Characterization of Lomofungin Gene Cluster Enables the Biosynthesis of Related Phenazine Derivatives.

Phenazine-based small molecules are nitrogen-containing heterocyclic compounds with diverse bioactivities and electron transfer properties that exhibit promising applications in pharmaceutical and electrochemical industries. However, the biosynthetic mechanism of highly substituted natural phenazines remains poorly understood. In this study, we report the direct cloning and heterologous expression of the lomofungin biosynthetic gene cluster (BGC) from Streptomyces lomondensis S015. Reconstruction and overexpression of the BGCs in Streptomyces coelicolor M1152 resulted in eight phenazine derivatives including two novel hybrid phenazine metabolites, and the biosynthetic pathway of lomofungin was proposed. Furthermore, gene deletion suggested that NAD(P)H-dependent oxidoreductase gene lomo14 is a nonessential gene in the biosynthesis of lomofungin. Cytotoxicity evaluation of the isolated phenazines and lomofungin was performed. Specifically, lomofungin shows substantial inhibition against two human cancer cells, HCT116 and 5637. These results provide insights into the biosynthetic mechanism of lomofungin, which will be useful for the directed biosynthesis of natural phenazine derivatives.

The Janus effect of colloidal self-assembly on the biological response of amphiphilic drugs.

In aqueous environment amphiphilic molecules organize themselves into supramolecular structures deeply affecting the chemo-physical properties. Supramolecular assemby is also crucial in the pharmaceutical development of bioactive lipophilic molecules whose attitude to self-aggregate is a recognized factor affecting the in vivo pharmacokinetic, but can also play a crucial role in the interaction with the biological targets in in vitro tests. In aqueous solution, amphiphilic drugs exist in a complex equilibrium involving free monomers, oligomers and larger supramolecular aggregates held together by noncovalent bonds. In this review we focus our attention on the dual effect of drugs self-assembly, which can both reduce the availability of active compounds and create multivalent scaffolds, potentially improving binding affinity and avidity to cellular targets. We examine the effect of aggregation on different classes of amphiphatic molecules with significant biological activities, such as immunomodulatory, anti-tumor, antiviral, and antibiotic. Our purpose is to provide a comprehensive overview of how supramolecular chemistry influences the pharmacological and biological responses of amphiphilic molecules, emphasizing the need to consider these effects in early-stage drug development and in vitro testing. By elucidating these phenomena, this review aims to offer insights into optimizing drug design and formulation to overcome challenges posed by self-aggregation.

Essential Oils of Neotropical Myrtaceae Species from 2011 until 2023: An Update.

The Myrtaceae family is renowned for its rich diversity of bioactive metabolites with broad applications across various industries. This review comprehensively explores the chemical composition and biological activities of Neotropical species within the Myrtaceae family from 2011 to 2023. A total of 170 papers were analyzed, covering 148 species from 28 genera, with notable emphasis on Eugenia, Eucalyptus, Myrcia, and Psidium. Compounds with relative abundance exceeding 10% were tabulated to highlight the most significant volatiles for each genus. Our findings were cross-referenced with previous reviews whenever feasible. Antioxidant, antibacterial, and antimicrobial activities emerged as the primary focus, collectively representing 41% of the studies, predominantly conducted in vitro. Additionally, we discuss less conventional approaches to essential oil studies in Myrtaceae species, underscoring avenues for future exploration. The investigation of essential oils from Myrtaceae holds promise for significant advancements in biotechnology, with potential benefits for the economy, environment, and human health. This review serves as a valuable resource for guiding future research strategies in this field.

Peanut (Arachis hypogaea L.) flour and oilcake flour: Exploring the influence of roasting and varietal differences on proximal composition, elemental profiling, antimicrobial and antioxidant properties.

