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Application of thiophene compound

A technology of compound and thiophene, which is applied in the field of herbal medicinal ingredients and anti-tumor compounds, can solve the problem of insensitivity to chemotherapy and radiotherapy treatment of toxic side effects of tumor cells, and achieve the effect of being conducive to popularization and application, simple structure and strong activity

Inactive Publication Date: 2009-12-16
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] At present, chemotherapy and radiotherapy are still the first choice for the treatment of cancer. Although the two have achieved considerable curative effect on the treatment of tumors, they have relatively large toxic and side effects due to the lack of specificity to tumor cells, and some tumor cells have a certain effect on chemotherapy. and insensitivity to radiotherapy, thus limiting their clinical application to a large extent

Method used

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  • Application of thiophene compound
  • Application of thiophene compound
  • Application of thiophene compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The in vitro antitumor effect of embodiment 1 compound I-a~I-c

[0023] Take the cells in the logarithmic phase 3×10 per well 4 Inoculate on a 96-well plate, discard the supernatant after 12 hours, and administer according to the following groups: the normal control group and the drug-dosed group (concentration 0-100 μ M), each group has 6 duplicate wells, cultured for 24 hours, discarded the supernatant, added Incubate 50 μl of culture solution with MTT for 4 hours (0.5 mg / mL), add 100 μl DMSO, shake for 1 hour, and measure the OD value at 570 nm on a microplate reader.

[0024] The results showed that after adding the drug, the tumor cell activity decreased significantly, and the tumor cell activity decreased with the increase of the drug concentration. See Table 1, PC3 (prostate cancer cells), U87 (glioma cells), Hela (cervical cancer cells), SGC-7901 (gastric cancer cells), H460 (lung cancer cells), HepG2 (liver cancer cells), SW480 (colon cancer cells) Cancer cel...

Embodiment 2

[0027] The quinone reductase induction experiment of embodiment 2 compound I-a~I-c

[0028] Take Hepa 1c1c7 and c1 cells in logarithmic phase, 2×10 per well 4 Inoculate on a 96-well plate, discard the supernatant after 24 hours, and administer according to the following groups: normal control group and drug-dosed group (concentration 0-100 μ M), each group has 6 duplicate holes, culture for 24 hours, discard the supernatant, add Digitonin was used to lyse the cells, and then 200 μl of culture medium with MTT was added to incubate for 5 minutes (0.5 mg / mL), and the OD value was measured at 550 nm on a microplate reader.

[0029] The results showed (see Table 2) that the drug could significantly induce the expression of quinone reductase after adding the drug, and the cells were all purchased from ATCC.

[0030] Table 2 The results of quinone reductase induction of thiophene compounds I-a~I-c

[0031]

Embodiment 3

[0032] NFkappaB inhibition experiment of embodiment 3 thiophene compound I-c

[0033] Take RAW264.7 cells in the logarithmic phase, inoculate them on a 10cm culture dish, discard the supernatant after 24 hours, and administer according to the following groups: normal control group and treatment group, cultivate for 24 hours, discard the supernatant, add cell lysate, and then By SDS-PAGE electrophoresis, it shows that it can significantly inhibit the expression of NFkappaB, see figure 1 . From figure 1 It can be seen that compound I-c can significantly inhibit the expression of NFkappa as the concentration of the compound increases after acting on the cells for 24 hours.

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Abstract

The invention provides application of a thiophene compound in preparing medicaments for resisting tumors. The tumors comprise cerebroma, lung cancer, liver cancer, mammary cancer, prostatic cancer, pancreatic cancer, cervical cancer, stomach cancer, esophageal cancer and the like. The results of screenings on anti-tumor actions and cancer chemical prophylaxis performed by an MTT method show that the thiophene compound is concentration-dependent to inhibit the multiplication of tumor cells and can remarkably induce the expression of quinone reductase; and the results of a research on anti-inflammatory actions performed by a Westernblot method show that the thiophene compound can remarkably inhibit the expression of NFkappaB. The thiophene compound can also be applied to preparing cancer chemical prophylaxis medicaments, anti-inflammatory medicaments and the medicaments for inhibiting the generation of tumor vessels.

Description

technical field [0001] The invention belongs to the field of herbal medicinal components and antitumor compounds, and particularly relates to the application of a thiophene compound extracted from Echinops grijisii Hance. Background technique [0002] At present, more than 6 million people die of cancer every year in the world, and 8 million new cases are diagnosed, and this number is still increasing year by year. Among the 1.3 billion people in my country, there are millions of new cancer patients every year, about 2 million patients waiting for treatment, and about 1.3 million deaths. It is estimated that by 2006, 1.7 million people will die of cancer in my country, and cancer has become the first cause of death. [0003] At present, chemotherapy and radiotherapy are still the first choice for the treatment of cancer. Although the two have achieved considerable curative effect on the treatment of tumors, they have relatively large toxic and side effects due to the lack o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/381A61P35/00C07D333/10C07D333/08C07D333/16C07D333/32C07D333/36
Inventor 马忠俊赵小峰张潇雨
Owner ZHEJIANG UNIV
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