scholarly journals Phytochemical characterization, anti-cancer and antimicrobial activity of isolated fractions of Alysicarpus vaginalis

2017 ◽  
Vol 12 (1) ◽  
pp. 77 ◽  
Author(s):  
Ganesh Tapadiya ◽  
Mayura A. Kale ◽  
Shweta Saboo
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Methanolic Extract ◽  
Hep G2 ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Anti Cancer ◽  
Proliferative Assay ◽  
Bacteria And Fungi

<p class="Abstract">The methanolic extract of <em>Alysicarpus </em>vaginalis was selected for fractionation due to its known reported biological activity. The four fractions were separated and subjected for<em> in vitro</em> antimitotic and anti-proliferative assays along with anti-cancer activity on two human cancers cell lines (SK-MEL-2 and Hep-G2). The antimicrobial potential of fractions had been evaluated against bacteria and fungi. From all fractions, acetone and n-butanol fractions were effective against the cell lines. They show strong inhibitory action with mitotic index 6.2 and 8.4 mg/mL and IC<sub>50 </sub>values of anti-proliferative assay in between 19.7 to 14.2 mg/mL respectively, which was found to be comparable to the standard methothrexate 5.9 mg/mL and 13.2 mg/mL respectively. In antimicrobial activity, the zone of inhibition had been observed in the range of 12-27 mm and MIC value was found in the range of 0.2-0.1 mg/mL. The acetone fraction was found to be most active against fungi, and<em> E. coli</em> whereas chloroform and n-butanol fractions were more effective against <em>S. aureus</em> and <em>B. </em>subtilis. The phytochemical characterization by HPLC analysis indicated the presence of important polyphenolic and steroidal compounds.</p>

scholarly journals Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

2021 ◽  
Author(s):  
Smita J. Pawar ◽  
Amol Kale ◽  
Priya Zori ◽  
Rahul Dorugade
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Property ◽  
Docking Study ◽  
Gram Negative Bacteria ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Good Antibacterial Activity ◽  
Comparable Activity ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi

Abstract Abstract The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.

Apoptosis Inducing Effects of Thymus linearis Methanolic Extract in HCT-116 Cells and LC-MS Chemical Profiling of Its Active Constituents

2021 ◽  
Vol 11 ◽  
Author(s):  
Rohina Bashir ◽  
Ovais Zargar ◽  
Qazi Parvaiz ◽  
Rabia Hamid
Keyword(s):  
Cell Lines ◽  
Antiproliferative Activity ◽  
Dna Cleavage ◽  
Methanolic Extract ◽  
Dependent Manner ◽  
Regulation Of Expression ◽  
Anti Cancer ◽  
Hct 116 ◽  
Hct 116 Cells

Background: Cancer is one of the major problems at present, to which vast research is being dedicated to find effective remedy. Medicinal plants are endowed with numerous molecules that could be effective in multiple diseases including cancer. Thymus linearis, being rich in phenols, terpenoid, and flavonoids have potential to provide anti-cancer entities. Methods: The extracts of Thymus linearis were investigated for in vitro anticancer activity using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay on a panel of cancer cell lines. The cellular and nuclear morphology was studied using microscopic techniques. Agarose gel electrophoresis was used for DNA fragmentation analysis. Protein expression was determined by western-blotting. LC-MS was used for phytochemical identification. Results: Among all the extracts, Thymus linearis methanolic (TLM) extract was found to exhibit antiproliferative activity on cell lines to varied degrees. TLM was found to be most potent against HCT-116 with an IC50 of 158μg/ml after 48hrs treatment, while being nontoxic to HEK-293 and FR-2 cells under similar concentrations. TLM decreased clonogenic potential of HCT-116 cells. It induced cell shrinkage, membrane blebbing and nuclear fragmentation characteristic of apoptotic in a dose dependent manner in HCT-116 cells. Prominent internucleosomal DNA cleavage was observed in HCT-116 cells after 48hrs TLM treatment. Western blot analysis revealed the up regulation of expression of Bax, caspases 9 and caspases 3 and downregulation of Bcl-2 proteins. The LC-MS data revealed the presence of Salvianolic acid H, Synparvolide C, Thymuside A and Jasmonic acid; 12-Hydroxy, O-β-D-glucopyranoside and polyphenolic flavonoids to which antiproliferative activity can be attributed. Conclusion: The results suggest that Thymus linearis methanolic extract could be valuable source of anti-cancer agents.

