scholarly journals In VitroAnticancer Activity of a Nonpolar Fraction fromGynostemma pentaphyllum(Thunb.) Makino

2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Yantao Li ◽  
Jiajun Huang ◽  
Wanjun Lin ◽  
Zhongwen Yuan ◽  
Senling Feng ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cell Cycle Progression ◽  
Chemical Components ◽  
Anticancer Activities ◽  
Cancer Cell Growth ◽  
Nonpolar Fraction ◽  
Induced Apoptosis ◽  
Regulation Of Cell Cycle

Gynostemma pentaphyllum(Thunb.) Makino (GpM) has been widely used in traditional Chinese medicine (TCM) for the treatment of various diseases including cancer. Most previous studies have focused primarily on polar fractions of GpM for anticancer activities. In this study, a nonpolar fraction EA1.3A from GpM showed potent growth inhibitory activities against four cancer cell lines with IC50ranging from 31.62 μg/mL to 38.02 μg/mL. Furthermore, EA1.3A also inhibited the growth of breast cancer cell MDA-MB-453 time-dependently, as well as its colony formation ability. EA1.3A induced apoptosis on MDA-MB-453 cells both dose-dependently and time-dependently as analyzed by flow cytometry and verified by western blotting analysis of apoptosis marker cleaved nuclear poly(ADP-ribose) polymerase (cPARP). Additionally, EA1.3A induced cell cycle arrest in G0/G1 phase. Chemical components analysis of EA1.3A by GC-MS revealed that this nonpolar fraction from GpM contains 10 compounds including four alkaloids, three organic esters, two terpenes, and one catechol substance, and all these compounds have not been reported in GpM. In summary, the nonpolar fraction EA1.3A from GpM inhibited cancer cell growth through induction of apoptosis and regulation of cell cycle progression. Our study shed light on new chemical bases for the anticancer activities of GpM and feasibilities to develop new anticancer agents from this widely used medicinal plant.

scholarly journals Extract of Juniperus indica Bertol Synergizes with Cisplatin to Inhibit Oral Cancer Cell Growth via Repression of Cell Cycle Progression and Activation of the Caspase Cascade

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2746 ◽  
Author(s):  
Xiao-Fan Huang ◽  
Kai-Fu Chang ◽  
Shan-Chih Lee ◽  
Chia-Yu Li ◽  
Hung-Hsiu Liao ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Oral Cancer ◽  
Anticancer Agents ◽  
Cell Cycle Progression ◽  
Anticancer Agent ◽  
Synergistic Effects ◽  
Cancer Cell Growth ◽  
Cycle Progression ◽  
Common Cancer ◽  
Caspase Cascade

Oral cancer—a type of head and neck cancer—is estimated to be the fifth most common cancer in Taiwan. However, efficacious therapies for oral cancer are still lacking due to drug resistance and recurrence. Consequently, the identification of new anticancer agents for clinical treatment is needed. Juniperus indica Bertol is a plant of the Juniperus genus often used as a treatment in traditional medicine due to its anti-inflammatory, antibacterial and diuretic functions. The biofunctions of Juniperus indica Bertol including its anticancer potential, have not been fully explored. As a result, the aim of this research was to investigate the anticancer activity of Juniperus indica Bertol extract (JIB extract) and determine whether JIB extract has synergistic effects with cisplatin in oral cancer. These results are the first to demonstrate that JIB extract exhibits anticancer capacity and synergizes with cisplatin to treat oral cancer. Our findings indicate that JIB extract has a potential to develop anticancer agent and chemo therapeutic adjuvant for oral cancer.

scholarly journals Design, Synthesis, In Vitro Anticancer Evaluation and Molecular Modelling Studies of 3,4,5-Trimethoxyphenyl-Based Derivatives as Dual EGFR/HDAC Hybrid Inhibitors

2021 ◽  
Vol 14 (11) ◽  
pp. 1177
Author(s):  
Tarek S. Ibrahim ◽  
Azizah M. Malebari ◽  
Mamdouh F. A. Mohamed
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Hydroxamic Acid ◽  
Phenyl Group ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Molecular Docking Study

Recently, combining histone deacetylase (HDAC) inhibitors with chemotherapeutic drugs or agents, in particular epidermal growth factor receptor (EGFR) inhibitors, is considered to be one of the most encouraging strategy to enhance the efficacy of the antineoplastic agents and decrease or avoid drug resistance. Therefore, in this work, based on introducing 3,4,5-trimethoxy phenyl group as a part of the CAP moiety, in addition to incorporating 4–6 aliphatic carbons linker and using COOH or hydroxamic acid as ZBG, 12 novel EGFR/HDAC hybrid inhibitors 2a–c, 3a–c, 4a–c and 5a–c were designed, constructed, and evaluated for their anticancer activities against 4 cancer cell lines (HepG2, MCF-7, HCT116 and A549). Among all, hybrids with hydroxamic acid 4a–c and 5a, exhibited the highest inhibition against all cancer cell lines with IC50 ranging from 0.536 to 4.892 μM compared to Vorinostat (SAHA) with IC50 ranging from 2.43 to 3.63 μM and Gefitinib with IC50 ranging from 1.439 to 3.366 μM. Mechanistically, the most potent hybrids 4a–c and 5a were further tested for their EGFR and HDACs inhibitory activities. The findings disclosed that hybrid 4b displayed IC50 = 0.063 µM on the target EGFR enzyme which is slightly less potent than the standard Staurosporine (IC50 = 0.044 µM). Furthermore, hybrid 4b showed less HDAC inhibitory activity IC50 against HDAC1 (0.148), 2 (0.168), 4 (5.852), 6 (0.06) and 8 (2.257) than SAHA. In addition, the investigation of apoptotic action of the most potent hybrid 4b showed a significant increase in Bax level up to 3.75-folds, with down-regulation in Bcl2 to 0.42-fold, compared to the control. Furthermore, hybrid 4b displayed an increase in the levels of Caspases 3 and 8 by 5.1 and 3.15 folds, respectively. Additionally, the cell cycle analysis of hybrid 4b revealed that it showed programmed cell death and cell cycle arrest at G1/S phase. Moreover, all these outcomes together with the molecular docking study recommended the rationalized target hybrids 4a–c and 5a, particularly 4b, may be considered to be promising lead candidates for discovery of novel anticancer agents via dual inhibition of both EGFR/HDAC enzymes.

