Significant Anticancer Activity Research Articles

Harnessing Desmochloris edaphica Strain CCAP 6006/5 for the Eco-Friendly Synthesis of Silver Nanoparticles: Insights into the Anticancer and Antibacterial Efficacy.

Microalgae-mediated nanoparticle (NP) biosynthesis is a promising green synthesis method that overcomes the challenges of conventional synthesis methods. The novel Desmochloris edaphica strain CCAP 6006/5 was isolated, purified, and characterized morphologically and genetically. GC-MS analysis of the algal biomass (DBio) phytochemicals showed the abundance for elaidic acid (18.36%) and monoolein (17.37%). UV-VIS spectroscopy helped analyze the effects of the AgNO3 concentration, algal/silver nitrate ratio, temperature, reaction time, illumination, and pH on AgNP synthesis. DBio extract or cell-free medium (DSup) of D. edaphica successfully biosynthesized small silver NPs (AgNPs), namely, DBio@AgNPs and DSup@AgNPs, under optimum reaction conditions. TEM and SEM showed a quasi-spherical shape, with average diameters of 15.0 ± 1.0 nm and 12.0 ± 0.8 nm, respectively. EDx and mapping analyses revealed that silver was the main element, the NP hydrodynamic diameters were 77.9 and 62.7 nm, and the potential charges were -24.4 and -25.8 mV, respectively. FTIR spectroscopy revealed that the DBio@AgNPs, and DSup@AgNPs were coated with algal functional groups, probably derived from algal proteins, fatty acids, or polysaccharides, representing reductant and stabilizer molecules from the synthesis process. They showed significant anticancer activity against breast cancer cells (MCF-7), low toxicity against normal kidney cells (Vero), and potent inhibitory activity against Staphylococcus aureus, Bacillus subtilis, and Shigella flexneri. D. edaphica is a novel biomachine for synthesizing small, stable and potent therapeutic AgNPs.

Microwave-assisted synthesis, characterization, and molecular docking studies of new chlorophthalazine derivatives as anticancer activity

A series of phthalazine derivatives have been synthesized using green protocol methods under microwave irradiation. This involved subjecting chlorophthalazine to microwave irradiation and employing various reagents, including hydrazine derivatives, primary and secondary amines, and active methylene, to generate the novel phthalazine derivatives. Subsequently, a comparison was made between the yield percentage and reaction time of the resulting products obtained from conventional methods and those obtained through microwave irradiation. The structures of all new compounds were confirmed by physical properties and spectral analysis. The phthalazine compounds demonstrated significant anticancer activity against three cancer cell lines and showed promising selectivity when compared with doxorubicin. Compound 6 exhibited the best anticancer activity, with IC50 1.739 µM, 0.384 µM, and 1.52 µM against MCF7, HCT116, and HepG2 cell lines, respectively. The docking results confirmed that the drugs exert their activity by inhibiting PARP-1. The binding scores were in accordance with the experimental IC50, with compound 6 exhibiting the best binding score and retaining the essential binding interactions with the active site. The results of our computational research have revealed that our phthalazine compounds possess a unique structure that effectively inhibits PARP-1.

Evaluation of Anticancer and Antibacterial Activities for Pluronic F-127 Encapsulated Magnesium Oxide Nanoparticles Using Alstoniayunnanensis Leaf Extract

Primary brain tumors caused by gliomas are most frequently found in the neurons of the central nervous system. The present study explores the effects of Pluronic F-127 coated magnesium oxide nanoparticles (PF-127 MgO NPs) using Alstonia yunnanensis leaf extract (A. yunnanensis) on C6 glioma cells (C6 cells). The vital part of nanotechnology is the formulation of environmentally friendly methods for making NPs. Because of their small size, NPs can pass easily through the holes in intracellular cell membranes and into living tissue. Numerous integrated protein therapies have shown enhanced medicinal qualities and thermo stability owing to PF-127. MgO is employed in cell therapy, tissue repair and the creation of cancer medicines. In this research, we synthesized PF-127 MgO NPs using A. yunnanensis leaf extract to study the activity of their anti-bacterial and anti-cancer activities on C6 cells. We examined the synthesized NPs by the UV-Vis, FT-IR, PL, TEM, SAED, FE-SEM, EDAX, XRD, and DLS techniques. The anti-bacterial effectiveness and anti-cancer activity C6 cells on MTT assay, AO/EtBr, DAPI, DCFH-DA and Rh-123 staining methods of synthesized PF-127 MgO NPs. Moreover, the synthesized NPs characterization studies can be used high activity anti-bacterial and significant anti-cancer activity were noticed. The study finds that the NPs increased ROS accumulation and resulting in apoptotic cell death. Overall, our findings show that synthesized PF-127 coated MgO NPs using A. yunnanensis leaf extract possess anti-bacterial and anti-cancer properties in C6 cells.

