Isochromophilones H-K, the new bioactive azaphilone derivatives isolated from fungal strain Diaporthe perseae associated with Pongamia pinnata plant.

The phytochemical study of the Diaporthe species has revealed significant classes of mycotoxins and phomopsins. Dihydroanthracenone derivatives, chromanones and isochromophilones have also been isolated from Diaporthe sp. These findings led us to explore the Diaporthe perseae for phytochemical analysis that resulted in the isolation of four new compounds designated as isochromophilones H-K (1-4), alongside three previously identified metabolites. Using extensive spectroscopic investigations such as NMR, and Mass spectroscopy, their structures were elucidated. Furthermore, the antimicrobial and anti-diabetic potentials of all isolated compounds were assessed. Compounds 1-3 demonstrated significant antibacterial activity, while compounds 4-7 exhibited comparatively lower effectiveness than the reference antibiotics. Compounds 2-3 showed potent diabetic inhibition, displaying IC50 values of 16.3 ± 0.3 and 25.4 ± 0.3, respectively. Compounds 1, 5, and 6 displayed mild anti-diabetic effects, with IC50 values of 56.5 ± 0.8, 37.6 ± 0.4, and 48.2 ± 0.6. However, compounds 4 and 7 were found least active.

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.

Anti-diabetic drug use and reduced risk of Parkinson's disease: A community-based cohort study.

BACKGROUND: Emerging evidence suggests a potential association between certain anti-diabetic drugs and a reduced risk of Parkinson's disease (PD). Limited population-based studies have investigated users of newer anti-diabetic drugs such as GLP-1 agonists or SGLT2 inhibitors. OBJECTIVE: The aim of this study was to assess the risk of PD among individuals with type 2 diabetes mellitus (T2DM) who were treated with various types of anti-diabetic drugs over time. METHODS: A population-based cohort comprising T2DM patients aged over 30 who used metformin, GLP-1 agonists, thiazolidinediones, sulfonylureas, DPP4 inhibitors, SGLT2 inhibitors, or meglitinides between January 1, 1999 and December 31, 2018. Data were obtained between the diabetes registration and drug purchase databases of Maccabi Healthcare Services. Time-dependent Cox regression models, adjusted for sex, age, and comorbidities were employed to calculate the adjusted hazard ratios (HRs) for the PD risk associated with different anti-diabetic drugs over time. RESULTS: The study population comprised 86,229 T2DM patients, with 53.9 % males. The mean age at the first anti-diabetic drug purchase was 59.0 ± 11.0 and 62.0 ± 11.0 years for men and women respectively. Compared to metformin, several drug types were associated with a significantly lower PD risk: thiazolidinediones (HR = 0.91, 95 % CI:0.074-1.14); DPP4 inhibitors (HR = 0.60, 95 % CI:0.53-0.67); meglitinides (HR = 0.63, 95 % CI:0.53-0.74); GLP-1 agonists (HR = 0.54, 95 % CI:0.39-0.73); and SGLT2 inhibitors (HR = 0.15, 95 % CI:0.10-0.21). CONCLUSIONS: Our results suggest a reduced risk of PD with certain anti-diabetic drugs, particularly SGLT2 inhibitors and GLP-1 agonists. Validation through extensive big-data studies is essential to confirm these results and to optimize PD prevention and management.

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.

Olive oil and flaxseed oil incorporating niosomes for enhanced in vivo anti-diabetic efficacy of canagliflozin.

