scholarly journals In-Vitro Evaluation of 52 Commercially-Available Essential Oils Against Leishmania amazonensis

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1248 ◽  
Author(s):  
Lianet Monzote ◽  
Isabel Herrera ◽  
Prabodh Satyal ◽  
William Setzer
Keyword(s):  
Essential Oils ◽  
Low Cost ◽  
Treatment Options ◽  
Clinical Manifestations ◽  
Peritoneal Macrophages ◽  
Current Treatment ◽  
Leishmania Amazonensis ◽  
Ic50 Values ◽  
Antileishmanial Activities

Leishmaniasis is a neglected tropical disease caused by members of the Leishmania genus of parasitic protozoa that cause different clinical manifestations of the disease. Current treatment options for the cutaneous disease are limited due to severe side effects, poor efficacy, limited availability or accessibility, and developing resistance. Essential oils may provide low cost and readily available treatment options for leishmaniasis. In-vitro screening of a collection of 52 commercially available essential oils has been carried out against promastigotes of Leishmania amazonensis. In addition, cytotoxicity has been determined for the essential oils against mouse peritoneal macrophages in order to determine selectivity. Promising essential oils were further screened against intracellular L. amazonensis amastigotes. Three essential oils showed notable antileishmanial activities: frankincense (Boswellia spp.), coriander (Coriandrum sativum L.), and wintergreen (Gualtheria fragrantissima Wall.) with IC50 values against the amastigotes of 22.1 ± 4.2, 19.1 ± 0.7, and 22.2 ± 3.5 μg/mL and a selectivity of 2, 7, and 6, respectively. These essential oils could be explored as topical treatment options for cutaneous leishmaniasis.

scholarly journals In vitro Anti-Trypanosomal Activities of Indanone-Based Chalcones

Drug Research ◽  
2018 ◽  
Vol 69 (06) ◽  
pp. 337-341 ◽  
Author(s):  
Richard M. Beteck ◽  
Lesetje J. Legoabe ◽  
Michelle Isaacs ◽  
Heinrich C. Hoppe
Keyword(s):  
Rural Areas ◽  
Human African Trypanosomiasis ◽  
Low Cost ◽  
Treatment Options ◽  
Current Treatment ◽  
Sar Studies ◽  
Ic50 Values ◽  
Life Threatening ◽  
Poor Efficacy

Human African trypanosomiasis is a neglected infectious disease that affects mostly people living in the rural areas of Africa. Current treatment options are limited to just four drugs that have been in use of four to nine decades. The life-threatening toxic side-effects associated with the use of these drugs are disconcerting. Poor efficacy, low oral bioavailability, and high cost are other shortcomings of current HAT treatments. Evaluating the potentials of known hits for other therapeutic areas may be a fast and convenient method to discover new hit compounds against alternative targets. A library of 34 known indanone based chalcones was screened against T.b. brucei and nine potent hits, having IC50 values between 0.5–8.9 µM, were found. The SAR studies of this series could provide useful information in guiding future exploration of this class of compounds in search of more potent, safe, and low cost anti-trypanosomal agents. Graphical Abstract

scholarly journals Potential Antileishmanial Activity of Essential Oils of Native Species from Southern Brazil

2016 ◽  
Vol 6 (4) ◽  
pp. 18 ◽  
Author(s):  
Carla Kauffmann ◽  
Eduardo M. Ethur ◽  
Barbara Buhl ◽  
Talita Scheibel ◽  
Gerzia M. C. Machado ◽  
...  
Keyword(s):  
Essential Oils ◽  
Native Species ◽  
Neglected Tropical Diseases ◽  
Antileishmanial Activity ◽  
Reference Drug ◽  
Ic50 Values ◽  
Brazilian Flora ◽  
South Of Brazil ◽  
Antileishmanial Activities

Leishmaniasis are a neglected tropical diseases that affecting 98 countries on three continents. Every year, 1.3 million of people are infected with the disease and 50.000 persons die because of this. The aim of this work was to evaluate antileishmanial activities in vitro from native species of South of Brazil belonging to the Myrtaceae family. The essential oils from leaves of Calyptranthes grandifolia, Calyptranthes tricona, Eugenia anomala, Eugenia arenosa, Eugenia pyriformis, Myrrhinium atropurpureum and Psidium salutare were analyzed in vitro for antileishmanial activity against promastigotes of Leishmania amazonensis, employed MTT assay. The essential oils from leaves of C. grandifolia, C. tricona, E. arenosa and E. pyriformis presented IC50 values of 31.27 ± 6.40 µg/mL, 26.13 ± 8.60 µg/mL, 13.72 ± 8.65 µg/mL and 19.73 ± 5.40 µg/mL, respectively, and not are statistically different from pentamidine (IC50 = 23.22 ± 9.04 µg/mL), the reference drug. The results show the potential of essential oils from leaves of C. grandifolia, C. tricona, E. arenosa and E. pyriformis as antileishmanial, as well as the importance of continuing studies to in order to advance in the search and development of new therapeutic options from of brazilian flora sources.

