Biphenyl compound and diterpenoid compound as well as preparation method and application thereof

A kind of technology of compound and diterpenoid, applied in the field of biphenyl compounds

Active Publication Date: 2021-08-06
子辰海洋医药科技(上海)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] There are no reports on the isolation of biphenyls and diterpenoids that can regulate neuronal excitability from this fungus

Method used

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  • Biphenyl compound and diterpenoid compound as well as preparation method and application thereof
  • Biphenyl compound and diterpenoid compound as well as preparation method and application thereof
  • Biphenyl compound and diterpenoid compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] The preparation of embodiment 1 biphenyl compound and diterpenoid compound

[0056] 1. Preparation of strain fermentation broth: inoculate the strain into biomalt extract (biomalt) agar (agar) medium (3% biomalt, 2% agar), and ferment at 28° C. for 28 days.

[0057] 2. Preparation of total crude extract

[0058] 20L of the fermentation liquid of the strain was subjected to conventional ethyl acetate ultrasonic extraction, and the extract was concentrated under reduced pressure to obtain 13.6 g of the total crude extract.

[0059] 3. Separation and purification

[0060] The crude extract was subjected to normal-phase silica gel column chromatography (200-300 mesh), and gradient elution was carried out with dichloromethane / methanol system (v / v 100:0, 100:1, 80:1, 60:1, 40:1 , 30:1, 20:1, 10:1, 4:1), the fractions were collected and combined by TLC analysis to obtain 13 fractions (Fr.1~Fr.13).

[0061] Component Fr.2 (52.7mg) was subjected to Sephadex LH-20 gel column c...

Embodiment 2

[0128] Example 2 Effects of Compounds of the Present Invention on the Spontaneous Synchronous Calcium Oscillation of Mouse Primary Cortical Neurons

[0129] 1. Isolation and culture of mouse cerebral cortex neurons

[0130] For the isolation and culture of C57Bl / 6J mouse cerebral cortex neurons, see references (Zheng, J.; Yu, Y.; Feng, W.; Li, J.; Liu, J.; Zhang, C.; Dong, Y. .; Pessah, IN.; Cao, Z. Environmental Health Perspectives 2019, 127, 67003). The 0-1 day old suckling mice were taken out, their heads were decapitated, and their brains were taken. The cerebral cortex was separated under a dissecting microscope, and the meninges were carefully peeled off. After being blown away with a Pasteur pipette, trypsin was digested at 37°C for 25 minutes. In the dissection buffer containing trypsin inhibitor (soybean) and deoxyribonuclease I, the cortex was blown into a single cell suspension, and the cell suspension was centrifuged (1000rmp / 5min). Resuspend with Neuron Plating...

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Abstract

The invention provides a biphenyl compound and a diterpenoid compound which are extracted from fermentation liquor of fungus Aspergillus candidus, the biphenyl compound and the diterpenoid compound are used as novel neuron calcium oscillation regulators for activity research, and results show that the biphenyl compound and the diterpenoid compound can effectively influence excitability of primary cerebral cortical neurons of mice, can relieve the stimulation effect of an epilepsy inducer 4-amino pyridine on neurons, and can be used for preparing neuro-protective drugs. Therefore, the invention provides a lead compound for the development of neuro-protective drugs, and is beneficial to the development and utilization of natural medicinal resources.

Description

technical field [0001] The invention belongs to the field of medical technology, and in particular relates to biphenyl compounds and diterpenoids derived from the fermentation liquid of fungus Aspergillus candidus, a preparation method thereof and an application in the field of research and development of neuroprotective drugs. Background technique [0002] The host coral Junceelafragillis is a marine invertebrate belonging to the whip gorgonian family Cord gorgonian. There are many studies on the coral Junceelafragillis, but less research on the chemical components of its symbiotic microorganisms. The compounds that have been isolated from this species of gorgonian are mainly terpenoids (see Ping-Jyun S, Su-Hui W for details. ,Chiang MY,et al.Discovery of New Chlorinated Briaranes from Junceella fragilis[J].Bull.Chem.Soc,2009,82(11):1426-1432; Sung P J,Lin M R,Chen W C,etal.Fragile A, a Novel Diterpenoid from Junceella fragilis[J].Cheminform,2010,35(6):1229-1230; García,Mi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C43/23C07C41/36C07D307/91C07D307/80C07D307/79C07D491/052C07D491/20C12N1/14C12P17/18C12P17/04C12P7/22A61K31/09A61K31/343A61K31/407A61P25/00A61P25/08C12R1/66
CPCC07C43/23C07D307/91C07D307/80C07D307/79C07D491/052C07D491/20C12N1/14C12P17/18C12P17/04C12P7/22A61P25/00A61P25/08Y02A50/30
Inventor 张文彭高杨
Owner 子辰海洋医药科技(上海)有限公司
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