scholarly journals Antimicrobial Activity, Cytotoxicity and Chemical Constituents of the Freshwater Microalga Oscillatoria princeps

2021 ◽  
Vol 12 (1) ◽  
pp. 961-977
Keyword(s):  
Antimicrobial Activity ◽  
Anticancer Activity ◽  
Hepg2 Cell ◽  
Chemical Constituents ◽  
Octadecenoic Acid ◽  
Bioactive Metabolites ◽  
Diethyl Ether Extract ◽  
Successive Extraction ◽  
Ic50 Values ◽  
Promising Source

The microalgae Oscillatoria sp. are promising sources of bioactive metabolites used in both pharmaceutical and nutraceutical applications. The main objective of present study is to determine the antimicrobial activity, cytotoxicity, and chemical profile of Oscillatoria princeps r extracts and its fractions. O. princeps extracts were prepared by successive extraction method, and chemical constituents were identified using GC-MS. Diethyl ether extract (DEE) had antimicrobial activity against all tested microorganisms and the highest inhibition zones 20.7 and 20.2 mm was observed against P. aeruginosa and A. flavus, respectively. Also, DEE showed an anticancer activity with IC50 values of 35.18, 46.6, and 79.18 µg ml-1 against breast cancer (MCF7), colon cancer (HCT116), and hepatocellular carcinoma (HePG2) cell lines, respectively. By DEE fractionation, fraction F7 showed the highest antimicrobial activity followed by fraction F4 with minimum inhibitory concentration (MIC) values ranged between 0.5 and 1.9 mg ml-1. Fraction F4 recorded anticancer activity against HCT116, MCF7, and HePG2 with IC50 of 22.62, 24.43, and 102.52 µg ml-1, respectively. While fraction F7 had anticancer activity against HCT116 and MCF7 without any effect on the HePG2 cell line. GC-MS analysis of fractions F4 and F7 represented that the main compounds responsible for the bioactivity were Pentadeconic acid,4-hexadecyl ester, and 9-Octadecenoic acid in F4, while the main compounds in F7 were Quercetin 7,3',4'-trimethoxy and Methyl tetradecanoate. The study concluded that O. princeps DEE extract and fractions had a sufficient amount of bioactive compounds that possess antimicrobial and anticancer activity, which could be a promising source for pharmaceutical and nutraceutical ingredients.

scholarly journals Characterization and Antimicrobial Activity of a Halophyte from the Asturian Coast (Spain): Limonium binervosum (G.E.Sm.) C.E.Salmon

Plants ◽  
2021 ◽  
Vol 10 (9) ◽  
pp. 1852
Author(s):  
Eva Sánchez-Hernández ◽  
Laura Buzón-Durán ◽  
Natalia Langa-Lomba ◽  
José Casanova-Gascón ◽  
Belén Lorenzo-Vidal ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Bioactive Metabolites ◽  
Tetradecanoic Acid ◽  
Diplodia Seriata ◽  
Flower Extract ◽  
Sea Lavender ◽  
Xylophilus Ampelinus ◽  
Gas Chromatography Mass Spectroscopy ◽  
Promising Source

The work presented herein deals with the characterization and valorization of a halophyte from the cliffs of the Asturian coast: Limonium binervosum (G.E.Sm.) C.E.Salmon (rock sea-lavender). Its biomass and hydromethanolic extracts were studied by elemental and thermal analysis, infrared spectroscopy and gas chromatography–mass spectroscopy. Tetradecanoic acid/esters and 1,2-tetradecanediol were identified in its flower extract, while the leaf extract was rich in linolenic and linoleic acids and their esters, hexadecanoic acid and its esters, and phytol. Both flower and leaf hydromethanolic extracts contained eicosane, sitosterol and tocopherols in significant amounts. With a view to its valorization, the antimicrobial activity of these extracts was investigated against three apple tree and grapevine phytopathogens. Both the hydroalcoholic extracts and their main constituents, alone or in combination with chitosan oligomers (COS), were tested in vitro. A remarkable antibacterial activity was observed for the conjugated complexes of the flower extract with COS, both against Xylophilus ampelinus (MIC = 250 μg·mL−1) and Erwinia amylovora (MIC = 500 μg·mL−1), and complete inhibition of the mycelial growth of Diplodia seriata was found at concentrations <1000 μg·mL−1. In view of these results, this extremophile plant can be put forward as a promising source of bioactive metabolites.

