Anti-Leishmania activity of extracts from Piper cabralanum C.DC. (Piperaceae)

2021 ◽  
Vol 76 (5-6) ◽  
pp. 229-241
Author(s):  
Layane Valéria Amorim ◽  
Davyson de Lima Moreira ◽  
Michel Muálem de Moraes Alves ◽  
Ygor Jessé Ramos ◽  
Enoque Pereira Costa Sobrinho ◽  
...  
Keyword(s):  
Cytotoxic Effect ◽  
Macrophage Activation ◽  
Inhibitory Concentration ◽  
Biological Properties ◽  
Activation Patterns ◽  
Etoac Extract ◽  
Etoac Fraction ◽  
Low Cytotoxicity ◽  
Macrophage Infectivity

Abstract Species of Piperaceae are known by biological properties, including antiparasitic such as leishmanicidal, antimalarial and in the treatment of schistosomiasis. The aim of this work was to evaluate the antileishmania activity, cytotoxic effect, and macrophage activation patterns of the methanol (MeOH), hexane (HEX), dichloromethane (DCM) and ethyl acetate (EtOAc) extract fractions from the leaves of Piper cabralanum C.DC. The MeOH, HEX and DCM fractions inhibited Leishmanina amazonensis promastigote-like forms growth with a half maximal inhibitory concentration (IC50) of 144.54, 59.92, and 64.87 μg/mL, respectively. The EtOAc fraction did not show any relevant activity. The half maximal cytotoxic concentration (CC50) for macrophages were determined as 370.70, 83.99, 113.68 and 607 μg/mL for the MeOH, HEX and DCM fractions, respectively. The macrophage infectivity was concentration-dependent, especially for HEX and DCM. MeOH, HEX and DCM fractions showed activity against L. amazonensis with low cytotoxicity to murine macrophages and lowering infectivity by the parasite. Our results provide support for in vivo studies related to a potential application of P. cabralanum extract and fractions as a promising natural resource in the treatment of leishmaniasis.

scholarly journals Comparison between Peritoneal Macrophage Activation by Bougainvillea xbuttiana Extract and LPS and/or Interleukins

2017 ◽  
Vol 2017 ◽  
pp. 1-11 ◽  
Author(s):  
Lluvia Arteaga Figueroa ◽  
Rodolfo Abarca-Vargas ◽  
Claudia García Alanis ◽  
Vera L. Petricevich
Keyword(s):  
Hydrogen Peroxide ◽  
Cytotoxic Effect ◽  
Macrophage Activation ◽  
Peritoneal Macrophages ◽  
Immunomodulatory Activity ◽  
Hydrogen Peroxide Production ◽  
Griess Reagent ◽  
Violet Crystal ◽  
Low Cytotoxicity

Activation of macrophages may be one of the possible approaches in modulating inflammation. We previously reported that Bougainvillea xbuttiana extract showed an immunomodulatory activity. Here we compare the activation of macrophages exposed to B. xbuttiana extract and compare it with the other treatments such as LPS, IL-4, and IL-10. The cytotoxic effect of extract on peritoneal macrophages was determined by the technique of violet crystal staining. To verify the activation of macrophages we used the tests of vacuolization, hydrogen peroxide production, and percentages of cellular expansion and phagocytosis. The levels of interleukins secreted by macrophages treated with the extract, LPS, and cytokines were determined by the biological assay for the determination of TNF levels and by ELISA for all other interleukins. NO levels were evaluated by colorimetric reactions using Griess reagent. Our results showed that B. xbuttiana extract induced (a) low cytotoxicity percentages, (b) increased vacuolization, hydrogen peroxide production and cell expansion and phagocytosis percentages, and (c) decreased production of TNF-α, IFN-γ, IL-1β, and IL-6 and potentiated production of IL-4, IL-10 and TGF-β. These results suggest that B. xbuttiana extract was able to activate the murine macrophages in a manner similar to those macrophages exposed to IL-4 and IL-10.

