24345-16-2
24345-16-2 结构式
基本信息
蜂针液明肽
APAMIN毒素肽
毒素多肽APAMIN
蜂毒明肽 (蜂针液明肽)
蜂毒明肽, ≥97% (HPLC)
APAMIN
apamine
APAMIN, BEE VENOM
Apamin, ≥97% (HPLC)
APAMIN FROM BEE VENOM
CNCKAPETALCARRCQQH-NH2
APAMIN FROM HONEY BEE VENOM
Apamin (trifluoroacetate salt)
M.W. 2027.34 C79H131N31O24S4
APAMIN (HONEYBEE, APIS MELLIFERA)
物理化学性质
安全数据
常见问题列表
蜂毒明肽是在蜂毒素中发现的一种 18 个氨基酸的肽类神经毒素，是一种 Ca2+ 激活的 K+ (SK) 通道的特异性和选择性的阻断剂，具有抗炎和抗纤维化的作用。
(1)对神经系统作用：能阻断支配胃肠道平滑肌神经的抑制性冲动的传导，使胃肠平滑肌兴奋性增强，而呈收缩状态；可作用于脊髓的中间 神经元、下行的网状脊髓束和前庭脊髓束，或大脑导水管周围的中央灰 质，影响动作的有机协同。 (2) 强心、抗心律失常作用：具有很强的p-肾上腺素样作用，扩冠， 增加心肌供血，使心肌收缩力明显增强，心率加快，心脏泵血功能增强， 可用于治疗心衰；具有异丙肾上腺素样作用，且比异丙肾上腺素维持时间 长（约10倍），抗心律失常。(3) 增加毛细血管的通透性，改善微循环。 (4) 抗炎、调整免疫：直接升高血浆皮质醇或刺激垂体-肾上腺系统 促进皮质激素的分泌；抑制5-羟色胺活性。(5) 营养修复肌营养不良细胞：强直肌肉中有蜂毒明肽受体，蜂毒明肽通过与其受体结合而发挥营养肌细胞达到治疗的作用。可用于治疗强直性脊柱炎、多发性硬化症。
K + channel
Apamin (0.5-2 µg/mL; 24 hours; HSC-T6 cells) treatment markedly reduces the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Apamin treatment abrogats the activation of p-Smad2/3 and Smad4 induced by TGF-β1.
Western Blot Analysis
| Cell Line: | HSC-T6 cells |
| Concentration: | 0.5 µg/mL, 1 µg/mL and 2 µg/mL |
| Incubation Time: | 24 hours |
| Result: | Markedly reduced the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Abrogated the activation of p-Smad2/3 and Smad4 induced by TGF-β1. |
Apamin (0.1 mg/kg; intraperitoneal injection; twice a week; for 4 weeks; C57BL/6 male mice) treatment results in decreased liver injury and proinflammatory cytokine levels. Apamin suppresses the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC)-fed mice.
| Animal Model: | 8-week-old C57BL/6 male mice (20-25 g) with DDC feeding |
| Dosage: | 0.1 mg/kg |
| Administration: | Intraperitoneal injection; twice a week; for 4 weeks |
| Result: | Resulted in decreased liver injury and proinflammatory cytokine levels. Suppressed the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the DDC-fed mice. |