Cobalt ferrite nanoparticles (CFN) have drawn attention as a theranostic agent. Unique physicochemical features of CFN and magnetic properties make CFN an outstanding candidate for biomedical, agricultural, and environmental applications. The extensive use of CFN may result in intentional inoculation of humans for disease diagnosis and therapeutic purposes or unintentional penetration of CFN via inhalation, ingestion, adsorption, or other means. Therefore, understanding the potential cytotoxicity of CFN may pave the way for their future biomedical and agricultural applications. This review scrutinized CFN biocompatibility, possible effects, and cytotoxic mechanisms in different biological systems. Literature indicates CFN toxicity is linked with their size, synthesizing methods, coating materials, exposure time, route of administration, and test concentrations. Some in vitro cytotoxicity tests showed misleading results of CFN potency; this might be due to the interaction of CFN with cytotoxicity assay regents. To date, published research indicates that the biocompatibility of CFN outweighed its cytotoxic effects in plant or animal models, but the opposite outcomes were observed in aquatic Zebrafish.

SCOPE: Nonalcoholic fatty liver disease (NAFLD) has a high and growing prevalence globally. Mitochondria are fundamental in regulating cell energy homeostasis. Nevertheless, mitochondria control mechanisms can be exceeded in this context of energy overload. Damaged mitochondria worsen NAFLD progression. Diet and lifestyle changes are the main recommendations for NAFLD prevention and treatment. Some polyphenols have improved mitochondrial function in different NAFLD and obesity models. OBJECTIVE: To discuss the potential role of polyphenols as a non-pharmacological approach targeting mitochondria to prevent and treat NAFLD, analyzing the influence of polyphenols' chemical structure, limitations and clinical projections. METHODS: In vivo and in vitro NAFLD models were considered. Study searches were performed using the following keywords: nonalcoholic fatty liver disease, liver steatosis, mitochondria, mitochondrial activity, mitochondrial dynamics, mitochondrial dysfunction, mitochondrial morphology, mitochondrial cristae, fusion, fission, polyphenols, flavonoids, anthocyanins, AND/OR bioactive compounds. CONCLUSION: Polyphenols are a group of diverse bioactive molecules whose bioactive effects are highly determined by their chemical structure. These bioactive compounds could offer an interesting non-pharmacological approach to preventing and treating NAFLD, regulating mitochondrial dynamics and function. Nevertheless, the mitochondria' role in subjects with NAFLD treatment is not fully elucidated. The dosage and bioavailability of these compounds should be addressed when studied.

Purine, one of nucleotide, is an important substance for metabolism regulation of the body. Purine plays a key role not only in the composition of coenzymes but also in the supply of energy. Since purine was artificially synthesized, it has always been an important scaffold for respiratory diseases, cardiovascular diseases, and anti-tumor and anti-viral drugs. In addition to being widely used as competitive antagonists in the treatment of diseases, purines can be used in combination with other drugs and as precursors to benefit human life. Unfortunately, few new discoveries have been made in recent years. In this article, purine drugs on the market have been classified according to their different targets. In addition, their mechanism of action and structure-activity relationship have been also introduced. This paper provides details of the signaling pathways from when the purine drugs bind to the respective receptors on the surface of cells and the consequent reactions within the cell which finally affect the targeted diseases. The various receptors and biological reactions involved in the signaling for respective disease targets within the cells are discussed in detail.

Alpha-lipoic acid (ALA) is a potent antioxidant used in the management of diabetic neuropathy due to its ability to prevent neuronal lipid peroxidation. ALA also chelates transition metals, which can be beneficial in some diseases related to metal overload. Because of its unique antioxidant properties, ALA has potential novel applications in other diseases related to oxidative stress and inflammation. This review summarizes aspects of recent clinical trials in addition to the well described uses to manage neuropathies. The unique pharmacological actions of ALA, coupled with a relatively low toxicity, has other led to several trials on the potential therapeutic uses of ALA in the management of other diseases associated with increases in oxidative stress, inflammation and metal overload.

Genome editing arose as a new promising approach for the treatment of innumerable intricate ailments including cancer. Over the past couple of decades, delivery technologies that have serendipitously been developed using viral vectors are successful to some extent in protein and nucleic acid delivery but their effectiveness still lags due to their efficiency, tissue targeting capabilities, and toxicity which must be further improved. With the infiltration of nanotechnology into every sphere of life, nano-vehicles can be implemented as an ideal modality that can overcome challenges, also can be introspective as new genome editing tools for cancer therapy owing to the safety and efficiency in clinical settings. Such projected substitution can help in developing highly efficacious therapy regimes which are successful in clinical settings. This emerging approach of incorporation of genome editors (CRISPR/Cas) in different nano vehicles and their utility in targeting various aspects of cancer therapy like treatment, diagnostics, modelling has been comprehensively done in this review.