Green Synthesis of Silver Nanoparticles using Morinda citrifolia Linn LeafExtract and its Antioxidant, Antibacterial and Anticancer Potential.

Nanomedicine has emerged as a revolutionary regimen for moderating communicable as well as non-communicable diseases. This study demonstrated the phytosynthesis of silver nanoparticles using M. citrifolia leaf extract (MC-AgNPs) and their in vitro antioxidant, antibacterial and anticancer potential. The Biosynthesis of MC-AgNPs was studied by spectroscopy and characterized by SEM, TEM, XRD and FTIR analysis. The antibacterial activity was checked by minimum inhibition concentration assay. The HeLa and MCF-7 cancer cell lines were used to explore the cytotoxicity and genotoxicity activity of biogenic MC-AgNPs. The free radical scavenging potential of MC-AgNPs was studied by in vitro DPPH and ABTS assays, which confirmed significant radical scavenging activity in a dose-dependent manner with IC50 of 17.70 ± 0.36 μg/mL for DPPH and 13.37 ± 3.15 μg/mL for ABTS radicals. The bactericidal effects of MC-AgNPs confirmed by MIC showed 0.1 mg/mL concentration of MC-AgNPs with greater sensitivity for E.coli (93.33 ± 0.89), followed by K. pneumoniae (90.99 ± 0.57), S. aureus (87.26 ± 2.80) and P. aeruginosa strains (44.68 ± 0.73). The cytotoxicity results depicted strong dose and timedependent toxicity of biogenic MC-AgNPs against cancer cell lines fifty percent inhibitory concentration MC-AgNPs against HeLa cells were 13.56 ± 1.22 μg/mL after 24h and 5.57 ± 0.12 μg/mL after 48 h exposure, likewise 16.86 ± 0.88 μg/mL and 11.60 ± 0.97 μg/mL respectively for MCF-7 cells. The present study revealed the green synthesis of silver nanoparticles using M. citrifolia and their significant antioxidant, antibacterial and anticancer activities.

Synthesis and biological evaluation of novel 3,6- amide and thioamide substituted- 2,3,4,9-tetrahydro-1H-carbazoles for anti-cancer activity

Herein, we report the synthesis of new compounds with demonstrated anticancer properties based on the 2,3,4,9-tetrahydro-1H-carbazole scaffold. The Fischer indolization method was used to close the heterocyclic motif. The synthesis method's scope and limitations were thoroughly assessed through a series of experiments. Biological assays revealed that two thioamide compounds exhibited significant anticancer activity against MCF-7, HTC116, and A596 cell lines. Comprehensive in vitro profiling included evaluation of cell cytotoxicity, morphological alterations, colony formation and cell adhesion in 3D cultures, cell cycle analysis, DNA damage induction, impact on mitochondria, and apoptosis. Ex ovo studies further demonstrated these compounds' potential to inhibit angiogenic processes. Our results indicate that the newly developed compounds activate processes leading to DNA damage and disruption of mitochondrial function.

Multifunctional Characterization and Anticancer Properties of Magnetic Zinc Ferrite Nanoparticles by Modified Ultrasonic Assisted Co-precipitation Method

Zinc Ferrite (ZnFe2O4) nanoparticles were synthesized successfully via the modified ultrasonic-assisted co-precipitation method. Structural characterization, conducted through X-ray diffraction (XRD) analysis and Rietveld refinement, revealed a single cubic phase with a mixed spinel structure. Fourier transform infrared spectroscopy confirmed the presence of functional groups indicative of the spinel ferrite structure. Morphological analysis using field-emission scanning electron microscopy showcased the nanoparticles’ uniform morphology and size distribution. UV–vis spectra revealed the optical properties, while the Tauc Plot method determined the optical band gap. Electron paramagnetic resonance spectra confirm the symmetric resonance peak with 1254 Oe line width and the Lande g value 2.133. Magnetic hysteresis loops confirm the soft magnetic nature of the nanoparticles with magnetic saturation and coercivity of 39.2 emu gm−1 and 77.5 Oe. The anticancer properties against various cancer cell lines (HeLa, HepG-2 and MCF-7) revealed significant anticancer activity against HepG-2 and HeLa cells compared to MCF-7 cancer cells, and the results were compared with the standard drug cisplatin. A comparative analysis of results among cancer cell lines was conducted and discussed.

