http://dkr.cdri.res.in:8080/xmlui/handle/123456789/514 2026-04-19T13:41:17Z 2026-04-19T13:41:17Z Ali, Abdul A. Gogoi, Dhrubajyoti Buragohain, Alak K. Saikia, Prakash J. Gehlot, Praveen S Kumar, Arvind Trivedi, Priyanka Chaturvedi, Vinita Sarma, Diganta http://dkr.cdri.res.in:8080/xmlui/handle/1/1718 2021-06-03T06:52:02Z 2016-01-01T00:00:00Z

Synthesis and Biological Evaluation of Novel 1,2,3-Triazole derivatives as Anti-TB Agents Ali, Abdul A.; Gogoi, Dhrubajyoti; Buragohain, Alak K.; Saikia, Prakash J.; Gehlot, Praveen S; Kumar, Arvind; Trivedi, Priyanka; Chaturvedi, Vinita; Sarma, Diganta A series of seventeen novel 1,2,3-Triazole derivatives were efficiently synthesized in excellent yields by the popular ‘click chemistry’ approach and evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Ra. Molecular docking of the target compounds into the active site of DprE1 (Decaprenylphosphoryl-β-D-ribose-2′-epimerase) enzyme revealed significant structural information on the plausible binding interactions

2016-01-01T00:00:00Z Maurya, C K Singh, Rohit Jaiswal, Natasha Venkateswarlu, K Narender, Tadigoppula Tamrakar, A K http://dkr.cdri.res.in:8080/xmlui/handle/1/1712 2018-05-02T06:51:49Z 2014-01-01T00:00:00Z

4‐Hydroxyisoleucine ameliorates fatty acid‐induced insulin resistance and inflammatory response in skeletal muscle cells Maurya, C K; Singh, Rohit; Jaiswal, Natasha; Venkateswarlu, K; Narender, Tadigoppula; Tamrakar, A K The 4‐Hydroxyisoleucine (4‐HIL), an unusual amino acid isolated from the seeds of Trigonella foenum‐graecum was investigated for the metabolic effects to ameliorate free fatty acid‐induced insulin resistance in skeletal muscle cells. An incubation of L6 myotubes with palmitate inhibited insulin stimulated‐ glucose uptake and ‐translocation of glucose transporter 4 (GLUT4) to cell surface. Addition of 4‐HIL strongly prevented this inhibition. We then examined insulin signaling pathway, where 4‐HIL effectively inhibited the ability of palmitate to reduce insulin‐stimulated phosphorylation of insulin receptor substrate‐1(IRS‐1), protein kinase B (PKB/AKT), AKT substrate of 160 KD (AS160) and glycogen synthase kinase 3β (GSK‐3 β) in L6 myotubes. Moreover, 4‐HIL presented strong inhibition on palmitate‐induced production of reactive oxygen species (ROS) and associated inflammation, as the activation of NF‐κB and, JNK1/2, ERK1/2 and p38 MAPK was greatly reduced. 4‐HIL also inhibited inflammation‐stimulated IRS‐1 serine phosphorylation and restored insulin‐stimulated IRS‐1 tyrosine phosphorylation in presence of palmitate, leading to enhanced insulin sensitivity. These findings suggested that 4‐HIL could inhibit palmitate‐induced, ROS‐associated inflammation and restored insulin sensitivity through regulating IRS‐1 function. 

2014-01-01T00:00:00Z Tamrakar, Akhilesh K Maurya, Chandan K. Rai, Amit K http://dkr.cdri.res.in:8080/xmlui/handle/123456789/1698 2017-06-13T07:04:43Z 2014-01-01T00:00:00Z

PTP1B inhibitors for type 2 diabetes treatment: a patent review (2011-2014) Tamrakar, Akhilesh K; Maurya, Chandan K.; Rai, Amit K Introduction: Protein tyrosine phosphatase 1B (PTP1B) plays an important role in the negative regulation of insulin signal transduction pathway and has emerged as novel therapeutic strategy for the treatments of type 2 diabetes. PTP1B inhibitors enhance the sensibility of insulin receptor, and has favourable curing effect for insulin resistance related diseases. A large number of PTP1B inhibitors, either synthetic or isolated as bioactive agents from natural products have developed and investigated for their ability to stimulate insulin signaling. Area covered: This review includes an updated summary (2011- 2014) of PTP1B inhibitors that have been published in patent applications, with an emphasis on their chemical structure, mode of action and therapeutic outcomes. The usefulness of PTP1B inhibitors as pharmaceutical agents for the treatment of type 2 diabetes is also discussed. Expert opinion: PTP1B inhibitors show beneficial effects to enhance sensibility of insulin receptor by restricting the activity of enzyme and have favourable curing effects. However, structural homologies in the catalytic domain of PTP1B with other PTPs like LAR, CD45, SHP-2, and TC-PTP presents a challenging task of achieving selectivity. Thus, for therapeutic application of PTP1B inhibitors, highly selective molecules exhibiting desired effects without side effects are expected to find clinical application.

2014-01-01T00:00:00Z Zahir, Abdul Abduz Chauhan, Indira Singh Bagavan, Asokan Kamaraj, Chinnaperumal Elango, Gandhi Shankar, Jai Arjaria, Nidhi Roopan, Mohana Rahuman, Abdul Abdul Singh, Neeloo http://dkr.cdri.res.in:8080/xmlui/handle/123456789/1674 2017-04-19T08:18:32Z 2014-01-01T00:00:00Z

Synthesis of Nanoparticles Using Euphorbia prostrata Extract Reveals a Shift from Apoptosis to G0/G1 Arrest in Leishmania donovani Zahir, Abdul Abduz; Chauhan, Indira Singh; Bagavan, Asokan; Kamaraj, Chinnaperumal; Elango, Gandhi; Shankar, Jai; Arjaria, Nidhi; Roopan, Mohana; Rahuman, Abdul Abdul; Singh, Neeloo The aim of the present investigation was to synthesize silver (Ag) and titanium dioxide (TiO2) nanoparticles (NPs) using the aqueous leaves extract of Euphorbia prostrata as antileishmanial agents and to explore the mechanism of induced cell death. In vitro antileishmanial activity of synthesized NPs was tested against promastigotes of Leishmania donovani by alamarBlue® cell viability reagent and propidium iodide uptake assay. The effective leishmanicidal activity of synthesized Ag NPs was further confirmed by cell cycle progression, externalized phosphatidylserine, DNA fragmentation assay, reactive oxygen species (ROS) level, intracellular non-protein thiols and transmission electron microscopy (TEM) of the treated parasites. TEM analysis of the synthesized Ag NPs and TiO2 NPs showed spherical shape with an average size of 12.82 ± 2.50 and 83.22 ± 1.50 nm, respectively. Ag NPs was found to be the most active agent against Leishmania parasites after 24 h exposure with IC50 value of 14.94 μg/mL. A significant increase in G0/G1 phase of the cell cycle with subsequent decrease in S and G2/M phases was observed when compared to control and thus confirming the growth inhibitory effect of synthesized Ag NPs. Decreased ROS level was also observed which could be responsible for caspase independent shift from apoptosis (G0/G1 arrest) to massive necrosis. High molecular weight DNA fragmentation as a positive consequence of necrotic cell death was also visualized. In the present study, the unique trypanothione/trypanothione reductase (TR) system of Leishmania cells was significantly inhibited by synthesized Ag NPs was reported. The green synthesized Ag NPs may provide promising leads for the development of cost effective and safer alternative treatment against visceral leishmaniasis.

2014-01-01T00:00:00Z