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Search Results (724)

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Keywords = Hypoglycemic activity

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16 pages, 3038 KiB  
Article
Comparative Effects of Maturity and Processing on Chemical Composition and Bioactivities in Toona sinensis Leaves
by Guohuo Wu, Zhaoyun Chen, Yan Tang, Shuolei Xu, Wenli Fan, Li Wu, Yuntao Ji and Changqing Qu
Foods 2025, 14(15), 2717; https://doi.org/10.3390/foods14152717 (registering DOI) - 2 Aug 2025
Abstract
Toona sinensis (“Heiyouchun”) is a traditional Chinese woody vegetable, the leaves of which can also be processed into tea, known for its distinctive flavor and diverse bioactivities. However, the effects of leaf maturity and processing methods on its phytochemical composition and functional properties [...] Read more.
Toona sinensis (“Heiyouchun”) is a traditional Chinese woody vegetable, the leaves of which can also be processed into tea, known for its distinctive flavor and diverse bioactivities. However, the effects of leaf maturity and processing methods on its phytochemical composition and functional properties remain unclear. In this study, metabolomic analysis revealed 35 significantly different metabolites between tender and mature leaves, with higher concentrations of flavonoids, flavonoid glycosides, limonoids, and amino acids in tender leaves. Additionally, comparative analysis revealed that black tea fermentation preserves bioactive compounds more effectively than hot-air drying, particularly in tender leaves. In vitro activity assays showed that toon leaf tea extracts exhibited significant antioxidant and hypoglycemic effects, with black tea fermented tender leaves displaying the most potent bioactivity. Correlation analysis further confirmed a strong positive relationship between flavonoid/polyphenol content and bioactivity. These findings provide a theoretical foundation for optimizing processing techniques to enhance the functional properties of toon leaf tea. Full article
(This article belongs to the Section Plant Foods)
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36 pages, 1730 KiB  
Review
Pharmacological Potential of Cinnamic Acid and Derivatives: A Comprehensive Review
by Yu Tian, Xinya Jiang, Jiageng Guo, Hongyu Lu, Jinling Xie, Fan Zhang, Chun Yao and Erwei Hao
Pharmaceuticals 2025, 18(8), 1141; https://doi.org/10.3390/ph18081141 - 31 Jul 2025
Viewed by 171
Abstract
Cinnamic acid, an organic acid naturally occurring in plants of the Cinnamomum genus, has been highly valued for its medicinal properties in numerous ancient Chinese texts. This article reviews the chemical composition, pharmacological effects, and various applications of cinnamic acid and its derivatives [...] Read more.
Cinnamic acid, an organic acid naturally occurring in plants of the Cinnamomum genus, has been highly valued for its medicinal properties in numerous ancient Chinese texts. This article reviews the chemical composition, pharmacological effects, and various applications of cinnamic acid and its derivatives reported in publications from 2016 to 2025, and anticipates their potential in medical and industrial fields. This review evaluates studies in major scientific databases, including Web of Science, PubMed, and ScienceDirect, to ensure a comprehensive analysis of the therapeutic potential of cinnamic acid. Through systematic integration of existing knowledge, it has been revealed that cinnamic acid has a wide range of pharmacological activities, including anti-tumor, antibacterial, anti-inflammatory, antidepressant and hypoglycemic effects. Additionally, it has been shown to be effective against a variety of pathogens such as Staphylococcus aureus, Pseudomonas aeruginosa, and foodborne Pseudomonas. Cinnamic acid acts by disrupting cell membranes, inhibiting ATPase activity, and preventing biofilm formation, thereby demonstrating its ability to act as a natural antimicrobial agent. Its anti-inflammatory properties are demonstrated by improving oxidative stress and reducing inflammatory cell infiltration. Furthermore, cinnamic acid enhances metabolic health by improving glucose uptake and insulin sensitivity, showing promising results in improving metabolic health in patients with diabetes and its complications. This systematic approach highlights the need for further investigation of the mechanisms and safety of cinnamic acid to substantiate its use as a basis for new drug development. Particularly in the context of increasing antibiotic resistance and the search for sustainable, effective medical treatments, the study of cinnamic acid is notably significant and innovative. Full article
(This article belongs to the Section Pharmacology)
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22 pages, 1071 KiB  
Article
Proximate Composition, Phytochemicals, Phenolic Compounds, and Bioactive Characterization of Mauritia flexuosa L.f. Seeds
by Claudia Cristina Pérez Jaramillo, Liceth N. Cuéllar Álvarez and Walter Murillo Arango
Plants 2025, 14(15), 2323; https://doi.org/10.3390/plants14152323 - 27 Jul 2025
Viewed by 432
Abstract
Mauritia flexuosa, commonly known as “canangucha,” holds significant nutritional and economic value in the Amazon region. While its pulp is widely utilized in local food products, the seed or kernel is largely underutilized. This study investigated the proximal and phytochemical composition of [...] Read more.
