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Acta Pharmacol Sin. 2008 Oct;29(10):1187-94. doi: 10.1111/j.1745-7254.2008.00859.x.

Identification of higenamine in Radix Aconiti Lateralis Preparata as a beta2-adrenergic receptor agonist1.

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College of Life Sciences, Nankai University, Tianjin 300071, China.



To screen beta2-adrenergic receptor (beta2-AR) agonists from Radix Aconiti Lateralis Preparata (RALP) as potential drug leads for asthma using a sensitive cell-based agonist assay.


The beta2-AR gene was stably expressed by Chinese hamster ovary (CHO) cells also stably expressing a cyclic adenosine monophosphate (AMP) response element-linked enhanced green fluorescent protein reporter gene. The cells were used to screen agonists from high-performance liquid chromatographic fractions of an extract of RALP. The fraction with the highest activity was selected for further compound isolation and the study of the structure-activity relationship. Its active compound was further identified by chromatography and mass spectrometry.


Bioactivity-directed fractionation of the crude extract of RALP led to the isolation and characterization of the effective compound, namely hignamine. It could dose-dependently relax the isolated guinea pig trachea strip precontraction with acetylcholine with EC(50) value of (2.60+/-0.36)x10(-5) mol/L. Further in vivo studies also displayed that hignamine could protect experimental asthma model induced by histamine in guinea pigs to prolong the latent periods of asthma.


Hignamine, as a beta2-AR agonist existing in the extract of RALP, is the key compound contributing to the successful relief of the bronchoconstriction.

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