Significant Antidiabetic Activity Research Articles

Synthesis, Crystal Structure, Spectroscopic Characterization, In Vitro and In Silico Molecular Docking Studies of Benzyl Tetrazole-N-Isobutyl Acetamide Hybrid

Background: Tetrazole-based compounds are of significant interest due to their potential pharmacological applications. The current study focuses on the synthesis and analysis of such a compound. Objective: This research aims to synthesize the title compound N-(3-methyl-1-phenyl-2-(1Htetrazol- 1-yl) butyl) acetamide, analyze its crystal structure, perform computational studies, and evaluate its potential pharmacological activities and it’s in silico and in vitro supports, specifically antidiabetic and anti-inflammatory properties. Methods: The title compound, C14H19N5O, was synthesized, and its crystal structure was confirmed using single-crystal X-ray diffraction analysis by default parameters. Density Functional Theory (DFT) calculations were performed using the Gaussian 09W software package with the B3LYP/6-311++G (d,p) method to optimize the compound's structure and calculate its HOMOLUMO energy gap, Molecular Electrostatic Potential (MEP), and Mulliken charge distribution. In vitro, antidiabetic and anti-inflammatory activities were assessed and compared with standard drugs by using reported protocols. Additionally, molecular docking studies were conducted with enzymes related to diabetes and inflammation with default parameters, and Auto-Dock 4.2 software was used. Results: The X-ray diffraction analysis confirmed the crystal structure, and the Density Functional Theory (DFT) calculations provided insights into the molecular properties of the compound. Molecular docking experiments with relevant enzymes further supported the significant antidiabetic and anti-inflammatory activities demonstrated in the in vitro tests. Conclusion: The synthesized tetrazole-based compound exhibits promising antidiabetic and antiinflammatory activities, supported by both experimental and theoretical studies, suggesting its potential for further pharmacological investigation.

Identification of the Hypoglycemic Active Components of Lonicera japonica Thunb. and Lonicera hypoglauca Miq. by UPLC-Q-TOF-MS

Lonicera japonica Thunb. and Lonicera hypoglauca are famous Chinese medicines used for hyperglycemia; however, the specific compounds that contributed to the hypoglycemic activity and mechanism are still unknown. In this study, the antidiabetic activity of L. japonica buds and L. hypoglauca buds, roots, stems, and leaves extracts was primarily evaluated, and the L. japonica buds and L. hypoglauca buds, roots, and stems extracts displayed significant hypoglycemic activity, especially for the buds of L. hypoglauca. A total of 72 high-level compounds, including 9 iridoid glycosides, 12 flavonoids, 34 organic acids, and 17 saponins, were identified by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) combined with the fragmentation pathways of standards from different parts of L. japonica and L. hypoglauca extracts. Among them, 19 metabolites, including 13 saponins, were reported for the first time from both medicines. Seven high-content compounds identified from L. hypoglauca buds extract were further evaluated for hypoglycemic activity. The result indicated that neochlorogenic acid, chlorogenic acid, isochlorogenic acid A, isochlorogenic acid B, and isochlorogenic acid C displayed significant antidiabetic activity, especially for isochlorogenic acid A and isochlorogenic acid C, which demonstrated that the five chlorogenic-acid-type compounds were the active ingredients of hypoglycemic activity for L. japonica and L. hypoglauca. The potential mechanism of hypoglycemic activity for isochlorogenic acid A and isochlorogenic acid C was inhibiting the intestinal α-glucosidase activity to block the supply of glucose. This study was the first to clarify the hypoglycemic active ingredients and potential mechanism of L. japonica and L. hypoglauca, providing new insights for the comprehensive utilization of both resources and the development of hypoglycemic drugs.