Peanuts are highly valued for their abundance of essential nutrients and health-promoting phenolic compounds. Peanut press cake, an inexpensive and underutilized agro-industrial by-product of oil production, is typically discarded or used as animal feed. This study investigated the influence of thermal processing and varietal disparities on the nutritional composition, phenolic content, and biological properties of peanut flour and oilcake flour, aiming to enhance their value as food ingredients. The findings showed that roasting significantly increased the oil (9.98 ± 0.11-44.13 ± 0.10 %), ash (1.28 ± 0.01-5.45 ± 0.05 %), carbohydrate contents (0.90 ± 0.01-28.09 ± 0.28 %), and energy value (406.69 ± 0.09-609.13 ± 1.08 kcal/100 g), along with the total polyphenol content (28.64 ± 0.19-62.79 ± 1.18 mg GAE/g), total flavonoid content (4.20 ± 0.07-18.35 ± 0.06 mg QE/g) and antioxidant activity in both peanut flour and its oilcake. Conversely, it led to a reduction in the moisture (1.48 ± 0.09-6.25 ± 0.15 %) and protein content (49.50 ± 0.05-54.24 ± 0.01 %). Notable variations were found between the two peanut varieties in terms of these nutritional parameters. Elemental analysis unveiled significant discrepancies among peanut varieties and with roasting, with potassium (12,237.56 ± 101.36-14,513.34 ± 168.62 mg/kg) emerging as the predominant macro-element followed by phosphorus (6156.86 ± 36.19-8815.22 ± 130.70 mg/kg) and magnesium (3037.92 ± 13.87-4096.44 ± 8.54 mg/kg), while zinc (53.98 ± 0.61-81.77 ± 0.44 mg/kg) predominated among the microelements. Moreover, peanut and oilcake flours demonstrated antibacterial activity against several bacteria. It can be inferred that roasted peanut and oilcake flours offer substantial nutritional value, making them promising candidates for addressing protein-energy malnutrition and serving as valuable ingredients in developing new food products.

Lactiplantibacillus plantarum P470 Isolated from Fermented Chinese Chives Has the Potential to Improve In Vitro the Intestinal Microbiota and Biological Activity in Feces of Coronary Heart Disease (CHD) Patients.

Traditional fermented foods are known to offer cardiovascular health benefits. However, the potential of fermented Chinese chives (FCC) in reducing coronary heart disease (CHD) remains unclear. This study employed anaerobic fermentation to investigate Lactiplantibacillus plantarum (L. plantarum) P470 from FCC. The results indicated that L. plantarum P470 enhanced hydroxyl radical scavenging and exhibited anti-inflammatory effects on RAW264.7 macrophages in the fecal fermentation supernatant of CHD patients. These effects were attributed to the modulation of gut microbiota and metabolites, including short-chain fatty acids (SCFAs). Specifically, L. plantarum P470 increased the abundance of Bacteroides and Lactobacillus while decreasing Escherichia-Shigella, Enterobacter, Veillonella, Eggerthella, and Helicobacter in CHD patient fecal samples. Furthermore, L. plantarum P470 regulated the biosynthesis of unsaturated fatty acids and linoleic acid metabolism. These findings suggest that L. plantarum P470 from FCC can improve the fecal physiological status in patients with CHD by modulating intestinal microbiota, promoting SCFA production, and regulating lipid metabolism.

Biologic activity and treatment resistance to gastrointestinal cancer: the role of circular RNA in autophagy regulation.

Circular RNAs (circRNAs) lack the 5'-end methylated guanine cap structure and 3' polyadenylate tail structure, classifying it as a non-coding RNA. With the extensive investigation of circRNA, its role in regulating cell death has garnered significant attention in recent years, establishing it as a recognized participant in cancer's biological processes. Autophagy, an essential pathway in programmed cell death (PCD), involves the formation of autophagosomes using lysosomes to degrade cellular contents under the regulation of various autophagy-related (ATG) genes. Numerous studies have demonstrated that circRNA can modulate the biological activity of cancer cells by influencing the autophagy pathway, exhibiting a dualistic role in suppressing or promoting carcinogenesis. In this review, we comprehensively analyze how autophagy-related circRNA impacts the progression of gastrointestinal cancer (GIC). Additionally, we discuss drug resistance phenomena associated with autophagy regulation in GIC. This review offers valuable insights into exploring potential biological targets for prognosis and treatment strategies related to GIC.

Exploring the potential of Hermetia illucens larvae extracts: A promising approach for dermocosmetic formulations.

