Antibacterial Activity and Untargeted Metabolomics Profiling of Acalypha arvensis Poepp.

The search for potent antimicrobial compounds is critical in the face of growing antibiotic resistance. This study explores Acalypha arvensis Poepp. (A. arvensis), a Caribbean plant traditionally used for disease treatment. The dried plant powder was subjected to successive extractions using different solvents: hexane (F1), dichloromethane (F2), methanol (F3), a 50:50 mixture of methanol and water (F4), and water (F5). Additionally, a parallel extraction was conducted using a 50:50 mixture of methanol and chloroform (F6). All the fractions were evaluated for their antimicrobial activity, and the F6 fraction was characterized using untargeted metabolomics using SPME-GC×GC-TOFMS. The extracts of A. arvensis F3, F4, and F5 showed antibacterial activity against Staphylococcus aureus ATCC 25923 (5 mg/mL), MRSA BA22038 (5 mg/mL), and Pseudomonas aeruginosa ATCC 27853 (10 mg/mL), and fraction F6 showed antibacterial activity against Staphylococcus aureus ATCC 29213 (2 mg/mL), Escherichia coli ATCC 25922 (20 mg/mL), Pseudomonas aeruginosa ATCC 27853 (10 mg/mL), Enterococcus faecalis ATCC 29212 (10 mg/mL), Staphylococcus aureus 024 (2 mg/mL), and Staphylococcus aureus 003 (2 mg/mL). Metabolomic analysis of F6 revealed 2861 peaks with 58 identified compounds through SPME and 3654 peaks with 29 identified compounds through derivatization. The compounds included methyl ester fatty acids, ethyl ester fatty acids, terpenes, ketones, sugars, amino acids, and fatty acids. This study represents the first exploration of A. arvensis metabolomics and its antimicrobial potential, providing valuable insights for plant classification, phytochemical research, and drug discovery.

Medicinal Plants and Plant-Based Remedies in Grande-Terre: An Ethnopharmacological Approach.

The island of Grande-Terre is a French overseas region that belongs to the Guadeloupean archipelago, a biodiversity hotspot with unique flora. Herbal medicine is widely used in the island for therapeutical purposes; however, there is a significant knowledge gap in the records relating to medicinal plants and their associated uses. Ethnobotanical survey methodology using quantitative parameters (informant consensus factor, species use value, relative frequency of citation, frequency use of a treatment and plant for an ailment) provided insights into the traditional medicinal use of a given plant. Ninety-six different plant species distributed among 56 families were identified and 523 remedies were documented in the survey. After data filtering, 22 plants species were associated with 182 remedies. The most frequent plant families were Poaceae, Myrtaceae, Cucurbitaceae and Rubiaceae. Aerial parts of these plants were the most common parts of the plant used for the remedies and the most frequent mode of administration was oral ingestion. This study highlights a valuable traditional knowledge of folklore medicine and helps to document and preserve the association of a plant with-and its use frequency for-a given ailment. These findings might be the starting point for the identification of biologically active phytocompounds to fight common health debilities.

Antidiabetic Potential of Plants from the Caribbean Basin.

Diabetes mellitus (DM) is a group of metabolic disorders characterized by hyperglycemia, insulin insufficiency or insulin resistance, and many issues, including vascular complications, glycative stress and lipid metabolism dysregulation. Natural products from plants with antihyperglycemic, hypolipidemic, pancreatic protective, antioxidative, and insulin-like properties complement conventional treatments. Throughout this review, we summarize the current status of knowledge of plants from the Caribbean basin traditionally used to manage DM and treat its sequelae. Seven plants were chosen due to their use in Caribbean folk medicine. We summarize the antidiabetic properties of each species, exploring the pharmacological mechanisms related to their antidiabetic effect reported in vitro and in vivo. We propose the Caribbean flora as a source of innovative bioactive phytocompounds to treat and prevent DM and DM-associated complications.

Spectroscopic, Electrochemical, and Biological Assays of Copper-Binding Molecules for Screening of Different Drugs and Plant Extracts against Neurodegenerative Disorders.

Neurodegenerative disorders, caused by prone-to-aggregation proteins, such as Alzheimer disease or Huntington disease, share other traits such as disrupted homeostasis of essential metal ions, like copper. In this context, in an attempt to identify Cu2+ chelating agents, we study several organic compounds (ethylenediaminetetraacetic acid, phenylenediamine, metformin, salicylate, and trehalose) and organic extracts obtained from Bacopa monnieri L., which has been used in Ayurvedic therapies and presented a broad spectrum of biological properties. For this purpose, UV-visible spectroscopy analysis and electrochemical measurements were performed. Further, biological assays were performed in Caenorhabditis elegans models of polyQ toxicity, in an attempt to obtain better insights on neurodegenerative disorders.

Helietta apiculata: a tropical weapon against Chagas disease.

The present study pretends to evaluate the in vivo efficacy of the crude chloroform bark extract of Helietta apiculata, then the activity will be compared with the reference drug, benznidazole, in acute Trypanosoma cruzi infected mice when administered by oral route. The chloroformic extract of Helieta apiculata was administered by oral route at 5, 10 and 50 mg/kg daily for two weeks. This study has shown a moderate efficacy of the H. apiculata bark extract in reducing T. cruzi parasitaemia in 42 to 54% after a monitoring of 60 days post-infection and when compared with control groups. Concerning mice mortality, only two only two mice died, one from the control group and the other one from the group threated with 10 mg of the chlorofom extract of H. apiculata, suggesting the potential of H. apiculta extracts as a safe and inexpensive treatment of Chagas disease.

Phytoelectrochemical analysis of Zanthoxylum chiloperone.

