Glucosidase Enzyme Research Articles

In-vivo and In- vitro Antidiabetic potential of Musa balbisiana colla and its different parts

The present study was performed to determine the antidiabetic activity of Musa balbisiana colla seed, peel, pulp and flower extract. The methanolic extract of Musa balbisiana was evaluated for its inhibition activity on α- amylase and α- glucosidase enzymes. The methanolic seed extract exhibited highest inhibition against α- amylase and α- glucosidase with IC50 values of 121±0.40 and 101±0.53. The effect of Musa balbisiana pulp, seed and flower on fasting blood glucose level in streptozotocin (STZ) induced diabetic rat was studied. On prolong administration of seed extract, it was seen that effectively reduced the blood glucose level and has effective slight increase in body weight. Thus the result indicates that extract of Musa balbisiana colla seed and flower posses potent antidiabetic property.

Biochemical, Toxicological, and in Silico Aspects of Trillium govanianum Wall. ex D.Don (Trilliaceae): A Rich Source of Natural Bioactive Compounds.

Trillium govanianum is a high-value medicinal herb, having multifunctional traditional and culinary uses. The present investigation was carried out to evaluate the phytochemical, biological and toxicological parameters of the T. govanianum Wall. ex D. Don (Family: Trilliaceae) roots collected from Azad Kashmir, Pakistan. Phytochemical profiling was achieved by determining total bioactive contents (total phenolic and flavonoid contents) and UHPLC-MS analysis. For biological evaluation, antioxidant activities (DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelation assays) and enzyme inhibition activities (against AChE, BChE, glucosidase, amylase, and tyrosinase) were performed. Moreover, cytotoxicity was assessed against three human carcinoma cell lines (MDA-MB-231, CaSki, and DU-145). The tested extract was found to contain higher total phenolics (7.56 mg GAE/g dry extract) as compared to flavonoid contents (0.45 mg RE/g dry extract). Likewise, for the antioxidant activity, higher CUPRAC activity was noted with 39.84 mg TE/g dry extract values. In the case of enzyme assays, higher activity was pointed out against the cholinesterase, glucosidase and tyrosinase enzymes. The plant extract displayed significant cytotoxicity against the cell lines examined. Moreover, the in-silico studies highlighted the interaction between the important phytochemicals and tested enzymes. To conclude, the assessed biological activity and the existence of bioactive phytochemicals in the studied plant extract may pave the way for the development of novel pharmaceuticals.

Antioxidant and antidiabetic flavonoids from the leaves of Dypsis pembana (H.E.Moore) Beentje & J.Dransf., Arecaceae: in vitro and molecular docking studies

BackgroundOxidative stress and diabetes are medical conditions that have a growing prevalence worldwide, significantly impacting our bodies. Thus, it is essential to develop new natural antioxidant and antidiabetic agents. Dypsis pembana (H.E.Moore) Beentje & J.Dransf (DP) is an ornamental palm of the family Arecaceae. This study aimed to broaden the understanding of this plant’s biological properties by evaluating its in vitro antioxidant and antidiabetic activities.MethodsThe in vitro antioxidant activities of the crude extract, fractions, and selected isolates were evaluated by DPPH method. While the in vitro antidiabetic activities of these samples were evaluated by assessing the degree of inhibition of α-glucosidase. Additionally, molecular docking analysis was performed to investigate the interactions of tested compounds with two potential targets, the cytochrome c peroxidase and alpha glucosidase.ResultsThe crude extract displayed the highest antioxidant activity (IC50 of 11.56 µg/ml), whereas among the fractions, the EtOAc fraction was the most potent (IC50 of 14.20 µg/ml). Among tested compounds, isoquercetrin (10) demonstrated the highest potency, with an IC50 value of 3.30 µg/ml, followed by rutin (8) (IC50 of 3.61 µg/ml). Regarding antidiabetic activity, the EtOAc (IC50 of 60.4 µg/ml) and CH2Cl2 fractions (IC50 of 214.9 µg/ml) showed activity, while the other fractions did not demonstrate significant antidiabetic effects. Among tested compounds, kaempferol-3-O-neohesperidoside (9) showed the highest antidiabetic activity, with an IC50 value of 18.38 µg/ml, followed by kaempferol (4) (IC50 of 37.19 µg/ml). These experimental findings were further supported by molecular docking analysis, which revealed that isoquercetrin and kaempferol-3-O-neohesperidoside exhibited strong enzyme-binding affinities to the studied enzyme targets. This analysis provided insights into the structure-activity relationships among the investigated flavonol-O-glycosides.ConclusionThe biological and computational findings revealed that isoquercetrin and kaempferol-3-O-neohesperidoside have potential as lead compounds for inhibiting cytochrome c peroxidase and alpha glucosidase enzymes, respectively.

