scholarly journals Inhibition of α-glucosidase, pancreatic lipase, and antioxidant property of Myrcia hatschbachiiD. Legrand containing gallic and ellagic acids

Author(s):  
Larissa Junqueira Gatto ◽  
◽  
Gustavo Rezende Bellei de Oliveira ◽  
Katlin Suellen Rech ◽  
Paula Francislaine Moura ◽  
...  

Several species of the Myrcia genus have been used in folk medicine to treat diabetes. Therefore, the aim of this work was to investigate the inhibitory activity of α-glucosidase and pancreatic lipase in the crude extract (EBF) and in the ethyl acetate fraction (FFA) of Myrcia hatschbachii, as well as to identify isolated phenolic compounds and to evaluate the antioxidant property and preliminary in vitro toxicity against Artemia salina. EBF (IC50: 3.21 μg/mL) and FFA (IC50: 1.14 μg/mL) showed inhibitory activity superior to acarbose (IC50: 193.65 μg/mL). In addition, they showed inhibitory effects of pancreatic lipase (IC50: 556.58 μg/mL for EBF and 532.68 μg/mL for FFA), antioxidant potential, absence of preliminary toxicity and presence of gallic andellagic acids in FFA. The relevant results in the inhibition of α-glucosidase and pancreatic lipase motivate new studies for the development of herbal medicines that assist in the treatment of diabetic patients.

2018 ◽  
Vol 10 (2) ◽  
pp. 81
Author(s):  
Pierre Alexandre Eric Djifaby SOMBIE ◽  
Rahman M HAFIZUR ◽  
Moussa COMPAORÉ ◽  
Martin KIENDREBEOGO ◽  
Muhammad Iqbal CHOUDHARY ◽  
...  

<p>The hypoglycemic activity of <em>Guiera senegalensis</em> used in Burkinabe folk medicine has been already reported. The aim of this study was to investigate the in <em>vitro</em> antidiabetic activity from galls of <em>G.senegalensis</em>. The extracts and methanol fractions from galls of <em>G. senegalensis</em> showed strong α-glucosidase inhibitory activity compared with acarbose. The ethyl acetate fraction from methanol extract (EA/ME) showed potent antiglycation activity in an <em>in vitro</em> assay system. The galls did not show inhibition activity against α-chymotrypsin. The α-glucosidase inhibitory activity along with its antiglycation activity may open a new perspective for the use of <em>G. senegalensis</em> for the diabetic subject. The data suggests that consumption of <em>G senegalensis</em> galls as an infusion or in food and pharmaceutical preparations may be useful for the management of diabetes and its complications.</p>


2015 ◽  
Vol 44 (2) ◽  
pp. 118-124 ◽  
Author(s):  
Gisely Naura Venâncio ◽  
Isis Costa Rodrigues ◽  
Tatiane Pereira de Souza ◽  
Raquel de Oliveira Marreiro ◽  
Maria Fulgência Costa Lima Bandeira ◽  
...  

Introduction Phytotherapy is the study of herbal medicines and their applicability to cure diseases in general, being a therapeutic method which can be used for the prevention and treatment of mouth diseases. Among the herbal studied, the Libidibia ferrea, known as jucá or ironwood, is widely used in folk medicine by presenting anti-inflammatory, analgesic, antimicrobial and antipyretic therapeutic properties. Objective To evaluate in vitro pharmacological stability of the Libidibia ferrea extract’s mouthwash (INPA - 228 022). Material and method It was held the mouthwash microbiological control by determining the total number of microorganisms and Salmonella sp, Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus; stability characteristics (color, odor, brightness and consistency), sedimentation test (centrifuge), the pH measurement (pH meter) and density evaluation (pycnometer) were analyzed. Result The mouthwash showed to be absent from microorganisms and no changes were observed in the organoleptics and sedimentation characteristics. The average pH values were 6.21, 6.15 and 5.85 at 0, 30 and 60 days, respectively, and 1.029, 1.033 and 1.035 g/ mL density values, respectively, without interfering with the final characteristic of the formulation. Conclusion The mouthwash presented pharmacological stability and quality conditions.


