scholarly journals Evaluation of antimicrobial, antioxidant and cytotoxic activities and characterization of bioactive substances from freshwater blue-green algae

<p>Organic solvent extracts of three cyanobacterial species (Anabaena oryzae, Oscillatoria sp. and Stigonema ocellatum) were tested for antimicrobial activity against human pathogenic fungal and bacterial strains as well as for antioxidant and cytotoxic activity against human breast adenocarcinoma (MCF-7). The acetone extract of Anabaena oryzae was found to be the most active one against tested fungal and bacterial strains. It showed a maximum antimicrobial activity against Serratia marcescens and Candida albicans. The methanol extract of Oscillatoria sp. exhibited the best total antioxidant capacity compared to the other solvents and algal species. Acetone and methanol extracts of Anabaena oryzae exhibited high toxicity against MCF-7 cell line with IC50 of 45.1 and 44.4 µg/L, respectively. Acetone was the best solvent for extracting the active material. The acetone extracts were characterized by Gas Chromatography Mass Spectrophotometer (GC–MS) to identify the compounds responsible for such activities. Pharmaceutical important compounds in the acetone extract of cyanobacterial species like diacetone alcohol, acetic acid butyl ester mesityl oxide and heptadecane were present as a major component. These results indicate that extracts of studied cyanobacterial species exhibited appreciable antimicrobial, antioxidant and cytotoxic activity and could be a source of valuable bioactive materials for health products.</p>

2018 ◽  
Vol 8 (3) ◽  
pp. 159 ◽  
Author(s):  
Meghan Fragis ◽  
Abdulmonem I. Murayyan ◽  
Suresh Neethirajan

Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity


2021 ◽  
Vol 11 (11) ◽  
pp. 5300
Author(s):  
Jozef Hudec ◽  
Jan Mojzis ◽  
Marta Habanova ◽  
Jorge A. Saraiva ◽  
Pavel Hradil ◽  
...  

Sarcopoterium spinosum (L.) is a medicinal plant traditionally used for the treatment of various diseases including cancer in the Near- and Middle East. The fractions and constituents of the ethanol extract of S. spinosum were screened for in vitro cytotoxic activities on Jurkat (acute T-lymphoblastic leukemia), HeLa (cervical adenocarcinoma), MCF-7 (mammary gland adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), and MDA-MB-231 (mammary gland adenocarcinoma) cell lines using the MTT (3-(dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The ethanol extract was subsequently re-extracted with ethyl acetate and in its sub-fraction obtained by column chromatography three compounds (stachydrine, benzalkonium chloride and rutine) were the first time identified by nuclear magnetic resonance (NMR) analyses. The most active subfraction showed cytotoxic activity against HeLa, MCF-7, and Caco-2 cell lines. The three compounds mentioned, as standards of high-performance liquid chromatography (HPLC) quality, were studied individually and in combination. Cytotoxic activity observed might be due to the presence of benzalkonium chloride and rutin. Benzalkonium chloride showed the strongest growth suppression effect against HeLa cells (IC50 8.10−7 M) and MCF-7 cells (IC50 5.10−6 M). The mixture of stachydrine and benzalkonium chloride allowed a synergistic cytotoxic effect against all tested cancer and normal cells to be obtained. Anti-cancer activity of the plant extract of S. spinosum remains under-investigated, so this research describes how the three major compounds identified in the ethyl acetate extract can exert a significant dose dependent in vitro cytotoxicity.


Marine Drugs ◽  
2020 ◽  
Vol 18 (8) ◽  
pp. 405
Author(s):  
Reda F. A. Abdelhameed ◽  
Enas E. Eltamany ◽  
Dina M. Hal ◽  
Amany K. Ibrahim ◽  
Asmaa M. AboulMagd ◽  
...  

Bioactivity-guided fractionation of a methanolic extract of the Red Sea cucumber Holothuria spinifera and LC-HRESIMS-assisted dereplication resulted in the isolation of four compounds, three new cerebrosides, spiniferosides A (1), B (2), and C (3), and cholesterol sulfate (4). The chemical structures of the isolated compounds were established on the basis of their 1D NMR and HRMS spectral data. Metabolic profiling of the H. spinifera extract indicated the presence of diverse secondary metabolites, mostly hydroxy fatty acids, diterpenes, triterpenes, and cerebrosides. The isolated compounds were tested for their in vitro cytotoxicities against the breast adenocarcinoma MCF-7 cell line. Compounds 1, 2, 3, and 4 displayed promising cytotoxic activities against MCF-7 cells, with IC50 values of 13.83, 8.13, 8.27, and 35.56 µM, respectively, compared to that of the standard drug doxorubicin (IC50 8.64 µM). Additionally, docking studies were performed for compounds 1, 2, 3, and 4 to elucidate their binding interactions with the active site of the SET protein, an inhibitor of protein phosphatase 2A (PP2A), which could explain their cytotoxic activity. This study highlights the important role of these metabolites in the defense mechanism of the sea cucumber against fouling organisms and the potential uses of these active molecules in the design of new anticancer agents.


Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 544 ◽  
Author(s):  
Eman Assirey ◽  
Azhaar Alsaggaf ◽  
Arshi Naqvi ◽  
Ziad Moussa ◽  
Rawda M. Okasha ◽  
...  

Novel flavanones that incorporate chromene motifs are synthesized via a one-step multicomponent reaction. The structures of the new chromenes are elucidated by using IR, 1H-NMR, 13C-NMR, 1H-1H COSY, HSQC, HMBC, and elemental analysis. The new compounds are screened for their in vitro antimicrobial and cytotoxic activities. The antimicrobial properties are investigated and established against seven human pathogens, employing the agar well diffusion method and the minimum inhibitory concentrations. A majority of the assessed derivatives are found to exhibit significant antimicrobial activities against most bacterial strains, in comparison to standard reference drugs. Moreover, their cytotoxicity is appraised against four different human carcinoma cell lines: human colon carcinoma (HCT-116), human hepatocellular carcinoma (HepG-2), human breast adenocarcinoma (MCF-7), and adenocarcinoma human alveolar basal epithelial cell (A-549). All the desired compounds are subjected to in-silico studies, forecasting their drug likeness, bioactivity, and the absorption, distribution, metabolism, and excretion (ADME) properties prior to their synthetic assembly. The in-silico molecular docking evaluation of all the targeted derivatives is undertaken on gyrase B and the cyclin-dependent kinase. The in-silico predicted outcomes were endorsed by the in vitro studies.


PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e4839 ◽  
Author(s):  
Wafa M. Al-Madhagi ◽  
Najihah Mohd Hashim ◽  
Nasser A. Awad Ali ◽  
Abeer A. Alhadi ◽  
Siti Nadiah Abdul Halim ◽  
...  

Background Peperomia belongs to the family of Piperaceae. It has different uses in folk medicine and contains rare compounds that have led to increased interest in this genus. Peperomia blanda (Jacq.) Kunth is used as an injury disinfectant by Yemeni people. In addition, the majority of Yemen’s population still depend on the traditional remedy for serious diseases such as cancer, inflammation and infection. Currently, there is a deficiency of scientific evidence with regards to the medicinal plants from Yemen. Therefore, this study was performed to assess the chemical profile and in vitro antioxidant and cytotoxic activities of P. blanda. Methods Chemical profiling of P. blanda was carried out using gas chromatography mass spectrometry (GCMS) followed by isolation of bioactive compounds by column chromatography. DPPH• and FRAP assays were used to evaluate antioxidant activity and the MTT assay was performed to estimate the cytotoxicity activity against three cancer cell lines, namely MCF-7, HL-60 and WEHI-3, and three normal cell lines, MCF10A, WRL-68 and HDFa. Results X-ray crystallographic data for peperomin A is reported for the first time here and N,N′-diphenethyloxamide was isolated for the first time from Peperomia blanda. Methanol and dichloromethane extracts showed high radical scavenging activity with an IC50 of 36.81 ± 0.09 µg/mL, followed by the dichloromethane extract at 61.78 ± 0.02 µg/mL, whereas the weak ferric reducing activity of P. blanda extracts ranging from 162.2 ± 0.80 to 381.5 ± 1.31 µg/mL were recorded. In addition, petroleum ether crude extract exhibited the highest cytotoxic activity against all the tested cancer cell lines with IC50 values of 9.54 ± 0.30, 4.30 ± 0.90 and 5.39 ± 0.34 µg/mL, respectively. Peperomin A and the isolated mixture of phytosterol (stigmasterol and β-sitosterol) exhibited cytotoxic activity against MCF-7 and WE-HI cell lines with an IC50 of (5.58 ± 0.47, 4.62 ± 0.03 µg/mL) and (8.94 ± 0.05, 9.84 ± 0.61 µg/mL), respectively, compared to a standard drug, taxol, that has IC50 values of 3.56 ± 0.34 and 1.90 ± 0.9 µg/mL, respectively. Conclusion The activities of P. blanda extracts and isolated compounds recorded in this study underlines the potential that makes this plant a valuable source for further study on anticancer and antioxidant activities.


2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.


2015 ◽  
Vol 10 (6) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Prabodh Satyal ◽  
Bhuwan K. Chhetri ◽  
Noura S. Dosoky ◽  
Ambika Poudel ◽  
William N. Setzer

The essential oil from the dried rhizome of Nardostachys grandiflora, collected from Jaljale, Nepal, was obtained in 1.4% yield, and a total of 72 compounds were identified constituting 93.8% of the essential oil. The rhizome essential oil of N. grandiflora was mostly composed of calarene (9.4%), valerena-4,7(11)-diene (7.1%), nardol A (6.0%), 1(10)-aristolen-9-ol (11.6%), jatamansone (7.9%), valeranal (5.6%), and cis-valerinic acid (5.7%). The chemical composition of N. grandiflora rhizome oil from Nepal is qualitatively very different than those from Indian, Chinese, and Pakistani Nardostachys essential oils. In this study we have evaluated the chemical composition and biological activities of N. grandiflora from Nepal. Additionally, 1(10)-aristolen-9-ol was isolated and the structure determined by NMR, and represents the first report of this compound from N. grandiflora. N. grandiflora rhizome oil showed in-vitro antimicrobial activity against Bacillus cereus, Escherichia coli, and Candida albicans (MIC = 156 μg/mL), as well as in-vitro cytotoxic activity on MCF-7 cells.


