Synthesis,Characterization, and Assessment of Anti-Cancer Potential of ZnO Nanoparticles in an In Vitro Model of Breast Cancer

Advanced innovations for combating variants of aggressive breast cancer and overcoming drug resistance are desired. In cancer treatment, ZnO nanoparticles (NPs) have the capacity to specifically and compellingly activate apoptosis of cancer cells. There is also a pressing need to develop innovative anti-cancer therapeutics, and recent research suggests that ZnO nanoparticles hold great potential. Here, the in vitro chemical effectiveness of ZnO NPs has been tested. Zinc oxide (ZnO) nanoparticles were synthesized using Citrullus colocynthis (L.) Schrad by green methods approach. The generated ZnO was observed to have a hexagonal wurtzite crystal arrangement. The generated nanomaterials were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), UV-visible spectroscopy. The crystallinity of ZnO was reported to be in the range 50–60 nm. The NPs morphology showed a strong absorbance at 374 nm with an estimated gap band of 3.20 eV to 3.32 eV. Microscopy analysis proved the morphology and distribution of the generated nanoparticles to be around 50 nm, with the elemental studies showing the elemental composition of ZnO and further confirming the purity of ZnO NPs. The cytotoxic effect of ZnO NPs was evaluated against wild-type and doxorubicin-resistant MCF-7 and MDA-MB-231 breast cancer cell lines. The results showed the ability of ZnO NPs to inhibit the prefoliation of MCF-7 and MDA-MB-231 prefoliation through the induction of apoptosis without significant differences in both wild-type and resistance to doxorubicin.     

Açai (Euterpe oleracea Mart.) Seed Extract Induces ROS Production and Cell Death in MCF-7 Breast Cancer Cell Line

Euterpe oleracea Mart. (açai) is a native palm from the Amazon region. There are various chemical constituents of açai with bioactive properties. This study aimed to evaluate the chemical composition and cytotoxic effects of açai seed extract on breast cancer cell line (MCF-7). Global Natural Products Social Molecular Networking (GNPS) was applied to identify chemical compounds present in açai seed extract. LC-MS/MS and molecular networking were employed to detect the phenolic compounds of açai. The antioxidant activity of açai seed extract was measured by DPPH assay. MCF-7 breast cancer cell line viability was evaluated by MTT assay. Cell death was evaluated by flow cytometry and time-lapse microscopy. Autophagy was evaluated by orange acridin immunofluorescence assay. Reactive oxygen species (ROS) production was evaluated by DAF assay. From the molecular networking, fifteen compounds were identified, mainly phenolic compounds. The açai seed extract showed cytotoxic effects against MCF-7, induced morphologic changes in the cell line by autophagy and increased the ROS production pathway. The present study suggests that açai seed extract has a high cytotoxic capacity and may induce autophagy by increasing ROS production in breast cancer. Apart from its antioxidant activity, flavonoids with high radical scavenging activity present in açai also generated NO (nitric oxide), contributing to its cytotoxic effect and autophagy induction.     

Eco-friendly synthesis of gold nanoparticles using fruit extracts and in vitro anticancer studies

Gold nanoparticles are biocompatible and are having several applications in biomedical Sciences and Engineering. Integration of nanoscience in medicine leads to the development of biomedical products that helps the Society in a faster and safer manner. In the present research work, bioreduction and biofunctionalization of gold nanoparticles are performed with fruit extracts of Aegle marmelos, Eugenia jambolana and soursop. The nanoparticles are characterized using UV–Vis spectroscopy, Transmission Electron Microscopy, Fourier Transform Infrared Spectroscopy and Zeta potentiometer. The qualitative phytochemical analysis of the fruit extracts shows the presence of alkaloids, amino acid, flavonoids, phenol, proteins, tannin, reducing sugars and total Sugars. The in vitro anticancer activity was confirmed by MTT assay on the human breast cancer cell line MCF-7 at different concentrations. The flavonoids present in the fruit extracts are potential reducing agent which is responsible for the formation of gold nanoparticles. Stabilization of gold nanoparticles are performed by the carboxylate group present in the proteins. Also, the nanoparticles are held apart from each other by the electrostatic repulsions that exist due to the presence of like charges surrounding the gold nanoparticles. This study proves that the fruit extracts can be used for the synthesis and stabilization of gold nanoparticles. Further, the engineered nanoparticles capped with bioactive compounds are potential anticancer agents against breast cancer cell line MCF-7.     

