Search Results (1,491)

Polyscias fruticosa (L.) Harms, a Southeast Asian medicinal plant of the Araliaceae family, has gained increasing attention due to its rich phytochemical profile and potential pharmacological applications. This review provides an up-to-date synthesis of biotechnological strategies and chemical investigations related to this species. In vitro propagation methods, including somatic embryogenesis, adventitious root, and cell suspension cultures, are discussed with emphasis on elicitation and bioreactor systems to enhance the production of secondary metabolites. Phytochemical analyses using gas chromatography–mass spectrometry (GC-MS), high-performance liquid chromatography (HPLC), and nuclear magnetic resonance (NMR) have identified over 120 metabolites, including triterpenoid saponins, polyphenols, sterols, volatile terpenoids, polyacetylenes, and fatty acids. Several compounds, such as tocopherols, conjugated linoleic acids, and alismol, were identified for the first time in the genus. These constituents exhibit antioxidant, anti-inflammatory, antimicrobial, antidiabetic, anticancer, and neuroprotective activities, with selected saponins (e.g., chikusetsusaponin IVa, Polyscias fruticosa saponin [PFS], zingibroside R1) showing confirmed molecular mechanisms of action. The combination of biotechnological tools with phytochemical and pharmacological evaluation supports P. fruticosa as a promising candidate for further functional, therapeutic, and nutraceutical development. This review also identifies knowledge gaps related to compound characterization and mechanistic studies, suggesting future directions for interdisciplinary research. Full article

Chaya leaf has long been used in folk medicine and is gaining scientific interest for its potential role in diabetes management. Recent research indicates that chaya leaf may help to regulate glucose, enhance insulin secretion, and reduce related complications, primarily due to the presence of bioactive compounds such as polyphenols and flavonoids. These compounds are believed to enhance insulin sensitivity and offer protection against oxidative stress, a key contributor to diabetes-related complications. Chaya extracts, particularly methanolic and aqueous forms, have shown anti-diabetic effects in animal models, lowering blood glucose, cholesterol, and triglycerides and reducing inflammation; their bioactive compounds, like quercetin, rutin, and ferulic acid, may enhance the insulin response, reduce inflammation, and improve antioxidant activity. Some studies warn of potential interactions with metformin. This review compiles findings from the past five years, drawing from databases such as PubMed, SciELO, ScienceDirect, Dialnet, Web of Science, and Google Scholar. It highlights chaya’s phytochemical profile, explores proposed anti-diabetic mechanisms, and summarizes evidence from in vivo, in vitro, and clinical studies. The results indicate that adding chaya leaf to the diet may help people with diabetes as a complementary therapy to conventional treatment; nonetheless, further clinical studies are required to comprehend the exact mechanisms and define specific usage instructions. Further investigation into the specific types of compounds present in chaya, their effective dosages, and their safety in human populations is essential to support its integration into medical practice. Full article

This review explores the therapeutic potential of Allium cepa (onion) and Allium sativum (garlic), focusing specifically on their antidiabetic, cardioprotective, and antibacterial effects. These widely used medicinal plants are rich in bioactive compounds that contribute to their broad spectrum of pharmacological activities. Based on over two decades of scientific literature, this review synthesizes findings from more than 20 years of research to highlight the efficacy of these plant extracts. Rising chronic disease rates and antimicrobial resistance have renewed interest in plant-derived therapies; in the UAE context, Allium cepa and Allium sativum are promising candidates for integrative, sustainable interventions. This review further elucidates the mechanisms through which those bioactive constituents exert therapeutic effects, current extraction strategies, and challenges in enhancing formulations for functional health applications. Additionally, it addresses their role in sustainable healthcare practices due to their renewable nature and minimal environmental impact compared to synthetic pharmaceuticals. Full article

