Hypopigmentation diseases are usually managed using UVB light which increases the patients' risk for skin cancer. Here, we evaluated the melanogenesis stimulatory effects of leaf extracts of Erica multiflora, a medicinal plant from the Mediterranean region, and its active component, lup-20(29)-en-3-one, as possible therapeutic agents to address hypopigmentation disorders. B16 murine melanoma cells were treated with E. multiflora extracts or its active component lupenone to evaluate their effects on melanin biosynthesis. The mechanism underlying the observed effects was also determined. Bioactivity-guided fractionation of fifteen ethyl acetate fractions identified fraction 2 to have melanogenesis stimulatory effects due to its ability to decrease mitogen-activated protein kinase phosphorylated extracellular signal-regulated kinases 1 and 2 activation. Preparative TLC of ethyl acetate fraction 2 revealed the presence of lup-20(29)-en-3-one as the major bioactive component. B16 cells treated with lup-20(29)-en-3-one increased melanin content without cytotoxicity. To determine the mechanism for the observed effects of lup-20(29)-en-3-one, the tyrosinase enzyme activity, the tyrosinase protein expression, and the activation of phosphorylated extracellular signal-regulated kinases 1 and 2 were determined. In addition, the expression of the tyrosinase mRNA was quantified using real-time PCR. Results showed that lup-20(29)-en-3-one has no effect on the tyrosinase enzyme activity but can increase tyrosinase expression at both the transcriptional and translational levels. The increase in the tyrosinase mRNA expression was most likely due to the inhibited mitogen-activated protein kinase phosphorylated extracellular signal-regulated kinases 1 and 2 activation. We report for the first time that E. multiflora ethyl acetate extract and its active compound lup-20(29)-en-3-one stimulate melanogenesis by increasing the tyrosinase enzyme expression via mitogen-activated protein kinase phosphorylated extracellular signal-regulated kinases 1 and 2 phosphorylation inhibition, making it a possible treatment for hypopigmentation diseases.
"Tannins, proanthocyanidols and flavonoids represent major compounds of the flowers (Bruneton, 1987). The E. multiflora leaves ethyl acetate extract and its active compound lupenone (lup-20(29)-en-3-one) stimulate melanogenesis by increasing the tyrosinase enzyme expression at both the transcriptional and translational levels, making it a possible treatment for hypopigmentation diseases (Villareal et al., 2013). A. unedo, known as " strawberry tree " , is an evergreen shrub widely distributed in the Mediterranean basin (Ait Youssef, 2006; Fortalezas et al., 2010) and South-Western Asia (Ait Youssef, 2006). "
[Show abstract][Hide abstract] ABSTRACT: Herbs of the Ericaceae family are commonly found in Algeria and used in traditional medicine as antiseptic, diuretic, astringent, depurative, and to treat scalds and wounds. The methanolic extracts of three species, Arbutus unedo L. (A. unedo, leaves), Erica arborea L. (E. arborea, flowered aerial parts), and Erica multiflora L. (E. multiflora, flowered aerial parts), were compared regarding their content in phenolic compounds, their antioxidant, and antibacterial activities. A. unedo harbors the highest content in total phenolics and flavonoids, followed by E. arborea E. multiflora. The contents in total phenolics and flavonoids showed a correlation with the measured antioxidant (hydrogen-donating) activities; this was particularly the case for flavonoids content. The A. unedo extract showed antibacterial activity against all the tested strains (Staphylococcus aureus ATCC 6538, S. aureus C100459, Escherichia coli ATCC 25922, and Pseudomonas aeruginosa ATCC 9027); however, the E. arborea and E. multiflora extracts showed antibacterial activity only against Gram positive bacteria. Some polyphenols were identified in the three herbs by thin-layer chromatography and high-performance liquid chromatography coupled with diode array and mass spectrometry detection; from these, caffeic acid, p-coumaric acid, naringin, quercetin and kaempferol are reported for the first time in E. multiflora.
"Many immunotherapeutic protocols have been tested using the murine B16 melanoma cell line (and its sublines) that originates in the syngeneic C57BL/6 (H-2b) mouse strain. Although B164A5 is one of the most widely used cell line for the murine melanoma model, as evidenced by the latest papers in the field (Danciu et al. 2013a,b; Lee et al. 2013; Villareal et al. 2013; Ookubo et al. 2014), several subline derivates have been obtained to study different therapeutic strategies. "
[Show abstract][Hide abstract] ABSTRACT: With the aim of characterizing the active ingredients lupenone and β-sitosterol in Rhizoma Musae samples a reversed-phase HPLC method for the separation of these two compounds in Rhizoma Musae samples was developed (regression coefficient > 0.9996). The method was further applied to quantify lupenone and β-sitosterol content in Rhizoma Musae samples cultured in different growth environments. Different variables such as geographical location, growth stage, and harvest time, demonstrated differential effects on lupenone and β-sitosterol levels. Moreover, we determined the optimum conditions for cultivation and harvesting of Rhizoma Musae herbs. Lupenone administration caused a significant reduction in fasting blood glucose (FBG) levels in diabetic rats at doses of 1.78, 5.33, and 16.00 mg·kg-1·day-1 for 14 days, the glycated hemoglobin (HbA1c) levels of diabetic rats also significantly reduced at doses of 5.33, and 16.00 mg·kg-1·day-1, indicating a robust antidiabetic activity. To our knowledge, this is the first report of an optimized HPLC method successfully applied to quantify lupenone and β-sitosterol, and its applicability in optimizing Rhizoma Musae growth. Animal experiments also showed for the first time that lupenone from Rhizoma Musae has anti-diabetic activity.
Joachim Fentz, Rasmus Kjøbsted, Caroline Maag Kristensen, Janne Rasmus Hingst, Jesper Bratz Birk, Anders Gudiksen, Marc Foretz, Peter Schjerling, Benoit Viollet, Henriette Pilegaard, Jorgen F P Wojtaszewski
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