In Vitro Cytotoxic Potential and In Vivo Antitumor Effects of NOS/PDK-Inhibitor T1084.

Previously, we showed the antitumor activity of the new NOS/PDK inhibitor T1084 (1-isobutanoyl-2-isopropylisothiourea dichloroacetate). The present study included an assessment of in vitro cytotoxicity against human malignant and normal cells according to the MTT-test and in vivo antitumor effects in solid tumor models in comparison with precursor compounds T1023 (NOS inhibitor; 1-isobutanoyl-2-isopropylisothiourea hydrobromide) and Na-DCA (PDK inhibitor; sodium dichloroacetate), using morphological, histological, and immunohistochemical methods. The effects of T1084 and T1023 on the in vitro survival of normal (MRC-5) and most malignant cells (A375, MFC-7, K562, OAW42, and PC-3) were similar and quantitatively equal. At the same time, melanoma A375 cells showed 2-2.5 times higher sensitivity (IC50: 0.39-0.41 mM) to the cytotoxicity of T1023 and T1084 than other cells. And only HeLa cells showed significantly higher sensitivity to the cytotoxicity of T1084 compared to T1023 (IC50: 0.54 ± 0.03 and 0.81 ± 0.02 mM). Comparative studies of the in vivo antitumor effects of Na-DCA, T1023, and T1084 on CC-5 cervical cancer and B-16 melanoma in mice were conducted with subchronic daily i.p. administration of these agents at an equimolar dose of 0.22 mmol/kg (33.6, 60.0, and 70.7 mg/kg, respectively). Cervical cancer CC-5 fairly quickly evaded the effects of both Na-DCA and T1023. So, from the end of the first week of Na-DCA or T1023 treatment, the tumor growth inhibition (TGI) began to decrease from 40% to an insignificant level by the end of the observation. In contrast, in two independent experiments, CC-5 showed consistently high sensitivity to the action of T1084: a significant antitumor effect with high TGI (43-58%) was registered throughout the observation, without any signs of neoplasia adaptation. The effect of precursor compounds on melanoma B-16 was either minimal (for Na-DCA) or moderate (for T1023) with TGI only 33%, which subsequently decreased by the end of the experiment. In contrast, the effect of T1084 on B-16 was qualitatively more pronounced and steadily increasing; it was accompanied by a 3-fold expansion of necrosis and dystrophy areas, a decrease in proliferation, and increased apoptosis of tumor cells. Morphologically, the T1084 effect was 2-fold superior to the effects of T1023-the TGI index reached 59-62%. This study suggests that the antitumor effects of T1084 develop through the interaction of NOS-dependent and PDK-dependent pathophysiological effects of this NOS/PDK inhibitor. The NOS inhibitory activity of T1084 exerts an anti-angiogenic effect on neoplasia. At the same time, the PDK inhibitory activity of T1084 enhances the cytotoxicity of induced intratumoral hypoxia and suppresses the development of neoplasia adaptation to anti-angiogenic stress. Such properties allow T1084 to overcome tumor resistance and realize a stable synergistic antitumor effect.

Cytotoxic Effects of Oleanane-type Saponins from Lysimachia laxa.

Phytochemical investigation of the methanol extract of the aerial parts of Lysimachia laxa led to the isolation of four new oleanane-type saponins, lysimosides A-D (1-4) and one known compound, lysimachigenoside B (5). Their structures were elucidated using a combination of HR-ESI-MS, 1D and 2D-NMR spectral data, chemical methods, and comparison with previous literature. The cytotoxic activity of these compounds was evaluated against human lung cancer (A-549) and human breast cancer (MCF-7) cell lines. All compounds exhibited cytotoxic activity against A-549 and MCF-7 cell lines with IC50 values ranging from 6.1 to 16.0 µM, comparable to the positive control, mitoxantrone. Interestingly, oleanane-type saponins with an acetyl group (2-4) exhibited increased cytotoxic activities compared to those without an acetyl group (1).

Cytotoxic, antioxidant, antibacterial activity of phytochemicals from Phragmanthera austroarabica.

