Three piericidin natural products and application thereof to preparation of anti-kidney cancer medicines

A pteromycin and kidney cancer technology, applied in the field of microbial natural products, can solve the problems of weak research on the mechanism of action, anti-tumor potential to be further explored, etc.

Active Publication Date: 2019-02-26
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 o

Method used

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  • Three piericidin natural products and application thereof to preparation of anti-kidney cancer medicines
  • Three piericidin natural products and application thereof to preparation of anti-kidney cancer medicines
  • Three piericidin natural products and application thereof to preparation of anti-kidney cancer medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: the preparation of piericidins G, I, and J of piericidins compound

[0024] 1. Solid culture of Streptomyces sp.HBERC-58855

[0025] Streptomyces sp.HBERC-58855 (preservation number is CCTCC NO:M 2017186) is isolated from the mangrove bottom mud, and the strain is preserved on the slant of ISP-2 medium. The composition of ISP-2 medium is: yeast extract powder 4g, glucose 4g, malt extract powder 10g, coarse sea salt 30g, agar powder 20g, water 1000mL, pH 7.2-7.4, sterilized for later use.

[0026] 2. Amplified fermentation of Streptomyces sp.HBERC-58855

[0027] Take a small amount of Streptomyces sp.HBERC-58855 slant strains for seed fermentation culture. The medium is 20 grams of mannitol, 10 grams of soybean peptone, 2.5 grams of soybean oil, 0.35 grams of dipotassium hydrogen phosphate, 950 ml of deionized water, and adjust the pH to 7.0 , dilute to 1000 ml, fill 100 ml in a 500 ml Erlenmeyer bottle, and sterilize for later use. The culture condition...

Embodiment 2

[0030] Example 2: Structural identification of Piericidins G, I, and J

[0031] 1.Piericidins G, I, and J physicochemical property data

[0032] Compounds Piericidins G, I, and J were subjected to structural analysis and testing, and the following physical and chemical property data were obtained:

[0033] Compound piericidin G: colorless oil, -5.5(c 0.218, MeOH); IR(ATR)ν max 3312,2945,2835,1635,1472,1417,1126,1018,667,600,562cm -1 ; CD (0.2mg / ml, MeOH), λmax (Δε) 240 (5.8), 223 (-7.8); 1 H and 13 C NMR data in Table 1 and Table 2; (+)-HR-ESIMS m / z 414.2657[M+H] + (calcd for C 25 h 36 NO 4 414.2600).

[0034] Compound piericidin I: colorless oil, 0.08(c 0.12, MeOH); IR(ATR)ν max 3335,2945,2833,1448,1416,1020,667,600,552cm -1 ; CD (0.342mg / ml, MeOH), λmax (Δε) 237 (-1.5), 205 (3.5); 1 H and 13 C NMR data in Table 1 and Table 2; (+)-HR-ESIMS m / z 504.3320[M+H] + (calcdforC 29 h 45 NO 6 504.3280).

[0035] Compound piericidin J: colorless oil, 2.22 (c 0...

Embodiment 3

[0052] Example 3: Inhibitory Activity of Piericidins G, I, and J on Renal Cancer Cells

[0053] Two human kidney cancer cell lines were ordered from the Shanghai Cell Resource Center of the Chinese Academy of Sciences: ACHN human kidney cancer cell line (Cat#TCHu199); OS-RC-2 human kidney cancer cell line (Cat#TCHu40); human renal tubular epithelial cell HK- 2Provided by School of Pharmacy, Southern Medical University.

[0054] The same type of natural product piericidin A (PiericidinA) and the marketed drug Sorafenib for the treatment of renal cancer were used as positive controls.

[0055] The cell inhibitory activity experiment adopts CCK-8 detection method. 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. ...

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Abstract

The invention discloses three piericidin natural products and application thereof to preparation of anti-kidney cancer medicines. The three piericidin compounds, namely piericidins G, I and J, are unreported novel compounds. The invention discloses that the piericidin compounds, namely piericidins G, I and J, have the obvious activity in inhibiting two kidney cancer cells, and the piericidins canbe applied to the preparation of the anti-kidney cancer medicines. Therefore, the invention provides alternative compounds for development of the novel anti-kidney cancer medicines and is of a great significance in developing marine microbial medicine resources in China.

Description

Technical field: [0001] The invention belongs to the field of microbial natural products, and in particular relates to three natural products of penicillins and their application in the preparation of anti-kidney cancer drugs. Background technique: [0002] For a long time, malignant tumors have become one of the major diseases that seriously endanger human life and quality of life. According to reports, malignant tumors have become the leading cause of death among Chinese residents, and the mortality rate of malignant tumors in my country has shown an upward trend in the past 20 years, and even ranks at the forefront of the mortality rate of malignant tumors in the world. 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 the anti-tumor drugs on the market, and the number of new natural products and their ...

Claims

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Application Information

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IPC IPC(8): C07D213/69A61K31/44A61P35/00
CPCA61P35/00C07D213/69
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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