scholarly journals Selected Enzyme Inhibitory Effects of Euphorbia characias Extracts

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Antonella Fais ◽  
Benedetta Era ◽  
Amalia Di Petrillo ◽  
Sonia Floris ◽  
Dario Piano ◽  
...  
Keyword(s):  
Inhibitory Effects ◽  
Quercetin Derivatives ◽  
Plot Analysis ◽  
Euphorbia Characias ◽  
Ethanolic Extracts ◽  
Ethanol Extracts ◽  
Potential Inhibitors ◽  
Promising Source ◽  
Natural Inhibitors

Extracts of aerial part of Euphorbia characias were examined to check potential inhibitors for three selected enzymes involved in several metabolic disorders. Water and ethanol extracts from leaves and flowers showed in vitro inhibitory activity toward α-amylase, α-glucosidase, and xanthine oxidase. IC50 values were calculated for all the extracts and the ethanolic extracts were found to exert the best effect. In particular, for the α-glucosidase activity, the extracts resulted to be 100-fold more active than the standard inhibitor. The inhibition mode was investigated by Lineweaver-Burk plot analysis. E. characias extracts display different inhibition behaviors toward the three enzymes acting as uncompetitive, noncompetitive, and mixed-type inhibitors. Moreover, ethanolic extracts of E. characias showed no cytotoxic activity and exhibited antioxidant capacity in a cellular model. The LC-DAD metabolic profile was also performed and it showed that leaves and flowers extracts contain high levels of quercetin derivatives. The results suggest that E. characias could be a promising source of natural inhibitors of the enzymes involved in carbohydrate uptake disorders and oxidative stress.

scholarly journals In Vitro Anti-Inflammatory and In Vivo Antiarthritic Activities of Aqueous and Ethanolic Extracts of Dissotis thollonii Cogn. (Melastomataceae) in Rats

2019 ◽  
Vol 2019 ◽  
pp. 1-17 ◽  
Author(s):  
Stephanie Flore Djuichou Nguemnang ◽  
Eric Gonzal Tsafack ◽  
Marius Mbiantcha ◽  
Ateufack Gilbert ◽  
Albert Donatien Atsamo ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Protein Denaturation ◽  
Inflammatory Diseases ◽  
Ros Production ◽  
Zymosan A ◽  
Ethanolic Extracts ◽  
Anti Inflammatory ◽  
Promising Source

Dissotis thollonii Cogn. (Melastomataceae) is a tropical plant widely used in traditional Cameroonian medicine to relieve and treat many pathologies. It is widespread in the western region where it is used to treat typhoid fever, gastrointestinal disorders, and inflammatory diseases. The purpose of this study is to scientifically demonstrate the anti-inflammatory and antiarthritic properties of the aqueous and ethanolic extracts of the leaves of Dissotis thollonii. The anti-inflammatory properties were evaluated in vitro by inhibition tests for cyclooxygenase, 5-lipoxygenase, protein denaturation, extracellular ROS production, and cell proliferation; while antiarthritic properties were evaluated in vivo in rats using the zymosan A-induced monoarthritis test and the CFA-induced polyarthritis model. This study shows that aqueous and ethanolic extracts at a concentration of 1000 μg/ml inhibit the activity of cyclooxygenase (47.07% and 63.36%) and 5-lipoxygenase (66.79% and 77.7%) and protein denaturation (42.51% and 44.44%). Similarly, both extracts inhibited extracellular ROS production (IC50 = 5.74 μg/ml and 2.96 μg/ml for polymorphonuclear leukocytes, 7.47 μg/ml and 3.28 μg ml for peritoneal macrophages of mouse) and cell proliferation (IC50 = 16.89 μg/ml and 3.29 μg/ml). At a dose of 500 mg/kg, aqueous and ethanolic extracts significantly reduce edema induced by zymosan A (69.30% and 81.80%) and CFA (71.85% and 79.03%). At the same dose, both extracts decreased sensitivity to mechanical hyperalgesia with 69.00% and 70.35% inhibition, respectively. Systemic and histological analyzes show that both extracts maintain the studied parameters very close to normal and greatly restored the normal architecture of the joint in animals. Dissotis thollonii would therefore be a very promising source for the treatment of inflammatory diseases.