Phytochemical profiling and antidiabetic evaluation of Peperomia pellucida as a potential alpha glucosidase inhibitor

Abstract. Hidayati S, Agustin AT, Sari EK, Sari SM, Destiawan RA, Silvana WA. 2023. Phytochemical profiling and antidiabetic evaluation of Peperomia pellucida as a potential alpha glucosidase inhibitor. Biodiversitas 24: 5972-5978. One strategy in post-prandial hyperglycemic control can be done by inhibiting the digestion of dietary carbohydrates through the inhibition of alpha glucosidase enzymes. This study was conducted to determine the antidiabetic activity of Peperomia pellucida in inhibiting the alpha glucosidase. An inhibitory activity analysis test was carried out on alpha glucosidase in vitro and in silico using alpha glucosidase. Molecular docking between receptors and ligands was performed using Hex 8.0 software. The setting column is set in Shape+Electro+DARS mode. The results showed ethanol extract and ethyl acetate fraction in vitro showed the ability to inhibit the activity of alpha glucosidase enzyme with C50 values of 13.43 mg/mL and 9.73 mg/mL respectively with IC50 positive control acarbose values of 8.11 mg/mL. The results of in silico analysis showed that the Patuloside A component was able to bind to the binding site of alpha glucosidase and gave the smallest binding energy value with a value of -321.4 kcal/mol compared to isovitexin, isoswertisin, pellucidatin, and caryatin-7-O-?-rhamnoside compounds. P. pellucida has the potential to be developed as an antidiabetic agent that has activity in inhibiting the work of the enzyme alpha glucosidase so that it can reduce blood glucose levels.

A Model-Based 13C-Sucrose Breath Test Diagnostic for Gut Function Disorders Characterized by a Loss of Sucrase-Isomaltase Enzymatic Activity

BackgroundEnvironmental enteric dysfunction (EED) causes malnutrition in children in low-resource settings. Stable-isotope breath tests have been proposed as noninvasive tests of altered nutrient metabolism and absorption in EED, but uncertainty over interpreting the breath curves has limited their use. The activity of sucrose-isomaltase, the glucosidase enzyme responsible for sucrose hydrolysis, may be reduced in EED. We previously developed a mechanistic model describing the dynamics of the 13C-sucrose breath test (13C-SBT) as a function of underlying metabolic processes. ObjectivesThis study aimed to determine which breath test curve dynamics are associated with sucrose hydrolysis and with the transport and metabolism of the fructose and glucose moieties and to propose and evaluate a model-based diagnostic for the loss of activity of sucrase-isomaltase. MethodsWe applied the mechanistic model to 2 sets of exploratory 13C-SBT experiments in healthy adult participants. First, 19 participants received differently labeled sucrose tracers (U-13C fructose, U-13C glucose, and U-13C sucrose) in a crossover study. Second, 16 participants received a sucrose tracer accompanied by 0, 100, and 750 mg of Reducose, a sucrase-isomaltase inhibitor. We evaluated a model-based diagnostic distinguishing between inhibitor concentrations using receiver operator curves, comparing with conventional statistics. ResultsSucrose hydrolysis and the transport and metabolism of the fructose and glucose moieties were reflected in the same mechanistic process. The model distinguishes these processes from the fraction of tracer exhaled and an exponential metabolic process. The model-based diagnostic performed as well as the conventional summary statistics in distinguishing between no and low inhibition [area under the curve (AUC): 0.77 vs. 0.66–0.79] and for low vs. high inhibition (AUC 0.92 vs. 0.91–0.99). ConclusionsCurrent summary approaches to interpreting 13C breath test curves may be limited to identifying only gross gut dysfunction. A mechanistic model-based approach improved interpretation of breath test curves characterizing sucrose metabolism.

