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Excoecaria agallocha endophytic fungus sourced indene derivative, and applications thereof in preparation of anti-inflammatory drugs

A technology of endophytic fungi and derivatives, applied in the field of pharmaceutical compounds, can solve problems such as injury, adverse reactions, kidney damage, etc., and achieve good results in application prospects

Active Publication Date: 2018-07-13
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although they all have certain clinical anti-inflammatory effects, long-term large-scale use will produce a series of adverse reactions and tolerance, such as gastric mucosal damage, liver damage, kidney damage, etc.

Method used

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  • Excoecaria agallocha endophytic fungus sourced indene derivative, and applications thereof in preparation of anti-inflammatory drugs
  • Excoecaria agallocha endophytic fungus sourced indene derivative, and applications thereof in preparation of anti-inflammatory drugs
  • Excoecaria agallocha endophytic fungus sourced indene derivative, and applications thereof in preparation of anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The acquisition of embodiment 1 sea paint endophytic fungus Diaporthe sp.SYSU-HQ3

[0042] The inventor team isolated an endophytic fungus Diaporthe sp.SYSU-HQ3 from the fresh leaves of the mangrove plant Excoecaria agallocha L. in the sea area of ​​Zhuhai, Guangdong Province, and preserved it in Guangdong Microbial Bacteria on August 4, 2017. Species Collection Center (GDMCC), the deposit number is GDMCC No: 60217.

Embodiment 2

[0043] The separation of embodiment 2 compound

[0044] Novel indene derivatives were isolated from the fermentation broth of endophytic fungus Diaporthe sp.SYSU-HQ3.

[0045] The specific method is as follows:

[0046] (1) Seed liquid culture of the fungus Diaporthe sp.SYSU-HQ3: The composition of the medium is by weight: 0.3% glucose, 0.1% yeast extract, 0.5% peptone, 2.5% agar, 3% sodium chloride, and 98% water ; Make a test tube slant, pick the strains into the slant, and culture at 30°C for 6 days.

[0047] (2) Fermentation culture of the fungus Diaporthe sp.SYSU-HQ3: use solid rice fermentation medium: rice: seawater = 1:1; moon;

[0048] (3) Extracting the product after the above-mentioned fermentation culture with methanol three times, concentrating the extract, and extracting the obtained concentrated extract with ethyl acetate to obtain a crude ethyl acetate extract.

[0049] (4) The ethyl acetate crude extract is separated by silica gel normal phase chromatograp...

Embodiment 3

[0050] The structural analysis of embodiment 3 compound

[0051] Structural analysis of new compounds 1-4 was carried out, and the following experimental data were obtained:

[0052] New Compound 1: C 25 h 30 o 6 , HRESI-MS: 425.1961 [M-H] - (calculated value 425.1964).

[0053] New compound 2: C 25 h 30 o6 , HRESI-MS: 425.1968 [M-H] - (calculated value 425.1964).

[0054] New Compound 3: C 25 h 30 o 6 , HRESI-MS: 425.1964 [M-H] - (calculated value 425.1964).

[0055] New Compound 4: C 25 h 30 o 6 , HRESI-MS: 425.1968 [M-H] - (calculated value 425.1964).

[0056] The NMR data of compounds 1-4 are shown in Table 1 and Table 2.

[0057] Table 1. NMR data of compounds 1 and 2 (CDCl 3 , 500MHz / 125MHz,ppm)

[0058]

[0059]

[0060] Table 2. NMR data of compounds 3 and 4 (CDCl 3 , 500MHz / 125MHz,ppm)

[0061]

[0062]

[0063] The structural formulas of compounds 1-4 are as follows:

[0064]

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Abstract

The invention discloses an Excoecaria agallocha endophytic fungus sourced indene derivative, and applications thereof in preparation of anti-inflammatory drugs. The Excoecaria agallocha endophytic fungus sourced indene derivative is obtained via separation from Excoecaria agallocha endophytic fungus Diaporthe sp.SYSU-HQ3, the Excoecaria agallocha endophytic fungus Diaporthe sp.SYSU-HQ3 is preserved at Guangdong Microbial Culture Collection Center on 4th, August, 2017, and the preservation number is GDMCC No:60217. The Excoecaria agallocha endophytic fungus sourced indene derivative is capableof inhibiting generation of LPS induced NO obviously, possesses clinical application potential in anti-inflammatory treatment, can be used for preparing anti-inflammatory drugs, and is promising in application prospect, the IC<50> is 8.5mM(1), 5.9mM(2), 4.2mN(3), and 4.2mM(4).

Description

technical field [0001] The invention belongs to the technical field of medical compounds. More specifically, it relates to a novel compound derived from endophytic fungus of sea lacquer, which belongs to indenoid derivatives, and its application in the preparation of anti-inflammatory drugs. Background technique [0002] Inflammation is an immune defense process adopted by the body when it is stimulated by exogenous antigens. The occurrence of inflammation will produce a series of complex changes in local tissues, mainly manifested as redness, swelling, heat, pain and dysfunction. At the same time, inflammation can cause systemic reactions, including fever, lethargy, and accelerated muscle protein degradation. When the body is invaded by inflammatory factors, it will activate monocytes and macrophages in the body to synthesize and release a variety of endogenous bioactive substances, such as prostaglandins, nitric oxide, vasoactive amines, etc., resulting in vascular permea...

Claims

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Application Information

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IPC IPC(8): C12N1/14C12P17/06C12R1/645
CPCC12P17/06C12N1/145C12R2001/645
Inventor 佘志刚崔辉潘亚宏黄锡山刘红菊李闯彪梅秀丽
Owner SUN YAT SEN UNIV
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