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.
Design and synthesis of novel pyranone-based insulin sensitizers exhibiting in vivo hepatoprotective activity
Goel, Atul,Parihar, Amrita,Mishra, Pratibha,Varshney, Salil,Nag, Pankaj,Beg, Muheeb,Gaikwad, Anil,Rath
supporting information, p. 1532 - 1536 (2013/12/04)
Serious hepatic and cardiovascular complications after treatment with the thiazolidinedione (TZD) class of insulin sensitizers have significantly retarded the advancement of new TZD-based peroxisome proliferator-activated receptor agonists that bind with high affinity and selectivity. The aim of the present study is to design new antihyperglycemic agents that promote insulin sensitivity through partial adipogenesis as well as demonstrate beneficial hepatoprotective activity. The results indicated that among forty screened compounds, three of the novel pyranones at a dose of 10 μM increased the preadipocyte differentiation into adipocytes in 3T3-L1 cell lines. They showed an insulin-sensitizing effect by significantly increasing the glucose uptake and exhibited insulin resistance reversal. These compounds at a dose of 20 mg kg-1 significantly protected against thioacetamide-induced hepatotoxic changes in the serum biochemistry as compared to standard hepatoprotectant silymarin and also ameliorated the histopathological alterations in the liver tissues after acute liver injury in Swiss mice.
