scholarly journals Cytotoxicity andIn VitroAntileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Marcele Neves Rocha ◽  
Paula Monalisa Nogueira ◽  
Cynthia Demicheli ◽  
Ludmila Gonçalvez de Oliveira ◽  
Meiriane Mariano da Silva ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Chemical Modification ◽  
Hepg2 Cells ◽  
Antimicrobial Properties ◽  
Etiologic Agent ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Murine Macrophages ◽  
Wide Range

Leishmania amazonensisis the etiologic agent of the cutaneous and diffuse leishmaniasis often associated with drug resistance. Lapachol [2-hydroxy-3-(3′-methyl-2-butenyl)-1,4-naphthoquinone] displays a wide range of antimicrobial properties against many pathogens. In this study, using the classic microscopicin vitromodel, we have analyzed the effects of a series of lapachol and chlorides complexes with antimony (V), bismuth (V), and tin (IV) againstL. amazonensis. All seven compounds exhibited antileishmanial activity, but most of the antimony (V) and bismuth (V) complexes were toxic against human HepG2 cells and murine macrophages. The best IC50values (0.17±0.03 and 0.10±0.11 μg/mL) were observed for Tin (IV) complexes (3) [(Lp)(Ph3Sn)] and (6) (Ph3SnCl2), respectively. Their selective indexes (SIs) were 70.65 and 120.35 for HepG2 cells, respectively. However, while analyzing murine macrophages, the SI decreased. Those compounds were moderately toxic for HepG2 cells and toxic for murine macrophages, still underlying the need of chemical modification in this class of compounds.

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 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.

In Vitro Antitumor Efficacy of Puerarin Nanosuspension against Human HepG2 Cells

2015 ◽  
Vol 1083 ◽  
pp. 27-31 ◽  
Author(s):  
Wen Liang Lu ◽  
Hui Zhe Shi ◽  
Qun Zhou ◽  
Zhi Ping Wang ◽  
Sheng Xiong ◽  
...  
Keyword(s):  
Particle Size ◽  
Hepg2 Cells ◽  
Current Issue ◽  
Human Life ◽  
Pharmacological Properties ◽  
High Pressure Homogenization ◽  
Natural Remedy ◽  
Wide Range ◽  
A Current

Hepatocarcinoma, a malignant cancer, threaten human life badly. It is a current issue to seek the effective natural remedy from plant to treat cancer due to the resistance of the advanced hepatocarcinoma to chemotherapy. Puerarin (Pue), a major active ingredient in the traditional Chinese medicine Gegen, has a wide range of pharmacological properties and is considered to have anti-hepatocarcinoma effects. However its low oral bioavailability restricts its wide application. In this report, Pue-nanosuspension (Pue-NS) composed of Pue and poloxamer 188 was prepared by high pressure homogenization technique. The in vitro anti-hepatocarcinoma effects of Pue-NS relative to efficacy of bulk Pue were evaluated. The particle size and zeta potential of Pue-NS were 218.5 nm and −18.8 mV, respectively. MTT assay showed that Pue-NS effectively inhibited the proliferation of HepG2 cells, and the corresponding IC50 values of Pue-NS and bulk Pue were 3.39 and 5.73 μg/ml. These results suggest that the delivery of Pue-NS is a promising approach for treating tumors.

scholarly journals In-Vitro Evaluation of Biological Activity of New Series of 1, 3, 4-Oxadiazole Derivatives Against Bap Gene Expression in Acinetobacter bumanni Biofilm

2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Sedigheh Akbarnezhad Ghareh Lar ◽  
Nakisa Zarrabi Ahrabi ◽  
Yasin SarveAhrabi
Keyword(s):  
Biofilm Formation ◽  
Functional Group ◽  
Biological Activities ◽  
Antimicrobial Properties ◽  
Housekeeping Gene ◽  
Bacterial Biofilm ◽  
Wide Range ◽  
Oxadiazole Derivatives ◽  
The Impact

Background: Acinetobacter bumanni is one of the most common opportunistic pathogens in health centers that is resistant to many antibiotics due to biofilm production. 1, 3, 4-oxadiazoles have a wide range of biological activities. Objectives: The aim of this research was to examine the impact of new 1, 3, 4-oxadiazole derivatives on the expression of biofilm-associated surface protein (Bap), playing an important role in promoting the biofilm formation ability of A. baumannii strains. Methods: Derivatives of 1, 3, 4-oxadiazole were synthesized through a one-step synthesis. A. baumannii strains were identified and isolated in the laboratory. The antimicrobial properties of the synthesized materials against the isolated strains were investigated. DNA, RNA, and cDNA were extracted, and the relative expression of BAP gene in A. baumannii isolates was evaluated by real-time polymerase chain reaction. Results: The compound with methoxyphenyl functional group with MIC = 62.50 mg/mL had the best inhibitory performance among all derivatives. Also, the combination of 4i reduced the expression of the Bap gene by about 24 times, but it had no effect on the expression of the 16srRNA housekeeping gene. Conclusions: 1, 3, 4-oxadiazole derivatives, especially the methoxyphenyl functional group, act as an inhibitor of bacterial biofilm formation and have the potential to be used in the pharmaceutical and biological industries.

