•Cytotoxicity of cyclic C5-curcuminoids against CNS tumors is described.•Their IC50 value on astrocytoma is in the low nanomolar and picomolar range.•These cyclic C5-curcumunoids penetrate the ...blood-brain barrier in different ratios.•The antitumoral activity did not show correlation with experimental logP.•The synthesis of these novel C5-curcuminoids is simple and economical in large scale.
Novel series of cyclic C5-curcuminoids 17a-j and 19-22 were prepared as cytotoxic agents and evaluated against human neuroblastoma (SH-SY5Y) or human grade IV astrocytoma (CCF-STTG1) cell lines in low (∼0.1 nM - 10 nM) concentrations. Among the tested 21 derivatives, 16 displayed potent antiproliferative activity with IC50 values in the low nanomolar to picomolar range (IC50 = 7.483-0.139 nM). Highly active compounds like N-monocarboxylic derivative 19b with IC50 = 0.139 nM value against neuroblastoma and N-alkyl substituted 11 with IC50 = 0.257 nM against astrocytoma proved some degree of selectivity toward non-cancerous astrocytes and kidney cells. This potent anticancer activity did not show a strong correlation with experimental logPTLC values, but the most potent antiproliferative molecules 11-13 and 19-22 are belonging to discrete subgroups of the cyclic C5-curcuminoids. Compounds 12, 17c and 19b were subjected to blood-brain barrier (BBB) penetration studies, too. The BBB was revealed to be permeable for all of them but, as the apparent permeability coefficient (Papp) values mirrored, in different ratios. Lower toxicity of 12, 17c and 19b was observed toward primary rat brain endothelial cells of the BBB model, which means they remained undamaged under 10 µM concentrations. Penetration depends, at least in part, on albumin binding of 12, 17c and 19b and the presence of monocarboxylic acid transporters in the case of 19b. Permeation through the BBB and albumin binding, we described here, is the first example of cyclic C5-curcuminoids as to our knowledge.
: New cyclic C5-curcuminoids are synthesized with superior cytotoxic activity on neuroblastoma and astrocytoma cell lines. IC50 values in low nanomolar and picomolar range, experimental logPTLC, structure-activity relationship, BBB penetration and selective cytotoxicity are described
Display omitted
•ZnO-NPs were green synthesized in water and ethanol usingO. majorana.•ZnO-NPs were generated in a spherical structure with a size range of 15–30 nm.•OE-ZnO-NPs exhibited higher anticancer activity ...than OW-ZnO-NPs.•OE-ZnO-NPs showed lower cytotoxicity against normal cell lines than OW-ZnO-NPs.
This work aims to generate green synthesized ZnO-NPs using Origanum majorana (O. majorana) with water (OW-ZnO-NPs) or ethanol (OE-ZnO-NPs) and compare their anticancer and cytotoxicity activities. We studied the effect of preparation using water and ethanol with different techniques, including the color change to brownish yellow and yellowish white, respectively. In addition, Zeta-potential showed a negatively charged surface, and the Energy Dispersive X-ray (EDX) exhibited different elements with various ratios (zinc > oxygen > carbon). Furthermore, Transmission and Scanning Electron Microscopy (TEM and SEM) were used to illustrate the spherical structures. Next, the cytotoxicity for the synthesized nanoparticles was determined by MTT assay, and 50 % cytotoxic concentration (CC50) for OW-ZnO-NPs were 152.95, 92.89, >1000 and > 1000 μg/mL, and for OE-ZnO-NPs, 105.14, 52.54, >1000 and 736.57 μg/mL were evaluated against MCF7, HepG2, HSF and OEC cells, respectively. In conclusion, the results of this study demonstrate a simple, affordable, and eco-friendly method for synthesizing ZnO-NPs using readily available plant extract. In addition, OE-ZnO-NPs have higher anticancer activity than OW-ZnO-NPs and less toxic activity against normal cell lines.
•Honey is used to biosynthesize ZnO-NPs with spherical and hexagonal shapes.•The biosynthesized ZnO-NPs with a size range of 20-40 nm.•The IC50 for ZnO-NPs shows lower cytotoxicity against HSF than ...the HepG2 cell line.
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.
