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Application of α-mangostin derivatives in the preparation of anti-cerebral palsy drugs and anti-cerebral palsy drug composition

A technology of mangostin and its derivatives, which is applied in the field of medicine, can solve the problems of unclear exact mechanism, achieve the effect of restoring the ability of learning and memory, improving the ability of gait balance, and broad application prospects

Active Publication Date: 2021-04-06
上海如凌生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To some extent, α-mangostin also reduces the gene expression of tumor necrosis factor TNF-α and interleukin IL-6, but the exact mechanism is still unclear

Method used

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  • Application of α-mangostin derivatives in the preparation of anti-cerebral palsy drugs and anti-cerebral palsy drug composition
  • Application of α-mangostin derivatives in the preparation of anti-cerebral palsy drugs and anti-cerebral palsy drug composition
  • Application of α-mangostin derivatives in the preparation of anti-cerebral palsy drugs and anti-cerebral palsy drug composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Effects of α-Mangostin Derivatives Administration on Morris Water Maze Test in Rats with Cerebral Palsy

[0036] 1. Animal groups: SD rats (6 days old, 12-18 g, 15 rats in each group), randomly divided into groups. The grouping is shown in Table 1.1.

[0037] Table 1.1 Animals and groups required in Example 1

[0038]

[0039] 2. Administration and dosage: α-mangostin derivatives with a purity of more than 99% are dissolved in ethyl oleate for injection, and the animals are administered by intraperitoneal injection. The dosage is: 5mg / kg, 10mg / kg, 20mg / kg; Positive drug ganglioside GM1 dose: 20 mg / kg, as a positive control; both the model group and the sham operation group were intraperitoneally injected with the same amount of solvent (ethyl oleate). Administration was administered at 9:00 every day, and the administration was continued for 20 days after modeling.

[0040] 3. Surgical procedure: After the animal is anesthetized, the neck skin is prepared, the nec...

Embodiment 2

[0044] Effects of administration of α-mangostin derivatives on foot fault behavior test in rats with cerebral palsy.

[0045] Animal grouping and dosage are the same as in Example 1. The foot fault test is completed by a stainless steel mesh with a diameter of 0.4cm and a single grid area of ​​3cm*3cm. The mesh surface was raised about 1m from the ground. In order to reduce accidental errors, each rat was placed on the mesh for 2 minutes to adapt. The rats would step on the steel bars as much as possible, and the rats with poor balance would step on the air. Record the number of times the rats made mistakes with the right forelimb in 50 steps of grid crawling, and the number of times with the right hind legs in 50 steps in another 5 min.

[0046] The experimental results showed that in the right forelimb test, the number of right forelimb mistakes in the model group was significantly increased compared with the sham operation group (P<0.001), and the 20mg / kg administration gr...

Embodiment 3

[0048] To observe the effect of administration of α-mangostin derivatives on the submicroscopic structure of neurons in rats with cerebral palsy.

[0049] After the rats were anesthetized with chloral hydrate, the brain tissue was separated after perfusion with 4% paraformaldehyde (0.1M phosphate buffer, PH=7.4), and the sampling site was determined to minimize mechanical damage such as stretching, contusion and extrusion. The volume of the tissue generally does not exceed 1mm×1mm×1mm, and it is quickly put into the electron microscope fixative solution and fixed at 4°C for 2-4h. The cells were centrifuged until mung bean-sized cell agglomerates could be seen at the bottom of the tube, the culture medium was discarded and the electron microscope fixative was added to fix at 4°C for 2-4h. Rinse 3 times with 0.1M phosphate buffered solution PBS (PH7.4), 15 min each time. 1% osmic acid 0.1M phosphate buffer PBS (pH7.4) fixed at room temperature (20°C) for 2h. Rinse 3 times with...

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Abstract

The invention discloses the application of an α-mangostin derivative in the preparation of an anti-cerebral palsy drug, and an anti-cerebral palsy drug composition. The active ingredient of the anti-cerebral palsy drug composition is an α-mangostin derivative. The application of the α-mangostin derivatives provided by the present invention in the preparation of anti-cerebral palsy drugs can restore the learning and memory ability reduction caused by hypoxia-ischemia combined with infection in the brain, improve the gait balance ability, and reduce the damage of neuron organelles.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the application of an α-mangostin derivative in the preparation of anti-cerebral palsy drugs and an anti-cerebral palsy drug composition. Background technique [0002] Cerebral palsy (CP) was first described in 1862 by orthopedic surgeon William Little. Recently, the International Cerebral Palsy Definition Executive Committee proposed the following definition: Cerebral palsy is a description of a group of disorders in the developing fetus or infant brain due to non-progressive brain damage, permanent impairment of movement and posture, causing activity restricted. Movement disturbances in cerebral palsy are often accompanied by disturbances in sensation, perception, cognition, communication, and behavior as well as epilepsy and secondary musculoskeletal problems. [0003] Treatment is mainly based on rehabilitation training combined with drugs, but there is no ideal drug for tre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P25/00
Inventor 陈艳李彩凤单伟光占扎君王建伟龚婷婷
Owner 上海如凌生物医药有限公司
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