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Phthalide isoquinoline alkaloid as well as preparation method and application thereof

A technology of phthalide isoquinoline and alkaloid, which is applied in the field of phthalide isoquinoline alkaloid and its preparation, and can solve the problems of limited therapeutic effect, adverse reactions and the like

Inactive Publication Date: 2021-06-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, anticonvulsant drugs such as gabapentin are clinically used to treat neuropathic pain, but the therapeutic effect is limited and often accompanied by various adverse reactions

Method used

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  • Phthalide isoquinoline alkaloid as well as preparation method and application thereof
  • Phthalide isoquinoline alkaloid as well as preparation method and application thereof
  • Phthalide isoquinoline alkaloid as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] This example is used to illustrate the preparation process and structure identification of phthalide isoquinoline alkaloid corydecumbine G.

[0038] 1. The extraction, separation and purification process of the new natural product phthalide isoquinoline alkaloid corydecumbine G is as follows:

[0039] Take 35Kg of dry summer rhizomes, extract with 100L of 95% ethanol under reflux, recover ethanol under reduced pressure to obtain extract, and the pressure under reduced pressure is -0.1MPa.

[0040] The extract is completely dissolved with 20L of 3% tartaric acid solution, filtered to remove insoluble matter, and the filtrate is extracted with 20L ethyl acetate and then washed with Na 2 CO 3 Adjust the pH to 9, extract with 20L chloroform until the addition of potassium bismuth iodide has no precipitation, that is, no alkaloid reaction, then extract with 20L n-butanol, and recover the solvent to obtain ethyl acetate extract and chloroform extraction respectively substan...

Embodiment 2

[0051] This example is used to illustrate the inhibitory effect of the natural product phthalide isoquinoline alkaloid corydecumbine G on the excitability of cerebral cortex neurons provided by the present invention.

[0052] 1. Isolation and culture of primary neurons in cerebral cortex:

[0053] Pregnant C57BL / 6 mice that were pregnant for 15 to 16 days were killed by decapitation, soaked in 75% ethanol for about 10 minutes for disinfection, and the abdominal cavity of the female mice was opened in a biological safety cabinet to take out the fetuses. The whole brain of the fetal mouse was taken out, and the meninges and non-cortical parts were peeled off under a dissecting microscope to obtain the cerebral cortex, which was digested with trypsin at 37°C for 25 minutes. In the dissection buffer containing Soybean Trypsin Inhibitor and DNase I, the cortex was blown into a single cell suspension, and the cell suspension was centrifuged (1000rpm / 5min), and resuspended with Neuro...

Embodiment 3

[0061] This example is used to illustrate that the natural product phthalide isoquinoline alkaloid corydecumbine G provided by the present invention can restore mechanical pain and heat hypersensitivity in CCI rats.

[0062] 1. Establishment of sciatic nerve chronic compression model and animal grouping

[0063] Rats were anesthetized by intraperitoneal injection of 1% pentobarbital sodium (6mL / kg), placed in a prone position, scraped and incised the left thigh skin, bluntly separated the biceps femoris, exposed the trunk of the sciatic nerve, and used 4-0 The trunk of the sciatic nerve was ligated with chrome catgut for 4 circles with a distance of 1 mm between each circle, and the sciatic nerve was ligated until its outer membrane was slightly depressed (slight tremor of the posterior calf muscle could be seen). The sciatic nerve was reset, the skin was sutured, and penicillin sodium (200,000 U) was intramuscularly injected to prevent surgical infection in rats (ie, the left...

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PUM

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Abstract

The invention discloses a phthalide isoquinoline alkaloid as well as a preparation method and an application thereof, the phthalide isoquinoline alkaloid is a new natural product extracted and separated from a traditional Chinese medicine corydalis amabilis, and is named as corydecumbine G, and the structural formula is shown as formula (I). The phthalide isoquinoline alkaloid corydecumbine G is a brand new inhibitor developed based on inhibition of neuronal excitability, and experiments prove that the phthalide isoquinoline alkaloid corydecumbine G can significantly inhibit neuronal excitability and improve neuropathic pain, can be used as a lead compound, and can be used for preparation of drugs for inhibiting neuronal excitability and research and development of drugs for treating neuropathic pain.

Description

technical field [0001] The invention relates to the field of natural medicines, and specifically discloses a new phthalide isoquinoline alkaloid, a preparation method and application thereof. Background technique [0002] Neuropathic pain is a common chronic pain caused by abnormal function or structural damage of the peripheral or central nervous system, mainly manifested as allodynia, hyperalgesia and spontaneous pain, affecting 7% to 10% of the world's population , seriously endangering human health, because of its long duration and repeated attacks, it has brought great pain to patients and their families. At present, anticonvulsant drugs such as gabapentin are used clinically to treat neuropathic pain, but the therapeutic effect is limited and often accompanied by various adverse reactions. [0003] The occurrence and maintenance of neuropathic pain mainly depend on peripheral sensitization and central sensitization. When the nervous system is damaged, the damaged neur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04A61P25/04
CPCC07D493/04A61P25/04
Inventor 张春磊曹征宇刘菊张心怡
Owner CHINA PHARM UNIV
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