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Keywords = anti-lipase activity

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23 pages, 8387 KiB  
Article
Solvent Fractionation of Polygonum cuspidatum Sieb. et Zucc. for Antioxidant, Biological Activity, and Chromatographic Characterization
by Yuchen Cheng, Yuri Kang and Woonjung Kim
Int. J. Mol. Sci. 2025, 26(14), 7011; https://doi.org/10.3390/ijms26147011 - 21 Jul 2025
Viewed by 330
Abstract
This study investigated the natural bioactive compounds in Polygonum cuspidatum Sieb. et Zucc. (P. cuspidatum) by fractionating a 70% ethanol extract using n-hexane, chloroform, ethyl acetate, n-butanol, and water. The total polyphenol and flavonoid contents of each fraction were [...] Read more.
This study investigated the natural bioactive compounds in Polygonum cuspidatum Sieb. et Zucc. (P. cuspidatum) by fractionating a 70% ethanol extract using n-hexane, chloroform, ethyl acetate, n-butanol, and water. The total polyphenol and flavonoid contents of each fraction were determined, and their antioxidant activities were evaluated using DPPH, ABTS, and FRAP assays. Additionally, the anti-diabetic potential was assessed via α-glucosidase inhibitory activity, while anti-obesity activity was evaluated using lipase inhibitory activity. The fractions were also tested for tyrosinase and elastase inhibitory activities to assess their skin-whitening and anti-wrinkle potential, and their antibacterial activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa was determined using the agar diffusion method. Finally, bioactive compounds were identified and quantified using HPLC and GC–MSD. The results showed that the ethyl acetate fraction possessed the highest total polyphenol content (0.53 ± 0.01 g GAE/g) and total flavonoid content (0.19 ± 0.02 g QE/g). It also exhibited strong antioxidant activity, with the lowest DPPH radical scavenging IC50 (0.01 ± 0.00 mg/mL), ABTS radical scavenging IC50 (0.06 ± 0.00 mg/mL), and the highest FRAP value (6.02 ± 0.30 mM Fe2+/mg). Moreover, it demonstrated potent enzyme inhibitory activities, including tyrosinase inhibitory activity (67.78 ± 2.50%), elastase inhibitory activity (83.84 ± 1.64%), α-glucosidase inhibitory activity (65.14 ± 10.29%), and lipase inhibitory activity (85.79 ± 1.04%). In the antibacterial activity, the ethyl acetate fraction produced a clear inhibitory zone of 19.50 mm against Staphylococcus aureus, indicating notable antibacterial activity. HPLC-PDA and GC–MSD analyses identified tannic acid and emodin as the major bioactive constituents. These findings suggest that the ethyl acetate fraction of P. cuspidatum extract, rich in polyphenol and flavonoid compounds, is a promising natural source of bioactive ingredients for applications in the food, pharmaceutical, and cosmetic industries. Further research is needed to explore its mechanisms and therapeutic applications. Full article
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18 pages, 1769 KiB  
Article
Antioxidant and Pancreatic Lipase Inhibitory Activities of Panax japonicus (T. Nees) C.A. Meyer
by Jinfeng Yang, Wenxuan Jiang, Ju Hee Park, Eun Soo Seong, Yong Soo Kwon and Myong Jo Kim
Plants 2025, 14(13), 2003; https://doi.org/10.3390/plants14132003 - 30 Jun 2025
Viewed by 316
Abstract
Obesity and its associated complications, including oxidative stress, pose significant global health challenges. Natural products offer a promising avenue for developing novel therapeutic strategies. In this study, we investigated the potential of Panax japonicus (T. Nees) C.A. Meyer, a traditional medicinal plant known [...] Read more.
