Furanocoumarins from Ruta chalepensis with Amebicide Activity

Entamoeba histolytica (protozoan; family Endomoebidae) is the cause of amoebiasis, a disease related to high morbidity and mortality. Nowadays, this illness is considered a significant public health issue in developing countries. In addition, parasite resistance to conventional medicinal treatment has increased in recent years. Traditional medicine around the world represents a valuable source of alternative treatment for many parasite diseases. In a previous paper, we communicated about the antiprotozoal activity in vitro of the methanolic (MeOH) extract of Ruta chalepensis (Rutaceae) against E. histolytica. The plant is extensively employed in Mexican traditional medicine. The following workup of the MeOH extract of R. chalepensis afforded the furocoumarins rutamarin (1) and chalepin (2), which showed high antiprotozoal activity on Entamoeba histolytica trophozoites employing in vitro tests (IC50 values of 6.52 and 28.95 µg/mL, respectively). Therefore, we offer a full scientific report about the bioguided isolation and the amebicide activity of chalepin and rutamarin.

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Antiprotozoal Activity against Entamoeba histolytica of Plants Used in Northeast Mexican Traditional Medicine. Bioactive Compounds from Lippia graveolens and Ruta chalepensis

Molecules ◽

10.3390/molecules191221044 ◽

2014 ◽

Vol 19 (12) ◽

pp. 21044-21065 ◽

Cited By ~ 15

Author(s):

Ramiro Quintanilla-Licea ◽

Benito Mata-Cárdenas ◽

Javier Vargas-Villarreal ◽

Aldo Bazaldúa-Rodríguez ◽

Isvar Kavimngeles-Hernández ◽

...

Keyword(s):

Traditional Medicine ◽

Entamoeba Histolytica ◽

Bioactive Compounds ◽

Antiprotozoal Activity ◽

Ruta Chalepensis

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Antiprotozoal Activity Against Entamoeba histolytica of Flavonoids Isolated from Lippia graveolens Kunth

Molecules ◽

10.3390/molecules25112464 ◽

2020 ◽

Vol 25 (11) ◽

pp. 2464

Author(s):

Ramiro Quintanilla-Licea ◽

Javier Vargas-Villarreal ◽

María Julia Verde-Star ◽

Verónica Mayela Rivas-Galindo ◽

Ángel David Torres-Hernández

Keyword(s):

Entamoeba Histolytica ◽

Inhibitory Concentration ◽

Public Health Problem ◽

In Vitro Tests ◽

Antiprotozoal Activity ◽

Subsequent Work ◽

Antiamoebic Activity ◽

Work Up ◽

First Time

Amebiasis caused by Entamoeba histolytica is nowadays a serious public health problem worldwide, especially in developing countries. Annually, up to 100,000 deaths occur across the world. Due to the resistance that pathogenic protozoa exhibit against commercial antiprotozoal drugs, a growing emphasis has been placed on plants used in traditional medicine to discover new antiparasitics. Previously, we reported the in vitro antiamoebic activity of a methanolic extract of Lippia graveolens Kunth (Mexican oregano). In this study, we outline the isolation and structure elucidation of antiamoebic compounds occurring in this plant. The subsequent work-up of this methanol extract by bioguided isolation using several chromatographic techniques yielded the flavonoids pinocembrin (1), sakuranetin (2), cirsimaritin (3), and naringenin (4). Structural elucidation of the isolated compounds was achieved by spectroscopic/spectrometric analyses and comparing literature data. These compounds revealed significant antiprotozoal activity against E. histolytica trophozoites using in vitro tests, showing a 50% inhibitory concentration (IC50) ranging from 28 to 154 µg/mL. Amebicide activity of sakuranetin and cirsimaritin is reported for the first time in this study. These research data may help to corroborate the use of this plant in traditional Mexican medicine for the treatment of dyspepsia.

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Role of in vivo and in vitro Tests in the Diagnosis of Severe Cutaneous Adverse Reactions (SCAR) to Drug

Current Pharmaceutical Design ◽

10.2174/1381612825666191107104126 ◽

2019 ◽

Vol 25 (36) ◽

pp. 3872-3880 ◽

Cited By ~ 3

Author(s):

Marcel M. Bergmann ◽

Jean-Christoph Caubet

Keyword(s):

