scholarly journals Synthesis, Cytotoxicity and Anti−Proliferative Activity Against AGS Cells of New 3(2H)−Pyridazinone Derivatives Endowed with a Piperazinyl Linker

2021 ◽  
Vol 14 (3) ◽  
pp. 183
Author(s):  
Mehmet Abdullah Alagöz ◽  
Zeynep Özdemir ◽  
Mehtap Uysal ◽  
Simone Carradori ◽  
Marialucia Gallorini ◽  
...  
Keyword(s):  
Morphological Changes ◽  
Biological Effects ◽  
Phenyl Group ◽  
Positive Control ◽  
Ags Cells ◽  
Cancerous Cell ◽  
Cell Blebbing ◽  
Microscopy Analysis ◽  
Light Microscopy Analysis ◽  
Pyridazinone Derivatives

Novel twenty−three 3(2H)−pyridazinone derivatives were designed and synthesized based on the chemical requirements related to the anti−proliferative effects previously demonstrated within this scaffold. The introduction of a piperazinyl linker between the pyridazinone nucleus and the additional (un)substituted phenyl group led to some compounds endowed with a limited cytotoxicity against human gingival fibroblasts (HGFs) and good anti−proliferative effects against gastric adenocarcinoma cells (AGS) as evaluated by MTT and LDH assays, using doxorubicin as a positive control. Successive analyses revealed that the two most promising representative compounds (12 and 22) could exert their effects by inducing oxidative stress as demonstrated by the hydrogen peroxide release and the morphological changes (cell blebbing) revealed by light microscopy analysis after the haematoxylin−eosin staining. Moreover, to further assess the apoptotic process induced by compounds 12 and 22, Bax expression was measured by flow cytometry. These findings enlarged our knowledge of the structural requirements in this scaffold to display valuable biological effects against cancerous cell lines.

scholarly journals The Discrepancy between Clove and Non-Clove Cigarette Smoke-Promoted Candida albicans Biofilm Formation with Precoating RNA-aptamer

F1000Research ◽  
2021 ◽  
Vol 10 ◽  
pp. 372
Author(s):  
Boy Muchlis Bachtiar ◽  
Basri A. Gani ◽  
Astri Deviana ◽  
Nastiti Rilo Utami ◽  
Anissa Dien Andriyani ◽  
...  
Keyword(s):  
Cigarette Smoke ◽  
Growth Medium ◽  
Biofilm Formation ◽  
Morphological Changes ◽  
Inhibitory Effect ◽  
Yeast Cells ◽  
Hypha Formation ◽  
Microscopy Analysis ◽  
Light Microscopy Analysis ◽  
Biofilm Development

This study explores the influence of precoating aptamer (Ca-apt1) on C. albicans viability while the fungus was growing in the presence of exposing condensed cigarette smoke (CSC), prepared from clove (CCSC) and non-clove (NCSC) cigarettes, for 48 h. Using qPCR, we found that mRNA expression of adhesion-associated genes (ALS3 and HWP1) was impaired by precoating C. albicans yeast cells with the aptamer. Conversely, the gene transcription was upregulated when aptamer-uncoated yeast was pre-treated with either CSC. In addition, by analysing the result of MTT ([3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide] assay, we found that the presence of added CCSC or NCSC in growth medium for 48 h was significantly enhanced C. albicans biofilm development. However, the presence of precoated aptamer was significantly impaired biofilm development accelerated by the NCSC. The inhibitory effect of the Ca-apt1 was not dependent on the precoated aptamer (1 and 10%). Interestingly, we noted that the enhancer effect of treated CCSC was no longer effective when the yeast had been precoated with 10% aptamer tested. Additionally, light microscopy analysis revealed that precoating aptamer alleviates morphological changes of C. albicans (from yeast to hypha formation) that are enhanced by adding CCSC or NCSC in the growth medium. In conclusion, these results suggest that administration on Ca-ap1 exhibits a significant protective effect on CSC-induced biofilm formation by C. albicans.