Mauritia flexuosa, commonly known as “canangucha,” holds significant nutritional and economic value in the Amazon region. While its pulp is widely utilized in local food products, the seed or kernel is largely underutilized. This study investigated the proximal and phytochemical composition of M. flexuosa, alongside its biological properties, specifically focusing on the hypoglycemic activity of an ethanolic extract from M. flexuosa seeds (MFSs). Proximal analysis revealed that MFSs are a notable source of crude fiber (28.4%) and a moderate source of protein (9.1%). Phytochemical screening indicated a high total polyphenol content (123.4 mg gallic acid equivalents/100 mg dry weight) and substantial antiradical capacity against the ABTS radical (IC50 = 171.86 µg/mL). Notably, MFS ethanolic extracts exhibited significant in vitro antihyperglycemic activity via inhibiting α-amylase and α-glucosidase enzymes, demonstrating comparable inhibition to acarbose at higher concentrations. This hypoglycemic effect was further corroborated in an in vivo rat model with induced diabetes, where the administration of 100 mg/kg of MFS ethanolic extract significantly reduced blood glucose levels compared to the diabetic control group (p < 0.05). A moderate antihypertensive effect was observed at a concentration of 150 mg/kg, correlating with ACE inhibition. High-performance liquid chromatography–mass spectrometry (UHPLC-ESI-HRMS) analysis of the seed extract identified phenolic compounds including ellagic, p-coumaric, and chlorogenic acids, as well as flavonoids such as quercetin, myricetin, and epicatechin. This study provides the first evidence of the hypoglycemic activity of MFSs, offering valuable insights into their phytochemistry and potential therapeutic applications. Full article
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17 pages, 5515 KiB  
Article
Hypoglycemic Effects of Silphium perfoliatum L. In Vitro and In Vivo and Its Active Composition Identification by UPLC-Triple-TOF-MS/MS
by Guoying Zhang, Liying Liu, Wenjing Jia, Luya Wang, Jihong Tao, Wei Zhang, Huilan Yue, Dejun Zhang and Xiaohui Zhao
Pharmaceuticals 2025, 18(8), 1087; https://doi.org/10.3390/ph18081087 - 23 Jul 2025
Viewed by 226
Abstract
Background: Reducing postprandial blood glucose (PBG) is a crucial strategy for treating diabetes and minimizing the risk of complications. Developing efficient and safe α-glycosidase inhibitors from natural products to lower PBG has attracted much attention. Silphium perfoliatum L. (SP), a traditional herbal [...] Read more.
