Search Results (4,091)

Plants of the genus Salacia (Celastraceae) have long been used in traditional medical systems of South and Southeast Asia for the management of diabetes and related metabolic disorders. Modern phytochemical and pharmacological studies have confirmed the antidiabetic potential of several Salacia species, leading to the identification of a distinctive group of sulfur-containing sugars as their principal bioactive constituents. Salacinol, neosalacinol, kotalanol, neokotalanol, and related analogues represent a novel class of thiosugar sulfonium compounds that act as potent and selective α-glucosidase inhibitors, providing a clear mechanistic basis for their glucose-lowering effects. Simpler thiosugars, such as 5-thiomannose, further contribute to the overall metabolic activity of Salacia extracts and may serve as biosynthetic or functional precursors. Beyond Salacia, sulfur-containing natural products are widespread in nature and perform diverse biological roles. In particular, the genus Allium is well known for producing organosulfur compounds, including thioethers and polysulfides, which exhibit antidiabetic, hypolipidemic, antioxidant, and cardioprotective activities. In a different context, sulfur-containing hopanes have been identified in sediments and petroleum as products of early diagenetic sulfurization of bacterial hopanoids. Although these compounds have been studied primarily as geochemical biomarkers, recent QSAR/PASS analyses suggest that sulfur hopanes may also possess biologically relevant activities, particularly related to metabolic and cardiovascular regulation. Recent PASS-based QSAR evaluations of Salacia-derived thiosugars and sulfur hopanes predict significant antidiabetic activity, including potential type 2 diabetes-related pharmacological effects, supported by predicted α-glucosidase inhibitory, hypoglycemic, hepatic, and gastrointestinal activities. Collectively, these findings highlight sulfur-containing natural products from both plant and sedimentary sources as chemically diverse yet functionally convergent scaffolds with promising potential for the development of functional foods and therapeutic agents targeting metabolic disorders. Full article

The integration of rooted plant flour into traditional noodle matrices, such as rice noodles and qingke noodles, represents a novel approach to enhancing the nutritional and sensory profiles of staple foods. This study investigates the volatile flavor components and functional compounds derived from rooted plant flours, including Gongmi “tribute rice”, qingke “highland barley” flour, kudzu vine flour, Gastrodia elata blume flour, dried ginger flour, and fishwort root flour, when incorporated into rice and qingke noodles. The novelty of this research lies in its comprehensive analysis of how these flours influence not only the nutritional and textural properties but also the volatile organic compounds (VOCs) that define sensory acceptance and health benefits. Using advanced gas chromatography mass spectrometry (GC-MS), we identified key VOCs, such as esters, aldehydes, and terpenes, which contribute to unique flavor profiles like umami, sweetness, and earthy notes in fortified noodles. Additionally, the study highlights the best functional compounds for health, including polyphenols, resistant starch, and polysaccharides, which demonstrate significant antioxidants, anti-inflammatory, and cholesterol-lowering properties. For instance, highland barley enriched flour exhibited high levels of phenolic compounds and carotenoids, which correlated with improved antioxidant activity and a reduced glycemic index. Similarly, Gongmi flour contributed elevated levels of γ-aminobutyric acid (GABA) and rutin, enhancing the rice noodles’ potential to manage metabolic diseases and support cardiovascular health. Molecular docking analyses predicted strong interactions between key volatile compounds (e.g., 3-dihydro-1, 3-trimethyl-33-phenyl-1H-indene) and metabolic targets like ACE and SGLT1, suggesting mechanisms for their cardioprotective and anti-diabetic effects. This research provides a groundbreaking framework for developing next generation functional foods by leveraging rooted plant flours to bridge the gap between sensory appeal and health efficacy, offering strategic insights for personalized nutrition and sustainable food production. Full article