The cytotoxic, antioxidant, anticancer, and antibacterial properties of ethanolic extracts from Phragmanthera austroarabica is of interest. Plants of P. austroarabica were gathered from the southern Saudi Arabian region of Albaha. P. austroarabica extract was assessed using DPPH (2, 2-diphenyl-1-picrylhydrazyl). The German Collection of Microorganisms and Cell Cultures (DSMZ) cancer cell lines used in this investigation. The cytotoxic activity of P. austroarabica extract was explored against MCF-7 breast and A549 lung cancer cell lines, along with doxorubicin as a positive control. In both treated cells, P. austroarabica showed a remarkable activity via suppressing the cell's survival. In terms of IC50 (concentration equivalent to a survival rate of 50%), MCF-7 breast cancer cells were more sensitive to P. austroarabica extract.) DPPH colorimetric assay was employed to assess the antioxidant properties of P. austroarabica extract, the antioxidant activity was increased along with increment of extract concentrations. The leaves aqueous extract of P. austroarabica inhibited the growth of S. aureus by 6.3±0.12 mm and 24±0.43 mm and 15±0.56 mm respectively for seed, leaf and stem at concentrations 50 µl. However, the same concentrations inhibited the growth of E. coli by 25±0.75, 0.00 mm and 24±0.18 mm, following the same order. Different superscript letters indicate means that are significantly different at level (p<0.05). Minimal inhibitory concentrations (MIC) of P. austroarabica ethanolic extracts against the tested microorganisms were 1.5, 1.6 and 1.5, respectively for seed, leaf and stem against Staph. Aureus and were 1.2, 0.00 and 1.2, respectively for seed, leaf and stem against E. coli.

Characterization and Biomedical Applications of Green-Synthesized Selenium Nanoparticles Using Tridax procumbens Stem Extract.

Background Selenium nanoparticles (SeNPs) are one of the metal nanoparticles that have been widely utilized for their anti-microbial, anti-oxidant, anti-inflammatory activities, and other biomedical applications. Tridax procumbens (TP) stem extract is a promising herb species rich in flavonoids, tannins, alkaloids, phytosterols, and hydroxycinnamates, which play a major role in wound healing applications.  Aim The study aims to synthesize SeNPs using TP stem extract, characterizations, and its biomedical applications. Materials and methods SeNPs were synthesized using TP stem extract. The green synthesis of SeNPs was confirmed by ultraviolet-visible (UV-vis) spectra analysis. The synthesized SeNPs were characterized using Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The agar well diffusion method was utilized to evaluate the anti-bacterial properties of the green synthesized SeNPs using TP stem extract. The anti-oxidant effect of SeNPs was tested using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, ferric-reducing anti-oxidant power assay (FRAP), and hydroxyl radical scavenging assay (H2O2). The anti-inflammatory effect was investigated using the bovine serum albumin assay and egg albumin denaturation method, and the cytotoxic effect of the green synthesized SeNPs was tested using the brine shrimp lethality (BSL) assay. Results The green synthesis of SeNPs was confirmed using different types of analysis techniques. The characterizations were done by UV-visible spectroscopy analysis, exhibiting a maximum peak at the range of 330 nm. SEM analysis revealed the shape of the nanoparticle to be hexagonal. The agar well diffusion method exhibited the anti-bacterial efficacy of SeNPs against wound microorganisms with a zone of inhibition of 14.6 mm for Escherichia coli (E. coli), 15.8 mm for Staphylococcus aureus (S. aureus), and 15.4 mm for Pseudomonas aeruginosa (P. aeruginosa). The TP stem-mediated SeNPs showed potential effects in anti-oxidant, anti-inflammatory, and cytotoxic activity, which shows very little toxicity. Conclusion Overall, the green synthesis of TP-stem-mediated SeNPs has great potential in biomedical applications. Thus, the synthesized SeNPs exhibit significant anti-bacterial efficacy against wound pathogens. The TP stem-mediated SeNPs showed potential effects in anti-oxidant, anti-inflammatory, and cytotoxic activity, which shows low toxicity. Furthermore, the green-synthesized SeNPs can be utilized in therapeutic management.

