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New application of ligustrazine stilbene derivative

A technology of ligustrazine stilbene derivatives, which is applied in the field of new applications of ligustrazine stilbene derivatives, and can solve the problems of short half-life, low occurrence rate, and low bioavailability

Inactive Publication Date: 2017-06-30
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ligustrazine has few toxic and side effects, mild degree, and low incidence. Adverse reactions are rare in decades of clinical application. In view of the shortcomings of Ligustrazine, such as short half-life, fast metabolism, and low bioavailability, Ligustrazine derivatives (antihypertensive drugs) with high efficiency and low toxicity have been developed, and Ligustrazine derivatives have been studied in depth. , to provide a theoretical basis for the prevention and treatment of clinical hypertension and the further development and utilization of ligustrazine

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 1. Establishment of arterial ring model

[0032] Using the Powerlab 8-channel tissue-organ bath system at the isolated tissue level, three positive drugs, norepinephrine (NE), acetylcholine (Ach), and sodium nitroprusside (SNP), were used to establish contraction of isolated rat thoracic aortic rings and diastolic response model, to determine the optimal concentration of norepinephrine (NE) to induce vascular ring contraction and the concentration of acetylcholine (Ach) to test the integrity of vascular endothelium.

[0033] experimental method:

[0034] 1. Preparation of Intact Endothelial Artery Rings

[0035] ① After weighing SD male rats, inject 10% chloral hydrate intraperitoneally at 0.4mL / 100g to anesthetize the rats;

[0036] ②Carefully open the chest cavity, open the heart and lungs, carefully remove the thoracic aorta, and quickly place it in 95% O 2 +

[0037] 5%CO 2 In the 4℃ pre-cooled K-H solution saturated with mixed standard gas;

[0038] ③ After r...

Embodiment 2

[0047] Screening of Vasoactive Activity of Tetramethylpyrazine and Stilbene Derivatives

[0048] Select the endothelial complete vascular ring, 10 -6 When mol / L NE is pre-shrunk to the maximum tension, give

[0049] 3×10 -5 mol / L ligustrazine stilbene derivatives, record the tension change curves of different drugs in different vascular rings, the results show that: through screening of vasoactivity, most of ligustrazine stilbene derivatives have no significant vasoactivity, 63 kinds of ligustrazine stilbene There are 17 kinds of vasodilation activity among the derivatives of C124444 that are relatively obvious (relaxation rate > 20%), and the most suitable monomer for vasodilation becomes C 26b , accumulatively given a concentration of 10 -6 mol / L~10 -4 mol / L, C 26b No obvious dose-dependent relaxation, the optimal concentration is 3×10 -5 mol / L, the relaxation rate is 44.97%, such as figure 2 , image 3 shown.

Embodiment 3

[0051] C 26b Calcium Channel Mechanism of Vasodilation

[0052] 1. Obtain an endothelial-free vascular ring according to the method in Example 1, and set aside.

[0053] 2.C 26b Relaxation of vascular rings preconstricted by norepinephrine / potassium chloride (NE / KCl)

[0054] Take the non-endothelial vascular ring, respectively with 10 -6 mol / L / 60mmol / L NE / KCl was pre-contracted, and after reaching the maximum contraction, 3×10 -5 mol / L C 26b , record the tension change curve of the vascular ring within 20 minutes, see Figure 4 .

[0055] 3.C 26b Effects on high potassium-induced extracellular calcium influx in smooth muscle cells

[0056] Select an endothelial-free vascular ring, wash it twice with calcium-free K-H solution, and then use 3×10 -5 mol / L C 26b Treat the vascular ring in calcium-free high potassium 60mmol / L K-H solution for 20min, and give CaCl sequentially 2 Reach (0.5, 1.0, 1.5, 2.0, 2.5) mmol / L, different concentrations of CaCl 2 The degree of con...

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Abstract

The invention relates to a ligustrazine stilbene derivative. The vascular activity of 63 new ligustrazine stilbene derivatives is screened, and a vascular ring separation perfusion method is used for researching the pharmacology mechanism for vessel dilatation, so that the vessel dilatation activity of C26b has notable endothelial dependence, and is mediated by an eNOS way. The vessel dilatation mediated by smooth muscle is mainly relevant to external calcium influx, calcium-activated potassium channels (KCa), and inward rectification type potassium channels (KIR) caused by restraining VDCC opening, and at the later stage, the ligustrazine stilbene derivative can be used for preparing drugs for vessel dilatation.

Description

technical field [0001] The present invention relates to a new application of compounds, especially a new application of ligustrazine stilbene derivatives. Background technique [0002] Hypertension is one of the common diseases that threaten human health, manifested as elevated systemic arterial systolic pressure. It is also a risk factor for many other diseases. If it is not treated in time, it can damage the kidneys, heart and other organs. The first step in the treatment of hypertension is to control blood pressure to prevent cardiovascular diseases and complications. Although antihypertensive drugs emerge in endlessly, how to find ideal antihypertensive drugs and methods with good curative effect, small adverse reactions and high safety is still a arduous task before us. [0003] Chuanxiong is the rhizome of Ligusttcum chuanxiong Hort. It is mainly produced in Sichuan, Guizhou, and Yunnan, and those produced in Sichuan are the best. Department of artificial cultivati...

Claims

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Application Information

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IPC IPC(8): A61K31/4965A61P9/08A61P9/12
CPCA61K31/4965
Inventor 朱彦苏桂发潘成学张思明焦艳晓王晓明
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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