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41.
In our continuous search for new nitric oxide (NO) inhibitory compounds as potential anti-inflammatory agents or lead compounds for inflammatory diseases, the chemical constituents of Euonymus verrucosus var. pauciflorus were investigated, leading to the isolation of eleven terpenoids including six new diterpenoids, designated as euonymupenes A–F. The structures were elucidated on the basis of NMR and ECD data analysis. Euonymupenes A, C, and F feature rare labdane-type norditerpenoid skeletons. The NO inhibitory effects were evaluated and all of the isolates were found to inhibit lipopolysaccharide (LPS)-induced NO production in murine microglial BV-2 cells. Western blotting analysis indicated that the most active compound (5) can regulate iNOS (inducible nitric oxide synthase) expression. The further molecular docking studies exhibited the affinities of bioactive compounds with iNOS. 相似文献
42.
《Current biology : CB》2020,30(14):2777-2790.e4
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43.
Green tea contains active ingredients which are beneficial for health. While numerous studies have been conducted on the components extracted from green tea, few studies have investigated the active ingredients in tea residue. In this study, proteins were extracted from green tea residue via an optimised alkaline extraction combined with enzymatic hydrolysis, of which, an acidic protease was selected to prepare an enzymatic hydrolysate because of its high angiotensin converting enzyme (ACE) inhibitory activity. The composition characteristics of extracted green tea proteolysis products were elucidated, including amino acid composition, molecular weight distribution and possible amino acid sequences. In addition, the protein hydrolysate had anti-digestive properties, maintained its activity of inhibiting ACE enzyme at different temperatures, pH and metal ions, and exhibited antihypertensive activity in animals. In conclusion, the optimised alkaline extraction and enzymatic hydrolysis conditions of a ACE inhibitory peptide from green tea residue is an optimal extraction method to maintain its antihypertensive activity, providing the basis for the clinical application of green tea for blood pressure reduction. 相似文献
44.
Black cumin (Nigella sativa) seed protein (BCSP) was individually hydrolyzed with pepsin, trypsin, and α-chymotrypsin. After ultrafiltration, the α-chymotrypsin hydrolysate (< 3 kDa) exhibited the highest ACE inhibitory (ACEI) activity with an IC50 value of 34.4 ± 1.5 μg/mL. This hydrolysate was orthogonally fractionalized using reversed-phase high-performance liquid chromatography (RP-HPLC) and strong cation exchange (SCX) chromatography, and the most active RP-HPLC and SCX fractions (F7 and H4, respectively) were individually screened out by ACEI assay. These two fractions were analyzed with liquid chromatography-tandem mass spectrometry (LC–MS/MS) followed by automated de novo peptide sequencing, and totally 43 ACEI candidate peptides were identified. Three overlapping peptides (VTPVGVPKW, VVTPVGVPKW, and LVLTL) were simultaneously contained in both fractions, and VTPVGVPKW (VW-9) was speculated as to the most potent ACEI peptide based on the in silico analysis. Synthetic VW-9 was used to confirm the identity, and a remarkable IC50 value of VW-9 (1.8 ± 0.09 μM) was determined. Preincubation and inhibition mechanism studies indicated that VW-9 was a true inhibitor as well as a non-competitive inhibitor on ACE, which was further illustrated with the molecular docking simulation. Our study revealed that the application of VW-9 to antihypertensive products is promising. 相似文献
45.
This work studied the effects of ultrasound-assisted liquid-state fermentation on the content of peptides and bioactivity of fermented soybean meal (FSBM) with Bacillus subtilis. Based on the optimization of basic ultrasonic parameters, effects of the main parameters including power density, incubation temperature and ultrasonic time on in vitro ACE inhibitory activity, peptides content and biomass of B. subtilis were investigated via Box-Behnken experimental design. Three mathematical models were determined to show the effects of each variable and their combinatorial interactions on dependent variables. A set of preferred condition was determined to be at power density of 0.08 W/mL for 1 h with an initial incubation temperature of 36.7 °C, according to the desirability function analyses. Under these conditions, the experimental values of in vitro ACE inhibitory activity, peptides content and biomass increased by 26.4%, 36.2% and 55.0% compared to those of the control, respectively, accompanied by the improvement of the peptides yield, purity and conversion rate in varying degrees. Additionally, FSBM resulted in a significant decrease of systolic blood pressure by 20.7 ± 1.8 mmHg in spontaneously hypertensive rats at 3 h. These results suggest that ultrasonication is an efficient solution for enhancing fermentation to produce bioactive components from agroindustrial by-products. 相似文献
46.
