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Institution

Central Drug Research Institute

FacilityLucknow, Uttar Pradesh, India
About: Central Drug Research Institute is a facility organization based out in Lucknow, Uttar Pradesh, India. It is known for research contribution in the topics: Leishmania donovani & Brugia malayi. The organization has 4357 authors who have published 7257 publications receiving 143871 citations. The organization is also known as: Central Drug Research Institute, Lucknow & CDRI.


Papers
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Journal ArticleDOI
TL;DR: It is suggested that AT2R, via PP2A-mediated inhibition of PKC, prevents the NOX activation, ROS generation, and subsequent pro-inflammatory activation of microglia.
Abstract: Microglia-induced reactive oxygen species (ROS) production and inflammation play an imperative role in neurodegenerative diseases like Alzheimer's disease (AD) and Parkinson's disease (PD). It has been established that angiotensin II type-2 receptor (AT2R) activation is neuroprotective in central nervous system diseases like stroke and AD. However, the involvement of AT2R in NADPH oxidase (NOX)-mediated microglia activation is still elusive. Therefore, the present study investigated the role of AT2R in angiotensin II (Ang II) or Phorbol 12-myristate 13-acetate (PMA)-induced microglia activation in BV2 cells, primary microglia, p47phox knockout (p47KO) microglia, and in vivo. Treatment of microglia with Ang II or PMA induced a significant ROS generation and promoted pro-inflammatory microglia in a NOX-dependent manner. In contrast, AT2R activation by CGP42112A (CGP) inhibited NOX activation, ROS production, and pro-inflammatory microglia activation, while promoting the immunoregulatory microglia. This inhibitory effect of AT2R on NOX and pro-inflammatory activation was attenuated by AT2R antagonist, PD123319. Essentially, NOX inhibition (by DPI) or scavenging cellular ROS (by NAC) or p47KO microglia were immune to Ang II- or PMA-induced pro-inflammatory microglia activation. Mechanistically, AT2R, via activation of protein phosphatase-2A (PP2A), prevented the Ang II- or PMA-induced protein kinase C (PKC) activation and phosphorylation of p47phox, an effect that was reversed by the addition of PP2A inhibitor, Okadaic acid (OA). Importantly, PKC inhibitor, Rottlerin, inhibited the Ang II- or PMA-induced p47phox phosphorylation and ROS generation to the similar extent as AT2R activation. In addition, AT2R activation or p47KO prevented ROS production, pro-inflammatory microglial activation, and sickness behavior in mice model of neuroinflammation. Therefore, the present findings suggested that AT2R, via PP2A-mediated inhibition of PKC, prevents the NOX activation, ROS generation, and subsequent pro-inflammatory activation of microglia.

53 citations

Journal ArticleDOI
TL;DR: It is suggested that HA coated LPT-NCs formulation enhances the activity of LPT against triple negative breast cancer, exhibiting magnificent therapeutic outcome at low dose thus presenting a strategy to reduce dose administrations and minimize dose related toxicity.

53 citations

Journal ArticleDOI
TL;DR: The benzopyran 16 was found to be more effective antiestrogen than tamoxifen while being as effective as LY-117018 and has thus emerged as a new class of potent antiestrogens.
Abstract: A series of 2,3-diaryl-1-benzopyran analogues substituted at position 4 of 2-phenyl with a hydroxy or pyrrolidinoethoxy residue were synthesized as models for (E)-triarylpropenones constrained in the s-trans conformation. The prototypes, belonging to five chemical series, were evaluated for their estrogen receptor affinity and for estrogen agonist-antagonist activities. The 4H-1-benzopyran-4-one, the 2,3-dihydro-4H-1-benzopyran-4-one, the 4H-1-benzopyran, and the 2,3-dihydro-1-benzopyran derivatives were found to be inactive or only marginally activate as receptor ligands or estrogen agonists-antagonists. In the 2H-1-benzopyran category the parent phenol was also inactive whereas the basic ethers 16 and 26 were modest receptor ligands while being quite active as antiestrogens. In a comparative study the benzopyran 16 was found to be more effective antiestrogen than tamoxifen while being as effective as LY-117018. The benzopyrans have thus emerged as a new class of potent antiestrogens.

53 citations

Journal ArticleDOI
TL;DR: The first dual colorimetric and ratiometric fluorescent probe naphtho[2,1-b][1,10]phenanthroline for selective and 'direct' visualization of labile iron(III) pools in a multicellular organism, Caenorhabditis elegans is reported.

53 citations

Journal ArticleDOI
TL;DR: Piper longum fruit possessed a demonstrable immunostimulatory activity, both specific and nonspecific, as evident from the standard test parameters such as haemagglutination titre (HA), plaque forming cell (PFC) counts, macrophage migration index (MMI) and phagocytic index (PI).
Abstract: Piper longum fruit, used in traditional remedies as well as in the Ayurvedic system of medicine against intestinal disorders, was tested for its efficacy against experimental infection of Giardia lamblia in mice. On in vitro test, an aqueous extract of P. longum fruit powder (PF) at 250 microg/mL and its ethanol extract at 125 microg/mL showed 100% giardicidal activity. A low order activity was found in the n-butanol extract. Further fractionation in hexane and chloroform resulted in a total loss of activity. The survival of-trophozoites in mice at 900 mg/kg body weight was 11.12 in PF, 8. 54 in aqueous extract, 5.81 in ethanol extract. The antigiardial activity of PF in hexane, chloroform and n-butanol soluble fractions was comparable to the drug-untreated control (47.63). Piper longum possessed a demonstrable immunostimulatory activity, both specific and nonspecific, as evident from the standard test parameters such as haemagglutination titre (HA), plaque forming cell (PFC) counts, macrophage migration index (MMI) and phagocytic index (PI). A maximum effect was found at 225 mg/kg body weight in mice. The effect was marginally reduced at higher doses of 450 and 900 mg/kg or the lower dose of 112.5 mg/kg.

53 citations


Authors

Showing all 4385 results

NameH-indexPapersCitations
Sanjay Kumar120205282620
John A. Katzenellenbogen9569136132
Brajesh K. Singh8340124101
Gaurav Sharma82124431482
Sudhir Kumar82524216349
Pramod K. Srivastava7939027330
Mohan K. Raizada7547321452
Syed F. Ali7144618669
Ravi Shankar6667219326
Ramesh Chandra6662016293
Manoj Kumar6540816838
Manish Kumar61142521762
Anil Kumar Saxena5831010107
Sanjay Krishna5662413731
Naibedya Chattopadhyay562429795
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Performance
Metrics
No. of papers from the Institution in previous years
YearPapers
20233
202255
2021306
2020232
2019246
2018289