Study on the extraction of Phycocyanin and the impact of in vitro simulated digestion on its anti-diabetic ability

Phycocyanin (PC) has significant anti-diabetic activity. However, research on the impact of digestion on the anti-diabetic properties of PC is still rare. In this study, we successfully extracted food-grade PC with a purity of 1.64 ± 0.06 from Ge Xian Mi. The results of antioxidant and enzyme activity inhibition experiments indicate that the biological activity of PC is positively correlated with its purity. Fluorescence and UV–Vis spectroscopy revealed the degradation of apolipoprotein and chromophore structures in PC during digestion. During digestion, the characteristic peaks of chromophores gradually disappeared, accompanied by a continuous decrease in antioxidant activity. The results of secondary structure determination indicate that after 0.5 h of digestion, the α-helix content decreased by approximately 50%, while the β-sheet content decreased by 6.87%. At the end of digestion, the α-helix structure was completely lost. The inhibitory effect of PC on the two enzymes decreased by approximately 20% after digestion started, followed by a rebound at 1.0 h, and then declined again at 3.0 h. At the end of digestion, the inhibition rates against α-amylase and α-glucosidase were only 22.09% and 25.76%, respectively. Digestion significantly decreased the antidiabetic ability of PC.

2‐Chloroquinolinyl‐thiazolidine‐2,4‐dione Hybrids as Potential α‐Amylase Inhibitors: Synthesis, Biological Evaluations, and In Silico Studies

AbstractRecently, molecular hybridization strategy has paved a way to develop novel lead compounds for the α‐amylase targeted antidiabetic therapy. In this study, we disclosed a series of new hybrids of thiazolidine‐2,4‐diones with 2‐chloroquinoline‐3‐yl moiety as potential antidiabetic agents. The molecular structures of all the synthesized hybrids (15a–n) were confirmed by spectroscopic studies (FT‐IR, ESI‐MS, 1H, 13C NMR, and elemental analysis). When in vitro antidiabetic evaluation of these agents was carried out in a dose‐dependent manner, it was revealed that several compounds (15f–h, 15j, and 15n) were endowed with significant antidiabetic activities and exhibited more than 50% α‐amylase inhibition at a dose of 50 µg/mL. Particularly, hybrid 15n was found to be more potent than acarbose with 95% inhibition of α‐amylase and IC50 of 5.00 ± 0.18 µM under given conditions. Further, it was demonstrated that 15n bearing 2‐chloroquinolinyl and thiazolidin‐2,4‐dione scaffolds functionalized with 3‐OMe and 4‐OH groups was not only able to effectively bind with α‐amylase receptor site with best docking score (−9.644 kcal/mol) but also possessed drug‐likenesses properties with no violations of Lipinski rule. Overall, this study discovered new 2‐chloroquinolinyl‐thiazolidine‐2,4‐diones hybrids as novel α‐amylase inhibitors and compound 15n as promising lead for its further development as antidiabetic agent.

Antidiabetic Potential of Nypa fruticans Fronds: Inhibition of α-Amylase, α-Glucosidase, and Glucose Absorption In Vivo

Background: Diabetes mellitus (DM) results from insulin resistance or impaired insulin secretion, leading to hyperglycemia, which, in advanced stages, causes macrovascular and microvascular complications. Effective management of postprandial hyperglycemia is critical to reducing these complications. Inhibition of carbohydrate hydrolyzing enzymes such as α-amylase and α-glucosidase offers a therapeutic approach for controlling postprandial glucose levels. While acarbose is a known inhibitor of these enzymes, its long-term use can cause gastrointestinal side effects. Therefore, alternative treatments, such as medicinal plants, are being explored. This study focuses on the antidiabetic potential of the Nipah frond (Nypa fruticans Wurmb), a traditional remedy, which is believed to inhibit glucose absorption and carbohydrate degradation. Methods; Nipah frond powder was extracted using ethanol through maceration. Phytochemical screening was conducted to detect bioactive compounds, and in vivo and in vitro assays were performed to evaluate antidiabetic properties. The inverted intestinal pouch technique assessed glucose absorption, while the Oral Glucose Tolerance Test (OGTT) was conducted on male Wistar rats. Enzyme inhibition assays for α-amylase and α-glucosidase were carried out to measure the extract's effectiveness in inhibiting carbohydrate degradation. Results: In vitro tests demonstrated that the ethanol extract exhibited inhibitory activity against both α-amylase and α-glucosidase enzymes, with IC50 values of 38.493 ± 0.900 ppm and 40.401 ± 0.558 ppm, respectively. In vivo studies using the everted sac technique showed that the extract reduced glucose absorption by 74.10% compared to the control group, similar to acarbose. In the OGTT, administration of 1000 mg/kg BW of Nipah frond extract significantly reduced postprandial glucose levels, with an area under the curve (AUC) comparable to glibenclamide. Conclusion: The ethanol extract of Nypa fruticans fronds demonstrated significant antidiabetic activity by inhibiting α-amylase and α-glucosidase, reducing glucose absorption, and suppressing postprandial hyperglycemia in vivo.

