Biological activity survey of Pereskia aculeata Mill. and Pereskia grandifolia Haw. (Cactaceae)

Background: Pereskia aculeata and P. grandifolia are non-traditional Brazilian vegetables with high nutritional value used in traditional medicine. The antioxidant, anticholinesterase, molluscicidal, cytotoxic, and antiproliferative properties of hydroethanolic extracts of P. aculeata and P. grandifolia leaves (PAL, PGL) and fruits (PAF, PGF) are investigated in this study. Methods: All extracts were prepared by maceration with ethanol 70%. Their antioxidant properties were assessed through DPPH, ABTS, FRAP, and β-carotene bleaching inhibition assays. A TLC bioautography method was employed to evaluate the inhibiting capacity of the acetylcholinesterase enzyme. The molluscicidal activity was tested against the snail Biomphalaria glabrata, which serves as an intermediate host for Schistosoma mansoni. The cytotoxic activity was assessed by a Artemia salina lethality test and the antiproliferative properties against seven human carcinoma cell lines. Results: Compounds with anticholinesterase activity were found in all extracts. Polar compounds present in PAF and PGL extracts were the most active (IC50 < 25 μg of dry mass) and had an adequate inhibition capacity of the AChE. PGF and PGL were classified as moderate (LC50 = 19.2 μg/ml) and modest molluscicidal agents (LC50 = 66.6 μg/ml), respectively. All extracts exhibited selective antiproliferative activity against human chronic myeloid leukemia cell lines (K562). PAL, PGL, and PGF presented potent antiproliferative activity (TGI ≤ 5 μg/ml). Conclusion: Both species exhibited anticholinesterase, cytotoxic and antiproliferative properties. This research supports the potential of these species as sustainable sources of nutraceutical compounds.

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Anti-leukemia properties of cadmium nanoparticles in the in vitro and in vivo condition: A chemobiological study

Archives of Medical Science ◽

10.5114/aoms/142465 ◽

2021 ◽

Author(s):

Yudi Miao ◽

Behnam Mahdavi ◽

Mohammad Zangeneh

Keyword(s):

Acute Myeloid Leukemia ◽

Cell Lines ◽

Aqueous Extract ◽

Myeloid Leukemia ◽

Antioxidant Properties ◽

Leukemia Cell ◽

Sem Images ◽

Acute Myeloid

IntroductionThe present study investigated the anti-acute myeloid leukemia effects of Ziziphora clinopodides Lam leaf aqueous extract conjugated cadmium nanoparticles.Material and methodsTo synthesize CdNPs, Z. clinopodides aqueous extract was mixed with Cd(NO3)2 .4H2O. The characterization of the biosynthesized cadmium nanoparticles was carried out using many various techniques such as UV-Vis. and FT-IR spectroscopy, XRD, FE-SEM, and EDS.ResultsThe uniform spherical morphology of NPs was proved by FE-SEM images with NPs the average size of 26.78cnm. For investigating the antioxidant properties of Cd(NO3)2, Z. clinopodides, CdNPs, and Daunorubicin, the DPPH test was used. The cadmium nanoparticles inhibited half of the DPPH molecules in a concentration of 196 µg/mL. To survey the cytotoxicity and anti-acute myeloid leukemia effects of Cd(NO3)2, Z. clinopodides, CdNPs, and Daunorubicin, MTT assay was used on the human acute myeloid leukemia cell lines i.e., Murine C1498, 32D-FLT3-ITD, and Human HL-60/vcr. The IC50 of the cadmium nanoparticles was 168, 205, and 210 µg/mL against Murine C1498, 32D-FLT3-ITD, and Human HL-60/vcr cell lines, respectively. In the part of in vivo study, DMBA was used for inducing acute myeloid leukemia in mice. CdNPs similar to daunorubicin ameliorated significantly (p≤0.01) the biochemical, inflammatory, RBC, WBC, platelet, stereological, histopathological, and cellular-molecular parameters compared to the other groups.ConclusionsAs mentioned, the cadmium nanoparticles had significant anti-acute myeloid leukemia effects. After approving the above results in the clinical trial studies, these cadmium nanoparticles can be used as a chemotherapeutic drug to treat acute myeloid leukemia in humans.

