Application of Ginsenosides in the Preparation of Molecular Targeted Therapy Drugs for Antiphospholipid Syndrome

A technology of molecular targeted therapy and ginsenosides, which can be used in drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of high recurrence rate of antiphospholipid antibody syndrome

Active Publication Date: 2018-10-02
延边安帝康华生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the above-mentioned drugs are not target-specific drugs, they are accompanied by relatively obvious side effects during the treatment process, and at the same time cannot solve the problem of high recurrence rate of antiphospholipid antibody syndrome

Method used

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  • Application of Ginsenosides in the Preparation of Molecular Targeted Therapy Drugs for Antiphospholipid Syndrome
  • Application of Ginsenosides in the Preparation of Molecular Targeted Therapy Drugs for Antiphospholipid Syndrome
  • Application of Ginsenosides in the Preparation of Molecular Targeted Therapy Drugs for Antiphospholipid Syndrome

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0030] Example 1 Safety Evaluation

[0031] The research results of the non-clinical safety evaluation of the present invention are as follows:

[0032] 1. Oral acute toxicity test in mice

[0033] Under the conditions of maximum dosage concentration and maximum dosage volume, mice were orally given (20S)-ginsenoside Rh212g / kg by gavage, and observed continuously for 14 days, no death or abnormal toxic reaction was found in the animals. Show that (20S)-ginsenoside Rh2 mice gavage maximum tolerated dose is 12g / kg.

[0034] 2. Beagle dog oral acute toxicity test

[0035] Under the conditions of the maximum dosage concentration and maximum dosage volume, Beagle dogs were given (20S)-ginsenoside Rh2 2g / kg orally by gavage, and observed continuously for 14 days. No death or abnormal toxic reaction was found in the animals. It shows that (20S)-ginsenoside Rh2Beagle canine gavage maximum tolerated dose is 2g / kg.

[0036] 3. Long-term toxicity of intragastric administration in rats ...

Embodiment 2

[0044] Embodiment 2 pharmacodynamic evaluation

[0045] Research result of the present invention is as follows:

[0046] 1. (20S)-ginsenoside Rh2 binds Annexin A2 and weakens its interaction with β 2 -GP1 interaction

[0047] Materials: recombinant human Annexin A2 protein, recombinant human β 2 -GP1 expressed in Escherichia coli and purified by high performance liquid chromatography; (20S)-ginsenoside Rh2 (China National Institutes for Food and Drug Control, purity: 99.0%, batch number: 111748).

[0048] method

[0049] 1.1. Dilute 100 μg recombinant human Annexin A2 protein and 10 μg (20S)-ginsenoside Rh2 in 1.5 mL phosphate buffer, without adding (20S)-ginsenoside Rh2 to the control group, incubate at 37°C for 1 hour, and dispense 100 μl / tube to 12 tubes, heat 12 tubes at different temperatures (heating temperatures are 40, 43, 46, 49, 52, 55, 58, 61, 64, 67, 70, 73°C) for 3 minutes, centrifuge at 20000×g for 20 minutes, SDS polyacrylamide gel electrophoresis detects t...

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Abstract

The invention relates to application of ginsenoside in the pharmacy field, in particular to application of ginsenoside in preparing antiphospholipid syndrome molecular targeting treatment medicine. In a laboratory antiphospholipid syndrome mouse model, the compound can effectively lower the level of anticardiolipin antibodies, anti-beta2-GP1 antibodies and lupus anticoagulants in blood; meanwhile, in a pregnant mouse model, the compound effectively lower aCL activation, shortens partial thromboplastin time and reduces the blood platelet count and the abortion rate; safety study shows that the compound is high in safety, has no influence on the central nervous system, the cardiovascular system and the respiratory system and has no mutagenic action. It is indicated that the compound has high safety and a good inhibiting effect on the antiphospholipid syndrome at the test dose and can be used for treating the antiphospholipid syndrome.

Description

technical field [0001] The invention relates to the use of chemical substances in the field of medicine. More specifically, it is the application of ginsenosides in the preparation of anti-phospholipid body syndrome molecular targeted therapy drugs. technical background [0002] Antiphospholipid syndrome (APS) is a general term for the clinical signs of autoimmunity caused by antiphospholipid antibody (antiphospholipid antibody, APL antibody). APL antibodies refer to antibodies that can immunoreact with antigenic substances containing phospholipid structures, mainly including lupus anti-coagulant (LAC), anti-cardiolipid antibody (ACL), anti-phosphatidic acid antibody And antiphosphatidylserine antibody, etc., the clinical manifestations related to APL antibody mainly include thrombosis, habitual abortion, and low platelets. The prevalence of primary antiphospholipid antibody syndrome is currently unknown. About 30% to 40% of antiphospholipid antibody-positive patients may...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/58A61K31/575A61P37/02A61P7/02A61P15/06A61P19/04
CPCA61K31/575A61K31/58
Inventor 金英花王宇石林英嘉李杨李赫
Owner 延边安帝康华生物科技有限公司
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