scholarly journals Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4175 ◽  
Author(s):  
Acharya Balkrishna ◽  
Subarna Pokhrel ◽  
Meenu Tomer ◽  
Sudeep Verma ◽  
Ajay Kumar ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
Computational Study ◽  
Synergistic Effects ◽  
Tinospora Cordifolia ◽  
Herbal Extracts ◽  
Ache Inhibition ◽  
Product Release ◽  
Methanolic Extracts ◽  
Common Strategy

Alzheimer’s disease (AD), a neurodegenerative disease, is the most common form of dementia. Inhibition of acetylcholinesterase (AChE) is a common strategy for the treatment of AD. In this study, aqueous, hydro-methanolic, and methanolic extracts of five potent herbal extracts were tested for their in vitro anti-AChE activity. Among all, the Tinospora cordifolia (Giloy) methanolic fraction performed better with an IC50 of 202.64 µg/mL. Of the HPLC analyzed components of T. cordifolia (methanolic extract), palmatine and berberine performed better (IC50 0.66 and 0.94 µg/mL, respectively) as compared to gallic acid and the tool compound “galantamine hydrobromide” (IC50 7.89 and 1.45 µg/mL, respectively). Mode of inhibition of palmatine and berberine was non-competitive, while the mode was competitive for the tool compound. Combinations of individual alkaloids palmatine and berberine resulted in a synergistic effect for AChE inhibition. Therefore, the AChE inhibition by the methanolic extract of T. cordifolia was probably due to the synergism of the isoquinoline alkaloids. Upon molecular docking, it was observed that palmatine and berberine preferred the peripheral anionic site (PAS) of AChE, with π-interactions to PAS residue Trp286, indicating that it may hinder the substrate binding by partially blocking the entrance of the gorge of the active site or the product release.

Phenolic constituents and inhibitory effects of the leaf of Rauvolfia vomitoria Afzel on free radicals, cholinergic and monoaminergic enzymes in rat’s brain in vitro

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Olubukola H. Oyeniran ◽  
Adedayo O. Ademiluyi ◽  
Ganiyu Oboh
Keyword(s):  
Lipid Peroxidation ◽  
Free Radicals ◽  
Methanolic Extract ◽  
Array Detector ◽  
Oh Radicals ◽  
Inhibitory Effects ◽  
Methanolic Extracts ◽  
Phenolic Constituents ◽  
Rauvolfia Vomitoria

AbstractObjectivesRauvolfia vomitoria is a medicinal plant used traditionally in Africa in the management of several human diseases including psychosis. However, there is inadequate scientific information on the potency of the phenolic constituents of R. vomitoria leaf in the management of neurodegeneration. Therefore, this study characterized the phenolic constituents and investigated the effects of aqueous and methanolic extracts of R. vomitoria leaf on free radicals, Fe2+-induced lipid peroxidation, and critical enzymes linked to neurodegeneration in rat’s brain in vitro.MethodsThe polyphenols were evaluated by characterizing phenolic constituents using high-performance liquid chromatography coupled with diode array detector (HPLC-DAD). The antioxidant properties were assessed through the extracts ability to reduce Fe3+ to Fe2+; inhibit ABTS, DPPH, and OH radicals and Fe2+-induced lipid peroxidation. The effects of the extracts on AChE and MAO were also evaluated.ResultsThe phenolic characterization of R. vomitoria leaf revealed that there were more flavonoids present. Both aqueous and methanolic extracts of R. vomitoria leaf had inhibitory effects with the methanolic extract having higher significant (p≤0.05) free radicals scavenging ability coupled with inhibition of monoamine oxidases. However, there was no significant (p≤0.05) difference obtained in the inhibition of lipid peroxidation and cholinesterases.ConclusionThis study suggests that the rich phenolic constituents of R. vomitoria leaf might contribute to the observed antioxidative and neuroprotective effects. The methanolic extract was more potent than the aqueous extract; therefore, extraction of R. vomitoria leaf with methanol could offer better health-promoting effects in neurodegenerative condition.

scholarly journals Mammalian Arginase Inhibitory Activity of Methanolic Extracts and Isolated Compounds from Cyperus Species

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1694
Author(s):  
Kamel Arraki ◽  
Perle Totoson ◽  
Alain Decendit ◽  
Andy Zedet ◽  
Justine Maroilley ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Significant Inhibition ◽  
Isolation And Identification ◽  
Vasorelaxant Effect ◽  
Methanolic Extracts ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.

