scholarly journals Phytochemical screening, in vitro anti-oxidant activity, and in silico anti-diabetic activity of aqueous extracts of Ruellia tuberosa L

2020 ◽  
Vol 10 (3) ◽  
pp. 101-108 ◽  
Keyword(s):  
In Silico ◽  
Aqueous Extracts ◽  
Phytochemical Screening ◽  
Anti Oxidant ◽  
Screening In Vitro

α-Glucosidase Inhibition, Antioxidant and Docking Studies of Hydroxycoumarins and their Mono and Bis O-alkylated/acetylated Analogs

2018 ◽  
Vol 15 (2) ◽  
pp. 127-135 ◽  
Author(s):  
Parvesh Singh ◽  
Nomandla Ngcoya ◽  
Ramgopal Mopuri ◽  
Nagaraju Kerru ◽  
Neha Manhas ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Catalytic Site ◽  
Docking Simulations ◽  
In Silico Docking ◽  
Anti Oxidant

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g. anti-cancer, anti-HIV, anti-viral, anti-malarial, anti-microbial, anti-convulsant, anti-hypertensive properties. Besides this, coumarins have also shown potential to inhibit α-glucosidase leading to a generation of new promising antidiabetic agents. However, the testing of O-substituted coumarins for α-glucosidase inhibition has evaded the attention of medicinal chemists. Methods: For O-alkylation/acetylation reactions, the hydroxyl coumarins (A-B) initially activated by K2CO3 in dry DMF were reacted with variedly substituted haloalkanes at room temperature under nitrogen. The synthesized compounds were tested for their α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity and anti-oxidant activity using DPPH radical scavenging activity. In silico docking simulations were conducted using CDocker module in DS (Accelrys) to explore the binding modes of the representative compounds in the catalytic site of α-glucosidase. Results: All the coumarin analogues (A1, B1, A2-A10, B2-B8) including their precursors (A-B) were evaluated for their in vitro α-glucosidase inhibition using acarbose as a standard inhibitor. All the mono O-alkylated coumarins (except A1) showed significant (p <0.05) α-glucosidase inhibition relative to the hydroxyl coumarin (A) with IC50 values ranging between 11.084±0.117 to 145.24± 29.22 µg/mL. Compound 7-(benzyloxy)-4, 5-dimethyl-2H-chromen-2-one (A9) bearing a benzyl group (Ph-CH2-) at position 7 showed a remarkable (p <0.05) increase in the activity (IC50 = 11.084±0.117 µg/mL), almost four-fold more than acarbose (IC50 = 40.578±5.999 µg/mL). The introduction of –NO2 group dramatically improved the anti-oxidant activity of coumarin, while the O-alkylation/acetylation decreased the activity. Conclusion: The present study describes the synthesis of functionalized coumarins and their evaluation for α-glucosidase inhibition and antioxidant activity under in vitro conditions. Based on IC50 data, the mono O-alkylated coumarins were observed to be stronger inhibitors of α-glucosidase with respect to their bis O-alkylated analogues. Coumarin (A9) bearing O-benzyloxy group displayed the strongest α-glucosidase inhibition, even higher than the standard inhibitor acarbose. The coumarin (A10) bearing –NO2 group showed the highest anti-oxidant activity amongst the synthesized compounds, almost comparable to the ascorbic acid. Finally, in silico docking simulations revealed the role of hydrogen bonding and hydrophobic forces in locking the compounds in catalytic site of α-glucosidase.

scholarly journals IN VITRO SCREENING OF INSECTICIDAL EFFECT OF PLANT AQUEOUS EXTRACTS ON THE COWPEA APHID APHIS CRACCIVORA

AGROFOR ◽  
2018 ◽  
Vol 2 (2) ◽  
Author(s):  
Salim LEBBAL ◽  
Aissa LEBBAL ◽  
Azzeddine ZERAIB
Keyword(s):  
Chemical Control ◽  
Aphis Craccivora ◽  
Aqueous Extracts ◽  
Control Methods ◽  
Phytochemical Screening ◽  
Juniperus Thurifera ◽  
Negative Effects ◽  
Insecticidal Effect ◽  
Cowpea Aphid

The research of new control methods that have low negative effects represent analternative aiming to limit disadvantages of chemical control of pests. This studyaimed to test the effect of 11 aqueous plant extracts belonging to four species(Santolina africana, Juniperus thurifera, Artemisia herba-alba and Pituranthosscoparius), on the larvae of the aphid Aphis craccivora installed on the leaves ofRobinia pseudoacacia under laboratory conditions. The insecticidal effect ofaqueous extracts on the mortality of aphids was evaluated by the introduction ofacacia leaflet into an extract and infestation of them by 10 larvae of the aphid.Later, a counting of dead larvae after 3, 6, 12 and 24 h was performed. In addition,we investigated the effect of the aqueous extracts on the orientation of the aphidsby putting the latter in a position of choice between six leaflets, each treated with adifferent extract. In addition, a phytochemical screening was carried out to detectthe presence of saponins and polyphenols in the extracts studied. Through ourstudy, the extract obtained from S. africana at a concentration of 15% was the mosteffective with a mortality rate higher than 80% after 24 h of artificial infestation.As for the effect of the four extracts on the orientation of the cowpea aphid, theydid not attract the larvae massively. Regarding phytochemical screening,differences in the chemical composition of the analyzed extracts were observed.These differences may explain in part the variation of aphicidal effects of testedplant extracts.

