scholarly journals Linking the Phytochemicals and the α-Glucosidase and α-Amylase Enzyme Inhibitory Effects of Nigella sativa Seed Extracts

Foods ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 1818
Author(s):  
Salima Tiji ◽  
Mohamed Bouhrim ◽  
Mohamed Addi ◽  
Samantha Drouet ◽  
Jose Manuel Lorenzo ◽  
...  

Nigella sativa L. (Ranunculaceae), commonly referred to as black seeds or black cumin, is used in popular medicine (herbal) all over the world for the treatment and prevention of several diseases, including diabetes. This study aims to investigate the inhibitory effect of N. sativa extracts and fractions against the activities of intestinal α-glucosidase and pancreatic α-amylase in vitro, and to explain the inhibitory effect of these fractions against these enzymes by identifying their active compounds responsible for this effect and determine their modes of inhibition. To do so, N. sativa hexane and acetone extracts were prepared and analyzed by GC–MS and HPLC–DAD, respectively. The hexane extract was further fractioned into eight different fractions, while the acetone extract generated eleven fractions. The extracts as well as the resulting fractions were characterized and evaluated for their potential in vitro antidiabetic activity using intestinal α-glucosidase and pancreatic α-amylase inhibitory assays in vitro. Hexane extract and fractions were less active than acetone extract and fractions. In the case of intestinal α-glucosidase activity, the acetone fraction SA3 had a high inhibitory effect on intestinal α-glucosidase activity with 72.26 ± 1.42%, comparable to the effect of acarbose (70.90 ± 1.12%). For the pancreatic α-amylase enzymatic inhibitory assay, the acetone fractions showed an inhibitory capacity close to that for acarbose. In particular, the SA2 fraction had an inhibitory effect of 67.70 ± 0.58% and was rich in apigenin and gallic acid. From these fractions, apigenin, (−)-catechin, and gallic acid were further characterized for their inhibitory actions. IC50 and inhibition mode were determined by analyzing enzyme kinetic parameters and by molecular modeling. Interestingly, (−)-catechin showed a possible synergistic effect with acarbose toward α-glucosidase enzyme inhibition, whereas apigenin showed an additive effect with acarbose toward α-amylase enzymatic inhibition. Furthermore, we studied the toxicity of N. sativa hexane and acetone extracts as well as that of acetone fractions. The result of acute toxicity evaluation demonstrated that N. sativa extracts were nontoxic up to a concentration of 10 g/kg, except for fraction SA3. Taken together, these results indicate that N. sativa extracts and/or derived compounds could constitute promising nutraceuticals for the prevention and treatment of type 2 diabetes mellitus.

2020 ◽  
Vol 12 (1) ◽  
pp. 57-73
Author(s):  
Mansurat B. FALANA ◽  
Quadri O. NURUDEEN

Extraction of the leaves of Carica papaya (family Caricaceae) and Azadirachta indica (family Meliacea) were done using solvents with varying polarities (acetone, hexane and ethylacetate). The crude extracts were screened for phytoconstituents using the preliminary method and high-performance liquid chromatography (HPLC) for separation and quantification of the constituents. Susceptibility of three medically important microorganisms (Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922 and Candida alblicans) to the solvent extracts was tested at 100 mg/mL, 50 mg/mL and 25 mg/mL concentrations the disc diffusion technique. Tannins, saponins, alkaloids, steroids, flavonoids and anthraquinone were present in all the solvent extracts of A. indica and C. papaya. Protein was present in all the solvent extracts of A. indica but absent in all the solvent extracts of C. papaya. Terpenoid was only present in hexane extract of A. indica but absent in other solvent extracts of A. indica and C. papaya. Flavonoid was present in all but only absent in ethylacetate extract of A. indica. Glycoside was present in all but absent in hexane extract of A. indica. Coumarin was only present in acetone extracts of both plants and absent in other solvent extracts of the two plants. Extracts of Carica papaya and Azadirachta indica displayed varying inhibitory activities (between 5.00-15.00 mm) against the organisms at all the tested concentrations. Acetone extract of A. indica produced zones of inhibition ranging from 5.00-14.00 mm while acetone extract of C. papaya produces a range of 4.00-10.00 mm. Also, hexane extract of A. indica produced inhibition range of 7.00-10.00 mm whereas hexane extract of C. papaya produces a range of 5.00-15.00 mm. However, ethylacetate extract of A. indica produced inhibition range of 5.00-13.67 mm, while ethylacetate extract of C. papaya produce a range of 5.00-15.00 mm. Different compounds quantified as different peaks by HPLC in the different solvent extracts of Carica papaya are acacic acid, genistein, protodioscin, betulinic acid, phorbolester, creptolepinone, brusatol and alpha ionone while the fractions from the solvent extracts of Azadirachta indica are myricetin, azadirachtol, azadirachtin a, pentadecane, phytol, azadirachnol, quercetin, b caryophyllen, alpha ionone, ascaridole, trams.b.farnes. Results obtained in this work indicated that all the solvent extracts of Carica papaya and Azadirachta indica contained active phytoconstituents and the extracts displayed good potentials at preventing diseases associated with the microorganisms tested in this work.


