Penem enol e1 derived from Trichoderma aurantii and its application in the preparation of anti-oral epidermal cancer drugs

A technology of Trichoderma citrinum and penemol, which is applied in the field of medicinal chemistry, can solve problems such as drugs that have not yet been seen, and achieve the effect of significant anti-oral epidermal cancer activity.

Inactive Publication Date: 2019-05-10
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The study found that the alkaloid compound shown has anti-tumor activity against oral epidermal cancer. There is no report on the chemical structure of the compound and its anti-proliferation inhibitory activity on oral epidermal cancer cells. Therefore, there are no related drugs on the market.

Method used

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  • Penem enol e1 derived from Trichoderma aurantii and its application in the preparation of anti-oral epidermal cancer drugs
  • Penem enol e1 derived from Trichoderma aurantii and its application in the preparation of anti-oral epidermal cancer drugs
  • Penem enol e1 derived from Trichoderma aurantii and its application in the preparation of anti-oral epidermal cancer drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Fermentative production and separation and purification of the compound of embodiment 1

[0016] 1 Fermentation production

[0017] Fermentation culture of production bacteria: according to the conventional method of cultivating microorganisms, take Trichoderma auranthoderma ( Trichoderma citrinoviride. ) IBPT-4 (preserved in China Center for Type Culture Collection on January 25, 2013, address: Wuhan University, Wuhan, deposit number is: CCTCC NO: M 2013055) appropriate amount, inoculated on PDA solid slant medium at 28 Cultivate in an incubator for 4 days.

[0018] Get the Trichoderma auranthoderma ( Trichoderma citrinoviride. ) appropriate amount of IBPT-4, inoculated into 400mL culture medium [Culture medium composition (g / L): mannitol 20.0, yeast extract 3.0, maltose 20.0, monosodium glutamate 10.0, glucose 10.0, KH 2 PO 4 0.5 , MgSO 4 0.3, NaCl 6.0, fixed volume into 1000mL Erlenmeyer flask], after static culture at 28°C for 30 days, mycelia and fermenta...

Embodiment 2

[0027] Example 2 Test of Anti-tumor Activity in Vitro

[0028] 1 Experimental samples and experimental methods

[0029] Preparation of the tested sample solution The test sample is the pure product of the compound separated and refined in the above-mentioned implementation 1. Accurately weigh an appropriate amount of sample, and prepare a solution with the required concentration with methanol for activity measurement.

[0030] Cell lines and cell subculture The oral epidermal carcinoma cell line was used, and the cells were subcultured in RPMI-1640 medium containing 10% FBS at 37°C in an incubator filled with 5% carbon dioxide.

[0031] Cell Proliferation Inhibitory Activity Test Method

[0032] Tetrazolium salt (MTT) method Take cells in the logarithmic growth phase and adjust the cell density to 2×10 per ml 5 Cells were inoculated into 96-well cell culture plates at 200 microliters per well, and filled with 5% CO at 37°C 2 for 4 hours in an incubator. Add 2 microliters ...

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Abstract

The invention relates to penem enol E1 derived from trichoderma citrinoviride and application in preparation of an anti-oral epidermoid carcinoma drug. The compound is structurally characterized by containing a molecular skeleton of pentacyclic amide, a carbonyl connected with a long n-decyl saturated aliphatic chain, a methyl connected to N and molecules existing in two hydroxyl groups. An experiment proves that the alkaloid compound has good oral epidermoid carcinoma inhibiting activity. The penem enol E1 can serve as a drug for inhibiting oral epidermoid carcinoma cell proliferation or the anti-oral epidermoid carcinoma drug for antitumor research.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to penemenol E1 derived from Trichoderma auranthoderma and its application in the preparation of anti-oral epidermal cancer drugs. Background technique [0002] Alkaloids are a type of nitrogen-containing organic compounds produced by biological secondary metabolism. There are many types of alkaloids in nature, most of which come from plants, so they are also called plant alkaloids. Alkaloids have important physiological effects on humans and animals, including anti-asthma and antitussive, hypoglycemic, hypolipidemic, antibacterial, antitumor, analgesic, etc., among which antibacterial and antitumor activities are the most prominent. Natural structural alkaloids are an important source for discovering lead compounds in the research of innovative drugs, and there are nearly a hundred kinds of alkaloid drugs currently used in clinical practice. Studies have found that s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/38A61K31/4015A61P35/00C12P17/10C12R1/885
CPCA61K31/4015C07D207/38C12P17/10
Inventor 陈立李欣欣刘沁颖李亚平毕延雪赵杨杨张其清
Owner FUZHOU UNIV
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