The Wnt/β-catenin signaling pathway plays a key role in the progression of human colorectal cancers (CRCs) and is one of the leading targets of chemotherapy agents developed for CRC. The present study aimed to investigate the anti-cancer effects and molecular mechanisms of 19-O-triphenylmethyl andrographolide (RS-PP-050), an andrographolide analogue and determine its activity in the Wnt/β-catenin pathway. RS-PP-050 was found to potently inhibit the proliferation and survival of HT-29 CRC cells. It induces cell cycle arrest and promotes apoptotic cell death which was associated with the activation of PARP-1 and p53. Furthermore, RS-PP-050 exerts inhibitory effects on β-catenin transcription by suppressing T-cell factor/lymphocyte enhancer factor (TCF/LEF) activity in cells overexpressing β-catenin and by down-regulating the endogenous expression of Wnt target genes. RS-PP-050 also decreased the protein expression of the active form of β-catenin but functions independently of GSK-3β, a negative regulator of Wnt. Interestingly, RS-PP-050 extensively blocks phosphorylation at Ser675 of β-catenin which links to interference of the nuclear translocation of β-catenin and might contribute to Wnt inactivation. Collectively, our findings reveal the underlying anti-cancer mechanism of an andrographolide analogue and provide useful insight for exploiting a newly chemotherapeutic agent in Wnt/β-catenin-overexpressing CRC cells.

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A mild, efficient and metal-free method was described for the green synthesis of dipyrromethanes from aldehydes and unsubstituted pyrrole catalyzed by SO3H-functionalized ionic liquids (SO3H-ILs) in aqueous media at room temperature. Notably, SO3H-ILs, 1-butylsulfonic-3-methylimidazolium hydrogen sulfate ([bsmim][HSO4]) was the most efficient catalyst for moderate to good yields of the corresponding desired products.

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A new strategy for the synthesis of bis-indoletriazoles was developed using a sequential one-pot four-step procedure via I2 and H2SO4–SiO2 catalyzed Friedel–Crafts reactions of indole with aldehyde followed by N-alkylation with propargyl bromide, azidation, and copper­(I)-catalyzed azide alkyne cycloaddition (CuAAC). The reaction proceeded smoothly at room temperature in a short time, and a series of bis-indoletriazoles were obtained in good to excellent yields proving the generality of this one-pot methodology.

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Thai wisdom knows the benefits of mangrove palm fruits to be boiled in water and drink as herbal medicines for healing gout. However, there is no scientific paper to confirm the relief of gout symptoms by mangrove palm, this is the first report. The mangrove palm: exocarp/mesocarp, endocarp, endosperm, and the whole of fruit in the ripe stage were extracted with water and ethanol. The crude extracts were studied for the phytochemical and inhibitory activity of xanthine oxidase, one of the causes of gout. Most of the crude extracts showed similar phytochemicals as, phenolic compounds, flavonoids, terpenoids, and steroids, but there was no alkaloid, anthraquinone, and iridoid glycoside. The endocarp extracted with ethanol showed the highest phenolic content (102.85±5.73 mg GAE/g), flavonoid content (531.02±10.46 mg QUE/g), and strongest antioxidant activity (26.79±0.57 mg VCE/g). The ethanolic and water extract (heating at 60 °C) of endocarp showed the strongly inhibited xanthine oxidase activity with IC50 of 0.029±0.001 mg/mL and 0.14±0.04 mg/mL, respectively. Therefore, this research has already confirmed that the fruit of mangrove palm could inhibit xanthine oxidase enzyme. It would be useful for further development as an herbal medicine or supplementary food for gout likely in the form of hot brewed teas or products that are safe for consumers. Moreover, it also adds value to the peel of the leftovers from consumption. HIGHLIGHTS This is the first report to use Nypa fruticans fruit for healing gout The ethanolic and water extract of endocarp gave the strongly inhibition of xanthine oxidase enzyme The endocarp of Nypa fruticans fruit can be developed for supplementary food or treatment for gout GRAPHICAL ABSTRACT