Insight Into the Cellular Activities of Tranexamic Acid as an Option for Melasma Treatment

Area of Science:

• Dermatology
• Cell Biology
• Pharmacology

Background:

• Melasma and hyperpigmentation pose significant dermatological challenges.
• Tranexamic acid (TXA), known for antifibrinolytic effects, is a potential depigmenting agent.
• TXA's cellular mechanisms in skin pigmentation are not fully understood.

Purpose of the Study:

• To investigate the cellular effects of TXA on melanocytes, keratinocytes, and inflammatory cells.
• To elucidate TXA's role in melanogenesis and inflammation pathways.
• To support the therapeutic potential of TXA in skin conditions.

Main Methods:

• Investigated TXA's impact on B16 melanoma cells for melanin synthesis.
• Assessed TXA's effect on inflammatory responses in keratinocytes and macrophages via the plasminogen/plasmin pathway.
• Evaluated TXA's influence on lipopolysaccharide-induced inflammation in mouse macrophages.

Main Results:

• TXA directly inhibited melanin synthesis in melanoma cells, showing additive effects with α-arbutin.
• TXA attenuated inflammatory responses in keratinocytes and macrophages mediated by the plasminogen/plasmin pathway.
• TXA reduced pro-inflammatory gene expression in macrophages, suggesting interference with Toll-like receptor signaling.

Conclusions:

• TXA exhibits multifaceted actions on skin cells relevant to pigmentation and inflammation.
• Findings support TXA's therapeutic potential for melasma and other skin disorders.
• TXA's anti-inflammatory properties may contribute to its efficacy in treating hyperpigmentation.