Cervical Cancer HeLa Research Articles

The Effect of Curcumin Administration on p53 and Caspase-3 Expression in Cervical Cancer HeLa Cell Culture

Introduction: Cervical cancer is a type of cancer with 605,000 new cases globally each year, with a mortality rate of 340,000. Curcuma longa, or curcumin, has the potential to enhance apoptosis in cervical cancer cells through the NF-kB-p53-caspase-3 pathway. Material and Methods: This in vitro experimental study employed a Completely Randomized Design (CRD) using HeLa cell cultures derived from cervical adenocarcinoma (ATCC® CCL2™). Cells were grown in Dulbecco's Modified Eagle Medium (DMEM) and treated with curcumin at concentrations of 25 µg/mL, 50 µg/mL, 100 µg/mL, 150 µg/mL, and 250 µg/mL. Cytotoxicity was assessed using the CCK-8 assay, apoptosis via flow cytometry, and p53 and caspase-3 expression using immunofluorescence. Statistical analysis was performed with IBM Statistics SPSS 25. Results: There was an increase in the percentage of apoptosis, p53 expression, and caspase-3 expression. At a dose of 100 µg/mL, total apoptosis increased significantly, reaching nearly 25% (p=0.000). P53 expression significantly increased at curcumin doses of 50 µg/mL and 100 µg/mL (p=0.021). There was a significant increase in caspase-3 expression, reaching approximately 86.2%, with a maximum effect at a dose of 100 µg/mL (p=0.002). Conclusion: Curcumin shows promising potential as an anticancer agent by reducing cell viability and enhancing apoptotic activity in HeLa cervical cancer cells.

Protopanaxadiol triggers G0/G1 cell cycle arrest and apoptosis in human cervical cancer HeLa cells through the PPER pathway

Protopanaxadiol (PPD) is considered to be the most active pharmacological element in ginseng and has been widely studied for its anticancer effects. However, the detailed anticancer mechanism of this compound in cervical cancer (CC) HeLa cells has yet to be thoroughly understood. In this research, we discovered that PPD effectively inhibits CC HeLa cell proliferation and cause morphological changes, with an IC50 measured at 34.18 μM. Based on mRNA-seq analysis, we revealed the mechanism by which PPD inhibits HeLa cell proliferation. The results from Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis indicated significant enrichment of DGEs in the cell cycle and protein processing in the endoplasmic reticulum (PPER) pathway. By inducing DNA damage, PPD resulted in G0/G1 phase cell cycle arrest, inhibited Bcl-2 to cause ROS production, upregulated cytochrome c (Cyto-c) expression, thereby further reducing mitochondrial membrane potential (Δψm), activated the caspase family, and induced cell apoptosis. In addition, PPD promoted Ca2+ leakage, downregulated the PPER pathway (PERK, ATF6, and IRE1α), increased Chop expression levels, and mediated programmed cell death. These observations imply that PPD can induce apoptosis in HeLa cells, highlighting its potential as a novel natural therapeutic for cervical cancer.

Discovery of amino acid-conjugated dimethylcardamonin analogues as potent anti-cervical cancer agents on SiHa cells targeting p53 signalling pathway

DMC (1) is a phytochemical found in the seeds of Syzygium nervosum, exhibiting anticancer activity in various cells through multiple pathways. Herein, the bioactivity of DMC (1) was enhanced by chemical modification through esterification, attaching fatty acid and amino acid moieties to yield 27 semi-synthetic derivatives. These compounds were evaluated for their in vitro cytotoxicity against three main types of cervical cancer cells, including SiHa, HeLa, and C-33A. As a result, the amino acid DMC derivative, 4´-(L-tyrosinyloxy)-DMC (7j), exhibited potent cytotoxicity against SiHa cells, which was approximately two-fold greater than that of 1. Further investigation into the mechanism of action of 7j was conducted, revealing its ability to induce cell cycle arrest and apoptosis. Gene expression analysis showed the downregulation of CDK2 and upregulation of the BAX/BCL2 ratio. Atomistic insight was studied on HPV 16 E6 via molecular dynamics simulation, revealing key interactions between tyrosinyl portion and C51 residue.

