scholarly journals Six New Diterpene Glycosides from the Soft Coral Lemnaliabournei

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 339
Author(s):  
Xia Yan ◽  
Han Ouyang ◽  
Te Li ◽  
Yutong Shi ◽  
Bin Wu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cell Lines ◽  
Soft Coral ◽  
Chemical Study ◽  
No Production ◽  
Cell Growth Inhibition ◽  
Isolation And Identification ◽  
Chemical Methods ◽  
Raw264.7 Macrophages ◽  
Low Cytotoxicity

A chemical study on the extracts of soft coral Lemnalia bournei resulted in the isolation and identification of six new bicyclic diterpene glycosides including three new lemnaboursides E–G (1–3), and three new lemnadiolboursides A–C (4–6), along with three known lemnaboursides (7–9). Their structures were elucidated by detailed spectroscopic analysis, ECD analysis, chemical methods, and comparison with the literature data. Lemnadiolboursides A–C (4–6) contained a lemnal-1(10)-ene-7,12-diol moiety compared with the lemnaboursides. All these compounds were evaluated for antibacterial activity; cell growth inhibition of A549, Hela, HepG2, and CCRF-CEM cancer cell lines; and inhibition of LPS-induced NO production in RAW264.7 macrophages. The results indicated that compounds 1, 2, and 4–6 exhibited antibacterial activity against Staphylococcus aureus and Bacillus subtilis (MIC 4–16 μg/mL); compounds 1–9 displayed low cytotoxicity on the CCRF-CEM cell lines (IC50 10.44–27.40 µM); and compounds 1, 2, and 5 showed weak inhibition against LPS-induced NO production (IC50 21.56–28.06 μM).

scholarly journals Effect of 1-Carbaldehyde-3,4-dimethoxyxanthone on Prostate and HPV-18 Positive Cervical Cancer Cell Lines and on Human THP-1 Macrophages

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3721
Author(s):  
Rui Medeiros ◽  
Bruno Horta ◽  
Joana Freitas-Silva ◽  
Jani Silva ◽  
Francisca Dias ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cervical Cancer ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Metabolic Activity ◽  
Cancer Cell Lines ◽  
No Production ◽  
Prostate Cell ◽  
Raw264.7 Macrophages

Xanthone derivatives have shown promising antitumor properties, and 1-carbaldehyde-3,4-dimethoxyxanthone (1) has recently emerged as a potent tumor cell growth inhibitor. In this study, its effect was evaluated (MTT viability assay) against a new panel of cancer cells, namely cervical cancer (HeLa), androgen-sensitive (LNCaP) and androgen-independent (PC-3) prostate cancer, and nonsolid tumor derived cancer (Jurkat) cell lines. The effect of xanthone 1 on macrophage functions was also evaluated. The effect of xanthone 1-conditioned THP-1 human macrophage supernatants on the metabolic viability of cervical and prostate cancer cell lines was determined along with its interference with cytokine expression characteristic of M1 profile (IL-1 ≤ β; TNF-α) or M2 profile (IL-10; TGF-β) (PCR and ELISA). Nitric oxide (NO) production by murine RAW264.7 macrophages was quantified by Griess reaction. Xanthone 1 (20 μM) strongly inhibited the metabolic activity of the cell lines and was significantly more active against prostate cell lines compared to HeLa (p < 0.05). Jurkat was the cell most sensitive to the effect of xanthone 1. Compound 1-conditioned IL-4-stimulated THP-1 macrophage supernatants significantly (p < 0.05) inhibited the metabolic activity of HeLa, LNCaP, and PC-3. Xanthone 1 did not significantly affect the expression of cytokines by THP-1 macrophages. The inhibiting effect of compound 1 observed on the production of NO by RAW 264.7 macrophages was moderate. In conclusion, 1-carbaldehyde-3,4-dimethoxyxanthone (1) decreases the metabolic activity of cancer cells and seems to be able to modulate macrophage functions.

scholarly journals Imidazole and Imidazolium Antibacterial Drugs Derived from Amino Acids

2020 ◽  
Vol 13 (12) ◽  
pp. 482
Author(s):  
Adriana Valls ◽  
Jose J. Andreu ◽  
Eva Falomir ◽  
Santiago V. Luis ◽  
Elena Atrián-Blasco ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cell Lines ◽  
Culture Media ◽  
Pure Water ◽  
Control Cell ◽  
Eukaryotic Cell ◽  
Imidazolium Salts ◽  
Bacterial Strains ◽  
Hek 293 ◽  
Low Cytotoxicity

