Pladienolide B 是一种有效的癌细胞生长抑制剂，其作用靶向剪接体的SF3B1亚单位。Pladienolide B 通过抑制前 mRNA 剪接发挥抗肿瘤作用，诱导调亡。
| 生物活性 | Pladienolide B is a potentcancercell growth inhibitor that targets theSF3B1subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B inducesapoptosis[1][2][3]. |
体外研究
(In Vitro) | Pladienolide B (0.1-2 nM; 24-72 hours) inhibits human cervical carcinoma cells viability[3].
Pladienolide B (0.1-2 nM; 24-48 hours) reduces SF3b1 expression in human cervical carcinoma cells[3].
Pladienolide B induces (0.1-2 nM; 24 hours) cell cycle arrest and apoptosis[3].
Cell Viability Assay[3] | Cell Line: | HeLa cells | | Concentration: | 0.1, 0.5, 1, 1.5, 2 nM | | Incubation Time: | 24, 48, 72 hours | | Result: | Significantly decreased cell viability, and the decrease was concentration- and time-dependent. |
Apoptosis Analysis[3] | Cell Line: | HeLa cells | | Concentration: | 0.1, 0.5, and 2 nM | | Incubation Time: | 24 hours | | Result: | The apoptotic cells were highly induced at 24 hours. |
RT-PCR[3] | Cell Line: | HeLa cells | | Concentration: | 0.1, 0.5, and 2 nM | | Incubation Time: | 24, 48 hours | | Result: | Induced a time- and concentration-dependent decrease in cellular SF3b1 proteins. |
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体内研究
(In Vivo) | Pladienolide B (2.5-10 mg/kg; i.v.; daily for 5 days) has strong antitumor activities[4].
| Animal Model: | Female or male BALB/c nu/nu mice (7 weeks of age) (PC-3, OVCAR-3, DU-145, WiDr, and HCT-116, BSY-1 xenografts)[4] | | Dosage: | 2.5, 5, and 10 mg/kg | | Administration: | I.v.; daily for 5 days | | Result: | Showed strong growth inhibitory or regressive activities against these xenografts. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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