TY - JOUR
T1 - Ecology- and bioassay-guided drug discovery for treatments of tropical parasitic disease
T2 - 5a,8a-epidioxycholest-6-en-3β-ol isolated from the mollusk dolabrifera dolabrifera shows significant activity against leishmania donovani
AU - Clark, Kathryn E.
AU - Capper, Angela
AU - Togna, Gina Della
AU - Paul, Valerie J.
AU - Romero, Luz I.
AU - Johns, Timothy
AU - Cubilla-Rios, Luis
AU - Capson, Todd L.
PY - 2013/11/1
Y1 - 2013/11/1
N2 - An ecology- and bioassay-guided search employed to discover compounds with activity against tropical parasitic diseases and cancer from the opisthobranch mollusk, Dolabrifera dolabrifera, led to the discovery of antileishmanial properties in the known compound, 5a,8a-epidioxycholest-6- en-3ß-ol (1). Compound 1 was identified through nuclear magnetic resonance spectroscopy (1H, 13C) and mass spectrometry. The compound was concentrated in the digestive gland of D. dolabrifera, but was not detected in other body parts, fecal matter or mucus. Compound 1 showed an IC50 of 4.9 μM towards the amastigote form of Leishmania donovani compared with an IC50 of 281 μM towards the control Vero cell line, a 57.3-fold difference, and demonstrated no measurable activity against Plasmodium falciparum, Trypanosoma cruzi, and the breast cancer cell line, MCF-7.
AB - An ecology- and bioassay-guided search employed to discover compounds with activity against tropical parasitic diseases and cancer from the opisthobranch mollusk, Dolabrifera dolabrifera, led to the discovery of antileishmanial properties in the known compound, 5a,8a-epidioxycholest-6- en-3ß-ol (1). Compound 1 was identified through nuclear magnetic resonance spectroscopy (1H, 13C) and mass spectrometry. The compound was concentrated in the digestive gland of D. dolabrifera, but was not detected in other body parts, fecal matter or mucus. Compound 1 showed an IC50 of 4.9 μM towards the amastigote form of Leishmania donovani compared with an IC50 of 281 μM towards the control Vero cell line, a 57.3-fold difference, and demonstrated no measurable activity against Plasmodium falciparum, Trypanosoma cruzi, and the breast cancer cell line, MCF-7.
KW - Antileishmanial
KW - Chemical ecology
KW - Endoperoxide
KW - Marine invertebrate
UR - https://www.scopus.com/pages/publications/84887422439
U2 - 10.1177/1934578X1300801109
DO - 10.1177/1934578X1300801109
M3 - Article
C2 - 24427935
AN - SCOPUS:84887422439
SN - 1934-578X
VL - 8
SP - 1537
EP - 1540
JO - Natural Product Communications
JF - Natural Product Communications
IS - 11
ER -
