CN108815155A - Rotenone is preparing the application in medicament for treating systemic lupus erythematosus - Google Patents
Rotenone is preparing the application in medicament for treating systemic lupus erythematosus Download PDFInfo
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- CN108815155A CN108815155A CN201810962043.6A CN201810962043A CN108815155A CN 108815155 A CN108815155 A CN 108815155A CN 201810962043 A CN201810962043 A CN 201810962043A CN 108815155 A CN108815155 A CN 108815155A
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- rotenone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Abstract
The present invention relates to rotenone to prepare the application in medicament for treating systemic lupus erythematosus, belongs to field of traditional Chinese medicine pharmacy.Rotenone is able to suppress the generation of lupus mice antinuclear antibodies; alleviate lupus mice myocardial damage; inhibit lupus mice bone-marrow-derived lymphocyte abnormal activation and spleen enlargement, lupus mice lymph node tumour is inhibited to be formed, to provide a kind of new drug candidate in Therapy for Systemic Lupus Erythematosus.
Description
Technical field
The present invention relates to the application of rotenone in medicine preparation, and in particular to rotenone is in preparation treatment system erythema
Application in lupus drug.
Background technique
Systemic loupus erythematosus (Systemic lupus erythematosus, SLE) is a kind of the chronic multiple of multisystem
Hair property autoimmune disease, complicated clinical manifestation show as multiple organ and are damaged, including heart, lung, skin, immune system etc..
The main pathological characteristics of SLE be generate autoantibody and immune complex precipitating, can be detected in patients serum it is a variety of from
Body antibody, wherein using antinuclear antibodies as main representative.China SLE patient is about 1,000,000, illness rate office the second in the world, and is surpassed
There is hematological system involvement in the patient for crossing 50%.It is related to immune system disorder, science of heredity and environmental factor Various Complex in view of SLE
Mechanism is directed to SLE still drug or treatment means without radical cure at present.Therefore the drug of novel therapeutic system lupus erythematosus is developed
It is the key that clinical research.
Rotenone (Rotenone, molecular formula C23H22O6) is primarily present in the produced pulse family trifoliate jewelvine platymiscium in subtropical zone area
Root also separates in some Chinese herbal medicines such as thickfruit millettia seed or fruit, wayaka yambean seed leatherleaf millettia root.Start after the 1940s
It is widely used in agricultural as insecticide, there is the characteristics of not soluble in water, to be dissolved in carbon tetrachloride, acetone, chloroform, alcohol, ether.Highly
It is fat-soluble to make rotenone need not rely on Dopamine Transporter to be directly entered in cytoplasm by biomembrane.Rotenone is line
One of the classical inhibitor of complex I on mitochondrial respiratory chain, is highly efficient depressor of the nadh dehydrogenase to ubiquinone oxide-reductase enzyme,
Can disorder mitochondrial function, increase the generation of ROS, oxidative damage protein, lipid, nucleic acid, so as to cause cell to the benefit of oxygen
With obstacle, enough energy cannot be generated.
Summary of the invention
The present invention in order to solve the above technical problems, provides rotenone in preparing medicament for treating systemic lupus erythematosus
Application, to provide a kind of new drug candidate in systemic lupus erythematosus.
The technical solution that the present invention solves above-mentioned technical problem is as follows：Rotenone is preparing systemic lupus erythematosus medicine
Application in object.
Application described above, the specific can be that rotenone inhibits the anti-core of systemic loupus erythematosus disease blood serum in preparation
Application in antibody tormation drug.
The specific can be that rotenone alleviates answering in systemic loupus erythematosus disease myocardial function damage medicine in preparation
With.
The specific can be that rotenone preparation inhibit systemic loupus erythematosus disease spleen bone-marrow-derived lymphocyte abnormal activation and
Application in spleen enlargement drug.
The specific can be that application of the rotenone in preparation inhibition systemic loupus erythematosus Diseases Tumor is formed.
Further, rotenone the specific can be that is made the drug of systemic lupus erythematosus by above-mentioned described application
Or pharmaceutical composition.
The solution have the advantages that rotenone can inhibit lupus mice using MRL/Ipr lupus mice as research object
Lupus mice myocardial damage is alleviated in the generation of antinuclear antibodies, inhibits lupus mice bone-marrow-derived lymphocyte abnormal activation and spleen enlargement,
Lupus mice lymph node tumour is inhibited to be formed, to provide a kind of new drug candidate in Therapy for Systemic Lupus Erythematosus.
