scholarly journals ­Chemical profiling and biological activity of Peperomia blanda (Jacq.) Kunth

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e4839 ◽  
Author(s):  
Wafa M. Al-Madhagi ◽  
Najihah Mohd Hashim ◽  
Nasser A. Awad Ali ◽  
Abeer A. Alhadi ◽  
Siti Nadiah Abdul Halim ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Radical Scavenging ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Standard Drug ◽  
Chemical Profiling ◽  
First Time ◽  
Mcf 7

Background Peperomia belongs to the family of Piperaceae. It has different uses in folk medicine and contains rare compounds that have led to increased interest in this genus. Peperomia blanda (Jacq.) Kunth is used as an injury disinfectant by Yemeni people. In addition, the majority of Yemen’s population still depend on the traditional remedy for serious diseases such as cancer, inflammation and infection. Currently, there is a deficiency of scientific evidence with regards to the medicinal plants from Yemen. Therefore, this study was performed to assess the chemical profile and in vitro antioxidant and cytotoxic activities of P. blanda. Methods Chemical profiling of P. blanda was carried out using gas chromatography mass spectrometry (GCMS) followed by isolation of bioactive compounds by column chromatography. DPPH• and FRAP assays were used to evaluate antioxidant activity and the MTT assay was performed to estimate the cytotoxicity activity against three cancer cell lines, namely MCF-7, HL-60 and WEHI-3, and three normal cell lines, MCF10A, WRL-68 and HDFa. Results X-ray crystallographic data for peperomin A is reported for the first time here and N,N′-diphenethyloxamide was isolated for the first time from Peperomia blanda. Methanol and dichloromethane extracts showed high radical scavenging activity with an IC50 of 36.81 ± 0.09 µg/mL, followed by the dichloromethane extract at 61.78 ± 0.02 µg/mL, whereas the weak ferric reducing activity of P. blanda extracts ranging from 162.2 ± 0.80 to 381.5 ± 1.31 µg/mL were recorded. In addition, petroleum ether crude extract exhibited the highest cytotoxic activity against all the tested cancer cell lines with IC50 values of 9.54 ± 0.30, 4.30 ± 0.90 and 5.39 ± 0.34 µg/mL, respectively. Peperomin A and the isolated mixture of phytosterol (stigmasterol and β-sitosterol) exhibited cytotoxic activity against MCF-7 and WE-HI cell lines with an IC50 of (5.58 ± 0.47, 4.62 ± 0.03 µg/mL) and (8.94 ± 0.05, 9.84 ± 0.61 µg/mL), respectively, compared to a standard drug, taxol, that has IC50 values of 3.56 ± 0.34 and 1.90 ± 0.9 µg/mL, respectively. Conclusion The activities of P. blanda extracts and isolated compounds recorded in this study underlines the potential that makes this plant a valuable source for further study on anticancer and antioxidant activities.

Cytotoxic activity and anti-cancer potential of Ontario grown onion extracts against breast cancer cell lines

2018 ◽  
Vol 8 (3) ◽  
pp. 159 ◽  
Author(s):  
Meghan Fragis ◽  
Abdulmonem I. Murayyan ◽  
Suresh Neethirajan
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Cancer Line ◽  
Mcf 7

Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity

scholarly journals Synthesis, Cytotoxic Activity, Crystal Structure, DFT Studies and Molecular Docking of 3-Amino-1-(2,5-dichlorophenyl)-8-methoxy-1H-benzo[f]chromene-2-carbonitrile

Crystals ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 184
Author(s):  
Menna El Gaafary ◽  
Tatiana Syrovets ◽  
Hany M. Mohamed ◽  
Ahmed A. Elhenawy ◽  
Ahmed M. El-Agrody ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Dna Methyltransferase ◽  
Human Cancer ◽  
Theoretical Calculations ◽  
Cancer Cell Lines ◽  
Molecular Structures ◽  
Cytotoxic Activities ◽  
X Ray

The target compound 3-amino-1-(2,5-d ichlorophenyl)-8-methoxy-1H-benzo[f]-chromene-2-carbonitrile (4) was synthesized via a reaction of 6-methoxynaphthalen-2-ol (1), 2,5-dichlorobenzaldehyde (2), and malononitrile (3) in ethanolic piperidine solution under microwave irradiation. The newly synthesized β-enaminonitrile was characterized by FT-IR, 1H NMR, 13C NMR, mass spectroscopy, elemental analysis and X-ray diffraction data. Its cytotoxic activity was evaluated against three different human cancer cell lines MDA-MB-231, A549, and MIA PaCa-2 in comparison to the positive controls etoposide and camptothecin employing the XTT cell viability assay. The analysis of the Hirshfeld surface was utilized to visualize the reliability of the crystal package. The obtained results confirmed that the tested molecule revealed promising cytotoxic activities against the three cancer cell lines. Furthermore, theoretical calculations (DFT) were carried out with the Becke3-Lee-Yang-parr (B3LYP) level using 6-311++G(d,p) basis. The optimization geometry for molecular structures was in agreement with the X-ray structure data. The HOMO-LUMO energy gap of the studied system was discussed. The intermolecular-interactions were studied through analysis of the topological-electron-density(r) using the QTAIM and NCI methods. The novel compound exhibited favorable ADMET properties and its molecular modeling analysis showed strong interaction with DNA methyltransferase 1.

