同义名 :	-
	CAS号 :	1393922-01-4
	货号 :	A1263334
	分子式 :	C22H22O4
	纯度 :	97%
	分子量 :	350.41
	MDL号 :	N/A
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Millepachine (MIL), a bioactive natural chalcone from Chinese herbal medicine Millettia pachycarpa Benth, exhibits strong antitumor effects against many human cancer cells both in vitro and in vivo. MIL significantly inhibited the proliferation of cisplatin-resistant A2780CP cells via inducing obvious G2/M arrest and apoptosis and down-regulating the activity of topoisomerase II protein. MIL did not only significantly inhibit the tumor growth in cisplatin-sensitive A2780S xenograft model, with an inhibitory rate of 73.21%, but also inhibited the tumor growth in the cisplatin-resistant A2780CP xenograft model, with an inhibitory rate of 65.68%. In addition, MIL did not induce acquired drug resistance in A2780S tumor-bearing mice with an inhibitory rate of 60.03%[2]. MIL induced multipolar spindles by inhibiting the activity of Eg5 and inhibited mitotic spindle formation and chromatin condensation by the activation of the spindle assembly checkpoint (SAC) in tumor cells[3]. MIL exhibited anti-tumor activity through inhibiting topoisomerase II activity to induce tumor cells DNA damage, and MIL-activated NF-κB pathway showed a pro-apoptotic function in response to DNA damage[4]. MIL-1 exerted much better antitumor activity than millepachine, manifesting as a 24- to 201-fold increase in vitro cytotoxicity and a 2.4-fold increase in in vivo antitumor activity in hepatocellular cell lines-derived models. MIL-1 displayed remarkable antitumor activity with an IC50 of 31-207 nM towards various human cancer cell lines derived from various organs and tissues, and it exerted no evidence of toxicity against normal cells[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.85mL 0.57mL 0.29mL	14.27mL 2.85mL 1.43mL	28.54mL 5.71mL 2.85mL

参考文献

[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. [2]Wu W, Liu Y, Ye H, Li Z. 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 [3]Wu W, Liu F, Su A, Gong Y, Zhao W, Liu Y, Ye H, Zhu J. The effect and mechanism of millepachine-disrupted spindle assembly in tumor cells. Anticancer Drugs. 2018 Jun;29(5):449-456 [4]Wu W, Ma B, Ye H, Wang T, Wang X, Yang J, Wei Y, Zhu J, Chen L. Millepachine, a potential topoisomerase II inhibitor induces apoptosis via activation of NF-κB pathway in ovarian cancer. Oncotarget. 2016 Aug 9;7(32):52281-52293 [5]Yan J, Zhuang Q, Li Z, Xiong Y, He M, Kang C, Zhang Q, Han L, Liang E, Liu H, Ke P, Huang X. MIL-1, a novel antitumor agent derived from natural product millepachine, acts as tubulin polymerization inhibitor for the treatment of hepatocellular carcinoma. Eur J Pharmacol. 2021 May 5;898:173975