Unveiling new myrsinoic acids and AChE ligands from Myrsine guianensis (Aubl.) Kuntze.

Molecular dereplication and drug-like discovery are important tools for exploring the chemical profile of metabolites in a complex mixture. In order to establish a workflow for discovering novel acetylcholinesterase (AChE) ligands, we performed the chemical study of Myrsine guianensis (Aubl.) Kuntze (Primulaceae).

Fungal Cultivars of Higher Attine Ants Promote Escovopsis Chemotropism.

In varied environments, microorganisms search for partners or nutritional resources using chemical signals. Microbes are drawn (chemotaxis) or grow directionally (chemotropism) towards the chemical source, enabling them to establish and maintain symbiosis. The hypocrealean fungi Escovopsis enhance their growth towards the basidiomycete fungus Leucoagaricus gongylophorus, which is cultivated by leaf-cutting attine ants for food.

Chemodiversity and Anti-Leukemia Effect of Metabolites from CMLD 18.

represents a species recently described, with little up-to-date information about its metabolic and biological potential. Due to this scenario, we performed chemical and biological studies of CMLD18, a strain isolated from (Rutaceae). HRMS-MS guided dereplication strategies and anti-leukemia assays conducted the isolation and characterization of six compounds after several chromatographic procedures: 2-chloroemodic acid (), 2-chloro-1,3,8-trihydroxy-6- (hydroxymethyl)-anthraquinone (), 7-chloroemodin (), bisdethiobis(methylthio)acetylaranotine (), fellutanine C (), and 4-methyl-5,6-diihydro-2H-pyran-2-one ().

Exploring the chemical diversity of phytopathogenic fungi infecting edible fruits.

Two fungi, and were cultured under different conditions to obtain fourteen compounds. The axenic cultures of and in potato dextrose broth (PDB) medium yielded fusaric acid (), 9,10-dehydrofusaric acid (), and tyrosol, whereas their co-cultivation produced fusarinol (), a fusaric acid complex with magnesium (), 9,10-dehydrofusaric acid complex with magnesium (), and 5-butyl-5-(hydroxymethyl) dihydrofuranone (). Upon changing the medium from PDB to Czapek, different compounds (uracil, -hydroxy acetophenone, and cyclo(L-Leu-L-Pro) were obtained.

Limonoids and insecticidal activity on (J.E. Smith) (Lepidoptera: Noctuidae) of A. Juss. (Meliaceae).

The aim of the study was to evaluate the effects of the seeds, exocarp and aril extracts from A. Juss. (Meliaceae) against and present the phytochemical study carried out with the aril extract of .

Anacardic Acid Derivatives Affect the in Vitro Reactions of Photosynthesis.

The dichloromethane extract of the cashew nuts from Anacardium occidentale was fractionated by rotation locular countercurrent chromatography aimed at discovering metabolites that could be useful as new models for photosynthesis inhibitors. The chemical fractionation afforded a complex mixture of anacardic acids, which upon catalytic hydrogenation yielded anacardic acid (1). Methylation of 1 via reaction with diazomethane afforded an ester 2.

Combination of GC-MS Molecular Networking and Larvicidal Effect against for the Discovery of Bioactive Substances in Commercial Essential Oils.

Dengue is a neglected disease, present mainly in tropical countries, with more than 5.2 million cases reported in 2019. Vector control remains the most effective protective measure against dengue and other arboviruses.

Chemometrics applied to H NMR and UV-Vis spectroscopy as a way to evaluate solid-liquid extraction of leaves of artichoke.

Artichoke has several biological actions, which are related to the synergistic action of its bioactive compounds. Solid-liquid extraction influence the type and quantity of compounds extracted and, consequently, the biological activity of the plant extract. This study aims to investigate which extraction method (maceration, infusion, or Soxhlet) and which green solvent (ethanol or acetone) would be more suitable to obtain bioactive artichoke extracts.

Insecticidal activity of copper (II) complexes with flavanone derivatives.

In this work, we describe the insecticidal activity against of flavanone derivatives (naringin, naringenin and hesperidin) complexed to copper (II). For the assays, the compounds were incorporated into an artificial diet and offered to during its larval period. The duration of larval and pupal phases, the weight of pupae and the percentage of dead insects at the end of the larval phase were evaluated.

Potential insecticidal activity of aminonaphthoquinone Mannich bases derived from lawsone and their copper (II) complex derivatives.

The fall armyworm, , is a polyphagous pest that causes important damage in different regions of America and mainly affects corn crops in both tropical and subtropical areas. Currently, control relies on both transgenic plants and/or chemical pesticides. In this work, we describe insecticidal activity against the fall armyworm from a series of Mannich bases (), derived from 2-hydroxy-1,4-naphthoquinone (lawsone), substituted benzaldehydes, and two primary amines, and their Cu complexes ().

[10]-Gingerol improves doxorubicin anticancer activity and decreases its side effects in triple negative breast cancer models.

Purpose: Although doxorubicin is widely used to treat cancer, severe side effects limit its clinical use. Combination of standard chemotherapy with natural products can increase the efficacy and attenuate the side effects of current therapies. Here we studied the anticancer effects of a combined regimen comprising doxorubicin and [10]-gingerol against triple-negative breast cancer, which does not respond to hormonal or targeted therapies.

Plant Natural Products for the Control of : The Main Vector of Important Arboviruses.

