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: Two new metal-based anticancer chemotherapeutic
agents, [(Ph2Sn)2(HGuO)2(phen)Cl2] 1 and [(Ph3Sn)(HGuO)(phen)]-
Cl.CH3OH.H2O 2, were designed, prepared and characterized by
analytical and spectral (IR, ESI-Mass, 1H, 13C and 119Sn NMR)
techniques. The proposed geometry of Sn(IV) in 1 and 2 is distorted
octahedral and distorted trigonal-bipyramidal, respectively. Both 1
and 2 exhibit potential cytotoxicity in vitro against MCF-7, HepG-2
and DU-145 cell lines. The intrinsic binding constant (Kb) values of 1
(2.33 × 105 M-1) and 2 (2.46 × 105 M-1) evaluated from UV-Visible
absorption studies suggest non-classical electrostatic mode of
interaction via phosphate backbone of DNA double helix. The Stern-
Volmer quenching constant (Ksv) of 1 (9.74 × 105 M-1) and 2 (2.9 ×
106 M-1) determined by fluorescence studies suggests the groove
binding and intercalation mode for 1 and 2, respectively. Effective
cleavage of pBR322 DNA is induced by 1.Their interaction with
DNA of cancer cells may account for potency.
Abstract: Breast cancer is the most common malignancy in the
world among women. Many therapies have been designed to treat
this disease. Mamectomy, chemotherapy and radiotherapy are still
the main therapies of breast cancer. However, the results were
unsatisfactory and still far from the ideal treatment.
PM 701is a natural product, has anticancer activity. The bioactive
fraction PMF and subfraction PMFK had been isolated from PM701.
PM 701 and its fractions were proved to have a cytotoxic properties
against different cancer cell lines. This article is directed for the
further examination of lyophilized PM701 and its active fractions on
the growth of breast cancer cells (MCF-7). PM 701, PMF or PMFK
were adding to the cultural medium, where MCF-7 is incubated.
PM 701, PMF or PMFK were able to inhibit significantly the
proliferation of MCF-7 cells, Moreover these new agents were
proved to induce apoptosis of the breast cancer cells; through its
direct effect on the nuclei.
Abstract: Cancer becomes one of the leading cause of death in
many countries over the world. Fourier-transform infrared (FTIR)
spectra of human lung cancer cells (A549) treated with PMF (natural
product extracted from PM 701) for different time intervals were
examined. Second derivative and difference method were taken in
comparison studies. Cesium (Cs) and Rubidium (Rb) nanoparticles in
PMF were detected by Energy Dispersive X-ray attached to Scanning
Electron Microscope SEM-EDX. Characteristic changes in protein
secondary structure, lipid profile and changes in the intensities of
DNA bands were identified in treated A549 cells spectra. A
characteristic internucleosomal ladder of DNA fragmentation was
also observed after 30 min of treatment. Moreover, the pH values
were significantly increases upon treatment due to the presence of Cs
and Rb nanoparticles in the PMF fraction. These results support the
previous findings that PMF is selective anticancer agent and can
produce apoptosis to A549 cells.