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Epigynum auritum pregnane glycoside compound and application thereof

A kind of technology of pregnane glycoside and simao vine, applied in simao vine pregnane glucoside compound and its application field

Inactive Publication Date: 2017-08-18
KUNMING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Driven by the interest in discovering new drug lead compounds, we have carried out a large number of biological activity screening experiments on these new compounds. The pregnane glycoside compounds provided by the present invention and their use as immunosuppressive drugs have not been reported yet

Method used

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  • Epigynum auritum pregnane glycoside compound and application thereof
  • Epigynum auritum pregnane glycoside compound and application thereof
  • Epigynum auritum pregnane glycoside compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: Preparation of pregnane glycosides

[0022] Take 4.5 kg of dry powder of Simao vine leaves, reflux extraction with 75% ethanol for 3 times, each time for 48 hours, filter and remove the filter residue, combine the filtrate extracted three times, concentrate under reduced pressure, then extract with ethyl acetate for 3 times, concentrate ethyl acetate for extraction The layer weighed to obtain 57g; the ethyl acetate layer extract was roughly divided with macroporous adsorption resin D101, and eluted with methanol water with a volume percentage of 20%, 40%, 60%, 80%, and 100% to obtain a total of 5 Parts (Fr.A-E). Fr.B (4.6g) was prepared by gradient elution with 30%-70% methanol and water to obtain six fractions Fr.B1-B6. Then pass Fr.B2 (2.5g) through a 200-300 mesh silica gel column, and use chloroform-acetone (10:1-3:1) as the eluent to elute to obtain a total of four parts Fr.B2a-Fr .B2d. Fr.B2b (298 mg) was prepared through a gel column Sephadex LH-...

Embodiment 2

[0030] Embodiment 2: Immunosuppression detection test

[0031] (1) Preparation of spleen lymphocyte suspension

[0032] Take 18-22g of healthy BABL / c mice and kill them by bloodletting, put them in 75% alcohol for 5 minutes and sterilize them, take them out, put them in a sterile tray with the left side up, and clamp them with sterilized tweezers in an ultra-clean bench. Remove the fur in the middle of the abdomen, make an incision, use another set of instruments to cut open the layers of the abdominal wall, use the third set of instruments to take out the spleen, remove fat and connective tissue, put it in PBS (phosphate buffer saline), and wash away the floating blood . Then move the spleen tissue to a plate filled with RPMI 1640 incomplete culture medium, cut it into small pieces with scissors, grind the spleen in a 200-mesh stainless steel screen with a sterile syringe core, wash it with a small amount of PBS several times, and The suspension was transferred to a 15mL ce...

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Abstract

The invention discloses an epigynum auritum pregnane glycoside compound and application thereof in preparation of immunosuppressive drugs. An experiment result shows that the compound has strong activity of suppressing proliferation of splenic lymphocytes. The invention provides a leading compound for research on a new immunosuppressor, and facilitates development and utilization of plant medicinal resources.

Description

technical field [0001] The invention relates to a class of Simaoteng pregnane glycoside compounds and the application thereof in the preparation of immunosuppressive drugs, especially the application in the preparation of immune drugs for treating organ transplantation anti-rejection and autoimmune diseases. Background technique [0002] In recent years, with the gradual improvement of the degree of industrialization, autoimmune diseases, hypersensitivity diseases and other diseases caused by excessive immune response are also increasing. Finding high-efficiency and low-toxicity immunosuppressants has become a current research hotspot. [0003] Immunopharmaceuticals are a new class of therapeutic drugs developed after the 1970s. Immunotherapy achieves the purpose of curing diseases by regulating the immune function of the body and correcting the abnormal immune response. Most drugs that act on the immune system have both positive and negative effects, that is, immune enhanc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00A61K31/704A61P37/02A61P37/06
CPCC07J17/005
Inventor 程桂广曹建新赵天瑞樊建
Owner KUNMING UNIV OF SCI & TECH
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