2018 ◽  
Vol 13 (3) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Alfarius Eko Nugroho ◽  
Hitomi Nakamura ◽  
Daisuke Inoue ◽  
Yusuke Hirasawa ◽  
Chin Piow Wong ◽  
...  

Two new polyisoprenylated acylphloroglucinols, 7- epi-isoxanthochymol and 7- epi-cycloxanthochymol (1 – 2), were isolated from the barks of Garcinia nervosa together with their 7-epimers isoxanthochymol (3) and cycloxanthochymol (4). Their structures were determined on the basis of NMR spectroscopic data. The cytotoxic activity of the isolated compounds against HL-60, MCF-7 (human breast adenocarcinoma), A549 (human lung adenocarcinoma) and HepG2 (human hepatocellular carcinoma) cells were evaluated, and all compounds showed cytotoxic activity against all cell lines.


2019 ◽  
Vol 12 (1) ◽  
pp. 34 ◽  
Author(s):  
Ana Ferreira Farias ◽  
Alex Lobato Rodrigues ◽  
Rosany Lopes Martins ◽  
Érica de Menezes Rabelo ◽  
Carlos Ferreira Farias ◽  
...  

The present study aimed to evaluate the chemical composition, antioxidant potential, and the cytotoxic and antimicrobial activity of the essential oil of the plant species Tithonia diversifolia (Hemsl) A. Gray. The essential oil obtained was used to identify the chemical compounds present through the techniques of GC-MS and NMR. The antioxidant potential was calculated by the sequestration method of 2,2-diphenyl-1-picrylhydrazyl. For cytotoxic activity, the larval mortality of Artemia salina was evaluated. The main chemical constituents identified are αpinene (9.9%), Limonene (5.40%), (Z)-β-ocimene (4.02%), p-cymen-8-ol (3.0%), Piperitone (11.72%), (E)-nerolidol (3.78%) and Spathulenol (10.8%). In the evaluation of the antimicrobial activity, bacterial strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa were used. The results showed that the bacterium E. coli were more susceptible to the presence of the essential oil, presenting minimal inhibitory concentration at the concentrations that were exposed. The essential oil presented antioxidant activity of 54.6% at the concentration of 5 mg·mL−1 and provided a CI50 of 4.30. It was observed that the essential oil of this species was highly toxic against A. salina lavas, as its cytotoxic activity showed an LC50 of 3.11. Thus, it is concluded that T. diversifolia oils are effective in inhibiting bacterial growth and reducing oxidative stress.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 597 ◽  
Author(s):  
Zuhier A. Awan ◽  
Usama A. Fahmy ◽  
Shaimaa M. Badr-Eldin ◽  
Tarek S. Ibrahim ◽  
Hani Z. Asfour ◽  
...  

Statins, including simvastatin (SMV), are commonly used for the control of hyperlipidaemia and have also proven therapeutic and preventative effects in cardiovascular diseases. Besides that, there is an emerging interest in their use as antineoplastic drugs as demonstrated by different studies showing their cytotoxic activity against different cancer cells. In this study, SMV-loaded emulsomes (SMV-EMLs) were formulated and evaluated for their cytotoxic activity in MCF-7 breast cancer cells. The emulsomes were prepared using a modified thin-film hydration technique. A Box–Behnken model was used to investigate the impact of formulation conditions on vesicle size and drug entrapment. The optimized formulation showed a spherical shape with a vesicle size of 112.42 ± 2.1 nm and an entrapment efficiency of 94.34 ± 1.11%. Assessment of cytotoxic activities indicated that the optimized SMV-EMLs formula exhibited significantly lower half maximal inhibitory concentration (IC50) against MCF-7 cells. Cell cycle analysis indicated the accumulation of cells in the G2-M phase as well as increased cell fraction in the pre-G1 phase, suggesting an enhancement of anti-apoptotic activity of SMV. The staining of cells with Annex V revealed an increase in early and late apoptosis, in line with the increased cellular content of caspase-3 and Bax. In addition, the mitochondrial membrane potential (MMP) was significantly decreased. In conclusion, SMV-EMLs demonstrated superior cell death-inducing activity against MCF-7 cells compared to pure SMV. This is mediated, at least in part, by enhanced pro-apoptotic activity and MMP modulation of SMV.


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