scholarly journals Synthesis and Biological Activity Studies of Methyl-5-(Hydroxymethyl)-2-Furan Carboxylate and Derivatives

2019 ◽  
Vol 35 (3) ◽  
pp. 080-1085 ◽  
Author(s):  
Weerachai Phutdhawong ◽  
Siwaporn Inpang ◽  
Thongchai Taechowisan ◽  
Waya S. Phutdhawong
Keyword(s):  
Biological Activity ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Furfuryl Alcohol ◽  
Methyl Acetate ◽  
Biological Activities ◽  
Hela Cell Line ◽  
Amine Derivative

Methyl-5-(hydroxymethyl)-2-furan carboxylate and derivatives were prepared from furfuryl alcohol and their biological activities were studied for cytotoxicity against cancer cell lines HeLa, HepG2 and Vero, and Gram (+) and Gram (-) bacteria. The amine derivative, (5-(((2-(1H-indol-3-yl)ethyl)amino)methyl) furan-2-yl)methyl acetate, was found to have the most potent biological activity with IC50 62.37 µg/mL against the HeLa cell line and MIC 250 µg/mL against the photogenic bacteria.

scholarly journals Evaluating the in vitro Cytotoxicity of Thymus vulgaris Essential Oil on MCF-7 and HeLa Cancer Cell Lines

2021 ◽  
pp. 2862-2871
Author(s):  
Alsafa N. Khalaf ◽  
Ibrahim J. Abed
Keyword(s):  
Essential Oil ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Thymus Vulgaris ◽  
Hela Cell Line ◽  
Significant Difference ◽  
Mcf 7

     Thyme essential oil (TEO) was extracted from dried leaves of Thymus vulgaris. The air-dried aerial parts of the plant produced 1.0% yield of TEO. The detection of this essential oil’s compounds was performed by GC-MASS. The cytotoxic activity of TEO was evaluated against two human cancer cell lines, namely HeLa (human epithelial cervical cancer) and MCF-7 (human breast carcinoma). Cells grown in 96 multi-well plates were treated with six concentrations of EO (6.25, 12.5, 25, 50, 100, 200 ppm) and incubated at 37 °C for 72 hrs. Cancer cell lines elicited various degrees of sensitivity to the cytotoxic effect of essential oil. The TEO exhibited significant differences (p≤ 0.01) between the effects of all concentrations against these two human cell lines. The results showed the highest toxicity of TEO on HeLa cell line (78.67%) and MCF-7 cell line (83.60%) at 200 ppm concentration. Also the values of half-maximal inhibitory concentration (IC50) of TEO against HeLa and MCF-7 cell lines were 34.63 and 27.66 ppm, respectively. Cells treated with the IC50 of TEO showed a significant difference (p ≤ 0.01) in p53 fold expression between HeLa cell line (4.33±0.41 folds) and MCF-7 cell line (5.10±0.32 folds). In general, a dose-dependent decrease the survival of the two cell lines was observed. In addition, MCF-7 cell line revealed higher sensitivity against TEO than HeLa cell line.

scholarly journals Synthesis, structural analysis, solution equilibria and biological activity of rhodium(iii) complexes with a quinquedentate polyaminopolycarboxylate

RSC Advances ◽  
2017 ◽  
Vol 7 (9) ◽  
pp. 5282-5296 ◽  
Author(s):  
Marija S. Jeremić ◽  
Hubert Wadepohl ◽  
Vesna V. Kojić ◽  
Dimitar S. Jakimov ◽  
Ratomir Jelić ◽  
...  
Keyword(s):  
Biological Activity ◽  
Structural Analysis ◽  
Antitumor Activity ◽  
Hela Cell ◽  
Cell Line ◽  
Hela Cell Line ◽  
Solution Equilibria ◽  
Line P

Two new Rh(iii)–ed3a complexes [Rh(ed3a)(OH2)]·H2O and Na[Rh(ed3a)Cl]·H2O have shown good antitumor activity, especially against HeLa cell line.

