Antidiabetic Activity Research Articles

Antidiabetic Potential of Apiaceae Family Plants- A Critical Update

Apiaceae is one of the biggest and most important plant families, comprising about 3700 species and 434 genera. Most of them are aromatic, flowering plants. The plants in this family are beneficial for everyday use and treating diseases. They are a rich source of nutraceuticals and secondary metabolites attributed to different pharmacological activities. Some plants under this family possess antidiabetic activity through different mechanisms, such as inhibiting carbohydrate hydrolyzing enzymes, stimulating insulin secretion, and regulating glucose transporters. Diabetes mellitus has become a chronic metabolic disorder whose management is of utmost importance in recent days. The present review aims to establish the use of Apiaceae family plants in treating diabetes mellitus. The availability of plants, their bio-constituents, mode of action, and experimental studies have also been briefly described here.

Optimization of Polyphenol Extraction Conditions from Rhizomes of Curcuma zedoaria with Antioxidant, Anti-Inflammatory and Anti-Diabetic Activities In Vitro

The recovery of polyphenol compounds is seen as an arduous task because polyphenol compounds are available as free aglycones, as sugar or ester conjugates, or as polymers with several monomeric components. The response surface method (RSM) as a tool to optimize the factors that affect extraction efficacy as well as to obtain maximum recovery of the compounds of interest. This study optimizes ultrasound-assisted polyphenol extraction from Curcuma zedoaria rhizomes using response surface methodology (RSM). Three variables were considered: Ethanol concentration (70 - 90 %, v/v), temperature (60 - 80 °C), and ultrasound time (15 - 25 min). Data were analyzed by ANOVA, yielding an R2 of 0.9993, a significant interaction effect (p < 0.0001), and an insignificant lack-of-fit test (p = 0.6684). Optimal conditions for maximum polyphenol content (TPC = 31.05 ± 0.53 mg GAE/g powder) were 80.02 % ethanol, 68 °C, 20.47 min ultrasound time, and 1/10 (w/v) raw material/solvent ratio. Experimental values matched RSM predictions, confirming successful extraction optimization from Curcuma zedoaria rhizomes. The polyphenol-rich optimum extract from Curcuma zedoaria rhizomes has been studied for its antioxidant, anti-inflammatory and anti-inflammatory properties in vitro. The results were found, the optimum extract of Curcuma zedoaria rhizomes could perform effective neutralization activities of free radicals performed in DPPH test (IC50 = 5.89 ± 0.23 µg/mL), NO· (IC50 = 5.89 ± 0.23 µg/mL) and ABTS·+ (IC50 = 8.28 ± 0.12 µg/mL). Besides, this optimum extract had the ability to protect red blood cell membranes and inhibit protein denaturation due to heat with IC50 times values ​​such as 29.06 ± 0.35 and 30.24 ± 0.32 µg/mL. In addition, it also significantly inhibited α-amylase, α-glucosidase enzyme activities with IC50 values ​​of 5.89 ± 0.23 and 9.62 ± 0.11 μg/mL, respectively. This investigation showed that the polyphenol-rich optimum extract from Curcuma zedoaria rhizomes was a promising antioxidant, anti-inflammatory and anti-diabetic agent. HIGHLIGHTS Using ultrasound and the Box-Behnken design to extract polyphenols from Curcuma zedoaria rhizomes can speed up and improve extraction efficiency. The goal of this study is to maximize the extraction parameters for polyphenols from the rhizomes of Curcuma zedoaria. There is strong agreement between the experimental data and the model that predicts the polyphenol content in the Box-Behnken design. In vitro biological activities such as anti-inflammatory, antidiabetic and antioxidant properties are significantly correlated with polyphenol concentration. The findings of our investigation show a noteworthy enhancement in the bioavailability of polyphenol compounds through increased extraction efficiency and bioactivity. GRAPHICAL ABSTRACT

HPTLC, Pharmacognostic standardisation and Biological activity of Cannabis sativa

