Analgesic effects of bulleyaconitine A: new advances in research from ion channel targets to clinical translation
Zili Yin, Xinlian Song, Changcheng Zhu, Anguo Hou, Rong Chen
TL;DR
Bulleyaconitine A (BLA) is a plant-derived compound with strong pain-relieving effects and low addiction risk, offering a promising alternative to opioids.
Contribution
The paper reviews recent advances in understanding BLA's mechanisms and strategies to improve its clinical translation.
Findings
BLA blocks sodium channels, activates opioid receptors, and reduces inflammation to relieve various types of pain.
New drug delivery systems and structural modifications are addressing BLA's poor bioavailability and toxicity.
BLA shows potential for treating conditions like visceral hypersensitivity and pain-related anxiety disorders.
Abstract
Chronic pain represents a significant global health concern, posing a severe threat to human wellbeing and affecting up to 20% of the adult population. Bulleyaconitine A (BLA), a diterpenoid alkaloid derived from plants of the Aconitum genus with in the Ranunculaceae family, demonstrates remarkable analgesic properties with a low potential for addiction, thus broad clinical application prospects compared to opioids. Extensive research has elucidated multiple pharmacological mechanisms underlying the analgesic effects of BLA, including state-dependent blockade of voltage-gated sodium channels, activation of the κ-opioid receptor pathway in spinal microglia, and anti-inflammatory immunomodulatory effects through inhibition of the NF-κB pathway. These mechanisms have been validated in various pain models, including neuropathic pain, cancer pain, rheumatoid arthritis pain, and visceral…
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Taxonomy
TopicsPlant-based Medicinal Research · Berberine and alkaloids research · Neuropeptides and Animal Physiology