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Advances in Chemistry of Cosmetics

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 15 October 2025 | Viewed by 5667

Special Issue Editor


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Guest Editor
Department of Chemistry and Cosmetics, Jeju National University, Jeju 63243, Republic of Korea
Interests: natural product chemistry; melanogenesis; skin inflammation; anti-aging; hair growth
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The modern cosmetics industry is increasingly innovative and scientific, employing a variety of methodologies and technologies. With these scientific advancements, scientifically validated and eco-friendly cosmetic ingredients have become integral to maintaining healthy skin, scalp, hair, and nails. For this reason, natural products and their derivatives are an interesting and largely unexplored source of new functional ingredients. The global market demand for natural ingredients, such as plant extracts with skincare applications and other human health uses, is also increasing. In fact, many companies around the world are striving to develop inhibitors or activators associated with oxidation, melanogenesis, inflammation, hair growth, and obesity. Additionally, more mindful consumers who use such health products tend to carefully review the mechanisms of action of these inhibitors or activators.

This Special Issue on "Advances in the Chemistry of Cosmetics" serves as a platform not only for presenting novel data on natural products and compounds with human health benefits (acting either at the enzymatic or cellular level) through original papers and short communications but also for providing an overview of the current knowledge in this field through reviews.

Prof. Dr. Chang-Gu Hyun
Guest Editor

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Keywords

  • melanocytes (melanogenesis)
  • fibroblasts (anti-wrinkles)
  • papilla (hair growth)
  • keratinocytes (skin health)
  • macrophages (inflammation)
  • adipocytes (obesity)
  • natural products
  • organic synthesis
  • enzyme inhibitors
  • molecular docking

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Published Papers (5 papers)