Antidiabetic activity and Safety evaluation of Triticum aestivum (wheatgrass) extract in Alloxan-induced diabetic rats model.

Triticum aestivum (wheatgrasses) extract was studied for antidiabetic activity using alloxan-induced diabetes mellitus in rats. Triticum aestivum at 50, 100, and 200 mg/kg showed significant antidiabetic activity; it effected profound reductions in blood glucose over 28 days, especially the higher doses of 100 and 200 mg/kg, which were more effective than Glibenclamide. At 2000 mg/kg, the extract did not lower the blood glucose of normoglycemic rats- an indication of its safety and lack of hypoglycemic responses under non-diabetic conditions. It would appear that the antidiabetic activity of Triticum aestivum is through the protection and regeneration of beta cells that enhance insulin secretion, which in turn increases the utilization of glucose and normalizes carbohydrate, fat, and protein metabolism. This gradual lowering of blood glucose levels brought on by Triticum aestivum is clinically highly desired. The elicited antidepressant effect of Triticum aestivum was very likely due to its antioxidant effects and beta-cell regeneration activity. Thus, Triticum aestivum can meet the demand for a nontoxic, safe alternative to orthodox antidiabetic agents. Triticum aestivum, antidiabetic activity, alloxan-induced diabetes, insulin secretion, beta-cell regeneration, glucose metabolism, safety, and Glibenclamide.

Nutritional, phytochemistry, antioxidant, and antidiabetic potentials of Hippocratea velutina (Afzel.) leaves: In vitro, ex vivo and in silico studies

BackgroundHippocratea velutina is a novel folk plant that is used for lowering blood glucose and is hence a potential source of new antidiabetic medication. Therefore, this study was designed to investigate the antidiabetic and antidiabetic potential of the methanol extract of Hippocratea velutina leaves. MethodsThe nutritional, elemental, and phytochemical properties of H. velutina leaves were investigated. 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging ability, Fe2+chelation and nitric oxide scavenging abilities, FeSO4-induced pancreatic injury parameters such as catalase, GSH, ENTPase, Na/K ATPase activities, α-glucosidase and α-amylase inhibitory activities were used to assess the antioxidant and antidiabetic properties of H. velutina leaf. Furthermore, HPLC-identified constituents of H. velutina leaf methanol extract were docked against human α-glucosidase (3TOP) and human α-amylase (1B2Y). ResultsThe results revealed that H. velutina contains protein, crude fat, flavonoids, anthraquinones, magnesium, sodium, and iron. Compared with quercetin, H. velutina significantly scavenged NO• radicals and chelated Fe2+. H. velutina exhibited a greater inhibitory effect on FeSO4-induced pancreatic injury. Furthermore, H. velutina showed a dose-dependent increase in the activity of ENTPDase and the Na/K ATPase enzyme, and it also had a significantly greater inhibitory effect on α-amylase and α-glucosidase enzymes than metformin. Computational study revealed that lutein showed the highest binding free energy to 3TOP, while apigenin offered the highest binding free energy to 1B2Y. ConclusionHippocratea velutina leaf possesses significant antioxidant and antidiabetic activities.

Molecular hybridization, synthesis, in vitro α-glucosidase inhibition, in vivo antidiabetic activity and computational studies of isatin based compounds

In the pursuit of novel antidiabetic agents, a series of isatin-thiazole derivatives (7a-7j) were synthesized and characterized using a range of spectroscopic techniques. The enzyme inhibitory activities of the target analogues were assessed using both in vitro and in vivo assays. The tested compounds 7a-7j demonstrated In vitro inhibitory potential against α-glucosidase, as indicated by their IC50 values ranging from 28.47 to 46.61 µg/ml as compared to standard drug acarbose IC50 value of 27.22 ± 2.30 µg/ml. Additionally, compounds 7d and 7i were chosen for in vivo evaluation of their antidiabetic efficacy in streptozotocin-induced diabetic Wistar rats. These compounds exhibited significant antidiabetic activity both in vitro and in vivo, compound 7d produces therapeutic effects compared to standard pioglitazone by decreasing glycaemia and triglyceride levels in diabetic animals. Furthermore, a molecular docking study was conducted to elucidate the binding interactions of the compounds within the α-glucosidase enzyme binding pocket (PDB ID 3A47) and stability was confirmed by dynamics simulation trajectories. Thus, from the above findings, it may demonstrate that isatin-thiazole hybrids constitute promising candidates in the pursuit of developing newer oral antidiabetic agents.