scholarly journals Antibacterial Profile in vitro and in vivo of New 1,4-Naphthoquinones Tethered to 1,2,3-1H-Triazoles against the Planktonic Growth of Streptococcus mutans

2022 ◽  
Author(s):  
Mônica Gomes ◽  
Eduardo Correia ◽  
Max Gomes ◽  
Claudio dos Santos ◽  
Caroline Barros ◽  
...  
Keyword(s):  
Streptococcus Mutans ◽  
Cytotoxic Effect ◽  
Inhibitory Concentration ◽  
Disc Diffusion ◽  
Diffusion Test ◽  
In Vivo Test ◽  
Slight Alteration ◽  
Antibacterial Evaluation

The cariogenic processes are mainly caused by the bacterium Streptococcus mutans (S. mutans) and consist of the demineralization of the tooth that occurs when the acid production overcomes the natural repair or if a problem occurs in the last one. In this work, we performed the synthesis of twenty-one 1,4-naphthoquinones tethered to 1,2,3-1H-triazoles (8a-8k and 9a-9j), antibacterial evaluation against the S. mutans in vitro and the acute toxicity of the better ones in vivo. We observed strong inhibition results in the disc diffusion test ranging, the halos of inhibitions, from 18.66 (± 0.57) to 29 (± 2.64) mm, and good values in the minimum inhibitory concentration (5 to 50 μg), for the compounds 9e, 9h, 9i and 9j. Furthermore, they do not have a cytotoxic effect at the concentrations tested. Besides that, in the in vivo test, they show some slight alteration in the histopathological analyses and the biochemistry. Thus, we found four potential candidates to become instruments for the treatment of cavities.

scholarly journals Production, purification, characterization, and biological properties of Rhodosporidium paludigenum polysaccharide

PLoS ONE ◽  
2021 ◽  
Vol 16 (1) ◽  
pp. e0246148
Author(s):  
Mengjian Liu ◽  
WenJu Zhang ◽  
Jun Yao ◽  
Junli Niu
Keyword(s):  
Pathogenic Bacteria ◽  
Inhibitory Concentration ◽  
Biological Properties ◽  
Molecular Weights ◽  
Fermentation Parameters ◽  
Main Components ◽  
Image Position ◽  
G Ratio

The yield of marine red yeast polysaccharide (MRYP) obtained from Rhodosporidium paludigenum was increased by optimizing fermentation conditions, and the pure polysaccharide was extracted by column chromatography. The molecular weight of pure MRYP and the ratio of mannose to glucose in components of MRYP were determined. Antioxidant and antibacterial abilities of MRYP were investigated in vitro and in vivo. The optimal fermentation parameters were as follows: Medium 4, pH = 6.72, temperature = 30.18°C, blades speed = 461.36 r/min; the optimized yield reached 4323.90 mg/L, which was 1.31 times the original yield. The sequence of factors that affected the MRYP yield was the blades speed>pH>temperature. The main components of MRYP were MYH-1 and MYH-2. The molecular weights of MYH-1 and MYH-2 were 246.92 kDa and 21.88 kDa, respectively; they accounted for 53.60% and 28.75% of total polysaccharide. In MYH-1 and MYH-2, the proportion of glucose and mannose accounted for 46.94%, 38.46%, and 67.10%, 7.17%, respectively. In vitro, the ability of scavenging DPPH•, •OH, and •O2− radical was 32.26%, 24.34%, and 22.09%; the minimum inhibitory concentration (MIC) of MRYP was 480 μg/mg. In vivo, MRYP improved the lambs’ body weight, antioxidant enzyme activity, and the number of probiotics, but it reduced the feed/gain (F/G) ratio and the number of pathogenic bacteria in 60-days-old lambs.

scholarly journals Comparison of the biocompatibility of calcium silicate-based materials to mineral trioxide aggregate: Systematic review

