Application of dibrompropamidine dihydrochloride to preparation of medicine for inhibiting bladder cancer EGFR (Epidermal Growth Factor Receptor) target spot

A technology of dibromopropionamidine dihydrochloride and bladder cancer, applied in the field of diamidine series compound medicine, can solve the problems such as unreported antitumor effect of dibromopropionamidine dihydrochloride, and save cost and time , reduce costs and improve efficiency

Inactive Publication Date: 2016-11-09
KUNMING MEDICAL UNIVERSITY +2
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Problems solved by technology

Dibromopropamidine Dihydrochloride has not been reported to have anti-tumor effects

Method used

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  • Application of dibrompropamidine dihydrochloride to preparation of medicine for inhibiting bladder cancer EGFR (Epidermal Growth Factor Receptor) target spot
  • Application of dibrompropamidine dihydrochloride to preparation of medicine for inhibiting bladder cancer EGFR (Epidermal Growth Factor Receptor) target spot
  • Application of dibrompropamidine dihydrochloride to preparation of medicine for inhibiting bladder cancer EGFR (Epidermal Growth Factor Receptor) target spot

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Experimental program
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Embodiment Construction

[0029] 1. MTT experiment:

[0030] Experimental method: Bladder cancer cells SW780 and RT112 were used at 6×10 per well 3 Among them, SW780 uses 0.125% FBS L-15 medium, RT112 uses 0.125% FBS RPMI-1640 medium, cultures in 96-well plate for 24 hours, discards the medium and uses 1, 3, 10, 30 μmol / L Concentration of dibromopropamidine dihydrochloride 10% complete medium, that is, SW780 uses 10% FBS L-15 medium, RT112 uses 10% FBS RPMI-1640 medium (the same below), respectively cultured for 24, 48, 72h. The SW780 and RT112 cells cultured above were incubated with 0.5% 3-(4,5)-dimethylthiazole-(2,5)-diphenyl blue tetrazolium bromide (thiazolium blue for short) for 4 hours. The generated formazan was dissolved in 200 μL of dimethyl sulfoxide and detected at a wavelength of 570 nm. IC 50 Calculated with the software GraphPadPrism 5.

[0031] Experiments confirm:

[0032] MTT analysis of human bladder cancer cell survival rate as figure 1 , 2 . MTT experiment confirmed that d...

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Abstract

The invention provides application of dibrompropamidine dihydrochloride to the preparation of a medicine for inhibiting a bladder cancer EGFR (Epidermal Growth Factor Receptor) target spot and belongs to diamidine series compound medicines and application thereof. The dibrompropamidine dihydrochloride can be used for inhibiting IC50 of SW780and RT112 cell growth to be 5Mumol / L-8Mumol / L; and the concentration has positive correlation with effect of promoting SW780 and RT112 apoptosis and has inverse correlation with p-EGFR, p-AKT and p-ERK phosphorylation degrees. The invention takes the dibrompropamidine dihydrochloride as a medicine for inhibiting a tyrosine kinase structure domain of the human bladder cancer EGFR; and the utilization efficiency of a medicine is improved and a market prospect is wide.

Description

technical field [0001] The invention belongs to diamidine series compound medicine and application thereof. Background technique [0002] Bladder cancer is one of the most common and costly malignancies. The incidence ratio of male to female is 3.5:1, and the peak age of onset is 50-70 years old. Although the incidence of bladder cancer ranks ninth, it has become one of the most expensive tumors due to its high recurrence rate and long treatment time. The pathogenesis of bladder cancer is complex. The latest research found that EGFR (epidermal growth factor receptor, epidermal growth factor receptor) plays a role in bladder cancer: EGFR can lead to dedifferentiation of bladder cells; the proportion of EGFR overexpression in bladder cancer is about 12-53%, which is the same as that of non-muscle layer Compared with invasive bladder cancer, the proportion of EGFR overexpression in muscle invasive bladder cancer was as high as 53%; 9% of muscle invasive bladder cancer had EG...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/155A61P35/00
CPCA61K31/155
Inventor 柯坤彬孔祥复李宏健梁广锡王文汉林李家宓刘旭刘孝东
Owner KUNMING MEDICAL UNIVERSITY
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