Application of cedilanid in preparation of anti-liver cancer and anti-bladder cancer medicament

A cedilan and anti-liver cancer technology, applied in drug delivery, drug combination, anti-tumor drugs, etc., can solve the problem of damaging the functions of multiple organs in the human body, and achieve the effect of low toxicity, low drug price and good effect

Inactive Publication Date: 2012-04-18
GUILIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment of cancer generally requires surgical resection combined with radiotherapy and chemotherapy. However, radiotherapy and chemotherapy often kill cancer cells

Method used

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  • Application of cedilanid in preparation of anti-liver cancer and anti-bladder cancer medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1: In vitro anticancer experiment of cedilan and cardiac glycosides:

[0017] The experimental method is: culture human tumor cell line in DMEM medium (containing 10% inactivated fetal bovine serum, 100U / ml penicillin and 100μg / ml streptomycin), human normal liver cell line HL-7702 in RPMI1640 culture base (containing 10% inactivated newborn bovine serum, 100 U / ml penicillin and 100 μg / ml streptomycin). All six cell lines were stored at 37°C, 5% CO 2 Cultivate in a saturated humidity incubator, change the medium every two to three days and passage once, and take the cells in the logarithmic growth phase for the experiment.

[0018] The MTT method was used to detect the effect of anticancer drugs on the proliferation activity of tumor cells, and the cells in the logarithmic growth phase were taken as 1×10 4 180 μl per well in a 96-well plate. The test set a negative control group (PBS), a positive control group (5-FU) (final concentration of 10 -1 mmol / L), di...

Embodiment 2

[0028] Example 2: In vitro anti-human bladder cancer cell (HepG2) experiment of cardiac glycosides

[0029] Experimental method is the same as embodiment 1

[0030] The in vitro anti-human bladder cancer cell (HepG2) results of cardiac glycosides are shown in Table 3

[0031] drug Concentration (mmol / L) OD value Inhibition rate(%) PBS — 0.5762±0.02 0 Digoxigenin 2×10 -2 0.443±0.04 23.11 4×10 -3 0.723±0.04 -25.44 8×10 -4 0.734±0.05 -27.38 1.6×10 -4 0.696±0.03 -20.86 3.2×10 -5 0.688±0.02 -19.43 Digoxin 2×10 -2 0.244±0.01* 57.61 4×10 -3 0.525±0.04 8.92 8×10 -4 0.670±0.08 -16.27 1.6×10 -4 0.633±0.03 -9.82298 3.2×10 -5 0.695±0.08 -20.65 Cediland 2×10 -2 0.239±0.01* 58.62 4×10 -3 0.224±0.01* 61.19 8×10 -4 0.291±0.07* 49.53 1.6×10 -4 0.507±0.07 11.97 3.2×10 -5 0.747±0.25 -29.60 5Fu 10 -1 0.293±0.02 49....

Embodiment 3

[0034] Example 3 Effect of Cedilan on Cell Na+ / K+-ATPase Activity

[0035] HepG2 cells and HL-7702 cells in the logarithmic growth phase were divided into 1×10 5 / ml density inoculated in 6-well culture plate, 1.8ml per well, at 37℃, 5%CO 2 After culturing in the incubator overnight, the culture solution was aspirated, and the final concentration was 2×10 -2 , 4×10 -3 , 8×10 -4 , 1.6×10 -4 , 3.2×10 -5 Add 0.2ml of cedilan in mmol / L, and add 0.2ml of PBS to the negative control group. After acting for 6 hours, suck out the medium in all the wells, wash them twice with NS, centrifuge, discard the supernatant, and leave a layer of cells. Add 1ml NS to each well of cells to prepare a solution containing 10 6 The suspension of two cells was crushed with an ultrasonic breaker (200-300w, 90-100 times, 3 seconds to run, 3 seconds to stop), and the prepared cells were operated according to the instructions of "Sodium Potassium ATPase Assay Kit". At the same time, the non-centr...

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Abstract

The invention discloses an application of cedilanid in the preparation of anti-liver cancer and anti-bladder cancer medicaments; cedilanid is prepared into an injection, and is used for liver cancer and bladder cancer resistance; the concentration IC50 of the injection is 8*10-4 mmol/L. According to the invention, in an in-vitro experiment, the IC50 of cedilanid for liver cancer and bladder cancer cells is 8*10-4 mmol/L, and the effect is better than other cardiac glycoside medicaments; when compared with a common medicament of 5-fluorouracil with an IC50 of 1*10-1 mmol/L, cedilanid has a potency stronger by 100 times; in an antitumor experiment in animal body, cedilanid has a tumor inhibition rate of 34.26-48.43%; if application methods are proper, cedilanid is an ideal anticancer medicament.

Description

technical field [0001] The invention relates to cedilan medicine, in particular to the application of cedilan in the preparation of anti-liver cancer and bladder cancer medicines. Background technique [0002] Cancer is still one of the incurable diseases so far. The treatment of cancer generally requires surgical resection combined with radiotherapy and chemotherapy. However, radiotherapy and chemotherapy often kill cancer cells and seriously damage the functions of multiple organs in the human body. For this reason, scientists have been working hard to find a better and more direct method with less side effects to treat cancer. [0003] Cedilan, also known as Digigenin C and C, or Cedi-lanid in English, is one of the traditional Chinese medicines commonly used in traditional Chinese medicine and is usually used to treat heart failure. At present, there is no report about the treatment of liver cancer and bladder cancer by Cedilan. Contents of the invention [0004] Th...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K9/08A61P35/00
Inventor 何松青徐庆陈果韦京辰杨成芳梁荣感张均智
Owner GUILIN MEDICAL UNIVERSITY
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