Potent Anticancer Activity Research Articles

Synthesis of Silver and Zinc Oxide Nanoparticles Using Polystichum lentum Extract for the Potential Antibacterial, Antioxidant, and Anticancer Activities

The present research involves a green synthesis of silver and zinc oxide nanoparticles using an aqueous extract of Polystichum lentum and a comparison of bioactivities. Phenolics, flavonoids, alkaloids, steroids, and saponins were present in the aqueous extract. The highest TPC and TFC were found in ethanol extract with 124.93 ± 9.36 mg GAE/g and 28.73 ± 1.98 mg QE/g. The formation of Ag and ZnO NPs was confirmed by the appearance of peaks at 421 nm and 362 nm in UV‐visible spectra. The involvement of plant secondary metabolites in nanoparticle synthesis was indicated by the shifts in peak positions and peak intensities in FTIR spectra. SEM and XRD analyses established spherical morphology (average size 61.33 ± 15.31 nm) and FCC crystal structure for Ag NPs and hexagonal to round morphology (average size 97.20 ± 12.92 nm) and hexagonal wurtzite crystal structure for ZnO NPs. EDX analysis revealed the elemental composition of nanoparticles. The IC50 values of 51.95 ± 3.11 and 83.79 ± 6.63 μg/mL for Ag NPs and ZnO NPs in the DPPH assay were significantly higher than 32.07 ± 1.03 and 6.53 ± 1.57 μg/mL for aqueous and methanol extracts. ZnO nanoparticles showed comparatively higher ZOI of 14 and 16 mm against Shigella sonnei and Klebsiella pneumoniae. It also displayed the lowest MIC and MBC of 3.125 and 6.25 mg/mL against Staphylococcus aureus and Klebsiella pneumoniae. The nanoparticles also exhibit potent cytotoxicity with IC50 of 76.82 ± 1.67 μg/mL against cervical cancer cell lines. Both nanoparticles and aqueous extract were mildly toxic towards the brine shrimp nauplii with the lowest LC50 being 661.80 ± 64.21 μg/mL for the aqueous extract. In conclusion, the findings of the present study demonstrate the high antioxidant, antibacterial, and anticancer activities in Ag and ZnO nanoparticles synthesized using an aqueous extract of Polystichum lentum.

Imatinib inhibits oral squamous cell carcinoma by suppressing the PI3K/AKT/mTOR signaling pathway.

Oral squamous cell carcinoma (OSCC) is a prevalent oral and maxillofacial cancer with high mortality as OSCC cells readily invade tissues and metastasize to cervical lymph nodes. Although imatinib exhibits potential anticancer and remarkable clinical activities that therapeutically affect several cancer types, its specific impact on OSCC has yet to be fully explored. Therefore, this study investigated the potential anticancer effect of imatinib on OSCC cells and the underlying mechanisms. The Cell Counting Kit-8 was used to determine the impact of imatinib on cell viability. Then, morphological cell proliferation analysis was conducted to examine how imatinib impacted OSCC cell growth. Moreover, OSCC cell migration was determined through wound-healing assays, and colony formation abilities were investigated through the soft agar assay. Lastly, the effect of imatinib on OSCC cell apoptosis was verified with flow cytometry, and its inhibitory mechanism was confirmed through Western blot. Our results demonstrate that imatinib effectively inhibited OSCC cell proliferation and significantly curtailed OSCC cell viability in a time- and concentration-dependent manner. Furthermore, imatinib suppressed migration and colony formation while promoting OSCC cell apoptosis by enhancing p53, Bax, and PARP expression levels and reducing Bcl-2 expression. Imatinib also inhibited the PI3K/AKT/mTOR signaling pathway and induced OSCC cell apoptosis, demonstrating the potential of imatinib as a treatment for oral cancer.

A bis-quinoline ruthenium(II) arene complex with submicromolar cytotoxicity in castration-resistant prostate cancer cells.