The antibacterial activity of imidazole and imidazolium salts is highly dependent upon their lipophilicity, which can be tuned through the introduction of different hydrophobic substituents on the nitrogen atoms of the imidazole or imidazolium ring of the molecule. Taking this into consideration, we have synthesized and characterized a series of imidazole and imidazolium salts derived from L-valine and L-phenylalanine containing different hydrophobic groups and tested their antibacterial activity against two model bacterial strains, Gram-negative E. coli and Gram-positive B. subtilis. Importantly, the results demonstrate that the minimum bactericidal concentration (MBC) of these derivatives can be tuned to fall close to the cytotoxicity values in eukaryotic cell lines. The MBC value of one of these compounds toward B. subtilis was found to be lower than the IC50 cytotoxicity value for the control cell line, HEK-293. Furthermore, the aggregation behavior of these compounds has been studied in pure water, in cell culture media, and in mixtures thereof, in order to determine if the compounds formed self-assembled aggregates at their bioactive concentrations with the aim of determining whether the monomeric species were in fact responsible for the observed antibacterial activity. Overall, these results indicate that imidazole and imidazolium compounds derived from L-valine and L-phenylalanine—with different alkyl lengths in the amide substitution—can serve as potent antibacterial agents with low cytotoxicity to human cell lines.

Synthesis and Antibacterial Activity of Mefloquine-Based Analogs Against Sensitive and Resistant Mycobacterium tuberculosis Strains

2019 ◽  
Vol 19 (9) ◽  
pp. 683-689 ◽  
Author(s):  
Adriele da Silva Araújo ◽  
Adriana M. Moraes ◽  
Maria C.S. Lourenço ◽  
Cláudia O. Pessoa ◽  
Emerson T. da Silva ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Mycobacterium Tuberculosis ◽  
Cell Lines ◽  
Cancer Cell ◽  
Resistant Strain ◽  
Cancer Cell Lines ◽  
Active Compounds ◽  
Low Cytotoxicity ◽  
New Compounds

Background and Introduction:Mefloquine, a drug used to prevent and treat malaria is described possessing activity against the Mycobacterium tuberculosis (Mtb) as well as against multidrugresistant tuberculosis (MDR) and other types of bacteria. Despite their importance, few compounds based on the Mefloquine nucleus have been synthesized and evaluated against TB.Materials and Methods:For the synthesis of all the compounds based on the Mefloquine nucleus we used a synthetic route which utilized the key derivative 4-methoxy-2,8-bis(trifluoromethyl)quinoline 2 as starting material. The compounds 3 (a-c), 4 (a-b) were synthesized after one step by reaction of 2 with appropriate amines substituted. The chloro derivatives 5 and 6 were obtained from compounds 4b and 4a by treatment with SOCl2 in CH2Cl2 at reflux in 75 and 80% yield, respectively. The analogue 6 was converted to 7 after treatment with ethanolamine under heating at 90oC in 64% yield and to the azido derivative 8 in 56% after reaction with sodium azide in MeOH at reflux for 2 h. The analogue 9 was obtained after reaction of 5 with ethanolamine at 90oC for 1 h in 90% yield. All the new compounds were identified by detailed spectral data, including 1H NMR, 13C NMR and high resolution mass spectra. All the compound were evaluated for their in vitro antibacterial activity against sensitive Mycobacterium tuberculosis ATCC 27294, using the microplate Alamar Blue assay (MABA). The more active compounds 3c, 7, and 9 were also evaluated against resistant strain SR 2571/0215 (resistant to Rifampicin and Isoniazid) by above method. All compounds were tested against three cancer cell lines: SF-295 (glioblastoma), HCT-116 (colon) and PC-3 (prostate) using the MTT assay.Results:All the planned ten compounds were synthetically obtained in good global yield, displaying activity against sensitive Mycobacterium tuberculosis in vitro, with exception of one, with MIC values between 37.2 and 154.8 µM. The compounds 3c (37.2 µM), 7 (68.1 µM) and 9 (65.6 µM) showed the highest activity in this series with MIC values similar when compare to the standard Mefloquine (30 – 60 µM), being 3c the most potent. The more active compounds 3c, 7, and 9 were also evaluated against resistant strain, displaying MIC of 37.2, 136.2 and 65.6 µM, respectively. All compounds were tested against three cancer cell lines and showed low cytotoxicity.Conclusion:All synthesized compounds, with the exception of 5, exhibited activity against the Mtb. Compound 3c was the most potent against resistant and sensitive Mtb in this series, with MIC value of 37.2 µM. All compounds showed low cytotoxicity. These findings could be considered a good model to develop possible lead compounds in the fight against TB based on Mefloquine nucleus.

