Anticancer Research Research Articles

Colony-Forming and Cell Viability Assay to Assess Nanotoxicity of Maleic Acid and N-vinyl Caprolactam-Based Nanoarchitectures

Abstract Organo-montmorillonite (Org-MMT) is a widely used silicate in polymer nanotechnology, enhancing the durability of nanocomposites by improving polymer strength and thermal stability. This study evaluates the anticancer effects of poly(maleic anhydride-alt-N-vinyl caprolactam) [poly(MA-alt-VCL)]-Org-MMT nanocomposites synthesized with varying clay concentrations. The cytotoxicity of Org-MMT, poly(MA-alt-VCL), and their nanocomposites were tested on HeLa (cervical carcinoma), A549 (lung cancer), and HDF (human dermal fibroblast) cells using MTT and colony formation assays. Our results indicate that cell viability is significantly inhibited in both cancer cell types with an IC50 value of 2 mg/mL especially in A549 cells, while 10 mg/mL in HDF cells. Nanocomposites significantly inhibited colony formation in both cancer cell lines, particularly in the HeLa cell line. The data indicated an inverse correlation between clay content in the copolymer complex and cell viability. The copolymer complex without clay had no negative impact on the cells. These findings suggest organo-clay nanocomposites as promising candidates for anticancer drug research.

Progress in the discovery and development of anticancer agents from marine cyanobacteria.

Covering 2010-April 2024There have been tremendous new discoveries and developments since 2010 in anticancer research based on marine cyanobacteria. Marine cyanobacteria are prolific sources of anticancer natural products, including the tubulin agents dolastatins 10 and 15 which were originally isolated from a mollusk that feeds on cyanobacteria. Decades of research have culminated in the approval of six antibody-drug conjugates (ADCs) and many ongoing clinical trials. Antibody conjugation has been enabling for several natural products, particularly cyanobacterial cytotoxins. Targeting tubulin dynamics has been a major strategy, leading to the discovery of the gatorbulin scaffold, acting on a new pharmacological site. Cyanobacterial compounds with different mechanisms of action (MOA), targeting novel or validated targets in a range of organelles, also show promise as anticancer agents. Important advances include the development of compounds with novel MOA, including apratoxin and coibamide A analogues, modulating cotranslational translocation at the level of Sec61 in the endoplasmic reticulum, largazole and santacruzamate A targeting class I histone deacetylases, and proteasome inhibitors based on carmaphycins, resembling the approved drug carfilzomib. The pipeline extends with SERCA inhibitors, mitochondrial cytotoxins and membrane-targeting agents, which have not yet advanced clinically since the biology is less understood and selectivity concerns remain to be addressed. In addition, efforts have also focused on the identification of chemosensitizing and antimetastatic agents. The review covers the state of current knowledge of marine cyanobacteria as anticancer agents with a focus on the mechanism, target identification and potential for drug development. We highlight the importance of solving the supply problem through chemical synthesis as well as illuminating the biological activity and in-depth mechanistic studies to increase the value of cyanobacterial natural products to catalyze their development.

Punica granatum L. Peel: Anticancer Activity on Hep3B, Drug‐likeness, ADMET Prediction, and Molecular Docking with EGFR‐TK

AbstractThe side effects of the cancer treatment medications that have sparked renewed interest in herbal formulation research. Due to its high phytochemical content, Punica granatum L. (different parts of pomegranate), a basic traditional medicine source, is an excellent option for the anticancer research. In this study, the anticancer activity of Punica granatum L. (Hicaz variety) peel extract on the Hep3B cell line was determined by the MTT test. The results showed that P. granatum L. peel extract showed a cytotoxic effect on the Hep3B cell line (cancer) but no effect on the AML12 cell line (healthy). To explain the anticancer effect, the main bioactive components of P. granatum L. peel, which are ellagic acid, abscisic acid, ethyl gallate, phlorizin, gallic acid, and myricetin, were performed in a docking study with the EGFR‐TK (PDB ID: 1M17). The docking poses showed that all selected compounds that bind to the same site as the EGFR‐TK inhibitor erlotinib, while ellagic acid (−8.8 kcal/mol), myricetin (−8.9 kcal/mol), and phlorizin (−8.7 kcal/mol) have lower binding energy. Also, drug similarity, physicochemical, and ADMET properties of these selected phenolic compounds were evaluated. All results indicated that P. granatum L. peel could be a potential therapeutic candidate against liver cancer.

