Hydroxy-α-sanshool has anti-inflammatory and antioxidant effects and affects the NF-κB/STAT3 pathway via TRPV1 in acne

Hydroxy- α-sanshool (HAS), an extract derived from Zanthoxylum plants, possesses anti-inflammatory and antioxidant effects. However, its potential effects on acne have not been reported. In this study, 2% absolute ethanol formulation of HAS was effective in inflammatory rashes in a rabbit ear model of acne, surpassing the performance of 0.1% adapalene and matching the effectiveness of 10% benzoyl peroxide, but with a faster onset of action. HAS effectively inhibited Cutibacterium acnes (C. acnes) growth with a minimum inhibitory concentration of 1.25 mg/mL. HAS could effectively inhibit the expression of reactive oxygen species (ROS), various inflammatory factors, and the activation of NF-κB and STAT3 pathways induced by C. acnes in HaCat and THP-1 cells. HAS's antioxidant and anti-inflammatory effects in acne may be mediated through TRPV1. Notably, 2% HAS lotion alone display efficacy in reducing inflammatory rashes in patients with mild to moderate acne, but studies with large samples are needed.