Use of ptilumine e in the preparation of a medicament for treating diabetic retinopathy

Abstract

The application discloses application of pinaite E in preparation of a medicine for treating diabetic retinopathy and belongs to the technical field of natural medicines. The application of pinaite E in preparation of the medicine for treating diabetic retinopathy. The application of pinaite E or pharmaceutically acceptable salts thereof in preparation of the medicine for treating diabetic retinopathy. The pharmaceutically acceptable salt is a salt formed by pinaite E and an organic base or an inorganic base. The salt is a sodium salt, a potassium salt, a calcium salt, an iron salt, a magnesium salt, a zinc salt, an aluminum salt, a barium salt or an ammonium salt. A medicine for treating diabetic retinopathy contains pinaite E as an active ingredient and pharmaceutically acceptable adjuvants and is prepared into a pharmaceutically acceptable dosage form. The application finds that pinaite E has a significant effect on treating diabetic retinopathy, and lays a foundation for development and utilization of pinaite and pinaite E.

Description

Technical Field

[0001] This invention relates to the application of a physostigmine E in the preparation of a drug for treating diabetic retinopathy, belonging to the field of natural medicine technology. Background Technology

[0002] The Chinese name of 2-(4-(2,4-dimethoxybenzoyl)phenyl)-N-(2-methoxyphenyl)acetamide and the English name of 2-(4-(2,4-dimethoxybenzoyl)phenyl)-N-(2-methoxyphenyl)acetamide are benzophenone compounds isolated from *Bryophytum comosum* var. *truncatum*. This compound has good anti-colon cancer activity.

[0003] This invention is proposed to develop and expand its medicinal applications. Summary of the Invention

[0004] To address the above-mentioned problems, the purpose of this invention is to provide an application of physostigmine E in the preparation of a drug for treating diabetic retinopathy.

[0005] To solve the above-mentioned technical problems, the technical solution adopted by the present invention is as follows:

[0006] Application of physostigmine E in the preparation of drugs for the treatment of diabetic retinopathy.

[0007] The structural formula of goldenrodone E is as follows:

[0008]

[0009] Use of physostigmine E or a pharmaceutically acceptable salt thereof in the preparation of drugs for the treatment of diabetic retinopathy.

[0010] Pharmaceutically acceptable salts are those formed by the reaction of physostigmine E with organic or inorganic bases.

[0011] Salts can be sodium, potassium, calcium, iron, magnesium, zinc, aluminum, barium, or ammonium salts.

[0012] The drug uses physostigmine E as its active ingredient and also contains pharmaceutically acceptable excipients, and is formulated into a pharmaceutically acceptable dosage form.

[0013] The excipients include any one or more of the following: solvents, propellants, solubilizers, cosolvents, emulsifiers, colorants, binders, disintegrants, fillers, lubricants, wetting agents, osmotic pressure regulators, stabilizers, flow aids, flavoring agents, preservatives, suspending agents, coating materials, fragrances, anti-adhesion agents, binding agents, penetration promoters, pH adjusters, buffers, plasticizers, surfactants, foaming agents, defoamers, thickeners, encapsulating agents, humectants, absorbents, diluents, flocculants, anti-flocculation agents, filter aids, and release inhibitors.

[0014] Dosage forms include tablets, capsules, injections, and oral solutions.

[0015] A drug for treating diabetic retinopathy, prepared from physostigmine E or a pharmaceutically acceptable salt thereof.

[0016] A drug for treating diabetic retinopathy, with physostigmine E as the active ingredient, also containing pharmaceutically acceptable excipients, and formulated into a pharmaceutically acceptable dosage form.

[0017] The use of physostigmine E or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating retinopathy.

[0018] A drug for treating retinopathy, prepared from physostigmine E or a pharmaceutically acceptable salt thereof.

[0019] A drug for treating retinopathy, with physostigmine E as the active ingredient, also containing pharmaceutically acceptable excipients, and formulated into a pharmaceutically acceptable dosage form.

[0020] The use of physostigmine E or a pharmaceutically acceptable salt thereof in the preparation of drugs that promote the proliferation of retinal pigment epithelial cells.

