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抑二肽素A

抑二肽素A用途

Diprotin A (Ile-Pro-Ile) 是二肽基肽酶 IV (DPP-IV) 的抑制剂。

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抑二肽素A名称

[ CAS 号 ]:
90614-48-5

[ 中文名 ]:
抑二肽素A

[ 英文名 ]:
Diprotin A

[英文别名 ]:

MFCD00038707
H-ILE-PRO-ILE-OH
ILE-PRO-ILE H2O
Ile-Pro-Ile-OH
H-ILE-PRO-ILE-OH H2O
DIPEPTIDYLPEPTIDASE IV INHIBITOR I
L-Isoleucyl-L-prolyl-L-isoleucine
ILE-PRO-ILE
L-Ile-L-Pro-L-Ile-OH

抑二肽素A生物活性

[ 描述 ]:

Diprotin A (Ile-Pro-Ile) 是二肽基肽酶 IV (DPP-IV) 的抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 二肽基肽酶

研究领域 >> 代谢疾病

[ 靶点 ]

IC50: DPP-IV[1]

[体外研究]

在正常氧和H/R条件下,二质子蛋白A(100μM；CXCR4阻断剂或Src抑制剂治疗后30分钟)诱导人内皮细胞HEC中Src[Tyr 416]和VE钙粘蛋白[Tyr731]的磷酸化,并扰乱内皮细胞与细胞的连接,它们被CXCR4(SDF-1α受体)阻断剂或Src抑制剂减弱[1]。Western Blot分析[1]细胞系：人内皮细胞[1]浓度：100μM孵育时间：CXCR4阻断剂或Src抑制剂处理后30分钟。结果：诱导hECs中Src[Tyr 416]和VE-钙粘蛋白[Tyr731]磷酸化。

[体内研究]

diprotina(腹腔注射,70μg/kg,每日2次,7天)可增加Src和VE-cadherin的磷酸化,加重视网膜血管渗漏。总的来说,diprotina通过增加SDF-1α/CXCR4/Src/VE钙粘蛋白信号通路来诱导血管渗漏[1]。动物模型：链脲佐菌素诱导野生型C57/BL6小鼠糖尿病视网膜病变模型[1]剂量：70μg/kg腹腔注射,每日2次,7天。结果：通过增强SDF-1α/CXCR4/Src/VE钙黏蛋白信号通路,诱导血管渗漏。

[参考文献]

[1]. Lee CS, et al. Dipeptidyl Peptidase-4 Inhibitor Increases Vascular Leakage in Retina through VE-cadherin Phosphorylation. Sci Rep. 2016 Jul 6;6:29393.

抑二肽素A物理化学性质

[ 密度 ]:
1.14 g/cm3

[ 沸点 ]:
583.1ºC at 760 mmHg

[ 分子式 ]:
C₁₇H₃₁N₃O₄

[ 分子量 ]:
341.44600

[ 闪点 ]:
306.5ºC

[ 精确质量 ]:
341.23100

[ PSA ]:
112.73000

[ LogP ]:
1.99540

[ 外观性状 ]:
白色粉末

[ 折射率 ]:
1.517

[ 储存条件 ]:
−20°C

抑二肽素A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NR4737000

CHEMICAL NAME :: L-Isoleucine, N-(1-L-isoleucyl-L-prolyl)-

CAS REGISTRY NUMBER :: 90614-48-5

LAST UPDATED :: 199212

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C17-H31-N3-O4

MOLECULAR WEIGHT :: 341.51

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >250 mg/kg

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

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 37,422,1984

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抑二肽素A安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
NR4737000

抑二肽素A文献

In vitro assessment of the multifunctional bioactive potential of Alaska pollock skin collagen following simulated gastrointestinal digestion.

J. Sci. Food Agric. 95(7) , 1514-20, (2015)

Dietary mineral deficiency, hypertension and diabetes have become serious human health problems. Dietary approaches are increasingly being investigated to address these issues. Identification of food-...

Antidiabetic property of Symplocos cochinchinensis is mediated by inhibition of alpha glucosidase and enhanced insulin sensitivity.

PLoS ONE 9(9) , e105829, (2014)

The study is designed to find out the biochemical basis of antidiabetic property of Symplocos cochinchinensis (SC), the main ingredient of 'Nisakathakadi' an Ayurvedic decoction for diabetes. Since di...

Utilisation of the isobole methodology to study dietary peptide-drug and peptide-peptide interactive effects on dipeptidyl peptidase IV (DPP-IV) inhibition.

Food Funct. 6(1) , 313-20, (2015)

Inhibition of dipeptidyl peptidase-IV (DPP-IV) is used as a means to regulate post-prandial serum glucose in type 2 diabetics. The effect of drug (Sitagliptin®)/peptide and binary peptide mixtures on ...

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