Ameliorative inhibition of sirtuin 6 by imidazole derivative triggers oxidative stress-mediated apoptosis associated with Nrf2/Keap1 signaling in non-small cell lung cancer cell lines.

Redox homeostasis is the vital regulatory system with respect to antioxidative response and detoxification. The imbalance of redox homeostasis causes oxidative stress. Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2, also called Nfe2l2)/Kelchlike ECH-associated protein 1 (Keap1) signaling is the major regulator of redox homeostasis.

and functional validation of imidazole derivatives as potential sirtuin inhibitor.

Introduction: Epigenetic enzymes can interact with a wide range of genes that actively participate in the progression or repression of a diseased condition, as they are involved in maintaining cellular homeostasis. Sirtuins are a family of Class III epigenetic modifying enzymes that regulate cellular processes by removing acetyl groups from proteins. They rely on NAD as a coenzyme in contrast to classical histone deacetylases (HDACs) (Class I, II, and IV) that depend on Zn for their activation, linking their function to cellular energy levels.

Dietary tannic acid attenuates elastase-induced pulmonary inflammation and emphysema in mice.

Emphysema is one of the major components of chronic obstructive pulmonary disease (COPD), which is characterised by the destruction and enlargement of air spaces, leading to airflow limitation and dyspnoea, finally progressing to oxygen dependency. The alveolar wall destruction is due to chronic inflammation, oxidative stress, apoptosis, and proteinase/anti-proteinase imbalance. So far, there has been no effective therapy for patients with COPD.

Knockdown of sirtuin6 positively regulates acetylation of DNMT1 to inhibit NOTCH signaling pathway in non-small cell lung cancer cell lines.

Background And Aim: Sirtuin proteins (1-7) are nicotinamide adenine dinucleotide (NAD)-dependent deacetylases and ADP-ribosyl transferases (class III histone deacetylase enzymes (HDAC)) mainly involved in the removal of the acetyl group from histone proteins. SIRT6, one of the sirtuins, plays a major role in cancer progression in many types of cancer conditions. We recently reported that SIRT6 acts as an oncogene in NSCLC; thus, silencing of SIRT6 inhibits cell proliferation and induces apoptosis in NSCLC cell lines.

Wnt Signaling Pathway Collapse upon β-Catenin Destruction by a Novel Antimicrobial Peptide SKACP003: Unveiling the Molecular Mechanism and Genetic Activities Using Breast Cancer Cell Lines.

Despite progress in breast cancer treatment, the survival rate for patients with metastatic breast cancer remains low due to chemotherapeutic agent resistance and the lack of specificity of the current generation of cancer drugs. Our previous findings indicated that the antimicrobial peptide SKACP003 exhibited anticancer properties, particularly against the MCF-7, MDA-MB-231, and MDA-MB-453 breast cancer cell lines. However, the mechanism of SKACP003-induced cancer cell death is unknown.

N-(2-hydroxyphenyl)-2-phenazinamine from Nocardiopsis exhalans induces p53-mediated intrinsic apoptosis signaling in lung cancer cell lines.

The present study aims to investigate the effect and the molecular mechanism of N-(2-hydroxyphenyl)-2-phenazinamine (NHP) isolated from Nocardiopsis exhalans against the proliferation of human lung cancer cells. The cytotoxic activity of NHP against A549 and H520 cells was determined using MTT assay. The cytotoxic activity of NHP against A549 and H520 lung cancer cells showed excellent activity at 75 μg/mL and damage the mitochondrial membrane and nucleus by generating oxidative stress.

Structural exploration of common pharmacophore based berberine derivatives as novel histone deacetylase inhibitor targeting HDACs enzymes.

Histone deacetylase (HDAC) inhibitors, are new class of cancer chemotherapeutics used in clinical development. It plays a pivotal role in restoring the acetylation balance and lysine residual deacetylation in histone and non-histone proteins. Notably, HDAC inhibitors have been approved by FDA to treat different malignancies.

A mouse testis serine protease, TESP1, as the potential SPINK3 receptor protein on mouse sperm acrosome.

Serine protease inhibitor Kazal type 3 (SPINK3) from mouse seminal vesicles is a Kazal-type trypsin inhibitor. It has been shown to bind to the sperm acrosome and modify sperm activity by influencing the sub-cellular Ca2+ influx. Previously, SPINK3 was reported to suppress in vitro sperm capacitation.

An overview on the role of plant-derived tannins for the treatment of lung cancer.

Lung cancer is the leading cause of cancer-related death globally. Despite many advanced approaches to treat cancer, they are often ineffective due to resistance to classical anti-cancer drugs and distant metastases. Currently, alternative medicinal agents derived from plants are the major interest due to high bioavailability and fewer adverse effects.

Repurposing of histone deacetylase inhibitors: A promising strategy to combat pulmonary fibrosis promoted by TGF-β signalling in COVID-19 survivors.

Coronavirus disease 2019 (COVID-19) has rapidly spread around the world causing global public health emergency. In the last twenty years, we have witnessed several viral epidemics such as severe acute respiratory syndrome coronavirus (SARS-CoV), Influenza A virus subtype H1N1 and most recently Middle East respiratory syndrome coronavirus (MERS-CoV). There were tremendous efforts endeavoured globally by scientists to combat these viral diseases and now for SARS-CoV-2.

Silencing Sirtuin 6 induces cell cycle arrest and apoptosis in non-small cell lung cancer cell lines.

Sirtuins (SIRT1-7), are NAD-dependent deacetylases and ADP-ribosyl transferases, plays a major part in carcinogenesis. The previous report suggests that in cancer, sirtuins gained tremendous interest and critical regulators of the unusual processes. In carcinogenesis, sirtuins possess either tumor suppressor or promoter.

Annona muricata assisted biogenic synthesis of silver nanoparticles regulates cell cycle arrest in NSCLC cell lines.

With plenteous accessible therapeutics, lung cancer endures a preeminent cause of the worldwide fatality. Apart from medical advancements, various plant parts are still used to treat cancer based on proven tradition. The present study focuses on analysing the anticancer efficacy of silver nanoparticles coupled with the aqueous leaf extract of Annona muricata.

Incorporated plant extract fabricated silver/poly-D,l-lactide-co-glycolide nanocomposites for antimicrobial based wound healing.

Polymeric nanocomposites have gained extensive attention in modern nanotechnology by reason of its design, flexibility, sole applications and lower life cycle costs. Preparation of composites using spreading of inorganic metal nanoparticles in organic polymeric matrices has plenty of scope and applications in the biomedical field. Poly-D,l-lactide-co-glycolide (PLGA) is an appreciated polymer for composites preparation because of its non-toxic and promising biodistribution.

Multifarious Pharmacological Applications of Green Routed Eco-Friendly Iron Nanoparticles Synthesized by Streptomyces Sp. (SRT12).

A simple, eco-friendly, green routine co-precipitation method was experimented to synthesize iron nanoparticles (Fe-NPs) using the cell-free supernatant of actinobacteria. The biosynthesized nanoparticles were characterized by UV-Vis spectroscopy, X-ray diffractometer (XRD), energy-dispersive X-ray (EDX), scanning electron microscopy (SEM), atomic force microscopy (AFM), zeta potential analyser and Fourier transform infrared (FTIR) spectroscopy. The synthesized nanoparticles were crystalline, quasi-spherical in shape and their average size ranged from 65.

Antibacterial and anticancer potential of marine endophytic actinomycetes Streptomyces coeruleorubidus GRG 4 (KY457708) compound against colistin resistant uropathogens and A549 lung cancer cells.

The aim of the current study is to identify bioactive compound from marine endophytic actinomycetes (MEA) isolated from Gulf of Mannar region, Southeast coast of India. Among the isolated actinomycetes, strain GRG 4 exhibited excellent ability to inhibit isolated colistin resistant (CR) Pseudomonas aeruginosa (P. aeruginosa) and Klebsiella pneumoniae (K.

p53 mediated transcriptional regulation of long non-coding RNA by 1-hydroxy-1-norresistomycin triggers intrinsic apoptosis in adenocarcinoma lung cancer.

Over a few decades, systemic chemotherapy and surgery are the only treatment options for lung cancer. Due to limited efficacy and overall poor survival of patients, it is necessary to develop a newer therapeutic strategy which specifically targets cancer cell proliferation pathway. Deciphering the role of long non-coding RNAs (lncRNAs) in tumorigenesis and pathogenesis of cancer cells has recently emerged.

Target delivery of doxorubicin tethered with PVP stabilized gold nanoparticles for effective treatment of lung cancer.

Development of drug delivery system conjugated with doxorubicin (dox) on the surface of AuNPs with polyvinylpyrrolidone (Dox@PVP-AuNPs), we have demonstrated that human lung cancer cells can significantly overcome by the combination of highly effective cellular entry and responsive intracellular release of doxorubicin from Dox@PVP-AuNPs complex. Previously drug release from doxorubicin-conjugated AuNPs was confirmed by the recovered fluorescence of doxorubicin from quenching due to the nanosurface energy transfer between doxorubicinyl groups and AuNPs. Dox@PVP-AuNPs achieved enhanced inhibition of lung cancer cells growth than free Doxorubicin and PVP-AuNPs.