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Research

22 pages, 4180 KiB  
Article
Inhibition of Tyrosinase and Melanogenesis by Carboxylic Acids: Mechanistic Insights and Safety Evaluation
by Yu-Pei Chen, Mingyu Li, Zirong Liu, Jinxiong Wu, Fangfang Chen and Shudi Zhang
Molecules 2025, 30(7), 1642; https://doi.org/10.3390/molecules30071642 - 7 Apr 2025
Viewed by 364
Abstract
It is well established that certain carboxylic acid compounds can effectively inhibit tyrosinase activity. This study investigated the mechanisms by which four carboxylic acid compounds—3-phenyllactic acid, lactic acid, L-pyroglutamic acid, and malic acid—inhibit tyrosinase and melanogenesis. IC50 values for mushroom tyrosinase inhibition [...] Read more.
It is well established that certain carboxylic acid compounds can effectively inhibit tyrosinase activity. This study investigated the mechanisms by which four carboxylic acid compounds—3-phenyllactic acid, lactic acid, L-pyroglutamic acid, and malic acid—inhibit tyrosinase and melanogenesis. IC50 values for mushroom tyrosinase inhibition ranged from 3.38 to 5.42 mM, with 3-phenyllactic acid (3.50 mM), lactic acid (5.42 mM), and malic acid (3.91 mM) exhibiting mixed-type inhibition, while L-pyroglutamic acid (3.38 mM) showed competitive inhibition, as determined by enzymatic kinetic analysis. Additionally, the acidification effects of lactic acid, L-pyroglutamic acid, and malic acid contributed to the reduction in tyrosinase activity. Furthermore, all four carboxylic acid compounds effectively inhibited DOPA auto-oxidation (IC50 = 0.38–0.66 mM), ranking in potency as follows: malic acid (0.38 mM) > lactic acid (0.57 mM) > 3-phenyllactic acid (0.63 mM) > L-pyroglutamic acid (0.66 mM). These compounds also demonstrated a dose-dependent reduction in melanin production in B16-F10 cells. Proteomic analysis further revealed that these compounds not only inhibit key proteins involved in melanin synthesis, such as tyrosinase, tyrosinase-related protein 1, and tyrosinase-related protein 2, but also potentially modulate other genes associated with melanogenesis and metabolism, including Pmel, Slc45a2, Ctns, Oca2, and Bace2. Network toxicology analysis indicated that these four compounds exhibit a low risk of inducing dermatitis. These findings suggest that these compounds may indirectly regulate melanin-related pathways through multiple mechanisms, highlighting their potential for further applications in cosmetics and pharmaceuticals. Full article
(This article belongs to the Special Issue Advances in Chemistry of Cosmetics)
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18 pages, 4554 KiB  
Article
Whitening and Anti-Inflammatory Activities of Exosomes Derived from Leuconostoc mesenteroides subsp. DB-21 Strain Isolated from Camellia japonica Flower
by Byeong-Min Choi, Gibok Lee, Hyehyun Hong, Chang-Min Park, Areum Yeom, Won-Jae Chi and Seung-Young Kim
Molecules 2025, 30(5), 1124; https://doi.org/10.3390/molecules30051124 - 28 Feb 2025
Viewed by 667
Abstract
In the present study, we investigated the anti-inflammatory and anti-melanogenic effects of Leuconostoc mesenteroides subsp. DB-21-derived exosomes (DB-21 exosomes), isolated from Camellia japonica flower in lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cells and melanocyte-stimulating hormone (α-MSH)-induced B16F10 melanoma cells. We confirmed that DB-21 exosomes [...] Read more.
In the present study, we investigated the anti-inflammatory and anti-melanogenic effects of Leuconostoc mesenteroides subsp. DB-21-derived exosomes (DB-21 exosomes), isolated from Camellia japonica flower in lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cells and melanocyte-stimulating hormone (α-MSH)-induced B16F10 melanoma cells. We confirmed that DB-21 exosomes were not toxic to LPS-induced RAW 264.7 macrophage cells and α-MSH-induced B16F10 melanoma cells. Moreover, we confirmed that DB-21 exosomes inhibit the pro-inflammatory cytokines IL-6, IL-1β, TNF-α, PGE2, and the expression of inflammatory factors iNOS and COX-2. We also found that DB-21 exosomes have a concentration-dependent ability to inhibit melanin, TRP-1, TRP-2, tyrosinase, and MITF, which are factors involved in melanogenesis. Additionally, it inhibits the phosphorylation of Akt and GSK-3β, and MAP kinase pathway proteins such as ERK, JNK, and p38. We confirmed that DB-21 exosomes inhibit melanin synthesis in B16F10 cells through various pathways, and based on previous results, they may be used as a functional cosmetic material with anti-inflammatory and anti-melanogenic activities. Full article
(This article belongs to the Special Issue Advances in Chemistry of Cosmetics)
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18 pages, 2493 KiB  
Article
Rifampicin Repurposing Reveals Anti-Melanogenic Activity in B16F10 Melanoma Cells
by Ye-Jin Lee and Chang-Gu Hyun
Molecules 2025, 30(4), 900; https://doi.org/10.3390/molecules30040900 - 15 Feb 2025
Viewed by 732
Abstract
Drug repurposing is a cost-effective and innovative strategy for identifying new therapeutic applications for existing drugs, thereby shortening development timelines and accelerating the availability of treatments. Applying this approach to the development of cosmeceutical ingredients enables the creation of functional compounds with proven [...] Read more.
Drug repurposing is a cost-effective and innovative strategy for identifying new therapeutic applications for existing drugs, thereby shortening development timelines and accelerating the availability of treatments. Applying this approach to the development of cosmeceutical ingredients enables the creation of functional compounds with proven safety and efficacy, adding significant value to the cosmetic industry. This study evaluated the potential of rifampicin, a drug widely used for the treatment of tuberculosis and leprosy, as a cosmeceutical agent. The anti-melanogenic effects of rifampicin were assessed in B16F10 melanoma cells, showing no cytotoxicity at concentrations up to 40 µM and a significant reduction in intracellular tyrosinase activity and melanin content. Mechanistically, rifampicin reduced the expression of melanogenic enzymes, including tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2, via a protein kinase A (PKA)-dependent pathway, leading