Obesity and its associated complications, including oxidative stress, pose significant global health challenges. Natural products offer a promising avenue for developing novel therapeutic strategies. In this study, we investigated the potential of Panax japonicus (T. Nees) C.A. Meyer, a traditional medicinal plant known for its antioxidant and anti-obesity properties. A methanol extract of Panax japonicus and its fractions were evaluated for their in vitro antioxidant activities (tested using DPPH and reducing power assays), pancreatic lipase (PL) inhibitory capacities, and underlying mechanisms of action. The results indicated that the ethyl acetate fraction of P. japonicus (PJEA) exhibited the greatest potency, demonstrating strong antioxidant activity and significantly inhibiting digestive enzyme activity (pancreatic lipase). Mechanistic studies revealed that the PL inhibition was of a mixed type, combining both competitive and non-competitive mechanisms. Furthermore, PJEA demonstrated the ability to inhibit the differentiation of preadipocytes, primarily exerting its anti-adipogenic effects by downregulating the mRNA expression of PPARγ and the gene expression of C/EBPα. In addition, the extract suppressed the gene expression of FAS and ACC in adipose tissue. Isolation of the bioactive compounds from PJEA identified kaempferol 3-O-α-L-rhamnoside and catechin, which potentially contribute to the observed anti-obesity effects. Overall, this study highlights P. japonicus as a promising natural ingredient for scavenging free radicals and managing obesity, suggesting its potential for development into functional foods or therapeutic agents. Full article
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21 pages, 3940 KiB  
Article
Therapeutic Potential of Plantago ovata Bioactive Extracts Obtained by Supercritical Fluid Extraction as Influenced by Temperature on Anti-Obesity, Anticancer, and Antimicrobial Activities
by Husam Qanash, Abdulrahman S. Bazaid, Naif K. Binsaleh, Amirah S. Alshammari and Reem Eltayeb
Plants 2025, 14(12), 1813; https://doi.org/10.3390/plants14121813 - 12 Jun 2025
Viewed by 1749
Abstract
Plantago ovata has been utilized as an effective natural remedy with minimal side effects, offering a promising alternative to synthetic pharmaceuticals. The supercritical fluid extraction (SFE) of Plantago ovata leaves yielded 0.417 g and 0.532 g at 40 °C and 80 °C, respectively. [...] Read more.
Plantago ovata has been utilized as an effective natural remedy with minimal side effects, offering a promising alternative to synthetic pharmaceuticals. The supercritical fluid extraction (SFE) of Plantago ovata leaves yielded 0.417 g and 0.532 g at 40 °C and 80 °C, respectively. The 40 °C extract exhibited stronger antimicrobial activity, with minimum inhibitory concentrations (MICs) as low as 15.62 µg/mL and minimum bactericidal concentrations (MBCs) as low as 31.25 µg/mL against Bacillus subtilis and Candida albicans. In contrast, the 80 °C extract demonstrated reduced activity, with MICs and MBCs up to 250 and 500 µg/mL, respectively. The 40 °C extract also showed superior lipase inhibition (IC50 = 17.21 µg/mL) compared to the 80 °C extract (IC50 = 26.42 µg/mL), although orlistat remained the most potent (IC50 = 6.02 µg/mL). In addition, cytotoxicity assays revealed stronger effects of the 40 °C extract on Caco-2 colon cancer cells (IC50 = 109.47 µg/mL) compared to the 80 °C extract (IC50 = 174.81 µg/mL). These results suggest that the lower-temperature SFE of P. ovata yields extracts with enhanced antimicrobial, anti-obesity, and anticancer activities, supporting its potential for pharmaceutical and nutraceutical applications. Full article
(This article belongs to the Special Issue Biological Activities of Plant Extracts, 2nd Edition)
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19 pages, 11778 KiB  
Article
Lipid-Lowering Potential of Almond Hulls (Quercetin, Baicalein, and Kaempferol): Insights from Network Pharmacology and Molecular Dynamics
by Qiming Miao, Lu Sun, Jiayuan Wu, Xinyue Zhu, Juer Liu, Roger Ruan, Guangwei Huang, Shengquan Mi and Yanling Cheng
Curr. Issues Mol. Biol. 2025, 47(6), 450; https://doi.org/10.3390/cimb47060450 - 12 Jun 2025
Viewed by 684
Abstract
The advancement of modern lifestyles has precipitated excessive consumption of energy-dense foods, driving the escalating global burden of lipid metabolism dysregulation-related pathologies—including obesity, type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and cardiovascular disorders—which collectively pose a formidable challenge to global [...] Read more.
