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This study describes the extraction and identification by electrophoretic and spectrometric techniques of protease inhibitor from the medicinal plant Alocasia macrorrhizos as well as investigates their immunomodulatory properties and cell viability. The A. macrorrhizos tubers were subjected to protease inhibitor extractions and characterised using SDS-PAGE and MALDI-TOF. The protein extracts were assessed for activities trypsin inhibition stoichiometry, haemagglutinating, cell viability, NO and TNF-α production inhibition. Concerning the protease inhibitors analysis through SDS-PAGE, the results showed two bands with 11 and 24 kDa, and the MS analysis detected the ions more intense of m/z 4276.795 and 8563.361 in the roasted protein extract. The IC 50 of trypsin inhibition was 0.119 and 0.302 mg L -1 in the roasted and crude tuber, respectively. The protease inhibitors extract from the roasted tubers showed a reduction in the production of NO and TNF-α at concentrations lower than 100 µg mL -1 , without a reduction in cell viability.

The present study aims to assess the cytotoxic effect of the aqueous and protease inhibitors extracts of Sterculia striata on breast cancer cell lines. The in vitro results showed significant reductions in the highest concentrations from the S. striata seed extract for all cell lines. The aqueous extract reduced the viability by up to 35% in the MCF-7, 25% in the 4T1, and 35% in the MDA-MB-231 cell lines. Regarding the protease inhibitor extract, a 50% reduction in cell viability was observed in the MDA-MB-231 at concentration of 333 µg/mL. The aqueous and the protease inhibitor extracts showed mild reduction in the viability of macrophage cell lines. Chemical characterisation analysis revealed several polyphenols such as flavonoids, tannins, phenolic acids, and other secondary metabolites including terpenes, steroids, fatty acids, and organic acids, which may be related to the promising bioactivity observed. The S. striata showed antitumor activity, emphasising its pharmacological potential.

Siparuna brasiliensis is a medicinal plant widely used by indigenous communities of the Amazon rainforest to treat inflammatory diseases and related pathologies. Considering its ethnopharmacological application, it constitutes an important source of biologically active molecules in the development of anti-inflammatory drugs. This study describes a dereplication methodology of the bioactive extract from S. brasiliensis leaves and the evaluation of the anti-inflammatory potential in an in vivo inflammatory model with mice of the BALB/c lineage and in vitro using cell lines, as well as determining the production of an inflammatory mediator. From their charge-to-mass ratios ( m/z ) and elemental composition obtained through Ultrahigh-resolution mass spectrometry analysis by ESI(-)-Orbitrap MS and chromatographic profile by RP-HPLC-PDA, it was possible to annotate polyphenols with anti-inflammatory properties classified as flavonoids and organic acids. The administration of the extract significantly inhibited carrageenan-induced paw edema and showed effects similar to those of drug dexamethasone without affecting cell viability.

In traditional Brazilian medicine, tubers extracts from Alocasia macrorrhizos are widely used in the treatment of skin pigmentation disorder. However, studies that evaluate its benefits in the treatment of this disorder are non-existent. Thus, this work aims to investigate the bioactivity of A. macrorrhizos extracts in cell culture and murine model of Vitiligo and correlating with its phenolic profile. The metabolic profiling from the bioactive extracts was obtained by LC-DAD-MS, FTIR, NMR, and CE-UV. The murine model of Vitiligo was induced with 5% hydroquinone in C57BL/6 male mice, which were treated or not with 100 mg/kg of roasted tuber aqueous extract. In Vitiligo model assay was observed hair follicle repigmentation and reduction of the epidermal layer thickness at the histopathological level, in the animals treated with aqueous extract of roasted tubers. The present study provides new molecular insight and scientific evidence on the potential utility of the extract of A. macrorrhizos against Vitiligo.

Employing a combination of liquid chromatography electrospray ionization and paper spray ionization high-resolution tandem mass spectrometry, extracts from cupuassu ( Theobroma grandiflorum ) pulp prepared with either water, methanol, acetonitrile or combinations thereof were subjected to metabolite fingerprinting. Among the tested extractors, 100% methanol extracted preferentially phenols and cinnamic acids derivatives, whereas acetonitrile and acetonitrile/methanol were more effective in extracting terpenoids and flavonoids, respectively. And while liquid chromatography- mass spectrometry detected twice as many metabolites as paper spray ionization tandem mass spectrometry, the latter proved its potential as a screening technique. Comprehensive structural annotation showed a high production of terpenes, mainly oleanane triterpene derivatives. of the mass spectra Further, five major metabolites with known antioxidant activity, namely catechin, citric acid, epigallocatechin-3'-glucuronide, 5,7,8-trihydroxyflavanone, and asiatic acid, were subjected to molecular docking analysis using the antioxidative enzyme peroxiredoxin 5 (PRDX5) as a model receptor. Based on its excellent docking score, a pharmacophore model of 5,7,8-trihydroxyflavanone was generated, which may help the design of new antioxidants.