Green synthesis and chemical characterization of silver nanoparticles obtained using Allium saralicum aqueous extract and survey of in vitro antioxidant,cytotoxic, antibacterial and antifungal properties

Allium saralicum R.M. Fritsch has been used in Iranian traditional medicine as a remedial supplement for microbial diseases. This paper reports the green synthesis, chemical characterization and antioxidant, cytotoxic, antibacterial and antifungal properties of silver nanoparticles obtained using aqueous extract of A. saralicum leaves. In this synthesis, no surfactants or stabilizers were used. For characterization, UV–visible spectroscopy, transmission electron microscopy, X‐ray diffraction, energy‐dispersive X‐ray spectroscopy and field emission scanning electron microscopy were used. 2,2‐Diphenyl‐1‐picrylhydrazyl was used in experiments to assess the antioxidant potential of the silver nanoparticles, which revealed an impressive prevention in comparison with butylated hydroxytoluene. The synthesized silver nanoparticles at low doses (1–250 μg dl^?1) did not show marked cytotoxic activity (against cervical cancer cells (Hela), breast cancer cells (MCF‐7) and human embryonic kidney cells (HEK‐293)). Agar diffusion tests were applied to determine the antibacterial and antifungal characteristics. Compared with all standard antimicrobials, the silver nanoparticles showed higher antibacterial and antifungal activities (p ≤ 0.01). Also, the silver nanoparticles inhibited the growth of all bacteria and fungi at concentrations of 31–250 μg ml^?1, and destroyed them at concentrations of 31–500 μg ml^?1 (p ≤ 0.01). Because the silver nanoparticles obtained using aqueous extract of A. saralicum leaves have antioxidant, non‐cytotoxic, antifungal and antibacterial potentials, they can be used as a medical supplement or drug.     

Lignans and Triterpenes from the Root of Pseuderanthemum carruthersii var. atropurpureum

Two new lignans, pseuderesinol (1), pseuderanoside (2) and a new triterpene, pseuderanic acid (3) were isolated from the dried root of Pseuderanthemum carruthersii (SEEM.) GUILL. var. atropurpureum (BULL.) FOSB. (Acanthaceae), together with ten known compounds, including five lignans, (+)-eudesmin (4), (+)-magnolin (5), (+)-syringaresinol (6), (+)-episyringaresinol (7), (+)-1-hydroxysyringaresinol (8) and five triterpenes, squalene (9), oleanolic acid (10), lupeol (11), betulin (12), betulinic acid (13). Their chemical structures were elucidated by 1D- and 2D-NMR, computational quantum chemistry, as well as high resolution-electrospray ionization (HR-ESI)-MS spectroscopic analysis. The acetylcholinesterase inhibition and cytotoxic activities against HeLa and MCF-7 cancer cell lines were evaluated on some purified compounds at the concentration of 100?μg/mL. Pseuderesinol (1) and magnolin (5) exhibited moderate cytotoxic activities against the MCF-7 cancer cell line.     

Synthesis,cytotoxic assessment,and molecular docking studies of 2,6-diaryl-substituted pyridine and 3,4- dihydropyrimidine-2(1H)-one scaffolds

