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Ren, Yulin
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article
The Cytotoxic Cardiac Glycoside (-)-Cryptanoside A from the Stems of <i>Cryptolepis dubia</i> and Its Molecular Targets.
Abstract
A cardiac glycoside epoxide, (-)-cryptanoside A (<b>1</b>), was isolated from the stems of <i>Cryptolepis dubia</i> collected in Laos, for which the complete structure was confirmed by analysis of its spectroscopic and single-crystal X-ray diffraction data, using copper radiation at a low temperature. This cardiac glycoside epoxide exhibited potent cytotoxicity against several human cancer cell lines tested, including HT-29 colon, MDA-MB-231 breast, OVCAR3 and OVCAR5 ovarian cancer, and MDA-MB-435 melanoma cells, with the IC<sub>50</sub> values found to be in the range 0.1-0.5 μM, which is comparable with that observed for digoxin. However, it exhibited less potent activity (IC<sub>50</sub> 1.1 μM) against FT194 benign/nonmalignant human fallopian tube secretory epithelial cells when compared with digoxin (IC<sub>50</sub> 0.16 μM), indicating its more selective activity toward human cancer versus benign/nonmalignant cells. (-)-Cryptanoside A (<b>1</b>) also inhibited Na<sup>+</sup>/K<sup>+</sup>-ATPase activity and increased the expression of Akt and the p65 subunit of NF-κB but did not show any effects on the expression of PI3K. A molecular docking profile showed that (-)-cryptanoside A (<b>1</b>) binds to Na<sup>+</sup>/K<sup>+</sup>-ATPase, and thus <b>1</b> may directly target Na<sup>+</sup>/K<sup>+</sup>-ATPase to mediate its cancer cell cytotoxicity.