scholarly journals The Discrepancy between Clove and Non-Clove Cigarette Smoke-Promoted Candida albicans Biofilm Formation with Precoating RNA-aptamer

F1000Research ◽  
2021 ◽  
Vol 10 ◽  
pp. 372
Author(s):  
Boy Muchlis Bachtiar ◽  
Basri A. Gani ◽  
Astri Deviana ◽  
Nastiti Rilo Utami ◽  
Anissa Dien Andriyani ◽  
...  
Keyword(s):  
Cigarette Smoke ◽  
Growth Medium ◽  
Biofilm Formation ◽  
Morphological Changes ◽  
Inhibitory Effect ◽  
Yeast Cells ◽  
Hypha Formation ◽  
Microscopy Analysis ◽  
Light Microscopy Analysis ◽  
Biofilm Development

This study explores the influence of precoating aptamer (Ca-apt1) on C. albicans viability while the fungus was growing in the presence of exposing condensed cigarette smoke (CSC), prepared from clove (CCSC) and non-clove (NCSC) cigarettes, for 48 h. Using qPCR, we found that mRNA expression of adhesion-associated genes (ALS3 and HWP1) was impaired by precoating C. albicans yeast cells with the aptamer. Conversely, the gene transcription was upregulated when aptamer-uncoated yeast was pre-treated with either CSC. In addition, by analysing the result of MTT ([3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide] assay, we found that the presence of added CCSC or NCSC in growth medium for 48 h was significantly enhanced C. albicans biofilm development. However, the presence of precoated aptamer was significantly impaired biofilm development accelerated by the NCSC. The inhibitory effect of the Ca-apt1 was not dependent on the precoated aptamer (1 and 10%). Interestingly, we noted that the enhancer effect of treated CCSC was no longer effective when the yeast had been precoated with 10% aptamer tested. Additionally, light microscopy analysis revealed that precoating aptamer alleviates morphological changes of C. albicans (from yeast to hypha formation) that are enhanced by adding CCSC or NCSC in the growth medium. In conclusion, these results suggest that administration on Ca-ap1 exhibits a significant protective effect on CSC-induced biofilm formation by C. albicans.

scholarly journals The discrepancy between Clove and Non-Clove Cigarette Smoke-Promoted Candida albicans Biofilm Formation with precoating RNA-aptamer

F1000Research ◽  
2021 ◽  
Vol 10 ◽  
pp. 372
Author(s):  
Boy Muchlis Bachtiar ◽  
Basri A. Gani ◽  
Astri Deviana ◽  
Nastiti Rilo Utami ◽  
Anissa Dien Andriyani ◽  
...  
Keyword(s):  
Cigarette Smoke ◽  
Growth Medium ◽  
Biofilm Formation ◽  
Morphological Changes ◽  
Inhibitory Effect ◽  
Yeast Cells ◽  
Hypha Formation ◽  
Microscopy Analysis ◽  
Light Microscopy Analysis ◽  
Biofilm Development

This study explores the influence of precoating aptamer (Ca-apt1) on C. albicans viability while the fungus was growing in the presence of exposing condensed cigarette smoke (CSC), prepared from clove (CCSC) and non-clove (NCSC) cigarettes, for 48 h. Using qPCR, we found that mRNA expression of adhesion-associated genes (ALS3 and HWP1) was impaired by precoating C. albicans yeast cells with the aptamer. Conversely, the gene transcription was upregulated when aptamer-uncoated yeast was pre-treated with either CSC. In addition, by analysing the result of MTT ([3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide] assay, we found that the presence of added CCSC or NCSC in growth medium for 48 h was significantly enhanced C. albicans biofilm development. However, the presence of precoated aptamer was significantly impaired biofilm development accelerated by the NCSC. The inhibitory effect of the Ca-apt1 was not dependent on the precoated aptamer (1 and 10%). Interestingly, we noted that the enhancer effect of treated CCSC was no longer effective when the yeast had been precoated with 10% aptamer tested. Additionally, light microscopy analysis revealed that precoating aptamer alleviates morphological changes of C. albicans (from yeast to hypha formation) that are enhanced by adding CCSC or NCSC in the growth medium. In conclusion, these results suggest that administration on Ca-ap1 exhibits a significant protective effect on CSC-induced biofilm formation by C. albicans.