Cancer cells accumulate iron to supplement their aberrant growth and metabolism. Depleting cells of iron by iron chelators has been shown to be selectively cytotoxic to cancer cells
and
. Iron ...chelators are effective at combating a range of cancers including those which are difficult to treat such as androgen insensitive prostate cancer and cancer stem cells. This review will evaluate the impact of iron chelation on cancer cell survival and the underlying mechanisms of action. A plethora of studies have shown iron chelators can reverse some of the major hallmarks and enabling characteristics of cancer. Iron chelators inhibit signalling pathways that drive proliferation, migration and metastasis as well as return tumour suppressive signalling. In addition to this, iron chelators stimulate apoptotic and ER stress signalling pathways inducing cell death even in cells lacking a functional p53 gene. Iron chelators can sensitise cancer cells to PARP inhibitors through mimicking BRCAness; a feature of cancers trademark genomic instability. Iron chelators target cancer cell metabolism, attenuating oxidative phosphorylation and glycolysis. Moreover, iron chelators may reverse the major characteristics of oncogenic transformation. Iron chelation therefore represent a promising selective mode of cancer therapy.
Manganese oxide containing nanoparticles (MnOx NPs) have emerged as promising antimicrobial and anticancer agents due to their unique properties. However, the different initial materials and ...synthesis techniques often yield nanoparticles with highly different properties which limit their applications especially in the biomedical field. Thus, we aimed to explore the suitability of pyrolusite as a new and sustainable manganese mineral source for MnOx production. Moreover, we examined the effect of various synthesis methods on the physicochemical characteristics and biological activity of MnOx NPs to explore their therapeutic utilization potential against microbes and in cancer treatment. We produced MnOx NPs from a naturally occurring mineral via mechanochemical, chemical, and electrochemical processes, characterized them thoroughly, and assessed their cytotoxicity against bacteria, fungi, and human cancerous and non-cancerous cells. We verified that the synthesis method utilized to obtain MnOx NPs impacted significantly nanoparticle properties leading to distinct structural, morphological, and biological characteristics. Although none of the particles was effective against the tested bacterial strains, electrochemically produced NPs demonstrated significant antifungal activity. These nanoparticles were also the most potent anticancer agents, exhibiting cancer-selective toxicity attributed to apoptosis induction rather than altered cell proliferation or direct necrotic effects. These results are relevant for the development of effective and safe nanotherapeutics and highlight the potential of MnOx nanoparticles - obtained through carefully selected initial mineral source and adequate synthetic approach - in antimicrobial and anticancer therapy.
Display omitted
Heracleum persicum, commonly called Persian hogweed, is widely used as a spice in Iran. H. persicum comprises many natural compounds which are used in the treatment of multiple disorders. H. persicum ...stem extract was used for green synthesis of silver nanoparticles (Hp-AgNPs) and their phytochemical contents and antioxidant, and anti-proliferative activities were evaluated against human breast cancer cells (MDA-MB231) in this study. We found an optimal reaction medium consists of 5% of stem extract and 2 mM of aqueous AgNO3 solution. Characterization studies including UV–visible spectrophotometry at a range of 300-700 nm, Field Emission Scanning Electron Microscopy (FESEM), Energy Dispersive Xray (EDX), X-ray Diffraction (XRD), Dynamic Light Scattering (DLS), Zeta potential, Fourier Transform Infrared (FTIR) and Surface-Enhanced Raman Spectroscopy (SERS) confirmed the optimal shape, size and stability of biosynthesized Hp-AgNPs. Results revealed that Hp-AgNPs contains higher TPC (Total Phenolic Content) and TFC (Total Flavonoid Content) and indicate a high level of antioxidant activity. The anticancer activity of Hp-AgNPs validated with inhibitory activity on growth of MDA-MB-231 cells. Results of Hp-AgNPs-treated MDA-MB-231 cells indicated an IC50 value of 63.29 μg/mL at 48h. Results of this study provide a simple, rapid, non-toxic and eco-friendly protocol for biosynthesis of Hp-AgNPs, which could be used as an alternative approach for safe and simple synthesis of silver nanoparticles for biomedical applications.
•Black peel pomegranate is a rare cultivar of pomegranate distinguished by a deep red color.•The peel extract of the pomegranate shows unique pharmaceutical properties such as antioxidant and ...antibacterial.•This extract synthesis silver nanoparticles in an ultra-fast pace without any heating or additional accelerators.
