Dichloroacetyl chloride conjugated peptide-based probes: design, synthesis, and in vitro evaluation in breast cancer cells

This research discusses the design and synthesis of therapeutic peptides conjugated to dichloroacetyl chloride (DAC) followed by their characterization and cytotoxic evaluation. The conjugates demonstrated cytotoxic effect following in vitro evaluation using MTT and the brine shrimp lethality assay....

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Bibliographic Details
Published inInternational journal of polymeric materials Vol. 70; no. 12; pp. 841 - 848
Main Authors Joshi, Rajendra, Acharya, Baku, Bhandari, Kritisha, Bhandari, Suzeeta, Duwal, Rajina, Ghimire, Ranju, Shakya, Rajani, Sweidan, Kamal A., Shrestha, Bhupal G.
Format Journal Article
LanguageEnglish
Published Philadelphia Taylor & Francis 13.08.2021
Taylor & Francis Ltd
Subjects
Apoptosis
Brine shrimp lethality assay
Cell death
Chlorides
Conjugates
Cytotoxicity
dichloroacetyl chloride
Lethality
MTT assay
octaarginine
Peptides
RGD peptide
solid-phase synthesis
Synthesis
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Summary:This research discusses the design and synthesis of therapeutic peptides conjugated to dichloroacetyl chloride (DAC) followed by their characterization and cytotoxic evaluation. The conjugates demonstrated cytotoxic effect following in vitro evaluation using MTT and the brine shrimp lethality assay. Significant cell death for octaarginine-DAC conjugate and 100% cell death was observed for the RGD-DAC conjugate. The LC 50 values of R8-DAC conjugate and RGD-DAC were 6.5 µg/mL and 10.01 µg/mL respectively. Our study successfully showed that the derivatization of peptides with dichloroacetyl chloride could hold promises in the development of target specific drug delivery devices in therapeutic planning of a wide range of tumors.
ISSN:0091-4037
1563-535X
DOI:10.1080/00914037.2020.1765358