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

The prediction of the spectrum of biological activity and antimicrobial properties of diaminoazoles

2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Antimicrobial Properties ◽  
Biological Properties ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Wide Range ◽  
Alternative Drugs

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.

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 Anticancer Potential of Berberis lycium Royle Extracts against Human Hepatocarcinoma (HepG2) Cells

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Kiren Mustafa ◽  
Hassan Mohamed ◽  
Aabid Manzoor Shah ◽  
Shaoxuan Yu ◽  
Muhammad Akhlaq ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Hepg2 Cells ◽  
Apoptotic Cell ◽  
Cancer Cell Line ◽  
Ethanolic Extract ◽  
Health Concern ◽  
Mrna Levels ◽  
Dependent Manner ◽  
Wide Range

Human liver cancer has emerged as a serious health concern in the world, associated with poorly available therapies. The Berberis genus contains vital medicinal plants with miraculous healing properties and a wide range of bioactivities. In this study, different crude extracts of B. lycium Royle were prepared and screened against Human Hepatocarcinoma (HepG2) cell lines. The water/ethanolic extract of B. lycium Royle (BLE) exhibited significant antiproliferative activity against the HepG2 cancer cell line with an IC50 value of 47 μg/mL. The extract decreased the clonogenic potential of HepG2 cells in a dose-dependent manner. It induced apoptotic cell death in HepG2 cells that were confirmed by cytometric analysis and microscopic examination of cellular morphology through DAPI-stained cells. Biochemical evidence of apoptosis came from elevating the intracellular ROS level that was accompanied by the loss of mitochondrial membrane potential. The mechanism of apoptosis was further confirmed by gene expression analysis using RT-qPCR that revealed the decline in Bcl-2 independent of p53 mRNA and a rise in CDK1 while downregulating CDK5, CDK9, and CDK10 mRNA levels at 48 h of BLE treatment. The most active fraction was subjected to HPLC which indicated the presence of berberine (48 μg/mL) and benzoic acid (15.8 μg/mL) as major compounds in BLE and a trace amount of luteolin, rutin, and gallic acid. Our study highlighted the importance of the most active BLE extract as an excellent source of nutraceuticals against Human Hepatocarcinoma that can serve as an herbal natural cure against liver cancer.

scholarly journals In Vitro Activities of Iboga Alkaloid Congeners Coronaridine and 18-Methoxycoronaridine against Leishmania amazonensis

2002 ◽  
Vol 46 (7) ◽  
pp. 2111-2115 ◽  
Author(s):  
Jan Carlo Delorenzi ◽  
Leonardo Freire-de-Lima ◽  
Cerli R. Gattass ◽  
Deise de Andrade Costa ◽  
Liwen He ◽  
...  
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Causative Agent ◽  
New World ◽  
Cytokine Production ◽  
Indole Alkaloid ◽  
Stem Bark ◽  
Leishmania Amazonensis ◽  
Murine Macrophages

ABSTRACT In previous studies, we demonstrated the leishmanicide effect of coronaridine, a natural indole alkaloid isolated from stem bark of Peschiera australis (Delorenzi et al., Antimicrob. Agents Chemother. 45:1349-1354, 2001). In this study we show the leishmanicidal effect of the synthetic coronaridine and its racemic 18-methoxylated analog, 18-methoxycoronaridine. Both alkaloids revealed a potent leishmanicide effect against Leishmania amazonensis, a causative agent of cutaneous and diffuse cutaneous leishmaniasis in the New World. Despite their potent leishmanicide effect, both alkaloids were neither toxic to murine macrophages nor did they modulate their oxidative or cytokine production responses.

scholarly journals Inhibitory activity of stilbenes against filamentous fungi

2021 ◽  
Vol 10 (1) ◽  
Author(s):  
Luce Mattio ◽  
Giorgia Catinella ◽  
Marcello Iriti ◽  
Lisa Vallone
Keyword(s):  
Antifungal Activity ◽  
Filamentous Fungi ◽  
Antimicrobial Properties ◽  
Microbial Infection ◽  
Wide Range ◽  
Mycotoxigenic Fungi ◽  
Wild Strains ◽  
Diffusion Assay ◽  
Inflammatory Action

Stilbenoids (resveratrol and its derivatives) are secondary metabolites produced by plants as defence mechanism to microbial infection. These compounds are known for their anti-inflammatory action and health benefits in preventing a wide range of disorders (e.g. cancer and cardiovascular diseases). However, their antimicrobial properties are less investigated. A series of 8 stilbenoid compounds were synthesized and their antifungal activity against 19 wild strains of filamentous fungi and yeasts (isolated from the environment and food) was tested in vitro. Using an agar diffusion assay, compounds were tested at the concentration of 100 μg/ml on filamentous fungi and yeasts at 104 CFU/ml. The results showed that tested derivatives possess moderate antifungal activity: in particular, monomeric stilbenoids 3’-hydroxy-pterostilbene and piceatannol, and dimeric stilbenoids (±)-trans-δ-viniferin and pallidol were active against mycotoxigenic fungi.

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