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Therapeutic Effects of Plant Based Bioactive Compounds on Cancer

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 19645

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Special Issue Editors

Prof. Dr. Doo Hwan Kim

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Guest Editor

Department Horticultural Sciences/Molecular Biotechnology, Konkuk University, Seoul, Korea
Interests: food chemistry; phytomedicine; nanotechnology; antioxidants; antioxidant activity; flavonoids; medicinal plants; bioactivity
Special Issues, Collections and Topics in MDPI journals

Dr. Shivraj Hariram Nile

E-Mail Website
Guest Editor

Department of Bio-Resources and Food Science, Konkuk University, Seoul 143701, Korea
Interests: medicinal plants; antioxidants; flavonoids
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is a world health issue, affecting and leading to mortality in all communities around the globe, with a considerable social impact and high socio-economic costs. In recent decades, medicinal plants have been considered as an important source of bioactive compounds, predominating in the treatment of various diseases including cancer, oxidative stress, cardiovascular diseases and inflammation. Phytochemicals, mainly phenolics and flavonoids, are ubiquitously present in medicinal plants, plant-based foods and natural health products. Scientific evidence has strongly shown that regular intake of these natural plant bioactive compounds, especially flavonoids and phenolics, helps to reduce the risk of the generation of free radicals, oxidative-stress, and chronic inflammation-mediated pathogenesis of human diseases, such as certain cancers and inflammatory disorders. The significant effects of plant-based bioactive compounds, especially phenolics and flavonoids, are mainly documented in the context of oxidative-stress-related diseases (such as cancer, cardiovascular diseases and neurological diseases). The pro-oxidative activity of these bioactive compounds may be beneficial because it may induce the pooling of antioxidant enzymes, thus showing preventive effects in a variety of health problems. The physiological benefits of bioactive flavonoids and phenolics have been demonstrated to have multiple mechanisms of action, including regulating redox homeostasis, epigenetic regulations, the activation of survival genes, apoptotic effects, the suppression of oncogenes, and regulating signaling pathways, and the modulation of inflammation response.

Therefore, this Special Issue is dedicated to original research articles which cover the latest findings on the role of plant-based bioactive compounds, especially flavonoids phenolics and related phytochemicals, in the prevention and treatment of cancer, oxidative stress and inflammation. Other plant-based bioactive compounds included should be those whose chemical structures have been revealed chemically. In this Issue, research on plant extracts with unknown compositions is not welcomed. Papers published in IJMS are encouraged to include results at a molecular level, i.e., extracted and charactrised bioactive compounds showing a functional activity relatinship for the treatment of cancer and related diseases.

Authors are mainly invited to submit original articles, short communications and reviews related to the mentioned topics, comprehensively exploring and summarizing the effect of flavonoids, polyphenols and other related plant bioactive metabolites on cancer and cytotoxicity.

Prof. Dr. Doo Hwan Kim
Dr. Shivraj Hariram Nile
Guest Editors

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 submissions that pass pre-check are 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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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
polyphenolics
flavonoids
phenolics
terpenoids
carotenoids
cytotoxicity
functional foods
signaling mechanism
cell cycle
apoptosis

Published Papers (6 papers)

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Research

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28 pages, 3496 KiB

Open AccessArticle

Acetylenic Synthetic Betulin Derivatives Inhibit Akt and Erk Kinases Activity, Trigger Apoptosis and Suppress Proliferation of Neuroblastoma and Rhabdomyosarcoma Cell Lines

by Sylwia K. Król, Ewa Bębenek, Magdalena Dmoszyńska-Graniczka, Adrianna Sławińska-Brych, Stanisław Boryczka and Andrzej Stepulak

Int. J. Mol. Sci. 2021, 22(22), 12299; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222212299 - 14 Nov 2021

Cited by 3 | Viewed by 2002

Abstract

Neuroblastoma (NB) and rhabdomyosarcoma (RMS), the most common pediatric extracranial solid tumors, still represent an important clinical challenge since no effective treatment is available for metastatic and recurrent disease. Hence, there is an urgent need for the development of new chemotherapeutics to improve the outcome of patients. Betulin (Bet), a triterpenoid from the bark of birches, demonstrated interesting anti-cancer potential. The modification of natural phytochemicals with evidenced anti-tumor activity, including Bet, is one of the methods of receiving new compounds for potential implementation in oncological treatment. Here, we showed that two acetylenic synthetic Bet derivatives (ASBDs), EB5 and EB25/1, reduced the viability and proliferation of SK-N-AS and TE671 cells, as measured by MTT and BrdU tests, respectively. Moreover, ASBDs were also more cytotoxic than temozolomide (TMZ) and cisplatin (cis-diaminedichloroplatinum [II], CDDP) in vitro, and the combination of EB5 with CDDP enhanced anti-cancer effects. We also showed the slowdown of cell cycle progression at S/G₂ phases mediated by EB5 using FACS flow cytometry. The decreased viability and proliferation of pediatric cancers cells after treatment with ASBDs was linked to the reduced activity of kinases Akt, Erk1/2 and p38 and the induction of apoptosis, as investigated using Western blotting and FACS. In addition, in silico analyses of the ADMET profile found EB5 to be a promising anti-cancer drug candidate that would benefit from further investigation. Full article

