Antitumor effects of candidone extracted from Derris indica (Lamk) Bennet in cholangiocarcinoma cells

Purpose: To investigate the antitumor effect of candidone extracted from Derris indica, against human cholangiocarcinoma (CCA) cells.Methods: Candidone was purified from the hexane extract of Derris indica fruit. CCA cell lines, KKUM156 and KKU-M213, were treated with candidone. Sulforhodamine B (SRB) assay and acridine orange/ethidium bromide (AO/EB) staining were used to investigate the effects of candidone on cell proliferation and induction of apoptosis, respectively. The effect on cell migration was assessed by wound healing assay. Reverse transcription-quantitative polymerase chain reaction (RT-qPCR) was employed to assess the effects of candidone on the expression of genes that regulate proliferation and apoptosis.Results: Candidone exerted strong anticancer effects on CCA cells. The agent suppressed CCA cell proliferation and induced apoptotic cell death. RT-qPCR assay revealed that candidone significantly increased the expression of anti-proliferative and pro-apoptotic genes, including p21 and Bax, and decreased the expression of anti-apoptotic genes, including Bcl-2 and survivin. Moreover, candidone inhibited the migration of CCA cells induced by IGF-1.Conclusion: Candidone exhibits potent antitumor effect on CCA cells. These findings suggest that candidone is potentially suitable for the management of CCA and, therefore, warrants further investigation.Keywords: Candidone, Derris indica, Cholangiocarcinoma, Cytotoxicity, Apoptosi

Cytotoxicity of flavonoids and isoflavonoids from <i>Crotalaria bracteata</i>

<p>A new flavonoid, crotakanda (<b>1</b>), and seven known compounds including a flavonoid, four isoflavonoids, a pterocarpan and a cinnamaldehyde were isolated from the stems and roots of <i>Crotalaria bracteata.</i> Their structures were elucidated by a combination of spectroscopic methods. Compound <b>2</b> showed cytotoxicity against MCF-7 with an IC₅₀ value of 79.90 μM whereas <b>2</b> and <b>4</b> exhibited cytotoxicity against the NCI-H187 cell line with IC₅₀ values of 71.57 and 95.47 μM, respectively.</p

Inhibition of capsaicin and dihydrocapsaicin derivatives towards histone deacetylase and molecular docking studies

The natural products, capsaicin and dihydrocapsaicin, were modified at double-bond and phenolic moieties to provide twelve capsaicin and dihydrocapsaicin derivatives. The natural products and synthesized compounds were evaluated as histone deacetylase inhibitors via in vitro fluorometric assay at 500 mM concentrations. The results revealed that a methyl ester derivative and a silyl-protected dihydrocapsaicin were the best histone deacetylase inhibitors among the tested compounds with 87% and 85% inhibitions, respectively. Molecular docking experiments were conducted on the obtained compounds with the human HDAC8 enzyme. These data show a new method for providing putative histone deacetylase inhibitors from common natural products

A new furanocoumarin from the fruits of <i>Scaevola taccada</i> and antifungal activity against <i>Pythium insidiosum</i>

<p>A new coumarin, scataccanol (<b>1</b>) and 10 known compounds were isolated from the fruits of <i>Scaevola taccada</i> (Gaertn.) Roxb<i>.</i> All compounds were evaluated for antifungal activity against <i>Pythium insidiosum</i>. Compounds <b>5</b> and <b>7</b> showed strong antifungal activity with minimum inhibitory concentration values of 5 and 10 μg/mL, respectively. Structural determination of all compounds was accomplished by 1D and 2D-NMR, IR and MS.</p

Cytotoxic flavonoids from the fruits of <i>Derris indica</i>

<p>Chemical investigation of the ethyl acetate extract from the fruits of <i>Derris indica</i> has led to the isolation of a new furanoflavonoid derivative, 4′-hydroxypinnatin (<b>1</b>), and five known compounds. Pinnatin (<b>2</b>) showed strong cytotoxicity against cholangiocarcinoma (KKU-100) and human hepatoma (HepG2) cell lines with IC₅₀ values of 6.0 ± 2.7 and 9.0 ± 4.1 μg/ml, respectively, and showed maximal cell killing effect of about 88–90%. Flavone <b>5</b> exhibited the most cytotoxicity against KKU-100 but it showed moderate efficacy (Emax = 50.7%).</p