BACKGROUND: Canagliflozin is broadly implicated for the management of type 2 diabetes mellitus. Unfortunately, it has low oral bioavailability due to poor solubility behaviour and restricted membrane permeability. OBJECTIVE: The current work focuses on development of canagliflozin encapsulated niosomes for enhanced oral anti-diabetic efficacy. METHODOLOGY: Niosomes comprising span 60 and cholesterol were formulated both in absence and presence of olive oil or flaxseed oil. These were evaluated in vitro for average vesicular size, structural morphology, canagliflozin entrapment efficiency, and drug release. Additionally, the oral hypoglycemic effect of canagliflozin encapsulated niosomes was explored in diabetic rats. Results: The fabricated niosomes were negatively charged spherical vesicles with a size range of 103.0- 141.7nm. These entrapped canagliflozin with efficiency ranging from 92.3% to 96.0%. Drug release investigations reflected that incorporating canagliflozin into niosomes significantly sustained drug release compared to the aqueous drug dispersion. Oral administration of niosomal formulations significantly enhanced the oral antidiabetic effect of canagliflozin. Comparing the tested niosomes, similar efficiency was shown eliminating the effect of composition. CONCLUSION: The enhanced oral bioavailability of niosomes' encapsulated drugs is related to niosomal vesicular structure which allows intact niosomes absorption. The study presented niosomes as promising carriers for improved oral anti-diabetic activity of canagliflozin.

In Vitro and in Silico Analysis of α -Amylase Inhibitory Activity of Ethanolic Extract of Adhatoda vasica Leaves.

Objective: Diabetic individuals have a higher probability of suffering from illness and death due to small blood vessel-related problems such as retinopathy, neuropathy, nephropathy, and stroke than other complications. There are many synthetic anti-diabetic agents available, but these can be expensive and have undesirable pathological effects. The enzyme α-amylase (hydrolase), catalyzes the hydrolysis of starch to maltose and glucose via the cleavage of α-1,4-glucosidic linkages. Diabetes mellitus patients may benefit from a therapeutic strategy that involves slowing the hydrolysis of starch by inhibiting the activity of α-amylase. Thus, looking for cost-effective, natural, and safe antidiabetic agents is essential. This study aims to screen phytoconstituents and evaluate the in-vitro and in-silico α-amylase inhibitory activity of the ethanolic extract of Adhatoda vasica leaves. Methods: The extraction of Adhatoda vasica leaves was performed using ethanol via the Soxhlet extraction process. Different concentrations (100 µg/mL to 1000 µg/mL) of ethanolic extract, Acarbose, and Sitagliptin, were prepared and evaluated for α-amylase inhibitory activity using the spectrophotometric method. Molecular docking (AutodockVina 1.2.0) and toxicity profiling (SToPToX web server) studies were performed. Results: The ethanolic extract of Adhatoda vasica leaves showed the highest percentage inhibition against α-amylase (56.763 ± 0.0035) at a concentration of 1000 µg/mL. The in-silico study supported this inhibitory activity. Vasicoline (C5) and Quercetin (C9), the active constitute of Adhatoda vasica, showed the best binding energies of -8.3 and -8.0 Kcal/mol, respectively against α-amylase enzyme (PDBID: 4W93). A toxicity study revealed the safety profile of the plant extract. Conclusion: It was concluded that Adhatoda vasica leaves possess some bioactive compounds that are responsible for controlling blood glucose levels, and their identification, purification, and isolation may lead to the development of new therapeutic agents with fewer side effects than the available drugs.

Assessment of the in vitro anti-diabetic activity with molecular dynamic simulations of limonoids isolated from Adalia lemon peels.