(This article belongs to the Special Issue Therapeutic Effects of Plant Based Bioactive Compounds on Cancer)

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16 pages, 3221 KiB

Open AccessArticle

Quercetin-3-Glucoside Extracted from Apple Pomace Induces Cell Cycle Arrest and Apoptosis by Increasing Intracellular ROS Levels

by Arti Nile, Shivraj Hariram Nile, Juhyun Shin, Gyunseok Park and Jae-Wook Oh

Int. J. Mol. Sci. 2021, 22(19), 10749; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms221910749 - 04 Oct 2021

Cited by 15 | Viewed by 2726

Abstract

Cervical cancer is a life-threatening disease and the fourth most common cancer among women worldwide. Apple pomace is a multifunctional phenolic compound possessing effective biological activity against cervical cancer cells. This study aimed to investigate the anticancer effects of quercetin-3-glucoside (Q3G) extracted from apple pomace in HeLa cell lines and analyze its molecular mechanisms. High-performance liquid chromatography revealed that Q3G, coumaric acid, phloridzin, quercetin, and phloretin are the major polyphenolic compounds constituting apple pomace. Among them, Q3G possessed the greatest antioxidant and anti-inflammatory effects in vitro and exhibited significant cytotoxic effects in HeLa cells in a dose-and time-dependent manner. Flow cytometric analysis indicated that Q3G induced cell cycle arrest at the S phase in a time-dependent manner by altering cyclin-dependent kinase 2. Moreover, it induced apoptosis via chromosomal DNA degradation and increased reactive oxygen species generation. Furthermore, Q3G treatment altered the apoptosis-associated protein expression in the cells by activating caspase-9/-3, downregulating anti-apoptosis protein B-cell lymphoma (Bcl)-2 expressions and up regulating the pro-apoptotic Bcl-2-associated X protein. BH3-interacting domain death agonist cleavage occurred prior to the degradation of an anti-apoptotic Mu-2-related death-inducing gene involved in cell death signaling. Consequently, apple pomace Q3G holds promise as an anti-inflammatory and anticancer agent for treating cervical cancer. Full article

(This article belongs to the Special Issue Therapeutic Effects of Plant Based Bioactive Compounds on Cancer)

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Graphical abstract

18 pages, 3354 KiB

Open AccessArticle

Comparative Analysis of Phenolic Composition of Six Commercially Available Chamomile (Matricaria chamomilla L.) Extracts: Potential Biological Implications

by Maria Valeria Catani, Federica Rinaldi, Valentina Tullio, Valeria Gasperi and Isabella Savini

Int. J. Mol. Sci. 2021, 22(19), 10601; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms221910601 - 30 Sep 2021

Cited by 19 | Viewed by 2979

Abstract

Several phytochemical-containing herbal extracts are increasingly marketed as health-promoting products. In particular, chamomile (Matricaria recutita L.) is well known for its anti-inflammatory, analgesic, and antitumor properties. Here, we evaluated differences in chemical composition among six commercially available products and their potential impact on biological activity in human immortalized colonocytes. Our investigation encompassed: (i) preparation of dry extracts and yield evaluation; (ii) qualitative and quantitative analysis of phenol content; (iii) modulation of redox state; and (iv) bioavailability of main bioactive compounds. We demonstrated that apparently identical products showed huge heterogeneity, in terms of yield extraction, chemical composition, and antioxidant effects. All samples contained high amounts of flavonoids and cinnamic acid derivatives, but differentially concentrated in the six extracts. Depending on polyphenol content, chamomile samples possessed variable antioxidant potential, in terms of decreased radical generation and increased reduced glutathione levels. The observed effects might be ascribed to flavones (apigenin, luteolin, and their glycones) highly represented in the six extracts. Nonetheless, chamomile extracts exerted cytotoxic effects at high concentrations, suggesting that a herbal medicine is not always safe. In conclusion, due to the complexity and variability of plant matrices, studies evaluating effectiveness of chamomile should always be accompanied by preliminary characterization of phytochemical composition. Full article

(This article belongs to the Special Issue Therapeutic Effects of Plant Based Bioactive Compounds on Cancer)

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15 pages, 3560 KiB

Open AccessArticle

Polyphenol Containing Sorghum Brans Exhibit an Anti-Cancer Effect in Apc Min/+ Mice Treated with Dextran Sodium Sulfate

by Seong-Ho Lee, Hee-Seop Lee, Jihye Lee, Darshika Amarakoon, Zhiyuan Lou, Leela E. Noronha, Thomas J. Herald, Ramasamy Perumal and Dmitriy Smolensky

Int. J. Mol. Sci. 2021, 22(15), 8286; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22158286 - 01 Aug 2021

