A novel necroptosis inhibitor—necrostatin-21 and its SAR study

Wu, Zhijie; Li, Ying; Cai, Yu; Yuan, Junying; Yuan, Chengye

doi:10.1016/j.bmcl.2013.06.073

Cited by 28 publications

(18 citation statements)

References 13 publications

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“…Nec1 has been used to help researchers to distinguish whether or not an observed cell death is necroptotic. Newer versions of Nec-1 with improved target specificity and drug-like properties have since been developed [66,67]. Interestingly, Nec-1 also inhibits TLR3/4 mediated necrosis even when RIP1 kinase activity is not required.…”

Section: Necrosis Inhibitorsmentioning

confidence: 96%

A new kind of cell suicide: mechanisms and functions of programmed necrosis

Sun

Wang

2014

Trends in Biochemical Sciences

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Section: Necrosis Inhibitorsmentioning

confidence: 96%

A new kind of cell suicide: mechanisms and functions of programmed necrosis

Sun

Wang

2014

Trends in Biochemical Sciences

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“…1 H NMR (CD 2 Cl 2 , 500 MHz): δ = 9.13 (s, 1 H), 7.30-7.22 (m, 3 H), 7.14-7.13 (m, 2 H), 6.78-6.77 (m, 1 H), 6.18-6.17 (m, 1 H), 6.14 (q, J = 2. 6,140.0,130.1,128.9,128.3,127.5,118.7,109.1,108.3,106.0,52.4,42.3,28.5,27.5. HRMS (ESI+): m/z [M + H] + calcd for C 17 H 18 NO 4 : 300.1236; found: 300.1258.…”

Section: 2-dimethyl-5-[phenyl(1h-pyrrol-2-yl)methyl]-13-dioxane-4mentioning

confidence: 98%

“…1 H NMR (acetone-d 6 ,2 H),4 H),6.68 (d,J = 8.8 Hz,2 H), , 1 H) 3, 165.1, 137.8, 136.7, 130.5, 129.3, 129.1, 113.8, 105.3, 51.6, 48.6, 41.4, 28.5, 27.9, 21.3 …”

Section: 2-dimethyl-5-[4-nitrophenyl(furan-2-yl)methyl]-13-dioxanementioning

confidence: 99%

Practical Method for the Preparation of 2,2-Dimethyl-5-{aryl[(hetero)aryl]methyl}-1,3-dioxane-4,6-diones: Synthesis and Mechanistic Study

et al. 2016

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“…Although some scientists recently have synthesized necroptosis inhibitors, such as Nec-3 [ 16 ], Nec-5 [ 17 ], Nec-7 [ 18 ], Nec-21 [ 19 ], etc., the mechanism still needs to be further clarified. Nec-1 is a synthetic small molecular compound which is the most commonly used in necroptosis inhibition [ 1 ].…”

Section: Introductionmentioning

confidence: 99%

The effect and underlying mechanism of Timosaponin B-II on RGC-5 necroptosis induced by hydrogen peroxide

Jiang

Shang

Xue

et al. 2014

BMC Complement Altern Med

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BackgroundNecroptosis is an important mode of cell death, which is due to oxidant stress accumulation. Our previous study indicated that oxidant stresses could be reduced by Timosaponin B-II (TBII), a kind of Chinese herb RhizomaAnemarrhenae monomer extraction. We wonder the possible effect of Timosaponin B-II, whether it can protect cells from necroptosis via reducing the oxidant stress, in RGC-5 following hydrogen peroxide (H2O2) insult.MethodsRGC-5 cells were grown in DMEM, the model group was exposed in H2O2 with the concentration of 300 μM, and the experimental group was pre-treated with Timosaponin B-II at different concentrations (1 μM, 10 μM, 100 μM and 1000 μM) for 24 hrs. MTT assay was carried out to measure the cytotoxicity of H2O2, MDA concentration assay was executed to evaluate the degree of oxidative stress, TNF-α ELISA Assay was used to measure the concentration of TNF-α, finally, the degree of necrosis were analyzed using flow cytometry.ResultsWe first constructed the cell injury model of necroptosis in RGC-5 upon H2O2 exposure. Morphological observation and MTT assay were used to evaluate the degree of RGC-5 death. MDA assay were carried out to describe the degree of oxidant stress. Annexin V/PI staining was used to detect necroptotic cells pre-treated with or without Timosaponin B-II following H2O2 injury. TNF-α ELISA was carried out to detect the TNF-α accumulation in RGC-5. Upon using Timosaponin B-II with concentration of 100 μM, the percentage of cell viability was increased from 50% to 75%, and the necrosis of cells was reduced from 35% to 20% comparing with H2O2 injury group. Oxidant stress and TNF-α was reduced upon injury which decreased the ratio of RGC-5 necroptosis.ConclusionOur study found out that Timosaponin B-II might reduce necroptosis via inhibition of ROS and TNF-α accumulation in RGC-5 following H2O2 injury.

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A novel necroptosis inhibitor—necrostatin-21 and its SAR study

Cited by 28 publications

References 13 publications

A new kind of cell suicide: mechanisms and functions of programmed necrosis

A new kind of cell suicide: mechanisms and functions of programmed necrosis

Practical Method for the Preparation of 2,2-Dimethyl-5-{aryl[(hetero)aryl]methyl}-1,3-dioxane-4,6-diones: Synthesis and Mechanistic Study

The effect and underlying mechanism of Timosaponin B-II on RGC-5 necroptosis induced by hydrogen peroxide

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