Developing Supramolecular metallogel derived from Pd2L4 Cage Molecule for Delivering an Anti-cancer Drug to Melanoma Cell B16-F10.

Supramolecular gels are an important class of materials that are promising for its wide range of applications including drug delivery. While supramolecular gels are intrinsically porous because of the 3D nano-matrix (gel matrix) that is being formed due to supramolecular self-assembly process involving the gelator molecules during gelation, additional nanopores can be introduced to the overall gel if the gelator molecule itself holds molecular cavity such as metal-organic-cage (MOC) molecules. A MOC having the molecular formula [(Pd2L24).4NO3].3H2O.2DMF.MeOH (Pd-cage) (L2=5-Azido-N,N'-di-pyridin-3-yl-isophthalamide) was successfully synthesized and characterized by FT-IR, 1H NMR, ESI-MS and single crystal X-ray diffraction. Stimuli-reversible supramolecular metallogel PdG could easily be formed from Pd-cage in DMSO/water mixture. The molecular cage of Pd-cage was demonstrated to be available for loading an anti-cancer drug namely doxorubicin (DOX). Subsequently, DOX was also loaded within PdG and delivered to melanoma cell line B16-F10 displaying significant anti-cancer activity as revealed by both MTT and scratch assay. Rheoreversibility of PdG and its ability to load and deliver DOX to cancer cells clearly raised hope for developing this metallogel further as topical anticancer gel.

Metabolomic insights and bioactive efficacies of Tragopogon dubius root fractions: Antioxidant and antiproliferative assessments

Tragopogon dubius is commonly consumed as a vegetable and used in traditional medicine for treating inflammatory skin conditions and cutaneous swelling. Despite known pharmacological properties of its leaves and roots, many of its biological characteristics and active phytochemicals remain unexplored. The present study investigates the phytochemical composition, antioxidant, and anticancer properties of methanolic root extracts and isolated fractions (TdRM-1 and TdRM-2) of T. dubius. Utilizing preparative thin-layer chromatography, the crude extract was successfully separated into TdRM-1 and TdRM-2, characterized by GC-MS and FTIR analysis, revealing a diverse range of bioactive compounds including terpenes, flavonoids, and phenolic acids. Qualitative phytochemical screening indicated the presence of carbohydrates, tannins, alkaloids, and other phytoconstituents. Advanced UPLC-ESI-QTOF-MS analysis identified 54 metabolites, significantly contributing to the chemical profiling of the extract. The antioxidant activities of the fractions were quantitatively assessed using ABTS, DPPH, and superoxide radical scavenging assays, where TdRM-2 exhibited superior activity with IC50 values ranging from 51.29 to 60.03 μg/mL. Anticancer potential was evaluated against A549, LN-18, and MCF-7 cancer cell lines, demonstrating that TdRM-2 significantly inhibited cell proliferation with GI50 values as low as 31.62 μg/mL for A549 cells. Additionally, fluorescence microscopy revealed that TdRM-2 induces apoptosis, indicated by changes in nuclear morphology and loss of mitochondrial membrane potential. Annexin V-FITC/PI double staining indicate that the TdRM-2 fractions from T. dubius can significantly inhibit the growth of A-549, LN-18, and MCF-7 cancer cell lines by inducing apoptosis These findings suggest that T. dubius root extracts, particularly the TdRM-2 fraction, hold promising therapeutic potential due to their significant antioxidant and anticancer activities, underpinned by their rich phytochemical composition. This study underscores the importance of T. dubius as a source of natural bioactive compounds with potential health benefits.

Synthesis, characterization and bioactivity of new pyridine-2(H)-one, nicotinonitrile, and furo[2,3-b]pyridine derivatives.

