Cardenolide glycosides from the seeds of Digitalis purpurea exhibit carcinoma-specific cytotoxicity toward renal adenocarcinoma and hepatocellular carcinoma cells. Issue 2 (1st February 2015)

• Record Type: Journal Article
• Authors: Fujino, Tomofumi; Kuroda, Minpei; Matsuo, Yukiko; Kubo, Satoshi; Tamura, Chikako; Sakamoto, Nami; Mimaki, Yoshihiro; Hayakawa, Makio
• Is Part Of: Bioscience, biotechnology, and biochemistry. Volume 79:Issue 2(2015)
• Page Start: 177
• Page End: 184
• Publication Date: 2015-02-01
• Subjects: cardenolide glycoside -- carcinoma-specific cytotoxicity -- adenocarcinoma -- hepatocellular carcinoma -- CDK inhibitor; Biotechnology -- Periodicals; Biochemistry -- Periodicals; 660.6
• DOI: 10.1080/09168451.2014.975183
• Languages: English
• ISSNs: 0916-8451

Abstract

Abstract: Four cardenolide glycosides, glucodigifucoside (2), 3′- O -acetylglucoevatromonoside (9), digitoxigenin 3- O -β-D-glucopyranosyl-(1→4)-β-D-glucopyranosyl-(1→4)-3- O -acetyl-β-D-digitoxopyranoside (11), and purpureaglycoside A (12), isolated from the seeds of Digitalis purpurea, exhibited potent cytotoxicity against human renal adenocarcinoma cell line ACHN. These compounds exhibited significantly lower IC50 values against ACHN than that against normal human renal proximal tubule-derived cell line HK-2. In particular, 2 exhibited the most potent and carcinoma-specific cytotoxicity, with a sixfold lower IC50 value against ACHN than that against HK-2. Measurement of cyclin-dependent kinase inhibitor levels revealed that upregulation of p21/Cip1 expression was involved in the carcinoma-specific cytotoxicity of 2. Further, compound 2 also exhibited the carcinoma-specific cytotoxicity toward hepatocellular carcinoma cell line. Graphical abstract: : Glucodigifucoside (compound 2) from the seeds of Digitalis purpurea exhibit carcinoma-specific cytotoxicity towards renal adenocarcinoma cells in p53/p21-dependent manner.