93800-59-0

93800-59-0 structure

Name: 8α,9α-Epoxycoleon-U-quinone
Chemical Name: 8α,9α-Epoxycoleon-U-quinone
CAS Number: 93800-59-0
Molecular Formula: C₂₀H₂₄O₆
Molecular Weight: 360.40
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P-glycoprotein
Create Date: 2022-10-08 17:21:25
Modify Date: 2024-01-19 16:02:17
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].

Name	8α,9α-Epoxycoleon-U-quinone

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein
In Vitro	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.
References	[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.

Molecular Formula	C₂₀H₂₄O₆
Molecular Weight	360.40

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