47.
Gloria Gutirrez‐Venegas Manuel Alejandro Snchez‐Carballido Claire Delmas Surez Juan Arturo Gmez‐Mora Nomie Bonneau 《Cell biology international》2020,44(3):686-720
Squamous cell carcinoma (SCC) of the tongue is associated with tobacco use, alcohol abuse, and human papillomavirus (HPV) infections. While clinical outcomes have recently improved for HPV‐positive patients in general, 50% of patients suffering from tongue cancer die within 5 years of being diagnosed. Flavonoids are secondary plant metabolites with a wide range of biological activities including antioxidant, anti‐inflammatory, and anticancer activities. Flavonoids have generated high interest as therapeutic agents owing to their low toxicity and their effects on a large variety of cancer cell types. In this literature review, we evaluate the actions of flavonoids on SCC of the tongue demonstrated in both in vivo and in vitro models. 相似文献
48.
《Fungal biology》2020,124(7):671-681
Silver nanoparticles (Ag NP) were synthesized using rice leaf extract and optimized synthetic conditions were found to be 0.4 % leaf extract, 0.6 mM AgNO3 and 30 min of autoclaving. Produced NP were characterized using UV–vis, DLS, zeta potential, XRD, TEM and FTIR. Ag NP formation was established from UV–vis spectra and NP showed zeta potential value of −27.4 mV. NP were spherical, polydisperse and average size was 16.5 ± 6.2 nm. Antifungal activity of Ag NP was assessed by poisoned food technique and resazurin broth dilution against mycelium and sclerotia of fungus R. solani, the causative agent of sheath blight disease in rice. Results confirmed effective hyphal growth inhibition and % growth inhibition was dose dependent (2.5–10 μg/mL). Ag NP showed enhanced mycelial inhibition (81.7–96.7 %) at 10 μg/mL. MIC values of Ag NP were in the range of 5–10 and 15–20 μg/mL towards fungal mycelium and sclerotia, respectively. Ag NP treatment (20 μg/mL) completely inhibited the disease incidence at 20 μg/mL. Ag NP treatment (10 μg/mL) caused 1.3 and 1.5 times enhancement in seedling vigor index. Hence, Ag NP can be utilized towards management and control of various fungal diseases of crops. 相似文献
49.
《Bioorganic & medicinal chemistry letters》2020,30(12):127192
The identification of a novel series of DprE1 inhibitors based on a 2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-N-phenylpropanamide scaffold is described herein. SAR exploration around the HTS hit 1 led to the identification of multiple analogues with potent DprE1 inhibition and good whole-cell antimycobacterial activity. 相似文献
50.
Roberto Arredondo-Valdés Francisco D. Hernández-Castillo Mario Rocandio-Rodríguez Julia C. Anguiano-Cabello Madai Rosas-Mejía Venancio Vanoye-Eligio Salvador Ordaz-Silva Imelda V. López-Sánchez Laura D. Carrazco-Peña Julio C. Chacón-Hernández 《Phyton》2021,90(3):895-906
The tomato (Solanum lycopersicum L.) is one of the world’s most important vegetable crops. Still, phytopathogenic bacteria affect the yield and quality of tomato cultivation, like Agrobacterium tumefeciens (At), Clavibacter
michiganensis subsp. michiganensis (Cmm), Pseudomonas syringae pv. tomato (Pst), Ralstonia solanacearum (Rs),
and Xanthomonas axonopodis (Xa). Synthetic chemical products are used mostly on disease plant control, but
overuse generates resistance to bacterial control. This study aimed to evaluate the in vitro antibacterial activity
of the ethanolic extract of Moringa oleifera Lam. leaves against At, Cmm, Pst, Rs, and Xa, as well as information
about this plant species’ chemical composition. Antibacterial activity against pathogens observed by microplate
technique, phytochemical screening, and FTIR analysis revealed different bio-active compounds on ethanolic
extracts with antibacterial activity. The growth inhibition rate ranged between 0.08% and 99.94%. The inhibitory
concentration, IC50, required to inhibit 50% of At, Cmm, Pst, Rs, and Xa bacterial growth, was 276.67, 350.48,
277.85, 351.49, and 283.22 mg/L, respectively. Inhibition of phytopathogen bacteria’s growth increased as the concentrations of the extract also increased. Moringa oleifera extract can be recommended as a potent bio-bactericide. 相似文献