Background: Reducing postprandial blood glucose (PBG) is a crucial strategy for treating diabetes and minimizing the risk of complications. Developing efficient and safe α-glycosidase inhibitors from natural products to lower PBG has attracted much attention. Silphium perfoliatum L. (SP), a traditional herbal medicine of North American Indigenous tribes, has efficacy of treating metabolic diseases, but its hypoglycemic activity and bioactive components have not been fully studied. Methods: In vitro α-glucosidase inhibition and in vivo sucrose/maltose/starch tolerance assays were performed to assess the hypoglycemic effects of SP extracts, and UPLC-Triple-TOF-MS/MS analysis was used to tentatively identify its chemical structure composition. In vitro enzyme inhibition and molecular docking were used to verify the effective ingredients. Results: In vitro hypoglycemic activities of four extracts of SP (SP-10/SP-40/SP-60/SP-C) showed that SP-10 exhibited strong α-glucosidase (sucrase and maltase) inhibitory effects with IC50 of 67.81 μg/mL and 62.99 μg/mL, respectively. Carbohydrate tolerance assays demonstrated that SP-10 could significantly reduce the PBG levels of diabetic mice, with a significant hypoglycemic effect at a dosage of 20 mg/kg. A total of 26 constituents, including 11 caffeoylquinic acids (CQAs) and 15 flavonol glycosides, were tentatively identified by mainly analyzing secondary MS fragmentation. Moreover, three CQAs rich in SP-10, namely chlorogenic acid (CGA), neochlorogenic acid (NCGA), and cryptochlorogenic acid (CCGA), may be the main hypoglycemic substances, as evidenced by their inhibitory effects on sucrase and maltase. Conclusions: The α-glucosidase inhibitory effects of SP extract both in vitro and in vivo and its active ingredients were systematically studied for the first time. Results indicated that SP extract, rich in CQAs, had significant hypoglycemic activity, supporting the considerable potential of SP as hypoglycemic functional food or cost-effective therapeutic agents for diabetes treatment. Full article
(This article belongs to the Section Natural Products)
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22 pages, 3640 KiB  
Review
Progress in Research on Animal Collagen Peptides: Preparation, Bioactivity, and Application
by Xuanxuan Ma, Po-Hsiang Chuang, Yu-Hui Tseng, Xiao Wang, Ziteng Ma, Haofei Chen, Wenye Zhai, Wenwen Yang, Zhaoqing Meng and Jing Xu
Molecules 2025, 30(15), 3061; https://doi.org/10.3390/molecules30153061 - 22 Jul 2025
Viewed by 466
Abstract
Type I collagen is a major protein in animals, and its hydrolyzed products, collagen peptides, have wide-ranging applications. This article reviews collagen peptides’ preparation methods, biological activities, and application progress in the fields of food, cosmetics, and medicine. By employing various extraction and [...] Read more.
Type I collagen is a major protein in animals, and its hydrolyzed products, collagen peptides, have wide-ranging applications. This article reviews collagen peptides’ preparation methods, biological activities, and application progress in the fields of food, cosmetics, and medicine. By employing various extraction and hydrolysis methods, collagen peptides with different molecular weights can be obtained, and their biological activities are closely related to their molecular weight and amino acid sequence. Studies have revealed that collagen peptides possess a variety of biological activities, including antioxidant, hematopoietic promotion, osteogenic differentiation promotion, antihypertensive, and anti-diabetic effects. In the food industry, their antioxidant and hypoglycemic properties have opened new avenues for the development of healthy foods; in the cosmetics field, the moisturizing, anti-aging, and repair functions of collagen peptides are favored by consumers; in the medical field, collagen peptides are used in wound dressings, drug carriers, and tissue engineering scaffolds. Looking to the future, the development of green and efficient preparation technologies for collagen peptides and in-depth research into the relationship between their structure and function will be important research directions. The multifunctional properties of collagen peptides provide a broad prospect for their further application in the health industry. Full article
(This article belongs to the Special Issue New Achievements and Challenges in Food Chemistry)
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24 pages, 1190 KiB  
Review
An Overview of Buckwheat—A Superfood with Applicability in Human Health and Food Packaging
by Alexandra Andreea Lițoiu, Adriana Păucean, Claudiu Lung, Alexandru Zmuncilă and Maria Simona Chiș
Plants 2025, 14(14), 2200; https://doi.org/10.3390/plants14142200 - 16 Jul 2025
Viewed by 937
Abstract
Buckwheat, a dicotyledonous pseudocereal from the Polygonaceae family, has emerged as a crop of scientific and industrial interest due to its exceptional phytochemical profile, adaptability to different environments, and minimal agronomic input requirements. This paper aims to highlight the proximate composition (carbohydrates, protein, [...] Read more.