scholarly journals A New Strategy for Rapidly Screening Natural Inhibitors Targeting the PCSK9/LDLR Interaction In Vitro

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2397 ◽  
Author(s):  
Li Li ◽  
Chen Shen ◽  
Ya-Xuan Huang ◽  
Ya-Nan Li ◽  
Xiu-Feng Liu ◽  
...  
Keyword(s):  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Lipoprotein Receptor ◽  
Drug Candidates ◽  
Promising Target ◽  
New Strategy ◽  
Density Lipoprotein Receptor ◽  
Potential Inhibitors ◽  
Natural Inhibitors

The interaction between proprotein convertase subtilisin/kexin type 9 (PCSK9) and the low-density lipoprotein receptor (LDLR) is a promising target for the treatment of hyperc-holesterolemia. In this study, a new method based on competitive affinity and tag detection was developed, which aimed to evaluate potent natural inhibitors preventing the interaction of PCSK9/LDLR directly. Herein, natural compounds with efficacy in the treatment of hypercholesterolemia were chosen to investigate their inhibitory activities on the PCSK9/LDLR interaction. Two of them, polydatin (1) and tetrahydroxydiphenylethylene-2-O-glucoside (2), were identified as potential inhibitors for the PCSK9/LDLR interaction and were proven to prevent PCSK9-mediated LDLR degradation in HepG2 cells. The results suggested that this strategy could be applied for evaluating potential bioactive compounds inhibiting the interaction of PCSK9/LDLR and this strategy could accelerate the discovery of new drug candidates for the treatment of PCSK9-mediated hypercholesterolemia.

scholarly journals Antioxidant and antifungal activities in vitro of essential oils and extracts of twelve Algerian species of Thymus against some mycotoxigenic Aspergillus genera

2022 ◽  
Author(s):  
Yamina Ben Miri ◽  
Aldjia Taoudiat ◽  
Mohamed Mahdid
Keyword(s):  
Antifungal Activity ◽  
Essential Oils ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antifungal Activities ◽  
Minimum Fungicidal Concentration ◽  
Ethanolic Extracts ◽  
Ethanol Extracts ◽  
Phenolic And Flavonoid

The aim of the study was to determine the phenolic and flavonoid content of essential oils (EOs), chloroform and ethanolic extracts of 12 Algerian Thymus species and evaluate their antioxidant and antifungal activities. EOs (1.73 ± 0.30–15.00 ± 1.24 μg/mg), chloroform extracts (33.8 ± 2.42–160.93 ± 3.88 μg/mg) and ethanol extracts (27.01 ± 3.56 –148.46 ± 4.40 μg/mg) showed considerable phenolic content. Flavonoids values of chloroform extracts ranged between 3.39± 0.17 and 20.27 ± 0.29 μg/ml while ethanolic extracts values ranged between 2.81 ± 0.11 and 26.64 ± 0.18 μg/mg. Results of DPPH showed that EOs, chloroform and ethanolic extracts exhibited strong radical scavenging activity (IC50 = 21.75 ± 6.54–338.22 ± 2.99 μg/ml, 22.91 ± 5.59–90.93 ± 1.36 μg/ml, and 33.51 ± 5.72–103.80 ± 4.54 μg/ml, respectively). Inhibition of β-carotene bleaching was potentially performed by all EOs (66.48 ± 2.41–94.06 ± 2.68 %), chloroform extracts (68.98± 1.58–95.30± 1.99%), and ethanolic extracts (62.15 ± 2.51–92.36± 1.15%). The antifungal activity of EOs and extracts was tested using the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC). The EOs (0.1 ± 0.00 mg/ mL – 1.06 ± 0.46 mg/mL), chloroform (0.1 ± 0.00 mg/ mL –1.06 ± 0.46 mg/mL) and ethanol (0.1 ± 0.00 mg /mL–1.6 ± 0.00 mg/mL) showed remarkable antifungal activity against mycotoxigenic Aspergillus genera. The MFC of EOs (1.0 ± 0.34 mg/mL and > 4.8 mg/mL) , chloroform (0.26 ± 0.11 mg/mL and > 1.6 mg/mL) and ethanol (0.2 ± 0.00 mg/mL and > 1.6 mg/mL) were fungicidal in nature higher than MICs. The findings of the study indicated that Thymus spp. EOs and extracts could be used as natural alternatives for food industry.