2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Hayat Ouassou ◽  
Touda Zahidi ◽  
Saliha Bouknana ◽  
Mohamed Bouhrim ◽  
Hassane Mekhfi ◽  
...  

Many medicinal plants around the world are used for therapeutic purposes against several diseases, including diabetes mellitus. Due to their composition of natural substances that are effective and do not represent side effects for users, unlike synthetic drugs, in this study, we investigated the inhibitory effect of Caralluma europaea (CE) on α-glucosidase activity in vitro; then the kinetics of the enzyme were studied with increasing concentrations of sucrose in order to determine the inhibition type of the enzyme. In addition, this effect of Caralluma europaea (CE) was confirmed in vivo using rats as an experimental animal model. Among the five fractions of CE, only the ethyl acetate fraction of C. europaea (EACe) induced a significant inhibition of α-glucosidase and its inhibition mode was competitive. The in vivo studies were conducted on mice and rats using glucose and sucrose as a substrate, respectively, to determine the oral glucose tolerance test (OGTT). The results obtained showed that the EACe and the aqueous extract of C. europaea (AECe) have significantly reduced the postprandial hyperglycemia after sucrose and glucose loading in normal and diabetic rats. AECe, also, significantly decreased intestinal glucose absorption, in situ. The results obtained showed that Caralluma europaea has a significant antihyperglycemic activity, which could be due to the inhibition of α-glucosidase activity and enteric absorption of glucose.


2017 ◽  
Vol 30 (3) ◽  
pp. 10
Author(s):  
Maroof Sabti Juma Al-Ammash

 The present study included experimental effect of Metronidazole drug and Alcoholic extract of Nigella sativa seeds on T. vaginalis that cultivated on  i               i    Results showed that the numbers of parasite began increasing during a period after 24-48 hrs then began decreasing after 72-96 hrs, so that 72 hrs from growth considered logarithmic phase of T. vaginalis growth. Present results showed poisonous effect of N. sativa alcoholic extract that was prepared in laboratory and imported at concentrations (450, 550, 650 and 750) mg/ml on T. vaginalis by observing gradual decrease of trophozoite numbers with concentrate increase of extracts during growth periods (24, 48, 72 and 96) hrs.         Different concentrations of Metronidazole were used as chemical therapy and control model, the results of the drug effects were followed-up daily, where current results showed (after 24 hours of concentration added) a high reduction in number and activity of the parasites at all concentrations of the drug were     ,   p ci lly 150     200 μg/ l, th  parasites disappeared completely after 96 hours, also the inhibitory concentration50 (IC50) of the parasit   w   100 μg/ l ( ft r 48 h  r  incubation).        The inhibitory effect of N. sativa alcoholic extract on the number and activity of T. vaginalis parasite was noted that the concentrations (450 and 550 mg/ml) were approximated in their effect on parasite growth, while the concentrations 650 and 750 mg/ml were the best in their inhibitory activity for parasite growth after 96 hours of addition. The concentration that causes 50% of death inculture (IC50) was 550 mg/ml (after 72 hours of concentration addition).


2020 ◽  
Vol 10 (3) ◽  
pp. 31-35
Author(s):  
R ARATHY ◽  
K MURUGAN ◽  
KV DINESH BABU ◽  
GS MANOJ

Diabetes is a notorious and growing clinical and public health issue. The International Diabetes Federation assumes that 592 million had diabetes by 2035 and that by 2040 the number will increase to 642 million. Cardiovascular corollary accounts for four million deaths annually attributable to diabetes. Evidence reveals that certain glucose-lowering phytochemicals can improve vascular outcomes with type 2 diabetes, which, together with better understanding of using multiple therapies concurrently, offers opportunities for beneficial personalization of medication regimens. Anthocyanins are coloured pigments and are natural antioxidants. Keeping this in focus, this study was undertaken to evaluate the in vitro antidiabetic activity in the petals of wild Impatiens balsamina L. The anthocyanin was extracted from floral petals of wild balsam species and purified to homogeneity using chromatographic techniques. Evaluation of in vitro antidiabetic properties of anthocyanin extract revealed a dose-dependent increase in the inhibitory effect on the alpha-glucosidase (200 μg/ml) and alpha-amylase enzymes (500 μg/ml) and was comparable with the standard acarbose drug (189 μg/ml and 50 μg/ml). These results indicated that anthocyanin could be used as a source of functional food and nutraceuticals. This information from wild species will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Future studies are planned to substantiate the antidiabetic power of anthocyanin using in vivo animal models. Keywords: Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L.


