title: Aaptamines, marine spongean alkaloids, as anti-dormant mycobacterial substances.
abstract: A new aaptamine class alkaloid, designated 2-methoxy-3-oxoaaptamine (1), together with seven known aaptamines (2-8) were isolated from a marine sponge of Aaptos sp. as anti-mycobacterial substances against active and dormant bacilli. The chemical structure of 1 was determined on the basis of spectroscopic analysis. Compound 1 was anti-mycobacterial against Mycobacterium smegmatis in both active growing and dormancy-inducing hypoxic conditions with a minimum inhibitory concentration (MIC) of 6.25 μg/ml, and compounds 2, 5, 6, and 7 showed anti-mycobacterial activities under hypoxic condition selectively, with MIC values of 1.5-6.25 μg/ml.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Osaka University, Yamada-oka 1-6, Suita, Osaka, 565-0871, Japan, araim@phs.osaka-u.ac.jp.
authors.forename: Masayoshi
authors.initials: M
authors.lastname: Arai
authors.forename: Chisu
authors.initials: C
authors.lastname: Han
authors.forename: Yoshi
authors.initials: Y
authors.lastname: Yamano
authors.forename: Andi
authors.initials: A
authors.lastname: Setiawan
authors.forename: Motomasa
authors.initials: M
authors.lastname: Kobayashi
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D020102:Mycobacterium smegmatis / Q000187:drug effects; D009287:Naphthyridines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D011161:Porifera / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D000900:Anti-Bacterial Agents; D009287:Naphthyridines; C043986:aaptamine