Cancer is one of the main global health problems. In order to develop novel antitumor agents, we synthesized 3,4-dihydropyrimidine-2(1H)-one (DHPM) and 2,6-diaryl-substituted pyridine derivatives as potential antitumor structures and evaluated their cytotoxic effects against several cancer cell lines. An easy and convenient method is reported for the synthesis of these derivatives, employing cobalt ferrite (CoFe ₂ O ₄ @SiO ₂ -SO ₃ H) magnetic nanoparticles under microwave irradiation and solvent-free conditions. The structural characteristics of the prepared nanocatalyst were investigated by FTIR, XRD, SEM, and TGA techniques. In vitro cytotoxic effects of the synthesized products were assessed against the human breast adenocarcinoma cell line (MCF-7), gastric adenocarcinoma (AGS), and human embryonic kidney (HEK293) cells via MTT assay. The results indicated that compound 4r (DHPM derivative) was the most toxic molecule against the MCF-7 cell line (IC ₅₀ of 0.17 μg/mL). Moreover, compounds 4j and 4r (DHPM derivatives) showed excellent cytotoxic activities against the AGS cell line, with an IC ₅₀ of 4.90 and 4.97 μg/mL, respectively. Although they are pyridine derivatives, compounds 5g and 5m were more active against the MCF-7 cell line. Results showed that the candidate compounds exhibited low cytotoxicity against HEK293 cells. The kinesin Eg5 inhibitory potential of the candidate compounds was evaluated by molecular docking. The docking results showed that, among the pyridine derivatives, compound 5m had the most free energy of binding (–9.52 kcal/mol) and lowest Ki (0.105 μM), and among the pyrimidine derivatives, compound 4r had the most free energy of binding (–7.67 kcal/mol) and lowest Ki (2.39 μM). Ligand-enzyme affinity maps showed that compounds 4r and 5m had the potential to interact with the Eg5 binding site via H-bond interactions to GLU116 and GLY117 residues. The results of our study strongly suggest that DHPM and pyridine derivatives inhibit important tumorigenic features of breast and gastric cancer cells. Our results may be helpful in the further design of DHPMs and pyridine derivatives as potential anticancer agents.     

A novel CuFe2O4@Ag nanocomposite biosynthesized by Spirulina platensis exhibits an anticancer effect on human gastric adenocarcinoma and Michigan Cancer Foundation-7 breast cancer cell lines

In recent years, the increasing cancer incidence and mortality rate has posed a significant challenge to scientists to develop novel therapeutic drugs against cancerous cells. One of the investigated techniques for cancer therapeutics is the green synthesis of nanoparticles (NPs). In this study, we reported the green synthesis and characterization of the CuFe₂O₄@Ag nanocomposite using Spirulina platensis and its cytotoxic activity on two cancer cell lines: human gastric adenocarcinoma (AGS) and Michigan Cancer Foundation-7 (MCF-7) breast cancer. The physical and chemical properties of the biosynthesized nanocomposite were characterized using Fourier-transform infrared spectroscopy, X-ray diffraction, energy-dispersive X-ray analysis, dynamic light scattering, ultraviolet–visible spectroscopy, scanning electron microscopy, transmission electron microscopy, and zeta potential analyses. The anticancer properties of the CuFe₂O₄@Ag nanocomposite and imatinib drug on both cancer cell lines were evaluated using 3-(4,5-dimethylthiazoyl-2-yl)-2,5-diphenyltetrazoliumbromide (MTT) assay. Also, apoptosis induced by the nanocomposite was assessed using annexin V/propidium iodide staining followed by flow cytometry analysis, Hoechst 33432 staining, and caspase-3 activity assay. Finally, the effect of the CuFe₂O₄@Ag nanocomposite on the expression of BAX and BCL2 genes was assessed by real-time polymerase chain reaction. The result of the MTT test showed an increase in the cellular uptake of CuFe₂O₄@Ag nanocomposite and cell viability loss in a concentration-dependent manner with the 50% minimum inhibitory concentration (IC₅₀) of 180 and 220 μg/ml for MCF-7 and AGS cell lines, respectively. The mean expression of BAX was significantly higher than that of BCL2 in cells treated with the nanocomposite. The results of flow cytometry, Hoechst 33432 staining, and caspase-3 activity assay indicated the stimulation of apoptosis through an increase in caspase-3 and nucleus fragmentation. In general, our results demonstrated the cytotoxic activity of the CuFe₂O₄@Ag nanocomposite. However, further in vivo studies are required to evaluate the accumulation of this nanocomposite in organs such as liver, kidneys, brain, and testes and its potential toxic effects.     