Antibacterial activity of some chemical constituents from Trichilia prieuriana (Meliaceae)

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Julio Issah Mawouma Pagna ◽  
Ines Michèle Kanko Mbekou ◽  
Armelle Tontsa Tsamo ◽  
Pierre Mkounga ◽  
Marcel Frese ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Ethyl Acetate ◽  
Shikimic Acid ◽  
Chemical Constituents ◽  
Chemical Study ◽  
Ethyl Acetate Fraction ◽  
Antibacterial Activities ◽  
Bacterial Strains ◽  
Isolation And Identification ◽  
Crude Extracts

Abstract The chemical study of hydroethanolic extracts from different parts of Trichilia prieuriana (Meliaceae) led to the isolation and identification of 22 compounds: 2β,3β,4β-trihydroxypregnan-16-one (1), prieurianin (2), flindissone (3), deoxyflindissone (4), picraquassin E (5), ursolic acid (6), 3β-acetoxy-11α-hydroxyurs-12-en (7), 3β-acetoxy-urs-12-en-11-one (8), 3β-acetoxy-β-amyrin (9), friedelin-3-ol (10), 3-oxo, friedelin (11), 3-oxo, fridelin-28-ol (12), oleanolic acid (13), hederagenin (14), mixture of stigmasterol (15), β-sitosterol (16), β-sitosterol-3-O-β-glucopyranoside (17) and stigmasterol-3-O-β-glucopyranoside (18), erythrodiol (19), scopoletin (20), 4-hydroxy-3,5-dimethoxybenzoic acid (21) and shikimic acid (22). The absolute configurations and crystal structures of compounds 1 and 2 are reported herein for the first time. Crude extracts, fractions and isolated compounds were evaluated for their antibacterial activities against nine bacterial strains. Crude extracts from the root wood of T. prieuriana exhibited good antibacterial potency with minimal inhibitory concentration (MIC) values ranging from 31.25 to 500 µg mL−1 on the test bacteria. The ethyl acetate fraction from root wood and n-hexane-ethyl acetate (3:1) fraction from leaves showed a moderate antibacterial activity with MIC value of 250 μg mL−1 on all test bacteria. Isolated compounds exhibited significant antibacterial activity with MIC values ranging from 4.09 to 71.8 µm. Compounds 3, 6 and 7 were the most active with a broad spectrum of activities.

Design, Synthesis and Docking Studies of Some Novel Fluoroquinolone Compounds with Antibacterial Activity

2018 ◽  
Vol 69 (4) ◽  
pp. 815-822 ◽  
Author(s):  
Lucia Pintilie ◽  
Amalia Stefaniu ◽  
Alina Ioana Nicu ◽  
Maria Maganu ◽  
Miron Teodor Caproiu
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Molecular Docking ◽  
Drug Discovery ◽  
Elemental Analysis ◽  
Docking Studies ◽  
Receptor Protein ◽  
Chemical Methods ◽  
Design Synthesis ◽  
Gram Negative

A new series of fluoroquinolone compounds have been obtained by Gould-Jacobs method. The compounds have been characterized by physic-chemical methods (elemental analysis, FTIR, NMR, UV-Vis) and by antimicrobial activity against Gram-positive and Gram-negative microorganisms. For the synthesized compounds have been performed calculations of characteristics and molecular properties, using Spartan�14 Software from Wavefunction, Inc. Irvine, CA. and molecular docking studies using CLC Drug Discovery Workbench 2.4 software, to identify and visualize the most likely interaction ligand (fluoroquinolone) with the receptor protein.

scholarly journals In Vitro Bioaccessibility of Bioactive Compounds from Citrus Pomaces and Orange Pomace Biscuits

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3480
Author(s):  
Adriana Maite Fernández-Fernández ◽  
Eduardo Dellacassa ◽  
Tiziana Nardin ◽  
Roberto Larcher ◽  
Adriana Gámbaro ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Total Phenol Content ◽  
No Production ◽  
Food Ingredient ◽  
Potential Health ◽  
Raw264.7 Macrophages ◽  
In Vitro Bioaccessibility ◽  
Health Promoting ◽  
Orange Pomace