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Antiproliferative Activity of Silver Nanoplates on Human Promyelocytic Leukemia Cell Lines

Chemistry Letters ◽

10.1246/cl.141085 ◽

2015 ◽

Vol 44 (3) ◽

pp. 327-329 ◽

Cited By ~ 4

Author(s):

Tatsuya Sakaguchi ◽

Kenta Mine ◽

Fuki Kudoh ◽

Rui Kamada ◽

Kazuyasu Sakaguchi

Keyword(s):

Cell Lines ◽

Antiproliferative Activity ◽

Leukemia Cell ◽

Promyelocytic Leukemia ◽

Human Promyelocytic Leukemia Cell ◽

Silver Nanoplates ◽

Leukemia Cell Lines

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Evaluation of the Antiproliferative Activity of Some Nanoparticulate Essential Oils Formulated in Microemulsion on Selected Human Carcinoma Cell Lines

Current Clinical Pharmacology ◽

10.2174/1574884713666180110144336 ◽

2018 ◽

Vol 12 (4) ◽

pp. 231-244 ◽

Cited By ~ 2

Author(s):

Ahmed A. Abd-Rabou ◽

Amr E. Edris

Keyword(s):

Essential Oils ◽

Cell Lines ◽

Antiproliferative Activity ◽

Carcinoma Cell ◽

Human Carcinoma ◽

Carcinoma Cell Lines ◽

Human Carcinoma Cell

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The preparation and in vitro antiproliferative activity of phthalimide based ketones on MDAMB-231 and SKHep-1 human carcinoma cell lines

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2008.10.024 ◽

2009 ◽

Vol 44 (6) ◽

pp. 2736-2740 ◽

Cited By ~ 24

Author(s):

Sau Hing Chan ◽

Kim Hung Lam ◽

Chung Hin Chui ◽

Roberto Gambari ◽

Marcus Chun Wah Yuen ◽

...

Keyword(s):

Cell Lines ◽

Antiproliferative Activity ◽

Carcinoma Cell ◽

Human Carcinoma ◽

Carcinoma Cell Lines ◽

Human Carcinoma Cell

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Antiproliferative properties of 7,8-Ethylene Diamine Chelator-Lipophilic Fluoroquinolone Derivatives Against colorectal cancer Cell Lines

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520621666210623111744 ◽

2021 ◽

Vol 21 ◽

Author(s):

Sara Khaleel ◽

Yusuf Al-Hiari ◽

Violet Kasabri ◽

Randa Haddadin ◽

Rabab Albashiti ◽

...

Keyword(s):

Colorectal Cancer ◽

Cell Lines ◽

Cancer Cell ◽

Antiproliferative Activity ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Colorectal Cancer Cell ◽