to the suppression of microphthalmia-associated transcription factor (MITF), which is a key regulator of melanogenesis. Additionally, rifampicin inhibited the p38 signaling pathway but was independent of the PI3K/protein kinase B (Akt) pathway. Furthermore, it decreased Ser9 phosphorylation, enhancing glycogen synthase kinase-3β (GSK-3β) activity, promoted β-catenin phosphorylation, and facilitated β-catenin degradation, collectively contributing to the inhibition of melanin synthesis. To evaluate the topical applicability of rifampicin, primary human skin irritation tests were conducted, and no adverse effects were observed at concentrations of 20 µM and 40 µM. These findings demonstrate that rifampicin inhibits melanogenesis through multiple signaling pathways, including PKA, MAPKs, and GSK-3β/β-catenin. This study highlights the potential of rifampicin to be repurposed as a topical agent for managing hyperpigmentation disorders, offering valuable insights into novel therapeutic strategies for pigmentation-related conditions. Full article
(This article belongs to the Special Issue Advances in Chemistry of Cosmetics)
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13 pages, 2681 KiB  
Article
Phenolic Contents and Antioxidant Properties of Bauhinia rufescens, Ocimum basilicum and Salvadora persica, Used as Medicinal Plants in Chad
by Hissein Hassan Abdel-razakh, Gaymary George Bakari, Jin-Soo Park, Cheol-Ho Pan and Abubakar Shaaban Hoza
Molecules 2024, 29(19), 4684; https://doi.org/10.3390/molecules29194684 - 2 Oct 2024
Cited by 1 | Viewed by 1577
Abstract
The plants Bauhinia rufescens, Ocimum basilicum and Salvadora persica are well known in traditional African medicine, and particularly in traditional Chadian medicine. They are commonly used to treat infectious diseases, inflammatory diseases, fevers, gastroenteritis and other medical conditions. The aim of this [...] Read more.
The plants Bauhinia rufescens, Ocimum basilicum and Salvadora persica are well known in traditional African medicine, and particularly in traditional Chadian medicine. They are commonly used to treat infectious diseases, inflammatory diseases, fevers, gastroenteritis and other medical conditions. The aim of this study was to perform a phytochemical screening to determine the antioxidant properties of different extracts and fractions from the three plants. Ethanolic extracts and solvent fractions were prepared and analyzed for total phenolic content (TPC), total flavonoid content (TFC) and total tannin content (TTC). LC-MS and an online screening HPLC-ABTS system identified phytochemicals with antioxidant activities. DPPH and ABTS reduction methods were used to test the extracts and fractions for their antioxidant potential. The results showed that the TPC of O. basilicum was higher than that of B. rufescens, ranging from 64.70 ± 5.2 to 411.16 ± 8.11 mgGAE/g DW. B. rufescens extracts and fractions, on the other hand, showed higher TFC, ranging from 69.5 ± 5.3 to 408.26 ± 8.42 mgQE/g DW, and higher TTC, ranging from 4.57 ± 2.45 to 62.19 ± 4.7 mgTAE/g DW. The maximum TPC, TFC and TTC in both plants were recorded in the ethyl acetate fractions. S. persica extracts and fractions showed a very low quantity of TPC, TFC and TTC. Based on LC-MS and HPLC-ABTS analysis, rosmarinic acid was identified as the major component in the extracts and all fractions of O. basilicum, and epicatechin, procyanidin B and quercetin were found in B. rufescens. S. persica did not exhibit specific substances with antioxidant activity and was therefore not considered for further assays. DPPH and ABTS results showed that ethyl acetate fractions of B. rufescens and O. basilicum have the strongest antioxidant activities. This study indicates that B. rufescens and O. basilicum are good sources of phytochemicals with antioxidant properties, suitable for medicinal use in Chadian communities. Additionally, the antioxidant-rich extracts from these plants hold significant potential for cosmetic development, enhancing skin health and protecting against oxidative-stress-induced damage. Full article
(This article belongs to the Special Issue Advances in Chemistry of Cosmetics)
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18 pages, 3302 KiB  
Article
Identification of Cellular Isoschaftoside-Mediated Anti-Senescence Mechanism in RAC2 and LINC00294
by Yun Haeng Lee, Byeong Hyeon So, Kyeong Seon Lee, Myeong Uk Kuk, Ji Ho Park, Jee Hee Yoon, Yoo Jin Lee, Du Yeol Kim, Min Seon Kim, Hyung Wook Kwon, Youngjoo Byun, Ki Yong Lee and Joon Tae Park
Molecules 2024, 29(17), 4182; https://doi.org/10.3390/molecules29174182 - 4 Sep 2024
Cited by 1 | Viewed by 1581
Abstract
As cellular senescence, reactive oxygen species (ROS) accumulate excessively, causing cellular damage. Flavonoids derived from natural products are known for their antioxidant effects and their ability to delay cellular senescence. Previous studies have attempted to mitigate cellular senescence using flavonoids from natural sources. [...] Read more.
As cellular senescence, reactive oxygen species (ROS) accumulate excessively, causing cellular damage. Flavonoids derived from natural products are known for their antioxidant effects and their ability to delay cellular senescence. Previous studies have attempted to mitigate cellular senescence using flavonoids from natural sources. However, the detailed mechanisms and regulatory targets of some flavonoids exhibiting antioxidant effects have not been fully elucidated. Therefore, we screened a library of flavonoids for antioxidant properties. Isoschaftoside, a glycosidic flavonoid, significantly reduced ROS levels in senescent cells. It was found that mitochondrial function was restored, and dependence on glycolysis was reduced in senescent cells treated with isoschaftoside. Additionally, we identified that isoschaftoside suppresses ROS by reducing the expression of RAC2 and LINC00294 in senescent cells. Taken together, this study establishes a novel mechanism for ROS inhibition and the regulation of cellular senescence by isoschaftoside. Our findings contribute important insights to antioxidant and anti-senescence research. Full article
(This article belongs to the Special Issue Advances in Chemistry of Cosmetics)
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