Dietary Phenolic Acids and Flavonoids as Potential Anti-Cancer Agents: Current State of the Art and Future Perspectives

2020 ◽  
Vol 20 (1) ◽  
pp. 29-48 ◽  
Author(s):  
Ramesh K. Bonta

Background: Cancer is a rapidly growing disease and the second most leading cause of death worldwide. Breast, colon, lung, and prostate cancer are the most diagnosed types of cancer among the majority of the population. The prevalence of these cancers is increasing rapidly due to the lack of effective drugs. The search for anti-cancer bioactive components from natural plant sources is gaining immense significance. The aim of the paper is to introduce the readers about the in vitro and in vivo biochemical mechanisms of phenolic acids and flavonoids in these four types of cancers. Methods: A literature search was carried out in databases, including Scopus, SciFinder, Springer, Science direct and Google. The main keywords used were fruits & vegetables, phenolic acids, flavonoids, anticancer, bioavailability, etc. The data obtained were integrated and analyzed. Results: The study revealed the potential molecular mechanisms of phenolic acids and flavonoids, which include the induction of apoptosis, inhibition of cell proliferation, cell-cycle arrest, induction of Poly ADP ribose polymerase cleavage, downregulation of Matrix metalloproteinases-2 and Matrix metalloproteinases-9 activities, decreased levels of B-cell lymphoma-2, etc. Promising effects of phenolic acids and flavonoids have been observed against breast, colon, lung and prostate cancers. Conclusion: The in vitro and in vivo anti-cancer mechanisms of phenolic acids and flavonoids have been revealed in this study. With the knowledge of specific molecular targets and the structural-functional relationship of bioactive compounds, the current review will open a new gateway for the scientific community and provide them a viable option to exploit more of these compounds for the development of novel and efficacious anticancer compounds.

2018 ◽  
Vol 18 (2) ◽  
pp. 156-165 ◽  
Author(s):  
Jiaqiang Wang ◽  
Chien-shan Cheng ◽  
Yan Lu ◽  
Xiaowei Ding ◽  
Minmin Zhu ◽  
...  

Background: Propofol, a widely used intravenous anesthetic agent, is traditionally applied for sedation and general anesthesia. Explanation: Recent attention has been drawn to explore the effect and mechanisms of propofol against cancer progression in vitro and in vivo. Specifically, the proliferation-inhibiting and apoptosis-inducing properties of propofol in cancer have been studied. However, the underlying mechanisms remain unclear. Conclusion: This review focused on the findings within the past ten years and aimed to provide a general overview of propofol's malignance-modulating properties and the potential molecular mechanisms.


Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 987
Author(s):  
Eric J. O’Neill ◽  
Deborah Termini ◽  
Alexandria Albano ◽  
Evangelia Tsiani

Cancer is a disease characterized by aberrant proliferative and apoptotic signaling pathways, leading to uncontrolled proliferation of cancer cells combined with enhanced survival and evasion of cell death. Current treatment strategies are sometimes ineffective in eradicating more aggressive, metastatic forms of cancer, indicating the need to develop novel therapeutics targeting signaling pathways which are essential for cancer progression. Historically, plant-derived compounds have been utilized in the production of pharmaceuticals and chemotherapeutic compounds for the treatment of cancer, including paclitaxel and docetaxel. Theaflavins, phenolic components present in black tea, have demonstrated anti-cancer potential in cell cultures in vitro and in animal studies in vivo. Theaflavins have been shown to inhibit proliferation, survival, and migration of many cancer cellswhile promoting apoptosis. Treatment with theaflavins has been associated with increased levels of cleaved poly (ADP-ribose) polymerase (PARP) and cleaved caspases-3, -7, -8, and -9, all markers of apoptosis, and increased expression of the proapoptotic marker Bcl-2-associated X protein (Bax) and concomitant reduction in the antiapoptotic marker B-cell lymphoma 2 (Bcl-2). Additionally, theaflavin treatment reduced phosphorylated Akt, phosphorylated mechanistic target of rapamycin (mTOR), phosphatidylinositol 3-kinase (PI3K), and c-Myc levels with increased expression of the tumour suppressor p53. This review summarizes the current in vitro and in vivo evidence available investigating the anti-cancer effects of theaflavins across various cancer cell lines and animal models.


Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 193 ◽  
Author(s):  
Yasuyoshi Miyata ◽  
Yohei Shida ◽  
Tomoaki Hakariya ◽  
Hideki Sakai

Prostate cancer is the most common cancer among men. Green tea consumption is reported to play an important role in the prevention of carcinogenesis in many types of malignancies, including prostate cancer; however, epidemiological studies show conflicting results regarding these anti-cancer effects. In recent years, in addition to prevention, many investigators have shown the efficacy and safety of green tea polyphenols and combination therapies with green tea extracts and anti-cancer agents in in vivo and in vitro studies. Furthermore, numerous studies have revealed the molecular mechanisms of the anti-cancer effects of green tea extracts. We believe that improved understanding of the detailed pathological roles at the molecular level is important to evaluate the prevention and treatment of prostate cancer. Therefore, in this review, we present current knowledge regarding the anti-cancer effects of green tea extracts in the prevention and treatment of prostate cancer, with a particular focus on the molecular mechanisms of action, such as influencing tumor growth, apoptosis, androgen receptor signaling, cell cycle, and various malignant behaviors. Finally, the future direction for the use of green tea extracts as treatment strategies in patients with prostate cancer is introduced.


2021 ◽  
Author(s):  
Le Ma ◽  
Qiang Gong ◽  
Zelin Chen ◽  
Yu Wang ◽  
Xu Tan ◽  
...  

Abstract Background: The MYC-expressing diffuse large B-cell lymphoma (DLBCL) is one of the refractory lymphomas. The pathogenesis of MYC-expressing DLBCL is still unclear, and there is a lack of effective therapy. In this study, we have explored the clinical significance and the molecular mechanisms of transcription co-activator 4 (PC4) in MYC-expressing DLBCL.Methods: We investigated PC4 expression in 54 cases of DLBCL patients’ tissues and matched normal specimens, and studied the molecular mechanisms of PC4 in MYC-expressing DLBCL both in vitro and in vivo.Results: We reported for the first time that targeting c-Myc could induce autophagic cell death in MYC-expressing DLBCL cell lines. We next characterized that PC4 was an upstream regulator of c-Myc, and PC4 was overexpressed in DLBCL and was closely related to clinical staging, prognosis and c-Myc expression. Further, our in vivo and in vitro studies revealed that PC4 knockdown could induce autophagic cell death of MYC-expressing DLBCL. And inhibition of c-Myc mediated aerobic glycolysis and activation of AMPK / mTOR signaling pathway were responsible for the autophagic cell death induced by PC4 knockdown in MYC-expressing DLBCL. Through the CHIP, DLRTM and EMSA assay, we also found that PC4 exerted its oncogenic functions by directly binding to c-Myc promoters.Conclusions: PC4 exerts its oncogenic functions by directly binding to c-Myc promoters. Inhibition of PC4 can induce autophagic cell death of MYC-expressing DLBCL. Our study provides novel insights into the functions and mechanisms of PC4 in MYC-expressing DLBCL, and suggests that PC4 might be a promising therapeutic target for MYC-expressing DLBCL.


Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4941
Author(s):  
Abdelwahab Khalil ◽  
Basem H. Elesawy ◽  
Tarek M. Ali ◽  
Osama M. Ahmed

Insects of the order Hymenoptera have a defensive substance that contains many biologically active compounds. Specifically, venom from honeybees (Apis mellifera) contains many enzymes and peptides that are effective against various diseases. Different research papers stated the possibility of using bee venom (a direct bee sting or in an injectable form) in treating several complications; either in vivo or in vitro. Other reports used the active fractions of bee venom clinically or at labratory scale. Many reports and publications have stated that bee venom and its constituents have multiple biological activities including anti-microbial, anti-protozoan, anti-cancer, anti-inflammatory, and anti-arthritic properties. The present review aims to refer to the use of bee venom itself or its fractions in treating several diseases and counteracting drug toxicities as an alternative protocol of therapy. The updated molecular mechanisms of actions of bee venom and its components are discussed in light of the previous updated publications. The review also summarizes the potential of venom loaded on nanoparticles as a drug delivery vehicle and its molecular mechanisms. Finally, the products of bee venom available in markets are also demonstrated.


2019 ◽  
Vol 20 (11) ◽  
pp. 2612 ◽  
Author(s):  
Chathurika D. B. Gamage ◽  
So-Yeon Park ◽  
Yi Yang ◽  
Rui Zhou ◽  
İsa Taş ◽  
...  

Deoxypodophyllotoxin (DPT) is a cyclolignan compound that exerts anti-cancer effects against various types of cancers. DPT induces apoptosis and inhibits the growth of breast, brain, prostate, gastric, lung, and cervical tumors. In this study, we sought to determine the effect of DPT on cell proliferation, apoptosis, motility, and tumorigenesis of three colorectal cancer (CRC) cell lines: HT29, DLD1, and Caco2. DPT inhibited the proliferation of these cells. Specifically, the compound-induced mitotic arrest in CRC cells by destabilizing microtubules and activating the mitochondrial apoptotic pathway via regulation of B-cell lymphoma 2 (Bcl-2) family proteins (increasing Bcl-2 associated X (BAX) and decreasing B-cell lymphoma-extra-large (Bcl-xL)) ultimately led to caspase-mediated apoptosis. In addition, DPT inhibited tumorigenesis in vitro, and in vivo skin xenograft experiments revealed that DPT significantly decreased tumor size and tumor weight. Taken together, our results suggest DPT to be a potent compound that is suitable for further exploration as a novel chemotherapeutic for human CRC.


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Devanesan Arul Ananth ◽  
Garlapati Deviram ◽  
Vijayaraghavan Mahalakshmi ◽  
V. Ratna Bharathi

Abstract Background Medicinal plants play a significant role in the progress of persuasive therapeutic agents. Earlier to the innovation of synthetic drugs, human beings completely relied on the plants for the treatment of various ailments. Natural product extracts, particularly those derived from different plant species, provided the main source of Siddha, Ayurveda and Folk medicines. P. daemia is a perennial climber, traditionally reported for the treatment in a variety of diseases. In present review, we focused on the present status of phytochemical and pharmacological activities P. daemia. Methodology With the support of electronic databases such as Science Direct, Google Scholar, Mendeley, Scirus and PubMed central. Traditional knowledge information collected by Indian taxonomical books, survey from local rural and tribal peoples. Pharmacological data’s obtained from scientific journals published from 2000 to 2020. Results P. daemia extract, contains several phytochemicals, especially rich in flavonoids. These secondary metabolites synthesized from P. daemia have been reported for the treatment of various chronic diseases. In recent years, P. daemia phytoconstituents set as a key role in natural drug development as it harbours many in vitro and in vivo pharmacological activities such as anti-inflammatory, anti-cancer, anti-fertility, anti-arthritic and antimicrobial etc., Conclusion P. daemia was the less studied plant compared to other medicinal plants. In this context more emphasis has to be laid on studies that discuss on the secondary metabolite activities and molecular mechanisms that work against various chronic diseases.


