Application of sphaelactone and derivatives thereof in treatment of traumatic craniocerebral injury

A craniocerebral injury and derivative technology, applied in the field of medicine, can solve problems such as restraint

Pending Publication Date: 2022-02-08
SHANGHAI SIXTH PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned efforts are only remedial treatment measures taken against the evil consequences caused by primary injury, and a series of pathological changes (secondary injury) caused by central nervous system injury, especially for TBI-mediated For the treatment of neuroinflammatory reactions in patients with neuropathy, most of them choose palliative and supportive therapy, which cannot be effectively curbed from the root cause. This has always been the Achilles' heel in TBI treatment strategies, and it is also an urgent problem to be solved on the road to TBI treatment in recent years. One of the hot issues

Method used

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  • Application of sphaelactone and derivatives thereof in treatment of traumatic craniocerebral injury
  • Application of sphaelactone and derivatives thereof in treatment of traumatic craniocerebral injury
  • Application of sphaelactone and derivatives thereof in treatment of traumatic craniocerebral injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] The preparation of embodiment 1 Milicolactone (MCL)

[0061] Take Taiwan Michelle as raw material, crush it into 20-40 meshes, put it into the extraction kettle, use anhydrous methanol as entrainer, and use supercritical CO 2 Extraction, collect the extract, recover methanol to obtain the extract, reflux with petroleum ether to remove fat-soluble impurities, then heat-dissolve the degreased matter with low-carbon alcohol, add activated carbon to reflux for decolorization, and recover the solvent to an appropriate volume from the decolorization solution. Purify with an ODS RP-C18 reverse-phase column, elute with a mixed solution of methanol and water, concentrate the corresponding components, and recrystallize from petroleum ether-acetone (2:1, V / V) to obtain the MCL product. The supercritical CO 2 The extraction conditions are that the extraction temperature is 45-60°C, the extraction pressure is 23-34MPa, the temperature of the separation tank I is 40-50°C, and the pr...

Embodiment 2

[0062] The preparation of embodiment 2 migna lactone derivatives (ACT001)

[0063] The preparation method of mimilactone derivative (ACT001): the Me 2 NH·HCl (1.5g, 18mmol), K 2 CO 3 (5.0g, 36mmol) and CH 2 Cl 2 (100 ml) were mixed at room temperature and a homogeneous solution was formed. Then MCL (300mg, 1.2mmol) was mixed with the homogeneous solution, and stirred at room temperature for 3h. The above reaction solution was used CH 2 Cl 2 After concentrating and resuspending, use deionized water chromatography to separate, and the obtained separation liquid is separated by Na 2 SO 4 Drain. The filtered material was washed with CH 2 Cl 2 (5ml) was dissolved and treated with fumarate (0.1N) to adjust the pH of the solution to 4. Finally use CH 2 Cl 2 (10ml) to extract the aqueous phase and freeze-dry to obtain compound ACT001. The drug wwACT001 in this experiment was dissolved in deionized water to form a 400mg / ml stock solution, which was then stored in a -80°C...

Embodiment 3

[0064] Example 3 Establishment of Mouse Controlled Cortical Impact (CCI, Controlled Cortical Impact) Model

[0065] Male C57BL / 6J mice (provided by Shanghai Slack Experimental Animal Co., Ltd., 8-10 weeks old, weighing 20-25 g). 0.6% pentobarbital solution, 80mg / kg, intraperitoneally inject anesthetized mouse; Mouse is fixed in brain stereotaxic apparatus (Stoeling Inc.USA); Make a midline incision, separate the scalp, and peel off the periosteum; make a skull burr hole 1.5-2 mm away from the midline between the right coronal suture and herringbone suture, and make a bone window with a diameter of about 4 mm to expose the complete dura mater; apply PinPoint TM PCI3000 fine craniocerebral impactor (Hatteras Instruments Inc. USA) set the impact parameters, and used the impact head with a diameter of 3mm to accurately impact the mouse cerebral cortex. Among them, the strike depth in the experiment is 1.5mm; the strike time is 100ms; the strike speed is 1.5m / s. Bleeding was stop...

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Abstract

The invention relates to an application of sphaelactone or a derivative thereof or a pharmaceutically acceptable salt thereof in preparation of a medicine for treating traumatic craniocerebral injury, and the specific mechanism is that sphaelactone or a derivative thereof or a pharmaceutically acceptable salt thereof can be used for treating the traumatic craniocerebral injury by inhibiting the inflammatory effect of microglial cells after the traumatic craniocerebral injury. The damage of the blood brain barrier and the apoptosis and necrosis of neurons are relieved, and finally the effects of relieving intracranial progressive hemorrhage after trauma and promoting neurological function repair are achieved.

Description

technical field [0001] The present invention relates to the field of medicines, in particular to the reduction of the destruction of the blood-brain barrier and the apoptosis and necrosis of neurons by inhibiting the inflammatory effect of microglial cells in the treatment of traumatic craniocerebral injury diseases by mimilactone and its derivatives , and finally achieve the relief of progressive intracranial hemorrhage after trauma, and promote new applications in neurological function restoration. Background technique [0002] Natural products are of great significance for the discovery, design and synthesis of new drugs, and are also an important source of biologically active substances and innovative drugs. Approved drugs such as Taxol, Docetaxel, Vinorelbine ( Vinorelbine), hydroxycamptothecin (camptothecin), artemisinin (Artemisinin) etc. are all derivatives or analogues of natural products. Natural products play a unique role in the development of drug sources, from...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P25/00A61P7/04A61P29/00
CPCA61K31/365A61P25/00A61P7/04A61P29/00
Inventor 田恒力蔡霖田春祺龚秋源陈浩袁方丁军
Owner SHANGHAI SIXTH PEOPLES HOSPITAL
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