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Anti-tumor function of raw panoxadiol derivative

A technology of protopanaxadiol and its derivatives, which is applied in the field of biomedicine and can solve problems such as low drug selectivity, unseen compounds, serious problems, etc.

Inactive Publication Date: 2008-06-18
SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After the 1950s and 1960s, the relative survival rate of cancer patients was mainly improved by the advancement of surgical treatment and radiotherapy. It has been more than 40 years now, and the progress of surgical surgery and radiotherapy has reached its peak. It is difficult to expect a greater breakthrough. Chemotherapy can successfully cure or significantly prolong the patient's life, and plays an increasingly important role in the treatment of cancer; however, chemotherapy basically focuses on directly killing tumor cells, and this treatment mode often has the following problems: slow growth Poor or almost no effect on solid tumors; drug selectivity is very small, toxic and side effects are many and serious
[0009] This compound is also a derivative of PPD, which has been reported in the literature of Zhao Yuqing et al. , have not seen the report that the compound can be used in the treatment of related tumors

Method used

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  • Anti-tumor function of raw panoxadiol derivative
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  • Anti-tumor function of raw panoxadiol derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、25

[0048] Example 1 , 25hdt specific growth inhibition of cancer cells in vitro

[0049] 1.1. Ginsenoside compounds 25hdt, 25-OH-PPT, PPD, Rh2 and Rg3 inhibit the growth of human cancer cells in vitro

[0050] In this example, the inhibitory effect of 25hdt on the growth of human cancer cells in vitro was investigated with reference to ginsenoside compounds 25-OH-PPT, PPD, Rh2 and Rg3.

[0051] 25hdt, 25-OH-PPT, PPD, Rh2 and Rg3 were prepared at the concentrations of 0, 1 μM, 10 μM, 25 μM, 100 μM, 250 μM and 500 μM respectively.

[0052] Using the prepared above solution, human glioma cell lines A172 (p53 wild / mutant heterozygous, p53wt / mt) and T98G (p53 mutant, p53mt), human pancreatic cancer cell line HPAC (p53 wild type, p53wt) and Panc-1 (p53mt), human lung cancer cell lines A549 (p53wt), H1299 (p53 deletion, p53null), H358 (p53wt) and H838 (p53null), human breast cancer cell lines MCF7 (p53wt) and MDA- MB-468(p53mt), human prostate cancer cell lines LNCaP(p53wt) and PC3(...

Embodiment 2

[0063] Example 2 Anti-lung cancer experiment of 25hdt in lung cancer cell line in vitro

[0064] In the following examples, using 25-OH-PPT, PPD, Rh2 and Rg3 as references, the anti-lung cancer effect of 25hdt in lung cancer cell lines H838 and H358 in vitro was investigated.

[0065] 2.1, 25hdt induces apoptosis of human lung cancer cells in vitro

[0066] According to the method of Example 1.1, human lung cancer cell line H838 was treated with 25hdt and other 4 kinds of ginsenoside compounds 25-OH-PPT, PPD, Rh2 and Rg3 with prepared concentrations of 0, 1 μM, 10 μM, 25 μM and 50 μM respectively. and H358, after 48 hours of treated cells, the incidence of apoptotic cells was detected with AnnexinV-FITC Apoptosis Detection Kit (purchased from Biovision Company), using the same literature (Li M, Zhang Z, Hill D, Chen X, Wang H , Zhang R. Cancer Res., 65:8200-8208.2005) detected by the same method. According to the detection data of early and late apoptosis, relative to the ...

Embodiment 3、25

[0076] Example 3 Anti-prostate cancer experiment of 25hdt in prostate cancer cell lines in vitro

[0077] In this example, using 25-OH-PPT as a reference, the anti-prostate cancer effect of 25hdt on prostate cancer cell lines LNCaP and PC3 in vitro was investigated.

[0078] 3.1, 25hdt induces apoptosis of human prostate cancer cells in vitro

[0079] Using the method of Example 1.1, the cells of the human prostate cancer cell lines LNCaP and PC3 were treated with 25hdt and 25-OH-PPT with prepared concentrations of 0, 1 μM, 10 μM, 25 μM and 50 μM respectively. After 48 hours, the treated cells were , using the Annexin V-FITC apoptosis detection kit to detect the incidence of apoptotic cells, using the same method as in the literature (Li M, Zhang Z, Hill D, Chen X, Wang H, Zhang R. Cancer Res., 65: 8200-8208.2005) method detection. According to the detection data of early and late apoptosis, compared with the normal cells without drug treatment, the apoptosis index AI was ...

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Abstract

The invention discloses a compound 25hdt of protopanaxadiol derivative, that is, 20 ( R ) -25- hydroxy-dammarane type-3- Beta, 12 Beta, 20-triol, for preparing anti-cancer drugs. The compound 25hdt better inhibits tumor cell lines outside the human than PPD, ginsenoside- Rg3 and Rh2. At the same time, the compound 25hdt inhibits the tumor cells of the human from regulating, induces the tumor cells of the human to be apoptotic, inhibits the tumor cells of the human from proliferating and specifically inhibits the tumor cells of the human from growing. When the compound 25hdt is used to treat the cancers, the compound 25hdt does not cause the obvious changes of the weight of the experimental animal without any other toxic effect. Matched with other embolic chemotherapy or radiation methods to treat the cancers, the compound 25hdt can better improve the efficacy.

Description

technical field [0001] The present invention relates to the field of biomedicine, in particular to a protopanaxadiol derivative 25hdt, and more specifically to the application of the protopanaxadiol derivative 25hdt in preparing medicines for treating cancer. Background technique [0002] Cancer is the second largest disease in the world that ravages human life, and its mortality rate is second only to cardiovascular and cerebrovascular diseases, and it is one of the most important factors of human death. Among the 6 billion people in the world, there are currently about 35 million cancer patients. Worldwide, the number of deaths from cancer is about 6.3 million per year; according to the statistics of international authoritative investigation agencies, the number of cancer deaths will double to more than 10 million by 2020. [0003] In recent years, large-scale industrial production has led to the continuous deterioration of the human living environment, and various carcin...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P35/00A61P1/18A61P11/00A61P13/08A61P15/14A61P25/00
Inventor 赵余庆张瑞稳王伟韩凌王慧孙宝山
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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