Several chronic diseases like cancer, diabetes, stroke, neurodegenerative disorders, etc. are rising globally at a faster rate basically due to the increasing free radicals overproduction and oxidative stress from current lifestyle, but can be suppressed or inhibited by antioxidant compounds (Chaturvedi & Beal, 2013;Halliwell, 2012). Now-a-days, the natural antioxidants have a higher demand than the synthetic ones (Kashyap et al., 2017). Among them, flavonoids have a higher value due to their role in human health. They are plantderived compounds having exotic colors which are secondarily produced from phenylalanine (Havsteen, 2002). They are the largest family of naturally occurring polyphenols which include the flavones, flavonols, flavanones, flavanols, isoflavonoids, and anthocyanidins
Recent analyses have highlighted the promotion of cancer migration and invasion, mediated through HDAC via MMP-2 and MMP-9. Since both class 1 HDACs and MMP-2/9 are involved in the migration and invasion of cancer, an attempt has been taken to design dual MMP-2/HDAC-8 inhibitors by pharmacophore mapping and molecular docking approaches. The designed molecules were synthesized and showed a range of inhibitory activity against different MMP subtypes. Most of these designed compounds were selective towards MMP-2 but less potent against anti-targets like MMP-8, -12, etc. The highly active MMP-2 inhibitors were also found to be active towards HDAC-8 but less potent against other class 1 HDACs (HDAC-1 and -2). Molecular dynamics simulations revealed that the designed compounds may be acting through a distinct mechanism of action in the 'acetate ion channel' of HDAC-8. Some potent dual MMP-2/HDAC-8 inhibitors were further explored for in vitro cellular assays against human lung carcinoma cell line A549. These analyses revealed that some of these dual inhibitors have considerable anti-migratory and anti-invasive properties. The work may help to obtain some useful dual inhibitors.
Molecular interaction of aromatic dyes with biological macromolecules are important for the development of minimally invasive disease diagnostic biotechnologies. In the present work, we have used Toluidine Blue (TB) as a model dye, which is a well-known staining agent for the diagnosis of oral cancer and have studied the interaction of various biological macromolecules (protein and DNA) with the dye at different pH. Our spectroscopic studies confirm that TB interacts with Human Serum Albumin (HSA), a model protein at very high pH conditions which is very hard to achieve physiologically. On the other hand, TB significantly interacts with the DNA at physiological pH value (7.4). Our molecular studies strengthen the understanding of the Toluidine Blue staining of cancer cells, where the relative ratio of the nucleic acids is higher than the normal intracellular content. We have also developed a non-invasive, non-contact spectroscopic technique to explore the possibility of quantitatively detecting oral cancer by exploiting the interaction of TB with DNA. We have also reported development of a prototype named "Oral-O-Scope" for the detection of Oral cancer and have carried out human studies using the prototype.
Consumption of excess fluorides through drinking water and its adverse effects on human health is of global concern. Given that people from at least 25 countries are suffering from fluorosis, global management of this issue is of immense importance. Here, we developed a sensor called FeFlu, based on an anionic micelle (SDS)−hematoporphyrin (Hp) complex, sensitized by Fe(III) chloride for the detection of fluoride in water. The micelle−hematoporphyrin (SDS−Hp) complex is almost nonfluorescent, but the prototype (FeFlu device) based on it displays a strong turn-on fluorescence upon recognition of F − in water. In addition, the detection of fluorides using FeFlu is found to suffer insignificant interference from environmentally relevant anions and cations. In the present study, we also fabricated a fluorescence-based prototype FeFlu device based on photophysical investigation of several sensitized micelle−Hp complexes and validated the results with a fluoride-ion-selective electrode, which is widely utilized for the detection of fluorides in drinking water in an easy and affordable manner.
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