The advancement of modern lifestyles has precipitated excessive consumption of energy-dense foods, driving the escalating global burden of lipid metabolism dysregulation-related pathologies—including obesity, type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and cardiovascular disorders—which collectively pose a formidable challenge to global public health systems. The almond hull, as a by-product of almond processing, is rich in polyphenolic compounds with demonstrated antioxidant, anti-inflammatory, and lipid-lowering potential, though its precise hypo-lipidemic mechanisms remain elusive. In this study, polyphenols were extracted from almond hulls using 50% ethanol with ultrasound-assisted extraction, followed by preliminary purification via solvent partitioning. The ethyl acetate fraction was analyzed by liquid chromatography–mass spectrometry (LC-MS). Network pharmacology and molecular docking were employed to investigate the interactions between key bioactive constituents (e.g., quercetin, baicalein, and kaempferol) and targets in lipid metabolism-related pathways. Molecular dynamics (MD) simulations further evaluated the stability of the lowest-energy complexes. Results revealed that the ethyl acetate fraction exhibited potent pancreatic lipase inhibitory activity (IC50 = 204.2 µg/mL). At 0.1 mg/mL after 24 h treatment, it significantly reduced free fatty acids (FFAs)-induced intracellular triglyceride accumulation (p < 0.01) and enhanced cellular antioxidant capacity. Network pharmacology and in vitro studies suggest almond hull extract modulates PI3K-AKT signaling and improves insulin resistance, demonstrating lipid-lowering effects. These findings support its potential in functional foods and pharmaceuticals, though further in vivo validation and mechanistic investigations are required. Full article
(This article belongs to the Section Molecular Pharmacology)
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14 pages, 1113 KiB  
Article
Effects of Dietary Sodium Butyrate on Growth Performance, Digestive Ability, Blood Biochemistry, and Ammonia Tolerance of Largemouth Bass (Micropterus salmoides)
by Xuan Chen, Wu Chen, Yanjie Tang, Muzi Zhang and Ming Li
Fishes 2025, 10(6), 259; https://doi.org/10.3390/fishes10060259 - 2 Jun 2025
Viewed by 472
Abstract
The aim of this study was to investigate the effects of sodium butyrate (SB) on growth performance, digestive ability, blood health, and ammonia tolerance of largemouth bass. During the experiment, largemouth bass were fed different diets (0.00%, 0.50% and 1.00% SB) followed by [...] Read more.
The aim of this study was to investigate the effects of sodium butyrate (SB) on growth performance, digestive ability, blood health, and ammonia tolerance of largemouth bass. During the experiment, largemouth bass were fed different diets (0.00%, 0.50% and 1.00% SB) followed by a 96-h ammonia challenge. In this study, dietary supplementation of SB can improve the growth (weight gain rate increased; GH and IGF 1 genes up-regulated) of largemouth bass. The addition of SB also significantly increased serum total protein, albumin and globulin contents and reduced triglycerides, cholesterol and aspartate transaminase contents. The digestive ability (pepsin, lipase, amylase, alkaline phosphatase, creatine kinase, gamma-glutamyltranspeptidase, sodium-potassium adenosine triphosphatase, villus height and muscular thickness increased) was significantly higher in the 0.50% and 1.00% SB groups. SB also improved the anti-inflammatory capacity (IL 1 and IL 8 genes down-regulated) of largemouth bass. The addition of SB to feed significantly reduced the cumulative mortality rate after 96 h of ammonia stress. SB significantly increased liver ammonia metabolism enzyme (arginase, argininosuccinate synthetase, ornithine transcarboxylase and argininosuccinate lyase) and inducible nitric oxide synthase activity, and significantly decreased the neuronal nitric oxide synthase activity. The results indicate that dietary supplementation of SB can promote growth and improve digestive ability, blood health, and ammonia tolerance in largemouth bass. Full article
(This article belongs to the Special Issue Fish Nutrition and Immunology)
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22 pages, 517 KiB  
Article
Erica spiculifolia Salisb. (Balkan Heath): A Focus on Metabolic Profiling and Antioxidant and Enzyme Inhibitory Properties
by Reneta Gevrenova, Anna Szakiel, Cezary Pączkowski, Gokhan Zengin, Inci Kurt-Celep, Alexandra Stefanova and Dimitrina Zheleva-Dimitrova
Plants 2025, 14(11), 1648; https://doi.org/10.3390/plants14111648 - 28 May 2025
Viewed by 552
Abstract
Erica spiculifolia Salisb. (formerly Bruckenthalia spiculifolia Benth.) (Balkan heath) is renowned for its traditional usage as a diuretic, anti-inflammatory and antioxidant agent. For the first time, acylquinic acids, flavonoids and numerous proanthocyanidin oligomers were annotated/dereplicated by liquid chromatography–high-resolution mass spectrometry in methanol–aqueous extracts [...] Read more.
