scholarly journals BIOACTIVE MARINE-DERIVED COMPOUNDS AS POTENTIAL ANTICANCER CANDIDATES

2018 ◽  
Vol 11 (11) ◽  
pp. 464 ◽  
Author(s):  
Mona S Ellithey ◽  
Hanaa H Ahmed
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Radical Scavenging Activity ◽  
Research Work ◽  
Radical Scavenging ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Vitro Assay ◽  
Safety Margins

Objective: The objective of this research was to evaluate for the 1st time the anticancer activities of sarcophytol M (1), alismol (2), alismoxide (5), 7β-acetoxy-24-methylcholesta-5-24(28)-diene-3,19-diol (7), erythro-N-dodecanoyl-docosasphinga-(4E,8E)-dienine (8), and 24 methylcholesta- 5,24(28)-diene-3β,7β,19-triol (9). Compounds were isolated from the soft coral Lithophyton arboreum and tested in liver (HepG2), lung (A549), and breast (MDA) cancer cell line.Methods: Anticancer activities of the compounds were tested using (XTT) 2,3-bis-(2-methoxy-4-nitro- 5-sulfophenyl)-2H-tetrazolium-5-carboxanilide, Na2) in vitro assay in order to estimate the cytotoxicity and to determine the IC50s. The free radical scavenging activity of the compounds were measured by 1,1-diphenyl-2-picryl-hydrazil (DPPH•). All compounds were screened at 100 μg/ml while the most potent active compounds were assayed at lower concentrations.Results: Compounds (7) and (9) showed a strong cytotoxic effect with IC50 of 6.07, 8.5 μg/ml in HepG2, 6.3, 5.5 μg/ml in MDA cells, and 5.2, 9.3 μg/ml in A549 cancer cell lines, respectively. In addition, moderate cytotoxicity was shown by compound (2) (IC50 16.5, 15, and 13 μg/mL) in HepG2, MDA, and A549 cancer cell lines, respectively.Conclusion: The results obtained in this research work indicated a promising potential cytotoxicity of compounds (7) and (9) compared to its safety margins in Vero cells, and the expected cytostatic effect of compound (2) can be used in drug cocktails for the treatment of the major cancer types’ lung, breast, and liver cancer. 

scholarly journals Some Wild Edible Mushroom Anticancer Activity Against Prostate Cell Lines

Proceedings ◽  
2019 ◽  
Vol 40 (1) ◽  
pp. 40
Author(s):  
Hatice Bekci ◽  
Mustafa Cam ◽  
Ahmet Cumaoglu
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Prostate Cancer Cell ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Prostate Cancer Cell Lines ◽  
Prostate Cell

Prostate cancer is one of the cause of mortality and morbidity in men. High nutritional quality mushrooms have been consumed as food for a long time and Thanks to their bioactive components, they can be used in many fields such as pharmaceuticals, cosmetic products, dietary supplements and functional food production. The purpose of the research was to evaluate these derivatives against in vitro to obtain novel specific and effective anticancer agents against prostate cancer. In the study, Amanita caesarea, Sparassis crispa, Lepista nuda, Auricularia auricula, Tricholoma terreum and Lentinus tigrinus fungi were used. Anticancer activities of the compounds were evaluated in vitro by using MTT method against PC-3 and DU-143 (androgen-independent human prostate cancer cell lines) prostate cancer cell lines. Cisplatin was used as the positive sensitivity reference standard. The most effective among these fungus species biological activity against PC3 cancer cell line (IC50 = 327.34 µM), against DU-145 (IC50 = 459.19 µM).

scholarly journals Trastuzumab gold-conjugates: synthetic approach and in vitro evaluation of anticancer activities in breast cancer cell lines

2019 ◽  
Vol 55 (10) ◽  
pp. 1394-1397 ◽  
Author(s):  
Natalia Curado ◽  
Guillaume Dewaele-Le Roi ◽  
Sophie Poty ◽  
Jason S. Lewis ◽  
Maria Contel
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Trojan Horse ◽  
Breast Cancer Cell Lines ◽  
Synthetic Approach ◽  
Anticancer Activities

