Role of natural compounds as anti anti-cancer agents
Closes 10 May, 2024
Issue Pre-order formJournal: Anti-Cancer Agents in Medicinal Chemistry
Guest editor(s):Dr. Giovanni Tossetta
Introduction
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though intrinsic or acquired resistance and metastasis are still major obstacles to a successful cure. However, outstanding progress in genetics and molecular biology has prompted the discovery of novel molecular targets an and new anticancer agents. Moreover, many studies suggested that cotreatment with natural compounds can increase the efficiency of chemotherapeutics or reduce/eliminate the side effects of these drugs. Importantly, it has been suggested that several natural compounds may prevent cancer onset. Despite the vast number of compounds that have reached the stage of preclinical and clinical studies, the research and development of new anticancer agents and therapeutic strategies must be an everlasting process and constitutes the main subject of this Special Issue.
Keywords
Chemoresistance, Radioresistance, Cancer, Natural, Compounds, Anti-cancer, Cancer progression
Advancing Therapeutic Frontiers in Breast Cancer Management: The Rising Significance of Flavonoids
Author(s): Supriya Mishra, Kamini Bhardwaj, Lubhan Singh, Faheem Hyder Pottoo and Mohd Yasir*
Abstract
Breast cancer is the leading cause of oncologic morbidity and mortality among women worldwide. According to the World Health Organization, there would be around 27 million cases until the year 2050. Mammograms, a specialized X-ray scan made to closely examine breast tissue, are frequently used to diagnose breast cancer. The rate of breast cancer increases with age, however, it slows down once women reach menopause. Several studies have suggested that estrogen is closely associated with the pathological process of breast cancer. Anthracyclines are one the most effective drugs as well as taxanes, paclitaxel, and docetaxel. Flavonoids, a type of plant polyphenol, have emerged as effective tools for breast cancer prevention and treatment. Flavonoids have an impact on the epigenetic mechanism in breast cancer, with studies showing that genistein, resveratrol, and epigallocatechin gallate all block DNA methyl-transferase and affect chromatin alteration in breast cancer. Flavonoids have also been discovered to competitively inhibit drug transporters such as the P-glycoprotein (P-gp), breast cancer receptor protein (BCRP) as well as multidrug resistance-associated proteins (MRP1 and MRP2). The association of flavonoids' various functional moieties with cyclin-dependent kinases is responsible for flavonoids' capacity to produce cell cycle arrest. The present review aimed to explore the existing targeted drug therapy and the role of flavonoids in breast cancer treatment along with the future prospective of flavonoids in breast cancer.
Curcumin and its analogues in oral squamous cell carcinoma: state-of-art and therapeutic potential
Author(s): Valentina Schiavoni , Monica Emanuelli, Davide Sartini, Eleonora Salvolini*, Valentina Pozzi and Roberto Campagna
Abstract
Abstract: Oral squamous cell carcinoma (OSCC) is the most common cancer arising from squamous epithelium in the oral cavity and is characterized by high aggressiveness and metastatic potential which, together with a late diagnosis, results in a 5-years survival rate of only 50% of patients. The therapeutic options for the OSCC management are limited and largely influenced by the cancer stage. While radical surgery can be curative in early stage of disease, most of cases require adjuvant therapies, including chemotherapy and radiotherapy which, however, often achieve poor curative rates and are associated with important negative effects. Therefore, there is an urgent need to discover new alternative treatment strategies to improve patients’ outcome. Several medicinal herbs are being studied for their preventive or therapeutic effect in several diseases, including cancer. In particular, the Indian spice Curcumin, largely used in oriental countries, has been studied as chemopreventive or adjuvant agent in different malignancies. Indeed, Curcumin is characterized by important biological properties, among which antioxidant, anti-inflammatory and anticancer effects, that could be exploited also in OSCC. However, due to its limited bioavailability and poor aqueous solubility, the research is also focused on designing new synthetic analogues and on developing novel types of curcumin delivery systems to improve its pharmacokinetic and biological properties. Thus, the aim of this review is to analyse the potential therapeutic role of curcumin in OSCC, by reporting an overview of current in vitro and in vivo studies demonstrating the beneficial effects of curcumin and its analogues in OSCC.