"Black Peel Pomegranate" is a rare pomegranate cultivar that its specific features are still uncovered particularly in the bio-nano researches. The present study was organized to evaluate this pomegranate's potential in the biosynthesis of silver nanoparticles as well as bio-medical activities. According to the results, the pomegranate peel extract incredibly inhibited 100 % of DPPH free radicals (EC50 = 5 μg/mL). This extract also induced more than 70 % cell death in the treated breast tumor cell lines, BT-20 and MCF-7. Interestingly, the extract was capable of biosynthesis very stable and small (15.6 nm) silver nanoparticles at ambient temperature in an ultra-fast pace. Likewise, these nanoparticles inhibited 77 % of DPPH free radicals (EC50 = 9 μg/mL). Although this antioxidant capacity was lower than that of the extract, instead, the anticancer activity of the synthesized nanoparticles was significantly enhanced, so that they led to more than 81 % and 89 % cell death in the breast tumor cell lines BT-20 and MCF-7, respectively. Considerably, neither the extract nor the biosynthesized silver nanoparticles, showed significant toxicity against non-tumor cell lines (L-929) at the same concentrations. These features of the biosynthesized nanoparticles were quite outstanding in comparison with chemical/commercial ones. Overall, the present study introduces black peel pomegranate as a worthy bio-agent in the biosynthesis of silver nanoparticles with unique activities as well as a cancer treatment.
•Modified graphene quantum dots are applied as a multifunctional drug carrier.•Multiple tasks are carried out simultaneously.•Cellular uptake of the nanoassembly and drug release are monitored in ...real time.•The nanoassembly targets tumor cells differentially and efficiently.•The nanoassembly exhibits significantly reduced cytotoxicity to non-target cells.
This study demonstrates that ligand-modified graphene quantum dots (GQDs) facilitate the simultaneous operation of multiple tasks without the need for external dyes. These tasks include selective cell labeling, targeted drug delivery, and real-time monitoring of cellular uptake. Folic acid (FA)-conjugated GQDs are synthesized and utilized to load the antitumor drug doxorubicin (DOX). The fabricated nanoassembly can unambiguously discriminate cancer cells from normal cells and efficiently deliver the drug to targeted cells. The inherent stable fluorescence of GQDs enables real-time monitoring of the cellular uptake of the DOX–GQD–FA nanoassembly and the consequent release of drugs. The nanoassembly is specifically internalized rapidly by HeLa cells via receptor-mediated endocytosis, whereas DOX release and accumulation are prolonged. In vitro toxicity data suggest that the DOX–GQD–FA nanoassembly can target HeLa cells differentially and efficiently while exhibiting significantly reduced cytotoxicity to non-target cells.
Silver nanoparticles (AgNPs) are of great interest due to their unique and controllable characteristics. Different synthesis methods have been proposed to produce these nanoparticles, which often ...require elevated temperatures/pressures or toxic solvents. Thus, green synthesis could be a replacement option as a simple, economically viable and environmentally friendly alternative approach for the synthesis of silver nanoparticles.
Here, the potential of the walnut green husk was investigated in the production of silver nanoparticles. An aqueous solution extracted from walnut green husk was used as a reducing agent as well as a stabilizing agent. Then, the synthesized nanoparticles were characterized with respect of their anticancer, antioxidant, and antimicrobial properties.
Results showed that the synthesized nanoparticles possessed an average size of 31.4 nm with a Zeta potential of -33.8 mV, indicating high stability. A significant improvement in the cytotoxicity and antioxidant characteristics of the green synthesized Ag nanoparticles against a cancerous cell line was observed in comparison with the walnut green husk extract and a commercial silver nanoparticle (CSN). This could be due to a synergistic effect of the synthesized silver nanoparticles and their biological coating. AgNPs and the extract exhibited 70% and 40% cytotoxicity against MCF-7 cancerous cells, respectively, while CSN caused 56% cell death (at the concentration of 60 µg/mL). It was observed that AgNPs were much less cytotoxic when tested against a noncancerous cell line (L-929) in comparison with the control material (CSN). The free radical scavenging analysis demonstrated profound anti-oxidant activity for the synthesized nanoparticles in comparison with the extract and CSN. It was also detected that the synthesized AgNPs possess antibacterial activity against nosocomial and standard strains of both Gram-positive and Gram-negative bacteria (minimum inhibitory concentration =5-30 µg/mL).
These findings imply that the synthesized nanoparticles using green nanotechnology could be an ideal strategy to combat cancer and infectious diseases.
PDF
