Bulleyanin - CAS 123043-54-9
Catalog number: 123043-54-9
Not Intended for Therapeutic Use. For research use only.
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Bulleyanin is a natural diterpenoid found in the herbs of Rabdosia bulleyana, which can be solved in Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
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(1α,3β,5β,7β,8α,9β,10α,11β,12α,13α)-12-Hydroxy-15-oxokaur-16-ene- 1,3,7,11-tetrayl tetraacetate
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1.Bulleyaconitine A isolated from aconitum plant displays long-acting local anesthetic properties in vitro and in vivo.
Wang CF;Gerner P;Wang SY;Wang GK Anesthesiology. 2007 Jul;107(1):82-90.
BACKGROUND: ;Bulleyaconitine A (BLA) is an active ingredient of Aconitum bulleyanum plants. BLA has been approved for the treatment of chronic pain and rheumatoid arthritis in China, but its underlying mechanism remains unclear.;METHODS: ;The authors examined (1) the effects of BLA on neuronal voltage-gated Na channels in vitro under the whole cell patch clamp configuration and (2) the sensory and motor functions of rat sciatic nerve after single BLA injections in vivo.;RESULTS: ;BLA at 10 microm did not affect neuronal Na currents in clonal GH3 cells when stimulated infrequently to +50 mV. When stimulated at 2 Hz for 1,000 pulses (+50 mV for 4 ms), BLA reduced the peak Na currents by more than 90%. This use-dependent reduction of Na currents by BLA reversed little after washing. Single injections of BLA (0.2 ml at 0.375 mm) into the rat sciatic notch not only blocked sensory and motor functions of the sciatic nerve but also induced hyperexcitability, followed by sedation, arrhythmia, and respiratory distress. When BLA at 0.375 mm was coinjected with 2% lidocaine (approximately 80 mm) or epinephrine (1:100,000) to reduce drug absorption by the bloodstream, the sensory and motor functions of the sciatic nerve remained fully blocked for approximately 4 h and regressed completely after approximately 7 h, with minimal systemic effects.
2.Studies on metabolites and metabolic pathways of bulleyaconitine A in rat liver microsomes using LC-MS(n) combined with specific inhibitors.
Bi Y;Zhuang X;Zhu H;Song F;Liu Z;Liu S Biomed Chromatogr. 2015 Jul;29(7):1027-34. doi: 10.1002/bmc.3388. Epub 2014 Nov 26.
Bulleyaconitine A (BLA) from Aconitum bulleyanum plants is usually used as anti-inflammatory drug in some Asian countries. It has a variety of bioactivities, and at the same time some toxicities. Since the bioactivities and toxicities of BLA are closely related to its metabolism, the metabolites and the metabolic pathways of BLA in rat liver microsomes were investigated by HPLC-MS(n). In this research, the 12 metabolites of BLA were identified according to the results of HPLC-MS(n) data and the relevant literature. The results showed that there are multiple metabolites of BLA in rat liver microsomes, including demethylation, deacetylation, dehydrogenation deacetylation and hydroxylation. The major metabolic pathways of BLA in rat liver microsomes were clarified by HPLC-MS combined with specific inhibitors of CYP450 isoforms. As a result, CYP3A and 2C were found to be the principal CYP isoforms contributing to the metabolism of BLA. Moreover, CYP2D6 and 2E1 are also more important CYP isoforms for the metabolism of BLA. While CYP1A2 only affected the formation rate of M11, its effect on the metabolism of BLA is very small.
3.Bulleyaconitine A attenuates hyperexcitability of dorsal root ganglion neurons induced by spared nerve injury: The role of preferably blocking Nav1.7 and Nav1.3 channels.
Xie MX;Yang J;Pang RP;Zeng WA;Ouyang HD;Liu YQ;Liu XG Mol Pain. 2018 Jan-Dec;14:1744806918778491. doi: 10.1177/1744806918778491.
Background Oral administration of Bulleyaconitine A, an extracted diterpenoid alkaloid from Aconitum bulleyanum plants, is effective for treating chronic pain in rats and in human patients, but the underlying mechanisms are poorly understood. Results As the hyperexcitability of dorsal root ganglion neurons resulting from the upregulation of voltage-gated sodium (Nav) channels has been proved critical for development of chronic pain, we tested the effects of Bulleyaconitine A on Nav channels in rat spared nerve injury model of neuropathic pain. We found that Bulleyaconitine A at 5 nM increased the threshold of action potentials and reduced the firing rate of dorsal root ganglion neurons in spared nerve injury rats but not in sham rats. Bulleyaconitine A preferably blocked tetrodotoxin-sensitive Nav channels over tetrodotoxin-resistant ones in dorsal root ganglion neurons of spared nerve injury rats. Bulleyaconitine A was more potent for blocking Nav1.3 and Nav1.7 than Nav1.8 in cell lines. The half maximal inhibitory concentration (IC;50;) 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.
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CAS 123043-54-9 Bulleyanin

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