scholarly journals Phytochemical and chromatographic characterization of Mimosa diplotricha Wright ex. Sauvalle ethanolic leaf extract and assessment of antioxidant potential and anti-proliferative effect on colorectal cancer (HCT-116) cell lines

2020 ◽  
Vol 11 (3) ◽  
pp. 4378-4387
Author(s):  
Sri Rashmy Madathil ◽  
Poornima Kannappan ◽  
Devaki Kanakasabapathy ◽  
Sincy Varghese ◽  
Perumalsamy Muneeswari
Keyword(s):  
Cell Lines ◽  
Mtt Assay ◽  
Leaf Extract ◽  
Antioxidant Potential ◽  
Antioxidant Power ◽  
Ms Analysis ◽  
Chromatographic Profile ◽  
Hct 116 ◽  
Ethanolic Leaf Extract

Present study aims to evaluate phytochemical and chromatographic profile, along with antioxidant and anti proliferative properties of Mimosa diplotricha ethanolic leaf extract. Qualitative screening of phytoconstituents by consecutive solvent extraction in increased polarity basis and standardization of potential extract based on phytochemical elution profile was done. Selected secondary metabolites like phenols, flavanoids, tannins and alkaloids were quantified in ethanolic extract. Chromatographic profile was determined by HPTLC and GC-MS analysis. In vitro antioxidant potential was assessed by DPPH, superoxide, nitric oxide, hydrogen peroxide and hydroxyl radical scavenging assay. Ferric-reducing antioxidant power assay (FRAP) and reducing potential of the respective extract were also determined. Anticancer potential was confirmed by cytotoxic screening in colorectal (HCT-116) cancer cell lines by MTT assay. Qualitative phytochemical analysis and chromatographic profile reveal a phytoconstituent rich profile for the ethanolic leaf extract. The amount of, phenols (56 ± 0.57 mg/g), flavanoids (27 ± 0.76 mg/g), tannins (33 ± 0.15 mg/g) were quantified as equivalent of gallic acid, quercetin and tannic acid standards respectively and alkaloids (2.51 ± 0.47 mg/g of extracted plant material) were expressed based on respective analysis. Results also reveal convincing antioxidant potential for respective extract. In vitro cytotoxicity confirmed by MTT assay represents an IC50 value of 97.82 µg/ml. From the above results it can be concluded that M.diplotricha has got pharmacologically significant phytoconstituents and therapeutic active ingredients as evident in HPTLC and GC-MS analysis. This is further supported by considerable antioxidant and anti proliferative properties observed in respective assays.

Synthesis and antioxidant activity of new selenium-containing quinolines

2020 ◽  
Vol 16 ◽  
Author(s):  
Benedetta Bocchini ◽  
Bruna Goldani ◽  
Fernanda S.S. Sousa ◽  
Paloma T. Birmann ◽  
Cesar A. Brüning ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Radical Scavenging ◽  
Building Blocks ◽  
Antioxidant Potential ◽  
In Vitro Assays ◽  
Pharmacological Activities ◽  
Antioxidant Power ◽  
Antioxidant Agents

Background: Quinoline derivatives have been attracted much attention in drug discovery and synthetic derivatives of these scaffolds present a range of pharmacological activities. Therefore, organoselenium compounds are valuable scaffolds in organic synthesis because their pharmacological activities and their use as versatile building blocks for regio-, chemio-and stereoselective reactions. Thus, the synthesis of selenium-containing quinolines has great significance, and their applicability range from simple antioxidant agents, to selective DNA-binding and photocleaving agents. Objective: In the present study we describe the synthesis and antioxidant activity in vitro of new 7-chloroN(arylselanyl)quinolin-4-amines 5 by the reaction of 4,7-dichloroquinoline 4 with (arylselanyl)-amines 3. Methods: For the synthesis of 7-chloro-N(arylselanyl)quinolin-4-amines 5, we performed the reaction of (arylselanyl)- amines 3 with 4,7-dichloroquinoline 4 in the presence of Et3N at 120 °C in a sealed tube. The antioxidant activities of the compounds 5 were evaluated by the following in vitro assays: 2,2- diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), ferric ion reducing antioxidant power (FRAP), nitric oxide (NO) scavenging and superoxide dismutase-like activity (SOD-Like). Results: 7-Chloro-N(arylselanyl)quinolin-4-amines 5a-d has been synthesized in yields ranging from 68% to 82% by the reaction of 4,7-dichloroquinoline 4 with arylselanyl-amines 3a-d using Et3N as base, at 120 °C, in a sealed tube for 24 hours and tolerates different substituents, such as -OMe and -Cl, in the arylselanyl moiety. The obtained compounds 5a-d presented significant results with respect to the antioxidant potential, which had effect in the tests of inhibition of radical’s DPPH, ABTS+ and NO, as well as in the test that evaluates the capacity (FRAP) and in the superoxide dismutase-like activity assay (SOD-Like). It is worth mentioning that 7-chloro-N(arylselanyl)quinolin-4-amine 5b presented excellent results, demonstrating a better antioxidant capacity when compared to the others. Conclusion: According to the obtained results 7-chloro-N(arylselanyl)quinolin-4-amines 5 were synthesized in good yields by the reaction of 4,7-dichloroquinoline with arylselanyl-amines and tolerates different substituents in the arylselanyl moiety. The tested compounds presented significant antioxidant potential in the tests of inhibition of DPPH, ABTS+ and NO radicals, as well as in the FRAP and superoxide dismutase-like activity assays (SOD-Like).