Investigation of extraction conditions and evaluation of the ability of antioxidants and lowering blood glucose levels of the Ensete glaucum extract

Diabetes is a type of metabolic disorder, which is the cause of many dangerous complications. Ensete glaucum (Musaceae family) has active ingredients with antioxidant and hypoglycemic characteristics in some parts of the plant. This study investigates the ability to reduce blood sugar based on the inhibition of α-amylase and α-glucosidase enzymes of Ensete glaucum stem extract. The results indicated that 70% ethanol, a material ratio of 1/30, and a temperature of 65oC for 360 minutes are the optimal conditions for the extraction process. Sonication has an extraction efficiency that is 1.8 times greater than that of a thermostatic bath or shaker. With the above conditions, the total polyphenol contents of the upper and the lower stem samples combined with sonication are higher than those without sonication. The ability to capture 2,2-Diphenyl-1-picrylhydrazyl (DPPH) free radicals of the extract used with sonication in the upper stem is four times higher than without sonication. In addition, the presence of sonication increases the capacity to inhibit the α-amylase enzyme (IC50 of the upper stem is 29.94 g/mL, the lower stem is 16.42 g/mL), compared to the absence of sonication (IC50 of the upper stem is 36 g/mL, the lower stem is 26.72 g/mL). Similar to the ability to inhibit α-glucosidase enzyme when using sonication (IC50 of the upper stem is 71.04 µg/mL, the lower stem is 91.91 µg/mL) is higher than not using sonication (IC50 of the upper stem is 142.99 µg/mL, the lower stem is 129.88 µg/mL). In general, the inhibition of α-amylase enzyme was higher than α–glucosidase enzyme in all extracts. In addition, the presence of sonication increased the polyphenol content, DPPH free radical scavenging, and hypoglycemic capacity of Ensete glaucum stem extract.

Synthesis of camphor thiazole derivates from Dryobalanops aromatica and its bioactivity as antioxidants and antidiabetes against alpha glucosidase enzymes

Camphor is synthesized from the Sumatran camphor plant (Dryobalanops aromatica) in previous experiments. It can be synthesized with thiosemicarbazide, ethy-2‑chloro acetoacetate, and sodium acetate (catalyze) to form camphor derivate with thiazole ring structure. Hydrazine and phenylhydrazine were both used to make the thiazole ring variations. All the compounds were purified by recrystallization method and characterized by TLC, FTIR, UV–vis, and LC-MS. Camphor thiazole (Product 1), camphor thiazole hydrazine (Product 2), and camphor thiazole phenylhydrazine (Product 3) were successfully synthesized with%yields of 73.24 %; 77.36 %; and 72.91 % respectively. Furthermore, their antioxidant activity was measured using the DPPH free radical method. Product 2 had the strongest antioxidant activity with IC50 value of 6.93 ppm. The antidiabetic activity was measured using the α-glucosidase enzyme. This indicated that product 1 had the best inhibitory activity against the α-glucosidase enzyme with IC50 values of 869.06 ppm.•We developed an alternative method to utilize camphor extracted from the D. aromatica plant to be used as an alternative medicinal ingredient related to antioxidants and antidiabetes.•All products were successfully synthesized and have the potential to be used as antioxidants with an IC50 value of 6.93 ppm for Product 2 and as antidiabetics by means of an α-glucosidase inhibitor with an IC50 value of 869.06 ppm for Product 1.

A MINI REVIEW ON ZINGIBERACEAE FAMILY AS ANTIDIABETIC PLANTS: ACTIVE INGREDIENTS AND MECHANISMS OF ACTIONS

Diabetes mellitus (DM) is a group of metabolic diseases characterized by hyperglycemia that occurs due to abnormalities in insulin secretion. Therapy using conventional anti-diabetic drugs is associated with serious side effects, and herbs to maintain chronic disease if conventional drugs not adequate. The purpose of this article review is to find out information about plants of the Zingiberaceae family that have anti-diabetic activity with the mechanism of action of ? -glucosidase enzyme inhibition, ? -amylase enzyme inhibition, and increased GLP-1 levels. The sources used consisted of 27 journals and reviewed 9 research journals originating from Google Scholar, Pubmed, NCBI, Elsevier, Science Direct with a span of under 10 years. The articles were then analyzed using the systematic literature review method, by collecting, evaluating, and developing research on a particular topic. From several studies conducted, the results showed that plants from the family that have antidiabetic activity include Zingiber officinale (ginger), Curcuma longa (turmeric rhizome), Curcuma aeruginosa (temu hitam), Curcuma zanthorrhiza (curcuma), Zingiber cassumunar (bangle), Kaempferia galanga (kencur), Alpinia galanga (lengkuas), Etlingera elatior (kecombrang, honje), and Elettaria cardamomum (kapulaga). Keywords: Antidiabetic; Diabetes Mellitus; Zingiberaceae