Erica spiculifolia Salisb. (formerly Bruckenthalia spiculifolia Benth.) (Balkan heath) is renowned for its traditional usage as a diuretic, anti-inflammatory and antioxidant agent. For the first time, acylquinic acids, flavonoids and numerous proanthocyanidin oligomers were annotated/dereplicated by liquid chromatography–high-resolution mass spectrometry in methanol–aqueous extracts from E. spiculifolia aerial parts harvested at the early and full flowering stage. Chlorogenic acid and proanthocyanidin tetra- and trimer A, B-type together with quercitrin and (+) catechin were the predominant compounds in the semi-quantitative analysis. Neutral triterpenoids, triterpenoid acids and phytosterols were determined in apolar extracts by gas chromatography–mass spectrometry. Triterpenoid acids accounted for 80% of the total triterpenoid content, dominated by ursolic and oleanolic acid, reaching up to 32.2 and 6.1 mg/g dw, respectively. Ursa/olean-2,12-dien-28-oic acids and 3-keto-derivatives together with α-amyrin acetate as a chemotaxonomic marker, α-amyrenone, α- and β-amyrin were evaluated. Total phenolic and flavonoid contents were 83.85 ± 0.89 mg gallic acid equivalents/g and 78.91 ± 0.41 mg rutin equivalents/g, respectively. The extract actively scavenged DPPH and ABTS radicals (540.01 and 639.11 mg Trolox equivalents (TE)/g), possessed high potential to reduce copper and iron ions (660.32 and 869.22 mg TE/g, respectively), and demonstrated high metal chelating capacity (15.57 Ethylenediaminetetraacetic acid equivalents/g). It exhibited prominent anti-lipase (18.32 mg orlistat equivalents/g) and anti-tyrosinase (71.90 mg kojic acid equivalents/g) activity. The extract inhibited α-glucoside (1.35 mmol acarbose equivalents/g) and acetylcholinesterase (2.56 mg galanthamin equivalents/g), and had moderate effects on α-amylase, elastase, collagenase and hyaluronidase. Balkan heath could be recommended for raw material production with antioxidant and enzyme inhibitory properties. Full article
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18 pages, 598 KiB  
Review
Research Progress of Nattokinase in Reducing Blood Lipid
by Chuyang Wei, Ruitao Cai, Yingte Song, Xiaoyong Liu and Hui-Lian Xu
Nutrients 2025, 17(11), 1784; https://doi.org/10.3390/nu17111784 - 24 May 2025
Viewed by 3815
Abstract
The purpose of this paper is to comprehensively review the research progress of nattokinase in lowering blood lipid, including its source, structure and physicochemical properties, mechanisms of functions, clinical research status, and safety considerations, so as to provide reference for further research on [...] Read more.
The purpose of this paper is to comprehensively review the research progress of nattokinase in lowering blood lipid, including its source, structure and physicochemical properties, mechanisms of functions, clinical research status, and safety considerations, so as to provide reference for further research on the application of nattokinase in the treatment of dyslipidemia. Natto is a traditional Japanese fermented food, which is made from soybeans fermented by Bacillus natto. During the fermentation process, natto will produce a variety of biologically active substances, including nattokinase. Nattokinase (NK) is a serine protease with stable enzyme activity and good freeze–thaw tolerance, which exerts lipid-lowering and anti-atherosclerotic effects by activating hormone-sensitive lipase (HSL), inhibiting hydroxymethylglutaryl monoacyl coenzyme A reductase (HMG-CoA reductase), and enhancing lipoprotein lipase (LPL) activity. Large-scale clinical trials have confirmed that nattokinase significantly improves the lipid profile and reduces the atherosclerotic plaque area and intima-media thickness with a favorable safety profile. Compared with traditional lipid-lowering drugs (e.g., statins and fibrates), nattokinase has a multifaceted lipid-lowering mechanism and lower risk of side effects, which makes it suitable for patients intolerant of traditional drugs; when combined with natural products such as statins, fibrates, red yeast, and lifestyle interventions, it can play a synergistic role and further reduce the risk of cardiovascular disease. There are various types of nattokinase preparations on the market, and consumers should choose regular products with high activity and purity, and pay attention to their safety and applicable population. Full article
(This article belongs to the Section Lipids)
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33 pages, 16266 KiB  
Article
Integrated Bioinformatics Analysis and Cellular Experimental Validation Identify Lipoprotein Lipase Gene as a Novel Biomarker for Tumorigenesis and Prognosis in Lung Adenocarcinoma
by Wanwan He, Meilian Wei, Yan Huang, Junsen Qin, Meng Liu, Na Liu, Yanli He, Chuanbing Chen, Yali Huang, Heng Yin and Ren Zhang
Biology 2025, 14(5), 566; https://doi.org/10.3390/biology14050566 - 19 May 2025
Viewed by 761
Abstract
Lung adenocarcinoma (LUAD) is one of the leading causes of death worldwide, and thus, more biomarker and therapeutic targets need to be explored. Herein, we aimed to explore new biomarkers of LUAD by integrating bioinformatics analysis with cell experiments. We firstly identified 266 [...] Read more.
