Potential Antidiabetic Activity Research Articles

An Update on Pharmacological and Phytochemical Aspects of Costus pictus D. Don - A Promising Anti-diabetic Plant.

The genus Costus is the largest genus in the family Costaceae and encompasses about 150 known species. Among these, Costus pictus D. Don (Synonym: Costus mexicanus) is a traditional medicinal herb used to treat diabetes and other ailments. Currently, available treatment options in modern medicine have several adverse effects. Herbal medicines are gaining importance as they are cost-effective and display improved therapeutic effects with fewer side effects. Scientists have been seeking therapeutic compounds in plants, and various in vitro and in vivo studies report Costus pictus D. Don as a potential source in treating various diseases. Phytochemicals with various pharmacological properties of Costus pictus D. Don, viz. anti-cancer, anti-oxidant, diuretic, analgesic, and anti-microbial have been worked out and reported in the literature. The aim of the review is to categorize and summarize the available information on phytochemicals and pharmacological properties of Costus pictus D. Don and suggest outlooks for future research. This review combined scientific data regarding the use of Costus pictus D. Don plant for the management of diabetes and other ailments. A systematic search was performed on Costus pictus plant with anti-diabetic, anti-cancer, anti-microbial, anti-oxidant, and other pharmacological properties using several search engines such as Google Scholar, PubMed, Science Direct, Sci-Finder, other online journals and books for detailed analysis. Research data compilation and critical review of the information would be beneficial for further exploration of its pharmacological and phytochemical aspects and, consequently, new drug development. Bioactivity-guided fractionation, isolation, and purification of new chemical entities from the plant as well as pharmacological evaluation of the same will lead to the search for safe and effective novel drugs for better healthcare. This review critically summarizes the reports on natural compounds, and different extract of Costus pictus D. Don with their potent anti-diabetic activity along with other pharmacological activity. Since this review has been presented in a very interactive manner showing the geographical region of availability, parts of plant used, mechanism of action and phytoconstituents in different extracts of Costus pictus responsible for particular action, it will be of great importance to the interested readers to focus on the development of the new drug leads for the treatment of diseases.

Evaluation of Antidiabetic Activity and Cytotoxic Effect of Strontium Nanoparticles Synthesized Using Mimosa Pudica.

Nanotechnology is emerging as a promising approach in the development of novel therapeutic strategies. Nanoparticles, due to their unique physicochemical properties and small size, have the potential to improve the delivery of therapeutic agents, enhance their bioavailability, and increase their efficacy. Among various types of nanoparticles, strontium nanoparticles have gained attention due to their potential antidiabetic activity and cytotoxic effects against cancer cells. Mimosa pudica, also known as "Sensitive Plant" or "Touch-Me-Not," is a medicinal plant known for its diverse pharmacological activities, including antidiabetic and anticancer properties. Recent research has focused on the synthesis of strontium nanoparticles by using Mimosa pudica as a green and sustainable approach. These nanoparticles have shown promising results in terms of their antidiabetic activity and cytotoxic effects against cancer cells. Thus, in this study, the antidiabetic effect was studied using the alpha-amylase inhibitor assay, and the cytotoxic effect was studied using the brine shrimp lethality assay. In these assays, increasing concentration of Mimosa pudica-mediated strontium nanoparticles exhibited increasing antidiabetic and cytotoxic effects, which was similar to the standard used, which is acarbose. Hence, this can be used as a novel antidiabetic and cytotoxic agent in the future.

Efficacy of Quercetin and Kaempferol from Methanolic Extracts of Adiantum lunulatum Burm. F. and Polystichum acrostichoides as Antidiabetic Activity