2018 ◽  
Vol 12 (02) ◽  
pp. 317-326 ◽  
Author(s):  
Natália Gomes de Oliveira ◽  
Pollyana Rodrigues de Souza Araújo ◽  
Marina Torreão da Silveira ◽  
Ana Paula Veras Sobral ◽  
Marianne de Vasconcelos Carvalho
Keyword(s):  
Systematic Review ◽  
Web Of Science ◽  
Mineral Trioxide Aggregate ◽  
Biological Properties ◽  
Exclusion Criteria ◽  
Pulp Inflammation ◽  
Prisma Statement ◽  
Low Cytotoxicity

ABSTRACTThe objective of this systematic review was to evaluate the biocompatibility and interaction of bioceramic materials with animal and human mesenchymal cells in vitro and in vivo and to compare them with mineral trioxide aggregate (MTA). Two independent researchers conducted PubMed/Medline, Web of Science, and Scopus searches to identify studies published in English, without restrictions on year of publication using the following keywords: “root canal sealer,” “root repair material,” “cytotoxicity,” and “bioceramics.” The articles were selected following the PRISMA statement. A total of 1486 titles were identified in the initial search. However, only 18 studies met the inclusion and exclusion criteria. The results showed that bioceramic materials have biological properties similar to those of MTA, including low cytotoxicity as well as promoting cell proliferation and adhesion, low expression of inflammatory cytokines, and reduced pulp inflammation. This systematic review therefore suggests that the choice of repair bioceramic materials or MTA based on biocompatibility should be the professional's decision.

scholarly journals Polymeric Nanoparticles Based on Tyrosine-Modified, Low Molecular Weight Polyethylenimines for siRNA Delivery

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 600 ◽  
Author(s):  
Ewe ◽  
Noske ◽  
Karimov ◽  
Aigner
Keyword(s):  
Molecular Weight ◽  
Polymeric Nanoparticles ◽  
Sirna Delivery ◽  
Biological Properties ◽  
Low Molecular Weight ◽  
Rna Molecules ◽  
Low Cytotoxicity ◽  
Tyrosine Modification

A major hurdle for exploring RNA interference (RNAi) in a therapeutic setting is still the issue of in vivo delivery of small RNA molecules (siRNAs). The chemical modification of polyethylenimines (PEIs) offers a particularly attractive avenue towards the development of more efficient non-viral delivery systems. Here, we explore tyrosine-modified polyethylenimines with low or very low molecular weight (P2Y, P5Y, P10Y) for siRNA delivery. In comparison to their respective parent PEI, they reveal considerably increased knockdown efficacies and very low cytotoxicity upon tyrosine modification, as determined in different reporter and wildtype cell lines. The delivery of siRNAs targeting the anti-apoptotic oncogene survivin or the serine/threonine-protein kinase PLK1 (polo-like kinase 1; PLK-1) oncogene reveals strong inhibitory effects in vitro. In a therapeutic in vivo setting, profound anti-tumor effects in a prostate carcinoma xenograft mouse model are observed upon systemic application of complexes for survivin or PLK1 knockdown, in the absence of in vivo toxicity. We thus demonstrate the tyrosine-modification of (very) low molecular weight PEIs for generating efficient nanocarriers for siRNA delivery in vitro and in vivo, present data on their physicochemical and biological properties, and show their efficacy as siRNA therapeutic in vivo, in the absence of adverse effects.

Nanodrugs as a new approach in therapy of cardiovascular diseases and cancer with tumor-associated angiogenesis

2020 ◽  
Vol 28 ◽  
Author(s):  
Justyna Hajtuch ◽  
Karolina Niska ◽  
Iwona Inkielewicz-Stepniak
Keyword(s):  
Cardiovascular Disease ◽  
Cardiovascular Diseases ◽  
Controlled Drug Release ◽  
Biological Properties ◽  
Comprehensive Information ◽  
Conventional Drug ◽  
Key Factor ◽  
Functionalized Materials