1997 ◽  
Vol 41 (7) ◽  
pp. 1500-1503 ◽  
Author(s):  
F F Franssen ◽  
L J Smeijsters ◽  
I Berger ◽  
B E Medinilla Aldana

We present an evaluation of the antiplasmodial and cytotoxic effects of four plants commonly used in Guatemalan folk medicine against malaria. Methanol extracts of Simarouba glauca D. C., Sansevieria guineensis Willd, Croton guatemalensis Lotsy, and Neurolaena lobata (L.)R.Br. significantly reduced parasitemias in Plasmodium berghei-infected mice. Dichloromethane fractions were screened for their cytotoxicities on Artemia salina (brine shrimp) larvae, and 50% inhibitory concentrations were determined for Plasmodium falciparum in in vitro cultures. Both chloroquine-susceptible and -resistant strains of P. falciparum were significantly inhibited by these extracts. Of all dichloromethane extracts, only the S. glauca cortex extract was considered to be toxic to nauplii of A. salina in the brine shrimp test.


INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 62-68
Author(s):  
S Mhatre ◽  
◽  
A. Bhagit ◽  
R. P Yadav

Pancreatic lipase inhibitory effect of some edible spices in light of percent inhibition, efficacy, reversibility/ irreversibility and effect of pH on inhibition is presented here. Lipase inhibitory activities of methanolic extracts of eighteen spices were evaluated. Extracts of Zanthoxylum armatum, Cinnamomum tamala, Syzygium aromaticum and Myristica fragrans were considered to be of high potency in synthetic substrate assay. Only Syzygium aromaticum showed high potency in natural substrate based lipase assay. Zanthoxylum armatum extract displayed lowest IC50 of 9.0 μg/mL. On dialysis, all extracts lost their lipase inhibitory activity indicating reversible nature of inhibition. pH significantly affected the performance of spice extracts during inhibition of pancreatic lipase. Most of the extracts lost their pancreatic lipase inhibitory activity at pH 3.0 with the exception of Brassica nigra and Cinnamomum tamala. Results showed spice are good source of pancreatic lipase inhibitor and its potential as drug for obesity can be explored by addressing various issues.


2017 ◽  
Vol 12 (4) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Maria Angélica Recalde-Gil ◽  
Luiz Carlos Klein-Júnior ◽  
Carolina dos Santos Passos ◽  
Juliana Salton ◽  
Sérgio Augusto de Loreto Bordignon ◽  
...  

Garcinia gardneriana is chemically characterized by the presence of biflavonoids. Taking into account that flavonoids are able to inhibit monoamine oxidase (MAO) activity, in the present study, the chemical composition of the branches’ extract of the plant is described for the first time and the MAO inhibitory activity of the isolated biflavonoids was evaluated. Based on spectroscopic and spectrometric data, it was possible to identify volkesiflavone, morelloflavone (1), Gb-2a (2) and Gb-2a-7- O-glucoside (3) in the ethyl acetate fraction from ethanol extract of the branches. Compounds 1-3 were evaluated in vitro and demonstrated the capacity to inhibit MAO-A activity with an IC50 ranging from 5.05 to 10.7 μM, and from 20.7 to 66.2 μM for MAO-B. These inhibitions corroborate with previous IC50 obtained for monomeric flavonoids, with a higher selectivity for MAO-A isoform. The obtained results indicate that biflavonoids might be promising structures for the identification of new MAO inhibitory compounds.


2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201
Author(s):  
Zhen-Tao Deng ◽  
Tong-Hua Yang ◽  
Xiao-Yan Huang ◽  
Xing-Long Chen ◽  
Jian-Gang Zhang ◽  
...  

Diospyros dumetorum is an important folk medicine for treating pulmonary abscess and inflammation. The leaves of D. dumetorum revealed xanthine oxidase (XOD) inhibitory activity. With the guidance of UFLC-MS-IT-TOF analyses combined with bioassay in vitro, 15 flavonoids were isolated from the active parts of D. dumetorum. Except for 11 (IC50 > 200μM), all compounds showed obvious XOD inhibitory activity with IC50 values of 32.5 ± 0.7 ~ 145.0 ± 3.3 μM. The preliminary structure-activity relationships study suggested that glycosylation on C-3 was unfavorable for XOD inhibitory activity; hydroxyl groups on ring B were essential for maintaining activity; the activity was closely related with the position of galloylation. This is the first recognition of the XOD inhibitory activity and active constituents of D. dumetorum, and will provide valuable information for this plant as a new resource for treating hyperuricemia and gout.


