scholarly journals New Cytotoxic Natural Products from the Red Sea Sponge Stylissa carteri

Marine Drugs ◽  
2020 ◽  
Vol 18 (5) ◽  
pp. 241 ◽  
Author(s):  
Reda F. A. Abdelhameed ◽  
Eman S. Habib ◽  
Nermeen A. Eltahawy ◽  
Hashim A. Hassanean ◽  
Amany K. Ibrahim ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Red Sea ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Spectroscopic Techniques ◽  
Standard Drug ◽  
Human Cancer Cell Lines ◽  
Stylissa Carteri ◽  
Mcf 7

Bioactivity-guided isolation supported by LC-HRESIMS metabolic profiling led to the isolation of two new compounds, a ceramide, stylissamide A (1), and a cerebroside, stylissoside A (2), from the methanol extract of the Red Sea sponge Stylissa carteri. Structure elucidation was achieved using spectroscopic techniques, including 1D and 2D NMR and HRMS. The bioactive extract’s metabolomic profiling showed the existence of various secondary metabolites, mainly oleanane-type saponins, phenolic diterpenes, and lupane triterpenes. The in vitro cytotoxic activity of the isolated compounds was tested against two human cancer cell lines, MCF-7 and HepG2. Both compounds, 1 and 2, displayed strong cytotoxicity against the MCF-7 cell line, with IC50 values at 21.1 ± 0.17 µM and 27.5 ± 0.18 µM, respectively. They likewise showed a promising activity against HepG2 with IC50 at 36.8 ± 0.16 µM for 1 and IC50 30.5 ± 0.23 µM for 2 compared to the standard drug cisplatin. Molecular docking experiments showed that 1 and 2 displayed high affinity to the SET protein and to inhibitor 2 of protein phosphatase 2A (I2PP2A), which could be a possible mechanism for their cytotoxic activity. This paper spreads light on the role of these metabolites in holding fouling organisms away from the outer surface of the sponge, and the potential use of these defensive molecules in the production of novel anticancer agents.

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

scholarly journals IN VITRO CYTOTOXIC ANTICANCER POTENTIAL OF BIOACTIVE FRACTION ISOLATED FROM INDONESIAN TIDAL SPONGE CALTHROPELLA SP.

2019 ◽  
Vol 12 (1) ◽  
pp. 380
Author(s):  
Fitria Susilowati ◽  
Respati Tri Swasono ◽  
Tatsufumi Okino ◽  
Winarto Haryadi
Keyword(s):  
High Resolution ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Bioactive Compounds ◽  
Human Cancer ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties ◽  
Bioactive Fraction ◽  
Mcf 7

Objective: This study was taken to examine the cytotoxicity of the bioactive fraction isolated from marine sponge Calthropella sp. as a preliminary anticancer assay and identify its bioactive compounds.Methods: The cytotoxic activity was assessed by 3-(4,5-dimethylthiazol-2-y1)-2,5-diphenyltetrazolium bromide assay against three human cancer cell lines, namely human breast (MCF-7), human lung (H-460), and human liver (HepG-2). The bioactive compounds were identified using a high-resolution liquid chromatography–mass spectroscopy (LC–MS).Results: The active fraction 7 showed moderate to strong cytotoxic activity on all cell lines tested and promising a strong potent cytotoxicity against MCF-7 cell lines with IC50 value as low as 1.925 μg/mL comparable to control, cisplatin (IC50 0.977 μg/mL). In regard to the promising bioactive compounds, the high-resolution LC–MS predicted the existing of several known compounds such as bengamide Q, clavepictine A, 4’-N-methyl-5’- hydroxystaurosporine, carteriofenone A, and one strong possibility of a new compound.Conclusion: This study has revealed that the isolated bioactive fraction of Indonesian tidal sponge, Calthropella sp., possesses potential anticancer properties with a promising significant cytotoxicity on MCF-7 cell lines (IC50 1.925 μg/mL).

scholarly journals SYNTHESIS OF SOME 2,3-DIHYDRO-1,3,4-OXADIAZOLES AND 4,5-DIHYDRO-1,2,4-TRIAZOLES AS ANTICANCER AGENTS

2020 ◽  
pp. 92-99
Author(s):  
TAWFEEK A. YAHYA ◽  
JALAL H. ABDULLAH
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
Colorimetric Assay ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Standard Drug ◽  
Mass Spectral ◽  
Oxadiazole Derivatives

