Millepachine 是来自中草药Millettia pachycarpaBenth 的生物活性天然查尔酮，在体内外对多种人类癌细胞均显示出强大的抗肿瘤作用。
| 生物活性 | Millepachine is a bioactive natural chalcone from Chinese herbal medicineMillettia pachycarpaBenth, exhibits strong antitumor effects against numerous humancancercells both in vitro and in vivo[1]. |
体外研究
(In Vitro) | 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 IC50of 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. |
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体内研究
(In Vivo) | 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. |
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| 来源 | - Plants
- Leguminosae
- Millettia pachycarpaBenth.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(285.38 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8538 mL | 14.2690 mL | 28.5380 mL | | 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | | 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (7.13 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (7.13 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.13 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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