Novel 2,4,6-Trimethylbenzenesulfonyl Hydrazones with Antibacterial Activity: Synthesis and In Vitro Study

This research describes the synthesis and in vitro antimicrobial activity study of a series of 2,4,6-trimethylbenzenesulfonyl hydrazones. Twenty-five hydrazones (2–26) were synthesized on the basis of condensation reaction. The in vitro bioactivity study confirmed the potential application of obtained derivatives as antimicrobial agents. Among the tested compounds, the highest activity was discovered for derivative 24, which possessed minimal inhibitory concentration (MIC) ranging from 7.81 to 15.62 µg/mL against Gram-positive reference bacterial strains. Synthesized benzenesulfonyl hydrazones can be applied as potential ligands for the synthesis of bioactive metal complexes.     

Evaluation of the In Vitro Cytotoxic Activity of Caffeic Acid Derivatives and Liposomal Formulation against Pancreatic Cancer Cell Lines

Pancreatic cancer belongs to the most aggressive group of cancers, with very poor prognosis. Therefore, there is an important need to find more potent drugs that could deliver an improved therapeutic approach. In the current study we searched for selective and effective caffeic acid derivatives. For this purpose, we analyzed twelve compounds and evaluated their in vitro cytotoxic activity against two human pancreatic cancer cell lines, along with a control, normal fibroblast cell line, by the classic MTT assay. Six out of twelve tested caffeic acid derivatives showed a desirable effect. To improve the therapeutic efficacy of such active compounds, we developed a formulation where caffeic acid derivative (7) was encapsulated into liposomes composed of soybean phosphatidylcholine and DSPE-PEG₂₀₀₀. Subsequently, we analyzed the properties of this formulation in terms of basic physical parameters (such as size, zeta potential, stability at 4 °C and morphology), hemolytic and cytotoxic activity and cellular uptake. Overall, the liposomal formulation was found to be stable, non-hemolytic and had activity against pancreatic cancer cells (IC₅₀ 19.44 µM and 24.3 µM, towards AsPC1 and BxPC3 cells, respectively) with less toxicity against normal fibroblasts. This could represent a promising alternative to currently available treatment options.     

Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes

A library of 21 novel chiral 1,2,3-triazole-based 2-azabicycloalkane conjugates was designed and synthesized using the copper(I)-catalyzed click reaction. The obtained hybrids were assessed for their antiproliferative potency against three selected human cancer cell lines: Hs294T (melanoma), MIA PaCa-2 (pancreas tumor) and NCI-H1581 (lung tumor). The majority of the synthesized compounds demonstrated moderate to potent activity, and some of them appeared more selective than cisplatin, with selectivity index exceeding 9.     

Green Synthesis of Silver Nanoparticles Using Populi gemmae Extract: Preparation,Physicochemical Characterization,Antimicrobial Potential and In Vitro Antiproliferative Assessment

Green route is an economic, facile and eco-friendly method, employed for the synthesis of various types of nanoparticles, having it as a starting point biological entity, especially as a plant extract. The present study aims to obtain silver nanoparticles (AgNPs) starting from an ethanolic extract of Populi gemmae (Pg), by adjusting the reaction parameters. The morphological and structural characterization exhibited that both the reaction temperature and the concentration of metal salt, contributes to the obtaining of Pg-AgNPs with adjustable size and shape. The newly synthesized nanoparticles exhibited a good antibacterial activity on Gram-positive bacteria as well as antifungal activity. The in vitro antiproliferative activity of Pg-AgNPs was assessed on two different cancer cell lines (breast cancer cells—MCF7 and lung carcinoma epithelial cells—A549). Results have shown that the green-synthetized Pg-AgNPs_S2 (obtained at 60 °C, using AgNO₃ of 5 M) induced a substantial decrease in tumor cell viability in a dose-dependent manner with an IC₅₀ ranging from 5.03 to 5.07 µg/mL on A549 cell line and 3.24 to 4.93 µg/mL on MCF7 cell line.     

In Vitro and In Vivo Studies of the Trypanocidal Activity of Four Terpenoid Derivatives against Trypanosoma cruzi

Abstract. Four terpenoid derivatives were examined for their activity against Trypanosoma cruzi. Our results show that two compounds were very active in vitro against both extra- and intracellular forms. These compounds, non-toxic for the host cells, are more effective than the reference drug benznidazole. The capacity to infect cells was negatively affected and the number of amastigotes and trypomastigotes was reduced. A wide range of ultrastructural alterations was found in the epimastigote forms treated with these compounds. Some metabolic changes occurred presumably at the level of succinate and acetate production, perhaps caused by the disturbance of the enzymes involved in sugar metabolism inside the mitochondria. In vivo results were consistent with those observed in vitro. The parasitic load was significantly lower than in the control assay with benznidazole. The effects of these products showed the reduction of the anti-T. cruzi antibodies level during the chronic stage.     