scholarly journals Anti-Hepatocellular-Cancer Activity Exerted by β-Sitosterol and β-Sitosterol-Glucoside from Indigofera zollingeriana Miq

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 3021
Author(s):  
Tuong Kha Vo ◽  
Qui Thanh Hoai Ta ◽  
Quang Truyen Chu ◽  
Thuy Trang Nguyen ◽  
Van Giau Vo
Keyword(s):  
Anticancer Activity ◽  
Chemical Constituents ◽  
Hepatocellular Cancer ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Huh7 Cells ◽  
Primary Fibroblasts ◽  
Ic50 Values ◽  
Normal Human ◽  
Indigofera Zollingeriana

Indigofera zollingeriana Miq (I. zollingeriana) is a widely grown tree in Vietnam. It is used to cure various illnesses. The purpose of this study was to investigate the chemical constituents of an I. zollingeriana extract and test its anticancer activity on hepatocellular cells (Huh7 and HepG2). The experimental results of the analysis of the bioactive compounds revealed that β-sitosterol (β-S) and β-sitosterol-glucoside (β-SG) were the main ingredients of the I. zollingeriana extract. Regarding anticancer activity, the β-S and β-SG of I. zollingeriana were found to exhibit cytotoxic effects against HepG2 and Huh7 cells, but not against normal human primary fibroblasts. The β-S was able to inhibit the proliferation of HepG2 and Huh7 cells in a dose-dependent manner with half-maximal inhibitory concentration (IC50) values of 6.85 ± 0.61 µg/mL and 8.71 ± 0.21 µg/mL, respectively (p < 0.01), whereas the β-SG IC50 values were 4.64 ± 0.48 µg/mL for HepG2 and 5.25 ± 0.14 µg/mL for Huh7 cells (p < 0.01). Remarkably, our study also indicated that β-S and β-SG exhibited cytotoxic activities via inducing apoptosis and activating caspase-3 and -9 in these cells. These findings demonstrated that β-S and β-SG from I. zollingeriana could potentially be developed into promising therapeutic agents to treat liver cancer.

Computer-aided structural optimization, synthesis, evaluation of the antimicrobial and cytotoxic activity of some pyrazoline derivatives

MedPharmRes ◽  
2021 ◽  
Vol 6 (1) ◽  
pp. 33-39
Author(s):  
Tai Duc Nguyen ◽  
Du Nguyen Hai Ly ◽  
Thi Hong Tuoi Do ◽  
Phuong Thi Ngoc Huynh
Keyword(s):  
Antimicrobial Activity ◽  
Anticancer Activity ◽  
Antibacterial Activities ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Moderate Activity ◽  
Docking Model ◽  
Ic50 Values ◽  
Relationship Of

Introduction: In the last few decades, pyrazoline-based substances have emerged as potential antimicrobial and anticancer candidates. In concern with antimicrobial activity, this study aims to build a docking model to predict the structure of potential 2-pyrazoline derivatives. The cytotoxicity of some compounds was also evaluated to get insight into the structure–anticancer activity relationship of the 2-pyrazoline derivatives. Methods: Docking models were built on virtual FabH enzymes using FlexX platform with 2-pyrazoline derivatives served as test sets. Afterward, derivatives with high docking scores were chemically synthesized and evaluated for antibacterial activity using the agar dilution method. Furthermore, MTT assay was used to assess the cytotoxicity of these compounds. Results: The docking score and the in vitro minimum inhibitory concentration (MIC) value on Staphylococcus aureus (S. aureus) bacteria strongly correlate with an R-square value of 0.6751 (p < 0.0001). Four 2 pyrazoline derivatives were synthesized and evaluated for antimicrobial activity. Their MIC values on S. aureus range between 4 and 16 μg/mL, consistent with ones predicted by the docking model. Apropos cytotoxic properties, a series of 2-pyrazolines exhibit a moderate activity on HepG2, RD, and MDA-MB-231. The most active compound, HP10, has the IC50 values on these cell lines. which are 26.62 μM, 17.74 μM, 14.47 μM, respectively. Conclusion: Our research built a docking model on the virtual S. aureus FabH enzyme with high potential in predicting antibacterial activities of different 2-pyrazoline derivatives. Moreover, our cytotoxicity results provided data for further studies on the anticancer activity of these promising derivatives.