Adverse Reactions ◽

Lymphocyte Transformation ◽

Stevens Johnson Syndrome ◽

In Vitro Tests ◽

High Morbidity ◽

Patch Tests ◽

Severe Cutaneous Adverse Reactions ◽

Cutaneous Adverse Reactions

Severe cutaneous adverse reactions (SCAR) are life-threatening conditions including acute generalized exanthematous pustulosis (AGEP), Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis (TEN) and drug reaction with eosinophilia and systemic symptoms (DRESS). Diagnosis of causative underlying drug hypersensitivity (DH) is mandatory due to the high morbidity and mortality upon re-exposure with the incriminated drug. If an underlying DH is suspected, in vivo test, including patch tests (PTs), delayed-reading intradermal tests (IDTs) and in vitro tests can be performed in selected patients for which the suspected culprit drug is mandatory, or in order to find a safe alternative treatment. Positivity of in vivo and in vitro tests in SCAR to drug varies depending on the type of reaction and the incriminated drugs. Due to the severe nature of these reactions, drug provocation test (DPT) is highly contraindicated in patients who experienced SCAR. Thus, sensitivity is based on positive test results in patients with a suggestive clinical history. Patch tests still remain the first-line diagnostic tests in the majority of patients with SCAR, followed, in case of negative results, by delayed-reading IDTs, with the exception of patients with bullous diseases where IDTs are still contra-indicated. In vitro tests have shown promising results in the diagnosis of SCAR to drug. Positivity is particularly high when the lymphocyte transformation test (LTT) is combined with cytokines and cytotoxic markers measurement (cyto-LTT), but this still has to be confirmed with larger studies. Due to the rarity of SCAR, large multi-center collaborative studies are needed to better study the sensitivity and specificity of in vivo and in vitro tests.

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Lactobacilli intra-tracheal administration protects from Pseudomonas aeruginosa pulmonary infection in mice – a proof of concept

Beneficial Microbes ◽

10.3920/bm2019.0069 ◽

2019 ◽

Vol 10 (8) ◽

pp. 893-900 ◽

Cited By ~ 1

Author(s):

M.S. Fangous ◽

Y. Alexandre ◽

N. Hymery ◽

S. Gouriou ◽

D. Arzur ◽

...

Keyword(s):

Pseudomonas Aeruginosa ◽

Murine Model ◽

Alveolar Epithelial Cell ◽

A549 Cells ◽

Respiratory Pathogen ◽

Public Health Issue ◽

Epithelial Cell Line ◽

High Morbidity ◽

Respiratory Pathogens

The spreading of antibiotic resistance is a major public health issue, which requires alternative treatments to antibiotics. Lactobacilli have shown abilities to prevent pneumonia in clinical studies when given by oral route, certainly through the gut-lung axis involvement. Rationally, respiratory administration of lactobacilli has been developed and studied in murine model, to prevent from respiratory pathogens. It allows a direct effect of probiotics into the respiratory system. To our knowledge, no study has ever focused on the effect of probiotic intra-respiratory administration to prevent from Pseudomonas aeruginosa (PA) pneumonia, a major respiratory pathogen associated with high morbidity rates. In this study, we evaluated the beneficial activity of three Lactobacillus strains (Lactobacillus fermentum K.C6.3.1E, Lactobacillus zeae Od.76, Lactobacillus paracasei ES.D.88) previously screened by ourselves and known to be particularly efficient in vitro in inhibiting PAO1 virulence factors. Cytotoxic assays in alveolar epithelial cell line A549 were performed, followed by the comparison of two lactobacilli prophylactic protocols (one or two administrations) by intra-tracheal administration in a C57BL/6 murine model of PA pneumonia. A549 cells viability was improved from 23 to 75% when lactobacilli were administered before PAO1 incubation, demonstrating a protective effect (P<0.001). A significant decrease of 2 log of PAO1 was observed 4 h after PAO1 instillation (3×106 cfu/mouse) in both groups receiving lactobacilli (9×106 cfu/mouse) compared to PAO1 group (P<0.05). One single prophylactic administration of lactobacilli significantly decreased the secretion by 50% in bronchoalveolar lavages of interleukin (IL)-6 and tumour necrosis factor-α compared to PAO1. No difference of secretion was observed for the IL-10 secretion, whatever the prophylactic study design. This is the first study highlighting that direct lung administration of Lactobacillus strains protect against PA pneumonia. Next step will be to decipher the mechanisms involved before developing this novel approach for human applications.

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About Minimization of Expenses on Allergy Diagnosis in Children: Analysis of Consistency of in Vitro- and in Vivo-Allergic Examinations Results

Annals of the Russian academy of medical sciences ◽

10.15690/vramn583 ◽

2015 ◽

Vol 70 (6) ◽

pp. 748-755

Author(s):

Marina Andreevna Snovskaya ◽

Anna Sergeevna Batyrova ◽

Leyla Seymurovna Namazova-Baranova ◽

Anna Aleksandrovna Alekseeva ◽

Elena Aleksandrovna Vishneva ◽

...

