74772-78-4Relevant articles and documents
A novel chrysin thiazole derivative polarizes macrophages to an M1 phenotype via targeting TLR4
Feng, Xiujing,Yu, Wen,Cao, Lingsen,Meng, Fanda,Cong, Mulin
, (2020/09/17)
Tumor-associated macrophages (TAMs) are an important cause of tumorigenesis and tumor development. M2 macrophages can promote tumor growth while M1 macrophages kill tumor cells, therefore, polarizing macrophages to achieve a functional M1 phenotype could effectively play its anti-tumor role. In the current study, we synthesized a novel chrysin derivative which is termed as ChR-TD. And we found ChR-TD might be a ligand of TLR4 that polarized the TAMs towards M1 phenotype and played its anti-tumor role. Further study indicated that ChR-TD reprogrammed the macrophages into an M1 phenotype via TLR4 activation. Moreover, ChR-TD activated TLR4/NF-κB signaling pathway and promoted the NF-κB/p65 translocated into the nuclear, leading to the activation of NF-κB and proinflammatory cytokines release. In addition, type I interferon signaling was also activated by ChR-TD, leading to the expressions of IFN-α and IFN-β and its targeted genes NOS2, MCP-1 and IP-10 were significantly increased in macrophages. Importantly, these effects were disturbed in TLR4?/? macrophages, which are constructed by using CRISPR/Cas9 system. And the molecule docking simulation further indicated that ChR-TD could bind to TLR4 and might be a ligand of TLR4. Hence, these findings suggested that ChR-TD might be a ligand of TLR4 and can be used as a potential lead compound for tumors treatment.
Whitening skin care productSkin-whitening cosmetic containing algae active extracts
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Paragraph 0042; 0043, (2019/01/08)
The invention discloses a skin-whitening cosmetica whitening skin care product containing algae active extracts. The skin-whitening cosmetics iswhitening skin care product is prepared from the following raw materials in percentage by mass: 2 to 5 percent of hyaluronic acid, 0.5 to 1 percent of lecithin, 4 to 8 percent of glycerol, 1 to 5 percent of cetostearyl alcohol, 1 to 5.5 percent of glycerylstearate, 0.5 to 3 percent of polydimethylsiloxane, 0.5 to 1.5 percent of algal active extracts, 0.2 to 0.8 percent of whitening and anti-blackening agents, 2 to 6 percent of natural whitening grease, 0.5 to 1 percent of VC, 0.5 to 1 percent of VE, 0.1 to 0.35 percent of pH regulators, 1 to 5 percent of propanediol and the balance of deionized water. The raw material ingredients are scientifically proportioned; the activity of tyrosinase is inhibited internally in an inner aspect; the problem of melanin generation is fundamentally solved; in an outer aspectexternally, the active free radicalsare cleared through irideae extracts; the immunologic function of the skin is improved, so that the durable and continuous skin whitening effects can be achieved.
SUBSTITUTED PIPERIDINE DERIVATIVES AND METHODS FOR PREPARING THE SAME
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, (2013/07/25)
The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof, a preparation method thereof and a pharmaceutical composition for treating metabolism-related disorder containing the same. Specifically, the present invention relates to a compound of the formula 1, which can activate GPR119 to treat metabolism-related disorders, including diabetes and related diseases, diabetes-related microvascular complications, diabetes-related macrovascular complications, cardiovascular abnormalities, metabolic syndrome and its constituent diseases, and obesity.