scholarly journals Cytotoxic Sterols from Philippine Mushrooms

2020 ◽  
Vol 32 (5) ◽  
pp. 1197-1202
Author(s):  
Consolacion Y. Ragasa ◽  
Glenn G. Oyong ◽  
Maria Carmen S. Tan ◽  
Mariquit M. De Los Reyes ◽  
Maria Ellenita G. De Castro
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Dermal Fibroblast ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Cell Viability Assay ◽  
Ic50 Values ◽  
Ht 29 ◽  
Mcf 7

Ergosterol peroxide (1) and ergosterol (2) were commonly isolated as the major compounds of Philippine mushrooms. Sterols 1 and 2 from the dichloromethane extract of Geastrum triplex and Termitomyces clypeatus, respectively, were evaluated for their cytotoxic activities against four human cancer cell lines, viz., breast cancer (MCF-7), colon cancer (HT-29), leukemia (THP-1), and small lung cell carcinoma (H69PR), and a human normal cell line, human dermal fibroblast-neonatal (HDFn), using the PrestoBlue® cell viability assay. Compounds 1 and 2 exhibited the strongest activities against HT-29 with IC50 values of 1.79 and 2.98 μg/mL, respectively, while Zeocin gave an IC50 of 4.89 μg/mL. These compounds also exhibited strong antiproliferative effects against MCF-7 with IC50 values of 4.13 for 1 and 4.20 μg/mL for compound 2, comparable to Zeocin with IC50 = 3.68 μg/mL. Only moderate cytotoxicity resulted when compounds 1 and 2 were tested against H69PR with IC50 values of 7.78 and 6.83 μg/mL, respectively, while Zeocin exhibited an IC50 of 9.81 μg/mL. Furthermore, compounds 1 and 2 showed no effects against THP-1 (IC50 > 100 μg/mL), while Zeocin showed an IC50 of 4.73 μg/mL. Although compounds 1 and 2 have been reported to exhibit different bioactivities in previous studies, the cancer cell lines tested and/or the polarities of the solvents for extraction varied. Therefore, comparisons of the cytotoxic activities of compounds 1 and 2 with earlier studies could not be made extensively.

scholarly journals Alkaloids From Zanthoxylum nitidum and Their Cytotoxic Activity

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984413
Author(s):  
Thi Hong Van Nguyen ◽  
Thi Tuyen Tran ◽  
Thi Inh Cam ◽  
Minh Quan Pham ◽  
Quoc Long Pham ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Spectroscopy Data ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Zanthoxylum Nitidum ◽  
Mcf 7

Zanthoxylum nitidum (Roxb.) DC (Rutaceae) is a traditional medicine used for the treatment of various diseases like toothache, gingivitis, fever, colic vomiting, diarrhea, and cholera. Three new alkaloids, zanthocadinanine C (1), 7-methoxy-8-demethoxynitidine (2), and zanthonitiside I (3) were isolated from the stems and twigs of Z. nitidum. Their structures were determined on the basis of extensive spectroscopic, including 1-dimensional and 2-dimensional nuclear magnetic resonance and mass spectroscopy data. Compounds 1–3 were evaluated for cytotoxic activity against 5 human cancer cell lines, KB, MCF-7, LNCaP, HepG-2, and LU-1. Compound 2 showed significant cytotoxic activity against all tested human cancer cell lines with IC50 values ranging from 10.3 to 12.6 µM.

scholarly journals Synthesis of pyrophosphate analogues and their cytotoxic activities

2021 ◽  
pp. 174751982110434
Author(s):  
Van-Tai Nguyen ◽  
Minh-Quan Pham ◽  
Thi-Ha Vu ◽  
Thi-Hong-Ha Tran ◽  
Duy-Tien Doan ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Dipolar Cycloaddition ◽  
Cytotoxic Activities ◽  
Cycloaddition Reactions