scholarly journals Phytochemical analysis, Antioxidant and Antiprotoscolices potential of ethanol extracts of selected plants species against Echinococcus granulosus: In-vitro study

2019 ◽  
Vol 17 (1) ◽  
pp. 874-883 ◽  
Author(s):  
Sumbal Haleem ◽  
Sadaf Niaz ◽  
Naveeda Akhtar Qureshi ◽  
Riaz Ullah ◽  
Hafiz Majid Mahmood ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Echinococcus Granulosus ◽  
Parasitic Infection ◽  
In Vitro Study ◽  
Living Cells ◽  
Phytochemical Analysis ◽  
Hydatid Cysts ◽  
Ethanol Extracts ◽  
Promising Source

AbstractCystic Echinococossis is a serious zoonotic parasitic infection caused by Echinococcus granulosus species complex. The current study was designed to evaluate the in-vitro antiprotoscolices effect of alcoholic extracts of three selected medicinal plants including Buxus Wallichiana, Berberis vulgaris and Euphorbia heliscopia against Echinococcus granulosus. Fertile hydatid cysts were collected from livestock and viability of the protoscolices was confirmed by 0.1% eosin red stain method. Protoscolices were subjected to three different concentrations of alcoholic extracts (10mg/ml, 30mg/ ml and 50mg/ml) for 10, 20 and 30 min. The highest efficacy was shown by B. vulgaris (97.92%) followed by B. wallichiana (65.98%) and E. heliscopia (61.22%) respectively, after exposure of 30 minutes at 50mg/ml concentration, that lead to the significant reduction in the viability of protoscolices. Alkaloids, flavonoids, tannins and saponnins were identified qualitatively and weighted quantitatively, that might help in the identification of bioactive compounds involved in selective action on the tegument layer of protoscolices. Alcoholic extracts of all the three selected medicinal plants showed toxic activities against protoscolices of Echinococcus granulosus. These findings suggest that all the selected medicinal plants could be a promising source of potent antiprotoscolices effect. However, the mechanism by which plant extracts killed protoscolices and also their safety for living cells are unclear and need to be investigated further.

In vitro and in silico study of 1,3-oxazol-4-yltriphenylphosphonium salts as potential inhibitors of Candida albicans transglycosylase

2021 ◽  
Vol 16 (1) ◽  
pp. 25-33
Author(s):  
Ivan Semenyuta ◽  
Maria Trush ◽  
Diana Hodyna ◽  
Maryna Kachaeva ◽  
Larysa Metelytsia ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Amino Acid ◽  
Protein Complexes ◽  
Homology Model ◽  
Binding Energies ◽  
Amino Acid Residues ◽  
Plot Analysis ◽  
Potential Inhibitors ◽  
Dual Mechanism

The previously established in vitro high antimicrobial potential of triphenylphosphonium salts (TPPs) against bacterial (Staphylococcus aureus ATCC 25923 and multi-drug resistant (MDR)) and fungal (Candida albicans ATCC 10231 and MDR) strains made it possible to propose a molecular mechanism of action of these compounds associated with transglycosylase (TG) activity. The hypothesis was based on the well-known literature data on TPPs as inhibitors of S. aureus TG. The created homology model of TG C. albicans is optimal in terms of such quality indicators as GMQE (0.61), ERRAT (overall quality factor 95.904) and Ramachandran plot analysis (90% amino acid residues in the favored regions). Molecular docking of the most active ligands 1a-d, 3c into the active center of the created homology C. albicans TG model demonstrated the formation of stable ligand-protein complexes with binding energies in the range from -8.9 to -9.7 kcal/mol due to the various types of interactions. An important role in complex formation belongs to amino acid residues TYR307, TYR107, GLU275, ALA108 and PRO136. The presented qualitative homologous model of C. albicans TG can be used to search and create new agents with a dual mechanism of antimicrobial action. 1,3-oxazol-4-yltriphenylphosphonium salts 1a-d, 3c perform the perspective objects for further study as antimicrobials against infectious MDR pathogens.

