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Immunosuppressant containing Withanolide type compound

A technology of immunosuppressants and compounds, which is applied in the field of immunosuppressants containing Withanolide-type compounds, can solve unclear problems, and achieve the effect of simple separation method, low cost and low toxicity immunosuppressive activity

Inactive Publication Date: 2009-05-06
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the anti-inflammatory mechanism of these plant ingredients, the specific Withanolide-type compounds contained in them, and the respective properties of these compounds are not clear.

Method used

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  • Immunosuppressant containing Withanolide type compound
  • Immunosuppressant containing Withanolide type compound
  • Immunosuppressant containing Withanolide type compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Total Withanolide compound screening sample preparation

[0046] 1. Physalis Total Withanolide Compound Screening Sample Preparation

[0047] Physalis 500g was extracted three times with 85% ethanol under reflux, concentrated, passed through macroporous adsorption resin (D101 type), first washed with 10% distilled water, then eluted with 75% ethanol, and concentrated under reduced pressure at the eluted part of 75% ethanol to get it out of the body Biological evaluation sample 1 (54 g).

[0048] 2. Sample preparation for screening of total withanolide compounds in Sophora oleifera:

[0049] 500g of bitter root was refluxed and extracted three times with 85% ethanol, concentrated, passed through macroporous adsorption resin (D101 type), washed with distilled water first, then eluted with 60% ethanol, and the 60% ethanol eluted part was concentrated under reduced pressure to be sent to in vitro biology Sample 2 (90 g) was evaluated.

Embodiment 2

[0050] Example 2 Separation of Withanolide-type compounds in Physalis

[0051] The aboveground part of Physalis allelengi was collected from Nanchuan County, Chongqing City, and was collected and identified as Physalis allelengi, a small plant of Solanaceae, by Mr. Yi Sirong of Chongqing Botanical Garden. The specimens are deposited in the Shanghai Modernization Research Center of Traditional Chinese Medicine.

[0052] Physalis aerial part (5.0Kg), with 3 times the amount of ethanol cold soaking extraction 3 times, each time for 2 days, combined filtrate, concentrated under reduced pressure to obtain extract (1.8kg), dissolved with a small amount of water, extracted with chloroform to obtain chloroform Fraction (197g), D-101 macroporous resin on the chloroform fraction, eluted with 25%, 75%, and 95% ethanol respectively to obtain 3 fractions (Fr.A-C). Fr.B (24.4g) was subjected to MCI column chromatography (MCI gel CHP 20P H 2 O / Me 2 CO 1:1) yielded 4 sites (Fr.B.1-B.4). F...

Embodiment 3

[0111] Example 3 Separation of Withanolide-type compounds in Radix Kulu

[0112] The aboveground part of Physalis angulata L was collected from Nanchuan County, Chongqing City, and was collected and identified as Physalis angulata L by Mr. Yi Sirong of Chongqing Botanical Garden.

[0113] 5.0Kg of the above-ground part of Physalis angulata L was extracted three times with 85% methanol to obtain 0.9Kg of extract, separated by polyamide column chromatography, 100% distilled water eluted part, 60% methanol eluted part, 80% methanol Elution part (containing chlorophyll), 60% methanol elution part (921g) silica gel column chromatography (petroleum ether / acetone 5:1-1:1) obtains four parts (part A-D), and part A passes ODS (C- 18) Column chromatography (methanol / water 85:15) and Sephadax LH-20 purification (chloroform / methanol) to obtain compounds Physagilin A (135 mg) and Withagulatin A (124 mg); part B was subjected to ODS (C-18) column chromatography (methanol / water 78:22) and S...

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Abstract

The invention discloses an immunosuppressor which containing a compound shown in the following general formula I and / or the general formula II, or an optical isomer thereof; wherein, R1, R2, R3, R4, R5, R6 and R7 are selected from H, OH, O-acyl, OMe, OEt, O<n>Pr, OPr, F, Cl, Br, NH2, NO2 or CN; wherein, site 5 and site 6 are an epoxy bond or a double bond; in the general formula I, the ether linkages of site 14 and site 27 are connected or disconnected; in the general formula II, the sites 14 and 15 and the sites 16 and 17 are the epoxy bond or the double bond, or a plant extract containing the compound. The immunosuppressor has stronger immuno-suppression effect, generates repression function to T and B lymphocyte periods which are excessively proliferated, and can be used for curing the self immunological diseases and relevant diseases.

Description

technical field [0001] The present invention relates to the technical field of immunosuppressants, more specifically, to an immunosuppressant containing a Withanolide compound. Background technique [0002] Withanolide-type compounds are a class of ergostane-type compounds with 28 carbon atoms, and their unique structure is that the 22-position and 26-position carbons are connected to form a side chain of a δ-lactone ring (see the following Withanolide skeleton structure). [0003] [0004] Withanolide can be used not only to represent ergostane-type 22,26-lactones, but also to represent all biologically related compounds. The former is a classical Withanolide-type compound, and the latter is a non-classical Withanolide-type compound. These compounds are mainly distributed in several genera of Solanaceae, such as Physalis, Withania, Datura, Jaborosa, Dunalia, Salpichroa, Deprea, Solanum, Vassobia, Exodeconus, Hyoscyamus, Iochroma, Discopodium, etc. (P.Chirsten.Withanolid...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61K31/366A61P37/08A61P37/06A61P29/00A61P21/04A61P19/02A61P17/00A61P11/06A61P7/00A61P3/10A61P1/16
Inventor 马磊刘建文胡立宏孙丽娟于有军
Owner EAST CHINA UNIV OF SCI & TECH
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