title: Dexniguldipine hydrochloride inhibits growth of human pancreatic adenocarcinoma cells and expression of protein kinase C isoforms alpha and zeta.
abstract: New therapeutic regimens are needed for the treatment of pancreatic cancer. In view of the importance of protein kinase C (PKC) in tumorigenesis, we evaluated the effects of dexniguldipine hydrochloride (DNIG) on the in vitro growth of CFPAC-1 human pancreatic adenocarcinoma cells and the expression of PKC isoforms. DNIG is a potent antineoplastic drug with well-established anti-PKC activity and the ability to reverse multidrug resistance. DNIG (1.6-25 mu M) decreased the number of cells in culture in a time- and dose-dependent manner with an EC(50) of 4.9 mu M on day 1 and 2.8 mu M on day 3. When PKC isoform expression in CFPAC-1 cells was analyzed by immunoblotting, the predominant isoforms were identified as alpha and zeta. The expression of PKC alpha and zeta was inhibited significantly by DNIG (0.63-2.5 mu M). These results suggest that DNIG suppresses the proliferation of CFPAC-1 pancreatic cancer cells, possibly by inhibiting the expression of specific PKC isoforms.
authors.affiliation: TULANE UNIV,SCH MED,DEPT PHARMACOL,NEW ORLEANS,LA 70112. TULANE UNIV,SCH MED,DEPT MED,NEW ORLEANS,LA 70112. TULANE UNIV,SCH MED,TULANE CANC CTR,NEW ORLEANS,LA 70112.
authors.forename: Y
authors.initials: Y
authors.lastname: Qin
authors.forename: Y
authors.initials: Y
authors.lastname: Tang
authors.forename: A
authors.initials: A
authors.lastname: Schally
authors.forename: B
authors.initials: B
authors.lastname: Beckman