Synthesis and in vitro cytotoxicity of cross-conjugated prostaglandin A and J series and their hydroxy derivatives

2015 ◽  
Vol 13 (25) ◽  
pp. 7000-7012 ◽  
Author(s):  
Remigiusz Żurawiński ◽  
Marian Mikołajczyk ◽  
Marcin Cieślak ◽  
Karolina Królewska ◽  
Julia Kaźmierczak-Barańska
Keyword(s):  
Anticancer Activity ◽  
In Vitro Cytotoxicity ◽  
Enantiomerically Pure ◽  
Cyclopentenone Prostaglandin

An efficient synthetic protocol for the synthesis of enantiomerically pure cyclopentenone prostaglandin derivatives is described and the anticancer activity of these derivatives was determined.

Synthesis, characterization and in vitro cytotoxicity of gold(iii) dialkyl/diaryldithiocarbamato complexes

RSC Advances ◽  
2015 ◽  
Vol 5 (99) ◽  
pp. 81599-81607 ◽  
Author(s):  
Muhammad Altaf ◽  
Anvarhusein A. Isab ◽  
Ján Vančo ◽  
Zdeněk Dvořák ◽  
Zdeněk Trávníček ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
In Vitro Cytotoxicity ◽  
Methyl Ethyl

A series of six dialkyl/diaryldithiocarbamato (dtc) gold(iii) complexes [Au(R2dtc)2]Cl (1,3, and5), and [Au(R2dtc)Cl2] (2,4, and6), (R = methyl, ethyl, and benzyl) was synthesised and evaluated for anticancer activity with promising results (EC50≈ 9.5 μM).

scholarly journals In-vitro Cytotoxicity and In-silico Insights of the Multi-target Anticancer Candidates from Haplophyllum tuberculatum

2021 ◽  
Vol 4 (3) ◽  
pp. 192-201
Author(s):  
Mosab Yahya Al-Nour ◽  
Ahmed H Arbab ◽  
Mohammad Khalid Parvez ◽  
Arwa Y Mohamed ◽  
Mohammed S Al-Dosari
Keyword(s):  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Lines ◽  
In Vitro Cytotoxicity ◽  
Binding Modes ◽  
Web Servers ◽  
Hela Cell Lines ◽  
Ic50 Values ◽  
Haplophyllum Tuberculatum

This study aimed to investigate the anticancer activity of Haplophyllum tuberculatum(Forsk.) aerial parts ethanol extract and fractions and reveal the potential anticancer targets, binding modes, pharmacokinetics, and toxicity properties of its phytoconstituents. MTT assay was used to investigate the anticancer activity. TargetNet, ChemProt version 2.0, and CLC-Pred web servers were used for virtual screening, and Cresset Flare software was used for molecular docking with the 26 predicted targets. Moreover, pkCSM, swiss ADME, and eMolTox web servers were used to predict pharmacokinetics and safety. Ethanolic extracts of H. tuberculatum on HepG2 and HeLa cell lines showed promising activities with IC50 values 54.12 and 48.1 µg/mL, respectively. Further, ethyl acetate fraction showed the highest cytotoxicity on HepG2 and HeLa cell lines with IC50 values 41.7 and 52.31 µg/mL. Of 70 compounds screened virtually, polygamain, justicidin A, justicidin B, haplotubine, kusunokinin, and flindersine were predicted as safe anticancer drugs candidates. They showed the highest binding scores with targets involved in cell growth, proliferation, survival, migration, tumor suppression, induction of apoptosis, metastasis, and drug resistance. Our findings revealed the potency of H. tuberculatum as a source of anticancer candidates that further studies should support.

The Smith Synthesis of ( + )-Lyconadin A

2011 ◽  
Author(s):  
Douglass Taber
Keyword(s):  
Total Synthesis ◽  
Aldol Condensation ◽  
Primary Alcohol ◽  
Selective Reduction ◽  
Axial Direction ◽  
In Vitro Cytotoxicity ◽  
University Of Pennsylvania ◽  
Enantiomerically Pure ◽  
The University

The pentacyclic alkaloid ( + )-lyconadin A 3, isolated from the club moss Lycopodium complanatum, showed modest in vitro cytotoxicity. A key step in the first reported (J. Am. Chem. Soc. 2007, 129, 4148) total synthesis of 3, by Amos B. Smith III of the University of Pennsylvania, was the cyclization of 1 to 2. The pentacyclic alkaloid (+)-lyconadin A 3, isolated from the club moss Lycopodium complanatum, showed modest in vitro cytotoxicity. A key step in the first reported (J. Am. Chem. Soc. 2007, 129, 4148) total synthesis of 3, by Amos B. Smith III of the University of Pennsylvania, was the cyclization of 1 to 2. The pentacyclic skeleton of 3 was constructed around a central organizing piperidine ring 9. This was prepared from the known (and commercial) enantiomerically-pure lactone 4. The akylated stereogenic center of 9 was assembled by diastereoselective hydroxy methylation of the acyl oxazolidinone 5 with s-trioxane, followed by protection. Reduction of the imide to the alcohol led to the mesylate 7, which on reduction of the azide spontaneously cyclized to give, after protection, the piperidine 8. Selective desilylation of the primary alcohol then enabled the preparation of 9. The plan was to assemble the first carbocyclic ring of 3 by intramolecular aldol condensation of the keto aldehyde 15. The enantiomerically-pure secondary methyl substituent of 15 derived from the commercial monoester 10. Activation as the acid fluoride followed by selective reduction led to the volatile lactone 11. Opening of the lactone with H3CONHCH3HCl gave, after protection, the Weinreb amide 12. Alkylation of the derived hydrazone 13, selectively on the methyl group, led, after deprotection, to 15. The intramolecular aldol condensation of 15 did deliver the unstable cyclohexenone 1. Under the acidic conditions of the aldol condensation, the enol derived from the piperidone added in a Michael sense, from the axial direction on the newly-formed ring, to give the trans-fused bicyclic diketone 2.