scholarly journals Investigation of the Antiviral Activity of Experimental Samples Obtained from the Grass and Roots of Alchemilla vulgaris L. Against Vaccinia Virus and Ectromelia Virus

2019 ◽  
Vol 8 (4) ◽  
pp. 9-15
Author(s):  
N. A. Mazurkova ◽  
M. A. Protsenko ◽  
E. I. Filippova ◽  
T. A. Kukushkina ◽  
G. I. Vysochina ◽  
...  
Keyword(s):  
Cell Culture ◽  
Antiviral Activity ◽  
Ethyl Acetate ◽  
Vaccinia Virus ◽  
Smallpox Vaccination ◽  
Experimental Sample ◽  
Ectromelia Virus ◽  
Ethanol Extracts ◽  
Promising Source

Introduction. The abolition of smallpox vaccination after its elimination in 1980 led to a decrease in the immunocompromised immunity in humans. Zoonotic monkeypox, camelpox, buffalopox and cowpox viruses that are close to the variola virus also pose a danger to humans. In Russia today there are no effective and safe medicines for the prevention and treatment of smallpox and other orthopoxvirus infections in humans and animals. The Lady's mantle (Alchemilla vulgaris) is a promising source for the development of new antiviral drugs. Previous studies have found that Alchemilla vulgaris shows activity against influenza virus and herpes simplex virus.Aim. The aim of this work was to study the chemical composition and antiviral activity of extracts from the roots and the grass of Alchemilla vulgaris against orthopoxviruses.Materials and methods. Qualitative analysis of the samples was performed by high performance liquid chromatography. Quantitative analysis was performed using a complex of spectrophotometric methods. To determine the toxicity and antiviral activity of experimental samples from Alchemilla vulgaris in vitro, a transplantable Vero cell culture was used. Antiviral activity of the obtained preparations was evaluated by reducing the infectivity (titer) of orthopoxviruses in the monolayer of Vero cells infected with orthopoxviruses in the presence of preparations with different concentrations relative to the cell culture infected with orthopoxviruses without the preparations.Results and discussion. It was shown that the experimental sample from Alchemilla vulgaris obtained by the method of ethyl acetate extraction from the roots of the studied plant and purified with chloroform contains mainly catechins and leucoanthocyanins (70 %). In parallel, extract from the raw mass of the grass of the plant purified with chloroform and ethanol contains the amount of flavonoids (71 %). Wherein the content of flavonoids in unpurified ethanol extracts from the roots and the grass of Alchemilla vulgaris composed 5 % and 6 %, respectively. It was revealed that purified preparations obtained from Alchemilla vulgaris roots when using ethyl acetate and ethanol as extractants showed antiviral activity against vaccinia virus and ectromelia virus, as well as preparations obtained from grass by ethanol extraction.Conclusion. Thus, purified ethyl acetate extracts from the roots and ethanol extracts from the wet grass mass of Alchemilla vulgaris exhibit antiviral activity against orthopoxviruses in vitro.  

scholarly journals In vitro biological activity of ethanolic extracts from plants of the Meliaceae family on Diaphorina citri Kuwayama 1908 (Hemiptera: Liviidae)

2021 ◽  
Vol 6 (3) ◽  
pp. 19-35
Author(s):  
Victor Gabriel Almada-Ruiz ◽  
◽  
Gabriel Antonio Lugo-García ◽  
Laura Delia Ortega-Arenas ◽  
Edgar Eduardo Mendoza-García ◽  
...  
Keyword(s):  
Integrated Management ◽  
Melia Azedarach ◽  
Diaphorina Citri ◽  
Murraya Paniculata ◽  
Ethanolic Extracts ◽  
Treated Leaf ◽  
Orange Leaf ◽  
Ethanol Extracts ◽  
Vitro Effect