Pyridone heterocycles, such as furo[2,3-b]pyridines, have emerged as prominent scaffolds in medicinal chemistry due to their versatile pharmacological properties, including significant anticancer activity. In this study, we successfully synthesized new pyridine-2(H)-one, nicotinonitrile, and furo[2,3-b]pyridine derivatives from chalcones bearing 4-(benzyloxy)phenyl and dichlorothiophenyl subunits to explore their therapeutic potential against breast cancer. By employing a synthetic strategy involving Claisen-Schmidt condensation followed by sequential cyclizations and functional modifications, we synthesized and characterized four compounds (MI-S0, MI-S1, MI-S2, and MI-S3) using various spectroscopic methods, including FT-IR, 1H-NMR, 13C-NMR, DEPT, H,H- and C,H-COSY, and HRMS. The in vitro cytotoxic activity of these compounds was evaluated against two breast cancer cell lines, MCF-7 and MDA-MB-231, and compared with a noncancerous breast cell line, MCF-10A. All compounds exhibited potent cytotoxic activities with minimal selectivity toward normal cells. Molecular docking studies targeting the serine/threonine kinase AKT1, estrogen receptor alpha (ERα), and human epidermal growth factor receptor 2 (HER2) revealed strong binding affinities, suggesting a mechanism involving the disruption of key cellular signaling pathways. These findings underscore the potential of furo[2,3-b]pyridine derivatives as promising candidates for further development into anticancer agents, laying the groundwork for future investigations into their selective therapeutic efficacy and molecular mechanisms of action.

Quinazoline-oxindole hybrids as angiokinase inhibitors and anticancer agents: Design, synthesis, biological evaluation, and molecular docking studies.

Two new sets of quinazoline-oxindole 8a-l and quinazoline-dioxoisoindoline 10a-d hybrids were designed as type II angiokinase inhibitors and anticancer agents. The design strategy was adjusted to account for the quinazoline scaffold's placement in the target kinases' hinge region, where it would form hydrogen bonding and hydrophobic interactions with the important amino acids to stabilize it, and the amide group's occupation in the gate region, which would direct the oxindole scaffold toward the hydrophobic back pocket. The two sets of quinazolines 8a-l and 10a-d displayed pronounced inhibitory activity on VEGFR-2 (IC50 = 0.46-2.20 µM). The quinazoline-oxindole hybrids 8d, 8f, and 8h displayed IC50 = 0.46, 0.49, and 0.49 µM, respectively. Compound 8f demonstrated potent multikinase activity with IC50 values of 0.95 and 0.67 µM against FGFR-1 and BRAF, respectively. Additionally, compound 8f showed significant anticancer activity against National Cancer Institute's cancer cell lines, with GI50 reaching 1.21 µM. Analysis of the impact of compound 8f on the MDA-MB-231 cell line's cell cycle and apoptosis revealed that 8f stalled the cell cycle at the G2/M phase and promoted its necrosis.

Preparation, characterization, single-crystal analysis, and cytotoxic assessment of complexes formed by Schiff base and 8-hydroxyquinoline co-ligand with Co(II), Ni(II), and Mn(II) metal ions

This study focuses on the preparation of mixed ligand complexes of Ni(II), Co(II), and Mn(II) by combining the co-ligands 2-(((4-fluorophenyl)imino)methyl)-4-methoxy-6-nitrophenol (L1) and 8-hydroxyquinoline (L2). The chemical structures of the all compounds were examined using various techniques, including 1H and 13C NMR, FT-IR, UV–Vis, TGA, molar conductivity, LC-MS/MS, elemental analysis and magnetic susceptibility. The crystal structure of the ligand L1 was determined using single crystal X-ray analysis revealing that the ligand favors the phenol-imine tautomeric form in the solid state. All complexes are suggested to have an octahedral structure. Finally, the MTT assay was used to determine the toxicity level of the mixed ligand complexes in human non-small cell lung cancer (A549) and normal bronchial epithelial cell lines (BEAS-2B). The results showed that the [Ni(L1)(L2).(H2O)2] complex (IC50: 5.97 µM) exhibited high cytotoxic activity at a lower dose than cisplatin compared to the other compounds. In contrast, the [Ni(L1)(L2).(H2O)2] complex was shown to exhibit significantly lower cytotoxic activity (IC50 > 100 s µM) in the BEAS-2B (normal bronchial epithelial cell) cell line. The other compounds [Co(L1)(L2).(H2O)2] and [Mn(L1)(L2).(H2O)2] were shown to have no significant anticancer activity in A549 cells due to their cytotoxic activity at higher doses than cisplatin (IC50 > 100 s µM).

The LDHC-STAT3 Signaling Network Is a Key Regulator of Basal-like Breast Cancer Cell Survival.

