scholarly journals Bioimaging of Nucleolin Aptamer-Containing 5-(N-benzylcarboxyamide)-2′-deoxyuridine More Capable of Specific Binding to Targets in Cancer Cells

2010 ◽  
Vol 2010 ◽  
pp. 1-9 ◽  
Author(s):  
Kyue Yim Lee ◽  
Hyungu Kang ◽  
Sung Ho Ryu ◽  
Dong Soo Lee ◽  
Jung Hwan Lee ◽  
...  
Keyword(s):  
Chemical Modification ◽  
Cancer Cells ◽  
Specific Binding ◽  
Confocal Imaging ◽  
Critical Parameters ◽  
Significant Activity ◽  
Imaging Analysis ◽  
Modified Nucleotides ◽  
Chemically Modified ◽  
Fluorescence Measurements

Chemically modified nucleotides have been developed and applied into SELEX procedure to find a novel type of aptamers to fit with targets of interest. In this study, we directly performed chemical modification of 5-(N-benzylcarboxyamide)-2′-deoxyuridine (called 5-BzdU) in the AS1411 aptamer, which binds to the nucleolin protein expressed in cancer cells. Forty-seven compounds of AS1411-containing Cy3-labeled 5-BzdU (called Cy3-(5-BzdU)-modified-AS1411) were synthesized by randomly substituting thymidines one to twelve in AS1411 with Cy3-labeled 5-BzdU. Both statistically quantified fluorescence measurements and confocal imaging analysis demonstrated at least three potential compounds of interest: number 12, 29 and 41 that significantly increased the targeting affinity to cancer cells but no significant activity from normal healthy cells. These results suggest that the position and number of substituents in AS1411 are critical parameters to improve the aptamer function. In this study, we demonstrated that chemical modification of the existing aptamers enhanced the binding and targeting affinity to targets of interest without additional SELEX procedures.

Recent Advances on Therapeutic Peptides for Breast Cancer Treatment

2020 ◽  
Vol 21 ◽  
Author(s):  
Samad Beheshtirouy ◽  
Farhad Mirzaei ◽  
Shirin Eyvazi ◽  
Vahideh Tarhriz
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Tumor Cells ◽  
Breast Cancer Cells ◽  
Specific Binding ◽  
High Specificity ◽  
The Novel ◽  
Anti Cancer ◽  
Therapeutic Peptides ◽  
Low Toxicity

: Breast cancer is a heterogeneous malignancy which is the second cause of mortality among women in the world. Increasing the resistance to anti-cancer drugs in breast cancer cells persuades researchers to search the novel therapies approaches for the treatment of the malignancy. Among the novel methods, therapeutic peptides which target and disrupt tumor cells have been of great interest. Therapeutic peptides are short amino acids monomer chains with high specificity to bind and modulate a protein interaction of interest. Several advantages of peptides such as specific binding on tumor cells surface, low molecular weight and low toxicity on normal cells make the peptides as an appealing therapeutic agents against solid tumors, particularly breast cancer. Also, National Institutes of Health (NIH) describes therapeutic peptides as suitable candidate for the treatment of drug-resistant breast cancer. In this review, we attempt to review the different therapeutic peptides against breast cancer cells which can be used in treatment and diagnosis of the malignancy. Meanwhile, we presented an overview of peptide vaccines which have been developed for the treatment of breast cancer.

Anticancer Activity and Topoisomerase II Inhibition of Naphthalimides with ω-Hydroxylalkylamine Side-Chains of Different Lengths

2019 ◽  
Vol 15 (5) ◽  
pp. 550-560
Author(s):  
Mateusz D. Tomczyk ◽  
Anna Byczek-Wyrostek ◽  
Klaudia Strama ◽  
Martyna Wawszków ◽  
Przemysław Kasprzycki ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Inhibitory Activity ◽  
Topoisomerase Ii ◽  
Significant Activity ◽  
Anticancer Activities ◽  
Human Colon Cancer ◽  
Substitution Pattern ◽  
Topo Ii

