Forward-reverse mutation cycles in cancer cell lines under chemical treatments.

Spontaneous forward-reverse mutations were reported by us earlier in clinical samples from various types of cancers and in HeLa cells under normal culture conditions. To investigate the effects of chemical stimulations on such mutation cycles, the present study examined single nucleotide variations (SNVs) and copy number variations (CNVs) in HeLa and A549 cells exposed to wogonin-containing or acidic medium. In wogonin, both cell lines showed a mutation cycle during days 16-18. In acidic medium, both cell lines displayed multiple mutation cycles of different magnitudes. Genomic feature colocalization analysis suggests that CNVs tend to occur in expanded and unstable regions, and near promoters, histones, and non-coding transcription sites. Moreover, phenotypic variations in cell morphology occurred during the forward-reverse mutation cycles under both types of chemical treatments. In conclusion, chemical stresses imposed by wogonin or acidity promoted cyclic forward-reverse mutations in both HeLa and A549 cells to different extents.

Benzimidazole-based small molecules as anticancer agents targeting telomeric G-quadruplex and inhibiting telomerase enzyme.

Telomeres, crucial for chromosomal integrity, have been related to aging and cancer formation, mainly through regulating G-quadruplex structures. G-quadruplexes are structural motifs that can arise as secondary structures of nucleic acids, especially in guanine-rich DNA and RNA regions. Targeting these structures by small compounds shows promise in the selective suppression of cell growth, opening up novel possibilities for anticancer treatment. A comprehensive investigation of the many structural forms of G-quadruplex ligands is required to create ground-breaking anticancer drugs. Recent research into using specific benzimidazole molecules in stabilizing telomeric DNA into G-quadruplex structures has highlighted their ability to influence oncogene expression and demonstrate antiproliferative characteristics against cancer cells. This review describes the benzimidazole derivative, designed to enhance the stability of the G-quadruplex structure DNA to suppress the activity of telomerase enzyme, exhibiting promising potential for anticancer therapy.

[Box: see text].

Lysosome-Targeted Bifunctional Therapeutics Induce Autodynamic Cancer Therapy.

Autodynamic cancer therapy possesses tremendous potential for enhancing therapeutic efficacy by initiating the treatment process autonomously within targeted cells. However, challenges related to biocompatibility and targeted delivery have hindered its clinical translation owing to the induction of adverse effects and cytotoxicity in healthy cells. In this study, a novel approach for auto-initiated dynamic therapy by conjugating zwitterionic near-infrared fluorophores to a cell-penetrating peptide is proposed. This enables efficient cellular uptake and specific targeting of therapy to desired cells while avoiding off-target uptake. The zwitterionic bioconjugate causes cancer-specific toxicity following its internalization into the targeted cells, triggered by specific intracellular conditions in lysosomes. This innovative approach enables selective targeting of lysosomes in malignant cells while minimizing cytotoxic effects on normal cells. By targeting lysosomes, the method overcomes inherent risks and side effects associated with conventional cancer treatments, offering a selective and effective approach to cancer therapy.

Recent Advances in Nanocatalyzed One-Pot Sustainable Synthesis of Bioactive N, N-Heterocycles with Anticancer Activities: An Outlook of Medicinal Chemistry.

N-heterocycles represent a predominant and unique class of organic chemistry. They have received a lot of attention due to their important chemical, biomedical, and industrial uses. Food and Drug Administration (FDA) approved about 75% of drugs containing N-based heterocycles, which are currently available in the market. N-Heterocyclic compounds exist as the backbone of numerous natural products and act as crucial intermediates for the construction of pharmaceuticals, veterinary items, and agrochemicals frequently. Among N-based heterocyclic compounds, bioactive N,N-heterocycles constitute a broad spectrum of applications in modern drug discovery and development processes. Cefozopran (antibiotic), omeprazole (antiulcer), enviradine (antiviral), liarozole (anticancer), etc., are important drugs containing N,N-heterocycles. The synthesis of N,Nheterocyclic compounds under sustainable conditions is one of the most active fields because of their significant physiological and biological properties as well as synthetic utility. Current research is demanding the development of greener, cheaper, and milder protocols for the synthesis of N,N-heterocyclic compounds to save mother nature by avoiding toxic metal catalysts, extensive application of energy, and the excessive use of hazardous materials. Nanocatalysts play a profound role in sustainable synthesis because of their larger surface area, tiny size, and minimum energy; they are eco-friendly and safe, and they provide higher yields with selectivity in comparison to conventional catalysts. It is increasingly demanding research to design and synthesize novel bioactive compounds that may help to combat cancer since the major causes of death worldwide are due to cancer. Hence, the important uses of nanocatalysts for the one-pot synthesis of biologically potent N,N-heterocycles with anticancer activities have been presented in this review.

