Many biosensor technologies that can precisely and sensitively identify biomarkers reflecting disease status are being developed to help with early cancer detection and anticancer treatment ...monitoring. The creation of sensors based on nanozymes is one of the novel approaches in the intricate diagnosis and treatment of cancers. Because natural enzyme sensors can be unstable and expensive, the use of nanozymes in biosensors offers a great substitute for this type of study. Nanozymes have a stable shelf life, great operational reliability, cheap cost, and outstanding catalytic activity. The technological approaches to generating nanozymes and their use in sensors are briefly described in the paper. A summary of the many kinds of biosensors based on diverse kinds of nanomaterials for the identification of cancer biomarkers is provided, along with a discussion of the latest developments and challenges in the field of nanozyme biosensors for use in cancer diagnosis.
•Novel approaches to nanozyme-based sensors for intricate diagnosis and cancer treatment are shown.•The main technological approaches to generating nanozymes and their use in sensors are described.•Recent advances in nanozyme sensors for tumor markers and cancer cells are reviewed.•Prospects for the use of nanozyme sensors in cancer diagnosis are shown.•Future trends to improve nanozyme biosensors in cancer diagnosis are considered.
We tested the effect of substituents at the (1) C3´, C3´N, (2) C10, and (3) C2-meta-benzoate positions of taxane derivatives on their activity against sensitive versus counterpart ...paclitaxel-resistant breast (MCF-7) and ovarian (SK-OV-3) cancer cells. We found that (1) non-aromatic groups at both C3´ and C3´N positions, when compared with phenyl groups at the same positions of a taxane derivative, significantly reduced the resistance of ABCB1 expressing MCF-7/PacR and SK-OV-3/PacR cancer cells. This is, at least in the case of the SB-T-1216 series, accompanied by an ineffective decrease of intracellular levels in MCF-7/PacR cells. The low binding affinity of SB-T-1216 in the ABCB1 binding cavity can elucidate these effects. (2) Cyclopropanecarbonyl group at the C10 position, when compared with the H atom, seems to increase the potency and capability of the derivative in overcoming paclitaxel resistance in both models. (3) Derivatives with fluorine and methyl substituents at the C2-meta-benzoate position were variously potent against sensitive and resistant cancer cells. All C2 derivatives were less capable of overcoming acquired resistance to paclitaxel in vitro than non-substituted analogs. Notably, fluorine derivatives SB-T-121205 and 121,206 were more potent against sensitive and resistant SK-OV-3 cells, and derivatives SB-T-121405 and 121,406 were more potent against sensitive and resistant MCF-7 cells. (4) The various structure-activity relationships of SB-T derivatives observed in two cell line models known to express ABCB1 favor their complex interaction not based solely on ABCB1.
•Established ovarian taxane-resistant SK-OV-3/PacR cells overexpress ABCB1 multidrug transporter.•Substituents at C3´ and C3´N positions of taxane affect cancer cell resistance.•Substituents at C3´ and C3´N positions of taxane affect its transport by ABCB1.•C2-meta-benzoyl substituents of taxane do not affect taxane transport by ABCB1.
Display omitted
•A comprehensive review on MOFs-based electrochemical biosensors for early diagnosis of cancers in vitro is presented.•Different strategies to construct MOFs-based electrochemical ...biosensors for detection of cancer biomarkers, microRNAs, and living cancer cells are summarized.•Various MOFs materials (monometallic/bimetallic/luminophore-combined MOFs and MOFs-based composites) for fabricating electrochemical biosensors are discussed.•The achievements, challenges, and future developments of MOFs-based electrochemical biosensors for cancer detection are analyzed.
Developing ultrasensitive and highly selective biosensors is significant for the early diagnosis of cancers and monitoring of the treatment process of cancer patients. Metal–organic frameworks (MOFs), as emerging porous crystalline materials, have received increased attention on account of their potential applications in many fields, such as energy, environment, storage, separation, and sensing. In light of their unique merits, such as large surface areas, tunable pore scales, and good adsorption capabilities, MOFs have been applied as sensitive platforms for anchoring diverse probes (e.g., antibodies, DNA, or aptamers) for the construction of electrochemical (EC) biosensors. Herein, we present a comprehensive overview of MOFs-based EC biosensors for detecting diverse targets (e.g., cancer markers, microRNA, and living cancer cells) that are considered as the indicators for early diagnosis of cancers. Different strategies for construction of EC biosensors with monometallic MOFs, bimetallic MOFs, luminophore-combined MOFs, and MOFs-based nanocomposites are reviewed. Further, the fabrication of MOFs-based EC biosensors toward specific analytes is described to promote and guide future studies on MOFs for biosensing applications.