Sri Lanka provides a home for a significant number of fruit species, and yet most of them are underutilised due to a lack of awareness regarding their therapeutic potential. Different plant parts from these fruits have been used for centuries to cure various diseases in traditional medicine, as fodder and to overcome hunger. Despite having remarkable health benefits and being resistant to extreme environmental conditions, these fruits are still confined to home gardens and forests, while some commercially cultivated major fruits remain dominant in the market. Hence, gathering information on the nutritional and health benefits of these fruit species will enhance people’s awareness, ensure food security through value-added food product development, facilitate livelihoods for rural farmers and also establish long-term sustainability. The main objective of this review is to highlight the phytochemical potential of some underutilised fruit varieties in Sri Lanka while exploring their health-promoting aspects, including antioxidant, anti-cancer, anti-diabetic, cardioprotective, anti-inflammatory and cytoprotective properties. Many research studies have been conducted on commonly available major fruits. However, there is a notable gap in research that explores pharmacological aspects of these fruits. Further research is warranted in developing methods for sustainable harvesting and postharvest practices for underutilised fruits from Sri Lanka. Characterisation of health benefits associated with underutilised fruits will help to develop awareness about their potential and possibly foster commercial interest. Developing nutraceuticals or functional foods from these fruits will help us to focus on enhancing their sustainable production. Full article

Plant foods have been the cornerstone of human diets since ancient times, fueling civilization and shaping cultures. Plants became central to sustainable food systems, offering diverse and nutritious options for the future. Sea buckthorn (Hippophae rhamnoides L.) has attracted growing scientific interest due to the presence of bioactive compounds, polyphenols, fatty acids, phytosterols, carotenoids, vitamins, and minerals in its fruit, seeds, and leaves. Moreover, sea buckthorn exhibit antioxidant, anti-inflammatory, antimicrobial, antidiabetic, antihyperlipidemic, anticancer, hepatoprotective, neuroprotective, and metabolic regulatory properties supported by in vitro and in vivo models. The biological activity of these phytochemical compounds plays a crucial role in regulating the AMP-activated protein kinase (AMPK) and phosphoinositide 3-kinase/protein kinase B (PI3K/Akt) signaling pathways, as well as pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6), cell proliferation, and apoptosis. Furthermore, its potential against microbial growth, including S. aureus, S. epidermidis, S. intermedius, and S. pyogenes, among others, not only expands its applications in the pharmaceutical industry but also attracts researchers to incorporate it into food products. This could lead to the discovery of plant-based therapeutic products without significant adverse effects. However, further exploration of each component’s potential side effects is necessary to support the commercialization of formulated products in either the pharmaceutical or food industries, ensuring the highest safety standards for consumers. Including studies on bioavailability and pharmacodynamics could further strengthen the scientific evidence supporting the specific phytochemicals in sea buckthorn and their mechanistic interactions. Full article

Elaeocarpus sylvestris (Lour.) Poir., an evergreen tree native to East and Southeast Asia, has gained increasing scientific attention owing to its broad pharmacological properties. Traditionally used in East Asian medicine to treat inflammation, fever, and infectious diseases, modern research has revealed diverse bioactivities, including potent antioxidant, anti-inflammatory, antiviral, anticancer, antidiabetic, and immunomodulatory effects. This therapeutic potential is primarily attributed to its rich phytochemical composition, particularly polyphenols such as geraniin, 1,2,3,4,6-penta-O-galloyl-β-D-glucose and quercetin. This review particularly focuses on the chemistry of E. sylvestris, summarizing structurally elucidated compounds, including hydrolysable tannins, flavonoids, and triterpenoids, along with recent insights into the structure–activity relationships that underpin these antiviral, antioxidant, and anticancer activities. Recent studies have demonstrated substantial antiviral efficacy of E. sylvestris extracts and isolated compounds against major human pathogens, including herpesviruses, influenza A virus, and SARS-CoV-2, supported by in silico, in vitro, in vivo, and early-phase clinical evaluations. Its cosmeceutical applications, including antioxidant, skin-whitening, and blue-light protective effects, further highlight its multifunctional potential. To our knowledge, this is the first comprehensive review summarizing the phytochemistry, pharmacological activities, therapeutic potential, and cosmeceutical applications of E. sylvestris. Despite these promising findings, challenges remain in elucidating precise molecular mechanisms, pharmacokinetics, and clinical validation. This review identifies current research gaps and future directions necessary to advance E. sylvestris as a scientifically validated natural therapeutic resource. Full article