Drug delivery systems based on nanotechnology exhibit a number of advantages over traditional pharmacological formulations. Polymeric nanoparticles are commonly used as delivery systems and consist of synthetic or natural polymers that protect drugs from degradation in physiological environments. In this context, indolamine melatonin has been associated with several biological functions, including antioxidant, antitumor, immunoregulatory, neuroprotective, and cardioprotective effects. However, its availability, half-life, and absorption depend upon the route of administration, and this can limit its therapeutic potential. An alternative is the use of polymeric nanoparticle formulations associated with melatonin to increase its bioavailability and therapeutic dose at sites of interest. Thus, the objective of this review is to provide a general and concise approach to the therapeutic association between melatonin and polymeric nanoparticles applied to different biological disorders and to also highlight its advantages and potential applications compared to those of the typical drug formulations that are available.

BACKGROUND: Breast cancer is considered to be 2nd most common cancer subtype investigated worldwide. It is mainly prevalent in postmenopausal women. Estrogen Receptor (ER) is a primary transcription factor for survival and growth of tumors. Around 80% BCs of all classes are ER-positive (ER+). Powerful evidence for estrogen proved to be involved in BC pathogenesis both exogenously and endogenously. It brings the concept of ER inhibitors to treat BC with distinct mechanisms into focus and ER PROTACs (Proteolysis-Targeting Chimeras), AIs (Aromatase inhibitors), SERMs (Selective estrogen receptor modulators), and SERDs (Selective estrogen receptor degrader) were developed. For over 30 years, Tamoxifen, a triphenylethylene SERM, was the drug of choice solely to treat ER+BC patients. Although several SERMs got approval by US FDA after tamoxifen, complicacies remain because of dangerous adverse effects like endometrial carcinoma, hot flashes, and VTE (Venous thromboembolism). In addition to that drug-resistant tumors put a surging need for novel, potent candidates with no or low adverse effects for ER+ BC prevention. OBJECTIVES: This article explores the possibilities of SERMs as effective BC agents. METHODS: A detailed literature survey of the history and recent advancements of SERMs has been carried out, taking BC as the primary target. This review provides information about ER structure, signaling, pharmacological action, chemical classification with SAR analysis, benefits and adverse effect of SERMs as potential BC agents. RESULTS: Exhaustive literature studies suggested that SERMs having an agonistic, antagonistic or mixed activity to ER could efficiently inhibit BC cell proliferation. CONCLUSION: Each chemical class of SERMs comprises of some salient features and potentials, which may be further investigated to obtain novel effective SERMs in BC therapy.

BACKGROUND: Histone deacetylase 3 (HDAC3) has been studied in chronic heart failure (CHF), while the regulatory mechanism of HDAC3 on the development of CHF though regulating microRNA (miR)-26b-3p/high mobility group AT-hook 2 (HMGA2) axis has not been extensively investigated. This study aimed to probe the effects of HDAC3, miR-26b-3p and HMGA2 on CHF. METHODS: CHF rat models were established using aortic coarctation. Then the HDAC3, miR-26b-3p and HMGA2 levels in CHF rats were examined. Thereafter, the CHF rats were injected with relative oligonucleotides and plasmids of HDAC3, miR-26b-3p and HMGA2 to detect the cardiac function, inflammatory reaction, myocardial tissue pathological changes, and cardiomyocyte apoptosis. The binding relationship between miR-26b-3p and HMGA2 and the interaction between HDAC3 and miR-26b-3p were validated. RESULTS: HDAC3 and HMGA2 were elevated while miR-26b-3p was decreased in CHF rats. The reduced HDAC3 or HMGA2 or enriched miR-26b-3p attenuated cardiac dysfunction, inflammatory reaction, myocardial tissue pathological changes and cardiomyocyte apoptosis in CHF rats, while the reduction of miR-26b-3p exerted the opposite effects. Furthermore, the inhibition of the miR-26b-3p or elevation of HMGA2 reversed the effect of reduced HDAC3 on mitigating CHF progression. Mechanically, miR-26b-3p targeted HMGA2 and HDAC3 bound to miR-26-3p. CONCLUSION: Downregulation of HDAC3 relieves cardiac function in CHF rats via mediating miR-26b-3p/HMGA2 axis. This study provides novel theory references and a distinct direction for the therapy strategies of CHF.