Antiviral Activity of 3D,a Butene Lactone Derivative Against Influenza A Virus In Vitro and In Vivo

Influenza A virus is a highly variable and contagious respiratory pathogen that can cause annual epidemics and it poses an enormous threat to public health. Therefore, there is an urgent need for a new generation of antiviral drugs to combat the emergence of drug-resistant strains of the influenza virus. A novel series of butene lactone derivatives were screened and the compound 3D was selected, as it exhibited in vitro potential antiviral activity against A/Weiss/43 H1N1 virus with low toxicity. In addition, 3D dose-dependently inhibited the viral replication, expression of viral mRNA and viral proteins. 3D exerted a suppressive effect on A/Virginia/ATCC2/2009 H1N1 and A/California/2/2014 H3N2 in vitro. The time-of-addition analysis indicated that 3D suppressed H1N1 in the early stage of its life cycle. A/Weiss/43 H1N1-induced apoptosis in A549 cells was reduced by 3D via the mitochondrial apoptosis pathway. 3D could decrease the production of H1N1-induced pro-inflammatory cytokines that are induced by H1N1 in vitro and in vivo. The administration of 3D reduced lung lesions and virus load in vivo. These results suggest that 3D, which is a butene lactone derivative, is a promising agent for the treatment of influenza A virus infection.     

Synthesis and Anticancer Activity of Bagasse Xylan/Resveratrol Graft-Esterified Composite Nanoderivative

Biomass materials are high-quality raw materials for the preparation of natural, green and highly active functional materials due to their rich active groups, wide sources and low toxicity. Bagasse xylan (BX) and resveratrol (Res) were used as raw materials to introduce ethylene glycol dimethacrylate (EGDMA) via grafting reaction to obtain the intermediate product BX/Res-g-EGDMA. The intermediate was esterified with 3-carboxyphenylboronic acid (3-CBA) to obtain the target product 3-CBA-BX/Res-g-EGDMA. The BX/Res-composite-modified nanoderivative with antitumor activity was synthesized with the nanoprecipitation method. The effects of the reaction conditions on the grafting rate (G) of BX/Res-g-EGDMA and the degree of substitution (DS) of 3-CBA-BX/Res-g-EGDMA were investigated using single-factor experiments. The results showed that under the optimized process conditions, G and DS reached 142.44% and 0.485, respectively. The product was characterized with FTIR, XRD, TG-FTC, ¹H NMR and SEM, and its anticancer activity was simulated and tested. The results showed that 3-CBA-BX/Res-g-EGDMA had a spherical structure with an average particle size of about 100 nm and that its crystalline structure and thermal stability were different from those of the raw materials. In addition, 3-CBA-BX/Res-g-EGDMA showed the best docking activity with 2HE7 with a binding free energy of −6.3 kJ/mol. The inhibition rate of 3-CBA-BX/Res-g-EGDMA on MGC80-3 (gastric cancer cells) reached 36.71 ± 4.93%, which was 18 times higher than that of BX. Therefore, this material could be a potential candidate for biomedical applications.     

Activity of Melatonin and Other Pineal Indoles on the In Vitro Synthesis of Cortisol, Cortisone, and Adrenal Androgens

The in vitro effects of 13 indole compounds on the synthesis of glucocorticoids and of adrenal androgens in sheep adrenal glands has been studied from 11-deoxycortisol as a precursor. This work demonstrates the activating effect of some indole compounds on 11 beta-hydroxylase and 17,20-desmolase and the inhibitory effect of most of them on 11 beta-hydroxysteroid dehydrogenase. Three categories could be distinguished: 1) compounds without any effect (5-hydroxytryptophan, 5-hydroxytryptamine); 2) compounds moderately increasing (10-30% as compared with controls) cortisol yields (tryptamine, melatonin, 6-hydroxymelatonin, 5-methoxytryptophol, indomethacin); and 3) compounds markedly increasing (80-100%) cortisol yields (5-methoxyindole acetic acid, 5-hydroxyindole acetic acid, 2-methylindole, 5-hydroxytryptophol, N-acetyl-5-hydroxytryptamine). In fact, since most of the studied indoles reduced 11 beta-hydroxysteroid dehydrogenase activity, the actual activation of cortisol synthesis was four to five times less. Lastly, all the studied compounds, but melatonin, increased the activity of 17,20 desmolase as seen from 11 beta-hydroxyandrostenedione and 11-ketoandrostenedione yields. The possible in vivo effects of the indoles for therapeutic use needs further studying.     