Lung adenocarcinoma (LUAD) is one of the leading causes of death worldwide, and thus, more biomarker and therapeutic targets need to be explored. Herein, we aimed to explore new biomarkers of LUAD by integrating bioinformatics analysis with cell experiments. We firstly identified 266 druggable genes that were significantly differentially expressed between LUAD tissues and adjacent normal lung tissues. Among these genes, SMR analysis with p-value correction suggested that declining lipoprotein lipase (LPL) levels may be causally associated with an elevated risk of LUAD, which was corroborated by co-localization analysis. Analyses of clinical data showed that LPL in lung cancer tissues has considerable diagnostic value for LUAD, and elevated LPL levels were positively associated with improved patient survival outcomes. Cell experiments with an LPL activator proved these findings; the activator inhibited the proliferation and migration of lung cancer cells. Next, we found that LPL promoted the infiltration of immune cells such as DCs, IDCs, and macrophages in LUAD by mononuclear sequencing analysis and TIMER2.0. Meanwhile, patients with low levels of LPL expression demonstrated superior immunotherapeutic responses to anti-PD-1 therapy. We conclude that LPL acts as a diagnostic and prognostic marker for LUAD. Full article
(This article belongs to the Special Issue Disease Biomarker Discovery and Validation)
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19 pages, 783 KiB  
Article
Physicochemical Composition and Bioactive Properties of Uruguayan Bee Pollen from Different Botanical Sources
by Adriana Gámbaro, Marcelo Miraballes, Nahir Urruzola, Maximiliano Kniazev, Cecilia Dauber, Melissa Romero, Adriana Maite Fernández-Fernández, Alejandra Medrano, Estela Santos and Ignacio Vieitez
Foods 2025, 14(10), 1689; https://doi.org/10.3390/foods14101689 - 10 May 2025
Viewed by 597
Abstract
Bee pollen is widely recognized for its health benefits, with its nutritional and bioactive properties varying by botanical origin. This study analyzed twelve bee pollen samples collected from six different apiaries in Uruguay during two seasons (spring and autumn) to determine their botanical [...] Read more.
Bee pollen is widely recognized for its health benefits, with its nutritional and bioactive properties varying by botanical origin. This study analyzed twelve bee pollen samples collected from six different apiaries in Uruguay during two seasons (spring and autumn) to determine their botanical composition; nutritional profile (protein, lipids, carbohydrates, dietary fiber, ash, and fatty acid profile); bioactive compound content (total phenols, vitamin C, tocopherols, and carotenoids); antioxidant activity (ABTS and ORAC); color; and ability to inhibit enzymes involved in carbohydrate and fat digestion. Among the samples collected in autumn, three were monofloral (one from Casuarina and two from Eucalyptus). The spring samples, however, were all multifloral, except for one monofloral Rapeseed sample. Monofloral samples had higher protein, fiber, tocopherol, and total phenol content, along with higher ABTS and ORAC values, but lower carotenoid levels. In contrast, autumn samples had lower protein and lipid content but higher fiber and vitamin C levels. The predominant fatty acids were palmitic, linolenic, linoleic, and oleic acids, with most samples showing a higher proportion of polyunsaturated fatty acids (40.7–57.9%). Compared to other food matrices, the α-glucosidase inhibition values of Uruguayan bee pollen are similar to those found in raw citrus pomace. This is the first report on bee pollen’s ability to inhibit pancreatic lipase in relation to its in vitro anti-obesity properties. Uruguayan bee pollen shows significant potential for combating metabolic syndrome, obesity, and type 2 diabetes. Full article
(This article belongs to the Section Nutraceuticals, Functional Foods, and Novel Foods)
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15 pages, 2149 KiB  
Article
Reference Whole Genome Sequence Analyses and Characterization of a Novel Carnobacterium maltaromaticum Distinct Sequence Type Isolated from a North American Gray Wolf (Canis lupus) Gastrointestinal Tract
by C. Cristoph Klews, Jessika L. Bryant, Jennifer McCabe, Ariel N. Atchley, Thomas W. Cousins, Maya Barnard-Davidson, Mark R. Ackermann, Michael Netherland, Nur A. Hasan, Peter A. Jordan, Evan S. Forsythe, Patrick N. Ball and Bruce S. Seal
Vet. Sci. 2025, 12(5), 410; https://doi.org/10.3390/vetsci12050410 - 27 Apr 2025
Viewed by 995
Abstract
We hypothesize that bacteria isolated from free-ranging animals could potentially be useful for practical applications. To meet this objective a Gram-positive bacterium was isolated from the gastrointestinal (GI) tract of a Gray Wolf (Canis lupus) using Brucella broth with hemin and [...] Read more.