In vitro effect of ethanolic extracts of Azadirachta indica seeds, Melia azedarach and Swietenia humilis (Meliaceae) were evaluated on the mortality, repellency and oviposition of Diaphorina citri (Hemiptera: Liviidae). Toxicity was determined by the placement of adults and nymphs on orange leaf discs (Citrus sinensis cv. Valencia) previously sprayed or immersed in the treatments. The repellency was estimated through an exposition of adults to the treated leaf, in an experimental arena for 24 h. In order to inhibit oviposition, Murraya paniculata sprouts sprinkled with 2.5 mL of solution were used. The ethanolic extracts from the three meliaceus showed toxicity on nymphs and adults; however, adults evidenced the toxic effect as of 100.0 mg/mL, while nymphs did at 4.10 mg/mL. With a repellent effect, the 100 mg/mL solution stands out, with 82 and 78% for A. indica and S. humilis, respectively; effect associated to the concentration and the time. The oviposition was affected by ethanolic extracts of S. humilis and A. indica at 100.0 mg/mL. It is inferred that the ethanol extracts from S. humilis and A. indica present potential to be considered in the development of alternatives for the integrated management of D. citri.

scholarly journals Comparative study of the in vitro phytochemicals and antimicrobial potential of six medicinal plants

F1000Research ◽  
2019 ◽  
Vol 8 ◽  
pp. 81
Author(s):  
Charles O. Nwonuma ◽  
Tabitha A. Adelani-Akande ◽  
Omorefosa O. Osemwegie ◽  
Abiola F. Olaniran ◽  
Toluwani A. Adeyemo
Keyword(s):  
Antimicrobial Activity ◽  
Medicinal Plants ◽  
Plant Parts ◽  
Medicinal Plant Extracts ◽  
Ethanolic Extracts ◽  
Percentage Yield ◽  
New Methodologies ◽  
Ethanol Extracts ◽  
Positive Controls

Background: This study sought to investigate the antimicrobial activity of six plants used in traditional medicine in Africa. Methods: The antimicrobial activity of the six medicinal plant extracts (aqueous and ethanol) were evaluated against Proteus mirabilis (ATCC 21784), Pseudomonas aeruginosa (ATCC27856) were Aspergillus fumigatus using the agar-well diffusion protocol. The activities of these extracts were compared with the positive controls chloramphenicol and griseofulvin. Similarly, the phytochemicals from the extracts were qualitatively assayed and their percentage yield calculated by standard methods. Results: The bacterial organisms used, P. mirabilis and P. aeruginosa, were slightly-to-highly susceptible to aqueous and ethanolic extracts from the various test plants, while A. fumigatus was insensitive to the treatments. The ethanolic extracts of the sampled plants showed superior inhibitory performance on the target bacteria to the aqueous extracts. Aqueous and ethanolic extracts of Aframomum melegueta, Moringa oleifera and Cola nitida showed inhibitory consistency against the target bacteria. Superior inhibitory activity was observed for ethanol extracts of A. melegueta seed and M. oleifera pod against P. mirabilis and P. aeruginosa. Variations in phytochemicals were noticed across solvents and plant parts for all plants. Phenols were detected in the aqueous and ethanolic extracts of C. nitida and Cola acuminate, but relatively appeared denser in extracts of A. melegueta seed and Chrysophyllum albidium fruits. The extracts of C. nitida, C. acuminate and A. melegueta tested positive for the presence of flavonoids, which were undetected in C. albidium and M. oleifera seed and pod extracts. None of the extracts showed the presence of every phytochemical assayed during the study. Conclusions: Extracts of the medicinal plants assessed in this study showed antibacterial potential. Developing new methodologies that preserve the bioactive potency of phyto-extracts for optimal microbicidal activity is promising for development of safe, non-reactive pharmaceuticals.

