scholarly journals Antiulcer Potential of Olea europea L. cv. Arbequina Leaf Extract Supported by Metabolic Profiling and Molecular Docking

Antioxidants ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 644
Author(s):  
Arafa Musa ◽  
Nourhan Hisham Shady ◽  
Shaimaa R. Ahmed ◽  
Taghreed S. Alnusaire ◽  
Ahmed M. Sayed ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Metabolic Profiling ◽  
Leaf Extract ◽  
Gastric Ulcers ◽  
Protective Mechanism ◽  
Potential Candidate ◽  
Alcoholic Extract ◽  
Gastric Mucosal Lesions ◽  
Olea Europea

Gastric ulceration is among the most serious humanpublic health problems. Olea europea L. cv. Arbequina is one of the numerous olive varieties which have scarcely been studied. The reported antioxidant and anti-inflammatory potential of the olive plant make it a potential prophylactic natural product against gastric ulcers. Consequently, the main goal of this study is to investigate the gastroprotective effect of Olea europea L. cv. Arbequina leaf extract. LC-HRMS-based metabolic profiling of the alcoholic extract of Olea europea L. cv. Arbequina led to the dereplication of 18 putative compounds (1–18). In vivo indomethacin-induced gastric ulcer in a rat model was established and the Olea europea extract was tested at a dose of 300 mg kg−1 compared to cimetidine (100 mg kg−1). The assessment of gastric mucosal lesions and histopathology of gastric tissue was done. It has been proved that Olea europea significantly decreased the ulcer index and protected the mucosa from lesions. The antioxidant potential of the extract was evaluated using three in vitro assays, H2O2 scavenging, xanthine oxidase inhibitory, and superoxide radical scavenging activities and showed promising activities. Moreover, an in silico based study was performed on the putatively dereplicated compounds, which highlighted that 3-hydroxy tyrosol (4) and oleacein (18) can target the 5-lipoxygenase enzyme (5-LOX) as a protective mechanism against the pathogenesis of ulceration. Upon experimental validation, both compounds 3-hydroxy tyrosol (HT) and oleacein (OC) (4 and 18, respectively) exhibited a significant in vitro 5-LOX inhibitory activity with IC50 values of 8.6 and 5.8 µg/mL, respectively. The present study suggested a possible implication of O. europea leaves as a potential candidate having gastroprotective, antioxidant, and 5-LOX inhibitory activity for the management of gastric ulcers.

scholarly journals Skrining Mekanisme Kerja Daun Malaka (Phyllanthus emblica L.) Sebagai Antidiabetes

2018 ◽  
Vol 1 (3) ◽  
pp. 106-110
Author(s):  
Novi Irwan Fauzi ◽  
Seno Aulia Ardiansyah ◽  
Saeful Hidayat
Keyword(s):  
Mechanism Of Action ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Test Method ◽  
Diabetic Rat ◽  
Phyllanthus Emblica ◽  
Insulin Sensitizer ◽  
Water Fraction

