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Application of Talaroconvolutin A in anticancer drugs and foods

An anticancer drug and drug technology, applied in the field of microbial metabolite application

Active Publication Date: 2020-09-11
JINING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there are no very effective natural compounds used in the treatment of digestive system cancers. Therefore, it is necessary to find an effective natural compound that can be used in the above-mentioned digestive system cancer drugs to overcome the problems caused by traditional chemotherapy drugs. Side effects and drug resistance in patients

Method used

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  • Application of Talaroconvolutin A in anticancer drugs and foods
  • Application of Talaroconvolutin A in anticancer drugs and foods
  • Application of Talaroconvolutin A in anticancer drugs and foods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] How to obtain Talaroconvolutin A: See: Antifungal Substances Against Pathogenic Fungi, Talaroconvolutins, From Talaromyces Convolutus Authors: Shohei Suzuki, Tomoo Hosoe, Koohei Nozawa, Ken-ichi Kawai, Takashi Yaguchi, and Shun-ichi Udagawa Journal: Journal of Natural Product.

[0108] At room temperature, first dissolve Talaroconvolutin A in DMSO at a concentration of 10 mg / mL, then use corn oil as a co-solvent to add to DMSO at a concentration of 0.5 mg / mL; dissolve Talaroconvolutin A in DMSO and set aside;

[0109] Cancer cells were inoculated at a co-density of 30%, and 24 hours later, different concentrations of Talaroconvolutin A were added;

[0110] After 48 hours, cell viability was detected by CCK8 method.

[0111] The cells in each group were treated without Talaroconvolutin A as the control (100% relative viability).

[0112] From attached figure 1 It can be seen that different concentrations of Talaroconvolutin A have tumor suppressor effects in three diff...

Embodiment 2

[0114] Regarding the effect of different concentrations of Talaroconvolutin A on the inhibition of cancer cell DNA synthesis in the colon cancer cell line SW480, the inventors also conducted a test. The specific method was to add different concentrations of Talaroconvolutin A after the cells were inoculated at a co-density of 30% for 12 hours. After incubation for 24 hours, the DNA synthesis rate of cancer cells was detected by Edu method. Thirty minutes after EdU was added to the medium, the medium was discarded and cells were fixed with 4% paraformaldehyde.

[0115] Then operate according to the instructions of the EdU cell proliferation kit of Beyontien Company. EdU is a substance that can only be embedded in newly synthesized DNA, but not in the original DNA, and it will appear red under a fluorescence microscope; while Hoechst33342 can be embedded in all DNA, and it will appear blue under a fluorescence microscope. Using the ratio of red to blue, the rate of DNA synthesi...

Embodiment 3

[0118] In order to study the long-term effect of different concentrations of Talaroconvolutin A on colon cancer cells, the inventors used 0.5-2.0 μg / mL of Talaroconvolutin A at 50 cells / cm 2 In the culture system, the inhibition of colony formation was observed every 2 days, with image 3 The results in showed that after 12 days of treatment, 0.5μg / mL Talaroconvolutin A can significantly inhibit the formation of colonies, and 2.0μg / mL can almost completely inhibit the formation of tumor cell clones.

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Abstract

The invention belongs to the field of applications of microbial metabolites, and particularly relates to an application of Talaroconvolutin A in preparation of drugs for treating cancers and health foods. The Talaroconvolutin A disclosed by the invention can be applied to the drugs and the foods. The beneficial effects are as follows: (1) the IC50 is low, the minimum IC50 of the Talaroconvolutin Aat the cellular level is less than 1 [mu]g / mL, and the effective concentration at the animal level can be as low as 5 mg / kg, which is obviously superior to that of cis-platinum chemotherapeutic drugs; (2) the Talaroconvolutin A kills cancer cells by inducing ferroptosis instead of inducing cell apoptosis and cell autophagy, so that the drug resistance caused by cell apoptosis and cell autophagy drugs is avoided, and the drug resistance problem of the antitumor chemotherapeutic drugs is expected to be solved when the Talaroconvolutin A is applied to the drugs for inhibiting the cancers; (3) the Talaroconvolutin A is more effective than a currently widely recognized ferroptosis inducer Erastatin; and (4) the Talaroconvolutin A has small toxic and side effects on animals, namely the Talaroconvolutin A does not cause weight change of mice in an effective dosage range, does not cause blood routine change, and has no obvious liver and kidney injury.

Description

technical field [0001] The invention belongs to the field of application of microbial metabolites, and in particular relates to the application of Talaroconvolutin A in the preparation of anticancer drugs, especially digestive system cancer drugs, respiratory system cancer drugs or food. Background technique [0002] Colon cancer, rectal cancer and other digestive system cancers are a kind of digestive tract tumors that occur in the human colon mucosal epithelium. With the lack of low-fiber foods and trace elements and vitamins in the human diet, the continuation of bad living habits, and the increase in the mental pressure of survival, patients are increasingly migrating to younger ages, and the incidence rate is higher in men. The incidence of bowel cancer is increasing worldwide. [0003] In the current medical level, comprehensive treatment is the mainstream direction for the treatment of the above-mentioned digestive system cancers, that is, the organic combination of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4015A23L33/135A61P35/00
CPCA23V2002/00A61K31/4015A23L33/135A61P35/00A23V2200/308
Inventor 夏勇杨小龙
Owner JINING MEDICAL UNIV
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