Velutin
(Synonyms: 毡毛美洲茶素) 目录号 : GC39096Velutin 是从槲寄生中提取的苷元,具有抑制黑色素生物合成的活性。Velutin 能通过 NF-κB 途径减少破骨细胞分化和下调HIF-1α。
Cas No.:25739-41-7
Sample solution is provided at 25 µL, 10mM.
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Velutin is an aglycone extracted from Korean Mistletoe, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway[1][2].
[1]. Jung SH, et al. Velutin, an Aglycone Extracted from Korean Mistletoe, with Improved Inhibitory Activity against Melanin Biosynthesis. Molecules. 2019 Jul 12;24(14). [2]. Brito C, et al. Cytotoxicity and potential anti-inflammatory activity of velutin on RAW 264.7 cell line differentiation: Implications in periodontal bone loss. Arch Oral Biol. 2017 Nov;83:348-356
Cas No. | 25739-41-7 | SDF | |
别名 | 毡毛美洲茶素 | ||
Canonical SMILES | O=C1C=C(C2=CC=C(O)C(OC)=C2)OC3=CC(OC)=CC(O)=C13 | ||
分子式 | C17H14O6 | 分子量 | 314.29 |
溶解度 | DMSO : 50 mg/mL (159.09 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.1818 mL | 15.9089 mL | 31.8177 mL |
5 mM | 0.6364 mL | 3.1818 mL | 6.3635 mL |
10 mM | 0.3182 mL | 1.5909 mL | 3.1818 mL |
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2.
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Anti-Melanogenic Properties of Velutin and Its Analogs
Molecules 2021 May 19;26(10):3033.PMID:34069624DOI:10.3390/molecules26103033.
Velutin, one of the flavones contained in natural plants, has various beneficial activities, such as skin whitening, as well as anti-inflammatory, anti-allergic, antioxidant, and antimicrobial activities. However, the relationship between the structure of Velutin and its anti-melanogenesis activity is not yet investigated. In this study, we obtained 12 Velutin derivatives substituted at C5, C7, C3', and C4' of the flavone backbone with hydrogen, hydroxyl, and methoxy functionalities by chemical synthesis, to perform SAR analysis of Velutin structural analogues. The SAR study revealed that the substitution of functional groups at C5, C7, C3', and C4' of the flavone backbone affects biological activities related to melanin synthesis. The coexistence of hydroxyl and methoxy at the C5 and C7 position is essential for inhibiting tyrosinase activity. However, 1,2-diol compounds substituted at C3' and C4' of flavone backbone induce apoptosis of melanoma cells. Further, substitution at C3' and C4' with methoxy or hydrogen is essential for inhibiting melanogenesis. Thus, this study would be helpful for the development of natural-derived functional materials to regulate melanin synthesis.
The potential role of herbal products in the treatment of Parkinson's disease
Clin Ter 2018 Jan-Feb;169(1):e23-e33.PMID:29446788DOI:10.7417/T.2018.2050.
Parkinson's disease (PD) is a multifactorial disorder of the nervous system in which there is a progressive loss of dopaminergic neurons. There is a disturbance in the movement in PD and these include resting tremors, rigidity, bradykinesia or akinesia, disturbance, posture and freezing (motor block). The substantia nigra and other parts of the brain are commonly affected. The disorder could be related to oxidative stress and there is an important role of reactive oxygen species (ROS). A number of herbal products contain active components which are known to possess antioxidant action. Hence, the potential role of herbal products in treating PD cannot be undermined. In the present narrative review, the main aim is to discuss the pathogenesis of PD, define the role of different potential herbal extracts on its pathogenesis which may form the basis of treatment. We also discuss in detail the active chemical compounds present each herb which are effective in the treatment of PD. These herbs include Baicalei, Erythrina Velutin, Resveratrol, Peganum Harmal, Curcuma longa (Zingiberaceae), Carthamus tinctorius L. (Safflower), Pueraria lobate, Juglandis Semen (Walnut), Tianma Gouteng Yin (TGY), Lycium barbarum L fruit, Mucuna pruriens (Velvet bean), Chunghyuldan (CHD), Paeoniae Alba Radix. The present review may be beneficial for designing future drugs for effective treatment of PD.