scholarly journals Biosurfactant Production by Marine Actinomycetes Isolates Streptomyces Althioticus RG3 and Streptomyces Californicus RG8 as a Promising Source of Antimicrobial and Antifouling Effects

2021 ◽  
Author(s):  
Mohamed Al-agamy ◽  
Moaz M Hamed ◽  
Mohammad R Alhuzani ◽  
Asmaa M Youssif
Keyword(s):  
Antimicrobial Activity ◽  
Bioactive Metabolites ◽  
Diffusion Method ◽  
Gulf Of Suez ◽  
Marine Actinomycetes ◽  
Alkaline Conditions ◽  
Pharmaceutical Industries ◽  
Metabolites Production ◽  
The Stability ◽  
Promising Source

Abstract Background: Because of the ability of their bioactive metabolites production, many researchers were attracted to investigate and isolating marine actinomycetes from unique location with a unique environment. Information on antimicrobial activity and antifouling agents by Streptomyces sp. from the Ras Garib area, Gulf of Suez, Egypt is limited. One of the metabolites produced by the actinomycetes was biosurfactant. This paper describes the possibility of marine actinomycetes isolates for the production of biosurfactants, In addition to the possibility of using it as antimicrobial and antifouling agents.Results: Marine actinobacterial isolates RG3 and RG8 had emulsification indexes of 76 and 68%, respectively. The two marine actinobacterial isolates were identified using 16srDNA as Streptomyces althioticus RG3 and Streptomyces californicus RG8, and submitted in the database of genetic information with accession number MW661230 and MW661234, respectively. Biosurfactants were stable at 10% NaCl, in case of Streptomyces althioticus RG3 and stable at 10%–15% NaCl in the case of Streptomyces californicus RG8. A temperature of 35℃ was suitable for the stability of biosurfactants produced by both strains. Both strains produced the most biosurfactant when exposed to alkaline conditions. We characterized the biosurfactants produced by both strains including features such as the chemical composition of the biosurfactants and FTIR analysis. The antimicrobial activity of biosurfactants extract evaluated using a well diffusion method against Vibrio alginolyticus MK170250, Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 4027, and Staphylococcus aureus ATTC 25923. Streptomyces althioticus RG3 biosurfactants have been shown to have better antimicrobial activity than Streptomyces californicus RG8, indicating that they may be used in pharmaceutical industries and in the manufacture of antifouling products.Conclusions: Streptomyces althioticus RG3 and Streptomyces californicus RG8, isolated from Ras Garib, Gulf of Suez, Egypt, were able to develop very stable biosurfactants under stress conditions, which could be useful in a variety of industries such as pharmaceuticals and antifouling manufacturing.

scholarly journals Antioxidant, antimicrobial and cytotoxicity of nhexane extract from Mollugo nudicaulis Lam.

2021 ◽  
Vol 17 (5) ◽  
pp. 573-582
Author(s):  
Siva Shankar Raj ◽  
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Plant Extract ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Hexane Extract ◽  
A2780 Cell ◽  
Ic50 Values

The antioxidant, antimicrobial and anticancer activity of n-hexane extract of Mollugo nudicaulis Lam. is of interest. The antioxidant activity of the extract was determined by separate methods of radical scavenging assays. Antimicrobial activity was analyzed by disc diffusion method on fungi species, gram positive and negative species. The anticancer potential of plant extract was evaluated on A2780 cell lines by MTT assay. Results exposed that, the n-hexane extract of M.nudicaulis possess comparable significant antioxidant activity with IC50 values of 12.79ą0.82, 36.65ą0.03 and 19.59ą0.26 μg/mL, on DPPH, nitric oxide and hydroxyl radical scavenging assays respectively, and also possess notable reducing power of 0.84ą0.04 (Reducing power assay) and 0.75ą0.02 (FRAB assay) at the maximum concentration of 200 μg/mL of the n-hexane extract. Antimicrobial activity of extract exhibited maximum zone of inhibition ranged from 11.1 ą 0.3 to 14 .5ą 0.3 mm on tested microorganism. The anticancer activity of plant extract found to be strong cell growth inhibitory activity with minimal IC50 values of 32.46ą0.92 μg/mL on A2780 cell lines. Collectively this study can be concluded that, the n-hexane extract of M.nudicaulis might act as possible antioxidant, antimicrobial and anticancer agents.