INTRODUCTION: An innovative application of the voltammetry of microparticles methodology to characterize the phytochemical composition of extracts of different parts of Zanthoxylum chiloperone var. angustifolium Engl. is described. OBJECTIVE: Characterize the phytochemical composition of extracts of different parts of plants by electrochemical methodologies. METHODS: The voltammetry of microparticles methodology was applied to alcoholic extracts from leaves, seeds, fruits, roots and stem bark of Zanthoxylum chiloperone. RESULTS: In contact with aqueous phosphate buffer, characteristic cathodic signals of its main natural products (canthin-6-one, 5-methoxycanthin-6-one and trans-avicennol) were recorded. The study of the voltammograns allows the estimation of the relative amounts of canthin-6-one, 5-methoxycanthin-6-one and trans-avicennol from the different parts of Zanthoxylum chiloperone. CONCLUSION: The voltammetric responses of alcoholic extracts from different parts of Zanthoxylum chiloperone var. angustifolium allows their phytochemical characterization without need of sample pretreatment thus illustrating the capabilities of the voltammetry of microparticles methodology to increase the tools applied to phytochemical analysis. Copyright © 2016 John Wiley & Sons, Ltd.

The antiplasmodium effects of a traditional South American remedy: Zanthoxylum chiloperone var. angustifolium against chloroquine resistant and chloroquine sensitive strains of Plasmodium falciparum

Zanthoxylum chiloperone var. angustifolium Engl., Rutaceae, is used in traditional medicine to treat fungal and protozoal infections in the central area of South America. Considering the increasing resistance of Plasmodium falciparum in malarial ridden areas, we explored the anti-plasmodial effects of three compounds isolated from Z. chiloperone. The pyranocoumarin transavicennol and the canthinone alkaloids, canthin-6-one and 5-methoxycanthin-6-one, were found to have IC50 on chloroquine/mefloquine resistant and sensitive strains of P. falciparum of 0.5-2.7, 2.0-5.3 and 5.1-10.4 ƒÊg/mL, respectively. Moreover, the formation of heme adducts by these compounds is described by a novel alternative method based on MS-CID methods. The alkylamide sanshool was also identified, for first time in this plant, in the dichloromethanic and ethanolic extracts and the extracts were found to be notably non-toxic and displayed good anti-plasmodial effects.

Zanthoxylum chiloperone leaves extract: first sustainable Chagas disease treatment.

ETHNOPHARMACOLOGICAL RELEVANCE: Zanthoxylum chiloperone var. angustifolium Engl. (Rutaceae) stem bark is used traditionally in Paraguay for its antiparasitic properties. Canthin-6-one is main compound isolated from Zanthoxylum chiloperone var angustifolium with broad spectrum antifungal, leishmanicidal and trypanocidal activities. AIM OF THE STUDY: The qualitative and quantitative characterization and the isolation of main alkaloidal components of different organs of Zanthoxylum chiloperone are investigated by HPLC-UV-MS. The in vitro biological activity of each extract against trypomastigote and amastigote forms of Trypanosoma cruzi parasites were evaluated, then comparison the in vivo efficacy of the ethanolic leaves extract of Zanthoxylum chiloperone with reference drug, benznidazole, in acute Trypanosoma cruzi infected mice when administered by oral route. We have also evaluated the mutagenic and cytotoxic activity of the main component of Zanthoxylum chiloperone, i.e. canthin-6-one, by mouse bone marrow micronucleus test. MATERIALS AND METHODS: The compositions of the ethanol extracts obtained after the maceration process were studied by HPLC-UV-MS methods. The quantitation analysis was performed by external standard method, using a calibration curve constructed utilizing solutions containing different concentrations of the reference samples. The anti-trypomastigote activity was evaluated by the lysis effect on mouse blood trypomastigotes (Y strain Trypanosoma cruzi). The anti-amastigote Trypanosoma cruzi activity was evaluated by a modified colorimetric method with chlorophenol red-ß-d-galactopyranoside (CPRG). The cytotoxicity of extracts and compounds was performed on NCTC 929 cells. The in vivo efficacy of the ethanolic leaves extract of Zanthoxylum chiloperone and benznidazole, in acute Trypanosoma cruzi (two different strains) was evaluated in Trypanosoma cruzi infected mice; the drugs were administered by oral route. The mortality rates were recorded and parasitaemias in control and treated mice were determined once weekly for 70 days. The mutagenic and cytotoxic activity of the main component of Zanthoxylum chiloperone, canthin-6-one, by mouse bone marrow micronucleus test. RESULTS: Canthin-6-one was the main compound of stem and root bark and 5-methoxy-canthin-6-one in leaves and fruits. The ethanolic leaves extract, canthin-6-one and benznidazole presented, approximately, the same level of in vitro activity against trypomastigote and amastigote forms of Trypanosoma cruzi. We have also evaluated the mutagenic and cytotoxic effects of canthin-6-one by micronucleus test in mice. This test showed any mutagenic and cytotoxic damages. The effects of oral or subcutaneous treatments at 10 mg/kg daily for 2 weeks with the ethanolic extract of leaves of Zanthoxylum chiloperone were examined in Balb/c mice infected acutely with Trypanosoma cruzi (CL or Y strain) and compared with benznidazole at 50 mg/kg for 2 weeks. In these experiments, 70 days after infection, parasitaemia and serological response were significantly reduced with the oral ethanolic extract treatment compared with reference drug. CONCLUSIONS: This study have shown the efficacy of the leaves extract of Zanthoxylum chiloperone in reducing Trypanosoma cruzi parasitaemia in vivo assays and could be welcomed by scientific and rural communities of Paraguay because it could help them towards the use of local resources to treat an endemic infection, Chagas disease, affecting 20% of the population of this country.