1180-46-7Relevant articles and documents
Synthesis of scutellarein derivatives with a long aliphatic chain and their biological evaluation against human cancer cells
Ni, Guanghui,Tang, Yanling,Li, Minxin,He, Yuefeng,Rao, Gaoxiong
, (2018)
Scutellarin is the major active flavonoid extracted from the traditional Chinese herbal medicine Erigeron breviscapus (Vant.) Hand-Mazz., which is widely used in China. Recently, accumulating evidence has highlighted the potential role of scutellarin and its main metabolite scutellarein in the treatment of cancer. To explore novel anticancer agents with high efficiency, a series of new scutellarein derivatives with a long aliphatic chain were synthesized, and the antiproliferative activities against Jurkat, HCT-116 and MDA-MB-231 cancer cell lines were assessed. Among them, compound 6a exhibited the strongest antiproliferative effects on Jurkat (IC50 = 1.80 μM), HCT-116 (IC50 = 11.50 μM) and MDA-MB-231 (IC50 = 53.91 μM). In particular, 6a even showed stronger antiproliferative effects than the positive control NaAsO2 on Jurkat and HCT-116 cell lines. The results showed that a proper long aliphatic chain enhanced the antiproliferative activity of scutellarein.
Synthesis and biological evaluation of scutellarein alkyl derivatives as preventing neurodegenerative agents with improved lipid soluble properties
Li, He-Min,Gu, Ting,Wu, Wen-Yu,Yu, Shao-Peng,Fan, Tian-Yuan,Zhong, Yue,Li, Nian-Guang
, p. 771 - 780 (2019/11/02)
Background: Exogenous antioxidants are considered as a promising therapeutic approach to treat neurodegenerative diseases since they could prevent and/or minimize the neuronal damage by oxidation. Objective: Three series of lipophilic compounds structurally based on scutellarein (2), which is one metabolite of scutellarin (1) in vivo, have been designed and synthesized. Methods: Their antioxidant activity was evaluated by detecting the 2-thiobarbituric acid reactive substance (TBARS) produced in the ferrous salt/ascorbate-induced autoxidation of lipids, which were present in microsomal membranes of rat hepatocytes. The lipophilicity of these compounds indicated as partition coefficient between n-octanol and buffer was investigated by ultraviolet (UV) spectrophotometer. Results: This study indicated that compound 5e which had a benzyl group substituted at the C4'-OH position showed a potent antioxidant activity and good lipophilicity. Conclusion: 5e could be an effective candidate for preventing or reducing the oxidative status associated with the neurodegenerative processes.
Preparation of 5, 6, 4 '-three hydroxy flavone-7-0-D-glucuro method
-
Paragraph 0065-0017, (2017/02/24)
The invention relates to the field of drug synthesis and discloses a method for preparing 5,6,4'-trihydroxy flavone-7-0-D-glucuronic acid. The method is characterized by taking 5,6,7,4'-tetrahydroxy flavone as a raw material, adopting a brand-new syntheti