Varenicline, a smoking cessation drug, improves alveolar expansion and inflammation in elastase-induced lung damage

2019 Fiscal Year Final Research Report

• Project/Area Number: 17K08329
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Pharmacology in pharmacy
• Research Institution: Fukuoka University
• Principal Investigator: Koga Mitsuhisa 福岡大学, 薬学部, 准教授 (60570801)
• Co-Investigator(Kenkyū-buntansha): 片岡 泰文 福岡大学, 薬学部, 教授 (70136513) ; 金岡 祐輝 福岡大学, 薬学部, 助教 (80761246)
• Project Period (FY): 2017-04-01 – 2020-03-31
• Keywords: バレンクリン / alpha7 nAChR / COPD

Outline of Final Research Achievements

Smoking cessation is the most effective treatment in patients with chronic obstructive pulmonary disease (COPD). Varenicline, a selective partial agonist of α4β2 nicotinic acetylcholine receptors (nAChRs) and full agonist of α7 nAChRs, is a widely used and effective drug for smoking cessation. The aim of the present study was to examine the effect of varenicline on emphysema in porcine pancreatic elastase (PPE)-inhaled mice. PPE-inhaled mice were treated with varenicline and an α7 nicotinic acetylcholine receptor (nAChR) antagonist, methyllycaconitine (MLA) for 5 and 21 days. varenicline markedly ameliorated PPE-induced alveolar expansion and inflammatory response in bronchoalveolar lavage fluid in PPE-inhaled mice. These blocking effects were blocked by MLA. In conclusion, varenicline likely has an anti-inflammatory property to protect PPE-induced alveolar expansion via α7 nAChR. Varenicline may be useful for patients with COPD and acute-phase inflammatory response of the lung.

Free Research Field

薬学

Academic Significance and Societal Importance of the Research Achievements

エラスターゼを気管内噴霧したモデルマウスを用いて、禁煙補助薬バレニクリンによる肺保護作用を検討した。バレニクリンは、エラスターゼによる肺胞径拡大を抑制し、また気管支洗浄液中の炎症性細胞の数を抑制した。これらの作用は、α7 ニコチン性アセチルコリン受容体を介した作用であることが示唆された。このようにバレニクリンは、禁煙補助薬としてだけでなく、COPDなどの炎症を介した肺疾患にも有効であるかもしれない。