Targeting MAO-B with Small-Molecule Inhibitors: A Decade of Advances in Anticancer Research (2012-2024).

Monoamine oxidase B (MAO-B) is a key enzyme in the mitochondrial outer membrane, pivotal for the oxidative deamination of biogenic amines. Its overexpression has been implicated in the pathogenesis of several cancers, including glioblastoma and colorectal, lung, renal, and bladder cancers, primarily through the increased production of reactive oxygen species (ROS). Inhibition of MAO-B impedes cell proliferation, making it a potential therapeutic target. Various monoamine oxidase B inhibitors have shown promise in inhibiting tumor growth and inducing apoptosis across different cancer types. In this review, we investigate MAO-B network biology, which highlighted glycolysis pathways as notable links between MAO-B and cancer. Further molecular modeling analysis illustrated the basis of MAO-B ligand binding, revealing a hydrophobic binding pocket, with key residues such as Tyr398 and Tyr435 playing crucial roles in substrate oxidation. MAO-B inhibitors that were reportsed in the literature (2012-2024) and their potential application in cancer therapy were discussed, highlighting key molecular scaffolds, such as propargyl analogs of phenyl alkyl amines, hydrazine derivatives, cyclopropylamine derivatives, MAO-B activated pro-drugs, and natural phenylpropanoid derivatives. The reported literature underscores the therapeutic potential of MAO-B inhibitors as versatile anticancer agents, warranting further investigation to optimize their efficacy and specificity across various malignancies.

Investigation of Cytotoxic Activity of Anthriscus nemorosa (M.Bieb.) Spreng. on Lung Cancer Cells

Medicinal plants are considered an important source of human health due to their therapeutic potential against various diseases including cancer. Cancer is a life-threatening disease characterized by uncontrolled cell growth and abnormal signaling processes. The incidence of cancer in society is increasing day by day. The search for active biological resources is important for the discovery of new anticancer drugs. Anthriscus nemorosa (M.Bieb.) Spreng. (Apiaceae) is a medicinal plant naturally distributed in Turkiye and traditionally used as food and against various diseases. This study investigated the methanol extracts of aerial parts and roots of A. nemorosa for cytotoxicity on lung cancer (A549) and non-cancerous (L929) cell lines. According to the results, both extracts showed significant dose-dependent cytotoxic effects on lung cancer cells. IC50 value was recorded as 8.29 μg/mL in the aerial parts extract. On the other hand, it was recorded as 3.57 μg/mL in the roots extract. Furthermore, the selectivity indexes were calculated as 5.93 and 3.38 for aerial parts and roots extracts, respectively. In light of the findings, it has been concluded that A. nemorosa deserves further anticancer research

Phytochemical and Cytotoxic Aspects of Amaryllidaceae Alkaloids in Galanthus Species: A Review.

The genus Galanthus (Amaryllidaceae) currently contains 25 plant species naturally occurring in Europe and the Middle East region. These perennial bulbous plants possess well-known medicinal and ornamental qualities. Alkaloid diversity is their most distinctive phytochemical feature. A total of 127 compounds (≈20% of all known Amaryllidaceae alkaloids) grouped in 16 structural types have been previously found in Galanthus extracts. Some structural types like galanthindole, graciline and plicamine were first discovered in Galanthus plants. Nine Galanthus species, however, remain unstudied regarding their alkaloid patterns. Intraspecific variability has only been studied in G. nivalis and G. elwesii. Amaryllidaceae alkaloids are molecules with anticholinesterase, antibacterial, antifungal, antiviral and anticancer properties. Galanthamine, isolated for the first time from Galanthus woronowii Losinsk., stands out as an acetylcholinesterase inhibitor approved for medical use by the FDA for the treatment of symptoms of Alzheimer's disease. Lycorine, narciclasine and pancratistatin are noteworthy cytotoxic and antitumor alkaloids. Structural types like galanthamine, homolycorine and haemanthamine are fairly well studied in anticancer research, but little to no information is available on galanthindole, graciline and other types. This review aims to present an update on the alkaloid diversity of Galanthus spp. and highlight the need for further research on the antitumor potential of these molecules.