Cannabis sativa belongs to the family Cannabinaceae and has notable medicinal properties as it is used as for psychoactive effects. Cannabis which contains CBD and THC exhibits a range of potential therapeutic benefits, including anti-inflammatory, analgesic, anxiolytic and neuroprotective properties. Methanolic extracts of Cannabis sativa were obtained through reflux extraction to perform further experiments. Various experimental tests were carried out to understand the physicochemical, fluorescence properties of Cannabis sativa. HPTLC and phytochemical profiles were also obtained. Preliminary phytochemical analysis showed the presence of alkaloids, flavonoids, Tannins, Phenols and steroids. Microscopy of the sample powder showed the presence of starch, stigma shaped papillae and Calcium oxalate crystals. HPTLC profiling showed 9 bands of a pattern unique to Cannabis sativa. The Cannabis sativa showed antidiabetic and anti oxidant activity when bioautography was done.

Synthesis, Characterization, Investigation of DNA Interactions and Biological Evaluation of Co(II), Ni(II), Cu(II) and Zn(II) Complexes with Newly Synthesized 2-methoxy 5-trifluoromethyl benzenamine Schiff Base.

The biologically active and thermally stable bivalent Co(II), Ni(II), Cu(II), and Zn(II) complexes (C1, C2, C3, and C4) of novel Schiff base ligand [(5-trifluoromethyl-2-methoxyphenylamino)methyl)-4,6-diiodophenol (L)] have been synthesized. The structural analysis of these complexes have been carried out by elemental analysis, 1H-NMR, FTIR, ESI mass, UV-visible, ESR, TGA techniques and magnetic measurements. The obtained results were confirmed as square planar geometry for Ni(II) and Cu(II) complexes, whereas octahedral geometry for Co(II) and Zn(II) complexes. The geometry optimized structures were developed by employing CHEM 3D software. The DNA binding interaction studies such as UV-vis absorption, viscosity, and fluorescence studies have been confirmed that the mode of binding of complexes with DNA is an intercalative binding. The DNA cleavage studies revealed that all the complexes are found to be potent to cleave the DNA into Form I & II. The in-vitro pathological studies of all the complexes against various microbial strains (Gram + and Gram -), revealed that Cu(II) complexes are more potent compared to other complexes and Schiff base. The anti diabetic activity studies revealed that the Cu(II) complex exhibited slightly higher activity than Co(II), Ni(II), and Zn(II) complexes. The results of antioxidant activity by DPPH method, suggested that the Cu(II) complex has higher activity and comparable with the standard compounds.

Formulation and evaluation of phytosomes containing bioactive from Carica papaya seeds

Background: Papaya seeds are a rich source of proteins, fat, fibers, vitamins, minerals, monounsaturated fatty acids, polyphenols, and powerful antioxidants like flavonoids. Low solubility limits the absorption and bioavailability of herbal constituents. Hence, phytosomes of Papaya seed extract were formulated to enhance its solubility and bioavailability. Methodology: Papaya seeds were extracted using ethanol as solvent, and all the phytoconstituents present in the extract were assessed during the phytochemical screening and LC-MS analysis. In-vitro antidiabetic activity pure extract was determined by alpha-amylase and alpha-glucosidase enzyme inhibitory assay. The phytosomes of extract were formulated using the lipid thin film formation method and Soya lecithin and Cholesterol as lipids. The formulated phytosomes were analyzed for parameters such as particle size, zeta potential, encapsulation efficiency, percent drug content, and In-vitro dissolution study. The chemical nature of the formulation was studied using FTIR analysis and powder X-ray diffractometry. Thermal stability of phytosomes analyzed with the help of Differential Scanning calorimetry. Results: LC-MS identified 16 phytoconstituents. In-vitro antidiabetic activity showed 59.97% and 51.17% inhibition of enzymes alpha-amylase and alpha-glucosidase, respectively. The encapsulation efficiency of the optimized formulation was 88.41±0.91% with a particle size of 188.0±53.7nm. TEM images of formulation confirm the formation of phytosomes. FTIR, DSC, and Powder X-ray diffractometry showed no unwanted peaks. The in vitro dissolution study showed 89.26±1.05% CDR of phytosome, while the extract showed 47.78±0.59% CDR. Conclusion: Evaluation results of phytosomes suggest that this formulation can be used as an effective herbal antidiabetic formulation