Breast cancer treatment has evolved drastically with the addition of immunotherapy and novel targeted drugs to the current treatment options. However, achieving long-term responses with minimal adverse events remains challenging. Cancer testis antigens (CTAs) offer novel opportunities for drug development thanks to their tumor specificity, immunogenicity, pro-tumorigenic functions, and negative prognostic connotations. We previously reported that lactate dehydrogenase C (LDHC) plays a key role in regulating genomic stability and that targeting LDHC significantly improved treatment response to DNA damage response drugs in breast cancer. Here, we explored the molecular mechanisms associated with LDHC silencing in two basal-like breast cancer cell lines, MDA-MB-468 and BT-549, and a Her2-enriched breast cancer cell line, HCC-1954. Transcriptomic analyses identified the cell line-dependent differential activation of the pro-survival STAT3 pathway following LDHC depletion. While LDHC silencing significantly compromised cell survival in basal-like breast cancer cells in conjunction with a downregulation of STAT3 signaling, the opposite effect was observed in Her2-enriched breast cancer cells, which demonstrated the enhanced activation of the pro-survival STAT3 signaling pathway. The inhibition of STAT3 not only reversed the unfavorable effect of LDHC silencing in the Her2-enriched cancer cells but also demonstrated significant anti-cancer activity when used as a single agent. Our findings suggest that the LDHC-STAT3 signaling axis plays a role in regulating breast tumor cell survival in a subtype-dependent manner. Thus, LDHC-targeted therapy could be a viable therapeutic approach for a subset of breast cancer patients, particularly patients with basal-like breast cancer, whereas patients carrying Her2-enriched tumors may likely benefit more from monotherapy with STAT3 inhibitors.

Omeprazole-Loaded Copper Nanoparticles for Mitochondrial Damage Mediated Synergistic Anticancer Activity against Melanoma Cells.

Metallic nanoparticles are promising candidates for anticancer therapies. Among the different metallic systems studied, copper is an affordable and biologically available metal with a high redox potential. Copper-based nanoparticles are widely used in anticancer studies owing to their ability to react with intracellular glutathione (GSH) to induce a Fenton-like reaction. However, considering the high metastatic potential and versatility of the tumor microenvironment, modalities with a single therapeutic agent may not be effective. Hence, to enhance the efficiency of chemotherapeutic drugs, repurposing them or conjugating them with other modalities is essential. Omeprazole is an FDA-approved proton pump inhibitor used in clinics for the treatment of ulcers. Omeprazole has also been studied for its ability to sensitize cancer cells to chemotherapy and induce apoptosis. Herein, we report a nanosystem comprising of copper nanoparticles encapsulating omeprazole (CuOzL) against B16 melanoma cells. The developed nanoformulation exerted significant synergistic anticancer activity when compared with either copper nanoparticles or omeprazole alone by inducing cell death through excessive ROS generation and subsequent mitochondrial damage.

Design and synthesis of magnesium and palladium hybrid nanoparticles using Cyperus rotundus: An assessment of antimicrobial and anticancer applications

Multidrug resistance is an instance of the increased use of traditional drug therapy, which includes the consumption of antibiotics and anticancer drugs. It will take alternative treatments to overcome this obstacle. Nanoparticles that are biosynthesized are extensively used to address a range of illnesses. This study aims to investigate the aqueous extracts of Cyperus rotundus used to biosynthesis hybrid nanoparticles using magnesium (Mg) and palladium (Pd) nanoparticles (NPs). Herein, different characterization techniques are used to the reveal desired physiochemical properties and potential biomedical applications of the biosynthesized NPs. With the use of centre composite design (CCD), the most significant parameters and their interactions that are likely to affect nanoparticle synthesis were assessed and identified in order to improve the quality of the experiments. The Mg/Pd NPs exhibit exerting antimicrobial activity against Gram positive and Gram negative bacterial and fungal pathogens. Significant anticancer activity was observed in the biogenic hybrid NPs against the human hepatocellular carcinoma (HuH-7) cell line. In silico molecular docking studies confirmed strong binding interactions of D-Glucose cyclic 1, 2-ethandiylmercaptal pentaacetate compound with the HuH-7 cancer cell line, as well as with EGFR tyrosine kinase inhibitor resistance and Bcl2 gene target proteins. The findings also point to intriguing possibilities for incorporating C. rotundus extract-assisted hybrid nano-biosynthesis, which is crucial for developing cutting-edge nanomedicines.

