Anti malignant tumour southern radix bupleuri extract preparing method

A technology of compounds and substituents, which is applied in the field of preparation of anti-malignant tumor Nanbupleurum extract, can solve the problems of paclitaxel failure, paclitaxel β microtubule binding, strong cytotoxicity, etc.

Inactive Publication Date: 2010-05-12
BUDDHIST TZU CHI GEN HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to the research of Rao et al. in 1995, these tumor cells (such as the human lung cancer cell line AT-12) will change the six subunit configurations (Subunit Configuration) that make up the β microtubules, so that paclitaxel not only cannot interact with the β microtubules Combined, it will be excluded by the cells as a foreign substance (Ion-pumping), causing tumor cells to gradually develop resistance to paclitaxel and gradually lose efficacy in the later stages of chemotherapy
[0011] And, with existing other anticancer drugs, such as 5-fluoropyrimidine diketone (5-Fluorouracil), epothilone (Epothilone), cisdiammine dichloroplatinum (commonly known as Cisplatin), procarbazine (Procarbazine) ) and cyclophosphamide (Cyclophosphamide) alone or in combination with paclitaxel to treat patients who are resistant to taxanes, the clinical treatment effect is not good, and it is also found from the cell experiment that the current anticancer drugs are difficult to inhibit the paclitaxel resistance. The drug-resistant tumor cell line (Taxol-resistance TumorCell Line) proliferates. However, if the dose of the drug is increased, for example, when the dose of paclitaxel is increased to 300 mg per kg and injected into rats, the cytotoxicity of paclitaxel is very strong, often in After administration, it causes massive necrosis of normal cells (Necrosis).

Method used

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  • Anti malignant tumour southern radix bupleuri extract preparing method
  • Anti malignant tumour southern radix bupleuri extract preparing method
  • Anti malignant tumour southern radix bupleuri extract preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0113] Example 1: Extraction Method of Antineoplastic Active Components of Southern Bupleuri

[0114] The Nan Bupleurum used in the present invention is all green single leaves alternate, and is the narrow leaf Bupleurum scorzonerifolium Willd (Bupleurum scorzonerifolium Willd in China). After drying and crushing, 6 kg of Nan Bupleurum will be processed at room temperature. Hu powder soaked in 20 liters of acetone, stirred for four hours, concentrated and filtered, and repeated rough extraction four times to obtain the acetone crude extract of Bupleurum chinensis (abbreviated as BS-A), and extract the residue with methanol to obtain the methanol extract of Bupleurum bupleurum ( referred to as the BS-M layer), and then extract the residue with water to obtain the South Bupleurum aqueous layer extract (abbreviated as the BS-W layer). After that, the South Bupleurum acetone crude extract was dissolved in 95% methanol aqueous solution, and After n-Hexane (n-Hexane) extraction th...

Embodiment 2

[0117] Example 2: The structure of the active components of Nanbupleurum tumor suppressor

[0118] The main representatives of the third component, the eighth component, the fourteenth component and the fifteenth component separated from the acetone extract of Bupleurum chinensis by the above-mentioned extraction method were analyzed by mass spectrometry (Mass Spectrum) and nuclear magnetic resonance spectrum (Nuclear Magnetic Resonance Spectrum, NMR) after defining the molecular weight and structure of each compound, the results are shown in the following table:

[0119] Table 1: Isolated Compounds with Tumor Suppressive Effects from Acetone Extract of Bupleurum chinensis

[0120]

[0121]

[0122] After molecular structure integration and induction, it was found that the South Bupleurum extract, which has an inhibitory effect on tumor cell lines of human liver cancer, ovarian cancer, lung cancer, malignant glioma and colorectal cancer, has a compound carbon skeleton ba...

Embodiment 3

[0138] Example 3: Effect of Bupleurum bupleuri extract on Cell Proliferation

[0139] South Bupleurum Acetone Crude Extract (BS-A), South Bupleurum Methanol Crude Extract (BS-M), South Bupleurum Water Layer Crude Extract (BS-W) and The eighth component (BS-(8)) isolated from the BS-A extract was added to the culture medium of human liver cancer cell lines, ovarian cancer cell lines, lung cancer cell lines, malignant glioblastoma and colorectal cancer cell lines During the 7 days of adding the drug, the inhibition of each tumor cell line was observed. In this example, the lung cancer cell line A549 and the colorectal cancer cell line HT-29 were taken as examples. When the extracts were administered for three days, the tumor cell counts (Tumor Cell Counts) were reduced by adding 60 mg of acetone crude extract of Bupleurum chinensis. Similar to the number of tumor cells reduced by 600 mg of Nabupleurum methanol crude extract, it shows that the content of tumor suppressor compo...

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Abstract

The invention is a kind of bupleurum root ext extracted from the southern bupleurum root and used to cure the hyperpiasia diseases and its method of extraction. The active components of the bupleurumroot ext at least includes the heterocyclic compound, with the Z or E position of the carbon 2(5), centered around the gamma- butyrolactone and the new bupleurum root lactone, isobupleurum root lactone, bupleurum root lactone similar and its ramification contained in the heterocyclic compound. From the results of the experiments of the drug toxicity, characteristics of the cell, animal experimentsand histologic section, we can know that the ext of the outhern bupleurum root can restrain the cancer cells of the liver cancer, lung cancer, oophoroma, large intestine cancer or swart brain glia cell tumour and specially kill the tomour cells with drug resistance to the taxales medicines after the chemotherapy. It can be a new resource of the drug screening of the tumor inhibitor.

Description

technical field [0001] The present invention relates to a kind of plant extract used in the field of cancer treatment, which is extracted from natural products to treat Cell Proliferative Disorder and its extraction method, especially about a plant extract isolated from Bupleurum scorzonerifolium ), and heterocyclic compounds with γ-Butyrolactone (γ-Butyrolactone) core as the treatment of human liver cancer (Hepatoma), lung cancer (Lung cancer), ovarian cancer (Ovarian cancer), malignant glioma (Human Malignant Glioblastoma) and colorectal cancer (Colorectal Cancer) and other cancer cells of the main active ingredient of South Bupleurum extract and its extraction method. Background technique [0002] Cancer, a cell proliferative disease, has become the top ten cause of death. According to the statistics of Boring et al. in 1993, about 526,000 people in the United States die of cancer every year. Taking breast cancer as an example, it has almost become the main killer of wom...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/26C07D307/33C07D333/32C07D345/00C07D407/06C07B63/00B01D11/02A61K31/365A61K31/40A61K31/381A61P35/00
Inventor 林欣荣韩鸿志
Owner BUDDHIST TZU CHI GEN HOSPITAL
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