Anti-Candida Activity of Pomegranate Peel Extract in Comparison with Curcumin Extract and their Synergism with Fluconazole and Nystatin

2021 ◽  
Vol 30 (2) ◽  
pp. 81-87
Author(s):  
Sara Y. Maxwell ◽  
Sally Elnawasany ◽  
Azza M. Hassan ◽  
Marwa M. E. Abd-Elmonsef
Keyword(s):  
Candida Species ◽  
Synergistic Effects ◽  
Systemic Disease ◽  
Antifungal Drugs ◽  
Diffusion Method ◽  
Oropharyngeal Candidiasis ◽  
Pomegranate Peel ◽  
Methanolic Extracts ◽  
Pomegranate Peel Extract

Background: Oropharyngeal candidiasis is an important sign that may reflect a serious systemic disease, especially in immunocompromised patients who face the intolerable side effects of the available antifungal drugs. This necessitates the development of safe and effective natural components. Objectives: to evaluate the in vitro activities of both pomegranate peel and curcumin extracts and to compare them with nystatin and fluconazole drugs against Candida species. As far as we know, this is the first study comparing between the antifungal potency of both extracts. Methodology: Different Candida species were isolated from patients with oropharyngeal candidiasis. The antifungal activities of methanolic extracts of pomegranate peel and curcumin were tested by disc diffusion method. Both extracts were added to each of nystatin and fluconazole discs to measure their synergistic effects. Results: Highly significant synergism was detected between both extracts and each of antifungal drugs. Curcumin extract was more potent than pomegranate extract. Conclusion: When used in combination with nystatin and fluconazole, curcumin and pomegranate peel extracts are promising and effective anti-Candida agents.

scholarly journals Evaluation of In Vitro Antimicrobial and Anti-Inflammatory Potentials of Crude Methanolic Extracts of Excoecaria agallocha (Leaves)

2016 ◽  
Vol 5 ◽  
pp. 25-33
Author(s):  
Md. Abdur Rahman ◽  
Md. Saddam Hussain ◽  
Md. Shalahuddin Millat ◽  
Md. Mizanur Rahman Moghal
Keyword(s):  
Methanolic Extract ◽  
Salmonella Typhi ◽  
Diffusion Method ◽  
Hypotonic Solution ◽  
Gram Negative ◽  
Excoecaria Agallocha ◽  
Methanolic Extracts ◽  
Wide Range ◽  
Zones Of Inhibition

Excoecaria agallocha plant (Leaves) was analyzed to explore In Vitro antimicrobial and membrane stabilizing activities as a crude methanolic extract. Antimicrobial activity was performed against a wide range of Gram positive(+Ve) and Gram negative(-Ve) bacteria by using disc diffusion method and various methanolic extracts of leaves of E.agallocha was tested for determining membrane stabilizing activity at hypotonic solution and heat induce condition and standard acetyl salicylic acid (0.10 mg/mL) was employed as standard. the zones of inhibition created was found to be 1.3 cm at a concentration of 100 µL/ disc in case of Gram negative(-Ve) bacteria Salmonella typhi. The results obtained were compared with that of a standard Ampicillin (10 µL) and imipenem (10µL), penicillin (10µl), cefoxitine(30µl). Crude methanolic extract of 10mg/ml concentration showed maximum value of 17.67±0.0102 and 18.92±0.086% respectively under hypotonic solution and heat induced condition. Thus the result suggest that, crude methanolic extracts of E.agallocha possessed slight to moderate antimicrobial and membrane stabilizing properties.

