Beyond model interpretability using LDA and decision trees for α-amylase and α-glucosidase inhibitor classification studies.

Background: Dialium guineense belongs to the Leguminosae family, and grows in dense forests in Africa along the southern edge of the Sahel. The bark, leaves and fruits of the plant have medicinal properties and are used to treat diseases such as stomatitis, toothache, fever, diarrhoea, palpitations, and microbial infections. Aim: The present study investigated the α-amylase and α-glucosidase inhibitory activities of extracts of Dialium guineense stem bark. Methods:Aqueous and ethanol extracts of D. guineense stem bark were prepared using standard method. Alpha amylase and alpha glucosidase inhibitory activities of the extracts were determined in vitro. Acarbose was used as the reference drug. Results: The results showed that both extracts of Dialium guineense possess α-amylase and α-glucosidase inhibitory activities. The aqueous extract (IC50 = 76.55 ± 3.01 µg/mL) showed a better α-amylase inhibitory activity when compared with the ethanol extract (IC50 = 137.78 ± 5.18 µg/mL) (p < 0.05), but there was no significant difference in the corresponding α-glucosidase inhibitory activity between the two extracts (p > 0.05). The α-amylase and α-glucosidase inhibitory activities of the extracts were concentration-dependent, and comparable to those of acarbose. Conclusion: The results of this study indicate that Dialium guineense shows great potential in the treatment of Diabetes mellitus.

Background: The Lamiaceae family, one of the most important herbaceous and shrub plant families, includes a wide variety of plants with biological and medicinal uses. This study aimed to conduct a comparative analysis of phenolic compounds content and biological activity of extracts from eight species of Lamiaceae plants, cultivated in a temperate climate, and to study the effect of the foliar salicylic acid application on these parameters. Methods: Lamiaceae plants (Lavandula angustifolia, Salvia officinalis, Hyssopus officinalis, Agastache foeniculum, Thymus serpyllum, Mentha × piperita, Origanum vulgare, Monarda didyma) cultivated on field experimental sites. Plants were sprayed with salicylic acid at a concentration of 1 mM. The untreated with salicylic acid plants were used as control. Results: The highest contents of hydroxycinnamic acids and flavonoids in control plants were observed in the Agastache foeniculum (6.4 ± 0.6 mg g-1 and 6.5 ± 0.4 mg g-1 respectively). The highest content of phenolic compounds was found in Monarda didyma (13.8 ± 0.7 mg g-1). Among the control plants, Agastache foeniculum, Hyssopus officinalis, and Mentha × piperita were characterized by the highest antioxidant activity. All the studied extracts had the ability to inhibit α-amylase and α-glucosidase. Significant positive correlations were revealed between the antioxidant activity and the contents of hydroxycinnamic acids, total phenolic compounds, and flavonoids. A high degree of correlation was found between the α-amylase inhibitory activity and the content of hydroxycinnamic acids (r = 0.72, p ≤ 0.05), as well as between the α-glucosidase inhibitory activity and the content of flavonoids (r = 0.83, p ≤ 0.05) and hydroxycinnamic acids (r = 0.81, p ≤ 0.05). The foliar treatment with salicylic acid led to an increase in the contents of hydroxycinnamic acids (in 6 species), flavonoids (in 2 species), total phenolic compounds (in 7 species), antioxidant activity (in 5 species), as well as in α-amylase (in 4 species) and α-glucosidase (in 5 species) inhibitory activity compared to the control plants. Lavandula angustifolia was the most susceptible to foliar treatment with salicylic acid. In this plant species, a significant increase in all studied biochemical parameters was noted. Conclusions: The results obtained on the stimulating effects of salicylic acid can be used to increase the nutritional and pharmacological value of plants of the Lamiaceae family cultivated in temperate climates.

New mixed Alcalase-hydrolysates were developed using corn gluten meal (CP) and soy protein (SP) hydrolysates, namely CPH, SPH, SPH30:CPH70, SPH70:CPH30, and SPH50:CPH50. Amino acid profile, surface hydrophobicity (H 0), molecular weight (MW) distribution, antioxidant activity, angiotensin-converting enzyme (ACE), α-amylase, and α-glucosidase inhibitory activities, and functional characteristics of hydrolysates were determined. Hydrolysis changed the amount of hydrophilic and hydrophobic amino acid composition and significantly increased the H 0 values of hydrolysates, especially for CPH. The DPPH radical scavenging activity (RSA) was higher for CPH, SPH30:CPH70, and SPH50:CPH50 than SPH and SPH70:CPH30. Moreover, SPH, SPH70:CPH30, and SPH50:CPH50 showed lower MW than CPH, and this correlated with the higher hydrophilicity, and ABTS and hydroxyl RSA values obtained for SPH and the mixed hydrolysates with predominantly SPH. SPH70:CPH30 exhibited higher ACE, α-glucosidase, and α-amylase inhibitory activities among all samples due to its specific peptides with high capacity to interact with amino acid residues located at the enzyme active site and also low binding energy. At 15% degree of hydrolysis, both SPH and CPH showed enhanced solubility at pH4.0, 7.0 and 9.0, emulsifying activity, and foaming capacity. Taken together, SPH70:CPH30 displayed strong antioxidant, antihypertensive, and antidiabetic attributes, emulsifying activity and stability indexes, and foaming capacity and foaming stability, making it a promising multifunctional ingredient for the development of functional food products.

Antioxidant and anti-diabetic activities in commercial and homemade pomegranate molasses in Lebanon

Carlina curetum plant phytoconstituents, enzymes inhibitory and cytotoxic activity on cervical epithelial carcinoma and colon cancer cell lines

There is an increasing prevalence of diabetes mellitus throughout the world, and new compounds are necessary to combat this. The currently available antidiabetic therapies are long-term complicated and side effect-prone, and this has led to a demand for more affordable and more effective methods of tackling diabetes. Research is focused on finding alternative medicinal remedies with significant antidiabetic efficacy as well as low adverse effects. In this research work, we have focused our efforts to synthesize a series of 1,2,4-triazole-based bis-hydrazones and evaluated their antidiabetic properties. In addition, the precise structures of the synthesized derivatives were confirmed with the help of various spectroscopic techniques including 1H-NMR, 13C-NMR, and HREI-MS. To find the antidiabetic potentials of the synthesized compounds, in vitro α-glucosidase and α-amylase inhibitory activities were characterized using acarbose as the reference standard. From structure-activity (SAR) analysis, it was confirmed that any variation found in inhibitory activities of both α-amylase and α-glucosidase enzymes was due to the different substitution patterns of the substituent(s) at variable positions of both aryl rings A and B. The results of the antidiabetic assay were very encouraging and showed moderate to good inhibitory potentials with IC50 values ranging from 0.70 ± 0.05 to 35.70 ± 0.80 μM (α-amylase) and 1.10 ± 0.05 to 30.40 ± 0.70 μM (α-glucosidase). The obtained results were compared to those of the standard acarbose drug (IC50 = 10.30 ± 0.20 μM for α-amylase and IC50 = 9.80 ± 0.20 μM for α-glucosidase). Specifically, compounds 17, 15, and 16 were found to be significantly active with IC50 values of 0.70 ± 0.05, 1.80 ± 0.10, and 2.10 ± 0.10 μM against α-amylase and 1.10 ± 0.05, 1.50 ± 0.05, and 1.70 ± 0.10 μM against α-glucosidase, respectively. These findings reveal that triazole-containing bis-hydrazones act as α-amylase and α-glucosidase inhibitors, which help develop novel therapeutics for treating type-II diabetes mellitus and can act as lead molecules in drug discovery as potential antidiabetic agents.

The fruits of Viburnum fordiae can be consumed both as food and for medicinal purposes, with the effect of regulating postprandial blood glucose levels. In this study, the optimised extraction and enrichment process has been utilised to produce the total polyphenols of V. fordiae fruits (VFTP), which exhibited potential α-amylase and α-glucosidase inhibitory activities. Further fractionation on VFTP led to the acquirement of two previously undescribed phenolic glycosides, vibumorsides A and B (1 and 2), along with thirteen known analogues (3–15). The structures of the new compounds were identified through comprehensive spectroscopic and chemical methods. In addition, the α-amylase and α-glucosidase inhibitory activities of these compounds were assessed. Among them, compound 2 showed the strongest inhibitory activity against α-amylase and α-glucosidase with IC50 values of 16.53 and 10.76 μM, respectively, and its molecular docking with the corresponding enzyme was also further conducted.

ABSTRACTOrmenis africana is an endemic North African species used in folk medicine because of its hypoglycemic property. In this study, the α-amylase and α-glucosidase inhibition and antioxidant activities of the polyphenolic-rich extract from O. africana were determined. The chemical composition was made using liquid chromatography with photodiode array and electrospray ionization mass spectrometry method and the identification of phenolics was assessed by comparing their retention times and ultraviolet and mass spectra with those of the standards and/or reported in the literature. The total phenolic content was estimated by the Folin–Ciocalteu method. The antidiabetic potential was estimated by the determination of α-amylase and α-glucosidase inhibition in vitro. Four assays were used for the evaluation of antioxidant activity of the extracts. Seventeen phenolic compounds were detected. The major peaks are chlorogenic acid, 5-O-di-caffeoylquinic acid, and apigenin and luteolin derivatives. The polyphenolic-rich extract showed remarkable α-amylase and α-glucosidase inhibition activity in a concentration dependent manner. Furthermore, the extract also demonstrated high antioxidant activities. O. africana can serve as a potential natural source for the development of a novel α-amylase and α-glucosidase inhibitory agents against diabetic complications.

Targeting OPA1 protein for therapeutic intervention in autosomal dominant optic atrophy: In silico drug discovery.

Vernonia amygdalina L., commonly utilized in traditional Vietnamese folk medicine for the management of afflictions including liver diseases, hypertension, diabetes, and elevated cholesterol levels. Despite its extensive employment in local herbal remedies, there exists a scarcity of scientific investigations elucidating its pharmacological and therapeutic potential. This research investigated the antioxidant activity of leaf extracts using a range of solvents, including n-hexane, chloroform, ethyl acetate, n-butanol, ethanol, and water. The ethyl acetate extract was identified as the most potent antioxidant, exhibiting EC50 values of 8.42 and 71.88 µg/mL in ferric reduction and DPPH assays, respectively. The hepatoprotective activity, as measured using the cellular lipid peroxidation method of ethanol leaf extract (IC50 = 5.87 µg/mL) is 4.75 times stronger than the trolox. Additionally, the ethanol extract demonstrated significant inhibitory potential against α-amylase and α-glucosidase enzymes (IC50 of 480.00 and 72.53 µg/mL, respectively). The acute oral toxicity study conducted on a mouse model indicates a safety margin at the experimental dose Dmax = 18.44 g extract/kg. Additionally, this study encompassed a leaf microdissection of V. amygdalina, elucidating pivotal morphological features. So, it is safe for further studies and producing functional products for disease prevention.

Ideal extraction conditions were estimated based on the maximum phenolic content, antioxidant activity and inhibitory activity of angiotensin-converting enzyme (ACE), α-glucosidase and α-amylase enzymes from Mentha spicata L. The optimum extraction conditions for phenolic compounds with maximum ACE inhibitory activity occurred in a mixture of acetone and water (1:1) at 40C for 6 h. The optimal extraction conditions for phenolic compounds with maximum α-amylase and α-glucosidase inhibitory activity were obtained in a mixture of methanol, acetone and water extraction (1:1:1) and in a mixture of methanol and distilled water (1:1) at 50C for 8 h. The major free phenolic compound extracted with the various extraction solvents, times and temperatures was rutin. The predominant bound phenolic compounds were caffeic acid and chlorogenic acid, which did not exist as free phenolic compounds. Practical Applications This study suggested the optimum extraction conditions of phenolic compounds with maximum capacity of antioxidant, antihypertensive and antidiabetic properties recommended to be used in food industry as pharmaceutical and nutraceutical herbal extract.

Obesity, a global issue, is linked to cardiometabolic syndrome. Dietary modification is one of the recommended modes for managing cardiometabolic syndrome. Strawberries, a functional food, and kombucha, a fermented tea beverage, have gained attention for their health benefits. This study investigated the bioactive components of strawberry kombucha drink (SKD) and their effects on antioxidant activities and improving metabolic disorder markers. An in vitro experiment was performed to determine the effect of SKD on enzymatic parameters: lipase, α-glucosidase, and α-amylase activities. In addition, antioxidant activity using the DPPH method and quantification of the radical scavenging activity were also measured. Furthermore, untargeted metabolomic profiling of SKD and molecular docking simulation were conducted. The findings suggest that SKD, rich in secondary metabolites, can inhibit lipase, α-glucosidase, and α-amylase activities. It demonstrated in vitro anti-obesity, anti-diabetic, and antioxidant properties, potentially reducing metabolic and inflammatory issues. Thus, SKD could be a therapeutic beverage to alter metabolic issues associated with obesity. Nevertheless, further preclinical study is warranted to determine SKD’s potential in vivo.

Chemical profiling of secondary metabolites from Himatanthus drasticus (Mart.) Plumel latex with inhibitory action against the enzymes α-amylase and α-glucosidase: In vitro and in silico assays

The difference among structure, physicochemical and functional properties of dietary fiber extracted from triticale and hull-less barley

Diabetes, a chronic metabolic disorder, is characterized by persistent hyperglycemia. This study aimed to evaluate the hypoglycemic and antioxidant activities of lactic acid bacteria strains isolated from humans and food products and investigate the probiotic properties of the selected four strains. The hypoglycemic activity of the isolated strains was examined by evaluating the α-glucosidase and α-amylase inhibitory activities. The antioxidant activity was measured using the DPPH, ABTS, and FRAP assays. Four strains (Lactiplantibacillus plantarum MG4229, MG4296, MG5025, and Lacticaseibacillus paracasei MG5012) exhibited potent α-glucosidase inhibitory (>75%) and α-amylase inhibitory (>85%) activities, which were comparable to those of acarbose (>50%; 1000 μg/mL). Similarly, the radical scavenging and antioxidant activities of the four strains were comparable to those of ascorbic acid (50 μg/mL). Additionally, the probiotic properties of the four selected strains were examined based on acid and bile salt tolerance, auto-aggregation ability, and antibiotic resistance. The four strains were resistant to pH 2 (>50% of survivability) and 0.5% bile salt (>80% of survivability). Therefore, we suggest that the selected strains with hypoglycemic, antioxidant, probiotic properties can potentially prevent diabetes.