Novel dibenzoxanthenes compounds inhibit human gastric cancer SGC-7901 cell growth by apoptosis

Xu, Yunran; Jia, Zhi; Liu, Yun-Jun; Wang, Xiuzhen

doi:10.1016/j.molstruc.2020.128588

Cited by 4 publications

(4 citation statements)

References 42 publications

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“…The dissipation of mitochondrial potential is strongly associated with mitochondrial production of reactive oxygen species (ROS) 71 , 73 . The production of ROS after 12c treatment at 50 and 250 nM, as well as CA-4 (50 nM) with hydrogen peroxide H 2 O 2 was followed with 2,7–dichlorofluorescin diacetate (H 2 -DCFDA).…”

Section: Resultsmentioning

confidence: 99%

“…Mitochondria membrane potential plays a crucial role in the propagation of apoptosis. Specifically, loss of mitochondrial membrane potential Dw mt (MMP) is characteristic of early stage of apoptosis [69][70][71] . To confirm whether compound 12c could decrease the MMP of MCF-7 cancer cells, MMP was monitored by the fluorescence of the dye DiOC2(3).…”

Section: Mitochondrial Membrane Potentialmentioning

confidence: 99%

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Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect

Ibrahim

Hawwas

Malebari

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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A new series of quinoline derivatives of combretastatin A-4 have been designed, synthesised and demonstrated as tubulin polymerisation inhibitors. These novel compounds showed significant antiproliferative activities, among them, 12c exhibited the most potent inhibitory activity against different cancer cell lines (MCF-7, HL-60, HCT-116 and HeLa) with IC 50 ranging from 0.010 to 0.042 mM, and with selectivity profile against MCF-10A non-cancer cells. Further mechanistic studies suggest that 12c can inhibit tubulin polymerisation and cell migration, leading to G 2 /M phase arrest. Besides, 12c induces apoptosis via a mitochondrial-dependant apoptosis pathway and caused reactive oxygen stress generation in MCF-7 cells. These results provide guidance for further rational development of potent tubulin polymerisation inhibitors for the treatment of cancer. HIGHLIGHTS A novel series of quinoline derivatives of combretastatin A-4 have been designed and synthesised. Compound 12c showed significant antiproliferative activities against different cancer cell lines. Compound 12c effectively inhibited tubulin polymerisation and competed with [ 3 H] colchicine in binding to tubulin. Compound 12c arrested the cell cycle at G 2 /M phase, effectively inducing apoptosis and inhibition of cell migration.

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Section: Resultsmentioning

confidence: 99%

Section: Mitochondrial Membrane Potentialmentioning

confidence: 99%

Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect

Ibrahim

Hawwas

Malebari

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…The cytotoxicity test was carried out according to a method described in the literature [ 24 ]. The cells were seeded into 96-well micro-assay culture plates and grown overnight in a 5% CO 2 incubator at 37 °C.…”

Section: Methodsmentioning

confidence: 99%

Synthesis, Characterization and Anticancer Efficacy Evaluation of Benzoxanthone Compounds toward Gastric Cancer SGC-7901

Fu¹,

Xu²,

Liu³

et al. 2022

Molecules

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Three benzoxanthone derivatives were synthesized through a new photochemical strategy. The in vitro cytotoxic activity of these compounds was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and their partition coefficients (logP) were measured by shake flask method. The pKa values of the compounds were detected by potentionmetric titration. The interaction of the compounds with calf thymus DNA (CT-DNA) was investigated by electronic absorption, luminescence spectra and viscosity. A molecular docking analysis was performed. The antitumor efficacy of the compounds was evaluated by cell apoptosis, cell cycle arrest, intracellular Ca2+ concentrations and reactive oxygen species (ROS) levels. The mitochondrial membrane potential was assayed using JC-1 (5,5′,6,6′-tetrachloro-1,1,3′,3′-tetraethyl-imidacarbocyanine iodide) as the fluorescence probe. The expression of Bcl-2 family protein, caspase 3 and poly ADP-ribose polymerase (PARP) was explored by western blot. The results showed that the compounds induced apoptosis through a ROS-mediated mitochondrial dysfunction pathway. This work provides an efficient approach to synthesize benzoxanthone derivatives, and is helpful for understanding the apoptotic mechanism.

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“…Also, GAL at dosages that lowered plasma glucose did not show any adverse effects in rats (Aloud et al, 2017). It was further demonstrated that GAL's effects were specified to cancer cells and did not cause cytotoxicity in normal cells (Xu et al, 2017; S. Yu et al, 2018; W. Zhang et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

The molecular mechanisms underlying anti‐inflammatory effects of galangin in different diseases

Hassanein

El-Maksoud

Ibrahim

et al. 2023

Phytotherapy Research

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When used as an alternative source of drugs to treat inflammation-associated diseases, phytochemicals with anti-inflammatory properties provide beneficial impacts.Galangin is one of the most naturally occurring flavonoids. Galangin has many biological activities, such as anti-inflammatory, antioxidant, antiproliferative, antimicrobial, anti-obesity, antidiabetic, and anti-genotoxic activities. We observed that galangin was well tolerated and positively impacted disease underlying inflammation for the renal, hepatic, central nervous system, cardiovascular, gastrointestinal system, skin, and respiratory disorders, as well as ulcerative colitis, acute pancreatitis, retinopathy, osteoarthritis, osteoporosis, and rheumatoid arthritis. Galangin anti-inflammatory effects are mediated mainly by suppressing p38 mitogen-activated protein kinases, nuclear factor-kappa B, and nod-like receptor protein 3 signals. These effects are confirmed and supported by molecular docking. Clinical translational research is required to accelerate the bench-to-bedside transfer and determine whether galangin can be utilised as a safe, natural source of pharmaceutical anti-inflammatory medication for humans.

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Novel dibenzoxanthenes compounds inhibit human gastric cancer SGC-7901 cell growth by apoptosis

Cited by 4 publications

References 42 publications

Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect

Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect

Synthesis, Characterization and Anticancer Efficacy Evaluation of Benzoxanthone Compounds toward Gastric Cancer SGC-7901

The molecular mechanisms underlying anti‐inflammatory effects of galangin in different diseases

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