Caesalpinia sappan L. Wood is a Potential Source of Natural Phosphodiesterase-1 Inhibitors
Penulis/Author
HELMI (1); Prof. Dr.rer.nat. Nanang Fakhrudin, M.Si., Apt. (2); Prof. Dr. apt. Arief Nurrochmad, M.Si., M.Sc. (3); Dr. B.S. Ari Sudarmanto, M.Si. (4); Prof. Dr. apt. Zullies Ikawati. (5)
Tanggal/Date
2020
Kata Kunci/Keyword
Abstrak/Abstract
Introduction: A decrease in cAMP and cGMP levels in the brain is linked to human cognitive
problems. The degradation of cellular cAMP and cGMP is attributed to phosphodiesterases
(PDEs), which constitute a superfamily of enzymes. The inhibition of PDE1 is a promising
mechanism to increase cAMP and cGMP levels associated with cognitive disorders.
Caesalpinia sappan L. (CS) wood is a natural coloring agent usually consumed as a traditional
refreshment or drink by people in Yogyakarta, Indonesia. However, scientific evidence regarding
the inhibitory activity of CS wood against PDE1 has yet to be obtained. This study aimed to
investigate the potency of CS wood as a PDE1 inhibitor. Methods: The ethanol extract of CS
wood and its fractions were evaluated in vitro by using a cyclic nucleotide phosphodiesterase
assay kit. The presence of brazilin in the extract and fractions was analyzed by thin-layer
chromatography. In silico assay was performed using MOE software to obtain insights into the
interaction between compounds in the CS wood and the enzyme. Results: Ethanol extract
and ethyl acetate soluble fraction effectively inhibited the PDE1 activity. Interestingly, brazilin,
the major compound in CS wood, also exhibited a potent inhibitory effect on the enzyme.
The in silico assay revealed that the interaction between tetraacetylbrazilin and brazilin with
the PDE1B active site involved hydrogen bonding and ?–? interactions. Conclusion: Ethanol
extract, ethyl acetate soluble fraction, and brazilin inhibited the PDE1 activity. CS wood and its
chemical constituent could be developed as natural cognitive enhancers.
