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Special Issue "Antitumoral Properties of Natural Products"

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

Deadline for manuscript submissions: 31 October 2019

Special Issue Editor

Guest Editor
Prof. Dr. Roberto Fabiani

Department of Chemistry, Biology and Biotechnology - University of Perugia, Via del Giochetto, 06126 Perugia, Italy
Website | E-Mail
Interests: cancer chemoprevention; nutrition; olive oil; polyphenols; natural bioactive compounds; antioxidants; oxidative stress; genotoxicity; mutagenicity; apoptosis; cell cycle regulation;

Special Issue Information

Cancer is a major public health concern, being one of the main causes of morbidity and mortality worldwide. Carcinogenesis is a complex multistage process in which normal cells trough an alteration of DNA structure/function are transformed into malignant cells acquiring several properties, such as abnormal proliferation and reduced apoptosis. Studies have demonstrated both in vitro and in vivo that many bioactive compounds, from different natural sources, are able to influence a number of pathways related to tumor development. Many different cancer-specific molecular mechanisms and targets have been identified making it possible to use such compounds as alternative therapeutic or adjuvant treatments, or as chemopreventive agents. This Special Issue aims to identify the most recently-discovered new natural bioactive products with anticancer properties and will review their molecular mechanisms of action.

Prof. Dr. Roberto Fabiani
Guest Editor

Manuscript Submission Information

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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

  • Cancer
  • Chemoprevention
  • Bioactive compounds
  • Natural products
  • DNA damage
  • Apoptosis
  • Proliferation

Published Papers (13 papers)

