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Application of structure modified products of salvianolic acid B in pharmacy

A technology of salvianolic acid and product, which is applied in the application field of the new compound, the structural modification product of salvianolic acid B in pharmaceuticals, can solve the problems of fast elimination, short half-life, difficulty, etc., to reduce the level of MDA and alleviate the disease. , Improve the effect of myocardial ischemia

Inactive Publication Date: 2010-01-20
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, animal experiments also show that after intravenous injection of salvianolic acid B in rats, it is distributed quickly in the body, the drug concentration in the kidney is the highest, it is difficult to pass through the blood-brain barrier, and it is eliminated quickly and has a short half-life.

Method used

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  • Application of structure modified products of salvianolic acid B in pharmacy
  • Application of structure modified products of salvianolic acid B in pharmacy
  • Application of structure modified products of salvianolic acid B in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Protective effect of dihydrosalvianolic acid B on myocardial ischemia caused by coronary artery ligation

[0044] 50 Wistar rats, half male and half female, weighing 220-250 g, were randomly divided into three groups: the first group was the ischemic model group, the second group was the salvianolic acid B group, and the third group was the dihydrosalvianolic acid B group. In the group, the administration dose was 50 mg / kg intravenously; the electrocardiogram II was measured before the operation and 30 minutes after the ligation, and the ST segment and T wave changes of the electrocardiogram were observed.

[0045] In addition to the ischemia model group, the other two groups were dosed once 30 minutes after coronary artery ligation, and again after 4 hours, and blood was collected from the abdominal vein 24 hours later to measure serum LDH, CK, MDA, and SOD; Remove the rat heart, wash the remaining blood with normal saline, blot dry with filter paper, weigh, ...

Embodiment 2

[0058] Example 2 Effect of dihydrosalvianolic acid B on thrombus formation in rats

[0059] 30 Wistar rats, half male and half female, weighing 180-220g, were randomly divided into three groups: the first group was the blank control group, the second group was the salvianolic acid B group, and the third group was the dihydrosalvianolic acid B group , the dose of administration was intravenous injection of 50mg / kg; the first group was intravenously injected with the same volume of distilled water, and the other two groups were administered again after 3.5 hours of administration, a total of two administrations; anesthesia was performed 2 hours after the last administration , rats were fixed in the supine position, the common carotid artery was separated, and placed on the stimulating electrode and temperature probe hook of the BT87-3 experimental in vivo thrombosis analyzer. The time (s) required from the start of stimulation to the sudden drop of arterial blood vessel temperat...

Embodiment 3

[0065] Example 3 The protective effect of ethyl salvianolic acid B on myocardial ischemia caused by coronary artery ligation

[0066] Wistar rats, half male and half female, weighing 180-240g, were randomly divided into two groups: the first group was the ischemia model group, the second group was the salvianolic acid B ethyl ester group, and the dosage was 100 mg / kg by intragastric administration; Measure the lead II electrocardiogram before the operation and 30 minutes after the ligation, and observe the ST segment and T wave changes of the electrocardiogram.

[0067] After 30 minutes of coronary artery ligation, the dose was administered once, and again after 4 hours. After 24 hours, the heart of the rat was removed, the residual blood was washed with normal saline, dried with filter paper, weighed, and frozen. The ventricle was evenly cut into 5 parts, placed in 1% TTC solution (triphenyltetrazolium chloride) and stained for 15 minutes (temperature 37°C±0.5°C); after takin...

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Abstract

The invention relates to novel application of structure modified products of salvianolic acid B in pharmacy. The structure modified products of the salvianolic acid B can obviously inhibit the rise of CK and LDH in blood serum, obviously reduce MDA level and improve SOD activity, has effects of resisting oxidation and removing oxygen radical, can improve the condition of myocardial ischemia to obviously relieve the illness state of miocardial infarction, can obviously prolong the time for forming thrombus, and can be applied in preparing medicaments for resisting the myocardial ischemia, medicaments for protecting myocardial ischemia-reperfusion cardiac microvascular endothelial cells, medicaments for resisting cerebral ischemia, medicaments for resisting atherosclerosis, medicaments for resisting the thrombus, anti-ageing medicaments, antitumor medicaments, and medicaments for resisting liver injury and liver fibrosis. The novel application has the advantage that: the application range of the structure modified products of the salvianolic acid B in pharmacy is determined, so that the preparation of the novel medicaments of which the pharmacological activity and bioavailability are higher than those of the salvianolic acid B is possible.

Description

【Technical field】 [0001] The present invention relates to the technical field of chemical synthesis and application of medicines, in particular to the application of a new compound-salvianolic acid B structurally modified product in pharmacy. 【Background technique】 [0002] Salvia miltiorrhiza was first recorded in "Shen Nong's Materia Medica" and was listed as top grade. It is one of the commonly used medicines in traditional Chinese medicine. It has the effects of dispelling blood stasis and relieving pain, promoting blood circulation and stimulating menstruation, clearing heart and eliminating troubles, and has a long history of clinical application. Salvia miltiorrhiza has the functions of dilating blood vessels, lowering blood fat and anti-atherosclerosis, inhibiting platelet aggregation and anti-thrombosis, protecting myocardium, increasing coronary flow, antibacterial and anti-inflammatory, anti-tumor, etc., and has a wide range of medicinal prospects. Salvianolic aci...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61P9/10A61P7/02A61P25/28A61P35/00A61P1/16
Inventor 倪力军张立国程晓亮侯俊郭美兰王晓影
Owner EAST CHINA UNIV OF SCI & TECH
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