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Uses of ursolic acid saponin and oleanolic acid saponin in preparing medicine for increasing white blood cell and/or blood platelet

A technology of oleanolic acid saponin and ursolic acid saponin, which is applied in the application field of preparing white blood cell and/or platelet-increasing drugs, can solve the application of ursolic acid saponin, white blood cell and/or platelet-increasing drugs that have not been seen Issues such as reporting, difficulty in conversion, etc.

Active Publication Date: 2008-07-23
CHENGDU DIAO JIUHONG PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN03135776 discloses a class of triterpene saponins isolated from the traditional Chinese medicine Burnet, mainly consisting of 19-hydroxyursolic acid (also known as pomolic acid, English name pomolic acid) as aglycone, which has the ability to increase white blood cells and / or The significant role of platelets, due to the existence of a series of saponins with similar structures and similar polarities in the traditional Chinese medicine Bunetia burnet, and their content is limited, it is difficult to separate and purify effective monomers in batches for medicinal use. The distribution of glycosides in natural products is not much, so it is not easy to obtain a large amount from the perspective of separation and extraction; and from the perspective of synthesis, starting from the readily available raw material of ursolic acid, the 19-hydroxyl is not easy to convert easily, Therefore, there are certain limitations in its development and use
[0004] So far, there have been no reports on the application of ursolic acid saponin and oleanolic acid saponin in the preparation of drugs that increase white blood cells and / or platelets

Method used

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  • Uses of ursolic acid saponin and oleanolic acid saponin in preparing medicine for increasing white blood cell and/or blood platelet
  • Uses of ursolic acid saponin and oleanolic acid saponin in preparing medicine for increasing white blood cell and/or blood platelet
  • Uses of ursolic acid saponin and oleanolic acid saponin in preparing medicine for increasing white blood cell and/or blood platelet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Preparation of 3-O-(α-L-arabinopyranose) ursolic acid-28-O-(α-L-arabinopyranose) ester:

[0060] Ursolic acid 1g (2.2mmol) in 20ml dry CH 2 Cl 2 solution, N 2 Under atmosphere, with arabinose glycosylation donor 2,3,4-tri-O-benzoyl-β-L-arabinosyl trichloroacetimidate 3.4g (5.7mmol, 2.6eq) ( The synthesis method of this compound refers to J.Org.Chem.1999, 64, 7265-7266), after mixing 1.5 g of powdered 4 angstrom molecular sieves, trimethylsilyl trifluoromethanesulfonate TMSOTf (0.03 ml, 0.15eq), the reaction was gradually warmed to room temperature, stirred overnight, and a small amount of Et was added 3 N (0.3ml) quenched the reaction, filtered, and after the filtrate was concentrated, silica gel column chromatography was eluted with petroleum ether / ethyl acetate system (4 / 1-2 / 1) to obtain 1.47g (1.1 mmol), it was dissolved in methanol / dichloromethane (2 / 1, 30ml) and 378mgNaOMe (7mmol, 6.4eq) was added, reacted at room temperature for 4 hours, acidic resi...

Embodiment 2

[0066] Example 2: Preparation of 3-O-(α-L-rhamnopyranose) ursolic acid-28-O-(α-L-rhamnopyranose) ester:

[0067] Similar to the method of Example 1, 2,3,4-tri-benzoyl-β-L-rhamnopyranosyl trichloroacetimidate is the glycosylation donor, and 3-O-(α -L-rhamnopyranosyl)ursolic acid-28-O-(α-L-rhamnopyranosyl)ester. [ α ] D 20 = - 11.8 ( C 0.17 , DMF )

[0068] 1 HNMR (600MHz, d 5 -pyridine): δppm 6.75 (1H, s), 5.46 (1H, m), 5.32 (1H, s), 4.56-4, 57 (2H, m), 4.52 (1H, dd, J=9.12, 3.2Hz) , 4.47 (1H, dd, J = 8.9, 3.2Hz), 4.38 (1H, t, J = 9.3Hz), 4.29-4.34 (3H, m), 3.17 (H, dd, J = 11.8, 4.44Hz), 2.44(1H, d, J=11.3Hz), 1.81(1H, m), 1.70(3H, d, J=6Hz), 1.67(3H, d, J=6Hz), 1.17(3H, s), 1.08( 1H, m), 0.93(3H, s), 0.92(6H, s), 0.90(3H, d, J=6.4Hz), 0.88(3H, d, J=6.4Hz), 0...

Embodiment 3

[0071] Example 3: Preparation of 3-O-(β-D-glucopyranose) ursolic acid-28-O-(β-D-glucopyranose) ester:

[0072] Similar to the method of Example 1, the glycosylation donor is 2,3,4,6-tetra-O-benzoyl-α-D-glucosyl trichloroacetimidate, and 3-O-(β -D-glucopyranose)ursolic acid-28-O-(β-D-glucopyranose) ester. [ α ] D 20 = + 21.7 ( C 1.02 , MeOH )

[0073] IR(KBr)cm -1 : 3417, 2925, 1727, 1672, 1456, 1377, 1226, 1075, 1027, 896, 831

[0074] 1 HNMR (600MHz, CD 3 OD): δppm5.33 (d, J=8.3Hz, 1H, H-1″), 5.24 (t, 1H, H-12), 4.31 (d, J=7.8Hz, 1H, H-1′), 3.77-3.84(m, 2H), 3.65-3.68(m, 2H), 3.28--3.39(m, 7H), 3.16-3.18(m, 2H), 2.22(d, J=11.2Hz, 1H, H- 18), 1.12, 1.05, 0.96, 0.84, 0.83(s each, 3Heach, Me×5), 0.88(d, J=6.4Hz, 3H), 0.78(d, J=11.6Hz, 1H, H-5)

[0075] 13 CN...

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Abstract

The invention provides an application of ursolic acid saponin and oleanolic acid saponin with a general formula I in the preparation of medicines for increasing leucocyte and/or blood platelet. The invention also provides a medicine combination with the chemical compound. The invention adopts the low-cost ursolic acid and oleanolic acid which is easily available from natural products and introduces monosaccharide and oligosaccharyl through structure modification. Pharmacology experiments prove that the invention can notably increase the leucocyte and/or the blood platelet.

Description

technical field [0001] The invention belongs to the technical field of medicines. Specifically, it relates to the application of ursolic acid saponin and oleanolic acid saponin in the preparation of medicines for increasing white blood cells and / or platelets. Background technique [0002] White blood cells have the ability to phagocytose, can eliminate foreign pathogenic bacteria, and protect the health of the body, so people call it the body guard. The leukocytes in the blood circulation of normal people are 4000-10000 / m3. The most important white blood cells are neutrophils with defensive functions, accounting for 50-70% of the total. Generally speaking, the most common and most important leukopenia refers to neutropenia. When the total number of white blood cells is lower than 4000 / mm3, the body's resistance is low at this time, and it is extremely easy to cause bacterial infection, which is life-threatening in severe cases. Platelets are one of the formed components ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K9/00A61P37/02A61P7/00A61P35/00
Inventor 广兵刘军剑董光新彭向阳龚晓霞黄振周美荣占伟晏菊芳黄瑜秦东光姬建新李伯刚
Owner CHENGDU DIAO JIUHONG PHARMA FACTORY
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