Ethylene Diamine ◽

Dilution Method ◽

Antiproliferative Activities

Background: Cancer is one of the most overwhelming diseases nowadays. It is considered the second cause of death after cardiovascular diseases. Due to the diversity of its types, stages, and genetic origin, there is no available drug to treat all cancers. Serious side effects and resistance to existing drugs are other problems in this struggle against cancer. In such quest, fluoroquinolones (FQs) offer a future promise as antiproliferative compounds due to safety, low cost, and lack of resistance. Objectives: Therefore, this work aims at developing lipophilic FQs and screening their antiproliferative activity against colorectal cancer. Methods: Nine prepared FQs were investigated for antiproliferative activity utilizing in vitro SRB method. In comparison to the antiproliferative agent cisplatin, the assessment of antiproliferative activities of these novel FQs in a panel of colorectal cancer cell (crc) lines (HT29, HCT116, SW620, CACO2, SW480) and normal periodontal ligament fibroblasts for safety examination was performed. Antibacterial activity (MIC) was conducted against Staphylococcus aureus and Escherichia coli standard strains using the broth double dilution method. Antioxidant properties were suspected as the mechanism of antiproliferative activity; thus, a DPPH test was performed to analyze the radical scavenging potency of FQs compared to ascorbic acid as a reference agent. FQs compounds 3-5(a-c) were prepared, characterized and their structure was confirmed using spectroscopy techniques. Results: All compounds manifested good to excellent antiproliferative activity on HT29, HCT116, and SW620 with high safety index. The reduced series 4a, 4b, and 4c exerted excellent micro to nanomolar antiproliferative activities on HT29, HCT116, and SW620, which were stronger than the reference cisplatin against all cells. The reduced group of compounds 4(a-c) revealed higher potency vs. both nitro and triazolo groups. On cell lines HT29, HCT116, and SW620 reduced 4a with 7,8-ethylene diamine substitution revealed the highest antiproliferative efficacy (IC50 value) approaching nanomolar affinity with higher safety vs. cisplatin. The most active compound, 4a, exhibited significant potency against HCT116 and SW620 with IC50 0.6 and 0.16 µM, respectively. Novel FQs (4a, 4b, and 4c) also showed strong radical scavenging activity with IC50 values (µM) 0.06, 23, and 7.99, respectively. Exquisitely 4a revealed a similar pattern of activity to doxorubicin, indicating a similar mechanism of action. Strong antiproliferative and weak antibacterial activities of series 4 endorse that their mechanism involves eukaryotic topoisomerase II inhibition. This work has revealed novel FQs with excellent anticancer activity against 5 colorectal cancer (HT29, HCT116, SW620, CACO2, SW480) cell lines with a potential chelation mechanism due to 7,8-ethylene diamine chelator bridge. Conclusions: The new FQs have confirmed that more lipophilic compounds could be more active as hypothesized. The p-halogenated aniline, N1-Butyl group in addition to 3-COOH, 8-NH2 are all essential requirements for strong antiproliferative FQ of our FQ scaffold. This work emphasizes the role of C-8 amino as part of ethylene diamine group as an essential requirement for antiproliferative FQs for the first time in the literature, entailing its role toward potential antneoplastic FQs.

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Correlation between Antioxidant/Antimutagenic and Antiproliferative Activity of Some Phytochemicals

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666190528091648 ◽

2019 ◽

Vol 19 (12) ◽

pp. 1481-1490 ◽

Cited By ~ 6

Author(s):

Doaa T. Ramadan ◽

Mohamed A.M. Ali ◽

Shaymaa M. Yahya ◽

Wael M. El-Sayed

Keyword(s):

Cell Lines ◽

Anticancer Agents ◽

Antiproliferative Activity ◽

Ellagic Acid ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Liver Cells ◽

Antimutagenic Activity ◽

Apoptotic Pathway ◽

Mcf 7

Background: Chemotherapeutic drugs have high toxicity associated with undesirable side-effects. Now, natural products are the most important anti-cancer agents because of their low toxicity and potential effectiveness. Methods: The half maximal inhibitory concentration (IC50) of amygdalin, naringenin and ellagic acid against breast, colon, and liver cell lines was estimated. The antimutagenic, free radical-, superoxide radical-, and hydroxyl radical- scavenging activities of these phytochemicals were measured. The expression of p53, bid, bax, bcl2, and caspases 9, 3, and 7 was measured by quantitative real-time polymerase chain reaction (qRT-PCR) in breast and liver cells. In addition, the active Caspase 3 protein was estimated in liver cells. Results: Ellagic acid showed the highest antioxidant and antiproliferative activities. Amygdalin and naringenin with low and moderate antioxidant profiles showed a corresponding low and moderate cytotoxicity against cancer cell lines, respectively. Naringenin and ellagic acid had a significant antimutagenic activity which was detected by the Salmonella test. Ellagic acid offered a much better antimutagenic activity than naringenin. The apoptotic pathway evoked by ellagic acid in HepG2 and MCF-7 cells was investigated. The results showed that a caspase-dependent and a caspase-independent apoptosis occurred in MCF-7 and HepG2, respectively. Conclusion: The antimutagenic/antioxidant properties are well correlated with the antiproliferative activity of the phytochemicals investigated. This study proved that some easy, quick and cheap assays could predict the antiproliferative activity of many nutraceuticals. Finally, this platform could help in the discovery of new anticancer agents where hundreds of compounds are investigated in the pipeline of drug discovery.