Phytochemical profiling, molecular docking and GLUT4 and PPAR-γ mRNA Expression study of Tamarindus indica seeds fraction for antidiabetic activity in Rats

Phytochemical profiling, molecular docking and GLUT4 and PPAR-γ mRNA Expression study of Tamarindus indica seeds fraction for antidiabetic activity in Rats

Bio-fabrication of zinc oxide nanoparticles from Brassica juncea (L.) Czern extract: Biological activity and DNA binding capability

Recent years have seen a great deal of interest in the exceptional biological activities such as antioxidant, antimicrobial, antiinflammation, antidiabetic and anticancer activity of various biosynthesized Metal Oxide nanoparticles. Among these metal oxide nanoparticle ZnO NPs is gaining its important in various biological applications is increasingly gain prominence. Thus, the green production of ZnO NPs using plant extract has been demonstrated as a one step, environmentally friendly and cost-effective process. This paper describes the utilization of an aqueous extract of Brassica juncea (L.) Czern seed as a reducing agent in the creation of ZnO NPs from Zinc Sulfate using a green synthesis approach. UV–visible spectroscopic peak at around 363 nm verifies the production of ZnO NPs. FE-SEM was confirmed the spherical forms of produced ZnO NPs. The average particle size of produced ZnO NPs was found to be 13.35 nm from TEM analysis. On screening the ZnO NPs for antioxidant activity it showed scavenging activity with 62.40 %, with IC50 value of 68.30 µg/mL through DPPH assay. The antidiabetic activity was found to be 72 %, with IC50 value of 71.76 μg/mL, using alpha amylase assay. In anti-inflammatory activity, the activity was recorded as 68.50 % and IC50 value as 64.67 µg/mL, using BSA denaturation assay. The synthesized nanoparticles exhibited anticancer activity against the MCF-7 and A549 cell lines. The determined IC50 value of produced ZnO NPs for these two cell lines was found to be 43.83 µg/mL and 41.48 µg/mL respectively. Additionally, a hyperchromic shift in the absorbance was noted when CT-DNA interacted with biosynthesized ZnO NPs. These findings confirm that the ZnO NPs synthesized from Brassica juncea (L.) Czern seed exhibit significant biological properties namely antioxidant, antidiabetic and cytotoxic activity. Among all these activities, the biosynthesized ZnO NPs showed excellent cytotoxic activity with the IC50 values, thus proving its effectiveness.

Analyze and assess the spectral, DFT, and medicinal characteristics through targeted pharmacological investigation of 2-(3-(5-(4-chlorophenyl)furan-2-yl)acryloyl)-3,4-dihydro-2H-naphthalen-1-one (CHFADN)

The compound 2-(3-(5-(4-chlorophenyl)furan-2-yl)acryloyl)-3,4-dihydro-2H-naphthalen-1-one (CHFADN) was synthesized using the Claisen-Schmidt condensation method, reacting aromatic aldehydes with methyl ketones. Characterization was performed using NMR, FTIR, and UV–visible spectroscopy. A theoretical model was developed with Gaussian 09 software, utilizing the B3LYP/6–311++G(d,p) basis set, to investigate geometric, electronic, and spectroscopic properties, including geometry optimization, harmonic vibration simulations, molecular electrostatic potential (MEP), frontier molecular orbitals (FMOs), and Mulliken's population analysis. A scaling factor of 0.9600 ensured alignment between the compound's vibrational spectrum and the experimental IR spectrum.In-vitro testing showed notable bactericidal efficacy,H2O2 scavenging activity and antidiabetic activity. In silico molecular docking using AutoDock 4.0, focusing on the 1HD2 protein's active pocket, revealed a binding interaction energy of -6.5 kcal/mol. ADME properties were predicted based on retention data (RM0). The compound showed no mutagenic effects in toxicity testing, indicating a promising safety profile for new drug candidates.

