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Application of piericidin compound Piericidin A in preparation of anti-renal cancer drugs

A technology of fenopteromycin and compounds, applied in the field of natural products, can solve problems such as weak research on mechanism of action

Inactive Publication Date: 2017-04-19
SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Penidaemycins have been reported to have insecticidal and antibacterial activities, and also have inhibitory activity on some tumor cells, but the mechanism of action is very weak, and the anti-tumor potential needs to be further explored [4]

Method used

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  • Application of piericidin compound Piericidin A in preparation of anti-renal cancer drugs
  • Application of piericidin compound Piericidin A in preparation of anti-renal cancer drugs
  • Application of piericidin compound Piericidin A in preparation of anti-renal cancer drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Inhibitory activity of Piericidin A (Piericidin A) on three renal cancer cell lines

[0035] Three human renal cell lines were ordered from Shanghai Cell Resource Center, Chinese Academy of Sciences: 786-O human renal cell line (Cat#TCHu186); ACHN human renal cell line (Cat# TCHu199); OS-RC-2 human renal cell line strain (Cat# TCHu40).

[0036] The inhibitory activity of renal cancer cells was tested by CCK-8 assay. Collect the cells in the logarithmic growth phase, count them, resuspend the cells with complete medium, adjust the cell concentration to an appropriate concentration (determined according to the results of the cell density optimization test), inoculate a 96-well plate, and add 100 μl of cell suspension to each well. Cells were incubated for 24 hours at 37°C, 100% relative humidity, 5% CO2 incubator. Dilute the compound to be tested to an appropriate concentration with complete medium, and add 25 μl / well to the cells. For ACHN cells, the final ...

Embodiment 2

[0048] Example 2: Effects of Piericidin A on the Apoptosis of Three Renal Cancer Cell Lines ACHN Cells

[0049]Take the ACHN cells in the logarithmic growth phase and adjust the cell concentration to 2×10 6 / ml, inoculated in 50mL culture flasks, divided into three batches, each batch was divided into four groups, group 1 was blank control, group 2, 3, and 4 were added Piericidin A respectively, so that the final concentration was 50, 200 and 400nM. After the cells adhered to the wall, the culture medium was replaced and drugs were added. Two batches were cultured for 24 hours and 48 hours respectively, and the cells were digested and collected after light microscope observation and photography. The third batch was cultured until 72 hours for light microscope observation and photography. The collected cells were washed with pre-cooled PBS at 4°C, centrifuged at 1000r / min, 2×5min. After the cells were resuspended in the buffer, 100 μL of the cell suspension was taken in a flow...

Embodiment 3

[0052] Embodiment 3: Piericidin A suppresses the experiment of Bcl-2 protein expression

[0053] ACHN cells in logarithmic growth phase were taken, and Piericidin A was added to make the final concentration of 0, 10, 50 and 200nM, and the effect was 48h. ① Extraction of total protein: After washing twice with PBS, add 200 μL of protein lysate RIPA and 5 μL / mL of PMSF to each sample, place in an ice box for 40 min; centrifuge at 15 000 r / min, 4°C for 20 min; take the supernatant That is the required protein extract, and aliquoted in 100 μL tubes. After detecting the protein concentration with a micro-ultraviolet spectrometer, store it at -80°C for later use. ② Polyacrylamide gel electrophoresis (SDS-PAGE electrophoresis): Take 100 μL of protein sample and add 4×loading buffer, denature at 100°C for 10 minutes; load the sample, and run electrophoresis for about 1.5 hours. ③Membrane transfer: The protein was transferred to nitrocellulose membrane (PVDF) by semi-dry electrotrans...

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Abstract

The invention discloses an application of a piericidin compound Piericidin A in preparation of anti-renal cancer drugs. The Piericidin A having the structure represented by the formula (I) has inhibitory effect with different intensities on three human renal cancer cell strains, especially has the strongest inhibitory activity on human adrenal carcinoma cells ACHN, and has the half inhibition rate IC50 reaching 0.40 [mu]M. Cell apoptosis experiments show that the Piericidin A can obviously induce late apoptosis of the human adrenal carcinoma cells ACHN, and a fact of inhibiting an anti-apoptosis protein Bcl-2 is one of anti-renal cancer action mechanisms. Therefore, the lead compound Piericidin A can be used as a Bcl-2 inhibitor for development of the anti-renal cancer drugs. The invention provides the new lead compound for development of new microbial-source anticancer drugs.

Description

[0001] Technical field: [0002] The invention belongs to the field of natural products, and in particular relates to the application of piericidin A compound piericidin A in the preparation of anti-kidney cancer drugs. [0003] Background technique: [0004] For a long time, malignant tumors have become one of the major diseases that seriously endanger human life and quality of life. [1] . According to reports, malignant tumors have become the leading cause of death among Chinese residents. For the treatment of malignant tumors, natural products and their derivatives play an important role. According to reports, from 1981 to 2008, anti-tumor drugs derived from natural products accounted for more than 60% of anti-tumor drugs on the market, and the number of new natural products and their derivatives as new anti-tumor drugs is still increasing [2] . Kidney cancer is one of the ten deadliest cancers in the world, and its incidence rate is second only to bladder cancer among u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61P35/00
CPCA61K31/44
Inventor 周雪峰唐斓方伟李坤龙刘永宏
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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