PHYTOCHEMICAL SCREENING, ANTIOXIDANT, ANTI-CYTOTOXIC AND ANTICANCER EFFECTS OF GALINSOGA PARVIFLORA AND VERNONIA POLYANTHES (ASTERACEAE) EXTRACTS

2020 ◽  
Vol 8 (10) ◽  
pp. 84-98
Author(s):  
Sula M. V. Feleti ◽  
Renê L. Aleluia ◽  
Suiany V. Gervásio ◽  
Jean Carlos V. Dutra ◽  
Jessica R. P. Oliveira ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Phenolic Acids ◽  
Unsaturated Fatty Acids ◽  
Biological Effects ◽  
Human Lymphocytes ◽  
Chemical Characterization ◽  
Total Content ◽  
Ags Cells ◽  
Ft Icr Ms ◽  
Ft Icr

The study was designed to investigate the chemical composition and the biological effects of G. parviflora and V. polyanthes ethanolic extracts in vitro. Total content of phenols, flavonoids and tannins was quantified by spectrophotometry; chemical characterization was permed by mass spectrometry (ESI (-) FT-ICR MS and APCI (+) FT-ICR MS analysis). Antioxidant activities were determined by FRAP and Fe2+ chelating methods. Extracts cytotoxicity was evaluated in human lymphocytes, sarcoma-180 (S-180) and human gastric adenocarcinoma (AGS) cells, by MTT assay. V. polyanthes presented higher total content of tannins and G. parviflora presented higher amount of phenols and flavonoids. Chemical characterization showed the presence of flavonoids, phenolic acids and sesquiterpene lactones in V. polyanthes extract, and steroids, phenolic acids and fatty acids (Poly Unsaturated Fatty Acids - PUFA) in G. parviflora extract. V. polyanthes extract stood out in the Fe2+ chelation test. G. parviflora extract did not present outstanding antioxidant results in the tested protocols. Both species showed a tendency to promote cytotoxicity in human lymphocyte cells. Regarding the antiproliferative effect, both species were able to reduce S-180 cell viability and G. parviflora extract showed high antiproliferative potential in the assay with AGS cells. These findings reinforce the medicinal use of these plants, as well as suggest their potential use for the development of new drugs and for the treatment of cancers.

scholarly journals Morphological changes and bioaccumulation in response to cadmium exposure in Morchella spongiola, a fungus with potential for detoxification

2021 ◽  
Author(s):  
Hongyan Xu ◽  
Jing Guo ◽  
Qing Meng ◽  
Zhanling Xie
Keyword(s):  
Electron Microscopy ◽  
Morphological Changes ◽  
Intracellular Accumulation ◽  
Tolerance Mechanism ◽  
Edible Fungi ◽  
Transmission Electron Microscopy Analysis ◽  
Transmission Electron ◽  
Electron Microscopy Analysis ◽  
Microscopy Analysis ◽  
Micro Morphology

<i>Morchella</i> is a genus of edible fungi with strong resistance to Cd and the ability to accumulate it in the mycelium. However, the mechanisms conferring Cd resistance in <i>Morchella</i> are unknown. In the present study, morphological and physiological responses to Cd were evaluated in the mycelia of <i>Morchella spongiola</i>. Variations in hyphal micro-morphology including twisting, folding and kinking in mycelia exposed to different Cd concentrations (0.15, 0.9, 1.5, 2.4, 5.0 mg/L) were observed using scanning electron microscopy. Deposition of Cd precipitates on cell surfaces (at Cd concentrations > 2.4 mg/L) was shown by SEM-EDS. Transmission electron microscopy analysis of cells exposed to different concentrations of Cd revealed the loss of intracellular structures and the localization of Cd depositions inside/outside the cell. FTIR analysis showed that functional groups such as C=O, -OH, -NH and -CH could be responsible for Cd binding on the cell surface of <i>M. spongiola</i>. In addition, intracellular accumulation was observed in cultures at low Cd concentrations (< 0.9 mg/L), while extracellular adsorption occurred at higher concentrations. These results provide valuable information on the Cd tolerance mechanism in <i>M. spongiola</i> and constitute a robust foundation for further studies on fungal bioremediation strategies.