Melatonin, mainly released from the pineal gland, also produced in the reproductive organs and cells, plays important roles in rhythms of the sleep-wake cycle, retardation of ageing processes, and antioxidant/anti-inflammatory functions. As a key mediator in reproductive systems, melatonin is participated in the reproductive process via regulating gamete and embryo development, and influences reproductive diseases and pregnancy outcome. The underlying mechanisms include epigenetic and other regulations, which are interesting for exploring new targets in prevention and treatments of reproductive diseases. This review discusses the relationship between melatonin and reproductive functions and dysfunction, as well as potential clinical applications of melatonin in reproductive medicine. Notably, Developmental Origins of Health and Diseases (DOHaD) is closely linked to reproduction, this article is the first to review the new progress in studies on possible relationship between melatonin and DOHaD.

Cinnamaldehyde (CNM) is a cyclic terpene alcohol found as the major compound of essential oils from some plants of the genus Cinnamomum (Lauraceae). CNM has several reported pharmacological activities that include antimicrobial, antivirulence, antioxidant and imunommodulatory effects. These properties make CNM an attractive lead molecule for development of anti-infective agents. In this descriptive review, we discuss the application of CNM in experimental models of microbial infection using invertebrate and vertebrate organisms. CNM (pure or in formulations) has been successfully applied in the treatment of infections caused by a range of bacterial (such as Cronobacter sakazakii, Escherichia coli, Listeria monocytogenes, Mycobacterium tuberculosis, Pseudomonas aeruginosa, Salmonella enterica, Staphylococcus aureus, Streptococcus agalactiae, Vibrio cholerae) and fungal (such as Aspergillus fumigatus, Candida albicans and Cryptococcus neoformans) pathogens. All these experimental evidence-based lessons have promoted the use of cinnamaldehyde as leading molecule for the development of new anti-infective drugs.

BACKGROUND: In the last few years in silico tools, including drug repurposing coupled with structure-based virtual screening, have been extensively employed to look for anti-COVID-19 agents. OBJECTIVE: The present review aims to provide readers with a portrayal of computational approaches that could conduct more quickly and cheaply to novel anti-viral agents. Particular attention is given to docking-based virtual screening. METHOD: The World Health Organization website was consulted to gain the latest information on SARS-CoV-2, its novel variants and their interplay with COVID-19 severity and treatment options. The Protein Data Bank was explored to look for 3D coordinates of SARS-CoV-2 proteins in their free and bound states, in the wild-types and mutated forms. Recent literature related to in silico studies focused on SARS-CoV-2 proteins was searched through PubMed. RESULTS: A large amount of work has been devoted thus far to computationally targeting viral entry and searching for inhibitors of the S-protein/ACE2 receptor complex. Another large area of investigation is linked to in silico identification of molecules able to block viral proteases -including Mpro- thus avoiding maturation of proteins crucial for virus life cycle. Such computational studies have explored the inhibitory potential of the most diverse molecule databases (including plant extracts, dietary compounds, FDA approved drugs). CONCLUSION: More efforts need to be dedicated in the close future to experimentally validate the therapeutic power of in silico identified compounds in order to catch, among the wide ensemble of computational hits, novel therapeutics to prevent and/or treat COVID-19.

Genistein (4',5,7-trihydroxyisoflavone) is a natural plant-derived phytoestrogen that can be found, for example, in soybean seeds. Genistein is present mainly in the human diet and is a common precursor in the antimicrobial phytoalexins biosynthesis and phytoanticipins in vegetables. The interest in genistein has increased due to its pharmacological effects, including anti-cancer activity, neuroprotective effects, cardiovascular protection, anti-inflammatory effects, antioxidant activity, and prevention of obesity. The most challenging issue for improving genistein is its low oral bioavailability, which has led to many animal and human pharmacokinetic studies and numerous clinical trials. Several drug delivery systems have been developed to protect and stabilize genistein to overcome the challenge of low bioavailability. This work concerns a revision of the literature reporting nano and microformulations for genistein encapsulation, including lipid nanoparticles, liposomes, tocotrienol-rich nanoemulsions, polymeric nanoparticles, dextran complexes, chitosan complexes, and Fe3O4 nanoparticles with carboxymethylated chitosan. Regarding the enormous potential of genistein, several clinical trials and marketed formulations can be found in the market.

