scholarly journals Anthelmintic Activity and Cytotoxic Effects of Compounds Isolated from the Fruits of Ozoroa insignis Del. (Anacardiaceae)

Biomolecules ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 1893
Author(s):  
Mthandazo Dube ◽  
Mohamad Saoud ◽  
Robert Rennert ◽  
Ghislain Wabo Fotso ◽  
Kerstin Andrae-Marobela ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Anthelmintic Activity ◽  
Heligmosomoides Polygyrus ◽  
Cytotoxic Effects ◽  
Ic50 Value ◽  
Hookworm Infections ◽  
Newly Transformed Schistosomula ◽  
Ht 29

Ozoroa insignis Del. is an ethnobotanical plant widely used in traditional medicine for various ailments, including schistosomiasis, tapeworm, and hookworm infections. From the so far not investigated fruits of Ozoroa insignis, the anthelmintic principles could be isolated through bioassay-guided isolation using Caenorhabditis elegans and identified by NMR spectroscopic analysis and mass spectrometric studies. Isolated 6-[8(Z)-pentadecenyl] anacardic (1), 6-[10(Z)-heptadecenyl] anacardic acid (2), and 3-[7(Z)-pentadecenyl] phenol (3) were evaluated against the 5 parasitic organisms Schistosoma mansoni (adult and newly transformed schistosomula), Strongyloides ratti, Heligmosomoides polygyrus, Necator americanus, and Ancylostoma ceylanicum, which mainly infect humans and other mammals. Compounds 1–3 showed good activity against Schistosoma mansoni, with compound 1 showing the best activity against newly transformed schistosomula with 50% activity at 1µM. The isolated compounds were also evaluated for their cytotoxic properties against PC-3 (human prostate adenocarcinoma) and HT-29 (human colorectal adenocarcinoma) cell lines, whereby compounds 2 and 3 showed antiproliferative activity in both cancer cell lines, while compound 1 exhibited antiproliferative activity only on PC-3 cells. With an IC50 value of 43.2 µM, compound 3 was found to be the most active of the 3 investigated compounds.

scholarly journals APRICOXIB

2018 ◽  
Vol 25 (12) ◽  
pp. 1915-1922
Author(s):  
Fatima Rizvi ◽  
Syed Mahboob Alam ◽  
Farah Asad ◽  
Hina Shams
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Mtt Assay ◽  
Cytotoxic Effects ◽  
Inflammatory Conditions ◽  
Ic50 Value ◽  
Ht 29 ◽  
Mcf 7

Background: Breast cancer is most frequently diagnosed cancer globally but there is not any ideal economical and safer agent that not only decreases the progression but also resolve complexities associated with breast cancer such as inflammatory conditions. There was strong link between inflammation and cancer specially breast cancer. Thus by inhibiting the COX enzyme may inhibit the progression of cancer beside of its role in inflammatory conditions of breast. Study Design: Interventional In Vitro trial. Setting: Department of Pharmacology in alliance with PCMD. Period: The duration of study from April 2016 to February 2017. Methodology: For this purpose we used five cancerous lines MCF-7, MDA-MB-231, MCF-10, HT-29 and Hela cell lines. For demonstrating the cytotoxic effects of Apricoxib we used MTT assay (for all cell Lines) and Trypan blue dye exclusion assay (Primarily for MCF-7 cell lines). For calculation of minimum dose required for exert cytotoxic effects of Apricoxib and its selectivitytowards cancerous cells of breast tissue we calculated its IC50 value and Selectivity Index (SI) by MTT assay. Results: Apricoxib significantly reduce the viability of MCF-7, MDA-MB-231, Hela, HT-29 as assessed by MTT assay in dose dependent manner (χ2 (2) = 26.483, p<0.001), (χ2 (2) = 26.49, p<0.001), (χ2 (2) = 26.062, p<0.001) and (χ2 (2) = 26.062, p<0.001) respectively. However Apricoxib had non-significant effects on % viability of MCF-10 cell line (χ2 (2) = 4.167, p=0.654) as assessed by MTT assay. Furthermore Apricoxib had lowest IC50 value against MCF-7 cell line. Conclusion: This study demonstrated that beside of primarily anti-inflammatory effects Apricoxib have additional benefits in term of exerting the cytotoxic effects (in vitro) on cancerous cell lines as indicated by reducing the % viability and reducing the Absorbance value of test sample as compare to control. This opens the newer path for researcher to evaluate different aspects of Apricoxib in field of chemotherapy.

scholarly journals Extraction, Chemical Composition, and Anticancer Potential of Origanum onites L. Essential Oil

