High Anticancer Activity Research Articles

Phytochemical Composition and Characterization of In Vitro Bioactivities from Pinus Using Green Process

Pinus species are notable in Mediterranean regions due to their ecological and economic importance. Various parts of these species are widely used in traditional medicine, especially pinecones, which are a significant source of bioactive compounds. The current study aimed to evaluate the phytochemical composition and biological properties of the aqueous extracts obtained by maceration from three Pinus petal fractions, from P. halepensis Mill., P. brutia Ten., and P. pinea L. (APW, BPW, and PPW respectively), and the core fractions of the same species (ACW, BCW, and PCW respectively). The results showed that APW demonstrated superior performance compared to other species and fractions (p ≤ 0.05), with the highest total polyphenol content (203.51 mg GAE/g DW) and the highest antioxidant potential (IC50 = 13.51 µg/mL) against DPPH free radical. All extracts showed high anticancer activity against HeLa and HepG2 cancer cell lines, and low inhibition against HEK-293, a normal cell line (<15%), indicating that none of extracts have any toxicity effect. Furthermore, only APW exhibits a significant inhibition against α-glucosidase with 77.20% at 50 µg/mL. HPLC-DAD analysis was conducted to identify 14 compounds. GC-MS analysis was conducted to identify 28 compounds, of which 11 were detected for the first time in this species. This study offers valuable insights into phytochemistry and potential therapeutic applications of pinecones.

Repurposing the antipsychotic drug penfluridol for cancer treatment (Review).

Cancer is one of the most prevalent diseases and the leading cause of death worldwide. Despite the improved survival rates of cancer in recent years, the current available treatments often face resistance and side effects. Drug repurposing represents a cost‑effective and efficient alternative to cancer treatment. Recent studies revealed that penfluridol (PF), an antipsychotic drug, is a promising anticancer agent. In the present study, a scoping review was conducted to ascertain the anticancer properties of PF. For this, a literature search was performed using the Scopus, PubMed and Web of Science databases with the search string 'penfluridol' AND 'cancer'. A total of 23 original articles with in vivo and/or in vitro studies on the effect of PF on cancer were included in the scoping review. The outcome of the analysis demonstrated the anticancer potential of PF. PF significantly inhibited cell proliferation, metastasis and invasion while inducing apoptosis and autophagy in vivo and across a spectrum of cancer cell lines, including breast, lung, pancreatic, glioblastoma, gallbladder, bladder, oesophageal, leukaemia and renal cancers. However, research on PF derivatives with high anticancer activities and reduced neurological side effects may be necessary.

Antibacterial and anticancer potential of bioactive compounds and secondary metabolites of endophytic fungi isolated from Anethum graveolens.

Fungal endophytes are known to produce bioactive chemicals and secondary metabolites that are often identical to those produced by their host plants. The main objective of the current study was to isolate and identify endophytic fungi associated with the medicinal plant Anethum graveolens, and to investigate their potential antibacterial and anticancer properties. The ethyl acetate extracts from the isolated endophytic fungi, as well as the host plant A. graveolens, were subjected to bioactivity assays to evaluate their antibacterial and anticancer potential against multi-drug resistant bacterial strains and the human hepatocellular carcinoma cell line HepG2. The endophytic fungi isolated and identified from the A. graveolens samples included Diaporthe, Auxarthron, Arthrinium, Aspergillus, Microsporum, Dothiorella, Trichophyton, Lophiostoma, Penicillium, and Trichoderma species. The minimum inhibitory concentration (MIC) assay revealed that the A. graveolens extract exhibited the strongest antibacterial activity, with an MIC value of 4 μg/ml, followed by the Trichoderma sp. (5 μg/ml) and Penicillium sp. (6 μg/ml) extracts. Additionally, the crude extracts of Trichoderma sp., Penicillium sp., and Fusarium sp. demonstrated high anticancer activity against HepG2 cells, with inhibition rates ranging from 89 to 92% at a concentration of 50 μg/ml. Interestingly, the A. graveolens extract showed the most potent anticancer activity, with a 95% inhibition rate against HepG2 cells at the same concentration. These findings highlight the significant potential of endophytic fungi associated with A. graveolens, as a source of bioactive compounds with promising antibacterial and anticancer properties. The results reinforce the hypothesis that medicinal plants and their endophytic fungi can serve as an attractive alternative for the development of novel therapeutic agents, potentially offering a more sustainable and less harmful approach to disease management compared to traditional chemical-based methods.