Self-assembled free nanocarrier prodrugs based on camptothecin and dihydroartemisinin exhibit accumulation and improved anticancer efficacy.

Small molecule targeted inhibitor therapies often have several drawbacks, including limited oral bioavailability, quick metabolism, toxic effects that limit dosage, and poor water solubility. This study aims to develop a nanodrug self-delivery system that does not require a carrier by utilizing the self-assembly of camptothecin (CPT) and dihydroartemisinin (DHA). CPT/DHA nanoparticles (NPs) with varying diameters can be synthesized without requiring further carrier materials or chemical modifications by changing the CPT-to-DHA ratio (10:1, 5:1, 2:1, 1:1). Even more crucially, CPT/DHA NPs generate an AIE impact when they self-assemble. CPT/DHA NPs are used for cell tracking and bioimaging fluorescent probes. We chose CPT/DHA NPs (2:1) with a size of approximately 140nm for the anticancer examinations. The A549 cells were used to assess the cytotoxicity, morphological changes by biochemical staining methods and apoptosis by flow cytometric techniques of CPT/DHA NPs. Finally, in vitro anticancer research proved that CPT/DHA NPs are biocompatible and have strong synergistic anticancer properties.

Evaluating the anti-cancer potential and pharmacological in-sights of Physalis angulata Root Extract as a strong candidate for future research

The research targeting the prevention of complications through natural constituents, instigated by the cancer has recently drawn much more attention over the globe. The research in this direction also revealed that the use of natural constituents would considered a promising strategy for diminishing the aforementioned disease and its consequences. Because of the easy availability and safe nature, the recent years, natural resources as strong anticancer agents. In this regard, here we introduced the possibility of using the methanolic extract of Physalis angulata root as a strong candidate and implemented the applicability of LC-MS to unveil the presence of various phytocompounds. The anticancer potential exhibited by Physalis angulata root followed by its ability to induce toxicity against the microbial population enhanced the interest in unveiling the phytochemical compounds including Absintholide, Curcumin dimer 1, Mytilin A, Ginsenoside F1, Encecalin , Ganoderic acid TQ, Alnustone, Rhamnetin 3-sophoroside, Gibberellin A14 aldehyde, Thiolutin, Euglobal III and Epomusenin B. The presence of various macro and micronutrients suggested that Physalis angulata is a prominent resource for future research targeting pharmacological research, especially anticancer research.

Identification of tanshinone I as a natural Cu(II) ionophore

The development of Cu(II) ionophores for targeted disruption of aberrant redox homeostasis in cancer cells has been considered an appealing strategy in the field of anticancer research. This study presents the first identification of tanshinone I (Ts1), a natural o-quinone, as a Cu(II) ionophore. Structure-activity relationship studies on tanshinones and mechanistic investigations reveal that the presence of Cu(II) effectively promotes the tautomerization of Ts1 from its diketo to keto-enol forms, thereby facilitating its sequential proton-loss Cu(II) chelation, and enabling it to function as a Cu(II) ionophore due to its structural features including the presence of an o-quinone moiety, a benzyl hydrogen, and a large conjugated system. The unique property allows Ts1 to preferentially induce copper accumulation in human hepatoma HepG2 cells over human umbilical vein endothelial cells, by releasing copper driven by reduced glutathione (GSH). This copper accumulation leads to a reduction in the GSH-to-oxidized glutathione ratio and the generation of reactive oxygen species, ultimately triggering apoptosis of HepG2 cells. The findings not only provide support for o-quinones as innovative types of anticancer Cu(II) ionophores, but also shed light on the previously unrecognized role of Ts1 as a potent Cu(II) ionophore for eradicating cancer cells by selectively disrupting their redox regulation programs, resembling a "Trojan horse".