In present investigation, the aerial parts of two fern species viz. Polystichum acrostichoides (PA) and Adiantum lunulatum (AL) were used to evaluate the potent antidiabetic activity. Methanol solvent was used for extraction by soxhlation method followed by LC-MS analysis to identify the presence of compounds in both the extracts. Further, isolation of the major compounds was carried out and characterized by IR, mass and NMR techniques. Thereafter, in vitro α-amylase inhibitory activity for both the extracts was determined by comparing with acarbose as standard. Thereafter, α-glucosidase inhibition activity followed by glucose uptake was studied using L6 cell line study. Practical yield for both the fern extracts was calculated and observed A. lunulatum extract showed more yield (7 g) than P. acrostichoides (3 g). Based on the analytical data, isolated compound was identified as quercetin and kaempferol from the A. lunulatum and P. acrostichoides extracts, respectively. A. lunulatum extract even showed better dose dependent α-amylase inhibition and α-glucosidase inhibition activity than P. acrostichoides furthermore, L6 cell line study showed increased glucose uptake by A. lunulatum extract than P. acrostichoides extract when compared with standard insulin. Based on the findings, it appears that the both A. lunulatum and P. acrostichoides have the potential to be used as antidiabetic drugs due to presence of major isolated flavonoids i.e. quercetin and kaempferol as among the bioactive compounds. Antidiabetic efficacy was dosage dependent and A. lunulatum extract was more effective in inhibiting glucose uptake than P. acrostichoides extract.

Oral glucose tolerance assay of extract from Mangifera foetida l. and Pandanus amaryllifolius roxb. leaves

This study examines the potential antidiabetic activity of a combination of Mangifera foetida L. and Pandanus amaryllifolius Roxb. leaves. Mangifera leaves contain a compound called mangiferin, which acts as an antidiabetic and antioxidant. On the other hand, Pandanus leaves, are rich in terpenoids and steroids that also possess anti-diabetic effects. An Oral Glucose Tolerance Test (OGTT) was conducted on male mice of the Babl/c strain to assess the antidiabetic effects. The test involved administering a combination of ethanolic leaf extracts from Mangifera foetida L. and Pandanus amaryllifolius Roxb. in a 1:1 ratio. The study followed a pre-test design with a control group, comprising six treatment groups, each consisting of four male mice. The groups were described as follows: Group 1 was served as the normal group without any treatment. Groups II-IV received single extracts or combinations of extracts at doses of 62.5 mg/200g BW, 125 mg/200g BW, and 250 mg/200g BW. Group V acted as the positive control and was given oral glucose and glibenclamide at a dose of 0.09 mg/200g BW. Group VI was served as the negative control, receiving oral glucose and distilled water. The group that exhibited the highest percentage of decreased blood sugar levels was the one given oral glucose at a dose of 0.078g/20g BW of mice, along with the combination of Mangifera foetida L. and Pandanus amaryllifolius Roxb. leaves extract (1:1) at a dose of 35 mg/20g BW. This group demonstrated a decrease of 71.985 ± 4.858 in blood glucose levels. The ANOVA analysis confirmed that the percentage decrease in blood sugar levels was significantly different from the positive control, indicating a higher effectiveness of the combination treatment in reducing blood glucose levels than the positive control.

Potential Antidiabetic Activity of Apis mellifera Propolis Extraction Obtained with Ultrasound.

Recent studies have linked phenolic compounds to the inhibition of digestive enzymes. Propolis extract is consumed or applied as a traditional treatment for some diseases. More than 500 chemical compounds have been identified in propolis composition worldwide. This research aimed to determine Mexican propolis extracts' total phenolic content, total flavonoid content, antioxidant activity, and digestive enzyme inhibitory activity (ɑ-amylase and ɑ-glucosidase). In vitro assays measured the possible effect on bioactive compounds after digestion. Four samples of propolis from different regions of the state of Oaxaca (Mexico) were tested (Eloxochitlán (PE), Teotitlán (PT), San Pedro (PSP), and San Jerónimo (PSJ)). Ethanol extractions were performed using ultrasound. The extract with the highest phenolic content was PE with 15,362.4 ± 225 mg GAE/100 g. Regarding the flavonoid content, the highest amount was found in PT with 8084.6 ± 19 mg QE/100 g. ABTS•+ and DPPH• radicals were evaluated. The extract with the best inhibition concentration was PE with 33,307.1 ± 567 mg ET/100 g. After simulated digestion, phenolics, flavonoids, and antioxidant activity decreased by 96%. In contrast, antidiabetic activity, quantified as inhibition of ɑ-amylase and ɑ-glucosidase, showed a mean decrease in enzyme activity of approximately 50% after the intestinal phase. Therefore, it is concluded that propolis extracts could be a natural alternative for treating diabetes, and it would be necessary to develop a protective mechanism to incorporate them into foods.

