Kumar NS

References (5)

Title : Phytomedicines as potential inhibitors of beta amyloid aggregation: significance to Alzheimer's disease - Kumar_2014_Chin.J.Nat.Med_12_801
Author(s) : Kumar NS , Nisha N
Ref : Chin J Nat Med , 12 :801 , 2014
Abstract : Throughout the history of drug development, plants have been an important source for the discovery of novel therapeutically active compounds for many diseases. The ethnopharmacological approach has provided several leads to identify potential new drugs from plant sources, including those for memory disorders. For the treatment of Alzheimer's disease the drug discovery focus shifted from cholinesterase inhibitors, to other targets primarily based on two key neuropathological hallmarks, namely the hyperphosphorylation of the tau protein resulting in the formation of neurofibrillary tangles (NFTs), and the increased formation and aggregation of amyloid-beta peptide (Abeta) derived from amyloid precursor protein (APP). The present article aims to provide a comprehensive literature survey of plants and their constituents that have been tested for Abeta aggregation, thus possibly relieving several features of Alzheimer's disease (AD).
ESTHER : Kumar_2014_Chin.J.Nat.Med_12_801
PubMedSearch : Kumar_2014_Chin.J.Nat.Med_12_801
PubMedID: 25480511

Title : Design, synthesis and biological evaluation of 4-(1-(4(sulphanilamide)phenyl)-3-(methyl)-1H-pyrazol-5-yl)dine urea and N-acyl derivatives as a soluble epoxide hydrolase inhibitors - Nimbarte_2014_Med.Chem.Res_23_2178
Author(s) : Nimbarte VD , Murtuza H , Phaniraj S , Shrivastava S , Naidu NGM , Kumar NS , Atcha KR
Ref : Med Chem Res , 73 :1357 , 2014
Abstract : A series of novel sEH inhibitors containing a N-substituted piperidine ring [N-urea (8a-i) (9a-l) and amide derivatives (6a-l) (7a-l)] with pyrazole (a five-membered polar heterocycle) as a pharmacophore lead for sEH inhibition have been designed, synthesized and evaluated as novel analogues to reduce blood pressure elevation and inflammatory roles by acting as sEH inhibitors. The synthesized compound shows varying degree of selectivity towards the sEH enzymes. Particularly compounds 9g and 8h emerged as the most potent sEH inhibitor displaying IC50 values of 0.224 +/- 0.014 and 0.220+/- 0.03 muM for in vitro sEH inhibition. Molecular docking studies of the designed sEH dual inhibitors are performed using 1ZD5 for sEH as the targeted proteins and which revealed H-bond interactions similar to AUDA. Structure-activity relationships provided useful insights in these classes of compounds and paved the way to design novel analogues with increased potency.
ESTHER : Nimbarte_2014_Med.Chem.Res_23_2178
PubMedSearch : Nimbarte_2014_Med.Chem.Res_23_2178
PubMedID:

Title : Anticholinesterase activity of standardized extract of Illicium verum Hook. f. fruits - Bhadra_2011_Fitoterapia_82_342
Author(s) : Bhadra S , Mukherjee PK , Kumar NS , Bandyopadhyay A
Ref : Fitoterapia , 82 :342 , 2011
Abstract : Illicium verum is a well known spice in traditional Indian system for its therapeutic potential. The present study was aimed to evaluate the acetylcholinesterase (AChE) and butyrylcholinesterase inhibitory (BChE) activity of standardized extracts of I. verum and its oil. Present study confirmed that anethole contributed to the anticholinesterase activity of I. verum, with more specificity towards AChE. IC(50) for AChE and BChE inhibitory activity of anethole was 39.89+/-0.32 mug/mL and 75.35+/-1.47 mug/mL, whereas for the oil, 36.00+/-0.44 mug/mL and 70.65+/-0.96 mug/mL respectively. Therefore I. verum can be a good lead as anti-cholinesterase agent from natural resources.
ESTHER : Bhadra_2011_Fitoterapia_82_342
PubMedSearch : Bhadra_2011_Fitoterapia_82_342
PubMedID: 21075180

Title : Acetylcholinesterase inhibitory potential of a carbazole alkaloid, mahanimbine, from Murraya koenigii - Kumar_2010_Phytother.Res_24_629
Author(s) : Kumar NS , Mukherjee PK , Bhadra S , Saha BP , Pal BC
Ref : Phytother Res , 24 :629 , 2010
Abstract : In the search for acetylcholinesterase (AChE) inhibitors from Indian medicinal plants, via bioassay-guided isolation, a carbazole alkaloid, mahanimbine [3, 5-dimethyl-3-(4- methylpent-3-enyl)-11H-pyrano [5, 6-a] carbazole], was isolated from the petroleum ether extract of the leaves of Murraya koenigii. Inhibition of AChE was evaluated based on Ellman's method using 96-well microplate readers. Mahanimbine inhibited AChE activity in a dose-dependent manner with an IC(50) value of 0.03 +/- 0.09 mg/mL, while galantamine was used as a standard. The AChE inhibitory activity of this carbazole alkaloid has not been reported so far, and this study is the first to reveal this activity in carbazole alkaloid mahanimbine, isolated from Murraya koenigii.
ESTHER : Kumar_2010_Phytother.Res_24_629
PubMedSearch : Kumar_2010_Phytother.Res_24_629
PubMedID: 19943242

Title : Cholinesterase activity in clam Meretrix casta: possible biomarker for organophosphate pesticide pollution -
Author(s) : Devi KP , Pandian K , Kumar NS
Ref : Bulletin of Environmental Contamination & Toxicology , 74 :250 , 2005
PubMedID: 15841964