Considering the reported activity of carvone in the literature, this study aimed to evaluate the antimicrobial, cytotoxic and chemopreventive activities of (+)-and (-)-carvone, (+)-and (-)-hydroxydihydrocarvone and α,β-epoxycarvone. (+)-Hydroxydihydrocarvone (HC+), (-)-hydroxydihydrocarvone (HC-) and α,βepoxycarvone (EP) were obtained by synthesis using (+)-carvone (C+) or (-)-carvone (C-) as precursors. The antifungal activity (MIC and MFC) were evaluated against Candida parapsilosis, C. tropicalis, C. krusei and C. albicans and the antibacterial activity (MIC and MBC) against Escherichia coli and Staphylococcus aureus. The cytotoxicity assays were performed with human cancer cell lines HepG-2 and SiHa and the normal strain MRC-5 through sulphorrodamine B assay. Chemoprevention was evaluated through quinone reductase assay. Our results showed no cytotoxicity on tumor and normal cell lines and no induction of the quinone reductase enzyme. C-and HC-presented activity against E. coli. All compounds presented weak antifungal activity against C. tropicalis and C. parapsilosis. EP and C+ showed moderate activity against C. krusei. Results suggest the potential use of carvones and its derivatives as antifungal agents against Candida yeasts. The absence of cytotoxicity in cell lines indicates safety in the use of these compounds.
Emerging resistance to insecticides has influenced pharmaceutical research and the search for alternatives to control the common bed bug Cimex lectularius. In this sense, natural products can play a major role. Tagetes patula, popularly known as dwarf marigold, is a plant native to North America with biocide potential. The aim of this work was to evaluate the biological activity of T. patula essential oil (EO) against adult common bed bugs via exposure to dry residues by the Impregnated Paper Disk Test (IPDT) using cypermethrin as a positive control. We selected the enzyme acetylcholinesterase as a target for modeling studies, with the intent of investigating the molecular basis of any biological activity of the EO. Chemical analysis of the EO was performed using gas chromatography coupled to mass spectrometry (GC-MS). Additionally, oral and dermal acute toxicity tests were performed according to Organization for Economic Cooperation and Development (OECD) guidelines. The sulforhodamine B assay (SRB) was performed to verify the cytotoxicity of EO to HaCaT cells. The EO eliminated 100 % of the bed bugs at 100 mg mL with an LC value of 15.85 mg mL. GC-MS analysis identified α-terpinolene, limonene, piperitenone, and piperitone as major components of the mixture. Molecular modeling studies of these major compounds suggested that they are acetylcholinesterase inhibitors with good steric and electronic complementarity. The in vitro cytotoxicity evaluation revealed a LC = 37.06 μg mL and in vivo acute toxicity showed an LC >4000 mg kg, indicating that the EO presents low risk of toxic side effects in humans. The T. patula essential oil components provide a promising strategy for controlling bed bug populations with low mammalian toxicity. These findings pave the way for further in vivo studies aimed at developing a safe and effective insecticide.
Cervical cancer is the second most common malignant tumor in women worldwide and has a high mortality rate, especially when it is associated with human papillomavirus (HPV). In US, an estimated 12,820 cases of invasive cervical cancer and an estimated 4210 deaths from this cancer will occur in 2017. With rare and very aggressive conventional treatments, one sees in the real need of new alternatives of therapy as the delivery of chemotherapeutic agents by nanocarriers using nanotechnology. This review covers different drug delivery systems applied in the treatment of cervical cancer, such as solid lipid nanoparticles (SNLs), liposomes, nanoemulsions and polymeric nanoparticles (PNPs). The main advantages of drug delivery thus improving pharmacological activity, improving solubility, bioavailability to bioavailability reducing toxicity in the target tissue by targeting of ligands, thus facilitating new innovative therapeutic technologies in a too much needed area. Among the main disadvantage is the still high cost of production of these nanocarriers. Therefore, the aim this paper is review the nanotechnology based drug delivery systems in the treatment of cervical cancer.
The excessive use of anthelmintics to control nematodes has resulted in anthelminthic resistance. Essential oils (EOs) are a rich source of bioactive molecules that can be assessed for their ability to control resistant parasite populations. The aims of this study were to screen EOs from 10 plant species in vitro for anthelmintic activity against , evaluate the cytotoxicity of those EOs in a human immortalized keratinocyte cell line (HaCaT), and test the most promising EO candidate in vivo in Santa Inês sheep. The efficacy was investigated in vitro using an egg hatch test (EHT) and a larval development test (LDT). EO cytotoxicity was evaluated with the sulforhodamine-B assay. In the in vivo experiment, 28 Santa Inês sheep naturally infected were distributed into groups: G1- (EO), 200 mg kg; G2-menthol, 160 mg kg; G3-negative control; and G4-positive control (monepantel). EO, from (86.7% menthol), had the lowest LC and LC values in the EHT (0.10, 0.27 mg mL, respectively), good performance in the LDT (0.015, 0.072 mg mL, respectively), and the lowest cytotoxicity (190.9 µg mL) in HaCaT cells. In the in vivo test, a single dose of the EO (200 mg kg BW) had an efficacy of approximately 50% on days 1, 14, and 21; however, values were not significantly from day 0. Conversely, pure menthol at a dose of 160 mg kg BW showed no in vivo efficacy. This can be attributed to key factors related to bioavailability and pharmacology of terpenes in the host organism, as well as to the fact that menthol is mainly excreted as glucuronides in urine. Thus, further studies should be conducted with formulation systems that deliver bioactives directly to the abomasum, focusing on terpenes, whose excretion route is mainly via faeces.
The cattle tick Rhipicephalus microplus is a great sanitary problem and causes huge losses to livestock, being a vector of important diseases. The aim of this work was to verify the action of plant-derived material obtained from Tagetes patula on the life cycle of R. microplus, as well as to analyze the action of these extracts on ovary cells of engorged females.
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