872-26-4Relevant articles and documents
8-Cetylcoptisine, a new coptisine derivative, induces mitochondria-dependent apoptosis and G0/G1 cell cycle arrest in human A549?cells
Han, Bing,Jiang, Pu,Xu, Heshan,Liu, Wuyang,Zhang, Jian,Wu, Siqi,Liu, Liangyu,Ma, Wenyu,Li, Xuegang,Ye, Xiaoli
, p. 27 - 36 (2019)
Lung cancer is the worldwide leading cause of cancer-related death. Here, we described the synthesis and the anticancer activity of a novel coptisine derivative 8-cetylcoptisine (CCOP) on lung carcinoma in vitro and in vivo. CCOP inhibited the cell viability of A549, BGC-823, MDA-MB-231, HCT-116 and HepG2 cell lines. In A549 cells, CCOP induced apoptosis, G0/G1 cell cycle arrest and decreased mitochondrial membrane potential (MMP) in a dose-dependent manner. Western blot analysis showed that CCOP increased the expression of Bcl-2-associated X protein (Bax), cleaved caspase 3 and 9, while decreased B-cell lymphoma 2 (Bcl-2), cyclins D and E, cyclin dependent kinases (CDKs) 2, 4 and 6, along with the inactivation of the upstream phosphoinositide 3-kinase (Pi3k)/protein kinase B (Akt) signaling. Further in vivo studies showed that CCOP (10 mg/kg) significantly delayed tumor growth in A549 xenograft nude mice, which is stronger than that of coptisine (100 mg/kg). These data suggested that CCOP could be a candidate for lung cancer therapy.
MODIFIED AMINE LIPIDS
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Page/Page column 173, (2020/07/04)
The disclosure provides ionizable amine lipids and salts thereof (e.g., pharmaceutically acceptable salts thereof) useful for the delivery of biologically active agents, for example delivering biologically active agents to cells to prepare engineered cells. The ionizable amine lipids disclosed herein are useful as ionizable lipids in the formulation of lipid nanoparticle-based compositions.
Chromium(II)-Catalyzed Diastereoselective and Chemoselective Csp2-Csp3 Cross-Couplings Using Organomagnesium Reagents
Li, Jie,Ren, Qianyi,Cheng, Xinyi,Karaghiosoff, Konstantin,Knochel, Paul
supporting information, p. 18127 - 18135 (2019/11/19)
A simple protocol for performing chromium-catalyzed highly diastereoselective alkylations of arylmagnesium halides with cyclohexyl iodides at ambient temperature has been developed. Furthermore, this ligand-free CrCl2 enables efficient electrophilic alkenylations of primary, secondary, and tetiary alkylmagnesium halides with readily available alkenyl acetates. Moreover, this chemoselective C-C coupling reaction with stereodefined alkenyl acetates proceeds in a stereoretentive fashion. A wide range of functional groups on alkyl iodides and alkenyl acetates are well tolerated, thus furnishing functionalized Csp2-Csp3 coupling products in good yields and high diastereoselectivity. Detailed mechanistic studies suggest that the in situ generated low-valent chromium(I) species might be the active catalyst for these Csp2-Csp3 cross-couplings.
Tolerizing and desensitizing compounds, compositions and methods of treatment against dermatological conditions caused by allergens from plants and trees of the Anacardiaceae and Ginkgoaceae families
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, (2008/06/13)
Compounds, compositions and a method of treatment to tolerize and desensitize mammals sensitive to the allergenic moities found in plants of the Anacardiaceae and Ginkgoaceae families comprising the reaction product of poison ivy urushiol, poison oak urushiol, poison sumac urushiol & mixtures thereof, 3-n-alkane substituted catechol derivatives having 11 to 19 carbon atoms and the unsaturated olefinic congeners thereof with an acyl ester functioning group esterifying the catecholic hydroxy constituents of the aforementioned compounds or cell membrane residues.