scholarly journals New biological findings of ethanol and chloroform extracts of fungi Suillellus rubrosanguineus and Tylopilus felleus

2018 ◽  
Vol 11 (3) ◽  
pp. 204-208
Author(s):  
Ivana Šušaníková ◽  
Adriána Kvasnicová ◽  
Žofia Brzková ◽  
Ondrej Ďuriška ◽  
Pavel Mučaji
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Middle Europe ◽  
Dragendorff Reagent ◽  
Nih 3T3 ◽  
Clinical Experiments ◽  
Mcf 7

Abstract The aim of the research was to determine some basic biological activities of less biomedically studied but commonly known two fungi from the Boletaceae family Suillellus rubrosanguineus and Tylopilus felleus, which grow in the forests of Middle Europe. The cytotoxicity tests of the ethanol and chloroform extracts were carried out using NIH-3T3 and MCF-7 cell lines. The presence of alkaloids in the extracts was assessed by the reaction with Dragendorff reagent. In all of the extracts the positive reaction with the reagent was observed. In general, the extracts from Suillellus rubrosanguineus were more cytotoxic than the extracts from Tylopilus felleus and exhibited no selectivity of activities on healthy and cancer cell lines. However, the extracts from Tylopilus felleus proved to be selectively cytotoxic for cancer cell line. Tylopilus extracts or their isolated bioactive compounds could be considered for further study in pre-clinical experiments.

scholarly journals Novel C-ring Analogs of Ursolic acid: Synthesis and Cytotoxic Evaluation

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Uppuluri V. Mallavadhani ◽  
Banita Pattnaik ◽  
Nitasha Suri ◽  
Ajit K. Saxena
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Ursolic Acid ◽  
Parent Compound ◽  
Acid Synthesis ◽  
Hela Cell Line ◽  
Hela Cell Lines ◽  
Protective Groups

Ursolic acid (1), a natural pentacyclic triterpenic acid, afforded a variety of ring-C transformed products (5–11) when treated with N-bromosuccinimide under the influence of a range of protective groups and solvents. The synthesized compounds have been evaluated for cytotoxic activity against prostate PC 3, leukemia THP 1, cervical Hela and lung A-549 cancer cell lines. Among the tested analogs, compounds 5, 8, 9 and 10 showed potent activity against PC 3, THP 1 and Hela cell lines. Especially, compound 10 showed enhanced activity against the Hela cell line than the parent compound. Compounds 5, 8 and 9 showed comparable activities against PC 3 and THP 1 cell lines.

Biological Activity, Apoptotic Induction and Cell Cycle Arrest of New Hydrazonoyl Halides Derivatives

2019 ◽  
Vol 19 (9) ◽  
pp. 1141-1149 ◽  
Author(s):  
Magda F. Mohamed ◽  
Hamdi M. Hassaneen ◽  
Emad M. Elzayat ◽  
Salwa M. El-Hallouty ◽  
May El-Manawaty ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Activities ◽  
Breast Epithelial Cell ◽  
Human Cancer Cell ◽  
Hydrazonoyl Halides

