scholarly journals Chemistry and Leishmanicidal Activity of the Essential Oil from Artemisia absinthium from Cuba

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901 ◽  
Author(s):  
Lianet Monzote ◽  
Abel Piñón ◽  
Ramón Scull ◽  
William N. Setzer

Historically, natural products have been a rich source of lead molecules in drug discovery. In particular, products to treat infectious diseases have been developed and several reports about potentialities of essential oils (EO) against Leishmania could be found. In this study, we report the chemical characterization, anti-leishmanial effects and cytotoxicity of the EO from Artemisia absinthium L. Chemical analysis revealed the EO to be composed of 18 compounds, 11 of which were identified, accounting for 64.1% of the composition. The main component of the EO was trans-sabinyl acetate, which made up 36.7%. In vitro anti-leishmanial screening showed that the A. absinthium EO inhibited the growth of promastigotes (14.4 ± 3.6 μg/mL) and amastigotes (13.4 ± 2.4 μg/mL) of L. amazonensis; while cytotoxicity evaluation caused 6 fold higher values than those for the parasites. In a model of experimental cutaneous leishmaniasis in BALB/c mice, five doses of EO at 30 mg/kg by intralesional route demonstrated control of lesion size and parasite burden ( p< 0.05) compared with animals treated with glucantime and untreated mice. In conclusion, in vitro and in vivo results showed the potential of EO from A. absinthium as a promising source for lead or active compounds against Leishmania, which could be explored.

2020 ◽  
pp. 1379-1384
Author(s):  
Alex Rodrigues Silva Caetano ◽  
Sara Maria Chalfoun ◽  
Mario Lúcio Vilela Resende ◽  
Caroline Lima Angélico ◽  
Wilder Douglas Santiago ◽  
...  

Essential oils, also known as volatile oils, are substances produced through the secondary metabolism of plants. In this study, we determined the chemical composition and the in vitro and in vivo antifungal activity of the essential oils from four species of Eucalyptus, Eucalyptus citriodora, Eucalyptus camaldulensis, Eucalyptus grandis and Eucalyptus microcorys, against the Hemileia vastatrix fungus. The essential oils from these four species of Eucalyptus were extracted from their leaves by the hydrodistillation technique using a modified Clevenger apparatus. The chemical characterization was performed by gas chromatography coupled with a mass spectrometer detector and by gas chromatography using a flame ionization detector. The antifungal activities of the essential oils against H. vastatrix were studied by evaluating the percentage of spore germination using the microdilution test for in vitro assays. The curative and preventive effects were evaluated in in vivo tests. The principal constituents of the essential oil from E. citriodora were citronellal, citronellol and isopulegol, while E. camaldulensis produced 1,8-cineole, α-terpineol and α-pinene. 1,8-cineole, α-pinene and α-terpineol were obtained from E. grandis and 1,8-cineole, α-pinene and trans-pinocarveol were the principal components in the essential oil of E. microcorys. In vitro and in vivo antifungal activities against the fungus under study were observed for most of the essential oils, except the essential oil from E. microcorys, for which no preventive antifungal activity was observed. Only the curing of infection by the H. vastatrix fungus was observed with this oil.


2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Manuel Enrique Ávila-Blanco ◽  
Martín Gerardo Rodríguez ◽  
José Luis Moreno Duque ◽  
Martin Muñoz-Ortega ◽  
Javier Ventura-Juárez

Amebiasis is a parasitic disease that extends worldwide and is a public health problem in developing countries. Metronidazole is the drug recommended in the treatment of amebiasis, but its contralateral effects and lack of continuity of treatment induce low efficiency, coupled with the appearance of resistant amoebic strains. Therefore, the search of new compounds with amoebicidal activity is urgent and important. In this study, we evaluated the in vitro and in vivo antiamoebic activity of the essential oilDysphania ambrosioides(L.) Mosyakin & Clemants. It exhibited an IC50= 0.7 mg/mL against trophozoites. The oral administration of essential oil (8 mg/kg and 80 mg/kg) to hamster infected withEntamoeba histolyticareverted the infection. Ascaridole was identified as the main component of essential oil ofD. ambrosioides. The identification of amoebicidal activity of Ascaridole gives support to the traditional use. Further studies with Ascaridole will be carried out to understand the mechanism involved.


Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1394 ◽  
Author(s):  
Pablo Bilbao-Ramos ◽  
Dolores R. Serrano ◽  
Helga Karina Ruiz Saldaña ◽  
Juan J. Torrado ◽  
Francisco Bolás-Fernández ◽  
...  

Leishmaniasis affects around 12 million people worldwide and is estimated to cause the ninth-largest disease burden. There are three main forms of the disease, visceral (VL), cutaneous (CL), and mucocutaneous (MCL), leading to more than one million new cases every year and several thousand deaths. Current treatments based on chemically synthesized molecules are far from ideal. In this study, we have tested the in vitro and in vivo efficacy of ursolic acid (UA), a multifunctional triterpenoid with well-known antitumoral, antioxidant, and antimicrobial effects on different Leishmania strains. The in vitro antileishmanial activity against the intracellular forms was six and three-fold higher compared to extracellular forms of L. amazonensis and L. infantum, respectively. UA also showed to be a potent antileishmanial drug against both VL and CL manifestations of the disease in experimental models. UA parenterally administered at 5 mg/kg for seven days significantly reduced the parasite burden in liver and spleen not only in murine acute infection but also in a chronic-infection model against L. infantum. In addition, UA ointment (0.2%) topically administered for four weeks diminished (50%) lesion size progression in a chronic infection model of CL caused by L. amazonensis, which was much greater than the effect of UA formulated as an O/W emulsion. UA played a key role in the immunological response modulating the Th1 response. The exposure of Leishmania-infected macrophages to UA led to a significant different production in the cytokine levels depending on the Leishmania strain causing the infection. In conclusion, UA can be a promising therapy against both CL and VL.


2013 ◽  
Vol 62 (7) ◽  
pp. 1001-1010 ◽  
Author(s):  
Vinícius Pinto Costa Rocha ◽  
Fabiana Regina Nonato ◽  
Elisalva Teixeira Guimarães ◽  
Luiz Antônio Rodrigues de Freitas ◽  
Milena Botelho Pereira Soares

The currently used treatments for leishmaniasis, a neglected parasitic disease, are associated with several side effects, high cost and resistance of the Leishmania parasites. Here we evaluated in vitro and in vivo the antileishmanial activity of five antimalarial drugs against Leishmania amazonensis. Mefloquine was effective against promastigotes in axenic cultures and showed an IC50 (concentration giving half-maximal inhibition) value of 8.4±0.7 µM. In addition, mefloquine, chloroquine and hydroxychloroquine were active against intracellular amastigotes in macrophage-infected cultures, presenting IC50 values of 1.56±0.19 µM, 0.78±0.08 µM and 0.67±0.12 µM, respectively. The ultrastructural analysis of chloroquine- or mefloquine-treated amastigotes showed an accumulation of multivesicular bodies in the cytoplasm of the parasite, suggesting endocytic pathway impairment, in addition to the formation of myelin-like figures and enlargement of the Golgi cisternae. CBA mice were infected with L. amazonensis in the ear dermis, and treated by oral and/or topical routes with chloroquine and mefloquine. Treatment of L. amazonensis-infected mice with chloroquine by the oral route reduced lesion size, which was associated with a decrease in the number of parasites in the ear, as well as the parasite burden in the draining lymph nodes. In contrast, mefloquine administration by both routes decreased the lesion size in infected mice without causing a reduction in parasite burden. Our results revealed a promising antileishmanial effect of chloroquine and suggest its use in cutaneous leishmaniasis treatment.