Morchella conica, Morchella esculenta and Morchella delicosa Induce Apoptosis in Breast and Colon Cancer Cell Lines via Pro-apoptotic and Anti-apoptotic Regulation.

OBJECTIVE: To explore the potential apoptotic mechanisms of 3 Morchella extracts (Morchella conica, Morchella esculenta and Morchella delicosa) on breast and colon cancer cell lines using apoptotic biomarkers. METHODS: Human breast cell line (MCF-7) and colon cancer cell line (SW-480) were treated with methanol and ethanol extracts of 3 Morchella species with concentration ranging from 0.0625 to 2 mg/mL. After that their effects on gene expression of apoptosis related markers (pro-apoptotic markers including Bax, caspase-3, caspase-7, and caspase-9, and the antiapoptotic marker including Bcl-2) were determined using reverse transcription polymerase chain reaction. RESULTS: All Morchella extracts reduced breast and colon cancer cells proliferation at half inhibitory concentration (IC50) of 0.02 ±0.01 to 0.68 ±0.30 mg/mL. As expected, all Morchella extracts significantly increased gene expressions of Bax, caspase-3, caspase-7, and caspase-9 and downregulated the gene expression of Bcl-2 in MCF-7 and SW-480 cell lines (P<0.05). CONCLUSIONS: Morchella extracts demonstrated significant anti-proliferative activity against breast and colon cancer cell lines via an apoptosis induction mechanism. Anticancer activity of Morchella extracts and activation of apoptosis in breast and colon cancer cells suggest that it may be used to develop chemotherapeutic agents against cancer in future.

Bioinspired Synthesis and Characterization of Dual-Function Zinc Oxide Nanoparticles from Saccharopolyspora hirsuta: Exploring Antimicrobial and Anticancer Activities.

Microbial synthesis offers a sustainable and eco-friendly approach for nanoparticle production. This study explores the biogenic synthesis of zinc oxide nanoparticles (ZnO-NPs) utilizing the actinomycete Saccharopolyspora hirsuta (Ess_amA6) isolated from Tapinoma simrothi. The biosynthesized ZnO-NPs were characterized using various techniques to confirm their formation and properties. UV-visible spectroscopy revealed a characteristic peak at 372 nm, indicative of ZnO-NPs. X-ray diffraction (XRD) analysis confirmed the crystalline structure of the ZnO-NPs as hexagonal wurtzite with a crystallite size of approximately 37.5 ± 13.60 nm. Transmission electron microscopy (TEM) analysis showed the presence of both spherical and roughly hexagonal ZnO nanoparticles in an agglomerated state with a diameter of approximately 44 nm. The biogenic ZnO-NPs exhibited promising biomedical potential. They demonstrated selective cytotoxic activity against human cancer cell lines, demonstrating higher efficacy against Hep-2 cells (IC50 = 73.01 µg/mL) compared to MCF-7 cells (IC50 = 112.74 µg/mL). Furthermore, the biosynthesized ZnO-NPs displayed broad-spectrum antimicrobial activity against both Pseudomonas aeruginosa and Staphylococcus aureus with clear zones of inhibition of 12.67 mm and 14.33 mm, respectively. The MIC and MBC values against P. aeruginosa and S. aureus ranged between 12.5 and 50 µg/mL. These findings suggest the potential of S. hirsuta-mediated ZnO-NPs as promising biocompatible nanomaterials with dual applications as antimicrobial and anticancer agents.

Efficient synthesis of novel 1,10 phenanthroline-substituted imidazolium salts: Exploring their anticancer applications.