Alzheimer's disease (AD) is a progressive neurodegenerative disease characterized by marked cognitive decline, memory loss, and spatio-temporal troubles and, in severe cases, lack of recognition of family members. Neurological symptoms, cognitive disturbances, and the inflammatory frame due to COVID-19, together with long-term effects, have fueled renewed interest in AD based on similar damage. COVID-19 also caused the acceleration of AD symptom onset. In this regard, the morbidity and mortality of COVID-19 were reported to be increased in patients with AD due to multiple pathological changes such as excessive expression of the viral receptor angiotensin-converting enzyme 2 (ACE2), comorbidities such as diabetes, hypertension, or drug-drug interactions in patients receiving polypharmacy and the high presence of proinflammatory molecules. Furthermore, the release of cytokines, neuroinflammation, oxidative stress, and ferroptosis in both diseases showed common underlying mechanisms, which together worsen the clinical picture and prognosis of these patients.

BACKGROUND: The topical use of vitamin C has been explored for many decades due to its antioxidant potential, whitening action, and the essential role it plays in the synthesis and maintenance of collagen. As Ascorbic Acid (AA) is unstable, derivative molecules and stabilization strategies have been explored to facilitate its incorporation into dermatological products. Even though these molecules are already for sale, there is still a shortage of scientific data regarding efficacy studies of these assets, especially in vivo. OBJECTIVE: The purpose of this review was to investigate and discuss issues regarding the topical application of vitamin C and its most common derivatives, including the difficulties, biases, and prospects for future clinical studies to better elucidate its effects. METHOD: A literature review was carried out to select studies that evaluated the topical use of ascorbic acid and/or its derivatives. The studies which are "fully available", "in vivo", and "in vitro" were used as inclusion criteria. RESULTS: Due to the instability of Ascorbic Acid, it is essential to study derivative molecules that maintain or even improve their effectiveness in dermatological products. Despite this, the studies of these derivatives, presented in the scientific literature, are mostly in vitro. In recent years, it has been possible to observe an increase in in vivo efficacy tests, and this trend is expected to continue in the future. However, they present very different approaches and issues. CONCLUSION: Studies of stability, safety, adverse reactions, and especially in vivo efficacy studies with a relevant number of subjects and standardized parameters are essential for better elucidating the effects of the topical application of vitamin C derivatives in comparison with ascorbic acid formulations for the skin.

OBJECTIVE: The purpose of this article is to describe the state-of-art of neuroanatomical and cellular aspects of the cerebellum in epilepsy. BACKGROUND: Over the years, cerebellum epileptogenesis has been widely studied. There is growing evidence linking the cerebellum with this pathology by several other structures involved: mainly the limbic system, thalamus, cerebral cortex, red nucleus, and reticular formation. As a result, these anatomical and cellular changes in the cerebellum might trigger the genesis and propagation of seizures. DISCUSSION: We herewith outline the cerebellum's deep nuclei physiological pathways, responsible for seizure spread via ion channels and neurotransmitter dysfunction. Additionally, we describe the shifts in seizures produced after cell death, gene expression, and protein interaction with their respective molecular and anatomical pathways. CONCLUSION: Finally, we highlight the role played by the cerebellum in seizure propagation to the brain and how it can be counteracted in some subtypes of drug-resistant epilepsy.

Atherosclerosis is a multifactorial result of complicated pathophysiology. Changes in the expression of polygenes, coupled with environmental and lifestyle factors, trigger a cascade of adverse events involving a variety of cell types, such as vascular endothelial cells, smooth muscle cells, and macrophages. In this review, we summarize the function and therapeutic targets of atherosclerotic cells. This article reviews the role of endothelial cells, smooth muscle cells, macrophages and foam cells in the development of atherosclerosis and the progress in the treatment of atherosclerosis by targeting these cells. Atherosclerotic plaque involves a variety of cells and biomolecules, and its complex biological environment is a difficult point for the study and treatment of atherosclerosis. For treating atherosclerosis, a large number of studies emerged based on blocking or inhibiting factors affecting the formation and development of plaque. Cardiovascular stent intervention is currently the main method for the treatment of atherosclerosis. In recent decades, numerous studies on cardiovascular, stents mainly involve drug coating or biomolecular modification of stents to enhance anti-thrombosis, anti-restenosis and endothelialization. This paper introduces the research status of cardiovascular stents and new strategies for surface modification. The treatment of atherosclerosis based on the level of molecular biology and cell biology is becoming a research hotspot in the coming decades.