A new Ru(II) arene chlorido organometallic complex [(η6-p-cymene)(L)RuCl]PF6 (named as pCYRuL) using 2-bis(quinolin-2-ylmethylene) hydrazine (L) was developed that exhibits potent anticancer activity against castration-resistant prostate cancer (CRPC) (IC50 = 0.71 μM), and it is 45 times more effective than the standard drug cisplatin (IC50 = 31.3 μM) in a castration-resistant human prostatic adenocarcinoma cell line (PC-3) but non-toxic in normal human kidney cells (HK2) as well as normal breast cells (MCF10A) and found that pCYRuL exerted anticancer activity via apoptosis induction and cell cycle arrest in the G2/M phase of PC-3 cells.

Biological evaluation of benzothiazoles obtained by microwave-green synthesis.

Benzothiazole compounds are known as an important bicyclic ring system with multiple applications. These compounds have a wide range of biological activities, including anticancer, antimicrobial, anti-inflammatory and antiviral activities. In this study, benzothiazole compounds were synthesized and their various biological activities were examined. The synthesized benzothiazoles were evaluated for their antimicrobial properties against various bacterial and fungal strains. The compound 6e is most active ligand in the series against bacteria and fungi as compared to standard antibiotics. Especially, this compound significant effect against Staphylococcus aureus (32.00 ± 1.73 mm). These compounds exhibited potent anticancer activity against gastrointestinal cancer cells, demonstrating their potential as therapeutic agents. The lowest antiproliferative response after administration of the compounds was observed in HCT116 cells, while the most effective antiproliferative response was observed in AGS cells (> 10 µg/mL). In all cell lines, 40 and 100 µg/mL application values of the selected compounds showed significant increases in the expression of caspase-3, 8 and 9. We also utilized a computational docking approach to investigate the interaction of these benzothiazoles with VEGFR-2 kinase. Our docking studies showed that compounds 6a and 6d may be promising therapeutic agents against gastrointestinal system cancers due to their ability to bind to VEGFR-2 kinase.

Leaf Extract from European Olive (Olea europaea L.) Post-Transcriptionally Suppresses the Epithelial-Mesenchymal Transition and Sensitizes Gastric Cancer Cells to Chemotherapy.

The overall survival of patients with the advanced and recurrent gastric cancer (GC) remains unfavorable. In particular, this is due to cancer spreading and resistance to chemotherapy associated with the epithelial-mesenchymal transition (EMT) of tumor cells. EMT can be identified by the transcriptome profiling of GC for EMT markers. Indeed, analysis of the TCGA and GTEx databases (n = 408) and a cohort of GC patients (n = 43) revealed that expression of the CDH2 gene was significantly decreased in the tumors vs. non-tumor tissues and correlated with the overall survival of GC patients. Expression of the EMT-promoting transcription factors SNAIL and ZEB1 was significantly increased in GC. These data suggest that targeting the EMT might be an attractive therapeutic approach for patients with GC. Previously, we demonstrated a potent anti-cancer activity of the olive leaf extract (OLE). However, its effect on the EMT regulation in GC remained unknown. Here, we showed that OLE efficiently potentiated the inhibitory effect of the chemotherapeutic agents 5-fluorouracil (5-FU) and cisplatin (Cis) on the EMT and their pro-apoptotic activity, as was demonstrated by changes in the expression of the EMT markers (E- and N-cadherins, vimentin, claudin-1) in GC cells treated with the aforementioned chemotherapeutic agents in the presence of OLE. Thus, culturing GC cells with 5-FU + OLE or Cis + OLE attenuated the invasive properties of cancer cells. Importantly, upregulation of expression of the apoptotic markers (PARP cleaved form) and increase in the number of cells undergoing apoptosis (annexin V-positive) were observed for GC cells treated with a combination of OLE and 5-FU or Cis. Collectively, our data illustrate that OLE efficiently interferes with the EMT in GC cells and potentiates the pro-apoptotic activity of certain chemotherapeutic agents used for GC therapy.

Homologous polydopamine ameliorates haemolysis of melittin for enhancing its anticancer efficacy.

