picropodophyllin

Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast stem cell growth factor (KIT).

Picropodophyllin-β-D-glucoside (compound 3), a podophyllotoxin glucoside, has been isolated from Chinese medicinal plants [1].

Picropodophyllin-4-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (compound 17), a lignan, has been isolated from the roots and rhizomes of Podophyllum sinensis [1].

Picropodophyllotoxin (AXL 1717) is a cyclolignan alkaloid found in the mayapple plant family (Podophyllum peltatum), and a small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Picropodophyllotoxin (AXL 1717) specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT). This agent shows potent activity in the suppression o f tumor cell proliferation and the induction of tumor cell apoptosis. IGF1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a critical role in the growth and survival of many types of cancer cells.

β-Apopicropodophyllin, a natural product isolated from Hyptis wticillata, promotes apoptosis through mechanisms including microtubule disruption, DNA damage, cell cycle arrest, and ER stress. This compound holds potential for cancer research applications [1].