scholarly journals Novel 11-Substituted Ellipticines as Potent Anticancer Agents with Divergent Activity against Cancer Cells

2019 ◽  
Vol 12 (2) ◽  
pp. 90 ◽  
Author(s):  
Charlotte M. Miller ◽  
Elaine C. O’Sullivan ◽  
Florence O. McCarthy
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Natural Product ◽  
Anticancer Agents ◽  
Cellular Growth ◽  
Growth Effects

Ellipticines have well documented anticancer activity, in particular with substitution at the 1-, 2-, 6- and 9-positions. However, due to limitations in synthesis and coherent screening methodology the full SAR profile of this anticancer class has not yet been achieved. In order to address this shortfall, we have set out to explore the anticancer activity of this potent natural product by substitution. We currently describe the synthesis of novel 11-substituted ellipticines with two specific derivatives showing potency and diverging cellular growth effects.

scholarly journals NBM-HD-1: A Novel Histone Deacetylase Inhibitor with Anticancer Activity

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Wei-Jan Huang ◽  
Yu-Chih Liang ◽  
Shuang-En Chuang ◽  
Li-Ling Chi ◽  
Chi-Yun Lee ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Xenograft Model ◽  
Cyclin B1 ◽  
Dependent Manner ◽  
Cell Cycle Regulators ◽  
Anticancer Activities ◽  
Gene Expressions

HDAC inhibitors (HDACis) have been developed as promising anticancer agents in recent years. In this study, we synthesized and characterized a novel HDACi, termed NBM-HD-1. This agent was derived from the semisynthesis of propolin G, isolated from Taiwanese green propolis (TGP), and was shown to be a potent suppressor of tumor cell growth in human breast cancer cells (MCF-7 and MDA-MB-231) and rat glioma cells (C6), with an IC50ranging from 8.5 to 10.3 μM. Western blot demonstrated that levels of p21(Waf1/Cip1), gelsolin, Ac-histone 4, and Ac-tubulin markedly increased after treatment of cancer cells with NBM-HD-1. After NBM-HD-1 treatment for 1–4 h, p-PTEN and p-AKT levels were markedly decreased. Furthermore, we also found the anticancer activities of NBM-HD-1 in regulating cell cycle regulators. Treatment with NBM-HD-1,p21(Waf1/Cip1)gene expression had markedly increased whilecyclin B1andD1gene expressions had markedly decreased. On the other hand, we found that NBM-HD-1 increased the expressions of tumor-suppressor genep53in a dose-dependent manner. Finally, we showed that NBM-HD-1 exhibited potent antitumor activity in a xenograft model. In conclusion, this study demonstrated that this compound, NBM-HD-1, is a novel and potent HDACi with anticancer activityin vitroandin vivo.

ANTICANCER POTENTIAL OF PLANT EXTRACTS FROM RIYADH (SAUDI ARABIA) ON MDA-MB-231 BREAST CANCER CELLS

2018 ◽  
Vol 15 (4) ◽  
pp. 46 ◽  
Author(s):  
Fahd A. Nasr ◽  
Nael Abutaha ◽  
Mohammad Al-Zahrani ◽  
Muhammad Farooq ◽  
Mohammad A Wadaan
Keyword(s):  
Breast Cancer ◽  
Saudi Arabia ◽  
Medicinal Plants ◽  
Traditional Medicine ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Breast Cancer Cells ◽  
Morphological Changes ◽  
Cell Integrity