We hypothesize that bacteria isolated from free-ranging animals could potentially be useful for practical applications. To meet this objective a Gram-positive bacterium was isolated from the gastrointestinal (GI) tract of a Gray Wolf (Canis lupus) using Brucella broth with hemin and vitamin K (BBHK). By small ribosomal RNA (16S) gene sequencing the bacterium was initially identified as a novel Carnobacterium maltaromaticum strain. The bacterium could be propagated both anaerobically and aerobically and was both catalase/oxidase negative and negative by the starch hydrolysis as well as negative using lipase assays. The reference whole genome sequence (WGS) was obtained using both Illumina and Nanopore sequencing. The genome assembly was 3,512,202 bp in length, encoding core bacterial genes with a GC% content of 34.48. No lysogenic bacteriophage genes were detected, although the genome harbors genes for the expression of bacteriocin and other secondary metabolites with potential antimicrobial properties. Multilocus sequence typing (MLST), WGS phylogenetics, average nucleotide identity (ANI), and single nucleotide polymorphism (SNP) analyses of the isolate’s genome indicate this bacterium is a newly identified Carnobacterium maltaromaticum sequence type (ST). Members of the Carnobacteria have anti-listeria activities, highlighting their potential functional properties. Consequently, the isolate could be a potential probiotic for canids and this is the first report on an axenic C. maltaromaticum culture from the genus Canis. Full article
(This article belongs to the Section Veterinary Microbiology, Parasitology and Immunology)
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15 pages, 2625 KiB  
Article
Effects of Probiotic-Fermented Chinese Herb on Immune Response and Growth Performance in Common Carp (Cyprinus carpio)
by Wenzheng Zou, Xuanxuan Huang, Fang Han and Zhongqin Li
Fishes 2025, 10(5), 196; https://doi.org/10.3390/fishes10050196 - 26 Apr 2025
Viewed by 619
Abstract
This study investigated the effects of fermented Chinese herb (FCH) on the growth indices, leukocyte activity, and biochemical indices of carp (Cyprinus carpio). Astragalus membranaceus (AM), Pericarpium Citri Reticulatae (PCR), and Glycyrrhizae Radix et Rhizoma (GRR) as feed additives enhance immune [...] Read more.
This study investigated the effects of fermented Chinese herb (FCH) on the growth indices, leukocyte activity, and biochemical indices of carp (Cyprinus carpio). Astragalus membranaceus (AM), Pericarpium Citri Reticulatae (PCR), and Glycyrrhizae Radix et Rhizoma (GRR) as feed additives enhance immune function, promote growth, and exert anti-inflammatory effects, respectively. Therefore, this study investigated the effects of co-fermented blends of these three herbs on growth performance and related parameters in common carp. By adding 2%, 5%, and 10% of the FCH to co-incubate with carp leukocytes, the results show that all three experimental treatments could enhance the respiratory burst activity and phagocytic activity of carp leukocytes. After 28 days of feeding with basal feed supplemented with 2%, 5%, and 10% (w/v) of the FCH, the weight gain rate and specific growth rate of carp were significantly higher than those of the control treatment without additives (ANOVA, p < 0.05), with the 5% treatment showing the highest. The activities of intestinal digestive enzymes were significantly increased (ANOVA, p < 0.05). On the 21st day, the activities of amylase (AMS), lipase (LPS), and chymotrypsin were increased compared to the control treatment. The 5% and 10% treatments showed significantly higher intestinal digestive enzyme activities compared to the 2% treatment. The serum superoxide dismutase (SOD) levels in both the control and experimental treatments initially increased and then decreased, with all three experimental treatments having higher levels than the control treatment. The activities of liver glutamic-oxaloacetic transaminase (GOT) and glutamic-pyruvic transaminase (GPT) in the experimental treatments showed no significant changes compared to the control treatment (ANOVA, p > 0.05). However, the serum GPT activity in the 5% treatment was significantly lower than that of the control treatment (ANOVA, p < 0.05), while no significant differences were observed in the other treatments. The results indicate that adding 2~10% of FCH to carp feed can improve intestinal digestion, enhance phagocytic activity and the body’s antioxidant defense capabilities, and effectively promote the growth of carp. It can significantly improve farming efficiency and economic benefits, reduce dependence on chemical drugs, and lower environmental pollution, showing good application prospects in production. Full article
(This article belongs to the Special Issue Intestinal Health of Aquatic Organisms)
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13 pages, 1088 KiB  
Article
Bioactivity of Synthesized Trifluoromethyl Thioxanthone Analogues
by Murad Abualhasan, Hussein Haider, Ahmad Odeh and Amer Daraghmeh
Pharmaceuticals 2025, 18(4), 561; https://doi.org/10.3390/ph18040561 - 11 Apr 2025
Viewed by 1618
Abstract
Background: The study aims to evaluate the potential of trifluoromethyl thioxanthene derivatives across various biological activities, including antioxidant properties, anti-amylase effects, pancreatic lipase inhibition, anticancer activity, and COX inhibition. This research offers insights into the therapeutic applications of these compounds for managing metabolic [...] Read more.