Limonoids are important constituents of citrus that have a significant impact on promoting human health. Therefore, the primary focus of this research was to assess the overall limonoid content and isolate limonoids from Adalia lemon (Citrus limon L.) peels for their potential use as antioxidants and anti-diabetic agents. The levels of limonoid aglycones in the C. limon peel extract were quantified through a colorimetric assay, revealing a concentration of 16.53 ± 0.93 mg/L limonin equivalent. Furthermore, the total concentration of limonoid glucosides was determined to be 54.38 ± 1.02 mg/L. The study successfully identified five isolated limonoids, namely limonin, deacetylnomilin, nomilin, obacunone 17-O-ß-D-glucopyranoside, and limonin 17-O-ß-D-glucopyranoside, along with their respective yields. The efficacy of the limonoids-rich extract and the five isolated compounds was evaluated at three different concentrations (50, 100, and 200 µg/mL). It was found that both obacunone 17-O-ß-D-glucopyranoside and limonin 17-O-ß-D-glucopyranoside possessed the highest antioxidant, free radical scavenging, and anti-diabetic activities, followed by deacetylnomilin, and then the limonoids-rich extract. The molecular dynamic simulations were conducted to predict the behavior of the isolated compounds upon binding to the protein's active site, as well as their interaction and stability. The results revealed that limonin 17-O-ß-D-glucopyranoside bound to the protein complex system exhibited a relatively more stable conformation than the Apo system. The analysis of Solvent Accessible Surface Area (SASA), in conjunction with the data obtained from Root-Mean-Square Deviation (RMSD), Root-Mean-Square Fluctuation (RMSF), and Radius of Gyration (ROG) computations, provided further evidence that the limonin 17-O-ß-D-glucopyranoside complex system remained stable within the catalytic domain binding site of the human pancreatic alpha-amylase (HPA)-receptor. The research findings suggest that the limonoids found in Adalia lemon peels have the potential to be used as effective natural substances in creating innovative therapeutic treatments for conditions related to oxidative stress and disorders in carbohydrate metabolism.

Investigation of Phytochemical Composition, Radical Scavenging Potential, Anti-obesogenic Effects, and Anti-diabetic Activities of Kaempferia parviflora Rhizomes.

Kaempferia parviflora or commonly known as "Kunyit hitam" by locals, is an edible plant, native to tropical regions, has been extensively utilized for culinary and medicinal applications. The present study aimed to investigate the phytochemical composition and biological activities of the rhizomes of K. parviflora. The ethanol crude and fractionated extracts (hexane and chloroform) of the rhizomes were evaluated for their total phenolic content, total steroidal content, as well as antioxidant, anti-obesogenic, and anti-diabetic activities. The chloroform extract demonstrated the highest concentration of plant sterols (432 ± 0.23 mg BSE/g extract) and a substantial amount of phenolic compounds (1.19 × 103 ± 0.41 mg GAE/g extract). Gas chromatography-mass spectrometry (GC/MS) analysis revealed that the chloroform extract of the rhizomes is predominantly composed of bioactive flavonoids including tectochrysin (1), 5,7-dimethoxyflavone (2), 3,5,7-trimethoxyflavone (3), 3,4',5,7-tetramethoxyflavone (4), and 4',5,7-trimethoxyflavone (5). Furthermore, the chloroform extract exhibited the highest overall radical scavenging and α-glucosidase inhibitory activities, which can be attributed to the presence of compounds 1-5 in the extract. Collectively, these findings suggest that the chloroform extract of the rhizomes of K. parviflora is a potentially valuable source of bioactive compounds with antioxidant, anti-obesogenic, and anti-diabetic properties, with potential application in therapeutics and functional foods.

Exploring sesquiterpene lactone as a dual therapeutic agent for diabetes and oxidative stress: insights into PI3K/AKT modulation.

Diabetic mellitus (DM) is characterized by hyperglycaemia and defective macromolecular metabolism, arising from insulin resistance or lack of insulin production. The present study investigates the potential of artemisinin, a sesquiterpene lactone isolated from Artemisia annua, to exert anti-diabetic and antioxidant effects through modulation of the phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT) signalling pathway. Our computational analyses demonstrated a high binding affinity of artemisinin with proteins belonging to the PI3K/AKT signalling cascade. α-Amylase and α-glucosidase studies revealed a notable increase in inhibition percentages with artemisinin treatment across concentrations ranging from 10 to 160 µM. A similar significant (p < 0.05) dose-dependent inhibition of free radicals was observed for the in vitro anti-oxidant assays. Further, toxicological profiling of artemisinin in the in vivo zebrafish embryo-larvae model from 4 to 96 h post-fertilization (hpf) did not exhibit any harmful repercussions. In addition, gene expression investigations confirmed artemisinin's potential mechanism in modulating hyperglycaemia and oxidative stress through the regulation of the PI3K/AKT pathway. Overall, our investigation suggests that artemisinin can be used as a therapeutic intervention for diabetes and oxidative stress, opening up opportunities for future investigation in clinical settings. Supplementary Information: The online version contains supplementary material available at 10.1007/s13205-024-04050-2.

