Synthesis, Biological, and Computational Evaluations of Conformationally Restricted NAD-Mimics as Discriminant Inhibitors of Human NMN-Adenylyltransferase Isozymes.

Nicotinamide adenine dinucleotide (NAD) cofactor metabolism plays a significant role in cancer development. Tumor cells have an increased demand for NAD and ATP to support rapid growth and proliferation. Limiting the amount of available NAD by targeting critical NAD biosynthesis enzymes has emerged as a promising anticancer therapeutic approach.

Synthesis of Carlina Oxide Analogues and Evaluation of Their Insecticidal Efficacy and Cytotoxicity.

Compounds isolated from botanical sources represent innovative and promising alternatives to conventional insecticides. Carlina oxide is a compound isolated from L. (Asteraceae) essential oil (EO) with great potential as bioinsecticide, being effective on various arthropod vectors and agricultural pests, with moderate toxicity on non-target species.

Efficacy of L. Essential Oil (Linalool/Linalool Acetate Chemotype) against Insect Vectors and Agricultural Pests.

In recent years, agrochemical industries have been focused on the development of essential oil (EO)-based biopesticides, which can be considered valuable alternatives to traditional chemical products. The genus (Lamiaceae) comprises 30 species characterized by a wide range of biological activities, and some of their EOs showed good potential as pesticidal agents. In this regard, the aim of this study was to evaluate the insecticidal activity of the EO obtained from a rare linalool/linalool acetate chemotype of L.

A Versatile Continuous Fluorometric Enzymatic Assay for Targeting Nicotinate Phosphoribosyltransferase.

The maintenance of a proper NAD pool is essential for cell survival, and tumor cells are particularly sensitive to changes in coenzyme levels. In this view, the inhibition of NAD biosynthesis is considered a promising therapeutic approach. Current research is mostly focused on targeting the enzymes nicotinamide phosphoribosyltransferase (NAMPT) and nicotinate phosphoribosyltransferase (NAPRT), which regulate NAD biosynthesis from nicotinamide and nicotinic acid, respectively.

A Review of the Chemistry and Biological Activities of ("jambù", Asteraceae), with a View to the Development of Bioinsecticides and Acaricides.

Human pathologies, environmental pollution, and resistance phenomena caused by the intensive use of chemical pesticides have shifted the attention of the agrochemical industries towards eco-friendly insecticides and acaricides. (L.) R.

Potent and selective anticancer activity of half-sandwich ruthenium and osmium complexes with modified curcuminoid ligands.

We have recently reported a series of half-sandwich ruthenium(II) complexes with curcuminoid ligands showing excellent cytotoxic activities (particularly ionic derivatives containing PTA (PTA = 1,3,5-triaza-7-phosphaadamantane). In the present study, new members of this family of compounds have been prepared with the objective to investigate the effect of a long hydrophobic chain obtained by replacing the OH-groups, present in curcumin and bisdemethoxycurcumin, with the palmitic acid ester. We report the synthesis of ruthenium(II) and osmium(II) p-cymene derivatives containing palmitic acid curcumin ester ligands ((1,3,6)-3-hydroxy-5-oxohepta-1,3,6-triene-1,7-diyl)bis(2-methoxy-4,1-phenylene)dipalmitate () and ((1,3,6)-3-hydroxy-5-oxohepta-1,3,6-triene-1,7-diyl)bis(4,1-phenylene)dipalmitate ().

Insecticidal Activity of Four Essential Oils Extracted from Chilean Patagonian Plants as Potential Organic Pesticides.

Patagonia is a geographical area characterized by a wide plant biodiversity. Several native plant species are traditionally used in medicine by the local population and demonstrated to be sources of biologically active compounds. Due to the massive need for green and sustainable pesticides, this study was conducted to evaluate the insecticidal activity of essential oils (EOs) from understudied plants growing in this propitious area.

Comparative Analysis of the Antimicrobial Activity of Essential Oils and Their Formulated Microemulsions against Foodborne Pathogens and Spoilage Bacteria.

The antimicrobial activity of several essential oils (EOs) and their related microemulsions (MEs) was investigated. EOs were obtained from Cannabis sativa L. cv CS (C.

