A kind of monoterpene indole compound and its preparation method and application

A technology of indole compounds and compounds, applied in the field of monoterpene indole compounds and their preparation, can solve problems such as poor recovery and toxic side effects

Active Publication Date: 2021-09-28
YUNNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, chemotherapy and surgery have obvious toxic and side effects on the human body, and the recovery situation is not optimistic. Therefore, the development of anti-tumor drugs with high efficiency and low toxicity has very important practical significance for human health.

Method used

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  • A kind of monoterpene indole compound and its preparation method and application
  • A kind of monoterpene indole compound and its preparation method and application
  • A kind of monoterpene indole compound and its preparation method and application

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preparation example Construction

[0040] The present invention also provides a preparation method of the monoterpene indole compound described in the above technical scheme, comprising the following steps:

[0041] Fermenting Penicillium polandii to obtain a fermented product of Penicillium polandii;

[0042] mixing the Penicillium polandii fermented product with alcohol, and performing ultrasonic extraction to obtain an alcohol extract;

[0043] Purifying the alcohol extract to obtain the monoterpene indole compound;

[0044] Described purification comprises the following steps:

[0045] Dissolving the ethanol extract in chloroform-methanol to obtain a solution to be purified;

[0046] The solution to be purified is subjected to the first silica gel column chromatography, the elution procedure of the first silica gel column chromatography is the first gradient elution, and the eluent for the first gradient elution is a chloroform-methanol mixture, Collect the eluate obtained by eluting with the eluent whos...

Embodiment 1

[0076] Inoculate 15 mg of Penicillium poleensis on a 30 mL PDA slant medium, and culture it at a constant temperature at 28°C for 6 days to obtain activated Penicillium polishe, and store it in an environment of 5°C for later use;

[0077] 4.8kg of potatoes peeled and cut into 1cm volume 3 The potato cubes were packed in 60 tissue culture bottles with a volume of 350mL (60g / bottle), and then the tissue culture bottles were capped and sterilized at 121°C for 30 minutes, cooled to obtain the fermentation medium;

[0078] inoculating the activated Penicillium polandii into the fermentation medium according to the inoculation amount of 1%, and culturing at a constant temperature at 28° C. for 30 days after being covered to obtain a Penicillium polandane fermentation product;

[0079] Mix 60.4 g of the Penicillium polandina fermented product with 120 mL of methanol, perform ultrasonication (300 W, 30 min), filter, take the filtrate and carry out vacuum distillation (vacuum degree o...

Embodiment 2

[0091] According to the method for embodiment 1, Penicillium polandii is activated;

[0092] Soak 60g of rice in 50mL of water for 12h, place the soaked rice in a tissue culture bottle with a volume of 350mL, cover the tissue culture bottle, sterilize at 121°C for 30min, and cool to obtain a fermentation medium;

[0093] Inoculating the activated Penicillium polandii into the fermentation medium according to the inoculum amount of 1%, and culturing at a constant temperature at 26° C. for 25 days after being covered, to obtain a Penicillium polish fermentation product;

[0094] Mix 60 g of the fermented product of Penicillium polandii with 120 mL of methanol, perform ultrasonication (300 W, 30 min), filter, and take the filtrate for vacuum distillation (vacuum degree of 12 kPa, 50 ° C) until there is no alcohol smell, and 12 g of ethanol extract is obtained;

[0095] The 12g ethanol extract was dissolved in 40mL of chloroform-methanol solution (volume ratio of 1:1) to obtain a ...

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Abstract

The invention belongs to the technical field of medicine, and in particular relates to a monoterpene indole compound and a preparation method and application thereof. The monoterpene indole compound (polonidine A) provided by the present invention has good inhibitory activity on liver cancer cell MHCC97H, breast cancer cell BT549, lung cancer cell H1299, colon cancer cell SW620, glioma T98G and lung cancer cell A549, its IC 50 The values ​​were 7.08 μg / mL, 6.05 μg / mL, 20.39 μg / mL, 7.64 μg / mL, 17.97 μg / mL and 15.96 μg / mL, respectively. The polonidine A provided by the invention provides a new approach for the development of antitumor drugs. The invention prepares monoterpene indole compounds through microbial fermentation, has short preparation period, mild culture conditions, few by-products, low cost, and is easy to realize industrialization.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a monoterpene indole compound and a preparation method and application thereof. Background technique [0002] With the development of industry, air pollution is becoming more and more serious, and the quality of human living environment is continuously declining, even affecting human health. According to relevant statistics, the incidence of tumor diseases is increasing year by year, and has become one of the major diseases that threaten human health. However, chemotherapy and surgery have obvious toxic and side effects on the human body, and the recovery situation is not optimistic. Therefore, the development of anti-tumor drugs with high efficiency and low toxicity is of great practical significance to human health. Contents of the invention [0003] In view of this, the present invention provides a monoterpene indole compound, which has significant antitumor ac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/08A61P35/00C12P17/16C12R1/80
CPCA61P35/00C07D209/08C12P17/165
Inventor 蔡乐丁中涛蔡学芸王家鹏
Owner YUNNAN UNIV
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