scholarly journals Solvothermal Synthesis of Multiple Dihydropyrimidinones at a Time as Inhibitors of Eg5

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1925
Author(s):  
Xiao-Qiang Jiang ◽  
Shi-Quan Chen ◽  
Yan-Fei Liu ◽  
Xin-Guang Pan ◽  
Dan Chen ◽  
...  
Keyword(s):  
Cell Line ◽  
Solvothermal Synthesis ◽  
Motor Protein ◽  
L929 Cell ◽  
Binding Interaction ◽  
Discovery Studio ◽  
Atpase Assay ◽  
Cell Line Hela ◽  
T24 Cell Line

Solvothermal synthesis of multiple dihydropyrimidinones at a time has been developed in inexpensive and green bio-based solvent lactic acid without any additional catalysts or additives. By this method, thirty new dihydropyrimidinone derivatives were synthesized in two batches and characterized. All of the compounds were screened by Eg5 motor protein ATPase assay, and the positive compounds were tested against the Caco-2 cell line, HeLa cell line, L929 cell line and T24 cell line in vitro. Among them, compound C9 exhibited the best inhibitory activity against motor protein ATPase with an IC50 value of 30.25 μM and significant cytotoxic activity in the micromolar range against the cells above. The Lineweaver–Burk plot revealed that compound C9 was a mixed-type Eg5 inhibitor. A molecular modeling study using the Discovery Studio program was performed, where compound C9 exhibited good binding interaction with Eg5 motor protein ATPase, and this was consistent with the attained experimental results.

scholarly journals CIC missense variants contribute to susceptibility for spina bifida

2021 ◽  
Author(s):  
Xiao Han ◽  
Xuanye Cao ◽  
Vanessa Aguiar-Pulido ◽  
Wei Yang ◽  
Menuka Karki ◽  
...  
Keyword(s):  
Spina Bifida ◽  
Cell Line ◽  
Neural Tube ◽  
Folate Receptor ◽  
Spinocerebellar Ataxia Type ◽  
Loss Of Function ◽  
Missense Variants ◽  
Increased Risk ◽  
Cell Line Hela

Neural Tube Defects (NTDs) are congenital malformations resulting from abnormal embryonic development of the brain, spine, or spinal column. The genetic etiology of human NTDs remains poorly understood despite intensive investigation. CIC, homolog of the Capicua transcription repressor, has been reported to interact with ataxin-1 (ATXN1) and participate in the pathogenesis of spinocerebellar ataxia type 1. Our previous study demonstrated that CIC loss of function (LoF) variants contributed to cerebral folate deficiency by downregulating folate receptor 1 (FOLR1) expression. Given the importance of folate transport in neural tube formation, we hypothesized that CIC variants could contribute to increased risk for NTDs by depressing embryonic folate concentrations. In this study, we examined CIC variants from whole genome sequencing (WGS) data of 140 isolated spina bifida cases and identified 8 missense variants of CIC gene. We tested the pathogenicity of the observed variants through multiple in vitro experiments. We determined that CIC variants decreased FOLR1 protein level and planar cell polarity (PCP) pathway signaling in a human cell line (HeLa). In a murine cell line (NIH3T3), CIC loss of function variants down regulated PCP signaling. Taken together, this study provides evidence supporting CIC as a risk gene for human NTD.

In vitro studies on potentiation of cytotoxic effects of anticancer drugs by interferon on a human neoplastic cell line (HeLa)

1983 ◽  
Vol 20 (2) ◽  
pp. 131-138 ◽  
Author(s):  
Shoichi Yamamoto ◽  
Hiroyoshi Tanaka ◽  
Toshinori Kanamori ◽  
Masahiro Nobuhara ◽  
Masayoshi Namba
Keyword(s):  
Cell Line ◽  
Anticancer Drugs ◽  
Neoplastic Cell ◽  
In Vitro Studies ◽  
Cytotoxic Effects ◽  
Cell Line Hela ◽  
Line Hela

scholarly journals In VitroEvaluation of the Antioxidant Activity and Wound Healing Properties of Jaboticaba (Plinia peruviana) Fruit Peel Hydroalcoholic Extract

