scholarly journals The Anticancer Activity of Phytoconstituents of the Stem of Bouea macrophylla

2021 ◽  
Vol 14 (4) ◽  
pp. 1955-1964
Author(s):  
Tarso Rudiana ◽  
Nani Suryani ◽  
Dimas D. Indriatmoko ◽  
Yusransyah Yusransyah ◽  
Muhammad A. Hardiyanto ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Line ◽  
Cell Lines ◽  
Metastatic Breast ◽  
Alveolar Epithelial Cells ◽  
Ic50 Values ◽  
Stem Extract ◽  
Mcf 7

Gandaria (Bouea macrophylla Griff) is a typical Asian plant that is commonly found in In-donesia with various secondary metabolite compounds such as phenolic, flavonoid and ter-penoid. The purpose of this study was to isolate secondary metabolites from the stem extract of B. macrophylla and determine their activity against cancer cells MCF-7, A549, MDA-MB 231 and HCC-1954. The isolation of the compounds was conducted using various chromatographic techniques, the determination of the chemical structure of the isolates was performed using physicochemical methods including mass spectrometer and nuclear magnetic resonance, the determination of anticancer activity was carried out using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) i.e. MCF-7 and A549 cell lines; and dimetiltiazol-2-il) -2,5-diphenyltetrazolium bromide (MTT) for MDA-MB 231 and HCC-1954 cell lines. Four compounds namely stigmasterol (1), fustin (2), garbanzol (3) and methyl galat (4) were successfully isolated from the stem extract of B. macrophylla, which was obtained from Serang Regency, Indonesia. These compounds were then tested their anticancer activity against the cancer cells of Michigan Cancer Foundation-7 (MCF-7), human alveolar epithelial cells (A549), human breast cancer cell line-1954 (HCC-1954) and M.D. Anderson-Metastatic Breast-231 (MDA-MB-231). The results of anticancer test indicated that based on the IC50 values for all compounds tested, the compounds 2 and 4 were more active on HCC-1954 cell with IC50 values of 134.35 ± 44.62 and 153.69 ± 12.54 µg/mL, respectively, while the compound 3 was found to be the most active against MDA-MB-231 cell line with IC50 value of 233.41 ± 91.57 µg/mL

scholarly journals Antiproliferative Activity, Proapoptotic Effect, and Cell Cycle Arrest in Human Cancer Cells of Some Marine Natural Product Extract

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Hong Cui ◽  
Mansour A. E. Bashar ◽  
Islam Rady ◽  
Hussein A. El-Naggar ◽  
Lamiaa M. Abd El-Maoula ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Line ◽  
Antiproliferative Activity ◽  
Hepg2 Cell Line ◽  
Cycle Arrest ◽  
Ic50 Values ◽  
Hct 116 ◽  
Mcf 7

Bioactive constituents of numerous marine organisms have been investigated recently for their preclinical and clinical anticancer activity. Three marine organisms: black-spotted sea cucumber: Pearsonothuria graeffei (Pg), lollyfish: Holothuria atra (Ha), and sea hare: Aplysia dactylomela (Ad), were collected during winter 2019 from Gulf of Aqaba, Red Sea, Egypt, and macerated with ethanol into three different extracts: PgE, HaE, and AdE, where each was in vitro assessed for its antiproliferative and proapoptotic properties on HepG2, HCT-116, and MCF-7 cancer cells. PgE dose-dependently inhibited the growth of HepG2, HCT-116, and MCF-7 cells within IC50 values 16.22, 13.34, and 18.09 μg/mL, respectively, while the IC50 values for the antiproliferative activity of HaE were 12.48, 10.45, and 10.36 μg/mL, respectively, and the IC50 values of AdE were 6.51, 5.33, and 6.87 μg/mL, respectively. All extracts were found to induce G0/G1 cell cycle arrest for HepG2 cells side by side with their inhibition of CDK2 on all three cell lines while all extracts were also showed to induce apoptosis in HepG2 cell line at pre-G1 phase supplemented by their anticancer activity via proapoptotic protein Bax, caspase-3, and cleavage PARP increase, and antiapoptotic protein Bcl-2 downturn. Moreover, necrosis has been relatively noticed in HepG2 cell line as an additional anticancer activity for each extract. Our data introduced three ethanolic marine extracts as natural chemotherapeutic agents to be further developed for cancer control.

scholarly journals The influence of a single and double biotinylation of xanthohumol on its anticancer activity

