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Novel medical use of cucurbitacin

A technology of cucurbitacin and isocucurbita, applied in the field of medicine, can solve the problem of reducing serum CA125 in patients with ovarian cancer

Active Publication Date: 2013-03-20
SHENYANG PHARMA UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there is no application of cucurbitacin B, cucurbitacin B substances and cucurbitacin BE in ovarian cancer, and there is no cucurbitacin, including cucurbitacin B and cucurbitacin B substances (such as dihydrocucurbitacin B, iso Cucurbitacin B) and cucurbitacin BE, cucurbitacin I, cucurbitacin Q or one or more components of cucurbitacin are used to reduce serum CA125 in patients with ovarian cancer. Decrease serum CA125 in patients with ovarian cancer

Method used

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  • Novel medical use of cucurbitacin
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  • Novel medical use of cucurbitacin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Cucurbitacin B (CuB, the purity determined by HPLC area normalization method is greater than 99%) in vitro anti-human ovarian cancer cells

[0023] 1. In vitro test (MTT)

[0024] method:

[0025] 1. Human ovarian cancer cell line SK-OV-3 was cultured with RPMI1640 medium containing 10% fetal bovine serum at 37°C and 5% CO 2 In the incubator, subculture once every 3-4 days. Cells in the logarithmic growth phase were selected for the experiment.

[0026] 2. Digest the adherent cells with 0.25% trypsin (containing EDTA 1mM / L) and suspend them in the culture medium to adjust the cell concentration to 2.5×10 4 / mL, inoculate 100 μL per well on a 96-well plate, with 3 replicate wells in each well. Only culture solution was added to the blank control wells.

[0027] 3. After culturing for 18-24 hours and waiting for the cells to adhere to the wall, add different concentrations of drugs (0.5 μL) into groups, and the other group is the control group (without adding drugs)...

Embodiment 2

[0035] Pharmacodynamic study of cucurbitacin B (CuB, the purity determined by HPLC area normalization method is greater than 98%) against ovarian cancer cell line SK-OV-3 in nude mice

[0036] method:

[0037] 18-20 grams of nude mice (BALB / C, 5-6 weeks, female, purchased from the Institute of Experimental Animals, Chinese Academy of Medical Sciences, Chinese Union Medical University) 40, inoculated cells in the right armpit 5 × 10 6 / only, when the tumor grows to be larger than 60mm 3 At the same time, they were randomly divided into 4 groups, which were negative control group (0.9% sodium chloride, 0.2ml / day, intravenous injection), CuB low-dose group (50μg / kg ·day, intravenous injection), middle-dose group ( 100μg / kg·day, intravenous injection), high-dose group (200μg / kg·day, intravenous injection), continuous administration for 14 days. The animals were sacrificed within 24 hours after the last administration, and the tumors were weighed. Calculate the tumor inhibitio...

Embodiment 3

[0041] Pharmacodynamic study of dihydrocucurbitacin B (purity determined by HPLC area normalization method greater than 95%) against ovarian cancer cell line SK-OV-3 in nude mice

[0042] Refer to the method of "Example 2"

[0043] 18 nude mice of 18-20 grams, inoculated with 5×10 cells in the right armpit 6 / only, when the tumor grows to be larger than 50mm 3 At the same time, they were randomly divided into 3 groups, which were negative control group (distilled water, intragastric administration, 0.2ml / day), dihydrocucurbitacin B group (gastric administration, 300μg / kg·day), dihydrocucurbitacin group Group B (gastric administration, 400 μg / kg·day), continuous administration for 14 days. The animals were sacrificed within 24 hours after the last administration, and the tumors were weighed to calculate the tumor inhibition rate. Results The tumor inhibition rates of the dihydrocucurbitacin B group were 39.2% and 51.6% respectively; compared with the normal control group, t...

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Abstract

The invention belongs to the technical field of medicine and discloses novel application of Cucurbitacins, namely novel application of Cucurbitacin B, Cucurbitacin B substances, Cucurbitacin BE and a pharmaceutical composition thereof in a medicine for treating ovarian cancer and improving the quantity of leukocytes of radiotherapy patients. The Cucurbitacin can also be a cucurbitacin B monomer, an isocucurbitacin B monomer, a dihydrocucurbitacin B monomer, a cucurbitacin I monomer, and a cucurbitacin O monomer. The Cucurbitacins or pharmaceutical compositions thereof can be matched with a pharmaceutically acceptable carrier and prepared into a tablet, a capsule, a granule, powder, a plaster, an ointment, an aerosol, a suspension, a syrup, an oral liquid, and an injection, and can also be prepared into special dosage forms such as a liposome, microspheres, nanoparticles and an emulsion for cavity administration, external use, oral administration and injection. The individual administration or the combined treatment can be performed, the administration dosage of the Cucurbitacins is calculated according to the total Cucurbitacins, the dosage for healthy adults is between 0.1 and 5mg / d, the best dosage is between 0.3 and 3mg / d, and the administration is performed for 1 to 4 times.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a new medical application of a known substance cucurbitacin, that is, a new application of cucurbitacin B, cucurbitacin B-type substances and cucurbitacin BE. Specifically, it refers to the new application of cucurbitacin B, cucurbitacin B-like substances, cucurbitacin BE, cucurbitacin I, cucurbitacin Q and their pharmaceutical compositions in treating ovarian cancer and increasing the white blood cell count of radiotherapy patients. It can also be cucurbitacin B monomer, isocucurbitacin B monomer, dihydrocucurbitacin B monomer, cucurbitacin I monomer, or cucurbitacin Q monomer. Background technique: [0002] Cucurbitacins belong to a class of tetracyclic triterpenoids with a 19-methyl group appearing at the C-9 position. They are mainly distributed in Cucurbitaceae plants. It is also found in higher plants such as wood family and some large fungi. Qiu Minghua, a researcher at ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61P35/00
Inventor 邓意辉张美侠
Owner SHENYANG PHARMA UNIVERSITY
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