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Identification of Anti-Asthmatic Compounds in Pericarpium Citri Reticulatae and Evaluation of Their Synergistic Effects

Identification of Anti-Asthmatic Compounds in Pericarpium Citri Reticulatae and Evaluation of Their Synergistic Effects

Qian Shi, Ze Liu, Yang Yang, Peng Geng, Yuan-yuan Zhu, Qi Zhang, Fang Bai, Gang Bai

Acta Pharmacol Sin. 2009 May;30(5):567-75.

PMID: 19363516

Abstract:

Aim:
To investigate the anti-asthmatic mechanisms of the traditional Chinese medicine Pericarpium citri reticulatae (PCR).
Methods:
The alkaloid section (AS) of PCR was extracted using an ion exchange resin, separated, and purified into different fractions by semi-preparative HPLC. These fractions were screened for beta2-adrenergic receptor (beta(2)AR) agonistic activity using rat beta(2)AR-transfected CHO-CRE-EGFP cells. AS and its isolated components were characterized by ultra-performance liquid chromatography/quadrupole time-of-flight MS (UPLC/Q-Tof MS) and were evaluated for their spasmolytic and antitussive activities both in vitro and in vivo in a guinea pig model.
Results:
We demonstrated that the AS component responsible for activating beta(2)AR signaling was synephrine. Both AS and synephrine showed significant spasmolytic effects on acetylcholine chloride (ACh)-induced contractions in isolated guinea pig trachea, and they protected against histamine-induced experimental asthma by prolonging the latent period. We further identified stachydrine as the antitussive component that could significantly reduce citric acid-induced coughing. The combination of these two bioactive compounds had a more potent spasmolytic activity in comparison with the single use of synephrine or stachydrine.
Conclusion:
We conclude that synephrine and stachydrine are the key components of AS that mediate asthma relief due to their synergism when used in combination.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP4136372	Stachydrine chloride		4136-37-2	Price

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