Millepachine

Millepachine is a bioactive natural chalcone from Chinese herbal medicine Millettia pachycarpa Benth, exhibits strong antitumor effects against numerous human cancer cells both in vitro and in vivo[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Millepachine (1.25-20 μM; 48 h) remarkably inhibits the proliferation of cisplatin-resistant A2780CP cells[1]. Millepachine (2-8 μM; 24 or 48 h) induces G2/M arrest and apoptosis cisplatin-sensitive A2780S and cisplatin-resistant A2780CP cells[1]. Millepachine (2-8 μM; 24 h) decreases topoisomerase II levels in A2780S and A2780CP cells[1]. Millepachine (2-8 μM; 24 h) inhibits ATP-binding cassette transporter activity in A2780CP cells[1]. Cell Proliferation Assay[1] Cell Line: A2780CP cells Concentration: 0, 1.25, 2.5, 5, 10, 20 μM Incubation Time: 48 hours Result: Inhibited the cells proliferation with an IC50 of 4 μM. Cell Cycle Analysis[1] Cell Line: A2780S and A2780CP cells Concentration: 2, 4, 8 μM Incubation Time: 24 or 48 hours Result: Induced significant G2/M arrest both in both cells. The percentage of cells in the G2/M fraction increased from 15.99% in vehicle cells to 24.93%, 60.67%, and 77.31% at dose of 2, 4, and 8 μM in A2780S cells, respectively. Apoptosis Analysis[1] Cell Line: A2780S and A2780CP cells Concentration: 2, 4, 8 μM Incubation Time: 24 or 48 hours Result: The percentage of apoptotic cells increased from 1.49% in vehicle cells to 10.98%, 20.60%, and 39.43% at dose of 2, 4, and 8 μM in A2780S cells, respectively. The percentage of apoptotic cells increased from 0.87% to 10.97%, 25.28%, and 37.59% in A2780CP cells, respectively. Western Blot Analysis[1] Cell Line: A2780S and A2780CP cells Concentration: 0, 2, 4, 8 μM Incubation Time: 24 hours Result: Decreased the levels of topoisomerase II (TOPO II) in both cells.

Millepachine (20 mg/kg; i.v. every two days for 14 day) inhibits tumor growth in mice[1]. Millepachine (20 mg/kg; i.v. every two days for 14 day) does not induce acquired drug resistance in an excised A2780S xenograft model[1]. Animal Model: Female BALB/c nude mice (6 weeks) are injected A2780S or A2780CP cells[1] Dosage: 20 mg/kg Administration: I.v. every two days for 2-14 days Result: Reduced tumor volume and tumor weight with the inhibitory rate of 73.21% and 65.58% in A2780S (after seven times injection) and A2780CP (after six times injection) xenograft model, respectively. With low toxicity in vivo.

[1]. Wu W, et, al. Millepachine showed novel antitumor effects in cisplatin-resistant human ovarian cancer through inhibiting drug efflux function of ATP-binding cassette transporters. Phytother Res. 2018 Dec; 32(12):2428-2435.