Author(s):  
Abdulhafiz Damilola Oso ◽  
Idris Bello ◽  
Yusuf Sa’idu ◽  
Onu Andrew

The aim of the current study is to evaluate the inhibition of α-glucosidase activity by stem bark extract of Albizia chevalieri. The activity of alpha glucosidase was assayed in vitro using 50 mM acetate buffer pH 6.0 (prepared from acetic acid and sodium acetate) and various concentration of maltose (0.5 mM to 10 mM). Five test tubes, labeled TA – TE, each containing 1.5 ml of acetate buffer, 0.5 ml of alpha glucosidase and 0.5 ml of a known concentration of plant extract and control tubes (CA – CE) were assessed for Alpha glucosidase activity. The results showed that hexane, ethyl acetate and methanol extracts inhibited α-glucosidase activity. The results further indicated that the extracts act by competitive inhibition with inhibition constant of 232 mg/ml, 157 mg/ml and 67 mg/ml for hexane, ethyl acetate and methanol extracts, respectively. The value for the inhibition constants shows that there is a strong binding of the enzyme to the inhibitor as the polarity of solvent increases. The inhibitory activity of Albizia chevalieri may be due one or more of the phytochemicals present in the extracts.


Author(s):  
Sushant A Shengule ◽  
Sanjay Mishra ◽  
Shweta Bodhale

 Objective: The present study was initiated to screen the hydroethanolic bark extract for α-amylase inhibitory activity and standardization of the Terminalia arjuna for polyphenolic phytochemicals using high-performance liquid chromatography-photo diode array (HPLC-PDA) method.Methods: The T. arjuna bark sample was extracted with ethanol: water (70:30 v/v) using Soxhlet extraction. A Dionex P680 HPLC system was used to acquire chromatograms. The screening of extract of T. arjuna bark has performed for in vitro α-amylase inhibitory assay. Each experiment was repeated 3 times. All values were expressed mean ± standard deviation.Results: The content of arjunetin, arjungenin, gallic acid, ellagic acid, and quercetin was 0.47, 8.22, 2.443, 7.901, and 3.20 mg/g, respectively, in a hydroethanolic extract of T. arjuna. The hydroethanolic extract of T. arjuna bark and acarbose has shown an inhibitory activity with an IC50 value 145.90 and 62.35 μg/mL, respectively.Conclusion: The hydroethanolic extract T. arjuna bark demonstrates α-amylase inhibitory activity due to a synergistic effect of the phytochemical constituents present in it. This study suggests that one of the mechanisms of this plant for antidiabetic activity is through the inhibition of α-amylase enzyme.


Author(s):  
Kumari Smita

Objective: The present investigation was designed to study the inhibitory effects of methanolic leaf extract of Ocimum canum (O. canum) on α-glucosidase using in vitro model followed by an assessment of bioactive compounds.Methods: The methanolic leaf extract was prepared by Soxhlet extraction method and partially purified by thin layer chromatography (TLC). Each band was subjected to α-glucosidase inhibition study. The positive bands were further characterized by high-performance liquid chromatography (HPLC) and quadrupole time of flight (Q-TOF) micro mass spectrometer.Results: Out of the several combinations of solvent systems, toluene, ethyl acetate and formic acid combination in the ratio of 7:2:1 revealed 5 bands on the TLC sheet. Among all the TLC bands, 2 bands (band A and B) showed the significant inhibitory effect on α-glucosidase activity. HPLC analysis of band A and B revealed the presence of two important polyphenolic compounds, namely rosmarinic acid (RA) and ursolic acid (UA). Q-TOF micromass spectrometer analysis revealed the percentage availability of RA, caffeic acid, tartaric acid, quercetin and other polyphenolic components in the bioactive bands.Conclusion: The study revealed that methanolic leaf extract of O. canum exhibits potent inhibition of α-glucosidase activity. Inhibition of α-glucosidase activity might be attributed to the presence of the polyphenolic compounds like RA and UA. Therefore, this finding can lead to the development of natural α-glucosidase inhibitors by the O. canum leaf extract.