scholarly journals In vitro evaluation of anticaries, antimycobacterial, antileishmanial and cytotoxic activities of essential oils from Eremanthus erythropappus and of α-bisabolol, their major sesquiterpene

2020 ◽  
pp. 236-243
Author(s):  
Cassia Cristina Fernandes ◽  
Priscila Mileide de Andrade ◽  
Tainá Caroline Lucena dos Santos ◽  
Mariana Brentini Santiago ◽  
Antônio Eduardo Miller Crotti ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Essential Oils ◽  
Peritoneal Macrophages ◽  
Culture Collection ◽  
Cytotoxic Activities ◽  
Therapeutic Effects ◽  
Herbaceous Plant ◽  
Microdilution Method ◽  
Ic50 Values

Interest in researches into medicinal plants and therapeutic effects of essential oils (EOs) on humans has increased over the last few years. Eremanthus erythropappus, known as candeia, is a Brazilian aromatic herbaceous plant whose α-bisabolol-rich oil has been used in several cosmetic preparations. This paper reports in vitro anticaries, antimycobacterial, antileishmanial and cytotoxic activities of EOs from E. erythropappus leaves (EL-EO) and stalks (ES-EO), besides α-bisabolol, their main sesquiterpene. EL-EO and ES-EO were extracted by hydrodistillation and analyzed by GC-FID and GC-MS. α-Bisabolol, cis-α-bisabolene and β-bisabolene were identified as their major constituents. Antibacterial activity of EOs was evaluated against eight standard strains of pathogens from the American Type Culture Collection (ATCC) by determining minimum inhibitory concentrations (MICs) with the use of the microdilution method. Antibacterial activity was evaluated against Streptococcus mutans, S. mitis, S. sanguinis, S. sobrinus, S. salivarius, Mycobacterium tuberculosis, M. avium and M. kansasii. EL-EO, ES-EO and α-bisabolol exhibited high leishmanicidal activity against promastigote forms of Leishmania amazonensis; IC50 values were 9.22 µg/mL, 6.00 µg/mL and 3.12 µg/mL, respectively. The 50% cytotoxic concentrations (CC50) of EL-EO, ES-EO and α-bisabolol against mouse peritoneal macrophages were 24.65 µg/mL, 8.87 µg/mL and 1021.00 µg/mL, respectively. These results suggest that EOs from E. erythropappus seem to be very promising for the development of new bactericidal and leishmanicidal agents.

scholarly journals Different Microfluidic Environments for In Vitro Testing of Lipid Nanoparticles against Osteosarcoma

2021 ◽  
Vol 8 (6) ◽  
pp. 77
Author(s):  
Oihane Mitxelena-Iribarren ◽  
Sara Lizarbe-Sancha ◽  
Jay Campisi ◽  
Sergio Arana ◽  
Maite Mujika
Keyword(s):  
Target Therapy ◽  
Treatment Options ◽  
Lipid Nanoparticles ◽  
Cell Number ◽  
Current Treatment ◽  
Drug Dose ◽  
Free Drug ◽  
Tumor Treatment ◽  
Equal Dose

The use of lipid nanoparticles as biodegradable shells for controlled drug delivery shows promise as a more effective and targeted tumor treatment than traditional treatment methods. Although the combination of target therapy with nanotechnology created new hope for cancer treatment, methodological issues during in vitro validation of nanovehicles slowed their application. In the current work, the effect of methotrexate (MTX) encapsulated in different matrices was evaluated in a dynamic microfluidic platform. Effects on the viability of osteosarcoma cells in the presence of recirculation of cell media, free MTX and two types of blank and drug-containing nanoparticles were successfully assessed in different tumor-mimicking microenvironments. Encapsulated MTX was more effective than the equal dose free drug treatment, as cell death significantly increased under the recirculation of both types of drug-loaded nanoparticles in all concentrations. In fact, MTX-nanoparticles reduced cell population 50 times more than the free drug when 150-µM drug dose was recirculated. Moreover, when compared to the equivalent free drug dose recirculation, cell number was reduced 60 and 100 points more under recirculation of each nanoparticle with a 15-µM drug concentration. Thus, the results obtained with the microfluidic model present MTX-lipid nanoparticles as a promising and more effective therapy for pediatric osteosarcoma treatment than current treatment options.

