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Compound for activating AMPK and application thereof

A compound and drug technology, applied in the field of adenine, can solve problems such as abnormal cell growth, and achieve the effect of preventing scar tissue formation

Active Publication Date: 2015-04-15
ENERGENESIS BIOMEDICAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Dysregulation of cellular signaling pathways may lead to abnormal cell growth and ultimately cancer

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] AMPK Activity Assay

[0048] In mouse muscle cell C2C12, mouse fibroblast 3T3, human liver cancer cell Hep G2, human breast cancer cell MCF7 and human colon cancer cell HT29, human umbilical vein endothelial cell HUVEC, human acute mononuclear leukocyte cell line THP1, human macrophage Cell U937, mouse microglial cell BV-2, neuroblastoma cell Neuro2A and pilomastoid cell Dermal Papilla were used to analyze the effect of adenine on AMPK phosphorylation. Cells were incubated in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal bovine serum (FBS), 4mM L-glutamine, 2 mM sodium pyruvate and 1% penicillin / streptomycin (Invitrogen GibcoBRL, Carlsbad, CA, USA) at 37 °C, 5 %CO 2 cultivated in the environment. 3×10 5 Cells were seeded in 6-well dishes, and after 24 hours, cells were treated with the indicated compounds for 30 minutes, and then cells were lysed and analyzed by western blotting. Equal amounts of proteins were separated by sodium dodecyl sulfate p...

Embodiment 2

[0053] Glucose Uptake - In Vitro Assay

[0054]The effect of adenine on glucose uptake was analyzed in muscle cells C2C12 using a fluorescent glucose analogue (2-NBDG, Molecular Probes). After C2C12 cells were treated with various concentrations of adenine at 37°C for 30 minutes, 500 μM fluorescent glucose analogs were added, and after incubation at room temperature for 5 minutes, the cells were washed three times with Kreb-Hepes buffer solution and fixed with 70% ethanol. Fluorescence of intracellular glucose analogs was detected with a fluorometer.

[0055] The effect of adenine on glucose uptake is summarized in Table 2. Adenine significantly promoted glucose uptake in C2C12 cells in a concentration-dependent manner. Data are expressed as mean ± standard deviation of three independent experiments.

[0056] Table 2)

[0057] Reagent Concentration (microM) Glucose uptake (% to control) Adenine 1 117±8.1 10 261±13.4 100 315±11.9 ...

Embodiment 3

[0059] Antidiabetic effect of adenine

[0060] In order to further evaluate the effect of adenine on the regulation of plasma glucose level, mice were fed with high-fat diet as an animal model of type 2 diabetes. C57BL / 6J mice were housed at 22°C on a 12-h day / night cycle and fed either a high-fat chow (60% kcal% fat) or normal chow without restriction. 0.1-50 mg / kg adenine was given to 24-week-old mice by intraperitoneal injection, and blood glucose was measured 1 and 3 hours after injection. The mice were fed intraperitoneally with high-fat feed twice a day for 6 days. One hour after the last administration, the plasma was collected and the plasma glucose and triglyceride levels were measured.

[0061] Compared with high-fat diet-fed mice injected with normal saline, adenine was found to reduce plasma glucose by more than 30%, lower triglyceride by more than 35%, and reduce body weight by more than 15%.

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Abstract

The invention discloses a compound for activating AMPK. The compound is adenine and / or pharmaceutically-acceptable salts thereof. The invention further discloses the application of the compound. The compound is used to activate AMPK (AMP-kinase) and prevent / treat physiological discomfort or diseases. Thus the compound can be applied to prevention and treatment on physiological discomfort or diseases that can be relieved by AMPK for mammals.

Description

technical field [0001] The present invention relates to adenine, this compound is suitable for the activation of AMPK (AMP-activated protein kinase), and the use of this compound for the prevention or treatment of physiological conditions or diseases. Background technique [0002] AMPK is clearly a sensor of cellular energy and a responder to energy needs. AMPK is a heteroternary body composed of catalytic α subunits, regulatory β and γ subunits, and all subunits are highly retained in eukaryotes. AMPK is activated by its upstream kinases such as LKB1, calcium ion / calcitonin-dependent protein phosphokinase (Ca 2+ / Calmodulin dependent kinase) and the 172th threonine residue in phosphorylated α-subunit of TAK1, the high AMP / ATP ratio caused by physiological or pathological stress also activates AMPK. AMPK activation promotes catabolic pathways and inhibits anabolism, thereby restoring cellular energy balance by reducing ATP consumption and promoting ATP production. [0003...

Claims

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Application Information

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IPC IPC(8): A61K31/52A61P29/00A61P3/10A61P3/00A61P5/48A61P25/28A61P17/02A61P39/06A61P35/00A61P3/04A61P9/00A61P25/14A61P25/16C07D473/34
CPCA61K31/52
Inventor 邱壬乙陈翰民郭正宜林俊材黄纯芳
Owner ENERGENESIS BIOMEDICAL
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