This study reports a new series of 1,10-phenanthroline-substituted imidazolium salts (1a-f), examining their design, synthesis, structure and anticancer activities. The structures of these salts (1a-f) were characterized using 1H, 13C NMR, elemental analysis, mass spectrometry and Fourier transform infrared (FT-IR) spectroscopies. The salts' cytotoxic activities were tested against cancer cell lines, specifically MCF-7, MDA-MB-231 and non-tumorigenic MCF-10A mammary cells. The study compared the impact of aliphatic and benzylic groups in the salts' structure on their anticancer activity. Screening results revealed that compound 1c, in particular, showed promising inhibitory activity against the growth of MDA-MB-231 breast cancer cells, with an IC50 value of 12.8 ± 1.2 µM, indicating its potential as a chemotherapeutic agent. Cell apoptosis analysis demonstrated a tendency for compound 1c to induce early apoptosis in breast cancer cells. The stability/aquation of compound 1c was investigated using 1H NMR spectroscopy and its binding modes with DNA were explored via UV-Vis spectroscopy. Additionally, the study investigated the interaction residues and docking scores of compound 1c and the reference drug doxorubicin against Bax and Bcl-2 proteins using molecular docking.

Amine-Rich Carbon Dots Synthesized from Kappa-Carrageenan and l-Lysine as a Dual Probe for Detection of Folic Acid and Tumor-Targeted Delivery of Therapeutics.

Strategically designed, heteroatom-rich surface functionalized blue fluorescent carbon dots (CDs) were synthesized for high-throughput detection of folic acid (vitamin B9). The highly stable CDs could particularly detect vitamin B9 in the presence of 35 analytes, even up to 40 nM of the vitamin. The versatile CDs were found to have a high affinity for folic acid in wastewater, folic acid tablets, and food samples enriched with folic acid. The hemocompatibility of the CDs was also studied by using a hemolysis assay, confirming the CDs to be nontoxic to human blood samples up to 400 µg/mL. The CDs were then covalently conjugated to biotin, which possesses receptors that are overexpressed in tumor cells. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye) assay and confocal bioimaging studies proved the biotin-modified CDs (CDBT) were remarkably nontoxic in healthy cell lines (HEK-293) and highly target-specific toward tumor cells (HeLa), including triple-negative breast cancer cells (MDA-MB-231). The cytotoxicity assay of 5-fluorouracil encapsulated CDs (CDBTFu) showed the IC50 value to be 81 µM in HeLa cells and 185 µM in MDA-MB-231 cells, respectively, and significantly higher in HEK-293 cells (over 300 µM), owing to high specificity toward tumor cells.

Isocoumarins incorporating chalcone moieties act as isoform selective tumor-associated carbonic anhydrase inhibitors.

Aim: A series of isocoumarin-chalcone hybrids were prepared and assays for the inhibition of four isoforms of human carbonic anhydrase (hCA; EC 4.2.1.1), hCA I, II, IX and XII. Materials & methods: Isocoumarin-chalcone hybrids were synthesized by condensing acetyl-isocoumarin with aromatic aldehydes. They did not significantly inhibit off-target cytosolic isoforms hCA I and II (KI >100 µM) but acted as low micromolar or submicromolar inhibitors for the tumor-associated isoforms hCA IX and XII. Results & conclusion: Our work provides insights into a new and scarcely investigated chemotype which provides interesting tumor-associated CA inhibitors, considering that some such derivatives like sulfonamide SLC-0111 are in advanced clinical trials for the management of metastatic advanced solid tumors.

A series of isocoumarin­chalcone hybrids was prepared and assays for the inhibition of four isoforms of the metalloenzyme carbonic anhydrase (CA; EC 4.2.1.1), i.e., human (h) isoforms hCA I, II, IX and XII. Isocoumarins were less investigated as inhibitors of this enzyme. Here we show that the isocoumarin­chalcone hybrids do not significantly inhibit the off-target cytosolic isoforms hCA I and II (K_Is >100 µM) but act as low micromolar inhibitors for the tumor-associated isoforms hCA IX and XII. Our work thus provides insights into a new and scarcely investigated chemotype which may provide interesting tumor-associated CA inhibitors, because some such compounds, e.g., the sulfonamide SLC-0111, are presently in advanced clinical trials for the management of metastatic advanced solid tumors.

Eco-Friendly Synthesis, Characterization, and Biomedical Applications of Biosynthesized Bimetallic Silver-Gold Nanoparticles by Culture Supernatant of Aspergillus niger.