[0021] A drug that promotes the proliferation of retinal pigment epithelial cells, prepared from physostigmine E or a pharmaceutically acceptable salt thereof.

[0022] A drug that promotes the proliferation of retinal pigment epithelial cells, with physostigmine E as the active ingredient, also containing pharmaceutically acceptable excipients, and formulated into a pharmaceutically acceptable dosage form.

[0023] Compared with the prior art, the present invention has the following advantages:

[0024] Studies have found that bryophyllone E has a significant therapeutic effect on diabetic retinopathy. This invention lays the foundation for the development and utilization of bryophyll plants and bryophyllone E. Attached Figure Description

[0025] Figure 1Figure showing the effect of different treatment groups on the proliferative activity of retinal pigment epithelial cells. Note: Compared with the Control group, ####P<0.0001; compared with the high glucose group, ****P<0.0001. Detailed Implementation

[0026] The present invention will now be described in further detail with reference to the accompanying drawings and specific embodiments. The following embodiments are for illustrative purposes only and are not intended to limit the scope of the invention.

[0027] Application of physostigmine E in the preparation of drugs for the treatment of diabetic retinopathy.

[0028] Use of physostigmine E or a pharmaceutically acceptable salt thereof in the preparation of medicaments for the treatment of diabetic retinopathy. Pharmaceutically acceptable salts are salts formed from physostigmine E with organic or inorganic bases. These salts are sodium, potassium, calcium, iron, magnesium, zinc, aluminum, barium, or ammonium salts.

[0029] A drug for treating diabetic retinopathy, with physostigmine E as the active ingredient, also containing pharmaceutically acceptable excipients, and formulated into a pharmaceutically acceptable dosage form.

[0030] The use of physostigmine E or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating retinopathy.

[0031] A drug for treating retinopathy, prepared from physostigmine E or a pharmaceutically acceptable salt thereof.

[0032] A drug for treating retinopathy, with physostigmine E as the active ingredient, also containing pharmaceutically acceptable excipients, and formulated into a pharmaceutically acceptable dosage form.

[0033] The use of physostigmine E or a pharmaceutically acceptable salt thereof in the preparation of drugs that promote the proliferation of retinal pigment epithelial cells.

[0034] A drug that promotes the proliferation of retinal pigment epithelial cells, prepared from physostigmine E or a pharmaceutically acceptable salt thereof.

[0035] A drug that promotes the proliferation of retinal pigment epithelial cells, with physostigmine E as the active ingredient, also containing pharmaceutically acceptable excipients, and formulated into a pharmaceutically acceptable dosage form.

[0036] The excipients include any one or more of the following: solvents, propellants, solubilizers, cosolvents, emulsifiers, colorants, binders, disintegrants, fillers, lubricants, wetting agents, osmotic pressure regulators, stabilizers, flow aids, flavoring agents, preservatives, suspending agents, coating materials, fragrances, anti-adhesion agents, binding agents, penetration promoters, pH adjusters, buffers, plasticizers, surfactants, foaming agents, defoamers, thickeners, encapsulating agents, humectants, absorbents, diluents, flocculants, anti-flocculation agents, filter aids, and release inhibitors.

[0037] Dosage forms include tablets, capsules, injections, and oral solutions.

[0038] Pharmacological activity: Goldenrodone E has good activity in treating diabetic retinopathy.

[0039] Cell source: ARPE-19 retinal pigment epithelial cells were purchased from the Cell Bank of the Chinese Academy of Sciences.

[0040] Cell culture and experimental grouping: The ARPE-19 cell line was used and cultured in DMEM / F-12 medium containing 10% fetal bovine serum and 1% penicillin / streptomycin in a conventional incubator at 37°C and 5% CO2. When the cells reached approximately 85% confluence, they were randomly divided into 6 groups: Control group, DMSO group, high glucose group, high glucose + 25 μmol / L phycocyanin E group, high glucose + 50 μmol / L phycocyanin E group, and high glucose + 100 μmol / L phycocyanin E group. A stock solution of 10 mmol / L phycocyanin E was prepared by dissolving it in 0.1% dimethyl sulfoxide (DMSO) for later use.

