scholarly journals Modes of Inhibition ofα-Amylase andα-Glucosidase by Aqueous Extract ofMorinda lucidaBenth Leaf

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
M. I. Kazeem ◽  
J. O. Adamson ◽  
I. A. Ogunwande
Keyword(s):  
Diabetes Mellitus ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Leaf Extracts ◽  
Glucosidase Inhibitors ◽  
Ethanolic Extracts ◽  
Insulin Secretagogues ◽  
Percentage Yield ◽  
Oral Hypoglycemic Drugs

Diabetes mellitus is a metabolic disorder of glucose metabolism. The management of blood glucose level is the hallmark in the treatment of this disease. This may be achieved through the use of oral hypoglycemic drugs such as biguanides, insulin secretagogues, andα-glucosidase inhibitors. The purpose of the present study was to investigate the inhibitory effect ofMorinda lucidaleaf extracts on the activities ofα-amylase andα-glucosidase. This was performed usingα-amylase fromAspergillus oryzaeandα-glucosidase fromSaccharomyces cerevisiae.Aqueous extract ofMorinda lucidagave the highest percentage yield (9.99%) of the plant out of the three extracts (compared to acetone and ethanolic extracts) and possesses the highest inhibitory activity againstα-amylase (IC50value of 2.30 mg/mL) andα-glucosidase (IC50value of 2.00 mg/mL). Kinetic analysis revealed that the aqueous extract of this plant leaf inhibited theα-amylase competitively but displayed mixed noncompetitive mode of inhibition towardsα-glucosidase. It can be concluded that aqueous extract ofMorinda lucidaexhibited the best inhibitory activity on the two enzymes studied and the presence of phytochemicals like flavonoids, saponins, and tannins may have contributed greatly to the inhibitory activity of the plant extract.

scholarly journals Phytochemical evaluation and in vitro antidiabetic efficiency of isopropanolic leaf extract of pimenta racemosa

2020 ◽  
Vol 7 (2) ◽  
pp. 50-55
Author(s):  
Anitha T A ◽  
Pakutharivu T ◽  
Nirubama K ◽  
Akshaya V
Keyword(s):  
Diabetes Mellitus ◽  
Glucose Uptake ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Yeast Cells ◽  
Antidiabetic Activity ◽  
Leaf Extracts ◽  
Pimenta Racemosa

The traditional herbal medicines are mainly obtained from plants are used in the management of Diabetes mellitus. The main objective of this work was to assess the presence of phytochemical compounds and to evaluate the in vitro antidiabetic activity of isopropanolic extracts of Pimenta racemosa leaves by studying their α-amylase inhibitory activity and glucose transport across yeast cells. Screening of phytochemicals showed positive results for alkaloids, steroids, cardiac glycosides, terpenoids, reducing sugars, anthraquinones, and results of in vitro α-amylase inhibitory studies demonstrated there was a dose-dependent increase in percentage inhibitory activity by the isopropanolic leaf extracts of Pimenta racemosa. At a concentration of 1 mg/ml, the extract showed a percentage inhibition 33.6 and for 5 mg/ml it was 91.2. The glucose uptake study was also studied through yeast cells by analyzing theamount of glucose remaining in the medium after a specific time intervals. It serves as an indicator for the capability of isopropanolic leaf extracts of Pimenta racemosa to transport the glucose into yeast cells. As a result, we found that the isopropanolic leaf extract of Pimenta racemosa have inhibitory activity against αamylase and also, which is efficient in glucose uptake. This therapeutic potentiality of Pimenta racemosa could be exploited in the treatment of Type 2 Diabetes mellitus. Further studies are also required to elucidate whether the plant have antidiabetic potential by in vivo for corroborating the traditional claim of the plant.

scholarly journals Chemical Composition andα-Glucosidase Inhibitory Activity of VietnameseCitrusPeels Essential Oils

2016 ◽  
Vol 2016 ◽  
pp. 1-5 ◽  
Author(s):  
Nguyen Hai Dang ◽  
Pham Huong Nhung ◽  
Bui Thi Mai Anh ◽  
Dinh Thi Thu Thuy ◽  
Chau Van Minh ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Potential Use