Identification and molecular docking of a novel antidiabetic peptide from protamex-camel milk protein hydrolysates against α-amylase and DPP-IV

Antidiabetic peptides were identified from camel milk protein hydrolysates, and their inhibitory activities against α-amylase and dipeptidyl peptidase-IV (DPP-IV) were determined. The possible binding mechanism between the enzymes and the peptide was elucidated through molecular docking. Camel milk proteins were hydrolyzed using protamex, and the hydrolysates were divided into three fractions (>10, 3–10, and <3 kDa) through ultrafiltration. Fraction <3 kDa was more effective at inhibiting α-amylase and DPP-IV and was purified through gel chromatography and identified through LC-MS/MS. In total, 20 peptides were considered as potential bioactive peptides, mainly derived from β-casein. The novel peptide QEPVPDPVRGL exhibited the most potent antidiabetic activity and spontaneously interacted with α-amylase and DPP-IV through hydrogen bonds, salt bridges, and pi–alkyl, thereby occupying their active cavities. This study indicated that camel milk protein hydrolysates are good sources of peptides with antidiabetic potential.

Innovation of 6-sulfonamide-2H-chromene derivatives as antidiabetic agents targeting α-amylase, α-glycosidase, and PPAR-γ inhibitors with in silico molecular docking simulation.

A new series of 2-imino or 2-oxo-2H-chromene-6-sulfonamide derivatives 2-9 with potential anti-diabetic activity were designed and synthesized. The new 6-sulfonamide chromenes were synthesized by reacting 3-formyl-4-hydroxybenzenesulfonyl chloride with activated methylene derivatives in the presence of ammonium acetate as a catalyst. The structure of the products was confirmed by spectroscopic analysis. All the designed derivatives 2-9 were evaluated for their activity against α-amylase and exhibited inhibitory percentage values higher than 93% at 100 μg mL-1. Additionally, the IC50 values represented a variable degree of activity with two derivatives 2 and 9 exhibiting the most promising derivative results with IC50 values of 1.76 ± 0.01 and 1.08 ± 0.02 μM, respectively, compared to Acarbose (IC50 = 0.43 ± 0.01 μM). Additionally, these derivatives showed potency against the α-glucosidase enzyme with IC50 values of 0.548 ± 0.02 and 2.44 ± 0.09 μg mL-1, compared to Acarbose (0.604 ± 0.02 μg mL-1). Moreover, the in vitro PPAR-γ transactivation assay revealed that chromene-6-sulfonamide derivatives 2 and 9 exhibited potential PPAR-γ activity with IC50 values of 3.152 ± 0.03 and 3.706 ± 0.32 μg mL-1, respectively, compared to Pioglitazone (4.884 ± 0.29 μg mL-1). This indicates that these derivatives have insulin sensitivity and glucose metabolism activity. The in silico ADMET prediction showed that these derivatives have an acceptable range of oral bioavailability, drug-likeness, and a safe toxicity profile, including being non-cytotoxic, non-mutagenic, non-immunotoxic, and non-carcinogenic. Finally, computational docking analysis demonstrated the ability of these derivatives to interact with α-amylase, α-glucosidase, and PPAR-γ enzymes, with confirmed successful placement due to good binding energy values and various interactions within the pocket.

Design, Synthesis, and Molecular Docking Studies of Integrated Benzylidenethiazolidine‐2,4‐Dione and Thieno[2,3‐d]pyrimidine‐6‐Carboxylate Derivatives as Potent Antidiabetic agents

AbstractThe present work describes the synthesis of new series of 5‐arylidene‐thiazolidine‐2,4‐dione, thieno[2,3‐d]pyrimidine‐6‐carboxylate derivatives 9 a–o. A variety of spectroscopic techniques like IR, 13CNMR, 1HNMR and LCMS were used to establish the presence of the every synthesized scaffold. The antioxidant activity of the target compounds has been studied by three different methods indicated the significant DPPH, NO and H2O2. Further, all the derivatives were evaluated for the in vitro antidiabetic potential against human pancreatic α‐amylase (PDB ID: 5NN3) and human lysosomal acid α‐glucosidase (PDB ID: 2QV4) enzymes followed by Molecular docking studies to ascertain the binding interactions of the compounds with the enzymes. The compounds 9 b and 9 g containing methoxy groups were found to exhibit potent antidiabetic and antioxidant activity. Therefore, it was rationalized that two privileged pharmacophores i. e. aryledenethiazolidine‐2,4‐dione and thieno[2,3‐d]pyrimidine‐6‐carboxylate assimilated hybrids, may be beneficial as lead template for the advance of future anti‐diabetic agents. Thus, benzylidenethiazolidine‐2,4‐dione and thieno[2,3‐d], the two preferred pharmacophores, were rationalized. Assimilation of ‐pyrimidine‐6‐carboxylate hybrids could be advantageous as a lead template for the development of new anti‐diabetic drugs.