Silver Nanoparticles Effects on In Vitro Germination,Growth, and Biochemical Activity of Tomato,Radish, and Kale Seedlings

The interactions between nanoparticles and plant cells are still not sufficiently understood, and studies related to this subject are of scientific and practical importance. Silver nanoparticles (AgNPs) are one of the most commonly produced and used nanomaterials. This study aimed to investigate the influence of AgNPs applied at the concentrations of 0, 50, and 100 mg·L⁻¹ during the process of in vitro germination as well as the biometric and biochemical parameters of developed seedlings in three vegetable species: Solanum lycopersicum L. ‘Poranek’, Raphanus sativus L. var. sativus ‘Ramona’, and Brassica oleracea var. sabellica ‘Nero di Toscana’. The application of AgNPs did not affect the germination efficiency; however, diverse results were reported for the growth and biochemical activity of the seedlings, depending on the species tested and the AgNPs concentration. Tomato seedlings treated with nanoparticles, particularly at 100 mg·L⁻¹, had shorter shoots with lower fresh and dry weights and produced roots with lower fresh weight. Simultaneously, at the biochemical level, a decrease in the content of chlorophylls and carotenoids and an increase in the anthocyanins content and guaiacol peroxidase (GPOX) activity were reported. AgNPs-treated radish plants had shorter shoots of higher fresh and dry weight and longer roots with lower fresh weight. Treatment with 50 mg·L⁻¹ and 100 mg·L⁻¹ resulted in the highest and lowest accumulation of chlorophylls and carotenoids in the leaves, respectively; however, seedlings treated with 100 mg·L⁻¹ produced less anthocyanins and polyphenols and exhibited lower GPOX activity. In kale, AgNPs-derived seedlings had a lower content of chlorophylls, carotenoids, and anthocyanins but higher GPOX activity of and were characterized by higher fresh and dry shoot weights and higher heterogeneous biometric parameters of the roots. The results of these experiments may be of great significance for broadening the scope of knowledge on the influence of AgNPs on plant cells and the micropropagation of the vegetable species. Future studies should be aimed at testing lower or even higher concentrations of AgNPs and other NPs and to evaluate the genetic stability of NPs-treated vegetable crops and their yielding efficiency.     

Interaction of Lactoferrin with Unsaturated Fatty Acids: In Vitro and In Vivo Study of Human Lactoferrin/Oleic Acid Complex Cytotoxicity

As shown recently, oleic acid (OA) in complex with lactoferrin (LF) causes the death of cancer cells, but no mechanism(s) of that toxicity have been disclosed. In this study, constitutive parameters of the antitumor effect of LF/OA complex were explored. Complex LF/OA was prepared by titrating recombinant human LF with OA. Spectral analysis was used to assess possible structural changes of LF within its complex with OA. Structural features of apo-LF did not change within the complex LF:OA = 1:8, which was toxic for hepatoma 22a cells. Cytotoxicity of the complex LF:OA = 1:8 was tested in cultured hepatoma 22a cells and in fresh erythrocytes. Its anticancer activity was tested in mice carrying hepatoma 22a. In mice injected daily with LF-8OA, the same tumor grew significantly slower. In 20% of animals, the tumors completely resolved. LF alone was less efficient, i.e., the tumor growth index was 0.14 for LF-8OA and 0.63 for LF as compared with 1.0 in the control animals. The results of testing from 48 days after the tumor inoculation showed that the survival rate among LF-8OA-treated animals was 70%, contrary to 0% rate in the control group and among the LF-treated mice. Our data allow us to regard the complex of LF and OA as a promising tool for cancer treatment.     