GC-MS-employed Phytochemical Characterization and Anticancer, Antidiabetic, and Antioxidant Activity Screening of Lagerstroemia Thorelli.

Lagerstroemia thorelli (L. thorelli) is a member of the Lythraceae family and has not been previously researched. Thus, this study aimed to investigate its unexplored potential and identify novel therapeutic prospects. This research evaluated antioxidant, antidiabetic, and cytotoxic potentials along with compound characterization of the ethanolic leaf extract of L. thorelli. The antioxidant potential was assessed using 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical and hydrogen peroxide (H2O2) scavenging assays, total antioxidant capacity (TAC), total phenolic content (TPC), total flavonoid content (TFC) determination, antidiabetic property was assessed using α-amylase inhibition, and the cytotoxic effect was examined on HeLa and Vero cells using MTT colorimetric assay. Chemical characterization was performed using gas chromatography-mass spectrometry (GC-MS). The findings demonstrated strong antioxidant, strong antidiabetic, and moderate cytotoxic activities. Comprehensive phytochemical analysis revealed its abundance in flavonoids, phenols/phenolics, tannins, glycosides, steroids, resin, etc. GC-MS analysis of the L. thorelli extract identified 80 important compounds including cis-11-eicosenamide, beta-D-glucopyranoside, methyl-, alpha-D-glucopyranoside, methyl-, phthalic acid, gamma-sitosterol, phytol, silicic acid, squalene, butanoic acid, cyclobarbital, etc. which are well-documented for their antioxidant, antidiabetic, and anticancer effects. Thus, it can be inferred that L. thorelli could hold new promises in treating diseases like diabetes and free radical-induced conditions, including neurodegenerative diseases.

Bio Evaluation of Mirabilis Jalapa Leaves Extract for Anxiolytic Activity in Animal Model

Anxiety is an exaggerated feeling of apprehension, uncertainty and fear. It is an unpleasant state of tension with an anticipation of imminent danger. It may be regarded as a particular form of behavioral inhibition that occurs in response to environmental events that are Novel. In recent times, there are many indigenous plants have beneficial properties to treat mental disease and psychic complaints. Mirabilis Jalapa Linn (family- Nyctanginaceae) is one of the plants that used for health care and medicinal purpose for thousands of years. It has traditionally been used in the treatment of gastrointestinal disorders, muscle pain, abdominal colic, and diarrhea. However, studies have evidenced its antibacterial, antiviral, antioxidant, anti-diabetic, anti-inflammatory, anti-stress and many other activities. The purpose of this study was to prepare & evaluate Methanolic extract of leaves of mirabilis Jalapa for the treatment of anxiety in animal models. The dried leaves were extracted with methanol separately and administered the dose of 200mg/kg and employed in elevated plus maze test and open field test with 2mg/kg i.p.of Diazepam as a standard drug to assess the anxiolytic activity. The result reveled that methanol leaf extract was more impetus due to high amount of flavonoid, phenolic compound, steroids; terpenoid contents possess tremendous anti-anxiety activity. This study suggested that the M.Jalapa is much more active compound consistent medicinal plant to derive a potent drug against Anxiety

Antidiabetic and Anti-Inflammatory Effect of Cinnamomum cassia Oil in Alloxan-Induced Diabetic Rats.

