Giant Centella asiatica , a novel cultivar rich in madecassoside and asiaticoside, suppresses α‑melanocyte‑stimulating hormone‑induced melanogenesis through MC1R binding
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(CA) cataloged by the Korea Forest Service in 2022, and compared its efficacy with that of traditional CA. GCA has a high yield per unit area and enhanced antioxidant properties. The anti‑melanogenic effects of GCA were investigated using B16F10 melanoma cells and a 3D human skin‑equivalent model. Key molecular mechanisms were elucidated through western blotting, cAMP assays and molecular docking studies. Focus was addressed on the effect of GCA on skin whitening by comparing the ability of a GCA extract to inhibit melanin production in B16F10 melanoma cells and a 3D human skin‑equivalent model to that of CA. The results showed that the GCA extracts more effectively reduced melanin production, which was attributed to their higher content of two active components, madecassoside and asiaticoside. Further investigation revealed that GCA primarily inhibited melanogenesis through the PKA‑cAMP response element‑binding (CREB)‑microphthalmia‑associated transcription factor (MITF) axis, a key regulatory pathway in melanin synthesis. Notably, the present study, to the best of our knowledge, is the first to demonstrate that madecassoside and asiaticoside, the two principal compounds in GCA, directly bound to MC1R, which contributed to the significant skin‑whitening effects. Moreover, GCA reduced melanin production in a 3D human skin‑equivalent model, showing efficacy within a complex skin environment. These results demonstrated the superior effectiveness of GCA to that of CA for skin anti‑melanogenesis, indicating its potential as a promising natural material for targeting pigmentation disorders.
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GCA has been shown to exhibit superior anti-melanogenic effects compared to conventional Centella asiatica, attributed to higher content of madecassoside and asiaticoside which directly bind to MC1R.
“Notably, the source plant, GCA, has been shown to exhibit superior anti-melanogenic effects compared to conventional Centella asiatica [7]. This enhanced activity is attributed to its higher content of madecassoside and asiaticoside, which directly bind to MC1R.”
From Anti-Photoaging and Anti-Melanogenic Effects of a Novel <i>Lactiplantibacillus plantarum</i> RKBP Isolated from Giant <i>Centella asiatica</i> (2026) · cites this paper as [7]
UVB irradiation stimulates α-MSH secretion from keratinocytes, leading to activation of PKA-CREB-MITF signaling and upregulation of tyrosinase expression.
“UVB irradiation stimulates α-melanocyte-stimulating hormone (α-MSH) secretion from keratinocytes. α-MSH binds to melanocortin-1 receptor (MC1R) on melanocytes. This activation leads to increased intracellular cAMP levels, subsequently activating the PKA-CREB-MITF signaling cascade and upregulating tyrosinase expression [7].”
From Anti-Photoaging and Anti-Melanogenic Effects of a Novel <i>Lactiplantibacillus plantarum</i> RKBP Isolated from Giant <i>Centella asiatica</i> (2026) · cites this paper as [7]
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“Notably, the source plant, GCA, has been shown to exhibit superior anti-melanogenic effects compared to conventional Centella asiatica [7].”
Self-citation
- Authors
- Seo, J., Jeong, C., Oh, S., Lee, S.-Y., Park, H., Seo, D., Yoo, D., Sim, W.-J., Lim, T.-G., Park, J. H. Y., Lee, C., & Lee, K.
- Affiliations
- Seoul National University (KR)
- ASK Company Co., Ltd., Daegu 42176, Republic of Korea
- Sejong University (KR)
- Corresponding author
- Lee, Chang
- Lee, Ki
- ORCID
- Venue
- International Journal of Molecular Medicine
- Publisher
- Spandidos Publications
- Published
- 2024-11-04
- Volume
- 55
- Issue
- 1
- ISSN
- 1107-3756 (ISSN-L)
- 1791-244X
- PMC
- PMC11573313
- OpenAlex
- W4404045325
- Cited by
- 6
- References
- 43
- Citations by year
- 2026: 4 · 2025: 2
- FWCI
- 1.34
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- cc-by-nc-nd
- Locations
- International Journal of Molecular Medicine (publishedVersion, cc-by-nc-nd)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- Funders
- National Research Foundation (2020M3H1A1073304)
- Seoul National University
- Ministry of Science and ICT, South Korea (2020M3H1A1073304)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › melanin and skin pigmentation
- Health Sciences › Medicine › Dermatology › Skin Protection and Aging
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
- Keywords
- Centella asiatica, madecassoside, asiaticoside, anti-melanogenic activity, melanogenesis, MITF, CREB, PKA signaling, B16F10 melanoma cells, skin lightening, skin pigmentation disorders
- MeSH terms
- Melanogenesis, alpha-MSH, Animals, Humans, Melanins, Melanoma, Experimental, Plant Extracts, Skin Pigmentation, Triterpenes, Centella, Receptor, Melanocortin, Type 1, Cell Line, Tumor, Mice, Molecular Docking Simulation
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