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Compound with anti-tumor activity as well as preparation method and application thereof

A technology of anti-tumor activity and compounds, applied in the field of medicine, can solve problems affecting the quality of life of patients, non-specificity, drug resistance, etc., and achieve significant anti-tumor activity

Active Publication Date: 2022-07-01
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Radiotherapy and chemotherapy can properly prolong the survival time of patients, but their side effects are often very serious, which may be accompanied by a series of adverse reactions, affecting the quality of life of patients after surgery, and complications caused by surgical treatment may lead to death of patients
Because most of the traditional cytotoxic drugs are non-specific and have serious adverse reactions, and there are also problems such as drug resistance, they are subject to many limitations in clinical treatment.

Method used

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  • Compound with anti-tumor activity as well as preparation method and application thereof
  • Compound with anti-tumor activity as well as preparation method and application thereof
  • Compound with anti-tumor activity as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Separation, purification and identification of the compound of Example 1

[0044] 1. Separation and purification of compounds

[0045] (1) The seeds of Garcinia cambogia (collected from Menglun Town, Xishuangbanna, Yunnan Province) were naturally dried, pulverized with a pulverizer at a speed of 30,000 r / min for 2 min, and immersed in methanol solution with a volume fraction of 70% at room temperature to extract 3 times (solid-to-liquid ratio 2:1, g / ml), combined the three extracts, concentrated under reduced pressure with a rotary evaporator at a vacuum of about 90 kPa and a water bath temperature of 40 °C to remove the solvent to obtain an extract. The concentrated 70% methanol solution extract was reconstituted with deionized water to make an aqueous suspension, and extracted 3 to 5 times with an equal volume of petroleum ether reagent (petroleum ether: aqueous suspension=1:1, v / v), The extracts were combined and concentrated to remove the solvent by a rotary evapor...

Embodiment 2

[0057] Antitumor activity assay of the compound of Example 2

[0058] (1) Cell inoculation culture

[0059] In this experiment, five types of tumor cells were selected: leukemia (HL-60), lung cancer (A549), liver cancer (SMMC-7721), breast cancer (MCF-7) and colon cancer (SW480). The tumor cells used in this experiment were obtained from the Natural Medicine Activity Screening Center of Kunming Institute of Botany, Chinese Academy of Sciences. A single cell suspension was prepared with a culture medium (DMEM or RMPI640) containing 10% (v / v) fetal bovine serum (FBS), and the cells in the logarithmic growth phase were seeded on 96 cells at a density of 3000-15000 cells / well. The volume of each well is 100 μL, and the cells are inoculated and cultured 12 to 24 hours in advance.

[0060] (2) Determination of tumor cytotoxicity by MTS method

[0061] The cells were cultured for 24 hours before drug treatment, and compound 1 was treated with DMSO solvent at a final concentration ...

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Abstract

The invention discloses a compound with anti-tumor activity as well as a preparation method and application thereof. The molecular formula of the compound is C31H44O5, and the structural formula is shown as a formula (I). The compound is obtained by taking seeds of gamboge macrophyllum as a raw material, performing methanol extraction and petroleum ether extraction, then performing gradient elution separation on a petroleum ether layer extract through a silica gel column, then performing elution separation through a gel column, and finally performing purification through high performance preparative liquid chromatography. The compound obtained in the invention has obvious antineoplastic activity on various tumor cells, such as leukemia cells, lung cancer cells, liver cancer cells, breast cancer cells and colon cancer cells, so that the compound can be used for developing new antineoplastic drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to a compound with antitumor activity and a preparation method and application thereof. Background technique [0002] Malignant tumors, also known as cancers, are characterized by uncontrolled growth, immortalization, invasiveness, and the ability to form distant metastases of malignant cells. Currently, the main treatments for cancer are radiation therapy, chemotherapy and surgery. Radiotherapy and chemotherapy can appropriately prolong the survival time of patients, but their toxic and side effects are often severe, and may be accompanied by a series of adverse reactions, which affect the quality of life of patients after surgery, and complications from surgical treatment may lead to death of patients. Because most of the traditional cytotoxic drugs have non-specific and serious adverse reactions, and also have drug resistance and other problems, they are subject to m...

Claims

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Application Information

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IPC IPC(8): C07D313/08A61K31/335A61P35/00A61P35/02
CPCC07D313/08A61P35/00A61P35/02Y02A50/30
Inventor 黎平颜健权帆
Owner SOUTH CHINA AGRI UNIV
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