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Application of class of norditerpenoid compounds Guankongjunchun derived from pitoporus betulinus

A technology of compounds and tube holes, applied in steroids, medical preparations containing active ingredients, organic chemistry, etc., can solve problems such as side reactions

Pending Publication Date: 2020-01-24
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs all have serious side effects. For example, the incidence of nephrotoxicity of cyclosporin

Method used

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  • Application of class of norditerpenoid compounds Guankongjunchun derived from pitoporus betulinus
  • Application of class of norditerpenoid compounds Guankongjunchun derived from pitoporus betulinus
  • Application of class of norditerpenoid compounds Guankongjunchun derived from pitoporus betulinus

Examples

Experimental program
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Effect test

Example

[0033] Application test example 1

[0034] 1. Using the cell viability assay method (MTT method) to screen the T and B lymphocytes for non-specific toxicity of the tubulin A-F obtained in the examples.

[0035] 2. Test principle: The succinate dehydrogenase in the mitochondria of living cells can reduce tetramethylazothiazole blue (MTT) to water-insoluble blue-purple crystal formazan (Formazan), while dead cells have no such function. After dissolving formazan with DMSO, the absorbance value is measured at 570nm wavelength, which can indirectly reflect the number of living cells. Within a certain range of cell number, the amount of MTT crystal formation is proportional to the number of cells, which can be used for cytotoxicity analysis. The cell viability assay (MTT method) was used to detect the toxicity of the compounds to mouse spleen lymphocytes.

[0036] 3. The specific steps of the cell viability determination method (MTT method) of this embodiment are as follows: the mouse i...

Example

[0038] Application test example 2

[0039] 1. Adopt 3 The H-TdR incorporation method was used to detect the effects of each compound on the proliferation of mouse spleen T and B lymphocytes.

[0040] 2. Test principle: T and B lymphocytes have recognition antigens and mitogen receptors on the surface, and the corresponding lymphocytes can proliferate and differentiate under the stimulation of specific antigens. Concanavalin A (ConA) and bacterial lipopolysaccharide (LPS) are two mitogens, which 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, mitogen-induced lymphocyte proliferation is often used as an indicator to evaluate lymphocyte function. 3 H-thymidine ( 3 H-TdR) incorporation method refers to adding tritium-labeled thymidine to the cell culture medium, then 3 H-TdR is taken into cells as a raw material for synthetic DNA and incorporated into newly syn...

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Abstract

The present invention relates to the technical field of microorganism medicinal chemistry and specifically relates to medicinal uses of six norditerpenoid compounds isolated and obtained from a fermentation product of a strain of pitoporus betulinus. An immunosuppressive activity screening test confirms that the six compounds have significant inhibitory activity on proliferation of T lymphocytes stimulated by concanavalin A and B lymphocytes stimulated by bacterial lipopolysaccharide, are non-toxic to the T and B lymphocytes, and have uses for preparing new immunosuppressive medicines.

Description

technical field [0001] The invention relates to the technical field of microbial medicinal chemistry, in particular to the application of six kinds of norditerpene compounds derived from Phyloporus betula in the development of drugs with immunosuppressive activity. Background technique [0002] The human immune system is composed of immune organs, immune cells and immune molecules, and is an important system for the body to execute immune responses and exert immune functions. The immune system is divided into innate immunity and adaptive immunity, of which adaptive immunity is further divided into humoral immunity and cellular immunity. In the innate immune response, T cells located in lymph fluid, blood and lymph nodes are mainly involved in cellular immune responses, and B cells are mainly involved in humoral immune responses. They not only have their own unique functions, but also cooperate with each other to exert immune effects together. The immune system of a normal b...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61K31/343A61K31/075A61P37/06A61P35/00C07J73/00C07D307/77C07C35/42
CPCA61K31/58A61K31/343A61K31/075A61P37/06A61P35/00C07J73/003C07D307/77C07C35/42C07C2603/26
Inventor 刘吉开赵珍珠陈贺平
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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