Background: Medicinal plants have been used in traditional medicine for the treatment of numerous diseases worldwide. There is a dire need for new anticancer agents and plants used in traditional medicine are a particularly useful source. Materials and methods: In this study, extracts of five different plants that grow in the desert of Saudi Arabia were evaluated to assess their cytotoxicity against the MDA-MB-231 breast cancer cell line. Soxhlet extraction was carried out on the leaves and stems using different solvents. The cytotoxicity of these extracts against MDA-MB-231 breast cancer cells was assessed using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays. The apoptotic cellular morphological changes were observed using inverted and fluorescence microscopes. Results: Our results showed that two of the five different medicinal plants (Rumex vesicarius and Malva parviflora) exhibited strong anticancer activity against the breast cancer cells. Specifically, 2 of the 40 extracts (from the five studied plants) showed promising activity. The chloroform extract of the stem of R. vesicarius (RSV CHCL3) exhibited moderate anticancer activity with a half-maximal inhibitory concentration (IC50) of 230 µg/mL while that of the hexane extract of M. parviflora stems (MPS Hex) was 248 µg/mL. Loss of cell integrity, shrinkage of the cytoplasm, and cell detachment were observed in the extract-treated MDA-MB-231 cells. Conclusion: R. vesicarius and M. parviflora chloroform and n-hexane stem extracts showed significant cytotoxicity against MDA-MB-231 human breast carcinoma cells.

scholarly journals Potential of Anti-Cancer Activity of Secondary Metabolic Products from Marine Fungi

2021 ◽  
Vol 7 (6) ◽  
pp. 436
Author(s):  
Efaq Noman ◽  
Muhanna Mohammed Al-Shaibani ◽  
Muhammed Adnan Bakhrebah ◽  
Reyad Almoheer ◽  
Mohammed Al-Sahari ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Marine Fungi ◽  
Metabolic Process ◽  
Anticancer Compounds ◽  
Current Review ◽  
Anti Cancer ◽  
Metabolic Products ◽  
Available Information

The promising feature of the fungi from the marine environment as a source for anticancer agents belongs to the fungal ability to produce several compounds and enzymes which contribute effectively against the cancer cells growth. L-asparaginase acts by degrading the asparagine which is the main substance of cancer cells. Moreover, the compounds produced during the secondary metabolic process acts by changing the cell morphology and DNA fragmentation leading to apoptosis of the cancer cells. The current review has analyed the available information on the anticancer activity of the fungi based on the data extracted from the Scopus database. The systematic and bibliometric analysis revealed many of the properties available for the fungi to be the best candidate as a source of anticancer drugs. Doxorubicin, actinomycin, and flavonoids are among the primary chemical drug used for cancer treatment. In comparison, the most anticancer compounds producing fungi are Aspergillus niger, A. fumigatus A. oryzae, A. flavus, A. versicolor, A. terreus, Penicillium citrinum, P. chrysogenum, and P. polonicum and have been used for investigating the anticancer activity against the uterine cervix, pancreatic cancer, ovary, breast, colon, and colorectal cancer.

Combretastatin A-4 inspired novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines as tubulin polymerization inhibitors, antimitotic and anticancer agents

MedChemComm ◽  
2014 ◽  
Vol 5 (6) ◽  
pp. 766-782 ◽  
Author(s):  
Nitesh Sanghai ◽  
Vaibhav Jain ◽  
Ranjan Preet ◽  
Somnath Kandekar ◽  
Sarita Das ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Tubulin Polymerization ◽  
Chromosomal Damage ◽  
Tubulin Polymerization Inhibitors

Novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines that exhibit potent tubulin polymerization inhibition, anticancer activity, anti-migration of cancer cells, chromosomal damage, and apoptosis have been developed.

scholarly journals In vitro Anticancer Activity of Marine Sponges Against T47D and HeLa Cell Lines

2020 ◽  
Vol 19 (1) ◽  
pp. 25-28
Author(s):  
Suciati ◽  
Lusiana Arifianti
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Marine Sponges ◽  
Hela Cell Lines