Correlative Studies Unravelling the Possible Mechanism of Cell Death in Tideglusib-Treated Human Ovarian Teratocarcinoma-Derived PA-1 Cells.

This study aims to unravel the use of GSK-3 inhibitors as viable apoptotic inducers for teratocarcinoma-derived ovarian PA-1 cells. MTT assay was carried out to assess inhibitory concentrations of LiCl and TDG. AO/EB staining and Hoechst 33258 staining were employed to assess the damage.

Structural characterization and anticancer activity (MCF7 and MDA-MB-231) of polysaccharides fractionated from brown seaweed Sargassum wightii.

The purpose of this study was to investigate the anticancer activity of polysaccharides from brown seaweed Sargassum wightii (SWP) on human breast cancer cells. Initially, two polysaccharide fractions (SWP1 and SWP2) were isolated and purified from the crude polysaccharides using DEAE-52 cellulose and Sephadex G-100 column chromatography. As a result, SWP1 was obtained with the yield of 21.

Design, synthesis, and characterization of α, β-unsaturated carboxylic acid, and its urea based derivatives that explores novel epigenetic modulators in human non-small cell lung cancer A549 cell line.

Histone deacetylase inhibitors (HDACi) are a small molecule chemotherapeutics that target the chromatin remodeling through the regulation of histone and non-histone proteins. These inhibitors directed against histone deacetylase (HDAC) enzymes have become an important therapeutic tool in oncology; consequently, scientific efforts have fortified the quest for newer and novel HDACi, which forces the design of structurally innovative HDACi. Various urea containing compounds exhibited admirable anticancer activity.

Copper oxide nanoparticles induce anticancer activity in A549 lung cancer cells by inhibition of histone deacetylase.

Objectives: Copper oxide nanoparticles (CuO NPs) promoting anticancer activity may be due to the regulation of various classes of histone deacetylases (HDACs).

Results: Green-synthesized CuO NPs significantly arrested total HDAC level and also suppressed class I, II and IV HDACs mRNA expression in A549 cells. A549 cells treated with CuO NPs downregulated oncogenes and upregulated tumor suppressor protein expression.

Synthesis, characterization, and evaluation of Cd[L-proline], a novel histone deacetylase inhibitor that induces epigenetic modification of histone deacetylase isoforms in A549 cells.

Histone deacetylases (HDACs) play an important role in the epigenetic regulation of gene expression through their effects on the compact chromatin structure. In clinical studies, several classes of histone deacetylase inhibitors (HDACi) have demonstrated potent anticancer activities with metal complexes. Hence, we synthesized cadmium-proline complexes using both the D- and L-isomers of proline and evaluated their biological activities by observing the efficiency of their inhibition of HDAC activity, ability to reduce the expression of HDAC isoforms in A549 cells and effect on apoptosis.

Anticancer activity of graphene oxide-reduced graphene oxide-silver nanoparticle composites.

In the present study, a chemical route was employed to synthesize graphene oxide (GO)-reduced graphene oxide (rGO)-Ag nanoparticle (AgNP) composites from graphite and AgNO using vitamin C as reducing agent. Powder X-ray diffraction pattern and field emission scanning electron microscope images revealed that the AgNP were uniformly distributed on the surface of GO and rGO nanosheets. For the first time, the cytotoxicity of GO, rGO, AgNP, GO-AgNP and rGO-AgNP composites were examined against human lung cancer A549 cells using MTT assay and reported quantitatively.

Plant Isoquinoline Alkaloid Berberine Exhibits Chromatin Remodeling by Modulation of Histone Deacetylase To Induce Growth Arrest and Apoptosis in the A549 Cell Line.

Histone deacetylases (HDACs) are a group of epigenetic enzymes that control gene expression through their repressive influence on histone deacetylation transcription. HDACs are probable therapeutic targets for cancer treatment, spurring the progress of different types of HDAC inhibitors. Further, natural-source-based derived bioactive compounds possess HDAC inhibitor property.

Preparation of Histone Deacetylase Inhibitor Vorinostat-Loaded Poly D, L-Lactide-co-Glycolide Polymeric Nanoparticles by Nanoprecipitation Method.

Nanotechnology is a comparatively new branch of science that includes harnessing the unique properties of particles that are nanometers in scale. Nanoparticles can be tailored in a precise fashion where their size, composition, and surface chemistry can be carefully controlled. The nanoprecipitation is a simple, powerful, and low-energy requiring technique, commonly used for the preparation of defined nanoparticles.