Examination of Biological Activity of Passiflora edulis (Çarkıfelek) Extract via Phytochemical Analysis

In recent years, the use of medicinal plants as sources of drugs or herbal extracts has been of great importance. Passiflora edulis is nowadays widely studied for its antimicrobial, anticancer, and antioxidant potential. Therefore, this study aimed to determine the phytochemical structure of ethanol extract of P. edulis leaves and to investigate its biological properties such as antimicrobial and anticancer activities. The ethanol extract of P. edulis leaves was obtained and analyzed by GC-MS. The antimicrobial activity of P. edulis leaf extract was determined by MIC test. XTT method was used to determine the antiproliferative activity. In the phytochemical analysis of P. edulis extract, dodecanoic acid, tetradecanoic acid, and n-hexadecanoic acid were found the most. The antimicrobial effect of P. edulis leaf extract was found against pathogenic microorganisms. In addition, P. edulis leaf extract was found to have high anticancer activity against OvCar and MCF-7 cell lines, while it had the highest effect on the PC-3 cell line. It is thought that the effectiveness of this antiproliferative and antimicrobial activity is related to the secondary metabolites determined by GC-MS analysis

Oral delivery of Sunitinib malate using carboxymethyl cellulose/poly(acrylic acid-itaconic acid)/Cloisite 30B nanocomposite hydrogel as a pH-responsive carrier.

This work aimed to fabricate a Cloisite 30B-incorporated carboxymethyl cellulose graft copolymer of acrylic acid and itaconic acid hydrogel (Hyd) via a free radical polymerization method for controlled release of Sunitinib malate anticancer drug. The synthesized samples were characterized by FTIR, XRD, TEM, and SEM-dot mapping analyses. The encapsulation efficiency of Hyd and Hyd/Cloisite 30B (6 wt%) was 81 and 93%, respectively, showing the effectiveness of Cloisite 30B in drug loading. An in vitro drug release study showed that drug release from all samples in a buffer solution with pH 7.4 was higher than in a buffer solution with pH 5.5. During 240min, the cumulative drug release from Hyd/Cloisite 30B (94.97% at pH 7.4) is lower than Hyd (53.71% at pH 7.4). Also, drug-loaded Hyd/Cloisite 30B (6 wt%) demonstrated better antibacterial activity towards S. Aureus bacteria and E. Coli. High anticancer activity of Hyd/Cloisite 30B against MCF-7 human breast cancer cells was shown by the MTT assay, with a MCF-7 cell viability of 23.82 ± 1.23% after 72-hour incubation. Our results suggest that Hyd/Cloisite 30B could be used as a pH-controlled carrier to deliver anticancer Sunitinib malate.

Synthesis, spectral characterization, anti-cancer activity evaluation, and molecular docking of substituted 1,2-bis(3-butyl-2,6-diphenylpiperidin-4-ylidiene)hydrazone derivatives

