623-11-0Relevant articles and documents
Effect of Malt-PEG-Abz@RSL3 micelles on HepG2 cells based on NADPH depletion and GPX4 inhibition in ferroptosis
Cheng, Xu,Gao, Chuya,Gong, Chen,Li, Wenhua,Liu, Xiaoying,Peng, Haisheng,Tang, Shukun,Tao, Haiquan,Yang, Bo,Zhang, Wenyuan
, (2021)
Ferroptosis is a regulated cell death pathway which depends on iron. Ferroptosis can be induced by limiting intracellular glutathione (GSH) synthesis, or inhibiting the activity of GPX4, or increasing intracellular accumulation of PE-AA-OOH, all of which involve NADPH. Therefore, NADPH depletion, excessive PE-AA-OOH, and GPX4 deficiency are generally considered to be the main characteristics of ferroptosis. In this research, the novel self-assembly nanomicelles modified by maltose ligand (Malt-PEG-Abz@RSL3) with superior nano characteristics were designed and fabricated. Malt-PEG-Abz@RSL3 micelles achieved active targeted drug delivery due to the high expression of glucose transporter (GLUT) and high uptake by HepG2 cells. Maltose-polyethylene glycol broke to release RSL3 for inhibiting GPX4 activity when Malt-PEG-Abz@RSL3 micelles entered the cells. Meanwhile, key coenzyme NADPH that participated in synthesis of GSH and Trx(SH)2 was depleted by azobenzene moiety, resulting in decreasing GSH and Trx(SH)2, which dually induced ferroptosis in tumour cells and promoted cell apoptosis.
Understanding Mechanistic Differences between 3-Diazoindolin-2-Imines and N-Sulfonyl-1,2,3-Triazoles in the Rh2(II)-Catalyzed Reactions with Nitrosoarenes
Bao, Xiaoguang,Fu, Rui,Gao, Ke,Kou, Luyao,Zhou, Shaofang
supporting information, p. 1565 - 1572 (2021/05/28)
The employment of α-iminometallocarbenes to construct valuable N-containing compounds has attracted significant research interest. Herein, the nucleophilic addition of nitrosoarenes with the α-imino rhodium carbene species (I), which is derived from Rh2(II)-catalyzed denitrogenation of 3-diazoindolin-2-imines, to produce synthetically useful 2-iminoindolin-nitrones is described. Mechanistically, the N-attack of nitrosoarenes with the carbene site of I is proposed. For the analogous Rh2(II)-catalyzed reaction of nitrosoarenes with N-sulfonyl-1,2,3-triazoles reported by Li and co-workers (Org. Lett. 2014, 16, 6394), however, the O-attack of nitrosoarenes with the carbene site of α-imino rhodium carbene species (II) is more favorable to occur than the N-attack. The subsequent transformation to yield the product of N-acylamidines is rationalized based on computational studies. The mechanistic differences for the reactions of nitrosoarenes with α-imino rhodium carbene species I and II are discussed.
Photochromic controlled permeable small molecule cross-linked vesicle as well as preparation method and application thereof
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Paragraph 0033-0036, (2021/09/01)
The invention discloses a photochromic controlled-permeation small-molecule crosslinked vesicle CSMVs as well as a preparation method and application thereof. Belong to micromolecule self-assembly technical field. The invention firstly synthesizes an azobenzene amphiphilic compound, and then further cross-linking to prepare the photochromic controllable permeable small-molecule cross-linked vesicle. The controlled release system is simple to prepare, high in stability, intelligent in control, and capable of exhibiting real-time controllable permeability in time and space, CSMVs at the molecular level due to the molecular structure of the vesicle wall, and instantaneous controlled release is exhibited. In cancer. The method has wide application prospects in the accurate treatment of diseases such as diabetes and bacterial infection.