Cardenolides cytotoxic activity

N Kaneda, H Chai, JM Pezznto, AD Kinghom, NR Farnsworth, P Tnchinda, J Udchachon, T Sunstisuk, V Rentraknl. Cytotoxic activity of cardenolides from Beanmontia brevi-tuba stems. Planta Medica 58 429-431, 1992. 

Interest in the possible cytotoxic activity of the amino-glyco-cardenolides has led to the synthesis of 3/S-(4 -amino-4, 6 -dideoxy-) -D-galactopyranosyl)-14j5-hydroxy-5) -card-20(22)-enolide (33) and the 2-amino-2-deoxy- -D-gluco-pyranosides of digitoxigenin, of strophanthidine (34), and of pregnenolone. ... 

For instance, cardenolide glycosides, such as 2 -acetylneriifolin, exhibited a specific pattern of cytotoxic activity in the NCI panel of cell lines (54). Certain cell lines, particularly those among the non-small-cell lung, brain tumor, and renal-cell lines are exceptionally sensitive to 2 -acetylneriifolin, whereas most of the leukemia and colon cell lines were less sensitive to it. From the similar pattern of activity produced by crude extracts of plants of the classes Apocyanaceae and Asclepiadaceae, NCI scientists concluded in this study that similar cardenolide glycosides are present in these extracts. 

Piacente, S., Masullo, M., De Ne ve N., Dewelle, J., Hamed,A., Kiss, R., Mijatovic, T. (2009). Cardenolides from Pergularia tomentosa display cytotoxic activity resulting from their potent inhibition of Na+/K+-ATPase. J.NatProd, 72,1087-1091. 

Recent studies on Asclepias curassavica [197], and Bersama abyssinica [198, 199] have shown that bufadienolides and cardenolides are cytotoxic and that hellebrigenin 3-acetate (XLIX) inhibits W 256 at 8 mg/kg. Structure-activity relationship studies on bufadienolides and cardenolides have failed to reveal the structural features required for activity [194]. 

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