The mosquito species is one of the main vectors of arboviruses, including dengue, Zika and chikungunya. Considering the deficiency or absence of vaccines to prevent these diseases, vector control remains an important strategy. The use of plant natural product-based insecticides constitutes an alternative to chemical insecticides as they are degraded more easily and are less harmful to the environment, not to mention their lower toxicity to non-target insects.

Liquid Fungal Cocultivation as a Strategy to Access Bioactive Metabolites.

Fungi are a rich source of bioactive compounds. Fungal cocultivation is a method of potentiating chemical interactions and, consequently, increasing bioactive molecule production. In this study, we evaluated the bactericidal, antiprotozoal, and cathepsin V inhibition activities of extracts from axenic cultures of 6 fungi (, and ) that infest tropical fruits and 57 extracts obtained by their cocultivation.

Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors.

Cathepsin K (CatK) is a cysteine protease known for its potent collagenolytic activity, being recognized as an important target to the development of therapies for the treatment of bone disorders. Epoxypeptidomimetics have been reported as potent inhibitors of cathepsins, thus in this work we present a green synthesis of new peptidomimetics by using a one-pot asymmetric epoxidation/Ugi multicomponent reaction. The compounds were evaluated against CatK showing selectivity when compared with cathepsin L, with an inhibition profile in the low micromolar IC range.

Mycotoxins from Fusarium proliferatum: new inhibitors of papain-like cysteine proteases.

Papain-like cysteine proteases (PLCPs) in plants are essential to prevent phytopathogen invasion. In order to search for cysteine protease inhibitors and to investigate compounds that could be associated to pineapple Fusarium disease, a chemistry investigation was performed on Fusarium proliferatum isolated from Ananas comosus (pineapple) and cultivated in Czapek medium. From F.

Acetylation of cedrelone increases its cytotoxic activity and reverts the malignant phenotype of breast cancer cells in 3D culture.

Cedrelone is a limonoid isolated from the plant Trichilia catigua (Meliaceae). Previous studies have demonstrated that cedrelone (1) has several damaging effects on triple negative breast tumor (TNBC) cell line MDA-MB-231. In this work we investigated two new derivatives of cedrelone, the acetate (1a) and the mesylate (1b), to examine whether their effects are improved in comparison to the lead molecule.

A new approach for identifying antagonism among fungi species and antifungal activity.

New antifungals are increasingly needed due to the emergence of resistant fungal strains. Traditional antifungal assays are laborious and require significant amounts of samples. The present work presents a new proposal to evaluate antifungal activity and antagonism among fungal species, based on experiments of fungal culture and co-culture, H NMR profile of fungal culture extracts and chemometrics.

Picraviane A and B: Nortriterpenes with limonoid-like skeletons containing a heptanolide E-ring system from Picramnia glazioviana.

Two highly oxygenated nortriterpenes, picraviane A and B, were isolated from the ethanolic extract of Picramnia glazioviana Engl. The structures were determined by analysis of HRMS and 2D NMR spectroscopic data. Single-crystal X-ray diffraction data was also obtained for picraviane B.

Isolation of Chavibetol and Methyleugenol from Essential Oil of by High Performance Liquid Chromatography.

A high performance liquid chromatography (HPLC) method was developed for the simultaneous isolation, on a semi-preparative scale, of chavibetol and methyleugenol from the crude essential oil of leaves. The purity of the isolated compounds and their quantifications were developed using GC/FID. Chavibetol was isolated with high purity (98.

[10]-Gingerol Affects Multiple Metastatic Processes and Induces Apoptosis in MDAMB- 231 Breast Tumor Cells.

Background: Triple Negative Breast Cancer (TNBC) represents the approximately 15% of breast cancers that lack expression of Estrogen (ER) and Progesterone Receptors (PR) and do not exhibit amplification of the human epidermal growth factor receptor 2 (HER2) gene, imposing difficulties to treatment. Interactions between tumor cells and their microenvironment facilitate tumor cell invasion in the surrounding tissues, intravasation through newly formed vessels, and dissemination to form metastasis. To treat metastasis from breast and many other cancer types, chemotherapy is one of the most extensively used methods.

Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase.

This study describes the activity of five natural hydroxycinnamic acids and derived compound: caffeic (1), rosmarinic (2), chlorogenic (3), and cryptochlorogenic (4), acids and isoverbascoside (5). All compounds inhibited Leishmania amazonensis arginase with IC -in range of 1.5-11 μM.

Biological and Chemical Control of Sclerotinia sclerotiorum using Stachybotrys levispora and Its Secondary Metabolite Griseofulvin.

Sclerotinia sclerotiorum is responsible for the white mold of soybeans, and the difficulty to control the disease in Brazil is causing million-dollar damages. Stachybotrys levispora has shown activity against S. sclerotiorum.

Cathepsin D immobilized capillary reactors for on-flow screening assays.

The treatment of diseases using enzymes as targets has called for the development of new and reliable methods for screening. The protease cathepsin D is one such target involved in several diseases such as tumors, degenerative processes, and vital processes of parasites causing schistosomiasis. Herein, we describe the preparation of a fused silica capillary, cathepsin D (CatD)-immobilized enzyme reactor (IMER) using in a multidimensional High Performance Liquid Chromatography-based method (2D-HPLC) and zonal affinity chromatography as an alternative in the search for new ligands.