Current developments of coumarin-based anti-cancer agents in medicinal chemistry

Emami, Saeed; Dadashpour, Sakineh

doi:10.1016/j.ejmech.2015.08.033

Cited by 391 publications

(184 citation statements)

References 168 publications

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“…Recently, because it possesses minimum side effects along with multidrug reversal activity and specially an anti-inflammatory activity, studies about coumarin derivatives as potential anticancer agents have been developed [34–36]. Additionally, ellagic acid appears to exhibit an antineoplastic action on antimetastatic breast cancer [37] and antimetastatic potential of ovarian neoplasia [38].…”

Section: Resultsmentioning

confidence: 99%

Organic Extract of Justicia pectoralis Jacq. Leaf Inhibits Interferon-γ Secretion and Has Bacteriostatic Activity against Acinetobacter baumannii and Klebsiella pneumoniae

Nunes

Cordeiro

Beserra

et al. 2018

Evidence-Based Complementary and Alternative Medicine

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Justicia pectoralis Jacq. (Acanthaceae) leaves currently found in the Brazilian north-east are widely used to treat diabetes, menstrual pains, asthma, and other disorders. This work aimed to identify the phytochemical characterization and biological activities of J. pectoralis leaf extracts. The plant material was ground and the crude extracts were obtained with water or acetone: water (7:3 v/v), yielding aqueous (JPA), and organic (JPO) extracts. Phytochemical characterization was performed by thin-layer chromatography (TLC) and high-performance liquid chromatography (HPLC). Cytotoxicity was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay and trypan blue (TB) exclusion assay in peripheral blood mononuclear cells (PBMCs), BALB/c splenocytes, and neoplastic cells (TOLEDO, K562, DU-145, and PANC-1) at 1, 10, and 100 μg/mL. Antibacterial activity was evaluated using the microdilution test to obtain the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). Cytokines, IFN-γ, and IL-17A from culture supernatants of BALB/c mice splenocytes were measured by sandwich ELISA. In the TLC analysis, both JPA and JPO extracts presented coumarin and flavonoids. In addition, HPLC was able to identify coumarin, apigenin, and ellagic acid in both extracts. JPO IC50 was 57.59 ± 1.03 μg/mL (MTT) and 69.44 ± 8.08 μg/mL (TB) in TOLEDO. MIC value of JPO against Acinetobacter baumannii and Klebsiella pneumoniae was 500 μg/mL. JPO (100 μg/mL) significantly inhibited IFN-γ levels (p=0.03). J. pectoralis is a potential candidate to be further investigated as an IFN-γ inhibitory agent and against Acinetobacter baumannii and Klebsiella pneumoniae.

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Section: Resultsmentioning

confidence: 99%

Organic Extract of Justicia pectoralis Jacq. Leaf Inhibits Interferon-γ Secretion and Has Bacteriostatic Activity against Acinetobacter baumannii and Klebsiella pneumoniae

Nunes

Cordeiro

Beserra

et al. 2018

Evidence-Based Complementary and Alternative Medicine

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“…Many compounds showed cytotoxic activity against several human cancer cell lines (gastric carcinoma, colon carcinoma, hepatoma-derived cell line, and lymphoblastic cell line) in vitro and in xenograft models (Emami and Dadashpour 2015) and the treatment of prostate cancer, renal cell carcinoma, leukemia (Rohini and Srikumar 2014), and pancreatic cancer (Jun et al 2014).…”

Section: Coumarins: Classifications and Propertiesmentioning

confidence: 99%

Fungi as a source of natural coumarins production

Costa

Tavares

Oliveira

2016

Appl Microbiol Biotechnol

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Natural coumarins and derivatives are compounds that occur naturally in several organisms (plant, bacteria, and fungi) consisting of fused benzene and α-pyrone rings. These compounds show high technological potential applications in agrochemical, food, pharmaceuticals, and cosmetics industries. Therefore, the need for bulk production of coumarins and the advancement of the chemical and pharmaceutical industries led to the development of synthetic coumarin. However, biotransformation process, synthetic bioengineering, metabolic engineering, and bioinformatics have proven effective in the production of natural products. Today, these biological systems are recognized as green chemistry innovation and business strategy. This review article aims to report the potential of fungi for synthesis of coumarin. These microorganisms are described as a source of natural products capable of synthesizing many bioactive metabolites. The features, classification, properties, and industrial applications of natural coumarins as well as new molecules obtained by basidiomycetes and ascomycetes fungi are reported in order to explore a topic not yet discussed in the scientific literature.

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“…As the structural core, coumarin occurs widely in natural products, drugs and agrochemicals (Figure 1), these important applications have generated considerable interest in this ring system and various fused coumarin derivatives have been reported [3][4][5][6]: Osthole, a natural O-methylated coumarin found in Cnidium Monnieri, a traditional Chinese herbal medicine that has been used as as a fungicidein China for a long history,and shows antifungal activity against Rhizoctonia solani and a broad spectrum of other phytopathogenic fungi [7][8][9]; Warfarin and Acenocoumarol are anticoagulants normally used in the prevention of thrombosis and thromboembolism, function as the vitamin K antagonists [10][11][12]; and Coumoxystrobin (SYP-3375) is a coumarin-containing strobilurin fungicide that contains an (E)-methyl 3-methoxy-2-phenylacrylate substructure and displays a broad spectrum of antifungal activity [13][14][15]. In our previous work, Osthole was used as the lead structure to carry out structural optimization, and some synthesized furan [3,2-c]coumarin derivatives showed potent antifungal activity [16][17][18].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Antifungal Activity of Coumarin Ring-Opening Derivatives

2016

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Based on our initial design, we synthesized two series of coumarin ring-opening derivatives by the reactions of hydrolysis and methylation. Results of antifungal screening in vitro showed that the target compounds exhibited potent activity against the six common pathogenic fungi. Compounds 6b, 6e, 6g, 6i, 7b and 7c were identified as the most active ones, and the EC 50 values of these active compounds were further tested. Compared to the commonly used fungicide Azoxystrobin (0.0884 µM), compounds 6b (0.0544 µM) and 6e (0.0823 µM) displayed improved activity against Botrytis cinerea.

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Current developments of coumarin-based anti-cancer agents in medicinal chemistry

Cited by 391 publications

References 168 publications

Organic Extract of Justicia pectoralis Jacq. Leaf Inhibits Interferon-γ Secretion and Has Bacteriostatic Activity against Acinetobacter baumannii and Klebsiella pneumoniae

Organic Extract of Justicia pectoralis Jacq. Leaf Inhibits Interferon-γ Secretion and Has Bacteriostatic Activity against Acinetobacter baumannii and Klebsiella pneumoniae

Fungi as a source of natural coumarins production

Design, Synthesis and Antifungal Activity of Coumarin Ring-Opening Derivatives

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