Bayesian modeling for analyzing heterogeneous response in preclinical mouse tumor models.

In anticancer research, tumor growth measured in mouse models is important for assessing treatment efficacy for a treatment to progress to human clinical trials. Statistical analysis of time-to-event tumor volume data is complex because of heterogeneity in response and welfare-related data loss. Traditional statistical methods of testing the mean difference between groups are not robust because they assume common responses across a population. Heterogeneity in response is also seen in the clinic, and consequently, the assessment of the treatment considers the diversity through classification of the individual's response using the RECIST (Response Evaluation Criteria in Solid Tumors). To provide a comparable and translatable assessment of in vivo tumor response, we developed a statistical method called INSPECT (IN vivo reSPonsE Classification of Tumors) for analyzing heterogeneous responses through Bayesian modeling. This method can classify individual tumor behaviors into the categories of nonresponder, modest responder, stable responder, and regressing responder. Using both published and simulated data, we show that INSPECT methodology is more accurate and sensitive than existing methods with respect to balancing false-negative and false-positive rates. A case study demonstrates the value of INSPECT in drug projects for supporting the translation of drug efficacy from the preclinical phase into clinical trials. We also provide a package, "INSPECTumours," that launches a web interface to enable users to conduct the analysis and generate reports.

Novel 1,8-Naphthalimide Derivatives Inhibit Growth and Induce Apoptosis in Human Glioblastoma.

Given the rapid advancement of functional 1,8-Naphthalimide derivatives in anticancer research, we synthesized these two novel naphthalimide derivatives with diverse substituents and investigated the effect on glioblastoma multiforme (GBM) cells. Cytotoxicity, apoptosis, cell cycle, topoisomerase II and Western blotting assays were evaluated for these compounds against GBM in vitro. A human GBM xenograft mouse model established by subcutaneously injecting U87-MG cells and the treatment responses were assessed. Both compounds 3 and 4 exhibited significant antiproliferative activities, inducing apoptosis and cell death. Only compound 3 notably induced G2/M phase cell cycle arrest in the U87-MG GBM cells. Both compounds inhibited DNA topoisomerase II activity, resulting in DNA damage. The in vivo antiproliferative potential of compound 3 was further validated in a U87-MG GBM xenograft mouse model, without any discernible loss of body weight or kidney toxicity noted. This study presents novel findings demonstrating that 1,8-Naphthalimide derivatives exhibited significant GBM cell suppression in vitro and in vivo without causing adverse effects on body weight or kidney function. Further experiments, including investigations into mechanisms and pathways, as well as preclinical studies on the pharmacokinetics and pharmacodynamics, may be instrumental to the development of a new anti-GBM compound.

Recent Advancement in Drug Designing as Small Molecules in Targeted Cancer Therapy: Challenges and Future Directions.

The adverse outcome that patients experience as a result of anti-cancer therapy failure is primarily caused by metastasis. Making cancer a chronic disease with regular but controlled relapses is the real issue in increasing cancer patient lifespans. This can only be achieved by developing efficient therapeutic techniques that target critical targets in the metastatic process. New targeted therapy medications continue to emerge, and research into the molecular targeted therapy of tumors is flourishing. The ineffectiveness of conventional chemotherapy in targeting metastatic cells is primarily due to its ability to promote the selection of chemo-resistant cell populations that engage in epithelial-to-mesenchymal transition (EMT), which in turn encourages the colonization of distant sites and maintains the initial metastatic process. In considering this circumstance, research into a broad range of small molecules and biologics has been initiated to develop anti-metastatic medications that target particular targets implicated in the different stages of metastasis. With their ability to concentrate on cancer cells while avoiding normal cells, tar-geted medications offer a promising alternative to conventional chemotherapy that is both highly effective and relatively safe. Many obstacles, including an inadequate response rate and drug resistance, persist for small-molecule targeted anti-cancer medications, despite significant ad-vancements in this area. We encouraged small-molecule-focused anti-cancer therapy develop-ment by extensively assessing them by target classification. We reviewed current challenges, listed licenced drugs and key drug candidates in clinical trials for each target, and made sugges-tions for improving anti-cancer drug research and development. This review aims to discuss pre-sent and future small molecule inhibitor research and development for cancer treatment.

