CATIONIC PEPTIDE LACTOFERRICIN B INHIBITS GLUTATHIONE S-TRANSFERASE P1 FROM HUMAN PLACENTA AND BREAST CANCER CELL LINE MDA-MB-231 PREVENTING ANTICANCER DRUG METABOLISM
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 8
Abstract
Objective: To investigate the interaction of LfcinB (Lactoferricin B) with GSTP1 (Glutathione S-Transferase P1) from human placental and breast cancer cell line MDA-MB-231.Methods: We examined the interaction of Lfcin B with human placental GSTP1 and breast adenocarcinoma MD-MB-231 cell line. Enzyme activity of GSTP1 was measured with and without pre-incubation with Lfcin B. Kinetic variables were determined by incubating the enzyme reaction mixture with fixed GSH (reduced glutathione) concentration and varying CDNB (1-chloro-2, 4-dinitrobenzene) concentrations or fixed CDNB concentration and varying GSH concentrations.Results: Lfcin B is a competitive inhibitor with respect to GSH binding site (G site) and noncompetitive inhibitor with respect to hydrophobic substrate unit (H site) of human placental GSTP1 enzyme. Lfcin B was also incubated with GSTP1 from breast adenocarcinoma MDA-MB-231 cell line. The activity of GSTP1 was much higher (0.2665 μ mol/ml/min) in Lfcin B untreated MDA-MB-231 cell line, whereas MDA-MB-231 with Lfcin B treatment showed a very low activity (0.0254 μ mol/ml/min).Conclusion: Our Findings suggest that Lfcin B can inhibit the GSTP1 activity in human placental and MDA-MB-231 breast cancer cell lines, which may induce synergistic effects when used in combination with antineoplastic drugs that are substrates of GSTP1 enzyme. This combination will exert a double attack on cancers over expressing GSTP1, first sensitizing them to anticancer drugs by preventing their metabolism.Â
Authors and Affiliations
Amir Riyaz Khan, Pankaj Taneja
Keywords
Related Articles
- EP ID EP578312
- DOI -
- Views 53
- Downloads 0
PREPARATION AND CHARACTERIZATION OF ORAL NANOSUSPENSION LOADED WITH CURCUMIN
Objective: The principle objective of the present research work was to improve the bioavailability of curcumin (CUR) by decreasing its particle size. Nanosuspension (NS) of CUR was prepared using poloxamer-188 (P188) as...
THE EFFECT OF ROSELLA (HIBISCUS SABDARIFFA L) TREATMENT ON IL-10 AND IL-14 SECRETION ON DIMETHYLBENZ (A) ANTHRACENE (DMBA) INDUCED RAT
Objective: The objective of this study was to determine the effect of ethanolic extract rosella calyx pretreatment on increasing secretion of IL-10 and IL-14 on SD rats treated with DMBA.Methods: Rats were treated with a...
DEVELOPMENT OF SIMPLE HPLC METHOD TO ESTIMATE THE BLOOD PLASMA CONCENTRATION OF EFAVIRENZ IN RAT AFTER ORAL ADMINISTRATION
Objective: The present study was design with an objective of developing a simple and rapid high performance liquid chromatography (HPLC) method for the determination of Efavirenz (EFA) in rat plasma.Methods: Chromatograp...
DEPRESSION IN PREGNANCY - CONSEQUENCES AND TREATMENT MODALITIES
Depression is a mood disorder which can affect 1 in every 4 women at some point of life even during pregnancy. Depression is most often not properly diagnosed during pregnancy as it is assumed by people to be just anothe...
ENHANCING ORAL BIOAVAILABILITY OF CARVEDILOL USING SOLID DISPERSION TECHNIQUE
Objective: Carvedilol (CRV) is a beta blocker drug that is basically used for the treatment of hypertension, heart failure and arrhythmias. The objective of this study is to increase the oral bioavailability of CRV by us...