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Application of miltirone in preparation of antitumor drugs

An anti-tumor drug, the technology of tanshinone, is applied in the directions of anti-tumor drugs, drug combinations, separation/purification of carbonyl compounds, etc., to achieve the effects of inhibiting tumor cell proliferation, sensitizing the formation of new blood vessels, and preventing tumors.

Active Publication Date: 2014-06-11
ZHEJIANG PROVINCIAL HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far there is no relevant research report that tanshinone has the effect of inducing tumor cell apoptosis, chemotherapeutic drug sensitization and inhibiting angiogenesis

Method used

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  • Application of miltirone in preparation of antitumor drugs
  • Application of miltirone in preparation of antitumor drugs
  • Application of miltirone in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: In order to further understand the present invention, the preparation of tanshinone with the structure of formula I will be described in detail below. Here, the present invention provides a preparation method or synthesis technology.

[0040] Salvia miltiorrhiza medicinal material (3kg) is 95% ethanol aqueous solution extraction with the ethanol mass percentage of 8 times weight, each 24Kg salvia miltiorrhiza medicinal material, altogether 3 times, merges and obtains ethanol extract, and ethanol extract is with sherwood oil, dichloromethane, n-butanol Sequential extraction yielded a petroleum ether layer, a dichloromethane layer, and n-butanol layer, respectively.

[0041] The dichloromethane layer (70 g) was dissolved in 100 mL of ethyl acetate, and 70 g of 200-300 mesh chromatography silica gel was added to mix the sample to obtain the mixed sample. Wet-pack the column with 300g 200-300 mesh chromatography silica gel, add the mixed sample, and fix the colum...

Embodiment 2

[0045] Example 2: Tanshinone inhibits lung cancer cell NCI-H1975p-stat3-tyr （705） Activation, no inhibition of p-stat3-ser

[0046] Western blot detection of p-STAT3-tyr in lung cancer cells NCI-H19754H (0, 5 μM, 10 μM, 20 μM) treated （705） , p-STAT3-ser （727） , STAT3[(antibodies were purchased from CST Company (CellSignalingTechnology, Inc)], the experimental results showed that with the increase of concentration, p-STAT3-tyr （705） showed an obvious downward trend, while p-STAT3-ser （727） There is no change, see the specific results figure 1 .

[0047] The specific implementation method is as follows:

[0048] Take the lung cancer cells NCI-H1975 in the logarithmic growth phase, prepare a single cell suspension, and count 1×10 6 Add each bottle into a 5mL culture flask. After the cells adhere to the wall the next day, add drugs of different concentrations (0, 5μM, 10μM, 20μM). After 4h, collect the cell samples into a 15ml centrifuge tube, 800rpm / 5min, discard the super...

experiment example 3

[0049] Experimental example 3: Effect of tanshinone on the phosphorylation levels of Stat3 upstream regulatory kinases P-Src and P-jak2 in lung cancer cell NCI-H1975.

[0050] After lung cancer cells NCI-H1975 (0, 5 μM, 10 μM, 20 μM) were treated for 4 hours, P-jak2, P-Src, and β-actin were detected by Western blot technique [(antibodies were purchased from CST Company (Cell Signaling Technology, Inc)], the experimental results It shows that the upstream kinases of STAT3 have no obvious changes, and the specific results are shown in figure 2 .

[0051] The specific implementation method is basically the same as in Example 2.

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Abstract

The invention discloses an application of miltirone in preparation of antitumor drugs. The miltirone has a structure of formula I; the miltirone serves as an inhibitor of STAT3 (Signal Transducer and Activator of Transcription 3) and is capable of inhibiting growth and proliferation of tumor cells which are abnormally activated by STAT3 so as to cause the apoptosis of the tumor cells and also capable of improving sensibility of cytotoxic drugs and inhibiting formation of tumor vessels. The miltirone with the structure of formula I can inhibit STAT3 kinase Tyr705 phosphorylation level to achieve the functions of accelerating the apoptosis of the tumor cells, improving the sensibility of chemotherapy drugs and inhibiting formation of new vessels; and the proliferation of tumor cells can be significantly inhibited due to the combined combination of the miltirone with low toxicity or non-toxic concentration and adriacin doxorubicin with low toxicity or non-toxic concentration and the combined application of the miltirone and cis-platinum with low toxicity or non-toxic concentration. The functions of the miltirone with the structure of formula I have positive significance to prevention and treatment of tumors.

Description

technical field [0001] The invention relates to the application field of tanshinone, in particular to the application of tanshinone in the preparation of antitumor drugs. Background technique [0002] Malignant tumors and their complications are a serious threat to human life and health, and their incidence is increasing rapidly year by year. Statistics from the World Health Organization show that in 2000, there were nearly 10 million new cases of malignant tumors in the world, and its incidence rate is second only to cardiovascular and cerebrovascular diseases. Current cancer treatments include surgery, chemotherapy, and radiotherapy. Surgical resection is currently the preferred treatment method, but surgical resection is only suitable for a small number of patients with early localized tumors, and postoperative recurrence and metastasis are often accompanied. Therefore, chemotherapy is the most commonly used tumor treatment method at this stage. Conventional chemotherap...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61P35/00A61P35/02A61K31/704A61K33/24C07C49/675C07C45/78
Inventor 陈喆许冠华马忠俊
Owner ZHEJIANG PROVINCIAL HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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