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Special Issue "Curcumin an Example of Pleiotropic Agents—Design, Synthesis and Biological Evaluation of Curcumin Analogues or Curcumin Derivatives"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (10 June 2017)

Special Issue Editor

Guest Editor
Prof. Dr. Dimitra Hadjipavlou-Litina

Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Greece
Website | E-Mail
Phone: +302310997627
Interests: design; synthesis; bilogical evaluation; inflammation; cancer; cardiovascular diseases; COX and LOX inhibitors; QSAR

Special Issue Information

Dear Colleagues,

Curcumin is a natural phytochemical obtained from the dried root and rhizome of Turmeric (Curcuma Longa). It is a pleiotropic agent, showing interference with multiple cell signaling pathways, including apoptosis, proliferation (HER-2, EGFR, and AP-1), angiogenesis (VEGF), and inflammation (NF-κB, TNF, IL-6, IL-1, COX-2, and 5-LOX). In the last decade, various synthetic analogues have been prepared and evaluated for pleiotropic therapeutic  applications.

Our target within this Special Issue will be to highlight contemporary research considering the design (in silico) synthesis and biological activities (evaluation and critical discussion), as well as reviews referring to the pleiotropic activities of curcuminoids, curcumin derivatives and curcumin analogues.

Additionally, we would like to have as many cases of multitaget applications of the above chemical structures in order to point out the importance of this chemical structure

Prof. Dr. D. Hadjipavlou-Litina
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • curcumin
  • pleiotropic agent
  • anti-cancer
  • anti-inflammatory
  • antioxidant
  • structure activity relationships
  • curcumin analogues
  • curcumin derivatives
  • Michael acceptors

Published Papers (4 papers)

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Research

Open AccessArticle Synthesis and Evaluation of Curcuminoid Analogues as Antioxidant and Antibacterial Agents
Molecules 2017, 22(6), 971; doi:10.3390/molecules22060971
Received: 11 May 2017 / Revised: 3 June 2017 / Accepted: 7 June 2017 / Published: 11 June 2017
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Abstract
Diazocoupling reaction of curcumin with different diazonium salts of p-toluidine, 2-aminopyridine, and 4-aminoantipyrine in pyridine yielded the arylhydrazones 2ac. Arylhydrazone of p-toluidine reacted with urea, thiourea, and guanidine nitrate to produce 5,6-dihydropyrimidines. Further reaction of 2a with 2,3-diaminopyrdine
[...] Read more.
Diazocoupling reaction of curcumin with different diazonium salts of p-toluidine, 2-aminopyridine, and 4-aminoantipyrine in pyridine yielded the arylhydrazones 2ac. Arylhydrazone of p-toluidine reacted with urea, thiourea, and guanidine nitrate to produce 5,6-dihydropyrimidines. Further reaction of 2a with 2,3-diaminopyrdine in sodium ethoxide solution yielded 1H-pyrido[2,3-b][1,4]diazepine derivative. Bis(2,5-dihydroisoxazole) is obtained from the reaction of 2a with hydroxylamine hydrochloride, while its reactions with hydrazines afforded the respective 4,5-dihydro-1H-pyrazoles. The target compounds were evaluated as antioxidant and antibacterial agents. The tested compounds showed good to moderate activities compared to ascorbic acid and chloramphenicol, respectively. Full article
Figures

