Abstract
A series of C15 triene urushiol derivatives were synthesized and evaluated for their anti-HepG2 aggregation in vitro. The results indicated that all compounds had an effective anti-HepG2 vitality. Compound 1 was a potent inhibitor of HepG2 with IC50 of 7.886 μM and 150 μM against LO2. Moreover, compound 1 increased the apoptosis of HepG2. Compound 1’s thiol sulfur formed hydrogen bonding interactions with Gly154 and Tyr308, respectively, and made it bound more closely to HDAC2. In addition, it also formed hydrophobic interactions with the residues His33, Pro106, Val107, Gly154, Phe155, and His183, and was provided with a strong van der Waals force by the hydrophobic action.
Highlights
As a natural alkyl phenol, urushiol is similar to SAHA which is efficient for tumor HDACs, but has mutagenic, carcinogenic and genotoxic potential [1]
The total protein was extracted from the logarithmic growth phase of hepatoma HepG2 cell line, The total protein was extracted from the logarithmic growth phase of hepatoma HepG2 cell and the expression of HDAC2 was detected by Western blot method with urushiol derivative line, and the expression of HDAC2 was detected by Western blot method with urushiol derivative compound 1(see Figure 3)
We found that urushiol derivatives have a better inhibitory effect on HepG2 of hepatoma cells after screening the broad-spectrum anticancer activity of urushiol derivatives, which inspired us to select hepatoma cell HepG2 as the research object
Summary
As a natural alkyl phenol, urushiol is similar to SAHA which is efficient for tumor HDACs, but has mutagenic, carcinogenic and genotoxic potential [1]. Urushiol is able to modulate the activity of SIRT inhibitors [2] and prevent lung cancer cell-A549 proliferation [3]. It has a good antibacterial effect on Helicobacter pylori [4,5,6], and stimulates the activity of certain cells of mice, reducing the risk of fatty liver in mice and changing microbial morphology [5,7]. Overexpression of HDACs has been linked to the development of cancers in humans [12]. This evidence suggests that urushiol has potential antitumor effect.
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