Background: The substituted 1,8-Naphthalimides (1H-benzo[de]isoquinoline-1,3(2H)- diones) are known as DNA intercalators stabilizing DNA-Topoisomerase II complexes. This interaction disrupts the cleavage-relegation equilibrium of Topo II, resulting in formation of broken strands of DNA. Objective: To investigate the influence of type of substituents and substitution positions in 1,8- naphthalimde skeleton on the inhibition of Topoisomerase II activity. Methods: The starting 1,8-naphthalimide were prepared from acenaphthene by introduction of appropriate substituents followed by condensation with ω-hydroxylakylamines of different chain length. The substituents were introduced to 1,8-naphthalimide molecule by nucleophilic substitution of leaving groups like nitro or bromo present in 4 or 4,5- positions using the ω- hydroxylalkylamines. The bioactivity of obtained compounds was examined in model cell lines. Results: Antiproliferative activity of selected compounds against HCT 116 human colon cancer cells, human non-small cell lung cells A549 and non-tumorigenic BEAS-2B human bronchial epithelium cells was examined. Several of investigated compounds exhibit a significant activity (IC50 µM to 7 µM) against model cancer cell lines. It was demonstrated that upon treatment with concentration of 200 µM, all derivatives display Topo II inhibitory activity, which may be compared with activity of Amonafide. Conclusion: The replacement of the nitro groups in the chromophore slightly reduces its anticancer activities, whereas the presence of both nitro group and ω-hydroxylalkylamine chain resulted in seriously increased anticancer activity. Obtained compounds showed Topo II inhibitory activity, moreover, influence of the substitution pattern on the ability to inhibit Topo II activity and cancer cells proliferation was observed.

Abilities of berberine and chemically modified berberines to inhibit proliferation of pancreatic cancer cells

2019 ◽  
Vol 71 ◽  
pp. 172-182 ◽  
Author(s):  
Stephen L. Abrams ◽  
Matilde Y. Follo ◽  
Linda S. Steelman ◽  
Kvin Lertpiriyapong ◽  
Lucio Cocco ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Cancer Cells ◽  
Chemically Modified ◽  
Pancreatic Cancer Cells

scholarly journals Phosphated Avocado Seed: A Renewable Biomaterial for Preparing a Flame Retardant Biofiller

2021 ◽  
Author(s):  
DAVID Zuluaga-Parra ◽  
L.F Ramos-deValle ◽  
Saul Sanchez ◽  
J.R. Torres-Lubián ◽  
J.A. Rodríguez-Gonzalez ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Chemical Modification ◽  
Flame Retardant ◽  
Photoelectron Spectroscopy ◽  
Morphological Changes ◽  
Ethylene Vinyl Acetate ◽  
Chemically Modified ◽  
Air Atmosphere ◽  
Thermal Stability Of ◽  
Avocado Seed

Abstract The cellulose and starch present in the avocado seed can be chemically modified to obtain biofillers with fire retarding characteristics. The resulting composites could be used as substitute of the corresponding halogenated composites. For this, the avocado seed was first washed, dehydrated and pulverized, and thereafter, chemically modified with phosphoric acid in the presence of urea. This was studied using infrared spectroscopy, nuclear magnetic resonance and X-Ray photoelectron spectroscopy, in order to determine the resulting chemical structure and confirm the presence of the proposed functional groups. In addition, scanning electron microscopy and elemental analysis were used, respectively, to establish the resulting morphological changes, as well as the elements present on the surface of the modified material. Thermogravimetric analysis was also carried out in order to establish the thermal stability of the material and predict the effect on the flame retardancy due to the mentioned chemical modification. Further tests established that the obtained modified structure and morphology of the avocado seed was highly dependent on the method used to dehydrate the pulverized avocado seed. It was also determined that chemical modification greatly increased the thermal stability of the avocado seed in air atmosphere. The flame-retardant effect of the modified avocado seed was assessed in polyethylene/ethylene-vinyl-acetate (PE/EVA) composites via cone calorimeter tests. These results showed that the modified avocado seed decreased the peak of the heat release rate (pHRR) by 50% and the total heat released (THR) by 15%. This phosphated avocado seed could be a good option as a renewable biofiller for polymer composites with enhanced flame-retardant properties.

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