Thioredoxin reductase inhibition and glutathione depletion mediated by glaucocalyxin A promote intracellular disulfide stress in gastric cancer cells.

Thioredoxin reductase 1 (TXNRD1) has been identified as one of the promising chemotherapeutic targets in cancer cells. Therefore, a novel TXNRD1 inhibitor could accelerate chemotherapy in clinical anticancer research. In this study, glaucocalyxin A (GlauA), a natural diterpene extracted from Rabdosia japonica var. glaucocalyx, was identified as a novel inhibitor of TXNRD1. We found that GlauA effectively inhibited recombinant TXNRD1 and reduced its activity in gastric cancer cells without affecting the enzyme's expression level. Mechanistically, the selenocysteine residue (U498) of TXNRD1 was irreversibly modified by GlauA through a Michael addition. Additionally, GlauA formed a covalent adduct with glutathione (GSH) and disrupted cellular redox balance by depleting cellular GSH. The inhibition of TXNRD1 and depletion of GSH by GlauA conferred its cytotoxic effects in spheroid culture and Transwell assays in AGS cells. The disulfide stress induced cytotoxicity of GlauA could be mitigated by adding reducing agents, such as DTT and β-ME. Furthermore, the FDA-approval drug auranofin, a TXNRD1 inhibitor, triggered oligomerization of the cytoskeletal protein Talin-1 in AGS cells, indicating that inhibiting TXNRD1 triggered disulfide stress. In conclusion, this study uncovered GlauA as an efficient inhibitor of TXNRD1 and demonstrated the potential of TXNRD1 inhibition as an effective anticancer strategy by disrupting redox homeostasis and inducing disulfide stress.

Targeted Therapy in Breast Cancer: Advantages and Advancements of Antibody-Drug Conjugates, a Type of Chemo-Biologic Hybrid Drugs.

Cancer is a significant health challenge globally, with millions of people affected every year, resulting in high morbidity and mortality. Although other treatment options are available with limitations, chemotherapy, either standalone or combined with other therapeutic procedures, is the most commonly used practice of treating cancer. In chemotherapy, cancer cells/malignant tumors are targeted; however, due to less target specificity, along with malignant cells, normal cells are also affected, which leads to various off-target effects (side effects) that impact the patient quality of life. Out of all the different types of cancers, breast cancer is the most common type of cancer in humans worldwide. Current anticancer drug discovery research aims to develop therapeutics with higher potency and lower toxicity, which is only possible through target-specific therapy. Antibody-drug conjugates (ADCs) are explicitly designed to target malignant tumors and minimize off-target effects by reducing systemic cytotoxicity. Several ADCs have been approved for clinical use and have shown moderate to good efficacy so far. Considering various aspects, chemotherapy and ADCs are useful in treating cancer. However, ADCs provide a more focused and less toxic approach, which is especially helpful in cases where resistance to chemotherapy (drug resistance) occurs and in the type of malignancies in which specific antigens are overexpressed. Ongoing ADC research aims to develop more target-specific cancer treatments. In short, this study presents a concise overview of ADCs specific to breast cancer treatment. This study provides insight into the classifications, mechanisms of action, structural aspects, and clinical trial phases (current status) of these chemo-biologic drugs (ADCs).

Family Malvaceae: a potential source of secondary metabolites with chemopreventive and anticancer activities supported with in silico pharmacokinetic and pharmacodynamic profiles.