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Research

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Open AccessArticle Evaluating Antitumor and Antioxidant Activities of Yellow Monascus Pigments from Monascus ruber Fermentation
Molecules 2018, 23(12), 3242; https://doi.org/10.3390/molecules23123242
Received: 23 November 2018 / Revised: 4 December 2018 / Accepted: 4 December 2018 / Published: 7 December 2018
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Abstract
Yellow Monascus pigments can be of two kinds: Natural and reduced, in which natural yellow Monascus pigments (NYMPs) attract widespread attention for their bioactivities. In this study, the antioxidative and antibreast cancer effects of the water-soluble NYMPs fermented by Monascus ruber CGMCC 10910
[...] Read more.
Yellow Monascus pigments can be of two kinds: Natural and reduced, in which natural yellow Monascus pigments (NYMPs) attract widespread attention for their bioactivities. In this study, the antioxidative and antibreast cancer effects of the water-soluble NYMPs fermented by Monascus ruber CGMCC 10910 were evaluated. Results showed that water-soluble NYMPs had a significantly improved antioxidative activities compared to the reduced yellow Monascus pigments (RYMPs) that were chemically derived from orange or red Monascus pigments. Furthermore, NYMPs exhibited a concentration-dependent inhibition activity on MCF-7 cell growth (p < 0.001). After a 48-h incubation, a 26.52% inhibition yield was determined with 32 μg/mL of NYMPs. NYMPs also significantly inhibited the migration and invasion of MCF-7 cells. Mechanisms of the activities were associated with a down-regulation of the expression of matrix metalloproteinases and vascular endothelial growth factor. Rather than being alternatively used as natural colorants or antioxidants, this work suggested that NYMPs could be selected as potential functional additives in further test of breast cancer prevention and adjuvant therapy. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle FAK and S6K1 Inhibitor, Neferine, Dually Induces Autophagy and Apoptosis in Human Neuroblastoma Cells
Molecules 2018, 23(12), 3110; https://doi.org/10.3390/molecules23123110
Received: 4 November 2018 / Revised: 24 November 2018 / Accepted: 25 November 2018 / Published: 28 November 2018
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Abstract
Human neuroblastoma cancer is the most typical extracranial solid tumor. Yet, new remedial treatment therapies are demanded to overcome its sluggish survival rate. Neferine, isolated from the lotus embryos, inhibits the proliferation of various cancer cells. This study aimed to evaluate the anti-cancer
[...] Read more.
Human neuroblastoma cancer is the most typical extracranial solid tumor. Yet, new remedial treatment therapies are demanded to overcome its sluggish survival rate. Neferine, isolated from the lotus embryos, inhibits the proliferation of various cancer cells. This study aimed to evaluate the anti-cancer activity of neferine in IMR32 human neuroblastoma cells and to expose the concealable molecular mechanisms. IMR32 cells were treated with different concentrations of neferine, followed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to assess cell viability. In an effort to determine the molecular mechanisms in neferine-incubated IMR32 cells, cell cycle arrest, cell migration, and focal adhesion kinase (FAK), the 70-kDa ribosomal S6 kinase 1 (S6K1), poly (ADP-ribose) polymerase (PARP), caspase-3, Beclin-1, and microtubule-associated protein 1A/1B-light chain 3 (LC3) protein expressions were investigated. Neferine strongly disrupted the neuroblastoma cell growth via induction of G2/M phase arrest. Furthermore, neferine provoked autophagy and apoptosis in IMR32 cells, confirmed by p-FAK, and p-S6K1 reduction, LC3-II accumulation, Beclin-1 overexpression, and cleaved caspase-3/PARP improvement. Finally, neferine markedly retarded cell migration of neuroblastoma cancer cells. As a result, our findings for the first time showed an explicit anti-cancer effect of neferine in IMR32 cells, suggesting that neferine might be a potential candidate against human neuroblastoma cells to improve clinical outcomes with further in vivo investigation. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Tumidulin, a Lichen Secondary Metabolite, Decreases the Stemness Potential of Colorectal Cancer Cells
Molecules 2018, 23(11), 2968; https://doi.org/10.3390/molecules23112968
Received: 9 October 2018 / Revised: 6 November 2018 / Accepted: 12 November 2018 / Published: 14 November 2018
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Abstract
Lichens produce various unique chemicals that are used in the pharmaceutical industry. To screen for novel lichen secondary metabolites that inhibit the stemness potential of colorectal cancer cells, we tested acetone extracts of 11 lichen samples collected in Chile. Tumidulin, isolated from Niebla
[...] Read more.
Lichens produce various unique chemicals that are used in the pharmaceutical industry. To screen for novel lichen secondary metabolites that inhibit the stemness potential of colorectal cancer cells, we tested acetone extracts of 11 lichen samples collected in Chile. Tumidulin, isolated from Niebla sp., reduced spheroid formation in CSC221, DLD1, and HT29 cells. In addition, mRNA expressions and protein levels of cancer stem markers aldehyde dehydrogenase-1 (ALDH1), cluster of differentiation 133 (CD133), CD44, Lgr5, and Musashi-1 were reduced after tumidulin treatment. Tumidulin decreased the transcriptional activity of the glioma-associated oncogene homolog zinc finger protein (Gli) promoter in reporter assays, and western blotting confirmed decreased Gli1, Gli2, and Smoothened (SMO) protein levels. Moreover, the tumidulin activity was not observed in the presence of Gli and SMO inhibitors. Together, these results demonstrate for the first time that tumidulin is a potent inhibitor of colorectal cancer cell stemness. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Quercetagetin and Patuletin: Antiproliferative, Necrotic and Apoptotic Activity in Tumor Cell Lines