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Heloisa da S. Pitz ◽  
Aline Pereira ◽  
Mayara B. Blasius ◽  
Ana Paula L. Voytena ◽  
Regina C. L. Affonso ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Wound Healing ◽  
Cell Line ◽  
Healing Process ◽  
L929 Cell ◽  
Wound Healing Process ◽  
Fruit Peel ◽  
Hydroalcoholic Extract ◽  
Exposure Evaluation

Jaboticaba is a fruit from a native tree to Brazil,Plinia peruviana. Jaboticaba peels are an important source of antioxidant molecules such as phenolic compounds. This study aimed to evaluatein vitrothe activity of a hydroalcoholic extract of jaboticaba fruit peels (HEJFP) in wound healing processes and antioxidant activity in murine fibroblasts (L929 cell line). HEJFP concentrations (0.5, 1, 5, 10, 25, 50, 100, and 200 µg/mL) were tested in MTT assay and cell proliferation was verified at 100 µg/mL after 24 h and at 25, 50, and 100 µg/mL after 48 h of extract exposure. Evaluation of antioxidant activity was performed at 0.5, 5, 25, 50, and 100 µg/mL HEJFP concentrations. Cell treatment with HEJFP at 25, 50, and 100 µg/mL for 24 h followed by H2O2exposure for 3 h showed a strong cytoprotective effect.In vitroscratch wound healing assay indicated that none of tested HEJFP concentrations (0.5, 5, 25, 50, and 100 µg/mL) were capable of increasing migration rate after 12 h of incubation. These results demonstrate a positive effect of HEJFP on the wound healing process on L929 fibroblasts cell line, probably due to the antioxidant activity exhibited by phytochemicals in the extract.

scholarly journals Docking-designed Green Synthesis and In-Vitro Anticancer Studies of New Binuclear Se-N-Heterocyclic Carbene Adducts and their Azolium Salts

2021 ◽  
Author(s):  
Muhammad Atif ◽  
Mansoureh Nazari V ◽  
Mohamed B Khadeer Ahamed ◽  
Maryam Aslam ◽  
Aman Shah Abdul Majid ◽  
...  
Keyword(s):  
Growth Factor ◽  
Cell Line ◽  
Angiogenic Factor ◽  
Breast Adenocarcinoma ◽  
Cervical Cancer Cell Line ◽  
Synthetic Approach ◽  
Standard Drug ◽  
Cell Line Hela ◽  
Benzimidazolium Salts

Abstract Two binuclear selenium adducts (5 and 6) were designed using molecular docking approach while finding their promising interaction to four angiogenic factor-proteins including COX-1 (Cyclooxygenase-1), VEGF-A (vascular endothelial growth factor A), HIF (Hypoxia-inducible factor) and EGF (human epidermal growth factor). They were consequently synthesized using In-situ coordination approach. The green synthetic approach was employed for coordination as it was carried out in water instead of organic solvents. The synthesized adducts as well as their respective bis-benzimidazolium salts (2 and 4) were confirmed by 1H and 13C-NMR along with FT-IR spectroscopy. The both were, then, subjected to In-vitro anticancer activities against breast adenocarcinoma cell line (MCF-7), cervical cancer cell line (Hela), mouse melanoma cell line (B16F10) and retinal ganglion cell line (RGC-5) using MTT assay while comparing their activities with a commercially established standard-drug 5-Fluorouracil. However, the exceptional activities of both adducts and bis-benzimidazolium salts were explored.

Synthesis, In Silico and In Vivo Evaluation of Novel 1, 3, 4-Thiadiazole Analogues as Novel Anticancer Agents

2020 ◽  
Vol 17 (4) ◽  
pp. 434-444 ◽  
Author(s):  
Swathi Krishna ◽  
Byran Gowramma ◽  
Manal Mohammed ◽  
Rajagopal Kalirajan ◽  
Lakshman Kaviarasan ◽  
...  
Keyword(s):  
Vero Cell ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Binding Interaction ◽  
Standard Drug ◽  
Discovery Studio ◽  
Vero Cell Lines ◽  
Mcf 7