Antiviral Activity of Umifenovir In Vitro against a Broad Spectrum of Coronaviruses,Including the Novel SARS-CoV-2 Virus

An escalating pandemic of the novel SARS-CoV-2 virus is impacting global health, and effective antivirals are needed. Umifenovir (Arbidol) is an indole-derivative molecule, licensed in Russia and China for prophylaxis and treatment of influenza and other respiratory viral infections. It has been shown that umifenovir has broad spectrum activity against different viruses. We evaluated the sensitivity of different coronaviruses, including the novel SARS-CoV-2 virus, to umifenovir using in vitro assays. Using a plaque assay, we revealed an antiviral effect of umifenovir against seasonal HCoV-229E and HCoV-OC43 coronaviruses in Vero E6 cells, with estimated 50% effective concentrations (EC50) of 10.0 ± 0.5 µM and 9.0 ± 0.4 µM, respectively. Umifenovir at 90 µM significantly suppressed plaque formation in CMK-AH-1 cells infected with SARS-CoV. Umifenovir also inhibited the replication of SARS-CoV-2 virus, with EC50 values ranging from 15.37 ± 3.6 to 28.0 ± 1.0 µM. In addition, 21–36 µM of umifenovir significantly suppressed SARS-CoV-2 virus titers (≥2 log TCID50/mL) in the first 24 h after infection. Repurposing of antiviral drugs is very helpful in fighting COVID-19. A safe, pan-antiviral drug such as umifenovir could be extremely beneficial in combating the early stages of a viral pandemic.     

胃癌患者胸苷磷酸化酶的表达与以氟尿嘧啶类药物为基础化疗方案的敏感性:系统评价与Meta分析

[目的]评价胃癌患者胸苷磷酸化酶(TP)的表达与以氟尿嘧啶类药物为基础化疗方案的敏感性的关系。[方法]采用Cochrane系统评价方法,通过检索CNKI、Wanfangdata、PubMed、Springerlink、Cochrane library等数据库,收集国内外公开发表的所有相关病例对照研究。应用Stata 12.0软件进行Meta分析。[结果]共纳入10篇文献包含TP与临床胃癌化疗敏感性相关,且一线化疗方案以氟尿嘧啶类药物为主的病例对照研究,累计TP阳性表达病例共289例,累计TP阴性表达共21 2例。结果显示10篇文献具有同质性,χ~2=7.84,P=0.550,I~2=0%,TP表达阳性的患者与TP表达阴性的患者对以氟尿嘧啶类为基础的化疗方案敏感性差异有统计学意义,OR=2.531,95%CI(1.702~3.762),[结论]TP表达阳性的胃癌患者对以氟尿嘧啶类为基础的化疗方案有较为明显的敏感性。     

Synthesis and Structure–Activity Relationship of 2,6-Disubstituted Thiosemicarbazone Derivatives of Pyridine as Potential Antituberculosis Agents

In this study, six new 2,6-disubstituted thiosemicarbazone derivatives of pyridine were synthesized (4–9), and their tuberculostatic activity was evaluated. All of them showed two- to eightfold higher activity (minimum inhibitory concentration (MIC) 0.5–4 µg/mL) against the resistant strain compared with the reference drug. Compounds 5 and 7, which contained the most basic substituents—pyrrolidine and piperidine—in their structure, strongly inhibited the growth of the standard strain (MIC 2 µg/mL). Furthermore, the same derivatives exhibited activity comparable to that of the reference drugs against some types of Gram-positive bacteria (MIC 0.49 µg/mL) and showed no cytotoxicity (IC50 > 50 µg/mL) in HaCaT cells. The zwitterionic structure of each compound was determined using X-ray crystallography. Absorption, distribution, metabolism, and excretion analyses showed that all compounds are good drug candidates. Thus, compounds 5 and 7 were identified as leading structures for further research on antituberculosis drugs with extended effects.     

In Silico Analysis and Synthesis of Nafamostat Derivatives and Evaluation of Their Anti-SARS-CoV-2 Activity

Inhibition of transmembrane serine protease 2 (TMPRSS2) is expected to block the spike protein-mediated fusion of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Nafamostat, a potent TMPRSS2 inhibitor as well as a candidate for anti-SARS-CoV-2 drug, possesses the same acyl substructure as camostat, but is known to have a greater antiviral effect. A unique aspect of the molecular binding of nafamostat has been recently reported to be the formation of a covalent bond between its acyl substructure and Ser441 in TMPRSS2. In this study, we investigated crucial elements that cause the difference in anti-SARS-CoV-2 activity of nafamostat and camostat. In silico analysis showed that Asp435 significantly contributes to the binding of nafamostat and camostat to TMPRSS2, while Glu299 interacts strongly only with nafamostat. The estimated binding affinity for each compound with TMPRSS2 was actually consistent with the higher activity of nafamostat; however, the evaluation of the newly synthesized nafamostat derivatives revealed that the predicted binding affinity did not correlate with their anti-SARS-CoV-2 activity measured by the cytopathic effect (CPE) inhibition assay. It was further shown that the substitution of the ester bond with amide bond in nafamostat resulted in significantly weakened anti-SARS-CoV-2 activity. These results strongly indicate that the ease of covalent bond formation with Ser441 in TMPRSS2 possibly plays a major role in the anti-SARS-CoV-2 effect of nafamostat and its derivatives.     