Background: Cancer along with cardiovascular diseases are globally defined as leading causes of death. Importantly, some risk factors are common to these diseases. The process of angiogenesis and platelets aggregation are observed in cancer development and progression. In recent years, studies have been conducted on nanodrugs in these diseases that have provided important information on the biological and physicochemical properties of nanoparticles. Their attractive features are that they are made of biocompatible, well-characterized and easily functionalized materials. Unlike conventional drug delivery, sustained and controlled drug release can be obtained by using nanomaterials. Methods: In this article, we review the latest research to provide comprehensive information on nanoparticle-based drugs for the treatment of cancer, cardiovascular disease associated with abnormal haemostasis, and the inhibition of tumorassociated angiogenesis. Results: The results of the analysis of data based on nanoparticles with drugs confirm their improved pharmaceutical and biological properties, which gives promising antiplatelet, anticoagulant and antiangiogenic effects. Moreover, the review included in vitro, in vivo research and presented nanodrugs with chemotherapeutics approved by Food and Drug Administration. Conclusion: By the optimization of nanoparticles size and surface properties, nanotechnology are able to deliver drugs with enhanced bioavailability in treatment of cardiovascular disease, cancer and inhibition of cancer-related angiogenesis. Thus, nanotechnology can improve the therapeutic efficacy of the drug, but there is a need for a better understanding of the nanodrugs interaction in the human body, because this is a key factor in the success of potential nanotherapeutics.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

Neuropharmacological Screening of Chiral and Non-chiral Phthalimide- Containing Compounds in Mice: in vivo and in silico Experiments

2019 ◽  
Vol 15 (1) ◽  
pp. 102-118 ◽  
Author(s):  
Carolina Campos-Rodríguez ◽  
José G. Trujillo-Ferrara ◽  
Ameyali Alvarez-Guerra ◽  
Irán M. Cumbres Vargas ◽  
Roberto I. Cuevas-Hernández ◽  
...  
Keyword(s):  
Locomotor Activity ◽  
In Silico ◽  
Biological Properties ◽  
Chiral Molecules ◽  
Chiral Compounds ◽  
Plus Maze ◽  
In Silico Studies ◽  
The Central Nervous System

Background: Thalidomide, the first synthesized phthalimide, has demonstrated sedative- hypnotic and antiepileptic effects on the central nervous system. N-substituted phthalimides have an interesting chemical structure that confers important biological properties. Objective: Non-chiral (ortho and para bis-isoindoline-1,3-dione, phthaloylglycine) and chiral phthalimides (N-substituted with aspartate or glutamate) were synthesized and the sedative, anxiolytic and anticonvulsant effects were tested. Method: Homology modeling and molecular docking were employed to predict recognition of the analogues by hNMDA and mGlu receptors. The neuropharmacological activity was tested with the open field test and elevated plus maze (EPM). The compounds were tested in mouse models of acute convulsions induced either by pentylenetetrazol (PTZ; 90 mg/kg) or 4-aminopyridine (4-AP; 10 mg/kg). Results: The ortho and para non-chiral compounds at 562.3 and 316 mg/kg, respectively, decreased locomotor activity. Contrarily, the chiral compounds produced excitatory effects. Increased locomotor activity was found with S-TGLU and R-TGLU at 100, 316 and 562.3 mg/kg, and S-TASP at 316 and 562.3 mg/kg. These molecules showed no activity in the EPM test or PTZ model. In the 4-AP model, however, S-TGLU (237.1, 316 and 421.7 mg/kg) as well as S-TASP and R-TASP (316 mg/kg) lowered the convulsive and death rate. Conclusion: The chiral compounds exhibited a non-competitive NMDAR antagonist profile and the non-chiral molecules possessed selective sedative properties. The NMDAR exhibited stereoselectivity for S-TGLU while it is not a preference for the aspartic derivatives. The results appear to be supported by the in silico studies, which evidenced a high affinity of phthalimides for the hNMDAR and mGluR type 1.

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