2021 ◽  
Vol 31 (2) ◽  
Author(s):  
Gholamrezaei Mostafa ◽  
Jalallou Nahid ◽  
Seyyedtabaei Seyyed javad ◽  
Dadashi Alireza ◽  
Salimi Sabour Ebrahim

BACKGROUND፡ Cutaneous leishmaniasis is considered one of the major neglected tropical diseases. Drug resistance, limitary efficacy, and severe side effects remain a challenge for treatment. Foeniculum vulgare is known as a medicinal plant belonging to the Apiaceae, and anti-microbial properties of this plant have already been confirmed.METHOD: The F.vulgare sterile aqueous and alcoholic extracts were prepared. In vitro has used RAW 264.7 cell line and L. major parasite (MRHO/IR/75/ER). Cytotoxicity assay on macrophages (CC50), cytotoxicity assay on promastigotes (IC50), and cytotoxicity assay on infected macrophages (EC50) were accomplished with both extracts by MTT and light microscopy methods. Four in vivo were allocated in four groups and five BALB/c mice each group. Stationary phase promastigotes were inoculated into the base of mice tails subcutaneously (SC).Measurement of the body weight, lesion size, parasite burden of the lesion, and spleen after 4 weeks for evaluation effects of the alcoholic extract on CL was done.RESULTS: The results of in vitro revealed that the optimal concentrations of both extracts reducing the promastigotes and amastigotes growth. Alcoholic extract no harmful side effects for the host macrophages, while were indicated has a potent action against L. major. In vivo results after 4 weeks did not show any variation in lesion size and body weight. Also, lesion size and spleen parasite burden decreased in comparison to no treatment group.CONCLUSION: The alcoholic extract could be a new alternative treatment for cutaneous leishmaniasis. However this extract needs more investigation for novel herbal drugs against CL. 


2021 ◽  
Vol 14 (3) ◽  
Author(s):  
Fatemeh Ghaffarifar ◽  
Soheila Molaei ◽  
Zuhair Mohammad Hassan ◽  
Mohammad Saaid Dayer ◽  
Abdolhossein Dalimi ◽  
...  

Background: The adverse effects and increased resistance of drugs necessities the discovery of novel combination therapy. Objectives: This study aimed to examine the effects of Artemisinin plus glucantime or shark cartilage extract on the Iranian strain of Leishmania major (MRHO/IR/75/ER) in vitro and in vivo. Methods: In in vitro experiments, the effects of drugs and their combination in different concentrations (3.12 - 400 µg/mL) on the promastigotes, amastigotes, and un-infected macrophage cells were evaluated. In in vivo experiments, infected BALB/c mice were used as a cutaneous leishmaniasis model to evaluate the effects of the drugs and their combinations with different routes of administrations (namely Artemisinin: oral, ointment, and intraperitoneal; glucantime: intraperitoneal, intramuscular, intralesional, and subcutaneous; shark cartilage extract: oral) on parasite burden, lesion size, and immune system modulation. Results: The results revealed that Artemisinin and glucantime in combination with shark cartilage extract had greater effects on promastigotes than either Artemisinin or glucantime (P < 0.05), and that the combinations also had high cytotoxic effects on promastigotes and uninfected macrophages (P = 0.001). These combinations had more inhibitory effects on amastigotes and infected macrophages than promastigotes. The lesion sizes and parasite burden in the spleen decreased against the combinations of the drugs in different administrations. It was also noticed that the best combination administration route of Artemisinin and glucantime, as strong inducers of INF-γ and Th1 immune response, were ointment and IM, respectively (P < 0.05). Conclusions: The findings indicate that Artemisinin- glucantime or Artemisinin- Shark cartilage combinations are effective inhibitors of L. major. However, further clinical trials are recommended to evaluate the effects of these combinations in human subjects.


