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 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 Antileishmanial and Antischistosomal Activities of Anemonin Isolated from the Fresh Leaves of Ranunculus multifidus Forsk

Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7473
Author(s):  
Betelhem Sirak ◽  
Kaleab Asres ◽  
Asrat Hailu ◽  
Mthandazo Dube ◽  
Norbert Arnold ◽  
...  
Keyword(s):  
Neglected Tropical Diseases ◽  
Antileishmanial Activity ◽  
Clinical Isolates ◽  
Moderate Activity ◽  
Cytotoxicity Assays ◽  
Leishmania Aethiopica ◽  
Reduction Assay ◽  
Ic50 Values ◽  
Intestinal Worms

Leishmaniasis and schistosomiasis are neglected tropical diseases (NTDs) infecting the world’s poorest populations. Effectiveness of the current antileishmanial and antischistosomal therapies are significantly declining, which calls for an urgent need of new effective and safe drugs. In Ethiopia fresh leaves of Ranunculus multifidus Forsk. are traditionally used for the treatment of various ailments including leishmaniasis and eradication of intestinal worms. In the current study, anemonin isolated from the fresh leaves of R. multifidus was assessed for its in vitro antileishmanial and antischistosomal activities. Anemonin was isolated from the hydro-distilled extract of the leaves of R. multifidus. Antileishmanial activity was assessed on clinical isolates of the promastigote and amastigote forms of Leishmania aethiopica and L. donovani clinical isolates. Resazurin reduction assay was used to determine antipromastigote activity, while macrophages were employed for antiamastigote and cytotoxicity assays. Antischistosomal assays were performed against adult Schistosoma mansoni and newly transformed schistosomules (NTS). Anemonin displayed significant antileishmanial activity with IC50 values of 1.33 nM and 1.58 nM against promastigotes and 1.24 nM and 1.91 nM against amastigotes of L. aethiopica and L. donovani, respectively. It also showed moderate activity against adult S. mansoni and NTS (49% activity against adult S. mansoni at 10 µM and 41% activity against NTS at 1 µM). The results obtained in this investigation indicate that anemonin has the potential to be used as a template for designing novel antileishmanial and antischistosomal pharmacophores.

scholarly journals Discovery of 2-(1-(3-(4-Chloroxyphenyl)-3-oxo- propyl)pyrrolidine-3-yl)-1H-benzo[d]imidazole-4-carboxamide: A Potent Poly(ADP-ribose) Polymerase (PARP) Inhibitor for Treatment of Cancer

Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 1901 ◽  
Author(s):  
Rui Min ◽  
Weibin Wu ◽  
Mingzhong Wang ◽  
Lin Tang ◽  
Dawei Chen ◽  
...  
Keyword(s):  
Cellular Proliferation ◽  
Parp Inhibitor ◽  
Parp Inhibition ◽  
Anticancer Activities ◽  
Reference Drug ◽  
Structure Activity ◽  
Ic50 Values ◽  
Proliferation Assays ◽  
Parp 1

A series of benzimidazole carboxamide derivatives have been synthesized and characterized by 1H-NMR, 13C-NMR and HRMS. PARP inhibition assays and cellular proliferation assays have also been carried out. Compounds 5cj and 5cp exhibited potential anticancer activities with IC50 values of about 4 nM against both PARP-1 and PARP-2, similar to the reference drug veliparib. The two compounds also displayed slightly better in vitro cytotoxicities against MDA-MB-436 and CAPAN-1 cell lines than veliparib and olaparib, with values of 17.4 µM and 11.4 µM, 19.8 µM and 15.5 µM, respectively. The structure-activity relationship based on molecular docking was discussed as well.

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.

Antileishmanial activities of leaf latex and compound isolated from Aloe ghibensis Sebsebe & Friis

2020 ◽  
Vol 35 (1) ◽  
pp. 51-58
Author(s):  
Tamirat Tekassa ◽  
Yitagesu Tewabe ◽  
Daniel Bisrat ◽  
Asrat Hailu ◽  
Kaleab Asres
Keyword(s):  
Leishmania Donovani ◽  
Leishmania Species ◽  
2D Nmr ◽  
Antileishmanial Activity ◽  
Spectroscopic Techniques ◽  
Monocytic Cell ◽  
Monocytic Cell Line ◽  
Phytochemical Constituents ◽  
Antileishmanial Activities

