In this article, we aim to examine the novel effects of β‐sitosterol on murine experimental colitis. β‐Sitosterol significantly reduces the weight loss, colon length, and alleviated microscopic appearances of colitis induced by dextran sulfate sodium. This compound also decreases the levels of TNF‐α, IL‐6, and IL‐1β in intestinal tissue of mice with experimental colitis in a concentration‐dependent manner. β‐Sitosterol treatment to intestinal epithelial cells significantly increases expression of antimicrobial peptides and reduces survival of intracellular Salmonella typhimurium. These results showed the multiple effects of β‐sitosterol against pathogenic bacteria for a novel approach to the treatment of colonic inflammation.
In this work, the inclusion complexes of hydrophobic herbicide bensulfuron-methyl (BSM) with β-cyclodextrin (β-CD) and (2-hydroxypropyl)-β-CD (2-HP-β-CD) were prepared and characterized. Phase solubility study showed that both β-CD and 2-HP-β-CD increased the solubility of BSM. Three-dimensional structures of the inclusion complexes were simulated by the molecular docking method. The docking results indicated that guest BSM could enter into the cavities of host CDs, folded, and centrally aligned inside the inclusion complexes. The benzene ring of the guest molecule was close to the wide rim of the host molecules; the pyrimidine ring and side chains of the guest molecule were oriented toward the narrow rim of the host molecule. The inclusion complexes were successfully prepared by the coprecipitation method. The physiochemical characterization data of 1H NMR, FT-IR, XRD, and DSC showed that the guest and host molecules were well included. BSM had lower soil adsorption and higher herbicidal activity in the complexation form with β-CD or 2-HP-β-CD than in the pure form. The present study provides an approach to develop a novel CDs-based formulation for hydrophobic herbicides.
A water-soluble inclusion complex for butachlor was prepared by complexation with (2-hydroxypropyl)-βcyclodextrin (HP-β-CD). Phase solubility results indicated a 1:1 stoichiometric ratio with an apparent stability constant of 864.3 M −1 in the obtained solid complex. The formation of the complex was confirmed by 1 H nuclear magnetic resonance, Fourier transform infrared, and differential scanning calorimetry spectra. Coupled with the molecular docking results, butachlor was considered to be completely included in HP-β-CD cavity. Butachlor complexation with HP-β-CD decreased its adsorption capacity and enhanced its mobility in soil. The inclusion complex displayed better herbicidal activities than free butachlor. The 96 h median lethal concentration values of the inclusion complex and free butachlor was 2.30 and 0.65 mg L −1 , respectively, for zebrafish, indicating that the complexation could significantly reduce toxicity to fishes. The present study provides an approach to develop environment-friendly formulations using CDs for herbicides.
Rice blast, caused by the ascomycete fungus Magnaporthe oryzae, is one of the most destructive plant diseases in the world and a serious threat to global food security. Biofungicide physcion, extracted from roots of Chinese traditional herb rhubarb, has been commercialized to control cucumber powdery mildew (Podosphaera fuliginea) in China as a new active and environmentally-friendly ingredient. This study investigated its bioactivity on rice blast and impact on the infection of M. oryzae. Physcion was effective on M. oryzae with 50% inhibition concentration of 18.19 mg/l on the fungus mycelium growth in vitro and provided 86 and 98% control efficacy in vivo at the concentrations of 40 and 60 mg/l, respectively. It inhibited the initial infection of M. oryzae by inhibiting growth of mycelia, the germination of conidia and the formation of appressoria. Moreover, it inhibited the secondary infection of the fungus at the concentration of 40 mg/l, but had no influence at the low concentrations of 1.25-20 mg/l. So physcion might be a promising natural plant extract that is worthy of being explored to apply on the control of rice blast.
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