Diabetes mellitus presents a great diversity of treatments that cause adverse effects; therefore, plants are a source of compounds that may have fewer adverse effects; Cinnamomum cassia (C. cassia) has compounds with potential antidiabetic activity. The objective was to evaluate the antidiabetic effect of C. cassia oil (CCO) and its impact on oxidative stress in Wistar rats. Five groups were evaluated: (1) sham (SH), (2) 300 mg/kg CCO (CCO), (3) diabetic (D) induced with alloxan, (4) D + 300 mg/kg of CCO (D + CCO), and (5) D + 500 mg/kg of metformin (D + MET); all were treated for 5 days. CCO did not show alteration in aspartate aminotransferase (AST) and alanine aminotransferase (ALT) vs. SH. D + CCO vs. D significantly reduced glucose (333 ± 109 vs. 458 ± 81 mg/dL), ALT (66 ± 15 vs. 160 ± 54 U/L), AST (119 ± 26 vs. 243 ± 104 U/L), and blood urea nitrogen (18.8 ± 2.3 vs. 29.2 ± 6.9 mg/dL). No significant changes were observed in D + CCO vs. D in malondialdehyde (MDA), reduced glutathione (GSH), and superoxide dismutase (SOD), whereas a significant reduction in MDA and GSH was achieved in D + MET, with an increase in SOD. There was a reduction in Rela and Gpx in D + CCO and D + MET vs. D. CCO has antidiabetic and anti-inflammatory effects and reduces ALT, AST, and BUN levels.

Antidiabetic potential of sea fish mass by inhibiting di-peptidyl peptidase-IV and augmenting glucagon-like peptide-1 on high lipid diet and streptozotocin induced diabetic rats

Many studies have revealed that sea fish is a rich source of nutrients, especially protein and there peptide. In this study, antidiabetic activity of the fish masses of three sea-fishes ‘volavetki’ (Panna microdon, Bleeker 1849), ‘ruli’ (Coilia dussumieri, Valenciennes 1848), ‘tapra’(Opisthopterus tardoore, Cuvier 1829) and one fresh-water fish ‘murola’(Amblypharyngodon mola, Hamilton 1822),evaluated high lipid diet (HLD) and STZ induced Type 2 Diabetic Mellitus (T2DM) rats. Supplementation of sea-fish masses and antidiabetic effect was monitored by fasting plasma blood glucose and HbA1c. Also, insulin, c-peptide, glucagon-like peptide-1, dipeptidyl peptidase-IV, glucokinase, glucose-6 phosphatase, superoxide dismutase, glutathione peroxidase, catalase, plasma total cholesterol, low density lipoprotein, triglycerides, high density lipoprotein and histopathology of free radical activity of pancreatic tissues were evaluated. Out of four fish masses, volavetki sea fish masses oral supplementation resulted in significant reduction of plasma blood glucose, HbA1c of T2DM rat. All other parameters in T2DM rats were returned to near normal by treatment of volavetki sea fish mass. Our findings strongly indicated that volavetki sea fish highly showed antidiabetic activity.

Evaluation of antidiabetic activity of Ocimum sanctum (Tulsi) through inhibition of alpha-amylase and alpha-glucosidase: an in vitro study

Evaluation of antidiabetic activity of Ocimum sanctum (Tulsi) through inhibition of alpha-amylase and alpha-glucosidase: an in vitro study

Evaluating the Efficacy of Metformin and Camel Milk on Streptozotocin-nicotinamide Induced Diabetic Albino Rats

Background: This study was intended to evaluate the anti-diabetic activity of metformin and camel milk solely or in combination in streptozotocin- nicotinamide induced type II diabetic albino Wistar rats. Methods: Thirty albino Wistar rats were induced with type II diabetes through streptozotocin (60 mg/kg), followed by the administration of nicotinamide (120 mg/kg) after 15 min. The rats were randomly divided into control, diabetic control, metformin-treated (100 mg/kg), camel milk-treated (50 ml/rat/day) and metformin + camel milk-treated groups for 30 days. For this study, rats with blood glucose levels higher than 250 mg/dL were included. Blood glucose levels and body weight were measured at the beginning of the study and at regular intervals throughout the experiment.Furthermore, histopathological examination of liver, kidney and pancreatic tissue was conducted to determine the effects of metformin and camel milk on these organs. Result: The results showed that treatment with metformin, camel milk, or a combination of both significantly reduced fasting blood glucose levels and improved body weight compared to the diabetic control group. Morphological improvements were also observed in the histopathological examination of liver, kidney and pancreatic tissue. The results of this study are consistent with previous research showing the anti-diabetic effects of metformin and support the emerging role of alternative therapies such as camel milk. However, further research is needed to explore the potential mechanisms underlying the observed effects.