Background. Inhibition ofα-glucosidase is an important factor to control postprandial hyperglycemia in type 2 diabetes mellitus.Citrusessential oils (CEO) are among the most widely used essential oils, and some of them exhibited promising antidiabetic effect. However, theα-glucosidase inhibition of CEO has not been investigated so far. The present work aims to evaluate theα-glucosidase inhibition of essential oils from six VietnameseCitruspeels.Methods. The chemical composition of essential oils obtained by hydrodistillation from sixCitruspeels was analyzed by GC-MS. All essential oils were tested for their inhibitory activity onα-glucosidase usingp-nitrophenyl-α-D-glucopyranoside as substrate.Results. In Buddha’s hand and lime peels, the major components were limonene (59.0–61.31%) andγ-terpinene (13.98–23.84%) while limonene (90.95–95.74%) was most abundant in pomelo, orange, tangerine, and calamondin peels. Among the essential oils, the Buddha’s hand oil showed the most significantα-glucosidase inhibitory effect with the IC50value of 412.2 μg/mL. The combination of the Buddha’s hand essential oil and the antidiabetic drug acarbose increased the inhibitory effect.Conclusions. The results suggested the potential use of Buddha’s hand essential oil as an alternative in treatment of type 2 diabetes mellitus.

scholarly journals The Effect of Alcoholic and Aqueous Extract of Piper nigrum on the Larvae of Culex pipiens molestus Forskal (Diptera:Culicidae)

2020 ◽  
Vol 17 (1) ◽  
pp. 0028
Author(s):  
Aulfat T. Yaseen
Keyword(s):  
Aqueous Extract ◽  
Culex Pipiens ◽  
Adult Life ◽  
Inhibitory Effect ◽  
Piper Nigrum ◽  
The Third ◽  
Significant Inhibitory Effect ◽  
Ethanolic Extracts ◽  
Growth Development ◽  
Culex Pipiens Molestus

          The present study includes the effect of the ethanolic and aqueous extract of Piper nigrum against the third instar of Culex pipiens molestus (Diptera:Culicidae) in different concentrations: 1, 1.5 ppm of ethanolic extracts of Piper nigrum causing 100% mortality of larvae in the second day of treatment, while the concentrations 5% of aqueous extracts of Piper nigrum caused 100% mortality of larvae in the second day of treatment. The concentration 2.5% caused 100% mortality of larvae after four days of treatment. The current study also detected the effect of 0.1% concentration of Piper nigrum aqueous extract. The effect of this concentration has been studied on the growth of the ovaries and their follicles along a period 96 hours after emergence of adult life. The results of this study has clearly shown that the concentration 0.1% of Piper nigrum aqueous extract gave a highly significant inhibitory effect on the growth development of the ovaries and their follicles.

2-Mercapto Benzothiazole Derivatives: As Potential Leads for the Diabetic Management

2020 ◽  
Vol 16 (6) ◽  
pp. 826-840
Author(s):  
Saeed Ullah ◽  
Salma Mirza ◽  
Uzma Salar ◽  
Shafqat Hussain ◽  
Kulsoom Javaid ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
Kinetic Studies ◽  
Binding Pocket ◽  
Docking Studies ◽  
Standard Drug ◽  
Dual Nature ◽  
Benzothiazole Derivatives ◽  
Glucosidase Inhibitors

Background: Results of our previous studies on antiglycation activity, and the noncytotoxicity of 2-mercapto benzothiazoles, encouraged us to further widen our investigation towards the identification of leads against diabetes mellitus. Methods: 33 derivatives of 2-mercapto benzothiazoles 1-33 were evaluated for in vitro α- glucosidase inhibitory activity. Mode of inhibition was deduced by kinetic studies. To predict the interactions of 2-mercapto benzothiazole derivatives 1-33 with the binding pocket of α-glucosidase enzyme, molecular docking studies were performed on the selected inhibitors. Results: Compounds 2-4, 6-7, 9-26, 28 and 30 showed many folds potent α-glucosidase inhibitory activity in the range of IC50 = 31.21-208.63 μM, as compared to the standard drug acarbose (IC50 = 875.75 ± 2.08 μM). It was important to note that except derivative 28, all other derivatives were also found previously to have antiglycating potential in the range of IC50 = 187.12-707.21 μM. Conclusion: A number of compounds were identified as dual nature as antiglycating agent and α- glucosidase inhibitors. These compounds may serve as potential lead candidates for the management of diabetes mellitus.

scholarly journals IDENTIFICATION OF THE ANTIBACTERIAL EFFICACY OF ETHANOLIC EXTRACTS FROM AGLAONEMA COMMUTATUM SCHOTT LEAVES AND ITS CULTIVARS AGAINST ESCHERICHIA COLI STRAIN