Antimicrobial, Antioxidant and Cytotoxic Effects of Essential Oil, Fatty Acids and Bioactive Compounds of Beta vulgaris var. crassa (Fodder Beet).

Beta vulgaris var. crassa is undoubtedly a very important plant that is not used enough in the world. In this study, it was aimed to determine the cytotoxic activities of the components (essential oils, fatty acids, total phenol and flavonoid) found in the leaf parts of Beta vulgaris var. crassa against PC-3, MCF-7 and HeLa cancer cell lines. In addition, the effectiveness of these ingredients against bacteria and fungi that can cause serious health problems in humans was tested. In experiments, three tumor cell lines were exposed to various plant extract concentrations (31.25, 62.5, 125, 250, 500 and 1000 µg/mL) for 72 h. It was found that plant extracts showed high (SI: 2.14 > 2) cytotoxicity to PC-3 cells, moderate (SI: 1.62 < 2) to HeLa cells, and low (SI: 0.93 < 2) cytotoxicity to MCF-7 cells. Also, different plant extract concentrations were found to cause an inhibition rate of 16.3-22.3% in Staphylococcus aureus, 16.8-23.5% in Streptococcus pyogenes and 12-16.2% in Cutibacterium acnes. Similarly, inhibition rates were determined between 9.5-20.7% for Candida albicans, 3.5-7.7% for Candida auris, and 5.5-15.1% for Candida glabrata. The results showed that the plant extract exhibited a concentration-dependent cytotoxic and antimicrobial effect against both cancer cell lines and microbial pathogens. Supplementary Information: The online version contains supplementary material available at 10.1007/s12088-024-01269-8.

New nano-complexes targeting protein 3S7S in breast cancer and protein 4OO6 in liver cancer investigated in cell line.

Cancer, a lethal ailment, possesses a multitude of therapeutic alternatives to combat its presence, metal complexes have emerged as significant classes of medicinal compounds, exhibiting considerable biological efficacy, especially as anticancer agents. The utilization of cis-platin in the treatment of various cancer types, including breast cancer, has served as inspiration to devise novel nanostructured metal complexes for breast cancer therapy. Notably, homo- and hetero-octahedral bimetallic complexes of an innovative multifunctional ether ligand (comprising Mn(II), Ni(II), Cu(II), Zn(II), Hg(II), and Ag(I) ions) have been synthesized. To ascertain their structural characteristics, elemental and spectral analyses, encompassing IR, UV-Vis, 1H-NMR, mass and electron spin resonance (ESR) spectra, magnetic moments, molar conductance, thermal analysis, and electron microscopy, were employed. The molar conductance of these complexes in DMF demonstrated a non-electrolytic nature. Nanostructured forms of the complexes were identified through electron microscopic data. At ambient temperature, the ESR spectra of the solid complexes exhibited anisotropic and isotropic variants, indicative of covalent bonding. The ligand and several of its metal complexes were subjected to cytotoxicity testing against breast cancer protein 3S7S and liver cancer protein 4OO6, with the Ag(I) complex (7) evincing the most potent effect, followed by the Cu(II) with ligand (complex (2)), Cis-platin, the ligand itself, and the Cu(II)/Zn(II) complex (8). Molecular docking data unveiled the inhibitory order of several complexes.

Identification and bioactivity evaluation of twelve previously undescribed depsidone derivatives from Garcinia oligantha.

Phytochemical studies on the leaves and twigs of Garcinia oligantha Merr. led to the isolation of twelve previously undescribed depsidone derivatives (oliganthdepsidones A-L, 1-12). Their structures were elucidated by extensive spectroscopic analysis including 1H and 13C NMR, HSQC, HMBC and NOESY along with HRESIMS. The structures of oliganthdepsidones G and J were finally determined using DFT-NMR chemical shift calculations and DP4+ methods. Cytotoxicity test in four human cancer cell lines indicated that oliganthdepsidone F had relatively strong cytotoxic effect against A375 (melanoma), A549 (lung cancer), HepG2 (liver cancer), and MCF-7 (breast cancer) cell lines with IC50 of 18.71, 15.44, 10.92, and 15.90 µM, respectively. The dose- and time-dependent antiproliferative effects of oliganthdepsidone F on these cell lines were also observed by CCK-8 test. As determined by fluorescent microscopy and flow cytometry in these cell lines, oliganthdepsidone F could promote cell apoptosis, leading to the inhibition of cell proliferation. The results of wound healing assay and transwell assay showed that oliganthdepsidone F could inhibit the migration and invasion of A549 and MCF-7 cell lines in a concentration-dependent manner.