Molecules ◽  
2019 ◽  
Vol 24 (14) ◽  
pp. 2612 ◽  
Author(s):  
Katerina Spyridopoulou ◽  
Eleni Fitsiou ◽  
Eleni Bouloukosta ◽  
Angeliki Tiptiri-Kourpeti ◽  
Manolis Vamvakias ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Biological Activities ◽  
Colorectal Cancer Cell Line ◽  
Ht 29 ◽  
Origanum Onites

Origanum species are plants rich in volatile oils that are mainly used for culinary purposes. In recent years, there has been a growing interest in the biological activities of their essential oils. Origanum onites L. is a plant mainly found in Greece, Turkey, and Sicily, whose oil is rich in carvacrol, a highly bioactive phytochemical. The aim of this study was to analyze the chemical composition of Origanum onites essential oil (OOEO), and investigate its potential anticancer effects in vitro and in vivo. GC/MS analysis identified carvacrol as OOEO’s main constituent. In vitro antiproliferative activity was assayed with the sulforhodamine B (SRB) assay against human cancer cell lines from four tumor types. HT-29, a colorectal cancer cell line, was the most sensitive to the antiproliferative activity of OOEO. Wound-healing assay and Annexin V-PI staining were employed to investigate the antimigratory and the pro-apoptotic potential of OOEO, respectively, against human (HT-29) and murine (CT26) colon cancer cells. Notably, OOEO attenuated migration and induced apoptosis-related morphological changes in both cell lines. Prophylactic oral administration of the oil in a BALB/c experimental mouse model inhibited the growth of syngeneic CT26 colon tumors. As far as we know, this is the first report on the antitumor potential of orally administered OOEO.

scholarly journals Cytotoxic and Apoptotic-inducing Effect of Fraction Containing Brazilein from Caesalpinia sappan L. and Cisplatin on T47D Cell Lines

2017 ◽  
Vol 6 (3) ◽  
pp. 89
Author(s):  
Prisnu Tirtanirmala ◽  
Annisa Novarina ◽  
Rohmad Yudi Utomo ◽  
Raisatun Nisa Sugiyanto ◽  
Riris Istighfari Jenie ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Annexin V ◽  
T47d Cell ◽  
Breast Cancer Cell Lines ◽  
Cytotoxic Effects ◽  
Caesalpinia Sappan ◽  
Main Compound ◽  
T47d Breast Cancer Cell ◽  
Ic50 Value

Anticancer activity of secang’s heartwood (Caesalpinia sappan L.) is based on its main compound: brazilin and brazilein. Brazilin, brazilein, and other compounds such as caesalpiniaphenol can affect proteins that have a role in apoptosis. In this study, we observed cytotoxic activity of fraction containing brazilein (FCB) alone or in combination with chemotherapeutic agent, cisplatin and the ability of the combination to induce apoptosis in T47D breast cancer cell lines. Cytotoxicity assay was determined using MTT assay, whereas the detection apoptosis induction was conducted using flow cytometry using Annexin-V and propidium iodide. FCB and cisplatin showed cytotoxic effect on T47D cells with IC50 value of 68 µg/mL and 16 µM, respectively. Combination of FCB and cisplatin result synergistic combination at the concentration ratio of 1/2 IC50 with CI value of 0.66. Its combination also able to induce apoptosis on T47D cell population 13% larger than the single treatment. Based on this study, we conclude that FCB is able to enhance the cytotoxic effects of cisplatin by inducing apoptosis.Keywords:  Caesalpinia sappan L., cisplatin, apoptosis, breast cancer

scholarly journals Synthesis, Characterization, and Antiproliferative Activity of Novel Chiral [QuinoxP*AuCl2]+ Complexes

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5735
Author(s):  
Adedamola S. Arojojoye ◽  
R. Tyler Mertens ◽  
Samuel Ofori ◽  
Sean R. Parkin ◽  
Samuel G. Awuah
Keyword(s):  
Cell Lines ◽  
Anticancer Drugs ◽  
Antiproliferative Activity ◽  
Cytotoxic Effects ◽  
X Ray ◽  
Biologically Relevant ◽  
X Ray Crystallography ◽  
Ic50 Values ◽  
Antiproliferative Activities

