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Article ; Online: Method for highly selective, ultrasensitive fluorimetric detection of Cu

Sharma, Shivani / Chayawan / Debnath, Joy / Sundar Ghosh, Kalyan

2023 Volume 217, Page(s) 27–35

Abstract: Schiff base probes (1 and 2) made from o-phenylenediamine and o-aminophenol were appeared as highly selective fluorimetric chemosensor of ... ...

Abstract	Schiff base probes (1 and 2) made from o-phenylenediamine and o-aminophenol were appeared as highly selective fluorimetric chemosensor of Cu
MeSH term(s)	Copper/chemistry ; Schiff Bases/chemistry ; Metals ; Ions ; Spectrometry, Fluorescence/methods ; Fluorescent Dyes/chemistry
Chemical Substances	Copper (789U1901C5) ; 1,2-diaminobenzene (8B713N8Q0F) ; 2-aminophenol (23RH73DZ65) ; Schiff Bases ; Metals ; Ions ; Fluorescent Dyes
Language	English
Publishing date	2023-07-01
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1066584-5
ISSN	1095-9130 ; 1046-2023
ISSN (online)	1095-9130
ISSN	1046-2023
DOI	10.1016/j.ymeth.2023.06.013
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Article ; Online: A comparative study of diaryl urea molecules with and without sulfonamide group on Carbonic anhydrase IX and XII inhibition and its consequence on breast cancer cells.

Debnath, Joy / Keshamasetthy, Dhananjaya / Combs, Jacob / Leon, Katherine / Vullo, Daniela / Chatterjee, Abhijit / McKenna, Robert / Supuran, Claudiu T

Bioorganic chemistry

2024 Volume 145, Page(s) 107192

Abstract: To investigate the intrinsic relation between carbonic anhydrase inhibition and anticancer activity, we have prepared four sets of diaryl urea molecules and tested for the inhibition of hCA-IX and XII on two breast cancer cell lines. Among 21 compounds, ... ...

Abstract	To investigate the intrinsic relation between carbonic anhydrase inhibition and anticancer activity, we have prepared four sets of diaryl urea molecules and tested for the inhibition of hCA-IX and XII on two breast cancer cell lines. Among 21 compounds, compound J2 (with -SO
MeSH term(s)	Humans ; Female ; Carbonic Anhydrase IX ; Structure-Activity Relationship ; Urea/pharmacology ; Breast Neoplasms/drug therapy ; Antigens, Neoplasm/metabolism ; Sulfonamides/pharmacology ; Sulfonamides/chemistry ; Carbonic Anhydrase Inhibitors/chemistry ; Molecular Structure
Chemical Substances	Carbonic Anhydrase IX (EC 4.2.1.1) ; Urea (8W8T17847W) ; Antigens, Neoplasm ; Sulfonamides ; Carbonic Anhydrase Inhibitors
Language	English
Publishing date	2024-02-10
Publishing country	United States
Document type	Journal Article
ZDB-ID	120080-x
ISSN	1090-2120 ; 0045-2068
ISSN (online)	1090-2120
ISSN	0045-2068
DOI	10.1016/j.bioorg.2024.107192
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Article: Air quality assessment using weighted interval type-2 fuzzy inference system

Debnath, Joy / Biswas, Animesh / Majumder, Debasish

Ecological informatics. 2018 July, v. 46

2018

Abstract: This paper presents an integrated model based on interval type-2 fuzzy reasoning approach and interval type-2 fuzzy analytic hierarchy process for assessment of air quality in urban areas. In the proposed model, interval type-2 fuzzy reasoning approach ... ...

Abstract	This paper presents an integrated model based on interval type-2 fuzzy reasoning approach and interval type-2 fuzzy analytic hierarchy process for assessment of air quality in urban areas. In the proposed model, interval type-2 fuzzy reasoning approach is employed to determine impacts of different air pollutants to describe complex relationship between air pollutants and air quality index by considering individual weights of different air pollutants through the aggregation of toxicological impacts and concentration level of different air pollutants using interval type-2 fuzzy analytic hierarchy process. The proposed approach is advantageous over its counterparts to model the inter-personal and intra-personal uncertainties involved in classification of air quality index. Finally, the developed air quality assessment model is applied on the historical data set collected from ambient air quality monitoring stations operating near by the Victoria memorial, in Kolkata Metropolitan area. The study shows that the air quality index increased significantly during the festive season due to extensive fireworks in those areas.
Keywords	air pollutants ; air pollution ; air quality ; data collection ; metropolitan areas ; models ; monitoring ; uncertainty
Language	English
Dates of publication	2018-07
Size	p. 133-146.
Publishing place	Elsevier B.V.
Document type	Article
ZDB-ID	2212016-6
ISSN	1878-0512 ; 1574-9541
ISSN (online)	1878-0512
ISSN	1574-9541
DOI	10.1016/j.ecoinf.2018.06.002
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Inhibition of copper-induced aggregation of human γD-crystallin by a diimine molecule and investigations on their molecular interactions.

