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New medical use of cucurbitacin in treating cancer

A technology of cucurbitacin, which is applied in the field of medicine, can solve problems such as limiting the scope of application, increasing risks, and patients with leukopenia, and achieves the effect of increasing the number of white blood cells, improving the quality of life, and good therapeutic effect

Inactive Publication Date: 2008-02-27
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The 30-minute intravenous infusion of gemcitabine is the standard treatment for advanced pancreatic cancer, but the median survival period of patients is only 5.4 months to 5.6 months, and the annual productivity is only 16%-19%. Moreover, there are side effects such as blood system, which lead to the occurrence of white blood cells in patients. Thrombocytopenia, and more inconveniently, gemcitabine must be infused intravenously, which greatly limits the scope of application, increases the cost, and increases the risk during treatment. There is an urgent clinical need for an effective therapeutic drug that can be administered orally

Method used

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  • New medical use of cucurbitacin in treating cancer
  • New medical use of cucurbitacin in treating cancer
  • New medical use of cucurbitacin in treating cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Cucurbitacin B (CuB, the purity determined by HPLC area normalization method is greater than 99%) in vitro anti-human pancreatic cancer cell research

[0020] In vitro test (MTT)

[0021] method:

[0022] 1. Human pancreatic cancer cells BxPC-3 were cultured with RPMI 1640 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.

[0023] 2. The adherent cells were digested with 0.25% trypsin (containing EDTA 1mM) and suspended in the culture medium to adjust the cell concentration to 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 blank control wells.

[0024] 3. Cultivate the cells overnight. After the cells 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

[0030] Example 2: Anti-human pancreatic cancer pharmacodynamics study of cucurbitacin B (CuB, the purity determined by HPLC area normalization method is greater than 99%) in vivo

[0031] method:

[0032] 1. Human pancreatic cancer cells BxPC-3 were cultured with RPMI1640 medium containing 10% fetal bovine serum in 37, 5% CO 2 In the incubator, subculture once every 3-4 days. Cells in the logarithmic growth phase were selected for the experiment.

[0033] 2. Digest the adherent cells with 0.25% trypsin (containing EDTA 1mM) and suspend them in normal saline to adjust the cell concentration to 2.5×10 7 / mL.

[0034] 3. 36 18-20 g nude mice (BALB / C, 5-6 weeks, female, purchased from the Institute of Experimental Animals, Chinese Academy of Medical Sciences, Chinese Union Medical University) were inoculated with 5×10 cells in the right underarm 6 / only, when the tumor grows to be larger than 100mm 3 At the same time, they were randomly divided into 6 groups, which were nega...

Embodiment 3

[0044] Example 3: Pharmacodynamic study of cucurbitacin administered orally and gavage against human pancreatic cancer, refer to the method in "Example 2"

[0045] 24 nude mice of 18-20 g, inoculated with 5×10 cells in the right armpit 6 / only, when the tumor grows to be larger than 100mm 3 At the same time, they were randomly divided into 4 groups, which were negative control group (MCT, 0.2ml / day), cucurbitacin group (cucurbitacin was dissolved with MCT, and the dosage was calculated according to the weight of cucurbitacin, administered by intragastric administration, 150 μg / day). kg·day, 300 μg / kg·day, 600 μg / kg·day), for 14 consecutive days. The animals were sacrificed within 24 hours after the last administration, and the tumors were weighed to calculate the tumor inhibition rate. The results are shown in Table 2.

[0046] The antitumor effect of table 2 cucurbitacin intragastric administration ( )

[0047]

[0048] Cucurbitacin

(Low)

Cucur...

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Abstract

The invention discloses a new application of cucurbitacins and drug composition to treat pancreatic cancer in the medical technical domain, which is characterized by the following: adopting cucurbitacins and drug composition as raw material to prepare multiple kinds of agent, such as tablet, powder medicine, capsule, particle, turbid liquor, syrup, oral liquor, chrisma, paster and injection; fitting for giving drug individually or integrally to treat low leucocyte of pancreatic cancer and tumour patient due to radiotherapy; setting the drug supplying content at 0. 001mg / kg-1mg / kg for mouse, 0. 1mg-5mg / d for health people with optimum content at 0. 01mg / kg-0. 5mg / kg for mouse, 0. 3mg-3mg / d for health people every 1-4 times one day.

Description

Technical field: [0001] The invention belongs to the technical field of medicine and relates to a new application of known substances cucurbitacins. Specifically, it refers to the new application of cucurbitacin and its pharmaceutical composition in the preparation and treatment of pancreatic cancer. 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 the Kunming Institute of Botany, Chinese Academy of Sciences, led scientific and technical personnel to study 229 almost all cucurbitacin compounds on the basis of the discovery of a series of new types of cucurbitacin compounds, and proposed a new structural classification model, which was reconstructed from the previous five structural types. Divided into 12 categories, it has...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K9/06A61K9/08A61K9/10A61K9/14A61K9/16A61K9/48A61K9/70A61P1/18A61P35/00
Inventor 邓意辉张美侠
Owner SHENYANG PHARMA UNIVERSITY
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