Herein is reported the synthesis of two Au(III) complexes bearing the (R,R)-(–)-2,3-Bis(tert-butylmethylphosphino)quinoxaline (R,R-QuinoxP*) or (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxaline (S,S-QuinoxP*) ligands. By reacting two stoichiometric equivalents of HAuCl4.3H2O to one equivalent of the corresponding QuinoxP* ligand, (R,R)-(–)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) (1) and (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) (2) were formed, respectively, in moderate yields. The structure of (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) (2) was further confirmed by X-ray crystallography. The antiproliferative activities of the two compounds were evaluated in a panel of cell lines and exhibited promising results comparable to auranofin and cisplatin with IC50 values between 1.08 and 4.83 µM. It is noteworthy that in comparison to other platinum and ruthenium enantiomeric complexes, the two enantiomers (1 and 2) do not exhibit different cytotoxic effects. The compounds exhibited stability in biologically relevant media over 48 h as well as inert reactivity to excess glutathione at 37 °C. These results demonstrate that the Au(III) atom, stabilized by the QuinoxP* ligand, can provide exciting compounds for novel anticancer drugs. These complexes provide a new scaffold to further develop a robust and diverse library of chiral phosphorus Au(III) complexes.

Assessment of anti-cancer effects of koenimbine on colon cancer cells

2020 ◽  
Vol 28 (3) ◽  
pp. 185-190
Author(s):  
Maliheh Astaneh ◽  
Soudeh Ghafouri-Fard ◽  
Zahra Fazeli ◽  
Zahra Taherian-Esfahani ◽  
Sepideh Dashti ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Annexin V ◽  
Colon Cancer Cells ◽  
Cytotoxic Effects ◽  
Anti Cancer ◽  
Ht 29

BACKGROUND: Recent studies have highlighted the role of natural elements in reduction of cancer cell growth and apoptosis. Koenimbine, a natural product isolated from Murraya koenigii (L) Spreng is a substance with cytotoxic effects on cancer cells. AIM: The effects of koenimbine on HT-29 and SW48 colon cancer cells were evaluated by MTT and Annexin V assays. Expression levels of Wnt/β-catenin pathway genes were quantified by real time PCR. RESULTS: The IC50 values of koenimbine in HT-29 and SW48 was calculated to be 50 μg/ml based on the results of MTT assay. This value was 75 μg/ml in IEC-18 cells which were used as normal control. Annexin V assays revealed induction of cell apoptosis and necrosis in HT-29 and SW48 cells but not IEG18 cells by koenimbine. Koenimbin treatment resulted in significant down-regulation of CYCLD1 expression in SW48 cell line, but up-regulation of this gene in HT29 cell line. Expression of TBLR1, DKK1, GSK3B and β-catenin was significantly decreased after koenimbin treatment in HT-19 cell line. Moreover, expression of DKK1 and GSK3B was significantly decreased after koenimbin treatment in SW-40 cell line. TCF4 expression was not detected in any of cell lines either before or after treatment with koenimbin. CONCLUSION: The current in vitro study showed the cytotoxic effects of koenimbin on two colon cancer cell lines and the effects of this substance on expression of selected genes from Wnt-β catenin pathway. Future in vivo studies are needed before suggestion of this substance as an anti-cancer drug.

scholarly journals Silver-Chitosan Nanocomposite Prepared With Aqueous Sodium-hydroxide and Aqueous Acetic Acid Solutions: Characteristics and Their Cytotoxic Effects

2021 ◽  
Author(s):  
Laya Ebrahimi ◽  
Saeid Hosseinzadeh ◽  
Maryam Montaseri ◽  
Enayat Berizi ◽  
Mohammad Hashem Yousefi ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Cell Viability ◽  
Sodium Hydroxide ◽  
Cell Lines ◽  
Aqueous Sodium Hydroxide ◽  
Staining Procedure ◽  
Aqueous Acetic Acid ◽  
Cytotoxic Effects ◽  
Aqueous Sodium ◽  
Ht 29

Abstract In this study cytotoxic effects of silver-chitosan nanocomposites with aqueous sodium-hydroxide solution (SCNC-ASHS), and aqueous acetic acid solution (SCNC-AAAS) were evaluated, in vitro. The morphology of the synthesized nanoparticles were characterized by Fourier-Transform Infrared Spectroscopy (FTIR), and Scanning Electron Microscopy (SEM). Their cytotoxicity were then evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) in concentrations of 1.56 to 400 µg/ml, and acridine orange/ethidium bromide (AO/EB) staining after 24h and 48h. Results showed the cytotoxicity of 400 µg/ml of SCNC-ASHS on Vero and HT-29 cells of 80.57% and 84.37% after 24h, and 82.20% and 84.84% after 48h. While, the values for SCNC-AAAS on Vero and HT-29 cell-lines were respectively 80.63% and 87.64% after 24h, and 83.60% and 87.44% after 48h. The most toxicity on HT-29 cells was belonged to SCNC-AAAS with IC50 of 40.4 µg/ml. In the staining procedure, cell viability for 25 µg/ml concentration of SCNC-AAAS was 41.84% in HT-29 cell and, for 6.25 µg/ml of SCNC-AAAS was 37.51% in Vero cells. A considerable decrease in cell viability was observed. Types of nanoparticles, synthesis methods, and different cell lines play role in inducing cytotoxicity. Anti-cancer effect of the nanoparticles on the colon cancerous cells (HT-29), of that SCNC-AAAS displayed higher effect than SCNC-ASHS.