Carnivorous plants have garnered attention as sources of pharmacologically active compounds, yet their floral tissues remain largely underexplored. In this study, we investigated the bioactive properties of Nepenthes miranda flower extracts prepared using water, methanol, ethanol, and acetone. Among these, the ethanol extract exhibited the highest total phenolic content (18.2 mg GAE/g), flavonoid content (68.9 mg QUE/g), and antioxidant activity (DPPH IC₅₀ = 66.9 μg/mL), along with strong antibacterial effects against Escherichia coli and Staphylococcus aureus. Cosmetically relevant enzyme inhibition assays revealed significant activity against tyrosinase (IC₅₀ = 48.58 μg/mL), elastase (IC₅₀ = 1.77 μg/mL), and hyaluronidase (IC₅₀ = 7.33 μg/mL), supporting its potential as an anti-skin aging agent. For antidiabetic evaluation, the ethanol extract demonstrated potent α-glucosidase inhibition (IC₅₀ = 24.53 μg/mL), outperforming standard inhibitors such as acarbose and quercetin. The extract also displayed marked cytotoxicity against A431 epidermoid carcinoma cells (IC₅₀ = 90.61 μg/mL), inducing dose-dependent apoptosis, inhibiting cell migration and colony formation, and causing significant DNA damage as shown by comet assay. Furthermore, the ethanol extract strongly inhibited the activity of purified human dihydroorotase (IC₅₀ = 25.11 μg/mL), indicating that disruption of pyrimidine biosynthesis may underlie its anticancer activity. Overall, this study provides the first characterization of N. miranda flower extracts, particularly the ethanol fraction, as a promising source of multifunctional bioactive compounds with possible applications in cosmetics, antidiabetic therapy, and cancer treatment. Full article

Background/Objectives: Pain is a growing public health concern worldwide, and the use of combinations of drugs can improve their analgesic effects while minimizing their adverse effects. Drugs such as metformin (antidiabetic) and melatonin (sleep regulator) have analgesic potential in combination. In this study, we evaluated the pharmacological interaction between metformin and melatonin when orally administered in a rat model, using the formalin test. Methods: Female Wistar rats (220–350 g) were injected with 50 µL of 1% formalin in the dorsal surface of the right hind paw. Formalin produces pain-related flinching behavior, and antinociception was evaluated as the reduction in this response. The percentage of the antinociceptive effect was determined after the oral administration of metformin (30–1000 mg/kg), melatonin (10–150 mg/kg), and their combination (MMC). To establish the nature of the interaction, isobolographic analysis was performed in a fixed-dose ratio (0.5:0.5), based on the effective dose 50 (ED₅₀) values for each drug: metformin (947.46 ± 242.60 mg/kg) and melatonin (126.86 ± 37.98 mg/kg). To evaluate the mechanism of action, the receptor antagonist for metformin compound C (dorsomorphin) for AMPK inhibition, MT1 and MT2 melatonin receptor antagonists (4-P-PDOT, luzindole), and an opioid antagonist (naloxone) were employed. The rotarod test was used to evaluate the safety profile of the combination. Results: The metformin–melatonin combination significantly reduced the number of flinches in the second phase of the formalin test. The theoretical ED₅₀ for the combination (ED₅₀ T) was 537.15 ± 122.76 mg/kg. Experimentally, the ED₅₀ (ED₅₀ E) was significantly lower (360.83 ± 23.36 mg/kg), indicating a synergistic interaction for the combination involving opioidergic pathways, MT2 receptors, and AMPK activation. Conclusions: Oral metformin–melatonin coadministration could provide a therapeutic alternative for inflammatory pain. Full article