Rana, Shiwani / Velappan, Anand Babu / Debnath, Joy / Ghosh, Kalyan Sundar

Journal of biomolecular structure & dynamics

2019 Volume 38, Issue 16, Page(s) 4914–4920

Abstract: Communicated by Ramaswamy H. Sarma. ...

Abstract	Communicated by Ramaswamy H. Sarma.
MeSH term(s)	Copper ; Humans ; gamma-Crystallins
Chemical Substances	gamma-Crystallins ; Copper (789U1901C5)
Language	English
Publishing date	2019-11-12
Publishing country	England
Document type	Letter
ZDB-ID	49157-3
ISSN	1538-0254 ; 0739-1102
ISSN (online)	1538-0254
ISSN	0739-1102
DOI	10.1080/07391102.2019.1686426
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Article ; Online: Synergic effect of eugenol oleate with amphotericin B augments anti-leishmanial immune response in experimental visceral leishmaniasis in vitro and in vivo.

Kar, Amrita / Jayaraman, Adithyan / Charan Raja, Mamilla R / Srinivasan, Sujatha / Debnath, Joy / Mahapatra, Santanu Kar

International immunopharmacology

2020 Volume 91, Page(s) 107291

Abstract: Present treatment regimen on visceral leishmaniasis has multiple limitations including severe side effects, toxicity, and resistance of Leishmania strains. Amphotericin B is a well-established pharmacologically approved drug; however, mainly toxicity is ... ...

Abstract	Present treatment regimen on visceral leishmaniasis has multiple limitations including severe side effects, toxicity, and resistance of Leishmania strains. Amphotericin B is a well-established pharmacologically approved drug; however, mainly toxicity is a foremost issue with that drug. Recently, our group identified eugenol oleate as an anti-leishmanial immunomodulatory compound. The important objectives of this present study was to evaluate the possible synergistic effect of eugenol oleate with amphotericin B to reduce the toxicity of this approved drug. Results obtained from this study signified that combination of eugenol oleate and amphotericin B showed indifferent combinatorial effect against promastigotes with xΣFIC 1.015, while, moderate synergistic activity with xΣFIC 0.456 against amastigotes. It was also notable that eugenol oleate (2.5 μM) with low concentrations of amphotericin B (0.3125 μM) showed 96.45% parasite reduction within L. donovani-infected murine macrophages. Furthermore, eugenol oleate and amphotericin B significantly (p < 0.01) enhanced the nitrite generation, and pro-inflammatory cytokines (IL-12, IFN-γ and TNF-α) in infected macrophages in vitro and in BALB/c mice in vivo. Eugenol oleate (10 mg/Kg b. wt.) with amphotericin B (1 mg/Kg b.wt.) significantly (p < 0.01) controlled the parasite burden in liver by 96.2% and in spleen by 93.12%. Hence, this study strongly suggested the synergic potential of eugenol oleate with low concentration of amphotericin B in experimental visceral leishmaniasis through anti-leishmanial immune response.
MeSH term(s)	Amphotericin B/pharmacology ; Animals ; Cells, Cultured ; Cytokines/metabolism ; Disease Models, Animal ; Drug Synergism ; Drug Therapy, Combination ; Female ; Host-Parasite Interactions ; Inflammation Mediators/metabolism ; Leishmania donovani/drug effects ; Leishmania donovani/immunology ; Leishmania donovani/pathogenicity ; Leishmaniasis, Visceral/drug therapy ; Leishmaniasis, Visceral/immunology ; Leishmaniasis, Visceral/metabolism ; Leishmaniasis, Visceral/parasitology ; Liver/drug effects ; Liver/immunology ; Liver/metabolism ; Liver/parasitology ; Macrophages, Peritoneal/drug effects ; Macrophages, Peritoneal/immunology ; Macrophages, Peritoneal/metabolism ; Macrophages, Peritoneal/parasitology ; Mice, Inbred BALB C ; Nitrites/metabolism ; Parasite Load ; Spleen/drug effects ; Spleen/immunology ; Spleen/metabolism ; Spleen/parasitology ; Th1 Cells/drug effects ; Th1 Cells/immunology ; Th1 Cells/metabolism ; Th1 Cells/parasitology ; Th1-Th2 Balance ; Th2 Cells/drug effects ; Th2 Cells/immunology ; Th2 Cells/metabolism ; Th2 Cells/parasitology ; Trypanocidal Agents/pharmacology ; Mice
Chemical Substances	Cytokines ; Inflammation Mediators ; Nitrites ; Trypanocidal Agents ; Amphotericin B (7XU7A7DROE)
Language	English
Publishing date	2020-12-21
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	2043785-7
ISSN	1878-1705 ; 1567-5769
ISSN (online)	1878-1705
ISSN	1567-5769
DOI	10.1016/j.intimp.2020.107291
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Article ; Online: Oral combination of eugenol oleate and miltefosine induce immune response during experimental visceral leishmaniasis through nitric oxide generation with advanced cytokine demand.

