Phyto-Facilitated Bimetallic ZnFe2O4 Nanoparticles via Boswellia carteri: Synthesis, Characterization and Anti-Cancer Activity.

2020 ◽  
Vol 21 ◽  
Author(s):  
Amer Imraish ◽  
Afnan Al-Hunaiti ◽  
Tuqa Abu-Thiab ◽  
Abed Al-Qader Ibrahim ◽  
Eman Hwaitat ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Metallic Nanoparticles ◽  
Bimetallic Nanoparticles ◽  
Iron Chloride ◽  
Nano Particles ◽  
Adverse Side Effect ◽  
Wide Range ◽  
Anti Cancer ◽  
Znfe2o4 Nanoparticles

Background: The growing unsatisfaction toward the available traditional chemotherapeutic agents enhanced the need to develop new methods for obtaining materials with more effective and safe anti-cancer properties. Over the past few years, usage of metallic nanoparticles has been a target for researchers of different scientific and commercial fields due to their tiny sizes, environment friendly properties and wide range applications. To overcome the obstacles of traditional physical and chemical methods for synthesis of such nanoparticles, a new less expensive and eco-friendly method has been adopted using natural existing organisms as a reducing agent to mediate synthesis of the desired metallic nanoparticles from their precursors, a process called green biosynthesis of nanoparticles. Objective: Here in the present study, zinc iron bimetallic nanoparticles (ZnFe2O4) were synthesized via an aqueous extract of Boswellia Carteri resin mixed with zinc acetate and iron chloride precursors, and they were tested for their anticancer activity. Methods: Various analytic methods were applied for the characterization of the Phyto synthesized ZnFe2O4 and they were tested for their anticancer activity against MDA-MB-231, K562, MCF-7 cancer cell lines and normal fibroblasts. Results: Our results demonstrate the synthesis of cubic structured bimetallic nanoparticles ZnFe2O4 with an average diameter 10.54 nm. MTT cytotoxicity assay demonstrate that our phyto-synthesized ZnFe2O4 nanoparticles exhibited a selective and potent anticancer activity against K562 and MDA-MB-231 cell lines with IC50 values 4.53 µM and 4.19 µM, respectively. Conclusion: In conclusion, our bio synthesized ZnFe2O4 nano particles show a promising environmentally friendly of low coast chemotherapeutic approach against selective cancers with a predicted low adverse side effect toward normal cells. Further in vivo advanced animal research should be done to execute their applicability in living organisms.

Green synthesis of mixed metallic nanoparticles using room temperature self-assembly

2017 ◽  
Vol 13 (2) ◽  
pp. 4671-4677 ◽  
Author(s):  
A. M. Abdelghany ◽  
A.H. Oraby ◽  
Awatif A Hindi ◽  
Doaa M El-Nagar ◽  
Fathia S Alhakami
Keyword(s):  
Self Assembly ◽  
Metallic Nanoparticles ◽  
Room Temperature ◽  
Bimetallic Nanoparticles ◽  
Reduction Process ◽  
Nano Particles ◽  
Nano Structure ◽  
Small Shift ◽  
Molar Ratios ◽  
Vis Spectroscopy

Bimetallic nanoparticles of silver (Ag) and gold (Au) were synthesized at room temperature using Curcumin. Reduction process of silver and gold ions with different molar ratios leads to production of different nanostructures including alloys and core-shells. Produced nanoparticles were characterized simultaneously with FTIR, UV/vis. spectroscopy, transmission electron microscopy (TEM), and Energy-dispersive X-ray (EDAX). UV/vis. optical absorption spectra of as synthesized nanoparticles reveals presence of surface palsmon resonance (SPR) of both silver at (425 nm) and gold at (540 nm) with small shift and broadness of gold band after mixing with resucing and capping agent in natural extract which suggest presence of bimetallic nano structure (Au/Ag). FTIR and EDAX data approve the presence of bimetallic nano structure combined with curcumin extract. TEM micrographs shows that silver and gold can be synthesized separately in the form of nano particles using curcumin extract. Synthesis of gold nano particles in presence of silver effectively enhance and control formation of bi-metallic structure.