Despite exhibiting potent anticancer activity, the strong hemolytic properties of melittin (MEL) significantly restrict its delivery efficiency and clinical applications. To address this issue, we have devised a strategy wherein homologous dopamine (DA), an essential component of bee venom, is harnessed as a vehicle for the synthesis of MEL-polydopamine (PDA) nanoparticles (MP NPs). The ingenious approach lies in the fact that MEL is a basic polypeptide, and the polymerization of DA is also conducted under alkaline conditions, indicating the distinctive advantages of PDA in MEL encapsulation. Furthermore, MP NPs are modified with folic acid to fabricate tumor-targeted nanomedicine (MPF NPs). MPF NPs can ameliorate the hemolysis of MEL in drug delivery and undergo degradation triggered by high levels of reactive oxygen species (ROS) within solid tumors, thereby facilitating MEL release and subsequent restoration of anticancer activity. After cellular uptake, MPF NPs induce cell apoptosis through the PI3K/Akt-mediated p53 signaling pathway. The tumor growth inhibitory rate of MPF NPs in FA receptor-positive 4T1 and CT26 xenograft mice reached 78.04% and 81.66%, which was significantly higher compared to that in FA receptor-negative HepG2 xenograft mice (45.79%). Homologous vehicles provide a new perspective for nanomedicine design.

Methyl Scanning Approach for Enhancing the Biological Activity of the Linear Peptidic Natural Product, Efrapeptin C

Efrapeptin C (1a) is a large peptidic natural product comprising a 15-mer linear sequence and exerts potent anticancer activity by inhibiting mitochondrial FoF1-ATP synthase. Residues 1–6 and 9–15 of 1a...

Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer

A ligand-centred strategy combined with phenotypic screening was used to develop novel antiproliferative inhibitors against oesophageal cancer and identified a lead compound that induces potent anticancer activity and inhibits Aurora kinase A.

Design, synthesis and potent anti-pancreatic cancer activity of new pyrazole derivatives bearing chalcone, thiazole and thiadiazole moieties: gene expression, DNA fragmentation, cell cycle arrest and SAR.

Less than 5% of pancreatic cancer patients survive for more than five years after diagnosis. Therefore, there is an urgent need for novel therapeutic drugs to treat pancreatic cancer. Herein, we report the synthesis and full characterization of fifteen novel pyrazole derivatives bearing chalcone (4-10), thiazole (16-19) and thiadiazole (23-26) moieties. All the newly synthesized pyrazole derivatives were tested in vitro as anti-cancer agents against pancreatic cancer (PaCa-2), breast cancer (MCF-7), prostate cancer (PC3), and normal cell lines (BJ1). Three pyrazolyl-chalcone derivatives (4, 5, and 7) and a pyrazolyl-thiadiazole derivative (25) showed potent anti-cancer activity against the PaCa-2 cell line with IC50 values of 13.0, 31.5, 24.9, and 5.5 μg mL-1, respectively, compared with doxorubicin (IC50 = 28.3 μg mL-1). Compound 25 showed potent anti-cancer activity against the PC3 cell line with an IC50 value of 11.8 μg mL-1. In contrast, compounds 4, 5 and 7 are safer against the normal human-cell line (BJ1) with IC50 values of 74.2, 76.6 and 81.1 μg mL-1, respectively, compared with compound 25, which has an IC50 value of 23.7 μg mL-1. The mechanism of action of compounds 4, 5 and 7 against pancreatic cancer cells was studied by investigating gene expression, DNA fragmentation, comet assay and flow cytometry experiments using doxorubicin as a reference drug. Moreover, the structure-activity relationship between the structures of these compounds and their biological properties was discussed.

P-Sulfonatocalix[4]arene turns peptide aggregates into an efficient cell-penetrating peptide.

