Molecules

Editorial

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8 pages, 262 KiB

Open AccessEditorial

Are Ancestral Medical Practices the Future Solution to Today’s Medical Problems?

by José A. Lupiáñez, Eva E. Rufino-Palomares and Amalia Pérez-Jiménez

Molecules 2021, 26(15), 4701; https://doi.org/10.3390/molecules26154701 - 3 Aug 2021

Cited by 1 | Viewed by 2557

Abstract

Our cells and organs are threatened and, in most cases, constantly subjected to the aggression of numerous situations, both endogenous, characterized by unfavorable genetics, and exogenous, by deficient or inadequate nutrition, and even by a hostile environment; in most cases, they ultimately cause [...] Read more.

Our cells and organs are threatened and, in most cases, constantly subjected to the aggression of numerous situations, both endogenous, characterized by unfavorable genetics, and exogenous, by deficient or inadequate nutrition, and even by a hostile environment; in most cases, they ultimately cause a cascade of degenerative and cardiovascular diseases, cancer, and infections, as well as those related to the metabolic syndrome, all of which eventually generate irreversible damage to the organism and, consequently, a significant deterioration in its survival [...] Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

Research

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25 pages, 6322 KiB

Open AccessArticle

Glycoconjugation of Betulin Derivatives Using Copper-Catalyzed 1,3-Dipolar Azido-Alkyne Cycloaddition Reaction and a Preliminary Assay of Cytotoxicity of the Obtained Compounds

by Mirosława Grymel, Gabriela Pastuch-Gawołek, Anna Lalik, Mateusz Zawojak, Seweryn Boczek, Monika Krawczyk and Karol Erfurt

Molecules 2020, 25(24), 6019; https://doi.org/10.3390/molecules25246019 - 18 Dec 2020

Cited by 21 | Viewed by 4101

Abstract

Pentacyclic lupane-type triterpenoids, such as betulin and its synthetic derivatives, display a broad spectrum of biological activity. However, one of the major drawbacks of these compounds as potential therapeutic agents is their high hydrophobicity and low bioavailability. On the other hand, the presence [...] Read more.

Pentacyclic lupane-type triterpenoids, such as betulin and its synthetic derivatives, display a broad spectrum of biological activity. However, one of the major drawbacks of these compounds as potential therapeutic agents is their high hydrophobicity and low bioavailability. On the other hand, the presence of easily transformable functional groups in the parent structure makes betulin have a high synthetic potential and the ability to form different derivatives. In this context, research on the synthesis of new betulin derivatives as conjugates of naturally occurring triterpenoid with a monosaccharide via a linker containing a heteroaromatic 1,2,3-triazole ring was presented. It has been shown that copper-catalyzed 1,3-dipolar azide-alkyne cycloaddition reaction (CuAAC) provides an easy and effective way to synthesize new molecular hybrids based on natural products. The chemical structures of the obtained betulin glycoconjugates were confirmed by spectroscopic analysis. Cytotoxicity of the obtained compounds was evaluated on a human breast adenocarcinoma cell line (MCF-7) and colorectal carcinoma cell line (HCT 116). The obtained results show that despite the fact that the obtained betulin glycoconjugates do not show interesting antitumor activity, the idea of adding a sugar unit to the betulin backbone may, after some modifications, turn out to be correct and allow for the targeted transport of betulin glycoconjugates into the tumor cells. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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13 pages, 3928 KiB

Open AccessArticle

Macrocybin, a Natural Mushroom Triglyceride, Reduces Tumor Growth In Vitro and In Vivo through Caveolin-Mediated Interference with the Actin Cytoskeleton

by Marcos Vilariño, Josune García-Sanmartín, Laura Ochoa-Callejero, Alberto López-Rodríguez, Jaime Blanco-Urgoiti and Alfredo Martínez

Molecules 2020, 25(24), 6010; https://doi.org/10.3390/molecules25246010 - 18 Dec 2020

Cited by 8 | Viewed by 3119

Abstract

Mushrooms have been used for millennia as cancer remedies. Our goal was to screen several mushroom species from the rainforests of Costa Rica, looking for new antitumor molecules. Mushroom extracts were screened using two human cell lines: A549 (lung adenocarcinoma) and NL20 (immortalized [...] Read more.

