•According to the structure of existing amide SDHI fungicides, 40 new coumarin-quinoline amide derivatives were designed and synthesized reasonably. The structures of the compounds were confirmed and ...characterized by 1H NMR, 13C NMR, FT-IR, and HRMS.•The compound 11g was confirmed by single-crystal X-ray diffraction.•Through a series of in vitro activity tests, compounds 11t and 12t were found to have good antifungal activity against Rice sheath blight, which provides theoretical support for further study of SDHI antifungal drugs.•The molecular docking studies of the representative compounds were performed.
Succinate dehydrogenase inhibitors (SDHI) are widely used in plant antifungal agents. To break the barrier of resistance, a series of new coumarin-quinolinamide SDHI derivatives containing monocyclic monoterpenes were designed and synthesized using natural camphor or natural menthol as lead compounds, and their structures were characterized by FT-IR, 1H NMR, 13C NMR and HRMS. In vitro antifungal activity test results showed that the target compounds had inhibitory activity against most plant pathogenic fungi, especially against Rhizoctonia solani and Phytophthora nicotianae var. nicotianae, which was superior to other fungi. Among them, compounds 11t and 12t showed better inhibitory effects on Rhizoctonia solani than the commercial fungicide tricyclazole, with EC50 of 16.90 mg/L and 27.09 mg/L, respectively. Based on this, the detached leaf assay was used to further explore the in vivo therapeutic and preventive effects of compounds 11t and 12t on rice sheath blight in plants. The results of the antifungal activity test in vivo showed that compound 11t was slightly better than the positive control, while compound 12t was close to the control effect of azoxystrobin. More importantly, the more bioactive compounds 11t and 12t did not affect the germination of cowpea seeds and also did not affect the growth of normal human hepatocytes and kidney cells. Molecular docking experiments showed that the introduction of the diethylamino group could promote the formation of hydrogen bonds between the hydrogen atom on the amide bond of the target compound and residue Tyr91, and compounds 11t and 12t had smaller free energy between the amino acid residue, which would enhance the antifungal activity of the compounds. These studies proved the potential value of this series of compounds for the study of novel amide-based SDHI fungicides.
•Excipient emulsions increase the bioaccessibility of β-carotene in spinach.•Mixed micelles promote osmotic absorption of β-carotene in the intestine.•LCT facilitates the entry of β-carotene into the ...circulation via the lymphatic pathway.•Excipient emulsions improve the biological activity of β-carotene in vivo.
This study sought to improve the biological fate of β-carotene obtained from spinach, using in vitro digestion, in situ single-pass intestinal perfusion, and in vivo approaches, to investigate the effects of excipient emulsions with medium- (MCT) and long-chain triglyceride (LCT) as a vehicle for improved health benefits of β-carotene. Results showed that the bioavailability and bioactivity of β-carotene were both significantly higher in the excipient emulsions relative to those without the emulsions. This was especially true when LCT was used as the vehicle. These results were confirmed by bioaccessibility, duodenal absorption, and in vivo absorption and metabolism. Furthermore, animal feeding studies revealed that LCT may have the potential to promote triglyceride and apo-B48 reconstitution and secretion. This suggested that LCT may facilitate the entry of carotenoids into circulation via the lymphatic pathway. These results highlight the importance of the optimization of excipient foods to improve the efficacy of lipophilic carotenoid.
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Three-dimensional (3D) bioprinting enables a controlled deposition of cells, biomaterials, and biological compounds (i.e., bioinks) to build complex 3D biological models, biological ...living systems, and therapeutic products. Developing responsive biomaterials as novel bioinks has been a central focus of research in the field of bioprinting because of their controllable material properties in response to printing-induced external or internal stimuli. In this review, we highlight the most recent advances of responsive biomaterials for 3D bioprinting applications. We review commonly used stimuli-responsive biomaterials and strategies for utilizing multifunctional responsiveness to achieve desirable printability, structural formability, cell viability, and construct bioactivity for 3D bioprinting. We also summarize major bioink formulation strategies currently adopted in 3D bioprinting. We subsequently discuss several promising applications of 3D printing involving responsive biomaterials, such as bioprinting in a supporting bath, 4D bioprinting, and bioprinting new controlled drug delivery systems. Future perspectives on the design and development of novel multifunctional bioinks based on responsive biomaterials and technological innovations are also presented.
Ingestion of fermented foods impacts human immune function, yet the bioactive food components underlying these effects are not understood. Here, we interrogated whether fermented food bioactivity ...relates to microbial metabolites derived from aromatic amino acids, termed aryl-lactates. Using targeted metabolomics, we established the presence of aryl-lactates in commercially available fermented foods. After pinpointing fermented food-associated lactic acid bacteria that produce high levels of aryl-lactates, we identified fermentation conditions to increase aryl-lactate production in food matrices up to 5 × 103 fold vs. standard fermentation conditions. Using ex vivo reporter assays, we found that food matrix conditions optimized for aryl-lactate production exhibited enhanced agonist activity for the human aryl-hydrocarbon receptor (AhR) as compared to standard fermentation conditions and commercial products. Reduced microbial-induced AhR activity has emerged as a hallmark of many chronic inflammatory diseases, thus we envision strategies to enhance AhR bioactivity of fermented foods to be leveraged to improve human health.
•Fermented foods contain bioactive microbe-derived aromatic amino acid metabolites.•Aromatic amino acid metabolism can be manipulated to increase aryl-lactates.•Optimized food ferments increase human aryl-hydrocarbon receptor activity.