Wpływ ekstraktu z wychmielin (Humulus lupulus L.) na przeżywalność ludzkich nowotworowych i prawidłowych komórek jelita

2018 ◽  
Vol 19 (4) ◽  
Author(s):  
Miłosz Caban ◽  
Katarzyna Chojnacka ◽  
Katarzyna Owczarek ◽  
Jakub Fichna ◽  
Anna Podsędek ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Epithelial Cells ◽  
Cell Line ◽  
Cell Lines ◽  
Proliferative Activity ◽  
Humulus Lupulus ◽  
Humulus Lupulus L ◽  
Ic50 Value ◽  
Spent Hops ◽  
Ht 29

Introduction. The hop (Humulus lupulus L.) is used in the production of beer and is responsible for its taste and specific aroma. The female cones of this plant as well as the spent hops after the hops extraction by supercritical CO2 are the source of the substances with high biological activity. These include phenolic compounds among others: catechin, epicatechin, quercetin, kaempferol having a lot of properties which could be used in the medicine. They also demonstrate anti-proliferative activity which is responsible for the inhibition of the cancer cells growth. Aim. The aim of the present study was to evaluate the effect of spent hops extract on the viability of cancer and normal colon epithelial cells. Materials and methods. Three cell lines were tested: two colon cancer lines (SW-480 and HT-29) and normal epithelial colon (CCD841CoN) cell line. The activity of the spent hops extract was tested on the basis of cell growth by means of the MTT test. The cells were incubated with the tested extract at 37°C with the constant of CO2 content in atmosphere for 24, 48, 72 hours. Results. The results showed that tested extract inhibited the growth of two colon cancer cell lines (SW-480 and HT-29) more than the growth of normal cell line (CCD841CoN). The IC50 value for SW-480 cell line was obtained at the concentration 400 μg/ml after 48-hours incubation, for HT-29 cell line at the concentration 200 μg/ml after 72-hours incubation while for normal epithelial CCD841CoN cell line the IC50 value was not received. Conclusions. The spent hops extract has anti-proliferative activity. The most susceptible to extract was SW-480 cell line. The normal CCD841CoN epithelial cells were the least sensitive to the extract activity.

Synthesis, Antiproliferative, and Antioxidant Activities of Substituted N-[(1,3,4-Oxadiazol-2-yl) Methyl] Benzamines

2020 ◽  
Vol 17 (2) ◽  
pp. 145-154 ◽  
Author(s):  
Mohamed Jawed Ahsan ◽  
Lakshya Bhandari ◽  
Shally Makkar ◽  
Rajan Singh ◽  
Mohd. Zaheen Hassan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antiproliferative Activity ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Cancer Drug ◽  
Cancer Drug Discovery ◽  
Drug Concentrations ◽  
Antioxidant Agents ◽  
Ic50 Value ◽  
Mcf 7

Background: Oxadiazole emerged as an important class of heterocyclic compound with diverse biological activities like anticancer, antitubercular, anticonvulsant, anti-tubulin, antimicrobial, anti-inflammatory, antioxidant etc. Objective: The objective of this study is to synthesis series of twelve substituted N-[(1,3,4-oxadiazol-2- yl)methyl]benzamines (6a-l) and their evaluation as antiproliferative and antioxidant agents. Methods: The substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) analogues were synthesized as per the reported procedure. The antiproliferative activity was tested against nine different panels cancer cell lines (leukemia, colon, renal, non-small cell lung, breast, CNS, melanoma, prostate, and ovarian cancer) at 10 µM drug concentrations as per the NCI US Protocol. Results: 2-(5-((3-Chloro-4-fluorophenylamino)methyl)-1,3,4-oxadiazol-2-yl)phenol (6e) revealed the significant antiproliferative activity among the series of title compounds (6a-l). The compound, 6e showed maximum sensitivity towards CCRF-CEM, MCF-7, MOLT-4, T-47D, and SR cell lines with percent growth inhibitions (%GIs) of 79.92, 56.67, 39.62, 34.71 and 33.35, respectively. Furthermore, the compounds, 6e and 6c showed promising antioxidant activity with an IC50 value of 15.09 and 19.02 µM, respectively in DPPH free radicals (FR) scavenging activity.R Conclusion: The present study may support a significant value in cancer drug discovery programme.

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