scholarly journals Chemical Compostions of Essential Oils and Antimicrobial Activity of Hyptis suaveolens (L.) Poit. (Lamiaceae) from Vietnam

2020 ◽  
pp. 114-123 ◽  
Author(s):  
Nguyen Thanh Chung ◽  
Le Thi Huong ◽  
Do Ngoc Dai ◽  
Isiaka Ajani Ogunwande
Keyword(s):  
Gas Chromatography ◽  
Antimicrobial Activity ◽  
Essential Oils ◽  
Antimicrobial Agents ◽  
Chemical Constituents ◽  
Authentic Sample ◽  
Moderate Activity ◽  
Hyptis Suaveolens ◽  
Ic50 Values ◽  
Leaf Oil

Aims: This present study described the chemical constituents and antimicrobial activity of essential oils hydrodistiled from the leaves and flowers of Hyptis suaveolens (L.) Poit. Study Design: This research was designed to accommodate different stages such as collection of authentic sample of Hyptis suaveolens, obtain essential oil by hydrodistillation, chemical analysis of the oil samples by gas chromatography (GC) and gas chromatography coupled with mass spectrometry (GC/MS) and screening of the essential oils for antimicrobial activity. Place and Duration of Study: School of Natural Science, Vinh University, Vinh City, Nghệ An Province, Vietnam, between August and December 2018. Methodology: The leaves and flowers of H. suaveolens used for this study were gotten from Đồng Văn Commune, Pù Hoạt Nature Reserve, Vietnam. The collection was done in December 2018. Essential oils were distilled off using hydrodistillation method according to established procedure. The determination of antimicrobial efficacy of essential oils of H. suaveolens will be achieved by the method of microdilution broth susceptibility assay. The minimum inhibitory concentration (MIC) and IC50 were evaluated accordingly. Results: The major compounds in the oil were b-caryophyllene (31.1% and 33.7%), caryophyllene oxide (17.6% and 3.9%), phytol (9.9% and 2.7%) and a-humulene (6.7% and 6.6%), respectively. The leaf oil displayed strong antimicrobial activity against Enterococcus faecalis ATCC299212, Bacillus cereus ATCC14579 and Candida albicans ATCC10231 with minimum inhibitory concentrations (MIC) of 16.0, 32.0 and 16.0 µg/mL respectively, while the IC50 values were 5.78, 9.35 and 6.78 µg/mL, respectively. The flower oil showed activity  towards the same organisms with MIC values of 64.0, 64.0 and 16.0 µg/mL, respectively;   with IC50 values of 20.45, 26.78 and 6.78 µg/mL, respectively. Both essential oils exhibited moderate activity towards Staphylococcus aureus ATCC25923 with MIC of 256.0 µg/mL. Conclusion: The results are indication of the potential of H. suaveolens essential oils as source of antimicrobial agents.

Isolation of New Glycosides from Anemarrhena Asphodeloides Rhizome and Screening of their Anticancer Activity

2019 ◽  
Vol 16 (6) ◽  
pp. 474-477 ◽  
Author(s):  
Pham Van Khang ◽  
Nguyen Thi Hien Lan ◽  
Le Quang Truong ◽  
Mai Thi Minh Chau ◽  
Mai Xuan Truong ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Spectral Data ◽  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
Ic50 Values ◽  
Nmr Techniques ◽  
Inhibitory Activities ◽  
Anemarrhena Asphodeloides

In this report, two new steroidal glycosides were isolated and determined from n-butanol fraction of A.asphodeloides. The structures were confirmed in comparison with the spectral data of known compounds by using different spectroscopic analysis approaches including 1D & 2D-NMR techniques and HRMS. The anti-proliferation screening against cancer cell lines A549 and HeLa indicated that compound 1 exhibited good inhibitory activities with IC50 values of 0.79 and 0.55 &#181;g/mL, respectively.