Trojan horse based design affords antibody gold conjugates containing linkers that display HER2-mediated toxicity in breast cancer cell lines.

scholarly journals Design, Synthesis, In Vitro Anticancer Evaluation and Molecular Modelling Studies of 3,4,5-Trimethoxyphenyl-Based Derivatives as Dual EGFR/HDAC Hybrid Inhibitors

2021 ◽  
Vol 14 (11) ◽  
pp. 1177
Author(s):  
Tarek S. Ibrahim ◽  
Azizah M. Malebari ◽  
Mamdouh F. A. Mohamed
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Hydroxamic Acid ◽  
Phenyl Group ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Molecular Docking Study

Recently, combining histone deacetylase (HDAC) inhibitors with chemotherapeutic drugs or agents, in particular epidermal growth factor receptor (EGFR) inhibitors, is considered to be one of the most encouraging strategy to enhance the efficacy of the antineoplastic agents and decrease or avoid drug resistance. Therefore, in this work, based on introducing 3,4,5-trimethoxy phenyl group as a part of the CAP moiety, in addition to incorporating 4–6 aliphatic carbons linker and using COOH or hydroxamic acid as ZBG, 12 novel EGFR/HDAC hybrid inhibitors 2a–c, 3a–c, 4a–c and 5a–c were designed, constructed, and evaluated for their anticancer activities against 4 cancer cell lines (HepG2, MCF-7, HCT116 and A549). Among all, hybrids with hydroxamic acid 4a–c and 5a, exhibited the highest inhibition against all cancer cell lines with IC50 ranging from 0.536 to 4.892 μM compared to Vorinostat (SAHA) with IC50 ranging from 2.43 to 3.63 μM and Gefitinib with IC50 ranging from 1.439 to 3.366 μM. Mechanistically, the most potent hybrids 4a–c and 5a were further tested for their EGFR and HDACs inhibitory activities. The findings disclosed that hybrid 4b displayed IC50 = 0.063 µM on the target EGFR enzyme which is slightly less potent than the standard Staurosporine (IC50 = 0.044 µM). Furthermore, hybrid 4b showed less HDAC inhibitory activity IC50 against HDAC1 (0.148), 2 (0.168), 4 (5.852), 6 (0.06) and 8 (2.257) than SAHA. In addition, the investigation of apoptotic action of the most potent hybrid 4b showed a significant increase in Bax level up to 3.75-folds, with down-regulation in Bcl2 to 0.42-fold, compared to the control. Furthermore, hybrid 4b displayed an increase in the levels of Caspases 3 and 8 by 5.1 and 3.15 folds, respectively. Additionally, the cell cycle analysis of hybrid 4b revealed that it showed programmed cell death and cell cycle arrest at G1/S phase. Moreover, all these outcomes together with the molecular docking study recommended the rationalized target hybrids 4a–c and 5a, particularly 4b, may be considered to be promising lead candidates for discovery of novel anticancer agents via dual inhibition of both EGFR/HDAC enzymes.

scholarly journals Apricot kernel possesses in vitro cytotoxic effect against breast cancer cell lines

2021 ◽  
Vol 17 (AAEBSSD) ◽  
pp. 252-256
Author(s):  
Shilpa Raina ◽  
Vikas Sharma ◽  
Shashank K. Singh
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Research Work ◽  
Cancer Cell Lines ◽  
Prunus Armeniaca ◽  
Breast Cancer Cell Lines ◽  
Chloroform Fraction

In the search for potential anticancer agents from fruits, the present research work was carried out to examine the in vitro cytotoxic potential of kernel part of Prunus armeniaca (apricot) against eight distinct human cancer cell lines from six different tissues: lung (A-549), colon (HCT-116), breast (MCF-7, MDAMB-231), pancreatic (MIAPaCa-2, Panc-1), prostrate (PC- 3) and CNS (N2A). Methanolic extract and subsequent fractions (n-hexane, chloroform, ethyl acetate, acetone and methanol) were used as test material and anticancer activity was determined via SRB assay at 100g/mL. Results revealed that chloroform fraction of kernel suppressed the proliferation of human breast cancer cellline with growth inhibition of 89%. The fraction of kernel was then evaluated at lower concentrations of 50, 40, 30, 20 and 10g/mL. Further IC50 value was calculated and it was observed that the fraction showed IC5038.66. To conclude, kernel part of Prunus armeniaca possesses certain constituents with cytotoxic properties that can be used to develop anticancer agents especially for breast cancer therapy and to provide a great service to cancer patients.Further studies are required for the isolation of active ingredients from the kernel part.

