8α,9α-Epoxycoleon-U-quinone

8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX[1].

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

8α,9α-Epoxycoleon-U-quinone (2, 5, 10, 20, 50 μM; 72 h) selective towards cancer cell lines, with a selectivity index of 2.0[1]. 8α,9α-Epoxycoleon-U-quinone (10 μM; 72 h) is able to inhibit P-glycoprotein (P-gp) activity in NCI-H460/R cells[1]. 8α,9α-Epoxycoleon-U-quinone (1, 2, 5 μM; 72 h) reverses the resistance of cancer cells to DOX and increase anti-cancer efficacy of DOX[1]. Cell Viability Assay[1] Cell Line: NCI-H460, NCI-H460/R, MRC-5 cells Concentration: 2, 5, 10, 20, 50 μM Incubation Time: 72 h Result: Showed inhibition of cancer cell viability (IC50≈20 μM) with a selectivity index of 2.0. Cell Viability Assay[1] Cell Line: NCI-H460/R cells Concentration: 10 μM Incubation Time: 72 h Result: Decreased the Rho123 accumulation in NCI-H460/R cells, and no influence on the ABCB1 expression. Cell Viability Assay[1] Cell Line: NCI-H460/R cells Concentration: 1, 2, 5 μM (combine with Doxorubicin (DOX)) Incubation Time: 72 h (pre-treat) Result: Promoted sensitization of NCI-H4l60/R cells to DOX with relative reversal indexes of 1.976 and 4.696 for concentration of 1 and 2 μM, respectively.

[1]. Ntungwe EN, et al. C20-nor-Abietane and Three Abietane Diterpenoids from Plectranthus mutabilis Leaves as P-Glycoprotein Modulators. ACS Med Chem Lett. 2022 Mar 11;13(4):674-680.