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Ascochlorin compound and application thereof in preparation of antitumor drugs or dihydroorotate dehydrogenase inhibitor drugs

A technology of ascochlorin and anti-tumor drugs, which is applied in the field of marine natural products, can solve the problems of weak mechanism of action and anti-tumor potential to be further explored, and achieve broad-spectrum significant tumor cell proliferation inhibitory activity and broad-spectrum significant Dihydroorotate dehydrogenase inhibitory activity, effect of novel structure

Active Publication Date: 2020-11-17
GUANGXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ascochlorins have been reported to have antioxidant and antibacterial activities, and also have inhibitory activity on some tumor cells, but the research on the mechanism of action is very weak, and the antitumor potential needs to be further explored

Method used

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  • Ascochlorin compound and application thereof in preparation of antitumor drugs or dihydroorotate dehydrogenase inhibitor drugs
  • Ascochlorin compound and application thereof in preparation of antitumor drugs or dihydroorotate dehydrogenase inhibitor drugs
  • Ascochlorin compound and application thereof in preparation of antitumor drugs or dihydroorotate dehydrogenase inhibitor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Sclerotinia acremonium (Acremonium sclerotigenum) GXIMD02501

[0033] Acremonium sclerotigenum GXIMD 02501 was isolated from the symbiotic bacteria collected from the Beibu Bay of Guangxi, China, and preserved in the Guangdong Microbial Culture Collection Center (GDMCC). Address: 5th Floor, Building 59, Guangdong Institute of Microbiology, No. 100 Xianlie Middle Road, Guangzhou City, Guangdong Province, Guangdong Institute of Microbiology, deposit number: GDMCC No.60670.

Embodiment 2

[0034] Preparation and separation of embodiment 2 ascochlorin compound acremochlorin A

[0035] 1. Medium

[0036] 1.1. Seed culture medium: Each liter of medium contains 15g of malt extract powder, 20g of coarse sea salt, and the balance is water, pH7.5. Mix evenly according to the above-mentioned components and contents, and then sterilize at 121°C for 30 minutes for later use.

[0037] 1.2. Fermentation medium: Each 1L Erlenmeyer flask medium contains: 120g rice, 1.5g bacteriological peptone, 3g coarse sea salt, 150mL water, pH7.5. Mix evenly according to the above-mentioned components and contents, and then sterilize at 121°C for 30 minutes for later use.

[0038]2. Fermentation

[0039] 2.1. Seed culture: Inoculate activated Acremonium sclerotigenum GXIMD02501 into 1L triangular culture flasks each containing 300mL of seed culture medium, culture at 25°C and 180rpm for 72 hours to obtain seed solution.

[0040] 2.2. Fermentation culture: the seed liquid was inserted i...

Embodiment 3

[0044] Example 3 Structural identification of ascochlorin compound acremochlorin A

[0045] The ascochlorin compound acremochlorin A is a colorless needle-like crystal, and its NMR data assignment is shown in Table 1; its high-resolution mass spectrum HRESIMS gives a quasi-molecular ion peak m / z407.1968[M+H] + (calcd forC 23 h 32 ClO 4 , 407.1989) determined that its molecular formula is C 23 h 31 ClO 4 , containing 8 degrees of unsaturation. 1 The HNMR spectrum shows a phenolic hydroxyl group 2-OH (δ H 12.89,s), 1 aldehyde group (δ H 10.17,s), 3 alkene protons H-10(δ H 5.20,t,J=7.0Hz) and terminal methylene H 2 -21(δ H 4.79, s, H-21a; 4.53, s, H-21b), a oxymethine H-18 (δ H 3.27, overlapped) and 1 methine H-14 (δ H 1.63,m), 5 methylene H 2 -9(δ H 3.36–3.40, d, J=7.0Hz), H 2 -12(δ H 2.04,m; 1.79,m), H 2 -13(δ H 1.61, m), H 2 -16(δ H 2.25,m; 1.82,m) and H 2 -17(δ H 1.73,m; 1.44,m), and four unimodal methyl groups, H 3 -7(δ H 2.63), H 3 -20(δ H 0.96), H...

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Abstract

The invention provides an ascochlorin compound and application thereof in preparation of antitumor drugs or dihydroorotate dehydrogenase inhibitor drugs, and relates to the field of marine natural products. The structural formula of the disclosed ascochlorin compound is shown as a formula (I), a cyclohexanol fragment of the ascochlorin compound has rare gem-dimethyl and exocyclic double bonds, andthe compound has broad-spectrum remarkable tumor cell proliferation inhibition activity and dihydroorotate dehydrogenase inhibition activity, and therefore, the compound is an ideal candidate compound developed into an antitumor drug or a dihydroorotate dehydrogenase inhibitor drug which is novel in structure and high in activity.

Description

technical field [0001] The invention relates to the field of marine natural products, in particular to an ascochlorin compound and its application in the preparation of antitumor drugs or dihydroorotate dehydrogenase inhibitor drugs. Background technique [0002] Malignant tumors are still non-communicable diseases with extremely high morbidity and mortality worldwide, posing a serious threat to human life and health. Natural products are an important source of drug development. According to reports, from 1981 to 2019, anticancer drugs derived from natural products accounted for more than 75% of the anticancer drugs on the market. Marine microbial resources are abundant, and they are new ideal resources for discovering novel active metabolites. [0003] Dihydroorotate dehydrogenase (dihydroorotate dehydrogenase, DHODH) is an iron-containing flavin-dependent enzyme present in the inner mitochondrial membrane, which catalyzes the key reaction in step 4 of the de novo pyrimid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C47/57A61P35/00A61P35/02C12N1/14C12P7/26C12R1/645
CPCA61P35/00A61P35/02C07C47/57C12P7/26C07C2601/14C12N1/145C12R2001/645
Inventor 罗小卫刘永宏王军舰高程海蔡国弟
Owner GUANGXI UNIV OF CHINESE MEDICINE
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