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

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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) | Viewed by 22211

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Prof. Dr. Dimitra Hadjipavlou-Litina

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Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Interests: synthesis and biological studies on anti-inflammatory and antioxidant agents, on inhibitors of enzymes implicated in the inflammation and in the coagulation process in general; correlation of inflammation with cancer; neurodegeneration; antioxidant activity; theoretical and experimental calculation of physicochemical parameters implicated in biological response; use of computational chemistry in drug design as well as bioactive compounds of natural origin, e.g., essential oils
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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

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Keywords

curcumin
pleiotropic agent
anti-cancer
anti-inflammatory
antioxidant
structure activity relationships
curcumin analogues
curcumin derivatives
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Published Papers (4 papers)

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1146 KiB

Open AccessArticle

Synthesis and Evaluation of Curcuminoid Analogues as Antioxidant and Antibacterial Agents

by Dalia R. Emam, Ahmad M. Alhajoj, Khaled M. Elattar, Nabila A. Kheder and Ahmed A. Fadda

Molecules 2017, 22(6), 971; https://doi.org/10.3390/molecules22060971 - 11 Jun 2017

Cited by 10 | Viewed by 4209

Abstract

Diazocoupling reaction of curcumin with different diazonium salts of p-toluidine, 2-aminopyridine, and 4-aminoantipyrine in pyridine yielded the arylhydrazones 2a–c. 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

(This article belongs to the Special Issue Curcumin an Example of Pleiotropic Agents—Design, Synthesis and Biological Evaluation of Curcumin Analogues or Curcumin Derivatives)

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2378 KiB

Open AccessArticle

Curcumin Inhibits LIN-28A through the Activation of miRNA-98 in the Lung Cancer Cell Line A549

by Wei-Lun Liu, Jia-Ming Chang, Inn-Wen Chong, Yi-Li Hung, Yung-Hsiang Chen, Wen-Tsung Huang, Hsuan-Fu Kuo, Chong-Chao Hsieh and Po-Len Liu

Molecules 2017, 22(6), 929; https://doi.org/10.3390/molecules22060929 - 03 Jun 2017

Cited by 53 | Viewed by 6537

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 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

(This article belongs to the Special Issue Curcumin an Example of Pleiotropic Agents—Design, Synthesis and Biological Evaluation of Curcumin Analogues or Curcumin Derivatives)

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651 KiB

Open AccessArticle

Synthesis of Curcuminoids and Evaluation of Their Cytotoxic and Antioxidant Properties

by María Concepción Lozada-García, Raúl G. Enríquez, Teresa O. Ramírez-Apán, Antonio Nieto-Camacho, Juan Francisco Palacios-Espinosa, Zeltzin Custodio-Galván, Olivia Soria-Arteche and Jaime Pérez-Villanueva

Molecules 2017, 22(4), 633; https://doi.org/10.3390/molecules22040633 - 14 Apr 2017

Cited by 31 | Viewed by 6904

Abstract

Curcumin (1) and ten derivatives (2–11) 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

(This article belongs to the Special Issue Curcumin an Example of Pleiotropic Agents—Design, Synthesis and Biological Evaluation of Curcumin Analogues or Curcumin Derivatives)

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4740 KiB

Open AccessCommunication

Novel Palladium(II) Complexes that Influence Prominin-1/CD133 Expression and Stem Cell Factor Release in Tumor Cells

by Eva Fischer-Fodor, Roman Mikláš, Lucia Rišiaňová, Mihai Cenariu, Ioana Georgeta Grosu, Piroska Virag, Maria Perde-Schrepler, Ciprian Tomuleasa, Ioana Berindan-Neagoe, Ferdinand Devínsky and Natalia Miklášová

Molecules 2017, 22(4), 561; https://doi.org/10.3390/molecules22040561 - 30 Mar 2017

Cited by 11 | Viewed by 3979

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 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

(This article belongs to the Special Issue Curcumin an Example of Pleiotropic Agents—Design, Synthesis and Biological Evaluation of Curcumin Analogues or Curcumin Derivatives)

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

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