Daun malaka (Phyllanthus emblica L.) mempunyai potensi digunakan sebagai alternatif obat antidiabetes. Daun malaka menunjukkan efek hipoglikemia pada tikus yang diinduksi aloksan. Namun, mekanisme kerjanya belum diketahui pasti. Penelitian ini dilakukan dalam rangka skrining mekanisme kerja daun malaka sebagai antidiabetes. Skrining mekanisme kerja dilakukan terhadap fraksi air daun malaka melalui uji aktivitas inhibisi enzim α-glukosidase serta α-amilase secara in vitro dan pengujian aktivitas insulin-sensitizer terhadap ekstrak daun malaka dengan metode tes toleransi insulin secara in vivo. Fraksi air daun malaka menunjukkan aktivitas inhibisi terhadap enzim α-glukosidase serta α-amilase dengan nilai IC50 (Inhibitor Concentration 50) pada kedua enzim tersebut berturut-turut adalah 0,87% dan 8,64% b/v. Pada uji aktivitas insulin sensitizer, pemberian ekstrak daun malaka dapat meningkatkan sensitivitas insulin pada tikus diabet dengan kondisi resistensi insulin. Nilai KTTI pada kelompok tikus diabet yang diberi ekstrak daun malaka dosis 100 dan 500 mg/kgbb tikus (74,89 dan 75,57) lebih tinggi dibandingkan kelompok tikus diabet (38,41) dan kadar glukosa darah yang lebih rendah selama interval waktu pengukuran. Daun malaka telah diketahui mampu meningkatkan sekresi insulin dan pada penelitian ini menunjukkan aktivitas inhibisi enzim α-glukosidase serta α-amilase secara in vitro dan menunjukkan aktivitas insulinsensitizer pada tikus diabet dengan kondisi resistensi insulin.   Malaka leaf (Phyllanthus emblica L.) has the potential to be used as an alternative antidiabetic drug. Malacca leaves showed hypoglycemia effect in rat induced by alloxan. However, the mechanism of action is not yet known. This study was conducted to evaluate the mechanism of action of Malaka leaves as antidiabetic. Screening of the mechanism of action was carried out on the water fraction of Malaka leaf  byinhibitory activity examination  on α-glucosidase and α-amylase by in vitro studyand Evaluation of insulin-sensitizer activity of Maaka leaf leaf extract was conducted by invivo  insulin tolerance test method. Malaka leaf water fraction showed inhibitory activity against the α-glucosidase and α-amylase with IC50 values ​​(Inhibitory Concentration 50)  of0.87% and 8.64% b / v on both enzyme, respectively. The evaluation of insulin sensitizer revelead that administration ofMalaka  leaf extract can increase insulin sensitivity in diabetic rat with insulin resistance.KTTI values ​​in diabetic rats given malaka extract  at the dose of 100 and 500 mg / kg BW (74.89 and 75.57) were higher than diabetics rat (38.41) and the extract also decrease blood glucose levels during measurement time intervals . Malaka leafhas been known to increase insulin secretion and the study showedthe  inhibitory activity on α-glucosidase and α-amylase by in vitro study and showed insulinsensitizer activity in diabetic rat with insulin resistance.

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 Phenolic Acids from Lycium barbarum Leaves: In Vitro and In Silico Studies of the Inhibitory Activity against Porcine Pancreatic α-Amylase

Processes ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 1388
Author(s):  
Luna Pollini ◽  
Alessandra Riccio ◽  
Cristina Juan ◽  
Carmela Tringaniello ◽  
Federica Ianni ◽  
...  
Keyword(s):  
Phenolic Acids ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Lycium Barbarum ◽  
Plant Materials ◽  
Vitro Assay ◽  
In Silico Studies

Nowadays, bioactive compounds from vegetable food and waste are of great interest for their inhibitory potential against digestive enzymes. In the present study, the inhibitory activity of methanolic extract from Lycium barbarum leaves on porcine pancreas α-amylase has been studied. The α-amylase inhibitory activity of the constituent phenolic acids was also investigated. The leaves were extracted by ultrasound-assisted method, one of the most efficient techniques for bioactive extraction from plant materials, and then the phenolic acids were identified by Accurate-Mass Quadrupole Time-of-Flight (Q-TOF) Liquid Chromatography/Mass Spectrometry (LC/MS). Chlorogenic and salicylic acids were the most abundant phenolic acids in L. barbarum leaf extract. The inhibitory effect against α-amylase, determined for individual compounds by in vitro assay, was higher for chlorogenic, salicylic, and caffeic acids. L. barbarum leaf extract showed an appreciable α-amylase inhibitory effect in a concentration-dependent manner. Docking studies of the considered phenolic acids into the active site of α-amylase suggested a conserved binding mode that is mainly stabilized through H-bonds and π-π stacking interactions.

scholarly journals Effect of Cuttlebone on Healing of Indomethacin-Induced Acute Gastric Mucosal Lesions in Rats

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Lifeng Qiu ◽  
Lingya Yao ◽  
Yanfei Fang ◽  
Lan Wang ◽  
Meng Xue ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Gastric Ulcers ◽  
Potential Candidate ◽  
Dependent Manner ◽  
Gastric Lesions ◽  
Gastric Mucosal Lesions ◽  
Antioxidant Parameters ◽  
Epidermal Growth ◽  
Mucosal Lesions ◽  
Underlying Mechanisms