Chemical composition and bioactivity of Codium dwarkense collected from the earthquake crack region of Ras Muhammad National Park, Red Sea, Egypt

Ras Muhammad National Park, located at the southern tip of the Sinai Peninsula, Egypt, is well-known for its unique marine biodiversity. One interesting region of the park is the Earthquake Crack, a tidal-influenced inland cave formed by a 1968 earthquake, that known for its rich seaweed community, with dominance of Codium dwarkense. This study evaluates the bioactive compounds and bioactivities of C. dwarkense from the crack region. The sample were collected, processed, and assessed for hydrographic parameters, nutritional composition, minerals, bioactive compounds, and bioactivity. Results showed high levels of carbohydrates and significant mineral content, with potassium and calcium being predominant. C. dwarkense also showed considerable amounts of vitamin C (32.4 mg/100g), vitamin E (400 mg/100g), phenolics (250.08 mg GAE/g), and flavonoids (85.4 mg rutin/g). The HPLC profile was dominated with quercetin, apigenin, pyrogallol, zeaxanthin, and benzoic acid. The GC-MS analyses identified several fatty acids, which were dominated with Hexadecanoic acid and Oleic acid. Bioactivity assays demonstrated significant antimicrobial, antioxidant, antidiabetic, anti-inflammatory, and anticancer activities. This study highlights the influence of the unique features of the Earthquake Crack region on C. dwarkense ability to produce valuable bioactive compounds with diverse health benefits. These findings contribute to the recognition of C. dwarkense as a functional food and nutraceutical resource.

An Eco-Friendly Approach for the Synthesis of Ni/NiO/g-C3N4 Nanocomposite Using Cleome Gynandra Leaf Extract for Biomedical and Photocatalytic Applications

The (Ni/NiO)[Formula: see text]/g-C3N4 nanocomposite was green synthesized using Cleome gynandra via sol–gel method. The photocatalytic dye decomposition, antioxidant and antidiabetic activities of the nanocomposite were studied and compared with those of (Ni/NiO)[Formula: see text] and g-C3N4. The nanocomposite exhibited enhanced photocatalytic efficiency of 97% compared to (Ni/NiO)[Formula: see text] (63%) and g-C3N4 (80%) due to the synergistic effect between both the composite partners. The nanocomposite, (Ni/NiO)[Formula: see text]/g-C3N4 showed notable antioxidant activity in DPPH (IC[Formula: see text] of [Formula: see text][Formula: see text][Formula: see text]g/mL with 87.06% of inhibition at 500[Formula: see text][Formula: see text]g/mL) and ABTS (IC[Formula: see text] of [Formula: see text][Formula: see text][Formula: see text]g/mL with 88.40 % of inhibition at 500[Formula: see text][Formula: see text]g/mL) radical scavenging assays. The green synthesized nanocomposite also exhibited significant antidiabetic activity in [Formula: see text]-amylase and [Formula: see text]-glucosidase enzyme inhibition assays with the IC[Formula: see text] of [Formula: see text][Formula: see text][Formula: see text]g/mL and [Formula: see text][Formula: see text][Formula: see text]g/mL, respectively. The XRD and SEM analyses confirmed the nanocomposite formation of (Ni/NiO)[Formula: see text]/g-C3N4. The results showed that the green synthesized (Ni/NiO)[Formula: see text]/g-C3N4 has desirable dye degradation, antidiabetic and antioxidant properties. This paper presents the results of the remarkable photocatalytic dye decomposition, antidiabetic and antioxidant properties of the nanocomposite (Ni/NiO)[Formula: see text]/g-C3N4 synthesized via an eco-friendly greeny way using Cleome gynandra leaf extract which may be the first report of this kind utilizing this plant.

A Comparative Analysis on Impact of Extraction Methods on Carotenoids Composition, Antioxidants, Antidiabetes, and Antiobesity Properties in Seagrass Enhalus acoroides: In Silico and In Vitro Study.

