产品
编 号:F435369
分子式:C45H53NO14
分子量:831.9
产品类型
结构图
CAS No: 71610-00-9
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产品详情
生物活性:
Cephalomannine is a Paclitaxel (HY-B0015) alkaloidal analog that can be isolated from most Cephalotaxus species. Cephalomannine is an orally active anti-tumor agent and can be used as a chemotherapy agent for cancer research.
体内研究:
Cephalomannine (0.4 mg/kg,腹腔注射,10天)在裸鼠异种移植瘤模型中能显著抑制肺癌细胞的生长,未见明显副作用。Cephalomannine 能通过与 APEX1 的竞争性结合而中断 APEX1 与 HIF-1α 的相互作用。Animal Model:BALB/C nude mice xenograft model
Dosage:0.4 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Reduced the volume and weight of H460 xenograft tumors.
Animal Model:BALB/c nude mice bone metastasis xenograft model
Dosage:10 mg/kg, 20 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Decreased bone destruction, reduced bioluminescence intensity and number of bone metastases, significantly extended time to endpoint events, decreased UBE2S expression and number of osteoclasts, and did not produce significant toxicity to the heart, liver, or kidney of nude mice.
体外研究:
Cephalomannine 在常氧条件下对 H460, A549 和 H1299 细胞的增殖都具有显著的抑制作用,IC50 值分别为 0.18, 0.20 和 0.37 μM。Cephalomannine 还能显著抑制缺氧条件下的细胞活力。Cephalomannine (0, 0.025, 0.05, 0.1 μM; 0, 12, 24h) 通过抑制 APEX1/HIF-1α 的相互作用,能够显著抑制缺氧肺癌细胞的细胞活力,ROS 生成,细胞内 pH,迁移以及缺氧下人脐静脉内皮细胞 HUVECs 的血管生成。Cephalomannine 可以剂量依赖性地抑制 UBE2S 的表达,从而抑制前列腺癌 (PCa) 的生长和转移。