They key toxic component of oleander is oleandrin. It only accounts for 0.08 % of total cardenolides and have a bioavailability of 30 %. The yellow flowered oleander contains Peruvoside. The primary mode of action of these cardenolides is inhibition of Na+/K+-ATPase pump on cardiomyocytes, which results in intracellular Na+ build up. Upon Na+/K+-ATPase, intracellular K+ is elevated, leading to cytosolic Ca2+ buildup through Na+/Ca2+ exchanger on plasma membrane. Increasing of intracellular Ca2+ induces more Ca2+ release form the sarcoplasmic reticulum. The cytosolic Ca2+ binds to troponin-C (actin binding protein) and induces inotropy, resulting in cardiac muscle contraction and vasoconstriction.
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On the hand, Peruvoside can be used for the research of heart failure. On the one hand, Peruvoside can be used for cancer research.
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. First, Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside (50-1000 nM, 24 h) inhibits the viability and proliferation in PC9, PC9/gef, H3255, and H1975 cell lines. Second, Peruvoside (0.005-0.5 μM, 72 h) sensitizes A549, PC9/gef and H1975 to Gefitinib when in combination with Gefitinib (0.01~0.5 μM). Third, Peruvoside (0-100 μM, 24 h) induces cell cycle arrest and apoptosis in MCF-7, HpG2, and A549 cells. Meanwhile, Peruvoside (0.1 mg/kg for i.p.; once daily for 28 days) suppresses the tumour growth in lung cancer mice model. Peruvoside (0.59 mg/kg for i.p.; once daily for 7 days) reduces mortality in EV-A71-infected mice model.
Furthermore, Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses.
Reference:
[1] Dey P. Biomed Pharmacother. 2020 Sep;129:110422.
[2] Lai Y, et al. Am J Cancer Res. 2022 Jun 15;12(6):2576-2593.
[3] Reddy D, et al. Life Sci. 2020 Jan 15;241:117147.