Globally, the yearly disposal of 1.3 billion tonnes of food raises environmental and public health concerns. Black soldier fly (BSF) larvae present a sustainable solution, converting organic waste into nutrient-rich biomass. The extracted oil from BSF larvae, rich in fatty acids (FA), offers an eco-friendly alternative for the cosmetic industry. In this study, larvae sourced from a Portuguese company were fed olive pomace, a by-product of olive oil production. The lipidic sample extracted revealed a composition high in oleic acid, valuable for cosmetics. Investigating the biological activity of lipid extractions from larvae fed with olive pomace is a novel approach. Notably, the n-hexane ultrasound-assisted extraction method demonstrated potent antioxidant properties, and some extracts displayed antimicrobial activity. Five non-cytotoxic extracts; three with no relevant activity (IC50 from 236 to >400 µg/mL). These findings highlight BSF larvae as an environmentally friendly source of fatty acids, offering promising alternatives for diverse applications.

Modification of natural compounds through biotransformation process by microorganisms and their pharmacological properties.

The biotransformation of natural compounds by fungal microorganisms is a complex biochemical process. Tandem whole-cell biotransformation offers a promising, alternative, and cost-effective method for modifying of bioactive novel compounds. This approach is particularly beneficial for structurally complex natural products that are difficult to be synthesize, through total chemical synthesis. Biotransformation also provides significant regio- and stereoselectivity, making it a valuable tool for the chemical modification of natural compounds. By utilizing microbial conversion reactions, the biological activity and structural diversity of natural products can be enhanced. In this review, we have summarize 282 novel metabolites resulting from microbial transformation by various microorganisms. We discuss the chemical structures and pharmacological properties of these novel biotransformation products. The review aims to assist scientists working in the fields of biotechnology, organic chemistry, medicinal chemistry, and pharmacology.

Microencapsulation of the Biocide Benzisothiazolinone (BIT) by Inclusion in Methyl-ß-cyclodextrin and Screening of Its Antibacterial and Ecotoxicity Properties.

The excessive use of biocides has considerable environmental and economic impacts; this is why new technologies have been sought to decrease the concentration levels applied in an effort to reduce the use of these substances. Microencapsulation using cyclodextrins has been widely used in the food and pharmaceutical industries as a way of reducing the concentrations of the active substance necessary to achieve a biological effect and/or eliminate its irritating or toxicological effects. In this study, the inclusion complexation behavior and binding ability of benzothiazolinone (BIT) with different ß-cyclodextrins (ß-CD, HP-ß-CD, and Me-ß-CD) was investigated. The intermolecular interactions were examined through UV and FTIR spectroscopy, DSC, 1D 1H NMR, and 2D ROESY. The highest stability constant was observed for the BIT/Me-ß-CD inclusion complex (299.5 ± 2.9 M-1). Antibacterial activity was investigated against Staphylococcus aureus and Escherichia coli, and the results revealed that the BIT/Me-ß-CD inclusion complex displays a higher antibacterial activity than BIT. The acute toxicity of the biocide and inclusion complex was also examined using the photobacterium Aliivibrio fischeri. Although BIT exhibited higher toxicity than the inclusion complex, further investigation is needed due to the quorum quenching effect of ß-CDs. The data found suggest that BIT microencapsulation can increase its aqueous solubility and can be used as an effective tool to improve its chemical, biological, and ecotoxicological properties.

Chemical and biological prospection of marine sponges belonging to the class Demospongiae: a review.

Marine sponges belonging to the class Demospongiae have been shown to be promising sources of bioactive compounds, investigated from the perspective of potential medical applications. This review aimed to collect studies on biological activities of clinical importance and the chemical composition of sponge species from that class, highlighting the structure/activity relationship. To carry out this work, collections were carried out in the Science Direct, Pubmed, Scielo and Google Scholar databases, using the following descriptors: antimicrobial marine sponges, antioxidant marine sponges and marine sponges biological activity. The inclusion criteria were considered: (1) publications from the year 2022 onwards; (2) written in English or Portuguesen and (3) with information on biological assays of extracts, fractions or isolated compounds. The following were excluded: (1) duplicate works; (2) works whose content was not within the scope of the study and (3) studies that did not evaluate biological activities. Results demonstrate that 274 compounds were isolated from different metabolic classes, being evaluated in several biological assays. From the analysis of the data, it is concluded that the compounds studied demonstrate promise for the development of medicines for the control of microorganisms and the treatment of tumors, acting through different mechanisms of action.