BACKGROUND: graphene oxide (GO)-based systems are among the drug delivery systems and have drawn a lot of interest in the field of medicine. METHODS: In this work, two novel phosphoramides with the formulas of (NHCHCH2C(CH3)2NHC(CH3)2CH2P(S)(OEt)2 (L1) and (NHCHCH2C(CH3)2NHC(CH3)2CH2P (O) (NHC6H5) (OC5H6) (L2) were synthesized and characterized by spectroscopic methods. Then, graphene oxide (GO) was functionalized by L1 and L2. FT-IR, XRD, FE- SEM/ MAP, and Zeta potential analyses were applied to confirm the synthesis of phosphoramide-functionalized graphene oxides (GO-L1 and GO-L2). Cytotoxicity of synthesized compounds was evaluated against breast cancer cell line (SK-BR-3) using MTT assay. Moreover, the flow cytometry assay was performed to evaluate the cell death mechanisms. RESULTS: The results showed that GO-L1 and GO-L2 had more inhibitory effect against cancer cells than that of L1 and L2, and GO-L2 showed the highest cytotoxicity with IC50 value of 38.13 µg/ml. The Quantum calculations were employed to optimize structures. HOMO and LUMO energy values, and physical adsorption of synthesized compounds were obtained by the DMol3 module in Material studio 2017. The docking studies were used to investigate the binding of L1, L2, GO-L1, and GO-L2 to DNA polymerase IIα. CONCLUSION: Anticancer activity of phosphoramide compounds was increased after attachment on GO surface and the docking studies' results were in good accordance with the experimental cytotoxicity results.

Cocaine, also known as methyl benzoylecgonine, is one of the most famous drugs of abuse and one of the most ancient; however, there has been a recent increase in consumption of this substance. This trend has once again caught the attention of the scientific community. We discuss the current knowledge about this drug, focusing our attention on the forensic approach. Despite the fact that the cut-off of positivity to cocaine in drug tests is quite high, most current tests are able to detect much lower concentrations and could improve forensic sciences in both post-mortem investigations and in people screening. Immunological assays possessing substantial cross-reactivity to cocaine are particularly useful for screening oral fluid, hair, and post-mortem blood, where significant concentrations of the drug can be found. Liquid chromatography has now supplanted the previous techniques because it is very sensitive and specific and allows samples to be analyzed in a shorter time with only minimal sample preparation. Recent studies focus on increased sensitivity, reduced processing times, and cheaper analysis.

BACKGROUND: Cervical cancer is one of the most common types of cancer among women. Therefore, cancer studies are underway for a new chemo-agent with more effect on cancer cells and fewer side effects on normal human healthy cells. The currently studied novel ligand L2b as a reduced salicylaldimine derivative was examined in seven cell lines, HeLa, DU-145, PC3, DLD-1, ECC, HT-29, and PNT1-A as a control. AIM: Because of the antiproliferative ability of L2b, this study intends to look at the apoptotic, cytotoxic, and genotoxic activity of L2b on HeLa. METHODS: For this purpose, MTT assay is for screening cytotoxic effects, comet assay for looking for DNA damaging or genotoxicity levels, ELISA and DNA fragmentation for apoptotic measuring, AO/EB stain test for checking the rates of live, apoptotic and necrotic cells were performed. To reveal the oxidative state, OSI was assessed by total oxidant and antioxidant status ratios. FRAP assay was calculated for ferric-reducing antioxidant power, using total thiol and GSH assays to measure the antioxidant values of HeLa cells. RESULTS: Of this result, we have found a tremendous effect of L2b on HeLa cells, especially in raising the ROS rate, damaging their DNA, and causing a range of reactions leading to apoptosis. CONCLUSION: In conclusion, the data predict which ligand L2b is capable of rising apoptosis in vitro cervical cancer cell line studied. Further cancer studies are needed to reveal the apoptosis pathways of the ligand L2b in the HeLa cell line and its anticancer drug potency in vivo work.

