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"Bioactive compounds."
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A Novel Drug Combination of Mangiferin and Cinnamic Acid Alleviates Rheumatoid Arthritis by Inhibiting TLR4/NFκB/NLRP3 Activation-Induced Pyroptosis
Growing evidence shows that Baihu-Guizhi decoction (BHGZD), a traditional Chinese medicine (TCM)-originated disease-modifying anti-rheumatic prescription, may exert a satisfying clinical efficacy for rheumatoid arthritis (RA) therapy. In our previous studies, we verified its immunomodulatory and anti-inflammatory activities. However, bioactive compounds (BACs) of BHGZD and the underlying mechanisms remain unclear. Herein, an integrative research strategy combining UFLC-Q-TOF-MS/MS, gene expression profiling, network calculation, pharmacokinetic profiling, surface plasmon resonance, microscale thermophoresis, and pharmacological experiments was carried out to identify the putative targets of BHGZD and underlying BACs. After that, both in vitro and in vivo experiments were performed to determine the drug effects and pharmacological mechanisms. As a result, the calculation and functional modularization based on the interaction network of the “RA-related gene–BHGZD effective gene” screened the TLR4/PI3K/AKT/NFκB/NLRP3 signaling-mediated pyroptosis to be one of the candidate effective targets of BHGZD for reversing the imbalance network of “immune-inflammation” during RA progression. In addition, both mangiferin (MG) and cinnamic acid (CA) were identified as representative BACs acting on that target, for the strong binding affinities between compounds and target proteins, good pharmacokinetic features, and similar pharmacological effects to BHGZD. Notably, both BHGZD and the two-BAC combination of MG and CA effectively alleviated the disease severity of the adjuvant-induced arthritis-modified rat model, including elevating pain thresholds, relieving joint inflammation and bone erosion via inhibiting NF-κB via TLR4/PI3K/AKT signaling to suppress the activation of the NLRP3 inflammasome, leading to the downregulation of downstream caspase-1, the reduced release of IL-1β and IL-18, and the modulation of GSDMD-mediated pyroptosis. Consistent data were obtained based on the in vitro pyroptosis cellular models of RAW264.7 and MH7A cells induced by LPS/ATP. In conclusion, these findings offer an evidence that the MG and CA combination identified from BHGZD may interact with TLR4/PI3K/AKT/NFκB signaling to inhibit NLRP3 inflammasome activation and modulate pyroptosis, which provides the novel representative BACs and pharmacological mechanisms of BHGZD against active RA. Our data may shed new light on the mechanisms of the TCM formulas and promote the modernization development of TCM and drug discovery.
Journal Article
Plant associated fungal endophytes as a source of natural bioactive compounds
Endophytes are a potent source of bioactive compounds that mimic plant-based metabolites. The relationship of host plant and endophyte is significantly associated with alteration in fungal colonisation and the extraction of endophyte-derived bioactive compounds. Screening of fungal endophytes and their relationship with host plants is essential for the isolation of bioactive compounds. Numerous bioactive compounds with antioxidant, antimicrobial, anticancer, and immunomodulatory properties are known to be derived from fungal endophytes. Bioinformatics tools along with the latest techniques such as metabolomics, next-generation sequencing, and metagenomics multilocus sequence typing can potentially fill the gaps in fungal endophyte research. The current review article focuses on bioactive compounds derived from plant-associated fungal endophytes and their pharmacological importance. We conclude with the challenges and opportunities in the research area of fungal endophytes.
Journal Article
Drought stress enhances nutritional and bioactive compounds, phenolic acids and antioxidant capacity of Amaranthus leafy vegetable
Background
Bioactive compounds, vitamins, phenolic acids, flavonoids of
A. tricolor
are the sources of natural antioxidant that had a great importance for the food industry as these detoxify ROS in the human body. These natural antioxidants protect human from many diseases such as cancer, arthritis, emphysema, retinopathy, neuro-degenerative cardiovascular diseases, atherosclerosis and cataracts. Moreover, previous literature has shown that drought stress elevated bioactive compounds, vitamins, phenolics, flavonoids and antioxidant activity in many leafy vegetables. Hence, we study the nutritional and bioactive compounds, phenolic acids, flavonoids and antioxidant capacity of amaranth under drought stress for evaluation of the significant contribution of these compounds in the human diet.