The disproportionately severe disease course of diabetic patients with SARS-CoV-2 infection was repeatedly observed by clinicians during the COVID-19 pandemic. The overlap between metabolic impairment, viral pathophysiology, and chronic inflammation created a pattern that urged deeper examination. The aim of this paper was to review and synthesize evidence regarding the interaction between diabetes mellitus and COVID-19. We synthesized evidence across mechanistic pathways (immune dysregulation, chronic inflammation, ACE2/DPP-4-related signaling, endothelial dysfunction, and pancreatic involvement) and key clinical outcomes (severity, intensive care unit (ICU) admission, mortality, dysglycaemia/new-onset diabetes, and DKA). This systematic search was conducted in PubMed, Clinical Key, and Google Scholar. The eligibility criteria included papers on adults (≥18 years) with pre-existing diabetes mellitus (type 1 or type 2) or newly diagnosed diabetes/hyperglycemia and confirmed SARS-CoV-2 infection, published between January 2020 and October 2025, in English language. The PRISMA guidelines were used for data extraction. We identified 412 articles, out of which only 30 met all the inclusion criteria. Diabetes was consistently evoked as a major risk factor for severe COVID-19, being associated with higher susceptibility to pneumonia, respiratory failure, ICU admission, and mortality. The explanation lies in the impaired immune system, endothelial dysfunction, and metabolic repercussions imposed by hyperglycemia. Several antidiabetic drugs appeared protective in multiple cohorts. In conclusion, the accumulated evidence underscores the tight interplay between metabolic disease and COVID-19. Essentially, the clinical management of these patients would be a thoughtful selection of antidiabetic therapy and close metabolic monitoring. Full article

Background/Objectives: Onion (Allium cepa) peems are an underutilized by-product rich in polyphenols. This study evaluated the physicochemical profile, and bioactive potential (antidiabetic, antimicrobial, antioxidant, and anticoagulant) of Moroccan red onion peels using integrated in vivo, in vitro, and in silico approaches. Methods: Moisture, pH, ash content, and mineral elements were determined, followed by phytochemical screening and three extractions: decoction E0, aqueous Soxhlet E1, and hydroethanolic Soxhlet E2 (70/30; ethanol/water, v/v). The measurement of polyphenols, flavonoids, and tannins was carried out using colorimetric methods, while the molecular profile was studied by high-performance liquid chromatography coupled to ultraviolet detection and electrospray ionization mass spectrometry (HPLC/UV-ESI-MS). Biological activities were determined using 2,2-diphenyl-1-picrylhydrazyl, ferric reducing antioxidant power, and total antioxidant capacity assays (in vitro antioxidant); microdilution (antimicrobial); prothrombin time and activated partial thromboplastin time (anticoagulant); and α-amylase/α-glucosidase enzymatic inhibition and oral glucose tolerance tests on normoglycemic rats. Also, acute toxicity was evaluated, and molecular interactions between these proteins and ligands (docking, molecular dynamics, and MM-PBSA) were analyzed. Results: Physicochemical analyses showed an acidic pH (3.06) and high ash content (15.21%), with the concentration of regulated elements remaining within FAO/WHO limits. The extractive content was between 6.90% E0 and 19.18% E2. The E1 extract had the maximum amount of total polyphenols (178.95 mg GAE/g); on the other hand, E2 was the richest in flavonoids by 121.43 mg QE/g. The HPLC/ESI-MS analysis of E0 revealed 20 compounds, among which flavonoids (84.93%) were predominant, with isorhamnetin (30.26%), followed by quercetin and its glycosylated forms. E1 showed the most potent antioxidant effects (IC₅₀ DPPH, 22.38 µg/mL, as that of ascorbic acid). The antibacterial activity of E0 was especially potent towards Enterobacter cloacae and Pseudomonas aeruginosa (MIC 75 µg/mL). A mild dose-dependent anticoagulant effect was seen. Antidiabetic activity was found to be outstanding: α-amylase (IC₅₀ 62.75 µg/mL) and α-glucosidase (IC₅₀ 8.49 µg/mL, stronger than acarbose) inhibitions were corroborated in vivo by a considerable decrease in the glycemic area under the curve. The molecular docking study in silico demonstrated strong molecular interactions, especially for quercetin 4′-O-glucoside with good binding energies. Conclusions: A. cepa peels from Morocco can be considered a safe plant matrix containing bioactive flavonoids with strong antioxidant and selective antimicrobial activities and promising antidiabetic effects, supported by molecular modeling. Full article