Background: The study aims to evaluate the potential of trifluoromethyl thioxanthene derivatives across various biological activities, including antioxidant properties, anti-amylase effects, pancreatic lipase inhibition, anticancer activity, and COX inhibition. This research offers insights into the therapeutic applications of these compounds for managing metabolic disorders and inflammation. Method: Tertiary alcohols were synthesized using Grignard reagents and subsequently combined with L-cysteine, with their structures confirmed via NMR and IR spectroscopy. Results: The results indicated compound 3 exhibited the highest antioxidant potential, with 46.6% at 80 µg/mL in the DPPH assay. Compound 4 showed moderate pancreatic lipase inhibition, exhibiting an IC50 range of 100.6 to 277 µM. Compound 1 revealed potent anticancer activity against HeLa cells, with an IC50 of 87.8 nM. Compound 2 showed a potent antioxidant and anti-amylase activity with IC50 of 1.67 ± 0.5 and 60.2 ± 0.8 µM, respectively. Furthermore, the synthesized compounds 1, 3, and 4 displayed promising COX-2 inhibition with IC50 values ranging from 6.5 to 27.4 nM, suggesting potential anti-inflammatory benefits. Conclusions: This study highlights the significant biological activities of trifluoromethyl thioxanthene derivatives, positioning them as promising candidates for the treatment of cancer, metabolic disorders, and inflammation. These compounds demonstrated noteworthy antioxidant and enzyme inhibition properties, warranting further in vivo studies to confirm their therapeutic efficacy. Full article
(This article belongs to the Section Pharmacology)
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18 pages, 3777 KiB  
Article
The Effect of Bauhinia bowkeri Extracts on Hypercholesterolemia: Insights from In Vitro and In Silico Investigations
by Siphelele T. Thethwayo, Evelyn Madoroba, Sphamandla Masikane, Andrew R. Opoku and Nkosinathi D. Cele
Plants 2025, 14(6), 979; https://doi.org/10.3390/plants14060979 - 20 Mar 2025
Viewed by 548
Abstract
Despite the many current cholesterol-lowering drugs on the market, the persistent surge of hypercholesterolemic-related complications ignites a fascinating search for the discovery of novel therapeutics. This study aimed at investigating the anti-hypercholesterolemic effect of Bauhinia bowkeri extracts. The plant material was sequentially extracted [...] Read more.
Despite the many current cholesterol-lowering drugs on the market, the persistent surge of hypercholesterolemic-related complications ignites a fascinating search for the discovery of novel therapeutics. This study aimed at investigating the anti-hypercholesterolemic effect of Bauhinia bowkeri extracts. The plant material was sequentially extracted with n-hexane, dichloromethane (DCM), and 70% ethanol. The phytochemical constituents of the extracts were analyzed through GC-MS and the antioxidant activity of the extracts was screened against a wide range of free radicals (ABTS, DPPH, hydroxyl radical, and nitric oxide). The extracts were also screened for the metal iron chelating and reducing power potential. The enzyme inhibitory activity of the extracts on pancreatic lipase, cholesterol esterase, and HMG-CoA reductase as well as the bile acid binding capacity were evaluated. Among the total of 122 compounds detected in the three extracts, only 7 compounds (E-15-Heptadecenal, Diethyl Phthalate, 9,12,15-Octadecatrienoic acid ethyl ester, (Z,Z) Tetradecane 5-methyl, and Octadecane 5-methyl) were found to be common in all the extracts. The extract displayed a varying degree of efficiency on free radicals with IC50 values ranging from 0.07 mg/mL to 0.41 mg/mL. A concentration-dependent inhibition of pancreatic lipase and cholesterol esterase activities, along with a reduction in the bile-binding capacity exhibited by the extracts, was noted. In silico investigations of some of the phytoconstituent revealed significant inhibition of HMG-CoA reductase, cyclooxygenase, and hormone-sensitive lipase with a binding affinity that ranged between −5.1 and −7.0 kcal/mol. These findings suggest that Bauhinia bowkeri extracts possess potential antioxidant and anti-hypercholesterolemic properties. Full article
(This article belongs to the Special Issue Chemical Analysis and Biological Activities of Plant Essential Oils)
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17 pages, 7810 KiB  
Article
Two-Step Tandem Synthesis of Coumarin Derivatives Containing Bioamide Skeleton Catalyzed by Lipozyme TL IM from Thermomyces lanuginosus in Sustainable Continuous-Flow Microreactors
by Li-Hua Du, Hang Lin, Guo-Neng Fu, Zong-Hao Huang, Yi-Min Chen, Han-Jia Xie, Bing-Lin Yan, Miao-Miao Xue, Ao-Ying Zhang, Lin Wang and Xi-Ping Luo
Catalysts 2025, 15(3), 268; https://doi.org/10.3390/catal15030268 - 12 Mar 2025
Viewed by 940
Abstract
Due to their remarkable biological and pharmacological activities such as antibacterial, antifungal, anticoagulant, antioxidant, anticancer, and anti-inflammatory properties, synthesis of coumarins and their derivatives has attracted considerable attention in research and development among both organic and medicinal chemists. In this paper, we demonstrated [...] Read more.