ANTIMICROBIAL ACTIVITY OF 3- (1- (3- HYDROXYPHENYL) AMINO) ETHYLIDENE) CHROMAN-2,4-DIONE AND ITS CORRESPONDING PALLADIUM(II) COMPLEX

2021 ◽  
Author(s):  
Edina Avdović ◽  
◽  
Žiko B. Milanović ◽  
Milanka Radulović ◽  
Dušan S. Dimić
Keyword(s):  
Antimicrobial Activity ◽  
Inhibitory Concentration ◽  
Antimicrobial Effect ◽  
Coumarin Derivative ◽  
The Other ◽  
Disc Diffusion ◽  
Zone Of Inhibition ◽  
Microdilution Method ◽  
Bacteria And Fungi

In this manuscript, the in vitro antimicrobial activity of the previously synthesized coumarin derivative 3- (1- (3-hydroxyphenyl) amino) ethylidene) chroman-2,4-dione (L) and its corresponding palladium (II) complex (C) were examined. Their antimicrobial activity was screened against four strains of bacteria Bacillus cereus (ATCC 11778) G+; Staphylococcus aureus (ATCC 13709) G+; Klebsiella pneumoniae (ATCC 27736) G-; and Escherichia coli (ATCC 2592) G-) and three strains of fungi (Aspergillus flavus (ATCC15517); Candida albicans (ATCC 10231); Fusarium oxysporum (ATCC 695) using disc diffusion and microdilution method. The obtained minimum inhibitory concentration (MIC) values by microdilution method for ligand and complex are similar for all tested bacteria and fungi, which means that both compounds have a similar antimicrobial effect. On the other hand, analysis of zone of inhibition (ZI) values for the tested compounds shows that the complex is generally somewhat more active than the ligand.

Synthesis and Structural Elucidation of Aminoacetylenic Derivatives of 7-Methoxy- 2-Naphthole as Antimicrobial Agents

2017 ◽  
Vol 9 (08) ◽  
Author(s):  
Abu- Safieh Rana ◽  
Muhi- Eldeen Zuhair ◽  
Alsarahni Aseel ◽  
Al-Kaissi Elham
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Naphthalene Derivatives ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Bacteria And Fungi ◽  
Aminoacetylenic Derivatives ◽  
Derivatives Of ◽  
Mic Value

A new series of 7-methoxy-2-[4-(t-amino-1-yl)oxy]-naphthalene derivatives; 7-methoxy-2-{[4-(2-methylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ2), 7-methoxy-2-{[4-(2,6-dimethylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ3), 7-methoxy-2{[4-(piperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ4), 7-methoxy-2-{[4-(pyrrolidine)but-2-yn-1-yl]oxy}-naphthalene (RZ5), 7-methoxy-2-{[4-(N-methylpiperazine)but-2-yn-1-yl]oxy}-naphthalene (RZ6), 7-methoxy -2-{[4-(hexamethyleneimine)but-2-yn-1-yl]oxy}-naphthalene (RZ7) were synthesized and screened in vitro as potential antimicrobial agents. Antimicrobial activity were evaluated by measuring the minimum inhibitory and bactericidal/fungicidal concentration (MIC, MBC and MFC). RZ2, RZ5, RZ6 and RZ7 showed the highest antimicrobial activity against S. aureus with MIC value 62.5 µg/ml, compounds RZ2, RZ4, RZ5, and RZ7 have the highest antimicrobial activity against B. subtilis with MIC vale 62.5 µg/ml, RZ3, RZ6 have the same antimicrobial activity with MIC value 125µg/ml, compounds. RZ4, RZ5, RZ6 and RZ7 have the highest antimicrobial activity against E. coli with MIC value 125 µg/ml, all compounds have the same MIC value against P. aeruginosa (125 µg/ml). RZ2, RZ4, RZ5, RZ6, RZ7 showed the highest antifungal activity with MIC of 62.5 µg/ml. In conclusion, the synthesized compounds showed good antimicrobial activity and promising potency against gram positive bacteria, gram negative bacteria and fungi.

scholarly journals Phytochemical, antimicrobial and antioxidant studies of the leaf extract of Hamelia patens

2020 ◽  
Vol 4 (02) ◽  
pp. 1-5
Author(s):  
S. Megala ◽  
G. Venkat Kumar ◽  
R. V. Shalini ◽  
V. P. Manjamadha
Keyword(s):  
Leaf Extract ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Experimental Models ◽  
Diffusion Method ◽  
Dpph Assay ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Vis Spectroscopy

