Aphadilactone B
Aphadilactone B shows significant antimalarial activity with the IC50 value of 1350 ± 150 nM.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
Mol Med Rep.2023 Oct;28(4):193.
Hanoi University of Pharmacy2023, 14(1):30-39.
Geroscience.2024, 01207-y.
Biomedicines.2022, 10(3):583.
Naunyn Schmiedebergs Arch Pharmacol.2021, 394(1):107-115.
Separations2023, 10(7), 411.
European Journal of Integrative Medicine2018, 20:165-172
Neuropharmacology2019, 151437
Pharmaceuticals.2022, 15(4), 402.
National Academy Science Letters2023, s40009.
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J Org Chem. 2014 Jan 17;79(2):599-607.
Aphadilactones A-D, four diterpenoid dimers with DGAT inhibitory and antimalarial activities from a Meliaceae plant.[Pubmed:
24344740 ]
METHODS AND RESULTS:
Aphadilactone A, Aphadilactone B, Aphadilactone C, Aphadilactone D (1-4), four diastereoisomers possessing an unprecedented carbon skeleton, were isolated from the Meliaceae plant Aphanamixis grandifolia. Their challenging structures and absolute configurations were determined by a combination of spectroscopic data, chemical degradation, fragment synthesis, experimental CD spectra, and ECD calculations.
CONCLUSIONS:
Aphadilactone C (3) with the 5S,11S,5'S,11'S configuration showed potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 ± 0.09 μM, selectivity index > 217) and is the strongest natural DGAT-1 inhibitor discovered to date. In addition, compounds 1-4 showed significant antimalarial activities with IC50 values of 190 ± 60, 1350 ± 150, 170 ± 10, and 120 ± 50 nM, respectively.