Due to their remarkable biological and pharmacological activities such as antibacterial, antifungal, anticoagulant, antioxidant, anticancer, and anti-inflammatory properties, synthesis of coumarins and their derivatives has attracted considerable attention in research and development among both organic and medicinal chemists. In this paper, we demonstrated for the first time a two-step tandem enzymatic synthesis of coumarin bioamide derivatives through sustainable continuous-flow technology. Salicylaldehyde and dimethyl malonate were firstly reacted to obtain coumarin carboxylate methyl derivatives, which were then reacted with various biogenic amines at 50 °C for about 40 min under the catalysis of lipase TL IM from Thermomyces lanuginosus to obtain coumarin bioamide derivatives in continuous-flow reactors. Reaction parameters such as reaction solvent, reaction catalyst type, reactant ratio, residence time, reaction temperature and comparative experiments with traditional batch process were studied. Ideal product yields (62.7–87.1%) were obtained. Environmentally friendly methanol was applied as the reaction medium. Substantially shorter reaction times as well as a significant increase in the product yield were obtained as compared to the batch process. This innovative approach provides a promising green, efficient and rapid synthesis strategy for pharmaceutical synthesis and further research on novel coumarin bioamide derivatives. Full article
(This article belongs to the Section Biocatalysis)
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Article
An Evaluation of Soybean Protein Concentrate as a Replacement for Fish Meal with Methionine Supplementation in Diets for Hybrid Sturgeon (Acipenser baerii ♀ × A. schrenckii ♂)
by Zhaolin Li, Kai Xie, Jiufeng Gu, Xinyu Li, Yong Shi, Junzhi Zhang, Yi Hu and Xuezhi Zhu
Animals 2025, 15(6), 787; https://doi.org/10.3390/ani15060787 - 10 Mar 2025
Viewed by 930
Abstract
Soy protein concentrate (SPC) is a cost-effective alternative to fish meal (FM) in aquaculture, but its deficiency in essential amino acids, particularly methionine, limits its application. This study evaluated the effects of methionine supplementation on growth, liver and intestinal health, and muscle quality [...] Read more.
Soy protein concentrate (SPC) is a cost-effective alternative to fish meal (FM) in aquaculture, but its deficiency in essential amino acids, particularly methionine, limits its application. This study evaluated the effects of methionine supplementation on growth, liver and intestinal health, and muscle quality in hybrid sturgeon (Acipenser baerii ♀ × A. schrenckii ♂) fed SPC-based diets. Four diets were formulated: an FM control diet, and SPC diets supplemented with 0% (M0), 0.25% (M2.5), and 0.50% (M5) methionine. Replacing FM with SPC without methionine (M0) significantly reduced weight gain and the protein efficiency ratio (PER) while increasing the feed conversion ratio (FCR) and hepatic lipid accumulation. Methionine supplementation (M5) restored growth performance, the PER, and muscle texture to levels comparable to the FM group. Intestinal enzyme activities (lipase and trypsin), villus height, and goblet cell counts significantly improved in the M5 group. Gene expression analysis showed that M5 upregulated tight junction genes (claudin1, occludin) and anti-inflammatory genes (tgfβ, lysozyme) while reducing pro-inflammatory cytokines (il1β, il8). In the liver, M5 reduced oxidative stress markers such as malondialdehyde (MDA) and improved antioxidant enzyme activities (SOD, CAT) while optimizing lipid metabolism, as evidenced by lower triglyceride (TG) and total cholesterol (TC) levels. Muscle quality analysis showed that M5 significantly increased muscle hardness, chewiness, and fiber density compared to M0. In conclusion, methionine supplementation at 0.50% effectively mitigates the negative effects of SPC, improving growth, liver and intestinal health, and muscle quality in hybrid sturgeon. Full article
(This article belongs to the Section Aquatic Animals)
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