scholarly journals In vitro antileishmanial activity of Anacardium othonianum and isolated compounds against Leishmania amazonensis

2021 ◽  
Vol 5 (1) ◽  
pp. 44
Author(s):  
Tavane Aparecida Alvarenga ◽  
Osvaine Júnior Alvarenga Alves ◽  
Mariana Cintra Pagotti ◽  
Wilson Roberto Cunha ◽  
Márcio Luís Andrade e Silva ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Anacardic Acid ◽  
Array Detector ◽  
Preparative Hplc ◽  
Moderate Activity ◽  
Phytochemical Study ◽  
Phenol Derivatives

This study analyzes the antileishmanial activity of the crude ethanol extract, fractions, and isolated compounds of A. othonianum nuts. Antileishmanial activity was evaluated against Leishmania amazonensis promastigotes in vitro. The phytochemical study was performed by high-performance liquid chromatography-high-resolution mass spectrometry-diode array detector (HPLC-HRMS-DAD) and by preparative HPLC. HPLC-HRMS-DAD analysis of the bioactive extract confirmed the presence of ten alkyl phenol derivatives that had previously been isolated from A. occidentale. Bioassay-guided isolation afforded cardanol triene, cardanol diene, cardanol monoene, cardol triene, anacardic acid triene, anacardic acid diene, and anacardic acid monoene. Cardol triene gave an IC50 of 80.66 µM. The obtained data suggest that the evaluated extract, fractions, and cardol triene had moderate activity against L. amazonensis promastigotes. This is the first description of alkyl phenols in A. othonianum.

Design, Synthesis and Antileishmanial Activity of Naphthotriazolyl-4- Oxoquinolines

2018 ◽  
Vol 18 (17) ◽  
pp. 1454-1464 ◽  
Author(s):  
Vanessa G. Oliveira ◽  
Viviane dos Santos Faiões ◽  
Gabrieli B.R. Gonçalves ◽  
Miriam F.O. Lima ◽  
Fernanda C.S. Boechat ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Cycloaddition Reaction ◽  
Public Health Problem ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Design Synthesis ◽  
Intracellular Amastigotes ◽  
Ic50 Values ◽  
Therapeutic Alternatives

Background: Leishmaniasis is a neglected public health problem caused by several protozoanspecies of the genus Leishmania. The therapeutic arsenal for treating leishmaniasis is quite limited, raising concerns about the occurrence of resistant strains. Furthermore, most of these drugs were developed more than 70 years ago and suffer from poor efficacy and safety and are not well adapted to the needs of patients. Therefore, research on novel natural or synthetic compounds with antiparasitic activity is urgently needed. In this paper, we evaluated the effect and the mechanism of action of naphthotriazolyl-4-oxoquinolines on promastigotes and intracellular amastigotes of Leishmania amazonensis. Materials and Methods: The naphthotriazolyl-4-oxoquinoline derivatives were obtained in good to moderate yields via the [3+2] cycloaddition reaction between 1,4-naphtoquinone and azido-4- oxoquinoline derivatives. HMPA at 100°C was established as the best solvent and temperature condition for this reaction. The structures of the compounds were confirmed by spectral analyses (infrared spectroscopy, one- and two-dimensional ¹H and ¹³C NMR spectroscopy, and high-resolution mass spectrometry). The compounds exhibited promising activities with IC50 values ranging from 0.7 to 2.0 µM against intracellular amastigotes of Leishmania amazonensis. The most selective compound was the Npentyl- substituted derivative, which showed a Selectivity Index (SI) of 8.6, making it less toxic than pentamidine (SI 4.5). Results: Our results demonstrated that all compounds, except the N-propyl-substituted derivative, induce ROS production by parasites early in the culture. As a proof of concept, we demonstrated that the most selective compound was able to interfere with sterol biosynthesis in L. amazonensis. Conclusion: The naphthotriazolyl-4-oxoquinoline derivatives were obtained in good to moderate yields. These conjugates have potent in vitro antileishmanial activity involving at least two different mechanisms of action, making them promising lead compounds for the development of new therapeutic alternatives for leishmaniasis.

scholarly journals Phytochemical Study and In Vitro Screening Focusing on the Anti-Aging Features of Various Plants of the Greek Flora

Antioxidants ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 1206
Author(s):  
Aimilia D. Sklirou ◽  
Maria T. Angelopoulou ◽  
Aikaterini Argyropoulou ◽  
Eliza Chaita ◽  
Vasiliki Ioanna Boka ◽  
...  
Keyword(s):  
Plant Species ◽  
High Performance ◽  
High Resolution Mass Spectrometry ◽  
Ultra Performance Liquid Chromatography ◽  
Skin Aging ◽  
Rosa Damascena ◽  
Phytochemical Study ◽  
Age Related

Skin health is heavily affected by ultraviolet irradiation from the sun. In addition, senile skin is characterized by major changes in the collagen, elastin and in the hyaluronan content. Natural products (NPs) have been shown to delay cellular senescence or in vivo aging by regulating age-related signaling pathways. Moreover, NPs are a preferable source of photoprotective agents and have been proven to be useful against the undesirable skin hyperpigmentation. Greek flora harvests great plant diversity with approximately 6000 plant species, as it has a wealth of NPs. Here, we report an extensive screening among hundreds of plant species. More than 440 plant species and subspecies were selected and evaluated. The extracts were screened for their antioxidant and anti-melanogenic properties, while the most promising were further subjected to various in vitro and cell-based assays related to skin aging. In parallel, their chemical profile was analyzed with High-Performance Thin-Layer Chromatography (HPTLC) and/or Ultra-Performance Liquid Chromatography High-Resolution Mass Spectrometry (UPLC-HRMS). A variety of extracts were identified that can be of great value for the cosmetic industry, since they combine antioxidant, photoprotective, anti-melanogenic and anti-aging properties. In particular, the methanolic extracts of Sideritis scardica and Rosa damascena could be worthy of further attention, since they showed interesting chemical profiles and promising properties against specific targets involved in skin aging.

Selective in vitro antileishmanial activity of Mimosa caesalpiniifolia stem barks and its main constituent betulinic acid against Leishmania amazonensis

2021 ◽  
Vol 140 ◽  
pp. 68-75
Author(s):  
Lucas Moreira Brito ◽  
Michel Muálem de Moraes Alves ◽  
Adriana Cunha Souza ◽  
Thaynara Parente de Carvalho ◽  
José Henrique Furtado Campos ◽  
...  
Keyword(s):  
Betulinic Acid ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Main Constituent

scholarly journals Anacardic acid derivatives from Brazilian propolis and their antibacterial activity

2008 ◽  
Vol 33 (3) ◽  
pp. 53-58 ◽  
Author(s):  
M. S. S. Silva ◽  
S. G. De Lima ◽  
E. H. Oliveira ◽  
J. A. D. Lopes ◽  
M. H. Chaves ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Dimethyl Disulfide ◽  
Ethanolic Extract ◽  
Anacardic Acid ◽  
Diffusion Method ◽  
Isolation And Identification ◽  
Phenol Derivatives ◽  
Shigella Spp ◽  
Brazilian Propolis

Propolis is a sticky, gummy, resinous substance collected by honeybees (Apis mellifera L.) from various plant sources, which has excellent medicinal properties. This paper describes the isolation and identification of triterpenoids and anacardic acid derivatives from Brazilian propolis and their antibacterial activity. Their structures were elucidated by ¹H and 13C NMR, including uni- and bidimensional techniques; in addition, comparisons were made with data from academic literature. These compounds were identified as: cardanols (1a + 1b), cardols (2a + 2b), monoene anacardic acid (3), a-amirine (4), b-amirine (5), cycloartenol (6), 24-methylene-cycloartenol (7) and lupeol (8). The determination of the position of the double bond after a reaction with Dimethyl disulfide (DMDS) is described for the phenol derivatives. The ethanolic extract was tested in vitro for antimicrobial activity by using the disc diffusion method and it showed significant results against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Shigella spp.

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 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 Phytochemical Study of Aqueous Extract of Ochna schweinfurthiana F. Hoffm Powder Bark and Evaluation of Their Anti-Inflammatory, Cytotoxic, and Genotoxic Properties

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Steve V. Djova ◽  
Maximilienne A. Nyegue ◽  
Angelique N. Messi ◽  
Alian D. Afagnigni ◽  
François-X. Etoa
Keyword(s):  
Bovine Serum Albumin ◽  
Serum Albumin ◽  
Salmonella Typhimurium ◽  
Aqueous Extract ◽  
Bovine Serum ◽  
Moderate Activity ◽  
Traditional Use ◽  
Phytochemical Study ◽  
Anti Inflammatory