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.

[Anti-diabetic active constituents of pomegranate peel-derived extracellular nanovesicles].

Pomegranate peel-derived extracellular nanovesicles(PPENs) were isolated and purified by ultra-high speed centrifugation and sucrose density gradient centrifugation. Their morphology and structure were characterized. In vitro α-glucosidase inhibition assay and model test of insulin resistance(IR) in HepG2 cells showed that PPENs had good anti-diabetic activity. The IC_(50) value of α-glucosidase inhibition was(35.3±1.1) µg·mL~(-1), significantly better than the positive drug acarbose. At a concentration of 100 µg·mL~(-1), PPENs could increase the glucose absorption of IR cells significantly. Lipidome, proteome, and metabolite analysis of PPENs were performed using chromatography-mass spectrometry. MicroRNA(miRNA) sequences were identified, and target genes of miRNA were predicted. The analysis results indicated that PPENs contained abundant lipids and transport proteins, providing a material basis for the transportation and distribution of PPENs in tissue. Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment analysis suggested that lipids and miRNAs may be the key components of PPENs to exert anti-diabetic activity.

Phytochemical screening, antioxidant, anti-diabetic, and anti-obesity activities, formulation, and characterization of a self-nanoemulsion system loaded with pomegranate (Punica granatum) seed oil.

Pomegranate (Punica granatum) is a tree of the Punicaceae family that is widespread all over the world and has several types and therapeutic uses. The current study aimed to investigate the phytochemical compounds by GC analysis and carried out physical characterization of the pomegranate seed oil and its self-nanoemulsifying system. Then antioxidant, anti-diabetic, and anti-lipase activities were investigated for both.The pomegranate seed oil was extracted, and its self-nanoemulsifying system was then prepared. Phytochemical compounds were analyzed by GC, and physical characterization was established of the pomegranate seed oil and its self-nanoemulsifying system. Then antioxidant, anti-diabetic, and anti-lipase activities were investigated for both.The GC-MS analysis revealed that punicic acid, ß-eleosteric acid, catalpic acid, α-eleosteric acid, and oleic acid were the most predominant compounds in pomegranate seed oil. Other active compounds like linoleic acid, palmitic acid, stearic acid, and α-linolenic acid were detected in trace percentages. The self-nanoemulsifying system was prepared using various concentrations of surfactant (Tween 80), co-surfactant (Span 80), and pomegranate seed oil. The selected formulation had a PDI of 0.229 ± 0.09 and a droplet size of 189.44 ± 2.1 nm. The free radical scavenging activity of pomegranate seed oil, the self-emulsifying system, and Trolox was conducted using DPPH. The oil-self-nanoemulsifying system showed potent antioxidant activity compared to Trolox. Also, pomegranate oil inhibited α-amylase with a weak IC50 value of 354.81 ± 2.3 µg/ml. The oil self-nanoemulsifying system showed potent activity compared to acarbose and had a weaker IC50 value (616.59 ± 2.1 µg/ml) and a potent IC50 value (43.65 ± 1.9 µg/ml) compared to orlistat.Pomegranate seed oil self-nanoemulsifying system could be applied in the future for the preparation of possible oral medications for the prevention and treatment of oxidative stress, diabetes, and obesity due to its high activity against free radical, amylase, and lipase enzymes compared to pomegranate seed oil itself and the references used. This study reveals that self-nanoemulsion systems can enhance oil drug formulations by improving pharmacokinetics and pharmacodynamics, acting as drug reservoirs, and facilitating efficient oil release.

Harnessing the power of Arctium lappa root: a review of its pharmacological properties and therapeutic applications.