Background: Hidradenitis suppurativa (HS) is a chronic inflammatory skin disease, which presents with painful nodules, abscesses and sinus tracts. Patients suffer from pain, drainage and worsening of mental health and quality of life. Treatment is often difficult. HS is typically associated with obesity and metabolic syndrome; thus, antidiabetics, especially GLP-1 agonists, present a potential therapy option. The aim of this review was to analyze the effects of GLP-1 agonists on patients with HS, including on their cardiovascular risk and quality of life. Methods: A literature search was conducted on Embase and PubMed, yielding 300 papers, of which 10 were used for this review. Results: HS patients using GLP-1 agonists showed improved clinical course with less pain and suppuration. Further, patients’ quality of life and mental health improved and their cardiovascular risk was reduced. Inflammatory parameters showed no significant changes. Patients receiving a higher drug dose of GLP-1 agonists were more likely to show clinical improvement. A reduction in weight or BMI did not correlate with improvements in Hurley stage, pain or depression. Hence, HS patients could be treated with GLP-1 agonists. Conclusions: Therefore, whether patients’ improvement is due to weight loss, or other mechanisms, i.e., GLP-1 agonists’ anti-inflammatory properties, remains to be determined in further studies. Full article

Diabetic retinopathy (DR), recognized as a progressive neurovascular and microvascular complication of diabetes, remains one of the leading causes of visual disability worldwide, within the context of a sustained increase in ophthalmic diseases and retinal vascular disorders that compromise vision. This study aimed to characterize the progression of diabetic retinopathy in a streptozotocin (STZ)-induced Wistar rat model. A single dose of 65 mg/kg body weight was administered, with follow-up periods at 2, 4, 8, and 10 weeks, compared to healthy controls. STZ-induced rats exhibited reduced weight gain compared to the control group. They also showed markedly variable hyperglycemia, with glucose concentrations ranging from 250 to 530 mg/dL. Histological analysis of retinal tissue at week 4 revealed early signs of vascular compromise, including early indications of a microenvironment conducive to neovascularization and edema. By week 8, retinal damage had progressed to hemorrhage, persistent edema, and layer-specific vascular disruption. At week 10, intensified neovascularization and exacerbated edema indicated advanced microvascular deterioration. Immunofluorescence analysis demonstrated a temporal accumulation of CD8⁺ T cells in the retina, correlating with photoreceptor degeneration. The coordinated dynamics of CD4⁺ and CD8⁺ T cells suggested transient immune activation during STZ-induced retinal degeneration. Gene expression profiling revealed a proinflammatory and pro-oxidative retinal microenvironment, characterized by the overexpression of angiogenic pathways and proliferative signals. Simultaneously, the antioxidant response appeared partially impaired. Collectively, these findings provide mechanistic perspective on the multifactorial nature of diabetic retinopathy. Oxidative stress, inflammation, and angiogenesis converge to disrupt retinal homeostasis. This experimental model may serve as a reliable platform for future studies aimed at elucidating disease pathophysiology, identifying novel therapeutic targets, and evaluating emerging ophthalmic antidiabetic interventions. Full article