Open AccessArticle Curcumin Inhibits LIN-28A through the Activation of miRNA-98 in the Lung Cancer Cell Line A549
Molecules 2017, 22(6), 929; doi:10.3390/molecules22060929
Received: 29 March 2017 / Revised: 4 May 2017 / Accepted: 25 May 2017 / Published: 3 June 2017
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Abstract
Metastasis is common in lung cancer and is associated with poor clinical outcomes and increased mortality. Curcumin is a natural anti-cancer agent that inhibits the metastasis of various cancers by modulating the expression of micro (mi) RNAs such as miR-98, which acts as
[...] Read more.
Metastasis is common in lung cancer and is associated with poor clinical outcomes and increased mortality. Curcumin is a natural anti-cancer agent that inhibits the metastasis of various cancers by modulating the expression of micro (mi) RNAs such as miR-98, which acts as a tumor suppressor. This study investigated the effect of curcumin on miR-98 expression and in vitro cell line growth and invasiveness in lung cancer. Curcumin treatment enhanced the expression of miR-98 and reduced that of the miR-98 target gene LIN28A as well as matrix metalloproteinase (MMP) 2 and MMP9 in vitro and in vivo. MiR-98 overexpression suppressed lung cancer cell migration and invasion by inhibiting LIN28A-induced MMP2 and MMP9 expression. Meanwhile, LIN28A level was downregulated by overexpression of miR-98 mimic. Induction of miR-98 by curcumin treatment suppressed MMP2 and MMP9 by targeting LIN28A. These findings provide insight into the mechanisms by which curcumin suppresses lung cancer cell line growth in vitro and in vivo and invasiveness in vitro. Full article
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Figure 1

Open AccessArticle Synthesis of Curcuminoids and Evaluation of Their Cytotoxic and Antioxidant Properties
Molecules 2017, 22(4), 633; doi:10.3390/molecules22040633
Received: 23 February 2017 / Revised: 4 April 2017 / Accepted: 11 April 2017 / Published: 14 April 2017
PDF Full-text (651 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Curcumin (1) and ten derivatives (211) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15,
[...] Read more.
Curcumin (1) and ten derivatives (211) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC50) values for the more active compounds against HCT-15 and K562 cell lines. Compounds 2 and 10 were the most active against both cell lines and were more active than curcumin itself. Thiobarbituric acid reactive substances (TBARS) assay showed that 7 has potent activity; even stronger than curcumin, α-tocopherol, and quercetin. Full article
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Open AccessCommunication Novel Palladium(II) Complexes that Influence Prominin-1/CD133 Expression and Stem Cell Factor Release in Tumor Cells
Molecules 2017, 22(4), 561; doi:10.3390/molecules22040561
Received: 20 February 2017 / Revised: 19 March 2017 / Accepted: 23 March 2017 / Published: 30 March 2017
PDF Full-text (4740 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
New Pd(II) complexes of 1,7-bis(2-methoxyphenyl)hepta-1,6-diene-3,5-dione were synthesized and structurally characterized. The complexes were tested in vitro on human colon and hepatic carcinoma cell lines, normal hepatic cells and hematopoietic progenitor cells. Biological tests proved that Pd(II) complexes 1 and 2 (containing a curcumin
[...] Read more.
New Pd(II) complexes of 1,7-bis(2-methoxyphenyl)hepta-1,6-diene-3,5-dione were synthesized and structurally characterized. The complexes were tested in vitro on human colon and hepatic carcinoma cell lines, normal hepatic cells and hematopoietic progenitor cells. Biological tests proved that Pd(II) complexes 1 and 2 (containing a curcumin derivative) exhibit a strong in vitro antitumor effect against the cells derived from human colorectal carcinoma and the hepatic metastasis of a colorectal carcinoma. Complex 1 has an outstanding inhibitory effect against BRAF-mutant colon carcinoma and hepatocarcinoma cell growth; 1 and 2 are both more active than the free ligand and have the capacity to trigger early apoptotic processes. By flow cytometric measurements, an important decrease of prominin-1 (CD133) molecule expression on tumor cells membrane was identified in cell populations subjected to 1 and 2. Quantitative immune enzymatic assay proved restrictions in stem cell factor (SCF) release by treated tumor cells. Although less cytotoxic, the free ligand inhibits the surface marker CD133 expression in hepatocarcinoma cells, and in HT-29 colon carcinoma. The new synthesized Pd(II) complexes 1 and 2 exhibit an important potential through their selective cytotoxic activity and by targeting the stem-like tumor cell populations, which leads to the tumor growth arrest and prevention of metastasis. Full article
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