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Anti-Melanogenesis Effects of a Cyclic Peptide Derived from Flaxseed via Inhibition of CREB Pathway
Ji Hye Yoon1, Won Young Jang2, Sang Hee Park1
1Department of Biocosmetics, Sungkyunkwan University, Suwon 16419, Republic of Korea.
Abstract:
Linosorbs (Los) are cyclic peptides from flaxseed oil composed of the LO mixture (LOMIX). The activity of LO has been reported as being anti-cancer and anti-inflammatory. However, the study of skin protection has still not proceeded. In particular, there are poorly understood mechanisms of melanogenesis to LO. Therefore, we investigated the anti-melanogenesis effects of LOMIX and LO, and its activity was examined in mouse melanoma cell lines. The treatment of LOMIX (50 and 100 μg/mL) and LO (6.25-50 μM) suppressed melanin secretion and synthesis, which were 3-fold increased, in a dose-dependent manner, up to 95%. In particular, [1-9-NαC]-linusorb B3 (LO1) and [1-9-NαC]-linusorb B2 (LO2) treatment (12.5 and 25 μM) highly suppressed the synthesis of melanin in B16F10 cell lines up to 90%, without toxicity. LOMIX and LOs decreased the 2- or 3-fold increased mRNA levels, including the microphthalmia-associated transcription factor (MITF), Tyrosinase, tyrosinase-related protein 1 (TYRP1), and tyrosinase-related protein 2 (TYRP2) at the highest concentration (25 μM). Moreover, the treatment of 25 μM LO1 and LO2 inhibited the expression of MITF and phosphorylation of upper regulatory proteins such as CREB and PKA. Taken together, these results suggested that LOMIX and its individual LO could inhibit melanin synthesis via downregulating the CREB-dependent signaling pathways, and it could be used for novel therapeutic materials in hyperpigmentation.
Insights
Flaxseed oil components, LinoSorb mixtures (LOMIX) and individual LinoSorb peptides (LO), effectively inhibit melanin production in melanoma cells. These compounds reduce melanin synthesis by downregulating key genes and signaling pathways, offering potential for hyperpigmentation treatments.
Area of Science:
- Biochemistry
- Dermatology
- Natural Products Chemistry
Background:
- LinoSorb (LO) peptides from flaxseed oil possess known anti-cancer and anti-inflammatory properties.
- The specific effects of LO on melanogenesis and skin protection remain largely uninvestigated.
- Understanding LO's mechanism in melanin production is crucial for developing new dermatological therapies.
Purpose of the Study:
- To investigate the anti-melanogenesis effects of LinoSorb mixtures (LOMIX) and individual LinoSorbs (LO).
- To elucidate the molecular mechanisms underlying LO's impact on melanin synthesis.
- To evaluate the potential of LOMIX and LO as therapeutic agents for hyperpigmentation disorders.
Main Methods:
- Treatment of mouse melanoma cell lines (B16F10) with varying concentrations of LOMIX and individual LO peptides (LO1, LO2).
- Quantification of melanin secretion and synthesis.
- Analysis of mRNA expression levels for key melanogenesis-related genes (MITF, Tyrosinase, TYRP1, TYRP2).
- Assessment of protein expression and phosphorylation in signaling pathways (MITF, CREB, PKA).
Main Results:
- LOMIX and LO significantly suppressed melanin secretion and synthesis in a dose-dependent manner, with up to 95% reduction.
- Specific LO peptides (LO1 and LO2) demonstrated potent melanin synthesis inhibition (up to 90%) without cellular toxicity.
- LOMIX and LOs downregulated mRNA levels of MITF, Tyrosinase, TYRP1, and TYRP2.
- LO1 and LO2 inhibited MITF expression and the phosphorylation of CREB and PKA signaling proteins.
Conclusions:
- LOMIX and individual LO peptides effectively inhibit melanin synthesis in melanoma cells.
- The anti-melanogenesis mechanism involves the downregulation of CREB-dependent signaling pathways.
- These findings suggest LOMIX and LOs are promising candidates for novel therapeutic materials targeting hyperpigmentation.
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