Triterpenoid compound and preparation method and use thereof

A technology of triterpene compounds and compounds, applied in the field of pharmaceutical applications, can solve problems such as decreased immune function and increased incidence of tumors, and achieve strong lymphocyte proliferation, significant biological activity, and the effect of inhibiting lymphocyte proliferation

Active Publication Date: 2018-03-06
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term application may also lead to the decline of the body's immune function, and may increase the incidence of tumors

Method used

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  • Triterpenoid compound and preparation method and use thereof
  • Triterpenoid compound and preparation method and use thereof
  • Triterpenoid compound and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1 Preparation of compounds in the present invention

[0053] Dried Herb Herb Powder (5Kg) was extracted three times with 95% ethanol at room temperature, and the ethanol was evaporated to obtain 300 g of extract. The extract was dissolved in ethyl acetate and water, separated, and the organic phase was evaporated to dryness to obtain 103 g of crude extract. The crude extract was eluted with a gradient of methanol-water mixed solvent with a volume ratio of 3:7 to 1:0 on the MCI column, and the eluate eluted with 80% v / v methanol-water mixed solvent was collected to obtain a 10 g group Point F3.

[0054] Component F3 was separated by a normal phase silica gel column, eluted with a mixed solvent of petroleum ether-acetone with a volume ratio of 10:1 to 1:2, and collected with a mixed solvent of petroleum ether-acetone with a volume ratio of 4:1. The eluent obtained component F3e, and the eluate eluted with a mixed solvent of petroleum ether-acetone with a volu...

Embodiment 2

[0070] Example 2 In vitro immunosuppressive activity test of compounds of the present invention

[0071] The in vitro immunosuppressive activity of compounds H-1, H-2 and H-3 of Example 1 was tested.

[0072] Concanavalin A (ConA), bacterial lipopolysaccharide (LPS), CCK-8 kit, and RPMI 1640 culture medium were purchased from Gibco BRL Biologicals in the United States. 3 H-thymidine nucleotide was purchased from Shanghai Institute of Atomic Energy.

[0073] Experimental principles: (1) T and B lymphocytes have antigen-recognizing receptors and mitogen receptors on the surface, and the corresponding lymphocyte clones can proliferate under the stimulation of specific antigens. Concanavalin A (ConA) and bacterial lipopolysaccharide (LPS) are mitogens that can stimulate the proliferation and differentiation of T and B lymphocytes, respectively. This process is similar to the activation process of lymphocytes in vivo. Therefore, mitosis Proliferation-induced lymphocyte proliferat...

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Abstract

The invention relates to a triterpenoid compound as shown below and a preparation method and use thereof. It is shown through several in vitro immunosuppressive activity tests that the compound has anobvious effect on inhibiting lymphocyte proliferation in mice and are expected to be used in the preparation of immunosuppressive drugs. The triterpenoid compound and the preparation method and use thereof can provide lead compounds for the development of new drugs for the treatment of autoimmune diseases and organ transplant rejection.

Description

technical field [0001] The invention belongs to the technical field of drug application, and in particular relates to a class of triterpene compounds with relatively rare skeletons, a preparation method of the compounds and an application in the preparation of drugs with strong immunosuppressive effect. Background technique [0002] Dysregulation of human immune function can lead to a variety of diseases, such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis, Sjögren's syndrome and autoimmune hepatitis. With the development of basic and clinical immunology, many diseases of unknown cause can also be explained by autoimmune responses. Autoimmune reaction can not only lead to the occurrence of autoimmune diseases, but also has a vicious circle in itself, which can make the disease protracted and the prognosis is poor. For a long time, people have mainly applied the principle of immune tolerance and used immunosuppressants to treat autoimmune diseases, and achi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J21/00A61K31/585A61P37/06
CPCC07J21/00
Inventor 岳建民左建平范耀月唐炜吴艳
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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