scholarly journals Giloy (Tinospora Cordifolia): In Vitro Evaluation of Antibacterial Properties

2021 ◽  
Vol 07 (06) ◽  
Author(s):  
Tulsa Devi ◽  
Keyword(s):  
Antibacterial Activity ◽  
Methanolic Extract ◽  
Water Extract ◽  
Hot Water ◽  
Tinospora Cordifolia ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Hot Water Extract ◽  
Agar Well Diffusion Method

Antibiotic resistance has become a global concern and hence, the search for other source of antimicrobials initiated to find a way to control infections in future. The main objective of this paper is to screen Giloy (Tinospora cordifolia) for its antibacterial activity. The stem of Tinospora cordifolia is used to prepare extract for determining it’s in vitro antibacterial activity as per the agar well diffusion method. In the agar well diffusion method 100μl of 24 hr broth culture of bacteria was aseptically and evenly swabbed on Mueller Hinton agar plates. Wells of about 8 mm diameter were aseptically cut using sterile cork-borer. 100 μl of plant extracts of different concentrations were then placed into the separate wells. The plates were incubated at 37 oC for 24hr. Antimicrobial activity of the giloy was determined by measuring the diameter of zone of inhibition. The methanolic extract of Tinospora cordifolia showed 13, 11, 9 and 5 mm zone of inhibition in S. aureus cultures by using 100, 75, 50 and 25 mg/ml concentration, respectively while hot water extract of Tinospora cordifolia showed 14, 12, 10 and 8 mm zone of inhibition for S. aureus by using 100, 75, 50 and 25 mg/ml concentration, respectively and the cold extract of Tinospora cordifolia showed 10, 8, 5 and 0 mm zone of inhibition for S. aureus by using 100, 75, 50 and 25mg/ml concentration, respectively. The methanolic extract of Tinospora cordifolia indicated 12, 10, 6 and 4 mm zone of inhibition in cultures of E.coli by using 100, 75, 50 and 25 mg/ml concentration, respectively and the hot water extract of Tinospora cordifolia showed 16, 14, 12 and 10 mm zone of inhibition in cultures of E.coli by using 100, 75, 50 and 25mg/ml concentration, respectively. The cold water extract of Tinospora cordifolia showed 13, 10, 8, and 5 mm zone of inhibition in cultures of E.coli by using 100, 75, 50 and 25 mg/ml concentration, respectively. It has been observed that Tinospora cordifolia showed very promising results as indicated by the zone of inhibition of bacterial culture through agar well diffusion method that varies from few mm to few cm. This study indicates the in-vitro antibacterial effect of Giloy which needs further validation through in-vivo studies.

Antioxidant and cytotoxic activity of stems of Smilax zeylanica in vitro

2015 ◽  
Vol 26 (5) ◽  
Author(s):  
Mohammad Nasir Uddin ◽  
Taksim Ahmed ◽  
Sanzida Pathan ◽  
Md. Mamun Al-Amin ◽  
Md. Sohel Rana
Keyword(s):  
Petroleum Ether ◽  
Methanolic Extract ◽  
Antioxidant Properties ◽  
In Vitro Assays ◽  
Dpph Assay ◽  
Cytotoxic Potential ◽  
Phytochemical Study ◽  
Methanolic Extracts ◽  
Standard Procedures

AbstractPlant-derived phytochemicals consisting of phenols and flavonoids possess antioxidant properties, eventually rendering a lucrative tool to scavenge reactive oxygen species. This study was carried out to evaluate in vitro antioxidant and cytotoxic potential of methanolic extract and petroleum ether extracts ofPhytochemical screening was done following standard procedures. Antioxidant activity was tested using several in vitro assays, viz., 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, NO assay, HPreliminary phytochemical study revealed the presence of flavonoids and glycosides in both extracts. Methanolic extract was found to possess stronger antioxidant potential than petroleum ether extracts in all assays. The ICThese findings demonstrate that methanolic extracts could be considered as potential sources of natural antioxidant, whereas petroleum ether extracts could be explored for promising anticancer molecules.

