Application of artemisinin B in preparation of antitumor drugs

An anti-tumor drug, artemisinin technology, applied in the field of biomedicine to achieve the effect of high bioavailability and good water solubility

Inactive Publication Date: 2012-08-01
于荣敏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many derivatives with higher antimalarial and antitumor activities have been found

Method used

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  • Application of artemisinin B in preparation of antitumor drugs
  • Application of artemisinin B in preparation of antitumor drugs
  • Application of artemisinin B in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1. The Inhibitory Effect of Artemisinin B on the Specific Proliferation of Tumor Cells in Vitro

[0028] 1.1 Methyl azolium salt (MTT) colorimetric method to determine the inhibitory effect of drugs on the proliferation of 8 tumor cell lines

[0029] In this experiment, cisplatin was used as a positive control for each solid tumor cell line, and Adriamycin (ADR for injection) was used as a positive control for K562 cell line, and conventional methylazozolate (MTT) colorimetric The inhibitory effect of the drug on the proliferation of 8 tumor cell lines was investigated.

[0030] Artemisinin B was first dissolved in DMSO to prepare a 100 mM mother solution, and stored at room temperature. When used, the maximum final volume of administration is ≤1%, and it is diluted into serial concentrations with 1640 complete medium. Positive control drug concentration settings: 1.22, 3.67, 11.11, 33.33 μM for cisplatin, 0.125, 0.25, 0.5, 1 μM for doxorubicin. Human cervica...

Embodiment 2

[0039] Embodiment 2, anti-tumor experiment of artemisinin B on human chronic myeloid leukemia cells (K562) in vitro

[0040] 2.1 Artemisinin B induces apoptosis of human chronic myeloid leukemia cells (K562) in vitro

[0041] According to the method of Experiment 1.1, 0, 10, 20, and 40 μM artemisinin B were prepared respectively, and after K562 cells were treated for 48 hours, cell apoptosis was detected by flow cytometry with FITC-AnnexinV / PI fluorescence double staining. Centrifuge at 1000rpm / min for 5min, and wash the cells twice with PBS at room temperature. Remove the supernatant, add 100 μL of apoptosis buffer containing Annexin V and PI, mix well, incubate in the dark for 20 min, and immediately detect by flow cytometry. According to the detection data of early and late apoptosis, the apoptosis rate AP was calculated and analyzed and compared. The result is as figure 2 shown.

[0042] figure 2 The results showed that artemisinin B induced apoptosis in a dose-depe...

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Abstract

The invention discloses an application of an artemisinin compound artemisinin B having a structure shown in the specification in the preparation of antitumor drugs. Pharmacological and pharmacodynamic experiments in the invention prove that the artemisinin B has effects of specific propagation inhibition, apoptosis induction, cell cycle affection and the like on in vitro cultured human tumor cells. The artemisinin B is a low-toxicity unique-effect compound obtained from a natural component Artemisia annua, and provides a new drug selection for the clinical tumor treatment.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of an artemisinin compound, that is, artemisinin B in the preparation of antitumor drugs. Background technique [0002] Malignant tumors are common and one of the major diseases that seriously threaten human life and quality of life. In 2000, there were about 10 million new cancer cases worldwide, 6.2 million deaths, and 22.4 million existing cases. The incidence of cancer has been on the rise for nearly 30 years in the late 20th century. According to the current trend, the World Health Organization (WHO) predicts that by 2020, with the global population reaching 8 billion, there will be 20 million new cancer cases, including deaths It will reach 12 million, and cancer will become the first killer of human beings in the new century. Statistics show that the common malignant tumors of human life and health in my country include: lung cancer, gastric cancer, esophageal c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P35/00A61P35/02C07D493/20
CPCA61K31/365C07D493/20A61P35/00A61P35/02
Inventor 于荣敏田甜朱建华宋丽艳
Owner 于荣敏
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