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Application of polyethylene glycol artesunate in preparation of antitumor drug

A technology of polyethylene glycol Artemisia annua and anti-tumor drugs, which is applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problem of unsatisfactory tumor inhibition effects, and achieve the effect of inhibiting proliferation and having a significant dose-effect relationship

Inactive Publication Date: 2017-05-31
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inhibitory effect of artemisinin compounds such as artesunate on tumors is not satisfactory

Method used

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  • Application of polyethylene glycol artesunate in preparation of antitumor drug
  • Application of polyethylene glycol artesunate in preparation of antitumor drug
  • Application of polyethylene glycol artesunate in preparation of antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Inhibitory effect of polyethylene glycol artesunate on proliferation of different tumor cell lines

[0035] 1. Test material

[0036] Polyethylene glycol artesunate Ⅰ, Ⅱ, Ⅲ, Ⅳ, made by Kunming Pharmaceutical Research Institute according to the methods disclosed in Chinese patent CN103450468B Example 1, Example 3, Example 2 and Implementation 4; artesunate, Chongqing Huafang Wulingshan Pharmaceutical Co., Ltd.; doxorubicin hydrochloride for injection (ADR), Zhejiang Hisun Pharmaceutical Co., Ltd.; human liver cancer cell line (HepG-2), human colon cancer cell line (HT-29), Human lung adenocarcinoma cell line (SPC-A-1), human prostate cancer cell line (PC-3), human gastric cancer cell line (MKN-28), human laryngeal cancer cell line (Hep2), human cervical cancer cell line ( Hela), human non-small cell lung cancer cell line (A549), human breast cancer cell line (MCF-7), human chronic myeloid leukemia cell line (K562), human promyelocytic leukemia cell line (HL-60...

Embodiment 2

[0056] Example 2 In vitro toxicity test of polyethylene glycol artesunate to normal cell human embryonic liver cells (L-02)

[0057] 1. Test material

[0058] Polyethylene glycol artesunate Ⅰ, Ⅱ, Ⅲ, Ⅳ, made by Kunming Pharmaceutical Research Institute according to the methods disclosed in Chinese patent CN103450468B Example 1, Example 3, Example 2 and Implementation 4; artesunate, Chongqing Huafang Wulingshan Pharmaceutical Co., Ltd.; human embryonic liver cell L-02, cell bank of Shanghai Institute of Biological Sciences, Chinese Academy of Sciences; XB-K-25 cell counting plate, glass instrument factory, Haimen County, Jiangsu Province; ZSBB-724 constant temperature water bath Pot, Shanghai Medical Constant Temperature Equipment Factory; synergy 2 multifunctional microplate reader, BioTek Company; HERA cell 150 C02 incubator, Thermo; RJ-TDL-508 cell centrifuge, Wuxi Ruijiang Centrifuge Factory; 96-well plate, Corning Corning.

[0059] 2. Test method

[0060] 2.1 Preparation ...

Embodiment 3

[0074] Example 3 Effect of polyethylene glycol artesunate on the growth of mouse transplanted sarcoma S180

[0075] 1. Experimental materials

[0076] Polyethylene glycol artesunate Ⅰ, Ⅱ, Ⅲ, Ⅳ, made by Kunming Pharmaceutical Research Institute according to the methods disclosed in Chinese patent CN103450468B Example 1, Example 3, Example 2 and Implementation 4; artesunate, Chongqing Huafang Wulingshan Pharmaceutical Co., Ltd.; S180 cell line, purchased from the cell bank of Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences; Kunming mice, 18-22g, half female, provided by the Experimental Animal Center of Kunming Pharmaceutical Group.

[0077] 2. Experimental method

[0078] 2.1 Drug preparation: Polyethylene glycol artesunate Ⅰ, Ⅱ, Ⅲ, Ⅳ and artesunate were prepared with normal saline to make three concentrations of 0.5, 1.0, 1.5mg / ml low, medium and high respectively, according to 0.2ml / 10g administration, the administration dosage is 10, 20, 30mg / kg r...

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Abstract

The invention provides an application of polyethylene glycol artesunate as shown in a formula (I) in preparation of an antitumor drug. Through in vitro tumor cytotoxicity tests and animal transplantation tumor tests, the polyethylene glycol artesunate as shown in the formula (I) can better inhibit proliferation of various human cancer cells without affecting proliferation of normal cells, so that the polyethylene glycol artesunate, as an anti-tumor drug, has a relatively good prospect. The formula is as shown in the specification.

Description

technical field [0001] The invention relates to the technical field of artesunate derivatives, in particular to the application of polyethylene glycol artesunate 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 affecting human life and health in my country include: lung cancer, gastric cancer, e...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61K31/77A61P35/00A61P35/02
CPCA61K31/357A61K31/77A61K2300/00
Inventor 黄照昌杨兆祥刘国光宋立明朱泽李鹏辉
Owner KPC PHARM INC
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