Keyword(s):

Atopic Disease ◽

Skin Tests ◽

Morbidity Rate ◽

In Vitro Tests ◽

High Morbidity ◽

Meadow Fescue ◽

Ige Antibodies ◽

High Morbidity Rate

High morbidity rate of atopic diseases among children, including high importance of grass pollen as a sensitizing agent, determine the relevance of studies on diagnostic examination systems for appointment of adequate therapy. The research of the most relevant allergens for patients to exclude of duplicating and uninformative tests became urgent after development of a new type of diagnostic tests that does not require expensive equipment. The objective of this research was to evaluate the results of in vitro- and in vivo-diagnostic examinations of children with various forms of atopic disease caused by pollen of meadow grasses, and to choose the most significant prognostic parameters for the diagnosis. Methods: 277 children aged 4–16 years with various forms of atopic disease were included in the study. There were performed skin prick tests and determination of IgE-antibodies levels to allergen extracts of cocksfoot (g3), meadow fescue (g4), timothy grass (g6). Results: In the studied group of patients 32–50% of children have antibodies to grass allergens. There was a close correlation of antibody response on the investigated allergens, quantitative coincidence of IgE-antibodies to g3 and g4 allergens levels. IgE (g6) concentration was close to the IgE(g3) and IgE(g4) levels (85,0±21,6%). Analysis of the skin tests results showed that 44% of patients have a positive response to grass allergens, and in vivo-tests results coincide with serological tests results, mostly in a qualitative sense. The most significant relationship was noted between in vivo and in vitro-tests in the results of testing the response to meadow fescue pollen.Conclusion: Based on these data IgE concentration index to meadow fescue allergens can be used as a prognostic marker to determine the sensitization of patients with different nosology forms of allergy and can help to improve allergic diagnostics.

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In vitro tests of biopolymers with extracts from plants used in Mexican traditional medicine on Candida albicans biofilm

Microorganisms in Industry and Environment ◽

10.1142/9789814322119_0106 ◽

2010 ◽

Author(s):

J. de Cássia Orlandi Sardi ◽

I. Teixeira Alves Peixoto ◽

J.F. Höfling ◽

R. Bruno Gonçalves ◽

A. Rodríguez García ◽

...

Keyword(s):

Candida Albicans ◽

Traditional Medicine ◽

In Vitro Tests

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In vitro antiprotozoal activity from the roots of Geranium mexicanum and its constituents on Entamoeba histolytica and Giardia lamblia

Journal of Ethnopharmacology ◽

10.1016/j.jep.2005.01.019 ◽

2005 ◽

Vol 98 (1-2) ◽

pp. 191-193 ◽

Cited By ~ 43

Author(s):

Fernando Calzada ◽

J. Antonio Cervantes-Martínez ◽

Lilian Yépez-Mulia

Keyword(s):

Entamoeba Histolytica ◽

Giardia Lamblia ◽

Antiprotozoal Activity

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Virtual Screening of FDA-Approved Drugs against Triose Phosphate Isomerase from Entamoeba histolytica and Giardia lamblia Identifies Inhibitors of Their Trophozoite Growth Phase

International Journal of Molecular Sciences ◽

10.3390/ijms22115943 ◽

2021 ◽

Vol 22 (11) ◽

pp. 5943

Author(s):

Alfredo Juárez-Saldivar ◽

Elizabeth Barbosa-Cabrera ◽

Edgar E. Lara-Ramírez ◽

Alma D. Paz-González ◽

Ana V. Martínez-Vázquez ◽

...

Keyword(s):

Virtual Screening ◽

Entamoeba Histolytica ◽

Giardia Lamblia ◽

Triosephosphate Isomerase ◽

Glycolytic Enzyme ◽

Public Health Issue ◽

Intestinal Protozoan ◽

Approved Drugs ◽

Fda Approved Drugs

Infectious diseases caused by intestinal protozoan, such as Entamoeba histolytica (E. histolytica) and Giardia lamblia (G. lamblia) are a worldwide public health issue. They affect more than 70 million people every year. They colonize intestines causing primarily diarrhea; nevertheless, these infections can lead to more serious complications. The treatment of choice, metronidazole, is in doubt due to adverse effects and resistance. Therefore, there is a need for new compounds against these parasites. In this work, a structure-based virtual screening of FDA-approved drugs was performed to identify compounds with antiprotozoal activity. The glycolytic enzyme triosephosphate isomerase, present in both E. histolytica and G. lamblia, was used as the drug target. The compounds with the best average docking score on both structures were selected for the in vitro evaluation. Three compounds, chlorhexidine, tolcapone, and imatinib, were capable of inhibit growth on G. lamblia trophozoites (0.05–4.935 μg/mL), while folic acid showed activity against E. histolytica (0.186 μg/mL) and G. lamblia (5.342 μg/mL).

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