Stereoselective Synthesis and Anticancer Activity of 2,6-Disubstituted trans-3-Methylidenetetrahydropyran-4-ones

In this report, we present efficient and stereoselective syntheses of 2,6-disubstituted trans-3-methylidenetetrahydropyran-4-ones and 2-(4-methoxyphenyl)-5-methylidenetetrahydropyran-4-one that significantly broaden the spectrum of the available methylidenetetrahydropyran-4-ones with various substitution patterns. Target compounds were obtained using Horner–Wadsworth–Emmons methodology for the introduction of methylidene group onto the pyranone ring. 3-Diethoxyphosphoryltetrahydropyran-4-ones, which were key intermediates in this synthesis, were prepared by fully or highly stereoselective addition of Gilman or Grignard reagents to 3-diethoxyphosphoryldihydropyran-4-ones. Addition occurred preferentially by axial attack of the Michael donors on the dihydropyranone ring. Relative configurations and conformations of the obtained adducts were assigned using a detailed analysis of the NMR spectra. The obtained methylidenepyran-4-ones were evaluated for cytotoxic activity against two cancer cell lines (HL-60 and MCF-7). 2,6-Disubstituted 3-methylidenetetrahydropyran-4-ones with isopropyl and phenyl substituents in position 2 were more cytotoxic than analogs with n-butyl substituent. Two of the most cytotoxic analogs were then selected for further investigation on the HL-60 cell line. Both analogs induced morphological changes characteristic of apoptosis in cancer cells, significantly inhibited proliferation and induced apoptotic cell death. Both compounds also generated DNA damage, and one of the analogs arrested the cell cycle of HL-60 cells in the G2/M phase. In addition, both analogs were able to inhibit the activity of topoisomerase IIα. Based on these findings, the investigated analogs may be further optimized for the development of new and effective topoisomerase II inhibitors.     

东方田鼠血清组分对日本血吸虫童虫的体外杀伤力

目的 探讨东方田鼠血清不同组分对日本血吸虫童虫的杀伤力，以期发现东方田鼠血清中参与其天然抗日本血吸虫的相关蛋白质。 方法 以离子交换柱层析及分子筛柱层析技术对东方田鼠血清蛋白质进行分离，将所得血清不同组分加入体外培养的2日龄日本血吸虫童虫中（100±20条/孔），计算童虫死亡率以判断血清不同组分对童虫的杀伤力。 结果 从东方田鼠血清分离出58个蛋白组分，其中6个组分具有明显的杀伤日本血吸虫童虫的活性，童虫死亡率均在37% 以上，特别是组分18.1的童虫死亡率达87.5%，而阴性对照组童虫死亡率为25.0%（P＜0.01）。 结论 东方田鼠血清中某些蛋白质参与其抗日本血吸虫的过程。     

Inhibition of Rat Brain Lipid Synthesis In Vitro by 4-Hydroxybutyric Acid

4-Hydroxybutyric acid (4HB) is accumulated in succinic semialdehyde dehydrogenase deficiency, an inherited metabolic disease severely affecting the CNS during postnatal development. Thus, the present study was designed to evaluate the in vitro influence of 4HB on lipid synthesis and CO₂ production from [U-¹⁴C] acetate in cerebral cortex of 30-day-old Wistar rats. In the presence of 4HB, there was an inhibition of lipid synthesis in cerebral cortex prisms and homogenates. However, no inhibition of lipid synthesis occurred in the homogenates free of nuclei and mitochondria. In addition, CO₂ production was inhibited by 4HB in cerebral cortex prisms, and homogenates and in the mitochondrial fraction. These results might possibly be explained by an impairment of mitochondrial metabolism by 4HB which may secondarily inhibit lipid synthesis. The results reported here may help to better understand the neuropathophysiology of 4-hydroxybutyric aciduria.     

