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1.
Metabolites ; 12(12)2022 Dec 01.
Article in English | MEDLINE | ID: mdl-36557241

ABSTRACT

Previous studies have reported that different blood groups are associated with the risk of chronic degenerative diseases that mainly involve inflammation and neoplastic processes. We investigate the relationship between blood groups and the erythroprotective effect of extracts from Navicula incerta against oxidative damage as a proposal to develop drugs designed for people with a specific blood type related to chronic pathology. The study was carried out through the elucidation of the erythroprotective potential, anti-inflammatory and antiproliferative activity of Navicula incerta. Research suggests that the presence or absence of certain blood groups increases or decreases the abilities of certain phytochemicals to inhibit oxidative stress, which is related to the systemic inflammatory response involved in the development of different types of cancer. The pigment-rich extracts from Navicula incerta inhibit ROO•- induced oxidative stress in human erythrocytes on the A RhD+ve antigen without compromising the structure of the cell membrane. This result is very important, since the A antigen is related to the susceptibility of contracting prostate cancer. Similarly, it was possible to inhibit the proliferation of cervical (HeLa) and prostate (PC-3) carcinoma. The combinatorial analysis of different biological activities can help design phytochemicals as new candidates for preventive drugs treating the chronic degenerative diseases associated with a specific blood group.

2.
Chem Biol Interact ; 286: 34-44, 2018 Apr 25.
Article in English | MEDLINE | ID: mdl-29476729

ABSTRACT

In this work, we report on the synthesis of two new mono-alkylated tetrandrine derivatives with acridine and anthracene units, MAcT and MAnT. The compounds were fully characterized by physicochemical techniques and single-crystal X-ray diffraction analysis. In addition, both derivatives were studied as nucleotide receptors and double-stranded DNA binders in aqueous phosphate buffer at pH = 7.2 using UV-vis and fluorescence spectroscopy. According to the molecular recognition studies, MAcT and MAnT exhibit high affinity (K ∼ 105 M-1) and selectivity for ds-DNA, presumably in an intercalation mode. Finally, the anti-proliferative effects of the tetrandrine derivatives on different cancer cell lines were explored, revealing promising activities. Particularly, the mono-anthracene tetrandrine derivative MAnT showed an IC50 of 2.74 µg/mL on the HeLa cervical cancer cell line, representing a value 3.3 times smaller than that obtained for unsubstituted tetrandrine. Examination of the cytotoxic effects on the HeLa cell line by inverted microscopy suggests that the cell death mechanism consists basically in apoptosis. The molecular modelling of three ds-DNA-MAcT complexes, suggested that the macrocycles may use an intercalation binding mode towards DNA. MAcT is predicted to bind into the major groove of the ds-DNA providing non-covalent interactions such as electrostatic, van der Waals and hydrophobic interactions that lead to selectivity. Overall experimental data supports the mode of action of MAnT and MAcT as cytotoxic compounds against cancer cell lines via a DNA interaction mechanism.


Subject(s)
Acridines/chemistry , Anthracenes/chemistry , Benzylisoquinolines/chemistry , Macrocyclic Compounds/chemical synthesis , A549 Cells , Acridines/chemical synthesis , Acridines/pharmacology , Anthracenes/chemical synthesis , Anthracenes/pharmacology , Apoptosis/drug effects , Benzylisoquinolines/chemical synthesis , Benzylisoquinolines/pharmacology , Binding Sites , Cell Line, Tumor , Cell Proliferation/drug effects , DNA/chemistry , DNA/metabolism , HeLa Cells , Humans , Hydrophobic and Hydrophilic Interactions , Intercalating Agents/chemical synthesis , Intercalating Agents/chemistry , Intercalating Agents/pharmacology , Macrocyclic Compounds/chemistry , Macrocyclic Compounds/pharmacology , Molecular Docking Simulation , Nucleic Acid Conformation , Static Electricity
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