Green synthesis of bimetallic nanoparticles of noble metals is highly desirable in nanomedicine because of their potential use as anticoagulant, thrombolytic and anticancer agents. In this study, it was discovered that the filamentous fungus Aspergillus niger proved effective in producing bimetallic Ag-Au nanoparticles. A. niger culture supernatant was able to produce Ag-AuNPs by reducing the solution of chloroauric acid/silver nitrate (1.0:1.0 mM) within 2 min at 100 °C and pH 8. Experimental Ag-AuNP detection was performed by visually observing the color change to reddish brown. The produced nanoparticles displayed maximal absorbance at 530 nm in UV-vis spectroscopy. According to transmission electron microscopy, most of the nanoparticles were spherical, with a mean diameter of 8-10 nm. The biosynthesis of Ag-AuNPs by A. niger was confirmed by Fourier transform infrared spectroscopy, X-ray diffraction and energy dispersive X-ray analytical techniques. Its zeta potential was discovered to be -34.01 mV. The biosynthesized Ag-AuNPs exhibited effective thrombolytic and antiplatelet aggregation actions by totally preventing and dissolving the blood clot which was verified by microscopic examination, amelioration of blood coagulation assays, and carrageenan-induced tail thrombosis model. The findings verified the effectiveness of biosynthesized Ag-AuNPs as a powerful antitumor agent against HepG2 and A549 cell lines with IC50 values of 15.57 and 27.07 µg/mL, respectively. Crystal violet assay validated the cytopathic effects of Ag-AuNPs on A549 and HepG2 cell lines. Therefore, the produced Ag-AuNPs from A. niger are a promising candidate in the management of thrombosis.

The Effect of Education and Monitoring via Tele-Nursing to Elderly Cancer Patients Using Oral Anticancer Agents on Self-efficacy and Medication Adherence: A Randomized Controlled Trial.

OBJECTIVES: This study was conducted as a randomized controlled trial to determine the effect of the education and monitoring provided via tele-nursing to elderly cancer patients using oral anticancer agents on their medication treatment adherence self-efficacy and medication adherence. METHODS: The sample of the study consisted of 60 elderly cancer patients who presented to the oncology outpatient clinics of a medical faculty hospital in Turkey. An Elderly Information Form, the Oral Chemotherapy Adherence Scale, the Medication Adherence Self-Efficacy Scale, a Tele-nursing Evaluation Form, and a Telephone Monitoring Form were used to collect data. Patients in the intervention group were sent text messages and educational videos via WhatsApp® for the first four weeks, and after the fifth week, they were monitored by phone for eight weeks. Data collection tools were applied to the control and intervention groups at weeks 1, 8, and 12. Independent samples t-test, Repeated measurements analysis of variance chi-square test, and Pearson correlation test were used to analyze the data. RESULTS: In the study, while there was no significant difference between the mean scores of the intervention and control groups on the pretest application of the Oral Chemotherapy Adherence Scale and the Medication Adherence Self-Efficacy Scale (p > .05), a significant difference was found between the mean posttest scores of the groups (p < .05). CONCLUSIONS: In this study, it was determined that the education and monitoring provided to elderly cancer patients via tele-nursing positively affected their self-efficacy and medication adherence. IMPLICATIONS FOR NURSING PRACTICE: In line with the research results, it is recommended that nurses use tele-nursing applications in the care of elderly cancer patients using oral anticancer agents.

1,3,5-Triazine as a promising scaffold in the development of therapeutic agents against breast cancer.

1,3,5-Triazine scaffold has garnered considerable interest due to its wide-ranging pharmacological properties, particularly in the field of cancer research. Breast cancer is the most commonly diagnosed cancer among women. Approximately one in eight women will receive a diagnosis of invasive breast cancer during their lifetime. The five-year survival rate for invasive breast cancer is less than 30 %, indicating a need to develop a more effective therapeutic agent targeting breast cancer. This review discusses bioactive 1,3,5-triazines targeting breast cancer cells by the inhibition of different enzymes, which include PI3K, mTOR, EGFR, VEGFR, FAK, CDK, DHFR, DNA topoisomerase, ubiquitin-conjugating enzyme, carbonic anhydrase, and matrix metalloproteinase. The anticancer agent search in some drug discovery programs is based on compound screening for antiproliferative activity. Often, multiple targets contribute to the anticancer effect of 1,3,5-triazines and this approach allows identification of active molecules prior to identification of their targets.

Polyoxygenated cembrane-type diterpenes from the Hainan soft coral Lobophytum crassum as a promising source of anticancer agents with ErbB3 and ROR1 inhibitory potential.