scholarly journals Identification of inhibitors of SARS-CoV-2 3CL-Pro enzymatic activity using a small molecule in-vitro repurposing screen

2020 ◽  
Author(s):  
Maria Kuzikov ◽  
Elisa Costanzi ◽  
Jeanette Reinshagen ◽  
Francesca Esposito ◽  
Laura Vangeel ◽  
...  
Keyword(s):  
Enzymatic Activity ◽  
Small Molecules ◽  
Drug Target ◽  
Treatment Options ◽  
Cleavage Sites ◽  
X Ray ◽  
Binding Characteristics ◽  
Main Protease ◽  
Ic50 Values

Compound repurposing is an important strategy for the identification of effective treatment options against SARS-CoV-2 infection and COVID-19 disease. In this regard, SARS-CoV-2 main protease (3CL-Pro), also termed M-Pro, is an attractive drug target as it plays a central role in viral replication by processing the viral polyproteins pp1a and pp1ab at multiple distinct cleavage sites. We here report the results of a repurposing program involving 8.7 K compounds containing marketed drugs, clinical and preclinical candidates, and small molecules regarded as safe in humans. We confirmed previously reported inhibitors of 3CL-Pro, and have identified 62 additional compounds with IC50 values below 1 uM and profiled their selectivity towards Chymotrypsin and 3CL-Pro from the MERS virus. A subset of 8 inhibitors showed anti-cytopathic effect in a Vero-E6 cell line and the compounds thioguanosine and MG-132 were analysed for their predicted binding characteristics to SARS-CoV-2 3CL-Pro. The X-ray crystal structure of the complex of myricetin and SARS-Cov-2 3CL-Pro was solved at a resolution of 1.77 Angs., showing that myricetin is covalently bound to the catalytic Cys145 and therefore inhibiting its enzymatic activity.

Mesenchymal stem cell-derived extracellular vesicles in the failing heart: past, present, and future

2021 ◽  
Author(s):  
Catherine Karbasiafshar ◽  
Frank W. Sellke ◽  
M. Ruhul Abid
Keyword(s):  
Stem Cell ◽  
Extracellular Vesicles ◽  
Treatment Options ◽  
Current Treatment ◽  
Lifestyle Changes ◽  
Challenges And Opportunities ◽  
Artery Disease ◽  
New Treatment

Cardiovascular disease (CVD) is the leading cause of death globally. Current treatment options include lifestyle changes, medication, and surgical intervention. However, many patients are unsuitable candidates for surgeries due to comorbidities, diffuse coronary artery disease or advanced stages of heart failure. The search for new treatment options has recently transitioned from cell-based therapies to stem-cell derived extracellular vesicles (EVs). A number of challenges remain in the EV field, including the effect of comorbidities, characterization, and delivery, However, recent revolutionary developments and insight into the potential of 'personalizing' EV contents by bioengineering methods to alter specific signaling pathways in the ischemic myocardium hold promise. Here, we discuss the past limitations of cell-based therapies, and recent EV studies involving in vivo, in vitro, and omics, and future challenges and opportunities in EV-based treatments in CVD.

Nitric Oxide Induction in Peritoneal Macrophages by a 1,2,3-Triazole Derivative Improves Its Efficacy upon Leishmania amazonensis In Vitro Infection

2021 ◽  
Author(s):  
Fernando Almeida-Souza ◽  
Verônica Diniz da Silva ◽  
Noemi Nosomi Taniwaki ◽  
Daiana de Jesus Hardoim ◽  
Ailésio Rocha Mendonça Filho ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Peritoneal Macrophages ◽  
Leishmania Amazonensis ◽  
Triazole Derivative

scholarly journals Potential Application of Prunus armeniaca L. and P. domestica L. Leaf Essential Oils as Antioxidant and of Cholinesterases Inhibitors

Antioxidants ◽  
2018 ◽  
Vol 8 (1) ◽  
pp. 2 ◽  
Author(s):  
Marco Bonesi ◽  
Maria Tenuta ◽  
Monica Loizzo ◽  
Vincenzo Sicari ◽  
Rosa Tundis
Keyword(s):  
Gas Chromatography ◽  
Essential Oils ◽  
Antioxidant Properties ◽  
Positive Control ◽  
Prunus Armeniaca ◽  
Gas Chromatography Mass Spectrometry ◽  
Flame Ionization ◽  
Ic50 Values ◽  
Comprehensive Comparison