Aloe ghibensis Sebsebe & Friis is traditionally used in Ethiopia for the treatment of various ailments including skin problem, wounds and malaria. Phytochemical constituents and antileshimanial properties of the leaf latex of A. ghibensis have not been reported. The objective of this study was, therefore, to determine the phytochemical constituents and in vitro antileishmanial activities of the leaf latex of A. ghibensis and its major compounds against two Leishmania species. Preparative TLC was used to isolate compounds from the leaf latex of A. ghibensis and spectroscopic techniques including 1D- and 2D-NMR as well as ESI-MS were employed to elucidate structures of the isolated compounds. In vitro antileishmanial activity was performed against promastigotes and axenically cultured amastigotes of Leishmania aethiopica and Leishmania donovani clinical isolates using Alamar Blue assay. Phytochemical investigation led to the isolation of two major anthrones, identified as aloin A/B and 7-hydroxyaloin A/B. Both the leaf latex of A. ghibensis and isolated compounds showed antileishmanial activity with IC50 values ranging from 1.6 ± 0.43 to 3.64 ± 0.09 µg/ml and 1.87 ± 0.21 to 3.72 ± 0.12 against promastigotes and axenically cultured amastigotes of L. aethopica and L. donovani, respectively. Moreover, the test substances were found to be less toxic (LC50 = 145 ± 0.72 to 156 ± 0.08 µg/ml) than amphotericin B (LC50 = 12.11 ± 0.51 µg/ml) towards human monocytic cell line (THP-1). The present study revealed that the latex and pure compounds possess genuine antileishmanial activity with high selectivity indices (SIs). Therefore, the isolated compounds can be used as a scaffold for the development of effective drugs for leishmaniasis.  

scholarly journals Efficacy of Synthetic Peptides RP-1 and AA-RP-1 against Leishmania SpeciesIn VitroandIn Vivo

2011 ◽  
Vol 56 (2) ◽  
pp. 658-665 ◽  
Author(s):  
Marie Crisel B. Erfe ◽  
Consuelo V. David ◽  
Cher Huang ◽  
Victoria Lu ◽  
Ana Claudia Maretti-Mira ◽  
...  
Keyword(s):  
Intravenous Administration ◽  
Synthetic Peptides ◽  
Antileishmanial Activity ◽  
Host Defense Peptides ◽  
Content Type ◽  
Causative Agents ◽  
Antileishmanial Activities ◽  
Conventional Antibiotics

ABSTRACTHost defense peptides are naturally occurring molecules that play essential roles in innate immunity to infection. Based on prior structure-function knowledge, we tested two synthetic peptides (RP-1 and AA-RP-1) modeled on the conserved, microbicidal α-helical domain of mammalian CXCL4 platelet kinocidins. These peptides were evaluated for efficacy againstLeishmaniaspecies, the causative agents of the group of diseases known as leishmaniasis.In vitroantileishmanial activity was assessed against three distinctLeishmaniastrains by measuring proliferation, metabolic activity and parasite viability after exposure to various concentrations of peptides. We demonstrate that micromolar concentrations of RP-1 and AA-RP-1 caused dose-dependent growth inhibition ofLeishmaniapromastigotes. This antileishmanial activity correlated with rapid membrane disruption, as well as with a loss of mitochondrial transmembrane potential. In addition, RP-1 and AA-RP-1 demonstrated distinct and significantin vivoantileishmanial activities in a mouse model of experimental visceral leishmaniasis after intravenous administration. These results establish efficacy of RP-1 lineage synthetic peptides againstLeishmaniaspeciesin vitroand after intravenous administrationin vivoand provide further validation of proof of concept for the development of these and related systemic anti-infective peptides targeting pathogens that are resistant to conventional antibiotics.

Screening of selected essential oils for their in vitro antileishmanial activity against Leishmania amazonensis

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
A Crotti ◽  
F Dos Santos ◽  
L Magalhães ◽  
K Wakabayashi ◽  
G Aguiar ◽  
...  
Keyword(s):  
Essential Oils ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity

scholarly journals Comparative Chemical, Cytotoxicity and Antileishmanial Properties of Essential Oils from Chenopodium ambrosioides

2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Lianet Monzote ◽  
Marcelina R. Nance ◽  
Marley García ◽  
Ramón Scull ◽  
William N. Setzer
Keyword(s):  
Essential Oil ◽  
Essential Oils ◽  
Chemical Characterization ◽  
In Vitro Cytotoxicity ◽  
Chenopodium Ambrosioides ◽  
Popular Medicine ◽  
Lead Compounds ◽  
Antileishmanial Activities ◽  
Treatment Alternatives