Mushrooms have been used for millennia as cancer remedies. Our goal was to screen several mushroom species from the rainforests of Costa Rica, looking for new antitumor molecules. Mushroom extracts were screened using two human cell lines: A549 (lung adenocarcinoma) and NL20 (immortalized normal lung epithelium). Extracts able to kill tumor cells while preserving non-tumor cells were considered “anticancer”. The mushroom with better properties was Macrocybe titans. Positive extracts were fractionated further and tested for biological activity on the cell lines. The chemical structure of the active compound was partially elucidated through nuclear magnetic resonance, mass spectrometry, and other ancillary techniques. Chemical analysis showed that the active molecule was a triglyceride containing oleic acid, palmitic acid, and a more complex fatty acid with two double bonds. The synthesis of all possible triglycerides and biological testing identified the natural compound, which was named Macrocybin. A xenograft study showed that Macrocybin significantly reduces A549 tumor growth. In addition, Macrocybin treatment resulted in the upregulation of Caveolin-1 expression and the disassembly of the actin cytoskeleton in tumor cells (but not in normal cells). In conclusion, we have shown that Macrocybin constitutes a new biologically active compound that may be taken into consideration for cancer treatment. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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15 pages, 2710 KiB

Open AccessArticle

Implication of Lactucopicrin in Autophagy, Cell Cycle Arrest and Oxidative Stress to Inhibit U87Mg Glioblastoma Cell Growth

by Rossella Rotondo, Maria Antonietta Oliva, Sabrina Staffieri, Salvatore Castaldo, Felice Giangaspero and Antonietta Arcella

Molecules 2020, 25(24), 5843; https://doi.org/10.3390/molecules25245843 - 10 Dec 2020

Cited by 15 | Viewed by 4358

Abstract

In this study, we propose lactucopicrin (LCTP), a natural sesquiterpene lactone from Lactucavirosa, as a molecule able to control the growth of glioblastoma continuous cell line U87Mg. The IC50 of U87Mg against LCTP revealed a strong cytotoxic effect. Daily administration of LCTP showed [...] Read more.

In this study, we propose lactucopicrin (LCTP), a natural sesquiterpene lactone from Lactucavirosa, as a molecule able to control the growth of glioblastoma continuous cell line U87Mg. The IC50 of U87Mg against LCTP revealed a strong cytotoxic effect. Daily administration of LCTP showed a dose and time-dependent reduction of GBM cell growth and viability, also confirmed by inhibition of clonogenic potential and mobility of U87Mg cells. LCTP activated autophagy in U87Mg cells and decreased the phosphorylation of proliferative signals pAKT and pERK. LCTP also induced the cell cycle arrest in G2/M phase, confirmed by decrease of CDK2 protein and increase of p53 and p21. LCTP stimulated apoptosis as evidenced by reduction of procaspase 6 and the increase of the cleaved/full-length PARP ratio. The pre-treatment of U87Mg cells with ROS scavenger N-acetylcysteine (NAC), which reversed its cytotoxic effect, showed the involvement of LCTP in oxidative stress. Finally, LCTP strongly enhanced the sensitivity of U87Mg cells to canonical therapy Temozolomide (TMZ) and synergized with this drug. Altogether, the growth inhibition of U87Mg GBM cells induced by LCTP is the result of several synergic mechanisms, which makes LCTP a promising adjuvant therapy for this complex pathology. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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23 pages, 8487 KiB

Open AccessArticle

Pogostemon cablin Triggered ROS-Induced DNA Damage to Arrest Cell Cycle Progression and Induce Apoptosis on Human Hepatocellular Carcinoma In Vitro and In Vivo

by Xiao-Fan Huang, Gwo-Tarng Sheu, Kai-Fu Chang, Ya-Chih Huang, Pei-Hsiu Hung and Nu-Man Tsai

Molecules 2020, 25(23), 5639; https://doi.org/10.3390/molecules25235639 - 30 Nov 2020

Cited by 13 | Viewed by 6769

Abstract

The purpose of the study was to elucidate the anti-hepatoma effects and mechanisms of Pogostemon cablin essential oils (PPa extract) in vitro and in vivo. PPa extract exhibited an inhibitory effect on hepatocellular carcinoma (HCC) cells and was less cytotoxic to normal cells, [...] Read more.

