Search

Your search keyword '"Vangala Venugopal"' showing total 10 results
Start Over Author "Vangala Venugopal"
10 results on '"Vangala Venugopal"'

2. Identification of Novel Isatin Derivative Bearing a Nitrofuran Moiety as Potent Multi-Isoform Aldehyde Dehydrogenase Inhibitor.

Author

Gowda, Krishne, Raza, Asif, Vangala, Venugopal, Lone, Nazir Ahmad, Jyh Ming Lin, Singh, Jaikee Kumar, Srivastava, Sandeep Kumar, Schell, Todd D., Robertson, Gavin P., Amin, Shantu, and Sharma, Arun K.

Abstract

Aldehyde dehydrogenases (ALDHs) are a family of enzymes that aid in detoxification and are overexpressed in several different malignancies. There is a correlation between increased expression of ALDH and a poor prognosis, stemness, and resistance to several drugs. Several ALDH inhibitors have been generated due to the crucial role that ALDH plays in cancer stem cells. All of these inhibitors, however, are either ineffective, very toxic, or have yet to be subjected to rigorous testing on their effectiveness. Although various drug-like compounds targeting ALDH have been reported in the literature, none have made it to routine use in the oncology clinic. As a result, new potent, non-toxic, bioavailable, and therapeutically effective ALDH inhibitors are still needed. In this study, we designed and synthesized potent multi-ALDH isoform inhibitors based on the isatin and indazole pharmacophore. Molecular docking studies and enzymatic tests revealed that among all of the synthesized analogs, compound 3 is the most potent inhibitor of ALDH1A1, ALDH3A1, and ALDH1A3, exhibiting 51.32%, 51.87%, and 36.65% inhibition, respectively. The ALDEFLUOR assay further revealed that compound 3 acts as an ALDH broad spectrum inhibitor at 500 nM. Compound 3 was also the most cytotoxic to cancer cells, with an IC50 in the range of 2.1 to 3.8 µM for ovarian, colon, and pancreatic cancer cells, compared to normal and embryonic kidney cells (IC50 7.1 to 8.7 µM). Mechanistically, compound 3 increased ROS activity due to potent multi-ALDH isoform inhibition, which increased apoptosis. Taken together, this study identified a potent multi-isoform ALDH inhibitor that could be further developed as a cancer therapeutic. [ABSTRACT FROM AUTHOR]

Published
2024
Full Text
View/download PDF

3. One- and Two-Photon Uncaging of Carbon Monoxide (CO) with Real-Time Monitoring: On-Demand Carbazole-Based Dual CO-Releasing Platform to Test over Single and Combinatorial Approaches for the Efficient Regression of Orthotopic Murine Melanoma In Vivo

Author

Venkatesh, Yarra, primary, Vangala, Venugopal, additional, Mengji, Rakesh, additional, Chaudhuri, Amrita, additional, Bhattacharya, Sayantan, additional, Datta, Prasanta Kumar, additional, Banerjee, Rajkumar, additional, Jana, Avijit, additional, and Singh, N. D. Pradeep, additional

Published
2022
Full Text
View/download PDF

4. ‘AIE + ESIPT’ assisted photorelease: fluorescent organic nanoparticles for dual anticancer drug delivery with real-time monitoring ability

Author

Sandipan Biswas, N. D. Pradeep Singh, Rakesh Mengji, Vangala Venugopal, Avijit Jana, and Shrabani Barman

Subjects
Time Factors, Cell Survival, Nanoparticle, Excited state intramolecular proton transfer, Antineoplastic Agents, 02 engineering and technology, 010402 general chemistry, Photochemistry, 01 natural sciences, Catalysis, Drug Delivery Systems, Materials Chemistry, Humans, Aggregation-induced emission, Fluorescent Dyes, Phenylacetates, Molecular Structure, Chemistry, Metals and Alloys, General Chemistry, Photochemical Processes, 021001 nanoscience & nanotechnology, Anticancer drug, Fluorescence, 0104 chemical sciences, Surfaces, Coatings and Films, Electronic, Optical and Magnetic Materials, Ceramics and Composites, Nanoparticles, Protons, 0210 nano-technology, HeLa Cells
Abstract

‘Aggregation Induced Emission + Excited State Intramolecular Proton Transfer (AIE + ESIPT)’-assisted photorelease of an anticancer drug by a p-hydroxyphenacyl (pHP) phototrigger with real-time monitoring has been demonstrated.