scholarly journals Insecticidal Effects of Organotin(IV) Compounds on Plutella Xylostella (L.) Larvae. II. Inhibitory Potencies Against Acetylcholinesterase and Evidence for Synergism in Tests With Bacillus Thuringiensis(BER.) and Malathion

1994 ◽  
Vol 1 (1) ◽  
pp. 1-17 ◽  
Author(s):  
Nazni W. Ahmad ◽  
Tay Siew Huang ◽  
S. Balabaskaran ◽  
K. M. Lo ◽  
V. G. Kumar Das
Keyword(s):  
Bacillus Thuringiensis ◽  
Plutella Xylostella ◽  
Resistant Strain ◽  
Synergistic Effects ◽  
Diamondback Moth ◽  
Ache Inhibition ◽  
Microbial Insecticide ◽  
In Vitro Inhibition ◽  
Sublethal Concentrations

Features of pesticide synergism and acetylcholinesterase (AChE) inhibition (in vitro) were studied using a selected range of organotin compounds against the early 4th instar larvae of a highly resistant strain of the diamondback moth (DBM), Plutella xylostella, a major universal pest of cruciferous vegetables.Fourteen triorganotin compounds were evaluated for their ability to enhance the toxicity of the microbial insecticide, Bacillus thuringiensis (BT) and of the commercial insecticide, Malathion to Plutella xylostella larvae. Supplemental synergism was observed with triphenyl- and tricyclopentyltin hydroxides in combinations with Bacillus thuringiensis. Increased synergism was observed with an increase in the number of cyclopentyl groups on tin in the mixed series, CypnPh3-n SnX, where X = OH, and 1-(1,2,4-triazolyl). The combination of (p-chlorophenyl)diphenyltin N,N-dimethyldithiocarbamate at LD10 and LD25 concentrations with sublethal concentrations of Malathion as well as of tricyclohexyltin methanesulphonate at the 0.01% (w/v) concentration with Malathion exerted strong synergistic effects (supplemental synergism) with toxicity index (T.I) values of 7.2, 19.8 and 10.1, respectively.Studies on the in vitro inhibition of acetylcholinesterase prepared from the DBM larvae showed that while most of the triorganotin Compounds tested were without effect on the enzyme, compounds containing the thiocarbamylacetate or the dithiocarbamylacetate moieties demonstrated appreciable levels of inhibition, being comparable in efficacy to commercial grades of Malathion and Methomyl.

scholarly journals Immune-Stimulatory and Therapeutic Activity of Tinospora cordifolia: Double-Edged Sword against Salmonellosis

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Sultan Alsuhaibani ◽  
Masood A. Khan
Keyword(s):  
Antioxidant Enzymes ◽  
Bacterial Load ◽  
Tinospora Cordifolia ◽  
Liver Inflammation ◽  
Inflammation Markers ◽  
Methanolic Extracts ◽  
Cytokine Levels ◽  
Culture Supernatants ◽  
Broth Dilution

The present study was aimed at determining the activity of aqueous and methanolic extracts of Tinospora cordifolia (AETC and METC) against Salmonella typhimurium. In vitro anti-Salmonella activity of T. cordifolia was determined through the broth dilution and agar well diffusion assays. The immune-stimulating potential of AETC or METC was determined by measuring the cytokine levels in the culture supernatants of treated murine J774 macrophages. Antibacterial activity of AETC or METC was determined by treating S. typhimurium-infected macrophages and BALB/C mice. The toxicity of AETC or METC was determined by measuring the levels of liver inflammation markers aspartate transaminase (AST) and alanine transaminase (ALT) and antioxidant enzymes. Macrophages treated with AETC or METC secreted greater levels of IFN-γ, TNF-α, and IL-1β. METC showed greater activity against S. typhimurium infection in macrophages and mice as well. Treatment with METC resulted in increased survival and reduced bacterial load in S. typhimurium-infected mice. Moreover, METC or AETC treatment reduced the liver inflammation and rescued the levels of antioxidant enzymes in S. typhimurium-infected mice. The results of the present study suggest that the use of T. cordifolia may act as a double-edged sword in combating salmonellosis.

