Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures

被引：10
作者：
Cartuche, Luis [1 ,2 ]
Reyes-Batlle, Maria [3 ]
Sifaoui, Ines [3 ]
Arberas-Jimenez, Inigo [3 ]
Pinero, Jose E. [3 ]
Fernandez, Jose J. [1 ,4 ]
Lorenzo-Morales, Jacob [3 ]
Diaz-Marrero, Ana R. [1 ]
机构：
[1] Univ La Laguna, IUBO AG, Ctr Invest Biomed Canarias CIBICAN, Avda Astrofis F Sanchez 2, E-38206 Tenerife, Spain
[2] UTPL, Dept Quim & Ciencias Exactas, Secc Quim Basica & Aplicada, San Cayetano Alto S-N, Loja 1101608, Ecuador
[3] Univ La Laguna, Inst Univ Enfermedades Trop & Salud Publ Islas Ca, Dept Obstet & Ginecol Pediat Med Prevent & Salud, Avda Astrofis F Sanchez S-N, E-38206 Tenerife, Spain
[4] Univ La Laguna, Dept Quim Organ, Avda Astrofis F Sanchez 2, E-38206 Tenerife, Spain
来源：
MARINE DRUGS | 2019年 / 17卷 / 10期
关键词：
indolocarbazole; staurosporine; Streptomyces sanyensis; antiparasitic activities; Acanthamoeba; PROTEIN-KINASE-C; PROGRAMMED CELL-DEATH; TOPOISOMERASE-I; STAUROSPORINE; INHIBITOR; BIOSYNTHESIS; ACANTHAMOEBA; PRODUCTS; TAXONOMY;
D O I：
10.3390/md17100588
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Indolocarbazoles are a family of natural alkaloids characterized by their potent protein kinase and topoisomerase I inhibitory activity. Among them, staurosporine (1) has exhibited promising inhibitory activity against parasites. Based on new insights on the activity and mechanism of action of STS in Acanthamoeba parasites, this work reports the isolation, identification, and the anti-Acanthamoeba activity of the minor metabolites 7-oxostaurosporine (2), 4'-demethylamino-4'-oxostaurosporine (3), and streptocarbazole B (4), isolated from cultures of the mangrove strain Streptomyces sanyensis. A clear correlation between the antiparasitic activities and the structural elements and conformations of the indolocarbazoles 1-4 was observed. Also, the study reveals that 7-oxostaurosporine (2) affects membrane permeability and causes mitochondrial damages on trophozoites of A. castellanii Neff.
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页数：15
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