Differentiation Between Anti-Epidermal Growth Factor Receptors Antibody Conjugated and Unconjugated Gold Nanoparticles Using Attenuated Total Reflectance–Fourier Transform Infrared Spectroscopy

Attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) along with UV-Vis was used to distinguish between structural differences between a normal human breast cell line (MCF-12 F) and a cancerous breast cell line (MCF-7) after both being treated with conjugated gold nanoparticles and unconjugated gold nanoparticles. The MCF-7 cell line possessed a small amount of epidermal growth factor receptors (EGFR) on its cell surface whereas the MCF-12 F cell line did not. The anti-EGFR antibodies blocked the binding of epidermal growth factors to this receptor which plays an important role in the regulation of cell growth, proliferation, and differentiation. The infrared (IR) spectra for both cell lines yield several differences between normal biological samples and cancerous samples. As the malignancy of the sample increases, the peak intensity and wavenumber positions decrease. The same conclusion was drawn from thin-layers of conjugated nanoparticles and nonconjugated nanoparticles. The presence of conjugated nanoparticles increased the peak intensity of the MCF-7 cell line whereas it decreased the peak intensity for the MCF-12 F cell line. UV-Vis was used to show the presence of the anti-EGFR antibodies on the surface of the gold nanoparticles which was 5 nm red shifted compared to the gold nanoparticles solution.     

A Novel Copper Oxide Nanoparticle Conjugated by Thiosemicarbazone Promote Apoptosis in Human Breast Cancer Cell Line

The current study highlights the apoptotic activity of copper oxide (CuO) nanoparticles functionalized by Glutamic acid and conjugated by thiosemicarbazone (TSC) toward human breast cancer (MCF-7) and normal (HEK293) cell lines. To this aim, the co-precipitation method was used for preparation the CuO nanoparticles. Afterward, the CuO nanoparticles functionalized by glutamic acid. After that the functionalized copper oxide nanoparticles (CuO@Glu) conjugated to thiosemicarbazone. In next step, the final nanoparticle product (CuO@Glu/TSC) was characterized by physico-chemical techniques including Fourier transform infrared (FT-IR) spectroscopy, Scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), Energy dispersive X-ray analysis (EDX), zeta potential analysis and dynamic light scattering (DLS). The effects of in vitro cell viability in CuO@Glu/TSC nanoparticles showed the anti-proliferative properties with a dose-dependent manner (IC₅₀?=?133.97 µg/ml). The IC₅₀ of CuO@Glu/TSC on normal cell line was 230.2 µg/ml. This IC₅₀ deference shows high cytotoxicity of CuO@Glu/TSC nanoparticles on tumor cells and low cytotoxicity on non-tumorigenic cells (HEK293) and is considered as an important aspect for this nanoparticles. Also, CuO@Glu/TSC nanoparticles had efficient effects in inhibiting the growth of breast cancer cell line (MCF-7). In addition, the CuO@Glu/TSC nanoparticle induced apoptosis symptoms which were assessed by Caspase-3 activation assay, Annexin V/ propidium iodide flow cytometry, and Hoechst 33258 staining. Further, Bax and Bcl-2 genes expression was estimated by real time PCR. The expression of Bax increased 1.69 fold, while the expression of Bcl-2 decreased 0.6 fold. The results of the current study propose that CuO@Glu/TSC nanoparticles reveal effective anti-cancer activity against breast cancer cell line.

     

A Comparative Study of Receptor-Targeted Magnetosome and HSA-Coated Iron Oxide Nanoparticles as MRI Contrast-Enhancing Agent in Animal Cancer Model

Magnetosomes are specialized organelles arranged in intracellular chains in magnetotactic bacteria. The superparamagnetic property of these magnetite crystals provides potential applications as contrast-enhancing agents for magnetic resonance imaging. In this study, we compared two different nanoparticles that are bacterial magnetosome and HSA-coated iron oxide nanoparticles for targeting breast cancer. Both magnetosomes and HSA-coated iron oxide nanoparticles were chemically conjugated to fluorescent-labeled anti-EGFR antibodies. Antibody-conjugated nanoparticles were able to bind the MDA-MB-231 cell line, as assessed by flow cytometry. To compare the cytotoxic effect of nanoparticles, MTT assay was used, and according to the results, HSA-coated iron oxide nanoparticles were less cytotoxic to breast cancer cells than magnetosomes. Magnetosomes were bound with higher rate to breast cancer cells than HSA-coated iron oxide nanoparticles. While 250 μg/ml of magnetosomes was bound 92 ± 0.2%, 250 μg/ml of HSA-coated iron oxide nanoparticles was bound with a rate of 65 ± 5%. In vivo efficiencies of these nanoparticles on breast cancer generated in nude mice were assessed by MRI imaging. Anti-EGFR-modified nanoparticles provide higher resolution images than unmodified nanoparticles. Also, magnetosome with anti-EGFR produced darker image of the tumor tissue in T2-weighted MRI than HSA-coated iron oxide nanoparticles with anti-EGFR. In vivo MR imaging in a mouse breast cancer model shows effective intratumoral distribution of both nanoparticles in the tumor tissue. However, magnetosome demonstrated higher distribution than HSA-coated iron oxide nanoparticles according to fluorescence microscopy evaluation. According to the results of in vitro and in vivo study results, magnetosomes are promising for targeting and therapy applications of the breast cancer cells.     