Foods ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 844
Author(s):  
Razia Sultana ◽  
Adeola M. Alashi ◽  
Khaleda Islam ◽  
Md Saifullah ◽  
C. Emdad Haque ◽  
...  

The aim of the study was to determine the in vitro enzyme inhibition activities of aqueous polyphenolic extracts of nine popular Bangladeshi vegetables, namely ash gourd, bitter gourd, brinjal, Indian spinach, kangkong, okra, ridge gourd, snake gourd, and stem amaranth. Polyphenolic glycosides were the major compounds present in the extracts. Inhibition of α-amylase (up to 100% at 1 mg/mL) was stronger than α-glucosidase inhibition (up to 70.78% at 10 mg/mL). The Indian spinach extract was the strongest inhibitor of pancreatic lipase activity (IC50 = 276.77 µg/mL), which was significantly better than that of orlistat (381.16 µg/mL), a drug. Ash gourd (76.51%), brinjal (72.48%), and snake gourd (66.82%) extracts were the most effective inhibitors of angiotensin-converting enzyme (ACE), an enzyme whose excessive activities have been associated with hypertension. Brinjal also had a significantly higher renin-inhibitory activity than the other vegetable extracts. We conclude that the vegetable extracts may have the ability to reduce enzyme activities that have been associated with hyperglycemia, hyperlipidemia, and hypertension.


Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4657
Author(s):  
Phuong Thuy Viet Nguyen ◽  
Han Ai Huynh ◽  
Dat Van Truong ◽  
Thanh-Dao Tran ◽  
Cam-Van Thi Vo

Inhibition of human pancreatic lipase, a crucial enzyme in dietary fat digestion and absorption, is a potent therapeutic approach for obesity treatment. In this study, human pancreatic lipase inhibitory activity of aurone derivatives was explored by molecular modeling approaches. The target protein was human pancreatic lipase (PDB ID: 1LPB). The 3D structures of 82 published bioactive aurone derivatives were docked successfully into the protein catalytic active site, using AutoDock Vina 1.5.7.rc1. Of them, 62 compounds interacted with the key residues of catalytic trial Ser152-Asp176-His263. The top hit compound (A14), with a docking score of −10.6 kcal⋅mol−1, was subsequently submitted to molecular dynamics simulations, using GROMACS 2018.01. Molecular dynamics simulation results showed that A14 formed a stable complex with 1LPB protein via hydrogen bonds with important residues in regulating enzyme activity (Ser152 and Phe77). Compound A14 showed high potency for further studies, such as the synthesis, in vitro and in vivo tests for pancreatic lipase inhibitory activity.


2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Abdur Rauf ◽  
Muhammad Saleem ◽  
Ghias Uddin ◽  
Bina S. Siddiqui ◽  
Haroon Khan ◽  
...  

Pistacia integerrimais one of twenty species among the genusPistacia. Long horn-shaped galls that develop on this plant are harvested and used in Ayurveda and Indian traditional medicine to make “karkatshringi”, a herbal medicine used for the treatment of asthma and different disorders of respiratory tract. However, until now, the molecular mechanisms of action of “karkatshringi” and its chemical characterization are partially known. This study deals with the isolation and characterization of the active constituents from the methanolic extract ofP. integerrimagalls and it was also oriented to evaluatein vitroandin silicotheir potential enzymatic inhibitory activity against phosphodiesterase-1 (PDE1), a well-known enzyme involved in airway smooth muscle activity and airway inflammation. Our results showed that the methanolic extract ofP. integerrimagalls and some of its active constituents [naringenin (1) and 3,5,7,4′-tetrahydroxy-flavanone (2)] are ablein vitroto inhibit PDE1 activity (59.20 ± 4.95%, 75.90 ± 5.90%, and 65.25 ± 5.25%, resp.) and demonstratein silicoan interesting interaction with this enzymatic site. Taken together, our results add new knowledge of chemical constituents responsible for the biological activity ofP. integerrimaand contextually legitimate the use of this plant in folk medicine.


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