1,3-O-di-galloyl-6-O-(S)-decapetalous caesalpinia acyl-beta-D-glucopyranose and application thereof

A galloyl and glucopyranose technology, applied in the direction of sugar derivatives, sugar derivatives, esterified saccharides, etc., can solve the problems of not disclosing the use of such compounds

Inactive Publication Date: 2008-02-13
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the above-mentioned article does not disclose the purpos

Method used

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  • 1,3-O-di-galloyl-6-O-(S)-decapetalous caesalpinia acyl-beta-D-glucopyranose and application thereof
  • 1,3-O-di-galloyl-6-O-(S)-decapetalous caesalpinia acyl-beta-D-glucopyranose and application thereof
  • 1,3-O-di-galloyl-6-O-(S)-decapetalous caesalpinia acyl-beta-D-glucopyranose and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0039] 1. Take 1.73kg of Japanese snake mushroom, chop it, soak it with 70% methanol at room temperature, filter it overnight, and concentrate the filtrate under reduced pressure with a rotary evaporator to obtain 223.7g of the total extract; dilute the extract with water and dilute it with ether Extraction, take the water phase, and then extract with ethyl acetate to obtain the dissolved part of ethyl acetate; pass the dissolved part of ethyl acetate through Chromatorex ODS, elute with water, and then elute with 10-80% methanol, collect 40-80% methanol to wash Remove liquid, recover methanol under reduced pressure, add a little methanol to dissolve the residue; then apply MCI-gel CHP20P, elute with water and then 10-80% methanol, collect 40-80% methanol eluate, recover methanol under reduced pressure, The residue was dissolved by adding a little methanol; then it was chromatographed on Sephadex LH-20, eluted with water and then eluted with 10% to 80% methanol, and 50% to 80% o...

example 1

[0057] 【prescription】

[0058] 1,3-O-Di-Galloyl-6-O-(S)-Celoyl-β-D-Glucopyranose 20g

[0059] Microcrystalline Cellulose 48g

[0060] Soluble starch 30g

[0061] Talc powder 2g

[0062] A total of 1000 tablets were produced, each containing 20 mg of the compound.

[0063] 【Preparation】

[0064] Weigh 20g of the compound, add soluble starch to dilute to 50g, mix well, then weigh 48g of microcrystalline cellulose, use 95% ethanol to make soft material, sieve and granulate, dry at low temperature at 50°C, granulate, add talc powder 2g , mixed evenly, compressed into tablets (0.1g each), inspected for quality, packaged, and obtained.

[0065] 【Dosage】

[0066] 4 tablets each time, 3 times a day.

[0067] 【For people】

[0068] Applicable to various tumor patients.

example 2

[0070] 【prescription】

[0071] 1,3-O-Di-Galloyl-6-O-(S)-Celoyl-β-D-Glucopyranose 10g

[0072] Microcrystalline Cellulose 48g

[0073] Soluble starch 40g

[0074] Talc powder 2g

[0075] A total of 1000 tablets were produced, each containing 20 mg of the compound.

[0076] 【Preparation】

[0077] Weigh 10g of the compound, add soluble starch to dilute to 50g, mix well, then weigh 48g of microcrystalline cellulose, use 95% ethanol to make soft material, sieve and granulate, dry at low temperature at 50°C, granulate, add talc powder 2g , mixed evenly, compressed into tablets (0.1g each), inspected for quality, packaged, and obtained.

[0078] 【Dosage】

[0079] 4 tablets each time, 3 times a day.

[0080] 【For people】

[0081] Applicable to various tumor patients.

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Abstract

The invention provides a novel hydrolytic tannins of the pyran glucose category containing the gall acyl, particularly a 1,3-O-2-galloyl-6-O-(S)-caesalpinia digyna acyl-beta-D-glucopyranosyl dextrose. The chemical structure is as shown in formula (1). The compound of the invention can inhibit the proliferation of tumor; the compound has the better anti-tumor activity and can be used to prepare the anti-tumor drug.

Description

technical field [0001] The invention relates to the field of organic chemistry, in particular to glucopyranose hydrolyzable tannins containing galloyl groups. Background technique [0002] Tannins, also known as vegetable tannins, are a class of complex polyphenolic compounds widely present in plants, among which hydrolyzable tannins are esters or glycosides formed of phenolic acids and polyols. [0003] In 2001, Zhi-hong Jiang and Yoko Hirose found a variety of glucopyranose hydrolyzable tannins containing caffeoyl and galloyl groups in snake mushroom (Balanophora japonica Makino), such as: 1-O-(E) -Caffeoyl-3-O-galloyl-β-D-glucopyranose, the compound is a yellow amorphous powder, [α] D 15 -48.9°(c=0.8, MeOH), can be hydrolyzed into gallic acid and 1-O-(E)-caffeoyl-β-D-glucopyranose under the action of tannase; 3-O-(E) -Caffeoyl-4-O-galloyl-D-glucopyranose, the compound is a yellow amorphous powder, [α] D 15 -144.2°(c=0.7, MeOH), under the action of tannase, it can be ...

Claims

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Application Information

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IPC IPC(8): C07H13/10A61K31/7048A61K36/185A61P35/00
Inventor 姜志宏文晓芸田中山中崇吴少瑜刘中秋岩田弘美河野高畑勋吴曙光广濑小野
Owner SOUTHERN MEDICAL UNIVERSITY
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