Synthesis, crystal structure, cytotoxicity (MCF-7 and HeLa) and free radical scavenging activity of the hydrazones derived from 2-methylsulfonyl-5-nitrobenzaldehyde

The rising levels of breast and cervical cancers among women have become public health problem with high economic burden globally and more especially in low- and middle-income countries. This necessitates discoving new and potent anticancer drugs with reduced or no side effects. The hydrazones derived from 2-formyl-4-nitrophenyl methanesulfonate were characterized using a combination of spectroscopic and single-crystal X-ray diffraction (XRD) techniques. The compounds were, in turn, evaluated for antigrowth effect in vitro against the human breast adenocarcinoma (MCF-7) and human cervical cancer (HeLa) cell lines and for cytotoxicity against the African Green Monkey kidney (Vero) cell line. The presence of a chlorine atom on the para position of the phenylhydrazone moiety of 3b resulted in increased cytotoxicity against the MCF-7 and the HeLa cell lines compared to camptothecin (IC50 = 9.15 ± 0.84 µM and 3.71 ± 0.16 µM, respectively) with IC50 values of 5.64 ± 0.84 µM and 2.40 ± 0.13 µM, respectively. Compounds 2, 3a and 3b were found to exhibit significantly reduced toxicity against the Vero cells compared to the anti-cancer drugs, doxorubicin (IC50 = 0.78 ± 0.04 µM) and nintedanib (IC50 = 0.24 ± 0.02 µM) with the IC50 values of 17.86 ± 1.12, 11.89 ± 1.01 and 24.42 ± 0.70 µM, respectively. The hydrazones 3a and 3b exhibited a strong inhibitory effect against the vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase (IC50 = 5.78 ± 0.039 μM and 5.79 ± 0.053 µM, respectively) compared to the carbaldehyde precursor 2 (IC50 = 8.01 ± 0.052 µM) though less active compared to nintedanib (IC50 = 1.05 ± 0.193 µM). The hydrazone derivatives exhibited significant 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity compared to ascorbic acid and the parent 2-formyl-4-nitrophenylmethanesulfonate. In silico molecular docking studies revealed the binding potential of the hydrazones at the active site of VEGFR-2 tyrosine kinase and cytochrome c peroxidase.

Evaluation of a Radioiodinated G-Quadruplex Binder in Cervical Cancer Models.

We herein describe the radiosynthesis of a 125I-labeled acridine orange derivative ([125I]-C8), acting as a G-quadruplex binder, and its biological evaluation in cervical cancer models, aiming to enlighten its potential as a radioligand for Auger Electron Radiopharmaceutical Therapy (AE-RPT) of cancer. [125I]-C8 was synthesized with a moderate radiochemical yield (ca. 60 %) by a [125I]iodo-destannylation reaction. Its evaluation in cervical cancer HeLa cells demonstrated that the radiocompound has a significant cellular internalization with a notorious accumulation in the cell nucleus. In line with these results, [125I]-C8 strongly compromised the viability of HeLa cells in a dose-dependent manner, inducing non-repairable DNA lesions that are most probably due to the AEs emitted by 125I in close proximity to the DNA molecule. Biodistribution studies in a murine HeLa xenograft model showed that [125I]-C8 has fast blood clearance and high in vivo stability but poor tumor uptake, after systemic administration. The respective supramolecular conjugate with the AS1411 aptamer ([125I]-C8/AS1411) led to a slower blood clearance in the same animal tumor model, although without improving the tumor uptake. To take advantage of the radiotoxicity of [125I]-C8 against cervical cancer cells other strategies need to be studied, based namely on alternative nanodelivery carriers and/or intratumoral injection approaches.

Design, Synthesis, and Screening for Anticancer and Antimicrobial Activities of New Dihydropyridine‐Anchored Pyrazole and 1,2,3‐Triazole Hybrids

AbstractTwo new libraries of diethyl and dimethyl dihydropyridines‐based pyrazole and 1,2,3‐triazole hybrids (7a–g and 7h–n) were synthesized via a series of reactions involving click chemistry, pyrazole synthesis, and multicomponent reaction. All the new compounds were screened for their in vitro anticancer activity and antimicrobial activities. The 4‐chloro substituted analogue (7i) in dimethyl ester series showed an excellent activity against all three, namely, human breast adenocarcinoma (MCF‐7), human cervical cancer (HeLa), and human breast cancer triple‐positive (BT‐474) cell lines with IC50 values of 0.119 ± 0.58 µM, 0.135 ± 0.13 µM, and 0.163 ± 0.31 µM, respectively compared to abemaciclib. Molecular docking studies performed on the best active compound 7i against crystal structure of CDK6 revealed its best binding score and interactions. Additionally, these libraries were screened for their antimicrobial activities and determined their MIC. Compounds with ─Cl (7b), ─OMe (7d), ─Me (7a) substitution, and without substitution (7e) significantly showed better MIC values in comparison to ampicillin and nystatin.