Detailed description of the invention
Fig. 1 is influence of the rotenone of the present invention to MRL/Ipr lupus mice serum antinuclear antibodies, and ordinate is antinuclear antibodies
Concentration；
Fig. 2 is influence of the rotenone of the present invention to MRL/Ipr lupus mice LDH, and ordinate is the concentration of LDH；
Fig. 3 is influence of the rotenone of the present invention to MRL/Ipr lupus mice AST, and ordinate is the concentration of AST；
Fig. 4 is influence of the rotenone of the present invention to MRL/Ipr lupus mice Spleen Size；
Fig. 5 is the influence that activate to MRL/Ipr lupus mice bone-marrow-derived lymphocyte of rotenone of the present invention, ordinate for B220 with
CD69 double positive cells account for the ratio of all spleen cells；
Fig. 6 is the influence that rotenone of the present invention forms MRL/Ipr lupus mice lymph node tumour.
Specific embodiment
Principles and features of the present invention are described below in conjunction with drawings and the specific embodiments, example is served only for solving
The present invention is released, is not intended to limit the scope of the present invention.
Rotenone in the present invention is purchased from Sigma company, and model of systemic lupus erythematosus is MRL/Ipr mouse model, purchase
From the livid purple blue Science and Technology Ltd. in Nanjing.
The female MRL/Ipr mouse for choosing 9 weeks or so, is divided into model group (SLE) and dosing group (SLE+Rotenone), together
When choose same strain normal female mouse of the same age as a control group (Control), SPF rank carry out conventinal breeding, from the 23rd
Week 100ppm rotenone is added in the food of dosing group mouse feeding, dosing group mouse is treated, model group and right
According to rotenone is not added in group food, raise to the 33rd week.
1 rotenone of embodiment inhibits the generation of antinuclear antibodies in MRL/Ipr lupus mice serum
Take raising to the 33rd week model group, dosing group and control group mice respectively, every group takes mouse 8, anesthetized mice
Blood is taken by inferior caval vein afterwards, is placed in anticoagulant tube, serum is centrifugated after being stored at room temperature 30 minutes, using anti-dsDNA-
Antibody kit detects the concentration of antinuclear antibodies in serum, and concrete operation step is referring to kit specification.As a result such as Fig. 1
Shown, the mean concentration of antinuclear antibodies is respectively 424IU/mL, 1602IU/ in control group, model group and dosing group mice serum
ML and 681IU/mL, antinuclear antibodies concentration is apparently higher than control group (p=0.033 in model group mice serum<0.05), dosing
Antinuclear antibodies concentration significantly reduces (p=0.048 compared with model group in group mice serum<0.05), there is statistical difference, it was demonstrated that fish
Rattan ketone can inhibit the generation of antinuclear antibodies in MRL/Ipr lupus mice serum.
2 rotenone of embodiment alleviates the myocardial function damage of MRL/Ipr lupus mice
Take raising to the 33rd week model group, dosing group and control group mice respectively, every group takes mouse 8, anesthetized mice
Blood is taken by inferior caval vein afterwards, is placed in anticoagulant tube, serum is centrifugated after being stored at room temperature 30 minutes, is detected through Biochemical Analyzer
The concentration of lactic dehydrogenase (LDH) and glutamic-oxalacetic transaminease (AST) in serum, as a result as shown in Figures 2 and 3, control group, model group
Mean concentration with LDH in dosing group mice serum is respectively 577U/L, 1312U/L and 487U/L, control group, model group and is added
The mean concentration of AST is respectively 73U/L, 223U/L and 81U/L in medicine group mice serum, LDH in model group mice serum and
AST concentration is apparently higher than control group, and LDH the and AST concentration of dosing group mice serum is significantly reduced compared with model group.Due to lactic acid
The raising of the concentration of dehydrogenase and glutamic-oxalacetic transaminease and myocardial function damage are closely related, hence it is demonstrated that rotenone can alleviate MRL/
The myocardial function of Ipr lupus mice damages.
3 rotenone of embodiment inhibits MRL/Ipr lupus mice spleen bone-marrow-derived lymphocyte abnormal activation and spleen enlargement
Take raising to the 33rd week model group, dosing group and control group mice respectively, every group takes mouse 5, separating mouse
Spleen observes Spleen Size, and as described in Figure 4, the spleen of the mouse of dosing group obviously becomes smaller compared to model group.Simultaneously by spleen grinding
200 meshes are crossed, pre-cooled PBS obtains single cell suspension after rinsing, after erythrocyte cracked liquid splitting erythrocyte, using difference
The B220 antibody and CD69 antibody of fluorescent marker are dyed, and 4 DEG C are protected from light incubation 30min, thin through streaming after cleaning 3 times with PBS
Born of the same parents' instrument detect and count the cell quantity of the bis- positives of B220 and CD69 and B220 and CD69 double positive cells to account for all spleens thin
The ratio of born of the same parents, as a result as shown in figure 5, in control group, model group and dosing group mouse B220 and CD69 double positive cells account for it is all
The ratio of spleen cell is respectively 0.6%, 6.8% and 4.37%, since CD69 is the mark of bone-marrow-derived lymphocyte activation, model group
The quantity of mouse spleen activation of B lymphocytes is significantly more than control group mice, and the activation of B lymphocytes of dosing group compares model group
Reduce 33% (p=0.047<0.05) left and right has statistical difference, it was demonstrated that rotenone can inhibit MRL/Ipr lupus mice
Spleen bone-marrow-derived lymphocyte abnormal activation and spleen enlargement.
