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蜂毒明肽

蜂毒明肽用途

Apamin 是一种在蜂毒中发现的18个氨基酸的肽神经毒素,可阻断Ca 2+激活的K+通道,且预防肝纤维化。

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蜂毒明肽名称

[ CAS 号 ]:
24345-16-2

[ 中文名 ]:
蜂针液明肽

[ 英文名 ]:
Apamin

[中文别名 ]:

蜂毒明肽

[英文别名 ]:

apamine
MFCD00167944
Apamin
APAMIN,BEE VENOM
APAMIN FROM BEE VENOM
CNCKAPETALCARRCQQH-NH2
M.W. 2027.34 C79H131N31O24S4
APAMIN FROM HONEY BEE VENOM
EINECS 246-182-7

蜂毒明肽生物活性

[ 描述 ]:

Apamin 是一种在蜂毒中发现的18个氨基酸的肽神经毒素,可阻断Ca 2+激活的K+通道,且预防肝纤维化。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

多肽产品

研究领域 >> 神经疾病

天然产物 >> 其他

[ 靶点 ]

K+ channel[1]

[体外研究]

Apamin是在apitoxin(蜂毒)中发现的18个氨基酸的肽神经毒素。长期以来,它一直被认为是Ca2 +激活的K +(SK)通道的特异性选择性阻断剂。通过苏木精和伊红染色测定,Apamin抑制3,5-二乙氧基羰基-1,4-二氢可乐定(DDC)诱导的小鼠模型中的肝纤维化。与DDC喂养组中的表达水平相比,Apamin治疗减弱炎性细胞因子表达,包括IL-6,IFN-γ,TNF-α和IL-1β[1]。 Apamin是在apitoxin(蜂毒)中发现的18个氨基酸的肽神经毒素。 Apamin是一种从蜂毒中提取的神经毒素,特异性结合特定类别的Ca2 +激活的K +通道,这些通道参与了许多可兴奋细胞中动作电位之后的慢性后超极化(S-AHP)[2]。

[体内研究]

为了研究Apamin对DDC喂养小鼠ECM沉积的抗纤维化作用,DDC诱导的肝纤维化通过诱导纤维化基因,FSP-1,α-平滑肌肌动蛋白(α-SMA)和I型胶原蛋白表达来证实。。在DDC喂养组中,α-SMA的表达在增生的胆管周围的肌成纤维细胞和HSC中强烈表达,并且在Apamin处理中明显表达。此外,DDC喂养组中的胶原蛋白I的表达显着增加,尤其是在门静脉[1]中。

[细胞实验]

HSC-T6细胞，一种永生化的大鼠肝星状细胞系，具有稳定的表型和生化特征。将细胞在37℃下在潮湿的培养箱中在5％CO 2气氛下培养。将HSC-T6细胞接种于完全培养基中24小时。将细胞更换为含有指定浓度的Apamin（0.5,1和2μg/ mL）的新鲜无血清培养基。 24小时后，用含有2ng / mL TGF-β1的新鲜无血清培养基替换细胞24小时[1]。

[动物实验]

小鼠[1]为了诱导肝损伤，选择8周龄的C57BL / 6雄性小鼠（20-25g）。给雄性C57BL / 6小鼠喂食对照饮食或DDC补充饮食（0.1％）4周以诱导晚期胆汁纤维化。小鼠每周两次腹膜内注射溶解在盐水中的Apamin（0.1mg / kg）。从第一次DDC饮食给药4周后处死小鼠。

[参考文献]

[1]. Kim JY, et al. Apamin suppresses biliary fibrosis and activation of hepatic stellate cells. Int J Mol Med. 2017 May;39(5):1188-1194.

[2]. Messier C, et al. Effect of apamin, a toxin that inhibits Ca(2+)-dependent K+ channels, on learning and memory processes. Brain Res. 1991 Jun 14;551(1-2):322-6.

[相关活性小分子]

蜂毒明肽物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 分子式 ]:
C₇₉H₁₃₁N₃₁O₂₄S₄

[ 分子量 ]:
2027.339

[ 精确质量 ]:
2025.886597

[ PSA ]:
1021.52000

[ LogP ]:
-14.24

[ 折射率 ]:
1.724

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放

蜂毒明肽MSDS

详细MSDS(安全技术说明书)

蜂毒明肽毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CD6899900

CHEMICAL NAME :: Apamin

CAS REGISTRY NUMBER :: 24345-16-2

LAST UPDATED :: 198708

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C79-H131-N31-O24-S4

MOLECULAR WEIGHT :: 2027.65

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3800 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TOXIA6 Toxicon. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.1- 1962- Volume(issue)/page/year: 22,308,1984

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2900 ug/kg

TOXIC EFFECTS :: Behavioral - ataxia

REFERENCE :: EJBCAI European Journal of Biochemistry. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1967- Volume(issue)/page/year: 56,35,1975

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Behavioral - changes in motor activity (specific assay)

REFERENCE :: NSAPCC Naunyn-Schmiedeberg's Archives of Pharmacology. (Springer Verlag, Heidelberger, Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.272- 1972- Volume(issue)/page/year: 300,189,1977

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intracerebral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1800 ng/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TOXIA6 Toxicon. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.1- 1962- Volume(issue)/page/year: 22,308,1984

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TOXIA6 Toxicon. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.1- 1962- Volume(issue)/page/year: 20,157,1982

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蜂毒明肽安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H334

[ 警示性声明 ]:
P261-P342 + P311

[ 危害码 (欧洲) ]:
Xn

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ RTECS号 ]:
CD6899900

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

蜂毒明肽文献

Type 2 diabetes: increased expression and contribution of IKCa channels to vasodilation in small mesenteric arteries of ZDF rats.

Am. J. Physiol. Heart Circ. Physiol. 307(8) , H1093-102, (2014)

Impaired endothelial function, which is dysregulated in diabetes, also precedes hypertension. We hypothesized that in Type 2 diabetes, the impaired endothelium-dependent relaxation is due to a loss of...

The effect of hyperpolarization-activated cyclic nucleotide-gated ion channel inhibitors on the vagal control of guinea pig airway smooth muscle tone.

Br. J. Pharmacol. 171(15) , 3633-50, (2014)

Subtypes of the hyperpolarization-activated cyclic nucleotide-gated (HCN) family of cation channels are widely expressed on nerves and smooth muscle cells in many organ systems, where they serve to re...

The GPR55 agonist lysophosphatidylinositol relaxes rat mesenteric resistance artery and induces Ca(2+) release in rat mesenteric artery endothelial cells.

Br. J. Pharmacol. 172 , 3043-57, (2015)

Lysophosphatidylinositol (LPI), a lipid signalling molecule, activates GPR55 and elevates intracellular Ca(2+). Here, we examine the actions of LPI in the rat resistance mesenteric artery and Ca(2+) r...

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