Dioscorea alata L. Tubers Ethanol Extract Improves Insulin Resistance and Estrogen Defectively in Type 2 Diabetic Ovariectomized Rats

Dioscorea alata L., commonly known as water yam, has attracted the attention of scientific researchers for its potential anti-diabetic and estrogenic properties. However, the existing literature lacks specific studies on the anti-diabetic and estrogenic effects of D. alata in the context of type 2 diabetic ovariectomized rats. Thus, Our research focuses on investigating the influence of D. alata on the antidiabetic and estrogenic properties in rats. These rats have developed diabetes through a high-fat diet and streptozotocin induction and have also undergone ovariectomy, making them type 2 diabetic ovariectomized rats (T2DM OVX). This comprehensive study both in vitro and in vivo methodologies. We conducted a phytochemical analysis, revealing the presence of key bioactive constituents, including flavonoids, alkaloids, terpenoids, tannins, saponins, cardiac glycosides, and steroids. The results of our phytochemical screening confirm the remarkable antidiabetic properties of the D. alata extract, as it effectively inhibits α-glucosidase activity, leading to a significant reduction in fasting blood glucose levels. Additionally, it enhances body weight, serum insulin levels, and pancreatic islet size. The extract also demonstrates notable estrogenic effects by significantly increasing uterine wet weight, endometrial and myometrium thickness, bone calcium, and overall bone density, while reducing bone porosity in the T2DM OVX rats. It is important to note that while the D. alata extract exhibits slightly less potent α-glucosidase inhibition compared to acarbose, it showcases potent antidiabetic activity at a dose of 1,000 mg/kg body weight, comparable to Metformin (250 mg/kg body weight). In terms of estrogenic activity, it is slightly less potent than 17β-estradiol (1 mg/kg body weight). These findings provide robust evidence supporting the traditional use of D. alata and its efficacy in the context of antidiabetic and estrogenic properties within the T2DM OVX model.

Determination of antioxidant, antimicrobial, anticholinesterase, antityrosinase, antidiabetic and antiglaucoma activities of essential oils from three different Thymus species and their chemical characterization by GC-MS analysis

The present study aims to perform a comprehensive chemical characterization of the essential oils of Thymus pubescens var. pubescens (TPEO), Thymus leucotrichus var. leucotrichus (TLEO), and the endemic Thymus canoviridis (TCEO) using GC-MS, besides evaluating the potential antidiabetic, anticholinesterase, antimicrobial, antioxidant, antiglocouma, and antityrosinase activities of these essential oils. The antioxidant activity was assessed using various bioassays including DPPH, ABTS, DMPD, FRAP, CUPRAC, and Fe3+ reducing assays. The IC50 values of TPEO, TLEO, and TCEO for α-glycosidase were 28.32, 28.79, and 57.57 μg/mL, respectively. For tyrosinase, the IC50 values were 359.9, 270.87, and 597.43 μg/mL, respectively. The IC50 values for acetylcholinesterase were calculated as 44.15, 36.75, and 34.99 μg/mL, respectively, while for carbonic anhydrase, the IC50 values were 21.70, 24.75, and 24.45 μg/mL, respectively. The quantitiy of total phenolics present in TPEO, TLEO, and TCEO were determined to be 10.50, 34.50, and 32.50 μg GAE/mg essential oil, respectively. The TPEO, TLEO, and TCEO exhibited distinct antioxidant activities on DPPH, ABTS, and DMPD. TPEO showed antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Acinetobacter baumannii bacterias. TLEO exhibited effective antimicrobial activity against S. aureus; The last of these TCEO demonstrated notable antimicrobial activity towards S. aureus, Enterococcus faecalis, E. coli, K. pneumoniae, Pseudomonas aeruginosa, P. mirabilis, A. baumannii. Additionaly, GC-MS revealed that the major components are TPEO (pulegone 29.01%, piperitenone 17.17%), TLEO (germacrene D 9.59%), and TCEO (carvacrol 52.87%). The essential oils possessed a range of biological activities, including antioxidant, antidiabetic, anticholinesterase, antityrosinase, antiglocouma and antimicrobial activities.