Author(s):  
Krishn Kumar Agrawal ◽  
Nitin Agrawal ◽  
Nidhi Jadon ◽  
Kuldeep Gangwar ◽  
Swarnim Jain ◽  
...  

Objective: The study was planned to investigate the extractive value and in-vitro anti-urolithiatic activity of different extracts of Embelia ribes Burn. F. and Ipomea hederacea Jacq seeds. Methods: Phytochemical analysis was undertaken to evaluate the phyto-constituents present in different extracts. The extracts were prepared by the maceration process. The in-vitro anti-urolithiatic activity was performed by dissolution and turbidity methods. Result: The extractive value of chloroform, ethanol, diethyl ether, n-hexane, acetone and water of Embelia ribes and Ipomea hederacea was found to be 2%, 2.5%, 2.5%, 2%, 1.5%, 1%w/w and 1.5%, 2%, 2.4%, 14%, 2%, 6% w/w respectively. The result of phytochemical analysis showed that aqueous, ethanolic, chloroform, diethyl ether, n-hexane and acetone extract of Embelia ribes and Ipomea hederacea have positive for alkaloids, proteins, carbohydrates, amino acids, tannins, protein, mucilage and glycoside. Moreover the result of anti-urolithiatic activity of ethanol and hexane extract of Embelia ribes and Ipomea hederacea were found to be 84.33±0.67%, 76.67±0.67%, 72.33±0.88 NTU and 73.00±1.15 NTU by dissolution and turbidity methods respectively. Conclusion: On the basis of result analysis, we can conclude that both the plants extract have anti-urolithiatic activity but ethanol and hexane extract have much significant activity than other extracts when compared to standard cystone.


2019 ◽  
Vol 50 (4) ◽  
pp. 631-640
Author(s):  
Kholowd AlKhaldi ◽  
Manal Daghestani ◽  
Thanaa Al-Haddad

Purpose The purpose of this paper is to evaluate the inhibition activity of Tribulus terrestris L. (T. terrestris) fruits extracts with solvents of increasing polarity against α-glucosidase and α-amylase, and to determine the inhibition mode of the most effective extract against both enzymes. Design/methodology/approach Hexane, acetone, ethanol and aqueous extracts of T. terrestris fruits were prepared using ultrasonic sequential extraction and analyzed for their α-amylase and α-glucosidase inhibitory activities by specific assay for each enzyme. The modes of inhibitions were detected using Lineweaver–Burk plots. Findings T. terrestris fruits extracts showed inhibition activity against α-glucosidase and α-amylase which was in the dose-dependent manner. Hexane extract had the highest α-glucosidase inhibition activity (IC50 = 27.28 μg/ml, p = 0.003), followed by acetone and ethanol extracts (IC50 = 60.58 μg/ml and IC50 = 84.21 μg/ml, respectively). The inhibition mode of hexane extract was noncompetitive. While acetone extract showed the highest inhibition activity against α-amylase (IC50 = 6.18 mg/ml, p = 0.002), hexane and ethanol extracts showed no significant difference (IC50 = 13.04 mg/ml and IC50 = 14.20 mg/ml, respectively, p = 0.09). The inhibition mode of acetone extract was competitive. Originality/value T. terrestris fruits extracts had strong inhibition activity against α-glucosidase and α-amylase, and they can be used as a promising anti-diabetic agent.


2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Subramaniam Ramachandran ◽  
Aiyalu Rajasekaran ◽  
Natarajan Adhirajan

The present study was aimed to investigate in vivo, in vitro antidiabetic activity of aqueous extract of Terminalia paniculata bark (AETPB) and characterize its possible phytoconstituents responsible for the actions. Type 2 diabetes was induced in rats by streptozotocin-nicotinamide (65 mg/kg–110 mg/kg; i.p.) administration. Oral treatment of AETPB using rat oral needle at 100 and 200 mg/kg doses significantly () decreased blood glucose and glycosylated haemoglobin levels in diabetic rats than diabetic control rats. AETPB-treated diabetic rats body weight, total protein, insulin, and haemoglobin levels were increased significantly () than diabetic control rats. A significant () reduction of total cholesterol and triglycerides and increase in high-density lipoprotein levels were observed in type 2 diabetic rats after AETPB administration. Presence of biomarkers gallic acid, ellagic acid, catechin, and epicatechin in AETPB was confirmed in HPLC analysis. AETPB and gallic acid showed significant () enhancement of glucose uptake action in presence of insulin in muscle cells than vehicle control. Also AETPB inhibited pancreatic α-amylase and α-glucosidase enzymes. In conclusion, the above actions might be responsible for the antidiabetic activity of AETPB due to presence of gallic acid and other biomarkers.


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