2,4,3′,4′-tetramethoxy-biphenyl induces apoptosis in MGC-803 cells through a mitochondrial/caspase pathway

Sui, Xin; Sun, Zhe; An, Wei; Cheng, Kai; Jiang, Shougang; Gong, Xun

doi:10.3329/bjp.v9i2.18430

Cited by 2 publications

(2 citation statements)

References 19 publications

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“…TMBP has also been reported to have anticancer activity through its action on increasing the production of reactive oxygen species (ROS), causing mitochondrial depolarization, inducing cell cycle arrest in the G2/M phase, and leading to the death by direct apoptosis on the lung cancer cell line A549 26 . The anti-proliferative and apoptosis-inducing effects of another biphenyl compound, viz., 2,4,3′,4′-tetramethoxybiphenyl, also reported apoptosis acting through a mitochondrial/caspase pathway on human gastric cancer MGC-803 cells 27 . Phenolic compounds furthermore have been reported in the literature as exhibiting antioxidant, antimicrobial, anti-carcinogenic, and anti-inflammatory activities 28 .…”

Section: Introductionmentioning

confidence: 90%

In-vitro biological evaluation of 3,3′,5,5′-tetramethoxy-biphenyl-4,4′-diol and molecular docking studies on trypanothione reductase and Gp63 from Leishmania amazonensis demonstrated anti-leishmania potential

Schirmann

Bortoleti

Gonçalves

et al. 2023

Sci Rep

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Available treatments for leishmaniasis have been widely used since the 1940s but come at a high cost, variable efficacy, high toxicity, and adverse side-effects. 3,3′,5,5′-Tetramethoxy-biphenyl-4,4′-diol (TMBP) was synthesized through laccase-catalysis of 2,6-dimethoxyphenol and displayed antioxidant and anticancer activity, and is considered a potential drug candidate. Thus, this study aimed to evaluate the anti-leishmanial effect of TMBP against promastigote and amastigote forms of Leishmania (L.) amazonensis and investigated the mechanisms involved in parasite death. TMBP treatment inhibited the proliferation (IC50 0.62–0.86 µM) and induced the death of promastigote forms by generating reactive oxygen species and mitochondrial dysfunction. In intracellular amastigotes, TMBP reduced the percentage of infected macrophages, being 62.7 times more selective to the parasite (CC50 53.93 µM). TMBP did not hemolyze sheep erythrocytes; indicative of low cytotoxicity. Additionally, molecular docking analysis on two enzyme targets of L. amazonensis: trypanothione reductase (TR) and leishmanolysin (Gp63), suggested that the hydroxyl group could be a pharmacophoric group due to its binding affinity by hydrogen bonds with residues at the active site of both enzymes. TMBP was more selective to the Gp63 target than TR. This is the first report that TMBP is a promising compound to act as an anti-leishmanial agent.

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Section: Introductionmentioning

confidence: 90%

In-vitro biological evaluation of 3,3′,5,5′-tetramethoxy-biphenyl-4,4′-diol and molecular docking studies on trypanothione reductase and Gp63 from Leishmania amazonensis demonstrated anti-leishmania potential

Schirmann

Bortoleti

Gonçalves

et al. 2023

Sci Rep

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“…32 Generally apoptosis happens though both intrinsic and extrinsic pathways. Both pathways have different caspases initiator.…”

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confidence: 99%

Assessment of Cytotoxicity of Smokeless Tobacco (Shammah) In Hepg2 and WRL68 Cells Line

Abdelwahab¹,

Mohan²,

Taha³

et al. 2015

Phcog J

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Shammah is a traditional form of chewing tobacco [Smokeless tobacco, (ST)] that is commonly used in the Middle east specially Saudi Arabia (KSA), Yemen and Sudan. The cytotoxicity of Sudanese and Yemenis ST hexane and methanol extracts was evaluated using MTT assay. Annexin-V assay has been used to detect the induction of apoptosis. Luminescence based assay also been conducted to check the level of caspases enzyme. The involvement of cell cycle check point arrest has been performed using flow cytometry analysis. The current study found that ST has the capacity to induce cell toxicity in human liver cells. The inhibitory capacity of ST in HepG2 and WRL 68 has been found to be 151 ± 2.5 and 305 ± 11.5 µg/ml for 24 h. An early apoptosis induction in HepG2 cells was observed by annexin V assay, which clearly exhibited significantly increased early and late apoptosis phases both at 24 and 48 h. Both the caspases-8 and-9 level was found to be increased by the introduction of ST to HepG2 cells significantly (p<0.05). Moreover the ST extract was able to arrest the cell cycle check point at G2/M phase. A significantly increasing pattern of hypodiploid phases of cells also been observed, which confirm the apoptosis induction again. Collectively, results presented in this study demonstrated that the ST, which is used as a euphoritic substance of abuse also, has significant level of toxicity in human cells. Moreover the mode of cell death was found to be though programmed cell death which is closely associated with cell cycle arrest.

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2,4,3′,4′-tetramethoxy-biphenyl induces apoptosis in MGC-803 cells through a mitochondrial/caspase pathway

Cited by 2 publications

References 19 publications

In-vitro biological evaluation of 3,3′,5,5′-tetramethoxy-biphenyl-4,4′-diol and molecular docking studies on trypanothione reductase and Gp63 from Leishmania amazonensis demonstrated anti-leishmania potential

In-vitro biological evaluation of 3,3′,5,5′-tetramethoxy-biphenyl-4,4′-diol and molecular docking studies on trypanothione reductase and Gp63 from Leishmania amazonensis demonstrated anti-leishmania potential

Assessment of Cytotoxicity of Smokeless Tobacco (Shammah) In Hepg2 and WRL68 Cells Line

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