Fluorescent Copper(II) Complexes of Asymmetric Bis(Thiosemicarbazone)s: Electrochemistry, Cellular Uptake and Antiproliferative Activity

2021 ◽  
Vol 6 (24) ◽  
pp. 6063-6070
Author(s):  
Deepti U. Kirtani ◽  
Niraj S. Ghatpande ◽  
Komal R. Suryavanshi ◽  
Prasad P. Kulkarni ◽  
Anupa A. Kumbhar
Keyword(s):  
Cellular Uptake ◽  
Antiproliferative Activity

Novel luminescent benzopyranothiophene- and BODIPY-derived aroylhydrazonic ligands and their dicopper(II) complexes: syntheses, antiproliferative activity and cellular uptake studies

2021 ◽  
Vol 26 (6) ◽  
pp. 675-688
Author(s):  
Jesica Paola Rada ◽  
Jérémy Forté ◽  
Geoffrey Gontard ◽  
Claude-Marie Bachelet ◽  
Nicolás A. Rey ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Antiproliferative Activity ◽  
Uptake Studies

scholarly journals Effective Cellular Transport of Ortho-Halogenated Sulfonamide Derivatives of Metformin Is Related to Improved Antiproliferative Activity and Apoptosis Induction in MCF-7 Cells

2020 ◽  
Vol 21 (7) ◽  
pp. 2389 ◽  
Author(s):  
Magdalena Markowicz-Piasecka ◽  
Ibrahim Komeil ◽  
Johanna Huttunen ◽  
Joanna Sikora ◽  
Kristiina M. Huttunen
Keyword(s):  
Cell Cycle ◽  
Chemical Modification ◽  
Cell Cycle Arrest ◽  
Cellular Uptake ◽  
Antiproliferative Activity ◽  
Breast Cancer Cell Lines ◽  
Cellular Transport ◽  
Apoptosis Induction ◽  
Cycle Arrest ◽  
Mcf 7

Metformin is a substrate for plasma membrane monoamine transporters (PMAT) and organic cation transporters (OCTs); therefore, the expression of these transporters and interactions between them may affect the uptake of metformin into tumor cells and its anticancer efficacy. The aim of this study was to evaluate how chemical modification of metformin scaffold into benzene sulfonamides with halogen substituents (compounds 1–9) may affect affinity towards OCTs, cellular uptake in two breast cancer cell lines (MCF-7 and MDA-MB-231) and antiproliferative efficacy of metformin. The uptake of most sulfonamides was more efficient in MCF-7 cells than in MDA-MB-231 cells. The presence of a chlorine atom in the aromatic ring contributed to the highest uptake in MCF-7 cells. For instance, the uptake of compound 1 with o-chloro substituent in MCF-7 cells was 1.79 ± 0.79 nmol/min/mg protein, while in MDA-MB-231 cells, the uptake was considerably lower (0.005 ± 0.0005 nmol/min/mg protein). The elevated uptake of tested compounds in MCF-7 was accompanied by high antiproliferative activity, with compound 1 being the most active (IC50 = 12.6 ± 1.2 µmol/L). Further studies showed that inhibition of MCF-7 growth is associated with the induction of early and late apoptosis and cell cycle arrest at the G0/G1 phase. In summary, the chemical modification of the biguanide backbone into halogenated sulfonamides leads to improved transporter-mediated cellular uptake in MCF-7 and contributes to the greater antiproliferative potency of studied compounds through apoptosis induction and cell cycle arrest.

Functionalized nonporous silica nanoparticles as carriers for Pt(iv) anticancer prodrugs

2016 ◽  
Vol 45 (43) ◽  
pp. 17233-17240 ◽  
Author(s):  
M. Ravera ◽  
E. Gabano ◽  
I. Zanellato ◽  
E. Perin ◽  
A. Arrais ◽  
...  
Keyword(s):  
Silica Nanoparticles ◽  
Cellular Uptake ◽  
Antiproliferative Activity

Conjugate Pt(iv)–silica nanoparticles exhibited better antiproliferative activity than cisplatin and Pt(iv) precursors, due to their more efficient cellular uptake.

scholarly journals Tyrosine–Chlorambucil Conjugates Facilitate Cellular Uptake through L-Type Amino Acid Transporter 1 (LAT1) in Human Breast Cancer Cell Line MCF-7