Background: 1,3,4-thiadiazole is a lead molécule which is versatile for a wide variety of biological activities and in continuation of our interest in establishing some novel heterocyclic compounds for antitumor activity. Objective: The objective of the study was to synthesize series of 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine derivative and evaluated for their possible in vitro and in vivo anticancer activity. Methods: The synthesis of 2-aminonaphthoxy-1,3,4-thiadiazole and 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine as intermediates were carried out by cyclization method. A mixture of thiosemicarbazide and naphthoxyacetic acid/piperonylic acid and phosphoryl chloride were subjected to cyclization with phosphorous oxychloride to obtain compound 3. Further compounds 1 and 3 were reacted with different aromatic aldehydes in methanol to form compounds 2a-e and 4a-e. The compounds 2a-e and 4a-e were characterized for the melting points, IR, Proton NMR and Mass spectra. The compounds were further evaluated for their anticancer activity. The docking study was performed using Discovery studio 4.1 (Accelrys) software against DNA-binding domain of STAT3. The compounds were analyzed for the ligand-protein binding interaction(s) by molecular docking into the active site of STAT3β using the CDOCKER protocol of Discovery studio (v4.1). Results: The title compounds were screened for in vitro anticancer on human breastadenocarcinoma cells (MCF-7 and Vero). Compounds 4c, 4d and 2d against MCF 7 and 4d against Vero cell lines were found to be the most active dérivatives with IC50 values of 1.03, 2.81 and 3.45 µg/ml against MCF 7 and 31.81 µg/ml against Vero cell lines, respectively. Conclusion: From the in vivo anticancer studies, it was concluded that the synthesized compounds 4c and 4d displayed anticancer activity comparable to the standard drug, while the rest of the compounds demonstrated mild potency for anticancer studies.

An in vitro study of biological safety of condoms and their additives

2003 ◽  
Vol 22 (12) ◽  
pp. 659-664 ◽  
Author(s):  
N A Motsoane ◽  
M J Bester ◽  
E Pretorius ◽  
P J Becker
Keyword(s):  
Hela Cell ◽  
Cell Viability ◽  
Cell Line ◽  
Tumor Cell Line ◽  
Toxic Effects ◽  
Specific Cell ◽  
Epithelial Tumor ◽  
Hela Cell Lines ◽  
Cell Line Hela

The use of condoms to prevent sexually transmitted diseases, especially HIV, is widely encouraged. Condoms contain latex, nonspermicidal lubricants (such as dimethylsiliconium) and other nonspecified compounds, such as colorants and flavorings. Latex causes allergy reaction in susceptible individuals but little is known regarding the cytotoxic effects of other additives. The objective of this study was to develop a sensitive in vitrosystem to determine the toxic effects of condom material. The modified L929 FDA method and a more specific cell type, such as the cervical epithelial tumor cell line HeLa, was used. Lubricated (LC), lubricated and flavored (LFC), and lubricated, flavored and colored condoms (LFCC) were evaluated. Washings containing condom surface material were prepared by washing condom fragments in medium for different time intervals. Changes in cell number, viability and lysosome integrity in the L929 and HeLa cell lines was determined using the Crystal Violet, MTT and Neutral Red assays, respectively. The condom type affected cell viability and lysosome integrity, with LC inducing an increase in cell viability and LFC a decrease in lysosome integrity. The HeLa cell line in combination with the MTT and NR assay was the most sensitive in vitro system to determine the toxic effects of condom material.

In vitro cytotoxic effects of DEHP-alternative plasticizers and their primary metabolites on a L929 cell line

Chemosphere ◽  
2017 ◽  
Vol 173 ◽  
pp. 452-459 ◽  
Author(s):  
Teuta Eljezi ◽  
Pierre Pinta ◽  
Damien Richard ◽  
Jérémy Pinguet ◽  
Jean-Michel Chezal ◽  
...  
Keyword(s):  
Cell Line ◽  
L929 Cell ◽  
Cytotoxic Effects ◽  
Primary Metabolites ◽  
L929 Cell Line

scholarly journals Assessment of cytotoxic and antimicrobial activity of selected gingival haemostatic agents – in vitro study