Evaluation of Antidiabetic Activity and Cytotoxic Effect of Strontium Nanoparticles Synthesized Using Mimosa Pudica.

Nanotechnology is emerging as a promising approach in the development of novel therapeutic strategies. Nanoparticles, due to their unique physicochemical properties and small size, have the potential to improve the delivery of therapeutic agents, enhance their bioavailability, and increase their efficacy. Among various types of nanoparticles, strontium nanoparticles have gained attention due to their potential antidiabetic activity and cytotoxic effects against cancer cells. Mimosa pudica, also known as "Sensitive Plant" or "Touch-Me-Not," is a medicinal plant known for its diverse pharmacological activities, including antidiabetic and anticancer properties. Recent research has focused on the synthesis of strontium nanoparticles by using Mimosa pudica as a green and sustainable approach. These nanoparticles have shown promising results in terms of their antidiabetic activity and cytotoxic effects against cancer cells. Thus, in this study, the antidiabetic effect was studied using the alpha-amylase inhibitor assay, and the cytotoxic effect was studied using the brine shrimp lethality assay. In these assays, increasing concentration of Mimosa pudica-mediated strontium nanoparticles exhibited increasing antidiabetic and cytotoxic effects, which was similar to the standard used, which is acarbose. Hence, this can be used as a novel antidiabetic and cytotoxic agent in the future.

Graphene-Functionalized Titanium Carbide Synthesis and Characterization and Its Cytotoxic Effect on Cancer Cell Lines.

Background Graphene is a versatile material with promising applications in various fields such as electronics, energy, biomedicine, and the environment due to its exceptional mechanical strength, thermal and electrical conductivity, transparency, and chemical stability. Graphene has been extensively used in biological and medical settings. MXene is a two-dimensional (2D) material that exhibits a strong affinity for water and electrical conductivity because of its surface terminations (oxygen {-O}, fluorine {-F}, and hydroxyl {-OH}) and transition metal carbide or nitride. MXene has attracted significant attention recently for its wide range of applications and unique properties. This study focuses on the synthesis and characterization of graphene-functionalized MXene. Furthermore, we investigated its cytotoxic effects on cancer cell lines. The characterization of graphene-functionalized MXene is carried out using scanning electron microscopy (SEM), X-ray diffraction(XRD), and Fourier transform infrared spectroscopy (FTIR) assays. Materials and methods Graphene powder was finely ground in isopropyl alcohol and then sonicated for two hours to produce solution A. MXene was synthesized by reacting titanium aluminum carbide (Ti3AlC3) with hydrofluoric acid (HF). A mixture of Ti3AlC3 and HF was heated to 40°C with continuous stirring for 24 hours to form solution B. Subsequently, solutions A and B were combined and stirred for 30 minutes. The resulting mixture was transferred to a hydrothermal reactor and maintained at 180°C for 12 hours. After the completion of the reaction, the resulting material was cooled to room temperature and purified through washing with distilled water, ethanol, and acetone. The sample was then dried at 80°C for 12 hours. Results The X-ray diffraction (XRD) study confirms the formation of graphene-functionalized titanium carbide (Ti3C2). The sharp peaks indicate a highly crystalline nature. Graphene is a sheet-like structure with numerous gaps. Particles exhibit a multitude of voids and pores on their surfaces. Upon incorporation, graphene displays a small sheet-like structure. Graphene-functionalized titanium carbide confirms the presence of distinct layered or sheet-like structures stacked together. Following the addition of the material, some cancer cells are eradicated, and they exhibit increased biocompatibility, demonstrating anticancer activity. Conclusion Graphene-functionalized titanium carbide has been successfully synthesized and characterized, as evidenced by various analytical methods such as X-ray diffraction (XRD), scanning electron microscopy (SEM), and methyl-thiazoldiphenyl-tetrazolium (MTT) assays. The cytotoxic impact of the synthesized graphene-functionalized titanium carbide on cancer cell lines was examined. The findings reveal a notable cytotoxic effect, indicating its potential as an anticancer agent. Further research in collaboration with experts from diverse fields will be crucial to advance and translate this technology into practical applications for cancer patients. Future scope Graphene and titanium carbide are promising materials for cancer research, biomedical applications, and imaging. Nevertheless, additional research is required to comprehend their mechanisms, enhance their properties, assess their safety and efficacy, and conduct clinical trials.