In Vitro Evaluation of Anti-Rift Valley Fever Virus,Antioxidant and Anti-Inflammatory Activity of South African Medicinal Plant Extracts

Rift valley fever virus (RVFV) is a mosquito-borne virus endemic to sub-Saharan African countries, and the first sporadic outbreaks outside Africa were reported in the Asia-Pacific region. There are no approved therapeutic agents available for RVFV; however, finding an effective antiviral agent against RVFV is important. This study aimed to evaluate the antiviral, antioxidant and anti-inflammatory activity of medicinal plant extracts. Twenty medicinal plants were screened for their anti-RVFV activity using the cytopathic effect (CPE) reduction method. The cytotoxicity assessment of the extracts was done before antiviral screening using the MTT assay. Antioxidant and reactive oxygen/nitrogen species’ (ROS/RNS) inhibitory activity by the extracts was investigated using non-cell-based and cell-based assays. Out of twenty plant extracts tested, eight showed significant potency against RVFV indicated by a decrease in tissue culture infectious dose (TCID₅₀) < 10⁵. The cytotoxicity of extracts showed inhibitory concentrations values (IC₅₀) > 200 µg/mL for most of the extracts. The antioxidant activity and anti-inflammatory results revealed that extracts scavenged free radicals exhibiting an IC₅₀ range of 4.12–20.41 µg/mL and suppressed the production of pro-inflammatory mediators by 60–80% in Vero cells. This study demonstrated the ability of the extracts to lower RVFV viral load and their potency to reduce free radicals.     

Initiation Characteristics for the Synthesis of Five T4 Phage-Specific Messenger RNAs In Vitro

The involvement of the nucleoside triphosphates in the initiation of the synthesis of the messenger ribonucleic acid of five T4 specific enzymes has been studied. Only one of these, the messenger RNA for deoxynucleosidemonophosphate kinase, can be initiated in the presence of one nucleoside triphosphate, namely ATP. All of the remaining four require the presence of at least two nucleoside triphosphates during the initiation period. The combination of ATP and UTP was best for the initiation of messenger RNA for dihydrofolate reductase, ATP and CTP for deoxycytidylate hydroxymethyltransferase and beta-glucosyltransferase, and ATP and GTP for alpha-glucosyltransferase. We have concluded that there is a great variation in the nucleotide composition and sequence of the initiation sites in T4 DNA. No correlation in the requirements of nucleoside triphosphates during the initiation period could be observed among the five systems studied according to their classification as one type or another of "early" T4 messenger RNA.     

Assessment of SnFe2O4 Nanoparticles for Potential Application in Theranostics: Synthesis,Characterization, In Vitro,and In Vivo Toxicity

In this research, tin ferrite (SnFe₂O₄) NPs were synthesized via hydrothermal route using ferric chloride and tin chloride as precursors and were then characterized in terms of morphology and structure using Fourier-transform infrared spectroscopy (FTIR), Ultraviolet–visible spectroscopy (UV-Vis), X-ray power diffraction (XRD), Scanning electron microscopy (SEM), Transmission electron microscopy (TEM), and Brunauer–Emmett–Teller (BET) method. The obtained UV-Vis spectra was used to measure band gap energy of as-prepared SnFe₂O₄ NPs. XRD confirmed the spinel structure of NPs, while SEM and TEM analyses disclosed the size of NPs in the range of 15–50 nm and revealed the spherical shape of NPs. Moreover, energy dispersive X-ray spectroscopy (EDS) and BET analysis was carried out to estimate elemental composition and specific surface area, respectively. In vitro cytotoxicity of the synthesized NPs were studied on normal (HUVEC, HEK293) and cancerous (A549) human cell lines. HUVEC cells were resistant to SnFe₂O₄ NPs; while a significant decrease in the viability of HEK293 cells was observed when treated with higher concentrations of SnFe₂O₄ NPs. Furthermore, SnFe₂O₄ NPs induced dramatic cytotoxicity against A549 cells. For in vivo study, rats received SnFe₂O₄ NPs at dosages of 0, 0.1, 1, and 10 mg/kg. The 10 mg/kg dose increased serum blood urea nitrogen and creatinine compared to the controls (P < 0.05). The pathology showed necrosis in the liver, heart, and lungs, and the greatest damages were related to the kidneys. Overall, the in vivo and in vitro experiments showed that SnFe₂O₄ NPs at high doses had toxic effects on lung, liver and kidney cells without inducing toxicity to HUVECs. Further studies are warranted to fully elucidate the side effects of SnFe₂O₄ NPs for their application in theranostics.