Ochna schweinfurthiana has been used in traditional medicine to treat pain, inflammation, and arthritis. It is a rich source of complex dimers of flavonoids with potential use as templates for the development of therapeutic drugs. Hence, the aim of this study was to study the phytochemical content and evaluate the in vitro cytotoxic, genotoxic, and anti-inflammatory activities of the aqueous extract of Ochna schweinfurthiana bark (OSE). Phytochemical study was carried out according to LC-MS procedures, while isolation was carried out using thin layer and column chromatographies. Cytotoxicity was investigated by the mitochondrial viability [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) method while genotoxicity potential of the extract was ascertained using the Salmonella typhimurium test strains TA98 and TA100. The anti-inflammatory effect of OSE was evaluated by the in vitro inhibition of 15-lipooxygenase enzyme and bovine serum albumin denaturation (BSA) assays. The investigation of compounds extracted from OSE led to the identification and isolation of six known compounds, namely, hemerocallone (9), 6,7-dimethoxy-3’-4’-dimethoxyisoflavone (10), lithospermoside (13), amentoflavone (14), agathisflavone (15), and β-D-fructofuranosyl-α-D-glucopyranoside (17). In the anti-inflammatory assay, aqueous extracts of the bark showed selective inhibition of 15-lipooxygenase with IC50 value of 32.2±0.36  μg/mL and the result of the bovine serum albumin denaturation assay with IC50 value of 130± 5.78 μg/mL showed moderate activity. The toxicity assay indicated that OSE are noncytotoxic on Vero cell line with LC50 value of 50 mg/mL and nongenotoxic toward Salmonella typhimurium tester strain TA98 and TA100. Result from this study supports the traditional use of the selected medicinal plants in Cameroon for the treatment of inflammatory conditions. Noncytotoxicity and nongenotoxicity of OSE suggest that this plant is safe for use.

scholarly journals In Vitro Assessment of Organic and Residual Fractions of Nematicidal Culture Filtrates from Thirteen Tropical Trichoderma Strains and Metabolic Profiles of Most-Active

2022 ◽  
Vol 8 (1) ◽  
pp. 82
Author(s):  
Felicia Amalia Moo-Koh ◽  
Jairo Cristóbal-Alejo ◽  
María Fé Andrés ◽  
Jesús Martín ◽  
Fernando Reyes ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Mass Spectrometry Analysis ◽  
Array Detector ◽  
Diode Array Detector ◽  
Trichoderma Species ◽  
Potato Dextrose Broth ◽  
Spectrometry Analysis ◽  
Second Stage ◽  
In Vitro Assessment

The nematicidal properties of Trichoderma species have potential for developing safer biocontrol agents. In the present study, 13 native Trichoderma strains from T. citrinoviride, T. ghanense (2 strains), T. harzianum (4), T. koningiopsis, T. simmonsii, and T. virens (4) with nematicidal activity were selected and cultured in potato dextrose broth to obtain a culture filtrate (CF) for each. Each CF was partitioned with ethyl acetate to obtain organic (EA) and residual filtrate (RF) fractions, which were then tested on second-stage juveniles (J2s) of the nematodes Meloidogyne javanica and M. incognita in a microdilution assay. The most lethal strains were T. harzianum Th43-14, T. koningiopsis Th41-11, T. ghanense Th02-04, and T. virens Th32-09, which caused 51–100% mortality (%M) of J2s of both nematodes, mainly due to their RF fractions. Liquid chromatography–diode array detector-electrospray-high resolution mass spectrometry analysis of the most-active fractions revealed sesquiterpene and polyketide-like metabolites produced by the four active strains. These native Trichoderma strains have a high potential to develop safer natural products for the biocontrol of Meloidogyne species.

scholarly journals Development of Nanoemulsions to Enhance the Antileishmanial Activity ofCopaifera pauperaOleoresins

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Igor A. Rodrigues ◽  
Aline de S. Ramos ◽  
Deborah Q. Falcão ◽  
José Luiz P. Ferreira ◽  
Silvia L. Basso ◽  
...  
Keyword(s):  
Leishmania Infantum ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
First Report ◽  
Crude Extracts

Based on the ethnopharmacological evidences about the antileishmanial activity ofCopaiferaspp. oleoresins, the effects of crude extracts and fractions of oleoresin of two specimens fromCopaifera pauperawere evaluated onLeishmania amazonensisandLeishmania infantumstrains. The oleoresin rich inα-copaene (38.8%) exhibited the best activity againstL. amazonensis(IC50= 62.5 μg/mL) and againstL. infantum(IC50= 65.9 μg/mL). The sesquiterpeneα-copaene isolated was tested alone and exhibited high antileishmanial activityin vitrowith IC50values forL. amazonensisandL. infantumof 17.2 and 11.4 μg/mL, respectively. In order to increase antileishmanial activity, nanoemulsions containing copaiba oleoresin andα-copaene were developed and assayed againstL. amazonensisandL. infantumpromastigotes. The nanoemulsion containingα-copaene (NANOCOPAEN) showed the best activity against both species, with IC50of 2.5 and 2.2 μg/mL, respectively. This is the first report about the antileishmanial activity ofα-copaene.

In vitro antileishmanial activity of hydroalcoholic extract, fractions, and compounds isolated from leaves of Piper ovatum Vahl against Leishmania amazonensis

Planta Medica ◽  
2009 ◽  
Vol 75 (09) ◽  
Author(s):  
D Rodrigues Silva ◽  
CV Nakamura ◽  
BP Dias Filho ◽  
T Ueda-Nakamura ◽  
LE Ranieri Cortez ◽  
...  
Keyword(s):  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Hydroalcoholic Extract
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