Disrupting melanin transfer: innovative strategy for anti-pigmentation drug discovery.

The excessive synthesis of melanin leads to skin hyperpigmentation. While tyrosinase activity inhibition has demonstrated efficacy in ameliorating hyperpigmentation, its effectiveness remains limited, and tyrosinase inhibitors may induce irritant contact dermatitis. Therefore, there is an imperative need to develop safer and more potent anti-pigmentation agents. Melanin transfer inhibition represents a novel therapeutic strategy for treating hyperpigmentation. This review systematically elucidates the complete process of melanin transfer and its underlying mechanisms. Furthermore, it provides a comprehensive analysis of natural products and small molecule compounds with melanin transfer-inhibiting capabilities, potential compounds that may exhibit anti-pigmentation effects, as well as the binding modes and structure-activity relationships (SARs) of representative compounds. The presented evidence is crucial for identifying and developing novel, highly effective anti-pigmentation medications.