Oridonin, a small molecule inhibitor of cancer stem cell with potent cytotoxicity and differentiation potential.

Cancer stem cells (CSCs) drive malignant tumor progression, recurrence, and metastasis with unique characteristics, including self-renewal and resistance to conventional treatments. Conventional differentiation inducers, although promising, have limited cytotoxicity and may inadvertently enhance CSC stemness. To address these challenges, ongoing efforts are dedicated to developing strategies that can effectively combine both cytotoxicity and differentiation-inducing effects. In this study, we introduce oridonin (Ori), a small molecule with dual differentiation-inducing and cytotoxicity properties capable of eliminating tumor CSCs. We isolated CSCs in B16F10 cells using the Hoechst side population method and assessed the differentiation effect of Ori. Ori's differentiation-inducing effect was further evaluated using human acute promyelocytic leukemia. The cytotoxic potential of Ori against MCF-7 and B16F10 cell lines was assessed through various methods. In vivo anti-tumor and anti-CSC efficacy of Ori was investigated using mouse melanoma and CSCs melanoma models. Safety evaluation included zebrafish embryotoxicity and mouse acute toxicity experiments. As a result, Ori effectively dismantles tumorspheres, inhibits proliferation, and reduces the expression of CSC-specific markers. It induces significant differentiation, especially in the case of NB4. Additionally, Ori upregulates TP53 expression, mitigates the hypoxic tumor microenvironment, suppresses stemness, and inhibits PD-L1 expression, prompting a robust anti-cancer immune response. Ori demonstrates pronounced cytotoxicity, inducing notable pro-apoptotic effects on B16F10 and MCF-7 cells, with specific triggering of mitochondrial apoptosis. Importantly, Ori maintains a commendable biosafety record. The dual-action prowess of Ori not only induces the differentiation of CSCs but also dispatches differentiated and residual tumor cells, effectively thwarting the relentless march of tumor progression.

Protocol for Testing the Effects of ssDNA Aptamer in HeLa and MCF-7.

Conventional approaches for treating tumors encompass chemotherapy, radiotherapy, and surgery. However, these methods come with their limitations when applied in clinical practice. Aptamers are often referred to as "chemical antibodies" and consist of short DNA or RNA molecules, designed to bind to a wide range of targets, including proteins or nucleic acid structures. They exhibit strong affinities and remarkable specificity for their target molecules, making them capable of functioning as therapeutic agents to directly impede tumor cell proliferation. This approach helps minimize the harm to normal cells, thus reducing toxicity through decreased side effects. Here we report the procedure to develop ssDNA aptamer and investigate its ability to inhibit cancer cell proliferation in HeLa and MCF-7 cancer cell lines.

New Thiosemicarbazide Derivatives with Multidirectional Biological Action.

Over the years, several new medicinal substances have been introduced for the treatment of diseases caused by bacteria and parasites. Unfortunately, due to the production of numerous defense mechanisms by microorganisms and parasites, they still pose a serious threat to humanity around the world. Therefore, laboratories all over the world are still working on finding new, effective methods of pharmacotherapy. This research work aimed to synthesize new compounds derived from 3-trifluoromethylbenzoic acid hydrazide and to determine their biological activity. The first stage of the research was to obtain seven new compounds, including six linear compounds and one derivative of 1,2,4-triazole. The PASS software was used to estimate the potential probabilities of biological activity of the newly obtained derivatives. Next, studies were carried out to determine the nematocidal potential of the compounds with the use of nematodes of the genus Rhabditis sp. and antibacterial activity using the ACCT standard strains. To determine the lack of cytotoxicity, tests were performed on two cell lines. Additionally, an antioxidant activity test was performed due to the importance of scavenging free radicals in infections with pathogenic microorganisms. The conducted research proved the anthelmintic and antibacterial potential of the newly obtained compounds. The most effective were two compounds with a 3-chlorophenyl substituent, both linear and cyclic derivatives. They demonstrated higher efficacy than the drugs used in treatment.

