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Jiang Tianyi,Kustermann Stefan,Wu Xiaoqin,Zihlmann Christine,Zhang Meifang,Mao Yi,Wu Waikwong,Xie Jianxun 대한독성 유전단백체 학회 2023 Molecular & cellular toxicology Vol.19 No.2
Background Antibiotics bear an inherent risk of mitochondrial toxicity due to the structural similarities between mitochondria and bacteria. Drug-induced mitochondrial dysfunction can contribute to organ toxicity and has resulted in a considerable number of market withdrawals. Fluoroquinolones were alerted for hepatotoxicity liability and were recently given black box warnings by FDA for the potential disabling side eff ects including tendonitis, pain in extremities and joints, neuropathies associated with paraesthesia, depression, impairment of memory, hearing, vision, etc. Objective In this study, the potential involvement of mitochondrial impairment in the toxicity of four fl uoroquinolones was investigated with a panel of mechanistic endpoints including ATP, mitochondrial respiration, as well as mitochondrial DNA and protein levels. Results Data revealed mitochondrial toxicity to diff erent extents, induced by the tested fl uoroquinolones and suggested mitochondrial protein synthesis as potential mechanism of action. Conclusion This study exemplifi es an integrated/holistic approach with a selected battery/panel of in vitro assays/endpoints serving to identify mitochondrial toxicity early on in the development of drugs, in particular, antibiotics.
Tianyi Wu,Wenxiao Qi,Haojie Shan,Bin Tu,Shilin Jiang,Ye Lu,Feng Wang 고려인삼학회 2022 Journal of Ginseng Research Vol.46 No.4
Background: During the pathogenesis of tendinopathy, the chronic inflammation caused by the injury and apoptosis leads to the generation of scars. Ginsenoside Rg1 (Rg1) is extracted from ginseng and has anti-inflammatory effects. Rg1 is a unique phytoestrogen that can activate the estrogen response element. This research aimed to explore whether Rg1 can function in the process of tendon repair through the estrogen receptor. Methods: In this research, the effects of Rg1 were evaluated in tenocytes and in a rat model of Achilles tendinitis (AT). Protein levels were shown by western blotting. qRT-PCR was employed for evaluating mRNA levels. Cell proliferation was evaluated through EdU assay and cell migration was evaluated by transwell assay and scratch test assay. Results: Rg1 up-regulated the expression of matrix-related factors and function of tendon in AT rat model. Rg1 reduced early inflammatory response and apoptosis in the tendon tissue of AT rat model. Rg1 promoted tenocyte migration and proliferation. The effects of Rg1 on tenocytes were inhibited by ICI182780. Rg1 activates the insulin-like growth factor-I receptor (IGF1R) and MAPK signaling pathway. Conclusion: Rg1 promotes injured tendon healing in AT rat model through IGF1R and MAPK signaling pathway activation.
Synthesis and properties of amino acid functionalized water-soluble perylene diimides
Yongshan Ma,Xuemei Li,Xiaofeng Wei,Tianyi Jiang,Junsen Wu,Huixue Ren 한국화학공학회 2015 Korean Journal of Chemical Engineering Vol.32 No.7
We prepared amino acid functionalized water-soluble perylene diimides: N,N'-bi(L-glutamic acid)-perylene- 3,4;9,10-dicarboxylic diimide (1), N,N'-bi(L-phenylalanine acid)-perylene-3,4;9,10-dicarboxylic diimide (2), N,N'-bi(Lglutamic amine)-perylene-3,4;9,10-dicarboxylic diimide (3) and N,N'-bi(L-phenylalanine amine)-perylene-3,4;9,10- dicarboxylic diimide (4). The structures of 3 and 4 were confirmed by 1H NMR, FT-IR and MS. The maximal absorption bands of compound 1 and 2 in concentrated sulfuric acid were red-shifted for about 48 and 74 nm, respectively, compared with that of Perylene-3,4,9,10-tetracarboxylic acid dianhydride (PTCDA). Nearly no fluorescence was observed for compounds 1 and 2 in water, while compounds 3 and 4 were significantly water-soluble and had very high fluorescent quantum. The mechanism of the optical properties change was discussed, and the π-π stacking caused by H+ led to the changes of fluorescence spectrum and absorption spectrum. The calculated molecular orbital energies and the frontier molecular orbital maps of compounds 1-2 based on density function theory (DFT) calculations were reported. Owing to the high water-soluble, the perylene derivatives 3 and 4 were successfully applied as high-performance fluorochromes for living hela cells imaging.