BAAE-AgNPs Improve Symptoms of Diabetes in STZ-induced Diabetic Rats.

Nanoparticles can be employed to improve the therapeutic activity of natural products. Type 2 diabetes mellitus is a serious health condition that has spread like a "modern pandemic" worldwide. In the present study, we developed silver nanoparticles, AgNPs, with an aqueous extract from Balanites aegyptiaca to investigate their antioxidant and anti-inflammatory activity in STZ-induced diabetic rats. Aqueous extracts of Balanites aegyptiaca seeds (BAAE) were used in the synthesis of BAAE-AgNPs, which were characterized using FTIR and TEM. Different doses of BAAE-AgNP (1/50 LD50; 29.4 mg/kg b.w. and 1/20 LD50:73.5 mg/kg b.w.) were administered to STZ-induced diabetic rats to evaluate their potential antidiabetic activity. FTIR spectral data indicated the presence of flavonoids and polyphenols in BAAE-AgNPs. The size of the BAAE-AgNPs, determined by TEM examination, was 49.33 ± 7.59 nm, with a zeta potential of +25.37. BAAE-AgNPs were characterized by an LD50 value of 1470 mg/kg b.w. In diabetic rats, the daily oral administration of both doses of BAAE-AgNPs (29.4 and 73.5 mg/kg b.w.) for 12 weeks resulted in a significant improvement in body weight, insulin homeostasis, HbA1c, HDL-C, MDA, and pancreatic SOD, CAT, and GSH. They reduced plasma glucose, cholesterol, and triglycerides. This treatment also resulted in a significant decrease in pancreatic IL-6, P53, and TNF-α in diabetic rats. Furthermore, BAAE-AgNPs down-regulated pancreatic TGF-β1 and Akt gene expression in diabetic rats and resulted in a significant decrease in the regulation of hepatic GLUT-2, as well as an increase in the regulation of hepatic GK and pancreatic B-cl2 gene expression. The histopathological results obtained indicated that BAAE-AgNPs improved pancreatic tissue metabolism by enhancing antioxidant enzymes, suppressing inflammatory cytokines, and scavenging free radicals. The findings implied that similar to the glibenclamide-treated groups, in the BAAE-AgNPs treated group, the compromised antioxidant status normalized in STZ-induced diabetes. By scavenging free radicals, BAAE-AgNPs protected against lipid peroxidation while reducing the risk of complications from diabetes. Compared to the daily dose of 29.4 mg, the impact was more prominent at 73.5 mg.

Green synthesis and evaluation of anti-microbial, antioxidant, anti-inflammatory, and anti-diabetic activities of silver nanoparticles from Argyreia nervosa leaf extract: An invitro study

The aim of the study is to develop an environmentally friendly development of isolating silver nanoparticles using Argyreia nervosa plant leaves and examine their potential pharmacological properties, including antibacterial, anti-inflammatory, antioxidant, and anti-diabetic activities. Various analytical techniques were employed to examine the isolated silver nanoparticles, encompassing UV spectroscopy, XRD, SEM, EDX, FTIR, zeta potential measurement, and particle size determination. Furthermore, Argyreia nervosa-mediated silver nanoparticles exhibited strong antioxidant, anti-inflammatory activity, and good anti-diabetic activity. Argyreia nervosa-mediated nanoparticles showed a significant antibacterial activity against selected pathogens. The findings indicate that Argyreia nervosa demonstrates encouraging pharmacological properties. However, additional in vivo research focusing on molecular-level investigations is necessary to substantiate these findings and explore the potential of Argyreia nervosa-mediated silver nanoparticles as a viable drug for antioxidant, antibacterial, and anti-diabetic purposes.

Bioactive potential of ripened white cheeses manufactured in different geographical regions of Turkey.