Published
2018

6. Intramolecular macrolactonization, photophysical and biological studies of new class of polycyclic pyrrole derivatives

Author

Arabinda Mandal, Avijit Jana, Suresh Kumar Mondal, Vangala Venugopal, Susanta Kumar Manna, Maidul Hossain, Sk Asraf Ali, and Shubhankar Samanta

Subjects
Reaction conditions, Biological studies, 010405 organic chemistry, Stereochemistry, Chemistry, Organic Chemistry, Intramolecular cyclization, 010402 general chemistry, 01 natural sciences, Biochemistry, Fluorescence, Combinatorial chemistry, Pyrrole derivatives, Coupling reaction, 0104 chemical sciences, Intramolecular force, Physical and Theoretical Chemistry
Abstract

Herein, we report an efficient synthesis of N-substituted pyrrole derivatives and their application to construct macrocyclic oxazocinone via a two-component coupling reaction followed by base mediated intramolecular cyclization. This methodology provides an easy two-step approach to constitute a library of fused pyrrolo-oxazocinone derivatives in good yields under mild reaction conditions. The present methodology offers an easy access to the synthesis of a library of fluorescent pyrole derivatives. Among them, tert-butyl 2-(2-(3-hydroxypropyl)-7-methoxy-4,5-dihydro-2H-benzo[e]isoindol-1-yl)acetate has been employed in bio-analytical imaging which shows efficient cellular internalization along with no obvious cellular toxicity.

Published
2017

10. Large Amino Acid Transporter 1 Selective Liposomes of l-DOPA Functionalized Amphiphile for Combating Glioblastoma

Author

Bhunia, Sukanya, Vangala, Venugopal, Bhattacharya, Dwaipayan, Ravuri, Halley Gora, Kuncha, Madhusudana, Chakravarty, Sumana, Sistla, Ramakrishna, and Chaudhuri, Arabinda

Abstract

Despite significant progress in neurosurgery and radiation therapy during the past decade, overall survivability (OS) of glioblastoma patients continues to be less than 2 years. The scope of systemic chemotherapy is greatly limited by poor drug transport across the blood brain barrier (BBB) and, thereby, suboptimal drug accumulation in glioma tissue. To this end, use of large amino acid transporter-1 (LAT1) overexpressed both on brain capillary endothelial cells (BCECs) and glioma cells has begun. Prior reports on the use of LAT1 mediated delivery of model drugs showed their brain accumulations. However, in depth in vivoglioblastoma regression studies aimed at examining the therapeutic potential of LAT1 mediated delivery of potent chemotherapeutics to brain tumor tissues have not yet been undertaken. Herein, we report on the development of a nanometric (100–135 nm) promising LAT1 selective liposomal drug carrier prepared from a novel l-3,4-dihydroxyphenylalanine (l-DOPA) functionalized amphiphile (Amphi-DOPA). In vitrostudies using Rh-PE labeled liposomes of Amphi-DOPA both in untreated glioma (GL261) cells and in GL261cells preincubated with LAT1 antibody revealed LAT1 mediated cellular uptake. Intravenously administered NIR-dye labeled liposomes of Amphi-DOPA in glioblastoma-bearing mice showed preferential accumulation of the dye in brain tissue. Notably iv administration of WP1066-loaded liposomes of Amphi-DOPA enhanced the overall survivability of C57BL/6J mice bearing orthotopically established mouse glioblastoma by ∼60% compared to that for the untreated mouse group. Furthermore, we show that the OS of established glioblastoma-bearing mice can be significantly enhanced (by >300% compared to that for the untreated mouse group) when the presently described LAT1 mediated targeted chemotherapy with WP1066-loaded liposomes of Amphi-DOPA is combined with in vivoDC-targeted DNA vaccination using a survivin (a glioblastoma antigen) encoded DNA vaccine. The present findings open a new door for LAT1 mediated systemic chemotherapy of glioblastoma.

Published
2024
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results