Molecules 2018, 23(10), 2579; https://doi.org/10.3390/molecules23102579
Received: 22 August 2018 / Revised: 3 October 2018 / Accepted: 4 October 2018 / Published: 9 October 2018
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Abstract
Quercetagetin and patuletin were extracted by the same method from two different Tagetes species that have multiple uses in folk medicine in Mexico and around the globe, one of which is as an anticancer agent. Their biological activity (IC50 and necrotic, apoptotic
[...] Read more.
Quercetagetin and patuletin were extracted by the same method from two different Tagetes species that have multiple uses in folk medicine in Mexico and around the globe, one of which is as an anticancer agent. Their biological activity (IC50 and necrotic, apoptotic and selective activities of these flavonols) was evaluated and compared to that of quercetin, examining specifically the effects of C6 substitution among quercetin, quercetagetin and patuletin. We find that the presence of a methoxyl group in C6 enhances their potency. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Ethylenediamine Derived Carboxamides of Betulinic and Ursolic Acid as Potential Cytotoxic Agents
Molecules 2018, 23(10), 2558; https://doi.org/10.3390/molecules23102558
Received: 11 September 2018 / Revised: 26 September 2018 / Accepted: 3 October 2018 / Published: 8 October 2018
Cited by 1 | PDF Full-text (1676 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Two easily accessible, natural occurring triterpenoids, betulinic and ursolic acid, were used as starting materials for the synthesis of novel cytotoxic agents. A set of 28 ethylenediamine-spacered carboxamides was prepared holding an additional substituent connected to the ethylenediamine group. The compounds were screened
[...] Read more.
Two easily accessible, natural occurring triterpenoids, betulinic and ursolic acid, were used as starting materials for the synthesis of novel cytotoxic agents. A set of 28 ethylenediamine-spacered carboxamides was prepared holding an additional substituent connected to the ethylenediamine group. The compounds were screened in SRB assays to evaluate their cytotoxic activity employing several human tumor cell lines. Betulinic acid-derived carboxamides 1730 showed significantly higher cytotoxicity than their ursolic acid analogs 316. In particular, compounds 25 and 26 were highly cytotoxic, as indicated by EC50 values lower than 1 μM. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Ganoderma tsugae Inhibits the SREBP-1/AR Axis Leading to Suppression of Cell Growth and Activation of Apoptosis in Prostate Cancer Cells
Molecules 2018, 23(10), 2539; https://doi.org/10.3390/molecules23102539
Received: 12 September 2018 / Revised: 1 October 2018 / Accepted: 3 October 2018 / Published: 5 October 2018
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Abstract
Recent research suggests that the activation of lipid biosynthesis (lipogenesis) is linked with prostate cancer (PCa) malignancy. Sterol regulatory element-binding protein-1 (SREBP-1) is a key transcriptional regulator controlling lipogenesis. Moreover, androgen receptor (AR) has been well defined to play an important role in
[...] Read more.
Recent research suggests that the activation of lipid biosynthesis (lipogenesis) is linked with prostate cancer (PCa) malignancy. Sterol regulatory element-binding protein-1 (SREBP-1) is a key transcriptional regulator controlling lipogenesis. Moreover, androgen receptor (AR) has been well defined to play an important role in lethal PCa aggressiveness from androgen-responsive to castration-resistant status. In this study, we showed that the quality-assured Ganoderma tsugae ethanol extract (GTEE), a Chinese natural and herbal product, significantly inhibited expression of SREBP-1 and its downstream genes associated with lipogenesis in PCa cells. Through inhibiting SREBP-1, GTEE reduced the levels of intracellular fatty acids and lipids in PCa cells. Importantly, GTEE also downregulated the expression of AR and prostate-specific antigen (PSA) in both androgen-responsive and castration-resistant PCa cells. By blocking the SREBP-1/AR axis, GTEE suppressed cell growth and progressive behaviors, as well as activating the caspase-dependent apoptotic pathway in PCa cells. These data provide a new molecular basis of GTEE for the development of a potential therapeutic approach to treat PCa malignancy. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Structural Characterization of Polysaccharides from Dendrobium officinale and Their Effects on Apoptosis of HeLa Cell Line
Molecules 2018, 23(10), 2484; https://doi.org/10.3390/molecules23102484
Received: 4 September 2018 / Revised: 24 September 2018 / Accepted: 25 September 2018 / Published: 27 September 2018
Cited by 1 | PDF Full-text (5411 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Dendrobium officinale is a widely used medicinal plant in China with numerous bio-activities. However, the main structure and anti-tumor activity of the polysaccharides from this plant have not been investigated. In this study, we elucidated the main structure of polysaccharides purified with DEAE