This study aimed to characterise the different extracts of the leaves of Hamelia patens Jacq. (Rubiaceae) and to evaluate their antibacterial and antioxidant activities in vitro. Phytochemical screening of the leaf extract revealed the presence of alkaloids, flavonoids, sterols, tannins and carotenoids. The extracts were further characterised with the help of FTIR and UV-VIS spectroscopy. The antibacterial activity was evaluated by agar well diffusion method and the zone of inhibition was measured. 1,1-diphenyl-2- picrylhydrazyl (DPPH) assay was used to evaluate the antioxidant capability of the extract. The extract was found effective in inhibiting the growth of both E. coli and S. aureus at 5 μg/mL concentration. The methanolic extract was also found to scavenge DPPH radicals. Although the extract is found effective in the present study, however, further research is required to evaluate the biological activity in higher experimental models.

scholarly journals Euphorbia graminea Jacq. (Euphorbiaceae): The antimicrobial assessment of the extract and fractions of the leaves

2020 ◽  
pp. 3809-3818
Author(s):  
Ikpefan E. O. ◽  
Enwa F. O. ◽  
Emebrado O.
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Chloroform Extract ◽  
Diffusion Method ◽  
E Coli ◽  
Staphyloccocus Aureus ◽  
Test Organisms ◽  
Zones Of Inhibition ◽  
Bacteria And Fungi

This study was carried out as a result of the belief that certain medicinal plants have antimicrobial activity against pathogenic bacteria and fungi species, hence the in vitro antimicrobial activity of the extract and fractions of Euphorbia graminea was performed against bacteria (Staphyloccocus aureus, Escherichia coli, Pseudomonas aeruginosa) and fungal (Candida albican) non-clinical isolates. The methanol extract of Euphorbia graminea was fractionated via solvent-solvent partitioning and vacuum liquid chromatographic techniques and the corresponding fractions were tested for phytochemicals and were biologically tested against the organisms employing the agar well diffusion method. While the extract and partitioned fractions were tested at concentrations between 4.69-300 mg/mL, the vlc subfractions were tested at 12.50-200 mg/mL against the organisms. The MIC of the active vlc subfractions was also tested (9.38-37.5 mg/mL). The alkaloids as well as glycosides, tannins, terpenes and steroids were detected among the extracts and fractions of E. graminea. The extract showed mild activities against the test organisms with the highest zone of inhibition of 7.00 mm recorded at 300 mg/mL against S.aureus. The activities of both extract at 300 mg/mL, showed notable increase against the organisms used, with zones of inhibition of the aqueous extract been 10.50 and 9.50mm and for the chloroform extract, 16.50 and 13.05mm (S. aureus and E. coli respectively). The vlc sub-fraction 6-8 (C) among the other subfractions was more potent against S. aureus, E. coli and C. albican as 16.50, 12.00 and 0.50 mm zones of inhibition were recorded at 100 mg/mL. The zones of inhibition against these organisms later increased to 20.00, 18.50 and 15.00 mm at 200 mg/mL. This study has highlighted the fact that the plant E. graminea has antimicrobial activity which occurs more in the partitioned chloroform and its chromatographic vacuum liquid subfraction (6-8) that gave the highest activity. However, in order to isolate the active biological components and to determine their safety in drug production, further studies are needed.

scholarly journals In vitro antibacterial activity of extracts of Dalbergia sissoo and Aegle marmelos against Enterotoxigenic Escherichia coli from calves

2021 ◽  
Vol 10 (5) ◽  
pp. 289-293
Author(s):  
Ashok Singh Rathor ◽  
◽  
Taruna Bhati ◽  
AP Singh ◽  
◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Aqueous Extract ◽  
Methanolic Extract ◽  
Enterotoxigenic Escherichia Coli ◽  
Dalbergia Sissoo ◽  
Zone Of Inhibition ◽  
Aegle Marmelos ◽  
E Coli ◽  
In Vitro Antibacterial Activity