•A brief introduction on piperazine derivatives endowed with anticancer activity via green synthetic approach.•Mode of action and SAR study of piperazine analogues as anticancer agents•Eco-friendly ...strategies towards the development of piperazine containing compounds•In-silico design as green approach for piperazine based anticancer therapeutics
Through the exploitation of several conventional strategies in subdisciplines of chemistry and the molecular sciences became challenging due to toxic chemicals in last few years. As a result, there is a growing appreciation towards the newly emerging field of green chemistry which is required as an avenue for sustainable development of heterocyclic derivatives over conventional techniques with improved therapeutic efficacy. Hence, researchers endeavored to adopt environmentally benign green methods for synthesis of piperazine as nitrogen containing heterocyclic derivatives against cancer. With considerable efforts towards green chemistry, this review provides recent insights on several sustainable chemistry dependent synthetic strategies for piperazine analogues with significant inhibition of cancer cells such as, microwave assisted techniques, photoredox catalysis, green solvent, multicomponent single pot reaction and catalyst free synthesis. Accordingly, efforts are continually made by researchers to include these techniques for safe & effective synthetic reactions with the involvement of green solvents and catalysts in order to get product in maximum yield with lesser time consumption. It comprises a 15-year synthetic literature search. The significance of this work lies in its thorough literature review on piperazine containing heterocyclic compounds, and researchers working on the synthesis of piperazines can find a lot of helpful information on environmentally benign synthetic strategies for their development. Additionally, some in-silico based literature has also been cited to inquire the stable interaction between the piperazine structure and several targeted proteins in order to offer insightful information for future anticancer drug development.
A brief introduction on piperazine derivatives endowed with anticancer activity via green chemistry strategies. Display omitted
CD90+ liver cancer cells have been described as cancer stem-cell-like (CSC), displaying aggressive and metastatic phenotype. Using two different in vitro models, already described as CD90+ liver ...cancer stem cells, our aim was to study their interaction with endothelial cells mediated by the release of exosomes.
Exosomes were isolated and characterized from both liver CD90+ cells and hepatoma cell lines. Endothelial cells were treated with exosomes, as well as transfected with a plasmid containing the full length sequence of the long non-coding RNA (lncRNA) H19. Molecular and functional analyses were done to characterize the endothelial phenotype after treatments.
Exosomes released by CD90+ cancer cells, but not by parental hepatoma cells, modulated endothelial cells, promoting angiogenic phenotype and cell-to-cell adhesion. LncRNA profiling revealed that CD90+ cells were enriched in lncRNA H19, and released this through exosomes. Experiments of gain and loss of function of H19 showed that this LncRNA plays an important role in the exosome-mediated phenotype of endothelial cells.
Our data indicate a new exosome-mediated mechanism by which CSC-like CD90+ cells could influence their tumor microenvironment by promoting angiogenesis. Moreover, we suggest the lncRNA H19 as a putative therapeutic target in hepatocellular carcinoma.
Despite the significant gains made in cancer therapy, cancer remains a major cause of global deaths due to rapid drug resistance. Therefore, urgent concerted efforts towards the discovery and ...development of newer and effective anticancer agents cannot be overemphasized. This study investigated
cytotoxicity potential of methanol extracts of the root, stem, and leaves of
. Leaf, stem and root samples were collected, authenticated, dried, separately pulverized and extracted in methanol. The methanol extracts were analysed for the presence of phytochemicals and cytotoxic potential evaluated by tetrazolium 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) colorimetric assay on selected human cancer cells lines, HeLa (cervical cancer) and HEp-2 (epidermal carcinoma of the larynx), using mammalian Vero cells as a negative control. Data generated was subjected to descriptive statistics. The flavonoids in the plant was between 40 - 67.2% and was significantly higher (
< 0.05) compared to alkaloids and saponins. At concentrations of ≥ 50 µg/mL, the extracts exhibited 100% cytotoxicity on the cancer cells. The methanol root and leaf extracts with CC
of 15.64 and 11.38 µg/mL were more cytotoxic on HeLa and HEp-2, respectively. In comparison to the stem and root extracts, the methanol leaf extract was selectively more toxic to cancer cell lines than Vero cells (CC
= 28.89 µg/mL). Preliminary investigation reveals that
contain bioactive compounds that possess promising anticancer potential that could be exploited.
The non-essential amino acid serine supports several metabolic processes that are crucial for the growth and survival of proliferating cells, including protein, amino acid and glutathione synthesis. ...As an important one-carbon donor to the folate cycle, serine contributes to nucleotide synthesis, methylation reactions and the generation of NADPH for antioxidant defence. Many cancer cells are highly dependent on serine, a trait that provides several novel therapeutic opportunities, either through the inhibition of de novo serine synthesis or by limiting the availability or uptake of exogenous serine.