Biosynthesis of silver nanoparticles using Onosma sericeum Willd. and evaluation of their catalytic properties and antibacterial and cytotoxic activity

In this study, silver nanoparticle (AgNP) synthesis was carried out using Onosma sericeum Willd. aqueous extract for the first time, with a simple, economical, and green method without the need for any other organic solvent or external reducing or stabilizing agent. A variety of AgNPs, all of different particle sizes, were synthesized by controlling the silver ion concentration, extract volume, temperature, and pH. It was determined that the optimum conditions for AgNP synthesis were 1 mM AgNO3, pH 8, 25 °C, 20 g/200 mL extract, silver nitrate, and extract ratio 5:1 (v/v). The AgNPs were defined using UV-Vis spectroscopy, field emission scanning electron microscopy (FESEM), energy dispersive X-ray analysis (EDAX), transmission electron microscopy (TEM), and X-ray diffraction (XRD). The particle size distribution and zeta potential measurements of the AgNPs were measured using the dynamic light scattering (DLS) technique. It was determined that the AgNPs with a particle size of less than 10 nm showed a higher catalytic effect in the reduction of 2-nitrobenzenamine. It was also found that these nanoparticles had a cytotoxic effect on the MCF-7 breast cancer cell line depending on dosage and time. The resulting IC50 values were between 76.63 µg/mL and 169.77 µg/mL. Furthermore, the biosynthesized AgNPs showed effective antibacterial activity against the Acinetobacter baumannii bacteria. The results of the study showed that synthesized AgNPs can have a promising role in biomedical and nanobiotechnology applications.     

Biofabrication of iron oxide nanoparticles by leaf extract of Rhamnus virgata: Characterization and evaluation of cytotoxic,antimicrobial and antioxidant potentials

In the present study, plant‐mediated synthesis of iron oxide nanoparticles (IONPs) using leaves extract of Rhamnus virgata (Roxb.) as a potential stabilizing, reducing and chelating agent is reported. The biogenic IONPs are extensively characterized for their physical and biological properties. The morphology, structure and physicochemical properties of biogenic IONPs were characterized using ultraviolet spectroscopy, X‐ray diffraction, Fourier transform‐infrared analysis, scanning electron microscopy, energy‐dispersive spectroscopy, transmission electron microscopy, Raman spectroscopy and dynamic light scattering. The Scherrer equation deduced a mean crystallite size of ~20 nm for IONPs. Detailed in vitro biological activities revealed significant therapeutic potentials for IONPs. Potential antibacterial and antifungal activities are reported for IONPs. Bioinspired IONPs have shown potential results against HepG2 cells (IC₅₀: 13.47 μg/ml). Dose‐dependent cytotoxicity assays were revealed against Leishmania tropica (KMH₂₃) promastigotes (IC₅₀: 8.08 μg/ml) and amastigotes (IC₅₀: 20.82 μg/ml) using different concentrations of IONPs (1–200 μg/ml). The cytotoxic activity was also studied using brine shrimps, and their IC₅₀ value was calculated as 32.41 μg/ml. Significant antioxidant [TAC (51.4%), DPPH (79.4%) and total reducing power (62%)], protein kinase and alpha amylase inhibition assays were revealed. The biocompatibility assays using red blood cells (> 200 μg/ml) and macrophages (> 200 μg/ml) confirmed the biosafe nature of IONPs. In conclusion, bioinspired IONPs have shown potential biological applications and should be subjected to further research work to develop their nano‐pharmacological relevance in biomedical applications.     