The purpose of the study was to elucidate the anti-hepatoma effects and mechanisms of Pogostemon cablin essential oils (PPa extract) in vitro and in vivo. PPa extract exhibited an inhibitory effect on hepatocellular carcinoma (HCC) cells and was less cytotoxic to normal cells, especially normal liver cells, than it was to HCC cells, exerting a good selective index. Additionally, PPa extract inhibited HCC cell growth by blocking the cell cycle at the G₀/G₁ phase via p53 dependent or independent pathway to down regulated cell cycle regulators. Moreover, PPa extract induced the FAS-FASL-caspase-8 system to activate the extrinsic apoptosis pathway, and it increased the bax/bcl-2 ratio and reduced ΔΨm to activate the intrinsic apoptosis pathway that might be due to lots of reactive oxygen species (ROS) production which was induced by PPa extract. In addition, PPa extract presented to the potential to act synergistically with sorafenib to effectively inhibit HCC cell proliferation through the Akt/mTOR pathway and reduce regrowth of HCC cells. In an animal model, PPa extract suppressed HCC tumor growth and prolonged lifespan by reducing the VEGF/VEGFR axis and inducing tumor cell apoptosis in vivo. Ultimately, PPa extract demonstrated nearly no or low system-wide, physiological, or pathological toxicity in vivo. In conclusion, PPa extract effectively inhibited HCC cell growth through inducing cell cycle arrest and activating apoptosis in vitro and in vivo. Furthermore, PPa extract exhibits less toxicity toward normal cells and organs than it does toward HCC cells, which might lead to fewer side effects in clinical applications. PPa extract may be developed into a clinical drug to suppress tumor growth or functional food to prevent HCC initiation or chemoprotection of HCC recurrence. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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18 pages, 8517 KiB

Open AccessArticle

From a Medicinal Mushroom Blend a Direct Anticancer Effect on Triple-Negative Breast Cancer: A Preclinical Study on Lung Metastases

by Elisa Roda, Fabrizio De Luca, Carlo Alessandro Locatelli, Daniela Ratto, Carmine Di Iorio, Elena Savino, Maria Grazia Bottone and Paola Rossi

Molecules 2020, 25(22), 5400; https://doi.org/10.3390/molecules25225400 - 18 Nov 2020

Cited by 9 | Viewed by 4340

Abstract

Bioactive metabolites isolated from medicinal mushrooms (MM) used as supportive treatment in conventional oncology have recently gained interest. Acting as anticancer agents, they interfere with tumor cells and microenvironment (TME), disturbing cancer development/progression. Nonetheless, their action mechanisms still need to be elucidated. Recently, [...] Read more.

Bioactive metabolites isolated from medicinal mushrooms (MM) used as supportive treatment in conventional oncology have recently gained interest. Acting as anticancer agents, they interfere with tumor cells and microenvironment (TME), disturbing cancer development/progression. Nonetheless, their action mechanisms still need to be elucidated. Recently, using a 4T1 triple-negative mouse BC model, we demonstrated that supplementation with Micotherapy U-Care, a MM blend, produced a striking reduction of lung metastases density/number, paralleled by decreased inflammation and oxidative stress both in TME and metastases, together with QoL amelioration. We hypothesized that these effects could be due to either a direct anticancer effect and/or to a secondary/indirect impact of Micotherapy U-Care on systemic inflammation/immunomodulation. To address this question, we presently focused on apoptosis/proliferation, investigating specific molecules, i.e., PARP1, p53, BAX, Bcl2, and PCNA, whose critical role in BC is well recognized. We revealed that Micotherapy U-Care is effective to influence balance between cell death and proliferation, which appeared strictly interconnected and inversely related (p53/Bax vs. Bcl2/PARP1/PCNA expression trends). MM blend displayed a direct effect, with different efficacy extent on cancer cells and TME, forcing tumor cells to apoptosis. Yet again, this study supports the potential of MM extracts, as adjuvant supplement in the TNBC management. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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18 pages, 3780 KiB