The unregulated and extensive application of synthetic compounds, such as preservatives, pesticides, and drugs, poses serious concerns to the environment, food security, and global health. Essential ...oils (EOs) are valid alternatives to these synthetic chemicals due to their therapeutic, antioxidant, and antimicrobial activities. Lavender essential oil (LEO) can be potentially applied in food, cosmetic, textile, agricultural, and pharmaceutical industries. However, its bioactivity can be compromised by its poor stability and solubility, which severely restrict its industrial applications. Encapsulation techniques can improve the functionality of LEO and preserve its bioactivity during storage. This review reports recent advances in the encapsulation of LEO by different methods, such as liposomes, emulsification, spray drying, complex coacervation, inclusion complexation, and electrospinning. It also outlines the effects of different processing conditions and carriers on the stability, physicochemical properties, and release behavior of encapsulated LEO. Moreover, this review focuses on the applications of encapsulated LEO in different food and non-food products.
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•The structure-activity relationship among negamycin analogs was evaluated.•Chemical synthesis of negamycin was summarized.•Key features in each individual synthesis was discussed.
In ...this Digest paper, various approaches toward chemical synthesis of negamycin, a natural dipeptide-like antibiotic, were summarized. The strategy and tactics in each individual synthesis were highlighted. Although the chemical structure of negamycin is relatively simple, the promising bioactivity against Gram-negative bacteria with a novel mechanism of action renders it as an intriguing lead compound for medicinal development.
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Peptaibols are a large family of linear, amphipathic polypeptides consisting of 5-20 amino acid residues generated from the fungal nonribosomal peptide synthetase (NRPS) pathway. With ...a relatively high content of non-proteinogenic amino acids such as α-aminoisobutyrate (Aib) and isovaline (Iva) in the skeleton, peptaibols exhibit a wide range of biological activities, including anti-microbial, cytotoxic, and neuroleptic effects. With five peptaibols brought to market for use as biocontrol agents, this class of peptides has received increasing attention from both biochemists and pharmacologists. In this review, we summarized the progress made in structural characterization, elucidation of biosynthetic pathways, and investigation of biosynthesis elucidation and bioactivities, to promote further efforts to develop peptaibols as pharmaceuticals.
To achieve the desired therapeutic objective, the drug product must deliver the active drug at an optimal rate and amount. By proper biopharmaceutic design, the rate and extent of drug absorption ...(also called as bioavailability) or the systemic delivery of drugs to the body can be varied from rapid and complete absorption to slow and sustained absorption depending upon the desired therapeutic objective. Phytomedicine have served as the foundation for a larger fraction of the current pharmacopeia. But the delivery of phytomedicine is always problematic due to poor aqueous solubility, poor permeation, low systemic availability, instability and extensive first pass metabolism. Current review will discuss in detail about how nanotechnology can enhance the bioavilability and bioactivity of the phytomedicine.
The integration of bioactive glasses (BGs) into hard tissues in in-vivo models can be evaluated through X-ray radiographs. The image contrast plays an important role and should be enhanced to improve ...accurate minimal invasive diagnostics of the performance of BGs containing implants after surgery. The present work shows the effect of the progressive addition of Bi2O3 (up to 12.2 wt%) on the structure, thermal properties, radiopacity, and bioactivity of 45S5-like BG obtained by quenching of the melt prepared from oxide precursors. The BG chemical composition, phase composition, structure, chemical state, thermal properties, and radiopacity were respectively investigated by X-ray fluorescence (XRF), X-ray diffraction (XRD), Raman spectroscopy, X-ray photoelectron spectroscopy (XPS), differential scanning calorimetry (DSC), and radiopacity analysis according to the ISO13116:2014 norm. The bioactivity of the glasses was monitored by immersing them in a simulated body fluid (SBF) under static conditions. The apatite formation ability and ion concentration in SBF after 3, 7, 14, and 21 days were investigated by XRD, scanning electron microscopy (SEM), inductively coupled plasma optical emission spectroscopy (ICP-OES), and ICP mass spectrometry (ICP-MS). All samples were found to be X-ray amorphous. Simultaneous formation of BiO3 and BiO6 units is noted in the BG. The glass radiopacity increased up to 1.8 and 4.2 times compared to the reference glasses without Bi2O3. Bi2O3 additions in the glass slow down the formation of apatite-like structures as a result of the network forming role of BiO3 and BiO6 units in the BG. Nevertheless, the BGs with the 12.2 wt % Bi2O3 still shows the ability to form apatite deposits after 7 days of immersion in simulated body fluid (SBF).
Essential oils (EOs) are liquid preparations, produced from plant materials. Although EOs showed a promising bioactivity in vitro, they could interact in foods with some components (fats, proteins, ...carbohydrates) and pH, thus many authors have reported that a significant effect of EOs toward spoiling and pathogenic microorganisms could be achieved in vivo by using higher amounts of oils. Different methods can be used to assess the bioactivity of EOs (disk diffusion and agar or broth dilution methods); however, there is not a standardized test and researchers propose and use different protocols (evaluating the Minimal Inhibitory Concentration, studying the survival curves, analysis through the scanning electron microscopy, etc.). Thereafter, the scope of this review is a focus on interactions of EOs with proteins, carbohydrates, oils, NaCl, and pH, as well as a brief description on the different protocols to assess their bioactivity both under in vivo and in vitro conditions.
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