Objective: The main objective of this work was to synthesize and evaluate the novel 2,3-dihydro-1,3,4-oxadiazole and 4,5-dihydro-1,2,4-triazole derivatives for cytotoxic activities. Methods: The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were synthesized by cyclization of N'-(substituted-benzylidene) isonicotinohydrazide 3a-e in refluxing acetic anhydride. The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were converted into the corresponding 4,5-dihydro-1,2,4-triazoles 5a-h using ammonia. All the synthesized compounds were identified, depending on the physical and spectral data. Title compounds were assessed for their cytotoxic activity against human cancer cell line (MCF-7) by using Sulforhodamine B (SRB) colorimetric assay. Results: All the synthesized compounds showed characteristic peaks in FTIR, 1HNMR and Mass spectral analysis. The results of the in vitro cytotoxic activity revealed that the compound 4c exhibited equipotent cytotoxic activity with an IC50 value of 8.04 µM when compared with that of standard drug doxorubicin (IC50= 8.02 µM). The reminder compounds have shown good to moderate cytotoxic activities when compared with that of a reference standard. Conclusion: We synthesized a series of title compounds in quantitative yields. Most derivatives showed moderate to good cytotoxic activity.  

scholarly journals Polyhydroxy Sterols Isolated from the Red Sea Soft Coral Lobophytum crassum and their Cytotoxic Activity

2017 ◽  
Vol 12 (2) ◽  
pp. 1934578X1701200
Author(s):  
Elsayed A. Aboutabl ◽  
Nabil M. Selim ◽  
Shadia M Azzam ◽  
Camilia G. Michel ◽  
Mohamed F. Hegazy ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Red Sea ◽  
Soft Coral ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Nmr Analysis ◽  
Human Cancer Cell Lines ◽  
Hct 116

One new (1) together with four known sterols (2 - 5) and a sesquiterpene (6) were isolated from a polar extract of the Red Sea soft coral Lobophytum crassum. The compounds were identified as 24-methylenecholest-5-ene-1α,3 1α,11α-triol 1-acetate (1), 24-methylenecholest-5-ene-1α,3β,11α-triol (2), 24-methylenecholest-5-ene-3β-ol (3), 24-methylenecholestane-1α,3β,5a,6P,1-pentol (4), 24-methylenecholestane-3β,5α,6β-triol (5) and alismoxide (6) based on extensive NMR analysis. The cytotoxicity of compounds 1 - 6 was evaluated in vitro using three human cancer cell lines viz., HepG2, Hep-2 and HCT-116. Compound 1 showed selective cytotoxic activity against HepG2, while 3 exhibited cytotoxicity against all tested cell lines.

scholarly journals Synthesis and In Vitro Cytotoxic Activity of Chromenopyridones

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Balwinder Singh ◽  
Vishal Sharma ◽  
Gagandeep Singh ◽  
Rakesh Kumar ◽  
Saroj Arora ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Hep G2 ◽  
Cytotoxic Potential ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Novel substituted chromenopyridones (3a–j and 6a–d) were synthesized and evaluated in vitro for the cytotoxic activity against various human cancer cell lines such as prostate (PC-3), breast (MCF-7), CNS (IMR-32), cervix (Hela), and liver (Hep-G2). preliminary cytotoxic screening showed that all the compounds possess a good to moderate inhibitory activity against various cancer cell lines. Particularly, compound 6b bearing allyl moiety displayed a significant cytotoxic potential in comparison to standard drugs.

scholarly journals Synthesis and screening of anticancer potentials of some new terephthaldehyde-derived nitrone compounds

2020 ◽  
Vol 19 (2) ◽  
pp. 341-349
Author(s):  
Husam Hamza Salman ◽  
Munther Abduljaleel Mohammed Ali ◽  
Eman Tariq Ali
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Condensation Reaction ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Anticancer Properties ◽  
Chemical Structures ◽  
Ic50 Values ◽  
Mcf 7

Purpose: To synthesize and screen some new nitrone compounds derived from terephthaldehyde for their anticancer potential. Methods: Six new compounds (H, p-Me,p-Br, p-Cl, o-Cl and m-Me) were synthesized via a condensation reaction between terephthaldehyde and a variety of aryl hydroxylamine compounds derived from nitrobenzene and its derivatives. The chemical structures of these compounds were identified using elemental CHN analysis and were elucidated using Fourier Transform infra-red (FT-IR), 1H-nuclear magnetic resonance (1H NMR), mass spectrometry (MS), and elemental analysis. The anticancer effects of the compounds were screened in vitro with respect to their cytotoxicity on MCF7 human cancer cells line. The IC50 values were obtained by MTT assay and their effects on apoptosis of MCF-7 cells were assessed using Acridine orange-ethidium bromide AO/EtBr staining method under a fluorescence microscope. Results: Only four compounds (2b, 2d, 2e, and 2f) inhibited more than 50 % of the growth of MCF-7 cells. The strongest anti-proliferation effect against MCF-7 cells was exhibited by 2f (m-Me), producing more apoptosis which increased membrane disruption and consistency of lysosome vacuoles; it also exhibited higher cytotoxic effects on human cancer cell lines (IC50 < 7.5) than the other synthesized compounds. Conclusion: The new nitrone compounds (2b, 2d, 2e, and 2f) synthesized from terephthaldehyde exhibit some anticancer properties, and so are potential anticancer agents. Keywords: Terephthaldehyde, Nitrone, Cytotoxicity, Anticancer, MCF-7 cells

