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Application of N6-(2-hydroxyethyl) adenosine in medicine for treating hypertension

A kind of hydroxyethyl, high blood pressure technology, applied in the application field of N6-adenosine

Pending Publication Date: 2019-06-28
ZHEJIANG SUB TROPICS CROP INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the antihypertensive mechanism and transport mechanism of HEA have not been reported yet.

Method used

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  • Application of N6-(2-hydroxyethyl) adenosine in medicine for treating hypertension
  • Application of N6-(2-hydroxyethyl) adenosine in medicine for treating hypertension
  • Application of N6-(2-hydroxyethyl) adenosine in medicine for treating hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1N6-(2-hydroxyethyl) adenosine (HEA) etc. obtain

[0032]N6-(2-Hydroxyethyl)adenosine (HEA) is an adenosine derivative extracted from Cordyceps mycelium. It is a calcium antagonist (calciumAntagonists, CCB) of biological origin and can also be synthesized artificially.

[0033] The molecular structural formula of N6-(2-hydroxyethyl)adenosine (HEA) is as follows:

[0034]

[0035] The laboratory planted artificial Cordyceps mycelium and used wheat as the medium to greatly reduce the content of heavy metals. The cicada was dried and crushed into 200 mesh particles. The extraction and separation of HEA: using 15%-75% ethanol as the solvent , the ratio of solvent to mycelia is 10mL / g, and the ethanol extract is obtained at a temperature of 50°C–100°C; the ethanol extract is intercepted by an ultrafiltration membrane to obtain a concentrate; the membrane concentrate is purified by AB-8 macroporous resin , after eluting the impurities, collect 15% and 30% ethan...

Embodiment 2

[0039] Example 2: The antihypertensive effect of N6-(2-hydroxyethyl)adenosine (HEA) on SD rats in hypertensive model.

[0040] Materials and Reagents:

[0041] Experimental animals: 20 male SD rats, 9 weeks old, weighing 200 ± 10g, purchased from the Animal Experiment Center of Wenzhou Medical University, animal quality certificate number: SCXK (Zhejiang) 2017-149, animals were raised in an independent animal room, room temperature 20-25°C, alternating light and dark light for 12 hours, relative humidity 50%, free access to food, water and feed, and adaptive feeding for one week.

[0042] Drugs and instruments: SoftronBP 2010 non-invasive blood pressure measuring instrument was purchased from Beijing Ruanlong Biotechnology Co., Ltd.; selective A1R antagonist DPCPX was purchased from Sigma Company; NO synthase inhibitor NG-nitro-L-arginine methyl ester (NG -Nitro-L-arginine methyl ester hydrochloride, L-NAME) was purchased from Sigma Company, and the required concentration was...

Embodiment 4

[0073] Example 4 Binding site of HEA-HSA system

[0074] According to the Scatchard equation, the binding constant (KA) and the number of binding sites (n) during the binding process were determined (Gao et al. 2004).

[0075]

[0076] In the formula, F0 is the fluorescence intensity of HSA, F is the fluorescence intensity of HEA-HSA complex, and [Q] is the concentration of HEA.

[0077] Measurement of fluorescence spectrum: Measure the fluorescence emission spectrum on a Thermo Scientific Lumina type fluorescence spectrometer, the excitation wavelength is 280nm, and the scanning range of the emission wavelength is 285nm to 500nm. A 3.5 mL solution of 3.0 μmol / L HSA was titrated by adding HEA. The excitation and emission slit widths are 2.5nm, the scanning speed is 600nm / min, the response time is 1.0s, the integration time is 20ms, and the photomultiplier tube voltage is 500V. Samples were tested at 298K and 308K.

[0078] Such as Figure 6 As shown, c(HSA)=3.0μmol / L, c...

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Abstract

The invention relates to an application of N6-(2-hydroxyethyl) adenosine in medicine for treating hypertension, the N6-(2-hydroxyethyl) adenosine reduces systolic and diastolic blood pressure throughan adenosine al receptor, which can be inhibited by an A1R antagonist DPCPX. The N6-(2-hydroxyethyl) adenosine can reduce the content of inflammatory factors (TNF-alpha and IL-6) and urea nitrogen / creatinine ratio (P (0.01) in serum of a mouse with high blood pressure. WB experiments show that HEA can up-regulate eNOS in mouse cardiomyocytes and down-regulate the expression of Erk1 / 2 protein, namely, the N6-(2-hydroxyethyl) adenosine acts on an MAPK pathway through negative regulation of inflammatory factors to achieve the aim of reducing blood pressure. The research result provides importantevidence for the application of the extract of the cordyceps cicadae in anti-inflammatory, kidney-protecting and blood pressure-lowering medicines, and has important significance for further expandingthe medicinal value of the traditional Chinese medicine cordyceps cicadae.

Description

technical field [0001] The invention relates to the application of N6-(2-hydroxyethyl)adenosine, in particular to the application of N6-(2-hydroxyethyl)adenosine in the medicine for treating hypertension. Background technique [0002] N6-(2-hydroxyethyl)adenosine (N6-(2-hydroxyethyl)adenosine, HEA) is an adenosine derivative extracted from the mycelium of Cordyceps cicadae, which has bactericidal, anticancer and anticonvulsant properties. effect. HEA is the first biological source of calcium antagonists (calcium Antagonists, CCB), but also adenosine A1 receptor agonist, using DPCPX (an adenosine A1 receptor antagonist) can prove that HEA acts on adenosine A1 receptor. The content of HEA is an important index to measure the quality of Cordyceps, and the unique medicinal value of Cordyceps cicadae promotes the continuous development of its pharmacological research. HEA can down-regulate the expressions of interleukin-1β, cell adhesion molecule-1 and tumor cell necrosis fact...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7076A61P9/12A61P13/12
Inventor 柴一秋张孟丽
Owner ZHEJIANG SUB TROPICS CROP INST
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