TY - JOUR
T1 - Dihydrolucilactaene, a Potent Antimalarial Compound from Fusarium sp. RK97-94
AU - A. Abdelhakim, Islam
AU - Bin Mahmud, Fauze
AU - Motoyama, Takayuki
AU - Futamura, Yushi
AU - Takahashi, Shunji
AU - Osada, Hiroyuki
N1 - Funding Information:
This work was supported in part by Grant-in-Aid for Scientific Research (KAKENHI A) 21H04720, Grant-in-Aid for Scientific Research on Innovative Areas 17H0642, and a grant from the Egypt-Japan Education Partnership (EJEP) fund through a collaborative arrangement between the Japan International Cooperation Agency (JICA) and the Egyptian Ministry of High Education (MOHE)-Cultural Affairs and Missions Sector. We would like to thank Dr. Toshihiko Nogawa for HR-MS analysis and Dr. Takeshi Shimizu for his support in structure elucidation. We are indebted to Ms. Harumi Aono, Ms. Emiko Sanada, Dr. Motoko Uchida, Dr. Rachael A. Uson-Lopez, and Ms. Keiko Watanabe (RIKEN) for their support in biological activity tests.
Publisher Copyright:
© 2021 American Chemical Society and American Society of Pharmacognosy
PY - 2022/1/28
Y1 - 2022/1/28
N2 - A recently discovered secondary metabolism regulator, NPD938, was used to alter the secondary metabolite profile in Fusarium sp. RK97-94. Three lucilactaene analogues were detected via UPLC-ESI-MS analysis in NPD938-treated culture. The three metabolites were successfully purified and identified as dihydroNG391 (1), dihydrolucilactaene (2), and 13α-hydroxylucilactaene (3) via extensive spectroscopic analyses. DihydroNG391 (1) exhibited weak in vitro antimalarial activity (IC50 = 62 μM). In contrast, dihydrolucilactaene (2) and 13α-hydroxylucilactaene (3) showed very potent antimalarial activity (IC50 = 0.0015 and 0.68 μM, respectively). These findings provide insight into the structure–activity relationship of lucilactaene and its analogues as antimalarial lead compounds.
AB - A recently discovered secondary metabolism regulator, NPD938, was used to alter the secondary metabolite profile in Fusarium sp. RK97-94. Three lucilactaene analogues were detected via UPLC-ESI-MS analysis in NPD938-treated culture. The three metabolites were successfully purified and identified as dihydroNG391 (1), dihydrolucilactaene (2), and 13α-hydroxylucilactaene (3) via extensive spectroscopic analyses. DihydroNG391 (1) exhibited weak in vitro antimalarial activity (IC50 = 62 μM). In contrast, dihydrolucilactaene (2) and 13α-hydroxylucilactaene (3) showed very potent antimalarial activity (IC50 = 0.0015 and 0.68 μM, respectively). These findings provide insight into the structure–activity relationship of lucilactaene and its analogues as antimalarial lead compounds.
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U2 - 10.1021/acs.jnatprod.1c00677
DO - 10.1021/acs.jnatprod.1c00677
M3 - Article
C2 - 34949088
AN - SCOPUS:85122573223
SN - 0163-3864
VL - 85
SP - 63
EP - 69
JO - Journal of Natural Products
JF - Journal of Natural Products
IS - 1
ER -