Millepachine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Millepachine 是一种在中草药中发现的天然产物，对多种人类癌细胞具有很强的抗肿瘤作用。

Millepachine is a natural product found in the Chinese herbal medicine with strong antitumor effects against numerous human cancer cells.(In Vitro):Millepachine (2-8 μM; 24 h) inhibits ATP-binding cassette transporter activity in A2780CP cells. Millepachine (2-8 μM; 24 or 48 h) induces significant G2/M arrest and apoptosis of cisplatin-sensitive A2780S and cisplatin-resistant A2780CP 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. Millepachine (2-8 μM; 24 h) decreases topoisomerase II levels in A2780S and A2780CP cells. Millepachine (1.25-20 μM; 48 h) remarkably inhibits the proliferation of cisplatin-resistant A2780CP cells with an IC50 of 4 μM.(In Vivo):Millepachine (20 mg/kg; i.v.) reduced tumor volume and tumor weight with the inhibitory rate of 73.21% and 65.58% in A2780S and A2780CP xenograft models, respectively. Millepachine does not induce acquired drug resistance in an excised A2780S xenograft model.

Millepachine (1.25-20 μM; 48 h) remarkably inhibits the proliferation of cisplatin-resistant A2780CP cells.Millepachine (2-8 μM; 24 or 48 h) induces G2/M arrest and apoptosis cisplatin-sensitive A2780S and cisplatin-resistant A2780CP cells.Millepachine (2-8 μM; 24 h) decreases topoisomerase II levels in A2780S and A2780CP cells.Millepachine (2-8 μM; 24 h) inhibits ATP-binding cassette transporter activity in A2780CP cells.Cell Proliferation Assay 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 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 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 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.Millepachine (20 mg/kg; i.v. every two days for 14 day) does not induce acquired drug resistance in an excised A2780S xenograft model. Animal Model:Female BALB/c nude mice (6 weeks) are injected A2780S or A2780CP cells 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.

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Apoptosis

Apoptosis

NO

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1393922-01-4

350.41

C22H22O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (285.38 mM)

CC(C)(C=Cc1c(cc2)OC)Oc1c2C(/C=C/c(cc1)ccc1OC)=O

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(-20℃)

With Ice Pack

≥ 2 years