Arctium lappa, widely recognized as burdock, is a perennial plant that is employed in the realm of traditional Chinese medicine for a wide range of medicinal applications. The herb is rich in bioactive metabolites with therapeutic potential, encompassing polyphenolic antioxidants in its leaves, and flavonoids and fructo-oligosaccharides in its underground parts. Nutraceuticals originating from botanical sources such as Arctium lappa provide supplementary health advantages alongside their nutritional content and have demonstrated effectiveness in the prevention and management of specific ailments. The utilization of Arctium lappa root extract has exhibited encouraging outcomes in addressing hepatotoxicity induced by cadmium, lead, chromium, and acetaminophen, ameliorating liver damage and oxidative stress. Additionally, the root extract displays properties such as antidiabetic, hypolipidemic, aphrodisiac, anti-rheumatic, anti-Alzheimer, and various other pharmacological actions.

Structure-activity relationship of Hydrazinylthiazole-5-carbaldehydes as potential anti-diabetic agents.

Diabetes is an emerging threat to the world due to large number of deaths reported within the last decade. To overcome its spread and complications, herein, we reported synthesis and anti-diabetic potential of twelve novel 2-[(arylidene)methylidene]hydrazinyl-1,3-thiazole-5-carbaldehydes (3a-l). All compounds have shown good to excellent α-amylase inhibition activity, among them ortho substituted analogues, the compound 3a (IC50= 14.6 mM) and 3l (IC50= 17.9 mM) showed excellent inhibition potential due to their strong electron donating nature of the substituents attached at the aryl ring. The compounds 3a to 3h (IC50= 6.70-10.80 ppm) exhibited excellent anti-glycation potential as compared to standard amino-guanidine (IC50= 11.92 ppm). Almost all the tested compounds are found biocompatible and very safe to the human erythrocyte cells at all tested concentrations. The molecular docking results have found that the binding energy score of all the tested compounds against human serum albumin protein (pdb: 1AO6) is between -5.1827 to -6.8661 kcal/mol far better than standard amino-guanidine (-4.234 kcal/mol).

Antioxidant, In Vitro Cytotoxicity, and Anti-diabetic Attributes of a Drug-Free Guar Gum Nanoformulation as a Novel Candidate for Diabetic Wound Healing.

The escalating intersection of diabetes and impaired wound healing poses a substantial societal burden, marked by an increasing prevalence of chronic wounds. Diabetic individuals struggle with hindered recovery, attributed to compromised blood circulation and diminished immune function, resulting in prolonged healing periods and elevated healthcare expenditures. To address this challenge, we report here a drug-free novel guar gum (GG)-based nano-formulation which is effective against diabetic wound healing. Nanoparticles with an average particle size of 32.4 nm display stability with negative zeta potential. Differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) analysis reveal alterations in thermal properties and molecular structures induced by the nano-particulation process. In vitro studies highlight the antioxidant potential of GGNP through concentration-dependent free radical scavenging activity in DPPH and ABTS assays. The nanoformulation also exhibits inhibitory effects on α-glucosidase and α-amylase enzymes. Cell viability studies have indicated moderate cytotoxicity in L929 cells and significant proliferation and migration in HaCaT cells, suggesting a positive impact on skin cells. In vitro enzymatic activity assessments under hyperglycaemic conditions reveal the potential of GGNP to modulate glutathione-S-transferase (GST), superoxide dismutase (SOD), and catalase activities as well as decreasing lipid peroxidation (LPO) levels, showcasing an antioxidant response. These results suggest GGNP as a promising candidate in diabetic wound healing.

Evaluation of destruction of bacterial membrane structure associated with anti-quorum sensing and ant-diabetic activity of Cyperus esculentus extract.

