Shenhan Xie,Yanyang Sun,Xu Yan,Yu Han,Chunyu Wang,Fengxi Li,Lei Wang,Zhi Wang
An efficient and environmental method was employed to synthesize multi-substituted 2H-pyran from methyl coumalate and β-keto esters or diketones. Porcine pancreas lipase (PPL) can catalyze this transformation in high yields (74–96%) in aqueous medium (H2O: DMSO = 2:1) under mild conditions (60 °C). The reported strategy exhibits high functional group compatibility and broad substrate scope. In addition, it provides access to a variety of tetra-substituted 2H-pyrans which are considered privileged scaffolds with diverse biological activities.
The litchi downy blight disease of litchi caused byPeronophythora litchiiaccounts for severe losses in the field and during storage. While ample quantitative studies have shown that 6-pentyl-2H-pyran-2-one (6PP) possesses antifungal activities against multiple plant pathogenic fungi, the regulatory mechanisms of 6PP-mediated inhibition of fungal pathogenesis and growth are still unknown. Here, we investigated the potential molecular targets of 6PP in the phytopathogenic oomycetesP. litchiithrough integrated deployment of RNA-sequencing, functional genetics, and biochemical techniques to investigate the regulatory effects of 6PP againstP. litchii. Previously we demonstrated that 6PP exerted significant oomyticidal activities. Also, comparative transcriptomic evaluation ofP. litchiistrains treated with 6PP Revealed significant up-regulations in the expression profile of TOR pathway-related genes, includingPlCytochrome Cand the transcription factorsPlYY1. We also noticed that 6PP treatment down-regulated putative negative regulatory genes of the TOR pathway, includingPlSpm1andPlrhoH12inP. litchii. Protein-ligand binding analyses revealed stable affinities between PlYY1, PlCytochrome C, PlSpm1, PlrhoH12 proteins, and the 6PP ligand. Phenotypic characterization ofPlYY1targeted gene deletion strains generated in this study using CRISPR/Cas9 and homologous recombination strategies significantly reduced the vegetative growth, sporangium, encystment, zoospore release, and pathogenicity ofP. litchii. These findings suggest that 6PP-mediated activation ofPlYY1expression positively regulates TOR-related responses and significantly influences vegetative growth and the virulence ofP. litchii. The current investigations revealed novel targets for 6PP and underscored the potential of deploying 6PP in developing management strategies for controlling the litchi downy blight pathogen.Keywords:P. litchii;6-pentyl-2H-pyran-2-one (6PP);TOR pathway;CRISPR/Cas 9;PlYY1
The 4[(Tetrahydro‑2H‑pyran‑2‑yl) oxy] phenol (XG‑d) hydroquinone analog, is found in Vaccinium vitis‑idaea L. Although it is known for its antioxidant properties and high level of safety, its antitumor activity remains to be elucidated. In the present study, the anticancer effect of XG‑d was determined in vitro and in vivo. The cytotoxicity of XG‑d against C26 murine colon carcinoma cells was found to occur in a time‑ and concentration‑dependent manner, whereas little effect was observed in the two normal cell lines (HK‑2 and L02) investigated. Oral administration of XG‑d (100 mg/kg) had effects on the tumor growth of tumor‑bearing mice. Furthermore, marked apoptosis was observed using Hoechst 33258 staining and flow cytometric analysis with annexin V/propidium iodide double staining. XG‑d also downregulated the expression of B‑cell lymphoma 2 (Bcl‑2), increased the expression levels of Bcl‑2‑associated X protein and activated caspase‑9, caspase‑3 and poly(adenosine diphosphate‑ribose) polymerase. The present study demonstrated for the first time, to the best of our knowledge, that XG‑d inhibited cancer cell growth via the induction of apoptosis and was also able to inhibit tumor growth in vivo. These results demonstrated that XG‑d may be used as a potential natural agent for cancer therapy with low toxicity.
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