scholarly journals ANTI PROLIFERATIVE ACTIVITY OF CALAMUS ROTANG AS A SPOTLIGHT ON EHRLICH’S ASCITES CARCINOMA TREATED PERITONEAL AS WELL AS SOLID TUMOR MODEL

2018 ◽  
Vol 10 (1) ◽  
pp. 85
Author(s):  
Subeer Roy ◽  
Diksha Kumari ◽  
Mainak Chakraborty ◽  
Pallab Kanti Haldar
Keyword(s):  
Life Span ◽  
Cell Count ◽  
Anticancer Activity ◽  
Solid Tumor ◽  
Tumor Volume ◽  
Hematological Parameters ◽  
In Vitro Cytotoxicity ◽  
Control Group

Objective: Methanol extract of Calamus rotang (MECR) root was appraised as a spotlight for the candidate of anticancer activity through the vehicle (Ehrlich Ascites Carcinoma) on Swiss albino mice.Methods: In vitro cytotoxicity assay has been accessed by trypan blue and MTT assay. In vivo anticancer activity was done using EAC cells (2 × 106) where in each groups mice were 6. After treatment with MECR at the lower dose of 200 and higher dose of 400 mg/kg respectively for 9 d, half of the mice of each group were sacrificed and the rest were kept to check prolongation of life span. The anticancer potential of MECR was evaluated by tumor volume, viable and nonviable tumor cell count, tumor weight, hematological parameters, biochemical estimations and Furthermore, tissue antioxidant parameters. Besides, solid tumor activity was also inspected.Results: In MECR treated groups (200 and 400 mg/kg) tumor volume, packed cell volume and viable cell count was significantly lessened as compared to that of the EAC control group. Life span, most reliable criteria for anticancer study, increased quite surprisingly by 50% and 100% in a dose dependant manner while compared to EAC control group. The hematological, biochemical and liver tissue antioxidant parameter are significantly (p<0.05) restored along with solid tumor case study (solid tumor volume) towards the normal level after treatment with MECR.Conclusion: From the above study it can be inferred that the MECR has impressive anticancer activity in dose dependent way.

scholarly journals Synthesis and in vitro Cytotoxicity Study of Novel 4-Substituted Quinazolines Encompassed with Thiazolidinone and Azetidinone

2020 ◽  
Vol 32 (10) ◽  
pp. 2617-2623
Author(s):  
Akash Jori ◽  
Sheshagiri R. Dixit ◽  
Gurubasavraj V. Pujar
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Dna Binding ◽  
Anticancer Activity ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
In Vitro Cytotoxicity ◽  
Free Radical Scavenging ◽  
Binding Studies

A series of quinazolines encompassed with thiazolidinone and azetidinone have been synthesized and evaluated for their antioxidant, anticancer and DNA binding studies. All the synthesized compounds were characterized by IR, 1H & 13C NMR and mass spectra. Antioxidant activity was carried out using % free radical scavenging by DPPH assay. Compounds 4b, 5b and 5d have shown better antioxidant activity (60, 67 and 66%, respectively) among the tested compounds. Compounds having % free radical scavenging activity more than 55% were evaluated for anticancer activity by MTT assay towards cell lines A-549 (lung carcinoma) and MDA-231 (human breast cancer). Results revealed that the tested compounds exhibited moderate to low anticancer activity. Further, DNA binding activity was studied by absorption titration method for all the synthesized compounds, and compound 5b showed a good binding constant of 70.05 and % hyperchromicity of 82.93%.

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.

Inclusion complexes of anhydrolycorine with cyclodextrins: preparation, characterization, and anticancer activity

2016 ◽  
Vol 94 (6) ◽  
pp. 575-582 ◽  
Author(s):  
Yafei Guo ◽  
Jiuling Li ◽  
Yuqi Liu ◽  
Yongping Ma ◽  
Huilin Cheng ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Anticancer Activity ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Inclusion Complexation ◽  
Human Colon ◽  
In Vitro Cytotoxicity ◽  
Human Colon Cancer ◽  
Ht 29

This article describes the preparation of a series of inclusion complexes of anhydrolycorine with three cyclodextrins (CDs), namely β-CD, γ-CD, and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), and their successful characterization through UV, TG, DSC, XRD, SEM, 1H NMR, and 2D NMR spectroscopies. The results demonstrated that the water solubility of anhydrolycorine increased notably by about 23–42 times after the inclusion complexation with these CDs. Furthermore, preliminary in vitro cytotoxicity experiments on human colon cancer cell lines HT-29, SW480, HCT116, and DLD-1 were also performed, and the complexes showed remarkable anticancer activity against HT-29, SW480, and HCT116. These results suggested that the inclusion complexes would be potentially useful for applications for human colon cancer chemotherapy.

scholarly journals Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges

2019 ◽  
Vol Volume 14 ◽  
pp. 4589-4599 ◽  
Author(s):  
Atefe Rezaei ◽  
Jaleh Varshosaz ◽  
Mehrafarin Fesharaki ◽  
Armin Farhang ◽  
Seid Mahdi Jafari
Keyword(s):  
Ferulic Acid ◽  
Anticancer Activity ◽  
In Vitro Cytotoxicity ◽  
Cyclodextrin Nanosponges
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