scholarly journals Synthesis, Characterisation, andIn VitroAnticancer Activity of Curcumin Analogues Bearing Pyrazole/Pyrimidine Ring Targeting EGFR Tyrosine Kinase

2013 ◽  
Vol 2013 ◽  
pp. 1-14 ◽  
Author(s):  
Mohamed Jawed Ahsan ◽  
Habibullah Khalilullah ◽  
Sabina Yasmin ◽  
Surender Singh Jadav ◽  
Jeyabalan Govindasamy
Keyword(s):  
Anticancer Activity ◽  
National Cancer Institute ◽  
Active Compound ◽  
Pyrimidine Ring ◽  
Curcumin Analogues ◽  
Anticancer Effects ◽  
Screening Protocol ◽  
One Dose Assay ◽  
Potential Therapeutics

In search of potential therapeutics for cancer, we described herein the synthesis, characterization, andin vitroanticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H-pyrazole-1-yl(phenyl)methanone (10) which showed mean growth percent of −28.71 in one-dose assay and GI50values between 0.0079 and 1.86 µM in 5-dose assay.

scholarly journals Synthesis, Characterization, andIn VitroAnticancer Evaluation of Novel 2,5-Disubstituted 1,3,4-Oxadiazole Analogue

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Salahuddin ◽  
Avijit Mazumder ◽  
Mohammad Shaharyar
Keyword(s):  
Cell Lines ◽  
National Cancer Institute ◽  
High Dose ◽  
Anticancer Activities ◽  
Single High Dose ◽  
Screening Protocol ◽  
One Dose Assay ◽  
Potential Therapeutics

In this series, we have synthesised a new 2,5-disubstituted 1,3,4-oxadiazole in search of potential therapeutics for cancer. The anticancer activities were evaluated on a panel of 60 cell lines by the National Cancer Institute according to its own screening protocol. Out of the 24 compounds, 11 were selected and evaluated via single high dose (10−5 M). In the next phase, two compounds have been selected for five-dose assay. The compounds 3-(5-benzyl-1,3,4-oxadiazol-2-yl)quinolin-2(1H)-one18(NSC-776965) and 3-[5-(2-phenoxymethyl-benzoimidazol-1-ylmethyl)-[1,3,4]oxadiazol-2-yl]-2-p-tolyloxy-quinoline27(NSC-776971) showed mean growth percentage of 66.23 and 46.61, respectively, in one-dose assay and their GI50values ranging between 1.41–15.8 μM and 0.40–14.9 μM, respectively, in 5-dose assay.

scholarly journals Piperine: Old Spice and New Nutraceutical?

2019 ◽  
Vol 25 (15) ◽  
pp. 1729-1739 ◽  
Author(s):  
Katarina Smilkov ◽  
Darinka G. Ackova ◽  
Aleksandar Cvetkovski ◽  
Tatjana Ruskovska ◽  
Bojana Vidovic ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Active Compound ◽  
Molecular Level ◽  
Current Knowledge ◽  
Physiological Activity ◽  
Antioxidant Properties ◽  
Anticancer Effects ◽  
Reported Data ◽  
Dose Dependent ◽  
Carrier Systems

Background: Many of the activities associated with pepper fruits have been attributed to piperine, the most active compound present in these spices. Objective: This paper aims to provide an overview of the known properties of piperine, i.e. piperine’s chemistry, its physiological activity, documented interactions as a bioenhancer and reported data concerning its toxicity, antioxidant properties and anticancer activity. Discussion: It is known that piperine possesses several properties. In its interaction with other drugs, it can act as a bioavailability enhancer; this effect is also manifested in combination with other nutraceuticals, e.g. with curcumin, i.e. piperine can modify curcumin’s antioxidant, anti-inflammatory, antimicrobial and anticancer effects. Piperine displays significant immunomodulating, antioxidant, chemopreventive and anticancer activity; these effects have been shown to be dose-dependent and tissue-specific. However, the main limitation associated with piperine seems to be its low bioavailability, a disadvantage that innovative formulations are overcoming. Conclusion: It is predicted that an increasing number of studies will focus on piperine, especially those directed towards unraveling its properties at molecular level. The current knowledge about the action of piperine will form a foundation for ways to improve piperine’s bioavailability e.g. exploitation of different carrier systems. The therapeutical applications of this compound will be clarified, and piperine will be recognized as an important nutraceutical.

scholarly journals Anti-proliferative effects of the combination of Sulfamethoxazole and Quercetin via caspase3 and NFkB gene regulation: An in vitro and in vivo study

2021 ◽  
Author(s):  
Heba Sahyon ◽  
Eman N.M. Ramadan ◽  
Fayez Althobaiti ◽  
Mohammad M.A. Mashaly
Keyword(s):  
Anticancer Activity ◽  
Antioxidant Activities ◽  
Ehrlich Ascites Carcinoma ◽  
Selective Toxicity ◽  
Apoptotic Pathway ◽  
Cycle Arrest ◽  
Anticancer Effects ◽  
Ehrlich Ascites

