Fluorescent Gadolinium(III)‐Oligopeptide Complexes and Carbon Nanotube Composite as Dual Modality Anticancer Agents

Abstract

In search of non-platinum based anticancer drugs, we have synthesized and characterized a new class of three gadoliniumand a carbon nanotube composite, 1@CNT 4. The three oligopeptides, L 1 -L 3 were prepared in a novel synthetic route using tetramethyl benzotriazolyl uronium hexaflurophosphate (HBTU) as a peptide coupling reagent. Confocal microscopic analysis of the gadolinium(III)-oligopeptides, 1, 2 and CNT composite, 1@CNT 4 indicate that they display white and green light emissions upon excitations at λ, 405 and 488 nm with characteristic patterns. The oligopeptides, L 1 & L 3 display in vitro anticancer activity on HeLa cells with IC 50 values in one mM concentration whereas the IC 50 of RGD-based oligopeptide was found to be 1 μM. The IC 50 of gadolinium(III)-oligopeptide, 1 and the CNT composite, 4 were found to be 1 μM and 10 nM. The transmission electron microscopic investigation of the HeLa cells treated with the composite 4 confirm the cellular uptake and indicate the presence of CNTs in the cytoplasm and that CNTs appear like bullets carrying the gadolinium(III)-triaspartate, 1.

The Advances in Biomedical Applications of Carbon Nanotubes

“…In this context, CNTs offer an opportunity to shelter anti-cancer drugs thus lowering their toxicity for an organism and enhancing local accumulation in the desired site. Up to date, different types of anti-cancer compounds have been proposed and tested in regards their conjunction and functionality with the CNTs [66,67].…”

Carbon-Based Nanomaterials for Delivery of Biologicals and Therapeutics: A Cutting-Edge Technology

“…Chemotherapy leads to the death of cancer cells along with normal cells instigating serious side effects. Considering these hindrances, CNTs can protect the chemotherapeutics, and in turn, lower their toxicity toward normal tissues by localizing the drug at the target site [78,79]. Their interaction with lipid membranes and intracellular transport mechanism is inadequately understood, but few studies have suggested that CNTs enter cells via various endocytic processes [80,81].…”

Synthesis, characterization, and biological evaluation of new spebrutinib analogues: potential candidates with enhanced activity and reduced toxicity profiles

“…In all the previously discussed findings, the proposed therapeutic doses are much lower than the "onetenth" portion of the STD 10. Accordingly, the therapeutic doses can be reduced to be equal or below the micromolar concentrations recommended by many researches [54,56] 4.…”