Kar, Amrita / Charan Raja, Mamilla R / Jayaraman, Adithyan / Srinivasan, Sujatha / Debnath, Joy / Kar Mahapatra, Santanu

Cytokine

2021 Volume 146, Page(s) 155623

Abstract: Conventional therapy of visceral leishmaniasis (VL) remains challenging with the pitfall of toxicity, drug resistance, and expensive. Hence, urgent need for an alternative approach is essential. In this study, we evaluated the potential of combination ... ...

Abstract	Conventional therapy of visceral leishmaniasis (VL) remains challenging with the pitfall of toxicity, drug resistance, and expensive. Hence, urgent need for an alternative approach is essential. In this study, we evaluated the potential of combination therapy with eugenol oleate and miltefosine in Leishmania donovani infected macrophages and in the BALB/c mouse model. The interactions between eugenol oleate and miltefosine were found to be additive against promastigotes and amastigotes with xΣFIC 1.13 and 0.68, respectively. Significantly (p < 0.001) decreased arginase activity, increased nitrite generation, improved pro-inflammatory cytokines, and phosphorylated p38MAPK were observed after combination therapy with eugenol oleate and miltefosine. >80% parasite clearance in splenic and hepatic tissue with concomitant nitrite generation, and anti-VL cytokines productions were observed after orally administered miltefosine (5 mg/kg body weight) and eugenol oleate (15 mg/kg body weight) in L. donovani-infected BALB/c mice. Altogether, this study suggested the possibility of an oral combination of miltefosine with eugenol oleate against visceral leishmaniasis.
MeSH term(s)	Administration, Oral ; Animals ; Cell Death/drug effects ; Cell Proliferation/drug effects ; Cytokines/biosynthesis ; Cytokines/metabolism ; Drug Interactions ; Drug Therapy, Combination ; Eugenol/administration & dosage ; Eugenol/pharmacology ; Eugenol/therapeutic use ; Female ; Immunity/drug effects ; Inhibitory Concentration 50 ; Leishmania donovani/drug effects ; Leishmania donovani/growth & development ; Leishmania donovani/immunology ; Leishmania donovani/ultrastructure ; Leishmaniasis, Visceral/drug therapy ; Leishmaniasis, Visceral/immunology ; Leishmaniasis, Visceral/parasitology ; Life Cycle Stages/drug effects ; Macrophages/drug effects ; Macrophages/immunology ; Macrophages/parasitology ; Macrophages/ultrastructure ; Male ; Mice, Inbred BALB C ; Nitric Oxide/biosynthesis ; Nitric Oxide Synthase Type II/metabolism ; Parasites/drug effects ; Parasites/growth & development ; Parasites/immunology ; Parasites/ultrastructure ; Phosphorylation/drug effects ; Phosphorylcholine/administration & dosage ; Phosphorylcholine/analogs & derivatives ; Phosphorylcholine/pharmacology ; Phosphorylcholine/therapeutic use ; T-Lymphocytes/drug effects ; T-Lymphocytes/immunology ; p38 Mitogen-Activated Protein Kinases/metabolism ; Mice
Chemical Substances	Cytokines ; Phosphorylcholine (107-73-3) ; Nitric Oxide (31C4KY9ESH) ; Eugenol (3T8H1794QW) ; miltefosine (53EY29W7EC) ; Nitric Oxide Synthase Type II (EC 1.14.13.39) ; p38 Mitogen-Activated Protein Kinases (EC 2.7.11.24)
Language	English
Publishing date	2021-06-16
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1018055-2
ISSN	1096-0023 ; 1043-4666
ISSN (online)	1096-0023
ISSN	1043-4666
DOI	10.1016/j.cyto.2021.155623
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Article ; Online: 1,3-Oxazine-2-one derived dual-targeted molecules against replicating and non-replicating forms of Mycobacterium tuberculosis.