Marine sponges have been known as the source of natural products. Various metabolites with potent bioactivities have been reported from this organism. The current study aims to investigate the anticancer potency of three marine sponges namely Diacarnus debeauforti, Haliclona amboinensis and Agelas cavernosa collected from Barrang Lompo Island, South Sulawesi, Indonesia. The ethyl acetate extracts of the sponges were screened against T47D breast cancer cells and HeLa cervical cancer cells by using the MTT method. The results showed that these sponges demonstrated anticancer activity against both cancer cell lines. The lowest IC50 of 18.2 μg/ml was given by the extract of A. cavernosa against T47D cell line, while in the screening against HeLa cancer cell line, the extract of D. debeauforti revealed the highest potency with IC50 of 15.7 μg/ml. Our results suggested that the marine sponges namely D. debeauforti, H. amboinensis and A. cavernosa can be good candidates for the development of anticancer agents. Dhaka Univ. J. Pharm. Sci. 19(1): 25-28, 2020 (June)

scholarly journals Anticancer Activity of Some Ruthenium (III) Complexes with Quinolone Antibiotics: In Vitro Cytotoxicity, Cell Cycle Modulation, and Apoptosis-Inducing Properties in LoVo Colon Cancer Cell Line

2021 ◽  
Vol 11 (18) ◽  
pp. 8594
Author(s):  
Mirela Mihaila ◽  
Camelia Mia Hotnog ◽  
Marinela Bostan ◽  
Alexandra Cristina Munteanu ◽  
Ileana Adela Vacaroiu ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Colon Cancer ◽  
Cell Proliferation ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Cycle Phase ◽  
Quinolone Antibiotics ◽  
Induction Of Apoptosis ◽  
Cell Cycle Phases

Cisplatin is one of the most effective anticancer agents used to treat colon cancer, which is the third malignancy between the most common human cancers in the world, but the resistance developed represents an obstacle against the full success of chemotherapy. An emerging interest appeared in finding other metallic compounds, such as ruthenium(III) complexes, for chemotherapeutic application in cancer. Our study focused on the anticancer activity of several ruthenium (Ru) complexes with quinolone antibiotics in colon tumor cell cultures. Real-time cell analysis and drug-mediated cytotoxicity tests monitored the inhibitory effects in the drug-treated LoVo colon cancer cells. Flow cytometry assays were performed to evaluate cell cycle phases distribution and apoptotic events. The obtained results showed dose-dependent increased levels of cell lysis and induction of apoptosis in LoVo cancer cells treated with the Ru(III) complexes. In addition, data showed a major decrease in cell proliferation, since the percentages of cells distributed in the S cell cycle phase diminished, and a G0/G1 cell arrest was observed. Therefore, our results strongly suggest that the newly synthesized Ru(III) complexes might play an important role in future chemotherapeutic approaches, since their activity is based on diminishing cell proliferation, induction of apoptosis, and modulation of cell cycle phases.

Selective Cytotoxic Activity and DNA Damage by an Epoxyalkyl Galactopyranoside

2018 ◽  
Author(s):  
Estefanía Burgos-Morón ◽  
Nuria Pastor ◽  
Manuel Luis Orta ◽  
Julio José Jiménez-Alonso ◽  
Margarita Vega-Holm ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Dna Damage ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Excision Repair ◽  
Lactate Production ◽  
Glucose Consumption ◽  
Lung Cancer Cells ◽  
Normal Cells

Several clinically useful anticancer drugs selectively kill cancer cells by inducing DNA damage; the genomic instability and DNA repair defects of cancer cells make them more vulnerable than normal cells to the cytotoxicity of DNA-damaging agents. Because epoxide-containing compounds can induce DNA damage, we have used the MTT assay to evaluate the selective cytotoxicity of three epoxyalkyl galactopyranosides against A549 lung cancer cells and MRC-5 lung normal cells. Compound (2S,3S)-2,3-Epoxydecyl 4,6-O-(S)-benzylidene-β-D-galactopyranoside (EDBGP) showed the highest selective anticancer activity and was selected for mechanistic studies. After observing that EDBGP induced cellular DNA damage (comet assay), we found that cells deficient in nucleotide excision repair were hypersensitive to the cytotoxicity of this compound; this suggests that EDBGP may induce bulky DNA adducts. EDBGP did not inhibit glycolysis (glucose consumption and lactate production). Pre-treatment of lung cancer cells with several antioxidants did not reduce the cytotoxicity of EDBGP, thereby indicating that reactive oxygen species do not participate in the anticancer activity of this compound. Finally, EDBGP was screened against a panel of cancer cells and normal cells from several tissues, including three genetically modified skin fibroblasts with increasing degree of malignancy. Our results suggest that epoxyalkyl galactopyranosides are promising lead compounds for the development of new anticancer agents.