scholarly journals Cytotoxic Phenanthrene, Dihydrophenanthrene, and Dihydrostilbene Derivatives and Other Aromatic Compounds from Combretum laxum

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3154
Author(s):  
Eder Bisoli ◽  
Talita Vilalva Freire ◽  
Nídia Cristiane Yoshida ◽  
Walmir Silva Garcez ◽  
Lyara Meira Marinho Queiróz ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Mammalian Cells ◽  
Human Cancer ◽  
Radical Scavenging ◽  
Cancer Cell Lines ◽  
In Vitro Cytotoxicity ◽  
Mass Spectrometry Data ◽  
Spectroscopic Techniques

The chemical investigation of the roots and stems of Combretum laxum yielded a new dihydrostilbene derivative, 4′-hydroxy-3,3′,4-trimethoxy-5-(3,4,5-trimethoxyphenoxy)-bibenzyl (1), two phenanthrenes (2–3), and three dihydrophenanthrenes (4–6), along with one lignan, three triterpenoids, one aurone, one flavone, one naphthoquinone, and two benzoic acid derivatives. Their structures were determined by 1D and 2D nuclear magnetic resonance (NMR) spectroscopic techniques and/or mass spectrometry data. The occurrence of dihydrostilbenoid, phenanthrene and dihydrophenanthrene derivatives is unprecedented in a Combretum species native to the American continent. 2,7-Dihydroxy-4,6-dimethoxyphenanthrene, 2,6-dihydroxy-4,7-dimethoxy-9,10-dihydrophenanthrene and 5-O-methyl apigenin are novel findings in the Combretaceae, as is the isolation of compounds belonging to the chemical classes of aurones and naphthoquinones, while (+)-syringaresinol is reported for the first time in the genus Combretum. Compounds 1–6 were also evaluated for their in vitro cytotoxicity against five human cancer cell lines, and radical-scavenging ability against 1,1-diphenyl-2-picryl-hydrazyl (DPPH). 6-Methoxycoelonin (4) was the most cytotoxic against melanoma cells (IC50 2.59 ± 0.11 µM), with a high selectivity index compared with its toxicity against nontumor mammalian cells (SI 25.1). Callosin (6), despite exhibiting the strongest DPPH-scavenging activity (IC50 17.7 ± 0.3 µM), proved marginally inhibitory to the five cancer cell lines tested, indicating that, at least for these cells, antioxidant potential is unrelated to antiproliferative activity.

scholarly journals Cytotoxic Effects of Chlorophyllides in Ethanol Crude Extracts from Plant Leaves

2019 ◽  
Vol 2019 ◽  
pp. 1-13 ◽  
Author(s):  
Yi-Ting Wang ◽  
Chih-Hui Yang ◽  
Ting-Yu Huang ◽  
Mi‐Hsueh Tai ◽  
Ru-Han Sie ◽  
...  
Keyword(s):  
Sweet Potato ◽  
Cell Lines ◽  
Cancer Cell ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cancer Cell Lines ◽  
Plant Leaves ◽  
Cytotoxic Effects ◽  
Crude Extracts ◽  
Antioxidant Effects

