Bioactivity of Carlina acaulis essential oil and its main component to the olive fruit fly, Bactrocera oleae: ingestion toxicity, electrophysiological and behavioural insights
In recent years, botanical insecticides based on essential oils (EOs), or their main components, have received much attention as promising tools for Integrated Pest Management, due to their environmental safety and low side effects on non-target organisms. In this study, Carlina acaulis EO and its main component, carlina oxide, recently proven to be effective larvicidal and adulticidal agents against some insect pests, were analyzed for their toxicity, electroantennographic (EAG), and behavioral responses to adult olive fruit fly (Bactrocera oleae). The C. acaulis EO was more toxic to the tephritid than the carlina oxide, and both were more toxic to the same insect pest than EOs from other …
From the covalent linkage of drugs to novel inhibitors of ribonucleotide reductase: synthesis and biological evaluation of valproic esters of 3'-C-methyladenosine
We synthesized a series of serum-stable covalently linked drugs derived from 3'-C-methyladenosine (3'-Me-Ado) and valproic acid (VPA), which are ribonucleotide reductase (RR) and histone deacetylase (HDAC) inhibitors, respectively. While the combination of free VPA and 3'-Me-Ado resulted in a clear synergistic apoptotic effect, the conjugates had lost their HDAC inhibitory effect as well as the corresponding apoptotic activity. Two of the analogs, 2',5'-bis-O-valproyl-3'-C-methyladenosine (A160) and 5'-O-valproyl-3'-C-methyladenosine (A167), showed promising cytotoxic activities against human hematological and solid cancer cell lines. A167 was less potent than A160 but had interesting featu…
Lethal and behavioural effects of a green insecticide against an invasive polyphagous fruit fly pest and its safety to mammals
Abstract 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). The carlina oxide was formulated in a mucilaginous solution containing carboxymethylcellulose sodium salt, sucrose, and hyd…
Carlina acaulis and Trachyspermum ammi essential oils formulated in protein baits are highly toxic and reduce aggressiveness in the medfly, Ceratitis capitata
Abstract Essential oil (EO)-based botanical insecticides are considered a promising option for Integrated Pest Management (IPM). However, the sublethal effects of EO-based insecticides are understudied. No information is available on the potential effects of EO exposure on insect aggressive traits. In this study, the toxicity of two EOs with documented efficacy on insect vectors and agricultural pests, and which were obtained from the roots of silver thistle (Carlina acaulis L., Asteraceae) and seeds (i.e. schizocarps) of ajwain (Trachyspermum ammi (L.) Sprague, Apiaceae), was evaluated against adults of the Mediterranean fruit fly, Ceratitis capitata (Wiedemann) (medfly), a cosmopolitan fr…
Identification of highly effective antitrypanosomal compounds in essential oils from the Apiaceae family
The Apiaceae family encompasses aromatic plants of economic importance employed in foodstuffs, beverages, perfumery, pharmaceuticals and cosmetics. Apiaceae are rich sources of essential oils because of the wealth of secretory structures (ducts and vittae) they are endowed with. The Apiaceae essential oils are available on an industrial level because of the wide cultivation and disposability of the bulky material from which they are extracted as well as their relatively cheap price. In the fight against protozoal infections, essential oils may represent new therapeutic options. In the present work, we focused on a panel of nine Apiaceae species (Siler montamon, Sison amomum, Echinophora spi…
Histone deacetylase inhibition modulates deoxyribonucleotide pools and enhances the antitumor effects of the ribonucleotide reductase inhibitor 3’-C-methyladenosine in leukaemia cells
Histone deacetylase (HDAC) inhibitors are a new class of epigenetic agents that were reported to enhance the cytotoxic effects of classical anticancer drugs through multiple mechanisms. However, which of the possible drug combinations would be the most effective and clinically useful are to be determined. We treated the HL60 and NB4 promyelocytic leukaemia cells with a combination of the ribonucleotide reductase (RR) inhibitor 3'-C-methyladenosine (3'-Me-Ado) and several hydroxamic acid-derived HDAC inhibitors, including two recently synthesized molecules, MC1864 and MC1879, and the reference compound trichostatin A (TSA). The results showed significant growth inhibitory and apoptotic syner…
Developing green insecticides to manage olive fruit flies? Ingestion toxicity of four essential oils in protein baits on Bactrocera oleae
Abstract Effective and eco-friendly plant-borne insecticides for developing lure and kill control tools against tephritid flies are scarce. Herein, the activity of four essential oils (EOs) obtained from two Apiaceae, Pimpinella anisum L. and Trachyspermum ammi (L.) Sprague, and two Lamiaceae, Thymbra spicata L. and Ocimum gratissimum L., was evaluated against the olive fruit fly, Bactrocera oleae (Rossi), a key pest of olive groves. The EO chemical composition was determined by gas chromatography coupled with mass spectrometry (GC-MS) analyses. The four EOs incorporated in protein baits were tested for ingestion toxicity on B. oleae adults, mimicking lure and kill assays. Results showed con…