A novel cell-penetrating peptide (CPP) called FAM-Y4R4, with FAM as a fluorescent probe, was developed. Initially, we aimed to use Y4 as a supramolecular host for water-insoluble drugs, with R4 driving the complex into cells. However, an unexpected hurdle was discovered; the peptide self-assembled into amorphous aggregates, rendering it ineffective for our intended purpose. Molecular dynamics simulations revealed that intermolecular cation-π interactions between arginine and tyrosine caused this aggregation. By decorating the R4 sidechains with p-sulfonatocalix[4]arene (CX4), we successfully dissolved most of the aggregates, significantly improved the peptide's solubility and enhanced the cell uptake with MCF7 and A549 cells via both direct penetration and endocytosis. The binding strength between CX4 and R4, as well as the interaction between curcumin and tyrosines was quantified. Encouragingly, our results showed that FAM-Y4R4, with CX4, effectively delivered curcumin - as a model for poorly water-soluble drugs - into cells which exhibited potent anticancer activity. Using R4/CX4 instead of the conventional R7-9 oligoarginine-based CPP simplifies peptide synthesis and offers higher yields. CX4 shows promise for addressing aggregation issues in other peptides that undergo a similar aggregation mechanism.

Levofloxacin reposition-based design: synthesis, biological evaluation of new levofloxacin derivatives targeting topoisomerase II beta polymerase as promising anticancer agents, molecular docking, and physicochemical characterization.

Repositioning of already approved medications through repurposing or re-profiling for new medical uses after certain structural modifications is a novel approach in drug discovery. Fluoroquinolone antibiotics are one of the cardinal agents investigated for potential anticancer activities. In this work, levofloxacin was repositioned for anticancer activities. A series of levofloxacin-based compounds were designed and synthesized through the derivatization of levofloxacin's carboxylic acid functionality. The newly synthesized compounds were screened for cytotoxic activities against breast, liver, and leukemia cancer cell lines. Their effect on normal cells was also investigated. The target compounds were evaluated for their proliferative inhibitory activity toward topoisomerase II beta polymerization. Compound 5 showed higher inhibitory activity against a breast cancer cell line (MCF-7) with IC50 = 1.4 μM and lesser side effects on a normal breast cell line (MCF-10a) with IC50 = 30.40 μM than reference drugs. The best activity against a liver cancer cell line (Hep3B) was exhibited by compounds 3c, 4b, 5, 7, 8, 13a and 13c with IC50 values ranging from 0.43 to 8.79 μM. Regarding the effect of compounds 5 and 13a on a leukemia cancer cell line (L-SR), their IC50 values were 0.96 and 3.12 μM, respectively. Compounds 3c and 5 showed Topo2β inhibitory effects on Hep3B cells (81.33% and 83.73%, respectively), which was better than levofloxacin and etoposide as reference drugs. Cytometry cell cycle analysis revealed that compounds 3c and 5 arrested the cell cycle at the S phase (37.56% and 39.09%, respectively). Compounds 3c and 5 exhibited an elevation in active caspase-3 levels by 4.9 and 4.5 folds, respectively. Molecular modeling simulation of compounds 3c and 5 demonstrated energy scores (-29.77 and -20.46 kcal mol-1, respectively) more than those of the reference drugs as they interact with the most essential amino acids required for good affinity towards human topoisomerase II beta enzyme (PDB ID: 3QX3). Physicochemical characteristics of the most promising cytotoxic compounds 3c and 5 were investigated and compared to etoposide and levofloxacin as reference drugs. However, they showed high gastrointestinal absorption and could not penetrate the blood-brain barrier.

Trifluoroethanol promoted formal nucleophilic substitution of indol-2-yl diaryl methanol for the synthesis of tetraarylmethanes.

The synthesis of tetraarylmethanes has long been a challenge in the field of synthetic chemistry. In this study, a series of tetraarylmethanes were successfully synthesized through the formal nucleophilic substitution reaction of indol-2-yl diaryl methanol catalyzed by Brønsted acid. The key success of this study lies in suppressing the influence of water molecules by forming hydrogen bonds with the TFE solvent. This process leads to the formation of active 2-indole imine methide (2-IIM) intermediates, ensuring the successful synthesis of tetraarylmethanes. Furthermore, some of the products also exhibited potential anticancer activity.

The incredible story of ophiobolin A and sphaeropsidin A: two fungal terpenes from wilt-inducing phytotoxins to promising anticancer compounds.