2020 ◽  
pp. 21-30
Author(s):  
Maryna Opryshko ◽  
Oleksandr Gyrenko ◽  
Lyudmyla Buyun ◽  
Halyna Tkachenko ◽  
Natalia Kurhaluk ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Antimicrobial Activities ◽  
Farm Animals ◽  
Leaf Extracts ◽  
Ethanolic Extracts ◽  
Inhibition Zones ◽  
In Vitro Inhibition

This study aimed to evaluate the antibacterial activity of ethanolic extracts obtained from the leaves of Aglaonema commutatum Schott and its cultivars («Malay Beauty», «Silver Queen», and «Silver King») against Escherichia coli (Migula) Castellani and Chalmers (ATCC® 25922™) strain. The leaves of Aglaonema commutatum plants and its cultivars, cultivated under glasshouse conditions, were sampled at M. M. Gryshko National Botanic Garden (NBG), National Academy of Science of Ukraine (Kyiv, Ukraine). The leaves were brought into the laboratory for antimicrobial studies. Freshly sampled leaves were washed, weighed, and homogenized in 96% ethanol (in proportion 1:19) at room temperature. The extracts were then filtered and investigated for their antimicrobial activity. Escherichia coli (Migula) Castellani and Chalmers (ATCC® 25922™) strain was used in our study. Antimicrobial activities of various ethanolic extracts obtained from leaves of Aglaonema commutatum plants and its cultivars («Malay Beauty», «Silver Queen», and «Silver King») against Escherichia coli (Migula) Castellani and Chalmers (ATCC® 25922™) strain was screened in the current study. The testing of the antibacterial activity of the plant extracts was carried out in vitro by the Kirby-Bauer disc diffusion technique. The leaf extracts from A. commutatum «Silver Queen» and A. commutatum 'Silver King' exhibited higher inhibitory activity than the extracts from A. commutatum and A. commutatum «Malay Beauty». Maximum in vitro inhibition was scored by A. commutatum «Silver Queen», followed by A. commutatum «Silver King», A. commutatum, and A. commutatum «Malay Beauty». In particular, the leaf extracts from A. commutatum «Silver Queen» and A. commutatum 'Silver King' exhibited higher inhibitory activity than the extracts from A. commutatum and A. commutatum «Malay Beauty». Maximum in vitro inhibition was scored by A. commutatum «Silver Queen», followed by A. commutatum «Silver King», A. commutatum, and A. commutatum «Malay Beauty», which presented inhibition zones of (18.6±1.2) mm, (16.1±0.9) mm, (15.7±1.1) mm, and (13.5±1.0) mm, respectively. In the case of the positive controls, 96% ethanol possesses a mild anti-E. coli effect, which presented inhibition zones of (9.5±1.2) mm. The inhibition zone diameters were increased by 96% (p<0.05) for A. commutatum «Silver Queen», by 69 % (p<0.05) for A. commutatum «Silver King», by 65 % (p<0.05) for A. commutatum, and by 42 % (p<0.05) for A. commutatum «Malay Beauty». Thus, the use of these plants in traditional medicine and veterinary medicine was experimentally confirmed as a potential source of raw materials for the development of medicines in the future, as well as for the development of innovative feed for farm animals.

scholarly journals Structure Related α-Glucosidase Inhibitory Activity and Molecular Docking Analyses of Phenolic Compounds From Paeonia Suffruticosa

2021 ◽  
Author(s):  
Po-Chun Chen ◽  
Bongani Sicelo Dlamini ◽  
Chiy-Rong Chen ◽  
Yueh-Hsiung Kuo ◽  
Wen-Ling Shih ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Phenolic Compounds ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Docking Studies ◽  
Inhibition Mechanism ◽  
Root Bark ◽  
Paeonia Suffruticosa ◽  
Glucosidase Inhibitors

Abstract In the continuous search for α-glucosidase inhibitors, eleven phenolic compounds (1-11) were isolated from the root bark of Paeonia suffruticosa. Their α-glucosidase inhibitory activity and inhibition mechanism were investigated using an in vitro inhibition assay and molecular docking studies. Compounds 2, 5, 6, and 8-11 (IC50 between 290 and 431 µM) inhibited α-glucosidase more effectively than the reference compound acarbose (IC50=1463 ± 29.5 µM). Among them, compound 10 exhibited the highest α-glucosidase inhibitory effect with an IC50 value of 290.4 ± 9.6 µM. Compounds 2, 5, 9 10 and 11 were found to be competitive inhibitors, while compounds 6 and 8 were noncompetitive inhibitors of α-glucosidase. Computational analyses showed that the main binding forces between the compounds and the main residues were hydrogen bonds. The results indicated that these compounds had considerable α-glucosidase inhibitory activity.