scholarly journals IN VITRO CYTOTOXIC ANTICANCER POTENTIAL OF BIOACTIVE FRACTION ISOLATED FROM INDONESIAN TIDAL SPONGE CALTHROPELLA SP.

2019 ◽  
Vol 12 (1) ◽  
pp. 380
Author(s):  
Fitria Susilowati ◽  
Respati Tri Swasono ◽  
Tatsufumi Okino ◽  
Winarto Haryadi
Keyword(s):  
High Resolution ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Bioactive Compounds ◽  
Human Cancer ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties ◽  
Bioactive Fraction ◽  
Mcf 7

Objective: This study was taken to examine the cytotoxicity of the bioactive fraction isolated from marine sponge Calthropella sp. as a preliminary anticancer assay and identify its bioactive compounds.Methods: The cytotoxic activity was assessed by 3-(4,5-dimethylthiazol-2-y1)-2,5-diphenyltetrazolium bromide assay against three human cancer cell lines, namely human breast (MCF-7), human lung (H-460), and human liver (HepG-2). The bioactive compounds were identified using a high-resolution liquid chromatography–mass spectroscopy (LC–MS).Results: The active fraction 7 showed moderate to strong cytotoxic activity on all cell lines tested and promising a strong potent cytotoxicity against MCF-7 cell lines with IC50 value as low as 1.925 μg/mL comparable to control, cisplatin (IC50 0.977 μg/mL). In regard to the promising bioactive compounds, the high-resolution LC–MS predicted the existing of several known compounds such as bengamide Q, clavepictine A, 4’-N-methyl-5’- hydroxystaurosporine, carteriofenone A, and one strong possibility of a new compound.Conclusion: This study has revealed that the isolated bioactive fraction of Indonesian tidal sponge, Calthropella sp., possesses potential anticancer properties with a promising significant cytotoxicity on MCF-7 cell lines (IC50 1.925 μg/mL).

scholarly journals Design, Synthesis, and Cytotoxic Evaluation of Etodolac-1,3,4-oxadiazole-1,2,3-triazole Molecules

SynOpen ◽  
2018 ◽  
Vol 02 (01) ◽  
pp. 0017-0024 ◽  
Author(s):  
Bhaskar Kummari ◽  
Perla Ramesh ◽  
Naveen Polkam ◽  
Shankaraiah Malthum ◽  
M. Vishnuvardhan ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Synthetic Sequence ◽  
A549 Lung ◽  
Mcf 7

A new series of etodolac-1,3,4-oxadiazole-1,2,3-triazole derivatives was designed and synthesized from commercially available starting materials by employing a simple synthetic sequence. The in vitro evaluation of the synthesized analogues displayed promising cytotoxic activity. Among the tested compounds 7c, 7l, and 7n exhibited highest cytotoxic activity against MCF-7 (breast), A549 (lung), and DU-145 (prostate) human cancer cell lines.

Anticancer Evaluation of Tris(triazolyl)triazine Derivatives Generated via Click Chemistry

2016 ◽  
Vol 69 (8) ◽  
pp. 905 ◽  
Author(s):  
Tamer El Malah ◽  
Hany F. Nour ◽  
A. A. Nayl ◽  
R. A. Elkhashab ◽  
Farouk M. E. Abdel-Megeid ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Standard Drug ◽  
Human Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Mcf 7

Click chemistry has been utilised for the preparation of new tris(triazolyl)triazines containing aliphatic and polar side chains through coupling of 2,4,6-triethynyl-[1,3,5]triazines, which possess free terminal alkyne moieties with substituted aromatic azides. The cytotoxic activity and in vitro anticancer potential of the newly synthesised compounds have been evaluated against seven human cancer cell lines including liver HepG2, breast MCF-7, lung A549, acute myeloid leukemia HL-60, colon HCT116, and prostate PC3 cancer cell lines in addition to human normal melanocyte, HFB4. The results revealed that all the compounds did not exhibit any activity against A549, HL-60, and PC3. However compound G2 was effective against MCF-7 and HepG2 cancer cell lines. On the other hand, compound G1a exhibited higher potency against MCF-7 and HepG2 cells with no toxicity on normal cells in comparison with the standard drug doxorubicin.

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

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