2020 ◽  
Vol 21 (6) ◽  
pp. 2132 ◽  
Author(s):  
Piman Pocasap ◽  
Natthida Weerapreeyakul ◽  
Juri Timonen ◽  
Juulia Järvinen ◽  
Jukka Leppänen ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Amino Acid ◽  
Cellular Uptake ◽  
Antiproliferative Activity ◽  
Human Breast Cancer ◽  
Amino Acid Transporter ◽  
Intracellular Uptake ◽  
Human Breast ◽  
Acid Transporter ◽  
Mcf 7

l-type amino acid transporter 1 (LAT1) is an amino acid transporter that is overexpressed in several types of cancer and, thus, it can be a potential target for chemotherapy. The objectives of this study were to (a) synthesize LAT1-targeted chlorambucil derivatives and (b) evaluate their LAT1-mediated cellular uptake as well as antiproliferative activity in vitro in the human breast cancer MCF-7 cell line. Chlorambucil was conjugated to l-tyrosine—an endogenous LAT1 substrate—via either ester or amide linkage (compounds 1 and 2, respectively). While chlorambucil itself did not bind to LAT1, its derivatives 1 and 2 bound to LAT1 with a similar affinity as with l-tyrosine and their respective cellular uptake was significantly higher than that of chlorambucil in MCF-7. The results of our cellular uptake study are indicative of antiproliferative activity, as a higher intracellular uptake of chlorambucil derivatives resulted in greater cytotoxicity than chlorambucil by itself. LAT1 thus contributes to intracellular uptake of chlorambucil derivatives and, therefore, increases antiproliferative activity. The understanding gained from our research can be used in the development of LAT1-targeted anticancer drugs and prodrugs for site-selective and enhanced chemotherapeutic activity.

scholarly journals Antiproliferative Activity and Cellular Uptake of Evodiamine and Rutaecarpine Based on 3D Tumor Models

Molecules ◽  
2016 ◽  
Vol 21 (7) ◽  
pp. 954 ◽  
Author(s):  
Hui Guo ◽  
Dongmei Liu ◽  
Bin Gao ◽  
Xiaohui Zhang ◽  
Minli You ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Antiproliferative Activity ◽  
Tumor Models

scholarly journals Evaluation of Floxuridine Oligonucleotide Conjugates Carrying Potential Enhancers of Cellular Uptake

2021 ◽  
Vol 22 (11) ◽  
pp. 5678
Author(s):  
Anna Aviñó ◽  
Anna Clua ◽  
Maria José Bleda ◽  
Ramon Eritja ◽  
Carme Fàbrega
Keyword(s):  
Folic Acid ◽  
Cellular Uptake ◽  
Antiproliferative Activity ◽  
Biological Effects ◽  
Metabolic Activation ◽  
Receptor Ligands ◽  
Short Oligonucleotide ◽  
Anti Cancer ◽  
Small Molecule Enhancers ◽  
Oligonucleotide Conjugates

Conjugation of small molecules such as lipids or receptor ligands to anti-cancer drugs has been used to improve their pharmacological properties. In this work, we studied the biological effects of several small-molecule enhancers into a short oligonucleotide made of five floxuridine units. Specifically, we studied adding cholesterol, palmitic acid, polyethyleneglycol (PEG 1000), folic acid and triantennary N-acetylgalactosamine (GalNAc) as potential enhancers of cellular uptake. As expected, all these molecules increased the internalization efficiency with different degrees depending on the cell line. The conjugates showed antiproliferative activity due to their metabolic activation by nuclease degradation generating floxuridine monophosphate. The cytotoxicity and apoptosis assays showed an increase in the anti-cancer activity of the conjugates related to the floxuridine oligomer, but this effect did not correlate with the internalization results. Palmitic and folic acid conjugates provide the highest antiproliferative activity without having the highest internalization results. On the contrary, cholesterol oligomers that were the best-internalized oligomers had poor antiproliferative activity, even worse than the unmodified floxuridine oligomer. Especially relevant is the effect induced by palmitic and folic acid derivatives generating the most active drugs. These results are of special interest for delivering other therapeutic oligonucleotides.

Water-soluble amphiphilic ruthenium(ii) polypyridyl complexes as potential light-activated therapeutic agents

2020 ◽  
Vol 56 (65) ◽  
pp. 9332-9335
Author(s):  
Sandra Estalayo-Adrián ◽  
Salvador Blasco ◽  
Sandra A. Bright ◽  
Gavin J. McManus ◽  
Guillermo Orellana ◽  
...  
Keyword(s):  
Cervical Cancer ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Therapeutic Agents ◽  
Water Soluble ◽  
Polypyridyl Complexes ◽  
Cervical Cancer Cells

Two new water-soluble amphiphilic Ru(ii) polypyridyl complexes were synthesised and their photophysical and photobiological properties evaluated; both complexes showed a rapid cellular uptake and phototoxicity against HeLa cervical cancer cells.

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