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Anibamine and Its Analogues: Potent Antiplasmodial Agents from Aniba citrifolia.
Du, Yongle; Valenciano, Ana Lisa; Dai, Yumin; Zheng, Yi; Zhang, Feng; Zhang, Yan; Clement, Jason; Goetz, Michael; Kingston, David G I; Cassera, Maria B.
Afiliação
  • Du Y; Department of Chemistry and Virginia Tech Center for Drug Discovery, M/C 0212, Virginia Tech, Blacksburg, Virginia 24061, United States.
  • Valenciano AL; Department of Biochemistry and Molecular Biology, and Center for Tropical and Emerging Global Diseases (CTEGD), University of Georgia, Athens, Georgia 30602, United States.
  • Dai Y; Department of Chemistry and Virginia Tech Center for Drug Discovery, M/C 0212, Virginia Tech, Blacksburg, Virginia 24061, United States.
  • Zheng Y; Department of Medicinal Chemistry, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia 23298, United States.
  • Zhang F; Department of Medicinal Chemistry, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia 23298, United States.
  • Zhang Y; Department of Medicinal Chemistry, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia 23298, United States.
  • Clement J; Natural Products Discovery Institute, Baruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, Pennsylvania 18902, United States.
  • Goetz M; Natural Products Discovery Institute, Baruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, Pennsylvania 18902, United States.
  • Kingston DGI; Department of Chemistry and Virginia Tech Center for Drug Discovery, M/C 0212, Virginia Tech, Blacksburg, Virginia 24061, United States.
  • Cassera MB; Department of Biochemistry and Molecular Biology, and Center for Tropical and Emerging Global Diseases (CTEGD), University of Georgia, Athens, Georgia 30602, United States.
J Nat Prod ; 83(3): 569-577, 2020 03 27.
Article em En | MEDLINE | ID: mdl-31577436
In our continuing search for novel natural products with antiplasmodial activity, an extract of Aniba citrifolia was found to have good activity, with an IC50 value less than 1.25 µg/mL. After bioassay-directed fractionation, the known indolizinium alkaloid anibamine (1) and the new indolizinium alkaloid anibamine B (2) were isolated as the major bioactive constituents, with antiplasmodial IC50 values of 0.170 and 0.244 µM against the drug-resistant Dd2 strain of Plasmodium falciparum. The new coumarin anibomarin A (3), the new norneolignan anibignan A (5), and six known neolignans (7-12) were also obtained. The structures of all the isolated compounds were determined based on analyses of 1D and 2D NMR spectroscopic and mass spectrometric data, and the absolute configuration of anibignan A (5) was assigned from its ECD spectrum. Evaluation of a library of 28 anibamine analogues (13-40) indicated that quaternary charged analogues had IC50 values as low as 58 nM, while uncharged analogues were inactive or significantly less active. Assessment of the potential effects of anibamine and its analogues on the intraerythrocytic stages and morphological development of P. falciparum revealed substantial activity against ring stages for compounds with two C-10 side chains, while those with only one C-10 side chain exhibited substantial activity against trophozoite stages, suggesting different mechanisms of action.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Piridinas / Lauraceae / Alcaloides / Antimaláricos Limite: Humans País/Região como assunto: America do sul / Caribe ingles / Guyana Idioma: En Revista: J Nat Prod Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Piridinas / Lauraceae / Alcaloides / Antimaláricos Limite: Humans País/Região como assunto: America do sul / Caribe ingles / Guyana Idioma: En Revista: J Nat Prod Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Estados Unidos