Abstract: Doxorubicin, also known as Adriamycin, is an
anthracycline class of drug used in cancer chemotherapy. It is used in
the treatment of non-Hodgkin’s lymphoma, multiple myeloma, acute
leukemia, breast cancer, lung cancer, endometrium cancer and ovary
cancers. It functions via intercalating DNA and ultimately killing
cancer cells. The major side effects of doxorubicin are hair loss,
myelosuppression, nausea & vomiting, oesophagitis, diarrhea, heart
damage and liver dysfunction. The minor modifications in the
structure of compound exhibit large variation in the biological
activity, has prompted us to carry out the synthesis of sulfonamide
derivatives. Sulfonamide is an important feature with broad spectrum
of biological activity such as antiviral, antifungal, diuretics, antiinflammatory,
antibacterial and anticancer activities. Structure of the
synthesized compound N-(1-methyl-2-oxo-2-N-methyl anilinoethyl)
benzene sulfonamide confirmed by proton nuclear magnetic
resonance (1H NMR),13C NMR, Mass and FTIR spectroscopic tools
to assure the position of all protons and hence stereochemistry of the
molecule. Further we have reported the binding potential of
synthesized sulfonamide analogues in comparison to doxorubicin
drug using Auto Dock 4.2 software. Computational binding energy
(B.E.) and inhibitory constant (Ki) has been evaluated for the
synthesized compound in comparison of doxorubicin against Poly
(dA-dT).Poly (dA-dT) and Poly (dG-dC).Poly (dG-dC) sequences.
The in vitro cytotoxic study against human breast cancer cell lines
confirms the better anticancer activity of the synthesized compound
over currently in use anticancer drug doxorubicin. The IC50 value of
the synthesized compound is 7.12 μM whereas for doxorubicin is 7.2
μM.
Abstract: This study determines the effect of naked and heparinbased
super-paramagnetic iron oxide nanoparticles on the human
cancer cell lines of A2780. Doxorubicin was used as the anticancer
drug, entrapped in the SPIO-NPs. This study aimed to decorate
nanoparticles with heparin, a molecular ligand for 'active' targeting
of cancerous cells and the application of modified-nanoparticles in
cancer treatment. The nanoparticles containing the anticancer drug
DOX were prepared by a solvent evaporation and emulsification
cross-linking method. The physicochemical properties of the
nanoparticles were characterized by various techniques, and uniform
nanoparticles with an average particle size of 110±15 nm with high
encapsulation efficiencies (EE) were obtained. Additionally, a
sustained release of DOX from the SPIO-NPs was successful.
Cytotoxicity tests showed that the SPIO-DOX-HP had higher cell
toxicity than the individual HP and confocal microscopy analysis
confirmed excellent cellular uptake efficiency. These results indicate
that HP based SPIO-NPs have potential uses as anticancer drug
carriers and also have an enhanced anticancer effect.