Recently, there has been an increasing demand for medicinal plants to control diseases for good health and well-being, as primary health facilities are inadequate in certain populations to cure infections. Since synthetic medicines are toxic to humans and other animals, the present research is thus focused on using traditional medicine for treating various ailments as they are harmless. Based on the above facts, the current study was conducted to assay the antimicrobial, anti-diabetic, anti-cholinesterase, anti-oxidant, anti-quorum sensing, and anti-antibiotic resistance modifying effect of extracts of Cyperus esculentus. This study found 37 and 30 chemicals in butanol and dichloromethane (DCM) extracts using a gas chromatograph mass spectrophotometer (GC-MS). Most active compounds identified were benzofuran, 2,3-dihydro-, 1,2,3-benzenetriol, 3-bornanone, oxime and oleic acid by extracts of butanol whereas dichloromethane extracted three major active compounds (2,3-dihydro-3,5-dihydroxy-, 4H-pyran-4-one 3-deoxy-d-mannoic lactone and 5-hydroxymethylfurfural). Both dichloromethane and butanol extracts showed the highest antimicrobial activity. Compared to aqueous extracts, dichloromethane, and butanol showed excellent anti-diabetic anti-cholinesterase activities and inhibited virulence factors regulated by quorum sensing (QS). Anti-oxidants increased in solvent extracts (DCM and butanol) compared to aqueous extracts. Results of scanning electron microscope (SEM) and Fourier Transmission Infrared (FTIR) indicated damage to the cell membrane of S. aureus by the formation of pits and breakage in functional groups exposed to the extracts of butanol and dichloromethane compared to aqueous extracts. The above results confirmed that C. esculentus can be an alternative medicine for treating diseases.

Curcumin, a bioactive compound of Turmeric (Curcuma longa) and its derivatives as α-amylase and α-glucosidase inhibitors.

Diabetes mellitus (DM) is a long-term metabolic disease characterised by a controlled metabolism of fat, carbohydrates, and proteins. In recent decades, it has grown into a significant global public health issue. According to the International Diabetes Federation, there were 425 million DM globally in 2017, and the number might be increased to 629 million by 2045 (a global 48% increase). Approximately 4.2 million deaths globally attributed to DM occur before the age of 60. The existing class of anti-diabetic medications is limited by side effects, which has led to the hunt for novel inhibitors that specifically target the α-amylase and α-glucosidase enzymes. Curcumin is a small-molecular-weight compound found in the roots of the Curcuma longa L (C. longa). plant, which has been used for culinary, medicinal, and other purposes throughout Asia for thousands of years. Curcumin has potent anti-inflammatory, anti-cancer, anti-angiogenic, antispasmodic, antibacterial, and anti-parasitic qualities. Even though the potential of curcumin to cure DM has been well investigated, its low solubility, rapid metabolism, and short plasma half-life have limited its application in DM. Therefore, the objectives of this review were to review the chemical composition of C. longa, the structure of curcumin, the degradation of curcumin, and the effects of curcumin derivatives on anti-diabetic properties against α-amylase and α-glucosidase enzymes. The results showed that C. longa contains carbohydrates, moisture, protein, fat, minerals, volatiles, fibre, and curcuminoids. Among the curcuminoids, curcumin is 60-70% present in C. longa. Moreover, curcumin and its derivatives have a lot of potential for treating DM, which was highlighted in this review. This review emphasises the several biological applications of curcumin, which collectively establish the foundation for its anti-diabetic characteristics. Considering these results, curcumin derivatives may be considered as potential agents in the pharmacotherapeutic management of patients with DM.

Oil/water (O/W) nanoemulsions developed from essential oil extracted from wildly growing Calotropis gigantea (Linn.) Aiton F.: synthesis, characterization, stability and evaluation of anti-cancerous, anti-oxidant, anti-inflammatory and anti-diabetic activities.