This work evaluated the metabolic profiling of Inga species with antitumor potential. In addition, we described the antigenotoxicity of polyphenols isolated from I. laurina and a proteomic approach using HepG2 cells after treatment with these metabolites. The in vitro cytotoxic activity against HepG2, HT-29 and T98G cancer cell lines was investigated. The assessment of genotoxic damage was carried out through the comet assay. The ethanolic extract from I. laurina seeds was subjected to bioassay-guided fractionation and the most active fractions were characterized. One bioactive fraction with high cytotoxicity against HT-29 human colon cancer cells (IC 50 = 4.0 µg mL -1 ) was found, and it was characterized as a mixture of p -hydroxybenzoic acid and 4-vinyl-phenol. The I. edulis fruit peel (IC 50 = 18.6 µg mL -1 ) and I. laurina seed (IC 50 = 15.2 µg mL -1 ) extracts had cytotoxic activity against the cell line T98G, and its chemical composition showed a variety of phenolic acids. The chemical composition of this species indicated a wide variety of aromatic acids, flavonoids, tannins, and carotenoids. The high concentration (ranging from 5% to 30%) of these polyphenols in the bioactive extract may be responsible for the antitumor potential. Regarding the proteomic approach, we detected proteins directly related to the elimination of ROS, DNA repair, expression of tumor proteins, and apoptosis.

Natural Products phytochemical provide a rich source for therapeutic discovery and has led to the development of many drugs. Thus, the aim of this study was to obtaining a metabolic profiling from ethanol extract of Inga semialata leaves (EEIS) selected by bioassay antimalarial and nematostatic and identify metabolites in mixture by co-injection experiments and NMR spectroscopy. The chemical composition of this species indicated a wide variety of aromatic acids (vanillic acid, 3,4,5-trimethoxy benzoic acid, gallic acid, methyl gallate , p -coumaric acid and ferulic acid), flavonoids (quercetin, myricetin-3- O - rhamnoside and myricetin-3- O -(2"-O- galloyl )- α -rhamnopyranoside), triterpenes (lupeol, α -amyrin, friedelin and oleanolic acid) and the 2-hydroxyethyl-dodecanoate. The antimalarial assay showed that the I. semialata n- hexane fraction presented higher inhibition percentage than the Chloroquine standard and may be considered a potential source of compounds with antimalarial activity while the EEIS and its fractions showed nematostatic potential below 17% in the assay of nematostatic evaluation against the parasite Meloidogyne incognita .

Inga edulis is traditionally used as anti-inflammatory and antidiarrheal and has been investigated as potential sources of biologically active natural products. In this study, dereplication strategy using HPLC-SPE-TT, RP-HPLC-PDA and NMR spectroscopy was employed, and this resulted in the identification of sixteen compounds from the leaves extract of I. edulis , including four triterpenes (lupeol, α-amirin, olean-18-ene acid and frideline), three flavonoids, eight phenolic acids, an anthocyanin derived from delphinidin-3-glycoside and a mixture of five acylated anthocyanins. The chemical identification was performed based on NMR data, chemosystematics aspects, UV spectra and by comparison with the retention time and UV spectra of authentic standards. The metabolic profile of the species indicated the presence of phenolic compounds as major constituents justifying its strong antioxidant potential performed in β -carotene test. The techniques used have shown effective strategies for the early detection of active natural products from plant extracts, as these approaches are still crucially absent.[Formula: see text].

This work describes a pharmacological screening of Brazilian medicinal plants through their anti-inflammatory and cytotoxicity activities. Cytotoxicity activity of Mouriri elliptica and Alchornea glandulosa as well as the drugs celecoxib and doxorubicin were evaluated in cultures of peritoneal macrophages. The immune system influence of these samples was analyzed by determining production/inhibition of NO, production of tumor necrosis factor-α and production of interleukin-10. Regarding the production/inhibition of NO, there was NO production by M. elliptica and NO inhibition when the cells were exposed to A. glandulosa; Macrophages generally produce more NO, plus TNF-α and less IL-10, when associated to the tumor phenomenon, characterizing the inflammation involved in cancer. A. glandulosa showed anti-inflammatory effect, inhibited NO production and it was associated with low TNF-α production, although not as low as the macrophages associated with celecoxib and doxorubicin. These cytokines were not different in animals with tumor. Celecoxib confirms its anti-inflammatory action by markedly inhibiting NO and TNF-α, but also inhibiting IL-10 which is an anti-inflammatory cytokine. Doxorubicin inhibited NO in a higher percentage in the group of animals with tumor, although the literature reports that this drug stimulates the production of NO and this collaborates with its cytotoxic effect.

This study aimed to identify and evaluate the cytotoxicity, genotoxicity, antigenotoxicity and chemoprevention assessment of flavonoids myricetin-3-O-(2″-O-galloyl)-α-rhamnopyranoside and myricetin-3-rhamnoside from Inga laurina leaves extract. The Quinone reductase induction as a biomarker for cancer chemoprevention was evaluated in murine hepatocellular carcinoma, the cytotoxicity was evaluated by sulforhonamide B assay and genotoxicity was evaluated by comet assay using HepG2 cell line. The results demonstrated that the flavonoids didn´t show cytotoxicity in HepG2 cells. In the chemoprevention evaluations were not able to promote the induction of Quinone Reductase and also no genotoxic effect was observed by evaluation of the comet assay in none of the concentrations tested. In the antigenotoxicity test, all compounds had a protective effect against damage induced by hydrogen peroxide and were repaired against damage. Although none of the flavonoids were capable of inducing the enzyme Quinone Reductase at the concentrations tested, the antigenotoxicity results showed a powerful chemoprotective action.