A series of 1,2-bis(3‑butyl‑2,6-diphenylpiperidin-4-ylidiene)hydrazone derivatives of the substituted compounds 1–7, were confirmed by the characterization of IR & 1H-, NMR spectrum, together with X-ray crystallography and Mass spectroscopy also incredibly revealed. Docking analysis of the synthesized compounds employed under the protein from PDB code as 5cqh1, 4i40, 5fan, 7nud, 6Ya1 offers more inhibition values from 2D and 3D structures of the compounds, followed by Anti-cancer activity of the carcinoma cell line displayed that, highly potent to be active in nature. The in-vitro performance of -Cl substituted compound 6 (high anticancer activity) was in good correlation with its protein binding behaviour (strong binding). The increasing order of anticancer effect was 5>7>1>2>4>3>6 and the increasing order of binding ability on proteins were 7>3>4>1>2>5>6. The computational investigations were aligned with experimental techniques using Density Functional Theory (DFT) with a 6–31 G (d, p) basis set. Calculated Highest Occupied Molecular Orbital (HOMO) and Lowest Unoccupied Molecular Orbital (LUMO) energies revealed Mulliken charges and charge transfer phenomena occurring within the molecule. Analysis of the Molecular Electrostatic Potential (MEP) unveiled reactive sites, with high electron density regions depicted in red and low electron density regions in blue.

A Novel Tetravalent Bispecific Immune Cell Engager Activates Natural Killer Cells to Kill Cancer Cells without Mediating Fratricide.

We previously reported the structure, affinity, and anticancer activity of a bivalent bispecific natural killer cell engager (BiKE) composed of one anti-CD16a VHH and one anti-HER2 VHH fused via a linker. In this study, we explored the engineering of a tetravalent BiKE by fusing two anti-CD16a and two anti-HER2 VHHs in tandem, using bivalent BiKE as a template. The tetravalent BiKE was genetically engineered, and its tertiary structure was predicted using in silico modeling. The antigen binding and affinity of the tetravalent BiKE were assessed using ELISA, flow cytometry, and biolayer interferometry. The ability of the BiKEs to kill cancer cells was evaluated through classical and residual antibody-dependent cellular cytotoxicity (ADCC) assays. Additionally, we investigated the potential for NK cell fratricide via CD16a-CD16a crosslinking. Our results revealed that the tetravalent BiKE exhibited at least 100-fold higher affinity toward its target antigens compared to its bivalent counterpart. The residual ADCC assay indicated that the tetravalent BiKE was more effective in killing cancer cells than the bivalent BiKE, attributable to its lower Koff value, which prolonged its binding to NK cell surfaces. Fratricide assays demonstrated that neither the bivalent nor the tetravalent BiKE mediated fratricide. Notably, our findings showed that daratumumab-induced NK fratricide was restricted to CD38-CD38 crosslinking and was not related to ADCC via CD16a-CD38 crosslinking. This study is the first in the literature to show the successful engineering of a tetravalent immune cell engager composed of tandem VHH units, which achieves high affinity and anticancer activity without mediating fratricide.

A Minor Groove Binder with Significant Cytotoxicity on Human Lung Cancer Cells: The Potential of Hesperetin Functionalised Silver Nanoparticles.

Natural drug functionalised silver (Ag) nanoparticles (NPs) have gained significant interest in pharmacology related applications due to their therapeutic efficiency. We have synthesised silver nanoparticle using hesperetin as a reducing and capping agent. This work aims to discuss the relevance of the hesperetin functionalised silver nanoparticles (H-AgNPs) in the field of nano-medicine. The article primarily investigates the anticancer activity of H-AgNPs and then their interactions with calf thymus DNA (ctDNA) through spectroscopic and thermodynamic techniques. The green synthesised H-AgNPs are stable, spherical in shape and size of 10 ± 3nm average diameter. The complex formation of H-AgNPs with ctDNA was established by UV-Visible absorption, fluorescent dye displacement assay, isothermal calorimetry and viscosity measurements. The binding constants obtained from these experiments were consistently in the order of 104 Mol-1. The melting temperature analysis and FTIR measurements confirmed that the structural alterations of ctDNA by the presence of H-AgNPs are minimal. All the thermodynamic variables and the endothermic binding nature were acquired from ITC experiments. All these experimental outcomes reveal the formation of H-AgNPs-ctDNA complex, and the results consistently verify the minor groove binding mode of H-AgNPs. The binding constant and limit of detection of 1.8μM found from the interaction studies imply the DNA detection efficiency of H-AgNPs. The cytotoxicity of H-AgNPs against A549 and L929 cell lines were determined by in vitro MTT cell viability assay and lactate dehydrogenase (LDH) assay. The cell viability and LDH enzyme release are confirmed that the H-AgNPs has high anticancer activity. Moreover, the calculated LD50 value for H-AgNPs against lung cancer cells is 118.49µl/ml, which is a low value comparing with the value for fibroblast cells (269.35µl/ml). In short, the results of in vitro cytotoxicity assays revealed that the synthesised nanoparticles can be considered in applications related to cancer treatments. Also, we have found that, H-AgNPs is a minor groove binder, and having high DNA detection efficiency.

