Discovery of metabolite from the insect-derived endophytic Penicillium chrysogenum and their COX-2 inhibitory activity

IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Fitoterapia Pub Date : 2024-09-24 DOI:10.1016/j.fitote.2024.106238
Chun-Yan Zhu , Qin Luo , Zi-Wei Zhang , Yan-Peng Li , Di Han , Yong-Ming Yan
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Abstract

Three new N-alkylated amino acid derivatives, penichrysoamides A-C (13), along with a new citric acid derivative, penichrysoacid A (4), a new chromanone lactone penichrysoacid B (5), and a new amide derivative, penichrysoamide D (6), as well as seven known benzamide derivatives (713), were isolated from the endophytic fungus Penicillium chrysogenum derived from the insect Periplaneta americana. The structures of these compounds, including their absolute configurations, were elucidated using spectroscopic and computational techniques. Biological evaluation revealed that compounds 813 exhibited significant COX-2 inhibitory activity, with IC50 values ranging from 275 nM to 1350 nM.

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从昆虫内生青霉中发现代谢物及其 COX-2 抑制活性
从源自昆虫 Periplaneta americana 的内生真菌 Penicillium chrysogenum 中分离出了三种新的 N-烷基化氨基酸衍生物 Penichrysoamides A-C (1-3)、一种新的柠檬酸衍生物 Penichrysoacid A (4)、一种新的色酮内酯 Penichrysoacid B (5)、一种新的酰胺衍生物 Penichrysoamide D (6),以及七种已知的苯甲酰胺衍生物 (7-13)。利用光谱和计算技术阐明了这些化合物的结构,包括它们的绝对构型。生物学评价显示,化合物 8-13 具有显著的 COX-2 抑制活性,IC50 值从 275 nM 到 1350 nM 不等。
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来源期刊
Fitoterapia
Fitoterapia 医学-药学
CiteScore
5.80
自引率
2.90%
发文量
198
审稿时长
1.5 months
期刊介绍: Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.
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