Biological Effects of Green Synthesized Al-ZnO Nanoparticles Using Leaf Extract from Anisomeles indica (L.) Kuntze on Living Organisms.

The synthesis of Al-ZnO nanoparticles (NPs) was achieved using a green synthesis approach, utilizing leaf extract from Anisomeles indica (L.) in a straightforward co-precipitation method. The goal of this study was to investigate the production of Al-ZnO nanoparticles through the reduction and capping method utilizing Anisomeles indica (L.) leaf extract. The powder X-ray diffraction, UV spectroscopy, Fourier transform infrared spectroscopy, and scanning electron microscopy with EDAX analysis were used to analyze the nanoparticles. X-ray diffraction analysis confirmed the presence of spherical structures with an average grain size of 40 nm in diameter, while UV-visible spectroscopy revealed a prominent absorption peak at 360 nm. FTIR spectra demonstrated the presence of stretching vibrations associated with O-H, N-H, C=C, C-N, and C=O as well as C-Cl groups indicating their involvement in the reduction and stabilization of nanoparticles. SEM image revealed the presence of spongy, spherical, porous agglomerated nanoparticles, confirming the chemical composition of Al-ZnO nanoparticles through the use of the EDAX technique. Al-ZnO nanoparticles showed increased bactericidal activity against both Gram-positive and Gram-negative bacteria. The antioxidant property of the green synthesized Al-ZnO nanoparticles was confirmed by DPPH radical scavenging with an IC50 value of 23.52 indicating excellent antioxidant capability. Green synthesized Al-ZnO nanoparticles were shown in in vivo studies on HeLa cell lines to be effective for cancer treatment. Additionally, α-amylase inhibition assay and α-glucosidase inhibition assay demonstrated their potent anti-diabetic activities. Moving forward, the current methodology suggests that the presence of phenolic groups, flavonoids, and amines in Al-ZnO nanoparticles synthesized with Anisomeles indica (L.) extract exhibit significant promise for eliciting biological responses, including antioxidant and anti-diabetic effects, in the realms of biomedical and pharmaceutical applications.

Black and Red Currant Pomaces as Raw Materials to Create Smoothies with In Vitro Health-Promoting Potential.

Pomace is a by-product resulting from the pressing of fruits and vegetables into juices, and it is typically treated as waste. Interestingly, pomace contains minimal amounts of protein and fat but is characterized by its high polyphenol and dietary fiber contents, which may have health benefits for human physiology. Therefore, they are a potentially attractive raw material for the food industry, but to our knowledge, no smoothies with their addition have been prepared and described so far. Consequently, products derived from apple juice, incorporating different doses of fresh (6% and 12%) and dried (3% and 6%) black or red currant pomace, were formulated, and their physical properties, chemical composition, bioactive compound content, and health-promoting potential (in vitro antioxidant and antidiabetic activity) were evaluated. Additionally, the products underwent sensory assessment by consumers. The fortified beverages exhibited different physical characteristics and chemical compositions than apple juice. All smoothies were characterized by higher concentrations of anthocyanins, flavonols, and procyanidin polymers compared to the base product. Moreover, 75% of them exhibited a significantly elevated phenolic acid content as well as a higher concentration of flavan-3-ols. The majority of fresh smoothies exhibited significantly higher in vitro antioxidant capacities and increased in vitro α-amylase and α-glucosidase inhibitory effects compared to the base product. The highest ABTS activity was recorded in the variant with 6% dried black currant pomace. In turn, the smoothie with 3% dried red currant pomace had the most effective FRAP effect and, together with the product containing 12% fresh black currant pomace, ORAC antioxidant activity and α-glucosidase inhibition also. The introduction of 6% dried red currant pomace led to the creation of a beverage that most effectively inhibited α-glucosidase. The study showed that the application of various types of pomace, mainly that of black currant, into apple juice enables the development of new functional products with sensory attributes that are favorably evaluated by consumers.