Molecular targets of plant-based alkaloids and polyphenolics in liver and breast cancer- An insight into anticancer drug development
Author(s): Salma Batool*, Laiba Asim, Fawad Raffaq Qureshi, Ammara Masood, Rahman Shah Zaib Saleem and Maria Mushtaq
Abstract
Liver and Breast cancer are ranked as the most prevailing cancers that cause high cancer-related mortality. As cancer is a life-threatening disease that effects the human population globally, there is a need to develop novel therapies. Among the available treatment options include radiotherapy, chemotherapy, surgery, and immunotherapy. The most superlative modern method is the use of plant-derived anticancer drugs that target the cancerous cells and inhibit their proliferation. Plant-derived compounds are generally considered safer than synthetic drugs/traditional therapies and could serve as potential novel targets to treat liver and breast cancer to revolutionize cancer treatment. Alkaloids and Polyphenols have been shown to act as anti-cancer agents through molecular approaches. They disrupt various cellular mechanisms, inhibit the production of cyclins and CDKs to arrest cell cycle, activate DNA repairing mechanism by up-regulating p53, p21 and p38 expression. In severe cases, when no repair is possible, they induce apoptosis in liver and breast cancer cells by activating caspase-3, 8 and 9 as well as increasing Bax/Bcl-2 ratio. They also deactivate several signaling pathways such as PI3K/AKT/mTOR, STAT3, NF-kB, Shh, MAPK/ERK and Wnt/β-catenin pathways to control cancer cell progression and metastasis. The highlights of this review are the regulation of specific proteins expression that are crucial in cancer such as in HER2 over-expressing breast cancer cells, alkaloids and polyphenols have been reported to reduce HER2 as well as MMPs expression. In this study, above 40 of the plant-based alkaloids and polyphenols with specific molecular targets against liver and breast cancer have been reviewed. As a lot of research is there on anticancer compounds, there is desideratum to compile data to move towards clinical trials and control the prevalence of liver and breast cancer
Urea and thiourea derivatives of salinomycin as agents targeting malignant colon cancer cells
Author(s): Michał Antoszczak*, Magdalena Mielczarek-Puta, Marta Struga and Adam Huczyński
Abstract
Background: A natural polyether ionophore salinomycin (SAL) has been capturing much attention of the scientific community since nearly a decade ago, when its selective inhibitory activity towards human cancer cells was disclosed. Objective: Thus, a very interesting research direction is the chemical modification of SAL structure, which could give more biologically active agents. Methods: We evaluated here the anticancer activity of a series of urea and thiourea derivatives of C20-epi-aminosalinomycin (compound 3b). These studies included the in vitro cytotoxic activity, proapoptotic activity, production of reactive oxygen species (ROS) and lipid peroxidation. Results: Thioureas 5a‒5d showed antiproliferative activity against human colon cancer cell lines greater than that of chemically unmodified SAL, with a 2~10-fold higher potency towards a metastatic variant of colon cancer cells (SW620). Mechanistically, SAL derivatives showed pro-apoptotic activity in primary colon cancer cells and induced the production of reactive oxygen species (ROS) in these cells. In SW620 cells, SAL derivatives increased lipid peroxidation with a weak effect on apoptosis and low ROS formation with cytotoxic effects followed by cytostatic ones, suggesting different modes of action of the compounds against primary and metastatic colon cancer cells. Conclusion: The results of this study suggest that urea and thiourea derivatives of SAL provide promising leads for the rational development of new anticancer active agents.
Potential Anticancer Leads of Natural Origin
Author(s): Rajwinder Kaur, Rajwinder Kaur, Damanpreet Kaur Lang, Diksha Choudhary, Ujjwal Kaushik, Ankita Sood, Balakumar Chandrasekaran*, Rashmi Arora and Nidhi Rani
Abstract
Abstract: Background: This review gives an unmet demand for the exploration of medicines from herbal resources, specified herbal medicinal products, and purified phytoconstituents to be used in research, development, and implementation of therapies against cancer. Objective: This study aimed to provide an insight into anticancer molecules form the natural origin. Methods: A systematic literature search was performed primarily involving impactful databases such as Google Scholar, Embase, Scopus, and Pubmed for the identification of appropriate data. A search was conducted using varied keywords such as “cancer”, “natural leads”, “herbal products”, “nutraceuticals” and “anti-cancer alkaloids”. The in vitro study reports were also taken into account. Moreover, research papers and review articles, clinical trial reports, and patents were sorted out by reviewing abstracts and scrutinizing corresponding reference lists. Results: Besides other natural lead compounds, an account of phytochemicals employed as potential anticancer agents was also compiled in this manuscript. Conclusion:The current review will explore and highlight the in-depth and updated information on the various natural herbal-based lead molecules in cancer treatment.
Interaction Studies of Natural Compounds derived from Inula Viscosa and Synthetic to Anti-inflammatory and breast cancer Targets a Molecular Docking Analysis
Author(s): Amina GHOMRI*, Houari Bendriss, Mohamed Benbouali and Noureddine Missoum
Abstract
Novel compounds with significant medicinal properties have gained much interest in therapeutic approaches for treating various inflammatory disorders and breast cancer. Different synthetic and natural product inhibitors were collected from the literature and docked against (5-LOX, PLA2, Aromatase, mTOR) receptors. The compounds binding affinity were calculated after minimising the interaction within the binding pockets of the macromolecules (5-LOX, PLA2, Aromatase, mTOR) receptors. In the work we use molecular docking methods to identify the ligand which has the best interaction energy with the forth macromolecules among synthetic and natural products extracted from Inula Viscosa and also descript binding affinity in purpose to design new inhibitor ligands. The result shows that ligands (Sulfasalazine 3-O-Acetylpadmatin), (3-Acetyl-7-O-methylaromadendrin, Silibinin), (Nepetin, OSI-027) and (3-O-Methylquercetin, Formestane) best inhibited 5-LOX, PLA2, Aromatase, mTOR respectively. This latter leads to same conclusion with experimentation inhibition study.