2019 ◽  
Author(s):  
Monika Stompor ◽  
Marta Świtalska ◽  
Joanna Wietrzyk
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Growth Inhibitor ◽  
Breast Cancer Cell Lines ◽  
Active Growth ◽  
Ic50 Values ◽  
4T1 Breast Cancer ◽  
Mcf 7

Two biotinylated derivatives of the main hop chalcone xanthohumol (1) were prepared by a one-step synthesis via esterification using biotin and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC×HCl) and 4-dimethylaminopyridine (DMAP) as coupling reagents. The products were characterized spectroscopically and their antiproliferative activity toward MCF-7, MCF-10A, HepG2, MDA-MB-231, 4T1 and Balb/3T3 cell lines was investigated using the SRB assay. For all three tested compounds the best activity was noted in the case of human (MCF-7) and mice (4T1) breast cancer cell lines (IC50 values < 9 μM). Both biotinylated derivatives showed slightly higher anticancer activity than xanthohumol (1) towards all types of tested breast cancer cells. Double biotinylated xanthohumol (3) proved to be the most active in inhibiting cell growth, with IC50 values equal to 5.35 ± 1.5 μM for 4T1 and 8.03 ± 0.53 µM for MCF-7 cell lines. Compound 3 was also more active than 1 and 2 against liver cancer cells HepG2 (IC50 = 17.37 ± 5.1 μM), while the IC50 values for 1 and 2 were equal to 21.5 ± 2.7 and 22.1 ± 3.9 µM, respectively. 4‑O‑biotinylxanthohumol (2) was the second most active growth inhibitor, particularly with respect to MCF-7 (IC50 = 6.19 ± 1.7 μM) and 4T1 (IC50 = 6.64 ± 0.4 μM) cell lines. Our preliminary study on biotinylated xanthohumol (1) have shown that this type of functionalization is an effective method for the production of active biomolecules and study on this area should be continued thereby extending their applications.

scholarly journals Comparison of the effect of rhodium citrate-associated iron oxide nanoparticles on metastatic and non-metastatic breast cancer cells

2019 ◽  
Vol 10 (1) ◽  
Author(s):  
Natalia Lemos Chaves ◽  
Danilo Aquino Amorim ◽  
Cláudio Afonso Pinho Lopes ◽  
Irina Estrela-Lopis ◽  
Julia Böttner ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Lines ◽  
Breast Cancer Cells ◽  
Human Tumor ◽  
Metastatic Breast ◽  
Cytotoxic Action ◽  
Dependent Manner ◽  
Metastatic Cells ◽  
Mcf 7

Abstract Background Nanocarriers have the potential to improve the therapeutic index of currently available drugs by increasing drug efficacy, lowering drug toxicity and achieving steady-state therapeutic levels of drugs over an extended period. The association of maghemite nanoparticles (NPs) with rhodium citrate (forming the complex hereafter referred to as MRC) has the potential to increase the specificity of the cytotoxic action of the latter compound, since this nanocomposite can be guided or transported to a target by the use of an external magnetic field. However, the behavior of these nanoparticles for an extended time of exposure to breast cancer cells has not yet been explored, and nor has MRC cytotoxicity comparison in different cell lines been performed until now. In this work, the effects of MRC NPs on these cells were analyzed for up to 72 h of exposure, and we focused on comparing NPs’ therapeutic effectiveness in different cell lines to elect the most responsive model, while elucidating the underlying action mechanism. Results MRC complexes exhibited broad cytotoxicity on human tumor cells, mainly in the first 24 h. However, while MRC induced cytotoxicity in MDA-MB-231 in a time-dependent manner, progressively decreasing the required dose for significant reduction in cell viability at 48 and 72 h, MCF-7 appears to recover its viability after 48 h of exposure. The recovery of MCF-7 is possibly explained by a resistance mechanism mediated by PGP (P-glycoprotein) proteins, which increase in these cells after MRC treatment. Remaining viable tumor metastatic cells had the migration capacity reduced after treatment with MRC (24 h). Moreover, MRC treatment induced S phase arrest of the cell cycle. Conclusion MRC act at the nucleus, inhibiting DNA synthesis and proliferation and inducing cell death. These effects were verified in both tumor lines, but MDA-MB-231 cells seem to be more responsive to the effects of NPs. In addition, NPs may also disrupt the metastatic activity of remaining cells, by reducing their migratory capacity. Our results suggest that MRC nanoparticles are a promising nanomaterial that can provide a convenient route for tumor targeting and treatment, mainly in metastatic cells.