[...] Read more.
Dendrobium officinale is a widely used medicinal plant in China with numerous bio-activities. However, the main structure and anti-tumor activity of the polysaccharides from this plant have not been investigated. In this study, we elucidated the main structure of polysaccharides purified with DEAE and Sephadex G-25 from Dendrobium officinale grown under different planting conditions. In addition, the anti-tumor activity was tested via MTT assays. The results showed that the polysaccharides of Dendrobium officinale grown under different conditions were almost the same, with slight differences in the branched chain; both polysaccharide fractions consisted of (1→4)-linked mannose and (1→4)-linked glucose, with an O-acetyl group in the mannose. After degradation, the polysaccharide fractions from wild plants showed significant anti-proliferation activity in HeLa cells. The fractions F1 and F3 induced apoptosis by up-regulating the expression of ERK, JNK, and p38. We concluded that polysaccharides from Dendrobium officinale planted in the wild exhibit significant anti-tumor effects only after being degraded to smaller molecular weight species. The planting mode is a significant factor in the pharmacological activity of Dendrobium officinale. We advise that the planting conditions for Dendrobium officinale should be changed. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Microbial Synthesis of Non-Natural Anthraquinone Glucosides Displaying Superior Antiproliferative Properties
Molecules 2018, 23(9), 2171; https://doi.org/10.3390/molecules23092171
Received: 17 July 2018 / Revised: 14 August 2018 / Accepted: 21 August 2018 / Published: 28 August 2018
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Abstract
Anthraquinones, naturally occurring bioactive compounds, have been reported to exhibit various biological activities, including anti-inflammatory, antiviral, antimicrobial, and anticancer effects. In this study, we biotransformed three selected anthraquinones into their novel O-glucoside derivatives, expressing a versatile glycosyltransferase (YjiC) from Bacillus licheniformis DSM
[...] Read more.
Anthraquinones, naturally occurring bioactive compounds, have been reported to exhibit various biological activities, including anti-inflammatory, antiviral, antimicrobial, and anticancer effects. In this study, we biotransformed three selected anthraquinones into their novel O-glucoside derivatives, expressing a versatile glycosyltransferase (YjiC) from Bacillus licheniformis DSM 13 in Escherichia coli. Anthraflavic acid, alizarin, and 2-amino-3-hydroxyanthraquinone were exogenously fed to recombinant E. coli as substrate for biotransformation. The products anthraflavic acid-O-glucoside, alizarin 2-O-β-d-glucoside, and 2-amino-3-O-glucosyl anthraquinone produced in the culture broths were characterized by various chromatographic and spectroscopic analyses. The comparative anti-proliferative assay against various cancer cells (gastric cancer-AGS, uterine cervical cancer-HeLa, and liver cancer-HepG2) were remarkable, since the synthesized glucoside compounds showed more than 60% of cell growth inhibition at concentrations ranging from ~50 μM to 100 μM. Importantly, one of the synthesized glucoside derivatives, alizarin 2-O-glucoside inhibited more than 90% of cell growth in all the cancer cell lines tested. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Zeylenone Induces Mitochondrial Apoptosis and Inhibits Migration and Invasion in Gastric Cancer
Molecules 2018, 23(9), 2149; https://doi.org/10.3390/molecules23092149
Received: 8 August 2018 / Revised: 20 August 2018 / Accepted: 23 August 2018 / Published: 27 August 2018
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Abstract
The mortality of gastric cancer (GC) is increasing due to its high rates of recurrence and metastasis. Zeylenone (Zey), a type of naturally occurring cyclohexene oxide, was demonstrated to be effective in cancer patients. The aim of this study is to explore the
[...] Read more.
The mortality of gastric cancer (GC) is increasing due to its high rates of recurrence and metastasis. Zeylenone (Zey), a type of naturally occurring cyclohexene oxide, was demonstrated to be effective in cancer patients. The aim of this study is to explore the anti-cancer effect of Zey against gastric cancer both in vitro and in vivo, as well as the underlying mechanisms. We found that Zey inhibited gastric tumor growth, as demonstrated by in vitro gastric cancer cell lines and in a human gastric cancer xenograft mouse model. Furthermore, Zey induced substantial apoptosis through a mitochondrial apoptotic pathway, involving mitochondrial transmembrane potential loss, caspase-3 activation, anti-apoptotic protein downregulation, and pro-apoptotic protein upregulation. Notably, we revealed for the first time that Zey suppressed invasion and migration by wound healing and transwell chamber assays. Through Western blotting, we further explored the potential mechanism of Zey’s anti-cancer activity. We found that Zey downregulated the expression of matrix metalloproteinase 2/9 (MMP 2/9) and inhibited the phosphorylation of AKT and ERK. In short, Zey, which induced mitochondrial apoptosis and inhibited proliferation, migration, and invasion, may be developed as a novel drug for the treatment of gastric cancer. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle JNK Inactivation Induces Polyploidy and Drug-Resistance in Coronarin D-Treated Osteosarcoma Cells