Synthesis and Anticancer Activity of 9-O-Pyrazole Alkyl Substituted Berberine Derivatives

2019 ◽  
Vol 18 (11) ◽  
pp. 1639-1648 ◽  
Author(s):  
Daipeng Xiao ◽  
Fen He ◽  
Dongming Peng ◽  
Min Zou ◽  
Junying Peng ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Molecular Docking ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Human Lung Cancer ◽  
Drug Candidate ◽  
Molecular Docking Study ◽  
Protective Function ◽  
Anti Cancer ◽  
Cancer Activity

Background: Berberine (BBR), an isoquinoline plant alkaloid isolated from plants such as Coptis chinensis and Hydrastis canadensis, own multiple pharmacological activities. Objective: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. Methods: The anti-cancer activity was measured by MTT assay, and apoptosis was demonstrated by the annexin V-FITC/PI staining assay. The intracellular oxidative stress was investigated through DCFH-DA assay. The molecular docking study was carried out in molecular operating environment (MOE). Results: Compound B3 and B5 showed enhanced anti-cancer activity compared with BBR, the IC50 for compound B3 and B5 were significantly lower than BBR, and compound B3 at the concentration of 64 or 128 µM induced apoptosis in HeLa and A549 cell lines. The reactive oxygen species (ROS) was generated in both cell lines when treated with 100 µM of all the compounds, and compound B3 and B5 induced higher activity in the generation of ROS, while compound B3 exhibited the highest activity, these results are in accordance with the cytotoxicity results, indicating the cytotoxicity were mostly generated from the oxidative stress. In addition, molecular docking analysis showed that compound B3 had the greatest affinity with Hsp90. Upon binding, the protective function of Hsp90 was lost, which might explain its higher cytotoxicity from molecular interaction aspect. Conclusion: All the results demonstrated that compound B3 and B5 showed significantly higher anti-cancer ability than BBR, and compound B3 is a promising anticancer drug candidate.

scholarly journals Regioselective synthesis of triazolo[3,4-e]purine derivatives and their anti-cancer activity against NCI-60 cell-lines

Folia Medica ◽  
2021 ◽  
Vol 63 (2) ◽  
pp. 213-220
Author(s):  
Khushal Kapadiya ◽  
Kishor Kavadia ◽  
Jyoti Gohel ◽  
Ranjan Khunt
Keyword(s):  
Cell Lines ◽  
Dose Response ◽  
Anticancer Agents ◽  
Triazole Ring ◽  
Purine Nucleoside ◽  
Step Procedure ◽  
Wide Range ◽  
Anti Cancer ◽  
Acid Catalyzed ◽  
Purine Ring

Introduction: Due to the vast medicinal importance of purine nucleoside, a hybrid molecule of triazole with purine ring might explode a lead molecule in the pharma sector and based on the last decade’s studies suggested that the nitrogen-rich molecules possess a wide range of medicinal importance. Aim: Due to the vast application of purine nucleoside itself in the field of cancer research, we synthesized triazolo[3,4-e]purines and screened them for their anti-cancer study against NCI-60 cell lines by the protocol used by NIH. Materials and methods: The targeted molecules, 4-chloro-5a,6-dihydro-8-substitutedphenyl-1H-[1,2,4]triazolo[3,4-e]purine derivatives (4a-4h) were synthesized in a two-step procedure by nucleophilic substitution (SN) at C-2 chlorine followed by formation of the triazole ring by acid-catalyzed reaction in the polar protic solvent. Results: It was observed that the regioselective approach followed in C-2 chlorine replacement instead of C-6 chlorine during SN reaction. One-dose response of selected three molecules (4a, 4b, and 4c) showed that 4b (K-562: 64.47 µM & SR: 63.38 µM; mean GI50: 99.09 µM) was found to be more potent than 4a and 4c. Conclusions: We have described in this study the general synthetic method for triazolo[3,4-e]purines as an innovative class of potential anticancer agents. The dose-response curve in the sense of mean GI50 for three compounds across all 60 cell lines, 4b can be served as lead after necessary modification.

scholarly journals Synthesis of Azide Functionalized Tetrahydrobenzofurans and their Antineoplastic Study

Folia Medica ◽  
2019 ◽  
Vol 61 (4) ◽  
pp. 551-558
Author(s):  
Chintan Pandit ◽  
Khushal M. Kapadiya
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Aromatic Aldehydes ◽  
Inhibitory Effect ◽  
Phenacyl Bromide ◽  
Azide Group ◽  
Anti Cancer ◽  
Comparable Activity ◽  
Derivatives Of