Results
The genotype VA3 was assessed at four drought stress levels that significantly affected nutritional and bioactive compounds, phenolic acids, flavonoids and antioxidant capacity. Protein, ash, energy, dietary fiber, Ca, K, Cu, S, Mg, Mn, Mo, Na, B content, total carotenoids, TFC, vitamin C, TPC, TAC (DPPH), betacarotene, TAC (ABTS
+
), sixteen phenolic acids and flavonoids were remarkably increased with the severity of drought stress. At moderate and severe drought stress conditions, the increments of all these components were more preponderant.
Trans
-cinnamic acid was newly identified phenolic acid in
A. tricolor
. Salicylic acid, vanilic acid, gallic acid, chlorogenic acid,
Trans
-cinnamic acid, rutin, isoquercetin,
m
-coumaric acid and
p
-hydroxybenzoic acid were the most abundant phenolic compounds in this genotype.
Conclusions
In
A. tricolor,
drought stress enhanced the quantitative and qualitative improvement of nutritional and bioactive compounds, phenolic acids, flavonoids and antioxidants. Hence, farmers of semi-arid and dry areas of the world could be able to grow amaranth as a substitute crop.
Journal Article
Bioactive Compounds in Anti-Diabetic Plants: From Herbal Medicine to Modern Drug Discovery
Natural products, including organisms (plants, animals, or microorganisms) have been shown to possess health benefits for animals and humans. According to the estimation of the World Health Organization, in developing countries, 80% of the population has still depended on traditional medicines or folk medicines which are mostly prepared from the plant for prevention or treatment diseases. Traditional medicine from plant extracts has proved to be more affordable, clinically effective and relatively less adverse effects than modern drugs. Literature shows that the attention on the application of phytochemical constituents of medicinal plants in the pharmaceutical industry has increased significantly. Plant-derived secondary metabolites are small molecules or macromolecules biosynthesized in plants including steroids, alkaloids, phenolic, lignans, carbohydrates and glycosides, etc. that possess a diversity of biological properties beneficial to humans, such as their antiallergic, anticancer, antimicrobial, anti-inflammatory, antidiabetic and antioxidant activities Diabetes mellitus is a chronic disease result of metabolic disorders in pancreas β-cells that have hyperglycemia. Hyperglycemia can be caused by a deficiency of insulin production by pancreatic (Type 1 diabetes mellitus) or insufficiency of insulin production in the face of insulin resistance (Type 2 diabetes mellitus). The current medications of diabetes mellitus focus on controlling and lowering blood glucose levels in the vessel to a normal level. However, most modern drugs have many side effects causing some serious medical problems during a period of treating. Therefore, traditional medicines have been used for a long time and play an important role as alternative medicines. Moreover, during the past few years, some of the new bioactive drugs isolated from plants showed antidiabetic activity with more efficacy than oral hypoglycemic agents used in clinical therapy. Traditional medicine performed a good clinical practice and is showing a bright future in the therapy of diabetes mellitus. World Health Organization has pointed out this prevention of diabetes and its complications is not only a major challenge for the future, but essential if health for all is to be attained. Therefore, this paper briefly reviews active compounds, and pharmacological effects of some popular plants which have been widely used in diabetic treatment. Morphological data from V-herb database of each species was also included for plant identification.
Journal Article
Distillery Stillage: Characteristics, Treatment, and Valorization
Distilleries are among the most polluting industries because ethanol fermentation results in the discharge of large quantities of high-strength liquid effluents with high concentrations of organic matter and nitrogen compounds, low pH, high temperature, dark brown color, and high salinity. The most common method of managing this wastewater (distillery stillage) is to use it for soil conditioning, but this requires thickening the wastewater and may cause soil pollution due to its high nitrogen content. Therefore, treatment of distillery stillage is preferable. This review discusses individual biological and physico-chemical treatment methods and combined technologies. In addition, special attention is paid to valorization of distillery stillage, which is a valuable source of polysaccharides and volatile fatty acids (VFAs), as well as natural antioxidants, including polyphenols and other bioactive compounds of interest to the pharmaceutical, cosmetic, and food industries. New directions in improvement of valorization technologies are highlighted, including the search for new eutectic solvents for extracting these compounds. Such technologies are essential for sustainable development, which requires the use of management and valorization strategies for recovery of valuable compounds with minimal disposal of waste streams.