Construction and anti-pancreatic cancer activity of selenium nanoparticles stabilized by Prunella vulgaris polysaccharide

Selenium nanoparticles (SeNPs), as a potential cancer therapeutic agent, have attracted extensive attention due to their high anticancer activity and low toxicity. Polysaccharides could be the modifiers and stabilizers to improve the stability and dispersibility of SeNPs in aqueous solution. This study aimed to investigate the physicochemical characterization, stability, and anti-pancreatic cancer cell activities of SeNPs stabilized by a heteroxylan PVP3-1 extracted from the clusters of Prunella vulgaris Linn. Our results showed that PVP3-1 with Mw of 154 kDa was composed of →4)-β-D-Xylp(1→, →2, 4)-β-D-Xylp(1→, t-α-L-Araf(1→ and 4-MeO-α-D-GlcpA(1→. Red, zero-valent, and uniform spherical SeNPs with an average diameter of about 60 nm and high stability in aqueous solution were constructed successfully by polysaccharide PVP3-1. Anti-pancreatic cancer cell activity assays showed that PVP3-1-SeNPs could inhibit the proliferation and migration of pancreatic cancer cells in vitro. Furthermore, PVP3-1-SeNPs induced apoptosis and autophagy of pancreatic cancer cells through inhibiting mTOR signaling pathway. In conclusion, these results indicated that PVP3-1-SeNPs could be potential anti-tumor nanoparticles for treating pancreatic cancer.

Expeditious assembly of N-heteroaryl substituted quercetin derivatives as potent anticancer agents

The synthesis of a small library of N-heteroaryl substituted quercetin derivatives (28 compounds) at the C8 position applying Suzuki-Miyaura cross-coupling reaction between 8-iodoquercetin methyl ether and various pyridylboronic acids or quinolylboronic acids is reported. The obtained quercetin derivatives 2a-2n and 3a-3n were well characterized by the 1H NMR, 13C NMR and HRMS data. Preliminary biological evaluations showed that some of the synthesized 8-heteroarylated quercetin derivatives possessed very high anti-cancer cell proliferation activity in HCC827 cancer cell line (IC50< 5.0 µmol/L) in vitro. Among these synthesized compounds, quinolin-7-yl substituted compound 2m exhibited best activity in HCC827 (IC50 = 3.20 µmol/L), while quinolin-3-yl substituted compound 2i showed best activity in MGC-803 cells (IC50 = 14.92 µmol/L). The 3-pyridyl compound 3c with ortho-fluorine showed best activity in OVCAR-3 cells (IC50 = 10.67 µmol/L). The disclosed structure-activity relationship provides hints that large steric hindrance at the C8 position of quercetin alter the anticancer activities and also offers new examples for new application of electronic and steric modifications as versatile tools in drug discovery.

Synthesis, spectroscopic analysis, molecular docking and DFT study of some new heterocyclic compounds tethered 4‑hydroxy-1-methylquinoline-2(1H)one

