Chu Simeng, Liu Wenjuan, Lu Yujie, Yan Menglin, Guo Yingying, Chang Nianwei, Jiang Min, Bai Gang
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, China.
Graduate School of Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Front Pharmacol. 2020 May 20;11:723. doi: 10.3389/fphar.2020.00723. eCollection 2020.
Millions of patients suffer from asthma worldwide. However, the first-line drugs used to treat asthma, namely, the beta-adrenergic receptors agonists (β-agonists), are not recommended for use as monotherapy because of their severe dose-related side effects. This limitation has prompted the search for new therapies, which can be used in conjunction with β--agonists so that lower doses can be administered. Sinigrin is a major compound found in many antiasthmatic medicinal plants. In this study, we explored the antiasthmatic activity of sinigrin when used in combination with β-agonists and its underlying mechanism. Sinigrin enhanced the asthma-relieving effects of isoproterenol and reduced the effective isoproterenol dose in an acute-asthma model in guinea pigs. Mechanistically, sinigrin enhanced the cAMP levels induced by β-agonists by inhibiting PDE4. The resulting increase in cAMP levels stimulated the activity of the downstream effector protein kinase A, which would be expected to ultimately induce the relaxation of airway smooth muscle. In conclusion, sinigrin enhances the asthma-relieving effects of β-agonists by regulating the cAMP signaling pathway and represents a potential add-on drug to β-agonists for the treatment of asthma.
全球数以百万计的患者患有哮喘。然而,用于治疗哮喘的一线药物,即β-肾上腺素能受体激动剂(β-激动剂),由于其严重的剂量相关副作用,不建议作为单一疗法使用。这一局限性促使人们寻找新的疗法,这些疗法可以与β-激动剂联合使用,从而能够使用更低的剂量。芥子碱是许多抗哮喘药用植物中发现的主要化合物。在本研究中,我们探究了芥子碱与β-激动剂联合使用时的抗哮喘活性及其潜在机制。在豚鼠急性哮喘模型中,芥子碱增强了异丙肾上腺素的平喘作用,并降低了异丙肾上腺素的有效剂量。从机制上讲,芥子碱通过抑制磷酸二酯酶4(PDE4)提高了β-激动剂诱导的环磷酸腺苷(cAMP)水平。cAMP水平的升高刺激了下游效应蛋白激酶A的活性,这有望最终诱导气道平滑肌舒张。总之,芥子碱通过调节cAMP信号通路增强了β-激动剂的平喘作用,是一种潜在的可与β-激动剂联合用于治疗哮喘的附加药物。