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Cyathane diterpene compound and application thereof

The technology of a compound, ornithane, applied in the field of medicine, can solve problems such as short half-life, unsatisfactory pharmacokinetics, and large relative molecular weight, and achieve the effect of promoting synaptic growth and significant neurotrophic activity

Active Publication Date: 2020-12-18
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the pharmacokinetics of NGF is not ideal, the relative molecular weight is relatively large, and the half-life is short, so it is difficult to cross the blood-brain barrier and enter the central nervous system.

Method used

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  • Cyathane diterpene compound and application thereof
  • Cyathane diterpene compound and application thereof
  • Cyathane diterpene compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] preparation of

[0035] 1. Liquid fermentation culture

[0036] Saccharomyces cerevisiae LSc-1 was transferred to liquid YPD medium, and cultured at 30° C. and 200 rpm for 2 days to obtain a seed culture medium. The seed solution was inoculated into the YPD medium at a ratio of 1:1000 (each 1000mL Erlenmeyer flask was filled with 500mL YPD medium, and 10 Erlenmeyer flasks were set). Culture at 30° C. and 200 rpm for 5 days to obtain a fermentation broth.

[0037] YPD medium (natural pH): Peptone 20g, Yeast Extract 10g, glucose 20g, distilled water to 1L.

[0038] 2. Preparation of compounds

[0039] Take the fermentation broth obtained in step 1, add 500 ml of ethyl acetate to each Erlenmeyer flask for leaching at room temperature (20°C) for 24 hours (perform ultrasonic treatment every 12 hours during this period, and each ultrasonic treatment is 50 Hz continuous ultrasonic for 20 min) , take the supernatant; add 500 milliliters of new ethyl acetate to the remaini...

Embodiment 2

[0052] preparation of

[0053] 1. Liquid fermentation culture

[0054] Saccharomyces cerevisiae LSc-2 was transferred to liquid YPD medium, and cultured at 30° C. and 200 rpm for 2 days to obtain a seed culture solution. The seed solution was inoculated into the YPD medium at a ratio of 1:1000 (each 1000mL Erlenmeyer flask was filled with 500mL YPD medium, and 10 Erlenmeyer flasks were set). Culture at 30° C. and 200 rpm for 5 days to obtain a fermentation broth.

[0055] YPD medium (natural pH): Peptone 20g, Yeast Extract 10g, glucose 20g, distilled water to 1L.

[0056] 2. Preparation of compounds

[0057] Take the fermentation broth obtained in step 1, add 500 ml of ethyl acetate to each Erlenmeyer flask for leaching at room temperature (20°C) for 24 hours (perform ultrasonic treatment every 12 hours during this period, and each ultrasonic treatment is 50 Hz continuous ultrasonic for 20 min) , take the supernatant; add 500 milliliters of new ethyl acetate to the remai...

Embodiment 3

[0069] preparation of

[0070] 1. Liquid fermentation culture

[0071] Saccharomyces cerevisiae LSc-3 was transferred to liquid YPD medium, and cultured at 30° C. and 200 rpm for 2 days to obtain a seed culture medium. The seed solution was inoculated into the YPD medium at a ratio of 1:1000 (each 1000mL Erlenmeyer flask was filled with 500mL YPD medium, and 10 Erlenmeyer flasks were set). Culture at 30° C. and 200 rpm for 5 days to obtain a fermentation broth.

[0072] YPD medium (natural pH): Peptone 20g, Yeast Extract 10g, glucose 20g, distilled water to 1L.

[0073] 2. Preparation of compounds

[0074] Take the fermentation broth obtained in step 1, add 500 ml of ethyl acetate to each Erlenmeyer flask for leaching at room temperature (20°C) for 24 hours (perform ultrasonic treatment every 12 hours during this period, and each ultrasonic treatment is 50 Hz continuous ultrasonic for 20 min) , take the supernatant; add 500 milliliters of new ethyl acetate to the remaini...

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Abstract

The invention discloses a cyathane diterpene compound and application thereof. The cyathane diterpene compound provided by the invention has remarkable neurotrophic activity and can remarkably promotesynaptic growth of PC-12 nerve cells.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to ornithane-type diterpenoids, a preparation method, and an application in treating neurodegenerative diseases. Background technique [0002] Neurodegenerative disease (Neurodegenerative disease, NDD) refers to the disease caused by the degeneration of central and peripheral nervous tissue, including Alzheimer's disease (Alzheimer's disease, AD), Parkinson's disease (Parkinson's disease, PD), Huntington's dance Disease (Huntington's disease, HD) and amyotrophic lateral sclerosis (Amyotrophic lateral sclerosis, ALS) and so on. As the world's population ages, there is a marked increase in neurodegenerative diseases. There are currently 24 million patients suffering from AD and other dementias worldwide, while the incidence of PD is 4.5-19 / 100,000 people per year. Research reports show that the number of AD and PD patients in my country will rise sharply, becoming the country wit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C35/37C07H15/203A61P25/28A61P25/14A61P25/16A61P25/00A61K31/047A61K31/704C12P7/02C12P19/56C12R1/865
CPCC07C35/37C07H15/203A61P25/28A61P25/14A61P25/16A61P25/00C12P7/02C12P19/56C07C2603/30
Inventor 刘宏伟马轲宝丽
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI