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Volumn 6, Issue 9, 2011, Pages 1572-1577

Bromophycolide A targets heme crystallization in the human malaria parasite Plasmodium falciparum

Author keywords

Antimalarial agents; Confocal imaging; Hemins; Macroalgae; Natural products

Indexed keywords

4 DIMETHYLAMINOPYRIDINE; AMODIAQUINE; ANTIMALARIAL AGENT; BROMOPHYCOLIDE A; ETHYLDIISOPROPYLAMINE; HEMATIN; HYDROXYL GROUP; N' (3 DIMETHYLAMINOPROPYL) N ETHYLCARBODIIMIDE; N,N DIMETHYLFORMAMIDE; QUININE; UNCLASSIFIED DRUG;

EID: 80052089004     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201100252     Document Type: Article
Times cited : (20)

References (38)
  • 5
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    • Klayman, D.L.1
  • 20
    • 80052086337 scopus 로고    scopus 로고
    • S. Cervantes, E.P. Stout, J. Prudhomme, S. Engel, M. Bruton, M. Cervantes, D. Carter, Y. Tae-Chang, M.E. Hay, W. Aalbersberg, J. Kubanek, K. LeRoch, 2011, unpublished results.
    • S. Cervantes, E.P. Stout, J. Prudhomme, S. Engel, M. Bruton, M. Cervantes, D. Carter, Y. Tae-Chang, M.E. Hay, W. Aalbersberg, J. Kubanek, K. LeRoch, 2011, unpublished results.
  • 22
    • 80052080071 scopus 로고    scopus 로고
    • The localization of probe 15 arose due to its natural product and not its pendant dyes, as compounds 14a and 14b did not localize within the neutral lipids. While the potential for dyes to localize within lipids and membranes is always an issue, the 7-dimethylamino-4-coumarin acetamide tag did not suffer from this issue here or within prior reports; see further references[16] and [24,25].
    • The localization of probe 15 arose due to its natural product and not its pendant dyes, as compounds 14a and 14b did not localize within the neutral lipids. While the potential for dyes to localize within lipids and membranes is always an issue, the 7-dimethylamino-4-coumarin acetamide tag did not suffer from this issue here or within prior reports; see further references[16] and [24, 25].
  • 29
    • 80052090801 scopus 로고    scopus 로고
    • Fe-OH coordination of bromophycolides with heme may require that the C18-OAc derivative 7 undergoes deacylation by esterases, making 7 a putative prodrug of the hydrophobic natural product 1. This is seemingly unsupported by the cellular studies with probe 15 as shown in Figures2 and 3, as release of the tags would fail to deliver the observed localization. However, proliferation assays need 72h of compound/parasite incubation, whereas microscopy studies only require 1-2h of probe exposure.
    • Fe-OH coordination of bromophycolides with heme may require that the C18-OAc derivative 7 undergoes deacylation by esterases, making 7 a putative prodrug of the hydrophobic natural product 1. This is seemingly unsupported by the cellular studies with probe 15 as shown in Figures2 and 3, as release of the tags would fail to deliver the observed localization. However, proliferation assays need 72h of compound/parasite incubation, whereas microscopy studies only require 1-2h of probe exposure.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.