Velappan, Anand Babu / Kesamsetty, Dhanunjaya / Datta, Dhrubajyoti / Ma, Rui / Hari, Natarajan / Franzblau, Scott G / Debnath, Joy

European journal of medicinal chemistry

2020 Volume 208, Page(s) 112835

Abstract: The high mortality rate and increasing prevalence of resistant Mtb are the major concerns for the Tuberculosis (TB) treatment in this century. To curtail the prevalence of resistant Mtb, we have prepared 1,3-oxazine-2-one based dual targeted molecules. ... ...

Abstract	The high mortality rate and increasing prevalence of resistant Mtb are the major concerns for the Tuberculosis (TB) treatment in this century. To curtail the prevalence of resistant Mtb, we have prepared 1,3-oxazine-2-one based dual targeted molecules. Compound 67 and 68 were found to be equally active against replicating and non-replicatiing form of Mtb (MIC
MeSH term(s)	Antitubercular Agents/chemical synthesis ; Antitubercular Agents/pharmacology ; Antitubercular Agents/toxicity ; Bacterial Proteins/antagonists & inhibitors ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/toxicity ; Leukocytes, Mononuclear/drug effects ; Methyltransferases/antagonists & inhibitors ; Microbial Sensitivity Tests ; Molecular Structure ; Mycobacterium smegmatis/drug effects ; Mycobacterium tuberculosis/drug effects ; Mycolic Acids/metabolism ; Oxazines/chemical synthesis ; Oxazines/pharmacology ; Oxazines/toxicity ; Structure-Activity Relationship
Chemical Substances	Antitubercular Agents ; Bacterial Proteins ; Enzyme Inhibitors ; Mycolic Acids ; Oxazines ; Methyltransferases (EC 2.1.1.-)
Language	English
Publishing date	2020-09-13
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2020.112835
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Article ; Online: Oral administration of eugenol oleate cures experimental visceral leishmaniasis through cytokines abundance.

Charan Raja, Mamilla R / Kar, Amrita / Srinivasan, Sujatha / Chellappan, Davidraj / Debnath, Joy / Kar Mahapatra, Santanu

Cytokine

2020 Volume 145, Page(s) 155301

Abstract: Visceral leishmaniasis (VL) is an endemic fatal infectious disease in tropical and subtropical nations. The limited treatment options, long treatment regimens, invasive mode of administration of drugs, and lack of effective vaccination are the main ... ...

Abstract	Visceral leishmaniasis (VL) is an endemic fatal infectious disease in tropical and subtropical nations. The limited treatment options, long treatment regimens, invasive mode of administration of drugs, and lack of effective vaccination are the main reasons for the search of new alternative therapeutics against VL. On this quest, from a series of eugenol derivatives, we had demonstrated eugenol oleate as a lead immunomodulatory anti-VL molecule earlier. In this report, the oral efficacy and mechanism of eugenol oleate in inducing immunomodulatory anti-VL activity has been studied in BALB/c mice model. The plasma pharmacokinetic and acute toxicity studies suggested that the eugenol oleate is safe with an appreciable pharmacokinetic profile. Eugenol oleate (30 mg/kg B.W.) showed 86.5% of hepatic and 84.1% of splenic parasite clearance. The increased Th1 cytokine profile and decreased Th2 cytokine profile observed from ELISA and qRTPCR suggested that the eugenol oleate induced the parasite clearance through the activation of the host immune system. Subsequently, the mechanistic insights behind the anti-leishmanial activity of eugenol oleate were studied in peritoneal macrophages in vitro by inhibitor response study and immunoblotting. The results inferred that eugenol oleate activated the PKC-βII-p38 MAPK and produced IL-12 and IFN-γ which intern activated the iNOS2 to produce NO free radicals that cleared the intracellular parasite.
MeSH term(s)	Administration, Oral ; Animals ; Cytokines ; Disease Models, Animal ; Eugenol/pharmacology ; Female ; Immune System/drug effects ; Immunomodulation/drug effects ; Leishmania donovani/drug effects ; Leishmaniasis, Visceral/drug therapy ; Macrophages, Peritoneal/parasitology ; Male ; Mice ; Mice, Inbred BALB C ; Oleic Acid/pharmacology ; Spleen/parasitology
Chemical Substances	Cytokines ; Oleic Acid (2UMI9U37CP) ; Eugenol (3T8H1794QW)
Language	English
Publishing date	2020-10-28
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1018055-2
ISSN	1096-0023 ; 1043-4666
ISSN (online)	1096-0023
ISSN	1043-4666
DOI	10.1016/j.cyto.2020.155301
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Article ; Online: 2-Aryl benzazole derived new class of anti-tubercular compounds: Endowed to eradicate mycobacterium tuberculosis in replicating and non-replicating forms.

