Cytotoxic and apoptosis-inducing effects of novel 8-amido isocoumarin derivatives against breast cancer cells

Isocoumarin is a lactone, a type of natural organic compound that is used as synthetic intermediates of several natural products and pharmaceutical compounds explored for their potential therapeutic applications like antifungal, antimicrobial, anti-inflammatory, and anticancer activities. In our pre...

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Vydáno v:Naunyn-Schmiedeberg's archives of pharmacology Ročník 394; číslo 7; s. 1437 - 1449
Hlavní autoři: Das, Vishal, Kaishap, Partha Pratim, Duarah, Gauri, Chikkaputtaiah, Channakeshavaiah, Deka Boruah, Hari Prasanna, Pal, Mintu
Médium: Journal Article
Jazyk:angličtina
Vydáno: Berlin/Heidelberg Springer Berlin Heidelberg 01.07.2021
Springer Nature B.V
Témata:
Annexin V
Antifungal agents
Antineoplastic Agents - toxicity
Apoptosis
Apoptosis - drug effects
Apoptosis - physiology
Biomedical and Life Sciences
Biomedicine
Breast cancer
Breast Neoplasms - pathology
Cell Survival - drug effects
Cell Survival - physiology
Cytotoxicity
Cytotoxins - toxicity
Dose-Response Relationship, Drug
Flow cytometry
Humans
Inflammation
Intermediates
Isocoumarins - toxicity
MCF-7 Cells
Natural products
Neurosciences
Organic compounds
Original Article
Pharmacology/Toxicology
Scanning electron microscopy
Therapeutic applications
Flow cytometry
DAPI-PI dual staining
Hematoxylin and eosin staining
8-Amido isocoumarin derivatives
MTT assay
Scanning electron microscope
ISSN:0028-1298, 1432-1912, 1432-1912
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Popis
Shrnutí:Isocoumarin is a lactone, a type of natural organic compound that is used as synthetic intermediates of several natural products and pharmaceutical compounds explored for their potential therapeutic applications like antifungal, antimicrobial, anti-inflammatory, and anticancer activities. In our previous work, we were the first group to report the use of amide C-N bond of isatins as the oxidizing directing group for the synthesis of 8-amido isocoumarin derivatives. Whereas in our present work, we have screened the cytotoxic effects of novel 8-amido isocoumarin derivatives (S1–S10) in human breast cancer MCF-7 and MDA-MB-231 cells. Our novel results revealed that N-(3-(4-methoxyphenyl)-1-oxo-4-(4-propylphenyl)-1H-isochromen-8yl)acetamide (S1) and N-(4-(3,5-difluorophenyl)-1-oxo-3-(p-tolyl)-1H-isochromen-8-yl) acetamide (S2) are the two potent compounds among the rest synthesized isocoumarin derivatives that are cytotoxic against MCF-7 and MDA-MB-231 cells, whereas less toxic to the non-tumorigenic IOSE-364 cells. Flow cytometry studies have confirmed the induction of apoptotic effects of compounds by Annexin V/PI double staining. We also observed the cytotoxic effects of S1 and S2, as evaluated by DAPI-PI immunostaining and H&E staining. The morphological alterations consistent with apoptotic blebs were observed in both cancer cells treated with compounds assessed by scanning electron microscopy. Overall, this present study strongly demonstrates that 8-amido isocoumarin derivatives have potent cytotoxic and apoptotic effects in breast cancer cells.
Bibliografie:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0028-1298
1432-1912
1432-1912
DOI:10.1007/s00210-021-02063-9