Covering: 2000 to 2023This review presents the exceptional story of ophiobolin A (OphA) and sphaeropsidin A (SphA), a sesterterpene and a diterpene, respectively, which were initially isolated as fungal phytotoxins and subsequently shown to possess other interesting biological activities, including promising anticancer activities. Ophiobolin A is a phytotoxin produced by different fungal pathogens, all belonging to the Bipolaris genus. Initially, it was only known as a very dangerous phytotoxin produced by fungi attacking essential cereals, such as rice and barley. However, extensive and interesting studies were carried out to define its original carbon skeleton, which is characterized by a typical 5 : 8 : 5 ring system and shared with fusicoccins and cotylenins, and its phytotoxic activity on host and non-host plants. The biosynthesis of OphA was also defined by describing the different steps starting from mevalonate and through the rearrangement of the acyclic C-25 precursor lead the toxin is obtained. OphA was also produced as a bioherbicide from Drechslera gigantea and proposed for the biocontrol of the widespread and dangerous weed Digitaria sanguinaria. To date, more than sixty ophiobolins have been isolated from different fungi and their biological activities and structure-activity relationship investigated, which were also described using their hemisynthetic derivatives. In the last two decades, thorough studies have been performed on the potential anticancer activity of OphA and its original mode of action, attracting great interest from scientists. Sphaeropsidin A has a similar story. It was isolated as the main phytotoxin from Diplodia cupressi, the causal agent of Italian cypress canker disease, resulting in the loss of millions of plants in a few years in the Mediterranean basin. The damage to the forest, environment and ornamental heritage are noteworthy and economic losses are also suffered by tree nurseries and the wood industry. Six natural analogues of SphA were isolated and several interesting hemisynthetic derivatives were prepared to study its structure-activity relationship. Surprisingly, sphaeropsidin A showed other interesting biological activities, including antibiotic, antifungal, and antiviral. In the last decade, extensive studies have focused on the anticancer activity and original mode of action of SphA. Furthermore, specific hemisynthetic studies enable the preparation of derivatives of SphA, preserving its chromophore, which showed a noteworthy increase in anticancer activity. It has been demonstrated that ophiobolin A and sphaeropsidin A are promising natural products showing potent activity against some malignant cancers, such as brain glioblastoma and different melanomas.

Biogenic Synthesis of Photosensitive Magnesium Oxide Nanoparticles Using Citron Waste Peel Extract and Evaluation of Their Antibacterial and Anticarcinogenic Potential.

Magnesium oxide nanoparticles (MgONPs) have been fabricated by several approaches, including green chemistry approach due to diverse application and versatile features. The current study aimed to prepare a convenient, biocompatible, and economically viable MgONPs using waste citron peel extract (CP-MgONPs) to evaluate their biological applications. The CP-MgONPs were synthesized by a sustainable approach from extract of waste citron peel both as capping and reducing agents without use of any hazardous material. The physicochemical features of formed CP-MgONPs were determined by sophisticated analytical and microscopic techniques. The biogenic CP-MgONPs were examined for their antibacterial, anticarcinogenic, and photocatalytic attributes. A prominent absorption peak in the UV-Vis spectra at 284 nm was the distinguishing characteristic of the CP-MgONPs. The scanning electron microscopy (SEM) reveals polyhedral morphology of nanoparticles with slight agglomeration of CP-MgONPs. The CP-MgONPs exerted excellent antibacterial potencies against six bacterial strains. The CP-MgONPs displayed significant susceptibility towards E. coli (20.72 ± 0.33 mm) and S. aureus (19.52 ± 0.05 mm) with the highest inhibition zones. The anticancer effect of CP-MgONPs was evaluated against HepG2 (IC50 : 15.3 μg·mL-1) cancer cells and exhibited potential anticancer activity. A prompt inversion of cellular injury manifested as impairment of the integrity of the cell membrane, apoptosis, and oxidative stress was observed in treated cells with CP-MgONPs. The biosynthesized CP-MgONPs also conducted successful photocatalytic potential as much as MgO powder under the UV-light using acid orange 8 (AO-8) dye. The degradation performance of CP-MgONPs showed over 94% photocatalytic degradation efficiency of acid orange 8 (AO-8) dyes within a short time. Outcomes of this research signify that biogenic CP-MgONPs may be advantageous at low concentrations, with positive environmental impacts.

