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New application of Ginkgolide B derivative in medicament preparation

A technology of ginkgolide and its effect is applied in the new application field of 10-O-ginkgolide B, and can solve the problems such as the application of 10-O-(dimethylaminoethyl) ginkgolide B that has not been seen yet.

Active Publication Date: 2011-05-25
JIANGSU CAREFREE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no application of 10-O-(dimethylaminoethyl) ginkgolide B in antipyretic, analgesic and treatment of various acute and chronic inflammatory diseases

Method used

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  • New application of Ginkgolide B derivative in medicament preparation
  • New application of Ginkgolide B derivative in medicament preparation
  • New application of Ginkgolide B derivative in medicament preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 110

[0015] The analgesic effect of embodiment 110-O-(dimethylaminoethyl) ginkgolide B

[0016] Take 30 mice weighing 18-22 g, half male and half male. Randomly divided into 3 groups, 10 in each group, numbered, and placed in a glass bell jar to observe the normal activities of the mice. The mice were injected intraperitoneally with 0.2% compound of formula 1 (0.2ml / 10g), 0.2% cranidinidine solution (0.2ml / 10g) and equal volume of normal saline respectively. After 30 minutes, each mouse was injected with 1% acetic acid solution 2ml / 10g intraperitoneally, and the number of mice with writhing reaction in each group was observed. Record the results in the table below, and calculate the analgesic percentage of analgesics by integrating all laboratory data.

[0017]

[0018] Table 1 formula 1 compound writhing reaction experiment result

[0019]

[0020] *p<0.01, compared with model group

[0021] It can be seen from Table 1 that the analgesic percentage of the compound of for...

Embodiment 210

[0021] It can be seen from Table 1 that the analgesic percentage of the compound of formula 1 is 37.5%, which has obvious analgesic effect. Anti-inflammatory test of fat-induced rat granuloma of embodiment 210-O-(dimethylaminoethyl) ginkgolide B

[0022] Get 40 Wistar male rats, remove the hair on the back 24 hours before the experiment, perform aseptic operation under light ether anesthesia, inject 2% agar solution 2ml / rat subcutaneously in the hair-removed area of ​​the back midline of the rats to cause inflammation, and from the day of inflammation, divide 4 groups were given intragastric administration. The compound of Formula 1 was divided into high concentration group and low concentration group. The administration concentration is shown in Table 1. The administration was once a day for a total of 14 days. On the 15th day, the rats were sacrificed, dissected, the granuloma agar block was peeled off, and the wet weight was weighed.

[0023] The influence of table 2 formu...

Embodiment 310

[0026] Example 310-O-(Dimethylaminoethyl) ginkgolide B is on the effect of carrageenan-induced joint swelling in rats

[0027] 3.1 Grouping and administration

[0028] Get 36 rats, be divided into 6 groups at random, be respectively: (1) blank control group: NS 10ml / kg; (2) dexamethasone group: 5mg / kg; (3) formula 1 compound I group: 20mg / kg kg; (4) Formula 1 compound II group: 40 mg / kg; (5) Formula 1 compound III group: 80 mg / kg; (6) Formula 1 compound IV group: 160 mg / kg. Rats in each group were intragastrically administered with the above-mentioned dose of 10ml / kg, once a day, for 5 consecutive days.

[0029] 3.2 Measuring indicators and methods

[0030] One hour after the last administration, subcutaneously inject 0.1% carrageenan solution 0.1ml / paw into the sole of the left hind foot to cause inflammation. The volume of the toe of the left hind paw of the mouse.

[0031] Record the results, and calculate the swelling rate (%) and inhibition rate (%) respectively accor...

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Abstract

The invention relates to application of 10-O-(dimethylaminoethyl) Ginkgolide B in preparing antipyretic, analgesic and anti-inflammatory medicaments. Indicated by tests, the 10-O-(dimethylaminoethyl) Ginkgolide B can inhibit cyclooxygenase-2, has obvious effects of dissociating heat, easing pain and resisting various acute and chronic inflammations and has the advantages of less side effect and low toxicity.

Description

technical field [0001] The invention relates to a new application of 10-O-(dimethylaminoethyl) ginkgolide B, which is used for antipyretic, analgesic and anti-acute and chronic inflammations, especially inflammations caused by collagen tissue lesions. Background technique [0002] 10-O-(dimethylaminoethyl) ginkgolide B (structural formula shown in formula 1) is a derivative of ginkgolide B, reported by Qin Yinlin and others in the patent (publication number CN 1749257A) related to this compound. [0003] [0004] Formula I [0005] Ginkgolide B (Ginkgolide B, GB) is a diterpene compound with a six-ring cage structure extracted from Ginkgo biloba. , can stimulate coronary arteries and cerebral arteries, causing their contraction, spasm, resulting in myocardial and brain tissue ischemia. Anything that can cause tissue damage can be a cause of inflammation. Although there are many kinds of inflammatory factors, they can be classified into the following categories: (1). P...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P29/00A61P17/00A61P27/02A61P11/02A61P27/16A61P1/02A61P11/04A61P11/00A61P1/04A61P9/00A61P1/16A61P1/00A61P13/12A61P13/08A61P15/00
CPCY02A50/30
Inventor 秦引林
Owner JIANGSU CAREFREE PHARM CO LTD
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