1343403-10-0Relevant articles and documents
Design, synthesis and in vivo anticancer activity of novel parthenolide and micheliolide derivatives as NF-κB and STAT3 inhibitors
Zeng, Binglin,Cheng, Yu,Zheng, Kailu,Liu, Shuoxiao,Shen, Longying,Hu, Jinping,Li, Yan,Pan, Xiandao
, (2021)
Parthenolide and micheliolide have attracted great attention in anticancer research due to their unique activities. In this study, thirteen parthenolide derivatives and twenty-three micheliolide derivatives were synthesized. Most synthesized compounds showed higher cytotoxicity than parthenolide or micheliolide. The in vivo anticancer activity of several representative compounds was evaluated in mice. One micheliolide derivative, 9-oxomicheliolide (43), showed promising in vivo antitumor activity compared with clinical drugs cyclophosphamide or temozolomide. Compound 43 was particularly effective against glioblastoma, with its tumor inhibition rate in mice comparable to the drug temozolomide. The discovery of compound 43 also demonstrates the feasibility of developing anticancer micheliolide derivatives by modification at C-9 position. Anticancer mechanism studies revealed that 9-oxomicheliolide exhibited inhibition effect against NF-κB and STAT3 signaling pathways, as well as induction effects of cell apoptosis. It is postulated that 9-oxomicheliolide is likely to be a modulator of the immune system, which regulates the anticancer immune responses.
Chamomile lactone derivative as well as preparation method and application thereof (by machine translation)
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Paragraph 0057-0063, (2020/08/30)
The invention relates to the technical field of organic synthesis, in particular to a small white chrysanthemum lactone derivative and a preparation method and application thereof. To the invention, small white chrysanthemum is used as the original main raw material, 11 small white chrysanthemum lactone derivatives are synthesized through a series of chemical reactions, and the derivatives have certain anti-proliferative activity on glioblastoma cells. The invention also proves that the deuterated derivative DMAPAPAPAPAPT-D6 can significantly induce accumulation of active oxygen of glioblastoma cells, thereby leading DNA damage in glioblastoma cells. Furthermore, DMAPAPAPAPAPT-D6 promotes exogenous apoptosis mediated by the death receptor of caspase, indicating DNA damage induced by DMAPAPAPAPAPT-D6 inducible glioblastoma apoptosis. , ROS accumulation caused by DMAPAPAPAPAPT-D6 treatment leads DNA damage and death receptor-mediated apoptosis, which indicates that DMAPAPAPAPAPT-D6 with novel ingredients has therapeutic potential for treating glioblastoma and can be applied to preparation of drugs for treating glioblastoma. (by machine translation)
Process for the preparation of Arglabin
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Paragraph 0019-0021, (2017/04/07)
The present invention relates to the preparation method of arglabin, comprising reacting micheliolide with epoxidation reagent to obtain 1,10-epoxy micheliolide and dehydration of 4-hydroxy and 3-hydrogen of 1,10-epoxy micheliolide to obtain arglabin. The character of the method is that arglabin is prepared from micheliolide through the crucial intermediate of 1,10-epoxy micheliolide.
Sesquiterpene lactone compound and its derivatives use in the preparation of medicament
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Paragraph 0064; 0065, (2016/10/10)
The invention relates to a sesquiterpene lactone compound and uses of a derivative thereof in preparation of drugs, belongs to the technical field of the drugs, specially relates to the uses of a formula (I) compound in preparation of the drugs, and particularly relates to the uses of a formula (I) compound in preparation of the drugs for treatment of rheumatoid arthritis and treatment of cancer through inhibition of cancer stem cells.
USES OF SESQUITERPENE LACTONE COMPOUNDS AND THEIR DERIVATIVES IN DRUGS PREPARATION
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Paragraph 0057; 0058, (2017/04/13)
The present invention relates to the uses of sesquiterpene lactone compounds and their derivatives in preparing drugs. It belongs to the field of drug technology, specifically relates to the uses of the compounds of Formula (I) in preparing the drugs, especially the uses in preparing the drugs to treat rheumatoid arthritis and treat cancers through inhibiting cancer stem cells.
SPHAELACTONE DERIVATIVES, THEIR PHARMACEUTICAL COMPOSITIONS, PREPARATION METHODS AND USES
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Paragraph 0037, (2013/03/26)
The present invention provides micheliolide derivatives or salts thereof of formula (I)
Sesquiterpene lactones and their derivatives inhibit high glucose-induced NF-κB activation and MCP-1 and TGF-β1 expression in rat mesangial cells
Jia, Qian-Qian,Wang, Jian-Cheng,Long, Jing,Zhao, Yan,Chen, Si-Jia,Zhai, Jia-Dai,Wei, Lian-Bo,Zhang, Quan,Chen, Yue,Long, Hai-Bo
, p. 13061 - 13077 (2013/11/06)
Diabetic nephropathy (DN) is one of the most common and serious chronic complications of diabetes mellitus, however, no efficient clinical drugs exist for the treatment of DN. We selected and synthesized several sesquiterpene lactones (SLs), and then used the MTT assay to detect rat mesangial cells (MCs) proliferation, ELISA to measure the expression level of monocyte chemoattractant protein-1 (MCP-1), transforming growth factor beta (TGF-β1) and fibronectin(FN), real-time fluorescent quantitative PCR analysis to measure the MCP-1 and TGF-β1 gene expression, western blot to detect the level of IκBα protein and EMSA to measure the activation of nuclear factor kappa B (NF-κB). We discovered that SLs, including parthenolide (PTL), micheliolide (MCL), arglabin, and isoalantolactone (IAL), as well as several synthetic analogs of these molecules, could effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs). These findings suggest that SLs and their derivatives have potential as candidate drugs for the treatment of DN.
Biomimetic semisynthesis of arglabin from parthenolide
Zhai, Jia-Dai,Li, Dongmei,Long, Jing,Zhang, Hao-Liang,Lin, Jian-Ping,Qiu, Chuan-Jiang,Zhang, Quan,Chen, Yue
experimental part, p. 7103 - 7107 (2012/10/07)
The semisynthesis of arglabin, an anticancer drug in clinical application, is developed from abundant natural product parthenolide via three steps. Each step in this sequence is highly stereoselective, and the substrate-dependent stereoselectivity in the epoxidation step can be explained by computational calculations. The success of chemical semisynthesis of arglabin suggests that the biosynthesis of arglabin might proceed in a similar pathway.