Cancer is the second most widespread cause of mortality following cardiovascular disorders, and it imposes a heavy global burden. Nowadays, herbal nutraceutical products with a plethora of bioactive metabolites represent a foundation stone for the development of promising chemopreventive and anticancer agents. Certain members of the family Malvaceae have traditionally been employed to relieve tumors. The literature concerning the chemopreventive and anticancer effects of the plant species along with the isolated cytotoxic phytometabolites was reviewed. Based on the findings, comprehensive computational modelling studies were performed to explore the pharmacokinetic and pharmacodynamic profiles of the reported cytotoxic metabolites to present basis for future plant-based anticancer drug discovery. All the available information about the anticancer research in family Malvaceae and its cytotoxic phytometabolites were retrieved from official sources. Extensive search was carried out using the keywords Malvaceae, cancer, cytotoxicity, mechanism and signalling pathway. Pharmacokinetic study was performed on the cytotoxic metabolites using SWISS ADME model. Acute oral toxicity expressed as median lethal dose (LD50) was predicted using Pro Tox 3.0 web tool. The compounds were docked using AutoDock Vina platform against epidermal growth factor receptor (EGFR kinase enzyme) obtained from the Protein Data Bank. Molecular dynamic simulations and MMGBSA calculations were performed using GROMACS 2024.2 and gmx_MMPBSA tool v1.5.2. One hundred forty-five articles were eligible in the study. Several tested compounds showed safe pharmacokinetic properties. Also, the molecular docking study showed that the bioactive metabolites possessed agreeable binding affinities to EGFR kinase enzyme. Tiliroside (25), boehmenan (30), boehmenan H (31), and isoquercetin (22) elicited the highest binding affinity toward the enzyme with a score of -10.4, -10.4, -10.2 and -10.1Kcal/mol compared to the reference drug erlotinib having a binding score equal to -9Kcal/mol. Additionally, compounds 25 and 31 elicited binding free energies equal to -42.17 and -42.68Kcal/mol, respectively, comparable to erlotinib. Overall, the current study presents helpful insights into the pharmacokinetic and pharmacodynamic properties of the reported cytotoxic metabolites belonging to family Malvaceae members. The molecular docking and dynamic simulations results intensify the roles of secondary metabolites from medicinal plants in fighting cancer.

The Microbial Sources of Bioactive Compounds: Potential Anticancer Therapeutic Options

Chemotherapy and other traditional anticancer treatments are losing their efficacy in the battle against cancer. As a result, cancer treatment strategies must be continually adjusted to meet the rising demand for alternative medicines. Several viral and non-viral vectors have been used previously. However, it has been shown that microorganisms are a strong contender for successfully combating cancer. They are a remarkable source of toxins, polysaccharides, tumor-specific anticancer genes, nanodrugs and gene-delivery vectors. One of the emerging key players in cancer therapy is bacteria. It has been demonstrated that traditional methods of altering the microbiome, such as antibiotics, probiotics and microbiota transplants, can sometimes increase the effectiveness of cancer therapies. However, problems with these methods, such as consistency and collateral damage to the commensal microbiota, spur the development of new technologies specifically aimed at the microbiome-cancer interface. In light of nanotechnology’s success in transforming cancer diagnostics and treatment, nanotechnologies with the capacity to control interactions that occur across microscopic and molecular length scales in the microbiome and the tumor microenvironment have the potential to provide innovative methods for cancer treatment. The relationship between nanotechnology, the microbiome and cancer offers tremendous potential. This paper highlights the contributions of significant bacterial groups to several anticancer research fields.

From Spheroids to Bioprinting: A Literature Review on Biomanufacturing Strategies of 3D In Vitro Osteosarcoma Models

AbstractOsteosarcoma (OS) is a rare primary malignant bone cancer affecting mainly young individuals. Treatment typically consists of chemotherapy and surgical tumor resection, which has undergone few improvements since the 1970s. This therapeutic approach encounters several limitations attributed to the tumor's inherent chemoresistance, marked heterogeneity and metastatic potential. Therefore, the development of in vitro platforms that closely mimic the OS pathophysiology is crucial to understand tumor progression and discover effective anticancer therapeutics. Contrary to 2D monolayer cultures and animal models, 3D in vitro platforms show promise in replicating the 3D tumor macrostructure, cell‐cell and cell‐extracellular matrix interactions. This review provides an overview of the biomanufacturing strategies employed in developing 3D in vitro OS models, highlighting their role in replicating different aspects of OS and improving OS anticancer research and drug screening. A variety of 3D in vitro models are explored, including both scaffold‐free and scaffold‐based models, encompassing cell spheroids, hydrogels, and innovative approaches like electrospun nanofibers, microfluidic devices and bioprinted constructs. By examining the distinctive features of each model type, this review offers insights into their potential transformative impact on the landscape of OS research and therapeutic innovation, addressing the challenges and future directions of 3D in vitro OS modeling.