Biosynthesis of chitosan encapsulated silver- nanoparticles using Probiotic-Lactobacillus plantarum strain and it's in vitro anticancer assessment on HeLa cells

Cervical cancer remains the deadliest cancer among women worldwide. Investigating the molecular mechanisms of tumor progression by targeting signaling pathways can provide insights into novel therapeutic strategies to overcome the limitations of conventional treatments. Green synthesis of nanoparticles addresses conventional treatment drawbacks like chemotherapy and radiation. This study aims to green synthesize, characterize, and evaluate chitosan-encapsulated silver nanoparticles (AgNPs) using Lactobacillus plantarum probiotics against cervical cancer HeLa cells, targeting the EMT mechanism. The green synthesized chitosan encapsulated Silver- Nanoparticles using probiotic -Lactobacillus plantarum (CS-LP-AgNPs) were characterized using UV–vis spectroscopy, which showed a peak at 420 nm confirming the reduction of AgNPs. Zeta and DLS analysis revealed the particle surface charge and stability. TEM analysis demonstrated that CS-LP-AgNPs are spherically shaped, with a size of approximately 15.3 nm. XRD patterns confirmed the crystalline nature of CS-LP-AgNPs. FTIR spectroscopy confirmed that CS-LP-AgNPs were functionalized with biomolecules. DAPI and double staining were employed to examine characteristic nuclear and morphological changes during apoptosis. Gene expression profiles of EMT in HeLa cell lines were performed to evaluate the anticancer potency of CS-LP-AgNPs. MTT assay demonstrated cytotoxic activity, whereas DAPI/(AO/EB) double staining images showed the induced apoptosis in HeLa cells by CS-LP-AgNPs treatment. CS-LP-AgNPs treated HeLa cells showed decreased SNAIL/EMT via enhancing apoptotic cascade mechanism. Green synthesized CS-LP-AgNPs may be considered an effective anti-cancer drug delivery system for the treatment of CC in the future.

Gamma irradiation green synthesis of (polyacrylamide/chitosan/silver nanoparticles) hydrogel nanocomposites and their using as antifungal against Candida albicans and anti-cancer modulator

Silver nanoparticles-loaded hydrogel nanocomposites are exploited for medicinal and pharmaceutical applications. Hydrogel nanocomposites were prepared from acrylamide (Am), chitosan (CS) and AgNO3 utilizing gamma rays. Diverse variables were applied in preparation of silver nanoparticles-laoded hydrogel nanocomposites of (PAm/CS)-AgNPs such as influence of radiation dose and influnece of CS concentration. Diverse techniques were utilized to characterize hydrogel nanocomposites; Fourier transform infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), X-ray diffraction (XRD), Transmission electron microscopy (TEM), energy dispersive X-ray (EDX) and scanning electron microscopy (SEM). Results confirmed formation of silver nanoparticles-loaded hydrogel nanocomposites of (PAm/CS)-AgNPs. Antifungal activity of (PAm/CS)-AgNPs hydrogel nanocomposites on viability of C. albicans was esitmated. Results displayed the efficient microbial inhibition activity of treatment against C. albicans compared to control. Furthermore, (PAm/CS)-AgNPs hydrogel nanocomposite against cervical cancer HeLa cell line was investigated. Cytotoxicity of (PAm/CS)-AgNPs hydrogel nanocomposites on prior cancer cell line empolyed to prohibition of cell growth assesssed by MTT test. HeLa cancer cell is treated by (PAm/CS)-AgNPs for 48 h exposed a potential apoptotic activity by noticeable up-regulation of p53 gene expression. Moreover, anticancer activity was investigated by down-regulation of platelet-based growth variable receptor beta (PDGFR-β), Bcl2, Cathepsine, and MMP-2 gene expression. antioxidant activity was investigated and results showed antioxidant activity of (PAm/CS) hydrogel and (PAm/CS)-AgNPs hydrogel nanocomposite are 87.8% and 62.9%, respectively.

