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Mixed-element terpene compound and preparation method and application thereof

A technology of terpenoids and compounds, applied in the field of medicine, can solve problems such as the regulation of neuronal excitability by mixed terpenoids

Pending Publication Date: 2020-07-03
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

There is no report on the regulation of neuronal excitability by mixed terpenoids
So far, there are no reports about the isolation of sulphane mixed terpenoids from this genus of fungi or the regulation of neuronal excitability

Method used

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  • Mixed-element terpene compound and preparation method and application thereof
  • Mixed-element terpene compound and preparation method and application thereof
  • Mixed-element terpene compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] The preparation of embodiment 1 mixed terpenoids

[0084] 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.

[0085] 2. Preparation of total crude extract

[0086] 12L 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 27 g of the total crude extract.

[0087] 3. Separation and purification

[0088] The total crude extract was separated by normal phase silica gel chromatography (200-300 mesh), and the 2 Cl 2 : MeOH=100:1-1:1 The eluent was used for gradient elution, and according to TLC monitoring, 11 partial eluates were collected according to the polarity difference of each fraction from small to large, and fraction 1-fraction 11 express.

[0089] Fraction 8 was passed through a Sephadex LH-20 gel column (mobile phase wa...

Embodiment 2

[0107] Example 2 Effects of Compounds of the Present Invention on the Spontaneous Synchronous Calcium Oscillation of Mouse Primary Cortical Neurons

[0108] 1. Isolation and culture of mouse cerebral cortex neurons

[0109] 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 relates to a mixed-element terpene compound and an application thereof. The preparation method comprises the following steps: extracting and separating a Durimane Meroterpenoid compoundfrom fermentation liquor of South China Sea soft coral co-epiphytic fungi Alternanthera sp. The mixed-element terpenoid compound can effectively inhibit excitability of mouse primary cerebral cortex neurons, can relieve the stimulation effect of epilepsy inducer 4-aminopyridine on neurons, and can be used for development of neuroprotective drugs. The invention provides a lead compound and a novelactive skeleton for research and development of neuroprotective drugs, and is beneficial to development and utilization of marine medicinal resources.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a mixed terpene compound and a preparation method and application thereof. Background technique [0002] Mixed terpenoids are a kind of mixed natural small molecules whose structural fragments are derived from terpenes, and are mainly divided into polyketide-mixed terpenes and non-polyketide-mixed terpenes (Geris, R.; Simpson, T.J.; Nat.Prod.Rep.2009,26,1063-1094;Wen,H.;Yang,X.;Liu,Q.;Li,S.;Li,Q.;Zang,Y.;Chen,C.;Wang , J.; Zhu, H.; Zhang, Y.J. Nat. Prod. 2020, 83, 99-104; Matsuda, Y.; Abe, I. Nat. Prod. Rep. 2016, 33, 26-53). The mixed source terpenoids of botanane are widely distributed in sponges, algae and fungi of marine origin. These compounds usually have phenol or quinone / hydroquinone groups attached to their sulphane backbone, which have a wide range of biological activities, such as antibacterial, antiviral, cytotoxic, osteoclast differentiation inhibition...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C323/52C07C319/20C07D493/04C07D303/32A61P25/08C12P11/00C12P17/18C12R1/645
CPCC07C323/52C07D493/04C07D303/32A61P25/08C12P11/00C12P17/181
Inventor 张文王洪亮李冉李娇
Owner 子辰海洋医药科技(上海)有限公司
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