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Naphthaquinone compound derived from marine microbes, and preparation method and application thereof

A compound, naphthoquinone technology, applied in the field of naphthoquinone compounds, can solve the problems of large toxic and side effects, limited dose increase and clinical treatment effect, etc., achieves low application cost, broad development and application prospects, improved targeting and high efficiency sexual effect

Inactive Publication Date: 2015-01-07
大丰海洋生物医药研究所 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, such drugs still have relatively large toxic and side effects, such as myelosuppression and cardiotoxicity, which greatly limit their dose increase and clinical therapeutic effect.

Method used

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  • Naphthaquinone compound derived from marine microbes, and preparation method and application thereof
  • Naphthaquinone compound derived from marine microbes, and preparation method and application thereof
  • Naphthaquinone compound derived from marine microbes, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Embodiment 1: the preparation of naphthoquinone compound CWL-168

[0026] Preparation of bacterial classification: use seawater PDA culture medium, high-temperature sterilization, make plate, place under normal temperature state, inoculate Penicillium chrysogenum (can be purchased from China Marine Microorganism Culture Collection and Management Center, preservation number: MCCC 3A00005) mycelia, cultured statically for 4-5 days at 28°C, as a strain; the seawater PDA medium consists of 200g of potatoes, 20g of glucose, 15-20g of agar, and 1L of seawater;

[0027] Preparation of fermented seed liquid: put seawater PDA liquid culture medium into multiple Erlenmeyer flasks respectively, after high temperature sterilization, inoculate the above strains, shake and cultivate at 180rpm / min at 28°C for 2-3 days, and use the culture as seed liquid;

[0028] Inoculation: adopt solid fermentation method, prepare fermentation bottle, add rice solid fermentation medium, sterilize a...

Embodiment 2

[0034] Embodiment 2: MTT method assays the antitumor activity of naphthoquinone compound CWL-168

[0035] In this example, an in vitro cytotoxicity test was used to determine the antitumor activity of the compound CWL-168 by detecting the survival rate of human or mouse cancer cells cultured in vitro after adding CWL-168.

[0036] The selected cell lines are: human non-small cell lung cancer H1299, A549, human large cell lung cancer H460, human small cell lung cancer H446, mouse melanoma B16, B16-F10, human breast cancer MD-MBA-231, MCF7, human gastric cancer MGC803 , human pancreatic cancer PANC-1, human cervical cancer HeLa, human osteosarcoma U2OS, human liver cancer HepG2, human colon cancer HCT116, and human laryngeal cancer HEP2. MTT method was used to determine the half-inhibitory concentration IC when the survival rate (or death rate) of each tumor cell was 50%. 50 (The above cells can all be purchased from ATCC).

[0037] The half-inhibitory concentration IC50 of th...

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Abstract

The invention discloses a naphthaquinone compound derived from marine microbes, and a preparation method and application thereof. The systematic name of the compound is 1,2,3,4-tetrahydro-1,2,5-trihydroxy-6,7-dimethoxy-3-methyl-9,10-anthracenone, and the structure is disclosed as Formula (I). The naphthaquinone compound can be continuously obtained by fermentation. The compound has the advantages of high antineoplastic activity, environment friendliness and low use cost, and can be used for preparing antineoplastic drugs. The active naphthaquinone compound derived from microbes is small in amount and simple in structure, and can be used as a precursor of antineoplastic drugs; the structural modification and reconstruction on the basis of the prior art enhance the antineoplastic targeting property and efficiency; and when being used for developing drugs for treating human stomach cancer, human lung cancer, mouse melanoma, human mammary cancer, human pancreatic cancer, human cervical carcinoma, human osteogenic sarcoma, human liver cancer, human colon cancer and human laryngocarcinoma, the naphthaquinone compound has wide application prospects.

Description

technical field [0001] The invention relates to the field of compounds, in particular to a naphthoquinone compound derived from marine microorganisms, a preparation method and an application thereof. Background technique [0002] Malignant tumors have been a serious threat to human health and life for a long time. According to the statistics of the World Health Organization, about 6 million people are killed by cancer every year in the world, and it is estimated that it will rise to 10 million people by 2020. However, there is still no good drug that can be used clinically to eliminate cancer. During the clinical use of many anti-tumor drugs, it was gradually found that their selectivity was low, and while inhibiting tumor growth, they also had great lethality to normal cells, resulting in strong toxic and side effects. Weak ones manifest as vomiting, fatigue, anorexia, and dizziness, while severe ones can cause damage to the heart. Therefore, it is imminent to seek new a...

Claims

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Application Information

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IPC IPC(8): C07C50/34C12P7/66A61P35/00C12R1/80
CPCC07C50/34C07C2603/24C12P7/66
Inventor 王伟毅李增鹏陈建明冯世秀苏洋
Owner 大丰海洋生物医药研究所
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