Levobupivacaine ((S)-(-)-Bupivacaine) 是一种长效的酰胺类局部麻醉剂。Levobupivacaine 通过可逆性阻断神经元钠通道 (sodium channel) 发挥麻醉镇痛作用。Levobupivacaine 可抑制心血管等组织的传递和传导冲动，具有一定的心脏和中枢神经毒性。Levobupivacaine 在体内由细胞色素P450 (CYP450) 代谢。Levobupivacaine 也可通过 miR-489-3p/SLC7A11 信号通路诱导胃癌铁死亡 (ferroptosis)。
| 生物活性 | Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronalsodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepaticcytochrome P450(CYP450) enzymesin vivo. Levobupivacaine can also induceferroptosisby miR-489-3p/SLC7A11 signaling in gastriccancer[1][2][3]. |
| IC50& Target | Sodium channels, Ferroptosis[1][2] |
体外研究
(In Vitro) | Levobupivacaine (0-4 mM; 24 h) does not affect the viability of GES-1 cells but inhibits the viability of HGC27 and SGC7901 cells[2].
Levobupivacaine (2 mM; 24, 48 or 72 h) enhances Erastin-induced inhibitory impact on HGC27 and SGC7901 cell viabilities; induces the levels of Fe2+, iron, and lipid ROS[2].
Levobupivacaine (2 mM; 24 h) enhances the expression of miR-489-3p in HGC27 and SGC7901 cells, increases the levels of Fe2+and iron[2].
Cell Viability Assay[2] | Cell Line: | GES-1, HGC27 and SGC790 | | Concentration: | 0, 0.5, 1, 2 and 4 mM | | Incubation Time: | 24 h | | Result: | Did not affect the viability of normal gastric epithelial GES-1 cell lines but inhibited the viability of HGC27 and SGC7901 cells in a dose-dependent manner. |
Cell Viability Assay[2] | Cell Line: | HGC27 and SGC7901 (incubated with 5 μM erastin) | | Concentration: | 2 mM | | Incubation Time: | 24, 48 or 72 h | | Result: | Enhanced erastin-induced inhibitory impact on HGC27 and SGC7901 cell viabilities; induced the levels of Fe2+, iron, and lipid ROS. |
RT-PCR[2] | Cell Line: | HGC27 and SGC7901 (incubated with 5 μM erastin) | | Concentration: | 2 mM | | Incubation Time: | 24 h | | Result: | Enhanced the expression of miR-489-3p in HGC27 and SGC7901 cells, increased the levels of Fe2+and iron. |
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体内研究
(In Vivo) | Levobupivacaine (40 μmol/kg; IP; once daily for 25 days) significantly inhibits SGC7901 cell growth, and enhances the lipid ROS accumulation[2].
Levobupivacaine (5 or 36 mg/kg; IP; single dosage) increases the latency to partial seizures and prevents the occurrence of generalized seizures at low dosage; reduces the latency to N-methyl-d-aspartate (NMDA)-induced seizures and increased seizure severity at high dosage[3].
| Animal Model: | CD1 mice (30-35 g; induced epileptic seizures by injecting with NMDA)[3] | | Dosage: | 5 or 36 mg/kg | | Administration: | IP; single dosage | | Result: | Increased the latency to partial seizures and prevented the occurrence of generalized seizures at 5 mg/kg; reduced the latency to NMDA-induced seizures and increased seizure severity at 36 mg/kg. |
| Animal Model: | SCID nude mice (6-8 weeks; subcutaneously injected with 5×106SGC7901 cells)[2] | | Dosage: | 40 μmol/kg | | Administration: | IP; once daily for 25 days | | Result: | Significantly inhibited SGC7901 cell growth, and enhanced the lipid ROS accumulation. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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