Background: Artocarpus heterophyllus, familiar as jackfruit, is a tropical fruit highly valued not only for its nutritional content but also for its medicinal properties, including potential antidiabetic effects. Objectives: This study aimed to evaluate the insulinotropic, β-cell proliferative and anti-hyperlipidaemic properties of the ethanol extract of unripe Artocarpus heterophyllus (EEAH) in high-fat-fed (HFF) diet-induced obese mice. Method: We evaluated acute insulin secretion and β-cell proliferation in BRIN-BD11 cells, and assessed in vitro glucose diffusion and starch digestion. In vivo, acute and chronic studies in HFF induced obese mice measured glucose tolerance, body weight, food and fluid intake, and lipid profiles. A preliminary phytochemical screening was also performed. Results: In this study, EEAH exhibited significant antidiabetic activity through multiple mechanisms. EEAH enhanced glucose-stimulated insulin secretion in BRIN-BD11 β-cells via K_ATP channel modulation and cAMP-mediated pathways, with partial dependence on extracellular calcium, and it also promoted β-cell proliferation. In vitro assays revealed its ability to inhibit starch digestion and glucose diffusion, indicating delayed carbohydrate digestion and absorption. In high-fat-fed (HFF) obese mice, the acute and chronic oral administration of EEAH improved oral glucose tolerance, reduced fasting blood glucose, decreased body weight, and normalized food and fluid intake. Lipid profile analysis showed increased HDL and reduced total cholesterol, LDL, and triglycerides, while higher doses of EEAH also enhanced gut motility. Phytochemical screening revealed the presence of bioactive compounds such as alkaloids, tannins, flavonoids, saponins, steroids, and terpenoids, which are likely responsible for these therapeutic effects. Conclusion: These findings highlight EEAH as a promising natural candidate for adjunctive therapy in managing type 2 diabetes and associated metabolic disorders and emphasize the importance of future multi-omics studies to elucidate its molecular targets and pathways. Full article

Studies utilizing cell-based systems to investigate plant-based diets for diabetes management are gaining attention due to the adverse effects associated with commercially available drugs. However, the molecular mechanisms underlying the anti-diabetic effects of specific plant-derived products remain inadequately explored. The major aim of our study was to elucidate the molecular mechanisms by which bioactive compounds in the fruit of Solanum spp. influence key proteins associated with type 2 diabetes. The expressions of genes such as glucose transporter protein 4 (GLUT4), myocyte enhancer factor-2 (MEF-2A), and nuclear respiratory factor-1 (NRF-1) were investigated in a palmitate-induced C2C12 cell model of type 2 diabetes mellitus. The structures of these proteins were retrieved from the protein database, while bioactive compounds previously identified in Solanum spp. were obtained from PubChem site. Drug-likeness properties of these compounds (ligands) were assessed. The docked protein-ligand complexes were further analyzed using the Protein-Ligand Profiler web server. Our results showed that the studied compounds from Solanum spp. profoundly upregulated GLUT4 expression (9–19-fold increase) in the C2C12 cell line, thus surpassing the effects of the standard anti-diabetic drug metformin. Additionally, activities of antioxidant enzymes catalase, superoxide dismutase, and glutathione peroxidase were elevated. Molecular docking showed that rutin, an abundant flavonoid from Solanum spp., had the highest binding affinity for the active sites of the target proteins. These findings provide new mechanistic insight into the anti-diabetic effects of Solanum spp., primarily due to its high rutin content, which plays a major role in the plant’s glucose-regulating and antioxidant actions. Our findings underscore the potential use of Solanum spp. as an affordable functional food for managing type 2 diabetes, especially in developing countries with limited resources for purchasing drugs. Although promising, our findings should be further validated by clinical studies. Full article