Abstract Combination therapy comprising natural polyphenols and anticancer drugs has been used to decrease the adverse effects and increase the effectiveness and antioxidant activities of the drugs. The antioxidant and anticancer effects of quercetin (Q), a nutritive polyphenol, have been observed both in vitro and in vivo. Likewise, the anticancer activity of sulfamethoxazole (S) has been demonstrated in vitro and in vivo. This study aimed to investigate the in vitro and in vivo anticancer effects of Q alone and in combination with S. The in vitro effects of S, Q, and S + Q on HCT-116, HepG2, MCF-7, and PC3 cell lines were examined. Additionally, the in vivo effects of these drugs were evaluated using Ehrlich ascites carcinoma (EAC) tumor-bearing mice. The in vitro data revealed the potent anticancer activity of S + Q through the induction of apoptosis and cell cycle arrest. The EAC-inoculated mice treated with S + Q presented with elevated SOD, GSH, CAT, and TAC levels and decreased malondialdehyde levels compared with the untreated EAC group, thus revealing the antioxidant and protective actions of S + Q against EAC cells invasion. Furthermore, the downregulation of NFkB and upregulation of the caspase3 gene in the EAC-inoculated mice treated with the S + Q indicated the induction of the apoptotic pathway and decrease in both cell proliferation and metastasis. In conclusion, the combination of S and Q might exert anticancer effects by inducing apoptosis and exhibiting selective toxicity against the cancer cells and thereby protecting the vital organs.

scholarly journals Evaluating the anticancer effects of high-dilution preparations of carcinogens such as HIV virus, Hepatitis C virus, Ethanol and Cancer tissues in in-vitro models

2021 ◽  
Vol 18 (1) ◽  
pp. 11-26
Author(s):  
Rajesh Shah
Keyword(s):  
Hepatitis C ◽  
Anticancer Activity ◽  
Cell Line ◽  
Leukemia Cell Line ◽  
Human Leukemia ◽  
High Dilution ◽  
Anticancer Effects ◽  
Anti Cancer ◽  
Mcf 7

Background Cancer is one of the leading causes of mortality. The recent experiments with high-diluted preparations have shown anticancer effects in in-vitro and vivo models. The fundamental principle of homeopathy suggests that the substances capable of producing certain diseases may have a capacity to alter the same disease if used in the ultra-dilute-potentized form. This hypothesis led certain carcinogens for examining their potential anti-cancer efficacy. Method Sulforhodamine B assay is useful in determining the cytotoxicity in cell-based studies in evaluating anticancer agents. The protocol involved preparation of homeopathy dilutions, incubation of cells with homeopathy dilutions, SRB binding, and measurement of absorbance. Cells were treated with 30 potencies of HIV nosode, Hepatitis C nosode, Carcinosin, Cancer nosode, and Ethanol along with positive control (Adriamycin). The preparations were tested in HeLa, HepG2, A549, MCF 7, T 24, Jurkat, SCC 40, and HL-60 cell-lines. Results The homeopathic preparations have shown the anticancer activity measured as percentage growth inhibition. All the homeopathy preparations studied, exhibited anticancer activity on HeLa, HepG2, A 549, T 24, and HL-60 cells. Carcinosin showed the anticancer activity on the SCC 40 cells. Hepatitis C nosode, Carcinosin, and Cancer nosode have shown the anticancer activity on breast cancer cell line MCF-7. None of the preparations exhibited anticancer activity on Human Leukemia Cell Line. Conclusion High-dilution, potentized preparations of certain carcinogens have demonstrated anti-cancer, cytotoxic effects in the cell-line model, supporting the rationale of the fundamental homeopathic principle the Law of Similars, opening windows to its wider applications in healthcare.

scholarly journals Preparation, Characterization, and Anticancer Effects of Capsaicin-Loaded Nanoliposomes

Nutrients ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 3995
Author(s):  
Ali Al-Samydai ◽  
Walhan Alshaer ◽  
Emad A. S. Al-Dujaili ◽  
Hanan Azzam ◽  
Talal Aburjai
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Therapeutic Potential ◽  
Drug Loading ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Anticancer Effects ◽  
Pharmacokinetic Properties ◽  
Quantitative Analyses

Background: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin’s pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity. Methods: Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC50. Results: Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. Conclusion: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.

scholarly journals Synthesis and Anticancer Activity of Novel Benzofurancarboxamides

2020 ◽  
Vol 10 (6) ◽  
pp. 6597-6609
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
National Cancer Institute ◽  
Efficient Synthesis ◽  
Anticancer Activities ◽  
Developmental Therapeutics Program ◽  
Activity Evaluation ◽  
Developmental Therapeutics

In our present work, we presented an efficient synthesis and anticancer activity evaluation of some novel benzofurancarboxamides. Our proposed approaches provide the possibility to design benzofurans diversity with a considerable chemical novelty. The synthesized substances were selected by the National Cancer Institute (NCI) Developmental Therapeutics Program for the in vitro cell line screening to investigate their anticancer activity. The compounds with significant levels of anticancer activities have been found that can be used for further optimization.

