Pharmacology of boldine: summary of the ﬁeld and update on recent advances

Frontiers in Pharmacology, 2024 · DOI: 10.3389/fphar.2024.1427147 · Published: September 13, 2024

Simple Explanation

Boldine, a natural compound found in plants like the Chilean Boldo tree, has shown promise in treating diseases in rodent models. It exhibits antioxidant, neuroprotective, and analgesic properties. Research suggests boldine works by blocking connexin hemichannels (CxHCs), which are involved in various injuries and diseases. This blockade is believed to be the primary mechanism behind boldine's therapeutic effects. This review summarizes the pharmacological properties of boldine, including its effects on rodent models of common human injuries and diseases, as well as its absorption, distribution, pharmacokinetics, and metabolism.

Study Duration

Not specified

Participants

Rodent models of human disease

Evidence Level

Review

Key Findings

1
Boldine blocks connexin (Cx) hemichannels (HCs), and many of its effects in rodent models are attributed to this blockade.
2
Boldine exhibits antioxidant, neuroprotective, anti-inflammatory, cardioprotective, and anticancer properties in rodent models.
3
Boldine has demonstrated efficacy in animal models of nervous system disorders, skeletal muscle diseases, renal disease, gastrointestinal disease, and liver damage.

Research Summary

Boldine is an orally active alkaloid with good tolerability in rodents, showing efficacy across various animal models of disease or injury. Open connexin hemichannels (CxHC) are consistently found in cytoplasmic membranes of cells in diseased tissues, and conditional knockouts of Cx genes in these tissues mimic the effects of boldine. Boldine blocks a cascade of deleterious signals triggered by open CxHC, which includes increased cytosolic calcium, inflammasome activation, and release of ATP and pro-inflammatory mediators.

Practical Implications

Therapeutic Potential

Boldine represents a promising therapeutic agent for various conditions, including nervous system disorders, skeletal muscle diseases, and inflammatory conditions.

Drug Development

Further investigation of boldine's mechanisms and therapeutic applications could lead to the development of new pharmaceuticals.

Disease Understanding

Studying boldine's effects provides insights into the role of connexin hemichannels in various diseases, potentially leading to novel therapeutic strategies.

Study Limitations

1
The review primarily focuses on rodent models, and further research is needed to confirm these findings in humans.
2
The specific mechanisms by which connexin hemichannels appear in the cytoplasmic membrane are not fully understood.
3
While boldine shows good tolerability in rodents, further studies are needed to assess its safety and efficacy in humans.

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