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Application of inhibitor of nlrp3 inflammasome in preparation of medicine for treating pituitary adenoma and medicine for treating pituitary adenoma

An inflammasome and inhibitor technology, which can be used in anti-tumor drugs, drug combinations, and medical preparations containing active ingredients, etc. Effect

Active Publication Date: 2022-03-22
武汉叶风生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bromocriptine is a dopamine D2 receptor (DRD2) agonist, which is effective in treating prolactinoma, but it is expensive and has certain side effects. For example, bromocriptine can effectively reduce PRL and restore Gonadal function, reduction or control of tumor growth, the main side effects are gastrointestinal reactions, dizziness, orthostatic hypotension, headache, drowsiness and constipation may occur when the dose is large
For patients who are resistant to bromocriptine or intolerant of its adverse reactions, there is no alternative treatment

Method used

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  • Application of inhibitor of nlrp3 inflammasome in preparation of medicine for treating pituitary adenoma and medicine for treating pituitary adenoma
  • Application of inhibitor of nlrp3 inflammasome in preparation of medicine for treating pituitary adenoma and medicine for treating pituitary adenoma
  • Application of inhibitor of nlrp3 inflammasome in preparation of medicine for treating pituitary adenoma and medicine for treating pituitary adenoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Significant activation of the pituitary NLRP3 inflammasome in estradiol-induced prolactinoma rats.

[0042] 1. Establish a prolactinoma model in rats.

[0043] SD rats were purchased from Hubei Experimental Animal Center, and 20 SD rats were randomly divided into normal group and model group, with 10 rats in each group. Rats in the model group were injected intraperitoneally with estradiol benzoate injection (purchased from Sichuan Jinke Pharmaceutical Co., Ltd., batch number 20170702), with a dose of 20 mg / kg, injected once every 5 days, and continuously injected for 50 days; The same dose of normal saline was injected intraperitoneally.

[0044]2. MRI detection and appearance observation of rat pituitary gland.

[0045] MRI detection and appearance map reference figure 1 shown by figure 1 It can be seen that compared with the normal control group rats, the pituitary gland volume of rats with prolactinoma induced by estradiol injection was significantly increased. ...

Embodiment 2

[0061] This example demonstrates that the expression of PRL significantly increases after the activation of NLRP3 inflammasome in pituitary tumor GH3 cells.

[0062] GH3 cells were purchased from Beijing Beina Chuanglian Biotechnology Research Institute, LPS was purchased from sigma company, and MSU was purchased from sigma company. When the confluence of GH3 cells after passage was 70-80%, three 6-well plates were planted (repeat 3 each time), add 1mL of cell solution to each well, add 1mL of culture medium, put them into a carbon dioxide incubator and cultivate for 24 hours, absorb 1mL of medium from each well and discard, add stimulators respectively, and the stimulators in the 6-well plate The order of adding samples is shown in Table 1 below.

[0063] Table 1 Sampling order.

[0064]

[0065] After adding stimulators and culturing for 24 hours, the GH3 cells in each group were extracted from cell lysates for Western blot detection.

[0066] Western blot test results ...

Embodiment 3

[0068] This example demonstrates that the NLRP3 inflammasome inhibitor MCC950 reduces the expression of PRL in GH3 cells by inhibiting the activation of NLRP3 inflammasome. MCC950 was purchased from MedChemexpress.

[0069] After GH3 cells were plated, stimulators and MCC950 were added. When the fusion degree of the passaged GH3 cells is 70-80%, plant three 6-well plates (repeated 3 times), add 1 mL of cell solution to each well, add 1 mL of medium, and culture in a carbon dioxide incubator for 24 After 1 hour, suck out 1 mL of medium in each well and discard, add LPS solution and Ni solution respectively, and add different concentrations of MCC950 solution after 6 hours, the sequence of adding reagents is shown in Table 2 below.

[0070] Table 2 Reagent loading order.

[0071]

[0072] After adding MCC950 and culturing for 24 hours, the lysate protein was extracted from GH3 cells in each group for Western blot detection.

[0073] Western blot detection results of GH3 ce...

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Abstract

The invention discloses the application of an inhibitor of NLRP3 inflammasome in the preparation of medicine for treating pituitary adenoma and the medicine for treating pituitary adenoma. NLRP3 inflammasome inhibitors are MCC950 or tranilast. Drugs containing NLRP3 inflammasome inhibitors may enable the treatment of pituitary adenomas. NLRP3 inflammasome inhibitors bring good news to patients with pituitary adenomas.

Description

technical field [0001] The invention relates to the application of an inhibitor of NLRP3 inflammasome in the preparation of medicine for treating pituitary adenoma and the medicine for treating pituitary adenoma. Background technique [0002] Pituitary tumor is one of the common benign intracranial tumors. Its incidence rate is second only to glioma and meningioma in intracranial tumors, accounting for about 10% of intracranial tumors. The rate has been increasing year by year. As the tumor continues to grow, it can compress the surrounding structures of the sella region, such as the optic nerve, cavernous sinus, base of the brain artery, hypothalamus, etc., and even involve the frontal lobe and brainstem, resulting in severe dysfunction. At the same time, tumor growth can also lead to disorders of pituitary hormone secretion. According to peripheral blood hormone levels, pituitary adenomas are divided into non-functioning pituitary adenomas (NFPA) and functional pituitary...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K31/196A61P35/00
CPCA61K45/00A61K31/196A61P35/00
Inventor 王雄马莉郭秀丽
Owner 武汉叶风生物科技有限公司
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