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Application of curcuma wenyujin diterpene compound C in drugs for treating gastrointestinal inflammation

A technology of warming turmeric and compounds is applied in the application field of preparing medicines for treating gastrointestinal inflammation, and achieves the effects of inhibiting inflammation and broadening the scope of medicine selection.

Inactive Publication Date: 2012-05-30
ZHEJIANG PROVINCIAL HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, there are no literature reports and patent disclosures about the inhibitory effect of turmeric diterpenoid C on gastrointestinal inflammation.

Method used

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  • Application of curcuma wenyujin diterpene compound C in drugs for treating gastrointestinal inflammation
  • Application of curcuma wenyujin diterpene compound C in drugs for treating gastrointestinal inflammation
  • Application of curcuma wenyujin diterpene compound C in drugs for treating gastrointestinal inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 warm turmeric diterpenoid C

[0021] Warm 10 kg of dried rhizomes of turmeric, extract 4 times with 8 times the amount (80 L) of 95% ethanol under reflux, and recover the solvent to obtain 247 g of crude extract. The total extract was uniformly dispersed with 500 mL of water, extracted with 1 times the amount (500 mL) of petroleum ether, dichloromethane, and n-butanol in turn to obtain 95.1 g of dichloromethane extract, and the dichloromethane part was based on petroleum ether / ethyl acetate. Eluent (volume ratio: 100:0, 100:10, 100:20, 100:30, 100:40, 100:50, 100:60, 100:70, 100:80, 100:90), silica gel Column chromatography obtained 10 fractions A, B, C, D, E, F, G, H, I, J. Fraction E uses acetonitrile (70%)-water (30%) as the mobile phase, and is further separated by preparative chromatography to obtain 8 fractions (0-80min, 1 fraction per 10 minutes), namely E1-E8, of which E8 is acetonitrile (45%)-water (55%) was eluted isocraticall...

Embodiment 2

[0022] Carrying out 2 structure identification of diterpenoid C in curcuma

[0023] White needle crystals prepared according to Example 1, HREIMS M + 380.2581, the molecular formula is determined to be C 22 h 36 o 5 (calculated M380.2563), its unsaturation is 5, ESI-MS (negative) gives m / z: 319[M-H] - .

[0024] 13 The C-NMR spectrum shows that there are 22 carbons, and the structure contains two carbonyl carbons from δ208.9 and δ170.4; δ70.4, δ76.0 and δ81.6 are three oxygen-carbon signals; δ111.4 and δ145.8 is two olefinic carbon signals; combined with the degree of unsaturation, it is speculated that the structure may contain two rings.

[0025] From 1 From the H-NMR spectrum, there are six consecutive quaternary carbon methyl proton signals: δ0.83 (3H, s), 0.86 (3H, s), 0.94 (3H, s), 1.22 (3H, s), 1.47 (3H, s) and δ2.13(3H, s); δ5.36(1H, m) suggested an oxo-methine signal; δ5.05(1H, d, J=12.0Hz), 5.10(1H , d, J=18.0Hz) and δ6.06 (1H, dd, J=12.0, 18.0Hz) are the th...

Embodiment 3

[0036] Example 3 Application of warm turmeric diterpenoid C on inhibition of gastrointestinal inflammation

[0037] (1) Cell culture

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Abstract

The invention discloses application of a curcuma wenyujin diterpene compound C of formula (I) in the drugs for treating gastrointestinal inflammation. The gastrointestinal inflammation comprises one of stomachache, chronic gastritis, acute gastritis, chronic enteritis, acute enteritis and gastric ulcer; and the daily effective dose of the curcuma wenyujin compound C for the human body is 0.001-0.01g / kg. The invention provides a list which can be used for preparing new drugs for treating gastrointestinal inflammation, broadens the drug selection range of the patients and provides new varietiesfor the screening of the drugs for treating gastrointestinal inflammation; and the curcuma wenyujin diterpene compound C of the invention can play a role of suppressing the inflammation through suppressing the nucleus translocation of NF-kappaB and the expression and secretion of COX-2, TNF-alpha, 1L-1beta and 1L-6 in gastrointestinal cells.

Description

(1) Technical field [0001] The present invention relates to a new application of warm turmeric diterpenoid C, in particular to the application of the warm turmeric diterpene C in the preparation of medicines for treating gastrointestinal inflammation. (2) Background technology [0002] In 1863, pathologist Virchow first proposed that tumors may arise from chronic inflammation. In recent years, epidemiological data have shown that chronic infection and inflammation may be an important factor in the occurrence and development of tumors. For example, some studies have suggested that about 15% of malignant tumors may be attributed to chronic infections such as bacteria, viruses or parasites (KUPER H, ADAMI HO, TRIEHOPOULOS D. Infections as a major preventable cause of human cancer [J]. J InterMed, 2000, 248: 171-183.). Chronic inflammation may form a tumor microenvironment, inflammatory macrophages generate reactive oxygen species and reactive nitrogen species (ROS), damage cel...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/22A61P1/04A61P1/00A61P29/00
Inventor 吕宾金海峰
Owner ZHEJIANG PROVINCIAL HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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