Synthesis and Evaluation of Gelatin-Chitosan Biofilms Incorporating Zinc Oxide Nanoparticles and 5-Fluorouracil for Cancer Treatment.

In this study, a novel multifunctional biofilm was fabricated using a straightforward casting process. The biofilm comprised gelatin, chitosan, 5-fluorouracil (5-FU)-conjugated zinc oxide nanoparticles, and polyvinyl alcohol plasticized with glycerol. The 5-FU-conjugated nanoparticles were synthesized via a single-step co-precipitation process, offering a unique approach. Characterization confirmed successful drug conjugation, revealing bar-shaped nanoparticles with sizes ranging from 90 to 100 nm. Drug release kinetics followed the Korsmeyer-Peppas model, indicating controlled release behavior. Maximum swelling ratio studies of the gelatin-chitosan film showed pH-dependent characteristics, highlighting its versatility. Comprehensive analysis using SEM, FT-IR, Raman, and EDX spectra confirmed the presence of gelatin, chitosan, and 5-FU/ZnO nanoparticles within the biofilms. These biofilms exhibited non-cytotoxicity to human fibroblasts and significant anticancer activity against skin cancer cells, demonstrating their potential for biomedical applications. This versatility positions the 5-FU/ZnO-loaded sheets as promising candidates for localized topical patches in skin and oral cancer treatment, underscoring their practicality and adaptability for therapeutic applications.

Ergosterol and its metabolites as agonists of Liver X receptor and their anticancer potential in colorectal cancer

Aberrant cholesterol homeostasis is a well-recognized hallmark of cancer and is implicated in metastasis as well as chemotherapeutic resistance, the two major causes of cancer associated mortality. Liver X receptors (LXRs) are the key transcription factors that induce cholesterol efflux via enhancing the expression of ABCA1 and ABCG1. Therefore, a comprehensive analysis of several novel sterols namely ergosta-7,22,24(28)-trien-3β-ol (Erg1), ergosta-5,22,25-trien-3-ol (Erg2), ergosta-5,7,22,24(28)-tetraen-3β-ol (Erg3), and ergosta-7,22-dien-3β-ol (Erg4) as LXR agonists has been performed. Molecular docking studies have shown that these sterols possess higher binding affinities for LXRs as compared to the reference ligands (GW3965 and TO901317) and also formed critical activating interactions. Molecular dynamic (MD) simulations further confirmed that docking complexes made of these sterols possess significant stability. To assess the extent of LXR activation, ABCA1 promoter was cloned into luciferase reporter plasmid and transfected into HCT116 cells. It was observed that treatment with Erg, Erg2 and Erg4 led to a significant LXR activation with an EC50 of 5.64 µM, 4.83 and 3.03 µM respectively. Furthermore, a significant increase in mRNA expression of NR1H2 and LXR target genes i.e. ABCA1, ABCG1 and ApoE was observed upon Erg treatment. Flow cytometric analysis have revealed a significant increase in the accumulation of ABCA1 upon Erg treatment. Cytotoxicity studies conducted on colorectal cancer cell and normal epithelial cell line showed that these sterols are selectively toxic towards cancer cells. Taken together, our findings suggests that ergosterol activates LXRs, have significant anticancer activity and could be a likely candidate to manage aberrant cholesterol homeostasis.

Click estradiol dimers with novel aromatic bridging units: synthesis and anticancer evaluation

Estradiol dimers (EDs) possess significant anticancer activity by targeting tubulin dynamics. In this study, we synthesised 12 EDs variants via copper-catalysed azide-alkyne cycloaddition (CuAAC) reaction, focusing on structural modifications within the aromatic bridge connecting two estradiol moieties. In vitro testing of these EDs revealed a marked improvement in selectivity towards cancerous cells, particularly for ED1–8. The most active compounds, ED3 (IC50 = 0.38 μM in CCRF-CEM) and ED5 (IC50 = 0.71 μM in CCRF-CEM) demonstrated cytotoxic effects superior to 2-methoxyestradiol (IC50 = 1.61 μM in CCRF-CEM) and exhibited anti-angiogenic properties in an endothelial cell tube-formation model. Cell-based experiments and in vitro assays revealed that EDs interfere with mitotic spindle assembly. Additionally, we proposed an in silico model illustrating the probable binding modes of ED3 and ED5, suggesting that dimers with a simple linker and a single substituent on the aromatic central ring possess enhanced characteristics compared to more complex dimers.

