Background/objectives: The root of Vitis amurensis Ruprecht, a sort of wild-growing grape, has been used in oriental medicine for treatment of skin ailments; however, its dermatological activity is not sufficiently understood. The aim of this study was to investigate tyrosinase inhibitory and anti-melanogenic activities of V. amurensis Ruprecht root methanol extract (VARM) in B16F10 mouse melanoma cells and to attempt to isolate and identify the active compound issued from VARM.
Materials/methods: Anti-melanogenic activity of VARM was analyzed in α-melanocyte stimulating hormone (MSH)-stimulated B16F10 cells through evaluation of antioxidative activity as well as inhibited tyrosinase activity and melanin contents compared with those of kojic acid and arbutin. After anti-melanogenic analysis of VARM, serial fractionation, nuclear magnetic resonance (NMR), and thin layer chromatorgraphy (TLC) were applied for identification of active compounds contained in VARM.
Results: VARM significantly inhibited oxidative stress and tyrosinase activity and attenuated α-MSH-induced melanin production in B16F10 cells. For isolation of active compounds, VARM was fractionated using a series of organic solvents, including dichloromethane (CH2Cl2), ethyl acetate (EtOAc), and n-butanol (n-BuOH). Among fractions showing anti-melanogenic activity, the CH2Cl2 fraction induced the most potent attenuation of melanogenesis without cytotoxicity and the major compound in the CH2Cl2 fraction was identified as betulinic acid. Betulinic acid isolated from the CH2Cl2 fraction of VARM significantly attenuated α-MSH-induced melanogenesis in a dose dependent manner, which was stronger than that of arbutin used as a positive control.
Conclusions: These results indicate that VARM inhibits oxidative stress, tyrosinase activity, and α-MSH-induced melanogenesis in B16F10 cells, due primarily to the active compound, betulinic acid, in the CH2Cl2 fraction.
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http://dx.doi.org/10.4162/nrp.2014.8.5.509 | DOI Listing |
Angew Chem Int Ed Engl
January 2025
University of Science and Technology of China School of Biomedical Engineering, Department of Polymer Science and Engineering, 96 Jinzhai Road, 230026, Hefei, CHINA.
Lipid nanoparticles (LNPs) based messenger RNA (mRNA) therapeutics hold immense promise for treating a wide array of diseases, while their nonhepatic organs targeting and insufficient endosomal escape efficiency remain challenges. For LNPs, polyethylene glycol (PEG) lipids have a crucial role in stabilizing them in aqueous medium, but they severely hinder cellular uptake and reduce transfection efficiency. In this study, we designed ultrasound (US)-assisted fluorinated PEGylated LNPs (F-LNPs) to enhance spleen-targeted mRNA delivery and transfection.
View Article and Find Full Text PDFACS Appl Mater Interfaces
January 2025
School of Life Sciences, Henan University, Kaifeng, Henan 475001, China.
Melanoma, a highly aggressive skin cancer, poses significant challenges due to its rapid metastases and high mortality rates. While metformin (Met), a first-line medication for type 2 diabetes, has shown promise in inhibiting tumor growth and metastases, its clinical efficacy in cancer therapy is limited by low bioavailability, short half-life, and gastrointestinal adverse reactions associated with oral administration. In this study, we developed a hollow mesoporous polydopamine nanocomposite (HMPDA-PEG@Met@AB) coloaded with Met and ammonia borane (AB), designed to enable a combined gas-assisted, photothermal, and chemotherapeutic approach for melanoma treatment.
View Article and Find Full Text PDFInt J Nanomedicine
January 2025
Department of Pharmacy, The Affiliated Hospital, Southwest Medical University, Luzhou, Sichuan, 646000, People's Republic of China.
Background: Melanoma is an aggressive form of skin cancer, and single-modality treatments often fail to prevent tumor recurrence and metastasis. Combination therapy has emerged as an effective approach to improve treatment outcomes.
Methods: In this study, we developed a multifunctional nanoplatform, MIL@DOX@ICG, utilizing MIL-101-NH(Fe) as a carrier to co-deliver the chemotherapeutic agent doxorubicin (DOX) and the photosensitizer indocyanine green (ICG).
Scand J Immunol
February 2025
Institute of Chemical Biology and Fundamental Medicine SB RAS, Novosibirsk, Russia.
Myeloid-derived suppressor cells (MDSCs) are a heterogeneous group of immature myeloid cells playing a critical role in immune suppression. In vitro-generated MDSCs are a convenient tool to study the properties of tumour-associated MDSCs. Here, we compared six protocols for in vitro generation of functional mouse MDSCs from bone marrow progenitors.
View Article and Find Full Text PDFMolecules
January 2025
Department of Manufacturing Pharmacy, College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan 46241, Republic of Korea.
Fifteen compounds (-) constructed on a hybrid structure combining a β-phenyl-α,β-unsaturated carbonyl template and a 2-aminothiazol-4(5)-one scaffold were designed and synthesized as potential novel anti-tyrosinase substances. Two compounds ( and ) showed more potent inhibition against mushroom tyrosinase than kojic acid, and the inhibitory activity of (IC value: 1.60 μM) was 11 times stronger than that of kojic acid.
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