A comprehensive assessment of phytochemicals from Phyla nodiflora (L.) Greene as a potential enzyme inhibitor, and their biological potential: An in-silico, in-vivo, and in-vitro approach

This work explored Phyla nodiflora (L.) Greene as a potential source of the bioactive medicinal agent. In this aspect, methanol (PN-M) and dichloromethane (PN-D) extracts were prepared from the whole plant and evaluated for phytochemical composition (total bioactive contents, UHPLC-MS analysis, and HPLC-PDA polyphenolic quantification), biological (antioxidant and enzyme inhibition) potential and in-vivo toxicity. The PN-M was found to contain higher phenolic (26.08 mg GAE/g extract) and flavonoid (50.25 mg QE/g extract) contents which might correlate to the higher radical scavenging (DPPH: 52.94 mg TE/g extract; ABTS: 72.11 mg TE/g extract) and reducing power (FRAP: 71.96 mg TE/g extract; CUPRAC: 142.65 mg TE/g extract) antioxidant potential, as well as AChE (4.33 mg GALAE/g extract), tyrosinase (125.36 mg KAE/g extract), and amylase (1.86 mmol ACAE/g extract) inhibition activity of this extract. In contrast, the PN-D extract was found to be most active for phosphomolybdenum (1.30 mg TE/ g extract) and metal chelation (54.84 mg EDTAE/g extract) assays in addition to BChE (4.70 mg GALAE/g extract) and glucosidase (0.62 mmol ACAE/g extract) enzyme inhibition activity. The PN-M extract on UHPLC-MS analysis revealed the tentative identification of 24 different secondary metabolites, most of which belonged to the flavonoid, glycoside, and terpenoid classes of phytochemicals. The polyphenolic composition of the extracts was appraised by HPLC-PDA. Seven phenolic compounds were identified in the extracts. PN-M was found to be rich in catechin (0.25 µg/extract) and 3-OH benzoic acid (0.64 µg/extract), while PN-D contained epicatechin (0.30 µg/extract), 3-OH-4-MeO benzaldehyde (0.21 µg/extract), and 2,3-Di-Meo benzoic acid (0.97 µg/extract) in higher amounts. The methanol extract was found to be non-toxic even at higher doses. Furthermore, the relationship between the phytochemicals and the tested enzymes was highlighted by molecular docking studies. In sum, this research showed that the studied extracts were effective as enzyme inhibitors and antioxidants, suggesting it would be worth investigating in more depth for further advanced studies to explore its pharmacological properties.

Effects of Selected Terminalia and Ficus Species in the Inhibition of α-Amylase and α- Glucosidase Enzymes

Effects of Selected Terminalia and Ficus Species in the Inhibition of α-Amylase and α- Glucosidase Enzymes

In vivo inhibitory effect of Panicum maximum root extract on alpha amylase and alpha glucosidase enzymes of rats

Panicum maximum Jacq, (Poaceae) a medicinal plant used traditionally in the treatment of diseases including diabetes was evaluated for effect on alpha amylase and alpha glucosidase enzymes in vivo. The leaf extract (137, 273, and 547 mg/kg) of Panicum maximum were investigated in vivo for inhibitory effect on alpha amylase and alpha glucosidase enzymes using starch, sucrose and maltose as substrates. Acarbose was used as reference drug. The leaf extract non dose-dependently caused significant (p<0.05) reduction in blood glucose levels of treated rats with the various substrates used. The results suggest that the leaf extract of Panicum maximum have the potentials to inhibit alpha amylase and glucosidase in rats.

Antioxidant and Enzyme Inhibitory Activities of Rhoifolin Flavonoid: In Vitro and in Silico Studies.