2020 ◽  
Vol 22 (3) ◽  
Author(s):  
Maria Szymonowicz ◽  
_ Agnieszka ◽  
Magdalena Pajączkowska ◽  
Joanna Nowicka ◽  
Kamila Wiśniewska ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cell Line ◽  
Mtt Assay ◽  
In Vitro Study ◽  
L929 Cell ◽  
Aluminium Chloride ◽  
Srb Assay ◽  
Haemostatic Agents ◽  
L929 Cell Line

Purpose: The present research aimed to determine whether and how the aluminium chloride – based materials affect the cell line of the bacterial line and fungi. Methods: Cytotoxicity of haemostatic astringents: Alustat (liquid), Alustat (gel), Alustat (foam), Alustin, Hemostat, Racestyptine and Traxodent containing AlCl3 was conducted on L929 cell line with the use of MTT and SRB assays. The antimicrobial activity (CFU and MIC) against C. albicans, S. mutans, L. rhamnosus was determined. Results: In the MTT results, cell viability for all agents were very low. In SRB, the lowest cytotoxicity was demonstrated for Hemostat and Alustat (foam), Traxodent and Racestyptine. Total reduction of the CFU of S. mutans was observed. Alustat (gel) and Alustat (liquid) completely inhibited the growth of C. albicans, S. mutans and L. rhamnosus. Conclusions: The viability of L929 cells obtained in the SRB assay is more reliable than that obtained in the MTT assay, in the case of gingival haemostatic agents.

scholarly journals IN VITRO ANTI-NEUROINFLAMMATORY EFFECT OF GENISTEIN (4',5,7-TRIHYDROXYISOFLAVONE) ON MICROGLIA HMC3 CELL LINE, AND IN SILICO EVALUATION OF ITS INTERACTION WITH ESTROGEN RECEPTOR-β

2021 ◽  
pp. 183-187
Author(s):  
BURHAN MA’ARIF ◽  
FAISAL A. MUSLIKH ◽  
WIRDA ANGGRAINI ◽  
MAXIMUS M. TAEK ◽  
HENING LASWATI ◽  
...  
Keyword(s):  
Cell Line ◽  
In Silico ◽  
In Silico Analysis ◽  
Physicochemical Characteristics ◽  
Dependent Manner ◽  
Discovery Studio ◽  
Mhc Ii ◽  
M1 Phenotype ◽  
Negative Controls

Objective: This study was aimed to evaluate the role of genistein or 4',5,7-trihydroxyisoflavone as a phytoestrogen in the treatment of estrogen deficiency-induced neuroinflammatory. The specific objectives of this study were to determine the anti-neuroinflammatory effect of genistein through measurement of MHC II and Arg1 expressions on microglia HMC3 cell line, as well as to prove that the effect occurs in an ER-dependent manner, through the measurement of free-ERβ expression. Methods: The cells were cultured in 24-well microplates, induced with 10 ng IFN-γ, and incubated for 24 h to activate the cell to M1 phenotype which has pro-inflammatory characteristics. Genistein with a concentration of 50 μM was added to the cells. The expression of MHC II, Arg1, and free-ERβ as markers was tested through an immunocytochemistry method and measured using the CLSM instrument. In silico approach was also conducted to determine the interaction between genistein and ERβ, compared to 17β-estradiol. Genistein structure was prepared with Avogadro 1.0.1, and molecular docking was done using PyRx 0.8 software. Biovia Discovery Studio Visualizer 2016 was used to visualize the structure of genistein against 3OLS protein. The physicochemical characteristics of genistein were analyzed using the SwissADME web tool. Results: Genistein can decrease MHC II expression and increase Arg1 expression in microglia HMC3 cells compared to negative controls (p<0.005), with expression value of 472.577±26.701 AU and 114.299±6.578 AU. But, genistein cannot decrease the free-ERβ expression in cells (p<0.005). The results of in silico analysis showed that genistein is an ERβ agonist. Conclusion: Genistein shows anti-neuroinflammatory effects by decreasing the MHC II expression and increasing Arg1 expression in the microglia HMC3 cell line. However, this effect does not occur through the binding of genistein to ERβ, but it is likely to occur through the binding of genistein with other types of ER.

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