Six pyrophosphate analogues are prepared from zerumbone, murrayafoline A, acridone, and 4-hydroxycoumarin via 1,3-dipolar cycloaddition reactions. Their in vitro cytotoxic activity is evaluated against HepG2, LU-1, and HeLa cancer cell lines. Among them, diisopropyl ((ethoxy((4-((1-methoxy-3-methyl-9 H-carbazol-9-yl)methyl)-1 H-1,2,3-triazol-1-yl)methyl)phosphoryl)methyl)phosphonate (6a) and diisopropyl ((ethoxy((4-(((3-methyl-9 H-carbazol-1-yl)oxy)methyl)-1 H-1,2,3-triazol-1-yl)methyl)phosphoryl)methyl)phosphonate (6b) are found to show activity against HepG2, LU-1, and HeLa cancer cell lines, with IC50 values ranging from 7.31 to 17.88 μM.

scholarly journals In Vitro Evaluation of Cytotoxic Activities of Marketed Herbal Products in Ghana

2018 ◽  
Vol 23 ◽  
pp. 2515690X1879072 ◽  
Author(s):  
Sylvester Languon ◽  
Isaac Tuffour ◽  
Emmanuel Ekow Quayson ◽  
Regina Appiah-Opong ◽  
Osbourne Quaye
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Jurkat Cells ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Hep G2 ◽  
Herbal Products ◽  
Mcf 7

There are numerous herbal products on the Ghanaian market that are purported to cure various ailments, including cancer. However, scientific investigations on efficacy and toxicity of most of these products are not done. The aim of the study was to assess the anticancer potentials of herbal products on the Ghanaian market. Antiproliferative effects of Kantinka BA (K-BA), Kantinka Herbaltics (K-HER), Centre of Awareness (COA), a stomach (STO) and multicancer (MUT) product were evaluated in vitro using liver (Hep G2), breast (MCF-7), prostate (PC-3 and LNCaP), and blood (Jurkat) cancer cell lines. Cytotoxicity of the medicinal products was assessed using tetrazolium-based colorimetric assay, and total phenolic content and antioxidant activity of the products were determined using Folin-Ciocalteau and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays, respectively. Phytochemical screening resulted in the detection of terpenoids and flavonoids in most of the products, and alkaloids were detected in only MUT. Tannins were absent from all the products. The highest and lowest concentrations of phenolics were recorded for MUT and K-BA, respectively. The highest and lowest antioxidant activities were measured for MUT and K-HER, respectively. Only 2 products (STO and MUT) were cytotoxic to Hep G2 cells; with MUT being the only product that was cytotoxic to MCF-7 cells. All but K-BA were cytotoxic to PC-3 cells, while all products except K-HER were cytotoxic to LNCaP and Jurkat cells. The study thus confirms that the herbal products have selective cytotoxic activities against the tested cancer cell lines. However, comprehensive toxicity studies must be conducted to establish their safety.

scholarly journals Synthesis of Novel 2(3H)-Benzoxazolone Mannich Bases as Potential Agents for Future Studies of Cancer Treatment

2021 ◽  
pp. 23-30
Author(s):  
Emine Erdag
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
In Silico ◽  
Cancer Cell Lines ◽  
Mannich Bases ◽  
Pharmaceutical Chemistry ◽  
Cytotoxic Activities ◽  
In Silico Prediction ◽  
Cytotoxicity Studies

Aims: In this study, a series of new Mannich bases of 2(3H)-benzoxazolone derivatives containing substituted cyclic amine moieties with a potential to show cytotoxic activity have been prepared. In order to develop effective anticancer agents against various cancer cell lines, it is essential to study the structure activity relationship and the effect of different substituents on the activity of heterocyclic scaffolds which were known to have cytotoxic activities. Study Design: In silico and experimental design. Place and Duration of Study: Pharmaceutical Chemistry Department, Faculty of Pharmacy, Near East University, Nicosia, Cyprus, between January 2019- September 2020. Methodology: In this work, 2(3H)-benzoxazolone derivatives were prepared by Mannich reaction. The synthesis and structural characterization of the compounds were performed experimentally by FT-IR, 1H NMR, 13C NMR spectra and elemental analysis. In silico prediction of cell line cytotoxicity with PASS based CLC-Pred tool was performed to predict cytotoxicity of the compounds against different tumor cell lines. Results: In silico prediction results for the compounds showed that all benzoxazolone derivatives have cytotoxic activity against different cell lines and tumor types. It was clearly understood that the cytotoxicity of the compounds was affected by the substituents on their piperazine moieties and by the substituents on benzoxazolone core structure. Conclusion: In conclusion, newly synthesized Mannich bases of benzoxazolone derivatives were reported for the first time which may have a potential to show anticancer activities at different cancer cell lines. The efficiency of new compounds against cancer could be found via PASS based CLC-Pred database and could be further investigated by in vivo experimental cytotoxicity studies in the future to design new anticancer drug candidates.