Imperative Bioactive Metabolites from Portieria hornemannii Exhibiting Anticancer Potentiality: A Mini-Review

Abstract: Seaweeds are regarded as an important and alternative source of bioactive metabolites. It has recently come to the attention of researchers that marine algae have important physiologically active metabolites capable of displaying a range of biological activities, and the compounds extracted from seaweeds are known to target key molecules that control the processes leading to cancer. Cancer is one of the most common and potentially fatal diseases worldwide. It is characterised by uncontrolled proliferation of cells and tumour development. Every year, the global cancer burden is increasing progressively as a result of the ability of cancer cells to acquire resistance against existing chemotherapeutic drugs. Thus, there is a need to develop new drugs that could hamper this process leading to cancer. Marine-derived natural bioactive compounds pose as major potential candidates to develop such molecules. Portieria hornemannii, a marine macroalgae belonging to the group Rhodophyta found in coastal plains of Indo-Pacific regions, has shown the presence of a variety of bioactive compounds that show significant anticancer activities and antioxidant properties. A number of chemical compounds are found in this species, which results in the macroalgae having significant anticancer activity. Therefore, the primary focus of the review is to highlight the bioactive compounds found in P. hornemannii that exhibit such anticancer potential.

Synthesis of 2-Aryl Indazole: Synthesis, Biological Evaluationand In-Silico Studies.

In this work, a highly effective synthesis technique for obtaining aryl indazole under mild circumstances is provided, using trimethyl phosphine as a powerful reagent. The procedure shows that a wide range of substrates can be investigated, yielding various 2-aryl indazole derivatives with acceptable to exceptional yields and a wide range of functional group tolerance. Additionally, based on In Silico studies tests were conducted to determine the anticancer activity In Vitro for all produced compounds (3 a-3 j) against A549, HT-29 and HepG2 cell lines. Compounds 3 c and 3 d, with IC50 values of 15, 53.55, 7.34, 7.10, 56.28, and 17.87 (μM) against A549, HT-29 and HepG2 respectively, showed significant anticancer activity.

Characterization of Polysaccharide Extracts of Four Edible Mushrooms and Determination of In Vitro Antioxidant, Enzyme Inhibition and Anticancer Activities.

Mushroom polysaccharides are important bioactive compounds derived from mushrooms with various beneficial properties. In this study, the chemical characterization and bioactivities of polysaccharide extracts from four different edible mushrooms, Clavariadelphus truncatus Donk, Craterellus tubaeformis (Fr.) Quél., Hygrophorus pudorinus (Fr.) Fr., and Macrolepiota procera (Scop.) Singer were studied. Glucose (13.24-56.02%), galactose (14.18-64.05%), mannose (2.18-18.13%), fucose (1.21-5.78%), and arabinose (0.04-5.43%) were identified in all polysaccharide extracts by GC-MS (gas chromatography-mass spectrometry). FT-IR (Fourier transform infrared spectroscopy) confirmed the presence of characteristic carbohydrate patterns. 1H NMR suggested that all polysaccharide extracts had α- and β-d-mannopyranose, d-glucopyranose, d-galactopyranose, α-l-arabinofuranose, and α-l-fucopyranose residues. Approximate molecular weights of polysaccharide extracts were determined by HPLC (high-performance liquid chromatography). The best antioxidant activity was found in M. procera polysaccharide extract in DPPH• (1,1-diphenyl-2-picrylhydrazyl) scavenging (39.03% at 800 μg/mL), CUPRAC (cupric reducing antioxidant capacity) (A0.50: 387.50 μg/mL), and PRAP (phosphomolybdenum reducing antioxidant power) (A0.50: 384.08 μg/mL) assays. C. truncatus polysaccharide extract showed the highest antioxidant activity in ABTS•+ scavenging (IC50: 734.09 μg/mL), β-carotene-linoleic acid (IC50: 472.16 μg/mL), and iron chelating (IC50: 180.35 μg/mL) assays. Significant anticancer activity was found in C. truncatus polysaccharide extract on HT-29 (IC50: 46.49 μg/mL) and HepG2 (IC50: 48.50 μg/mL) cell lines and H. pudorinus polysaccharide extract on the HeLa cell line (IC50: 51.64 μg/mL). Also, H. pudorinus polysaccharide extract possessed prominent AChE (acetylcholinesterase) inhibition activity (49.14% at 200 μg/mL).