Open AccessFeature PaperArticle

Antiproliferative and Pro-Apoptotic Effect of Uvaol in Human Hepatocarcinoma HepG2 Cells by Affecting G0/G1 Cell Cycle Arrest, ROS Production and AKT/PI3K Signaling Pathway

by Gloria C. Bonel-Pérez, Amalia Pérez-Jiménez, Isabel Gris-Cárdenas, Alberto M. Parra-Pérez, José Antonio Lupiáñez, Fernando J. Reyes-Zurita, Eva Siles, René Csuk, Juan Peragón and Eva E. Rufino-Palomares

Molecules 2020, 25(18), 4254; https://doi.org/10.3390/molecules25184254 - 16 Sep 2020

Cited by 24 | Viewed by 4774

Abstract

Natural products have a significant role in the development of new drugs, being relevant the pentacyclic triterpenes extracted from Olea europaea L. Anticancer effect of uvaol, a natural triterpene, has been scarcely studied. The aim of this study was to understand the [...] Read more.

Natural products have a significant role in the development of new drugs, being relevant the pentacyclic triterpenes extracted from Olea europaea L. Anticancer effect of uvaol, a natural triterpene, has been scarcely studied. The aim of this study was to understand the anticancer mechanism of uvaol in the HepG2 cell line. Cytotoxicity results showed a selectivity effect of uvaol with higher influence in HepG2 than WRL68 cells used as control. Our results show that uvaol has a clear and selective anticancer activity in HepG2 cells supported by a significant anti-migratory capacity and a significant increase in the expression of HSP-60. Furthermore, the administration of this triterpene induces cell arrest in the G₀/G₁ phase, as well as an increase in the rate of cell apoptosis. These results are supported by a decrease in the expression of the anti-apoptotic protein Bcl2, an increase in the expression of the pro-apoptotic protein Bax, together with a down-regulation of the AKT/PI3K signaling pathway. A reduction in reactive oxygen species (ROS) levels in HepG2 cells was also observed. Altogether, results showed anti-proliferative and pro-apoptotic effect of uvaol on hepatocellular carcinoma, constituting an interesting challenge in the development of new treatments against this type of cancer. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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17 pages, 3964 KiB

Open AccessArticle

Elaeagnus angustifolia Plant Extract Inhibits Epithelial-Mesenchymal Transition and Induces Apoptosis via HER2 Inactivation and JNK Pathway in HER2-Positive Breast Cancer Cells

by Ayesha Jabeen, Anju Sharma, Ishita Gupta, Hadeel Kheraldine, Semir Vranic, Ala-Eddin Al Moustafa and Halema F. Al Farsi

Molecules 2020, 25(18), 4240; https://doi.org/10.3390/molecules25184240 - 16 Sep 2020

Cited by 22 | Viewed by 4937

Abstract

Elaeagnus angustifolia (EA) is a medicinal plant used for treating several human diseases in the Middle East. Meanwhile, the outcome of EA extract on HER2-positive breast cancer remains nascent. Thus, we herein investigated the effects of the aqueous EA extract obtained [...] Read more.