Detouring NSAID into Mitochondria to Induce Apoptosis in Cancer Cells.

In recent years, impairing mitochondria in cancer cells gained attention as alternative cancer therapy. In this context, non-steroidal anti-inflammatory (NSAID) drugs are interesting candidates to damage mitochondria in cancer cells. However, routing NSAIDs specifically into the mitochondria remained a major challenge and less explored. Herein, we have synthesized a small library of Meclofenamic acid and Naproxen derivatives having ester and amide linkage with substituted triphenylphosphonium cations for mitochondria targeting. Screening in cervical cancer (HeLa), breast cancer (MCF7) and colon cancer (HCT-116) cells revealed a Meclofenamic acid derivative having ester linkage with tri (4-methoxyphenyl) phosphonium cation (8A3) which induced mitochondrial damage through mitochondrial outer membrane permeabilization (MOMP) followed by generation of reactive oxygen species (ROS) in the HCT-116 cells. This 8A3-mediated mitochondrial impairment triggered apoptosis by inhibiting Cox-2, reduction in Bcl-2/Bcl-xl expression and Caspase-3/9 cleavage leading to remarkable HCT-116 cell death. This novel mitochondrion targeted Meclofenamic acid derivative has the potential to be used as a chemical biology tool to understand the role of NSAIDs in mitochondria towards cancer therapy.

Group VA Aromatic Thiosemicarbazone Complexes: Synthesis, Characterization, Biological Activity, and Topological Studies.

The antiproliferative and antibacterial activities of thiosemicarbazones increase markedly with the presence of metal ions. One of the factors determining the activity of metal thiosemicarbazone complexes is the coordination structure. In this study, the biological effects of new antimony (III) and bismuth (III) thiosemicarbazone complexes with different binding modes and geometrical structures were demonstrated. Three new complexes, with the formulae {[SbCl3(µ2-S-Hacptsc)(η1-S-Hacptsc)], 2/3H2O,1/3CH2Cl2}, {[SbCl3(κ2-S,N-Hacpmtsc)(η1-S-Hacpmtsc)2CH2Cl2]}, and{[BiCl3(η1-S-Hbzmtsc)3]·C2H5OH}, where Hacptsc: acetophenone thiosemicarbazone, Hacpmtsc: acetophenone-N-methyl thiosemicarbazone, Hbzmtsc: benzaldehyde-N-methyl thiosemicarbazone) were elucidated by different methods and deeply analyzed in accordance with their structure by X-ray structure analysis and Atoms-In-Molecules topological analysis. This analysis provided a deeper understanding of the coordination spheres of the Sb/Bi complexes. For instance, the first reported two binding modes of the same ligand are observed in a single crystal structure of antimony (III) halide complexes. Additionally, in one of the complexes, a solid-to-solid phase transition was detected and analyzed in detail. Those complexes, very unique in terms of their geometry, have also been tested for their in vitro cytotoxic activity against human adenocarcinoma cervical cancer (HeLa) cells, whereas antimony (III) complex 1is the most active complex of this study. Further, the antibacterial activity of the complexes has been screened against two Gram-negative (Pseudomonas aeruginosa and Escherichia coli) and two Gram-positive (Staphylococcus epidermidis and Staphylococcus aureus) pathogenic bacteria. From the results, it is found that all the complexes exhibited significant activity against the Gram-negative pathogenic bacteria.

Biodiversity and Bioprospecting of Fungal Endophytes from Houttuynia cordata Thunb. as a Potential Antibacterial and Anticancer Agent.

Endophytic fungi are considered a new source of bioactive compounds that have important applications in agriculture and medicine. This study aims to investigate the biodiversity and potential of endophytic fungi isolated from Houttuynia cordata Thunb. as antimicrobials and anticancer agents. Out of ten isolated endophytes, four species have never been reported to be associated with H. cordata: Ceratobasidium sp., Cladosporium sp., Phomopsis sp., and Fusarium sp. The antibacterial activity assay revealed that the ethyl acetate extract of Ceratobasidium sp. HCS-3 possessed most potent antibacterial activity against Escherichia coli and Staphylococcus aureus. In addition, its cytotoxic activity test showed the promising anticancer activity on lung cancer A549, osteosarcoma MG-63, and cervical cancer HeLa cells with IC50 of 4.55±1.16, 32.14±2.78, and 1.54±0.66 ppm, respectively. Furthermore, metabolite profiling identified 66 compounds suggesting that benzoic acid, farnesol, and cyclopeptides may contribute to the antibacterial activity, while 4-methoxycinnamic acid may have anticancer potential.