scholarly journals ANTIPROLIFERATIVE ACTIVITY OF ELEPHANTOPUS SCABER MEDIATED SILVER NANOPARTICLES AGAINST MCF-7, A-549, SCC-40, AND COLO-205 HUMAN CANCER CELL LINES

2019 ◽  
pp. 163-167
Author(s):  
ASHWINI S SHINDE ◽  
VIJAY D MENDHULKAR
Keyword(s):  
Silver Nanoparticles ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Synergistic Activity ◽  
Standard Drug ◽  
Elephantopus Scaber ◽  
The Impact ◽  
Mcf 7

Objective: To unearth the applications of nanotechnology in medicine has become imperative with all the advancements in the technique. In the current study, we have attempted to exploit the anticancer ability of the green synthesized silver nanoparticles (AgNPs). Methods: The AgNPs were synthesized using 60% methanol (H-MeOH) Elephantopus scaber leaf extract, characterized, and discussed priorly. The effect of AgNPs was studied on the human breast (MCF-7), lung (A-549), oral (SCC-40), and colon (COLO-205) cancer cell lines through sulforhodamine B assay. We also carried out the synergistic activity with standard drug adriamycin (ADR). Results: According to the results obtained, AgNPs showed good antiproliferative activity with GI50 <10 μg/ml on MCF-7, A-549, and SCC-40 cell lines when compared with the standard drug ADR. However, for COLO-205 cell line, the impact was 17.4 μg/ml and thus the treatment was less effective. Conclusion: The synergistic effect of AgNPs+ADR was even better for all the four cell lines than that of the AgNPs alone.

scholarly journals Biological Effects of Glucosinolate Degradation Products from Horseradish: A Horse that Wins the Race

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 343 ◽  
Author(s):  
Marijana Popović ◽  
Ana Maravić ◽  
Vedrana Čikeš Čulić ◽  
Azra Đulović ◽  
Franko Burčul ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Degradation Products ◽  
Human Cancer ◽  
Biological Activities ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Minimal Inhibitory Concentrations

Horseradish degradation products, mainly isothiocyanates (ITC) and nitriles, along with their precursors glucosinolates, were characterized by GC-MS and UHPLC-MS/MS, respectively. Volatiles from horseradish leaves and roots were isolated using microwave assisted-distillation (MAD), microwave hydrodiffusion and gravity (MHG) and hydrodistillation (HD). Allyl ITC was predominant in the leaves regardless of the isolation method while MAD, MHG, and HD of the roots resulted in different yields of allyl ITC, 2-phenylethyl ITC, and their nitriles. The antimicrobial potential of roots volatiles and their main compounds was assessed against sixteen emerging food spoilage and opportunistic pathogens. The MHG isolate was the most active, inhibiting bacteria at minimal inhibitory concentrations (MICs) from only 3.75 to 30 µg/mL, and fungi at MIC50 between <0.12 and 0.47 µg/mL. Cytotoxic activity of volatile isolates and their main compounds were tested against two human cancer cell lines using MTT assay after 72 h. The roots volatiles showed best cytotoxic activity (HD; IC50 = 2.62 μg/mL) against human lung A549 and human bladder T24 cancer cell lines (HD; IC50 = 0.57 μg/mL). Generally, 2-phenylethyl ITC, which was tested for its antimicrobial and cytotoxic activities along with two other major components allyl ITC and 3-phenylpropanenitrile, showed the best biological activities.

Design, Synthesis, and Cytotoxic Activity of New Tubulysin Analogues

Synlett ◽  
2021 ◽  
Author(s):  
Anh Tuan Tran ◽  
Chien Van Tran ◽  
Hai Van Le ◽  
Loc Van Tran ◽  
Thao Thi Phuong Tran ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Ht 29

AbstractSynthesis of tubulysin analogues, containing an N-methyl substituent on tubuvaline-amide together with the replacement of either the hydrophobic N-terminal N-methyl pipecolic acid (Mep) or at both N- and C- terminal peptides with available heteroaromatic acids and an unsaturated tubuphenylalanine moiety, respectively, were described. The in vitro cytotoxic activity by SRB assay on five cancer cell lines for sixteen tubulysins was evaluated. Among them, five analogues exhibited strong cytotoxic activities against five human cancer cell lines, including human breast carcinoma (MCF7), human colorectal adenocarcinoma (HT-29), HL-60, SW-480, human lung adenocarcinoma (A459). Interestingly, one analogue showed the strongest cytotoxicity on all five tested cell lines even much higher toxicity than the reference compound ellipticine.

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