Enhalus acoroides, a tropical seagrass, is known for its significant contribution to marine ecosystems and its potential health benefits due to bioactive compounds. This study aims to compare the carotenoid levels in E. acoroides using green extraction via ultrasound-assisted extraction (UAE) and microwave-assisted extraction (MAE) and to evaluate the biological properties of these extracts against oxidative stress, diabetes, and obesity through in silico and in vitro analyses. E. acoroides samples were collected from Manado City, Indonesia, and subjected to UAE and MAE. The extracts were analyzed using UHPLC-ESI-MS/MS to identify carotenoids, including β-carotene, lutein, lycopene, β-cryptoxanthin, and zeaxanthin. In silico analysis was conducted to predict the compounds' bioactivity, toxicity, and drug-likeness using WAY2DRUG PASS and molecular docking with CB-Dock2. The compounds C3, C4, and C7 demonstrated notable interactions, with key metabolic proteins and microRNAs, further validating their potential therapeutic benefits. In vitro assays evaluated antioxidant activities using DPPH and FRAP assays, antidiabetic properties through α-glucosidase and α-amylase inhibition, and antiobesity effects via lipase inhibition and MTT assay with 3T3-L1 cells. Results indicated that both UAE and MAE extracts exhibited significant antioxidant, antidiabetic, and antiobesity activities. MAE extracts showed higher carotenoid content and greater biological activity compared to UAE extracts. These findings suggest that E. acoroides, mainly when extracted using MAE, has promising potential as a source of natural bioactive compounds for developing marine-based antioxidant, antidiabetic, and antiobesity agents. This study supplements existing literature by providing insights into the efficient extraction methods and the therapeutic potential of E. acoroides carotenoids.

Mango peel extracts and mangiferin chromatographic Fourier-transform infrared correlation with antioxidant, antidiabetic, and advanced glycation end product inhibitory potentials using in silico modeling and in vitro assays.

Mangifera indica peels are a rich source of diverse flavonoids and xanthonoids; however, generally these are discarded. Computational studies revealed that mangiferin significantly interacts with amino acid residues of transcriptional regulators 1IK3, 3TOP, and 4f5S. The methanolic extract of Langra variety of mangoes contained the least phenol concentrations (22.6 ± 0.32 mg/gGAE [gallic acid equivalent]) compared to the chloroform (214.8 ± 0.12 mg/gGAE) and ethyl acetate fractions (195.6 ± 0.14 mg/gGAE). Similarly, the methanolic extract of Sindhri variety contained lower phenol concentrations (42.3 ± 0.13 mg/gRUE [relative utilization efficiency]) compared with the chloroform (85.6 ± 0.15 mg/gGAE) and ethyl acetate (76.1 ± 0.32 mg/gGAE) fractions. Langra extract exhibited significant α-glucosidase inhibition (IC50 0.06 mg/mL), whereas the ethyl acetate fraction was highly active (IC50 0.12 mg/mL) in Sindhri variety. Mangiferin exhibited significant inhibition (IC50 0.026 mg/mL). A moderate inhibition of 15-LOX was observed in all samples, whereas mangiferin was least active. In advanced glycation end product inhibition assay, the chloroform fraction of Langra variety exhibited significant inhibition in nonoxidative (IC50 64.4μg/mL) and oxidative modes (IC50 54.7μg/mL). It was concluded that both Langra and Sindhri peel extracts and fractions possess significant antidiabetic activities. The results suggest the potential use of peel waste in the management and complications of diabetes.

Antibacterial, Antidiabetic, Antioxidant and DNA cleavage studies of novel N(3-(bis(pyridine-2ylmethyl)amino)-2-hydroxypropyl) benzene sulphonamide ligand

The novel N (3-(bis(pyridine-2ylmethyl)amino)-2-hydroxypropyl) benzene sulphonamide ligand have been synthesized from 1,3-Diamino-propan-2-ol. The structure of the ligand was confirmed by Mass spectroscopy and 1H NMR spectroscopy. The synthesized Schiff base ligand was tested for their in vitro anti bacterial action with Gram-positive and negative bacteria. The anti-diabetic activities have been tested with α-amylase inhibition method and antioxidant effect of the compound was established using DPPH method. Thus all the studies reveals that the synthesised Schiff base compound has significant antibacterial, antidiabetic and antioxidant activities. The DNA cleavage studies shown that, the DNA binding nature of the ligand was appreciably good. The Molecular docking characteristics were supported that the binding approach of the effective inhibitors with the active site of enzymes.