Synthesis,characterization, and antitumor activity of novel tumor-targeted platinum(IV) complexes

Four tumor-targeted platinum(IV) complexes with ammonia and cyclohexylamine as the carrier groups and biotin as the axial group were designed, synthesized, and characterized. In vitro evaluation of the antitumor activity of complexes C1–C4 against lung cancer cells (A549), liver cancer cells (SMMC-7721), breast cancer cells (MCF-7), and colon cancer cells (SW480) was carried out. Complex C3 had the best cellular activity. Compared with cisplatin, complex C3 showed good anticancer activity against A549 cell line,complex C3 (6.34±0.44) is 3 times more cytotoxic than cisplatin (19.40±0.71),and against MCF-7 cell line complex C3 (4.22±0.11) is 5.4 times more cytotoxic than cisplatin (22.96±0.58), and against SW480 cell line complex C3 (6.65±0.60) is 3.4 times more cytotoxic than cisplatin (23.15±0.22). (Table 1) Axial chloride increased the redox power of complex C3 to increase the intercellular accumulation and the introduction of mixed amine had the ability to overcome cisplatin resistance. Complex C3 works best on MCF-7, then SW480, A549, and SMMC-7721. Thus, complex C3 is targeted by the axial introduction of biotin.     

Green and one‐pot surface coating of iron oxide magnetic nanoparticles with natural amino acids and biocompatibility investigation

We report the synthesis of iron oxide magnetic nanoparticles (IONPs) coated with various natural amino acids (AAs) using a one‐pot reaction in an aqueous medium. Several AAs, which contained hydrophilic and hydrophobic groups, were selected to study their effects on size, morphology and toxicity of IONPs. Functionalized IONPs were characterized using X‐ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, and scanning and transmission electron microscopies. Furthermore, vibrating sample magnetometry analysis shows these nanoparticles have excellent magnetic properties. Cellular toxicity of IONPs was also investigated on HFF2 cell lines. The AA‐coated IONPs are non‐toxic and biocompatible. Natural AA‐coated IONPs show a potential for their development in in vitro and in vivo biomedical fields due to their non‐toxicity, good ζ‐potential and related small size and narrow size distribution.     

Cytotoxic Polyhydroxylated Oleanane Triterpenoids from Cissampelos pareira var. hirsuta

Three new polyhydroxylated oleanane triterpenoids, cissatriterpenoid A−C (1−3), along with one known analogue (4), were isolated from the whole plant of Cissampelos pareira var. hirsuta. Their chemical structures were elucidated by extensive spectroscopic data (IR, HR-ESI-MS, ¹H-NMR, ¹³C-NMR, DEPT, ¹H-¹H COSY, HSQC, HMBC, NOESY) and the microhydrolysis method. The isolation of compounds 1–4 represents the first report of polyhydroxylated oleanane triterpenoids from the family Menispermaceae. All isolated compounds were evaluated for their cytotoxicity against five human cancer cell lines, and the inhibitory activity against NO release in LPS-induced RAW 264.7 cells. Compound 3 showed the most potent cytotoxic activities against the A549, SMMC-7721, MCF-7, and SW480 cell lines, with IC₅₀ values of 17.55, 34.74, 19.77, and 30.39 μM, respectively, whereas three remaining ones were found to be inactive. The preliminary structure–activity relationship analysis indicated that the γ-lactone ring at C-22 and C-29, and the olefinic bond at C-12 and C-13 were structurally required for the cytotoxicity of polyhydroxylated oleanane triterpenoids against these four cell lines. Based on lipid-water partition coefficients, compound 3 is less lipophilic than 1 and 4, which agrees with their cytotoxic activities. This confirms the potential of C. pareira var. hirsuta in the tumor treatment.     