Medlar (Mespilus germanica L.) fruit presents a good source of bioactive compounds. This study aimed to optimize the traditional extraction method, maceration, in order to obtain extracts rich in polyphenols. The total phenolic compounds (TPC) from physiologically ripe (PRMFs) and consumable ripe (CRMFs) medlar fruits were extracted to develop models with high accuracy and prediction capacity by response surface methodology (RSM). Furthermore, the main phenolic compounds in the extracts were quantified using HPLC, and the extracts were tested for antioxidant activity and hypoglycemic activity. The extracts were prepared according to a central composite design. The extraction parameters for both PRMFs and CRMFs were time (30–210 min), ethanol concentration (20–80%) and solid-to-solvent ratio (1:10–1:50). The obtained results indicated that the optimal conditions for the extraction were 210 min, 66.55% ethanol, and 1:50 solid-to-solvent ratio (PRMF), and 120 min, 74.96% ethanol, and 1:50 solid-to-solvent ratio (CRMF). Under the optimized conditions, values for TPC were in agreement with the values predicted by RSM. Isoquercitrin, rutin, procyanidin B2, chlorogenic acid and caffeic acid were the most abundant compounds in both PRMF and CRMF optimized extracts. TPC, antioxidant activity, and inhibition of α-glucosidase and α-amylase enzymes did not show significant differences (p > 0.05) among PRMF and CRMF extracts. Full article

During 2022–2023, research groups from 40 nations contributed to the preclinical pharmacology of 173 structurally defined marine-derived compounds, unveiling innovative mechanisms of action. Peer-reviewed publications in the field of marine natural product pharmacology during 2022–2023 included mechanism-of-action studies with 43 compounds showing antibacterial, antifungal, antiprotozoal, antitubercular, and antiviral activity. Additional mechanism-of-action studies were reported for 74 marine compounds that exhibited antidiabetic and anti-inflammatory properties, as well as significant effects on both the immune and nervous systems. Finally, while 65 marine compounds revealed unique and diverse pharmacological mechanisms, further investigation will be required to determine whether they will contribute to a particular therapeutic category. Collectively, the pharmacology of 2022–2023 preclinical marine natural products demonstrated robust activity, offering both novel mechanistic insights and promising chemical scaffolds to enrich the 2026 marine pharmaceutical development pipeline (https://www.marinepharmacology.org/) which currently consists of 17 marine-derived pharmaceuticals approved for clinical use and 29 compounds in either Phase I, II or III of clinical pharmaceutical development. Full article

Background/Objectives: Metabolic diseases are increasingly associated with diets low in bioactive compounds. Native maize varieties possess functional potential; however, they remain underutilized. Moringa oleifera leaf flour (MF), rich in protein and polyphenols, represents a promising functional ingredient. This study evaluated the incorporation of MF into red native corn tortillas and its effects on nutritional composition and antioxidant capacity, as well as assessed its hypoglycemic and hypolipidemic effects in Wistar rats. Methods: Tortillas were formulated with 5% MF. Nutritional composition was determined using standard AOAC methods, while bioactive compounds (total phenolics and flavonoids) and antioxidant activity were evaluated using Folin–Ciocalteu, aluminum chloride (AlCl₃) colorimetric, DPPH^•, and ABTS^•+ assays, respectively. Male Wistar rats (12 weeks old, with an approximate weight ofs 360 g; n = 5/group) were fed the experimental diets for 21 days with either a standard diet, a high-fat diet, or high-fat diets supplemented with MF or MF-enriched tortillas. Serum glucose, triglycerides, total cholesterol, and HDL were measured using enzymatic colorimetric methods. Data were analyzed by ANOVA followed by Tukey’s test (p < 0.05). Results: MF incorporation increased protein (+19.85%), dietary fiber (+18.51%), and mineral content (+41.03%) compared to control tortillas. Total phenolics and flavonoids increased by 114.0% and 184.7%, respectively. Antioxidant activity improved significantly, as evidenced by reductions in IC₅₀ values of 41.1% (DPPH^•) and 43.1% (ABTS^•). In vivo, MF-enriched tortillas reduced triglycerides by 68.4%, total cholesterol by 16.2%, and hepatic lipid accumulation by 31.8% compared to the high-fat diet group. Glucose levels showed a reduction of 8.5%, although not statistically significant (p > 0.05). Conclusions: The incorporation of MF into red corn tortillas significantly enhances their nutritional and functional properties. In vivo results also showed improvements in lipid profile and a non-significant reduction in glucose levels. These findings support the development of functional foods based on traditional staples with potential health benefits. Full article