Journal Article
Valorization of Food Waste to Produce Value-Added Products Based on Its Bioactive Compounds
The rapid growth of the global population and changes in lifestyle have led to a significant increase in food waste from various industrial, agricultural, and household sources. Nearly one-third of the food produced annually is wasted, resulting in severe resource depletion. Food waste contains rich organic matter, which, if not managed properly, can pose a serious threat to the environment and human health, making the proper disposal of food waste an urgent global issue. However, various types of food waste, such as waste from fruit, vegetables, grains, and other food production and processing, contain important bioactive compounds, such as polyphenols, dietary fiber, proteins, lipids, vitamins, organic acids, and minerals, some of which are found in greater quantities in the discarded parts than in the parts accepted by the market. These bioactive compounds offer the potential to convert food waste into value-added products, and fields including nutritional foods, bioplastics, bioenergy, biosurfactants, biofertilizers, and single cell proteins have welcomed food waste as a novel source. This review reveals the latest insights into the various sources of food waste and the potential of utilizing bioactive compounds to convert it into value-added products, thus enhancing people’s confidence in better utilizing and managing food waste.
Journal Article
High-Pressure Homogenization: Principles and Applications Beyond Microbial Inactivation
(Ultra) high-pressure homogenization ((U)HPH) is one of the emerging technologies being studied and developed for various applications in the food industry. (U)HPH was suggested as an effective tool for achieving microbial safety and extending the product shelf life of liquid foods in a continuous process while minimizing some negative attributes of thermal processing. The valve geometry, pressure level, inlet temperature, and the number of homogenization cycles are all factors affecting the level of microbial inactivation and the extent of the techno-functionalities of food biopolymers and matrices. Turbulence, high shear, cavitation, and temperature increase induced by (U)HPH treatments enhance emulsion stability, stabilize proteins in solutions, reduce particle size distributions, and increase the accessibility of health-promoting compounds. This review is a comprehensive and updated overview of the engineering aspects of the (U)HPH process, specifically focusing on (U)HPH modification of food components such as polysaccharides, proteins, and bioactive compounds. A detailed description of the potential applications in food products beyond microbial inactivation is also included.
Journal Article
A Comprehensive Review of Bioactive Compounds from Lactic Acid Bacteria: Potential Functions as Functional Food in Dietetics and the Food Industry
Lactic acid bacteria (LAB) are beneficial microbes known for their health-promoting properties. LAB are well known for their ability to produce substantial amounts of bioactive compounds during fermentation. Peptides, exopolysaccharides (EPS), bacteriocins, some amylase, protease, lipase enzymes, and lactic acid are the most important bioactive compounds generated by LAB activity during fermentation. Additionally, the product produced by LAB is dependent on the type of fermentation used. LAB derived from the genera Lactobacillus and Enterococcus are the most popular probiotics at present. Consuming fermented foods has been previously connected to a number of health-promoting benefits such as antibacterial activity and immune system modulation. Furthermore, functional food implementations lead to the application of LAB in therapeutic nutrition such as prebiotic, immunomodulatory, antioxidant, anti-tumor, blood glucose lowering actions. Understanding the characteristics of LAB in diverse sources and its potential as a functional food is crucial for therapeutic applications. This review presents an overview of functional food knowledge regarding interactions between LAB isolated from dairy products (dairy LAB) and fermented foods, as well as the prospect of functioning LAB in human health. Finally, the health advantages of LAB bioactive compounds are emphasized.
Journal Article
Impact of drying temperature on the physicochemical and functional properties of butterfly pea flower powder
Butterfly pea flower (BPF) powder, which is rich in bioactive compounds, was evaluated for the impact of various drying methods on its solubility, physical properties, and chemical composition. Four drying methods were used: thermal drying at 50 °C, 60 °C, 70 °C, and natural sun drying. The powders were assessed for solubility time, hygroscopicity, density, flowability, and chemical stability using scanning electron microscopy (SEM), X-ray diffraction (XRD), and Fourier transform infrared (FTIR). Solubility times ranged from 148 to 162 s, with no significant differences. The 70 °C dried sample (Sample C) had the fastest dissolution rate and highest hygroscopicity. Total phenolic and anthocyanin contents increased with temperature, peaking in sun-dried samples (Sample D). Density measurements showed Sample C had the highest bulk density and optimal flowability, while Sample D had superior water holding capacity. The SEM analysis revealed morphological differences, with Sample A showing a smooth surface and Sample C exhibiting significant particle disintegration. The XRD analysis showed that Sample C had the highest crystallinity. The FTIR analysis confirmed the stability of key functional groups, with sun-dried samples retaining phenolic compounds. These findings suggest drying methods can optimize BPF powder’s properties, enhancing its bioactivity for health applications.
Journal Article