Indole alkaloid with anti-tumor activity as well as preparation method and application thereof

An indole alkaloid, anti-tumor activity technology, applied in the field of microbial engineering technology and pharmacology, can solve the problems of drug resistance, restricting the treatment effect and quality of life of leukemia patients, low treatment efficiency, etc. The effect of short cycle and low cost

Inactive Publication Date: 2018-11-16
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the face of leukemia, the current chemotherapy drugs still have problems such as low treatment efficiency and drug resistance, which seriously restrict the treatment effect and quality of life of leukemia patients.

Method used

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  • Indole alkaloid with anti-tumor activity as well as preparation method and application thereof
  • Indole alkaloid with anti-tumor activity as well as preparation method and application thereof
  • Indole alkaloid with anti-tumor activity as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: Liquid fermentation and feeding of mantis intestinal bacteria IFB-T01 (Daldinia eschscholzii)

[0030] The bacterial block of Daldinia eschscholzii IFB-TL01 derived from the intestinal bacteria of the activated mantis mantis was inoculated in 1L Erlenmeyer flasks, each containing 400mL of malt culture medium, inoculated 10 flasks on a shaker, and cultured at 200rpm, 28‐30℃ for 2 ‐3 days, as the seed liquid, and then inoculate the seed liquid into a new malt medium (400 mL / bottle x 200 bottles) with an inoculum amount of 20 mL each, and continue to cultivate for 2 days at 200 rpm and 28‐30 °C. Indole-3-carbinol was fed at 24, 48, and 72 hours respectively until the final concentration in the solution was 1.0 mM, and the fermentation was continued for 10 days at 200 rpm and 28-30°C.

Embodiment 2

[0031] Embodiment 2: Extraction and separation of indole alkaloids

[0032] In Example 1, the fermented liquid was filtered through gauze, the filtrate was extracted with ethyl acetate, and concentrated by centrifugation to obtain black extract A (146g); the extract A was subjected to silica gel column chromatography segmentation, and petroleum ether: acetone (volume ratio: 100: 0, 100:5, 10:1, 5:1, 3:1, 2:1, 1:1) for gradient elution to obtain 7 eluted fractions A1-A7;

[0033] Take segment A3 (petroleum ether: acetone = 10:1 elution site) and continue to use petroleum ether: acetone (volume ratio 100:2 → 1:1) gradient elution to obtain F1-F77 fractions. Take F3 (petroleum ether: acetone volume ratio 20:1 elution fraction) through Sephadex LH-20 column chromatography (methanol elution), high pressure preparative liquid phase [chromatographic column: ODS-2Hy0persil columns (5μm, 250×10mm)] MeOH / H 2 O (70:30) was eluted and purified to obtain compound 1 (2 mg).

[0034] And ...

Embodiment 3

[0043] Embodiment 3: MTT method (3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide salt method) measures the antitumor activity of compounds 1 and 2

[0044] 1. Medium configuration: the medium contains 10% newborn calf serum, penicillin 100U / ml and streptomycin 100U / ml.

[0045]

[0046] 2. Cell culture: Inoculate human breast cancer cells SW480, HL-60, HepG-2, A375, MCF-7, CaoV-3, A549 and MDA-MB-231 cells into culture flasks containing corresponding medium, Place at 37°C, 5% CO 2 Culture in an incubator under the condition of relative saturated humidity, pass passage every 3-5 days.

[0047] 3. Test drug treatment: Dissolve compounds 1 and 2 in an appropriate amount of DMSO (final concentration not exceeding 0.5%), then dilute it into a 10-fold working solution with complete medium, and store it at 4°C for later use.

[0048] 4. MTT colorimetric method to detect the effect of drugs on tumor cell proliferation: select tumor cells SW480, HL-60, HepG-2, A375, MCF...

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Abstract

The invention discloses indole alkaloid. The indole alkaloid is extracted from fermentation liquid of gastrointestinal fungi IFB-TL01 (Daldinia eschscholzii) of tenodera aridifolia sinensis fed on indol-3-methanol. The indole alkaloid Dalesindole B (compound 1) is a new compound, and the indole alkaloid Dalesindole C (compound 2) is a new skeleton compound. A pharmacological experimental result shows that the indole alkaloid has inhibition activity on the multiplication of various tumor cells, particularly can selectively inhibit HL-60 leukemia tumor cells, and can be used as an anti-tumor drug.

Description

technical field [0001] The invention belongs to the field of microbial engineering technology and pharmacology, and in particular relates to the fermentation liquid obtained from the intestinal fungus Daldinia genus Daldinia (Daldinia) light wheel charcoal shell IFB-TL01 (Daldinia eschscholzii) fed with indole-3-carbinol A class of extracted indole alkaloids and its preparation method and application. Background technique [0002] The discovery and application of new compounds plays a very important role in the development of new drugs. Among them, indole alkaloids are a class of organic molecules containing indole or indoline structures. Because indole compounds have a wide range of pharmacological activities, such as anti-platelet aggregation, anti-inflammation, antibacterial, anti-tumor, insecticidal and immunosuppressive, etc., they have attracted widespread attention. Especially the substitution of C-2 and C-3 positions in the indole ring is an effective method for pr...

Claims

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Application Information

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IPC IPC(8): C07D491/044C07D209/36A61K31/407A61K31/404A61P35/02C12P17/18C12P17/16C12R1/645
CPCA61P35/02C07D209/36C07D491/044C12P17/165C12P17/18
Inventor 谭仁祥林丽萍
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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