Biomolecules & Therapeutics  https://doi.org/10.4062/biomolther.2020.004
Repurposing Auranofin, an Anti-Rheumatic Gold Compound, to Treat Acne Vulgaris by Targeting the NLRP3 Inflammasome
Gabsik Yang1,ψ, Seon Joo Lee1, Han Chang Kang1, Yong-Yeon Cho1, Hye Suk Lee1, Christos C. Zouboulis2, Sin-Hee Han3, Kyung-Ho Ma3, Jae-Ki Jang3 and Joo Young Lee1,*
1BK21plus Team, College of Pharmacy, The Catholic University of Korea, Bucheon 14662, Republic of Korea
2Departments of Dermatology, Venereology, Allergology, and Immunology, Dessau Medical Center, Brandenburg Medical School Theodore Fontane, Dessau, Germany
3Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, Rural Development Administration, Eumsung 27709, Republic of Korea
E-mail: joolee@catholic.ac.kr
Tel: +82-2-2164-4095, Fax: +82-2-2164-4059
ψPresent Address
Department of Pharmacology, College of Korean Medicine, Woosuk University, Jeonbuk 55338, Republic of Korea
Received: January 13, 2020; Revised: March 9, 2020; Accepted: March 31, 2020; Published online: April 22, 2020.
© The Korean Society of Applied Pharmacology. All rights reserved.

Abstract
Activation of the NLRP3 inflammasome is critical for host defense as well as the progression of inflammatory diseases through the production of the proinflammatory cytokine IL-1β, which is cleaved by active caspase-1. It has been reported that overactivation of the NLRP3 inflammasome contributes to the development and pathology of acne vulgaris. Therefore, inhibiting activation of the NLRP3 inflammasome may provide a new therapeutic strategy for acne vulgaris. In this study, we investigated whether auranofin, an anti-rheumatoid arthritis agent, inhibited NLRP3 inflammasome activation, thereby effectively treating acne vulgaris. Auranofin suppressed NLRP3 inflammasome activation induced by Propionibacterium acnes, reducing the production of IL-1β in primary mouse macrophages and human sebocytes. In a P. acnes-induced acne mouse model, injection of P. acnes into the ears of mice induced acne symptoms such as redness, swelling, and neutrophil infiltration. Topical application of auranofin (0.5 or 1%) to mouse ears significantly reduced the inflammatory symptoms of acne vulgaris induced by P. acnes injection. Topical application of auranofin led to the downregulation of the NLRP3 inflammasome activated by P. acnes in mouse ear skin. These results show that auranofin inhibits the NLRP3 inflammasome, the activation of which is associated with acne symptoms. The results further suggest that topical application of auranofin could be a new therapeutic strategy for treating acne vulgaris by targeting the NLRP3 inflammasome.
Keywords: Skin disease, Inflammasome, Drug repurposing, Inflammation, Cytokine


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