scholarly journals In Vitro Anticancer Activity and Mechanism of Action of an Aziridinyl Galactopyranoside

Biomedicines ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 41
Author(s):  
Estefanía Burgos-Morón ◽  
Nuria Pastor ◽  
Manuel Luis Orta ◽  
Julio José Jiménez-Alonso ◽  
Carlos Palo-Nieto ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Excision Repair ◽  
Leukemia Cell ◽  
Normal Cells ◽  
Anticancer Effects ◽  
Leukemia Cell Lines ◽  
Bulky Dna Adducts ◽  
Inhibition Of Glycolysis

We recently screened a series of new aziridines β-D-galactopyranoside derivatives for selective anticancer activity and identified 2-methyl-2,3-[N-(4-methylbenzenesulfonyl)imino]propyl 2,3-di-O-benzyl-4,6-O-(S)-benzylidene-β-D-galactopyranoside (AzGalp) as the most promising compound. In this article, we explore the possible mechanisms involved in the cytotoxicity of this aziridine and evaluate its selective anticancer activity using cancer cells and normal cells from a variety of tissues. Our data show that AzGalp induces DNA damage (comet assay). Cells deficient in the nucleotide excision repair (NER) pathway were hypersensitive to the cytotoxicity of this compound. These results suggest that AzGalp induces bulky DNA adducts, and that cancer cells lacking a functional NER pathway may be particularly vulnerable to the anticancer effects of this aziridine. Several experiments revealed that neither the generation of oxidative stress nor the inhibition of glycolysis played a significant role in the cytotoxicity of AzGalp. Combinations of AzGalp with oxaliplatin or 5-fluorouracil slightly improved the ability of both anticancer drugs to selectively kill cancer cells. AzGalp also showed selective cytotoxicity against a panel of malignant cells versus normal cells; the highest selectivity was observed for two acute promyelocytic leukemia cell lines. Additional preclinical studies are necessary to evaluate the anticancer potential of AzGalp.

scholarly journals In Vitro Anticancer Activity and Mechanism of Action of an Aziridinyl Galactopyranoside

2018 ◽  
Author(s):  
Estefanía Burgos-Morón ◽  
Nuria Pastor ◽  
Manuel Luis Orta ◽  
Julio José Jiménez-Alonso ◽  
Carlos Palo-Nieto ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Excision Repair ◽  
Leukemia Cell ◽  
Normal Cells ◽  
Anticancer Effects ◽  
Leukemia Cell Lines ◽  
Bulky Dna Adducts ◽  
Inhibition Of Glycolysis

We recently screened a series of new aziridines &beta;-D-galactopyranoside derivatives for selective anticancer activity and identified 2-methyl-2,3-[N-(4-methylbenzenesulfonyl)imino]propyl 2,3-di-O-benzyl-4,6-O-(S)-benzylidene-&beta;-D-galactopyranoside (AzGalp) as the most promising compound. In this article, we explore possible mechanisms involved in the cytotoxicity of this aziridine and evaluate its selective anticancer activity using cancer cells and normal cells from a variety of tissues. Our data show that AzGalp induces DNA damage (detected with the comet assay). Cells deficient in the DNA repair pathway nucleotide excision repair (NER) were hypersensitive to the cytotoxicity of this compound. These results suggest that AzGalp induces bulky DNA adducts, and that cancer cells lacking a functional NER pathway may be particularly vulnerable to the anticancer effects of this aziridine. Several experiments revealed that neither the generation of oxidative stress nor the inhibition of glycolysis played a significant role in the cytotoxicity of AzGalp. The combinations of AzGalp with either oxaliplatin or 5-fluorouracil slightly improved the ability of both anticancer drugs to selectively kill cancer cells. AzGalp also displayed selective cytotoxicity against a panel of malignant cells versus normal cells; the highest selectivity was observed for two acute promyelocytic leukemia cell lines. Additional preclinical studies are necessary to evaluate the anticancer potential of AzGalp.

Discovery of New AKT1 Inhibitors by Combination of In silico Structure Based Virtual Screening Approaches and Biological Evaluations

2019 ◽  
Author(s):  
Filip Fratev ◽  
Denisse A. Gutierrez ◽  
Renato J. Aguilera ◽  
suman sirimulla
Keyword(s):  
Virtual Screening ◽  
Success Rate ◽  
Protein Interactions ◽  
In Silico ◽  
Biological Data ◽  
In Vitro Binding ◽  
Vitro Binding ◽  
Screening Protocol ◽  
Screening Approaches

AKT1 is emerging as a useful target for treating cancer. Herein, we discovered a new set of ligands that inhibit the AKT1, as shown by in vitro binding and cell line studies, using a newly designed virtual screening protocol that combines structure-based pharmacophore and docking screens. Taking together with the biological data, the combination of structure based pharamcophore and docking methods demonstrated reasonable success rate in identifying new inhibitors (60-70%) proving the success of aforementioned approach. A detail analysis of the ligand-protein interactions was performed explaining observed activities.<br>

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