A diversity of heterocyclic compounds (3, 6–8, 9, 11 and 12) linked 4‑hydroxy-1-methylquinoline-2(1H)one moiety have been synthesized from ring opening ring closure reaction (RORC) of 4‑hydroxy-6-methyl-3-nitro-2H-pyrano[3,2-c]quinoline-2,5(6H)‑dione (2) with various nucleophilic reagents namely hydrazine hydrate, phenylhydrazine, 3-hydrazino-5,6-diphenyl-1,2,4-triazine (4), 7‑chloro-4-hydrazino quinoline (5), 3-amino-1,2,4-triazole, 2-aminobenzimidazole and 3-amino-4,6-dimethyl-1H-pyrazolo[3,4-b]pyridine (10). The biological efficiency of the synthesized compounds against hepatocellular carcinoma cell lines (HepG-2) was analyzed both experimentally and theoretically (topoisomerase IIβ protein). Compound 12 (IC50=4.36 µM/L) has the highest anticancer activity against HepG-2 cell lines in comparison with the positive control (Cis-platin). The synthesized compounds were optimized by DFT/B3LYP functionality using the 6–311G++(d,p) basis set. Frontier molecular orbital analysis using global reactivity parameters indicated that compounds 1 and 12 have the largest) ∆E = 4.268 eV) and smallest) ∆E = 3.344 eV) energy gap, respectively. Thus, compound 1 (η= 2.134 eV) is harder than other compounds and has high stability. While compound 12 (S = 0.598eV-1) is softer than other compounds and more reactive. MEP surface and Fukui function were used to show charge distribution and show reactive zones within the molecules. For further validate of the NMR results, GIAO method was utilized to evaluation the 1HNMR and 13CNMR chemical shifts which were then correlate with the experimental spectra. Non-linear optical (NLO) behavior was further studied and compared to urea, which is a prototype substrate, and found to be greater than that of urea. Swiss-ADME (absorption, distribution, metabolism and excretion) analysis was performed to examine the drug-likeness properties of the current compounds. Finally, using the topoisomerase IIβ protein (PDB ID: 4G0U) receptor, molecular docking studies were used to examine the binding interactions of the synthesized compounds and correlated with anticancer activity.

A Review of the Benefits of the Sustainable Utilization of Shrimp Waste to Produce Novel Foods and the Impact on Human Health

In recent years, there has been an increase in the industrial processing of shrimp, aiming to cover the increasing demand for shrimp products for human consumption, and, consequently, an increase in shrimp by-products as shrimp waste. This waste includes the cephalothoraxes, heads, shells, tails, pleopods, and exoskeleton appendages of processed shrimps. The appropriate method for the enzymatic hydrolysis of shrimp waste can recover its bioactive substances, including carotenoids. Thus, these xanthophylls and carotenes are of high financial interest and have high antioxidant, anti-inflammatory, and anti-cancer activities. Therefore, these substances can be incorporated into fish feed as ingredients that improve fish health and simultaneously lead to the production of aquaculture fishes similar in coloration to the wild ones. Thus, the consumption of such novel food acts as a preventive factor for human health. In this regard, β-carotene has antioxidant and fat-soluble activities owing to vitamin A sufficiency and has an anti-cancer effect, too. Canthaxanthin can be used as a product for personal care and as a natural tanning agent for human skin. Zeaxanthin and lutein have positive effects on various eye and heart diseases, neuronal damage, human skin diseases, and certain types of cancer. Astaxanthin also has anti-diabetic and anti-obesity properties. Therefore, the purpose of this review is to highlight the sustainable utilization of shrimp waste via enzymatic hydrolysis, the benefits of a fish diet enriched with astaxanthin, the consumption of fish enriched with carotenoids, and the effects of carotenoids on human health. The problem of shrimp waste disposal affects the environment, does not contribute to sustainable development, and is directly related to the phenomenon of environmental change.

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.