A novel strategy to enhance inhibition of Hela cervical cancer by combining Lentinus β-glucan and autophagic flux blockage

Lentinus β-D-glucan (LNT), derived from artificially cultured mushrooms of Lentinus edodes, shows an important yet incompletely understood biological functions in cancer. In this work, the chemical structure of the refined LNT comprising a β-D-(1, 6)-branched β-D-(1,3)-glucan was further clarified via 1D- and 2D-NMR with high resolution, and its drug resistance resulted from autophagy in human cervical cancer (CC) Hela cells besides its anti-cancer function were revealed in vitro and in vivo. In detail, LNT destroyed cellular homeostasis by significantly increasing the intracellular Ca2+ levels and promoted autophagic flux in vitro Hela cells, which was found to at least partially depend on the PI3K/Akt/mTOR-mediated pathway by up-regulating LC3-II levels and down-regulating the expression of p62, PI3K, p-Akt, and mTOR in Hela cells-transplanted BALB/c nude mice. In particular, LNT-induced autophagy led to a drug resistance against LNT-induced proliferation inhibition and apoptosis in Hela cells, and the co-treatment of autophagy inhibitors and LNT significantly enhanced the inhibition of Hela cells and tumor growth in vitro and in vivo. Therefore, the combination of LNT and autophagy inhibitors will be a novel therapeutic strategy to reduce the resistance and improve the prognosis of CC patients in the clinical.

Molecular Actions of Enicostemma hyssopifolium Whole Plant Extract on HPV18-Infected Human Cervical Cancer (HeLa) Cells.

Enicostemma hyssopifolium (E. hyssopifolium) contains several bioactive compounds with anti-cancer activities. This study was performed to investigate the molecular effects of E. hyssopifolium on HPV18-containing HeLa cells. The methanol extract of E. hyssopifolium whole plant was tested for cytotoxicity by MTT assay. A lower and higher dose (80 and 160 μg/mL) to IC50 were analyzed for colonization inhibition (Clonogenic assay), cell cycle arrest (FACS analysis), and induction of apoptosis (AO/EtBr staining fluorescent microscopy and FACS analysis) and DNA fragmentation (comet assay). The HPV 18 E6 gene expression in treated cells was analyzed using RT-PCR and qPCR. A significant dose-dependent anti-proliferative activity (IC50 - 108.25±2 μg/mL) and inhibition of colony formation cell line were observed using both treatments. Treatment with 80 μg/mL of extract was found to result in a higher percent of cell cycle arrest at G0/G1 and G2M phases with more early apoptosis, while 160 μg/mL resulted in more cell cycle arrest at SUBG0 and S phases with late apoptosis for control. The comet assay also demonstrated a highly significant increase in DNA fragmentation after treatment with 160 μg/mL of extract (tail moments-19.536 ± 17.8), while 80 μg/mL of extract treatment showed non-significant tail moment (8.152 ± 13.0) compared to control (8.038 ± 12.0). The RT-PCR and qPCR results showed a significant reduction in the expression of the HPV18 E6 gene in HeLa cells treated with 160 μg/mL of extract, while 80 μg/mL did not show a significant reduction. The 160 μg/mL methanol extract of E. hyssopifolium demonstrated highly significant anti-cancer molecular effects in HeLa cells.

