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
View PDF0 Cites 23 Cited by
  • 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 Withanolid

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap