Anti-glucosidase Activities Research Articles

Multidirectional research for the therapeutic potential of Phlomoides molucelloides (Bunge) Salmaki: LC-MS/MS, antioxidant, enzyme inhibition, and antiproliferative characteristics

Medicinal plants offer natural cures and inspire modern medicine's development. This study examined the antioxidant, enzyme-inhibitory, and antiproliferative activities of various extracts obtained from aerial and root fragments of Phlomoides molucelloides (Bunge) Salmaki. The extracts' overall phenolics, flavonoids, and compounds were defined using colorimetric and LC-MS/MS analyses. The highest total phenolic and flavonoid content was measured in the methanol and infusion extracts of the aerial fragments, with 102.21 mg RE/g and 51.33 mg GAE/g, respectively. Most compounds were defined as flavonoids, predominantly as apigenin and quercetin glycosides. Methanol, 70 % methanol, and infusion extracts from aerial parts had the highest antioxidant activity determined by DPPH, ABTS, CUPRAC, FRAP, metal chelation, and phosphomolybdenum analyses. Moreover, the methanol extract of the roots had the highest anti-acetylcholinesterase, anti-butyrylcholinesterase, and anti-glucosidase activities. The dichloromethane extracts of the roots displayed the highest anti-tyrosinase and anti-amylase activities. The antiproliferative activity of the extracts was investigated against MDA-MB-231, MCF-7, and HeLa cell lines. The lowest IC50 value (875.7 µg/mL) was computed for the methanol extract of the aerial part on the MCF-7 cell line at the 48th h. The findings showed that P. molucelloides extracts may offer a promising therapeutic approach due to their rich bioactive content.

Glucosidase inhibition and compound identification of stingless bee honey and preserved fruits of Citrus japonica

Food preservation has many benefits, such as increasing shelf life, retaining nutritional values and biological activities. In the current study, total phenolic content (TCP), antioxidant and anti-glucosidase activities, and kinetic of glucose inhibition of stingless bee honey, honey mixed with fruits, and extracts of Citrus japonica were evaluated by measuring color of a reaction using a spectrophotometer. The result showed that high TPC was found in ethanol extract of C. japonica leaves and fruits (26.79 ± 6.94 and 12.79 ± 0.87 mg of gallic acid per g extract), while stingless bee honey revealed the highest antioxidant activity (1/EC50 = 0.2921) and honey mixed with fruits revealed the strongest anti-glucosidase activity (1/EC50 = 1.8181), significantly (P-value <0.05). Kinetic of glucosidase inhibition of honey were found as uncompetitive and mixed competitive inhibition, while the honey mixed with fruits showed mixed competitive inhibition. The FTIR and GC-MS analysis demonstrated the presence of several bioactive compounds. Very strong positive relationship between total phenolic content with GC-MS data was found (r = 0.926, P-value < 0.05). This knowledge confirmed that stingless bee honey and honey mixed with fruits had greater anti-diabatic potential in comparison with the extracts of C. japonica leaves and fruits.

Assessing the Chemical Profile and Biological Potentials of Tamarix aphylla (L.) H.Karst. and Tamarix senegalensis DC. by In Vitro, In Silico, and Network Methodologies.

The present study aimed to investigate the chemical profile, antioxidant, and enzyme inhibition properties of extracts from fruits and aerial parts (leaves and twigs) of Tamarix aphylla and T. senegalensis. Hexane, dichloromethane, ethyl acetate (EtOAc), and methanol extracts were prepared sequentially by maceration. Results revealed that EtOAc extracts of T. senegalensis and T. aphylla fruits contained the highest total phenolic content (113.74 and 111.21mg GAE/g) while that of T. senegalensis (38.47mg RE/g) recorded the highest total flavonoids content. Among the quantified compounds; ellagic, gallic, 3-hydroxybenzoic, caffeic, syringic, p-coumaric acids, isorhamnetin, procyanidin B2, and kaempferol were the most abundant compounds in the two species. EtOAc extracts of the two organs of T. senegalensis in addition to MeOH extract of T. aphylla aerial parts displayed the highest chelating power (21.00-21.30mg EDTAE/g, p > 0.05). The highest anti-AChE (3.11mg GALAE/g) and anti-BChE (3.62mg GALAE/g) activities were recorded from the hexane and EtOAc extracts of T. senegalensis aerial parts and fruits, respectively. EtOAc extracts of the fruits of the two species exerted the highest anti-tyrosinase (anti-Tyr) activity (99.44 and 98.65mg KAE/g, p > 0.05). Also, the EtOAc extracts of the both organs of the two species exhibited highest anti-glucosidase activity (0.88-0.90 mmol ACAE/g, p > 0.05) while the best anti-α-amylase activity was recorded from the dichloromethane extract of T. senegalensis fruits (0.74 mmol ACAE/g). In this study, network pharmacology was employed to examine the connection between compounds from Tamarix and their potential effectiveness against Alzheimer's disease. The compounds demonstrated potential interactions with pivotal genes including APP, GSK3B, and CDK5, indicating a therapeutic potential. Molecular docking was carried out to understand the binding mode and interaction of the compounds with the target enzymes. Key interactions observed, such as H-bonds, promoted the binding, and weaker ones, such as van der Waals attractions, reinforced it. These findings suggest that these two Tamarix species possess bioactive properties with health-promoting effects.

Proximate composition, physico-chemical properties, techno-functional properties, nutritional quality, and functional activity of Ferula assafoetida oleo-gum-resin

Mass and tear assafoetida are mainly composed of carbohydrates (61.14 and 61.50 g/100 g) followed by protein (13.45 and 14.28 g/100 g), fat (11.85 and 11.50 g/100 g), and essential oil (9.25 and 8.40 g/100 g). Also measured were electrical conductivity (1250 and 1237 microsiemens/cm), osmolarity (192 and 198 milliosmol/kg), surface tension (38 and 41 mN/m), zeta potential (–23.7 and –23.5 mV), particle size (265 and 275 nm), particle size distribution (0.73 and 0.93), and viscosity (1.40 and 1.35 mPa.s), along with water content (12.80 and 11.25%), water solubility (65.68 and 72.50%), water swelling (145.8 and 137.0%), hygroscopicity (39.84 and 41.20%), hydrophobicity (7.30 and 6.85 µg/g), emulsification activity (72.66 and 70.0%), emulsification stability (66.97 and 64.0%), foam activity (55.09 and 58.50%), foam stability (48.95 and 52.0%), water-holding capacity (3.86 and4.20 g/g) and oil-holding capacity (3.35 and 3.15 g/g). The major amino acids in assafoetida proteins were isoleucine, methionine, glycine, aspartic acid, alanine, glutamic acid, and lysine. The main fatty acids of assafoetida are myristic, palmitic, alpha-linolenic, oleic, linoleic, and lauric acids. The main volatile oil components of assafoetida are 1-propenyl butyl disulfide, α-pinene, bis (1-methyl thio)propyl disulfide, and 1-(propylthio)propyl propyl disulfide. Assafoetida showed good antioxidant capacity, anti-amylase, and anti-glucosidase activity similar to positive controls.

In vitro research to evaluate the antioxidant effects, inhibiting enzymes, methicillin-resistant Staphylococcus aureus strains of Terminalia catappa extracts

AimContribute to the well-being of the Ivorian population through scientific proof of the use of Terminalia cattapa leaves extracts in traditional medicine. MethodologyThe antioxidative effect of aqueous, water-alcoholic, ethyl acetate and hexane derivatives of Terminalia catappa leaves was measured by six tests: DPPH (2-diphenyl-1-picrylhydrazyl), ABTS (2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid)), FRAP (ferric ion reducing antioxidant power), PPBD (phosphomolybdenum), CUPRAC (cupric ion reducing antioxidant capacity) and MCA (metal chelating activity). The inhibition of the activity of five enzymes (acetylcholinesterase, butyrylcholinesterase, tyrosinase, amylase and glucosidase) was also determined. In addition, the broadcast method was used to evaluate impact of the samples on methicillin-resistant Staphylococcus aureus (MRSA) strains. ResultsHighest antioxidant capacity was obtained in the ethanolic sample for DPPH, ABTS, FRAP and PPBD tests. Ethyl acetate sample produced the best CUPRAC and MCA tests. Among inhibitory effect of samples on the five enzymes, aqueous sample showed the strongest anti-acetylCholynesterase and anti-butyrylCholynesterase activity. Best anti-tyrosinase and anti-amylase activity were obtained with the ethanolic sample. Hexane sample obtained the best anti-glucosidase activity while ethanolic and aqueous samples obtained none. All extracts showed no activity on the MRSA strains tested. ConclusionThe chemical compounds present in Terminalia cattapa leaves extracts would not be responsible for the use made in traditional medicine against infections.

A Comparative Study of Chemical Profiling and Bioactivities between Thai and Foreign Hemp Seed Species (Cannabis sativa L.) Plus an In-Silico Investigation.

Hemp (Cannabis sativa L.) is a plant widely used by humans for textiles, food, and medicine. Thus, this study aimed to characterize the chemical profiling of 12 hemp seed extracts from Thai (HS-TH) and foreign (HS-FS) samples using gas chromatography-mass spectrometry (GC-MS). Their antibacterial activity and α-glucosidase inhibitory activity were assayed. Linoleic acid (17.63-86.53%) was a major component presented in Thai hemp seed extracts, while α,β-gluco-octonic acid lactone (30.39%), clionasterol (13.42-29.07%), and glyceryl-linoleate (15.12%) were detected as the main metabolites found in foreign hemp seed extracts. Furthermore, eight extracts from both Thai and foreign hemp seed exhibited antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis, Methicillin-resistant Staphylococcus aureus, and Cutibacterium acnes, with MIC values ranging from 128 to 2048 µg/mL. Interestingly, the ethanol extract of Thai hemp seed (HS-TH-2-M-E) showed superior α-glucosidase inhibition (IC50 value of 33.27 ug/mL) over foreign species. The combination between Thai hemp species (HS-TH-2-M-E) and acarbose showed a synergistic effect against α-glucosidase. Furthermore, the docking investigation revealed that fatty acids had a greater impact on α-glucosidase than fatty acid esters and cannabinoids. The computational simulation predicts a potential allosteric binding pocket of guanosine on glucosidase and is the first description of gluco-octonic acid's anti-glucosidase activity in silico. The findings concluded that Thai hemp seed could be used as a resource for supplemental drugs or dietary therapy for diabetes mellitus.

Enzyme-Assisted Extraction of Fucosylated Chondroitin Sulfate from Sea Cucumber Holothuria scabra and Bohadschia argus and their Potential in Pharmaceutical Applications

Due to the health benefit of fucosylated chondroitin sulfate (FuCS), the efficient method for extraction of FuCS from raw materials is a crucial issue in reducing the production cost. In this study, enzymatic extraction of FuCS from two species of sea cucumber, Holothuria scabra and Bohadschia argus was undertaken using two protease enzymes, alcalase and papain. Response surface methodology (RSM) was employed in determining the optimal extraction conditions with the highest yield of FuCS concentration. The predicted optimal papain-assisted extraction conditions of Holothuria scabra and Bohadschia argus obtained a predicted FuCS yield of 1609.73 mg/100 g and 444.51 mg/100 g, respectively. To compare extraction efficiencies of two protease enzymes, employment of the RSM optimal conditions to Holothuria scabra resulted in 1538.76 ± 20.26 mg/ 100 g and 1295.50 ± 14.28 mg/100 g of purified FuCS for papain and alcalase, respectively. Whereas Bohadschia argus produced 412.39 ± 10.12 mg/100 g and 461.11 ± 8.45 mg/100 g purified FuCS for papain and alcalase, respectively. The acquired FTIR and NMR spectrums of extracted FuCS showed typical bands of sulfation patterns and were compared to commercial FuCS. The extracted FuCS showed enzyme type dependent antioxidant activity, and significant tyrosinase inhibitory activity than commercial FuCS. It also exhibited similar anti-glucosidase activity as commercial FuCS. Thus, this study reveals potential applications of enzyme-assisted FuCS from sea cucumber in food and pharmaceutical industries.

How Closely Does Induced Agarwood’s Biological Activity Resemble That of Wild Agarwood?

Continuous innovation in artificially-induced agarwood technology is increasing the amount of agarwood and substantially alleviating shortages. Agarwood is widely utilized in perfumes and fragrances; however, it is unclear whether the overall pharmacological activity of induced agarwood can replace wild agarwood for medicinal use. In this study, the volatile components, total chromone content, and the differences in the overall activities of wild agarwood and induced agarwood, including the antioxidant, anti-acetylcholinesterase, and anti-glucosidase activity were all determined. The results indicated that both induced and wild agarwood's chemical makeup contains sesquiterpenes and 2-(2-phenylethyl)chromones. The total chromone content in generated agarwood can reach 82.96% of that in wild agarwood. Induced agarwood scavenged 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) radicals and inhibited acetylcholinesterase activity and α-glucosidase activity with IC50 values of 0.1873 mg/mL, 0.0602 mg/mL, 0.0493 mg/mL, and 0.2119 mg/mL, respectively, reaching 80.89%, 93.52%, 93.52%, and 69.47% of that of wild agarwood, respectively. Accordingly, the results distinguished that induced agarwood has the potential to replace wild agarwood in future for use in medicine because it has a similar chemical makeup to wild agarwood and has comparable antioxidant, anti-acetylcholinesterase, and anti-glucosidase capabilities.

Comparison of FTIR fingerprint, phenolic content, antioxidant and anti-glucosidase activities among Phaseolus vulgaris L., Arachis hypogaea L. and Plukenetia volubilis L.

BackgroundInhibition of starch-hydrolysing enzymes is one of the major methods to reduce the risk of type−2 diabetes mellitus. Nowadays, there are no reports involving oil-rich and oil-low seeds of different botanical origins. The current study intended to extract Phaseolus vulgaris L. and Arachis hypogaea L. including Plukenetia volubilis L. using ethanol and water solvents, and to analyse Fourier-transform infrared (FTIR) fingerprint, total phenolic content, antioxidant and anti-glucosidase activities of the extracts by principal component analysis (PCA) and cluster analysis. ResultsThe result showed that the ethanol extracts of P. vulgaris L., A. hypogaea L., and P. volubilis L. showed total phenolic content higher than those of the aqueous extracts. The result also demonstrated that the aqueous and ethanol extracts from P. volubilis L. seed showed the highest antioxidant and anti-glucosidase activities, respectively. In comparison with the efficacy of the aqueous extracts of beans, A. hypogaea L. showed the highest antioxidant activity and anti-glucosidase activity. For the ethanol extract of beans, P. vulgaris L. (red kidney bean) showed the highest antioxidant activity, while P. vulgaris L. (white kidney beans) showed the highest anti-glucosidase activity. Moreover, significantly positive correlations between total phenolic content and anti-glucosidase activity (r = 0.41, P-value = 0.018), and between total phenolic content and FTIR data (r = 0.66, P-value = 0.000) were found. ConclusionsFTIR of the extracts showed functional groups corresponding with phenolic compounds. Moreover, the PCA and cluster analysis from FTIR data, phenolic content and biological activity could separate solvent types used for extraction.How to cite: Thummajitsakul S, Piyaphan P, Khamthong S, et al. Comparison of FTIR fingerprint, phenolic content, antioxidant and anti-glucosidase activities among Phaseolus vulgaris L., Arachis hypogaea L. and Plukenetia volubilis L. Electron J Biotechnol 2023;61. https://doi.org/10.1016/j.ejbt.2022.10.003.

Analysis of flower extract and natural dye solution from Sesbania javanica using Fourier-transform infrared spectroscopy (FTIR) chemometrics, and determination of its antioxidant and anti-glucosidase activities

Fourier-transform infrared spectroscopy (FTIR) chemometrics and determination of antioxidant and anti-glucosidase activities of flower extract and natural dye solution from Sesbania javanica were performed. Total phenolic content and total flavonoid content were the highest in ethanolic flower extract, while antioxidant activity (1/EC50 = 0.4935) and α-glucosidase inhibition (1/EC50 = 2.9671) were the highest in dye solution, obtained from mixing white clay filler with aqueous dye extract. The correlations of FTIR data, bioactive compound contents, and biological activities were assessed by partial least squares structural equation modelling. Results showed that a strongly positive relationship was significantly demonstrated between FTIR fingerprints and bioactive compound contents (β = 0.825, t = 17.037, p value &lt; 0.05), and between bioactive compound contents and biological activities (β = 0.563, t = 3.000, p value &lt; 0.05). However, a strongly negative relationship was significantly found between FTIR fingerprints and biological activities (β = -1.204, t = 6.065, p value &lt; 0.05). Moreover, the PCA and cluster analysis from FTIR data led to well grouping in PC plots and phylogenetic trees. Interestingly, the PCA and cluster analysis from FTIR data of plant extracts in powdered form provided better separation in PC plots and phylogenetic trees than in liquid form.

Hexane extract of Curcuma longa L. inhibits the activities of key enzymes and pro- inflammatory adipokines linked to obesity

IntroductionObesity is associated with chronic activation of low-grade inflammation produced mainly from adipose tissue, which is implicated in the pathogenesis of several diseases. Consequently, there is a need to screen for new anti-obesity medicines. Clinical evidence regarding the anti-obesity properties of Curcuma longa L. (C. longa) is inconclusive. Therefore, we aimed to investigate for the first time the influence of curcuminoids and hexane extract derived from C. longa 1) On the release of pro-inflammatory adipokines from human abdominal subcutaneous adipose tissue (ASAT) and induced-mononuclear cells (iMC) and 2) On the activities of α-amylase, α-glucosidase, and lipase enzymes. MethodsASAT explants and lipopolysaccharide-iMC were treated with either curcuminoids or hexane extract of C. longa. Protein concentration, anti-lipase, anti-amylase and anti-glucosidase activities were evaluated employing colorimetric methods. ResultsTreatment of ASAT with curcuminoids or hexane extract inhibited the secretion of leptin, CCL5 and Il-1β. Treatment of iMC cells with curcuminoids or hexane extract inhibited the secretion of TNF-α, CCL5 and Il-1β and leptin was not detected. Curcuminoids possessed a significant inhibitory activity against lipase, α-amylase and α-glucosidase in a dose-dependent manner. ConclusionWe demonstrate for the first time that curcuminoids and C. longa exert anti-inflammatory properties on human ASAT and iMC and inhibit the activities of lipase, α-amylase and α-glucosidase enzymes. This suggests that C. longa and curcuminoids not only may ameliorate obesity-associated comorbidities such as metabolic syndrome but may be used as a preventive approach against obesity. However, this requires in vivo validation.

Comprehensive Biological and Chemical Evaluation of Two Seseli Species (S. gummiferum and S. transcaucasicum).

Seseli L. is one of the largest genera of the Apiaceae family widely known for their traditional uses as herbal remedies. In the present study, the methanolic and water extracts of two Seseli species, S. gummiferum and S. transcaucasicum were evaluated for their bioactive contents and biological activities. The total phenolic and flavonoid contents in the extracts ranged from 19.09 to 24.33 mg GAE/g and from 0.45 to10.09 mg RE/g, respectively. Moreover, while narcissin was detected as the most abundant component in the methanolic extract of S. transcaucasicum (261.40 µg/g), chlorogenic acid was identified as the major component in all the other extracts, although a high amount was also present in the methanolic S. transcaucasicum extract (107.48–243.12 µg/g). The total antioxidant capacity was also determined by the phosphomolybdenum assay (0.66–1.18 mM TE/g). Other antioxidant assays such as the radical scavenging assays (DPPH: 5.51–11.45 mg TE/g; ABTS: 43.46–51.91 mg TE/g), reducing assays (CUPRAC: 41.67–53.20 mg TE/g; FRAP: 31.26–34.14 mg TE/g), as well as the metal chelating activity assay (14.38–38.57 mg EDTAE/g) were conducted. All the extracts showed inhibitory potential against the enzyme’s amylase (0.12–0.78 mM ACAE/g), acetyl- and butyryl-cholinesterase (0.15–9.71 mg GALAE/g), while only the methanolic extracts acted as inhibitors of tyrosinase (107.15 and 109.37 mg KAE/g) and only the water extract of S. gummiferum displayed anti-glucosidase activity (0.13 mM ACAE/g). Interestingly, the methanolic extracts of both Seseli species showed lower cytotoxicity towards HaCaT cells (IC50: >500 µg/mL), compared to the water extracts (IC50: 267.8 and 321.41 µg/mL). Besides, only the methanolic extracts showed a slight wound healing effect (28.21 and 31.23%). All extracts showed antibacterial action against Staphylococcus lugdunensis (minimum inhibitory and bactericidal concentrations: 0.025–2 mg/mL). S. gummiferum methanolic extract, which exhibited the highest antibacterial potency was found to inhibit adhesion and invasion of S. lugdunensis to HaCaT cells as well. Taken together, this study demonstrated the two Seseli species to harbour interesting bioactive components, in particular polyphenolics and to exhibit several biological properties that could be further investigated for their potential exploitation as healing agents as supported by various traditional medicinal uses.

Isolation and Biological Characterization of Homoisoflavanoids and the Alkylamide N-p-Coumaroyltyramine from Crinum biflorum Rottb., an Amaryllidaceae Species Collected in Senegal.

Crinum biflorum Rottb. (syn. Crinum distichum) is an Amaryllidaceae plant used in African traditional medicine but very few studies have been performed on this species from a chemical and applicative point of view. Bulbs of C. biflorum, collected in Senegal, were extracted with ethanol by Soxhlet and the corresponding organic extract was purified using chromatographic methods. The pure compounds were chemically characterized by spectroscopic techniques (1D and 2D 1H and 13C NMR, HR MS and ECD) and X-ray analysis. Four homoisoflavonoids (1–4) and one alkylamide (5) were isolated and characterized as 5,6,7-trimethoxy-3-(4-hydroxybenzyl)chroman-4-one (1), as 3-hydroxy-5,6,7-trimethoxy-3-(4-hydroxybenzyl)chroman-4-one (2), as 3-hydroxy-5,6,7-trimethoxy-3-(4-methoxybenzyl)chroman-4-one (3) and as 5,6,7-trimethoxy-3-(4-methoxybenzyl)chroman-4-one (4), and the alkylamide as (E)-N-(4-hydroxyphenethyl)-3-(4-hydroxyphenyl)acrylamide (5), commonly named N-p-coumaroyltyramine. The relative configuration of compound 1 was verified thanks to the X-ray analysis which also allowed us to confirm its racemic nature. The absolute configurations of compounds 2 and 3 were assigned by comparing their ECD spectra with those previously reported for urgineanins A and B. Flavanoids 1, 3 and 4 showed promising anticancer properties being cytotoxic at low micromolar concentrations towards HeLa and A431 human cancer cell lines. The N-p-coumaroyltyramine (5) was selectively toxic to A431 and HeLa cancer cells while it protected immortalized HaCaT cells against oxidative stress induced by hydrogen peroxide. Compounds 1–4 also inhibited acetylcholinesterase activity with compound 3 being the most potent. The anti-amylase and the strong anti-glucosidase activity of compound 5 were confirmed. Our results show that C. biflorum produces compounds of therapeutic interest with anti-diabetic, anti-tumoral and anti-acetylcholinesterase properties.

Chemical Constituents of the Essential Oil from Ecuadorian Endemic Species Croton ferrugineus and Its Antimicrobial, Antioxidant and α-Glucosidase Inhibitory Activity.

Croton ferrugineus Kunth is an endemic species of Ecuador used in traditional medicine both for wound healing and as an antiseptic. In this study, fresh Croton ferrugineus leaves were collected and subjected to hydrodistillation for extraction of the essential oil. The chemical composition of the essential oil was determined by gas chromatography equipped with a flame ionization detector and gas chromatography coupled to a mass spectrometer using a non-polar and a polar chromatographic column. The antibacterial activity was assayed against three Gram-positive bacteria, one Gram-negative bacterium and one dermatophyte fungus. The radical scavenging properties of the essential oil was evaluated by means of DPPH and ABTS assays. The chemical analysis allowed us to identify thirty-five compounds representing more than 99.95% of the total composition. Aliphatic sesquiterpene hydrocarbon trans-caryophyllene was the main constituent with 20.47 ± 1.25%. Other main compounds were myrcene (11.47 ± 1.56%), β-phellandrene (10.55 ± 0.02%), germacrene D (7.60 ± 0.60%), and α-humulene (5.49 ± 0.38%). The essential oil from Croton ferrugineus presented moderate activity against Candida albicans (ATCC 10231) with an MIC of 1000 μg/mL, a scavenging capacity SC50 of 901 ± 20 µg/mL with the ABTS method, and very strong antiglucosidase activity with an IC50 of 146 ± 20 µg/mL.

Antiamylase, Antiglucosidase, and Antiglycation Properties of Millets and Sorghum from Sri Lanka.

The present study evaluated a range of biological activities of selected millet types and sorghum varieties in Sri Lanka in relation to diabetes and its complications management. Five millet types, namely, proso millet, white finger millet, kodo millet, foxtail millet, and finger millet (Oshadha and Rawana), and two sorghum varieties, namely, sweet sorghum and sorghum ICSV 112, were used in this study. Methanolic extracts of whole grains were studied for antiamylase, antiglucosidase, and early- and middle-stage antiglycation and glycation reversing activities in vitro. Tested millets and sorghum showed significant (p < 0.05) and dose-dependent antiamylase (IC50: 33.34 ± 1.11–1446.70 ± 54.10 μg/ml), early-stage antiglycation (IC50: 15.42 ± 0.50–270.03 ± 16.29 μg/ml), middle-stage antiglycation (135.08 ± 12.95–614.54 ± 6.99 μg/ml), early-stage glycation reversing (EC50: 91.82 ± 6.56–783.20 ± 61.70 μg/ml), and middle-stage glycation reversing (393.24 ± 8.68–1374.60 ± 129.30 μg/ml) activities. However, none of the studied millet and sorghum showed antiglucosidase activity. Out of the samples studied, pigmented samples, namely, sweet sorghum, Oshadha, and Rawana, exhibited significantly high (p < 0.05) antiamylase and early- and middle-stage antiglycation and glycation reversing activities compared to other millet and sorghum samples. Interestingly, sweet sorghum exhibited nearly four times potent antiamylase activity compared to the standard drug acarbose (IC50 111.98 ± 2.68 μg/ml) and sweet sorghum, kodo millet, Oshadha, and Rawana showed comparable early-stage antiglycation activities in comparison to the reference standard Rutin (IC50 21.88 ± 0.16 μg/ml). Therefore, consumption of whole grains of pigmented millet and sorghum in Sri Lanka may play an important role in the prevention and management of diabetes and its complications. Interestingly, this is the 1st study to report all the tested biological activities for millet and sorghum in Sri Lanka and the 1st study to report both early- and middle-stage glycation reversing activities of millet and sorghum worldwide.

Hepatoprotective, nephroprotective, anti-amylase, and antiglucosidase effects of Ziziphus spina-christi (L.) against carbon tetrachloride-induced toxicity in rats

Purpose: To explore the hepatoprotective, nephroprotective, anti-amylase, and anti-glucosidase effects of the medicinal plant Ziziphus spina-christi (L.).&#x0D; Methods: Ziziphus spina-christi (L.) methanol extract (ZS-1) and its ethyl-acetate (ZS-2), n-butanol (ZS3), and aqueous (ZS-4) fractions were evaluated for their hepatoprotective, anti-amylase, and antiglucosidase activities. Adult male Wister rats were divided into 11 groups (I- XI) with 6 mice per group. Group I was normal control, while the treatment groups were as follows: group II, CCl4; group III, Silymarin + CCl4; group IV, Ziziphus spina-christi total methanol extract (ZS-1), 100 mg/kg) + CCl4; group V, ZS-1 (200 mg/kg) + CCl4; group VI, ethyl acetate fraction (ZS-2), 100 mg/kg + CCl4; group VII: ZS-2 (200 mg/kg) + CCl4; group VIII, butanol fraction (ZS-3), 100 mg/kg) + CCl4; group IX, ZS-3 (200 mg/kg) + CCl4; group X, aqueous fraction (ZS-4), 100 mg/kg) + CCl4; group XI: ZS-4 (200 mg/kg) + CCl4. Silymarin was used as the standard. Biomarkers of liver and kidney toxicity and histopathological changes were evaluated.&#x0D; Results: Liver and kidney malondialdehyde (MDA), non-protein sulfhydryls (NP-SH) and total protein levels were elevated in CCl4-treated rats; however, ZS-1 and ZS-4 of Z. spina-christi significantly reduced these levels. ZS-2 and ZS-3 did not significantly improve the studied parameters. These results were confirmed by results from histopathological examination. ZS-1 and ZS-2 showed mild inhibitory activities against α-amylase and α-glucosidase (54 and 43 % at 100 µg/ml, respectively).&#x0D; Conclusion: The results indicate that ZS-1 and ZS-4 samples displayed dose-dependent hepatoprotective and nephroprotective effects, whereas ZS-2 and ZS-3 samples did not exhibit these effects. Similarly, α-amylase and α-glucosidase enzymes are considerably inhibited by ZS-1 and ZS-2.

ECDYSTEROIDS AND GLYCOSYLFLAVONES OF SILENE SIBIRICA (CARYOPHYLLACEAE)

The present work realized the chemical study of Silene sibirica (L.) Pers. (Caryophyllaceae) high-performance liquid chromatography with diode array and mass spectrometric detection (electrospray ionization) (HPLC-DAD-ESI-MS). As a result, 25 compounds were found, including nine ecdysteroids and sixteen flavonoids. Ecdysteroids components were podecdysone C, integristerone A, turkesterone, polypodine B, 20-hydroxyecdysone and its 2-O-cinnamate, ecdysone, 2-deoxy-20-hydroxyecdysone, and 2-deoxyecdysone. Flavonoids were the glycosylflavones and derivatives of luteolin and apigenin. Luteolin glycosides included luteolin-7-O-rutinoside, lucenin-2, carlinoside, isoorientin and its 2″-O-arabinoside, as well as isoscoparin. The largest group of apigenin glycosides included O-glycosides as 7-O-glucoside and 7-O-rutinoside, C-glycosides as isovitexin, schaftoside, vicenin-2, and mixed C,O-glycosides as isovitexin-2′′-O-arabinoside and 2′′-O-rhamnoside. Three unidentified derivatives of apigenin were pre studied and their structural features discussed. Quantitative data about the content of selected compounds indicated that ecdysteroids accumulated in S. sibirica flowers (7.14–14.92 mg/g) and glycosylflavones were found predominantly in leaves (7.88–18.55 mg/g). The major ecdysteroid compound was 20-hydroxyecdysone, while flavonoids predominants were shaftoside and isovitexin-2″-O-ramnoside. A comparative analysis of the chemical composition of wild-growing and cultivated S. sibirica samples showed the stability of the metabolic profile of the plants during the introduction. The biological studies revealed the antiradical and antiglucosidase activity of the extracts. Thus, it was shown that the studied plant species (S. sibirica) is a source of ecdysteroids and glycosylflavones, and S. sibirica extracts have biological potency.

In Vitro Anti-diabetic Activity of Free Amino Acid and Protein Amino Acid Extracts from Four Iranian Medicinal Plants

Type 2 diabetes mellitus is a chronic metabolic disorder which is mainly correlated to hyperglycemia, hyperlipidemia, oxidative stress, and protein glycation. Bioactive compounds from herbal resources suggest a dietary approach for diabetes management by inhibiting carbohydrate-degrading enzymes and biomolecules oxidation. The anti-diabetic activities and amino acids composition of four medicinal plants, including Oliveria decumbens, Thymus kotschyanus, Trachyspermum ammi, and Zataria multiflora, were investigated. Free and protein amino acid extracts are mainly composed of amino acid and lower levels of monosaccharide, fatty acid, phenol compound, flavonoid, and tannins. The ratio of phenol/amino acid, flavonoid/amino acid, and tannins/amino acid in free amino acid extract was higher than protein amino acid extract. Liquid chromatography–mass spectrometry characterization showed that the main free amino acids among the plants analyzed in this study were asparagine (0.12–3.67 g/100 g), arginine (0.42–1.31 g/100 g), beta-aminoisobutyric acid (0.33–0.94 g/100 g), glutamine (0.20–0.54 g/100 g), aspartic acid (0.05–0.91 g/100 g), glutamic acid (0.07–0.49 g/100 g), proline (0.05–0.49 g/100 g), alanine (0.20–0.33 g/100 g), phenylalanine (0.04–0.32 g/100 g), valine (0.05–0.24 g/100 g), leucine (0.05–0.23 g/100 g), and serine (0.03–0.24 g/100 g). The main amino acids from plant-derived protein hydrolysate were aspartic acid (1.4–5.39 g/100 g), glycine (1.64–4.25 g/100 g), glutamic acid (1.37–3.93 g/100 g), leucine (1.35–2.92 g/100 g), alanine (1.45–2.79 g/100 g), lysine (1.38–2.67 g/100 g), arginine (1.33–2.97 g/100 g), serine (1.47–1.90 g/100 g), phenylalanine (0.79–1.96 g/100 g), valine (0.69–1.47 g/100 g), proline (0.84–1.25 g/100 g), and histidine (0.68–1.46 g/100 g). Free amino acid extract and protein amino acid extract exhibited moderate anti-glucose oxidation, anti-lipid oxidation, anti-protein oxidation, and anti-protein glycation, and anti-amylase, and anti-glucosidase activities. Antioxidant and anti-diabetic properties of free amino acids were considerably higher than the protein-hydrolyzed amino acids that may be attributed to higher phenol/amino acid, flavonoid/amino acid, and tannins/amino acid ratios.

New Flavonol Glycosides from Rhodiola quadrifida

Chromatographic separation of constituents in the EtOH extract of the herb of Rhodiola quadrifida (Pall.) Fisch. & C. A. Mey. (Crassulaceae) isolated 14 compounds including four new flavonol glycosides 1–4. UV and NMR spectroscopy and mass spectrometry found that the compounds were gossypetin and herbacetin derivatives, i.e., gossypetin-8-O-(2″-O-β-D-glucopyranosyl)-β-D-glucuronopyranoside (rhodiquadrin A, 1), gossypetin-3-O-(3″-O-acetyl)-β-D-glucopyranoside-8-O-β-D-glucuronopyranoside (rhodiquadrin B, 2), herbacetin-8-O-(2″-O-β-D-glucopyranosyl)-β-D-glucuronopyranoside (rhodiquadrin C, 3), and gossypetin-8-O-α-L-arabinopyranoside (rhodiquadrin D, 4). A study of the biological activities of the isolated flavonoids showed that the gossypetin derivatives possessed high antiradical and anti-glucosidase activity.

In vitro antioxidant and antidiabetic activity of essential oils encapsulated in gelatin-pectin particles against sugar, lipid and protein oxidation and amylase and glucosidase activity.

The in vitro antioxidant and antidiabetic activities of Oliveria decumbens, Thymus kotschyanus, Trachyspermum ammi, and Zataria multiflora essential oils incorporated into gelatin‐pectin composite were investigated. The gas chromatography–mass spectrometry characterization revealed that thymol (1.2%–86.4%), carvacrol (3.2%–52.4%), gamma‐terpinene (0.0%–12.7%), para‐cymene (3.2%–5.2%), geraniol (0.0%–14.5%), and spathulenol (0.0%–13.6%) are the major constituents of the essential oils. Gelatin‐pectin composite incorporated with the essential oils exhibited acidic pH (2.40–3.04), low conductivity (265–278 µS/cm), low surface tension (19.0–23.5 mN/m), low Newtonian viscosity (23.7–28.5 mPa.s), negative zeta‐potential (14.2–16.9 mV), and nanoscale particle size (313–336 nm). These rheological properties result in the production of globular gelatin‐pectin nanoparticles with a size range of 500–700 nm. The FTIR spectra of gelatin‐pectin and gelatin‐pectin‐essential oils to some extent were similar, suggesting the noncovalent interactions between them. Gelatin‐pectin composite incorporated with the essential oils displayed antiglucose oxidation (130–150 µg/ml) antilipid peroxidation (120–130 µg/ml), antiprotein oxidation (150–168 µg/ml), and antiprotein glycation (145–170 µg/ml) as well as antiamylase (216–230 µg/ml), and antiglucosidase (212–238 µg/ml) activity. The essential oils strongly improved the antioxidant capacity of the gelatin‐pectin composite so strongly which can be recommended as a natural compound for oxidative stress management.