Determination of Cytotoxic Activity of Aronia melanocarpa (Michx.) Elliot Fruit Extracts on Breast Cancer (MCF-7) and Cervical Cancer (HeLa) Cell Lines

Aronia (chokeberry) fruits are consumed as fresh fruit due to their high antioxidant activity, and are also preferred among the public in the production of natural medicines. Aronia melanocarpa (Michx.) Elliot, a species of the Rosaceae family, contains many phytochemical compounds such as flavonoids, phenolic compounds, lignans, terpenes, tocopherols, phospholipids, organic acids and high amounts of anthocyanins. In this study, it was aimed to determine the in vitro anticarcinogenic activities of A. melanocarpa (Michx.) Elliot fruit extracts prepared with 6 different solvents. In the study, the cytotoxic effects of the fruits were investigated using breast cancer cell line (MCF-7) and cervical cancer cell line (HeLa), and their effects on healthy cells were investigated using human endothelial cells (HUVEC) and mouse fibroblast cells (L929) by the MTT method. As a result of the study; It was determined that the highest cytotoxicity on the breast cancer (MCF-7) cell line was observed in the ethanol extract (IC50=111.44 µg/mL) and the lowest cytotoxicity was observed in the hexane extract (IC50=661.80 µg/mL). It was determined that the highest cytotoxicity on the cervical cancer (HeLa) cell line was observed in the ethanol extract (IC50=95.14 µg/mL) and the lowest cytotoxicity was observed in the ethyl acetate extract (IC50=319.51 µg/mL). According to these values; It was determined that all extracts of Aronia fruit had cytotoxic effects on MCF-7 and HeLa cell lines, selectivity index values were higher in HeLa cells, and they did not have cytotoxic effects on HUVEC and L929 healthy cell lines (IC50=411.25-663.27 µg/mL). Thus, it has been determined that the fruits of the Aronia melanocarpa species are promising in the development of new natural resources, new drugs and therapeutic agents in cancer treatment, thanks to their anticancer activities and low cytotoxicity. It is recommended that further research be conducted on the mechanisms of anticancer activity in the future

Insight into Romanian Wild-Grown Heracleum sphondylium: Development of a New Phytocarrier Based on Silver Nanoparticles with Antioxidant, Antimicrobial and Cytotoxicity Potential.

Background: Heracleum sphondylium, a medicinal plant used in Romanian ethnopharmacology, has been proven to have remarkable biological activity. The escalating concerns surrounding antimicrobial resistance led to a special attention being paid to new efficient antimicrobial agents based on medicinal plants and nanotechnology. We report the preparation of a novel, simple phytocarrier that harnesses the bioactive properties of H. sphondylium and silver nanoparticles (HS-Ag system). Methods: H. sphondylium's low metabolic profile was determined through gas chromatography-mass spectrometry and electrospray ionization-quadrupole time-of-flight-mass spectrometry. The morphostructural properties of the innovative phytocarrier were analyzed by X-ray diffraction, Fourier-transform infrared spectroscopy, Raman spectroscopy, dynamic light scattering, scanning electron microscopy, and energy-dispersive X-ray spectroscopy. The antioxidant activity was evaluated using total phenolic content, ferric reducing antioxidant power, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) in vitro assays. The antimicrobial activity screening against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, and Escherichia coli was conducted using the agar well diffusion method. The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay estimated the in vitro potential cytotoxicity on normal human dermal fibroblasts (NHDF) and cervical cancer (HeLa) cells. Results: A total of 88 biomolecules were detected, such as terpenoids, flavonoids, phenolic acids, coumarins, phenylpropanoids, iridoids, amino acids, phytosterols, fatty acids. The HS-Ag phytocarrier heightened efficacy in suppressing the growth of all tested bacterial strains compared to H. sphondylium and exhibited a significant inhibition of HeLa cell viability. Conclusions: The new HS-Ag phytocarrier system holds promise for a wide range of medical applications. The data confirm the capacity to augment the pertinent theoretical understanding in the innovative field of antimicrobial agents.

Biosynthesis of Silver Nanoparticles Using Barleria albostellata C.B. Clarke Leaves and Stems: Antibacterial and Cytotoxic Activity