The continuing use of nonsteroidal anti-inflammatory drugs (NSAIDs) usually increases the side effects such as peptic ulcer and acute gastric lesions in the gastrointestinal tract. Cuttlebone (CB), isolated from Sepiella maindroni de Rochebrune, was reported to have antioxidant activities, but its role in the treatment of indomethacin-induced gastric lesions has not yet been confirmed. In this research, we investigate the protective effect of cuttlebone on indomethacin-related ulcers in rats and possible mechanisms. Here, gastric ulcers were induced by oral administration of indomethacin, and then the rats were treated with omeprazole (4 mg/kg) or different doses (750, 1500, and 3000 mg/kg of body weight) of cuttlebone. We evaluated lesion index, inflammation score, and a series of oxidant/antioxidant parameters. The data demonstrated that cuttlebone could protect against gastric ulcers induced by indomethacin in a dose-dependent manner (positive correlation). Also, these effects were associated with attenuating the expression of malonaldehyde (MDA) and increasing the levels of some protective ingredients like epidermal growth factor (EGF), prostaglandin E2 (PGE2), and superoxide dismutase (SOD). Thus, considering its ability to protect indomethacin-induced acute gastric mucosal lesions and the underlying mechanisms, CB might be a potential candidate for treating gastric damage caused by NSAIDs.

scholarly journals IN VITRO AND IN SILICO EVALUATION OF XANTHINE OXIDASE INHIBITORY ACTIVITY OF QUERCETIN CONTAINED IN SONCHUS ARVENSIS LEAF EXTRACT

2017 ◽  
Vol 10 (14) ◽  
pp. 50
Author(s):  
Rini Hendriani ◽  
Nursamsiar Nursamsiar ◽  
Ami Tjitraresmi
Keyword(s):  
Free Energy ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
In Silico ◽  
Leaf Extract ◽  
Binding Free Energy ◽  
Uv Spectrophotometry ◽  
Docking Simulations ◽  
Oxidase Enzyme

Objective: The aim of the present study was to examine the inhibiting effects of quercetin contained in Sonchusarvensis leaf extract on the activity of xanthine oxidase, an essential enzyme for uric acid synthesis.Methods: Activity test was conducted in vitro by measuring the activity of xanthine oxidase using UV spectrophotometry and in silico by determining the interaction of quercetin and allopurinol (as comparation drug) with xanthine oxidase enzyme in terms of hydrogen bonds and binding free energy. Docking simulations were performed by Autodock4.2 package.Results: The active fraction, using the solvent n-hexane, ethyl acetate and water, tested the inhibitory activity of the xanthine oxidase enzyme in vitro obtained respectively IC50 of 263.19, 16.20 and 141.80 μg/ml. Isolates with highest activity identified as quercetin. The xanthine oxidase enzyme inhibitory activity insilico by molecular docking showed quercetin has free energy binding ˗7.71 kcal/mol, more negative than that of allopurinol ˗5.63 kcal/mol.Conclusion: This shows the affinity of quercetin stronger than that of allopurinol; so that it can be predicted that quercetin was more potential to inhibit xanthine oxidase enzyme activity. Thus the extract of the S. arvensis leaves containing the active compound quercetin was a potential use as antihyperuricemia.  

scholarly journals Comparative Study of Xanthine Oxidase Inhibitory Activity Of Methanolic Leaf Extracts Of CalophyllumBlancoi (Bitaog), Diospyrospilosanthera (Bolongeta) and SyzygiumCumini (Duhat)

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 531-537
Author(s):  
Jan Asuncion ◽  
Mariane May Domingo ◽  
Rave Harvey Sienna ◽  
ZhaineMarille Villa ◽  
Jennifer Anne Loyola
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Leaf Extracts ◽  
Standard Drug ◽  
Ic50 Value ◽  
Vitro Analysis ◽  
In Vitro Analysis

Gout is characterized as an inflammation and warmth in the joints. It is associated with hyperuricemia wherein an upregulation of xanthine oxidase in purine degradation leads to increased levels of uric acid in the blood. Gout is not fatal. However, it affects one’s quality of life. Thus, this research primarily focuses in determining the inhibitory activity of xanthine oxidase in the methanolic leaf extract of bitaog (Calophyllumblancoi), bolongeta (Diospyrospilosanthera), and duhat (Syzygiumcumini) in gout. A quantitative-experimental research method was used in the study and the data were obtained by measuring the percent inhibition of the samples using UV-Vis spectrophotometer at 290 nm. The results showed that the methanolic leaf extract of above stated plants exhibited exemplary inhibition in comparison with the standard drug, allopurinol. The IC50  value determines the ability of the inhibitor to decrease the biotransformation of a substrate. The principle behind IC50 is, the lower the value the higher the inhibition. The bitaog (Calophyllumblancoi) trials have the lowest IC50 value with an average of 124.3 after the standard drug, followed by bolongeta (Diospyrospilosanthera) have an average of 155.3 IC50 value. Then duhat (Syzygiumcumini) showed the highest IC50 an average of 208.8. The bitaog (Calophyllumblancoi), next to allopurinol, showed the highest inhibition among all the extracts followed by the bolongeta (Diospyrospilosanthera). The least inhibitory activity was observed in duhat (Syzygiumcumini). Hence, it can be concluded that bitaog (Calophyllumblancoi), bolongeta (Diospyrospilosanthera), and duhat (Syzygiumcumini) can inhibit xanthine oxidase using in vitro analysis.