Known Triterpenes and their Derivatives as Scaffolds for the Development of New Therapeutic Agents for Cancer

2018 ◽  
Vol 25 (10) ◽  
pp. 1259-1269 ◽  
Author(s):  
Gregorio Peron ◽  
Giovanni Marzaro ◽  
Stefano Dall`Acqua
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Tumor Development ◽  
Therapeutic Agents ◽  
Cellular Growth ◽  
New Drugs ◽  
Inflammatory Processes ◽  
And Migration

Background: Plants produce several bioactive secondary metabolites whose are used as therapeutic agents to treat several diseases, among whom cancer. Triterpenes are secondary metabolites that exert inhibitory activity against multiple intracellular and extracellular targets in euchariotic cells. These targets are proteins involved in apoptosis, cell development and differentiation, angiogenesis, metastasis and inflammatory processes. The inhibition of their functions leads to decreased cellular growth, differentiation and migration, resulting in antitumor activity, as shown by several authors. Furthermore, during recent years synthetic triterpenoid derivatives have also been developed to implement potency and efficacy of starting compounds, allowing the obtainment of new agents having promising anticancer activity. Objective: In this review we report the latest results regarding anticancer activity of some of the most studied triterpenes in the field, as well as of their semi-synthetic derivatives, with the aim to summarize the role of triterpenes as molecular leads for the development of new classes of antitumor agents. Methods: We focused on the most recent literature regarding triterpenes in cancer treatment, highlighting the potential of developing new drugs starting from these natural compounds. Conclusion: Several “old” triterpenes as ursolic, betulinic and oleanolic acids were recently reconsidered as model compounds for the development of innovative anticancer agents. Their activity against proteins involved in tumor development enhances the opportunity to exploit these compounds as new multi-target therapeutic agents. Furthermore, the possibility to synthetize new compounds from their natural-occurring structures could be an alternative to overcome cellular resistance to drugs and could improve their therapeutic efficacy.

scholarly journals Flavonoid Nanoparticles: A Promising Approach for Cancer Therapy

Biomolecules ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 1268
Author(s):  
Malgorzata Dobrzynska ◽  
Marta Napierala ◽  
Ewa Florek
Keyword(s):  
Cancer Therapy ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
English Language ◽  
Science Data ◽  
Anticancer Properties ◽  
Toxicity Of Drugs ◽  
Low Solubility ◽  
Anti Tumour Effect

Flavonoids, a ubiquitous group of naturally occurring polyphenolic compounds, have recently gained importance as anticancer agents. Unfortunately, due to low solubility, absorption, and rapid metabolism of dietary flavonoids, their anticancer potential is not sufficient. Nanocarriers can improve the bioavailability of flavonoids. In this review we aimed to evaluate studies on the anticancer activity of flavonoid nanoparticles. A review of English language articles published until 30 June 2020 was conducted, using PubMed (including MEDLINE), CINAHL Plus, Cochrane, and Web of Science data. Most studies determining the anticancer properties of flavonoid nanoparticles are preclinical. The potential anticancer activity focuses mainly on MCF-7 breast cancer cells, A549 lung cancer cells, HepG2 liver cancer cells, and melanoma cells. The flavonoid nanoparticles can also support the anti-tumour effect of drugs used in cancer therapy by enhancing the anti-tumour effect or reducing the systemic toxicity of drugs.

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