Elaeagnus angustifolia (EA) is a medicinal plant used for treating several human diseases in the Middle East. Meanwhile, the outcome of EA extract on HER2-positive breast cancer remains nascent. Thus, we herein investigated the effects of the aqueous EA extract obtained from the flowers of EA on two HER2-positive breast cancer cell lines, SKBR3 and ZR75-1. Our data revealed that EA extract inhibits cell proliferation and deregulates cell-cycle progression of these two cancer cell lines. EA extract also prevents the progression of epithelial-mesenchymal transition (EMT), an important event for cancer invasion and metastasis; this is accompanied by upregulations of E-cadherin and β-catenin, in addition to downregulations of vimentin and fascin, which are major markers of EMT. Thus, EA extract causes a drastic decrease in cell invasion ability of SKBR3 and ZR75-1 cancer cells. Additionally, we found that EA extract inhibits colony formation of both cell lines in comparison with their matched control. The molecular pathway analysis of HER2 and JNK1/2/3 of EA extract exposed cells revealed that it can block HER2 and JNK1/2/3 activities, which could be the major molecular pathway behind these events. Our findings implicate that EA extract may possess chemo-preventive effects against HER2-positive breast cancer via HER2 inactivation and specifically JNK1/2/3 signaling pathways. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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14 pages, 1932 KiB

Open AccessFeature PaperArticle

Unveiling the Differential Antioxidant Activity of Maslinic Acid in Murine Melanoma Cells and in Rat Embryonic Healthy Cells Following Treatment with Hydrogen Peroxide

by Khalida Mokhtari, Amalia Pérez-Jiménez, Leticia García-Salguero, José A. Lupiáñez and Eva E. Rufino-Palomares

Molecules 2020, 25(17), 4020; https://doi.org/10.3390/molecules25174020 - 3 Sep 2020

Cited by 26 | Viewed by 3280

Abstract

Maslinic acid (MA) is a natural triterpene from Olea europaea L. with multiple biological properties. The aim of the present study was to examine MA’s effect on cell viability (by the MTT assay), reactive oxygen species (ROS levels, by flow cytometry) and key [...] Read more.

Maslinic acid (MA) is a natural triterpene from Olea europaea L. with multiple biological properties. The aim of the present study was to examine MA’s effect on cell viability (by the MTT assay), reactive oxygen species (ROS levels, by flow cytometry) and key antioxidant enzyme activities (by spectrophotometry) in murine skin melanoma (B16F10) cells compared to those on healthy cells (A10). MA induced cytotoxic effects in cancer cells (IC₅₀ 42 µM), whereas no effect was found in A10 cells treated with MA (up to 210 µM). In order to produce a stress situation in cells, 0.15 mM H₂O₂ was added. Under stressful conditions, MA protected both cell lines against oxidative damage, decreasing intracellular ROS, which were higher in B16F10 than in A10 cells. The treatment with H₂O₂ and without MA produced different responses in antioxidant enzyme activities depending on the cell line. In A10 cells, all the enzymes were up-regulated, but in B16F10 cells, only superoxide dismutase, glutathione S-transferase and glutathione peroxidase increased their activities. MA restored the enzyme activities to levels similar to those in the control group in both cell lines, highlighting that in A10 cells, the highest MA doses induced values lower than control. Overall, these findings demonstrate the great antioxidant capacity of MA. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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14 pages, 3513 KiB

Open AccessArticle

Anti-Cancer Effect of 3-Hydroxy-β-Ionone Identified from Moringa oleifera Lam. Leaf on Human Squamous Cell Carcinoma 15 Cell Line

by Thitiya Luetragoon, Rungnapa Pankla Sranujit, Chanai Noysang, Yordhathai Thongsri, Pachuen Potup, Nungruthai Suphrom, Nitra Nuengchamnong and Kanchana Usuwanthim

Molecules 2020, 25(16), 3563; https://doi.org/10.3390/molecules25163563 - 5 Aug 2020

Cited by 28 | Viewed by 4398

Abstract

Squamous cell carcinoma is the most common type of head and neck cancer worldwide. Radiation and chemotherapy are general treatments for patients; however, these remedies can have adverse side effects and tumours develop drug resistance. Effective treatments still require improvement for cancer patients. [...] Read more.