scholarly journals In vitro thrombolytic, anthelmintic, anti-oxidant and cytotoxic activity with phytochemical screening of methanolic extract of Xanthium indicum leaves

2015 ◽  
Vol 10 (4) ◽  
pp. 854 ◽  
Author(s):  
Antara Ghosh ◽  
Sujan Banik ◽  
Md. Ariful Islam
Keyword(s):  
Cytotoxic Activity ◽  
Methanolic Extract ◽  
Radical Scavenging ◽  
Anthelmintic Activity ◽  
Positive Control ◽  
Clot Lysis ◽  
Total Phenolic ◽  
Phytochemical Screening ◽  
Anti Oxidant

<p class="Abstract"><em>Xanthium indicum</em> is an important medicinal plant traditionally used in Bangladesh as a folkloric treatment. The current study was undertaken to evaluate thrombolytic, anthelmintic, anti-oxidant, cytotoxic properties with phytochemical screening of methanolic extract of <em>X. indicum</em> leaves. The analysis of phytochemical screening confirmed the existence of phytosetrols and diterpenes. In thrombolytic assay, a significant clot lysis was observed at four concentrations of plant extract compare to the positive control streptokinase (30,000 IU, 15,000 IU) and negative control normal saline. The extract revealed potent anthelmintic activity at different concentrations. In anti-oxidant activity evaluation by two potential experiments namely total phenolic content determination and free radical scavenging assay by 2, 2-diphenylpicrylhydrazyl (DPPH), the leaves extract possess good anti-oxidant property. In the brine shrimp lethality bioassay, the crude extract showed potent (LC<sub>50</sub> 1.3 μg/mL) cytotoxic activity compare to the vincristine sulfate as a positive control (LC<sub>50</sub> 0.8 μg/mL). </p><p> </p>

scholarly journals In-Vitro Trial of Roots of Ishwarmuli (Aristolochia indica Linn.) for Anti-Microbial, Anti-Fungal & Anti-Oxidant Activity

2020 ◽  
Vol 11 (3) ◽  
pp. 405-409
Author(s):  
Sandeep Binorkar ◽  
Gajanan Parlikar ◽  
Ranjeet Sawant ◽  
Manish Bhoyar ◽  
Milind B Nikumbh
Keyword(s):  
Metabolic Diseases ◽  
Shigella Flexneri ◽  
Relevant Literature ◽  
Aqueous Extracts ◽  
Bacterial Strains ◽  
Minimum Concentration ◽  
Ethanolic Extracts ◽  
Anti Oxidant ◽  
Anti Fungal

Aristolochia indica is a plant belonging to the family Aristolochiaceae. The medicinal value of A. indica has been known in different system of traditional medicine including Ayurveda. A number of Aristolochia species has been used in herbal medicines throughout the world for the cure of several ailments including metabolic diseases to venomous bites of snake and insects. The current work was executed with an objective to explore the in vitro antimicrobial, anti-fungal and anti-oxidant activity of A. indica. The relevant literature was also pursued for the justification and comparing the resemblances in the results. Aqueous and ethanolic extracts of roots of Aristolochia indica Linn. were tested for their inhibitory effect against 6 bacterial strains [Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Salmonella typhi, Klebsiella pneumoniae & Shigella flexneri] and 3 fungi strains [Aspergillus niger, Aspergillus fumigatus, Candida albicans]. Agar-well method was used for the assessment of in-vitro antibacterial and antifungal activity of A. indica against selected standard bacterial strains. The minimum inhibitory concentration for each extract of various micro-organisms was also measured. Ethanolic extract of A. indica shows Minimum concentration (MIC) value of 50-100 μg/ml against selected bacterial strains which is better when compared to the aqueous extracts. Ethanolic extracts also showed moderate effects against the selected fungal strains, whereas the aqueous extracts failed to exhibit any effect even at higher concentrations.

scholarly journals Antiplasmodial activity of Anthocleista djalonensis leaves extracts against clinical isolates of Plasmodium falciparum and multidrug resistant K1 strains

2020 ◽  
Vol 8 (3) ◽  
pp. 130-138
Author(s):  
Brice Kouakou Bla ◽  
Oléfongo Dagnogo ◽  
Rolland Gueyraud Kipré ◽  
Opportune Gogo Ballé ◽  
Jonhson David Trébissou ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Multidrug Resistant ◽  
Traditional Healers ◽  
Antiplasmodial Activity ◽  
Clinical Isolates ◽  
Aqueous Extracts ◽  
Phytochemical Screening ◽  
Primary Health ◽  
Ethanolic Extracts

Information collected from nine (09) traditional healers in the Moronou village in the Department of Toumodi revealed that Anthocleista djanlonensis is regularly used by the population for primary health care in the processing of malaria. Evaluation of the In vitro antiplasmodial activity showed that the aqueous extracts inhibit growth of clinical isolates and chloroquinoresistant strains (K1) with IC50 of 8.29 µg/mL and 10.23 µg/mL while the ethanolic extracts had IC50 of 37.65 µg/mL and 46.07 µg/mL on the same strains respectively. Results of the In vitro antimalarial bioassay showed that aqueous extracts have promising antiplasmodial effects on clinical isolates and on Plasmodium falciparum multidrug resistant K1 strain (3 µg/mL <IC50 <15 µg/mL). Phytochemical screening revealed that the extracts contain mainly alkaloids, polyphenols, polyterpenes and flavonoids

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