Amelanchier alnifolia is a plant known for its nutritional and bioactive properties. Its leaves contain a high concentration of active compounds with significant antioxidant and antidiabetic effects, including strong α-glucosidase inhibitory potential. The combination of these bioactive leaf extracts with prebiotic substances, such as fructooligosaccharides (FOS), galactooligosaccharides (GOS), and chitooligosaccharides (COS), enables the development of functional systems with enhanced beneficial properties. In this study, process optimization for leaves extraction was performed using a Plackett–Burman screening design, which identified key parameters for further optimization using the Box–Behnken design. The optimal extraction conditions were determined as follows: methanol content 58.06%, solid-to-solvent ratio 26.03 m/v, and extraction time 73.56 min. These conditions yielded the highest the total phenolic content (TPC). A comparative analysis of different cultivars revealed significant variations in polyphenol content among them. The formulated lyophilized systems with GOS, FOS and COS positively influenced the chlorogenic acid release profile, while maintaining the extract’s antidiabetic and antioxidant properties. FT-IR analysis confirmed the molecular interactions responsible for these effects. The prebiotic effectiveness of the systems was quantitatively evaluated using two key parameters: the prebiotic index (PI), and the prebiotic activity score (PAS). Microbiological analyses demonstrated the beneficial effects of prebiotic-enriched systems characterized by better prebiotic action on Bifidobacterium strains than the pure extract. These findings suggest that A. alnifolia leaf extracts, in combination with prebiotics, could serve as promising functional ingredients with potential applications in health-promoting and antidiabetic formulations. Full article

Plant-derived pharmaceuticals represent a highly compelling area of research and continue to attract significant interest from countries, regions, scientific communities, and pharmaceutical companies worldwide. Among these, α- and β-amyrins have been identified as high-value triterpenoid compounds with a broad spectrum of potential therapeutic properties, including anti-inflammatory, antidiabetic, antiatherosclerotic, analgesic, antigout, neuroprotective, anti-Parkinsonian, anticancer, antibacterial, and anti-HIV activities. Relevant information and data were obtained through comprehensive searches of major scientific databases, including Web of Science, Elsevier, and the National Library of Medicine. This study highlighted the pharmaceutical potential of α- and β-amyrins, supported by specific evidence from in vivo, in vitro, and clinical trials. Various extraction methods for α- and β-amyrins are discussed, followed by recommendations for future directions in the development of these compounds as pharmaceutical agents and functional food ingredients. This review highlights the therapeutic of α- and β-amyrin compounds in the prevention and treatment of various serious diseases worldwide, potentially opening new opportunities and directions for the pharmaceutical industry. Full article

The search for natural sources of bioactive compounds with health-promoting properties has intensified in recent years. Among these, Tannat grape pomace (TGP), a primary byproduct of winemaking, stands out for its high phenolic content, although its bioactivity may be affected during gastrointestinal digestion. This study aimed to evaluate the impact of in vitro digestion on the antioxidant (ABTS, ORAC-FL, intracellular ROS inhibition), anti-diabetic (α-glucosidase inhibition), anti-obesity (lipase inhibition), and anti-inflammatory (NO inhibition) properties of five sugar-free biscuits formulated with varying percentages of TGP and sucralose. No significant differences were observed in the bioaccessible fractions (BFs, representing the compounds potentially released in the small intestine) between control biscuits and those enriched with TGP, suggesting limited release of phenolics at this stage. Conversely, the colonic fractions (CFs, simulating the material reaching the colon) from biscuits with higher TGP content exhibited greater bioactivities. HPLC-DAD-MS analysis of the CF from the biscuit containing 20% TGP and 4% sucralose revealed a high content of procyanidin trimers, indicating the persistence of these specific phenolic compounds after in vitro digestion. These findings suggest that TGP-enriched biscuits may deliver health benefits at the colonic level and support their potential application in the formulation of functional foods. Further microbiota and in vivo studies should be assessed to confirm the latter. Full article