scholarly journals In Vitro Selective Antibacterial and Antiproliferative Effects of Ethanolic Extracts from Cambodian and Philippine Plants Used in Folk Medicine for Diarrhea Treatment

2021 ◽  
Vol 12 ◽  
Author(s):  
Tomas Kudera ◽  
Barbora Fiserova ◽  
Marie Korytakova ◽  
Ivo Doskocil ◽  
Hana Salmonova ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Pathogenic Bacteria ◽  
Folk Medicine ◽  
Intestinal Bacteria ◽  
Intestinal Cancer ◽  
Inhibitory Effects ◽  
Isolation And Identification ◽  
Broth Microdilution Method ◽  
Ethanolic Extracts

Bacterial diarrhea remains a global health problem, especially in developing tropical countries. Moreover, dysbiosis caused by diarrheagenic bacteria and inappropriate antimicrobial treatment has been associated with intestinal carcinogenesis. Despite the rich tradition of the use of herbs for the treatment of gastrointestinal disorders in Cambodian and Philippine folk medicine, many of them have not yet been systematically studied for their in vitro selective inhibitory effects on intestinal bacteria and cells. In the present study, in vitro inhibitory activities of 35 ethanolic extracts derived from 32 Cambodian and Philippine medicinal plants were determined by broth microdilution method against 12 pathogenic bacteria. Furthermore, cytotoxicity against intestinal cancer cells (Caco-2 and HT-29) using thiazolyl blue tetrazolium bromide cytotoxicity assay and safety to six beneficial intestinal bacteria (bifidobacteria and lactobacilli) and intestinal normal cells (FHs 74 Int) were determined for the antimicrobially active extracts. Selectivity indices (SIs) were calculated among the averages of minimum inhibitory concentrations (MICs), half-maximal inhibitory concentrations (IC50), and 80% inhibitory concentrations of proliferation (IC80) for each type of the tested agents. The extracts of Artocarpus blancoi (Elmer) Merr. (Moraceae), Ancistrocladus tectorius (Lour.) Merr. (Ancistrocladaceae), and Pentacme siamensis (Miq.) Kurz (Dipterocarpaceae) produced significant growth-inhibitory effects (MICs = 32–512 μg/ml) against intestinal pathogenic bacteria at the concentrations nontoxic to normal intestinal cells (IC80 values >512 μg/ml; SIs = 0.11–0.2). Moreover, the extract of P. siamensis (Miq.) Kurz was relatively safe to beneficial bacteria (MICs ≥512 μg/ml; SI = 0.1), and together with A. blancoi (Elmer) Merr., they selectively inhibited intestinal cancer cells (IC50 values ≥51.98 ± 19.79 μg/ml; SIs = 0.3 and 0.6). Finally, a strong selective antiproliferative effect on cancer cells (IC50 values 37.89 ± 2.68 to 130.89 ± 13.99 μg/ml; SIs = 0.5) was exerted by Ehretia microphylla Lam. (Boraginaceae), Lagerstroemia cochinchinensis Pierre ex Gagnep. (Lythraceae), and Melastoma saigonense (Kuntze) Merr. (Melastomataceae) (leaves with flower buds). The results suggest that the above-mentioned species are promising materials for the development of new selective antibacterial and antiproliferative agents for the treatment of infectious diarrhea and associated intestinal cancer diseases. However, further research is needed regarding the isolation and identification of their active constituents.

scholarly journals α-Glucosidase inhibitors: consistency of in silico docking data with in vitro inhibitory data and inhibitory effect prediction of quercetin derivatives

2019 ◽  
Vol 10 (10) ◽  
pp. 6312-6321 ◽  
Author(s):  
Jianzhong Zhu ◽  
Bin Zhang ◽  
Chinping Tan ◽  
Qiang Huang
Keyword(s):  
In Silico ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Quercetin Derivatives ◽  
In Silico Docking ◽  
Glucosidase Inhibitors ◽  
The Relationship

The relationship between in silico and in vitro experiments regarding the inhibitory effects of polyphenols on α-glucosidase was investigated.

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