Synthesis and Reactivity of 6,8-Dibromo-2-ethyl-4H-benzo[d][1,3]oxazin-4-one Towards Nucleophiles and Electrophiles and Their Anticancer Activity

2019 ◽  
Vol 19 (4) ◽  
pp. 538-545 ◽  
Author(s):  
Maher A. El-hashash ◽  
Amira T. Ali ◽  
Rasha A. Hussein ◽  
Wael M. El-Sayed
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Repair Mechanisms ◽  
Breast Cells ◽  
Nitrogen Nucleophiles ◽  
Quinazolinone Derivatives ◽  
Benzaldehyde Derivatives ◽  
Mcf 7

Background: The genetic heterogeneity of tumor cells and the development of therapy-resistant cancer cells in addition to the high cost necessitate the continuous development of novel targeted therapies. Methods: In this regard, 14 novel benzoxazinone derivatives were synthesized and examined for anticancer activity against two human epithelial cancer cell lines; breast MCF-7 and liver HepG2 cells. 6,8-Dibromo-2- ethyl-4H-benzo[d][1,3]oxazin-4-one was subjected to react with nitrogen nucleophiles to afford quinazolinone derivatives and other related moieties (3-12). Benzoxazinone 2 responds to attack with oxygen nucleophile such as ethanol to give ethyl benzoate derivative 13. The reaction of benzoxazinone 2 with carbon electrophile such as benzaldehyde derivatives afforded benzoxazinone derivatives 14a and 14b.The structure of the prepared compounds was confirmed with spectroscopic tools including IR, 1H-NMR, and 13C-NMR. Results: Derivatives 3, 9, 12, 13, and 14b exhibited high antiproliferative activity and were selective against cancer cells showing no toxicity in normal fibroblasts. Derivative 3 with NH-CO group in quinazolinone ring was effective only against breast cells, while derivative 12 with NH-CO group in imidazole moiety was only effective against liver cells probably through arresting cell cycle and enabling repair mechanisms. The other derivatives (9, 13, and 14b) had broader antiproliferative activity against both cell lines. These derivatives enhance the expression of the p53 and caspases 9 and 3 to varying degrees in both cell lines. Derivative 14b caused the highest induction in the investigated genes and was the only derivative to inhibit the EGFR activity. Conclusions: The unique features about derivative 14b could be attributed to its high lipophilicity, high carbon content, or its extended conjugation through planar aromatic system. More investigations are required to identify the lead compound(s) in animal models.

scholarly journals Synthesis and Anticancer Activity Evaluation of Hydrolyzed Derivatives of Panaxnotoginseng Saponins

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 3021 ◽  
Author(s):  
Lei Xu ◽  
Shengnan Xiao ◽  
Weihui Yuan ◽  
Jiongmo Cui ◽  
Guangyue Su ◽  
...  
Keyword(s):  
Salicylic Acid ◽  
Epithelial Cells ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Human Lung Cancer ◽  
Cytotoxicity Test ◽  
Mcf 7

To increase the antitumor activity of ginsenosides and acetylsalicylic acid, acid hydrolysis products of Panaxnotoginseng saponin were used as raw materials to be combined with salicylic acid to obtain ginsenoside salicylic acid derivatives. All derivatives were assessed for anti-cancer activity. A total of 20 target compounds were designed and synthesized. The cytotoxic activity on five cancer cell lines, including human colon cancer (HT-29), gastric cancer (BGC-823), cervical cancer (Hela), human breast cancer (MCF-7), human lung cancer cells (A549), and two normal cancer cell lines (human gastric epithelial cells (GES-1), and human ovarian epithelial cells (IOSE144)) was evaluated following treatment with the compounds. The results showed that all compounds inhibited the growth of cancer cells. Compounds 1a, 3a, 7a, 1b, 2b, 3b and 8b showed strong anticancer activity. For MCF-7 cells, compound 3b showed the strongest inhibitory activity, IC50 = 2.56 ± 0.09 μM. In the cytotoxicity test, all compounds showed low toxicity or no toxicity (IC50 > 100 μM). In addition, a cell cycle distribution assay and wound healing assay demonstrated that compound 3b specifically inhibited MCF-7 proliferation and migration ability. Our results indicate that compound 3b represents a promising compound for further cancer studies.

scholarly journals Biotinylated xanthohumol: synthesis and in vitro biological evaluation for anticancer therapy