Molecules 2018, 23(9), 2121; https://doi.org/10.3390/molecules23092121
Received: 27 July 2018 / Revised: 19 August 2018 / Accepted: 21 August 2018 / Published: 23 August 2018
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Abstract
Inhibition of proliferating cells is a critical strategy for cancer therapy. In this study, we demonstrated that coronarin D, a natural component extracted from the rhizomes of Hedychium coronarium, significantly suppressed the proliferation of osteosarcoma cells. The treatment with coronarin D resulted
[...] Read more.
Inhibition of proliferating cells is a critical strategy for cancer therapy. In this study, we demonstrated that coronarin D, a natural component extracted from the rhizomes of Hedychium coronarium, significantly suppressed the proliferation of osteosarcoma cells. The treatment with coronarin D resulted in the activation of caspase-3 and apoptosis. This treatment induced the accumulation of cyclin B1 and DNA condensation indicating the treated osteosarcoma cells were arrested in mitotic phase. Furthermore, the treatment with coronarin D increased the levels of phosphorylated c-Jun NH2-terminal kinase (JNK) in human osteosarcoma cells. Pretreatment with JNK inhibitor blocked the accumulation of cyclin B1 and DNA condensation, resulting the accumulation of tetraploid cells in coronarin D-treated osteosarcoma HOS cells, indicating JNK inactivation blocked the mitotic entry and arrested cells in the 4 N state. After adaptation, the arrested tetraploid cells continued to duplicate their DNA resulting in polyploidy. Interestingly, when the arrested mitotic cells induced by coronarin D were treated with JNK inhibitor, the accumulated cyclin B1 and DNA condensation were immediately eliminated. These arrested 4 N cells loss the ability to undergo cytokinesis, and ultimately continued to duplicate DNA upon prolonged arrest resulting in the production of polyploid populations. JNK inactivation, either by the pretreatment with JNK inhibitor or the treatment with JNK inhibitor in coronarin D-induced mitotic cells, both caused resistance to coronarin D-induced cell death. Taken together, our findings indicate that coronarin D induces the apoptosis and mitosis arrest in human osteosarcoma cells. JNK has a crucial role in coronarin D-induced mitosis arrest and apoptosis. We hypothesize that functional evaluation of JNK may produce more specific and effective therapies in coronarin D-related trail for treatment of human osteosarcoma. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessArticle Novel Polyketides Produced by the Endophytic Fungus Aspergillus Fumigatus from Cordyceps Sinensis
Molecules 2018, 23(7), 1709; https://doi.org/10.3390/molecules23071709
Received: 21 June 2018 / Revised: 6 July 2018 / Accepted: 7 July 2018 / Published: 13 July 2018
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Abstract
Five new polyketides, including two pairs of enantiomers and a racemate, were isolated from the fermentation broth of Aspergillus fumigatus, an endophytic fungus isolated from Cordyceps sinensis. Their structures were identified using one-dimensional (1D) and two-dimensional (2D) NMR experiments, and the
[...] Read more.
Five new polyketides, including two pairs of enantiomers and a racemate, were isolated from the fermentation broth of Aspergillus fumigatus, an endophytic fungus isolated from Cordyceps sinensis. Their structures were identified using one-dimensional (1D) and two-dimensional (2D) NMR experiments, and the absolute configurations of the enantiomers were confirmed using electronic circular dichroism (ECD) calculations. Compounds 1a and 2a exhibited inhibitory activity against the MV4-11 cell line in vitro, with IC50 values of 23.95 µM and 32.70 µM, respectively. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Open AccessFeature PaperArticle Cytotoxic Triterpenes from Salacia crassifolia and Metabolite Profiling of Celastraceae Species
Molecules 2018, 23(6), 1494; https://doi.org/10.3390/molecules23061494
Received: 2 June 2018 / Revised: 15 June 2018 / Accepted: 18 June 2018 / Published: 20 June 2018
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Abstract
The new pentacyclic triterpene 11β-hydroxypristimerin (1), along with the known metabolites pristimerin (2), 6-oxopristimerol (3) and vitideasin (4), were isolated from a Salacia crassifolia root wood extract, following a bioassay-guided fractionation approach. Both
[...] Read more.
The new pentacyclic triterpene 11β-hydroxypristimerin (1), along with the known metabolites pristimerin (2), 6-oxopristimerol (3) and vitideasin (4), were isolated from a Salacia crassifolia root wood extract, following a bioassay-guided fractionation approach. Both the extract and the purified triterpenes displayed pronounced cytotoxic activity against human cancer cell lines. The NCI-60 cell line screen revealed that compound 2 was the most active, with a mean GI50 of 0.17 μM, while compound 1 had a mean GI50 of 8.7 μM. A COMPARE analysis of the screening results showed that pristimerin is likely to be the main compound responsible for the cytotoxic activity of the extract (mean GI50 of 0.3 μg·mL−1). A targeted search for pristimerin and related derivatives using LC-MS/MS revealed the presence of pristimerin (2) and 6-oxopristimerol (3) in all Celastraceae species examined and in all plant parts tested, while vitideasin (4) was only detected in the genus Salacia. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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Review