2021 ◽  
Vol 11 (23) ◽  
pp. 11288
Author(s):  
Mohammad Al Mijan ◽  
Woo-Jin Sim ◽  
Tae-Gyu Lim

Green-colored foods, such as broccoli, sprouts, soybean, and green leafy vegetables are considered one of the representative healthy foods for containing various functional ingredients that can combat chronic diseases, including diabetes, obesity, and cancer. Herein, we reviewed the anti-cancer activities and the underlying mechanisms of some important bioactive compounds, such as sulforaphane, catechins, chlorophyll, isoflavone, indole dervatives, and lutein, present in green-colored foods. In vivo and clinical studies suggest that sulforaphane, a sulfur-containing compound found in cruciferous vegetables, can ameliorate prostate and breast cancer symptoms by arresting cell-cycle progression and modulating Ki67 and HDAC expression. A green tea compound, known as epigallocatechin-3-gallate (EGCG), has shown remarkable anti-cancer effects against prostate cancer and lung adenocarcinoma in human trials through its antioxidative defense and immunomodulatory functions. Chlorophyll, a natural pigment found in all green plants, can regulate multiple cancer-related genes, including cyclin D1, CYP1A, CYP1B1, and p53. Epidemiological studies indicate that chlorophyll can substantially reduce aflatoxin level and can mitigate colon cancer in human subjects. Remarkably, the consumption of soy isoflavone has been found to be associated with the lower incidence and mortality of breast and prostate cancers in East Asia and in Canada. In vivo and in vitro data point out that isoflavone has modulatory effects on estrogen and androgen signaling pathways and the expression of MAPK, NfκB, Bcl-2, and PI3K/AKT in different cancer models. Other green food bioactive compounds, such as indole derivatives and lutein, also exhibited suppressing effects in rodent models of lung, liver, stomach, cervical, and prostate cancers. In addition, some micronutrients, such as folate, riboflavin, retinoic acid, and vitamin D3 present in green foods, also showed potential cancer suppressing effects. Taken together, these data suggest potential chemopreventive functions of the bioactive compounds from green-colored foods. This paper could be beneficial for further research on the anti-carcinogenic effects of green-colored food-derived compounds, in order to develop green chemotherapeutics for cancers.


2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Ye Xiong ◽  
Jianrong Huang

AbstractArtemisinin and its derivatives belong to a family of drugs approved for the treatment of malaria with known clinical safety and efficacy. In addition to its anti-malarial effect, artemisinin displays anti-viral, anti-inflammatory, and anti-cancer effects in vivo and in vitro. Recently, much attention has been paid to the therapeutic role of artemisinin in liver diseases. Several studies suggest that artemisinin and its derivatives can protect the liver through different mechanisms, such as those pertaining to inflammation, proliferation, invasion, metastasis, and induction of apoptosis and autophagy. In this review, we provide a comprehensive discussion of the underlying molecular mechanisms and signaling pathways of artemisinin and its derivatives in treating liver diseases. Further pharmacological research will aid in determining whether artemisinin and its derivatives may serve as promising medicines for the treatment of liver diseases in the future.


2020 ◽  
Author(s):  
Bing Wei ◽  
Shangli Yao ◽  
Ming Gao ◽  
Zujun Wang ◽  
Wenyan Wang ◽  
...  

Abstract Resveratrol (RES), a natural compound found in red wine, has previously reported to suppress ovarian cancer (OC) cell growth in vitro and in vivo; however, its potential molecular mechanisms are not fully elucidated. The aim of this study is to investigate the suppressive potential of RES in OC cell growth and invasion and reveal the underlying mechanisms. Herein, we found that RES treatment obviously suppressed the proliferative and invasive capacities of OC cells, and elevated cell apoptosis in vitro. Subsequent microarray and qRT-PCR analysis further showed that microRNA-34a (miR-34a) was significantly increased by RES treatment. Moreover, the inhibitory effects of RES on OC cells were enhanced by miR-34a overexpression, whereas weakened by miR-34a inhibition in OC cells. Of note, Bcl-2, an anti-apoptotic gene, was identified as a direct target of miR-34a. Then, we revealed that RES decreased the expression of Bcl-2 in OC cells in a dose dependent manner. Furthermore, the anti-tumor effects of RES were abolished by overexpression of Bcl-2 in OC cells. Overall, these results demonstrated that RES exerts the anti-cancer effects on OC cells through the miR-34a/Bcl-2 axis.


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