We are experiencing a revolution in regenerative medicine. Recent developments in organoid technology have provided unique opportunities for studying human biology and diseases. Indeed, organoid models have revolutionized the in vitro culture tools for biomedical research by creating robust three-dimensional (3D) architecture to recapitulate the primary tissues' cellular heterogeneity, structure, and functions. Such organoid technology enables researchers to re-create human organs and diseases model in a culture dish. It thus holds excellent promises for many translational applications such as regenerative medicine, drug discovery, and precision medicine. This review summarizes the current knowledge on the progression and promotion of organoid models, particularly with the heart disease approach. We discuss the usefulness of clinical applications of cardiac organoids and ultimately highlight the currently advanced therapeutic strategies in vitro model of organoids aimed at personalizing heart disease treatment.

In recent years RNA has emerged as a medium with a broad spectrum of therapeutic potential, however, for years, a group of short RNA fragments was studied and considered therapeutic molecules. In nature, RNA plays both functions, with coding and non-coding potential. For RNA, like for any other therapeutic, to be used clinically, certain barriers must be crossed. Among them, there are biocompatibility, relatively low toxicity, bioavailability, increased stability, target efficiency and low off-target effects. In the case of RNA, most of these obstacles can be overcome by incorporating modified nucleotides into its structure. This may be achieved by both, in vitro and in vivo biosynthetic methods, as well as chemical synthesis. Some advantages and disadvantages of each approach are summarized here. The wide range of nucleotide analogues has been tested for their utility as monomers for RNA synthesis. Many of them have been successfully implemented and a lot of pre-clinical and clinical studies involved modified RNA is carried out. Some of these medications have already been introduced into clinics. After the huge success of RNA-based vaccines that were introduced into widespread use in 2020, and the introduction to the market of some RNA-based drugs, RNA therapeutics containing modified nucleotides appear to be the future of medicine.

INTRODUCTION: Organophosphorus compounds (OP) make up an important class of inhibitors, mostly employed as pesticides, even as chemical weapons. These toxic substances act through the inhibition of the acetylcholinesterase (AChE) enzyme, which results in elevated synaptic acetylcholine (ACh) levels, leading to serious adverse effects under the cholinergic syndrome. Many reactivators have been developed to combat the toxic effects of these AChE inhibitors. In this line, the oximes highlight because of their good reactivating power of cholinesterase enzymes. To date, there are not universal antidotes able to reactivate AChE inhibited by any OP agent. AREAS COVERED: This review summarizes the intoxication process by neurotoxic OP agents, along with the development of reactivators capable of reversing their effects, approaching aspects like therapeutic and toxicological profile of these antidotes. EXPERT OPINION: Computational methods and conscious in vitro studies, capable of significantly predicting the toxicological profile of these drug candidates, might support the process of development of these reactivators before entering in vivo studies in animals, and then clinical trials. These approaches can assist in the design of safer and more effective molecules, reducing related cost and time for the process.

OBJECTIVE: A simple pH and redox dual stimuli-responsive diketopyrrolopyrrole (DPP)-Cu2+ complexes gated mesoporous silica nanoparticles (MSN) were prepared for precise drug delivery and controlled drug release. METHOD: MSN was prepared by sol-gel method and then laminated. Carboxylic acid (CA)-Pyrrolo[3,4-c] pyrrole-1,4-dione, 2,5-dihydro-3,6-di-2-pyridinyl (PyDPP) was grafted onto the surface of amino-functionalized MSN (MSN-NH2) through a simple amide reaction and then complexed with Cu2+ to form gated molecules after doxorubicin (DOX) loading. RESULTS: Scanning electron microscopy (SEM), transmission electron microscopy (TEM), and Low-angle X-ray diffraction (XRD) showed that MSN with uniform particle size (100 nm) and porous structure was successfully prepared. The prepared MSN, MSN-NH2, and MSN-DPP were fully characterized by Zeta potential, Fourier transforms infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS) and nitrogen adsorption-desorption. High DOX-loading capacity (18.22%) and encapsulation efficiency (89.16%) were achieved by optimizing the mass ratio of MSN to DOX. Release studies showed that the gated molecules of our designed DPP-Cu2+ complexes had a good blocking effect under physiological conditions (the cumulative release rate of drugs within 24 hours was only 4.18%) and responded well to the pH and redox glutathione (GSH) dual stimuli. In vitro cytotoxicity assay showed that MSN-DPP-Cu2+ had good biocompatibility in both Hep G2 cells and L02 cells (the relative cell viability of both cells within 48 hours was above 97%), and the MSN-DPP-Cu2+@DOX could be triggered for efficient drug release in Hep G2 cells. CONCLUSION: The MSN-DPP-Cu2+ described in this research may be a good delivery system for the controlled release of antitumor drugs and can provide a potential possibility for clinical application in the future.