Exploring the Therapeutic Potential of Lepidagathis pungens Nees Extracts as Novel Therapy Options in Streptozotocin and Nicotinamide-Induced Diabetes in Albino Wistar Rats

Diabetes mellitus remains a global health concern, necessitating innovative therapeutic approaches. This study explores the antidiabetic potential of aqueous and methanol extracts from Lepidagathis pungens Nees in albino Wistar rats induced with diabetes. Diabetes induction involves the administration of streptozotocin (STZ) and nicotinamide (NIC), mimicking pathological conditions observed in human diabetes. The study employed aqueous and methanol extracts of L. pungens Nees alongside a standard drug, glibenclamide. Diabetes induction was achieved through intraperitoneal injection of STZ and NIC. Extracts and the standard drug were orally administered, and various parameters, including blood glucose levels, body weight changes, insulin and hemoglobin levels, as well as liver and lipid profiles, were monitored at specified intervals. Furthermore, liver and pancreas tissues were evaluated histopathologically. In comparison to the diabetic group, both aqueous and methanol extracts demonstrated significant antidiabetic activity (p <0.001), with effects comparable to or better than the standard drug. A remarkable improvement in insulin and hemoglobin levels was observed, along with significant improvements in blood glucose levels and body weight changes. Furthermore, the extracts demonstrated positive effects on liver and lipid profiles, exhibiting potential to mitigate diabetes-induced complications. Histopathological studies revealed protective effects on liver and pancreas tissues, supporting the extracts’ therapeutic efficacy. In STZ- and NIC-induced diabetic rats, L. pungens Nees extracts show promising antidiabetic activity. The extracts demonstrated significant improvements in various physiological parameters, suggesting their potential as alternative or adjunctive therapies in the management of diabetes. Further research and clinical investigations are warranted to elucidate the underlying mechanisms and translate these findings into practical therapeutic applications.

Evaluation of Anti-Diabetic Activity of Datura Stramonium Leaves Extract in Diabetic Swiss Albino Mice

INTRODUCTIONDiabetes mellitus is defined as the increase in blood glucose levels associated with a relative insulin deficiency, insulin resistance or both. Datura stramonium is commonly known as Jimson weed or Datura belongs to family Solanaceae containing different types of alkaloids, saponins, tannins, steroids, flavonoids, phenols and glycosides. MATERIAL AND METHODSExtraction was done by maceration process using ethanol as solvent. Swiss albino mice of 20-35 gram were taken as study animal. Diabetes was induced by using Alloxan 20 mg/kg body weight and Glibenclamide 10 mg/kg body weight was used as standard. Ethanolic extract of low dose (50 mg/kg) and high dose (100 mg/kg) were subjected for Anti-diabetic activity. RESULTSThe extract treated 50 mg/kg, 100 mg/kg and standard 10 mg/kg showed highly significant reduction in blood glucose level (BGL) on 21st and 28th day respectively when compared to negative control group. Extract treated 100 mg/kg showed significant improvement on high density lipoprotein when compared to negative control group. Extract treated 50 mg/kg, 100 mg/kg and standard 10 mg/kg showed highly significant improvement in lipid profile when compared to negative control group. Extract treated 50 mg/kg, 100 mg/kg and standard 10 mg/kg showed significant body weight gain when compared to negative control group. Extract treated 50 mg/kg and 100 mg/kg showed significant improvement in food intake. Extract treated 50 mg/kg and 100 mg/kg showed highly significant but standard treated 10 mg/kg showed significant improvement in water intake. CONCLUSIONThe present study concludes that the extract possesses potent and significant anti-diabetic activity of Datura stramonium leaves.

Phytochemical and pharmacological properties of the genus Tamarix: a comprehensive review.