This study investigated the potential bioactive properties of white cheeses produced in different regions of Turkey, including their potential antioxidant, antihypertensive, antidiabetic, antimicrobial, and anticancer activities. The cheese samples were analyzed both before and after in vitro digestion. The study found that all cheese samples exhibited significant angiotensin-converting enzyme inhibition activity both before (45.5%-70.1% for 0.03gcheese/mL) and after in vitro digestion (25.5%-63.5% for 0.0167g cheese/mL), whereas α-amylase inhibition activity was present in all samples (in the range of 5.1%-50.0% for 3.0×10-5 gcheese/mL) but disappeared after digestion, and α-glucosidase inhibition activity was only detected after in vitro digestion (from 20.5% to 60.4% for 5.6×10-5 gcheese/mL), indicating potential antidiabetic properties. However, antimicrobial and anticancer activities were not observed in any of the samples. The results also suggest that the bioactivity potential of white cheese may vary depending on the region of production, as cheeses from the Marmara region exhibited high α-glucosidase inhibition activity after digestion. In conclusion, while white cheese is a valuable addition to the diet due to its high nutritional value and potential health benefits. This study revealed the bioactive potential of ripened white cheese and in vivo investigations of the cheese components would better show their possible benefits. PRACTICAL APPLICATION: Although the bioactivity potentials varied among the ripened white cheese samples produced in different regions of Turkey, a consistent trend was observed in terms of their presence or absence. Our research revealed that all ripened cheese samples demonstrated significant potential antioxidant and antihypertensive activities, as well as potential antidiabetic properties. Moreover, it can be interpreted that ripened white cheese has the potential to reduce the digestion of carbohydrates when consumed with carbohydrate-rich foods. Although the present results provide limited practical findings directly applicable to the industry, if the data and information obtained from this study are further explored and further studies delving into specific mechanisms of bioactive components could emerge.

Supercritical CO2 Extraction, Quantification and Pharmacological Screening of Steroidal Saponins from Fruits of Momordica charantia L

Momordica charantia L. (MC), a Cucurbitaceae family member, is the most recognized plant for its hypoglycemic activity. Charantin, a steroidal saponin, is the most studied potent phytochemical in MC for diabetes. This research paper aims at the extraction, quantification and pharmacological screening of charantin, from fruits of MC. Extraction was performed by using traditional soxhlet extraction and modified supercritical fluid extraction (SFE) techniques, and compared the results of both techniques in terms of percent extract yield, quantity of charantin and in-vitro antidiabetic activity of both extracts. (Soxhlet extract and SC-CO2 extract). Further, quantitative estimation of charantin in both extracts was done by HPLC-UV method and it was validated as per the ICH guidelines. When compared to soxhlet extract, the SC-CO2 extract displayed high antihyperglycemic activity by blocking α-amylase and α-glucosidase enzymes. Study also indicates that SC-CO2 extract had higher antioxidant activity (0.25 mg/mL) than soxhlet extract (0.33 mg/mL), signifying the SFE technique’s efficiency over the traditional soxhlet extraction method. In-vitro antidiabetic study indicated that the biomolecule charantin extracted from fruits of MC possess potent antidiabetic and high antioxidant activities and, therefore, hold potential for manufacturing innovative natural remedies to treat diabetes and its complications with no side effects.

Investigation of α-glucosidase and α-amylase inhibitory effects of phenoxy chalcones and molecular modeling studies.

Diabetes mellitus is one of the most critical health problems affecting the quality of life of people worldwide, especially in developing countries. According to the World Health Organization reports, the number of patients with diabetes is approximately 420 million, and this number is estimated to be 642 million in 2040. There are 2 main types of diabetes: Type 1 (T1DM), where the body cannot produce enough insulin, and Type 2 (T2DM), where the body cannot use insulin properly. Patients with T1DM are treated with insulin injections while oral glucose-lowering drugs are used for patients with T2DM. Oral antihyperglycemic drugs used in the treatment of type 2 diabetes mellitus have different mechanisms. Among these, α-Glucosidase and α-amylase inhibitors are one of the most important inhibitors. The antidiabetic effect of the chalcones, which show rich activity, draws attention. This research aims to synthesize chalcone derivatives that could show potential antidiabetic activity. In this study, the inhibitory activity of the chalcone compounds (4a-4g, 5a-5g) was tested against α-glucosidase and α-amylase enzymes. Besides, molecular modeling was utilized to predict potential interactions of the synthesized compounds that exhibit inhibitory effects. In both in vitro and in silico studies, the analyses revealed that compound 5e exhibits strong inhibitory effects against α-glucosidase enzymes (Binding energy: -7.75 kcal/mol, IC50 : 28.88 μM). Additionally, compound 4f demonstrates encouraging inhibitory effects against α-Amylase (Binding energy: -11.08 kcal/mol, IC50 : 46. 21 μM).