Phytochemical analysis and In vitro Antidiabetic activity of aqueous extract of Lagerstroemia speciosa and Aegle marmelos

2021 ◽  
pp. 4697-4701
Author(s):  
Anandhu K S ◽  
Manu Jose ◽  
Sweety Kuriakose ◽  
Jayalakshmi P M
Keyword(s):  
Aqueous Extract ◽  
Plant Extracts ◽  
Inhibitory Activity ◽  
Antidiabetic Activity ◽  
Inhibition Assay ◽  
Inhibitory Effects ◽  
Aegle Marmelos ◽  
Leaf Extracts ◽  
Ic50 Value ◽  
Glucose Diffusion

Diabetes Mellitus is a metabolic disorder characterized by hypoglycemia, resulting from absolute or relative deficiency of insulin. Worldwide about 220million people affected. Low-cost herbal treatment is recommended due to their lesser side effect. The aim of the current study was to determine the antidiabetic activity of aqueous leaf extracts of Lagerstroemia speciosa (Lythraceae) and Aegle marmelos (Rutaceae) using alpha amylase inhibition assay and glucose diffusion inhibition assay. In alpha amylase inhibition assay, the leaf extracts of A.marmelos (at a concentration 100µg/ml) exhibited 54.68% of α amylase inhibitory activity with an IC 50 values 92.04µg/ml whereas the leaf extracts of L. speciosa (at a concentration of 100µg/ml) exhibited 60.36% of α amylase inhibitory activity with an IC50 value of 68.19µg/ml .However the mixture of plant extracts (at a concentration of 100µg/ml) exhibited 94.87% inhibition with an IC50 value of 13.145µg/ml. Both plant extracts showed appreciable α amylase inhibitory effects, but the mixture showed more inhibitory effects than the individual plant extracts. In glucose diffusion inhibition assay, the aqueous extract of A. marmelos leaves exhibited maximum glucose diffusion inhibition (76.886%) at 150 minutes as well as L. Speciosa leaf extract showed the maximum inhibition of 79.5357% at the same time interval. The mixture of plant extracts exhibited 87.4274% inhibition at 150 minutes which produces more effects than the two plants.

scholarly journals First Identification of α-Glucosidase Inhibitors from Okra (Abelmoschus Esculentus) Seeds

2013 ◽  
Vol 8 (8) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Wannisa Thanakosai ◽  
Preecha Phuwapraisirisan
Keyword(s):  
Diabetes Mellitus ◽  
Kinetic Study ◽  
Inhibitory Effect ◽  
Seed Extract ◽  
Significant Decline ◽  
Hypoglycemic Effect ◽  
Competitive Behavior ◽  
Active Components ◽  
Glucose Residue ◽  
Glucosidase Inhibitors

Infusion of roasted okra seeds has long been consumed in Turkey for diabetes mellitus therapy. Previous reports of a hypoglycemic effect observed in rats administrated with okra seed extract indicated a possible connection with inhibition of intestinal α-glucosidase. An attempt to identify active components was first herein conducted using α-glucosidase-inhibition-guided isolation, yielding two major flavonol glucosides named isoquercetin (2) and quercetin-3- O-β-glucopyranosyl-(1″′ →6″)-glucoside (3). They selectively inhibited rat intestinal maltase and sucrase, in which isoquercetin (2) was 6–10 times more potent than its related diglucoside 3. This result suggested that an increase in hydrophilicity by the additional glucose residue in 3 led to a significant decline in the inhibitory effect and raised the possible involvement of the free 3-OH in exerting the inhibition. Our postulation was evaluated by examining α-glucosidase inhibition of quercetin (1), and the aglycone of 2 and 3, whose 3-OH is free from any glucose moiety. Interestingly, 1 displayed a broad inhibitory effect toward rat intestinal and baker's yeast α-glucosidases, with improved potency. A kinetic study of 1 indicated that it inhibited maltase by two distinct mechanisms, in competitive ( K i 462 μM) and noncompetitive ( K i 2153 μM) manners, whereas the mechanism underlying the inhibition of sucrase was verified as being of a competitive behavior ( K i 218 μM).