The genus Tamarix in the Tamaricaceae family consists of more than 100 species of halophyte plants worldwide that are mainly used to improve saline-alkali land and for coastal windbreaks, sand fixation, and afforestation in arid areas. A considerable number of species in this genus are also used as traditional medicines to treat various human diseases, especially in Asian and African countries. This review presents a comprehensive summary of 655 naturally occurring compounds derived from the genus Tamarix, categorized into flavonoids (18.0%), phenols (13.9%), tannins (9.3%), terpenoids (10.5%), essential oils (31.0%), and others (17.3%). The investigation revealed that the crude extracts and phytochemicals of this genus exhibited significant therapeutic potential, including anti-inflammatory, anti-Alzheimer, anticancer, antidiabetic, antibacterial, and antifungal activities. Six species of Tamarix have anticancer effects by causing cancer cell death, inducing autophagy, and stopping cell division. Seven species from the same genus have the potential for treating diabetes by inhibiting α-glycosidase activity, suppressing human islet amyloid polypeptide, regulating blood glucose levels, and modulating autophagy or inflammation. The focus on antibacterial and antidiabetic effects is due to the presence of volatile oil and flavonoid components. Extensive research has been conducted on the biological activity of 30 constituents, including 15 flavonoids, 5 phenols, 3 terpenoids, 1 tannin, and 6 others. Therefore, future research should thoroughly study the mechanisms of action of these and similar compounds. This is the most comprehensive review of the phytochemistry and pharmacological properties of Tamarix species, with a critical assessment of the current state of knowledge.

Phytochemical Profiling and Assessment of Antidiabetic Activity of Curcuma Angustifolia Rhizome Methanolic Extract: An In Vitro and In Silico Analysis.

Curcuma angustifolia Roxb. is a plant with medicinal potential, traditionally used to treat different diseases. The present study aimed to determine the antidiabetic activity of C. angustifolia rhizome in vitro and in silico. The methanolic extract of C. angustifolia rhizome was analyzed by FTIR and GC-MS to determine the phytochemicals present. The antidiabetic potential of the extract was evaluated by different assays in vitro. The extract inhibited both α-amylase and α-glucosidase enzymes and the glucose diffusion through the dialysis membrane in a concentration-dependent manner with IC50 values of 530.39±0.09, 293.75±0.11, and 551.74±0.3 μg/ml respectively. The methanolic extract also improved yeast cell's ability to take up glucose across plasma membranes and the adsorption of glucose. The findings were supported by molecular docking studies. The results showed that the methanol extract of C. angustifolia rhizome has significant antidiabetic activity and thus can be also studied to isolate the potential compound with antidiabetic activities.

Targeted Discovery of Glycosylated Natural Products by Tailoring Enzyme-Guided Genome Mining and MS-Based Metabolome Analysis.

Glycosides make up a biomedically important class of secondary metabolites. Most naturally occurring glycosides were isolated from plants and bacteria; however, the chemical diversity of glycosylated natural products in fungi remains largely unexplored. Herein, we present a paradigm to specifically discover diverse and bioactive glycosylated natural products from fungi by combining tailoring enzyme-guided genome mining with mass spectrometry (MS)-based metabolome analysis. Through in vivo genes deletion and heterologous expression, the first fungal C-glycosyltransferase AuCGT involved in the biosynthesis of stromemycin was identified from Aspergillus ustus. Subsequent homology-based genome mining for fungal glycosyltransferases by using AuCGT as a probe revealed a variety of biosynthetic gene clusters (BGCs) containing its homologues in diverse fungi, of which the glycoside-producing capability was corroborated by high-performance liquid chromatography-mass spectrometry (HPLC-MS) analysis. Consequently, 28 fungal aromatic polyketide C/O-glycosides, including 20 new compounds, were efficiently discovered and isolated from the three selected fungi. Moreover, several novel fungal C/O-glycosyltransferases, especially three novel α-pyrone C-glycosyltransferases, were functionally characterized and verified in the biosynthesis of these glycosides. In addition, a proof of principle for combinatorial biosynthesis was applied to design the production of unnatural glycosides in Aspergillus nidulans. Notably, the newly discovered glycosides exhibited significant antiviral, antibacterial, and antidiabetic activities. Our work demonstrates the promise of tailoring enzyme-guided genome-mining approach for the targeted discovery of fungal glycosides and promotes the exploration of a broader chemical space for natural products with a target structural motif in microbial genomes.