Dual protective role of Velutin against articular cartilage degeneration and subchondral bone loss via the p38 signaling pathway in murine osteoarthritis
Front Endocrinol (Lausanne) 2022 Jul 22;13:926934.PMID:35937813DOI:10.3389/fendo.2022.926934.
Osteoarthritis (OA) is a common degenerative joint condition associated with inflammation and characterized by progressive degradation of the articular cartilage and subchondral bone loss in the early stages. Inflammation is closely associated with these two major pathophysiological changes in OA. Velutin, a flavonoid family member, reportedly exerts anti-inflammatory effects. However, the therapeutic effects of Velutin in OA have not yet been characterized. In this study, we explore the effects of Velutin in an OA mouse model. Histological staining and micro-CT revealed that Velutin had a protective effect against cartilage degradation and subchondral bone loss in an OA mouse model generated by surgical destabilization of the medial meniscus (DMM). Additionally, Velutin rescued IL-1β-induced inflammation in chondrocytes and inhibited RANKL-induced osteoclast formation and bone resorption in vitro. Mechanistically, the p38 signaling pathway was found to be implicated in the inhibitory effects of Velutin. Our study reveals the dual protective effects of Velutin against cartilage degradation and subchondral bone loss by inhibiting the p38 signaling pathway, thereby highlighting Velutin as an alternative treatment for OA.
Velutin, an Aglycone Extracted from Korean Mistletoe, with Improved Inhibitory Activity against Melanin Biosynthesis
Molecules 2019 Jul 12;24(14):2549.PMID:31336931DOI:10.3390/molecules24142549.
The abnormal regulation of melanin synthesis leads to a wide range of pigmentary disorders. Although various melanin biosynthesis inhibitors have been developed, their efficacy and long-term safety needs to be further improved, and thus the goal of this study is to develop promising natural compound inhibitors of melanin biosynthesis. Here, we obtained aglycone flavonoid extract through the microwave-assisted hydrolysis of glycoside extract from Korean mistletoe in acidic condition. The aglycone extract inhibited tyrosinase activity more efficiently with better antioxidant activity than glycoside extract in vitro. The microwave-assisted aglycone extract of mistletoe was further analyzed for in vivo activity, and the results showed the aglycone extract inhibited both early melanocyte development and melanin synthesis more efficiently in zebrafish embryo in a dose-dependent manner. Our in vivo toxicity assay quantitatively measured cell death in zebrafish embryos and showed that the microwave-assisted aglycone extract of mistletoe had no significant effect on cell death (p < 0.001), indicating that aglycone extract is more biocompatible than glycoside extract. Furthermore, our in vitro and in vivo analyses successfully identified and characterized Velutin, an aglycone of a homoflavoyadorinin B glycoside, as a major inhibitory component in the microwave-assisted mistletoe extract. Ultimately, this study showed that the novel natural compound inhibitor Velutin, which was generated through microwave-assisted extraction from mistletoe, improved the efficacy of melanin biosynthesis inhibition with little toxicity.
Preparation and Evaluation of Nanostructured Lipid Carrier for Topical Delivery of Velutin: Synthetic Tyrosinase Inhibitor
J Nanosci Nanotechnol 2021 Jul 1;21(7):4093-4097.PMID:33715752DOI:10.1166/jnn.2021.19173.
The purpose of this study is to produce nanostructured lipid carrier (NLC) that can solubilize poorly water-soluble Velutin and verify an improved tyrosinase synthesis inhibition. A solubility test for Velutin was conducted. Cetyl palmitate and caprylic/capric triglyceride were selected as solubilizer. The lipid matrix was produced using the ultrasound dispersion method. The morphology and size distribution of the produced NLC was analyzed through scanning electron microscopy (SEM) and dynamic light scattering (DLS), and the release and tyrosinase inhibition of Velutin was evaluated through the Franz diffusion cell method and tyrosinase inhibition assay. Lipid matrix nanoparticles showed an average size of approximately 250 nm and polydispersity of 0.2, and it was confirmed that the Velutin incorporated within nanoparticles sustained release at a constant rate over 36 hours. Due to extremely low aqueous solubility, the tyrosinase synthesis inhibition of Velutin suspension was 0%, and the value of Velutin incorporated within the NLC formulation was greatly improved 56.5% (40 μg/mL). As a result, it was verified that lipid-based NLC nanoparticles are an efficient formulation for the topical delivery of poorly water-soluble flavonoids such as Velutin.