Squamous cell carcinoma is the most common type of head and neck cancer worldwide. Radiation and chemotherapy are general treatments for patients; however, these remedies can have adverse side effects and tumours develop drug resistance. Effective treatments still require improvement for cancer patients. Here, we investigated the anti-cancer effect of Moringa oleifera (MO) Lam. leaf extracts and their fractions, 3-hydroxy-β-ionone on SCC15 cell line. SCC15 were treated with and without MO leaf extracts and their fractions. MTT assay was used to determine cell viability on SCC15. Cell cycle and apoptosis were evaluated by the Muse™ Cell Analyser. Colony formation and wound closure analysis of SCC15 were performed in 6-well plates. Apoptosis markers were evaluated by immunoblotting. We found that Moringa extracts and 3-HBI significantly inhibited proliferation of SCC15. Moreover, they induced apoptosis and cell cycle arrest at G2/M phase in SCC15 compared to the untreated control. MO extracts and 3-HBI also inhibited colony formation and cell migration of SCC15. Furthermore, we observed the upregulation of cleaved caspase-3 and Bax with downregulation of anti-apoptotic Bcl-2, indicating the induction of cancer cell apoptosis. Our results revealed that MO extracts and 3-HBI provided anti-cancer properties by inhibiting progression and inducing apoptosis of SCC15. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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16 pages, 3021 KiB

Open AccessArticle

Anticancer Activity of Novel Plant Extracts and Compounds from Adenosma bracteosum (Bonati) in Human Lung and Liver Cancer Cells

by Ngoc Hong Nguyen, Qui Thanh Hoai Ta, Quang Thang Pham, Thi Ngoc Han Luong, Van Trung Phung, Thuc-Huy Duong and Van Giau Vo

Molecules 2020, 25(12), 2912; https://doi.org/10.3390/molecules25122912 - 24 Jun 2020

Cited by 91 | Viewed by 9637

Abstract

Cancer is the second leading cause of death globally, and despite the advances in drug development, it is still necessary to develop new plant-derived medicines. Compared with using conventional chemical drugs to decrease the side effects induced by chemotherapy, natural herbal medicines have [...] Read more.

Cancer is the second leading cause of death globally, and despite the advances in drug development, it is still necessary to develop new plant-derived medicines. Compared with using conventional chemical drugs to decrease the side effects induced by chemotherapy, natural herbal medicines have many advantages. The present study aimed to discover the potential cytotoxicity of ethanol extract and its derived fractions (chloroform, ethyl acetate, butanol, and aqueous) of Adenosma bracteosum Bonati. (A. bracteosum) on human large cell lung carcinoma (NCI-H460) and hepatocellular carcinoma (HepG2). Among these fractions, the chloroform showed significant activity in the inhibition of proliferation of both cancerous cells because of the presence of bioactive compounds including xanthomicrol, 5,4’-dihydroxy-6,7,8,3’-tetramethoxyflavone, and ursolic acid which were clearly revealed by nuclear magnetic resonance spectroscopy (¹H-NMR, ¹³C-NMR, Heteronuclear Multiple Bond Coherence, and Heteronuclear Single Quantum Coherence Spectroscopy) analyses. According to the radical scavenging capacity, the 5,4’-dihydroxy-6,7,8,3’-tetramethoxyflavone compound (AB2) exhibited the highest anticancer activity on both NCI-H460 and HepG2 with IC₅₀ values of 4.57 ± 0.32 and 5.67 ± 0.09 µg/mL respectively, followed by the ursolic acid with the lower percent inhibition at 13.05 ± 0.55 and 10.00 ± 0.16 µg/mL, respectively (p < 0.05). Remarkably, the AB2 compound induced to significant increase in the production of reactive oxygen species accompanied by attenuation of mitochondrial membrane potential, thus inducing the activation of caspase-3 activity in both human lung and liver cancer cells. These results suggest that A. bracteosum is a promising source of useful natural products and AB2 offers opportunities to develop the novel anticancer drugs. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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20 pages, 2750 KiB

Open AccessArticle

Polish Propolis—Chemical Composition and Biological Effects in Tongue Cancer Cells and Macrophages

by Joanna Wezgowiec, Anna Wieczynska, Wlodzimierz Wieckiewicz, Julita Kulbacka, Jolanta Saczko, Natalia Pachura, Mieszko Wieckiewicz, Roman Gancarz and Kazimiera A. Wilk