Rhoifolin (apigenin-7-O-β-neohesperidoside) belongs to the class of flavonoids and was reported to exhibit anti-inflammatory, cytotoxic, antidiabetic, hepatoprotective, and cardioprotective activities. The current study presents the in-vitro evaluation of the antioxidative effects of rhoifolin by many assays, namely DPPH, CUPRAC, ABTS, phosphomolybdenum, and FRAP. Enzyme inhibitory potential was also evaluated for acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, amylase, and glucosidase enzymes. While results revealed weak antioxidant activities for rhoifolin, the compound demonstrated some promising enzyme inhibitory effects against BChE (4.03 mg GALAE/g) and tyrosinase (7.44 mg KAE/g) but was not active on AChE. Regarding anti-diabetic enzymes, the compound was active on amylase but did not show any inhibition effect on glucosidase. In-silico molecular docking study was performed for rhoifolin on the active site of NADPH oxidase, BChE, and amylase enzymes to verify the observed enzyme inhibitory effect. Good binding affinities were observed for rhoifolin on all the docked enzymes, revealing numerous hydrogen bonds, carbon-hydrogen, van der Waals interactions. This is the first study to evaluate the enzyme inhibition potential of rhoifolin. We concluded that the increase in the degree of glycosylation might decrease the antioxidant abilities of flavonoids and that rhoifolin had moderate enzyme inhibition abilities to be investigated in future studies.

Dynamic changes occur in the cell wall composition and related enzyme activities during flower development in Rosa damascena.

The flowering period of oil-bearing rose is short and many physiological processes occur during flower development. Changes in the cell wall composition and associated enzyme activities are important as they allow cells to divide, differentiate and grow. In the present study, changes in seven cell wall components and six cell wall-related enzyme activities at five flower development stages were investigated and the relationships between these parameters and flowering were examined. Ash content did not change between stages I to II but decreased at later stages. Neutral detergent fiber (NDF), acid detergent fiber (ADF) and hemicellulose contents increased after stage I but did not change significantly at the other developmental periods. Total pectin content increased throughout flower development. An "increase-decrease" trend was observed in total cellulose content and a "decrease-increase" pattern in uronic acid content. The activities of both glycosidases (β-galactosidase, β-glucosidase and endoglucanase) and pectinases (pectin lyase, pectin methyl esterase and polygalacturonase) increased until stage IV and decreased significantly at stage V of flower development. Correlation analysis revealed 14 positive and one negative correlation with the studied parameters. Cell wall enzymes showed positive correlations with each other. Principal component analysis (PCA) showed that ADF, NDF and cellulose content were significantly altered at stage II of flower development, and significant changes occurred in all cell wall enzyme activities between stages III and V. Overall, blooming is correlated closely with increased pectin and decreased cellulose contents, and changes in cell wall glucosidase and pectin hydrolysis enzyme activities. These results show that cell wall modifying enzymes are part of the flower development process in oil-bearing rose. Therefore, remodeling of cell wall components in petals is a process of flower development.

Phytochemical Composition and Antidiabetic Potential of Gymnema sylvestre Extracts and Formulations

Gymnema sylvestre is an Ayurvedic medicinal plant commonly known as gurmar used for the treatment of diabetes. The current study evaluated the phytochemical composition and antidiabetic potential of G. sylvestre leaf extracts and commercially available formulations. The extracts were prepared using ethanol and water through soxhelation. Phytochemical analysis revealed the presence of alkaloids, flavonoids, saponins and triterpenoids in the extracts. Chromatographic and spectroscopic techniques were employed for qualitative and quantitative comparison of the extracts and formulations. The ethanolic extract showed higher total phenolic and flavonoid content compared to the aqueous extract. In vitro antidiabetic assays demonstrated dose-dependent inhibition of alpha amylase and alpha glucosidase enzymes by the extracts. The ethanolic extract exhibited higher antioxidant and antidiabetic activity compared to the aqueous extract and formulations. Overall, the results indicate that G. sylvestre extracts possess phytochemicals and antidiabetic potential that can be further explored.

DINAMIKA KARBON DAN AKTIVITAS β-GLUKOSIDASE DI TOPSOIL DAN SUBSOIL LAHAN PERTANIAN MONOKULTUR NAGARI ALAHAN PANJANG SUMATERA BARAT

This study aimed to determine the dynamics of carbon and glucosidase enzyme activity in the topsoil and subsoil of monoculture land. This research was in Nagari Alahan Panjang, West Sumatra. Soil samples were taken using a purposive random sampling method on three cropping patterns: monoculture, rotation and intercropping, and two depths of 0-15 cm and 15-30 cm. The parameters analyzed included total N, organic C, exchangeable K, Ca, Mg, and Na, glucosidase, biomass C, and respiration. Data from observations were analyzed with Pearson statistics 8 correlation. The results showed that β-glucosidase activity was positively correlated with total N and organic C, biomass C was positively correlated with exchangeable Mg, and respiration was positively correlated with N total and β-glucosidase.