scholarly journals In vitro growth-inhibitory activity of Calophyllum inophyllum ethanol leaf extract against diarrhoea-causing bacteria

2017 ◽  
Vol 16 (9) ◽  
pp. 2207
Author(s):  
Tomas Kudera ◽  
Johana Rondevaldova ◽  
Rashmi Kant ◽  
Mohammed Umar ◽  
Eva Skrivanova ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Leaf Extract ◽  
Calophyllum Inophyllum ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

scholarly journals Gastro-Protective Effects of Albizia anthelmintica Leaf Extract on Indomethacin-Induced Gastric Ulcer in Wistar Rats: In Silico and In Vivo Studies

Antioxidants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 176
Author(s):  
Mohamed Nabil ◽  
Mohamed A. El Raey ◽  
Walied Abdo ◽  
Mohamed A. O. Abdelfattah ◽  
Assem M. El-Shazly ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
In Vivo Studies ◽  
Gastric Ulcers ◽  
Potential Candidate ◽  
Protective Effects ◽  
Ulcer Model ◽  
Anti Inflammatory

We have previously reported that the leaf extract of Albizia anthelmintica exhibited substantial antioxidant, anti-inflammatory, analgesic, and antipyretic properties in vivo. We also comprehensively characterized the active phytoconstituents and found several flavonoids and galloyl glucosides derivatives. In the current work, we explored the gastroprotective effects of the leaf extract in an indomethacin-induced ulcer model and the mechanisms involved. The rats being pretreated with the tested extract (100 and 200 mg kg−1) significantly prevented gastric lesions by 87.4% and 92.3%, respectively, and they had no structural derangements in the gastric mucosa. The extract significantly reduced the elevated levels of IKκB, NF-κB, TNF-α, IL-6, iNOS, and lipid peroxidation; increased the reduced level of glutathione peroxidase (GPx) activity; and reduced glutathione (GSH) in the indomethacin-induced ulcer model. The protective activities of the extract were similar in most aspects to those exerted by the known anti-ulcer drug famotidine. These activities might be attributed to the anti-inflammatory and antioxidant activities, and the reduction of iNOS levels. In conclusion, Albizia anthelmintica is a potential candidate for management of gastric ulcers with antioxidant properties.

Cytoprotection by Propolis Ethanol Extract of Acute Absolute Ethanol-Induced Gastric Mucosal Lesions

2002 ◽  
Vol 30 (02n03) ◽  
pp. 245-254 ◽  
Author(s):  
Chi-Feng Liu ◽  
Chun-Ching Lin ◽  
Mei-Hsiu Lin ◽  
Yi-Shiu Lin ◽  
Song-Chow Lin
Keyword(s):  
Gastric Mucosa ◽  
Ethanol Extract ◽  
Absolute Ethanol ◽  
Protective Mechanism ◽  
Gastric Mucosal Lesion ◽  
Gastric Mucosal Lesions ◽  
Dose Dependent ◽  
Gross Examination

Acute p.o. administration of absolute ethanol (1.0 ml/kg) to fasted rats produced extensive necrosis of gastric mucosa. Pretreatment with p.o. administration of propolis ethanol extract (PEE) could effectively and dose-dependently prevent such necrosis. This protective effect is called "cytoprotection." The maximal cytoprotective effect against absolute ethanol (AE)-induced gastric mucosal lesion was observed 1 hour after PEE administration. A gross examination of the gastric mucosa showed a marked improvement in groups receiving PEE. In order to further investigate the gastric protective mechanism of PEE, lipid peroxidation (LPO) levels in vivo and in vitro were estimated. PEE exhibited dose-dependent superoxide scavenging activity and antioxidant effects on AE-induced LPO in rat gastric mucosal homogenates. It was concluded that the gastric protective mechanism of PEE was due, at least in part, to its ability to inhibit LPO, and hence indirectly protect the gastric mucosa from oxidative stress.

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