Buckwheat, a dicotyledonous pseudocereal from the Polygonaceae family, has emerged as a crop of scientific and industrial interest due to its exceptional phytochemical profile, adaptability to different environments, and minimal agronomic input requirements. This paper aims to highlight the proximate composition (carbohydrates, protein, dietary fiber, lipids, starch, vitamins, and minerals) of the buckwheat principal species, Fagopyrum esculentum Moench (common buckwheat) and Fagopyrum tataricum (L.) Gaertn (Tartary buckwheat). Other bioactive compounds, including flavonoids (e.g., rutin, quercetin), phenolic acids, and anthocyanins, were emphasized, together with their influence on human health. These constituents confer a broad range of biological activities such as anti-inflammatory, antimicrobial, antidiabetic, antihypertensive, and hypoglycemic effects. Moreover, buckwheat is inherently gluten-free, making it a valuable alternative in formulations targeting gluten-sensitive populations. Finally, the review addresses the possibility of using starch buckwheat as a raw material in starch-based films. Further research is needed to elucidate the potential of buckwheat starch as a viable material for the development of biodegradable food packaging films. Full article
(This article belongs to the Special Issue Bioactive Plants, Phytocompounds and Plant-Derived Food)
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27 pages, 891 KiB  
Review
The Antidiabetic Activity of Wild-Growing and Cultivated Medicinal Plants Used in Romania for Diabetes Mellitus Management: A Phytochemical and Pharmacological Review
by Diana Maria Trasca, Dalia Dop, George-Alin Stoica, Niculescu Stefan Adrian, Niculescu Elena Carmen, Renata Maria Văruț and Cristina Elena Singer
Pharmaceuticals 2025, 18(7), 1035; https://doi.org/10.3390/ph18071035 - 11 Jul 2025
Viewed by 598
Abstract
Diabetes mellitus is a chronic metabolic disease that has a significant impact on public health and is becoming more and more common worldwide. Although effective, conventional therapies are often limited by high cost, adverse effects, and issues with patient compliance. As a result, [...] Read more.
Diabetes mellitus is a chronic metabolic disease that has a significant impact on public health and is becoming more and more common worldwide. Although effective, conventional therapies are often limited by high cost, adverse effects, and issues with patient compliance. As a result, there is growing interest in complementary and alternative therapies. Medicinal plants have played an essential role in diabetes treatment, especially in regions such as Romania, where biodiversity is high and traditional knowledge is well preserved. The pathophysiology, risk factors, and worldwide burden of diabetes are examined in this review, with an emphasis on the traditional use of medicinal plants for glycemic control. A total of 47 plant species were identified based on ethnopharmacological records and recent biomedical research, including both native flora and widely cultivated species. The bioactive compounds identified, such as flavonoids, triterpenic saponins, polyphenols, and alkaloids, have hypoglycemic effects through diverse mechanisms, including β-cell regeneration, insulin-mimetic action, inhibition of α-glucosidase and α-amylase, and oxidative stress reduction. A systematic literature search was conducted, including in vitro, in vivo, and clinical studies relevant to antidiabetic activity. Among the species reviewed, Urtica dioica, Silybum marianum, and Momordica charantia exhibited the most promising antidiabetic activity based on both preclinical and clinical evidence. Despite promising preclinical results, clinical evidence remains limited, and variability in phytochemical content poses challenges to reproducibility. This review highlights the potential of Romanian medicinal flora as a source of adjunctive therapies in diabetes care and underscores the need for standardization and clinical validation. Full article
(This article belongs to the Section Natural Products)
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15 pages, 1267 KiB  
Review
Plant Heteropolysaccharides as Potential Anti-Diabetic Agents: A Review
by Dan He and Can Cui
Curr. Issues Mol. Biol. 2025, 47(7), 533; https://doi.org/10.3390/cimb47070533 - 9 Jul 2025
Viewed by 352
Abstract
Diabetes mellitus (DM), a chronic metabolic disease, poses a significant challenge to global health. Although type 1 diabetes mellitus (T1DM), type 2 diabetes mellitus (T2DM), gestational diabetes mellitus (GDM), and other types of diabetes mellitus differ in pathological mechanisms, they converge in that [...] Read more.