4 rotenone of embodiment inhibits MRL/Ipr lupus mice lymph node tumour to be formed
The model group raised to the 33rd week and dosing group mouse are taken respectively, and every group takes mouse 5, the subcutaneous lymph of separating mouse
Tumour is tied, the size of lymph node tumour is observed, as shown in fig. 6, the lymph node tumor size of dosing group mouse is significantly less than model
Group mouse, it was demonstrated that rotenone inhibits MRL/Ipr lupus mice lymph node tumour to be formed.
Above-mentioned each embodiment passes through multiple authentication, and rotenone can reach above-mentioned experiment effect.
The foregoing is merely presently preferred embodiments of the present invention, is not intended to limit the invention, it is all in spirit of the invention and
Within principle, any modification, equivalent replacement, improvement and so on be should all be included in the protection scope of the present invention.
Claims (5)
1. rotenone is preparing the application in medicament for treating systemic lupus erythematosus.
2. application according to claim 1, which is characterized in that inhibit the anti-core of systemic loupus erythematosus disease blood serum in preparation
Application in antibody tormation drug.
3. application according to claim 1, which is characterized in that alleviate systemic loupus erythematosus disease myocardial function in preparation
Application in damage medicine.
4. application according to claim 1, which is characterized in that inhibit systemic loupus erythematosus disease spleen B leaching in preparation
Application in bar cell abnormal activation and spleen enlargement drug.
5. application according to claim 1, which is characterized in that inhibit systemic loupus erythematosus Diseases Tumor to be formed in preparation
Application in drug.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810962043.6A CN108815155A (en) | 2018-08-22 | 2018-08-22 | Rotenone is preparing the application in medicament for treating systemic lupus erythematosus |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810962043.6A CN108815155A (en) | 2018-08-22 | 2018-08-22 | Rotenone is preparing the application in medicament for treating systemic lupus erythematosus |
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|---|---|
| CN108815155A true CN108815155A (en) | 2018-11-16 |
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| CN201810962043.6A Pending CN108815155A (en) | 2018-08-22 | 2018-08-22 | Rotenone is preparing the application in medicament for treating systemic lupus erythematosus |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115281152A (en) * | 2022-08-12 | 2022-11-04 | 浙江中医药大学 | Method for constructing mouse lupus encephalopathy model |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999062510A2 (en) * | 1998-06-01 | 1999-12-09 | Angiotech Pharmaceuticals, Inc. | Compositions comprising anti-microtubule agents for treating or preventing inflammatory diseases |
| US20160008376A1 (en) * | 2014-07-10 | 2016-01-14 | Biocopea Limited | Compositions, Methods and Uses for Treating Gender-Biased Immune Disorders |
-
2018
- 2018-08-22 CN CN201810962043.6A patent/CN108815155A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999062510A2 (en) * | 1998-06-01 | 1999-12-09 | Angiotech Pharmaceuticals, Inc. | Compositions comprising anti-microtubule agents for treating or preventing inflammatory diseases |
| US20160008376A1 (en) * | 2014-07-10 | 2016-01-14 | Biocopea Limited | Compositions, Methods and Uses for Treating Gender-Biased Immune Disorders |
Non-Patent Citations (1)
| Title |
|---|
| GARY S. GILKESON等: "Endothelial Nitric Oxide Synthase Reduces Crescentic and Necrotic Glomerular Lesions, Reactive Oxygen Prouction, and MCP 1 Production in Murine Lupus Nephritis", 《PLOS ONE》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115281152A (en) * | 2022-08-12 | 2022-11-04 | 浙江中医药大学 | Method for constructing mouse lupus encephalopathy model |
| CN115281152B (en) * | 2022-08-12 | 2024-03-12 | 浙江中医药大学 | Method for constructing mouse lupus encephalopathy model |
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Application publication date: 20181116 |
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| RJ01 | Rejection of invention patent application after publication |