Cited by 13 | Viewed by 2639

Abstract

Colon cancer (CC) is considered a high-risk cancer in developed countries. Its etiology is correlated with a high consumption of red meat and low consumption of plant-based foods, including whole grains. Sorghum bran is rich in polyphenols. This study aimed to determine whether different high-phenolic sorghum brans suppress tumor formation in a genetic CC rodent model and elucidate mechanisms. Tissue culture experiments used colorectal cancer cell lines SW480, HCT-116 and Caco-2 and measured protein expression, and protein activity. The animal model used in this study was APC Min+/mouse model combined with dextram sodium sulfate. High phenolic sorghum bran extract treatment resulted in the inhibition of proliferation and induced apoptosis in CC cell lines. Treatment with high phenolic sorghum bran extracts repressed TNF-α-stimulated NF-κB transactivation and IGF-1-stimulated PI3K/AKT pathway via the downregulation of β-catenin transactivation. Furthermore, high-phenolic sorghum bran extracts activated AMPK and autophagy. Feeding with high-phenolic sorghum bran for 6 weeks significantly suppressed tumor formation in an APC Min/+ dextran sodium sulfate promoted CC mouse model. Our data demonstrates the potential application of high-phenolic sorghum bran as a functional food for the prevention of CC. Full article

(This article belongs to the Special Issue Therapeutic Effects of Plant Based Bioactive Compounds on Cancer)

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15 pages, 5375 KiB

Open AccessArticle

Ampelopsin Inhibits Cell Proliferation and Induces Apoptosis in HL60 and K562 Leukemia Cells by Downregulating AKT and NF-κB Signaling Pathways

by Jang Mi Han, Hong Lae Kim and Hye Jin Jung

Int. J. Mol. Sci. 2021, 22(8), 4265; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22084265 - 20 Apr 2021

Cited by 14 | Viewed by 2791

Abstract

Leukemia is a type of blood cancer caused by the rapid proliferation of abnormal white blood cells. Currently, several treatment options, including chemotherapy, radiation therapy, and bone marrow transplantation, are used to treat leukemia, but the morbidity and mortality rates of patients with leukemia are still high. Therefore, there is still a need to develop more selective and less toxic drugs for the effective treatment of leukemia. Ampelopsin, also known as dihydromyricetin, is a plant-derived flavonoid that possesses multiple pharmacological functions, including antibacterial, anti-inflammatory, antioxidative, antiangiogenic, and anticancer activities. However, the anticancer effect and mechanism of action of ampelopsin in leukemia remain unclear. In this study, we evaluated the antileukemic effect of ampelopsin against acute promyelocytic HL60 and chronic myelogenous K562 leukemia cells. Ampelopsin significantly inhibited the proliferation of both leukemia cell lines at concentrations that did not affect normal cell viability. Ampelopsin induced cell cycle arrest at the sub-G1 phase in HL60 cells but the S phase in K562 cells. In addition, ampelopsin regulated the expression of cyclins, cyclin-dependent kinases (CDKs), and CDK inhibitors differently in each leukemia cell. Ampelopsin also induced apoptosis in both leukemia cell lines through nuclear condensation, loss of mitochondrial membrane potential, increase in reactive oxygen species (ROS) generation, activation of caspase-9, caspase-3, and poly ADP-ribose polymerase (PARP), and regulation of Bcl-2 family members. Furthermore, the antileukemic effect of ampelopsin was associated with the downregulation of AKT and NF-κB signaling pathways. Moreover, ampelopsin suppressed the expression levels of leukemia stemness markers, such as Oct4, Sox2, CD44, and CD133. Taken together, our findings suggest that ampelopsin may be an attractive chemotherapeutic agent against leukemia. Full article

(This article belongs to the Special Issue Therapeutic Effects of Plant Based Bioactive Compounds on Cancer)

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Review

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58 pages, 6771 KiB

Open AccessReview

Natural Cyclopeptides as Anticancer Agents in the Last 20 Years

by Jia-Nan Zhang, Yi-Xuan Xia and Hong-Jie Zhang

Int. J. Mol. Sci. 2021, 22(8), 3973; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22083973 - 12 Apr 2021

Cited by 23 | Viewed by 4751

Abstract

Cyclopeptides or cyclic peptides are polypeptides formed by ring closing of terminal amino acids. A large number of natural cyclopeptides have been reported to be highly effective against different cancer cells, some of which are renowned for their clinical uses. Compared to linear peptides, cyclopeptides have absolute advantages of structural rigidity, biochemical stability, binding affinity as well as membrane permeability, which contribute greatly to their anticancer potency. Therefore, the discovery and development of natural cyclopeptides as anticancer agents remains attractive to academic researchers and pharmaceutical companies. Herein, we provide an overview of anticancer cyclopeptides that were discovered in the past 20 years. The present review mainly focuses on the anticancer efficacies, mechanisms of action and chemical structures of cyclopeptides with natural origins. Additionally, studies of the structure–activity relationship, total synthetic strategies as well as bioactivities of natural cyclopeptides are also included in this article. In conclusion, due to their characteristic structural features, natural cyclopeptides have great potential to be developed as anticancer agents. Indeed, they can also serve as excellent scaffolds for the synthesis of novel derivatives for combating cancerous pathologies. Full article

(This article belongs to the Special Issue Therapeutic Effects of Plant Based Bioactive Compounds on Cancer)

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