A detailed chemical investigation of the Hainan soft coral Lobophytum crassum led to the identification of a class of polyoxygenated cembrane-type macrocyclic diterpenes (1-28), including three new flexible cembranoids, lobophycrasins E-G (2-4), and twenty-five known analogues. Their structures were elucidated by combining extensive spectroscopic data analysis, quantum mechanical-nuclear magnetic resonance (QM-NMR) methods, the modified Mosher's method, X-ray diffraction analysis, and comparison with data reported in the literature. Bioassays revealed that sixteen cembranoids inhibited the proliferation of H1975, MDA-MB231, A549, and H1299 cells. Among them, Compounds 10, 17, and 20 exhibited significant antiproliferative activities with IC50 values of 1.92-8.82 µM, which are very similar to that of the positive control doxorubicin. Molecular mechanistic studies showed that the antitumour activity of Compound 10 was closely related to regulation of the ROR1 and ErbB3 signalling pathways. This study may provide insight into the discovery and utilization of marine macrocyclic cembranoids as lead compounds for anticancer drugs.

The Bright Side of Curcumin: A Narrative Review of Its Therapeutic Potential in Cancer Management.

Curcumin, a polyphenolic compound derived from Curcuma longa, exhibits significant therapeutic potential in cancer management. This review explores curcumin's mechanisms of action, the challenges related to its bioavailability, and its enhancement through modern technology and approaches. Curcumin demonstrates strong antioxidant and anti-inflammatory properties, contributing to its ability to neutralize free radicals and inhibit inflammatory mediators. Its anticancer effects are mediated by inducing apoptosis, inhibiting cell proliferation, and interfering with tumor growth pathways in various colon, pancreatic, and breast cancers. However, its clinical application is limited by its poor bioavailability due to its rapid metabolism and low absorption. Novel delivery systems, such as curcumin-loaded hydrogels and nanoparticles, have shown promise in improving curcumin bioavailability and therapeutic efficacy. Additionally, photodynamic therapy has emerged as a complementary approach, where light exposure enhances curcumin's anticancer effects by modulating molecular pathways crucial for tumor cell growth and survival. Studies highlight that combining low concentrations of curcumin with visible light irradiation significantly boosts its antitumor efficacy compared to curcumin alone. The interaction of curcumin with cytochromes or drug transporters may play a crucial role in altering the pharmacokinetics of conventional medications, which necessitates careful consideration in clinical settings. Future research should focus on optimizing delivery mechanisms and understanding curcumin's pharmacokinetics to fully harness its therapeutic potential in cancer treatment.

Broccoli Consumption and Risk of Cancer: An Updated Systematic Review and Meta-Analysis of Observational Studies.

BACKGROUND: The scientific literature has reported an inverse association between broccoli consumption and the risk of suffering from several types of cancer; however, the results were not entirely consistent across studies. A systematic review and meta-analysis of observational studies were conducted to determine the association between broccoli consumption and cancer risk with the aim of clarifying the beneficial biological effects of broccoli consumption on cancer. METHODS: PubMed/MEDLINE, Web of Science, Scopus, Cochrane Library (CENTRAL), and Epistemonikos databases were searched to identify all published papers that evaluate the impact of broccoli consumption on the risk of cancer. Citation chasing of included studies was conducted as a complementary search strategy. The risk of bias in individual studies was assessed using the Newcastle-Ottawa Scale. A random-effects model meta-analysis was employed to quantitatively synthesize results, with the I2 index used to assess heterogeneity. RESULTS: Twenty-three case-control studies (n = 12,929 cases and 18,363 controls; n = 31,292 individuals) and 12 cohort studies (n = 699,482 individuals) were included in the meta-analysis. The results suggest an inverse association between broccoli consumption and the risk of cancer both in case-control studies (OR: 0.64, 95% CI from 0.58 to 0.70, p < 0.001; Q = 35.97, p = 0.072, I2 = 30.49%-moderate heterogeneity; τ2 = 0.016) and cohort studies (RR: 0.89, 95% CI from 0.82 to 0.96, p = 0.003; Q = 13.51, p = 0.333, I2 = 11.21%-low heterogeneity; τ2 = 0.002). Subgroup analysis suggested a potential benefit of broccoli consumption in site-specific cancers only in case-control studies. CONCLUSIONS: In summary, the findings indicate that individuals suffering from some type of cancer consumed less broccoli, suggesting a protective biological effect of broccoli on cancer. More studies, especially cohort studies, are necessary to clarify the possible beneficial effect of broccoli on several types of cancer.

Synthesis of selenophene-containing flavonols and 2-styrylchromones: Evaluation of their activities compared with selenophene-containing chalcones as potential anticancer agents.

