Application of EP300 inhibitor in preparation of medicine for treating pelvic inflammation

Abstract

The invention provides application of an EP300 inhibitor in preparation of a medicine for treating pelvic inflammation, and relates to the technical field of medicines. The EP300 inhibitor is adopted to carry out gavage treatment on a pelvic inflammation rat model, and an excellent treatment effect is shown. Meanwhile, clinical experiments show that the EP300 inhibitor can effectively treat pelvic inflammation and can be used as a medicine for treating pelvic inflammation.

Description

Technical Field

[0001] The invention provides use of an EP300 inhibitor in preparing a medicine for treating pelvic inflammatory disease, and belongs to the technical field of medicines. Background Art

[0002] EP300 is a histone acetyltransferase. In addition to its acetyltransferase activity, it also regulates gene expression by binding to transcription factors, thereby participating in cell growth, division, maturation and differentiation.

[0003] The main research direction of EP300 inhibitors is in the field of cancer treatment. The present invention has found through experiments that EP300 inhibitors have a good therapeutic effect on pelvic inflammatory disease and are expected to be used as drugs for the treatment of pelvic inflammatory disease. Summary of the invention

[0004] In view of this, the object of the present invention is to provide an application of an EP300 inhibitor in the preparation of a drug for treating pelvic inflammatory disease.

[0005] The EP300 inhibitor of the present invention is a CREBBP / EP300 inhibitor (SGC-CBP30), CAS No. 1613695-14-9, and the molecular formula is C 28 H 33 ClN4O3, the structural formula is as follows:

[0006]

[0007] Compared with the prior art, the present invention has the following beneficial effects:

[0008] The present invention found that EP300 inhibitors can effectively treat pelvic inflammatory disease without causing adverse side effects to patients, providing a new solution for the development of drugs for the treatment of pelvic inflammatory disease. DETAILED DESCRIPTION

[0009] In order to make the purpose, technical scheme and advantages of the present invention clearer, the preferred embodiments of the present invention are further described in detail in conjunction with the examples below. Based on the examples in the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention. The EP300 inhibitor used in the present invention has the molecular formula C 28 H 33 ClN4O3.

[0010] 1. Animal Experiments

[0011] 1.1 Experimental animals and drugs

[0012] 50 female SD rats, 10-12 weeks old, weighing 200-210 g

[0013] 1.2 Preparation of model mice

[0014] Forty rats were treated with estradiol (0.1 mL / 100 g, 2 mg / mL) for 1 week, and then injected into the rat uterine cavity with 2×10 9 0.1 ml of mixed bacterial solution of Escherichia coli and Staphylococcus aureus was added, and the mixed solution contained equal amounts of Escherichia coli and Staphylococcus aureus. The mixture was inoculated twice a week for 4 weeks. 5 weeks after the first inoculation, 2 ml of blood was collected from the rat's eye socket and injected into a clean dry test tube. After the blood sample coagulated naturally, it was centrifuged at 3500 r / min for 10 min, and serum was extracted and tested for serum MDA content and SOD activity to determine whether the model mouse was constructed.

[0015] 1.3 Administration

[0016] The model mice were randomly divided into control group, low concentration treatment group, medium concentration treatment group, and high concentration treatment group. The remaining 10 rats without modeling were used as normal group. The low concentration treatment group was gavaged with 100 mg / kg EP300 inhibitor diluted with 2 mL saline every day; the medium concentration treatment group was gavaged with 300 mg / kg EP300 inhibitor diluted with 2 mL saline every day; the high concentration treatment group was gavaged with 600 mg / kg EP300 inhibitor diluted with 2 mL saline every day. After 10 days of continuous gavage treatment. The control group and the normal group did not receive any drug treatment. Gavage treatment for 7 days.

[0017] 1.4 Results

[0018] Rats in the normal group: active mental state, shiny fur, normal eating and drinking.

[0019] Control group: The mental state was poor, the fur was messy and dull, the body was thin, the back was often hunched, curled up, and trembling, and the food and water intake was significantly reduced.

[0020] Rats in the low-concentration treatment group were in a general mental state, had dull fur, and consumed less food and water.

[0021] Rats in the medium and high concentration treatment groups had better mental states, shiny and smooth fur, normal movements, and significantly increased food and water intake.

[0022] At the same time, the uterus of the rats in the control group was obviously edematous, swollen and shortened, with poor elasticity, and was difficult to separate from the surrounding intestines and connective tissues. The uterus of the rats in the low-concentration treatment group was slightly congested and edematous, with a certain degree of flexibility, and the adhesion with the surrounding tissues was improved. The uterus of the rats in the medium and high concentration treatment groups was basically the same as that of the normal group.

[0023] The uterine coefficients of rats in each group were measured. Compared with the control group, the uterine coefficients of rats in the treatment group were significantly reduced, and the uterine coefficients of rats in the medium and high concentration treatment groups were significantly lower than those in the low concentration treatment group and the control group.

[0024] 2. Clinical Trials

[0025] One hundred patients with pelvic inflammatory disease aged between 30 and 50 years were selected. There was no significant difference in the general data of each patient (P>0.05).

[0026] The above patients took EP300 inhibitor 1.5g / day orally for 10 days, and then the condition of the patients in the treatment group and the blank control group was analyzed.

[0027] The criteria for determination are as follows:

[0028] (1) Cured: After treatment, symptoms such as lower abdominal pain and lumbar pain disappear, and gynecological examination is normal; the sum of symptom and sign scores decreases by ≥95%;

[0029] (2) Significantly effective: After treatment, symptoms such as lower abdominal pain and lumbar distension and pain were significantly alleviated, and gynecological examinations were significantly improved; the sum of symptom and sign scores decreased by ≥70% and <95%;

[0030] (3) Effective: After treatment, lower abdominal pain and lumbar pain were alleviated, and gynecological examinations were relatively improved; the sum of symptom and sign scores decreased by ≥30% and <70%;

[0031] (4) Ineffective: After treatment, lower abdominal pain, lumbar pain, and other symptoms did not improve or worsened; gynecological examination showed no improvement or worsened compared with before treatment; the sum of symptom and sign scores decreased by <30%.

[0032] According to statistics, among 100 patients with pelvic inflammatory disease, 17 were cured after 10 weeks of treatment, 75 were significantly effective, 8 were effective, and 0 were ineffective.

[0033] The embodiments described above are part of the embodiments of the present invention, rather than all of the embodiments. The detailed description of the embodiments of the present invention is not intended to limit the scope of the invention claimed for protection, but merely represents selected embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

Claims

1. Application of EP300 inhibitors in the preparation of drugs for the treatment of pelvic inflammatory disease.

2. The use according to claim 1, characterized in that The structural formula of the EP300 inhibitor is as follows:

3. The use according to claim 1, characterized in that The drug includes medically acceptable pharmaceutical excipients.

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