Plants as Modulators of Melanogenesis: Role of Extracts, Pure Compounds and Patented Compositions in Therapy of Pigmentation Disorders

Merecz-Sadowska, Anna; Sitarek, Przemysław; Stelmach, Joanna; Zajdel, Karolina; Kucharska, Ewa; Zajdel, Radosław

doi:10.3390/ijms232314787

Cited by 7 publications

(7 citation statements)

References 131 publications

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“…Plants are a rich source of phytochemicals and secondary metabolites with numerous desired medicinal properties [ 2 ]. Phytochemicals have received attention in recent decades due to their health benefits [ 3 ].…”

Section: Introductionmentioning

confidence: 99%

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Chen

Lin

et al. 2023

Plants

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Sinningia bullata is a tuberous member of the flowering plant family Gesneriaceae. Prior to this work, the antibacterial, antioxidant, and cytotoxic properties of S. bullata were undetermined. Here, we prepared different extracts from the leaf, stem, and tuber of S. bullata and investigated their pharmacological activities. The leaf extract of S. bullata, obtained by 100% acetone (Sb-L-A), had the highest total flavonoid content, antioxidation capacity, and cytotoxic and antibacterial activities. Sb-L-A displayed a broad range of antibacterial activities against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The inhibition zones of Sb-L-A ranged from 8 to 30 mm and were in the following order: S. aureus > E. coli > P. aeruginosa. Incubation of B16F10 melanoma cells with Sb-L-A at a concentration of 80 μg/mL caused deaths at the rate of 96%, reduced migration by 100%, suppressed proliferation and colony formation by 99%, and induced apoptosis, which was observed in 96% of the B16F10 cells. In addition, the cytotoxic activities of Sb-L-A were synergistically enhanced when coacting with the antitumor drug epothilone B. Sb-L-A was also used to determine the cytotoxic effects against 4T1 mammary carcinoma cells. Sb-L-A of 60 μg/mL boosted the distribution of the G2 phase from 1.4% to 24.4% in the B16F10 cells. Accordingly, Sb-L-A might suppress melanoma cell proliferation by inducing G2 cell-cycle arrest. The most abundant compounds in Sb-L-A were identified using gas chromatography–mass spectrometry. The top two contents in this extract were adlupulone and villosin. Overall, the collective data in this study may indicate the pharmacological potentials of Sb-L-A for possible medical applications.

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Section: Introductionmentioning

confidence: 99%

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Chen

Lin

et al. 2023

Plants

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“…Melanogenesis refers to the biological process of synthesizing melanin pigments, predominantly by specialized cells known as melanocytes ( 56 ). The principal role of melanocytes is synthesis of melanin pigments ( 57 ). Melanin pigments are regulated by positive and negative regulators ( 16 ).…”

Section: Melanogenesis and Melasma Treatmentmentioning

confidence: 99%

Carotenoids in red fruit (Pandanus conoideus Lam.) have a potential role as an anti‑pigmentation agent (Review)

Trisnawaty,

Gunadi,

Ratnawati

et al. 2024

Biomed Rep

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Melasma is a persistent condition characterized by excessive melanin production in the skin. The management of melasma necessitates a protracted treatment duration, which is associated with diminished levels of patient satisfaction. One effective strategy for mitigating occurrence of melasma is consumption of nutricosmetics with depigmentation properties. The present review aimed to investigate the potential of red fruit as a depigmentation agent. Carotenoids serve a crucial role in human nutrition as a precursor to vitamin A. Carotenoids serve as scavengers of reactive oxygen species generated by ultraviolet radiation. Carotenoids promote skin health. Red fruit, a fruit originating from Papua (Indonesia) has anti-pigmentation properties associated with its ability to block melanogenesis through various protein pathways such as PKA, ERK, and AKT signaling pathways. The consumption of food rich in carotenoids, such as red fruit, has advantageous properties to reduce hyperpigmentation and skin brightening.

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“…The mixture was extracted with DCM (10 mL, ×2); the combined organic layers were dried over Na 2 SO 4 and the solvent was removed in vacuo. Finally, the desired intermediate 1-[(3-chloro-4fluorophenyl)methyl]piperazine (6) was obtained by crystallization with diethyl ether. 247.4 Hz, C-4 ), 163.9 (C=O).…”

Section: General Procedures For the Synthesis Of Key Intermediate 1-[...mentioning

confidence: 99%

“…The melanogenesis is a very complex and multistep process; however, the TYR activity controls the rate-limiting step, thus determining its pivotal role in the whole process of the synthesis of the physiological pigment. To date, there is a large collection of anti-melanogenic agents from synthetic [1 -4] and natural sources [5][6][7][8][9]. They have been generally identified through the determination of inhibitory properties preventing the oxidation of physiological substrates (L-tyrosine or L-DOPA) in in vitro assays using enzyme from mushroom Agaricus bisporus (AbTYR) as a surrogate to perform a preliminary screening of potential TYR inhibitors (TYRIs).…”

Section: Introductionmentioning

confidence: 99%

Leveraging the 3-Chloro-4-fluorophenyl Motif to Identify Inhibitors of Tyrosinase from Agaricus bisporus

Mirabile

Ielo

Lombardo

et al. 2023

IJMS

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Tyrosinase (EC 1.14.18.1) is implicated in melanin production in various organisms. There is a growing body of evidence suggesting that the overproduction of melanin might be related to several skin pigmentation disorders as well as neurodegenerative processes in Parkinson’s disease. Based on this consideration, the development of tyrosinase inhibitors represents a new challenge to identify new agents in pharmaceutical and cosmetic applications. With the goal of identifying tyrosinase inhibitors from a synthetic source, we employed a cheap and facile preliminary assay using tyrosinase from Agaricus bisporus (AbTYR). We have previously demonstrated that the 4-fluorobenzyl moiety might be effective in interactions with the catalytic site of AbTYR; moreover, the additional chlorine atom exerted beneficial effects in enhancing inhibitory activity. Therefore, we planned the synthesis of new small compounds in which we incorporated the 3-chloro-4-fluorophenyl fragment into distinct chemotypes that revealed the ability to establish profitable contact with the AbTYR catalytic site. Our results confirmed that the presence of this fragment is an important structural feature to improve the AbTYR inhibition in these new chemotypes as well. Furthermore, docking analysis supported the best activity of the selected studied compounds, possessing higher potency when compared with reference compounds.

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Plants as Modulators of Melanogenesis: Role of Extracts, Pure Compounds and Patented Compositions in Therapy of Pigmentation Disorders

Cited by 7 publications

References 131 publications

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Carotenoids in red fruit (Pandanus conoideus Lam.) have a potential role as an anti‑pigmentation agent (Review)

Leveraging the 3-Chloro-4-fluorophenyl Motif to Identify Inhibitors of Tyrosinase from Agaricus bisporus

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