Calotropis gigantea essential oil is utilized in outmoded medicine, therapeutics, and the cosmetic industries. However, the extreme volatility, oxidation susceptibility, and instability of this oil restricts its application. Thus, encapsulation is a more effective method of shielding this oil from unfavorable circumstances. The creation of oil/water (O/W) nanoemulsions based on Calotropis gigantea essential oil (CEO), known as CNE (Calotropis gigantea essential oil nanoemulsions), and an assessment of its biological potential were the goals of this work. UV, fluorescence, and FT-IR methods were used for physiological characterization. Biological activities, including anti-inflammatory, anti-diabetic, and anti-cancer effects. Studies on the pharmacokinetics of CNE were conducted. CNEs encapsulation efficiency was found to be 92%. The CNE nanoemulsions had a spherical shape with polydispersity index of 0.531, size of 200 nm, and a zeta potential of -35.9 mV. Even after being stored at various temperatures for 50 days, CNE nanoemulsions remained stable. Numerous tests were used to determine the antioxidant capacity of CNE, and the following IC50 values (µl/mL) were found: iron chelating assay: 18, hydroxyl radical scavenging: 37, and nitric oxide radical scavenging activity: 58. The percentage of HeLa cells that remained viable after being treated with CNE was 41% at a higher dose of 1 µl. CNE inhibited α-amylase in a dose-dependent manner, with 72% inhibition at its higher dose of 250 µL. Research on the kinetics of drugs showed that nanoemulsions showed Higuchi pattern. This research showed potential use of Calotropis gigantea oil-based nanoemulsions in the food, cosmetic, and pharmaceutical industries.

Investigation of the phytochemical profiling and antioxidant, anti-diabetic, anti-inflammatory, and MDA-MB-231 cell line antiproliferative potentials of extracts from Ephedra alata Decne.

Ephedra is one of the many medicinal herbs that have been used as folk/traditional medicine in Jordan and other countries to cure various illnesses. Plants of this genus are well known for their antioxidant and antibacterial properties. In this study, three different solvents were used to obtain Ephedra extracts. When evaluated, the Ephedra alata Decne ethanolic extract reportedly had the greatest levels of total phenolic compounds (TPC) and total flavonoid compounds (TFC). The aqueous extracts displayed the highest antioxidant activity in the DPPH and ABTS assays, demonstrating their considerable capacity to neutralize free radicals. However, when evaluated using the FRAP method, the acetone extracts showed the strongest antioxidant activity, indicating their high reducing power. LC-MS/MS, a potent method of analysis that combines the liquid chromatographic separation properties with mass spectrometry detection and identification capabilities, was used in this study to detect and measure phytochemical content of a total of 24 phenolic compounds and 16 terpene compounds present in the extracts of Ephedra alata Decne. Various concentrations of these chemicals were found in these extracts. The extracts' inhibitory effects on albumin denaturation and alpha-amylase activity were also assessed; the findings demonstrated the potentials of these extracts as anti-inflammatory and anti-diabetic medicines, with the acetone extract having the lowest IC50 values in the concomitant tests (306.45 µg/ml and 851.23 µg/ml, respectively). Furthermore, the lowest IC50 value (of 364.59 ± 0.45 µg/ml) for the 80% ethanol extract demonstrated that it has the strongest antiproliferative impact regarding the MDA-MB-231 breast cancer cell line. This finding indicates that this particular extract can be potentially used to treat cancer.

Health Risk Assessment of Toxic Metal(loids) Consumed Through Plant-Based Anti-diabetic Therapeutics Collected in the Northern Divisional City of Rajshahi, Bangladesh.

The present study investigates human health risks upon consumption of herbal medicines in terms of ten toxic metalloids in 20 plant-based anti-diabetic therapeutics. The analysis of metalloids was determined by an atomic absorption spectrometer after microwave-assisted digestion. The computation of hazard quotients (HQ) and hazard indexes (HI) of metalloids leads to the assessment of non-carcinogenic health risks. Carcinogenic risk was assessed based on cancer slope factor (CSF) and chronic daily intake (CDI) values. Comparison with WHO regulatory cut-off points for each metalloid: seven samples for Mn, 12 samples for Hg, three samples for Cu, eight samples for Ni, four samples for Cd, two samples for Pb, one sample for Cr, and eight samples for Zn are unsafe to consume. Non-carcinogenic human health risk is predicted for Mn in seven samples, Fe in one sample, Hg in ten samples, Cu in three samples, Ni in one sample, and Pb in two samples. HI values greater than 1 predict non-carcinogenic health risk in thirteen samples. Incremental lifetime cancer risk (ILCR) remains for As (inorganic) in 12 samples, Cr (+ 6) in one sample, and Pb in no samples. To guarantee consumer safety, the implementation of strict monitoring is suggested.