CN-121987587-A - Ginsenoside Rg1 wrapped by neutrophil membrane vesicles and application thereof

Abstract

The invention relates to the technical field of medicines, and provides an application of ginsenoside Rg1 wrapped by a neutrophil-like membrane vesicle in preparing a medicine for treating or preventing cerebral apoplexy or demyelinating diseases. According to the invention, the DMSO is used for inducing HL-60 cells to differentiate into neutrophil-like granulocytes, a nitrogen cavitation device is used for preparing neutrophil-like granulocyte membrane vesicles, ginsenoside Rg1 is loaded into the vesicles, and a drug delivery system for targeting brain inflammatory diseases is constructed. Experiments prove that the neutrophil-like membrane vesicles have uniform particle size distribution and good inflammatory chemotaxis, brain targeting and biocompatibility. The ginsenoside Rg1 is wrapped by the neutrophil-like granulocyte membrane vesicle, so that the content of the Rg1 in the encephalitis of a mouse can be obviously improved, cerebral apoplexy damage is improved, nerve function recovery is promoted, the method is superior to free Rg1, demyelination damage is obviously improved, and the method is superior to free Rg1, and has obvious treatment effect on cerebral apoplexy or demyelination diseases.

Inventors

• CHEN NAIHONG
• ZHANG ZHAO
• CHU SHIFENG
• Hu Kaichao
• YAN XU
• WANG WANXUE
• Ye Junrui
• WANG HONGYUN

Assignees

• 中国医学科学院药物研究所

Dates

Publication Date

20260508

Application Date

20241107

Claims (5)

1. 1. Application of ginsenoside Rg1 or pharmaceutically acceptable salt thereof wrapped by neutrophil membrane vesicles in preparation of medicines for treating or preventing cerebral apoplexy or demyelinating diseases, wherein the ginsenoside Rg1 has the following structure:
2. 2. An application of a pharmaceutical composition in preparing a medicament for preventing or treating cerebral apoplexy or demyelinating diseases, which is characterized in that the pharmaceutical composition contains the neutral granulocyte membrane-like vesicle-wrapped ginsenoside Rg1 or pharmaceutically acceptable salt thereof according to claim 1,
3. 3. The stroke of claim 1 selected from the group consisting of ischemic stroke and hemorrhagic stroke.
4. 4. The use of stroke according to claim 1 selected from the group consisting of prophylaxis, acute phase, subacute phase, convalescence.
5. 5. The demyelinating disease of claim 1 selected from the group consisting of multiple sclerosis, neuromyelitis optica, acute disseminated encephalomyelitis, and demyelination associated with neurodegenerative diseases.

Description

Ginsenoside Rg1 wrapped by neutrophil membrane vesicles and application thereof Technical Field The invention mainly relates to ginsenoside Rg1 wrapped by a neutrophil membrane vesicle, which is used for preparing a medicament for treating or preventing cerebral apoplexy or demyelinating diseases, and belongs to the technical field of medicines. Background Cerebral tissue injury caused by cerebral vessel blockage or rupture and the like in cerebral apoplexy has the characteristics of high morbidity, high mortality, disability rate and the like, and causes heavy burden to society and families. At present, recombinant tissue plasminogen activator (rt-PA) is the only thrombolytic drug approved by the FDA, however, the application of rt-PA is limited by the disadvantages of short treatment time window and high bleeding risk. The search for effective therapeutic drugs has important significance in promoting functional repair after stroke. Myelin sheath is a membrane structure that wraps around the axons of neurons, which is the material basis for achieving rapid and accurate delivery of neural information. Demyelinating diseases can lead to dysfunction of nerve signaling, affecting white matter function, early symptoms including vision disorders and dyskinesias, etc. Although hormone therapy is a common method, the effect is limited, and long-term use can reduce immunity and increase recurrence risk. Therefore, there is an urgent need for therapeutic strategies in combination with the traditional chinese and western medicine to improve disease resistance and protect neurological function. Ginsenoside Rg1 (C 42H72O14, structural formula I) is a tetracyclic triterpene derivative, in vitro research shows that the ginsenoside Rg1 has good neuroprotective activity, however, the ginsenoside Rg1 has poor oral absorption, quick elimination and difficult permeation through a blood brain barrier, cannot reach high concentration in brain tissues, and can generate a treatment effect in animal experiments with very large dosage, thus preventing Rg1 from being used as a medicament for treating stroke and demyelinating diseases. Cerebral apoplexy and demyelinating diseases both trigger brain inflammatory reactions, and released inflammatory factors activate the expression of proteins such as neutrophil membrane surface integrin beta 2 and P-selectin glycoprotein ligand-1 (PSGL-1). Neutrophils bind to intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) expressed by inflammatory brain endothelial cells and infiltrate into the brain parenchyma. Using this property, drugs can be delivered to brain injury sites using neutrophil membrane encapsulation drugs. The envelope of the neutrophil membrane envelope ginsenoside Rg1 has not been reported at present, and the therapeutic effect of the neutrophil membrane envelope on cerebral apoplexy and demyelination has not been reported. The inventor finds that the content of Rg1 in the encephalitis of mice can be obviously improved, cerebral apoplexy damage is improved, nerve function recovery is promoted, the composition is superior to free Rg1, demyelinating damage is obviously improved, and the composition is superior to free Rg1, so that the composition has obvious treatment effect on cerebral apoplexy or demyelinating diseases. Disclosure of Invention The invention provides ginsenoside Rg1 wrapped by a neutrophil membrane vesicle and therapeutic application thereof. The therapeutic application is to prepare the medicine for treating or preventing cerebral apoplexy or demyelinating diseases. Therefore, the invention provides a novel ginsenoside Rg1 form and application thereof, namely, the compound Rg1 shown in the formula I is wrapped by a neutrophil-like membrane vesicle, and the ginsenoside Rg1 form is used for preparing a medicament for treating or preventing cerebral apoplexy or demyelinating diseases. The technical scheme of the invention provides application of the ginsenoside Rg1 wrapped by the neutrophil membrane vesicle in preparation of a medicine for treating or preventing cerebral apoplexy. Further, the cerebral apoplexy includes ischemic cerebral apoplexy and hemorrhagic cerebral apoplexy. Further, the application of the cerebral apoplexy comprises prevention, acute phase, subacute phase and recovery phase. Further, the demyelinating diseases include multiple sclerosis, neuromyelitis optica, acute disseminated encephalomyelitis, and demyelination associated with neurodegenerative diseases. Further, the effects of the compound Rg1 include therapeutic effects, as well as prophylactic effects; The technical scheme of the invention provides application of a pharmaceutical composition in preparing medicines for treating or preventing cerebral apoplexy and demyelinating diseases. The medicine composition is characterized by comprising the ginsenoside Rg1 wrapped by the neutrophil-like membrane vesicles. The pharmaceutical compositions may be