Synthesis, glycosidase inhibitory activity and computational studies of dideoxymethylnojirimycin and its derivatives

We report here the synthesis and biological evaluation of dideoxynojirimycin and its analogs and their functional effect on glucosidase enzyme inhibition against α-glucosidase(yeast), α-galactosidase and β-galactosidase (kluyveromyces lactis). All the compounds significantly inhibited the α-glucosidase(yeast) activity when compared to DNJ and shown strong inhibition against β-galactosidase (kluyveromyces lactis) when compared to DNJ. The molecular docking studies also reveals that these compounds showing strong ligand binding energies against yeast-ɑ-glucosidase- I, yeast β-galactosidase and human lysosomal acid–ɑ-glucosidase. Interestingly the analogues having N-H, N-alkyl and N-benzyl group along with ethyl group significantly inhibited the β-galactosidase activity when compared to DNJ. The in-silico studies are in correlation with invitro activity data; therefore, this study will be useful to develop further glycosidase inhibitors.

Analysis of Biological Activities of Two Novel Metal (II) Complexes of Andrographis Paniculata Crude Extract

Many diseases in nature have led to the death of many young and old. Many bacteria have developed resistance to the available antibiotics on the market. And many drugs employed in treating many diseases such as diabetes mellitus are expensive and are not locally available. Therefore, in order to search for more effective, inexpensive, and locally available drugs, this study synthesized and investigated the biological activities of Andrographis paniculata crude extract and its Co (II) and Ni (II) complexes. The crude extract and synthesized complexes were characterized using a solubility test, Infrared, and Ultraviolet-Visible spectroscopic analysis. Their antibacterial potentials were investigated against two gram-negative bacteria (Escherichia coli,Staphylococcus aureus) and three gram-negative bacteria (Proteus, Klebsiella, Pseudomonas) while their antidiabetic activities were examined against ?-amylase and ?-glucosidase enzymes. Acarbose was employed as a standard drug. The crude extract and its metal complexes showed different degrees of solubility in the employed solvents. Infrared analysis suggested coordination of the crude extract to the metal ions through the oxygen donor atom while the formation of the complexes was affirmed through the occurrence of d-d transitions in the visible region of the metal complexes. The metal complexes were found to display more antibacterial activity than the crude extract. Co (II) and Ni (II) complexes of the crude extract were found to exhibit better activities against ?-amylase and ?-glucosidase enzymes, respectively than the crude extract and acarbose. It is concluded that the metal complexes could be considered potential antibacterial and antidiabetic agents.

Novel Anti-diabesity Peptide Alkaloids from Allophylus africanus P. Beauv

Aim: The aim of the study was to characterize and investigate the mechanism of action of anti-hyperglycemic and anti-hyperlipidemic constitutents of Allophylus africanus. Background: Allophylus africanus P. Beauv is a medicinal plant commonly used in sub-Sahara Africa for the treatment of metabolic disorders and infectious diseases. Objectives: The objective of the study was to isolate and characterize anti-hyperglycemic and antihyperlipidemic chemical constituents from Allophylus africanus, and to investigate the mechanism of their enzymatic inhibitions. Methods: The chemical constituents were isolated using various column chromatographic techniques. The anti-hyperlipidemic and anti-hyperglycemic properties of the chemical constituents were investigated by measuring their inhibitory effects on porcine pancreatic lipase and α- glucosidase enzymes. Fluorescence quenching constants obtained from Stern−Volmer plots were used to determine the mechanisms of inhibitory action. Results: Twelve compounds, of which three were new peptide alkaloids, ethylamino asperphenamate (10), allophylane (11) and allophyline (12), were isolated. The new peptide alkaloids and asperphenamate (9) inhibited porcine pancreatic lipase in a dose-dependent manner with IC50 < 90 μM. Also, 9, 12, stigmasta-5, 22-dien-3-O-β-D-glucoside (3) and eudesmenol (5) inhibited α- glucosidase enzymes with IC50 < 165 μM, which was lower than that of standard drug, acarbose (432.16 ± 6.52 μM). From the Stern-Volmer plots, 9 and 10 indicated a static quenching, while 11 and 12 suggested the occurrence of both static and dynamic quenching mechanisms on porcine pancreatic lipase. On α-glucosidase, only 12 exhibited a concurrent static and dynamic quenching mechanism. Conclusion: The anti-diabesity compounds obtained from A. africanus established its potential for the treatment of metabolic disorders. Among the isolated compounds, three have been reported for the first time in nature while others have been reported for the first time in the plant.