Diabetes mellitus (DM), a chronic metabolic disease, poses a significant challenge to global health. Although type 1 diabetes mellitus (T1DM), type 2 diabetes mellitus (T2DM), gestational diabetes mellitus (GDM), and other types of diabetes mellitus differ in pathological mechanisms, they converge in that hyperglycemia is a universal clinical hallmark. Currently, the antidiabetic medications employed in clinical practice for blood glucose management require long-term administration and are associated with various side effects that can adversely impact human health. Plant heteropolysaccharides have emerged as promising candidates for anti-diabetic therapy, owing to their abundant natural sources, absence of toxicities, and confirmed hypoglycemic activities. This review aims to summarize the anti-diabetic mechanisms of plant heteropolysaccharides by dissecting the key biological pathways associated with clinical intervention in DM, including the modulation of insulin secretion, a reduction in insulin resistance, and an alteration in the composition of the gut microbiota. For these reasons, these findings provide a theoretical framework for the clinical application of plant heteropolysaccharides and indicate that they are expected to become natural agents used in treating DM. Full article
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17 pages, 1596 KiB  
Article
Flavonoids of Mao Jian Green Tea Ameliorate Glycemic Metabolism in Type-2-Diabetic Rats via AMPK Signaling Pathways and Gut Microbiota Regulation
by Lei Wu, Yao Niu, Fei Liu, Jiongling Tian, Zhilin Ma, Jiahui Yang, Xiaomeng Guo and Yaogui Sun
Foods 2025, 14(13), 2402; https://doi.org/10.3390/foods14132402 - 7 Jul 2025
Viewed by 367
Abstract
Mao Jian Green Tea flavonoids (MJGT_F) contain luteolin, luteolin-7-O-glucoside, eriodictyol, and eriodictyol-7-O-glucoside, among which the first three components have hypoglycemic effects; however, the overall hypoglycemic potential of MJGT_F remains unclear. This study demonstrated that MJGT_F inhibited α-glucosidase in vitro and improved metabolic parameters [...] Read more.
Mao Jian Green Tea flavonoids (MJGT_F) contain luteolin, luteolin-7-O-glucoside, eriodictyol, and eriodictyol-7-O-glucoside, among which the first three components have hypoglycemic effects; however, the overall hypoglycemic potential of MJGT_F remains unclear. This study demonstrated that MJGT_F inhibited α-glucosidase in vitro and improved metabolic parameters in a dose-dependent manner in T2DM (type 2 diabetes mellitus) rats (reducing blood glucose, triglyceride, total cholesterol, low-density lipoprotein, insulin, and the homeostatic model assessment of insulin resistance; increasing high-density lipoprotein, insulin sensitivity index, and glucagon-like peptide-1). High-dose MJGT_F (MJGT_F_H) showed optimal efficacy. Mechanistically, MJGT_F_H activated the AMPK pathway, evidenced by a significant increase in the p-AMPK/AMPK ratio and downregulation of hepatic gluconeogenic enzymes G6Pase and PEPCK. These coordinated effects collectively suggest enhanced hepatic glucose utilization and suppression of glucose overproduction. MJGT_F_H also modulated gut microbiota by enriching beneficial taxa (e.g., Akkermansia muciniphila, 11.17-fold vs. metformin) and reducing pathogens like Enterobacteriaceae. These findings highlight MJGT_F’s dual regulatory roles in glucose metabolism and microbiota, supporting its potential for diabetes management. Full article
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17 pages, 6326 KiB  
Review
Crithmum maritimum L.: Phytochemical Profile, Biological Activities, and Therapeutic Potential
by Velina Dzhoglova, Stanislava Ivanova, Michaela Shishmanova-Doseva and Kremena Saracheva
Molecules 2025, 30(13), 2832; https://doi.org/10.3390/molecules30132832 - 1 Jul 2025
Viewed by 496
Abstract
Members of the Apiaceae family have been recognized since antiquity for their health-promoting properties. The halophytic species Crithmum maritimum L. (commonly known as sea fennel) has been used in traditional medicine since antiquity, largely due to its diverse and bioactive phytochemical composition. The [...] Read more.
