24345-16-2
基本信息
蜂針液明肽
APAMIN毒素肽
毒素多肽APAMIN
蜂毒明肽 (蜂針液明肽)
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)
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見(jiàn)問(wèn)題列表
蜂毒明肽是在蜂毒素中發(fā)現(xiàn)的一種 18 個(gè)氨基酸的肽類神經(jīng)毒素,是一種 Ca2+ 激活的 K+ (SK) 通道的特異性和選擇性的阻斷劑,具有抗炎和抗纖維化的作用。
(1)對(duì)神經(jīng)系統(tǒng)作用:能阻斷支配胃腸道平滑肌神經(jīng)的抑制性沖動(dòng)的傳導(dǎo),使胃腸平滑肌興奮性增強(qiáng),而呈收縮狀態(tài);可作用于脊髓的中間 神經(jīng)元、下行的網(wǎng)狀脊髓束和前庭脊髓束,或大腦導(dǎo)水管周?chē)闹醒牖? 質(zhì),影響動(dòng)作的有機(jī)協(xié)同。 (2) 強(qiáng)心、抗心律失常作用:具有很強(qiáng)的p-腎上腺素樣作用,擴(kuò)冠, 增加心肌供血,使心肌收縮力明顯增強(qiáng),心率加快,心臟泵血功能增強(qiáng), 可用于治療心衰;具有異丙腎上腺素樣作用,且比異丙腎上腺素維持時(shí)間 長(zhǎng)(約10倍),抗心律失常。(3) 增加毛細(xì)血管的通透性,改善微循環(huán)。 (4) 抗炎、調(diào)整免疫:直接升高血漿皮質(zhì)醇或刺激垂體-腎上腺系統(tǒng) 促進(jìn)皮質(zhì)激素的分泌;抑制5-羥色胺活性。(5) 營(yíng)養(yǎng)修復(fù)肌營(yíng)養(yǎng)不良細(xì)胞:強(qiáng)直肌肉中有蜂毒明肽受體,蜂毒明肽通過(guò)與其受體結(jié)合而發(fā)揮營(yíng)養(yǎng)肌細(xì)胞達(dá)到治療的作用??捎糜谥委煆?qiáng)直性脊柱炎、多發(fā)性硬化癥。
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. |