2018 ◽  
Author(s):  
Monika Stompor ◽  
Rafał Podgórski ◽  
Marta Świtalska ◽  
Joanna Wietrzyk
Keyword(s):  
Breast Cancer ◽  
Antioxidant Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Biological Evaluation ◽  
Breast Cancer Cell Lines ◽  
Dpph Method ◽  
Ic50 Values ◽  
Mcf 7

Two biotinylated derivatives of the main hop chalcone xanthohumol (1) were prepared by a one-step synthesis via esterification using biotin and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC HCl) and 4-dimethylaminopyridine (DMAP) as coupling reagents. The products were characterized spectroscopically and their antiproliferative activity toward MCF-7, MCF-10A, HepG2, MDA-MB-231, 4T1 and Balb/3T3 cell lines was investigated using the SRB assay. For all three tested compounds the best activity was noted in the case of human (MCF-7) and mice (4T1) breast cancer cell lines (IC50 values &lt; 9 &mu;M). Both biotinylated derivatives showed higher anticancer activity than xanthohumol (1) towards all types of tested breast cancer cells. Double biotinylated xanthohumol (3) proved to be the most active in inhibiting cell growth, with IC50 values equal to 5.35 &plusmn; 1.5 &mu;M for 4T1 and 8.03 &plusmn; 0.53 &micro;M for MCF-7 cell lines. Compound 3 was also more active than 1 and 2 against liver cancer cells HepG2 (IC50 = 17.37 &plusmn; 5.1 &mu;M), while the IC50 values for 1 and 2 were equal to 21.5 &plusmn; 2.7 and 22.1 &plusmn; 3.9 &micro;M, respectively. 4‑O‑biotinylxanthohumol (2) was the second most active growth inhibitor, particularly with respect to MCF-7 (IC50 = 6.19 &plusmn; 1.7 &mu;M) and 4T1 (IC50 = 6.64 &plusmn; 0.4 &mu;M) cell lines. The antioxidant activity was evaluated using the 1.1-diphenyl-2-picrylhydrazyl radical (DPPH) method. All tested compounds (1-3) have antioxidant activity between 2.73 and 3.38 mM. It was reported for the first time that new prenylated chalcones containing the biotin moiety effectively inhibited proliferation of cancer cells in vitro.

Novel Artemisinin-Derived Dimers: Synthesis and Evaluation of Anti-cancer Activities

2016 ◽  
Vol 14 (1) ◽  
pp. 102-111 ◽  
Author(s):  
Vu Tuan Kien ◽  
Le Huy Binh ◽  
Phan Hai Phong ◽  
Doan Thi Hien ◽  
Nguyen Thi Thuy My ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Anticancer Compounds ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Mcf 7

In continuation of our study on anticancer compounds, a series of novel artemisinin dimers have been synthesized and evaluated for their cytotoxic effects against three human cancer cell lines, including HepG2 (liver cancer), MCF-7(breast cancer) and HL-60 (leukemia cancer). The assay results showed that most of the compounds displayed inhibitory effects against all three human cancer cell lines tested, and seemed to be more cytotoxic toward the blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. Among the synthesized artemisinin dimers, the compound 10d with a double bond bridge exhibited the most potent cytotoxicity with IC50 values of 5.08, 4.82 and 1.32 µg/mL against the HepG2, MCF-7, and HL-60 cell lines, respectively.

scholarly journals CYTOTOXICITY OF METABOLITES PRODUCED BY ENDOPHYTIC FUNGUS CLADOSPORIUM SP. ISOLATED FROM MARINE MACROALGAE ON IN­VITRO MCF­7, HELA, AND DU-145 CELL LINES

2018 ◽  
Vol 10 (8) ◽  
pp. 72
Author(s):  
Asri Peni Wulandari ◽  
R. R. Indry Noviarin Examinati ◽  
Madihah . ◽  
Desi Harneti Putri Huspa ◽  
Poniah Andayaningsih ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Ethyl Acetate Extract ◽  
In Vitro Cytotoxicity ◽  
Marine Macroalgae ◽  
Morphological Alteration ◽  
Mcf 7