Members of the Apiaceae family have been recognized since antiquity for their health-promoting properties. The halophytic species Crithmum maritimum L. (commonly known as sea fennel) has been used in traditional medicine since antiquity, largely due to its diverse and bioactive phytochemical composition. The plant’s complex chemical composition includes terpenoids, phenolic acids, flavonoids, tannins, dietary fibers, fatty acids, and essential vitamins. Essential oils (EOs) extracted from C. maritimum L. have demonstrated a wide range of biological activities, including antibacterial, antifungal, anti-inflammatory, antioxidant, and anticancer effects. Moreover, recent evidence suggests additional biofunctional roles such as cognitive enhancement and the inhibition of melanin synthesis in the skin. Extracts of the plant exhibit significant bioactivity, having shown antiparasitic, hypoglycemic, vasodilatory, and probiotic effects in preliminary studies. Despite this pharmacological potential, the number of experimental studies (particularly in vivo investigations) remains limited. The present review consolidates existing in vitro and in vivo research on C. maritimum L. with an analysis of 79 scientific studies aimed at elucidating its therapeutic potential and identifying future research directions necessary to support its broader application in biomedical and functional food contexts. Full article
(This article belongs to the Special Issue Chemical Composition and Anti-Inflammatory Activity of Essential Oils)
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19 pages, 1904 KiB  
Review
Research Progress on the Isolation, Purification, Structural Characteristics and Biological Activity Mechanism of Pleurotus citrinopileatus Polysaccharides
by Zixu Liu and Honglei Wang
Molecules 2025, 30(13), 2816; https://doi.org/10.3390/molecules30132816 - 30 Jun 2025
Viewed by 243
Abstract
Pleurotus citrinopileatus, a valuable edible fungus characterized by its distinctive light yellow coloration and saprophytic growth on elm wood, has garnered increasing scientific interest due to its diverse bioactive constituents. Among these, polysaccharides derived from P. citrinopileatus (PCPs) have received the most [...] Read more.
Pleurotus citrinopileatus, a valuable edible fungus characterized by its distinctive light yellow coloration and saprophytic growth on elm wood, has garnered increasing scientific interest due to its diverse bioactive constituents. Among these, polysaccharides derived from P. citrinopileatus (PCPs) have received the most extensive research attention. This review summarizes recent advances in the chemical structure and biological activities of PCPs. Structurally, PCPs are primarily composed of repeating units such as →3)-α-D-Glcp-(1→ and →6)-α-D-Galp-(1→. Functionally, PCPs exhibit a range of bioactivities, including immunomodulatory, hypoglycemic, and antitumor effects. Furthermore, the underlying mechanisms associated with these biological activities are also explored. This review aims to provide a comprehensive reference for future studies and facilitate the development and application of PCPs as potential functional food ingredients or therapeutic agents. Full article
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26 pages, 561 KiB  
Review
Probiotics as Antioxidant Strategy for Managing Diabetes Mellitus and Its Complications
by Max Denisson Maurício Viana, Sthefane Silva Santos, Anna Beatriz Oliveira Cruz, Maria Vitória Abreu Cardoso de Jesus, Pedro Santana Sales Lauria, Marvin Paulo Lins and Cristiane Flora Villarreal
Antioxidants 2025, 14(7), 767; https://doi.org/10.3390/antiox14070767 - 22 Jun 2025
Viewed by 656
Abstract
Diabetes mellitus (DM) is a chronic metabolic disorder characterized by impaired glycemic regulation and persistent hyperglycemia, which drives the onset of microvascular complications such as diabetic neuropathy and nephropathy. Chronic hyperglycemia activates oxidative stress pathways and alters gut microbiota composition, both of which [...] Read more.