Lactobacillus fermentum UCO-979C beneficially modulates the innate immune response triggered by Helicobacter pylori infection in vitro

2018 ◽  
Vol 9 (5) ◽  
pp. 829-841 ◽  
Author(s):  
V. Garcia-Castillo ◽  
H. Zelaya ◽  
A. Ilabaca ◽  
M. Espinoza-Monje ◽  
R. Komatsu ◽  
...  
Keyword(s):  
Immune Response ◽  
Helicobacter Pylori ◽  
Epithelial Cells ◽  
Morphological Changes ◽  
Helicobacter Pylori Infection ◽  
Lactobacillus Fermentum ◽  
Gastric Tissue ◽  
Gastric Epithelial Cells ◽  
Ags Cells ◽  
H Pylori

Helicobacter pylori infection is associated with important gastric pathologies. An aggressive proinflammatory immune response is generated in the gastric tissue infected with H. pylori, resulting in gastritis and a series of morphological changes that increase the susceptibility to cancer development. Probiotics could present an alternative solution to prevent or decrease H. pylori infection. Among them, the use of immunomodulatory lactic acid bacteria represents a promising option to reduce the severity of chronic inflammatory-mediated tissue damage and to improve protective immunity against H. pylori. We previously isolated Lactobacillus fermentum UCO-979C from human gastric tissue and demonstrated its capacity to reduce adhesion of H. pylori to human gastric epithelial cells (AGS cells). In this work, the ability of L. fermentum UCO-979C to modulate immune response in AGS cells and PMA phorbol 12-myristate 13-acetate (PMA)-differentiated THP-1 (human monocytic leukaemia) macrophages in response to H. pylori infection was evaluated. We demonstrated that the UCO-979C strain is able to differentially modulate the cytokine response of gastric epithelial cells and macrophages after H. pylori infection. Of note, L. fermentum UCO-979C was able to significantly reduce the production of inflammatory cytokines and chemokines in AGS and THP-1 cells as well as increase the levels of immunoregulatory cytokines, indicating a remarkable anti-inflammatory effect. These findings strongly support the probiotic potential of L. fermentum UCO-979C and provide evidence of its beneficial effects against the inflammatory damage induced by H. pylori infection. Although our findings should be proven in appropriate experiments in vivo, in both H. pylori infection animal models and human trials, the results of the present work provide a scientific rationale for the use of L. fermentum UCO-979C to prevent or reduce H. pylori-induced gastric inflammation in humans.

Phytochemicals and Tyrosinase Inhibitory Activity from Piper caninum and Piper magnibaccum

2019 ◽  
Vol 25 (4) ◽  
pp. 358-363
Author(s):  
Nur Athirah Hashim ◽  
Farediah Ahmad ◽  
Wan Mohd Nuzul Hakimi Wan Salleh ◽  
Shamsul Khamis
Keyword(s):  
Inhibitory Activity ◽  
Kojic Acid ◽  
Biological Effects ◽  
Positive Control ◽  
Aromatic Plants ◽  
Tyrosinase Inhibitory Activity ◽  
Potential Source ◽  
Phytochemical Constituents ◽  
Reported Data ◽  
Ethyl Acetate Extracts