In countries where leishmaniasis is endemic, there are not very many treatment alternatives and most options have problems associated with their use. Plants and their natural products constitute good sources of interesting lead compounds that could be potentially active against Leishmania. Chenopodium ambrosioides is a plant that is widely used in popular medicine and its antiparasitic effects have been documented, including the antileishmanial potentialities of Chenopodium oil. The objective of this study was to determine the chemical composition, in-vitro cytotoxicity and antileishmanial activity of essential oils extracted from C. ambrosioides, which received different treatments prior to extraction. The chemical characterization by GC-MS of the three essential oil samples showed similar composition and the major components were α-terpinene (17.0-20.7%), p-cymene (20.2-21.1%) and ascaridole (30.5-47.1%). The essential oils exhibited similar antileishmanial activities against intracellular amastigote form, with IC50 values between 4.7 and 12.4 μg/mL. However, a lower cytotoxicity was displayed by the essential oil extracted from fresh green vegetable material, which was statistically different ( P < 0.05) from the other samples. This study demonstrated that the prior treatment of plant material did not interfere with the antiparasitic activity of essential oils from C. ambrosioides but did change their cytotoxicity, which should be taken into account in further studies.

scholarly journals Improvement of In Vitro and In Vivo Antileishmanial Activities of 2′,6′-Dihydroxy-4′-Methoxychalcone by Entrapment in Poly(d,l-Lactide) Nanoparticles

1999 ◽  
Vol 43 (7) ◽  
pp. 1776-1778 ◽  
Author(s):  
Eduardo Caio Torres-Santos ◽  
José M. Rodrigues ◽  
Davyson L. Moreira ◽  
Maria Auxiliadora C. Kaplan ◽  
Bartira Rossi-Bergmann
Keyword(s):  
Polymeric Nanoparticles ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Antileishmanial Activities ◽  
Piper Aduncum

ABSTRACT The inhibition of intracellular Leishmania amazonensisgrowth by 2′,6′-dihydroxy-4′-methoxychalcone (DMC) isolated fromPiper aduncum was further enhanced after encapsulation of DMC in polymeric nanoparticles. Encapsulated DMC also showed increased antileishmanial activity in infected BALB/c mice, as evidenced by significantly smaller lesions and fewer parasites in the lesions.

scholarly journals IN VITRO ANTILEISHMANIAL ACTIVITIES OF THREE MEDICINAL PLANTS: ARGEMONE MEXICANA, MURRAYA KOENIGII AND CINNAMOMUM TAMALA AGAINST MILTEFOSINE RESISTANT PROMASTIGOTES OF LEISHMANIA DONOVANI PARASITES

2021 ◽  
pp. 27-33
Author(s):  
SIRIN SALMA SULTANA
Keyword(s):  
Medicinal Plants ◽  
Leishmania Donovani ◽  
Neglected Tropical Diseases ◽  
Protein Biosynthesis ◽  
New Drugs ◽  
Murraya Koenigii ◽  
Argemone Mexicana ◽  
Cinnamomum Tamala ◽  
Antileishmanial Activities

Objective: Leishmaniasis is one of the neglected tropical diseases in terms of drug development and discovery. Non-responsiveness and resistance to the drug in Leishmania species need to develop new antileishmanial potentials; herbal medicines could be the alternative one. Methods: In the present study, semi-purified fractions were prepared from the traditionally used three medicinal plants of India: Argemone mexicana (aerial shoot), Murraya koenigii (stem), and Cinnamomum tamala (bark) by using multiple solvent systems (non-polar to polar, beginning with petroleum ether followed by n-hexane, benzene, and chloroform) and an effort was given to assess the leishmanicidal activities against Leishmania donovani miltefosine resistant HePC-R (Ld/MIL-30) promastigotes in vitro and the IC50 concentrations were estimated. Results: The study revealed that the semi-purified fractions of A. mexicana, M. koenigii, and C. tamala have effective antileishmanial activities and the 50% inhibitory concentrations (IC50) are 50 μg/ml, 98 μg/ml, and 200 μg/ml, respectively. At these (IC50) concentrations, these plant semi-purified fractions were found to interfere in lipid and protein biosynthesis, alter cell morphology, DNA content, mitochondrial membrane potential, generating ROS, and apoptosis in promastigotes. The semi-purified fractions were also found noticeably non-toxic towards host splenocytes. Conclusion: These results could suggest that A. mexicana, M. koenigii, and C. tamala could carry potential novel compounds for the development of new drugs against Leishmaniasis.

Sign in / Sign up

Export Citation Format

Share Document