Chlorophyllide (chlide) is a natural catabolic product of chlorophyll (Chl), produced through the activity of chlorophyllase (chlase). The growth inhibitory and antioxidant effects of chlide from different plant leaf extracts have not been reported. The aim of this study is to demonstrate that chlide in crude extracts from leaves has the potential to exert cytotoxic effects on cancer cell lines. The potential inhibitory and antioxidant effects of chlide in crude extracts from 10 plant leaves on breast cancer cells (MCF7 and MDA-MB-231), hepatocellular carcinoma cells (Hep G2), colorectal adenocarcinoma cells (Caco2), and glioblastoma cells (U-118 MG) were studied using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) and DPPH (1,1-diphenyl-2-picrylhydrazyl) assays. The results of the MTT assay showed that chlide in crude extracts from sweet potato were the most effective against all cancer cell lines tested. U-118 MG cells were the most sensitive, while Caco2 cells were the most resistant to the tested crude extracts. The cytotoxic effects of chlide and Chl in crude extracts from sweet potato and of commercial chlorophyllin (Cu-chlin), in descending order, were as follows: chlide > Chl > Cu-chlin. Notably, the IC50 of sweet potato in U-118 MG cells was 45.65 μg/mL while those of Chl and Cu-chlin exceeded 200 μg/mL. In the DPPH assay, low concentrations (100 μg/mL) of chlide and Cu-chlin from crude extracts of sweet potato presented very similar radical scavenging activity to vitamin B2. The concentration of chlide was negatively correlated with DPPH activity. The current study was the first to demonstrate that chlide in crude extracts from leaves have potential cytotoxicity in cancer cell lines. Synergism between chlide and other compounds from leaf crude extracts may contribute to its cytotoxicity.

scholarly journals Polyphenol Profile and Pharmaceutical Potential of Quercus spp. Bark Extracts

Plants ◽  
2019 ◽  
Vol 8 (11) ◽  
pp. 486 ◽  
Author(s):  
Elansary ◽  
Szopa ◽  
Kubica ◽  
Ekiert ◽  
Mattar ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Ellagic Acid ◽  
Wide Spectrum ◽  
Radical Scavenging ◽  
Antibacterial Activities ◽  
Cancer Cell Lines ◽  
Antimicrobial Activities ◽  
Anticancer Activities ◽  
Polyphenol Profile

Targeted profiling of polyphenols in trees may reveal valuable sources of natural compounds with major applications in pharmacology and disease control. The current study targeted the profiling of polyphenols using HPLC-DAD in Quercus robur, Q. macrocarpa and Q. acutissima bark extracts. Free radical scavenging of each extract was investigated using antioxidant assays. Antimicrobial activities against a wide spectrum of bacteria and fungi were explored, as well as anticancer activities against different cancer cell lines. The HPLC-DAD analyses revealed the availability of several polyphenols in high amounts, including ellagic acid (in Q. robur) and caffeic acid (in Q. macrocarpa) in all three species. The bioactivity assay revealed high antioxidant activity in Q. robur compared to that of the other species, as well as phenolic standards. The three oak bark extracts showed clear antibacterial activities against most bacteria tested, with the highest antibacterial activities in the extracts of Q. robur. In addition, the three extracts showed higher antibacterial activities against Pseudomonas aeruginosa, Micrococcus flavus, and Escherichia coli compared to that of other bacteria. There were strong antifungal activities against some fungi, such as Aspergillus flavus, Penicillium funiculosum, and Penicillium ochrochloron. There were also noticeable anticancer activities against MCF-7, HeLa, Jurkat, and HT-29 cell lines, with the highest anticancer activity in the extracts of Q. robur. This is the first study that reveals not only novel sources of important polyphenols (e.g. ellagic acid) in Q. robur, Q. macrocarpa and Q. acutissima bark but also their anticancer activities against diverse cancer cell lines.

scholarly journals A REVIEW ON ANTICANCER POTENTIAL OF SOME PYRANOCARBAZOLE ALKALOIDS AND ITS DERIVATIVES

2021 ◽  
Vol 9 (06) ◽  
pp. 874-883
Author(s):  
Nitin Kumar ◽  
◽  
Krishna Kumar Singh ◽  
Pratibha Mehta Luthra ◽  
◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Review Literature ◽  
Anticancer Activities ◽  
Natural Sources ◽  
Plant Parts ◽  
Anticancer Drug Development

