Morus extracts rich in n-acids of imino sugars and or pipecolic acids

A technology of imino sugars and amino acids, applied in the field of extracts of N-acids and/or 2-pipercolic acids, can solve problems such as side effects, and achieve the effects of reducing side effects and improving bioavailability

Active Publication Date: 2014-10-15
PHYNOVA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0041] The problem with these and other mulberry extracts that contain large amounts of DNJ (typically 5-10% by weight of DNJ) is that DNJ is not a selective inhibitor of either α-glucosidase, and therefore, extracts containing large amounts of DNJ due to Inhibition of multiple glucosidases (including digestive disaccharidases) produces side effects

Method used

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  • Morus extracts rich in n-acids of imino sugars and or pipecolic acids
  • Morus extracts rich in n-acids of imino sugars and or pipecolic acids
  • Morus extracts rich in n-acids of imino sugars and or pipecolic acids

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0141] starting extract

[0142] Dry extract of mulberry leaves, batch ML091210

[0143] method

[0144] The sample was dissolved in water, and exchanged by strongly acidic cation (IR120H in column 2×30cm + Form resin) fractional distillation, get

[0145] i. Water-shifted unretained samples (expected to contain mostly sugars, flavonoids, etc.);

[0146] ii. 2M pyridine-shifted bound fraction (typically removes residual sugars, phenols, and neutral and acidic amino acids); and

[0147] iii. Bound fraction transferred from 2M ammonia solution (expected to contain any alkaloids [imino sugars] and basic amino acids)

[0148] Some DNJ was detected in the unretained material (perhaps due to sample overloading or pH), so it was passed through a second IR120 column (same size) to obtain a new unretained sample and a second ammonia fraction . The second unretained sample did not contain DNJ.

[0149] The fractions are listed in Table 1 below:

[0150]

[0151] This fraction...

Embodiment 2

[0183] The extract of Example 1 was fractionated into four fractions using cation exchange chromatography (IR120H+ form).

[0184] The unretained fraction contained sugars with imino sugars transferred with pyridine and then ammonia.

[0185] Some DNJ was present in each retained fraction, but most was present in the first ammonia fraction. Other imino sugars were also tested, including experimental mulberry alkaloids, DAB, certain hydroxylated imino acids, and other possible new imino sugars.

[0186] Table 4 below shows the enzyme inhibition observed by the fractions in Example 1.

[0187]

[0188]

[0189] In embodiment 2, purpose is:

[0190] a. Further decompose the components in all four fractions:

[0191] b. Analyze the compound by GC-MS and 500MHz NMR, identifying as many components as possible; and

[0192] c. Glycosidase assays were performed on the purified compounds to further discern the inhibitory effects conferred by the different components.

[0193] ...

Embodiment 3

[0246] The fractions described in Example 2 were analyzed to obtain additional information about the iminosugars and sugars of the samples.

[0247] The sugar fraction accounted for almost half of the samples and showed activity against various glycosidases and glycogen phosphorylases.

[0248] Sugars such as sucrose, trehalose and glucose do not significantly inhibit these enzymes.

[0249] In this example, an attempt was made to characterize the active components of the sugar fraction and further observe its activity.

[0250] At this point, it is further fractionated using a set of ion exchange columns.

[0251] method

[0252] The IR120 unretained fraction from Example 1 was placed on anion exchange resin CG400 (OH - Chromatographic analysis on (1-11) and two acetic acid fractions (Table 5 - Example 2) were obtained. Still in this example these fractions were further fractionated and the activity of said fractions was investigated further.

[0253] analyze

[0254] G...

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Abstract

This invention relates to extracts rich in N-acids of imino sugars (as opposed to neutral and basic imino sugars) and / or pipecolic acids obtainable from the plant leaves of mulberry (Morus). The extracts have been shown to have enzymatic activities making extracts rich in these compounds, and the compounds isolated from these extracts, to be good candidates for use in the treatment of diseases, particularly, but not exclusively, metabolic disorders, such as, for example, diabetes.

Description

[0001] The present invention relates to an extract rich in N-acids of imino sugars (as opposed to neutral and basic imino sugars) and / or 2-pipericolic acids obtainable from the leaves of the plant Morus. [0002] The extracts have been shown to have enzymatic activity, which makes the extracts enriched in these compounds, and the compounds isolated from these extracts, useful in the treatment of diseases, in particular but not exclusively metabolic disorders such as, for example, diabetes good candidate. [0003] definition [0004] Imino sugars are a widespread class of plant and microbial compounds that have the ability to interact with human glycosidases, other proteins, and sugar receptors. In this specification, they are considered polyhydroxylated secondary and tertiary amines, where the molecules resemble monosaccharide sugars, but where the epoxides are replaced by nitrogen. There are 5 ring structures that fit into this category, which are the most common in nature: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/605A61P3/08
CPCA61K36/605A61P3/00A61P3/06A61P3/08A61P43/00A61P5/50A61P3/10A23L33/105G01N2333/926
Inventor A·加拉格尔余虹雯
Owner PHYNOVA LTD
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