Background:The hydrazonoyl halides are presently an important target in the field of medicinal chemistry. The interest in the chemistry of hydrazonoyl halides is a consequence of the fact that they undergo a wide variety of reactions which provide routes to a myriad of both heterocyclic and acyclic compounds. In addition, they have diverse biological activities such as antiviral, anthelmintic, antiarthropodal, fungicidal, herbicidal, insecticidal, pesticidal, acaricidal and miticidal Activity correlated to the presence of hydrazonoyl halides. Moreover, many applications in both industrial and pharmaceutical fields have been found to be associated with these halides. Depending on the above facts and continuation to our work, we herein report on the evaluation of the anticancer activity of these two halides prepared according to the published work and trying to know their molecular mechanism that they proceed to stop proliferation and metastasis of tumor cells by molecular tools such as real time PCR using different apoptotic genes, and cell cycle assay.Objective:The goal of this present study is to bring attention to the biological activities of hydrazonoyl halides and the molecular pathway they follow to exert their role in apoptotic death of cancer cell.Methods:Synthesis of hydrazonoyl halides 2c and 2f. The cytotoxic effect against different human cancer cell lines PC3, HepG-2, HCT-116, MCF-7 and also on normal human cell lines as MCF-10 and MCF-12 in a monolayer culture model was evaluated. Their mechanism of action inside cancer cell was evaluated using different molecular tools.Conclusion:Strong and promising chemotherapeutic hydrazonoyl halides (2a-2f) were evaluated for their different biological activities. As antimicrobial agents, results indicated that three compounds 2a, 2e and 2f exhibited high activity against two tested gram positive bacteria Staphylococcus aureus, Bacillus subtilis, and gram negative ones Escherichia coli, and Pseudomonas aeruginosa, the rest of the compounds were found to be moderately active against the tested microorganisms. Regarding their antifungal effect, compound 2c exhibited potent and promising effect against Candida albicans, while 2b was the most potent toward Aspergillus flavus Link. The compound 2f has repellent effect. With respect to the in vitro antitumor screening, this was done on different human cancer cell lines; namely PC3, HepG-2, HCT-116, MCF-7 and also on normal human cell lines; as MCF-10 and MCF-12 (normal breast epithelial cell and non-tumorigenic breast epithelial cell line) in a monolayer culture model where screening has been conducted at 100μg/ml (single dose test). Single dose test (100μg/ml) showed that, in case of PC3, all compounds have cytotoxic activity over 90% inhibition, 4 compounds have cytotoxic activity with 100% inhibition with Human colon cancer cell line, 4 compounds showed over 90% inhibition with MCF7 cell line and 4 compounds showed cytotoxic activity over 90% inhibition with HepG-2. Results of IC50 values for most promising compounds showed compounds with values lower than 20μM for all tested human cancer cell line. The promising hydrazonoyl halide 2c and 2f were selected for molecular study to know how they could act inside cancer cell causing death. Two biochemical tests were performed using the two halides 2c and 2f to predict their mechanism of action against breast carcinoma. Real time PCR analysis indicates that the two compounds induced the apoptosis of MCF7 cells through the up regulation of caspase-3, BAX mediated P53 mechanism but unfortunately, they promote the expression of anti-apoptotic protein BCL2. Also, cell cycle assay was performed using two different cell lines MCF7 and HCT116 and data revealed that the two compounds 2c and 2f induced apoptotic cells death of both lines via cell growth arrest at G2/M phase. In addition, it was noted that 2c induced arrest in the two lines more efficiently than 2f at G2/M phase.

scholarly journals Evaluation of biological activities of some seaweed and seagrass species in the coastal area of Vietnam

2019 ◽  
Vol 19 (3) ◽  
pp. 405-414
Author(s):  
Tran Thi Hong Ha ◽  
Le Mai Huong ◽  
Le Huu Cuong ◽  
Nguyen Dinh Tuan ◽  
Hoang Kim Chi ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Cancer Cell Lines ◽  
Tropical Country ◽  
Lung Adenocarcinoma Cell Line ◽  
Long Time

Although seaweeds and seagrasses have been used for food and traditional medicine for centuries, merely a small amount of them is exploited and used. Positive biological activities of seaweed and seagrass products on humans, animals and plants have also been recorded for a long time. Vietnam is a tropical country with 3,260 km long coastline and about 350 species of seaweeds, including 60 widely used species. In this study, 57 seaweed and seagrass samples were extracted using CHCl3/MeOH solvent systems and their crude extracts were tested for selected biological actives, including antimicrobial, antioxidant activities and cytotoxicity. The results revealed that 13 out of 57 extracts (accounting for 24.07%) were cytotoxic to one of the two tested cancer cell lines (Hepatocellular carcinoma cell line Hep-G2 and human lung adenocarcinoma cell line LU-1), and 4 extracts (accounting for 7.4%) were cytotoxic to both cancer cell lines. In antimicrobial activity assay, 18 of all 57 extracts (accounting for 37.5%) were capable of inhibiting 1 to 2 test microorganisms and 16 extracts (accounting for 33.33%) inhibited at least 3 test microorganisms. There were solely 1 extract (accounting for 1.85%) of the 57 extracts performing antioxidant activity in DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging assay.

