Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是一种长效的酰胺类局部麻醉剂。Levobupivacaine hydrochloride 通过可逆性阻断神经元钠通道 (sodium channel) 发挥麻醉镇痛作用。Levobupivacaine hydrochloride 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 hydrochloride 在体内由细胞色素P450 (CYP450) 代谢。Levobupivacaine hydrochloride 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 hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronalsodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepaticcytochrome P450(CYP450) enzymesin vivo. Levobupivacaine hydrochloride can also induceferroptosisby miR-489-3p/SLC7A11 signaling in gastriccancer[1][2][3]. |
| IC50& Target | Sodium channels, Ferroptosis[1] |
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 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(307.80 mM;Need ultrasonic) H2O : ≥ 50 mg/mL(153.90 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.0780 mL | 15.3898 mL | 30.7796 mL | | 5 mM | 0.6156 mL | 3.0780 mL | 6.1559 mL | | 10 mM | 0.3078 mL | 1.5390 mL | 3.0780 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 (sealed storage, away from moisture)。-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: ≥ 3 mg/mL (9.23 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (9.23 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (9.23 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (9.23 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 30.0 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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