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Wikstroemia indeca extract, their production and use in the production of anti-inflammatory pharmaceutical

A technology of Gewang and medicine, which is applied in the field of Gewang extract, its preparation and its application in the preparation of anti-inflammatory drugs, can solve the problem of not being able to conduct in-depth research, not confirming the chemical structure and physical and chemical parameters of the active substance group, and not being able to understand clearly To better understand the properties of materials and other issues, to achieve the effect of no cytotoxicity, reduce tumor growth, and increase radiosensitivity

Inactive Publication Date: 2010-04-28
NIHON UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In the Chinese Patent Application No. 9811403.9, the patent "Preparation Method of New Anti-AIDS Drug Legewang Extract" describes the method of extracting active substances in Gewang, but does not confirm the chemical structure and physical and chemical parameters of the active substance group. Therefore, it is impossible to clearly understand the functioning material properties, and it is impossible to further in-depth research, etc.

Method used

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  • Wikstroemia indeca extract, their production and use in the production of anti-inflammatory pharmaceutical
  • Wikstroemia indeca extract, their production and use in the production of anti-inflammatory pharmaceutical
  • Wikstroemia indeca extract, their production and use in the production of anti-inflammatory pharmaceutical

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation of extract and determination of compound structure

[0029] The stem or whole grass of 2.3 kg of Gewang was crushed, 10 liters of 80% methanol (methanol: water = 8: 2) was added, extracted three times, concentrated and dried under reduced pressure at 40° C. to obtain 286 g of extract. Dissolve all the extracts in 2 liters of water, extract 3 times with 2 liters each of n-hexane, ethyl acetate, and n-butanol successively, and concentrate and dry these extracts under reduced pressure at 40°C to obtain 6.5 g of n-hexane extracts , 62.0 g of ethyl acetate extract, and 25.0 g of n-butanol extract. Various extracts are carried out NO generation inhibitory activity experiment (referring to embodiment 2), under the condition that the test sample concentration is 100 μ g / ml, n-hexane extract (76.1%), ethyl acetate extract (86.9%), For the butanol extract (6.45%), the NO production inhibition rate was affirmed; all the extracts were found to have no cytoto...

Embodiment 2

[0034] Embodiment 2: Determine the structure of physical and chemical parameters and compounds

[0035] The properties of the compound of formula (1) are shown in Table 1, 1 H and 13 See Table 2 for C-NMR data. And finally determined the structural formula of the compound by the above data.

[0036] Table 1:

[0037]

Compound 1

character

white oily

HR-EI-MS(m / z)

Calculated

Measurements

232.1463

232.1464

molecular weight

232

[0038]

Compound 1

molecular formula

C 15 h 20 o 2

[0039] Table 2 Compound (1) 1 H and 13 C-NMR spectral data (500MHz, CDCl 3 )

[0040]

1 H

13 C

1

133.5

2

2.92brs

39.3

3

203.6

4

139.9

5

167.2

6

2.80dd (15.4, 8.9)

2.86dd (15.4, 4.5)

34.0

7

2.53m

43.98

8

1.79m

1.98m

33....

Embodiment 3

[0044] Example 3: Activity test for inhibiting NO generation

[0045] The effect of inhibiting NO production by macrophages stimulated by interferon-r and lipopolysaccharide (the effect of inhibiting NO production) was determined by the following experimental method. And the inhibitory effect of NO production was evaluated based on the IC50 (μm) of the inhibitory effect.

[0046] Materials used:

[0047] RAW 264.7 cells (Dainippon Pharmaceutical Co., Ltd.)

[0048] N-1-naphthaleneethylenediamine hydrochloride (1g Wako Pure Chemical Industries)

[0049] Sulfa (500g Wako Pure Chemical Industries)

[0050] Ham's F12 medium (SIGMA N488500mL)

[0051] IFN-γ (Geneyme / Techne 100μg)

[0052] Lipopolysaccharide (LPS, 055:B5 10mg, Sigma)

[0053] Phosphoric acid (500ml Wako Pure Chemical Industries)

[0054] DMSO (500ml Wako Pure Chemical Industries)

[0055] 96-well microtiter plate (50 / box Sumitomo Bakelite, trade name [8096R])

[0056] Test method for NO production inhibitor...

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PUM

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Abstract

The invention relates to extracts from wilstroemia indeca C.A.Mey, the preparation method and pharmaceutical uses thereof, the formula of the extracted active compound.

Description

technical field [0001] The present invention relates to an extract of Ligewanga extract, its preparation method and its application in the preparation of medicine, in particular to extracting a compound with anti-inflammatory effect from plant Ligewanga. Background technique [0002] Daily inflammatory diseases that plague people include joint inflammation such as osteoarthritis, rheumatoid arthritis, rheumatoid spondylitis, gouty arthritis, etc.; inflammatory skin diseases such as eczema, psoriasis, dermatitis, etc.; Uveitis, conjunctivitis, etc.; lung diseases such as asthma, bronchitis, acute respiratory distress syndrome, etc.; bacteremia, that toxemia, aphthous ulcers, gingivitis, pancreatitis, etc.; Ileitis, atrophic gastritis, ulcerative colitis, celiac disease, peptic ulcer, irritable bowel syndrome such as mucosal inflammation caused by Helicobacter pylori infection or gastrointestinal tract caused by non-steroidal anti-inflammatory drugs illness and so on. [000...

Claims

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Application Information

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IPC IPC(8): C07C49/537A61K31/122A61K36/83A23K1/16A23L1/29A23L2/00A61P19/02A61P1/04A61P17/00A61P37/06A61P27/06A61P13/12A61P29/00A23L33/00
CPCA23K1/1609A61K36/83C07C49/733A61K31/122C07C45/78A23L1/3002A23K20/105A23L33/105A61P1/04A61P13/12A61P17/00A61P19/02A61P27/06A61P29/00A61P37/06
Inventor 王立岩北中进
Owner NIHON UNIVERSITY
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