Molecular Docking Study, Cytotoxicity, Cell Cycle Arrest and Apoptotic Induction of Novel Chalcones Incorporating Thiadiazolyl Isoquinoline in Cervical Cancer

2020 ◽  
Vol 20 (1) ◽  
pp. 70-83 ◽  
Author(s):  
Mohamed A. Tantawy ◽  
Farid M. Sroor ◽  
Magda F. Mohamed ◽  
Mostafa E. El-Naggar ◽  
Fatma M. Saleh ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Hela Cell ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
The Novel ◽  
Structural Element ◽  
Antioxidant Agents ◽  
Hela Cell Lines

Background: Chalcones are naturally occurring compounds found in various plant species which are widely used for the traditional popular treatments. Chalcones are distinguished secondary metabolites that are reported to display diverse biological activities such as antiviral, antiplatelet, anti-inflammatory, anticancer, antibacterial and antioxidant agents. The presence of a,ß-unsaturated carbonyl group in chalcones is assumed to be responsible for their bioactivity. In addition, heterocyclic compounds having nitrogen such as isoquinolines are of considerable interest as they constitute the core structural element of many alkaloids that have enormous pharmacological activities. Objective: The objective of this study is the synthesis and biological activity of novel chalcones incorporating thiadiazolyl isoquinoline as potential anticancer candidates. Different genetic tools were used in an attempt to know the mechanism of action of this compound against breast cancer. Methods: An efficient one pot synthesis of novel chalcones incorporating thiadiazolyl isoquinoline has been developed. The cytotoxic activity of the novel synthesized compounds was performed against four different kinds of cancer cell lines. Results: Among all the tested derivatives, chalcone 3 has the best cytotoxic profile against A549, MCF7, and HeLa cell lines, with IC50s (66.1, 51.3, and 85.1μM, respectively). Molecular docking studies for chalcone 3 revealed that CDK2, and EGFRTK domains have strong binding affinities toward the novel chalcone 3, while tubulin-colchicine-ustiloxin, and VEGFRTK domains illustrated moderate mode of binding. Conclusion: We have developed an efficient method for the synthesis of novel chalcones incorporating thiadiazolyl isoquinoline. All compounds showed better cytotoxicity results against four kinds of cancer cell lines (A549, MCF7, HCT116, and HELA cells). The results depicted that chalcone 3 has a high and promising cytotoxic effect against HELA cell line and the mechanism of cytotoxicity was widely studied through different theoretical and experimental tools. Thus, the newly synthesized derivative 3 can be utilized as a novel chemotherapeutic compound for cervical carcinoma.

Mapping the distribution of Golgi enzymes involved in the construction of complex oligosaccharides

1995 ◽  
Vol 108 (4) ◽  
pp. 1617-1627 ◽  
Author(s):  
C. Rabouille ◽  
N. Hui ◽  
F. Hunte ◽  
R. Kieckbusch ◽  
E.G. Berger ◽  
...  
Keyword(s):  
Golgi Apparatus ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Hela Cells ◽  
Stable Expression ◽  
Hela Cell Line ◽  
Specific Antibodies ◽  
Hela Cell Lines ◽  
Golgi Network

The distribution of beta 1,2 N-acetylglucosaminyltransferase I (NAGT I), alpha 1,3-1,6 mannosidase II (Mann II), beta 1,4 galactosyltransferase (GalT), alpha 2,6 sialyltransferase (SialylT) was determined by immuno-labelling of cryo-sections from HeLa cell lines. Antibody labelling in the HeLa cell line was made possible by stable expression of epitope-tagged forms of these proteins or forms from species to which specific antibodies were available. NAGT I and Mann II had the same distribution occupying the medial and trans cisternae of the stack. GalT and SialylT also had the same distribution but they occupied the trans cisterna and the trans-Golgi network (TGN). These results generalise our earlier observations on the overlapping distribution of Golgi enzymes and show that each of the trans compartments of the Golgi apparatus in HeLa cells contains unique mixtures of those Golgi enzymes involved in the construction of complex, N-linked oligosaccharides.