Inclusion Complexes of Litsea cubeba (Lour.) Pers Essential Oil into ß-Cyclodextrin: Preparation, Physicochemical Characterization, Cytotoxicity and Antifungal Activity.

The uses of natural compounds, such as essential oils (EOs), are limited due to their instability to light, oxygen and temperature, factors that affect their application. Therefore, improving stability becomes necessary. The objective of this study was to prepare inclusion complexes of Litsea cubeba essential oil (LCEO) with ß-cyclodextrin (ß-CD) using physical mixing (PM), kneading (KN) and co-precipitation (CP) methods and to evaluate the efficiency of the complexes and their physicochemical properties using ATR-FTIR, FT-Raman, DSC and TG. The study also assessed cytotoxicity against human colorectal and cervical cancer cells and antifungal activity against Aspergillus flavus and Fusarium verticillioides. The complexation efficiency results presented significant evidence of LCEO:ß-CD inclusion complex formation, with KN (83%) and CP (73%) being the best methods used in this study. All tested LCEO:ß-CD inclusion complexes exhibited toxicity to HT-29 cells. Although the cytotoxic effect was less pronounced in HeLa tumor cells, LCEO-KN was more active against Hela than non-tumor cells. LCEO-KN and LCEO-CP inclusion complexes were efficient against both toxigenic fungi, A. flavus and F. verticillioides. Therefore, the molecular inclusion of LCEO into ß-CD was successful, as well as the preliminary biological results, evidencing that the ß-CD inclusion process may be a viable alternative to facilitate and increase future applications of this EO as therapeutic medication, food additive and natural antifungal agent.

Establishment and characterization of a golden pompano (Trachinotus blochii) fin cell line for applications in marine fish pathogen immunology.

Pompano fishes have been widely farmed worldwide. As a representative commercial marine species of the Carangidae family, the golden pompano (Trachinotus blochii) has gained significant popularity in China and worldwide. However, because of rapid growth and high-density aquaculture, the golden pompano has become seriously threatened by various diseases. Cell lines are the most cost-effective resource for in vitro studies and are widely used for physiological and pathological research owing to their accessibility and convenience. In this study, we established a novel immortal cell line, GPF (Golden pompano fin cells). GPF has been passaged over 69 generations for 10 months. The morphology, adhesion and extension processes of GPF were evaluated using light and electron microscopy. GPF cells were passaged every 3 days with L-15 containing 20 % fetal bovine serum (FBS) at 1:3. The optimum conditions for GPF growth were 28 °C and a 20 % FBS concentration. DNA sequencing of 18S rRNA and mitochondrial 16S rRNA confirmed that GPF was derived from the golden pompano. Chromosomal analysis revealed that the number pattern of GPF was 48 chromosomes. Transfection experiments demonstrated that GPF could be utilized to express foreign genes. Furthermore, heavy metals (Cd, Cu, and Fe) exhibited dose-dependent cytotoxicity against GPF. After polyinosinic-polycytidylic acid (poly I:C) treatment, transcription of the retinoic acid-inducible gene I-like receptor (RLR) pathway genes, including mda5, mita, tbk1, irf3, and irf7 increased, inducing the expression of interferon (IFN) and anti-viral proteins in GPF cells. In addition, lipopolysaccharide (LPS) stimulation up-regulated the expression of inflammation-related factors, including myd88, irak1, nfκb, il1ß, il6, and cxcl10 expression. To the best of our knowledge, this is the first study on the immune response signaling pathways of the golden pompano using an established fin cell line. In this study, we describe a preliminary investigation of the GPF cell line immune response to poly I:C and LPS, and provide a more rapid and efficient experimental material for research on marine fish immunology.

