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A tetrahydroquinoline alkaloid with anti-prostate cancer activity and its preparation method and application

An anti-prostate cancer, tetrahydroquinoline technology, applied in biochemical equipment and methods, microorganism-based methods, microorganisms, etc., can solve problems such as drug resistance and failure of clinical treatment of CRPC.

Active Publication Date: 2022-04-08
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

Although second-generation androgen receptor (AR)-targeted drugs such as enzalutamide have made breakthroughs in the treatment of CRPC, patients almost inevitably develop drug resistance after receiving treatment, resulting in clinical treatment of CRPC. fail

Method used

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  • A tetrahydroquinoline alkaloid with anti-prostate cancer activity and its preparation method and application
  • A tetrahydroquinoline alkaloid with anti-prostate cancer activity and its preparation method and application
  • A tetrahydroquinoline alkaloid with anti-prostate cancer activity and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: Preparation and structure identification of compound 1

[0026] One, the preparation of compound 1 as shown in formula (I)

[0027] 1. Microbial culture conditions:

[0028] Each 1000mL medium is prepared as follows: Take 20g of glucose, 10g of yeast extract, 3g of beef extract, 3g of corn steep liquor, 10g of soluble starch, 0.5g of dipotassium hydrogen phosphate, 0.5g of magnesium sulfate, and 2g of calcium carbonate, and then dissolve them in an appropriate amount of In water, dilute to 1000mL with water, sterilize at 121°C for 20min, and set aside.

[0029] Streptomyces sp.HNM0561 was inoculated into the above-mentioned culture medium, and cultured on a shaker at 28°C for 3 days to obtain a seed culture solution, and then the seed culture solution was inoculated into the above-mentioned medium at a volume ratio of 1%, at 28°C The shaker culture was carried out under the conditions for 11 days, and the fermentation product of Streptomyces sp. HNM0561 ...

Embodiment 2

[0040] Example 2: Inhibitory activity of Malaymycin (1) on two human prostate cancer cell lines

[0041] Human prostate cancer cell C4-2B was ordered from UroCor Inc. Oklahoma City, OK, USA; human prostate cancer cell 22Rv1 was ordered from American Type Culture Collection (American Type Culture Collection, Manassas, VA, USA).

[0042] CCK-8 assay was used in the human prostate cancer cell inhibitory activity test. Culture in RPMI1640 medium, collect the cells in the logarithmic growth phase, count, resuspend the cells, adjust the cell concentration to an appropriate concentration, inoculate a 96-well plate (500–1000 cells per well), and add 100 μl of cell suspension to each well. Cells at 37°C, 100% relative humidity, 5% CO 2 Incubate for 24 hours in the incubator. Dilute the compound to be tested to an appropriate concentration with medium, and add 50 μl / well to the cells. For C4-2B and 22Rv1 cells, the final concentration of compound 1 (Malaymycin) and positive control ...

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Abstract

The invention discloses a tetrahydroquinoline alkaloid with anti-prostate cancer activity, a preparation method and application thereof. Tetrahydroquinoline alkaloids, as shown in formula (I). The present invention prepares a compound 1 with anti-prostate tumor activity from marine Streptomyces sp.HNM0561, which can be used to develop anti-prostate tumor drugs, so the present invention not only provides candidate compounds for the development of new anti-prostate tumor drugs, but also It is of great significance to the development of China's marine microbial drug resources.

Description

Technical field: [0001] The invention belongs to the field of natural products, in particular to the separation and purification of microbial natural products and their application in the preparation of antitumor drugs. Background technique: [0002] Prostate cancer is the most common malignant tumor in men, ranking second in the cause of cancer death in men worldwide, and the tumor with the highest incidence rate in urology in my country. most common tumor. Endocrine therapy is the main treatment for prostate cancer, but after a median time of 14-30 months, almost all patients will transform into castration-resistant prostate cancer (CRPC). Although second-generation androgen receptor (AR)-targeted drugs such as enzalutamide have made breakthroughs in the treatment of CRPC, patients almost inevitably develop drug resistance after receiving treatment, resulting in clinical treatment of CRPC. fail. Natural products are an important source of innovative drug research. Durin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/18A61P35/00C12P17/12C12N1/20C12R1/465
CPCC07D215/18A61P35/00C12P17/12C12N1/20
Inventor 王俊锋王军舰黄小龙刘永宏
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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