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Histone Deacetylase Inhibitory and Cytotoxic Activities of the Constituents from the Roots of Sophora Pachycarpa.

ABSTRACT: Four prenylated flavonoids, including isosophoranone, sophoraflavanone G, alopecurone J, alopecurone P, and a resveratrol derivative HPD (2-(4-hydroxyphenyl)-2,3-dihydrobenzo[b] furan-3,4,6-triol), were isolated from the roots of Sophora pachycarpa. The cytotoxic activity of obtained compounds was evaluated against A2780, A549, HeLa, and HCT116 human cancer cell lines. We also evaluated their histone deacetylase (HDAC) inhibitory activities. Of all compounds tested, alopecurone J was the most active with IC50 values in the range of 9.97-30.91 μM against four cancer cell lines with potent pan-HDAC inhibitory activity (IC50 = 0.08-3.85 μM). Molecular docking experiments of these compounds with HDAC8 displayed potential selective HDAC inhibitory. Molecular docking data showed consistent results in the in-vitro experiments with high selectivity towards HDAC8. The Resveratrol group plays an essential role in HDAC inhibition.

SUBMITTER: Soltani S 

PROVIDER: S-EPMC8019873 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature

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Histone Deacetylase Inhibitory and Cytotoxic Activities of the Constituents from the Roots of <i>Sophora Pachycarpa</i>.

Soltani Saba S   Boozari Motahareh M   Nejad Ebrahimi Samad S   Amin Gholam Reza GR   Iranshahi Mehrdad M  

Iranian journal of pharmaceutical research : IJPR 20200101 4

Four prenylated flavonoids, including isosophoranone, sophoraflavanone G, alopecurone J, alopecurone P, and a resveratrol derivative HPD (2-(4-hydroxyphenyl)-2,3-dihydrobenzo[b] furan-3,4,6-triol), were isolated from the roots of <i>Sophora pachycarpa</i>. The cytotoxic activity of obtained compounds was evaluated against A2780, A549, HeLa, and HCT116 human cancer cell lines. We also evaluated their histone deacetylase (HDAC) inhibitory activities. Of all compounds tested, alopecurone J was the  ...[more]

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