Diabetes mellitus (DM) is a chronic metabolic disorder characterized by impaired glycemic regulation and persistent hyperglycemia, which drives the onset of microvascular complications such as diabetic neuropathy and nephropathy. Chronic hyperglycemia activates oxidative stress pathways and alters gut microbiota composition, both of which contribute to disease progression. In this context, probiotics have emerged as promising therapeutic agents due to their ability to modulate oxidative stress, improve glycemic control, and influence gut microbial balance. This review summarizes preclinical and clinical evidence supporting the antioxidant potential of probiotics in DM management, with a focus on underlying mechanisms. Strains from the Lactobacillus and Bifidobacterium genera are the most extensively studied and have demonstrated hypoglycemic and antioxidant effects, including the enhancement of key antioxidant enzymes and reductions in lipid peroxidation and nitrosative stress markers. Probiotics have also shown beneficial effects in DM-associated complications, particularly diabetic neuropathy and nephropathy. While clinical data are still limited, recent findings underscore oxidative stress as a critical therapeutic target influenced by probiotic interventions. Overall, current evidence supports probiotics as a complementary strategy for managing DM and its complications, highlighting the need for further well-designed clinical trials exploring diverse strains, formulations, and dosing regimens. Full article
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15 pages, 2608 KiB  
Article
Effect of Sugarcane Polyphenol Extract on α-Amylase Inhibition and Mechanism Exploration
by Yumei Wang, Jiulong An, Shenghong Yao, Chengfeng Zhang, Yanv Zhou, Lu Li and He Li
Foods 2025, 14(13), 2174; https://doi.org/10.3390/foods14132174 - 21 Jun 2025
Viewed by 452
Abstract
Although α-amylase is crucial for postprandial glucose control, existing inhibitors present various side effects, necessitating the exploration of natural alternatives. The ability of sugarcane polyphenol (SP) to inhibit α-amylase remains unclear. This study assessed the inhibitory activity of SP via in vitro assays, [...] Read more.
Although α-amylase is crucial for postprandial glucose control, existing inhibitors present various side effects, necessitating the exploration of natural alternatives. The ability of sugarcane polyphenol (SP) to inhibit α-amylase remains unclear. This study assessed the inhibitory activity of SP via in vitro assays, circular dichroism (CD), fluorescence quenching, and stability analysis, while the mechanism of action was elucidated using molecular docking and molecular dynamics (MD). The results showed that the IC50 of the SP was 0.841 ± 0.029 mg/mL, with proanthocyanidin-B1 (PC-B1) presenting the most potent effect (IC50 = 0.504 ± 0.019 mg/mL). CD and barycentric mean (BCM) analysis indicated that the complexes might limit substrate binding. The mechanistic assessment showed that the polyphenols bonded to the active enzyme pockets to form stable complexes with reduced key residue fluctuations. In conclusion, SP, especially PC-B1, effectively inhibited α-amylase activity via structural regulation and molecular interactions, providing a theoretical basis for developing natural hypoglycemic agents. Full article
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22 pages, 3876 KiB  
Article
In Vivo PK-PD and Drug–Drug Interaction Study of Dorzagliatin for the Management of PI3Kα Inhibitor-Induced Hyperglycemia
by Guanqin Jin, Kewei Zheng, Shihuang Liu, Huan Yi, Wei Wei, Congjian Xu, Xiaoqiang Xiang and Yu Kang
Pharmaceuticals 2025, 18(6), 927; https://doi.org/10.3390/ph18060927 - 19 Jun 2025
Viewed by 476
Abstract
Objectives: The anticancer effects of PI3Kα inhibitors (PI3Ki) are constrained by their hyperglycemic side effects, while the efficacy of conventional hypoglycemic agents, such as insulin, metformin, and SGLT-2 inhibitors, in mitigating PI3Ki-induced hyperglycemia remains suboptimal. Dorzagliatin, a novel glucokinase activator, has been approved [...] Read more.