Recent Advances in Discovery, Structure, Bioactivity, and Biosynthesis of trans-AT Polyketides.

Bacterial trans-acyltransferase polyketide synthases (trans-AT PKSs) are among the most complex enzymes, which are responsible for generating a wide range of natural products, identified as trans-AT polyketides. These polyketides have received significant attention in drug development due to their structural diversity and potent bioactivities. With approximately 300 synthesized molecules discovered so far, trans-AT PKSs are found widespread in bacteria. Their biosynthesis pathways exhibit considerable genetic diversity, leading to the emergence of numerous enzymes with novel mechanisms, serving as a valuable resource for genetic engineering aimed at modifying small molecules' structures and creating new engineered enzymes. Despite the systematic discussions on trans-AT polyketides and their biosynthesis in earlier studies, the continuous advancements in tools, methods, compound identification, and biosynthetic pathways require a fresh update on accumulated knowledge. This review seeks to provide a comprehensive discussion for the 27 types of trans-AT polyketides discovered within the last seven years, detailing their sources, structures, biological activities, and biosynthetic pathways. By reviewing this new knowledge, a more profound understanding of the trans-AT polyketide family can be achieved.

Application of Difluoromethyl Isosteres in the Design of Pesticide Active Molecules.

Difluoromethyl (CF2H) groups have been found in many listed pesticides due to their unique physical and chemical properties and outstanding biological activity. In pesticide molecules, compared with the drastic changes brought by trifluoromethyl, difluoromethyl usually moderately regulates the metabolic stability, lipophilicity, bioavailability, and binding affinity of compounds. Therefore, difluoromethylation has become an effective means to modify the biological activity of pesticide molecules. This paper reviews the representative literatures and patents containing difluoromethyl groups in the past 10 years, and introduces the research progress. The aim is to provide an effective reference value for the study of difluoromethyl in pesticides.

Effect of H2O2/ascorbic acid degradation and gradient ethanol precipitation on the physicochemical properties and biological activities of pectin polysaccharides from Satsuma Mandarin.

In this work, three degraded polysaccharides (DMPP-40, DMPP-60, DMPP-80) were successfully obtained by H2O2/ascorbic acid degradation and gradient ethanol precipitation from Satsuma mandarin peel pectin (MPP), and their physicochemical properties, antioxidant and prebiotic activities were investigated. The molecular weight of MPP, DMPP-40, DMPP-60, DMPP-80 were determined to be 336.83 ±â€¯10.57, 18.93 ±â€¯0.54, 26.07 ±â€¯0.83 and 8.71 ±â€¯0.27 kDa, respectively. The ethanol concentration significantly affected the physicochemical properties of DMPPs. DMPP-60 showed the highest yield (69.07 %) and uronic acid content (64.85 %), DMPP-80 showed the lowest molecular weight (8.71 kDa), and the composition and proportion of monosaccharides of DMPPs were significantly different. Fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (1H NMR) confirmed that DMPPs exhibited similar functional groups, while X-ray diffraction (XRD) indicated that DMPP-40 possessed some crystallographic sequences. Scanning electron microscopy (SEM) images directly verified the fragmented structure and reduced surface area of DMPPs. Besides, the H2O2/ascorbic acid treatment could obviously reduce the apparent viscosity and thermal stability of MPP. Meanwhile, the results of bioactivity assay showed that DMPPs possessed better antioxidant activity and probiotics pro-proliferative effects compared with MPP. DMPP-80 could significantly inhibit lipopolysaccharides (LPS)-stimulated production of inflammatory factors (including nitric oxide (NO), interleukin (IL)-6, tumor necrosis factor (TNF)-α and interleukin (IL)-1ß) in RAW264.7 cells. Results suggest that the H2O2/ascorbic acid combined with gradient ethanol precipitation has potential applications in degradation and separation of MPP to improve its biological activities.

Sampling and analysis methods of air-borne microorganisms in hospital air: a review.