Design, synthesis, crystal structure and anticancer activity of organotin(IV)-rhein carboxylates

Two new rhein-organotin complexes Ph3Sn(O2CC14H7O4) (RS01) and Cy3Sn(O2CC14H7O4) (RS02) were synthesized and characterized by elemental analysis, IR, 1H NMR, 13C NMR, 119 Sn NMR, X-ray crystallography and thermo-gravimetric analysis. Both complexes has a triclinic crystal system P-1 space group and one-dimensional supramolecular chain structure. The MTT results demonstrated that rhein's anticancer activity was effectively increased by introducing organotin, RS01 and RS02 exhibited excellent anticancer activity in vitro, significantly superior to cisplatin and mitoxantrone. Interestingly, despite the fact that RS01 and mitoxantrone share the same 9,10-anthraquinone scaffold structure, RS01 not only showed high anticancer activity but also much lower nephrotoxicity than mitoxantrone. Flow cytometry showed that RS01 could significantly induce cell apoptosis and arrest cell cycle in G2 phase. Molecular docking and UV–Vis absorption spectra suggested that RS01 may be intercalation with DNA. Furthermore, western blot results showed that RS01 activated the DNA damage critical protein γ-H2AX and regulated the expression level of the mitochondrial apoptotic pathway critical protein (Bax/Bcl-2). Thus, RS01 induced cell death may be mediated through DNA damage and mitochondrial pathways. As a result, RS01 has significant development and application potential as an anticancer agent.

Synthesis and Characterization of Chemically and Green-Synthesized Silver Oxide Particles for Evaluation of Antiviral and Anticancer Activity.

Silver oxide (Ag2O) particles are wonderful candidates due to their unique properties, and their use in a wide range of research, industrial and biomedical applications is rapidly increasing. This makes it fundamental to develop simple, environmentally friendly methods with possible scaling. Herein, sodium borohydride and Datura innoxia leaf extract were applied as chemical and biological stabilizing and reducing agents to develop Ag2O particles. The primary aim was to evaluate the anticancer and antiviral activity of Ag2O particles prepared via two methods. XRD, UV-visible and SEM analyses were used to examine the crystallite structure, optical properties and morphology, respectively. The resulting green-synthesized Ag2O particles exhibited small size, spherically agglomerated shape, and high anticancer and antiviral activities compared to chemically synthesized Ag2O particles. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium-bromide) assay of green-synthesized Ag2O particles showed high anticancer activity against MCF-7 cells with IC50 = 17.908 µg/mL compared to chemically synthesized Ag2O particles with IC50 = 23.856 µg/mL. The antiviral activity of green-synthesized Ag2O particles and chemically synthesized Ag2O particles was also evaluated by a plaque-forming assay, and green-synthesized Ag2O particles showed higher antiviral ability with IC50 = 0.618 µg/mL as compared to chemically synthesized Ag2O particles with IC50 = 6.129 µg/mL. We propose the use of green-synthesized Ag2O particles in cancer treatment and drug delivery.

Identification of mitochondrial ATP synthase as the cellular target of Ru-polypyridyl-β-carboline complexes by affinity-based protein profiling.

Ruthenium polypyridyl complexes are promising anticancer candidates, while their cellular targets have rarely been identified, which limits their clinical application. Herein, we design a series of Ru(II) polypyridyl complexes containing bioactive β-carboline derivatives as ligands for anticancer evaluation, among which Ru5 shows suitable lipophilicity, high aqueous solubility, relatively high anticancer activity and cancer cell selectivity. The subsequent utilization of a photo-clickable probe, Ru5a, serves to validate the significance of ATP synthase as a crucial target for Ru5 through photoaffinity-based protein profiling. Ru5 accumulates in mitochondria, impairs mitochondrial functions and induces mitophagy and ferroptosis. Combined analysis of mitochondrial proteomics and RNA-sequencing shows that Ru5 significantly downregulates the expression of the chloride channel protein, and influences genes related to ferroptosis and epithelial-to-mesenchymal transition. Finally, we prove that Ru5 exhibits higher anticancer efficacy than cisplatin in vivo. We firstly identify the molecular targets of ruthenium polypyridyl complexes using a photo-click proteomic method coupled with a multiomics approach, which provides an innovative strategy to elucidate the anticancer mechanisms of metallo-anticancer candidates.