Background: In chemistry, the derivatives of benzofuran which are substituted on five-membered ring constitute one of the salient moieties in medicinal field and a survey of literature revealed that a good number of reports have shown that tetrahydrobenzofuran derivatives are of valuable biological activities. Aim: On the basis of previous survey, we aimed to generate a series of 2-(4-azidobenzoyl)-3-substitutedaryl-6,6-dimethyl-2,3,6,7-tetrahydrobenzofuran-4(5H)-one bearing azide group which were identified by anti-cancer screening against sixteen cell-lines of NCI (National Cancer Institute) using nine different cancer cell panels. Materials and methods: The tetrahydrobenzofuran derivatives were synthesized by multi-component reactions. It was achieved by coupling of dimedone (3.57 mmole), 4-azido phenacyl bromide (3.92 mmole) and various aromatic aldehydes (3.57 mmole) using two different bases i.e. pyridine and N,N- diethylethanamine under reflux condition. Anti-cancer activity was carried out by NCI-60 cell-lines using standard protocol by National Institute of Health. Results: The results from anti-cancer study shows that the compound 4a exhibited diverse cytotoxic activity against renal cancer panel (UO-31) with significant selectivity and had inhibitory effect on the generation of UO-31 (growth percent= 69.36%) and the compound 4e showed comparable activity in the same cell-line (UO-31: growth percent= 80.86%). Conclusions: In summary, a series of azide group containing tetrahydrobenzofuran derivatives have been synthesized and were evaluated for their anticancer activity. It was concluded that the derivatives 4a and 4e exhibited promising anticancer activity. Nature of substituent on phenyl ring seems to be the crucial factor affecting the activity in both the compounds.

A Venomics Approach to Identify and Characterize Biocactive Peptides (BAP) with Anti-Cancer Activity against Colorectal Cancer Cells from Animal Venoms (Preprint)

2021 ◽  
Author(s):  
Syeda Kiran Shahzadi ◽  
Noushad Karuvantevida ◽  
Yajnavalka Banerjee
Keyword(s):  
Colorectal Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Control Cell ◽  
Treatment Modalities ◽  
Health Issues ◽  
Anti Cancer ◽  
Pharmacologically Active ◽  
Animal Venoms ◽  
Cancer Activity

BACKGROUND Cancer is the third leading cause of death in the United Arab Emirates (UAE) after cardiovascular diseases and accidents. In UAE, colorectal cancer (CRC) is the first and fourth most common cancer in males and females respectively. Several treatment modalities have been employed for cancer treatment such as surgery, radiotherapy, chemotherapy, hormone replacement therapy, and immunotherapy. These treatment modalities often elicit adverse effects on normal cells, causing toxic side effects. To circumvent these toxicities, there has been an increased impetus towards the identification of alternate treatment strategies. Animal venoms are veritable gold mines of pharmacologically active polypeptides and proteins. OBJECTIVE In this proof-of-concept study, we avail a high throughput “Venomics” strategy to identify and characterize anticancer bioactive peptides (BAP) from 20 different animal venoms specifically targeting CRC. We chose to focus on CRC as it is one of the foremost health issues in the UAE. METHODS In initial study, we will screen 2500 different peptides derived from 20 different animal venoms for anticancer activity specifically directed against three CRC cell lines and two control cell lines employing the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric assay for cytotoxicity. Three venoms of the 20, which exhibited specific and potent anticancer activity directed against the three CRC cell lines will be selected; and from these three venoms the specific peptide(s) with anti-CRC activity will be isolated and characterized. RESULTS This study is at the protocol development stage only, and as such, no results are available. CONCLUSIONS In summary, the proposed study will not only generate therapeutic leads to manage/treat one of the leading health issues in the UAE i.e., CRC, but is also of commercial interest as the identified BAP with specific anti-cancer activity against CRC can be patented for commercialization.