Silver nanoparticles (AgNPs) have increasingly gained attention owing to their distinctive physicochemical and biological properties. The objective of the investigation was to biologically synthesize AgNPs using plant extracts from Barleria albostellata. The synthesized AgNPs, obtained from B. albostellata (leaves and stems), were characterized through various techniques including UV-visible spectroscopy, scanning electron microscopy (SEM), high-resolution transmission electron microscopy (HRTEM), energy-dispersive X-ray analysis, Fourier transform infrared (FTIR) spectral analysis, and nanoparticle tracking analysis (NTA). The antibacterial efficacy of the synthesized AgNPs was evaluated utilizing the disk diffusion method. The cytotoxicity effects of the synthesized AgNPs were determined using the MTT assay (3-[(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide]) in cervical cancer (HeLa), embryonic kidney (HEK293), and breast adenocarcinoma (MCF-7) cell lines. The results indicate that B. albostellata extracts could serve as eco-friendly biofactories for the synthesis of AgNPs. UV-vis spectroscopy of the leaf and stem extracts revealed absorption peaks within the range of 400–450 nm, thereby confirming the synthesis of AgNPs. Elemental Ag was highest in the methanol leaf extracts (16.87 ± 0.89%) and lowest in the powdered stem extracts (7.13 ± 1.44%). Synthesized AgNPs were predominantly spherical in shape. HRTEM revealed that synthesized AgNPs from the methanolic stem extracts (34.32 ± 16.99 nm) were larger in size, while those from the powdered stem extracts were smaller (16.57 ± 5.55 nm). AgNPs synthesized from both the leaf and stem extracts exhibited zeta potential values between −8.8 and −32.1 mV, with hydrodynamics diameters ranging from 34.3 to 111.3 nm. FTIR spectroscopy confirmed the presence of various functional groups on the AgNPs. AgNPs synthesized from the leaf and stem extracts displayed significant antibacterial activity and were sensitive to Gram-negative and Gram-positive bacteria. AgNPs exhibited significant antibacterial activity (diameter of the zone of inhibition) against Pseudomonas aeruginosa (21.67 ± 2.87 mm) in the leaf methanolic extract. Synthesized AgNPs exhibited selective in vitro cytotoxicity against HEK293, HeLa, and MCF-7 cell lines. The IC50 values of the AgNPs synthesized from the various extracts were all above 9 µg/mL. Significant cytotoxic levels (IC50 16.11 and 27.23 µg/mL) were observed for the MCF-7 cell line upon exposure to the methanolic leaf and stem AgNPs. This study recommends the use of medicinal plant extracts in producing economically effective AgNPs, due to their efficient capping. Overall, AgNPs synthesized from B. albostellata extracts comprised novel antibacterial and anticancer agents, and warrant further investigation. Bio-synthesized AgNPs show great potential in the area of nanotechnology and may be used as an affordable, eco-friendly alternative for the delivery of conventional therapeutics.

Antibacterial and Anticancer Properties of Endophenazines from Streptomyces prasinus ZO16, an Endophyte in Zingiber officinale Rosc.

<b>Background and Objective:</b> This study investigated a bacterial strain, ZO16, isolated from ginger (<i>Zingiber officinale</i>) roots. Analysis of its 16S ribosomal DNA (rDNA), along with chemical and physical properties, revealed it to be <i>Streptomyces prasinus</i>. This study aimed to isolate and characterize the main bioactive compounds from ZO16, evaluating their antibacterial and anticancer properties. <b>Materials and Methods:</b> Techniques like column chromatography and thin-layer chromatography (TLC) were used to purify the key compounds from ZO16's culture extract. Nuclear Magnetic Resonance (NMR) spectroscopy and mass spectrometry were utilized to confirm the identities of the purified compounds as endophenazine A (compound 1) and endophenazine B (compound 2). The antibacterial and anticancer properties of these compounds were then evaluated. <b>Results:</b> The isolated compounds displayed antibacterial activity against <i>Staphylococcus aureus</i> ATCC 25923 and Methicillin-Resistant <i>Staphylococcus aureus</i> (MRSA). The minimum inhibitory concentration (MIC) of the isolated compounds against bacteria ranged from 8 to 32 μg/mL, while the minimum bactericidal concentration (MBC) was between 32 and 128 μg/mL. These compounds exhibited effectiveness against tested cancer cells with IC<sub>50</sub> values ranging from 30.40 to 32.51 μg/mL for cervical cancer (HeLa), 78.32 to 86.45 μg/mL for liver cancer (HepG2) and 23.41 to 28.26 μg/mL for breast cancer (MDA-MB-231) cells. However, these compounds also showed moderate toxicity towards non-cancerous Vero cells (IC<sub>50</sub> = 317.44-328.63 μg/mL). <b>Conclusion:</b> The findings of this study suggest that <i>Streptomyces prasinus</i> strain ZO16 produces compounds with antibacterial and anticancer properties. Further investigation of these compounds has the potential to contribute to the development of improved methods for controlling and treating bacterial infections and some cancers.

