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1.
Org Med Chem Lett ; 4(1): 8, 2014 Dec.
Article in English | MEDLINE | ID: mdl-26548986

ABSTRACT

BACKGROUND: The current investigation sought to explore the nature of the secondary metabolites in the algae, Laurencia pacifica. RESULTS: This report details the first isolation of the sesquiterpenes isoaplysin (1), isolaurenisol (2), debromoisolaurinterol (3), debromoaplysinol (4), laur-11-en-10-ol (5), 10α-hydroxyldebromoepiaplysin (6), and the previously unknown 10-bromo-3,7,11,11-tetramethylspiro[5.5]undeca-1,7-dien-3-ol (7) from the algae, Laurencia pacifica. Isoaplysin (1) and debromoaplysinol (4) showed promising levels of growth inhibition against a panel cancer-derived cell lines of colon (HT29), glioblastoma (U87, SJ-G2), breast (MCF-7), ovarian (A2780), lung (H460), skin (A431), prostate (Du145), neuroblastoma (BE2-C), pancreas (MIA), murine glioblastoma (SMA) origin with average GI50 values of 23 and 14 µM. CONCLUSIONS: Isoaplysin (1) and debromoaplysinol (4) were up to fourfold more potent in cancer-derived cell populations than in non-tumor-derived normal cells (MCF10A). These analogues are promising candidates for anticancer drug development. Graphical Abstract ᅟ.

2.
J Nat Prod ; 72(1): 102-6, 2009 Jan.
Article in English | MEDLINE | ID: mdl-19132863

ABSTRACT

Investigation of an extract of the Australian marine sponge Psammoclema sp. for dynamin I inhibitory activity led to the isolation of four new trihydroxysterols (1-4) related to aragusterol G. These compounds were largely identified by 1D and 2D NMR spectroscopic methods. While 1 was found to be inactive in the dynamin bioassay, bioassays did reveal that compounds 1-4 inhibited the growth of colorectal, breast, ovarian, and prostate cancer cell lines (GI(50) 5-27 microM). The additional insight that these new compounds give to previous SAR studies is discussed briefly.


Subject(s)
Antineoplastic Agents/isolation & purification , Porifera/chemistry , Steroids/isolation & purification , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Australia , Drug Screening Assays, Antitumor , Humans , Male , Marine Biology , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Steroids/chemistry , Steroids/pharmacology , Structure-Activity Relationship
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