A Comprehensive Phytochemical Analysis of Terpenes, Polyphenols and Cannabinoids, and Micromorphological Characterization of 9 Commercial Varieties of L.

New hemp ( L.) strains developed by crossbreeding selected varieties represent a novel research topic worthy of attention and investigation. This study focused on the phytochemical characterization of nine hemp commercial cultivars.

Antitrypanosomal Activity of Nemorosa Essential Oils and Combinations of Their Main Constituents.

This study aimed to investigate the susceptibility of to the essential oils (EOs), isolated compounds from these oils, and artificial mixtures of the isolated compounds in their conventional and nanoencapsulated forms. The chemical composition of the essential oils from the aerial parts and roots of , obtained from a wild population growing in central Italy, were analyzed by gas chromatography/mass spectrometry (GC/MS). In both cases, the predominant class of compounds was monoterpene hydrocarbons, which were more abundant in the EOs from the roots (81.

Bioactivity of Essential Oil and Its Main Component towards the Olive Fruit Fly, : Ingestion Toxicity, Electrophysiological and Behavioral Insights.

Among botanical insecticides based on essential oils (EOs) or their main components, EO and the aromatic polyacetylene carlina oxide, constituting more than 90% of its EO, were recently proven to be effective against the larvae and adults of some insect vectors and pests. In this study, the toxicity of EO and carlina oxide were tested on adults using a protein bait formulation. The LC values of the EO and carlina oxide were 706 ppm and 1052 ppm, respectively.

Lethal and behavioural effects of a green insecticide against an invasive polyphagous fruit fly pest and its safety to mammals.

Plant essential oil-based insecticides, with special reference to those that may be obtained from largely available biomasses, represent a valuable tool for Integrated Pest Management. However, the sublethal effects and the potential effects on aggressive insect traits of these green insecticides are understudied. Herein, the lethal and sub-lethal effects of the carlina oxide, constituting more than 97% of the whole Carlina acaulis (Asteraceae) root essential oil (EO), were determined against an invasive polyphagous tephritid pest, Ceratitis capitata (medfly).

A Design of Experiment (DoE) Approach to Model the Yield and Chemical Composition of Ajowan ( L.) Essential Oil Obtained by Microwave-Assisted Extraction.

Ajowan ( L.) is a spice traditionally used in Middle Eastern medicine and contains a valuable essential oil (EO) exploited in different fields, such as pharmaceutics, agrochemicals and food additives. This EO is mostly characterized by the thymol to which most of its biological properties are related.

Isofuranodiene, a Natural Sesquiterpene Isolated from Wild Celery ( L.), Protects Rats against Acute Ischemic Stroke.

The myrrh-like furanosesquiterpene isofuranodiene (IFD) is the main constituent of wild celery ( L., Apiaceae), an overlooked vegetable that was cultivated during the Roman Empire. In the present study, we investigated the protective effects of IFD pre-treatment against oxidative stress and inflammatory response in an animal model of ischemic stroke.

Adenosine receptors as promising targets for the management of ocular diseases.

The ocular drug discovery arena has undergone a significant improvement in the last few years culminating in the FDA approvals of 8 new drugs. However, despite a large number of drugs, generics, and combination products available, it remains an urgent need to find breakthrough strategies and therapies for tackling ocular diseases. Targeting the adenosinergic system may represent an innovative strategy for discovering new ocular therapeutics.

Studying GGDEF Domain in the Act: Minimize Conformational Frustration to Prevent Artefacts.

GGDEF-containing proteins respond to different environmental cues to finely modulate cyclic diguanylate (c-di-GMP) levels in time and space, making the allosteric control a distinctive trait of the corresponding proteins. The diguanylate cyclase mechanism is emblematic of this control: two GGDEF domains, each binding one GTP molecule, must dimerize to enter catalysis and yield c-di-GMP. The need for dimerization makes the GGDEF domain an ideal conformational switch in multidomain proteins.

Developing a Highly Stable Essential Oil Nanoemulsion for Managing .

The growing interest in the development of green pest management strategies is leading to the exploitation of essential oils (EOs) as promising botanical pesticides. In this respect, nanotechnology could efficiently support the use of EOs through their encapsulation into stable nanoformulations, such as nanoemulsions (NEs), to improve their stability and efficacy. This technology assures the improvement of the chemical stability, hydrophilicity, and environmental persistence of EOs, giving an added value for the fabrication of natural insecticides effective against a wide spectrum of insect vectors and pests of public and agronomical importance.

Phytochemical Analysis and Trypanocidal Activity of Desr.

The rationale inspiring the discovery of lead compounds for the treatment of human parasitic protozoan diseases from natural sources is the well-established use of medicinal plants in various systems of traditional medicine. On this basis, we decided to select an overlooked medicinal plant growing in central Italy, Desr. (Lamiaceae), which has been used as a traditional remedy against protozoan diseases, and to investigate its potential against Human African trypanosomiasis (HAT).

Effectiveness of eight essential oils against two key stored-product beetles, Prostephanus truncatus (Horn) and Trogoderma granarium Everts.

The use of chemical pesticides to preserve food commodities is a global issue of concern due to their negative effect on the environment and public health. In recent years, the European Union is trying to reduce their use, favoring alternative or complementary approaches based on natural products. In this scenario, plant-borne essential oils (EOs) represent valid options for Integrated Pest Management (IPM) programs.

Insecticidal activity of two essential oils used in perfumery (ylang ylang and frankincense).

Nowadays, only a little part of essential oils produced at an industrial level is employed for insecticidal formulations, while thousand tons are used for perfumery purposes. This research explores the insecticidal potential of two essential oils largely used in perfumery, ylang ylang () and frankincense ( spp.) on three insects of economic importance, , and comparing their performances with a commercial pyrethrum extract.

Outstanding insecticidal activity and sublethal effects of Carlina acaulis root essential oil on the housefly, Musca domestica, with insights on its toxicity on human cells.

Carlina acaulis (Compositae) is traditionally used for food and medicinal purposes in central and southern Europe. Its root essential oil (EO), mainly composed by carlina oxide, is included in the BELFRIT botanical list of food supplements. It is also recognized as a potent mosquito larvicide.

Exploring the Molecular Mechanisms Underlying the in vitro Anticancer Effects of Multitarget-Directed Hydrazone Ruthenium(II)-Arene Complexes.

The molecular targets and the modes of action behind the cytotoxicity of two structurally established N,O- or N,N-hydrazone ruthenium(II)-arene complexes were explored in human breast adenocarcinoma cells (MCF-7) and paralleled in non-cancerous and cisplatin-resistant counterparts (MCF-10A and MCF-7CR respectively). Both complexes, [Ru(hmb)(L1)Cl] (1, L1=4-((2-(2,4-dinitrophenyl)hydrazono)(phenyl)methyl)-3-methyl-1-phenyl-1H-pyrazol-5-olate) and [Ru(cym)(L2)Cl] (2, L2=1-((3-methyl-5-oxo-1-phenyl-1H-pyrazol-4(5H)-ylidene)(phenyl)methyl)-2-(pyridin-2-yl)hydrazin-1-ide), reversibly interact with moderate-to-high affinity with a number of molecular targets in cell-free assays, namely serum albumin, DNA, the 20S proteasome and hydroxymethylglutaryl-CoA reductase. Most interestingly, only 2 readily crosses the cell membrane and preserves its binding/modulatory ability toward the targets of interest upon rapid cellular internalization.

Efficacy of Essential Oil against the Mosquito Vector and the Gastrointestinal Parasite , with Insights on Acetylcholinesterase Inhibition.

Developing effective and eco-friendly antiparasitic drugs and insecticides is an issue of high importance nowadays. In this study, we evaluated the anthelminthic and insecticidal potential of the leaf essential oil obtained from against the L3 larvae of the parasitic nematode and larvae and adults of the mosquito . Tests on were performed by standard larvicidal and penetration assays, while mosquito toxicity was assessed relying on larvicidal, tarsal contact, and fumigation tests.

Exploring the Insecticidal Potential of Boldo () Essential Oil: Toxicity to Pests and Vectors and Non-target Impact on the Microcrustacean .

Every year Chile exports about 2000 tons of boldo folium (), which is used around the world as a traditional herbal medicinal product (THMP), mostly to relieve gastrointestinal disorders. This biomass may be a resource for the agrochemical industry to manufacture botanical insecticides. In this regard, the insecticidal potential of boldo has been poorly investigated.