Previously, we documented the synthesis and assessed the biological effects of chalcones containing selenium against HT-29 human colorectal adenocarcinoma cells, demonstrating their significant potential. As research on selenium-containing flavonoids remains limited, this article outlines our design and synthesis of three selenium-based flavonols and three 2-styrylchromones. We conducted evaluations of these compounds to determine their impact on human lung cancer cells (A549, H1975, CL1-0, and CL1-5) and their influence on normal lung fibroblast MRC5 cells. Additionally, we included selenium-based chalcones in our testing for comparative purposes. Our findings highlight that the simplest compound, designated as compound 1, exhibited the most promising performance among the tested molecules.

Structure-Based De Novo Design for the Discovery of Miniprotein Inhibitors Targeting Oncogenic Mutant BRAF.

Being a component of the Ras/Raf/MEK/ERK signaling pathway crucial for cellular responses, the VRAF murine sarcoma viral oncogene homologue B1 (BRAF) kinase has emerged as a promising target for anticancer drug discovery due to oncogenic mutations that lead to pathway hyperactivation. Despite the discovery of several small-molecule BRAF kinase inhibitors targeting oncogenic mutants, their clinical utility has been limited by challenges such as off-target effects and suboptimal pharmacological properties. This study focuses on identifying miniprotein inhibitors for the oncogenic V600E mutant BRAF, leveraging their potential as versatile drug candidates. Using a structure-based de novo design approach based on binding affinity to V600E mutant BRAF and hydration energy, 39 candidate miniprotein inhibitors comprising three helices and 69 amino acids were generated from the substructure of the endogenous ligand protein (14-3-3). Through in vitro binding and kinase inhibition assays, two miniproteins (63 and 76) were discovered as novel inhibitors of V600E mutant BRAF with low-micromolar activity, with miniprotein 76 demonstrating a specific impediment to MEK1 phosphorylation in mammalian cells. These findings highlight miniprotein 76 as a potential lead compound for developing new cancer therapeutics, and the structural features contributing to its biochemical potency against V600E mutant BRAF are discussed in detail.

Synthesis of Flavonols and Assessment of Their Biological Activity as Anticancer Agents.

A series of flavanols were synthesized to assess their biological activity against human non-small cell lung cancer cells (A549). Among the sixteen synthesized compounds, it was observed that compounds 6k (3.14 ± 0.29 µM) and 6l (0.46 ± 0.02 µM) exhibited higher potency compared to 5-fluorouracil (5-Fu, 4.98 ± 0.41 µM), a clinical anticancer drug which was used as a positive control. Moreover, compound 6l (4'-bromoflavonol) markedly induced apoptosis of A549 cells through the mitochondrial- and caspase-3-dependent pathways. Consequently, compound 6l might be developed as a candidate for treating or preventing lung cancer.

Insights into the structure-activity relationship of the anticancer compound ZJ-101: A role played by the amide moiety.

ZJ-101, a structurally simplified analog of marine natural product superstolide A, was previously designed and synthesized in our laboratory. In the present study four new analogs of ZJ-101 were designed and synthesized to investigate the structure-activity relationship of the acetamide moiety of the molecule. The biological evaluation showed that the amide moiety is important for the molecule's anticancer activity. Replacing the amide with other functional groups such as a sulfonamide group, a carbamate group, and a urea group resulted in the decrease in anticancer activity.

Article review: Brazilin as potential anticancer agent.

Brazilin is the main compound in Caesalpinia sappan and Haematoxylum braziletto, which is identified as a homoisoflavonoid based on its molecular structure. These plants are traditionally used as an anti-inflammatory to treat fever, hemorrhage, rheumatism, skin problems, diabetes, and cardiovascular diseases. Recently, brazilin has increased its interest in cancer studies. Several findings have shown that brazilin has cytotoxic effects on colorectal cancer, breast cancer, lung cancer, multiple myeloma, osteosarcoma, cervical cancer, bladder carcinoma, also other cancers, along with numerous facts about its possible mechanisms that will be discussed. Besides its flavonoid content, brazilin is able to chelate metal ions. A study has proved that brazilin could be used as an antituberculosis agent based on its ability to chelate iron. This possible iron-chelating of brazilin and all the studies discussed in this review will lead us to the statement that, in the future, brazilin has the potency to be a chemo-preventive and anticancer agent. The article review aimed to determine the brazilin mechanism and pathogenesis of cancer.