ANTITUMOR EFFECT OF SUNITINIB AND BORTEZOMIB ON BREAST CANCER CELL LINE IN VITRO

2017 ◽  
Vol 63 (1) ◽  
pp. 141-145
Author(s):  
Yuliya Khochenkova ◽  
Eliso Solomko ◽  
Oksana Ryabaya ◽  
Yevgeniya Stepanova ◽  
Dmitriy Khochenkov
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Antitumor Effect ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Actual Problem

The discovery for effective combinations of anticancer drugs for treatment for breast cancer is the actual problem in the experimental chemotherapy. In this paper we conducted a study of antitumor effect of the combination of sunitinib and bortezomib against MDA-MB-231 and SKBR-3 breast cancer cell lines in vitro. We found that bortezomib in non-toxic concentrations can potentiate the antitumor activity of sunitinib. MDA-MB-231 cell line has showed great sensitivity to the combination of bortezomib and sunitinib in vitro. Bortezomib and sunitinib caused reduced expression of receptor tyrosine kinases VEGFR1, VEGFR2, PDGFRa, PDGFRß and c-Kit on HER2- and HER2+ breast cancer cell lines

Antioxidant effects and in vitro cytotoxicity on human cancer cell lines of flavonoid-rich Flamboyant (Delonix regia (Bojer) Raf.) flower extract

2020 ◽  
Vol 21 ◽  
Author(s):  
Putthiporn Khongkaew ◽  
Phanphen Wattanaarsakit ◽  
Konstantinos I. Papadopoulos ◽  
Watcharaphong Chaemsawang
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Leukemia Cell Line ◽  
Flower Extract ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Murine Leukemia Cell ◽  
Dose Dependent

Background: Cancer is a noncommunicable disease with increasing incidence and mortality rates both worldwide and in Thailand. Its apparent lack of effective treatments is posing challenging public health issues. Introduction: Encouraging research results indicating probable anti-cancer properties of the Delonix regia flower extract (DRE) have prompted us to evaluate the feasibility of developing a type of product for future cancer prevention or treatment. Methods and Results: In the present report, using High Performance Liquid Chromatography (HPLC), we demonstrate in the DRE, the presence of high concentrations of three identifiable flavonoids, namely rutin 4.15±0.30 % w/w, isoquercitrin 3.04±0.02 %w/w, and myricetin 2.61±0.01 % w/w respectively while the IC50 of DPPH and ABTS assay antioxidation activity was 66.88±6.30 µg/ml and 53.65±7.24 µg/ml respectively. Discussion: Our cancer cell line studies using the MTT assay demonstrated DREs potent and dose dependent inhibition of murine leukemia cell line (P-388: 35.28±4.07% of cell viability remaining), as well as of human breast adenocarcinoma (MCF-7), human cervical carcinoma (HeLa), human oral cavity carcinoma (KB), and human colon carcinoma (HT-29) cell lines in that order of magnitude. Conclusion: Three identifiable flavonoids (rutin, isoquercitrin and myricetin) with high antioxidation activity and potent and dose dependent inhibition of murine leukemia cell line and five other cancer cell lines were documented in the DRE. The extract’s lack of cytotoxicity in 3 normal cell lines is a rare advantage not usually seen in current antineoplastic agents. Yet another challenge of the DRE was its low dissolution rate and long-term storage stability, issues to be resolved before a future product can be formulated.

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