Objectives: The anticancer effects of PI3Kα inhibitors (PI3Ki) are constrained by their hyperglycemic side effects, while the efficacy of conventional hypoglycemic agents, such as insulin, metformin, and SGLT-2 inhibitors, in mitigating PI3Ki-induced hyperglycemia remains suboptimal. Dorzagliatin, a novel glucokinase activator, has been approved in China for the management of hyperglycemia, offering a promising alternative. This study aims to investigate the pharmacokinetic properties and potential mechanisms of drug interactions of dorzagliatin in the regulation of PI3K-induced hyperglycemia. Methods: Plasma concentrations of WX390, BYL719, and Dorz in mice were measured using high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. Pharmacokinetic (PK) parameters and PK/PD models were derived by using Phoenix WinNonlin 8.3.5 software. Blood glucose levels at various time points and tumor volume changes over a four-week period were assessed to explore the interactions when PI3Ki were combined with dorzagliatin. Results: The results indicated that, compared to the Dorz group, the combination groups (Dorz + BYL719, Dorz + WX390) exhibited increases in AUC0t of dorzagliatin by 41.65% and 20.25%, and in Cmax by 33.48% and 13.32%, respectively. In contrast, co-administration of these PI3Ki with dorzagliatin resulted in minimal increase in their plasma exposure. The combination therapy group (Dorz+BYL719) exhibited superior antitumor efficacy compared to the BYL719 group. Conclusions: Our findings indicate that the drug–drug interactions (DDIs) between dorzagliatin and multiple PI3Ki (including WX390 and BYL719) may partially account for the enhanced antitumor efficacy observed in the combination therapy group compared to PI3Ki monotherapy. This interaction may be explained by the inhibition of P-glycoprotein (P-gp) and the pharmacological mechanism of dorzagliatin regarding the activation of insulin regulation. Full article
(This article belongs to the Special Issue Mathematical Modeling in Drug Metabolism and Pharmacokinetics)
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18 pages, 1864 KiB  
Article
Effect of Chronic Administration of Justicia secunda Vahl in Mice Diabetized with Streptozotocin
by Tomás Fregoso-Aguilar, Perla Xóchitl Escamilla-Ramírez, Dulce E. Nicolás-Álvarez, Jorge Alberto Mendoza-Pérez, Eduardo Osiris Madrigal-Santillán, Judith Margarita Tirado-Lule, Elda Victoria Rodríguez-Negrete, Eduardo Madrigal-Bujaidar, Isela Álvarez-González, Gabriela Ibáñez-Cervantes, Ángel Morales-González and José A. Morales-Gonzalez
Diabetology 2025, 6(6), 56; https://doi.org/10.3390/diabetology6060056 - 18 Jun 2025
Viewed by 506
Abstract
Certain pharmacological properties of the methanolic extract of Justicia secunda Vahl leaves (Acanthaceae) were evaluated in Streptozotocin (STZ)-treated albino mice to confirm whether it could be considered an alternative candidate for the treatment of diabetes. Using qualitative phytochemistry, alkaloids, flavonoids, and [...] Read more.
Certain pharmacological properties of the methanolic extract of Justicia secunda Vahl leaves (Acanthaceae) were evaluated in Streptozotocin (STZ)-treated albino mice to confirm whether it could be considered an alternative candidate for the treatment of diabetes. Using qualitative phytochemistry, alkaloids, flavonoids, and tannins were detected. In an in vitro DPPH antioxidant activity test, high extract concentrations inhibited the radical by 90% during the first minutes of the reaction. The extract presented a slight genoprotective effect on mouse peripheral blood during the last days of the micronucleus test. Oral administration of the extract at a high dose every two days for 6 weeks caused a hypoglycemic effect in STZ-treated mice, protection against weight loss, and decreased blood triglyceride levels from week 3 of treatment. These effects could be mediated by the antioxidant activity of the detected metabolites and, perhaps, by an inhibitory effect on intestinal α-glucosidase. This renders J. secunda a good candidate for the long-term alternative treatment of diabetes without abandoning allopathic therapy. Full article
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