Swainsonine (Tridolgosir) 是一种天然的吲哚里西啶生物碱，是一种有效且可逆的 α-甘露糖苷酶 （α-mannosidase） 抑制剂。Swainsonine 诱导细胞凋亡 （apoptosis）和细胞周期停滞在 G2/M 期。Swainsonine 具有抗肿瘤活性。
| 生物活性 | Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversibleα-mannosidaseinhibitor. Swainsonine inducesapoptosisand cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity[1][2][3]. |
体外研究
(In Vitro) | Swainsonine (0-40 μM; 12 h) shows antiproliferative activity in U251 and LN444 cells[2].
Swainsonine (30 μM; 12 h) induces apoptosis and cell cycle arrest at G2/M phase, and decreases the expression of CyclinD1 and CDK4 protein levels, increases the expression of p16 protein level[2].
Swainsonine (30 μM; 12 h) reduces glioma cell migration and invasion[2].
Cell Viability Assay[2] | Cell Line: | U251, LN444 cells | | Concentration: | 0, 10, 20, 30, 40 μM | | Incubation Time: | 12 h | | Result: | Inhibited cell viability in a dose-dependent manner, and shows no cytotoxicity in normal brain cells. |
Cell Cycle Analysis[2] | Cell Line: | U251 cells | | Concentration: | 30 μM | | Incubation Time: | 12 h | | Result: | Induced cell cycle arrest at G2/M phase. |
Apoptosis Analysis[2] | Cell Line: | U251 cells | | Concentration: | 30 μM | | Incubation Time: | 12 h | | Result: | Induced apoptosis with the cleaved-Caspase-3 and cleaved-Caspase-9 expression were obviously increased. |
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体内研究
(In Vivo) | Swainsonine (1 mg/kg; i.p.; twice daily for ten days) and cisplatin increases the anti-tumor efficacy in mouse[3].
| Animal Model: | Eighty-seven sixty-day-old male C57BL/6 mice[3] | | Dosage: | 1 mg/kg (cisplatin; 0.25 mg/kg, i.p., every other day for 10 days) | | Administration: | I.p.; twice daily for ten days | | Result: | Showed a significant reduction in ascites volume of 63.5% was observed in mice and a significant reduction in the percentage of cells in the G0/G1, S and G2 phases. |
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| 结构分类 | - Alkaloids
- Pyrrole Alkaloids
- Alkaloids
- Piperidine Alkaloids
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| 来源 | - Plants
- Leguminosae
- Sphaerophysa salsula
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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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 10 mg/mL(57.73 mM;Need ultrasonic and warming) Ethanol : 10 mg/mL(57.73 mM;Need ultrasonic and warming) H2O : 3.57 mg/mL(20.61 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 5.7733 mL | 28.8667 mL | 57.7334 mL | | 5 mM | 1.1547 mL | 5.7733 mL | 11.5467 mL | | 10 mM | 0.5773 mL | 2.8867 mL | 5.7733 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。 |
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