Blood glucose lowering and anti-oxidant potential of erythritol: An in vitro and in vivo study.

Diabetes is a major cause of death worldwide and Nigeria is not an exception. The quest to lower sugar levels has become a major factor in the management of diabetes; this has occasioned the use of substitutes for refined sugar in beverages. Erythritol is a natural sweetener gaining immense interest in recent times. Like metformin, erythritol has shown hydroxyl radical scavenging ability and has metabolic profile suitable for diabetics. Therefore, the blood glucose-lowering and anti-oxidant properties of erythritol under in vitro and in vivo systems were accessed. Radical scavenging assay (ABTS and DPPH) and inhibition of carbohydrate digestive enzymes (alpha-amylase and alpha-glucosidase) were employed to determine in vitro anti-oxidant and glucose regulatory function of erythritol respectively. Molecular docking studies were performed between 3D structures of human pancreatic alpha-amylase and alpha-glucosidase, isomaltase from saccharomyces cerevisiae with erythritol. The drug-like activity of erythritol was also assessed.Thereafter, we investigated the effect of erythritol on blood glucose and antioxidant status of normal and streptozocin- nicotinamide-induced diabetes rats which were grouped into five (n = 5); Normal, Ery (normal and administered erythritol), Db (diabetic control), Db + Ery (diabetic and administered erythritol), and Db + Met (diabetic and administered metformin). Erythritol showed a considerable radical scavenging activity and an ability to inhibit alpha-amylase and alpha-glucosidase in vitro. Also, a significant reduction in glucose intolerance, blood glucose and hemoglobin A1c levels and improved antioxidant level was seen in erythritol-treated diabetic rats. Erythritol showed anti-oxidant activity, alpha amylase and glucosidase enzyme inhibition property, improved antioxidant status and ameliorated blood glucose, HbA1c, and glucose intolerance following diabetes.

The potential of five wild growing aromatic plants from Hemaq Beniung Customary Forest on antidiabetic activity

Abstract. Kuspradini H, Putri AS, Kiswanto, Sa’adah H, Fajriansyah, Rizqullah MA, Larasati AG, Zulfa NA, Egra S, Yamauchi K, Mitsunaga T. 2023. The potential of five wild growing aromatic plants from Hemaq Beniung Customary Forest on antidiabetic activity. Biodiversitas 24: 2156-2162. Several aromatic plants have been used for millennia across the globe for their hyperglycemic properties. The in vitro inhibitory activity of extracts from Blumea balsamifera (L.) DC., Cinnamomum parthenoxylon (Jack) Meisn., Clausena excavata Burm.fil., Neouvaria acuminatissima (Miq.) AiryShaw, and Piper porphyrophyllum N.E.Br. were tested. The aim of this study was to determine the phytochemical constituent, total phenolic and flavonoid content of five aromatic plant extracts obtained from West Kutai, East Kalimantan as well as the antioxidant and antidiabetic activity via in vitro assays. Assays for total phenol and flavonoid content were based on Follin-Ciocalteu and aluminum chloride reagents, respectively. In this study, the antidiabetic activity was determined by measuring the inhibitory activity of ?-glucosidase enzyme, while the in vitro antioxidant activity was measured using the DPPH scavenger method. The order of inhibition of DPPH free radical was P. porphyrophyllum ethanol extract > N. acuminatissima ethanol extract > B. balsamifera ethyl acetate extract, which was found to be directly proportional to their total phenolic content. On the other hand, the order of inhibition of ?-glucosidase enzyme was found to be N. acuminatissima ethanol extract > C. parthenoxylon ethanol extract > N. acuminatissima ethyl acetate extract. Out of the 10 extracts studied, only 3 showed inhibition activity on ?-glucosidase. These findings indicate the aromatic plant extract's potential as a natural therapy for preventing and treating carbohydrate metabolic problems. As a result, the N. acuminatissima ethanol extract, which exhibits both antidiabetic and antioxidant activity, can be used in the pharmaceutical industry for the production of functional foods and herbal medicines. This is our first report on N. acuminatissima as an antioxidant and antidiabetic agent.