Radical-Scavenging and Anti-inflammatory Activities of Fermented Eucheuma cottonii from Lombok

Eucheuma cottonii, a widely cultivated seaweed from the Island of Lombok, Indonesia, contains various bioactive compounds. Its utilization, however, is mainly limited based on its high carbohydrate content. Nevertheless, plant fermentation using lactic acid bacteria is renowned for increasing bioactive compounds and enhancing bioactivities. This study unveiled the potential of Lactobacillus plantarum-fermented E. cottonii as a functional food. E. cottonii was fermented using L. plantarum for 24 h. The folin-Ciocalteau method was used to determine the total phenolic content. The antioxidant capacity was measured using a 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay. Anti-inflammatory activity was carried out using cyclooxygenase (COX) inhibition assay against cervical cancer (HeLa) and colon cancer (WiDr) cells. Overall, fermentation successfully enhanced the bioactivities of E. cottonii. Fermented products exhibited higher antioxidant capacity than unfermented ones. Interestingly, the bioactivities only showed a moderate correlation with total phenolic content. Regarding anti-inflammatory activity, fermented extracts exhibited higher cyclooxygenase inhibition against HeLa cells, whereas no significant differences were observed between the fermented and unfermented products in WiDr cells. These findings indicate that L. plantarum-fermented E. cottonii holds promise to be a profitable functional food and has the potential to be utilized as an additional food therapy for cancer treatment. Keywords: Eucheuma cottonii; fermentation; Lactobacillus plantarum; antioxidant, anti-inflammation.

Electrodeposited zinc oxide nanoparticles: Synthesis, characterization, and anti-cervical cancer effects

In the present study, zinc oxide nanoparticles (ZnO NPs) were synthesized via the electrodeposition method and characterized. Then, the anticancer effects of ZnO NPs against cervical cancer HeLa cells were assessed by cell viability, oxidative stress, caspase activity, qRT-PCR, MMP, and ELISA assays. XRD analysis revealed the hexagonal wurtzite phase of ZnO. SEM image of ZnO NPs showed the homogeneous spherical/hexagonal-like structures of ZnO NPs, while TEM imaging revealed the successful synthesis of ZnO NPs with an average diameter of about 8 nm. The UV–vis absorption spectrum of ZnO NPs showed a characteristic absorption band around the wavelength of 368 nm with a band gap energy (Eg) of 3.36 eV. DLS study displayed that the obtained particle size of ZnO NPs has an average size of 29.24 nm and an average zeta potential value of −19 mV. Additionally, cellular findings indicated that the proliferation of cervical cancer HeLa cells was markedly mitigated after incubation with ZnO NPs at different concentrations of 10, 50 and 100 µg/ml, however, these concentrations were not able to trigger an apparent cytotoxic effect on HUVEC non-malignant cells. Also, it was detected that ZnO NPs led to overexpression of Bax/ Bcl-2, caspase-9/-3 genes, increased level of caspase-9/-3 activity, overproduction of MDA level, inhibition of SOD and CAT activity and reduction of GSH content, MMP collapse, and upregulation of cytoplasmic cytochrome c release. In general, these findings suggested that electrodeposited synthesized ZnO NPs can induce anticancer effects in cervical cancer HeLa cells through the mitochondrial-mediated apoptosis signaling pathway.

Synthesis and comparative anticancer studies of Novel amide functoinalised thienopyridine and pyridothienopyrimidinone derivatives

Amide functionalized trifluoromethyl thieno[2,3-b] pyridine derivatives as a series were prepared starting from reaction between 1,3 di-ketone and thiocyanoacetamide. Compound 3 reacts with bromoethyl acetate to give compound 4. Compound 4 on reaction with diverse substituted aromatic and aliphatic amines gives amide derivatives 5a-f and these amide derivatives on reaction with triethylorthoformate give pyridothienopyrimidinone derivatives 6a-f. All the final compounds were evaluated for anti cancer activity against four human cancer cell lines such as A549—Lung cancer (CCL-185), MCF7—Breast cancer (HTB-22), DU145—Prostate cancer (HTB-81) and HeLa—Cervical cancer (CCL-2) by using MTT assay. Promising compound 5d was identified.