2. Academic Validation
  3. Dihydrolucilactaene, a Potent Antimalarial Compound from Fusarium sp. RK97-94

Dihydrolucilactaene, a Potent Antimalarial Compound from Fusarium sp. RK97-94

  • J Nat Prod. 2022 Jan 28;85(1):63-69. doi: 10.1021/acs.jnatprod.1c00677.
Islam A Abdelhakim 1 2 3 4,  Fauze Bin Mahmud 3 5 6,  Takayuki Motoyama 3,  Yushi Futamura 3,  Shunji Takahashi 4,  Hiroyuki Osada 3
Affiliations

Affiliations

  • 1 Graduate School of Science and Engineering, Saitama University, Sakura, Saitama 338-8570, Japan.
  • 2 Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71515, Egypt.
  • 3 Chemical Biology Research Group, RIKEN CSRS, Wako, Saitama 351-0198, Japan.
  • 4 Natural Product Biosynthesis Research Unit, RIKEN CSRS, Wako, Saitama 351-0198, Japan.
  • 5 Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Penang 11800, Malaysia.
  • 6 Faculty of Science and Natural Resources, Universiti Malaysia Sabah, Sabah 88400, Malaysia.
PMID: 34949088 DOI: 10.1021/acs.jnatprod.1c00677
Abstract

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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