Background :

Calophyllum  soulattri  is  a  plant  that  contains  amentoflavone. Amentoflavone are able to inhibit angiogenesis by inhibiting the VEGFR -2. In this study,  screening  of  the  inhibitory  activity  of  amentoflavones  against  8  tyrosine kinase enzymes was carried out  in vitro  and continued with molecular  docking  of the most inhibited enzyme.

Methods :

Amentoflavone  were obtained by isolating the ethyl acetate fraction of C. soulattri leaves using vacuum liquid chromatography, column chromatography, and chromatotrone. Amentoflavone was tested for its activity as an inhibitor of the tyrosine  kinase  enzyme  in  vitro  using  the  ADP-Glo  kinase  assay  method. Amentoflavone  were also bound to the enzyme with the best inhibition based on the results of  in vitro  tests with AutoDock Vina and Biovia to determine the binding nergy and interactions that occur.

Results :

Amentoflavones (6.8 mg) were isolated from C. soulattri  leaves. The  in vitro  test showed the best inhibitory activity against the  KDR/VEGFR -2 enzyme (3%). Based on the binding of the molecule to VEGFR -2, the bond energy value of the amentoflavones produced was -3.1 kcal/mol. The docking visualization showed hydrogen interactions, hydrophobic interactions, electrostatic interactions,

and unvafourable interactions involving the CYS919 amino acid as the binding site

for ATP.

Conclusion :

Amentoflavones from C. soulattri have the potential to be inhibitors of the tyrosine kinase enzyme based on  in vitro  and  in silico  results. Molecular dynamics testing of VEGFR-2, IGF1R, InsR, PDGFR-α and PDGFR-β is required.

Key  word :

Amentoflavone,  KDR/VEGFR-2,  Calophyllum  soulattri,  Tyrosine kinase