Molecules 2020, 25(10), 2426; https://doi.org/10.3390/molecules25102426 - 22 May 2020

Cited by 42 | Viewed by 5281

Abstract

The purpose of this study was to compare the chemical composition and biological properties of Polish propolis. Ethanol, ethanol-hexane, hexane and hexane-ethanol extracts of propolis from three different regions of Poland were prepared. On the basis of the evaluation of their chemical composition [...] Read more.

The purpose of this study was to compare the chemical composition and biological properties of Polish propolis. Ethanol, ethanol-hexane, hexane and hexane-ethanol extracts of propolis from three different regions of Poland were prepared. On the basis of the evaluation of their chemical composition as well as the extraction yield and free radical scavenging activity, the ethanol and hexane-ethanol extractions were proposed as the most effective methods. Subsequently, the biological properties of the extracts were evaluated to investigate the selectivity of an anticancer effect on tongue cancer cells in comparison to normal gingival fibroblasts. The obtained products demonstrated anticancer activity against tongue cancer cells. Additionally, when the lowest extract concentration (100 µg/mL) was applied, they were not cytotoxic to gingival fibroblasts. Finally, a possible anti-inflammatory potential of the prepared products was revealed, as reduced mitochondrial activity and proliferation of macrophages exposed to the extracts were observed. The results obtained indicate a potential of Polish propolis as a natural product with cancer-selective toxicity and anti-inflammatory effect. However, further studies are still needed to thoroughly explain the molecular mechanisms of its action and to obtain the promising health benefits of this versatile natural product. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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Review

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21 pages, 1990 KiB

Open AccessReview

Biophysical Characterization and Anticancer Activities of Photosensitive Phytoanthraquinones Represented by Hypericin and Its Model Compounds

by Valéria Verebová, Jiří Beneš and Jana Staničová

Molecules 2020, 25(23), 5666; https://doi.org/10.3390/molecules25235666 - 1 Dec 2020

Cited by 23 | Viewed by 4068

Abstract

Photosensitive compounds found in herbs have been reported in recent years as having a variety of interesting medicinal and biological activities. In this review, we focus on photosensitizers such as hypericin and its model compounds emodin, quinizarin, and danthron, which have antiviral, antifungal, [...] Read more.

Photosensitive compounds found in herbs have been reported in recent years as having a variety of interesting medicinal and biological activities. In this review, we focus on photosensitizers such as hypericin and its model compounds emodin, quinizarin, and danthron, which have antiviral, antifungal, antineoplastic, and antitumor effects. They can be utilized as potential agents in photodynamic therapy, especially in photodynamic therapy (PDT) for cancer. We aimed to give a comprehensive summary of the physical and chemical properties of these interesting molecules, emphasizing their mechanism of action in relation to their different interactions with biomacromolecules, specifically with DNA. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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15 pages, 3245 KiB

Open AccessReview

Mitocanic Di- and Triterpenoid Rhodamine B Conjugates

by Sophie Hoenke, Immo Serbian, Hans-Peter Deigner and René Csuk

Molecules 2020, 25(22), 5443; https://doi.org/10.3390/molecules25225443 - 20 Nov 2020

Cited by 41 | Viewed by 4144

Abstract

The combination of the “correct” triterpenoid, the “correct” spacer and rhodamine B (RhoB) seems to be decisive for the ability of the conjugate to accumulate in mitochondria. So far, several triterpenoid rhodamine B conjugates have been prepared and screened for their [...] Read more.