Neonatal calf diarrhoea (NCD) is the most common cause of morbidity and mortality in pre-weaned dairy calves, causing huge economic and productivity losses to dairy industry worldwide. Enterotoxigenic E. coli (ETEC) is one of the important causes of neonatal diarrhoea and high mortality in very young calves. Shisham (Dalbergia sissoo) leaves and Bael (Aegle marmelous) unripe fruit have been used in diarrhoea and dysentery with very good results. Hence the present study was conducted to evaluate the in vitro antibacterial activity of the aqueous and methanolic extract of Dalbergia sissoo and Aegle marmelos against 16 E. coli isolated from colibacillosis affected diarrhoeic calves in Bikaner district of Rajasthan. The average zones of inhibitions of aqueous extract of Aegle marmelos and methanolic extract of Dalbergia sissoo against E. coli were 23.75±0.34 mm, 18.75±0.32 mm, 16.5±0.24 mm, 11.58 ±0.14 mm and 7.88±0.24 mm at concentrations of 1000 mg/ml, 500 mg/ml, 250 mg/ml 125 mg/ml and 62.5 mg/ml, respectively. The average zones of inhibition of aqueous extract of Dalbergia sissoo and methanolic extract of Aegle marmelos against E. coli were 24.75±0.20 mm, 19.87±0.34 mm, 17.25±0.24mm, 12.86±0.13 mm and 8.50±0.14 mm at concentrations of 1000 mg/ml, 500 mg/ml, 250 mg/ml 125 mg/ml and 62.5 mg/ml, respectively. The maximum zone of inhibition was reported by aqueous extract of Dalbergia sissoo and methanolic extract of Aegle marmelos (>24 mm of diameter) at concentration of 1000 mg/ml. Based on average zone of inhibition, the in vitro antibacterial activity of aqueous extract of Dalbergia sissoo and methanolic extract of Aegle marmelos was found to be more against E. coli as compared to aqueous extract of Aegle marmelos and methanolic extract of Dalbergia sissoo at varying concentrations. In conclusion, both combination of aqueous and methanolic extract of Dalbergia sissoo and Aegle marmelos showed in vitro antibacterial properties against E. coli

scholarly journals Delivery of melittin-loaded niosomes for breast cancer treatment: an in vitro and in vivo evaluation of anti-cancer effect

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Farnaz Dabbagh Moghaddam ◽  
Iman Akbarzadeh ◽  
Ehsan Marzbankia ◽  
Mahsa Farid ◽  
Leila khaledi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Treatment ◽  
Cell Lines ◽  
Encapsulation Efficiency ◽  
Inbred Mice ◽  
Breast Cancer Treatment ◽  
Anticancer Effect ◽  
Anti Cancer

Abstract Background Melittin, a peptide component of honey bee venom, is an appealing candidate for cancer therapy. In the current study, melittin, melittin-loaded niosome, and empty niosome had been optimized and the anticancer effect assessed in vitro on 4T1 and SKBR3 breast cell lines and in vivo on BALB/C inbred mice. "Thin-layer hydration method" was used for preparing the niosomes; different niosomal formulations of melittin were prepared and characterized in terms of morphology, size, polydispersity index, encapsulation efficiency, release kinetics, and stability. A niosome was formulated and loaded with melittin as a promising drug carrier system for chemotherapy of the breast cancer cells. Hemolysis, apoptosis, cell cytotoxicity, invasion and migration of selected concentrations of melittin, and melittin-loaded niosome were evaluated on 4T1 and SKBR3 cells using hemolytic activity assay, flow cytometry, MTT assay, soft agar colony assay, and wound healing assay. Real-time PCR was used to determine the gene expression. 40 BALB/c inbred mice were used; then, the histopathology, P53 immunohistochemical assay and estimate of renal and liver enzyme activity for all groups had been done. Results This study showed melittin-loaded niosome is an excellent substitute in breast cancer treatment due to enhanced targeting, encapsulation efficiency, PDI, and release rate and shows a high anticancer effect on cell lines. The melittin-loaded niosome affects the genes expression by studied cells were higher than other samples; down-regulates the expression of Bcl2, MMP2, and MMP9 genes while they up-regulate the expression of Bax, Caspase3 and Caspase9 genes. They have also enhanced the apoptosis rate and inhibited cell migration, invasion in both cell lines compared to the melittin samples. Results of histopathology showed reduce mitosis index, invasion and pleomorphism in melittin-loaded niosome. Renal and hepatic biomarker activity did not significantly differ in melittin-loaded niosome and melittin compared to healthy control. In immunohistochemistry, P53 expression did not show a significant change in all groups. Conclusions Our study successfully declares that melittin-loaded niosome had more anti-cancer effects than free melittin. This project has demonstrated that niosomes are suitable vesicle carriers for melittin, compare to the free form.

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