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Potential antimalarial derivatives from astraodorol.

Pitak Nasomjai1, Kittibhorn Arpha, Sirirath Sodngam

  • 1Natural Products Research Unit, Centre of Excellence for Innovation in Chemistry, Department of Chemistry, Faculty of Science, Khon Kaen University, Khon Kaen, 40002, Thailand, nphita@kku.ac.th.

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Modified Astraodorol compounds from Astraeus odoratus show potent antimalarial activity. Several derivatives displayed significant efficacy against malaria parasites, with some also exhibiting moderate cytotoxicity against cancer cell lines.

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Area of Science:

  • Natural Product Chemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Astraodorol, a lanostane-type triterpene from Astraeus odoratus, is a potential lead compound.
  • Triterpenes are known for diverse biological activities, including antimalarial properties.

Purpose of the Study:

  • To synthesize novel Astraodorol derivatives.
  • To evaluate the antimalarial and cytotoxic activities of these derivatives.

Main Methods:

  • Chemical synthesis of ten Astraodorol derivatives.
  • In vitro evaluation of antimalarial activity using IC50 values.
  • In vitro assessment of cytotoxicity against various cancer and normal cell lines (NCI-H187, KB, MCF-7, Vero).

Main Results:

  • Seven derivatives (compounds 5, 6, 7a, 7c, 7e, 7f, 7g) showed strong antimalarial activity (IC50 values ranging from 3.23 to 4.85 µg/mL).
  • Compounds 7a, 7c, and 7e exhibited moderate cytotoxicity against NCI-H187 cells (IC50 values 9.84–34.28 µg/mL).
  • Compound 7e displayed moderate cytotoxicity against KB, MCF-7, and Vero cell lines (IC50 values 16.94–49.60 µg/mL).

Conclusions:

  • Chemical modification of Astraodorol yields potent antimalarial compounds.
  • Derivative 7e shows a promising balance of antimalarial activity and moderate cytotoxicity, warranting further investigation.