The combination of the “correct” triterpenoid, the “correct” spacer and rhodamine B (RhoB) seems to be decisive for the ability of the conjugate to accumulate in mitochondria. So far, several triterpenoid rhodamine B conjugates have been prepared and screened for their cytotoxic activity. To obtain cytotoxic compounds with EC₅₀ values in a low nano-molar range combined with good tumor/non-tumor selectivity, the Rho B unit has to be attached via an amine spacer to the terpenoid skeleton. To avoid spirolactamization, secondary amines have to be used. First results indicate that a homopiperazinyl spacer is superior to a piperazinyl spacer. Hybrids derived from maslinic acid or tormentic acid are superior to those from oleanolic, ursolic, glycyrrhetinic or euscaphic acid. Thus, a tormentic acid-derived RhoB conjugate 32, holding a homopiperazinyl spacer can be regarded, at present, as the most promising candidate for further biological studies. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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22 pages, 2633 KiB

Open AccessReview

Role of Photoactive Phytocompounds in Photodynamic Therapy of Cancer

by Kasipandi Muniyandi, Blassan George, Thangaraj Parimelazhagan and Heidi Abrahamse

Molecules 2020, 25(18), 4102; https://doi.org/10.3390/molecules25184102 - 8 Sep 2020

Cited by 65 | Viewed by 5985

Abstract

Cancer is one of the greatest life-threatening diseases conventionally treated using chemo- and radio-therapy. Photodynamic therapy (PDT) is a promising approach to eradicate different types of cancers. PDT requires the administration of photosensitisers (PSs) and photoactivation using a specific wavelength of light in [...] Read more.

Cancer is one of the greatest life-threatening diseases conventionally treated using chemo- and radio-therapy. Photodynamic therapy (PDT) is a promising approach to eradicate different types of cancers. PDT requires the administration of photosensitisers (PSs) and photoactivation using a specific wavelength of light in the presence of molecular oxygen. This photoactivation exerts an anticancer effect via apoptosis, necrosis, and autophagy of cancer cells. Recently, various natural compounds that exhibit photosensitising potentials have been identified. Photoactive substances derived from medicinal plants have been found to be safe in comparison with synthetic compounds. Many articles have focused on PDT mechanisms and types of PSs, but limited attention has been paid to the phototoxic activities of phytocompounds. The reduced toxicity and side effects of natural compounds inspire the researchers to identify and use plant extracts or phytocompounds as a potent natural PS candidate for PDT. This review focusses on the importance of common photoactive groups (furanocoumarins, polyacetylenes, thiophenes, curcumins, alkaloids, and anthraquinones), their phototoxic effects, anticancer activity and use as a potent PS for an effective PDT outcome in the treatment of various cancers. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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33 pages, 1623 KiB

Open AccessReview

Bioactive Compounds and Metabolites from Grapes and Red Wine in Breast Cancer Chemoprevention and Therapy

by Danielly C. Ferraz da Costa, Luciana Pereira Rangel, Julia Quarti, Ronimara A. Santos, Jerson L. Silva and Eliane Fialho

Molecules 2020, 25(15), 3531; https://doi.org/10.3390/molecules25153531 - 1 Aug 2020

Cited by 42 | Viewed by 8721

Abstract

Phytochemicals and their metabolites are not considered essential nutrients in humans, although an increasing number of well-conducted studies are linking their higher intake with a lower incidence of non-communicable diseases, including cancer. This review summarizes the current findings concerning the molecular mechanisms of [...] Read more.

Phytochemicals and their metabolites are not considered essential nutrients in humans, although an increasing number of well-conducted studies are linking their higher intake with a lower incidence of non-communicable diseases, including cancer. This review summarizes the current findings concerning the molecular mechanisms of bioactive compounds from grapes and red wine and their metabolites on breast cancer—the most commonly occurring cancer in women—chemoprevention and treatment. Flavonoid compounds like flavonols, monomeric catechins, proanthocyanidins, anthocyanins, anthocyanidins and non-flavonoid phenolic compounds, such as resveratrol, as well as their metabolites, are discussed with respect to structure and metabolism/bioavailability. In addition, a broad discussion regarding in vitro, in vivo and clinical trials about the chemoprevention and therapy using these molecules is presented. Full article

(This article belongs to the Special Issue Anticancer Properties of Natural and Derivative Products)

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Anticancer Properties of Natural and Derivative Products

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