A comparative MS-based metabolomics study and in-vitro antidiabetic assay of galangals, turmeric and ginger aided by molecular networking and chemometrics

Ginger and turmeric and the less explored galangals, are economically important spices belonging to the Zingiberaceae family, widely used in traditional medicines and nutraceuticals. The present study provides the first comparative MS based metabolomics investigation of galangals compared to major ginger drugs and in relation to their in vitro antidiabetic effects. UPLC-MS/MS metabolomic profiles of galangals, turmeric, and ginger were analyzed using GNPS molecular networking leading to the annotation of 85 metabolites of which several are first time to be reported in galangals. Principle component analysis (PCA) and orthogonal projection to latent structures discriminant analysis (OPLS-DA) of UPLC-MS/MS profiles revealed the enrichment of flavonoids, styrenes and oxylipids in the extracts of both galangals, whereas gingerols, aryl- and diarylheptanoids were characteristic to ginger and turmeric, respectively. Aroma profiling using SPME–GC–MS identified 96 volatiles belonging to sesqui- and monoterpene derivatives. Multivariate data analysis of GC-MS dataset revealed calamenene, guaia-1(10),11-diene and selina-3,7(11)-diene as characteristic to ginger and turmeric aroma profiles. In contrast, greater galangal was enriched in acetoxychavicol acetate, aristolene, α-farnesene versus abundance of γ-elemene in lesser galangal. Additionally, methanolic extracts of both galangals exerted potential in vitro α-glucosidase inhibitory effect accentuating its potential antidiabetic activities.

Chemical compositions and different biological activity of leaf essential oil of Ocimum americanum L. grown in acidic soil conditions

s Ocimum americanum L. is a highly valued aromatic plant whose leaves are used not only in traditional cuisine but also in the food, cosmetic, and pharmaceutical industries. This study aimed to identify the chemical profile of essential oil extracted from the leaves of Ocimum americanum by GC-FID and GC/MS grown in acidic soil conditions in the NE region of India. Furthermore, the biological activities like antioxidant, anti-diabetic, anti-inflammatory, and anti-tyrosinase activity were analyzed, as per standard methods. GC and GC/MS analysis identified 16 compounds in which citral-a (48.25%) was found as a major compound, followed by carveol (41.64%). The antioxidant activity was performed using DPPH and ABTS methods; and IC50 value obtained was 8.85 μL/mL and 28.82 μL/mL, respectively. The leaf essential oil of O. americanum exhibited strong anti-diabetic and anti-inflammatory activities, whereas moderate anti-tyrosinase activities with IC50 values of 40.84, 12.81, and 182.74 μL/mL, respectively. Furthermore, the ant-microbial activity was evaluated for four bacterial and four fungal strains, revealing that O. americanum essential oil expresses antifungal activity against S. cereviaceae only with a MIC value of 5±0.47 μg/mL. These evidences clearly indicates that essential oil obtained from the leaf of O. americanum showed potential anti-inflammatory and anti-diabetic activity that can be used as an alternative in pharmaceuticals and food industries as a natural source.

Combined Experimental and Computational Study of V-Substituted Lindqvist Polyoxotungstate: Screening by Docking for Potential Antidiabetic Activity.

In the current work, a novel vanadotungstate compound, (C6H9N2)4[V2W4O19]·2H2O (1), is isolated by a simple stepwise synthesis method and characterized by a combined experimental and computational study. Molecular docking is conducted for the first time for this kind of substituted Lindqvist polyoxometalates to elucidate for potential antidiabetic activity. Hence, the modeling results revealed a significant docking score of the reported compound to bind to the active sites of α-glucosidase with the lowest binding energy of -5.7 kcal/mol, where the standard drug acarbose (ACB) had -4.6 kcal/mol binding energy. The stability of binding was enhanced by strong H-bonding, van der Waals, and electrostatic interactions occurring in the three-dimensional (3D) supramolecular network of polyanionic vanadotungstate subunits templated with organic moieties as shown by X-ray diffraction and Hirshfeld analyses. Furthermore, density functional theory (DFT) calculations supported with photophysical measurements are also discussed to predict the most chemical and biological reactivity. In this view, the complete description of electronic and biological features of (1) is enhanced by determination of the highest occupied molecular orbital (HOMO)/least unoccupied molecular orbital (LUMO) energy, electronic density, ionization potential, electron affinity, etc. These chemical descriptors, intermolecular interactions, docking score, and binding free energy estimation are essential in understanding the reactivity of this bioactive compound offering potential inhibition of the α-glucosidase enzyme.