The present investigation aimed to provide novel information on the chemical composition and in vitro bioaccessibility of bioactive compounds from raw citrus pomaces (mandarin varieties Clemenule and Ortanique and orange varieties Navel and Valencia). The effects of the baking process on their bioaccessibility was also assessed. Samples of pomaces and biscuits containing them as an ingredient were digested, mimicking the human enzymatic oral gastrointestinal digestion process, and the composition of the digests were analyzed. UHPLC-MS/MS results of the citrus pomaces flavonoid composition showed nobiletin, hesperidin/neohesperidin, tangeretin, heptamethoxyflavone, tetramethylscutellarein, and naringin/narirutin. The analysis of the digests indicated the bioaccessibility of compounds possessing antioxidant [6.6–11.0 mg GAE/g digest, 65.5–97.1 µmol Trolox Equivalents (TE)/g digest, and 135.5–214.8 µmol TE/g digest for total phenol content (TPC), ABTS, and ORAC-FL methods, respectively; significant reduction (p < 0.05) in Reactive Oxygen Species (ROS) formation under tert-butyl hydroperoxide (1 mM)-induced conditions in IEC-6 and CCD-18Co cells when pre-treated with concentrations 5–25 µg/mL of the digests], anti-inflammatory [significant reduction (p < 0.05) in nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 macrophages], and antidiabetic (IC50 3.97–11.42 mg/mL and 58.04–105.68 mg/mL for α-glucosidase and α-amylase inhibition capacities) properties in the citrus pomaces under study. In addition, orange pomace biscuits with the nutrition claims “no-added sugars” and “source of fiber”, as well as those with good sensory quality (6.9–6.7, scale 1–9) and potential health promoting properties, were obtained. In conclusion, the results supported the feasibility of citrus pomace as a natural sustainable source of health-promoting compounds such as flavonoids. Unfractionated orange pomace may be employed as a functional food ingredient for reducing the risk of pathophysiological processes linked to oxidative stress, inflammation, and carbohydrate metabolism, such as diabetes, among others.

scholarly journals Histatin-1 Attenuates LPS-Induced Inflammatory Signaling in RAW264.7 Macrophages

2021 ◽  
Vol 22 (15) ◽  
pp. 7856
Author(s):  
Sang Min Lee ◽  
Kyung-No Son ◽  
Dhara Shah ◽  
Marwan Ali ◽  
Arun Balasubramaniam ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Cytokine Production ◽  
Inflammatory Responses ◽  
Critical Role ◽  
Mapk Signaling ◽  
Response To Treatment ◽  
No Production ◽  
Inflammatory Signaling ◽  
Raw264.7 Macrophages ◽  
Inflammatory Mediator Production

Macrophages play a critical role in the inflammatory response to environmental triggers, such as lipopolysaccharide (LPS). Inflammatory signaling through macrophages and the innate immune system are increasingly recognized as important contributors to multiple acute and chronic disease processes. Nitric oxide (NO) is a free radical that plays an important role in immune and inflammatory responses as an important intercellular messenger. In addition, NO has an important role in inflammatory responses in mucosal environments such as the ocular surface. Histatin peptides are well-established antimicrobial and wound healing agents. These peptides are important in multiple biological systems, playing roles in responses to the environment and immunomodulation. Given the importance of macrophages in responses to environmental triggers and pathogens, we investigated the effect of histatin-1 (Hst1) on LPS-induced inflammatory responses and the underlying molecular mechanisms in RAW264.7 (RAW) macrophages. LPS-induced inflammatory signaling, NO production and cytokine production in macrophages were tested in response to treatment with Hst1. Hst1 application significantly reduced LPS-induced NO production, inflammatory cytokine production, and inflammatory signaling through the JNK and NF-kB pathways in RAW cells. These results demonstrate that Hst1 can inhibit LPS-induced inflammatory mediator production and MAPK signaling pathways in macrophages.

