链霉菌内酯A-D，从真菌CF-247251中分离出的一类抗疟大环内酯类化合物。

Strasseriolides A-D, A Family of Antiplasmodial Macrolides Isolated from the Fungus CF-247251.

作者信息

Annang Frederick, Pérez-Moreno Guiomar, González-Menéndez Víctor, Lacret Rodney, Pérez-Victoria Ignacio, Martín Jesús, Cantizani Juan, de Pedro Nuria, Choquesillo-Lazarte Duane, Ruiz-Pérez Luis M, González-Pacanowska Dolores, Genilloud Olga, Vicente Francisca, Reyes Fernando

机构信息

Fundación MEDINA, Avda. del Conocimiento 34, 18016 Armilla, Granada, Spain.

Instituto de Parasitologı́a y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientı́ficas (CSIC), Avda. del Conocimiento 17, 18016 Armilla, Granada, Spain.

出版信息

Org Lett. 2020 Sep 4;22(17):6709-6713. doi: 10.1021/acs.orglett.0c01665. Epub 2020 Aug 18.

DOI:10.1021/acs.orglett.0c01665

PMID:32808790

Abstract

A novel family of four potent antimalarial macrolides, strasseriolides A-D (-), has been isolated from cultures of CF-247251, a fungal strain obtained from plant tissues. The structures of these compounds, including their absolute configurations, were elucidated by HRMS, NMR spectroscopy, and X-ray single-crystal diffraction. The four compounds gave respective IC values of 9.810, 0.013, 0.123, and 0.128 μM against 3D7 parasites with no significant cytotoxicity against the HepG2 cell line.

摘要

从植物组织中获得的真菌菌株CF-247251的培养物中分离出了一个新的由四种强效抗疟大环内酯类化合物组成的家族，即链霉菌素A-D（-）。通过高分辨质谱（HRMS）、核磁共振光谱（NMR）和X射线单晶衍射阐明了这些化合物的结构，包括它们的绝对构型。这四种化合物对3D7疟原虫的半数抑制浓度（IC）分别为9.810、0.013、0.123和0.128 μM，对HepG2细胞系无明显细胞毒性。