Utilizing topological indices in QSPR modeling to identify non-cancer medications with potential anti-cancer properties: a promising strategy for drug repurposing.

The exploration of non-cancer medications with potential anti-cancer activity offers a promising avenue for drug repurposing, accelerating the development of new oncological therapies. This study employs Quantitative Structure-Property Relationship (QSPR) modeling to identify and predict the anti-cancer efficacy of various non-cancer drugs, utilizing topological indices as key descriptors. Topological indices, which capture the molecular structure's geometric and topological characteristics, provide critical insights into the pharmacological interactions relevant to anti-cancer activity. By analyzing a comprehensive dataset of non-cancer medications, this research establishes robust QSPR models that correlate topological indices with anti-cancer activity. The models demonstrate significant predictive power, highlighting several non-cancer drugs with potential anti-cancer properties. Further, we will use linear, quadratic and logarithmic regression to understand the structures of anti-cancer drugs and strengthen our ability to manipulate the molecular structures. The findings underscore the utility of topological indices in drug repurposing strategies and pave the way for further experimental validation and clinical trials. This integrative approach enhances our understanding of drug action mechanisms and offers a cost-effective strategy for expanding the repertoire of anti-cancer agents.

Modulating anti-inflammatory and anticancer properties by designing a family of metal-complexes based on 5-nitropicolinic acid.

A new family of six complexes based on 5-nitropicolinic acid (5-npic) and transition metals has been obtained: [M(5-npic)2]n (MII = Mn (1) and Cd (2)), [Cu(5-npic)2]n (3), and [M(5-npic)2(H2O)2] (MII = Co (4), Ni (5), and Zn (6)), which display 1D, 2D, and mononuclear structures, respectively, thanks to different coordination modes of 5-npic. After their physicochemical characterization by single-crystal X-ray diffraction (SCXRD), elemental analyses (EA), and spectroscopic techniques, quantum chemical calculations using Time-Dependent Density Functional Theory (TD-DFT) were performed to further study the luminescence properties of compounds 2 and 6. The potential anticancer activity of all complexes was tested against three tumor cell lines, B16-F10, HT29, and HepG2, which are models widely used for studying melanoma, colon cancer, and liver cancer, respectively. The best results were found for compounds 2 and 4 against B16-F10 (IC50 = 26.94 and 45.10 μg mL-1, respectively). In addition, anti-inflammatory studies using RAW 264.7 cells exhibited promising activity for 2, 3, and 6 (IC50 NO = 5.38, 24.10, and 17.63 μg mL-1, respectively). This multidisciplinary study points to complex 2, based on CdII, as a promising anticancer and anti-inflammatory material.

In Vitro Vitamin C Equivalent Antioxidant Capacity, Cytotoxicity and Anti-Cancer Activity of Methanolic Urtica dioica L. Leaf Extract as a Food Supplement

Antioxidant capacity, cytotoxicity on two vital cell lines and the anti-cancer activity of methanolic Urtica dioica L. leaf extract (UDE) collected from Duzkoy, Giresun, Turkey were studied by determining safe concentration. The antioxidant capacity of the extract was expressed as vitamin C equivalency by spectrophotometric MTT assay. The cytotoxic concentration 50% was measured by the linearity between UDE concentrations (CC50) and the cell viability of non-cancer kidney cell lines (BHK-21, MDBK). The anti-cancer activity was conducted on human hepatocellular carcinoma cells (HepG2) by determining inhibition concentration (IC50) on cell proliferation. The vitamin C equivalence of UDE increased linearly by increasing the concentration. The cytotoxic and non-toxic concentrations of UDE were determined on BHK-21 and MDBK with 15.71 mg/ml and 5.14 mg/ml of CC50 respectively. The extract inhibited the proliferation of human hepatocellular carcinoma cells with a 2.46 mg/ml of IC50. In conclusion, the present study tried to explain in detail the dose-dependent activity of Urtica dioica L. leaf extract. The dose-response results showed that Urtica dioica L. leaf extract could have low cytotoxicity, but potential anti-cancer activity at safe concentrations.