Facile preparation of Au nanoparticles mediated by Foeniculum Vulgare aqueous extract and investigation of the anti-human breast carcinoma effects

This experiment evaluated antioxidant, anti-human breast cancer activities, and cytotoxicity effects of green synthesis of Au nanoparticles (AuNPs) containing Foeniculum Vulgare aqueous extract. Mixing Foeniculum Vulgare aqueous with Au chloride solution produced Au nanoparticles. The characteristics of Au nanoparticles determined using Fourier Transformed Infrared Spectroscopy (FT‐IR), Transmission Electron Microscopy (TEM), UV–Visible Spectroscopy (UV–Vis), and Field Emission Scanning Electron Microscopy (FE‐SEM). To check the cytotoxicity and anti-breast cancer effects of Au chloride, Foeniculum Vulgare aqueous extract, and AuNPs on common breast cancer cell lines i.e., ZR-75-30, T47D, and HCC1187 was used MTT assay. AuNPs showed no cytotoxicity and the most effective anti-breast cancer features compared to other items that were tested. They had no cytotoxic effects on normal cell line (HUVEC) and had very low cell viability, high anti-breast cancer activities dose-dependently against ZR-75-30, T47D, and HCC1187 cell lines. In the presence of butylated hydroxytoluene as the positive control, the DPPH test was used to evaluate the antioxidant features of Au chloride, Foeniculum Vulgare aqueous extract, and Au nanoparticles. AuNPs showed the best antioxidant properties compared to other items that were tested. Perhaps remarkable anti-human breast cancer activities of Au nanoparticles synthesized by Foeniculum Vulgare aqueous extract due to its antioxidant properties. After clinical trial and confirmation of results, this formulation can be used as an effective drug to treat breast cancer.     

Therapeutic Potential of DNAzyme Loaded on Chitosan/Cyclodextrin Nanoparticle to Recovery of Chemosensitivity in the MCF-7 Cell Line

Commonly, acquired resistances to anticancer drug are mediated by overexpression of a membrane-associated protein that encode via multi-drug resistance gene-1 (MDR1). Herein, the mRNA-cleaving DNAzyme that targets the mRNA of MDR1 gene in doxorubicin-resistant breast cancer cell line (MCF-7/DR) loaded on the chitosan β-cyclodextrin complexes was used as a tropical agent. Chitosan/β-cyclodextrin complexes were used to deliver DNAzymes into cancer cells. Determination of the physicochemical characteristics of the particles was done by photon correlation spectroscopy and scanning electron microscopy. The encapsulation efficiency of the complexes was tested by using gel retardation assay. Positively charged nanoparticles interacted with DNAzyme that could perform as an efficient DNAzyme transfection system. The rationale usage of this platform is to sensitize MCF-7/DR to doxorubicin by downregulating the drug-resistance gene MDR1. Results demonstrated a downregulation of MDR1 mRNAs in MCF-7/DR/DNZ by real-time PCR, compared to the MCF-7/DR as control. WST1 assay showed the 22-fold decrease in drug resistance on treated cells 24 h after transfection. Results showed the intracellular accumulation of Rh123 increased in the treated cells with DNAzyme. Results suggested a potential platform in association with chemotherapy drug for cancer therapy and indicated extremely efficient at delivery of DNAzyme in restoring chemosensitivity.

     

Synthesis of chalcones with anticancer activities

Several chalcones were synthesized and their in vitro cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and human normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC?? values were chosen and studied in detail with MCF-7 cells. The compounds 1, 5, 23, and 25 were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (p < 0.05). The ROS level showed 1.3-fold increase (p < 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.     

Design,synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine

A library of acetamide and hydrazine analogues were generated on the pyrimidine ring through a multistep reaction starting from 5-nitro-pyrimidine-4,6-diol and pyrimidine-4,6-diol, respectively. The synthesized analogues were screened for in vitro cytotoxic activity against various human cancer cell lines like HCT-1 and HT-15 (colon), MCF-7(breast), PC-3 (prostrate), SF268 (CNS) using MTT method. From the bioassay results, it was observed that even though many of the synthesized derivatives exhibited a good potency against various screened cancer cell lines, compound 14a from the acetamide series was found to show potent anticancer activity on all the tested cancer cell lines with IC₅₀ value of 0.36μM on CNS cell line and 1.6μM on HT-21 cell line, and compound 19xxi from hydrazine series of pyrimidine showed potent activity against three tested cancer cell lines with IC₅₀ value of 0.76μM on HT-29 cell line, 2.6μM on HCT-15, and 3.2μM on MCF-7 cell line.