Pathogenic microorganisms can spread in the air as bioaerosols. When the human body is exposed to different bioaerosols, various infectious diseases may occur. As indoor diagnosis and treatment environments, hospitals are relatively closed and have a large flow rate of people. This indoor environment contains complex aerosol components; therefore, effective sampling and detection of microbial elements are essential in airborne pathogen monitoring. This article reviews the sampling and detection of different kinds of microorganisms in bioaerosols from indoor diagnostic and therapeutic settings, with a particular focus on microbial activity. This provides deeper insights into bioaerosols in diagnostic and therapeutic settings.

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Synthesis, crystal structure, biological and docking studies of 5-hydroxy-2-{[(2-methylpropyl)iminio]methyl}phenolate.

Background: Schiff base compounds are potential drugs.Results: A Schiff base compound prepared by condensing 2,4-dihydroxy benzaldehyde and isobutylamine was characterized for structure, thermal, physicochemical and biological properties. The keto-enol tautomerism and azomethine functionality enhances electron delocaliZation and biological activity. The compound showed good antibacterial and antifungal activity at 40 µg/ml against bacteria such as Escherichia coli and Staphylococcus aureus and fungi like Candida albicans and Candida tropicalis. The docking study exhibits a moderate binding affinity for the GyrB protein in E. coli with a binding energy of -4.26 kcal/mol.Conclusion: The compound exhibits enhanced biological activity and suppression of cell growth at concentrations as low as 30 µg/ml. The IC50 for MFC-7 was found to be 41.5 µg/ml.

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Integration of volatile and non-volatile metabolite profile, and in vitro digestion reveals the differences between different preparation methods on physico-chemical and biological properties of Gastrodia elata.

Gastrodia elata Blume (G. elata) is a traditional medicinal and edible plant whose quality is significantly influenced by post-harvest processing. To obtain an optimal post-harvest processing method for G. elata, this study employed sensory evaluation, scanning electron microscopy (SEM), gas chromatography-ion mobility spectrometry (GC-IMS), and non-targeted metabolomics, in conjunction with an in vitro digestion model, to assess the impact of different processing and drying methods on the quality of G. elata. The findings showed that the steam treatment followed by heat pump drying resulted in the highest levels of total phenols, total flavonoids, and polysaccharides in G. elata, and caused more pronounced damage to its microstructure. This treatment also maintained the highest antioxidant activities and optimal acetylcholinesterase (AChE) inhibition capacity throughout in vitro digestion, meanwhile, effectively eliminating the unpleasant odor and achieving the highest sensory scores. Furthermore, non-targeted metabolomic analysis revealed noteworthy alterations in the metabolite profile of G. elata, mainly related to purine metabolism and the biosynthesis of amino acids pathways. This study provides valuable insights into the post-harvest processing of G. elata.

Recent developments in enzymatic preparation, physicochemical properties, bioactivity, and application of resistant starch type III from staple food grains.

Resistant starch (RS) was classified into five types and referred to the starch that cannot be digested and absorbed by the small intestine of healthy human beings. Among them, RS3 has received a lot of attention from researchers because of its good functional properties and greater application prospects. Meanwhile, the enzymatic method is widely used in the preparation of RS3 because of its high efficiency and environmental protection. α-Amylase and pullulanase as the main enzymes can effectively improve the yield of RS3. The physical properties of RS3 have an excellent potential for application in improving food crispness, texture and producing low glycemic index (GI) foods. It is more valuable because it has biological activities such as inducing apoptosis in tumor cells, lowering intestinal pH, and regulating blood glucose, etc. This paper summarized the current research progress of RS3 from different staple food grains, including current applications of enzymes commonly used in the preparation of RS3, physical properties and biological activities of RS3, and the application of RS3 in different areas to provide a theoretical basis for future research on RS3 as well as further development and applications based on the market requirement.

Yeast polysaccharides: The environmentally friendly polysaccharides with broad application potentials.

