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Application of tangeretin in preparation of medicine for treating functional pituitary adenoma

A technology of pituitary adenoma and tangeretin, applied in the field of biomedicine, can solve the problems of side effects of dopamine agonists, patients taking long-term medication, and drug resistance

Inactive Publication Date: 2018-08-28
BEIJING NEUROSURGICAL INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although drug treatment can reverse the clinical symptoms of most patients, normalize prolactin levels and reduce tumor volume, there are still some shortcomings, such as long-term medication for most patients, intolerant side effects of drugs, and tumor resistance to dopamine agonists Wait

Method used

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  • Application of tangeretin in preparation of medicine for treating functional pituitary adenoma
  • Application of tangeretin in preparation of medicine for treating functional pituitary adenoma
  • Application of tangeretin in preparation of medicine for treating functional pituitary adenoma

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The anti-tumor effects were compared among 35 kinds of extracts, and 15 kinds of compounds were selected for cytological experiments. Using different doses of drug concentrations in GH3 and MMQ cell lines, MTS experiments showed that 6 drugs had the effect of inhibiting cell proliferation, and the results were as follows Figure 1-Figure 4 As shown, there are 3 kinds of inhibitory effects on both cells, namely Allylisothiocyante (35% inhibition rate at 24 hours), Tangeretin (38.4% inhibition rate at 24 hours) and Xanthohumol (24% inhibition rate at 24 hours); there are 3 kinds Drugs can promote the proliferation of pituitary adenoma cells, among which Luteolin has the most obvious effect. Annexin V method was used to detect the occurrence level of apoptosis after drug treatment, and it was found that 1 μM Allylisothiocyante treatment for 24 hours: the apoptosis rate of GH3 cells was 16.4%, and the apoptosis rate of MMQ cells was 17.4%; 1 μM Tangeretin treatment for 24 h...

Embodiment 2

[0028] Tangeretin was configured as a 10mM stock solution with DMSO, and then diluted to different concentrations with DMSO when used. Prolactinoma MMQ cells were suspended and cultured in DEME medium (containing 2.5% fetal bovine serum, 12.5% ​​horse serum, 1.176g / L sodium bicarbonate) in an incubator containing 5% carbon dioxide at 37°C After culturing for 48 hours, the cell viability was determined to be >99% by trypan blue, and the culture medium was replaced with DEME culture medium containing 15% fetal bovine serum, and the medium was changed every 48 hours and passaged once every 72 hours.

[0029] The MMQ cells in the logarithmic growth phase were adjusted to a concentration of 5×10 cells with culture medium. 4 / ml. Place the cells in a 96-well plate, 200 μl per well. After 24 hours of culture, different concentrations (0, 0.1, 1, 10 μM) of tangeretin were added, respectively, after 24, 48 and 72 hours of culture were continued, 40 μl of MTS was added to each well, a...

Embodiment 3

[0036] Under sterile conditions, MMQ cells in good condition in logarithmic growth phase were collected, centrifuged and washed with normal saline several times to remove serum, and diluted in normal saline. Each nude mouse was subcutaneously inoculated with 1×10 7 cells / nude mouse. The nude mice were weighed every two days to record the body weight changes. Measure the length and width of the tumor with a vernier caliper every two days, and use the formula V=a 2Calculate tumor volume by ×b / 2, where a is width and b is length, unit: cm. The tumor-bearing mice were randomly divided into 4 groups (PBS solvent control group containing 0.1% DMSO, 25mg / kg tangeretin group, 50mg / kg tangeretin group, 100mg / kg tangeretin group), 7 in each group, After 4 weeks of intragastric administration, the size of the tumor was peeled off, weighed and recorded. The results were as follows: Figure 7 shown.

[0037] according to Figure 7 The results showed that tangeretin can effectively in...

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Abstract

The invention provides application of tangeretin in preparation of a medicine for treating functional pituitary adenoma. According to the technical scheme, the tangeretin in the invention is capable of effectively inhibiting cell proliferation of prolactinomas MMQ on a cellular level and presents obvious time dependence and dose dependence. Meanwhile, the tangeretin can achieve effects of obviously inducing apoptosis of MMQ cells, effectively inhibiting tumor growth of tumor-bearing mice on an animal model level and prolonging the life cycle of the tumor-bearing mice. Therefore, due to use ofthe tangeretin, a novel solution is provided for treatment of the prolactinomas.

Description

technical field [0001] The present disclosure relates to the field of biomedicine, in particular to the use of tangeretin in the preparation of medicines for treating functional pituitary adenomas. Background technique [0002] Functional pituitary adenomas include prolactinomas, growth hormone tumors, and ACTH adenomas; prolactinomas are the most common functional pituitary adenomas, accounting for about 40%-45% of adult functional pituitary adenomas . The main clinical manifestation of pituitary prolactinoma is hypogonadism, which can secrete a large amount of prolactin, and women may have clinical manifestations such as amenorrhea, lactation, and infertility. Males can lead to low sexual function and infertility. In severe cases, it can invade surrounding tissues, leading to decreased vision, headaches, etc., and even life-threatening, seriously affecting the quality of life of patients. The exact pathogenesis of prolactinoma has not been fully elucidated yet. [0003]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P35/00
CPCA61K31/352
Inventor 刘潜高华张亚卓
Owner BEIJING NEUROSURGICAL INST
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