[0041] Control group: cultured with 5 mmol / L glucose for 24 h;

[0042] DMSO group: cultured with 0.1% DMSO + 5 mmol / L glucose for 24 h;

[0043] High glucose group: cultured with 30 mmol / L glucose for 24 h;

[0044] The drug is divided into three dosage groups.

[0045] The groups were: High glucose + 25 μmol / L goldenrodone E group: cultured with 30 mmol / L glucose and 25 μmol / L goldenrodone E for 24 h;

[0046] High glucose + 50 μmol / L goldenrod ketone E group: cultured with 30 mmol / L glucose and 50 μmol / L goldenrod ketone E for 24 h;

[0047] High glucose + 100 μmol / L goldenrod ketone E group: cultured with 30 mmol / L glucose and 100 μmol / L goldenrod ketone E for 24 h.

[0048] CCK-8 Experiment: 100 μL of cell suspension from each group was added to each well of a 96-well plate, and the plate was pre-cultured at 37℃ and 5% CO2 for 24 h. 10 μL of CCK-8 solution was added to each well, and the plate was incubated for 4 h. The absorbance at 450 nm was measured using a microplate reader. Cell proliferation activity was determined by calculating the ratio of absorbance of the drug-treated group to that of the control group. Compared with the control group, the proliferation activity of retinal pigment epithelial cells in the high-glucose group was significantly reduced (P < 0.0001). Different doses of high-glucose + physostigmine E significantly improved and upregulated the proliferation activity of retinal pigment epithelial cells under high-glucose conditions (P < 0.0001), showing a dose-dependent effect, indicating that physostigmine E can promote the proliferation of retinal pigment epithelial cells. Results are shown in Table 1. Figure 1 .

[0049] Table 1. Effects of different treatment groups on the proliferative activity of retinal pigment epithelial cells.

[0050]

[0051]

[0052] It should be understood that, in order to simplify this disclosure and aid in understanding one or more of the various aspects of the invention, features of the invention are sometimes grouped together in a single embodiment or in its description in the foregoing description of exemplary embodiments of the invention. However, this method of disclosure should not be construed as reflecting an intention that the claimed invention requires more features than expressly recited in each claim. Rather, as reflected in the claims, inventive aspects lie in fewer than all the features of the foregoingly disclosed embodiments. Therefore, the claims, following the detailed description, are hereby expressly incorporated into that detailed description, wherein each claim itself is a separate embodiment of the invention.

[0053] Although the invention has been described with reference to a limited number of embodiments, those skilled in the art will understand from the foregoing description that other embodiments are conceivable within the scope of the invention described herein. Furthermore, it should be noted that the language used in this specification has been chosen primarily for readability and instructional purposes, and not for the purpose of interpreting or limiting the subject matter of the invention. Therefore, many modifications and variations will be apparent to those skilled in the art without departing from the scope and spirit of the appended claims. The disclosure of the invention is illustrative and not restrictive, and the scope of the invention is defined by the appended claims.

[0054] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.

Claims

1. The application of physostigmine E in the preparation of drugs for treating diabetic retinopathy, characterized in that, The proliferative activity of retinal pigment epithelial cells was significantly reduced in the high glucose group; different doses of high glucose + styraxone E groups significantly improved and upregulated the proliferative activity of retinal pigment epithelial cells under high glucose conditions, and showed a dose-dependent effect.

2. The application according to claim 1, characterized in that, The structural formula of goldenrodone E is as follows: 。 3. The application according to claim 1, characterized in that, Use of physostigmine E or a pharmaceutically acceptable salt thereof in the preparation of drugs for the treatment of diabetic retinopathy.

4. The application according to claim 3, characterized in that, Pharmaceutically acceptable salts are those formed by the reaction of physostigmine E with organic or inorganic bases.

5. The application according to claim 4, characterized in that, Salts can be sodium, potassium, calcium, iron, magnesium, zinc, aluminum, barium, or ammonium salts.

6. The application according to claim 1, characterized in that, The drug uses physostigmine E as its active ingredient and also contains pharmaceutically acceptable excipients, and is formulated into a pharmaceutically acceptable dosage form.

7. The application according to claim 6, characterized in that, Dosage forms include tablets, capsules, injections, and oral solutions.

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