Medicines ◽  
2017 ◽  
Vol 4 (2) ◽  
pp. 38 ◽  
Author(s):  
Beatriz Tamargo ◽  
Lianet Monzote ◽  
Abel Piñón ◽  
Laura Machín ◽  
Marley García ◽  
...  

2017 ◽  
Vol 94 ◽  
pp. 292-306 ◽  
Author(s):  
Karuppusamy Arunachalam ◽  
Sikiru Olaitan Balogun ◽  
Eduarda Pavan ◽  
Guilherme Vieira Botelho de Almeida ◽  
Ruberlei Godinho de Oliveira ◽  
...  

Medicina ◽  
2019 ◽  
Vol 55 (5) ◽  
pp. 194 ◽  
Author(s):  
Maria Rayane Correia de Oliveira ◽  
Luiz Marivando Barros ◽  
Antônia Eliene Duarte ◽  
Maria Gabriely de Lima Silva ◽  
Bruno Anderson Fernandes da Silva ◽  
...  

Background and objectives: Natural products such as essential oils with antioxidant potential can reduce the level of oxidative stress and prevent the oxidation of biomolecules. In the present study, we investigated the antioxidant potential of Lantana montevidensis leaf essential oil (EOLM) in chemical and biological models using Drosophila melanogaster. Materials and methods: in addition, the chemical components of the oil were identified and quantified by gas chromatography coupled to mass spectrometry (GC-MS), and the percentage compositions were obtained from electronic integration measurements using flame ionization detection (FID). Results: our results demonstrated that EOLM is rich in terpenes with Germacrene-D (31.27%) and β-caryophyllene (28.15%) as the major components. EOLM (0.12–0.48 g/mL) was ineffective in scavenging DPPH radical, and chelating Fe(II), but showed reducing activity at 0.24 g/mL and 0.48 g/mL. In in vivo studies, exposure of D. melanogaster to EOLM (0.12–0.48 g/mL) for 5 h resulted in 10% mortality; no change in oxidative stress parameters such as total thiol, non-protein thiol, and malondialdehyde contents, in comparison to control (p > 0.05). Conclusions: taken together, our results indicate EOLM may not be toxic at the concentrations tested, and thus may not be suitable for the development of new botanical insecticides, such as fumigants or spray-type control agents against Drosophila melanogaster.


Author(s):  
Mostafa GHOLAMREZAEI ◽  
Soheila ROUHANI ◽  
Mehdi MOHEBALI ◽  
Samira MOHAMMADI-YEGANEH ◽  
Mostafa HAJI MOLLA HOSEINI ◽  
...  

Background: We aimed to investigate the effect of miR-15a mimic and inhibitor of miR-155 expression on apoptosis induction in macrophages infected with Iranian strain of Leishmania major in-vitro and in-vivo. Methods: RAW 264.7 cells were infected with L. major promastigotes (MRHO/IR/75/ER), and then were treated with miRNAs. For in-vivo experiment, BALB/c mice were inoculated with L. major promastigotes, and then they were treated with miRNAs. For evaluation of miRNA therapeutic effect, in-vitro and in-vivo studies were performed using quantitative Real-time PCR, Flow cytometry, lesion size measurement, and Limiting Dilution Assay (LDA). This study was performed in Shahid Beheshti University of Medical Sciences in 2019. Results: In-vitro results of flow cytometry showed that using miR-15a mimic, miR-155 inhibitor or both of them increased apoptosis of macrophages. In in-vivo, size of lesion increased during experiment in control groups (P<0.05) while application of both miR-155 inhibitor and miR-15a mimic inhibited the increase in the size of lesions within 6 wk of experiment (P=0.85). LDA results showed that microRNA therapy could significantly decrease parasite load in mimic or inhibitor receiving groups compared to the control group (P<0.05). Conclusion: miR-155 inhibitor and miR-15a mimic in L. major infected macrophages can induce apoptosis and reduce parasite burden. Therefore, miRNA-based therapy can be proposed as new treatment for cutaneous leishmaniasis.


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