Yeast cell wall (YCW) polysaccharides, including ß-glucans, mannans, chitins, and glycogens, can be extracted from the waste of beer industry. They are environmentally friendly, abundant, inexpensive raw materials, and have shown broad biological activities and application potentials. The exploitation of yeast polysaccharides is of great importance for environmental protection and resource utilization. This paper reviews the structural features and preparation of YCW polysaccharides. The solubility and emulsification of yeast polysaccharides and the properties of binding metal ions are presented. In addition, biological activities such as blood glucose and lipid lowering, immune regulation, antioxidant, promotion of intestinal health, and promotion of wound healing are proposed, highlighting the beneficial effects of yeast polysaccharides on human health. Through modification, the physical and chemical properties of yeast polysaccharides are changed, which emphasizes the promotion of their biological activities and properties. In addition, the food applications of yeast polysaccharides, including the food packaging film, emulsifier, thickening agent, and fat alternatives, are focused and discussed.

Synthesis, light-controlled antibacterial and anti-tumor activities of Ginkgo biloba leaves polyprenols-based polypyridine metal complexes.

In this study, Ginkgo biloba leave polyprenols (GBP) and polypyridine metal complex were individually utilized as functional ligand and main ligand, four kinds of novel GBP-based polypyridine metal complexes were successfully synthesized and their cell absorption capacity, light-dark stability, photodissociation efficiency, ROS production capacity, light-controlled antibacterial and anti-tumor activities as well as mechanisms were systematically investigated by ultraviolet visible spectrophotometer (UV-vis), confocal laser scanning microscope (CLSM), gel electrophoresis (GE), scanning electron microscope (SEM), oxford cup method, MTT method etc. The lipid water distribution coefficients of complex 1, 2 and 4 were all within the range of 0∼3, demonstrating their better cell absorption capacity and more competitive bioavailability potentiality compared with GBP. All of the synthesized complexes possessed excellent stability in a dark environment, and could conduct ligand dissociation under the condition of visible light irradiation except complex 1. In which, complex 2 and complex 4 were able to achieve degradation rates of 37.9 % and 54.4 % within 5 min, separately. In addition, complex 2 and complex 4 exhibited superior inhibitory activities on the HN-3 tumor cells on account of their stronger ROS production capacity. Moreover, the constricted expression of BCL-2 and NF-kB p-p65, especially the promoted expression of BAX may be one of the root cause. The four synthesized complexes had preferable inhibition effects against S. aureus under the condition of visible light irradiation in contrast to darkness, in which complex 4 was the best and its MIC and MBC values were 6.25 and 12.5 µg/mL, respectively. The antibacterial mechanism of the complex 4 may be in relation to the synergistic effect of multiple factors, including leakage of bacterial inclusion, change of cell membrane permeability and disruption of cell wall etc. All of the above generalized researches will pave a way for the high-value development and application of GBP-based functional products.

New solvated Mo(VI) complexes of isatin based asymmetric bisthiocarbohydrazones as potent bioactive agent: synthesis, DFT-molecular docking studies, biological activity evaluation and crystal structures.

New solvated Mo(VI) complexes were isolated from the reaction of [MoO2(acac)2] with asymmetric isatin bisthiocarbohydrazone ligands. The ligands were obtained from the reaction of isatin monothiocarbohydrazone with 3,5-dibromo salicylaldehyde (L1), 3,5-dichloro salicylaldehyde (L2) and 3-chloro-5-bromo salicylaldehyde (L3), respectively. In the complexes, the ligands serve as ONS donors and coordinate to the [MoO2]2+ nucleus. The bonding sites are azomethine nitrogen atom, phenolic oxygen atom and thiol sulfur atom. The sixth coordination site is completed by an oxygen atom from an ethanol solvent. The ethanol-coordinated Mo(VI) complexes, C1-C3, [MoO2L(EtOH)] (L: L1-L3), were characterized using elemental analysis, IR and 1H NMR spectroscopies, and conductivity measurements. By crystallizing ethanol-solvated solid complexes from an EtOH/DMSO mixture, DMSO-solvated complexes (C4-C6) suitable for X-ray crystallography were obtained. Crystal structure analysis supports the proposed complex structures and geometries, but the ethanol in the sixth coordination site has been replaced by DMSO. When the anticarcinogenic effects of the ligands and complexes (C1-C3) on the C6 cell line were examined, it was found that the complexes showed higher activity than the ligands. The C3 complex appears to have the best anti-cancer activity compared to doxorubicin. Additionally, all compounds were determined to have high total antioxidant capacity. Data obtained from theoretical studies (DFT and docking) support experimental studies.