Objective: To investigate the in vitro cytotoxicity effect of the crude ethyl acetate extract of Cladosporium sp. on MCF-7, HeLa, and DU-145 cell lines.Methods: In vitro cytotoxicity was evaluated by tetrazolium reduction assay. The percentage of cell inhibition was analyzed using probit analysis to obtain 50% inhibitory concentration (IC50). Morphological alteration of the cell lines after exposure with extract was observed under an inverted microscope.Results: The ethyl acetate extract of the metabolite performed an anticancer activity for cancer cell line MCF-7, HeLa, and DU-145 with IC50 respectively 8.46 μg/ml; 9.87 μg/ml; and 98.03 μg/ml. The extract shows greater the anticancer activity and has strong antiproliferative on MCF-7 and HeLa cell line than DU-145. Confirmation morphological were observed under the inverted microscope showed a morphological change in cancer cells when incubated with the extract.Conclusion: From the performed assay, the crude extract of Cladosporium sp. exhibit cytotoxic activity against MCF-7, HeLA, and DU-145.

scholarly journals Thiazolidinedione or Rhodanine: A Study on Synthesis and Anticancer Activity Comparison of Novel Thiazole Derivatives

2017 ◽  
Vol 20 (1) ◽  
pp. 415 ◽  
Author(s):  
Cigdem Ozen ◽  
Meltem Ceylan Unlusoy ◽  
Nazanin Aliary ◽  
Mehmet Ozturk ◽  
Oya Bozdag Dundar
Keyword(s):  
Hepatocellular Carcinoma ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Condensation Reaction ◽  
Huh7 Cell ◽  
Anticancer Activities ◽  
Thiazole Derivatives ◽  
Ic50 Values ◽  
Huh7 Cell Line

Purpose: A new series of thiazolyl-2,4-thiazolidinedione / rhodanine compounds T1-T23 was synthesized and tested for their anticancer activities. Hepatocellular carcinoma cell lines were chosen due to their strong drug resistance to test the new compounds. Methods: All compounds were synthesized via Knoevenagel Condensation reaction and thiazolidinedione ester compounds (T3,T9,T15,T20) were hydrolyzed for obtaining the acidic compounds (T6,T12,T17,T23). All compounds were firstly screened for their anticancer activity against two hepatocellular carcinoma (HCC) cell lines, Huh7 and Plc/Prf/5 (Plc) cell lines by sulforhodamine B assay. Further IC50 values were calculated for three candidates (T4, T15, T21) in five different HCC (Huh7, Plc, Snu449, HepG2, Hep3B) and one breast cancer (Mcf7) cell line. Results: Compounds T4, T15, T21 had very strong anticancer effects even though their 10 µM concentration in Huh7 cell line. According to IC50 values, T21 was the most effective compound with IC50 values in a range from 2 to 16 µM in 6 cancer cell lines. In terms of cytotoxicity T21 mostly affected Huh7 and interestingly it was less effective against Plc. Conclusions: Considering these results it can be suggested that compounds T4, T15 and T21 may lead to the development of more potent anticancer drugs in the future. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals EVALUATION OF IN VITRO ANTICANCER ACTIVITY OF AERIAL PARTS OF AVICENNIA ALBA PLANT METHANOLIC EXTRACT AGAINST HELA AND MCF-7 CELL LINES

2021 ◽  
pp. 73-79
Author(s):  
RA ZERUBABEL MICHAEL
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Methanolic Extract ◽  
Inhibitory Effect ◽  
Mangrove Plant ◽  
Standard Drug ◽  
Ic50 Values ◽  
Avicennia Alba ◽  
Mcf 7

Objective: The current study emphasizes the effects of stem and leaf methanolic extract of mangrove plant Avicennia alba on human tumor cell lines HeLa and MCF-7. Method: The collected mangrove plant sample was subjected to extraction with methanol and screened for anticancer activity according to 3-(4,5-dimethythiazol- 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay method. The ability of the plant extract to inhibit the proliferation of HeLa and MCF-7 cell lines procured from NCCS Pune was compared parallel to inhibitory effect of standard drug Cisplatin. The spectrophotometric optical densities obtained were plotted on graph and consecutive data were obtained to depict the inhibitory effect and IC50 values. The histopathology studies were also done for a clear insight to understand the depth of inhibition microscopically. Results: The MTT assay performed illustrates the plant samples with different concentrations (10, 20, 25, 30, and 50 μg) showed significant inhibitory effect on comparison with the standard drug Cisplatin. The IC50 values and the inhibitory OD values elucidate effective projection of plant as a potential source of anticancer activity based on comparative study. The histopathology studies revealed an insight to a clearer picture of how the cells growth was controlled. It was found that the methanolic extract of A. alba exhibited more activity against HeLa cell lines than MCF-7 cell lines. Conclusion: The synergistic effect of various phytochemicals present in the methanolic plant extract played a significant role in establishing the plant as a significant anticancer source.

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