After the first release of synthalin B (dodecamethylenbiguanide) in 1928 and its later retraction in the 1940s in Germany, the retraction of phenformin (N-Phenethylbiguanide) and of Buformin in the USA (but not outside) because of the lethal complication of acidosis seemed to have put an end to the era of the biguanides as oral antidiabetics. The strongly hygroscopic metformin (1-1-dimethylbiguanide), first synthesized 1922 and resuscitated as an oral antidiabetic (type 2 of the elderly) compound first released in 1959 in France and in other European countries, was used in the first large multicenter prospective long-term trial in England in the UKPDS (1977–1997). It was then released in the USA after a short-term prospective trial in healthy overweight “young” type 2 diabetics (mean age 53 years) in 1995 for oral treatment of type 2 diabetes. It was, however, prescribed to mostly multimorbid older patients (above 60–65 years of age). Metformin is now the most used oral drug for type 2 diabetes worldwide. While intravenous administration of biguanides does not have any glucose-lowering effect, their oral administration leads to enormous increase in their intestinal concentration (up to 300-fold compared to that measured in the blood), to reduced absorption of glucose from the diet, to increased excretion of glucose through the stool, and to decrease in insulin serum level through increased hepatic uptake and decreased production. Intravenously injected F18-labeled glucose in metformin-treated type 2 diabetics accumulates in the small and even more in the large intestine. The densitometry picture observed in metformin-treated overweight diabetics is like that observed in patients after bowel-cleansing or chronically taking different types of laxatives, where the accumulated radioactivity can even reach values observed in colon cancer. The glucose-lowering mechanism of action of metformin is therefore not only due to inhibition of glucose uptake in the small intestine but also to “attraction” of glucose from the hepatocyte into the intestine, possibly through the insulin-mediated uptake in the hepatocyte and its secretion into the bile. Furthermore, these compounds have also a diuretic effect (loss of sodium and water in the urine) Acute gastrointestinal side effects accompanied by fluid loss often lead to the drugs’ dose reduction and strongly limit adherence to therapy. Main long-term consequences are “chronic” dehydration, deficiency of vitamin B12 and of iron, and, as observed for all the biguanides, to “chronic” increase in fasting and postprandial lactate plasma level as a laboratory marker of a clinical condition characterized by hypotension, oliguria, adynamia, and evident lactic acidosis. Metformin is not different from the other biguanides: synthalin B, buformin, and phenformin. The mechanism of action of the biguanides as antihyperglycemic substances and their side effects are comparable if not even stronger (abdominal pain, nausea, vomiting, diarrhea, fluid loss) to those of laxatives. Full article

Quercetin is a biologically active flavonoid compound that exerts numerous beneficial effects in humans and animals, including anti-diabetic activity. Its action has been explored in rodent models of type 1 and type 2 diabetes. It was revealed that quercetin mitigated diabetes-related hormonal and metabolic disorders and reduced oxidative and inflammatory stress. Its anti-diabetic effects were associated with advantageous changes in the relevant enzymes and signaling molecules. Quercetin positively affected, among others, superoxide dismutase, catalase, glutathione peroxidase, glucose transporter-2, glucokinase, glucose-6-phosphatase, glycogen phosphorylase, glycogen synthase, glycogen synthase kinase-3β, phosphoenolpyruvate carboxykinase, silent information regulator-1, sterol regulatory element-binding protein-1, insulin receptor substrate 1, phosphoinositide 3-kinase, and protein kinase B. The available data support the conclusion that the action of quercetin was pleiotropic since it alleviates a wide range of diabetes-related disorders. Moreover, no side effects were observed during treatment with quercetin in rodents. Given that human diabetes affects a large part of the population worldwide, the results of animal studies encourage clinical trials to evaluate the potential of quercetin as an adjunct to pharmacological therapies. Full article

The Pelargonium genus, encompassing over 280 species, remains markedly underexplored despite extensive traditional use for respiratory, gastrointestinal, and dermatological disorders. This review of aqueous, alcoholic, and hydroalcoholic extracts reveals critical research gaps: only 10 species have undergone chemical characterization, while 17 have been evaluated for biological activities. Phytochemical analysis identified 252 unique molecules across all studies, with flavonoids emerging as the predominant class (n = 108). Glycosylated derivatives demonstrated superior bioactivity profiles compared to non-glycosylated analogs. Phenolic acids (n = 43) and coumarins (n = 31) represented additional major classes. Experimental studies primarily documented antioxidant, antibacterial, and anti-inflammatory effects, with emerging evidence for antidiabetic, anticancer, and hepatoprotective activities. However, methodological heterogeneity across studies limits comparative analysis and comprehensive understanding. In silico target prediction analysis was performed on 197 high-confidence molecular structures. Glycosylated flavonols, anthocyanidins, flavones, and coumarins showed strong predicted interactions with key inflammatory targets (ALOX15, ALOX5, PTGER4, and NOS2) and metabolic regulators (GSK3A and PI4KB), providing mechanistic support for observed therapeutic effects and suggesting potential applications in chronic inflammatory and metabolic diseases. These findings underscore the substantial therapeutic potential of underexplored Pelargonium species and advocate for systematic research employing untargeted metabolomics, standardized bioassays, and compound-specific mechanistic validation to fully unlock the pharmacological potential of this diverse genus. Full article