scholarly journals Inhibitory Activity of β-lactamases by Hydro-Ethanolic Extracts of Harungana madagascariensis, a Plant of the Ivorian Pharmacopoeia

2020 ◽  
pp. 157-162
Author(s):  
Toty Abalé Anatole ◽  
Aka Ayébé Edwige ◽  
Guédé Kipré Bertin ◽  
Konan K. Fernique ◽  
Adrien Jehaes ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Health Concern ◽  
Resistant Bacteria ◽  
Water Mixture ◽  
Phytochemical Screening ◽  
Public Health Concern ◽  
Ethanolic Extracts ◽  
New Antibiotics ◽  
Inhibitory Potential

Infection due to multi-resistant bacteria is a public health concern. Unfortunately, the prospect of developing new antibiotics seem not to be on the horizon. Faced with this impasse, medicinal plants could be an alternative for the development of new molecules. The aim of this study was to determine the inhibitory effect of H. madagascariensis extracts on β-lactamases. Extraction of bioactive compounds from trunk barks and leaves of the plant was done in an ethanol-water mixture (70:30). Anti-β-lactamase activity was evaluated by spectrophotometry after the removal of tannins and a phytochemical screening was used to identify the groups of compounds. Concentrations inhibiting 50% of enzyme activity were 0.005±0.001 mg/mL (CTX-M-15), 0.01±0.001 mg/mL (P99) and 0.027±0.009 mg/mL (NDM-1) for bark extracts and 0.704 mg/mL for leaves extracts. Phytochemical screening revealed the presence of flavonoids in bark extracts. The ethanolic extracts of the trunk bark exert a good inhibitory activity on CTX-M-15, P99 and NDM-1 β-lactamases and this activity could be attributed to the presence of the flavonoids. Further studies by bio-guided fractionation of the ethanolic extracts of the bark could yield fractions with high inhibitory potential of β-lactamases.

scholarly journals CYP-450 Mediated Herb-Drug Interactions of Ashwagandha and AYUSH-64 Used in COVID-19 Integrative Management: A Case Example of Remdesivir

2021 ◽  
Author(s):  
Siva Swapna Kasarla ◽  
Swapnil Borse ◽  
Yashwant Kumar ◽  
Neha Sharma ◽  
Madhu Dikshit
Keyword(s):  
Drug Interactions ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
In Silico ◽  
Withania Somnifera ◽  
Inhibitory Effect ◽  
Inhibition Studies ◽  
Good Oral Bioavailability ◽  
Integrative Management

Abstract AimWithania somnifera Dunal (WS), known as Ashwagandha and AYUSH-64, a polyherbal formulation are repurposed for the management of COVID-19. The extensive use of these botanicals as home remedy along with other drugs for managing multifarious disease conditions is increasing over nations. This raises high chances of herb-drug interactions (HDIs) which may be beneficial, harmful, or even fatal. Therefore, current study aimed to explore the CYP mediated herb-drug interactions (HDIs) of Ashwagandha and AYUSH-64 along with case example of remdesivir to harness the best of these HDIs for integrative management of COVID-19Materials and MethodsThe aqueous extract of Ashwagandha and AYUSH-64 were characterized by LC-MS/MS. The in-silico pharmacokinetic (ADME) parameters were studied by using ADME tool. The in-vitro CYP-450 (CYP3A4, 2C8, 2D6) inhibition studies of WS and AYUSH-64 alone and in combination with a remdesivir were carried out resembling clinically scenario.ResultsTotal of 11 and 24 phytoconstituents were identified from the aqueous extract of Aswagandha and AYUSH-64. The in-silico ADME studies revealed that most of the phytoconstituents showed good oral bioavailability, drug likeliness, GI affinity and some of them displayed CYP-450 inhibitory activity. The in-vitro CYP-450 studies of remdesivir showed moderate inhibitory effect on CYP3A4, 2C8, 2D6. The aqueous extract of Aswagandha did not show any inhibitory activity towards all the studied CYP’s alone and in combination with remdesivir (IC50 >100µg/ml). Whereas, AYUSH-64 also followed the same trend but showed moderate inhibitory effect on CYP2C8 (IC50 <100µg/ml).ConclusionAswagandha did not exhibit HDIs with the CYP3A4, CYP2C8 and CYP2D6 thereby seem to be safe to co-administer with respective substrates. Whereas, AYUSH-64 only showed moderate HDIs towards CYP2C8 substrate among studied CYP enzymes. Caution is therefore warranted for prescribing AYUSH 64 along with CYP2C8 substrate drugs.

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