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Abstract B82: Pinometostat (EPZ-5676) enhances the antiproliferative activity of MAP kinase pathway inhibitors inMLL-rearranged leukemia cell lines

10.1158/1535-7163.targ-15-b82 ◽

2015 ◽

Cited By ~ 2

Author(s):

Alejandra Raimondi ◽

Christine R. Klaus ◽

Jeffrey A. Keats ◽

Scott R. Daigle ◽

Robert A. Copeland ◽

...

Keyword(s):

Map Kinase ◽

Cell Lines ◽

Antiproliferative Activity ◽

Leukemia Cell ◽

Leukemia Cell Lines ◽

Map Kinase Pathway ◽

Kinase Pathway

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Assessment of the Antimicrobial, Antioxidant, and Antiproliferative Potential of Sideritis raeseri subps. raeseri Essential Oil

Foods ◽

10.3390/foods9070860 ◽

2020 ◽

Vol 9 (7) ◽

pp. 860 ◽

Cited By ~ 1

Author(s):

Gregoria Mitropoulou ◽

Marianthi Sidira ◽

Myria Skitsa ◽

Ilias Tsochantaridis ◽

Aglaia Pappa ◽

...

Keyword(s):

Oxidative Stress ◽

Dna Damage ◽

Essential Oil ◽

Cell Lines ◽

Antiproliferative Activity ◽

Inhibitory Concentration ◽

Antioxidant Properties ◽

Diffusion Method ◽

Hacat Cells ◽

Cytoprotective Activity

The aim of the present study was to investigate the antimicrobial potential of Sideritis raeseri subps. raeseri essential oil (EO) against common food spoilage and pathogenic microorganisms and evaluate its antioxidant and antiproliferative activity. The EO was isolated by steam distillation and analyzed by GC/MS. The main constituents identified were geranyl-p-cymene (25.08%), geranyl-γ-terpinene (15.17%), and geranyl-linalool (14.04%). Initially, its activity against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Listeria monocytogenes, Salmonella Enteritidis, Salmonella Typhimurium, Pseudomonas fragi, Saccharomyces cerevisiae, and Aspergillus niger was screened by the disk diffusion method. Subsequently, minimum inhibitory concentration (MIC), non-inhibitory concentration (NIC), and minimum lethal concentration (MLC) values were determined. Growth inhibition of all microorganisms tested was documented, although it was significantly lower compared to gentamycin, ciproxin, and voriconazole, which were used as positive controls. In a next step, its direct antioxidant properties were examined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, and the IC50 values were determined. The potential cytoprotective activity of the oil against H2O2–induced oxidative stress and DNA damage was studied in human immortalized keratinocyte (HaCaT) cells using the comet assay. Finally, the antiproliferative activity of the oil was evaluated against a panel of cancer cell lines including A375, Caco2, PC3, and DU145 and the non-cancerous HaCaT cell line using the sulforhodamine B (SRB) assay, and the EC50 values were determined. The oil demonstrated weak radical scavenging activity, noteworthy cytoprotective activity against H2O2–induced oxidative stress and DNA damage in HaCaT cells, and antiproliferative activity against all cell lines tested, being more sensitive against the in vitro model of skin melanoma.

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