Swertiamarin (SW), a natural iridoid glycoside primarily isolated from the genus Swertia, Gentianaceae family, has been extensively utilized in traditional medicine systems, including Ayurveda, Traditional Chinese Medicine, and Tibetan medicine, for treating fever, diabetes, liver disorders, and inflammatory conditions. Pharmacokinetic studies reveal that SW exhibits rapid absorption but demonstrates low oral bioavailability due to the first-pass effect. Pharmacological studies have demonstrated that SW possesses a wide range of pharmacological activities, including antioxidant, anti-inflammatory, anti-tumor, anti-diabetic, and neuroprotective activities. Our analysis demonstrates that SW exerts remarkable therapeutic potential across multiple pathological conditions through coordinated modulation of key signaling cascades, including Nrf2/HO-1, NF-κB, MAPK, PI3K/Akt, and PPAR pathways. This comprehensive review systematically consolidates current knowledge on SW’s pharmacokinetic characteristics, toxicity, diverse biological activities, and underlying molecular mechanisms based on extensive preclinical evidence, establishing a scientific foundation for future drug development strategies and potential clinical applications of the potential natural lead compound. Full article

The genera Allium (Liliaceae) and Anchusa (Boraginaceae) are flowering plant genera with a rich diversity, also including the Allium kharputense Freyn & Sint. and Anchusa azurea Mill. var. azurea species. The antioxidant, anti-Alzheimer’s disease (AD), antidiabetic, and antiglaucoma effects of the Allium kharputense Freyn & Sint. and Anchusa azurea Mill. var. azurea species, which are commonly eaten foods in the Southeast of Türkiye in the treatment of several diseases, were studied. To interpret the antioxidant capacities of ethanol extract of two plant species, aerial parts were analyzed by ABTS and DPPH assays. The IC₅₀ values of A. kharputense and A. azurea ethanol and water extracts for ABTS^•+ activities were recorded in the range of 30.93 to 33.94 µg/mL and 33.45 to 33.78 µg/mL, respectively. Also, DPPH^• activities were measured at 30.78 to 36.87 µg/mL and 31.67 to 32.45 µg/mL, respectively. The best of the IC₅₀ values was measured in the ethanol extract of A. kharputense as 30.78 µg/mL for DPPH scavenging activity. The total phenolic and flavonoid quantities in A. kharputense and A. azurea plants were measured. The highest phenolic and flavonoid contents of A. kharputense and A. azurea species were recorded in amounts of 445.52 and 327.35 mg GAE/g in ethanol extracts, respectively, and 332.88 and 234.03 mg QE/g in ethanol extracts, respectively. The effects of A. kharputense and A. azurea on diabetes, AD, and glaucoma were studied on the target enzymes of diseases. The most efficient IC₅₀ values were recorded at 10.72 μg/mL against α-glycosidase, 35.01 μg/mL against AChE, 38.05 μg/mL against BChE, 9.21 μg/mL towards hCA I, and 81.02 μg/mL towards hCA II isoenzymes. The kinds and amounts of phenolic compounds in A. kharputense and A. azurea were determined using LC-MS/MS against 53 standards. A. kharputense and A. azurea plants have prospective use in enhancing glaucoma, diabetes, AD, Parkinson’s disease, epilepsy, and cancerous disorders. Full article