Plant foods are consumed worldwide due to their immense energy density and nutritive value. Their consumption has been following an increasing trend due to several metabolic disorders linked to non-vegetarian diets. In addition to their nutritive value, plant foods contain several bioactive constituents that have been shown to possess health-promoting properties. Plant-derived bioactive compounds, such as biologically active proteins, polyphenols, phytosterols, biogenic amines, carotenoids, etc., have been reported to be beneficial for human health, for instance in cases of cancer, cardiovascular diseases, and diabetes, as well as for people with gut, immune function, and neurodegenerative disorders. Previous studies have reported that bioactive components possess antioxidative, anti-inflammatory, and immunomodulatory properties, in addition to improving intestinal barrier functioning etc., which contribute to their ability to mitigate the pathological impact of various human diseases. This review describes the bioactive components derived from fruit, vegetables, cereals, and other plant sources with health promoting attributes, and the mechanisms responsible for the bioactive properties of some of these plant components. This review mainly compiles the potential of food derived bioactive compounds, providing information for researchers that may be valuable for devising future strategies such as choosing promising bioactive ingredients to make functional foods for various non-communicable disorders.

https://www.mdpi.com/2304-8158/10/4/839/pdf

Potential Health Benefits of Plant Food-Derived Bioactive Components: An Overview.

Flavonoids are some of the most precious phytochemicals, believed to be found largely in terrestrial plants. With the advancement of phytochemical research and marine bioprospecting, flavonoids have also been reported by the research of microalgae and macroalgae. High growth rate with minimal nutritional and growth requirement, saving arable land and rich metabolic profile make microalgae an excellent repertoire of novel anticancer compounds, such as flavonoids. In addition, marine algae, especially seaweeds contain different types of flavonoids which are assumed to have unique chemical structures and bioactivities than their terrestrial counterparts. Flavonoids are not only good antioxidants but also have the abilities to kill cancer cells by inducing apoptosis and autophagy. However, the study of the anticancer properties of flavonoids is largely limited to terrestrial plants. This review offers an insight into the distribution of different classes of flavonoids in eukaryotic microalgae, cyanobacteria and seaweeds with their possible anticancer activities. In addition, extraction and purification methods of these flavonoids have been highlighted. Finally, prospects and challenges to use algal flavonoids as anticancer agents have been discussed.

Insight into Potential Anticancer Activity of Algal Flavonoids: Current Status and Challenges.

Nicotinamide N-methyltransferase (NNMT) plays multiple roles in improving the aggressiveness of colorectal cancer (CRC) and enhancing resistance to 5-Fluorouracil (5-FU), making it an attractive therapeutic target. Curcumin (Cur) is a promising natural compound, exhibiting multiple antitumor effects and potentiating the effect of 5-FU. The aim of the present study is to explore the effect of Cur on attenuating NNMT-induced resistance to 5-FU in CRC. A panel of CRC cell lines with different NNMT expressions are used to characterize the effect of Cur. Herein, it is observed that Cur can depress the expression of NNMT and p-STAT3 in CRC cells. Furthermore, Cur can induce inhibition of cell proliferation, G2/M phase cell cycle arrest, and reactive oxygen species (ROS) generation, especially in high-NNMT-expression CRC cell lines. Cur can also re-sensitize high-NNMT-expression CRC cells to 5-FU both in vitro and in vivo. In summary, it is proposed that Cur can reverse NNMT-induced cell proliferation and 5-FU resistance through ROS generation and cell cycle arrest. Given that Cur has long been used, we suppose that Cur is a promising anticancer drug candidate with minimal side effects for human CRC therapy and can attenuate NNMT-induced resistance to 5-FU.

Curcumin Reverses NNMT-Induced 5-Fluorouracil Resistance via Increasing ROS and Cell Cycle Arrest in Colorectal Cancer Cells.

Melanoma represents one of the most aggressive and drug resistant skin cancers with poor prognosis in its advanced stages. Despite the increasing number of targeted therapies, novel approaches are needed to counteract both therapeutic resistance and the side effects of classic therapy. Betulinic acid (BA) is a bioactive phytocompound that has been reported to induce apoptosis in several types of cancers including melanomas; however, its effects on mitochondrial bioenergetics are less investigated. The present study performed in A375 human melanoma cells was aimed to characterize the effects of BA on mitochondrial bioenergetics and cellular behavior. BA demonstrated a dose-dependent inhibitory effect in both mitochondrial respiration and glycolysis in A375 melanoma cells and at sub-toxic concentrations (10 μM) induced mitochondrial dysfunction by eliciting a decrease in the mitochondrial membrane potential and changes in mitochondria morphology and localization. In addition, BA triggered a dose-dependent cytotoxic effect characterized by apoptotic features: morphological alterations (nuclear fragmentation, apoptotic bodies) and the upregulation of pro-apoptotic markers mRNA expression (Bax, Bad and Bak). BA represents a viable therapeutic option via a complex modulatory effect on mitochondrial metabolism that might be useful in advanced melanoma or as reliable strategy to counteract resistance to standard therapy.

https://www.mdpi.com/1422-0067/22/9/4870/pdf

Assessment of Betulinic Acid Cytotoxicity and Mitochondrial Metabolism Impairment in a Human Melanoma Cell Line.

