MTBITC mediates cell cycle arrest and apoptosis induction in human HepG2 cells despite its rapid degradation kinetics in the in vitro model

The in vitro model of serum deprivation shows that the survival of SH-SY5Y neuronal cells is ensured by the intrinsic trophic activity of BDNF loop 4-th mimetic GSB‑106 (10-7 М), which is comparable to that of endogenous neurotrophin (10-9 М). The analysis of the cell cycle and S‑phase showed that GSB‑106, like BDNF, induces cell cycle arrest in the G1 phase, diminishes the number of cells in the S‑phase, reduces the number of apoptotic cells and does not stimulate proliferation.

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In vitro anticancer activity of pyrano[3, 2-c]chromene derivatives with both cell cycle arrest and apoptosis induction

Medicinal Chemistry Research ◽

10.1007/s00044-019-02494-3 ◽

2020 ◽

Vol 29 (4) ◽

pp. 617-629

Author(s):

Ahmed M. El-Agrody ◽

Ahmed M. Fouda ◽

Mohammed A. Assiri ◽

Ahmed Mora ◽

Tarik E. Ali ◽

...

Keyword(s):

Cell Cycle ◽

Anticancer Activity ◽

Cell Cycle Arrest ◽

Apoptosis Induction ◽

Cycle Arrest

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Pinocembrin-Enriched Fractions of Elytranthe parasitica (L.) Danser Modulates Apoptotic and MAPK Cellular Signaling in HepG2 Cells

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180911112127 ◽

2019 ◽

Vol 18 (11) ◽

pp. 1563-1572 ◽

Cited By ~ 1

Author(s):

Nimmy Kumar ◽

Akhila H. Shrungeswara ◽

Sanchari B. Mallik ◽

Subhankar Biswas ◽

Jesil Mathew ◽

...

Keyword(s):

Hepatocellular Carcinoma ◽

Cell Cycle ◽

Cell Cycle Arrest ◽

Cell Line ◽

Hepg2 Cells ◽

Mapk Pathway ◽

Mapk Signaling ◽

Expression Levels ◽

Cycle Arrest

Background: Hepatocellular carcinoma (HCC) is the fifth leading cause of cáncer mortality. Elytranthe parasitica (L.) Danser (EP), a hemiparasitic plant (Loranthaceae) has potent anti-cancer properties. Objective: In the study, we investigated the effect of EP fractions on the expression of apoptosis and mitogenactivated protein kinase (MAPK) markers deregulated in HCC. Bioactivity fractionation was performed to isolate the phytochemical(s) exerting anti-tumor activity in HepG2 cells. Method: Anti-proliferative, clonogenic and anti-metastatic effects of EP fractions were examined in hepatocellular carcinoma cell line, HepG2 by Sulphorhodamine B, colony formation and scratch wound assays respectively in hepatocellular cell line, HepG2. The effects of EP fractions on key markers of apoptosis and MAPK signaling pathways were explored. </P><P> Key findings: EP bioactive fractions showed significant anti-tumor potential, reduced clonogenicity and considerably inhibited cell migration in HepG2 cells in vitro. The fractions augmented annexin V binding and induced apoptosis by causing cell cycle arrest at G2/M and S phase checkpoints. The fractions increased expression levels of p53, bad, cleaved PARP (Poly ADP ribose polymerase) and cleaved Caspase-3. Expression levels of phosphorylated ERK1/2 (Extracellular signal-regulated kinase) were downregulated. Pinocembrin-7-O-ß-D-glucoside and chrysin were isolated and characterized for the first time from Elytranthe parasitica (L.) Danser. Conclusion: Our findings reveal that EP fractions induced cell cycle arrest and triggered apoptosis in HepG2 cells by upregulating apoptosis and deactivating MAPK pathway. It signifies that pinocembrin glycoside and chrysin are bioactive phytochemicals contributing to the potent anti-hepatocarcinoma effects on HepG2 cells. Hence, bioactive EP fractions could be used as a therapeutic agent for effective HCC therapy.

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Apoptosis Induction byPolygonum minusIs Related to Antioxidant Capacity, Alterations in Expression of Apoptotic-Related Genes, and S-Phase Cell Cycle Arrest in HepG2 Cell Line

BioMed Research International ◽

10.1155/2014/539607 ◽

2014 ◽

Vol 2014 ◽

pp. 1-13 ◽

Cited By ~ 5

Author(s):

Mohd Alfazari Mohd Ghazali ◽

Ghanya Al-Naqeb ◽

Kesavanarayanan Krishnan Selvarajan ◽

Mizaton Hazizul Hasan ◽

Aishah Adam

Keyword(s):

Cell Cycle ◽

Ethyl Acetate ◽

Antioxidant Capacity ◽

Cell Cycle Arrest ◽

Hepg2 Cells ◽

S Phase ◽

Antiproliferative Effect ◽

Phase Cell ◽

Apoptosis Induction ◽

Cycle Arrest

Polygonum minus(Polygonaceae) is a medicinal herb distributed throughout eastern Asia. The present study investigated antiproliferative effect ofP. minusand its possible mechanisms. Four extracts (petroleum ether, methanol, ethyl acetate, and water) were prepared by cold maceration. Extracts were subjected to phytochemical screening, antioxidant, and antiproliferative assays; the most bioactive was fractionated using vacuum liquid chromatography into seven fractions (F1–F7). Antioxidant activity was measuredviatotal phenolic content (TPC), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP) assays. Antiproliferative activity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Most active fraction was tested for apoptosis induction and cell cycle arrest in HepG2 cells using flow cytometry and confocal microscopy. Apoptotic-related gene expression was studied by RT-PCR. Ethyl acetate extract was bioactive in initial assays. Its fraction, F7, exhibited highest antioxidant capacity (TPC;113.16±6.2 mg GAE/g extract, DPPH;EC50:30.5±3.2 μg/mL, FRAP;1169±20.3 μmol Fe (II)/mg extract) and selective antiproliferative effect (IC50:25.75±1.5 μg/mL). F7 induced apoptosis in concentration- and time-dependent manner and caused cell cycle arrest at S-phase. Upregulation of proapoptotic genes (Bax,p53, andcaspase-3) and downregulation of antiapoptotic gene,Bcl-2, were observed. In conclusion, F7 was antiproliferative to HepG2 cells by inducing apoptosis, cell cycle arrest, andviaantioxidative effects.

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