Potential antioxidant, anticholinergic, antidiabetic and antiglaucoma activities and molecular docking of spiraeoside as a secondary metabolite of onion (Allium cepa)

Onion contains many dietary and bioactive components including phenolics and flavonoids. Spiraeoside (quercetin-4-O-β-D-glucoside) is one of the most putative flavonoids in onion. Several antioxidant techniques were used in this investigation to assess the antioxidant capabilities of spiraeoside, including 1,1-diphenyl-2-picrylhydrazyl radical (DPPH·) scavenging, N,N-dimethyl-p-phenylenediamine radical (DMPD•+) scavenging, 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS•+) scavenging activities, cupric ions (Cu2+) reducing and potassium ferric cyanide reduction abilities. In contrast, the water-soluble α-tocopherol analogue trolox and the conventional antioxidants butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), and α-tocopherol were utilized as the standards for evaluation. Spiraeoside scavenged the DPPH radicals an IC50 of 28.51 μg/mL (r2: 0.9705) meanwhile BHA, BHT, trolox, and α-tocopherol displayed IC50 of 10.10 μg/mL (r2: 0.9015), 25.95 μg/mL (r2: 0.9221), 7.059 μg/mL (r2: 0.9614) and 11.31 μg/mL (r2: 0.9642), accordingly. The results exhibited that spiraeoside had effects similar to BHT, but less potent than α-tocopherol, trolox and BHA. Also, inhibitory effects of spiraeoside were evaluated toward some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II) and α-glycosidase, which are related to a number of illnesses, such as Alzheimer’s disease (AD), diabetes mellitus and glaucoma disorder. Spiraeoside exhibited IC50 values of 4.44 nM (r2: 0.9610), 7.88 nM (r2: 0.9784), 19.42 nM (r2: 0.9673) and 29.17 mM (r2: 0.9209), respectively against these enzymes. Enzyme inhibition abilities were compared to clinical used inhibitors including acetazolamide (for CA II), tacrine (for AChE and BChE) and acarbose (for α-glycosidase). Spiraeoside demonstrated effective antioxidant, anticholinergic, antidiabetic and antiglaucoma activities. With these properties, it has shown that Spiraeoside has the potential to be a medicine for some metabolic diseases.

Synthesis and potential antidiabetic and lipid-lowering activities of putative asperidine B and its desmethyl analogue

Putative asperidine B is an unnatural 2,6-disubstituted piperidin-3-ol and a structural isomer of (+)-preussin, a well-known pyrrolidin-3-ol alkaloid. This work reports the first enantioselective synthesis of putative asperidine B and its desmethyl analogue via a chiron approach starting from d-isoascorbic acid as well as evaluation of their free-radical scavenging, antidiabetic, and anti-hyperlipidemic activities. Both putative asperidine B and its desmethyl analogue markedly reduced the total reactive oxygen species (ROS) without cytotoxicity in hepatocellular carcinoma (HepG2) cells. The desmethyl analogue was a potent inducer for two antioxidant gene expression, glutathione peroxidase and superoxide dismutase, whereas putative asperidine B only induced superoxide dismutase. In addition, putative asperidine B exerted potent antidiabetic activity via α-glucosidase inhibition (IC50 = 0.143 ± 0.001 mg/mL) comparable to that of acarbose, an antidiabetic drug. Consistent with the parent asperidine B (preussin), both putative asperidine B and its desmethyl analogue inhibited cholesterol absorption in the intestinal Caco-2 cells. These novel and promising antioxidant, antidiabetic, and lipid-lowering effects of piperidin-3-ols could offer a starting point for this class of compounds for obesity and diabetic drug discovery.