scholarly journals XRCC2 Promotes Colorectal Cancer Cell Growth, Regulates Cell Cycle Progression, and Apoptosis

Medicine ◽  
2014 ◽  
Vol 93 (28) ◽  
pp. e294 ◽  
Author(s):  
Kaiwu Xu ◽  
Xinming Song ◽  
Zhihui Chen ◽  
Changjiang Qin ◽  
Yulong He ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cell Cycle ◽  
Cell Growth ◽  
Cancer Cell ◽  
Cell Cycle Progression ◽  
Colorectal Cancer Cell ◽  
Cancer Cell Growth ◽  
Cycle Progression

scholarly journals Enzymatic and Biological Characterization of Novel Sirtuin Modulators against Cancer

2019 ◽  
Vol 20 (22) ◽  
pp. 5654 ◽  
Author(s):  
Vincenzo Carafa ◽  
Angelita Poziello ◽  
Laura Della Torre ◽  
Pia Giovannelli ◽  
Marzia Di Donato ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cell Cycle Progression ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cellular Level ◽  
Human Cancer Cell Lines ◽  
Regulation Of Cell Cycle

Sirtuins, a family of nicotinamide adenine dinucleotide (NAD+)-dependent lysine deacetylases, are promising targets for anticancer treatment. Recently, we characterized a novel pan-sirtuin (SIRT) inhibitor, MC2494, displaying antiproliferative effects and able to induce death pathways in several human cancer cell lines and decrease tumor growth in vivo. Based on the chemical scaffold of MC2494, and by applying a structure–activity relationship approach, we developed a small library of derivative compounds and extensively analyzed their enzymatic action at cellular level as well as their ability to induce cell death. We also investigated the effect of MC2494 on regulation of cell cycle progression in different cancer cell lines. Our investigations indicated that chemical substitutions applied to MC2494 scaffold did not confer higher efficacy in terms of biological activity and SIRT1 inhibition, but carbethoxy-containing derivatives showed higher SIRT2 specificity. The carbethoxy derivative of MC2494 and its 2-methyl analog displayed the strongest enzymatic activity. Applied chemical modifications improved the enzymatic selectivity of these SIRT inhibitors. Additionally, the observed activity of MC2494 via cell cycle and apoptotic regulation and inhibition of cell migration supports the potential role of SIRTs as targets in tumorigenesis and makes SIRT-targeting molecules good candidates for novel pharmacological approaches in personalized medicine.

scholarly journals 10-Gingerol Inhibits Ovarian Cancer Cell Growth by Inducing G2Arrest

2019 ◽  
Vol 9 (4) ◽  
pp. 685-689 ◽  
Author(s):  
Andrea Rasmussen ◽  
Kaylee Murphy ◽  
David W. Hoskin
Keyword(s):  
Cell Cycle ◽  
Ovarian Cancer ◽  
Cell Growth ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Cell Cycle Progression ◽  
Ovarian Cancer Cell ◽  
Cell Number ◽  
Ovarian Cancer Cells ◽  
Cancer Cell Growth

Purpose: Gingerol homologs found in the rhizomes of ginger plants have the potential to benefithuman health, including the prevention and treatment of cancer. This study evaluated the effectof 10-gingerol on ovarian cancer cell (HEY, OVCAR3, and SKOV-3) growth.Methods: Cell growth was measured by MTT assays, flow cytometry was used to assess cellproliferation, cytotoxicity and cell cycle progression, and western blotting was used to measurecyclin protein expression.Results: Ovarian cancer cells that were treated with 10-gingerol experienced a time- anddose-dependent decrease in cell number, which was due to a reduction in cell proliferationrather than a cytotoxic effect. Reduced proliferation of 10-gingerol-treated ovarian cancercells was associated with an increased percentage of cells in G2 phase of the cell cycle anda corresponding reduction in the percentage of cells in G1. Ovarian cancer cells also showeddecreased cyclin A, B1, and D3 expression following exposure to 10-gingerol.Conclusion: These findings revealed that 10-gingerol caused a G2 arrest-associated suppressionof ovarian cancer cell growth, which may be exploited in the management of ovarian cancer.<br />

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