25692-59-5Relevant articles and documents
Discovery of a novel inhibitor of nitric oxide production with potential therapeutic effect on acute inflammation
Zhu, Long-Qing,Fan, Xiao-Hong,Li, Jun-Fang,Chen, Jin-Hong,Liang, Yan,Hu, Xiao-Ling,Ma, Shu-Meng,Hao, Xiang-Yong,Shi, Tao,Wang, Zhen
supporting information, (2021/05/26)
Inflammation as a host's excessive immune response to stimulation, is involved in the development of numerous diseases. To discover novel anti-inflammatory agents and based on our previous synthetic work on marine natural product Chrysamide B, it and a series of derivatives were synthesized and evaluated for their anti-inflammatory activity on inhibition of LPS-induced NO production. Then the preliminary structure–activity relationships were conducted. Among them, Chrysamide B is the most potent anti-inflammatory agent with low cytotoxicity and strong inhibition on the production of NO (IC50 = 0.010 μM) and the activity of iNOS (IC50 = 0.082 μM) in LPS-stimulated RAW 264.7 cells. Primary studies suggested that the mechanism of action may be that it interfered the formation of active dimeric iNOS but not affected transcription and translation. Furthermore, its good performance of anti-inflammatory effect on LPS-induced multiple inflammatory cytokines production, carrageenan-induced paw edema, and endotoxin-induced septic mice, was observed. We believe that these findings would provide an idea for the further modification and research of these analogs in the future.
Synthesis and discovery of 18β-glycyrrhetinic acid derivatives inhibiting cancer stem cell properties in ovarian cancer cells
Li, Xiaojing,Liu, Yihua,Wang, Na,Liu, Yuyu,Wang, Shuai,Wang, Hongmin,Li, Aihua,Ren, Shaoda
, p. 27294 - 27304 (2019/09/12)
Despite advances in ovarian cancer treatment, the five-year overall survival rate is less than 30% with the presence of cancer stem cells (CSCs). To develop CSC-targeting therapy, a series of 18β-glycyrrhetinic acid (GA) derivatives containing cinnamamide moiety have been designed, synthesized, and screened for their antiproliferative activity in SKOV3 and OVCAR3 cells. Most of the compounds exhibited stronger antiproliferative activity than GA, and compound 7c was the most active one. Further biological studies showed that compound 7c could induce apoptosis and suppress migration. In addition, compound 7c could not only observably decrease the colony formation and sphere formation ability, but also significantly reduce the CD44+, CD133+, and ALDH+ subpopulation in SKOV3 and OVCAR3 cells. In conclusion, these results indicate that compound 7c is a promising anti-CSC agent for further anti-ovarian cancer studies.
Synthesis and structural characterization for novel mixed-donor ligand palladium (II) based on graphene and oxime: its application as a highly stable and efficient recyclable catalyst
Ashiri, Samira,Mehdipour, Ebrahim
, p. 2383 - 2393 (2018/08/28)
In this article, the palladium (II) mixed-ligand complex synthesized with reduced graphene oxides containing tetraethoxysilane and menthone oxime was used as an efficient solid catalyst for the Heck coupling reaction. To maintain stability and catalytic activity in the C–C bond reaction, graphene was considered due to the available surface as the solid support. Then, the structure of new heterogeneous catalyst was investigated by FT-IR, UV–Vis DRS, FE-SEM, EDX, AFM, XRD, ICP-OES, Raman, and TGA. The newly synthesized nanocatalyst have beneficial properties, including product’s easy separation, the shorter time to react, purity products (yield 79–99%), and easier work-up procedure. Furthermore, the catalyst was reused six times without significant degradation in catalytic activity and performance.