WITHDRAWN: Folic acid Grafted, cell-penetrating peptide conjugated pH-sensitive hydrophobically modified Glycol chitosan nanoparticles for drug delivery in breast cancer

Nanocarriers are an outcome of the fast development of nanotechnology; however, delivering drugs to tumor sites effectively is still a major difficulty. A pH-responsive drug carrier with good cell penetration and targeting ability was developed to release the drug exactly to the cancer site and overcome these limitations.The drug carrier FA-TAT-HGCNPs/PTX, which is pH-responsive, uses folic acid (FA) and TAT peptide to deliver paclitaxel (PTX) for target folate-receptor-overexpressing breast cancer cells. 2-(diisopropylamino) ethyl methacrylate was connected to glycol chitosan (GC) to form HGCNPs. Then TAT and HGCNPs were conjugated and FA was grafted onto the HGCNPs’ hydroxyl group. Physicochemical characterizations of FA-TAT-HGCNPs was also evaluated. The maximum DLE and EE values of the FA-TAT-HGCNPs at pH 8.0 were 74.0 ± 2.22 % and 93.7 ± 2.8 %, respectively. FA-TAT-HGCNPs, for instance, showed stability during long-term storage and lyophilization while exhibiting pH-responsive dissociation properties. The synthesized drug carrier was characterized by FTIR, XRD, SEM, HRTEM, DLS, and Zeta analysis. MTT assay exhibited the high anticancer activity of the FA-TAT-HGCNPs/PTX against the MCF-7 cells, whereas drug-free ones are highly biocompatible. The pharmacokinetic results showed twice the bioavailability of FA-TAT-HGCNPs/PTX compared to HGCNPs/PTX. Unlike FA-HGCNPs/PTX, CLSM analysis showed that FA-TAT-HGCNPs/PTX had a significantly more efficient intracellular uptake in MCF-7 cells. These data have shown the transmembrane ability of TATpeptide,the targeting effects of folate decoration, and the synergistic interaction between them.According to these findings, PTX-loaded FA-TAT-HGCNPs offer a potentially effective nanoscale drug delivery system for the treatment of breast cancer.

In-vitro Antioxidant, In-vitro and In-silico Ovarian Anticancer Activity (Ovarian Cancer Cells-PA1) and Phytochemical Analysis of Cissus quadrangularis L. Ethanolic Extract.

Cissus quadrangularis is a valuable natural source of traditional medicines. An in vitro investigation was performed to determine whether the ethanolic extract from the whole portions of C. quadrangularis had anticancer and free radical scavenging activities against ovarian cancer cells-PA1. C. quadrangularis is a herb collected from rural areas in Andhra Pradesh, India. C. quadrangularis was air-dried and crushed, and the powder and ethanol (0.5 kg) were used in a Soxhlet device for continuous extraction. Phytochemical analysis of the extracts was performed using a standard procedure. The antioxidant activity of the ethanolic extract of C. quadrangularis was evaluated using DPPH. An in vitro anticancer study used an ethanolic extract against the PA1 cell line. Apoptosis of ovarian cancer cells was studied using DAPI and carboxy-H2DCFDA staining. From LC-MS analysis, quercetin-3-O-alpha-Lrhamnopyranoside and erucic acid were docked with the threonine tyrosine kinase (TTK) enzyme using auto docking. The ethanolic extract of C. quadrangularis demonstrated significant dose-dependent antioxidant activity compared to ascorbic acid. The ethanolic extract of C. quadrangularis was found to have high anticancer activity against ovarian cancer cell lines (PA1), with an IC50 value of 482.057 ± 113.857 μg/ml. DAPI and carboxy-H2DCFDA staining confirmed that C. quadrangularis ethanolic extract induced apoptosis in ovarian cancer cells (p < .001). Molecular docking studies helped identify the binding affinities between the protein and ligand complexes, such as Quercetin-3-O-alpha-Lrhamnopyranoside binding sites of target proteins 5N7V (MET602, GLN672) and erucic acid 5N7V (GLY354). Quercetin-3-O-alpha-L-rhamnopyranoside was reported to bind with 5N7V by hydrogen bonding at MET602 and GLN672 amino acids with 2.02, 2.99 Å bonding length distance and binding affinity of -7.9 kcal/mol. Erucic acid was reported to bind with 5N7V by hydrogen bonding at GLY354 amino acid with 3.18, 2.93 Å bonding length (Å) distance and binding affinity of -4.3 kcal/mol. The current analysis showed that the ethanolic extracts of C. quadrangularis L. exhibited antioxidant and anticancer properties against ovarian PA1 cells. The experimental results confirmed that C. quadrangularis L. is a promising, safe chemotherapeutic plant for ovarian cancer PA1 cells. The docking results demonstrated that Quercetin-3-O-alpha-L-rhamnopyranoside strongly binds threonine tyrosine kinase at the MET602 and GLN672 positions. This study showed that the C. quadrangularis ethanolic extract has Quercetin-3-O-alpha-L-rhamnopyranoside, which can be used as an anticancer agent.

