Bufalin a major digoxin-like immunoreactive component of the Chinese medicine Chan Su; has been shown to exert a potential for anticancer activity against various human cancer cell lines in vitro. Bufalin is a potent small-molecule inhibitor of the steroid receptor coactivators steroid receptor coactivator (SRC)-3 and SRC-1, it also as a potentially broad-spectrum small-molecule inhibitor for cancer. Bufalin can partly reverse the MDR of K562/VCR cells, with a possible mechanism of down-regulating MRP1 expression and activating apoptosis pathway by altering Bcl-xL/Bax ratio. Bufalin is a 14beta-hydroxy steroid that is bufan-20,22-dienolide having hydroxy substituents at the 5beta- and 14beta-positions. It has been isolated from the skin of the toad Bufo bufo. It has a role as an antineoplastic agent, a cardiotonic drug, an anti-inflammatory agent and an animal metabolite. It is a 3beta-hydroxy steroid and a 14beta-hydroxy steroid. It is functionally related to a bufanolide.

Hyodeoxycholic acid is a member of the class of 5beta-cholanic acids that is (5beta)-cholan-24-oic acid substituted by alpha-hydroxy groups at positions 3 and 6. It is a bioactive compound extracted from Calculus bovis. It has a role as a mouse metabolite and a human metabolite. It is a C24-steroid, a bile acid, a member of 5beta-cholanic acids and a 6alpha,20xi-murideoxycholic acid. It is functionally related to a cholic acid. It is a conjugate acid of a hyodeoxycholate. Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells. Hyodeoxycholic acid has hypolipidemic effect through regulation of FXR activation, it is a candidate for antiatherosclerotic drug, by significantly increasing the expression of genes involved in cholesterol efflux, such as Abca1, Abcg1,and Apoe,in a macrophage cell line.

The cardiac glycosides digitoxin and digoxin have been used in cardiac diseases for many years, digitoxin also has growth inhibition activity in three human cancer cell line, digitoxin activates pro-apoptotic, anti-proliferative signaling cascades and cell cycle arrest. Digitoxin could as a candidate drug for suppressing IL-8-dependent lung inflammation in cystic fibrosis (CF), it can suppress hypersecretion of IL-8 from cultured cystic fibrosis (CF) lung epithelial cells, the specific mechanism is to block phosphorylation of the inhibitor of NF-kappa.Digitoxin actively inhibits Herpes simplex virus type 1 (HSV-1) replication with a 50% effective concentration (EC(50)) of 0.05 microM, the inhibitory effects of digitoxin are likely to be introduced at the early stage of HSV-1 replication and the virus release stage. Digitoxin is a cardenolide glycoside in which the 3beta-hydroxy group of digitoxigenin carries a 2,6-dideoxy-beta-D-ribo-hexopyranosyl-(14)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(14)-2,6-dideoxy-beta-D-ribo-hexopyranosyl trisaccharide chain. It has a role as an EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor. It is functionally related to a digitoxigenin. It is a conjugate acid of a digitoxin(1-).

Digoxin is a cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small. It has a role as an anti-arrhythmia drug, a cardiotonic drug, an epitope and an EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor. Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure. Digoxin and other cardiac glycosides can inhibit hypoxia-inducible factor 1 (HIF-1)α synthesis and block tumor growth.

Convallatoxin is a cardenolide glycoside that consists of strophanthidin having a 6-deoxy-alpha-L-mannopyranosyl (L-rhamnosyl) group attached at position 3. It has a role as a metabolite and a vasodilator agent. It is a steroid aldehyde, a steroid lactone, an alpha-L-rhamnoside, a 14beta-hydroxy steroid, a 19-oxo steroid and a 5beta-hydroxy steroid. It is functionally related to a strophanthidin. Convallatoxin, one cardiac glycoside, is a novel anti-angiogenic compound via dual inducing of autophagy and apoptosis, it shows antitumor effects that harbor inactivating mutations in the p53 signaling pathway. Convallatoxin as a novel antiviral, limiting mRNA translation has a dramatic impact on CMV infection and proliferation. Convallatoxin also anti-diabetic activity.