Abstract

Cortex phellodendri is used to reduce fever and remove dampness and toxin. Berberine is an active ingredient of C. phellodendri. Berberine from Argemone ochroleuca can relax airway smooth muscle (ASM); however, whether the nonberberine component of C. phellodendri has similar relaxant action was unclear. An n-butyl alcohol extract of C. phellodendri (NBAECP, nonberberine component) was prepared, which completely inhibits high K+- and acetylcholine- (ACH-) induced precontraction of airway smooth muscle in tracheal rings and lung slices from control and asthmatic mice, respectively. The contraction induced by high K+ was also blocked by nifedipine, a selective blocker of L-type Ca2+ channels. The ACH-induced contraction was partially inhibited by nifedipine and pyrazole 3, an inhibitor of TRPC3 and STIM/Orai channels. Taken together, our data demonstrate that NBAECP can relax ASM by inhibiting L-type Ca2+ channels and TRPC3 and/or STIM/Orai channels, suggesting that NBAECP could be developed to a new drug for relieving bronchospasm.

Highlights

  • Asthma is a common chronic respiratory disease [1]

  • We found that an n-butyl alcohol extract of C. phellodendri (NBAECP, nonberberine component) exerted inhibitory action on airway smooth muscle (ASM) contraction, and the underlying mechanism was investigated

  • These results indicated that NBAECP could inhibit agonist-induced sustained contraction of control and asthmatic ASM

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Summary

Introduction

Asthma is a common chronic respiratory disease [1]. Excessive airway obstruction is a cardinal symptom that results from the contraction of airway smooth muscle (ASM). We attempted to develop an effective and safe drug from bitter Chinese herbs to inhibit ASM contraction. Phellodendron amurense Rupr., which belongs to the group of Rutaceae arbor plants. It is bitter in flavor and cold in nature, categorized in kidney, urinary bladder, and large intestine meridians. The traditional functions are to clear heat, dry dampness, purge fire, and remove toxicity. It is one of fundamental traditional Chinese medicines. Berberine is one active ingredient of C. phellodendri; berberine from Argemone ochroleuca was demonstrated to have a relaxant effect in guinea-pig ASM [12]. Whether the nonberberine component has similar relaxant action has not been investigated

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