Natural products play a critical role in the discovery and development of numerous drugs for the treatment of various types of cancer. These phytochemicals have demonstrated anti-carcinogenic properties by interfering with the initiation, development, and progression of cancer through altering various mechanisms such as cellular proliferation, differentiation, apoptosis, angiogenesis, and metastasis. Treating multifactorial diseases, such as cancer with agents targeting a single target, might lead to limited success and, in many cases, unsatisfactory outcomes. Various epidemiological studies have shown that the steady consumption of fruits and vegetables is intensely associated with a reduced risk of cancer. Since ancient period, plants, herbs, and other natural products have been used as healing agents. Likewise, most of the medicinal ingredients accessible today are originated from the natural resources. Regardless of achievements, developing bioactive compounds and drugs from natural products has remained challenging, in part because of the problem associated with large-scale sequestration and mechanistic understanding. With significant progress in the landscape of cancer therapy and the rising use of cutting-edge technologies, we may have come to a crossroads to review approaches to identify the potential natural products and investigate their therapeutic efficacy. In the present review, we summarize the recent developments in natural products-based cancer research and its application in generating novel systemic strategies with a focus on underlying molecular mechanisms in solid cancer.

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The Role of Natural Products and Their Multitargeted Approach to Treat Solid Cancer

Despite the recent advances in the field of chemically synthetized pharmaceutical agents, nature remains the main supplier of bioactive molecules. The research of natural products is a valuable approach for the discovery and development of novel biologically active compounds possessing unique structures and mechanisms of action. Although their use belongs to the traditional treatment regimes, plant-derived compounds still cover a large portion of the current-day pharmaceutical agents. Their medical importance is well recognized in the field of oncology, especially as an alternative to the limitations of conventional chemotherapy (severe side effects and inefficacy due to the occurrence of multi-drug resistance). This review offers a comprehensive perspective of the first blockbuster chemotherapeutic agents of natural origin's (e.g. taxol, vincristine, doxorubicin) mechanism of action using 3D representation. In addition is portrayed the step-by-step evolution from preclinical to clinical evaluation of the most recently studied natural compounds with potent antitumor activity (e.g. resveratrol, curcumin, betulinic acid, etc.) in terms of anticancer mechanisms of action and the possible indications as chemotherapeutic or chemopreventive agents and sensitizers. Finally, this review describes several efficient platforms for the encapsulation and targeted delivery of natural compounds in cancer treatment.

https://www.mdpi.com/1420-3049/26/4/1109/pdf

Plant-Derived Anticancer Compounds as New Perspectives in Drug Discovery and Alternative Therapy.

Magnetic iron oxide nanoparticles are the most desired nanomaterials for biomedical applications due to their unique physiochemical properties. A facile single-step process for the preparation of a highly stable and biocompatible magnetic colloidal suspension based on citric-acid-coated magnetic iron oxide nanoparticles used as an effective heating source for the hyperthermia treatment of cancer cells is presented. The physicochemical analysis revealed that the magnetic colloidal suspension had a z-average diameter of 72.7 nm at 25 °C with a polydispersity index of 0.179 and a zeta potential of −45.0 mV, superparamagnetic features, and a heating capacity that was quantified by an intrinsic loss power analysis. Raman spectroscopy showed the presence of magnetite and confirmed the presence of citric acid on the surfaces of the magnetic iron oxide nanoparticles. The biological results showed that breast adenocarcinoma cells (MDA-MB-231) were significantly affected after exposure to the magnetic colloidal suspension with a concentration of 30 µg/mL 24 h post-treatment under hyperthermic conditions, while the nontumorigenic (MCF-10A) cells exhibited a viability above 90% under the same thermal setup. Thus, the biological data obtained in the present study clearly endorse the need for further investigations to establish the clinical biological potential of synthesized magnetic colloidal suspension for magnetically triggered hyperthermia.

Biocompatible Magnetic Colloidal Suspension Used as a Tool for Localized Hyperthermia in Human Breast Adenocarcinoma Cells: Physicochemical Analysis and Complex In Vitro Biological Profile

Stela Iurciuc

Papers

Plant-Derived Anticancer Compounds as New Perspectives in Drug Discovery and Alternative Therapy.

Biocompatible Magnetic Colloidal Suspension Used as a Tool for Localized Hyperthermia in Human Breast Adenocarcinoma Cells: Physicochemical Analysis and Complex In Vitro Biological Profile