Abstract Background: This is the first multicenter clinical and experimental study of the anti wrinkle efficacy of Argireline in Chinese subjects. Objective: To evaluate the safety and efficacy of Argireline in the treatment of periorbital lines in Chinese subjects, and to observe the effect of Argireline on microstructural changes of the skin in the aged mice induced by D-galactose. Methods: The study was comprised of two parts: i) Clinical study: A total of 60 subjects received a single treatment in a 3:1 randomization ratio of Argireline: placebo. Argireline or placebo was applied to their periorbital wrinkles twice daily for 4 weeks, evaluations were made for the improvements in wrinkles. ii) Animal study: Argireline was applied to the aged mice twice daily for 6 weeks and the histopathological changes of skin tissue were evaluated. Results: In humans, the total anti wrinkle efficiency in the Argireline group was 48.9%, the depth of the wrinkles was notably reduced(P<0.01). In the aged mice, there was improvements in the morphology of skin tissue, the amount of typeⅠcollagen fibers increased(P<0.01) while type Ⅲ collagen fibers decreased (P<0.05). Conclusions: The studies revealed that Argireline had significant anti wrinkle effects in Chinese subjects.