Polydatin from Polygoni Cuspidati Rhizoma et Radix regulates glucolipid metabolism in the liver of diabetic rats: Multiscale analysis of network pharmacology and multiomics

BackgroundPolygoni Cuspidati Rhizoma et Radix (Huzhang in Chinese), refers to the root and rhizome of Polygonum cuspidatum Sieb. et Zucc. Huzhang is commonly used in clinical practice for the prevention and treatment of diabetes and its complications, but its active components and regulatory mechanisms have not yet been thoroughly analyzed. PurposeThe network pharmacology combined with multi-omics analysis will be employed to dissect the substance basis and action mechanism of Huzhang in exerting its anti-diabetic activity. MethodsThis study employed phenotypic indicators for baseline assessment, followed by integrated analysis using network pharmacology, metabolomics, transcriptomics, and qPCR technology to elucidate the active components and pharmacological mechanisms of Huzhang. ResultsThe analysis of network pharmacology revealed that polydatin is a potential active component responsible for the anti-T2DM pharmacological effects of Huzhang. In vivo experimental results demonstrated that polydatin significantly regulates blood glucose, lipid levels, liver function, and liver pathological damage in diabetic rats. Analysis results from transcriptomics, metabolomics, and qPCR validation showed that polydatin comprehensively regulates glucose and lipid metabolism in T2DM by modulating bile acid metabolism, fatty acid oxidation, and lipogenesis. ConclusionPolydatin is a key component of Huzhang in treating T2DM, and its regulatory mechanisms are diverse, indicating significant development potential.

Discovery of novel thiazole derivatives containing pyrazole scaffold as PPAR-γ Agonists, α-Glucosidase, α-Amylase and COX-2 inhibitors; Design, synthesis and in silico study

A novel series of thiazole derivatives with pyrazole scaffold 16a-l as hybrid rosiglitazone/celecoxib analogs was designed, synthesized and tested for its PPAR-γ activation, α-glucosidase, α-amylase and COX-2 inhibitory activities. Regarding the anti-diabetic activity, all compounds were assessed in vitro against PPAR-γ activation, α-glucosidase and α-amylase inhibition in addition to in vivo hypoglycemic activity (one day and 15 days studies). Compounds 16b, 16c, 16e and 16 k showed good PPAR-γ activation (activation % ≈ 72–79 %) compared to that of the reference drug rosiglitazone (74 %). In addition, the same derivatives 16b, 16c, 16e and 16 k showed the highest inhibitory activities against α-glucosidase (IC50 = 0.158, 0.314, 0.305, 0.128 μM, respectively) and against α-amylase (IC50 = 32.46, 23.21, 7.74, 35.85 μM, respectively) compared to the reference drug acarbose (IC50 = 0.161 and 31.46 μM for α-glucosidase and α-amylase, respectively). The most active derivatives 16b, 16c, 16e and 16 k also revealed good in vivo hypoglycemic effect comparable to that of rosiglitazone. In addition, compounds 16b and 16c had the best COX-2 selectivity index (S.I. = 18.7, 31.7, respectively) compared to celecoxib (S.I. = 10.3). In vivo anti-inflammatory activity of the target derivatives 16b, 16c, 16e and 16 k supported the results of in vitro screening as the derivatives 16b and 16c (ED50 = 8.2 and 24 mg/kg, respectively) were more potent than celecoxib (ED50 = 30 mg/kg). In silico docking, ADME, toxicity, and molecular dynamic studies were carried out to explain the interactions of the most active anti-diabetic and anti-inflammatory compounds 16b, 16c, 16e and 16 k with the target enzymes in addition to their physiochemical parameters.

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.

Active Ingredients and Antidiabetic Activity of Fenugreek: A Review Article

Active Ingredients and Antidiabetic Activity of Fenugreek: A Review Article