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Open AccessReview Biochemical Basis of Anti-Cancer-Effects of Phloretin—A Natural Dihydrochalcone
Molecules 2019, 24(2), 278; https://doi.org/10.3390/molecules24020278
Received: 24 December 2018 / Revised: 8 January 2019 / Accepted: 10 January 2019 / Published: 13 January 2019
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Abstract
Apple is a rich source of bioactive phytochemicals that help improve health by preventing and/or curing many disease processes, including cancer. One of the apple polyphenols is phloretin [2′,4′,6′-Trihydroxy-3-(4-hydroxyphenyl)-propiophenone], which has been widely investigated for its antioxidant, anti-inflammatory and anti-cancer activities in a
[...] Read more.
Apple is a rich source of bioactive phytochemicals that help improve health by preventing and/or curing many disease processes, including cancer. One of the apple polyphenols is phloretin [2′,4′,6′-Trihydroxy-3-(4-hydroxyphenyl)-propiophenone], which has been widely investigated for its antioxidant, anti-inflammatory and anti-cancer activities in a wide array of preclinical studies. The efficacy of phloretin in suppressing xenograft tumor growth in athymic nude mice implanted with a variety of human cancer cells, and the ability of the compound to interfere with cancer cells signaling, have made it a promising candidate for anti-cancer drug development. Mechanistically, phloretin has been reported to arrest the growth of tumor cells by blocking cyclins and cyclin-dependent kinases and induce apoptosis by activating mitochondria-mediated cell death. The blockade of the glycolytic pathway via downregulation of GLUT2 mRNA and proteins, and the inhibition of tumor cells migration, also corroborates the anti-cancer effects of phloretin. This review sheds light on the molecular targets of phloretin as a potential anti-cancer and anti-inflammatory natural agent. Full article
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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