Comparative Analysis of the Antineoplastic Activity of C60 Fullerene with 5-Fluorouracil and Pyrrole Derivative In Vivo

O V Lynchak,U Ritter,V V Kostjukov,P Scharff,D Soloviov,Yu I Prylutskyy,V K Rybalchenko,O A Kyzyma,M P Evstigneev

doi:10.1186/s11671-016-1775-0

Abstract

The antitumor activity of pristine C60 fullerene aqueous solution (C60FAS) compared to 5-fluorouracil (5-FU) and pyrrole derivative 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2.5-dione (MI-1) cytostatic drugs was investigated and analyzed in detail using the model of colorectal cancer induced by 1.2-dimethylhydrazine (DMH) in rats. The number, size, and location of the tumors were measured, and the pathology was examined. It was found that the number of tumors and total lesion area decreased significantly under the action of C60FAS and MI-1. Because these drugs have different mechanisms of action, their simultaneous administration can potentially increase the effectiveness and significantly reduce the side effects of antitumor therapy.

Highlights

Introduction ofC60 fullerene aqueous solution (C60FAS) caused the reduction of the number of tumors in the cecum by 57% and the total lesion area by 65% (Table 1)
Since the C60 fullerene particles size directly correlates with their biodistribution and toxicity [3, 15, 16], Small-angle X-ray scattering (SAXS) study of C60FAS was performed
For spherical homogeneous approximation in the case of C60FAS [6, 40, 42, 43], the C60 fullerene nanoparticle size can be estimated as 2 × (5/3)1/2 × Rg, which gives the effective diameter about 52 nm

Summary

Introduction

Introduction ofC60FAS caused the reduction of the number of tumors in the cecum by 57% and the total lesion area by 65% (Table 1). The number of tumors had demonstrated a tendency to reduction and the total lesions area had decreased by 33% under the C60FAS action (Table 1). C60 fullerenes are soluble in nonpolar organic solvents [5] and can be transferred into the water by means of special procedures [6,7,8]. These properties enable fullerene to utilize in biological objects due to their ability to penetrate the cell lipid membrane [9,10,11,12]. It was reported that C60 fullerene can be used in antitumor therapy [18, 19], including the photodynamic therapy for the treatment of oncological diseases [20,21,22,23] as well as the targeted delivery of traditional drugs into cancer cells [24, 25]

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