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蜂毒肽

蜂毒肽用途

Melittin 是一种PLA₂激活剂。

蜂毒肽名称

[ CAS 号 ]:
20449-79-0

[ 中文名 ]:
蜂毒肽

[ 英文名 ]:
Melittin

[英文别名 ]:

EINECS 253-417-7
Melittin
MFCD00076868

蜂毒肽生物活性

[ 描述 ]:

Melittin 是一种PLA2激活剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

研究领域 >> 炎症/免疫

多肽产品

研究领域 >> 癌症

[ 靶点 ]

PLA2[1]

[体外研究]

蜂毒肽是一种免疫相关的来自蜂毒的PLA2刺激肽,可增加高分子量酶的活性[1]。蜂毒肽是来自蜂毒的细胞毒性肽。蜂毒肽对A2780CR和A2780细胞均显示出毒性,IC50值分别为4.5和6.8μg/ mL。蜂毒肽具有天然抗菌,抗病毒和抗炎特性。它还被证明在几种不同的癌细胞系中具有多种抗癌作用,包括胃癌,乳腺癌,卵巢癌,肝癌,前列腺癌,宫颈癌和肺癌细胞系。 Melittin,一种两亲性溶血肽,发挥其潜在的抗癌作用的机制包括抑制细胞增殖,诱导细胞凋亡和直接坏死。蜂毒肽还可以通过抑制PI3K/Akt/mTOR信号通路来预防EGF诱导的细胞侵袭,但这主要与乳腺癌细胞有关[2]。

[细胞实验]

通过反相液相色谱法从蜂毒中纯化蜂毒肽，并在无菌水中重构以形成1mg / mL的储备溶液，然后在-20℃储存直至需要进行分析。通过Alamar Blue（AB）细胞活力试剂评估细胞活力。将A2780和A2780CR细胞以1×10 4个细胞/孔接种在96孔板中，并在37℃和5％CO 2下在潮湿气氛中孵育24小时。在该温育期后，在100μL培养基中用各种浓度的0.5％至14μg/ mL的蜂毒肽处理细胞，并在37℃和5％CO 2下再孵育24小时。 1％（v / v）的Triton X和细胞培养基分别用作阳性和阴性对照。此后，以10％（v / v）的终浓度加入AB，并将所得混合物在37℃和5％CO 2下再温育4小时。然后，在560nm的激发波长下读板，在SpectraMax M3酶标仪上记录590nm的发射。通过将它们表示为相对于平均阴性对照值的百分比，将背景校正的荧光读数转换为每个测试孔的细胞活力数据[2]。

[参考文献]

[1]. Steiner MR, et al. Responses of purified phospholipases A2 to phospholipase A2 activating protein (PLAP) and Melittin. Biochim Biophys Acta. 1993 Feb 10;1166(1):124-30.

[2]. Alonezi S, et al. Metabolomic Profiling of the Effects of Melittin on Cisplatin Resistant and Cisplatin Sensitive Ovarian Cancer Cells Using Mass Spectrometry and Biolog Microarray Technology. Metabolites. 2016 Oct 13;6(4). pii: E35.

[相关活性小分子]

蜂毒肽物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 分子式 ]:
C₁₃₁H₂₂₉N₃₉O₃₁

[ 分子量 ]:
2846.463

[ 精确质量 ]:
2844.754150

[ PSA ]:
1152.34000

[ LogP ]:
-1.32

[ 折射率 ]:
1.635

[ 储存条件 ]:
2~8°C

蜂毒肽MSDS

详细MSDS(安全技术说明书)

蜂毒肽毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OS3965000

CHEMICAL NAME :: Melittin (honeybee)

CAS REGISTRY NUMBER :: 20449-79-0

LAST UPDATED :: 199707

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C131-H229-N39-O31

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17700 ug/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 37,367,1974

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1400 ug/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 37,367,1974

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7400 ug/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 37,367,1974

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7040 ug/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 37,367,1974

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 2750 ug/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 37,367,1974

蜂毒肽安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301 + H311 + H331

[ 警示性声明 ]:
P261-P280-P301 + P310-P311

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R23/24/25

[ 安全声明 (欧洲) ]:
36-45-36/37/39

[ 危险品运输编码 ]:
UN 3462 6.1/PG 1

[ WGK德国 ]:
3

[ RTECS号 ]:
OS3965000

[ 海关编码 ]:
2934999090

蜂毒肽海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

蜂毒肽文献

The Ribosome-Sec61 Translocon Complex Forms a Cytosolically Restricted Environment for Early Polytopic Membrane Protein Folding.

J. Biol. Chem. 290 , 28944-52, (2015)

Transmembrane topology of polytopic membrane proteins (PMPs) is established in the endoplasmic reticulum (ER) by the ribosome Sec61-translocon complex (RTC) through iterative cycles of translocation i...

Preparation and functional characterization of human vascular endothelial growth factor-melittin fusion protein with analysis of the antitumor activity in vitro and in vivo.

Int. J. Oncol. 47 , 1160-8, (2015)

Vascular endothelial growth factor and its tyrosine kinase receptors have been identified as key mediators of the regulation of pathologic blood vessel growth and maintenance in the promotion of angio...

Cationic methacrylate polymers as topical antimicrobial agents against Staphylococcus aureus nasal colonization.

Biomacromolecules 15(8) , 2933-43, (2014)

The in vitro and in vivo antimicrobial activity of primary ammonium ethyl methacrylate homopolymers (AEMPs) was investigated. AEMPs with different degrees of polymerization (DP = 7.7-12) were prepared...

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蜂毒肽