Wound healing, antidiabetic and antioxidant activity of Neolamarckia cadamba, quercetin rich, extract

IntroductionTraditional Chinese Medicine (TCM), Neolamarckia cadamba (NMCA), a member of the Rubiaceae family, is well-known for its rich assortment of phytochemicals and has a historical use in addressing various health issues. Quercetin is a bioactive compound that is widely used in botanical medicine and TCM because of its potent antioxidant activity. This study aimed to assess HPTLC analysis and explore the wound healing, antidiabetic, and antioxidant properties of optimized extracts from NMCA stems and bark. The objective of this study was to analyze the metabolites present in the plant and their potential health-related benefits. MethodsThe phytoconstituents in NMCA were identified by HPTLC analysis of its ethanolic extracts. The antioxidant activity was assessed using ABTS+ and DPPH assays. Furthermore, potential antidiabetic effects were investigated using inhibition assays targeting α-amylase and α-glucosidase. In addition, the evaluation included an MTT assay (HaCaT cell line) for cell viability and a wound healing scratch assay for cell migration. ResultThe ethanolic extract of NMCA was subjected to phytochemical analysis, which revealed the presence of diverse phytoconstituents, including alkaloids, flavonoid phenols, saponins, steroids, glycosides, and tannins. Subsequent HPTLC analysis confirmed the presence of quercetin in the extract. However, the MTT assay indicated the (IC50 313.3 ± 0.091 µg/ml) for NMCA plant extract. The wound healing scratch assay demonstrated significant cell migration. Notably, the ethanolic extract displayed significant antioxidant and antidiabetic activities in a dose-dependent manner. The antioxidant potential was evident in the ABTS+ radical scavenging assay (41.168 %) and DPPH radical scavenging assay, with an (IC50 185.275 µg/mL). Antidiabetic effects were demonstrated through the inhibition of α-amylase (IC50 37.23 ± 1.49 μM) and α-glucosidase (IC50 38.26 ± 1.72 μM). Comparatively, the standard acarbose exhibited (IC50 38.94 ± 0.45 μM) for α-glucosidase and (IC50 34.61 ± 3.71 μM) for α-amylase. Furthermore, the ethanolic extract of NMCA, which is rich in phytoconstituents and quercetin, displayed potent wound healing and antidiabetic and antioxidant properties, suggesting its potential therapeutic significance. DiscussionThese results further corroborate the longstanding medicinal use of NMCA, suggesting its therapeutic potential in addressing wound healing, oxidative stress, and diabetes mellitus.

Design, synthesis of new 2,4-thiazolidinediones: In-silico, in-vivo anti-diabetic and anti-inflammatory evaluation

In this study, a series of nine novel heterocyclic compounds were synthesized through a concise three-step reaction process. The synthesis involved Knoevenagel condensation at the 5th position of the 2,4-thiazolidinedione or rhodanine ring-system. Comprehensive physicochemical and spectral analyses, including FTIR, Mass, 1H NMR and 13C NMR, were performed to characterize the synthesized compounds. The synthesized derivatives were subjected to evaluation for their potential in various therapeutic domains. In-vivo anti-diabetic activity was assessed diabetes induced wistar rats, anti-inflammatory effects were gauged using the carrageenan and formalin induced rat paw edema model. Additionally, the in-vitro PPAR-γ modulatory activity, glucose uptake by using Saccharomyces cerevisiae and rat hemidiaphragm and cyclooxygenase inhibitory activity along with scavenge free radicals was tested by FRAP and DPPH method. According to the potential binding patterns of the most potent anti-diabetic compounds, namely 7a and 13a with the active sites of target PPAR-γ (PDB ID: 5U5L), was obtained through molecular docking using Schrodinger’s Glide model. Among the tested compounds, the compound 13a demonstrated significant antidiabetic activity with reduction in blood glucose levels (108.5 ± 2.171 mg/dL), comparable to the effect of pioglitazone (101.66 ± 0.95 mg/dL), similarly anti-inflammatory activity at fourth hour paw volume 93.6% and thickness at 3.99 ± 0.076 mm, respectively closer to that of standard drug diclofenac sodium (91.2% and 4.7 ± 0.057 mm) in carrageenan-induced paw edema in rat. The compound 13a displayed promising COX-2 inhibitory activity (IC50 = 7.82 μM) and DPPH antioxidant activity showcasing its multifaceted therapeutic potential. This study not only presents multi-targeting approach and highlights the significant potential compounds as a lead molecule for further therapeutic development.