Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Antiprotozoal activity and cytotoxicity of novel 1,7-dioxadispiro[5.1.5.2]pentadeca-9,12-dien-11-one derivatives from Amomum aculeatum
Autore:
Heilmann, J; Mayr, S; Brun, R; Rali, T; Sticher, O;
Indirizzi:
ETH Zurich, Inst Pharmaceut Sci, Dept Appl BioSci, CH-8057 Zurich, Switzerland ETH Zurich Zurich Switzerland CH-8057 ioSci, CH-8057 Zurich, Switzerland Swiss Trop Inst, CH-4002 Basel, Switzerland Swiss Trop Inst Basel Switzerland CH-4002 st, CH-4002 Basel, Switzerland PNG Biodivers Res PTY Ltd, Port Moresby, Papua N Guinea PNG Biodivers Res PTY Ltd Port Moresby Papua N Guinea y, Papua N Guinea
Titolo Testata:
HELVETICA CHIMICA ACTA
fascicolo: 11, volume: 83, anno: 2000,
pagine: 2939 - 2945
SICI:
0018-019X(2000)83:11<2939:AAACON>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRYPANOSOMA-BRUCEI; 1,6-DIOXASPIRO<4.5>DEC-3-ENES; RHODESIENSE; GAMBIENSE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
12
Recensione:
Indirizzi per estratti:
Indirizzo: Heilmann, J ETH Zurich, Inst Pharmaceut Sci, Dept Appl BioSci, Winterthurerstr 190, CH-8057 Zurich, Switzerland ETH Zurich Winterthurerstr 190 Zurich Switzerland CH-8057 and
Citazione:
J. Heilmann et al., "Antiprotozoal activity and cytotoxicity of novel 1,7-dioxadispiro[5.1.5.2]pentadeca-9,12-dien-11-one derivatives from Amomum aculeatum", HELV CHIM A, 83(11), 2000, pp. 2939-2945

Abstract

Cytotoxicity against the KB cancer cell line as a lead bioactivity-guided fractionation of the petroleum ether extract of rhizomes of Amomum aculeatum RoxB. led to the isolation of three novel dioxadispiro[5.1.5.2]pentadeca-9,12-dien-11-one derivatives. The structures of aculeatin A (1), aculeatin B (2),and aculeatin C (3) were established as rel-(2R,4R,6S)- and rel-(2R,4R,6R)-4-hydroxy-2-tridecyl-1,7-dioxadispiro[5.1.5.2]pentadeca-9,12-dien-11-one (1 and 2, resp.) and rel-(2R,4R,6S)-2-[4-(3-dodecyl-2-heptyl-3-hydroxy-6-oxocylohexa-1,4-dienyl)-2-oxobutyl]-4-hydroxy-1,7-dioxadispiro[5.1.5.2]pentadeca-9,12-dien-11-one (3) by extensive spectroscopic analyses, particularly C-13 NMR, inverse-gated C-13, HMQC, HMBC, NOESY, and INADEQUATE NMR experiments as well as mass spectrometry. The aculeatins represent a novel type of natural products. All compounds showed high cytotoxicity against the KB cell line: 1, IC50 = 1.7 muM; 2, IC50 = 2.0 muM; 3, IC50 = 1.6 muM. Additional testing against two Plasmodium falciparum strains as well as against trypomastigote forms of Trypanosoma brucei rhodesiense and Trypanosoma cruzi showed strong activities, particularly against P. falciparum strain K1 (1, IC50 = 0.18 muM; 2, IC50 = 0.43 muM; 3, IC50 = 0 37 muM).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/21 alle ore 03:35:42