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来自分生孢子梗梨形孢的具有抗炎、细胞毒性或α-葡萄糖苷酶抑制活性的环五肽。

Cyclic pentapeptides with anti-inflammatory, cytotoxic or α-glucosidase inhibitory activities from Basidiobolus meristosporus.

作者信息

Zhao Cheng, Qu Jiaojiao, Lu Ruili, Chen Renjie, Dong Quheng, Huang Bo, Bao Guanhu, Hu Fenglin

机构信息

Engineering Research Center of Fungal Biotechnology, Ministry of Education; Research Center on Entomogenous Fungi, Anhui Agricultural University, Hefei, 230036, China.

Natural Products Laboratory, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, Hefei, Anhui Province, 230036, China.

出版信息

Phytochemistry. 2023 May;209:113636. doi: 10.1016/j.phytochem.2023.113636. Epub 2023 Mar 5.

DOI:10.1016/j.phytochem.2023.113636
PMID:36871901
Abstract

Basidiobolus meristosporus is an opportunistic pathogen of mammals with unique habitats, but its metabolites have not been extensively studied. Through semi-preparative HPLC, nine undescribed cyclic pentapeptides were isolated from mycelia of B. meristosporus RCEF4516. The structure of the compounds 1-9 were identified with MS/MS and NMR data and designated as basidiosin D-L respectively. The absolute configurations were determined according to the advanced Marfey's method after compound hydrolysis. Bioactivity testing showed that compounds 1, 2, 3, 4 and 8 decreased NO production in LPS-activated RAW264.7 cells in a concentration-dependent manner. The nine compounds showed cytotoxicity against RAW264.7, 293 T and HepG2 cells. All the compounds except compound 7 showed stronger inhibitory effects on α-glucosidase than acarbose.

摘要

分生孢子梗状耳霉是一种具有独特生境的哺乳动物机会性病原菌,但其代谢产物尚未得到广泛研究。通过半制备高效液相色谱法,从分生孢子梗状耳霉RCEF4516的菌丝体中分离出9种未描述的环五肽。利用串联质谱和核磁共振数据鉴定了化合物1-9的结构,分别命名为basidiosin D-L。化合物水解后,根据改进的马尔菲方法确定了其绝对构型。生物活性测试表明,化合物1、2、3、4和8以浓度依赖的方式降低了脂多糖激活的RAW264.7细胞中一氧化氮的产生。这9种化合物对RAW264.7、293 T和HepG2细胞具有细胞毒性。除化合物7外,所有化合物对α-葡萄糖苷酶的抑制作用均强于阿卡波糖。

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