Pyranocarbazole alkaloids isolated from natural sources various plant parts of the flower-bearing geneses plants Murraya, Clausena, Glycosmis, species belongs to family Rutaceae. These pyranocarbazole alkaloids showed potential anticancer activities on various cancer cell lines. In this review, we discussed the anticancer potential of pyranocarbazole alkaloids like Mahanine, Koenimbine, Koenidine, Murrayozoline, Girinimbine, Mahanimbine mainly on the basis of reported review literature. In particular, we discuss in vitro anticancer activities of these pyranocarbazole alkaloids and its derivatives on various cancer cell lines, plausible target, also in vivo activity if reported in literature discussed. These pyranocarbazole structure-based alkaloids showed very interesting anticancer profile. This review can be fruitful for further investigation of these pyranocarbazole alkaloids as anticancer drug development against various types of cancer with minimum side effects.

Parallel Solid-Phase Synthesis using a New Diethylsilylacetylenic Linker and Leading to Mestranol Derivatives with Potent Antiproliferative Activities on Multiple Cancer Cell Lines

2019 ◽  
Vol 18 (10) ◽  
pp. 1469-1481 ◽  
Author(s):  
Raphaël Dutour ◽  
René Maltais ◽  
Martin Perreault ◽  
Jenny Roy ◽  
Donald Poirier
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Solid Phase ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Multiple Cancer ◽  
Anticancer Properties ◽  
Antiproliferative Agent

Background: RM-133 belongs to a new family of aminosteroid derivatives demonstrating interesting anticancer properties, as confirmed in vivo in four mouse cancer xenograft models. However, the metabolic stability of RM-133 needs to be improved. After investigation, the replacement of its androstane scaffold by a more stable estrane scaffold led to the development of the mestranol derivative RM-581. Methods: Using solid-phase strategy involving five steps, we quickly synthesized a series of RM-581 analogs using the recently-developed diethylsilylacetylenic linker. To establish structure-activity relationships, we then investigated their antiproliferative potency on a panel of cancer cell lines from various cancers (breast, prostate, ovarian and pancreatic). Results: Some of the mestranol derivatives have shown in vitro anticancer activities that are close to, or better than, those observed for RM-581. Compound 23, a mestranol derivative having a ((3,5-dimethylbenzoyl)- L-prolyl)piperazine side chain at position C2, was found to be active as an antiproliferative agent (IC50 = 0.38 ± 0.34 to 3.17 ± 0.10 µM) and to be twice as active as RM-581 on LNCaP, PC-3, MCF-7, PANC-1 and OVCAR-3 cancer cells (IC50 = 0.56 ± 0.30, 0.89 ± 0.63, 1.36 ± 0.31, 2.47 ± 0.91 and 3.17 ± 0.10 µM, respectively). Conclusion: Easily synthesized in good yields by both solid-phase organic synthesis and classic solution-phase chemistry, promising compound 23 could be used as an antiproliferative agent on a variety of cancers, notably pancreatic and ovarian cancers, both having very bad prognoses.

Anti-Cancer and Kinases Inhibitor Activities of Synthesized Heterocyclic Substituted Thiophene Fused with Cyclohexane Derivatives

2017 ◽  
Vol 14 (1) ◽  
pp. 768-774 ◽  
Author(s):  
Abd El-Galil E Amr ◽  
Hassan Z Ghanem ◽  
Mohamed A Al-Omar ◽  
Mohamed M Abdalla ◽  
Mohamed G Assy ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Mechanism Of Action ◽  
Sphingosine Kinase ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Kinase Inhibition ◽  
Wide Range ◽  
Anti Cancer

We herein report the anti-cancer and kinases inhibitor activities of some synthesized heterocyclic substituted thiophene fused with cyclohexane derivatives (Fig. 1) were synthesized before. Sixteen of these compounds were conveniently screened for their in vitro cytotoxicity against a wide range of cell lines, and showed potent activities against lung and leukemic cancer cell lines. The in vivo antilung and antileukemic cancers of the most active in vitro compounds was estimated and founded highly potent and compared to the standard drugs Bevacizumab and Etoposide. In search for the mechanism of action of anticancer activities it was found that these compounds exert its action via sphingosine kinase inhibition and inhibition of p53 ubiquitination.

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