Cytokine and inflammatory mediators are associated with cytotoxic, anti-inflammatory and apoptotic activity of honeybee venom

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Mohamed A. Salama ◽  
Mohamed A. Younis ◽  
Roba M. Talaat
Keyword(s):  
Nitric Oxide ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hela Cells ◽  
No Production ◽  
Hep G2 ◽  
Normal Cells ◽  
Tnf Α ◽  
Ifn Γ ◽  
Mcf 7

AbstractObjectiveThe present study aimed to evaluate cytotoxic, apoptotic, and anti-inflammatory properties of bee venom (BV) as well as changes in cytokine secretion levels and nitric oxide (NO) production using three different cancer cell lines [liver (Hep-G2), breast (MCF-7), and cervical (HPV-18 infected HeLa cells)] and two normal cells (splenocytes and macrophages (MQ).MethodsCytotoxic activity of BV against tumor cell lines and normal splenocytes/MQ was tested by MTT assay. By ELISA (ELISA); Tumor necrosis factor (TNF-α), Interleukine (IL-10) and interferon (IFN-γ) were measured. Caspase three expressions was evaluated using reverse transcription-polymerase chain reaction (RT-PCR). Nitric oxide (NO) was estimated using a colorimetric assay.ResultsBV has a significant cytotoxic effect on all cell lines in a dose- and time-dependent manner; none of them was toxic for normal cells. Treating Hep-G2 cells with BV showed a reduction in IL-10, elevation in TNF-α with no change in IFN-γ level. MCF-7 cells have low IL-10 and TNF-α and high IFN-γ production level. Elevation of IL-10 and IFN-γ coincides with a reduction in TNF-α level was demonstrated in HeLa cells. The expression of Caspase three was dramatically increased with elevation in BV concentration in all tested cancer cell lines. A gradual decrease in NO production by MQ with increasing BV dose was observed.ConclusionTaken together, our results stressed on the importance of BV as a potent anti-tumor agent against various types of cancers (Liver, Breast, and Cervix). Further steps towards the use of BV for pharmacological purposes must be done.

scholarly journals Pogonatherumol, a Novel Highly Oxygenated Norsesquiterpene with Flavone C-Glycosides from Pogonatherum crinitum

2018 ◽  
Vol 2018 ◽  
pp. 1-3
Author(s):  
Lin Ni ◽  
Wei Huang ◽  
He-shan Wang ◽  
Hui-you Xu
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Peritoneal Macrophage ◽  
Spectroscopic Data ◽  
Human Cancer ◽  
Mouse Peritoneal Macrophage ◽  
No Production ◽  
Human Cancer Cell ◽  
X Ray ◽  
Human Cancer Cell Lines

A novel highly oxygenated norsesquiterpene, pogonatherumol (1), with two known flavone C-glycosides (2-3), was isolated from Pogonatherum crinitum. The structure of the new compound was illuminated based on its spectroscopic data and X-ray analysis. Compounds 1 and 3 inhibited NO production in the mouse peritoneal macrophage (64.5 ± 7.2% and 61.6 ± 5.8%, respectively, at a concentration of 50 μM). The three compounds were inactive when tested against two human cancer cell lines (IC50 values > 50 μM).

scholarly journals Evaluation of the Biological Activity of Nickel Oxide Nanoparticles as Antibacterial and Anticancer Agents

2020 ◽  
pp. 2888-2896
Author(s):  
Maha Fakhry Altaee ◽  
Laith A. Yaaqoob ◽  
Zaid K. Kamona
Keyword(s):  
Antibacterial Activity ◽  
Nickel Oxide ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Lines ◽  
Oxide Nanoparticles ◽  
Caspase 9 ◽  
Nickel Oxide Nanoparticles ◽  
Nio Nps

In the present study, nickel oxide nanoparticles (NiO NPs) were evaluated as an antibacterial and anticancer agent. The nanoparticles of nikel oxide were synthesized using aloe vera leaves extract and characterized with AFM (showing an average diameter of 45.11 nm), XRD and FE-SEM analyses. Three different concentrations (125, 250 and 500 µg/ml) were prepared from the synthesized NiO NPs and investigated for their potential antibacterial activity against both Enterococcus faecalis (Gram-positive bacteria) and Acinobacter baumannii (Gram-negative bacteria). While cytotoxicity and apoptotic activity were measured on both MCF-7 and AMJ13 cancer cell lines by  MTT and caspase-9 luminescence assays. The results showed that NiO NPs inhibit bacterial growth, as indicated by large inhibition zones  against both tested bacteria, with all studied concentrations. Moreover, the results of cytotoxicity and caspase-9 activity assays were in concordance with those of  antibacterial activity, showing high cytotoxicity and apoptotic effects against both of the studied cancer cell lines and with all the tested concentrations of NiO NPs. Both the antibacterial and anticancer activities of NiO NPs were dose-dependent. 

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