High anticancer activity in short response time exhibited by a new azobenzene derivative and its copper complex

o‐Aminoazotoluene (OAT), capable of photoisomerization, and o‐vanillin, a potent comutagen, have been used to synthesize a new ligand, HL, [C6H4(CH3)N=NC6H3(CH3)N=CHC6H3(OH)(OCH3)], which, upon complexation with copper(II), results in a new copper(II) complex‐Cu(L)2, [Cu{C6H4(CH3)N=NC6H3(CH3)N=CHC6H3(OCH3)O}2]. Both HL and Cu(L)2 have been characterized by single‐crystal X‐ray diffraction measurements along with other analytical techniques, for example, IR spectroscopy, NMR spectroscopy, UV–Vis spectroscopy, elemental analysis and mass spectrometry. These compounds were tested with different in vitro anticancer assay as well as with in silico studies. A comparative study has been demonstrated on anticancer activity of HL and Cu(L)2 with the ligand HAZ, {C6H5N=NC6H4N=CHC6H3(OH)(OCH3)} and its Cu‐complex, [Cu(AZ)2, Cu{C6H5N=NC6H4N=CHC6H3(OCH3)O}2]. The sensing properties of HAZ, along with the synthesis and structural properties of both HAZ and Cu(AZ)2, have been reported by our group earlier. Cytotoxicity measurements on MCF7 cell lines show that Cu(L)2 and Cu(AZ)2 have higher anticancer activity than their corresponding ligands. The apoptotic effect of Cu‐complex was studied through nuclear fragmentation assay and AO/EB dual‐staining assay on MCF7 cell line. The IC50 value of Cu(L)2 in 0.01% DMSO/water after 24‐h treatment was found 4.2 μM, which is one of the lowest values with this response time compared to the other analogous anticancer compounds. Finally, we have evaluated the expression of hERα protein with respect to Cu‐complexes, and it was observed that Cu(L)2 caused more down‐regulation of hERα as compared to Cu(AZ)2.

The selective cytotoxicity effect of biosynthesized zinc oxide nanoparticles using honey

This work aims to produce biosynthesized zinc oxide nanoparticles using honey (Ho-ZnO-NPs). First, the process of characterization was completed using different techniques, including the color changing to light brown, Zeta-potential that shows a sharp peak at − 5.08 mV, Energy Dispersive X-ray (EDX), which represents the high percentage of Zinc (57.36 %), oxygen (35.03 %) and carbon (7.62 %), Transmission and Scanning Electron Microscopy (TEM and SEM) and X-ray Diffraction (XRD) analysis that illustrate the spherical and hexagonal structure. Then, the cytotoxicity activity was studied using an MTT assay on three cancer cell lines (MCF-7, HepG2, and A431) and an HSF normal cell line. Furthermore, the prepared nanoparticles Ho-ZnO-NPs show that the different IC50 are 118.1, 49.5, and 751.7 µg/mL for MCF-7, HepG2, and A431, respectively. In addition, IC50 is 1.47 mg/mL for HSF. In conclusion, the study reveals that the biosynthesized Ho-ZnO-NPs have higher anticancer activity against HepG2, plus their safety against normal skin cells.