The aim of this work is to investigate the in vitro acetylcholinesterase (AChE) and butyrycholinesterase (BChE) inhibitory activities of essential oils obtained by hydrodistillation from the leaves of Prunus armeniaca and P. domestica in relation to their composition, analysed by Gas Chromatography–Flame Ionization Detector (GC-FID) and Gas Chromatography-Mass Spectrometry (GC-MS) analyses, at different times. Moreover, considering the role of free radicals in the progression of neurodegenerative disorders, the antioxidant properties of essential oils were investigated by using, 2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and β-carotene bleaching tests. The relative antioxidant capacity index (RACI) was used to achieve more comprehensive comparison between analysed antioxidant effects of essential oils. P. armeniaca oils were more active than P. domestica oils against AChE. Against BChE, the most active was the essential oil from P. domestica leaves collected in August with an IC50 value of 95.80 μg/mL. This oil exerted the highest inhibitory activity of lipid peroxidation with IC50 values of 11.15 and 11.39 μg/mL after 30 and 60 min of incubation, respectively. All samples demonstrated a remarkable ABTS radicals scavenging activity, with IC50 values in the range 0.45–0.57 μg/mL in comparison to the positive control, ascorbic acid.

scholarly journals Essential Oils as a Potential Treatment Option for Pediculosis

Planta Medica ◽  
2020 ◽  
Vol 86 (09) ◽  
pp. 619-630 ◽  
Author(s):  
Kerdalidec Candy ◽  
Mohammad Akhoundi ◽  
Valérie Andriantsoanirina ◽  
Rémy Durand ◽  
Christiane Bruel ◽  
...  
Keyword(s):  
Essential Oils ◽  
Head Louse ◽  
Treatment Options ◽  
Residual Activity ◽  
Environmental Toxicity ◽  
Pediculus Humanus ◽  
Synthetic Chemicals ◽  
Major Factors ◽  
Ectoparasite Infestation

AbstractPediculosis is a prevalent ectoparasite infestation caused by lice. The head louse (Pediculus humanus capitis) and body louse (Pediculus humanus humanus) are obligatory parasites whose only known hosts are humans. Pediculosis is probably the most common ectoparasitic infestation, affecting up to 80% of the population in several countries, and particularly prevalent in the infant population worldwide. Several treatment options, including shampoos and creams containing insecticides, have been introduced for the treatment of pediculosis. Recently, the use of synthetic chemicals to control human lice has raised concerns pertaining to human health and the environment. Therefore, increasing efforts have been undertaken to develop effective pediculicides with low environmental toxicity and minimal environmental residual activity. In this study, we focus on the essential oils derived from 22 plant genera, their constituents, and the major factors that play important roles in the effectiveness of these oils in the treatment of pediculosis. Furthermore, we discuss the advantages and limitations of the mentioned essential oils, and ultimately suggest those demonstrating the most effective in vitro pediculicidal activities. The genera such as Aloysia, Cinnamomum, Eucalyptus, Eugenia, Lavandula, Melaleuca, Mentha, Myrcianthes, Origanum, Pimpinella, and Thymus appear to be more efficient against lice. These genera are rich in anethole, 1,8-cineole, cinnamaldehyde, p-cymene, eugenol, linalool, limonene, pulegone, terpinen-4-ol, and thymol compounds.

scholarly journals Naegleria fowleri: Pathogenesis, Diagnosis, and Treatment Options

2015 ◽  
Vol 59 (11) ◽  
pp. 6677-6681 ◽  
Author(s):  
Eddie Grace ◽  
Scott Asbill ◽  
Kris Virga
Keyword(s):  
Case Reports ◽  
Treatment Options ◽  
Clinical Manifestations ◽  
Naegleria Fowleri ◽  
Content Type ◽  
High Profile ◽  
Free Living Amoeba ◽  
Nægleria Fowleri ◽  
Amoebic Meningoencephalitis

ABSTRACTNaegleria fowlerihas generated tremendous media attention over the last 5 years due to several high-profile cases. Several of these cases were followed very closely by the general public.N. fowleriis a eukaryotic, free-living amoeba belonging to the phylum Percolozoa.Naegleriaamoebae are ubiquitous in the environment, being found in soil and bodies of freshwater, and feed on bacteria found in those locations. WhileN. fowleriinfection appears to be quite rare compared to other diseases, the clinical manifestations of primary amoebic meningoencephalitis are devastating and nearly always fatal. Due to the rarity ofN. fowleriinfections in humans, there are no clinical trials to date that assess the efficacy of one treatment regimen over another. Most of the information regarding medication efficacy is based on either case reports orin vitrostudies. This review will discuss the pathogenesis, diagnosis, pharmacotherapy, and prevention ofN. fowleriinfections in humans, including a brief review of all survivor cases in North America.

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