Pair of quinazolinone alkaloid enantiomers, and preparation method and application thereof

A quinazolinone and the technology of the quinazolinone, which are applied in the field of quinazolinone alkaloid enantiomers and their preparation, can solve problems such as toxic and side effects, and achieve the effect of good anti-inflammatory drug potential
CN110590769AActive Publication Date: 2019-12-20SUN YAT SEN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SUN YAT SEN UNIV
Publication Date
2019-12-20

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Abstract

The invention discloses a pair of quinazolinone alkaloid enantiomers, and a preparation method and application thereof. Penicillium canescens SYSU-MS4829 is preserved in the Guangdong Microbial Culture Collection Center on July 11, 2018 with the preservation number of GDMCC 60402, and the Penicillium canescens SYSU-MS4829 can ferment to produce compounds with the structures shown in a formula (I)and a formula (II) (please see the specification for the formula (I) and the formula (II)). The Penicillium canescens SYSU-MS4829 is isolated from sea squirts in Daao Bay, Shenzhen, and can metabolizeto produce the compound quinazolinone alkaloid enantiomers (+ / -)-penicamide A with the anti-inflammatory activity, optical voidness compounds (+)-penicamide A and (-)-penicamide A obtained after division of the Penicillium canescens SYSU-MS4829 have the same good anti-inflammatory effect and both can effectively inhibit production of NO by an LPS-induced inflammatory cell RAW264.7, and IC50 is 35.1 [mu]M, 47.5 [mu]M and 27.2 [mu]M respectively; meanwhile, all compounds have no cellular poison to the cell RAW264.7; therefore, a racemic compound (+ / -)-penicamide A and the optical voidness compounds (+)-penicamide A and (-)-penicamide A have good potential as anti-inflammatory drugs and can be used for preparing anti-inflammatory drugs.
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Description

technical field

[0001] The invention relates to the technical field of microbial fermentation and pharmaceutical compounds, and more specifically, to a pair of quinazolinone alkaloid enantiomers and a preparation method and application thereof. Background technique

[0002] Inflammation is the physiological and pathological response of the body to stimuli, manifested as redness, swelling, heat, pain and dysfunction. In general, inflammation, as a beneficial defense response, plays an important role in the body's resistance to external stimuli, but excessive and sustained inflammatory responses can cause tissue damage and functional impairment. The occurrence and development of many common diseases (such as tumors, asthma, hypertension, Alzheimer's disease, atherosclerosis, etc.) are closely related to inflammatory responses. Bacterial infectious inflammation induced by endotoxin component lipopolysaccharide (LPS) in the cell wall of Gram-negative bacteria is the most common...

Claims

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