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

scholarly journals In Vitro Cytotoxic Activity of Origanum vulgare L. on HCT-116 and MDA-MB-231 Cell Lines

Plants ◽  
2013 ◽  
Vol 2 (3) ◽  
pp. 371-378 ◽  
Author(s):  
Filip Grbović ◽  
Milan Stanković ◽  
Milena Ćurčić ◽  
Nataša Đorđević ◽  
Dragana Šeklić ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Origanum Vulgare ◽  
Hct 116

scholarly journals A Bottom-Up Synthesis Approach to Silver Nanoparticles Induces Anti-Proliferative and Apoptotic Activities Against MCF-7, MCF-7/TAMR-1 and MCF-10A Human Breast Cell Lines

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4332
Author(s):  
Nurul Izzati Zulkifli ◽  
Musthahimah Muhamad ◽  
Nur Nadhirah Mohamad Zain ◽  
Wen-Nee Tan ◽  
Noorfatimah Yahaya ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Silver Nanoparticles ◽  
Cell Lines ◽  
Leaf Extract ◽  
Breast Cancer Cell Lines ◽  
Face Centered Cubic ◽  
Human Breast ◽  
Bottom Up ◽  
Mcf 7

A bottom-up approach for synthesizing silver nanoparticles (AgNPs-GA) phytomediated by Garcinia atroviridis leaf extract is described. Under optimized conditions, the AgNPs-GA were synthesized at a concentration of 0.1 M silver salt and 10% (w/v) leaf extract, 1:4 mixing ratio of reactants, pH 3, temperature 32 °C and 72 h reaction time. The AgNPs-GA were characterized by various analytical techniques and their size was determined to be 5–30 nm. FTIR spectroscopy indicates the role of phenolic functional groups in the reduction of silver ions into AgNPs-GA and in supporting their subsequent stability. The UV-Visible spectrum showed an absorption peak at 450 nm which reflects the surface plasmon resonance (SPR) of AgNPs-GA and further supports the stability of these biosynthesized nanoparticles. SEM, TEM and XRD diffractogram analyses indicate that AgNPs-GA were spherical and face-centered-cubic in shape. This study also describes the efficacy of biosynthesized AgNPs-GA as anti-proliferative agent against human breast cancer cell lines, MCF-7 and MCF-7/TAMR-1. Our findings indicate that AgNPs-GA possess significant anti-proliferative effects against both the MCF-7 and MCF-7/TAMR-1 cell lines, with inhibitory concentration at 50% (IC50 values) of 2.0 and 34.0 µg/mL, respectively, after 72 h of treatment. An induction of apoptosis was evidenced by flow cytometry using Annexin V-FITC and propidium iodide staining. Therefore, AgNPs-GA exhibited its anti-proliferative activity via apoptosis on MCF-7 and MCF-7/TAMR-1 breast cancer cells in vitro. Taken together, the leaf extract from Garcinia atroviridis was found to be highly capable of producing AgNPs-GA with favourable physicochemical and biological properties.

scholarly journals In vitro Screening of Berberis lycium Root Extract on HCT-116 and MCF-7 Cell Lines

2020 ◽  
Vol 20 (s2) ◽  
Author(s):  
Xiaolin Hu ◽  
S. Islam ◽  
Fuad Ameen ◽  
Abdullah A. Alarfaj ◽  
G. Murtaza ◽  
...  
Keyword(s):  
Cell Lines ◽  
Root Extract ◽  
In Vitro Screening ◽  
Hct 116 ◽  
Berberis Lycium ◽  
Mcf 7
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