scholarly journals IN-VITRO ALPHA-AMYLASE AND ALPHA-GLUCOSIDASE INHIBITION ACTIVITY OF DECALEPIS HAMILTONII WIGHT AND ARN

2021 ◽  
pp. 1-3
Author(s):  
Srinivasan S ◽  
Rayar A
Keyword(s):  
Methanolic Extract ◽  
Biologically Active ◽  
Alpha Amylase ◽  
Postprandial Blood Glucose ◽  
Herbal Extracts ◽  
Inhibition Activity ◽  
H Nmr ◽  
Decalepis Hamiltonii ◽  
Alpha Glucosidase

Biologically active polyphenol, D-catechin was isolated from Decalepis hamiltonii and characterized by IR, 1 H- NMR 13C- NMR and evaluation of its in-vitro α-amylase and α-glucosidase inhibition activities. Bioactive compounds are deposited in many parts of the plants, such as in roots, stems, leaves, flowers, fruits and seeds. They protect the plants from diseases and contribute aroma, color and flavor. Inhibitors 𝛼 - amylase and 𝛼-glucosidase delay the breaking down of carbohydrates in the small intestine and lower the postprandial blood glucose excursion. Methanolic extract showed the greater % inhibition of the alpha glucosidase enzyme compared to D-catechin. The herbal extracts produced a slightly weak alpha glucosidase enzyme inhibition when compared with alpha amylase.

scholarly journals In vitro Activity of Ozoroa pulcherrima Schweinf. Extracts and Fractions on Schistosoma mansoni Cercariae and Adult Worms

2020 ◽  
pp. 17-30
Author(s):  
Nestor Gipwe Feussom ◽  
Hermine Boukeng Jatsa ◽  
Mérimé Christian Kenfack ◽  
Emilienne Tienga Nkondo ◽  
Ulrich Membe Femoe ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Methanolic Extract ◽  
Lower Abdominal Pain ◽  
In Vitro Assays ◽  
Dependent Manner ◽  
In Vitro Activity ◽  
Concentration Dependent Manner ◽  
Methanolic Extracts ◽  
Effective Drugs

Aims: Continuous attempts are being made to develop new and more effective drugs for the treatment of schistosomiasis. Ozoroa pulcherrima Schweinf. is a medicinal plant used in Africa for the treatment of dysmenorrhea, lower abdominal pain, dystocia and intestinal helminthiasis. This study provides findings on the cercaricidal and schistosomicidal activity of extracts and fractions of Ozoroa pulcherrima in in vitro assays. Methodology: The aqueous and methanolic extracts from Ozoroa pulcherrima root parts (62.5 – 2000 µg/mL), as well as the methanol derived fractions (n-hexane and ethyl acetate: 31.25 – 1000 µg/mL) were tested on cercariae and adult worms of Schistosoma mansoni. Niclosamide-olamine 5% (1 µg/mL) and praziquantel (10 µg/mL) were respectively used as reference drugs. During the assays, the mortality of cercariae after 2 hours, and adult worms’ mobility and mortality after 48 hours of incubation were evaluated. Results: Ozoroa pulcherrima extracts and fractions significantly increased cercariae and worm mortality in a concentration-dependent manner. The methanolic extract was the most active on cercariae with a LC50of 20.65 µg/mL after 30 minutes, while the n-hexane fraction was the most active on worm with a LC50 of 79.54 μg/mL (65.58 – 96.47 μg/mL) after 48 hours. Significant reduction of motor activity (18.47 to 100%) was recorded for surviving worms incubated in different concentrations of the extracts and fractions. Conclusion: This study proves that Ozoroa pulcherrima extracts and fractions have cercaricidal and schistosomicidal activities. Ozoroa pulcherrima may have great potential as an anti-schistosomal agent for further research.

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