Velappan, Anand Babu / Datta, Dhrubajyoti / Ma, Rui / Rana, Shiwani / Ghosh, Kalyan Sundar / Hari, Natarajan / Franzblau, Scott G / Debnath, Joy

Bioorganic chemistry

2020 Volume 103, Page(s) 104170

Abstract: The high mortality rate and the increasing prevalence of Mtb resistance are the major concerns for the Tuberculosis (TB) treatment in this century. To counteract the prevalence of Mtb resistance, we have synthesized 2-aryl benzazole based dual targeted ... ...

Abstract	The high mortality rate and the increasing prevalence of Mtb resistance are the major concerns for the Tuberculosis (TB) treatment in this century. To counteract the prevalence of Mtb resistance, we have synthesized 2-aryl benzazole based dual targeted molecules. Compound 9m and 9n were found to be equally active against replicating and non-replicating form of Mtb (MIC
MeSH term(s)	Antitubercular Agents/pharmacology ; Antitubercular Agents/therapeutic use ; Humans ; Mycobacterium tuberculosis/drug effects
Chemical Substances	Antitubercular Agents
Language	English
Publishing date	2020-08-27
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	120080-x
ISSN	1090-2120 ; 0045-2068
ISSN (online)	1090-2120
ISSN	0045-2068
DOI	10.1016/j.bioorg.2020.104170
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Article ; Online: Amino and carboxy functionalized modified nucleosides: a potential class of inhibitors for angiogenin.

Debnath, Joy / Dasgupta, Swagata / Pathak, Tanmaya

Bioorganic chemistry

2014 Volume 52, Page(s) 56–61

Abstract: The 3'-amino and carboxy functionalize thymidines execute their ribonucleolytic inhibition activity for angiogenin. These modified nucleosidic molecules inhibit the ribonucleolytic activity of angiogenin in a competitive manner like the other ... ...

Abstract	The 3'-amino and carboxy functionalize thymidines execute their ribonucleolytic inhibition activity for angiogenin. These modified nucleosidic molecules inhibit the ribonucleolytic activity of angiogenin in a competitive manner like the other conventional nucleotidic inhibitors, which have been confirmed from kinetic experiments. The improved inhibition constant (Ki) values 427 ± 7, 775 ± 6 μM clearly indicate modified nucleosides are an obvious option for the designing of inhibitors of angiogenesis process. The chorioallantoic membrane (CAM) assay qualitatively suggests that amino functionalized nucleosides have an effective potency to inhibited angiogenin-induced angiogenesis. Docking studies further demonstrate the interaction of their polar amino group with the P1 site residues of angiogenin, i.e., His-13 and His-114 residues.
MeSH term(s)	Animals ; Chick Embryo ; Chorioallantoic Membrane/blood supply ; Chorioallantoic Membrane/drug effects ; Drug Evaluation, Preclinical/methods ; Humans ; Kinetics ; Molecular Docking Simulation ; Molecular Structure ; Nucleosides/chemistry ; Nucleosides/pharmacology ; Ribonuclease, Pancreatic/antagonists & inhibitors ; Ribonuclease, Pancreatic/pharmacology ; Structure-Activity Relationship
Chemical Substances	Nucleosides ; angiogenin (EC 3.1.27.-) ; Ribonuclease, Pancreatic (EC 3.1.27.5)
Language	English
Publishing date	2014-02
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	120080-x
ISSN	1090-2120 ; 0045-2068
ISSN (online)	1090-2120
ISSN	0045-2068
DOI	10.1016/j.bioorg.2013.11.005
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