lipopolysaccharide-induced septic mice via its unique property of combining with lipopolysaccharide.Experimental and therapeutic medicine · 2015Article
- Therapeutic interventions in sepsis: current and anticipated pharmacological agents.British journal of pharmacology · 2014Review
- Discovery and evaluation of asymmetrical monocarbonyl analogs of curcumin as anti-inflammatory agents.Drug design, development and therapy · 2014Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeLipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA) are important pathogenic molecules for the induction of sepsis, and thus are drug targets for sepsis treatment. The present drugs for treating sepsis act only against either LPS or CpG DNA. Hence, they are not particularly efficient at combating sepsis as the latter two molecules usually cooperate during sepsis. In this study, a natural alkaloid compound kukoamine B (KB) is presented as a potent dual inhibitor for both LPS and CpG DNA. EXPERIMENTAL APPROACH: The affinities of KB for LPS and CpG DNA were assessed using biosensor technology. Direct interaction of KB with LPS and CpG DNA were evaluated using neutralization assays. Selective inhibitory activities of KB on pro-inflammatory signal transduction and cytokine expression induced by LPS and CpG DNA were analysed by cellular assays. Protective effects of KB in a sepsis model in mice were elucidated by determining survival and circulatory LPS and tumour necrosis factor-alpha (TNF-α) concentrations. KEY
resultsKB had high affinities for LPS and CpG DNA. It neutralized LPS and CpG DNA and prevented them from interacting with mouse macrophages. KB selectively inhibited LPS- and CpG DNA-induced signal transduction and expression of pro-inflammatory mediators without interfering with signal pathways or cell viability in macrophages. KB protected mice challenged with heat-killed Escherichia coli, and reduced the circulatory levels of LPS and TNF-α. CONCLUSIONS AND IMPLICATIONS: This is the first report of a novel dual inhibitor of LPS and CpG DNA. KB is worthy of further investigation as a potential candidate to treat sepsis.
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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.