Onco-therapeutic Effect of Novel Triterpenoid Compound Oleanolic Acid Isolated and Characterized from the Methanolic Extract of Coldenia procumbens (Linn.).

India is considered a hub for a wide range of phytochemicals due to its rich biodiversity, which indeed flourished with many folk medicines and treatments. Phytochemicals are secondary metabolites synthesized in plants to protect themselves from deteriorating environmental stress and defense against pathogens. In the present study, we aimed to explore the strong anticancer potential of the bioactive compound present in the leaf extract of Coldenia procumbens (L.). The bioactive compound oleanolic acid was first time reported in the plant and was successfully isolated, characterized with various spectroscopic analyses. The in vitro study results explored that oleanolic acid has shown a potent cytotoxic effect against human hepatocellular carcinoma cell lines with a low IC50 value (40.66µg/mL) and induced apoptotic cell death. Overall, the present findings clearly demonstrated that the natural triterpenoid compound oleanolic acid isolated from C. procumbens showed a potent cytotoxic effect against HepG2 cells and explored the strong anticancer potential against liver cancer.

Doxorubicin loaded cerium substituted hydroxyapatite nanoparticles: A promising new therapeutic approach for bone regeneration, doxorubicin delivery, and cancer treatment.

The current study used the precipitation method to prepare pure calcium hydroxyapatite (HA) and cerium-substituted hydroxyapatite (Ce-HA) nanoparticles, where cerium ions were exchanged into the HA structure at different concentrations ranging from 3 to 7 wt%. X-ray powder diffraction (XRD), field emission scanning electron microscopy (FE-SEM), high resolution transmission electron microscopy (HR-TEM), Fourier transform infrared (FTIR) spectroscopy, Brunauer-Emmett-Teller (BET) surface area measurements, and zeta potential were used to examine the structural characteristics of the nanoparticles. Additionally, the antibacterial and antifungal effects of the produced materials on Gram-positive, Gram-negative, and fungal bacterial species were studied. Nanoparticles with cerium doping showed effective antibacterial and antifungal properties. All samples were tested for bioactivity in simulated body fluid (SBF), and the formation of an apatite layer on their surfaces was highlighted using SEM in conjunction with energy-dispersive X-rays (EDX).Doxorubicin (DOX) release from Ce-HA nanoparticles and pure HA was tested in phosphate-buffered saline (PBS) for up to 28 days. Both nanoparticles were able to release the drug while still being semi-fully loaded. Similarly, the cytotoxic effect of all produced samples on the MG-63 cell line was evaluated, and all samples showed good cytocompatibility. The cytotoxic effect of doxorubicin-loaded nanoparticles showed promising anticancer activity against bone cancer cells, especially samples with high cerium content. The resulting nanoparticles show excellent promising ability for the delivery of doxorubicin to bone cancer with the capacity for bone regeneration.

Preparation of a Herbal Mouthwash With Lemongrass and Mint-Mediated Zinc Oxide Nanoparticles and Evaluation of Its Antimicrobial and Cytotoxic Properties.

Introduction Nanotechnology holds considerable importance in biomedical and dental applications. Nanoparticles synthesized using green synthesis methods with herbal formulations offer various benefits to humans. Zinc oxide nanoparticles (ZnONPs), being semiconductors, exhibit potent antibacterial properties. Notably, treatments utilizing lemongrass and mint ensure potentially lower toxicity and antibacterial qualities for oral infections. The goal of the study is to prepare a mouthwash mediated by ZnONPs and assess its cytotoxic potential and antibacterial efficacy. Materials and methods A lemongrass and mint formulation was used in the synthesis of ZnONPs, and the mouthwash was prepared using the synthesized nanoparticles. The produced ZnONPs were tested for their antimicrobial activity using agar well diffusion technique against oral pathogens, and the ZnONPs-mediated mouthwash was evaluated for its cytotoxic effect using the brine shrimp lethality assay and compared to commercial mouthwash.  Results The green-synthesized ZnONPs were initially confirmed using a UV-visible spectrophotometer and exhibited a maximum peak at 362 nm. The antimicrobial activity was tested for the synthesized ZnONPs against oral pathogens, which showed a maximum zone of inhibition of 22 mm in Enterococcus faecalis and 23 mm in Candida albicans, as estimated by the agar well diffusion technique. Additionally, ZnONPs-based herbal mouthwash demonstrated lower cytotoxicity than the commercial mouthwash in the brine shrimp lethality assay. Conclusion In the current study, lemongrass and mint-mediated ZnONPs demonstrated an effective antibacterial activity against E. faecalis and antifungal activity against C. albicans. Furthermore, the cytotoxic effect tested using the brine shrimp lethality assay for ZnONPs-mediated mouthwash demonstrated lower toxicity as compared to the commercial mouthwash. This suggests that the green-synthesized ZnONPs-based mouthwash could be used as an alternative to synthetic mouthwash.