Background: Piper species are aromatic plants used as spices in the kitchen, but their secondary metabolites have also shown biological effects on human health. In traditional medicine, Piper species have been used worldwide to treat several diseases such as urological problems, skin, liver and stomach ailments, for wound healing, and as antipyretic and anti-inflammatory agents. In the present study, we attempted to isolate the phytochemicals from Piper caninum and Piper magnibaccum and evaluate their tyrosinase inhibitory activity. Methods: Phytochemical constituents of the extracts were investigated using various chromatographic and spectroscopic methods. The structures of the isolated phytochemicals were established by analysis of their spectroscopic data, as compared to that of reported data. Tyrosinase inhibitory activity was also tested on the extracts and selected compounds using mushroom tyrosinase as the enzyme. Results: Fractionation and purification of the extracts of Piper caninum and Piper magni­baccum afforded nine known compounds which were cepharanone A (1), cepharadione A (2), aristolactam AII (3), 5,7-dimethoxyflavone (4), 24-methylenecycloartan-3-one (5), β-sitosterol (6), piperumbellactam A (7), 24S-ethylcholesta-5,22,25-trien-3β-ol (8) and stigmast-3,6-dione (9). Ethyl acetate extracts from leaves of P. magnibaccum gave the highest inhibition value at 48.35%, while the tested compounds displayed weak tyrosinase activity compared to the positive control, kojic acid. Conclusion: These phytochemical results suggested that the extracts could assist as a potential source of bioactive compounds. Further research is needed in which the extract could possibly be exploited for pharmaceutical use.

scholarly journals Dihydrocytochalasin B. Biological effects and binding to 3T3 cells.

1978 ◽  
Vol 76 (2) ◽  
pp. 360-370 ◽  
Author(s):  
S J Atlas ◽  
S Lin
Keyword(s):  
Cell Motility ◽  
Morphological Changes ◽  
Biological Effects ◽  
Sugar Transport ◽  
Sugar Uptake ◽  
3T3 Cells ◽  
Binding Studies ◽  
High Affinity ◽  
Undetermined Function ◽  
Induced Changes

Dihydrocytochalasin B (H2CB) does not inhibit sugar uptake in BALB/c 3T3 cells. Excess H2CB does not affect inhibition of sugar uptake by cytochalasin B (CB), indicating that it does not compete with CB for binding to high-affinity sites. As in the case of CB, H2CB inhibits cytokinesis and changes the morphology of the cells. These results demonstrate that the effects of CB on sugar transport and on cell motility and morphology involve separate and independent sites. Comparison of the effects of H2CB, CB, and cytochalasin D (CD) indicates that treatment of cells with any one of the compounds results in the same series of morphological changes; the cells undergo zeiosis and elongation at 2-4 microM CB and become arborized and rounded up at 10-50 microM CB. H2CB is slightly less potent than CB, whereas CD is five to eight times more potent than CB in causing a given state of morphological change. These results indicate that the cytochalasin-induced changes in cell morphology are mediated by a specific site(s) which can distinguish the subtle differences in the structures of the three compounds. Competitive binding studies indicate that excess H2CB displaces essentially all of the high-affinity bound [3H]CB, but, at less than 5 x 10(-5) M H2CB is not so efficient as unlabeled CB in the displacement reaction. In contrast, excess CD displaces up to 40% of the bound [3H]CB. These results suggest that three different classes of high-affinity CB binding sites exist in 3T3 cells: sites related to sugar transport, sites related to cell motility and morphology, and sites with undetermined function.

High throughput solubility measurement with automated polarized light microscopy analysis

2006 ◽  
Vol 95 (10) ◽  
pp. 2115-2122 ◽  
Author(s):  
Kiyohiko Sugano ◽  
Teruhisa Kato ◽  
Kentaro Suzuki ◽  
Kako Keiko ◽  
Tetsujo Sujaku ◽  
...  
Keyword(s):  
Light Microscopy ◽  
High Throughput ◽  
Polarized Light ◽  
Polarized Light Microscopy ◽  
Solubility Measurement ◽  
Microscopy Analysis ◽  
Light Microscopy Analysis
Sign in / Sign up

Export Citation Format

Share Document