Naphthoquinone-based hydrazone hybrids: synthesis and potent activity against cancer cell lines

2020 ◽  
Vol 16 ◽  
Author(s):  
Délis Galvão Guimarães ◽  
Arlan de Assis Gonsalves ◽  
Larissa Araújo Rolim ◽  
Edigênia Cavalcante Araújo ◽  
Victória Laysna dos Anjos Santos ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Supporting Electrolyte ◽  
Cancer Cell Lines ◽  
Molecular Structures ◽  
Cytotoxic Activities ◽  
Electrochemical Studies ◽  
Ic50 Values

Background: Natural naphthoquinones have shown diversified biological activities including antibacterial, antifungal, antimalarial, and cytotoxic activities. However, they are also compounds with acute cytotoxicity, immunotoxicity, carcinogenesis, and cardio- and hepatotoxicity, then the modification at their redox center is an interesting strategy to overcome such harmful activity. Objective: In this study, four novel semisynthetic hydrazones, derived from the isomers α- and β-lapachones (α and β, respectively) and coupled with the drugs hydralazine (HDZ) and isoniazid (ACIL), were prepared, evaluated by electrochemical methods and assayed for anticancer activity. Method: The semisynthetic hydrazones were obtained and had their molecular structures established by NMR, IR, and MS. Anticancer activity was evaluated by cell viability determined by reduction of 3-(4,5-dimethyl-2-thiazol)-2,5-diphenyl-2H-tetrazolium bromide (MTT). The electrochemical studies, mainly cyclic voltammetry, were performed, in aprotic and protic media. Result: The study showed that the compounds 2, 3, and 4 were active against at least one of the cancer cell lines evaluated, being compounds 3 and 4 the most cytotoxic. Toward HL-60 cells, compound 3 was 20x more active than β-lapachone, and 3x more cytotoxic than doxorubicin. Furthermore, 3 showed an SI value of 39.62 for HL-60 cells. Compound 4 was active against all cancer cells tested, with IC50 values in the range 2.90–12.40 μM. Electrochemical studies revealed a profile typical of self-protonation and reductive cleavage, dependent on the supporting electrolyte. Conclusion: These results therefore indicate that compounds 3 and 4 are strong candidates as prototypes of new antineoplastic drugs.

Chemical Constituents from Chloranthus elatior and Their Inhibitory Effect on Human Dihydroorotate Dehydrogenase

Planta Medica ◽  
2021 ◽  
Author(s):  
Qian Yang ◽  
An Jia ◽  
Xizi Liu ◽  
Shiyi Han ◽  
Siyang Fan
Keyword(s):  
Circular Dichroism ◽  
Chemical Constituents ◽  
Inhibitory Effect ◽  
Mass Spectrometric ◽  
Dihydroorotate Dehydrogenase ◽  
Active Compounds ◽  
Electronic Circular Dichroism ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Circular Dichroïsm

AbstractA new sesquiterpene, chlorantholide G (1), a new sesquiterpene dimer, elatiolactone (2), and 2 new diterpenes, elatiorlabdane B (3) and elatiorlabdane C (4), together with 51 known compounds, were isolated from the aerial parts of Chloranthus elatior. The new structures including their absolute configurations were mainly established by mass spectrometric, NMR, and electronic circular dichroism experiments. All isolated compounds were tested for their anti-hDHODH activity. (4S,6R)-4-hydroxy-6-isopropyl-3-methylcyclohex-2-enone (5) and (4S,5R,9S,10R)-8(17),12,14-labdatrien-18-oic acid (29) were the most active compounds with IC50 values of 18.7 and 30.7 µM, respectively.

scholarly journals Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors

Antibiotics ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 162
Author(s):  
Ahmed Ragab ◽  
Sawsan A. Fouad ◽  
Ola A. Abu Ali ◽  
Entsar M. Ahmed ◽  
Abeer M. Ali ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Fungal Growth ◽  
Dna Gyrase ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Dhfr Inhibitors ◽  
Positive Controls

Herein, a series of novel hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a–d, pyridine-2-one 3–10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis. All the synthesized compounds showed moderate to good antimicrobial activity against eight pathogens. The most promising six derivatives, 2a, 2b, 2d, 3a, 8, and 11, revealed to be best in inhibiting bacterial and fungal growth, thus showing bactericidal and fungicidal activity. These derivatives exhibited moderate to potent inhibition against DNA gyrase and DHFR enzymes, with three derivatives 2d, 3a, and 2a demonstrating inhibition of DNA gyrase, with IC50 values of 18.17–23.87 µM, and of DHFR, with IC50 values of 4.33–5.54 µM; their potency is near to that of the positive controls. Further, the six derivatives exhibited immunomodulatory potential and three derivatives, 2d, 8, and 11, were selected for further study and displayed an increase in spleen and thymus weight and enhanced the activation of CD4+ and CD8+ T lymphocytes. Finally, molecular docking and some AMED studies were performed.

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