Bulleyaconitine A is an alkaloid with analgesic and anti-inflammatory activities. It is found in Aconitum bulleyanum and used for the treatment of chronic pain and rheumatoid arthritis.
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Bulleyaconitine A (BLA) is a diterpenoid alkaloid isolated from Aconitum bulleyanum plants. Bulleyaconitine A preferably blocks tetrodotoxin-sensitive voltage-gated sodium channels in dorsal root ganglion neurons by inhibition of protein kinase C, and the effect is around 600 times more potent in neuropathic animals than in naïve ones. Bulleyaconitine A at 5 nM inhibits the hypersensitivity of dorsal root ganglion neurons in neuropathic rats but has no effect on excitability of dorsal root ganglion neurons in sham group[3]. Bulleyaconitine A was more potent for blocking Nav1.3 and Nav1.7 than Nav1.8 in cell lines. The half maximal inhibitory concentration (IC50) values for resting Nav1.3, Nav1.7, and Nav1.8 were 995.6 ± 139.1 nM, 125.7 ± 18.6 nM, and 151.2 ± 15.4 μM, respectively, which were much higher than those for inactivated Nav1.3 (20.3 ± 3.4 pM), Nav1.7 (132.9 ± 25.5 pM), and Nav1.8 (18.0 ± 2.5 μM)[4]. BLA was effective in inhibiting histamine-dependent and histamine-independent itches[5]. It is also activates PKC-δ/NF-κB to reduce airway inflammation in allergic asthma mice[6].
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