DNA Fragmentation, Cell Cycle Arrest, and Docking Study of Novel Bis Spiro-cyclic 2-oxindole of Pyrimido[4,5-b]quinoline-4,6-dione Derivatives Against Breast Carcinoma

2018 ◽  
Vol 18 (4) ◽  
pp. 372-381 ◽  
Author(s):  
Magda F. Mohamed ◽  
Amr Mohamed Abdelmoniem ◽  
Ahmed H.M. Elwahy ◽  
Ismail A. Abdelhamid
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Anticancer Activity ◽  
Cell Cycle Arrest ◽  
Cell Lines ◽  
A549 Cell ◽  
Cytotoxic Effect ◽  
Quinoline Derivatives ◽  
Cycle Arrest ◽  
Wide Range

Background: Recently, it is reported that heterocycles containing pyrimidoquinoline moiety show a broad spectrum of medicinal and pharmacological properties including anticancer, anti-microbial, anti-inflammatory activities, analgesic and antiviral. In additions, spirocyclicoxindole containing compounds represent an important class of compounds that exhibit wide range of biological properties. The asymmetric chiral spiro carbon is considered to be the main criteria of the bioactivities. Spirooxindole structures represent the main skeleton for various alkaloids and pharmaceutically important compounds. Among them, the naturally occurring pyrrolidinylespirooxindole alkaloid, horsifiline that exhibits anticancer activity against human brain cancer cell lines. Objective: The objective of this study is the synthesis of novel bis spiro-cyclic 2-oxindole of pyrimido[4,5-b]quinoline derivatives and evaluate the anticancer activity of new compounds for synergistic purpose. Different genetic tools were used in an attempt to know the mechanism of action of this compound against breast cancer. Method: An efficient one pot synthesis of bis spiro-cyclic 2-oxindole derivatives of pyrimido[4,5- b]quinoline-4,6-dione using 6-aminouracil, bis-isatin and dimedone has been developed. The cytotoxic effect against different human cell lines MCF7, HCT116 and A549 cell lines was evaluated. The derivative 6a, was found the most encouraging compound in this series and it was selected for molecular studies against MCF7. Results: Our data indicated that compound 6a is an attractive target for breast cancer, as it inhibits proliferation, cell cycle progression and induces apoptosis of tumor cells. This inhibition is mediated by fragmentation of genomic DNA, up-regulation of [caspase-3, tumor suppressor gene p53, and pro-apoptotic gene BAX], and down-regulation of anti-apoptotic BCL2 gene. In additions it caused cell cycle arrest in S phase. This work provides an evidence of the potent effect of the new compound 6a and assists in the progress of new healing agents for cancer. Conclusion: We have developed an efficient method for the synthesis of novel bioactive bis spirocyclic 2-oxindole derivatives incorporating pyrimido[4,5-b]quinoline derivatives. Most of our new derivatives give potent cytotoxic effect more than the standard drug Fluorouracil (5-FU) especially, compound 6a which was the most active and promising one in this series against MCF7, HCT116, and A549 cell lines.

Anti-Cancer and Kinases Inhibitor Activities of Synthesized Heterocyclic Substituted Thiophene Fused with Cyclohexane Derivatives

2017 ◽  
Vol 14 (1) ◽  
pp. 768-774 ◽  
Author(s):  
Abd El-Galil E Amr ◽  
Hassan Z Ghanem ◽  
Mohamed A Al-Omar ◽  
Mohamed M Abdalla ◽  
Mohamed G Assy ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Mechanism Of Action ◽  
Sphingosine Kinase ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Kinase Inhibition ◽  
Wide Range ◽  
Anti Cancer

We herein report the anti-cancer and kinases inhibitor activities of some synthesized heterocyclic substituted thiophene fused with cyclohexane derivatives (Fig. 1) were synthesized before. Sixteen of these compounds were conveniently screened for their in vitro cytotoxicity against a wide range of cell lines, and showed potent activities against lung and leukemic cancer cell lines. The in vivo antilung and antileukemic cancers of the most active in vitro compounds was estimated and founded highly potent and compared to the standard drugs Bevacizumab and Etoposide. In search for the mechanism of action of anticancer activities it was found that these compounds exert its action via sphingosine kinase inhibition and inhibition of p53 ubiquitination.

scholarly journals Synthesis and anticancer properties of 1-(2-isopropyl-5-methylphenoxymethyl)-3R-4-aryl-5,6,7,8-tetrahydro-2,2а,8а-triazacyclopenta[cd]azulene derivatives

