Piperidones

Publication Title: 
European Journal of Pharmaceutical Sciences: Official Journal of the European Federation for Pharmaceutical Sciences

Piplartine (piperlongumine, 5,6-dihydro-1-[(2E)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propenyl]-2(1H)-pyridinone) is a biologically active alkaloid/amide from peppers, as from long pepper (Piper longum L. - Piperaceae). Long pepper is one of the most widely used in Ayurvedic medicine, which is used to treat many diseases, including tumors.

Author(s): 
Bezerra, Daniel P.
Pessoa, Claudia
de Moraes, Manoel O.
Saker-Neto, Nicolau
Silveira, Edilberto R.
Costa-Lotufo, Leticia V.
Publication Title: 
Methods and Findings in Experimental and Clinical Pharmacology

The present study explores pharmacologically on the model spontaneously beating 3H-noradrenaline pretreated guinea-pig atrial preparation the mechanism(s) by which the representative central nervous system (CNS) stimulant drug 3-methyl-3-ethylglutarimide (bemegride, MEG) and its representative CNS depressant homologue 3-methyl-3-n-butylglutarimide (MBG) affect transmitter release and the force and rate of atrial contraction and contracture, as well as the relevance of these atrial mechanism(s) to those involved in the production of drug-evoked convulsions and hypnosis in the mammalian CNS.

Author(s): 
Arblaster, C. I.
Cameron, D. W.
Lavi, Y.
Laycock, G. M.
Shulman, A.
Publication Title: 
Cancer Research

Diphenyl difluoroketone (EF24), a molecule having structural similarity to curcumin, was reported to inhibit proliferation of a variety of cancer cells in vitro. However, the efficacy and in vivo mechanism of action of EF24 in gastrointestinal cancer cells have not been investigated. Here, we assessed the in vivo therapeutic effects of EF24 on colon cancer cells. Using hexosaminidase assay, we determined that EF24 inhibits proliferation of HCT-116 and HT-29 colon and AGS gastric adenocarcinoma cells but not of mouse embryo fibroblasts.

Author(s): 
Subramaniam, Dharmalingam
May, Randal
Sureban, Sripathi M.
Lee, Katherine B.
George, Robert
Kuppusamy, Periannan
Ramanujam, Rama P.
Hideg, Kalman
Dieckgraefe, Brian K.
Houchen, Courtney W.
Anant, Shrikant
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