Article review: Brazilin as potential anticancer agent.

Brazilin is the main compound in Caesalpinia sappan and Haematoxylum braziletto, which is identified as a homoisoflavonoid based on its molecular structure. These plants are traditionally used as an anti-inflammatory to treat fever, hemorrhage, rheumatism, skin problems, diabetes, and cardiovascular diseases. Recently, brazilin has increased its interest in cancer studies. Several findings have shown that brazilin has cytotoxic effects on colorectal cancer, breast cancer, lung cancer, multiple myeloma, osteosarcoma, cervical cancer, bladder carcinoma, also other cancers, along with numerous facts about its possible mechanisms that will be discussed. Besides its flavonoid content, brazilin is able to chelate metal ions. A study has proved that brazilin could be used as an antituberculosis agent based on its ability to chelate iron. This possible iron-chelating of brazilin and all the studies discussed in this review will lead us to the statement that, in the future, brazilin has the potency to be a chemo-preventive and anticancer agent. The article review aimed to determine the brazilin mechanism and pathogenesis of cancer.

Photosensitizing effects and physicochemical properties of chlorophyll a derivatives with hydrophilic oligoethylene glycol fragments at the macrocycle periphery.

In this work, screening studies of the cytotoxic effect of chlorins with fragments of di-, tri-, and pentaethylene glycol at the macrocycle periphery in relation to HeLa, A549, and HT29 cells were performed. It is shown that, despite different hydrophobicity, all the compounds studied have a comparable photodynamic effect. The conjugate of chlorin e6 with pentaethylene glycol, which has the lowest tendency to association among the studied compounds with tropism for low density lipoproteins and the best characteristics of the formation of molecular complexes with Tween 80, has a significant difference in dark and photoinduced toxicity (ratio IC50(dark)/IC50(photo) approximately 2 orders of magnitude for all cell lines), which allows to hope for a sufficiently large "therapeutic window". A study of the interaction of this compound with HeLa cells shows that the substance penetrates the cell and, after red light irradiation induces ROS appearance inside the cell, associated, apparently, with the photogeneration of singlet oxygen. These data indicate that photoinduced toxic effects are caused by damage to intracellular structures as a result of oxidative stress. Programmed type of cell death characterized with caspase-3 induction is prevailing. So, the conjugate of chlorin e6 with pentaethylene glycol is a promising antitumor PS that can be successfully solubilized with Tween 80, which makes it suitable for further in vivo studies.

Arenobufagin, isolated from Bufo viridis toad venom, inhibits A549 cells proliferation by inducing apoptosis and G2/M cell cycle arrest.

Lung cancer is a significant contributor to cancer morbidity and mortality globally. Arenobufagin, a compound derived from Bufo viridis toad venom, has demonstrated the ability to inhibit cell growth in various cancer cell lines. However, our understanding of the role and mechanism of arenobufagin in lung cancer remains incomplete, necessitating further researches to fully elucidate its action mechanism. In this study, we further explored the impact of arenobufagin on A549 cells. The results revealed that it exerted a potent cytotoxic effect on A549 cells by inhibiting cell colony formation, promoting cell apoptosis, increasing reactive oxygen species (ROS) levels, and arresting A549 cells in G2/M phase. Collectively, our findings suggested that arenobufagin may have potential as a future therapeutic for lung cancer treatment.