Novel Gluconobacter oxydans strains selected from Kombucha with potential postbiotic activity

Gastric and colorectal cancer are among the most frequently diagnosed malignancies of the gastrointestinal tract. Searching for methods of therapy that complements treatment or has a preventive effect is desirable. Bacterial metabolites safe for human health, which have postbiotic effect, are of interest recently. The study aimed to preliminary assessment of the safety, antimicrobial, and anti-cancer activity of cell-free metabolites of Gluconobacter oxydans strains isolated from Kombucha beverages as an example of the potential postbiotic activity of acetic acid bacteria (AAB). The study material consisted of five AAB strains of Kombucha origin and three human cell lines (gastric adenoma—AGS, colorectal adenoma—HT-29, and healthy cells derived from the endothelium of the human umbilical vein—HUVEC). Results of the study confirms the health safety and functional properties of selected AAB strains, including their potential postbiotic properties. The best potential anticancer activity of the AAB cell-free supernatants was demonstrated against AGS gastric adenoma cells. The conducted research proves the postbiotic potential of selected acetic acid bacteria, especially the KNS30 strain.Key points•The beneficial and application properties of acetic acid bacteria are poorly studied.•Gluconobacter oxydans from Kombucha show a postbiotic activity.•The best anticancer activity of the G. oxydans showed against gastric adenoma.

A Ru(II)-Strained Complex with 2,9-Diphenyl-1,10-phenanthroline Ligand Induces Selective Photoactivatable Chemotherapeutic Activity on Human Alveolar Carcinoma Cells via Apoptosis.

[Ru(bipy)2(dpphen)]Cl2 (where bipy = 2,2'-bipyridine and dpphen = 2,9-diphenyl-1,10-phenanthroline) (complex 1) is a sterically strained compound that exhibits promising in vitro photocytotoxicity on an array of cell lines. Since lung adenocarcinoma cancer remains the most common lung cancer and the leading cause of cancer deaths, the current study aims to evaluate the plausible effect and uptake of complex 1 on human alveolar carcinoma cells (A549) and mesenchymal stem cells (MSC), and assess its cytotoxicity in vitro while considering its effect on cell morphology, membrane integrity and DNA damage. MSC and A549 cells showed similar rates of complex 1 uptake with a plateau at 12 h. Upon photoactivation, complex 1 exhibited selective, potent anticancer activity against A549 cells with phototoxicity index (PI) values of 16, 25 and 39 at 24, 48 and 72 h, respectively. This effect was accompanied by a significant increase in A549-cell rounding and detachment, loss of membrane integrity and DNA damage. Flow cytometry experiments confirmed that A549 cells undergo apoptosis when treated with complex 1 followed by photoactivation. In conclusion, this present study suggests that complex 1 might be a promising candidate for photochemotherapy with photoproducts that possess selective anticancer effects in vitro. These results are encouraging to probe the potential activity of this complex in vivo.

Beta-sitosterol glycoside from Paraboea leuserensis and Cytotoxicity Test against MCF-7 Human Breast Cancer Cells

Background: Paraboea leuserensis, a plant endemic to the Leuser Mountain in the provinces of Aceh and North Sumatra, has been traditionally used for medicinal purposes by chewing or boiling, addressing conditions such as stomachaches and providing stamina enhancement. This study aimed to isolate secondary metabolite compounds from Paraboea leuserensis and conduct in vitro anticancer tests.
 Method: The ethyl acetate extract was isolated through column chromatography, yielding beta-sitosterol glycoside, and was tested for bioactivity against human breast cancer cells MCF-7 using the MTT method.
 Results: The compound demonstrated activity against breast cancer cells (MCF-7) with an IC50 value of 24.83 mg/L.
 Conclusion: Paraboea leuserensis exhibits potential anticancer activity. The isolation of beta-sitosterol glycoside from the plant and its demonstrated activity against MCF-7 human breast cancer cells suggest a promising avenue for further exploration of the plant's anticancer properties.