Momordica balsamina Linn. is widely used in traditional medicine for the management of diabetes; however, the specific bioactive compounds responsible for this activity have not been fully isolated and structurally elucidated from South African populations. This study reports, for the first time, the isolation and comprehensive characterization of antidiabetic compounds from South African samples of M. balsamina. Crude extracts were obtained through sequential solvent extraction, followed by isolation and purification using vacuum liquid chromatography. Structural elucidation was achieved using HPLC, UPLC–MS, FTIR, and NMR spectroscopy. The antidiabetic potential of the isolated compounds was evaluated through inhibition assays against α-amylase, α-glucosidase, and β-glucosidase. Molecular docking was employed to examine binding interactions with these target enzymes, while cytotoxicity was assessed using the MTT assay against Vero and HEK-293 cell lines. Two compounds, DD26.27 and EAEA1.2, were successfully isolated from dichloromethane and ethyl acetate extracts, respectively. Both compounds demonstrated concentration-dependent inhibition of the tested enzymes. Notably, molecular docking revealed strong binding affinities and favorable interactions with key catalytic residues, surpassing the standard drug acarbose and corroborating the in vitro results. Cytotoxicity studies confirmed that, at lower concentrations, the compounds were non-toxic to the tested cell lines. Collectively, these findings provide novel scientific validation of the traditional use of M. balsamina in South Africa and identify promising lead compounds for further in vivo studies and antidiabetic drug development targeting postprandial hyperglycemia. Full article

Polyphenols have attracted considerable scientific interest over recent years due to their broad spectrum of biological activities, including antioxidant, cardioprotective, anti-inflammatory, antidiabetic, and anticancer properties. However, their practical application is often limited by unfavorable physicochemical characteristics, particularly low aqueous solubility. Consequently, amorphous solid dispersions (ASDs) have been extensively investigated as a formulation strategy to overcome these limitations. This article represents the first part of a two-part review and presents the current state of the art in amorphous solid dispersions of polyphenols. The available literature is systematically summarized with respect to the investigated polyphenolic compounds, the employed carriers (with particular emphasis on polymeric systems), the preparation methods, and the solid-state characterization techniques used to confirm amorphization. Both single-component systems and binary combinations of polyphenols reported in the literature are considered. The collected data are presented in tabular form and complemented by a heat map illustrating the frequency of reported polyphenol–carrier combinations. The aim of this review is to organize the available knowledge, identify the most extensively studied systems, and highlight research areas that remain underexplored. A detailed discussion of the pharmaceutical benefits and mechanistic aspects of polyphenols in ASD systems will be provided in Part II. Full article

Gamma-aminobutyric acid (GABA), a non-protein amino acid, functions as the chief inhibitory neurotransmitter in mammals and is associated with several health benefits, including hypotensive, diuretic, tranquilizing, and antidiabetic effects. Although cocoa has been identified as a potential source of GABA, information regarding its concentration in cocoa-derived materials remains limited. This study evaluated the GABA content of dried germinated cocoa beans and dried cocoa husks (shells) collected from different geographical regions in Thailand. GABA was extracted using solid–liquid extraction with deionized water, 70% ethanol (v/v), and 90% ethanol (v/v), and quantified by high-performance liquid chromatography coupled with diode array detection (HPLC/DAD). The results revealed that both germinated cocoa beans and cocoa husks contain considerable amounts of GABA. The highest GABA content in cocoa beans was detected in samples from Tak province (242 ± 18 mg/100 g), while cocoa husks from Nan province exhibited the highest GABA content (361 ± 11 mg/100 g), both obtained using 70% ethanol extraction. Among the solvents tested, 70% ethanol demonstrated superior extraction efficiency compared with deionized water and 90% ethanol. In conclusion, germinated cocoa beans and cocoa husks represent promising natural sources of GABA, and extraction with 70% ethanol provides an effective approach for maximizing GABA recovery for potential functional foods and bioactive product development. Full article