2018 ◽  
pp. 51-60
Author(s):  
S. A. Demchenko ◽  
A. E. Dudnik ◽  
T. A. Bukhtiarova ◽  
L. S. Bobkova ◽  
A. M. Demchenko
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Wide Spectrum ◽  
Basic Structure ◽  
Cancer Cell Lines ◽  
Anticancer Effect ◽  
Anticancer Properties ◽  
Wide Range

In recent years, attention to itself is attracted to the problem of treatment of cancer that is caused by increase in patients, especially of working age. Therefore, the enlargement of the arsenal of anticancer medicines of a wide spectrum of action is actual. The purpose of the study was to synthesize substances with potentially antitumor properties in a series 1-(2-isopropyl-5-methylphenoxymethyl)-3R-4-aryl-5,6,7,8-tetrahydro-2,2а,8а-triazacyclopenta[cd]azulene derivatives and to study the effect of synthesized compounds on inhibition of growth (or their destruction) of a wide range of cancer. The objects of the study were derivatives of 1-(2-isopropyl-5-methylphenoxymethyl)-3R-4-aryl-5,6,7,8-tetrahydro-2,2а,8а-triazacyclopenta[cd]azulene, which were synthesized by refluxing 3-(2-isopropyl-5-methylphenoxymethyl)-6,7,8,9-tetrahydro-5Н-[1,2,4]triazolo[4,3-a]azepine with с appropriate α-halogenketones in ethyl acetate and further cyclization in an alkaline medium. Использовали данные NMR 1Н spectroscopy data were used. The primary evaluation of anticancer activity was carried out National Cancer Institute of Health, USA within the Development Therapeutic Program. A series of new of 1-(2-isopropyl-5-methylphenoxymethyl)-3R-4-aryl-5,6,7,8-tetrahydro-2,2а,8а-triazacyclopenta[cd]azulene derivatives was synthesized, their structure and purity were confirmed by NMR 1Н spectroscopy. The anticancer activity of the synthesized compounds was studied both at a concentration of  10-5 mol/l and in a concentration gradient of 10-4‒10-8 mol/l in experiments in vivo on cancer cell lines. It is shown that insertion of methyl group into position 3 of heterocyclic system of the basic structure of 4-aryl-5,6,7,8-tetrahydro-2,2a,8a-triazacyclopenta[cd]azulene leads to an increase in the anticancer effect. It is found that the tested compounds showed high anticancer effect on all types of cancer cell lines investigated – leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer.

scholarly journals Crude and Chitosan Nano-particles Extracts of Some Maggots as Antioxidant and Anticancer Agents

2019 ◽  
pp. 1-8 ◽  
Author(s):  
Ahmed I. Hasaballah
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Crude Extract ◽  
Chitosan Nanoparticles ◽  
Radical Scavenging ◽  
Nano Particles ◽  
Liver Carcinoma ◽  
Crude Extracts ◽  
Hct 116

The antioxidant effects besides anticancer activities of Musca domestica, Lucilia sericata and Chrysomya albiceps maggots extracts against human liver carcinoma (HepG-2) and human colon carcinoma (HCT-116) were investigated. Two kinds of extracts, crude and chitosan nanoparticles (CNPs) were prepared. The antioxidant activity of different tested extracts was performed by DPPH radical scavenging method, the results obtained revealed that, the highest levels of DPPH scavenging activity were exhibited by the crude extracts of tested maggots with preference to C. albiceps extract, which exhibited a much more potent activity followed by L. sericata and M. domestica in crude and CNPs extracts. Crude extracts have lower anticancer activity than the CNPs extracts; however, the lowest percentage of cell viability (6.7±0.7%) was recorded by L. sericata crude extract against HCT-116, followed by C. albiceps crude extract (7.57±1.25%) against HepG-2 at the highest used concentration 100 µg/ml. The strongest anticancer activity was observed with CNPs extracts and it was recorded at concentrations of 80, 90 and 100 µg/ml against cell lines tested. Depending on Median inhibitory concentrations (IC50) of maggots crude and CNPs extracts, the IC50 values were in the range of 37.3 to 74.3 µg/ml and the highest anticancer activity was obtained by C. albiceps CNPs extracts against cell lines tested. In conclusion, both tested extracts have optimistic antioxidant activity. CNPs extracts have great therapeutic potential due to its anticancer inducing activities.

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