Verteporfin is an effective inhibitor of HCMV replication

Human cytomegalovirus (HCMV), a double-stranded DNA virus from the Betaherpesvirinae subfamily, constitutes significant risks to newborns and immunocompromised individuals, potentially leading to severe neurodevelopmental disorders. The purpose of this study was to identify FDA-approved drugs that can inhibit HCMV replication through a drug repositioning approach. Using an HCMV progeny assay, verteporfin, a medication used as a photosensitizer in photodynamic therapy, was found to inhibit HCMV production in a dose-dependent manner, significantly reducing replication at concentrations as low as 0.5 µM, approximately 1/20th of the concentration used in anti-cancer research. Further analysis revealed that verteporfin did not interfere with HCMV host cell entry or nuclear transport but reduced viral mRNA and protein levels throughout the HCMV life cycle from the immediate-early stages. These results suggest that verteporfin has the potential to be rapidly and safely developed as a repurposed drug to inhibit HCMV infection.

In Vitro Anticancer Potential of Eugenol on Oral Cancer Cell Lines: A Systematic Review.

Oral cancer is one of the most common types of cancer and has become a global health concern. Oral squamous cell carcinoma (OSCC) is the most prevalent form of oral cancer worldwide. Eugenol, an aromatic phenolic compound, exhibits various pharmacological activities, including anticancer effects. Several studies have reported the anticancer activity of eugenol against OSCC via different pathways. However, no current review has discussed the extent of eugenol anticancer research on oral cancer cell lines using in vitro studies. This systematic review aimed to discuss the anticancer potential of eugenol against oral cancer cell lines in vitro. Articles were selected from PubMed, ScienceDirect, SpringerLink and EBSCOhost databases based on specified inclusion and exclusion criteria. Additional articles were identified through manual hand searching. The selection process followed PRISMA guidelines. A risk-of-bias assessment was performed to evaluate the reliability and relevance of the in vitro studies. Thirteen articles with high-quality results were assessed and analysed for further investigation. These studies investigated the ability of eugenol to induce cell death through apoptotic and non-apoptotic pathways, inhibit cell proliferation and affect oxidative stress, contributing to cell death in several oral cancer cell lines. Therefore, eugenol is a potential anticancer agent for OSCC, as it exhibited anticancer activity in oral cancer cell lines in vitro studies.

Preliminary anticancer activity of Carpobrotus edulis (L.) Bolus exposed to low and high temperature conditions against cervical cancer

Introduction: Environmental temperature conditions might influence the composition of secondary metabolites in certain medicinal plants. This study aimed to examine how some of the phytochemicals and anticancer properties of Carpobrotus edulis may be impacted by temperature conditions. Methods: The plant specimens were kept in growth chambers at 15/10 °C and 45/35 °C (day/night), and harvested at 48-hour intervals (48, 96, and 144 hours). Control conditions were maintained at 25/15 °C. Standard phytochemical colour tests were used to determine the presence of eight phytochemicals. The anticancer activity against cervical cancer cell lines was determined using cell viability assay, cell morphology, Hoechst staining, and wound healing assays. Results: The phytochemical screening showed the presence of all tested phytochemicals (phenolics, flavonoids, terpenoids, saponins, tannins, steroids, and cardiac glycosides) in all treatments except for saponins in the 96- and 144-hour temperature treatments. A noteworthy IC50 value of 284.9 µg/mL was determined from the methanolic leaf extract exposed to high temperatures for 144 hours against cervical cancer. Treatment with this extract suggested changes in cancer cell morphology, signs of apoptosis, and cell migration inhibition. Conclusion: The preliminary results obtained suggest that the C. edulis methanolic extract has potential anticancer properties against cervical cancer. These observations may have implications for the indigenous plant use in treating various ailments and broaden the type of anticancer research involving this plant.