The aim of this study was to synthesize three nitro substituted chalcones and to evaluate their anti-inflammatory activity in the model of carrageenan induced edema in rats. The nitro chalcone were prepared by aldol condensation using of mechanical agitation and environmentally friendly solvents with 72-73% yields in approximately 2h. The three structures were evaluated on biological activity at dose of 200mg/kg and they showed anti-inflammatory protective effect by both oral and intraperitoneal administration, this effect was time dependent.

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Haematoxylum campechianum is a medicinal plant employed as an astringent to purify the blood and to treat stomach problems such as diarrhea and dysentery. A bio-guided chemical fractionation of the methanolic extract obtained from this plant allowed for the isolation of five compounds: two chalcones known as sappanchalcone (1); 3-deoxysappanchalcone (2); three homoisoflavonoids known as hematoxylol A (3); 4-O-methylhematoxylol (4); and, hematoxin (5). The spasmolytic activity was determined in an in vitro model (electrically induced contractions of guinea pig ileum), and allowed to demonstrate that the methanolic extract (EC50 = 62.11 ± 3.23) fractions HcF7 (EC50 = 61.75 ± 3.55) and HcF9 (EC50 = 125.5 ± 10.65) and compounds 1 (EC50 = 16.06 ± 2.15) and 2 (EC50 = 25.37 ± 3.47) of Haematoxylum campechianum present significant relaxing activity as compared to papaverine (EC50 = 20.08 ± 2.0) as a positive control.

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Aristolochia odoratissima L. is employed for the treatment of pain and as an antidote against the poison of venomous animals in traditional medicine. However, reports have not been found, to our knowledge, about the evaluation of the antinociceptive activity of extracts nor about the presence of compounds associated with this activity. Thus, the purpose of this work was to evaluate the antinociceptive activity of extracts and compounds isolated from the stems of Artistolochia odoratissima L. The extracts were obtained with solvents of increasing polarity and the compounds were isolated and characterized by column chromatography, HPLC, and NMR. The antinociceptive activity was carried out by the formalin test in mice. Ethyl acetate (AoEA) and methanolic (AoM) extracts decreased the paw licking in both phases of the formalin test. The isolated compounds (kaurenoic acid and hinokinin) from AoEA showed the highest antinociceptive activity in both phases of the formalin test. These results confirmed the analgesic effect of this specie described in traditional medicine and provided a base for a novel analgesic agent. They also allowed an approach for the development of standardized plant extracts with isolated metabolites.

Background: Salvia gesneriflora Lindley is employed in traditional Mexican medicine for the treatment of several diseases. Materials and Methods: The chromatographic profile of three extracts (SgH, SgD and SgM) of this plant allowed the identification of 11 components in SgH, the presence of rosmarinic (1), chlorogenic (2) and caffeic (3) acids and quercetin glucoside (4) in SgM and of ursolic acid (5) in SgD. The spasmolytic (electrically induced contractions of guinea-pig ileum), anti-inflammatory (edema in mouse ear) and antioxidant potential (DPPH, ABTS and FRAP assays) of the extracts were evaluated. Results: SgM showed the highest percentage of relaxation (80.67 ± 1.633%) with no significant difference (p

There is a significant need to gain access to new and better antibacterial agents. Acalypha arvensis, a plant from the Euphorbiaceae family, has been used in traditional medicine for centuries to treat infectious diseases. This manuscript reports the isolation, characterization, and antibacterial screening of 8 natural products extracted from maceration of aerial parts of Acalypha arvensis. Specifically, three extracts were assessed (n-hexane, ethyl acetate, and ethanol), in which antibacterial activity was evaluated against diverse bacterial strains. The ethanolic extract showed the best activity against methicillin-sensitive and methicillin-resistant Staphylococcus aureus, Klebsiella pneumoniae, and Pseudomonas aeruginosa strains, which supports the medicinal properties attributed to this plant. The chromatographic fractions AaR4 and AaR5 were the most bioactive, in which the ellagitannin natural product known as corilagin (1) was identified for the first time in this plant. Therefore, it can be said that this is the main chemical responsible for the observed antibacterial activity. However, we also identified chlorogenic acid (2), rutin (3), quercetin-3-O-glucoside (4), caffeic acid (5), among others (6–8). Hence, this plant can be considered to be a good alternative to treat health-related issues caused by various bacteria.

Three functionalized chalcones containing combinations of nitro functional groups have been synthesized via Claisen-Schmidt condensation between 2-nitroacetophenone and nitrobenzaldehyde, and the crystal structures obtained ((E)-1,3-bis(2-nitrophenyl)prop-2-en-1-one, 1a, (E)-1-(2-nitrophenyl)-3-(3-nitrophenyl)prop-2-en-1-one, 1b and (E)-1-(2-nitrophenyl)-3-(4-nitrophenyl)prop-2-en-1-one, 1c), C15H10N2O5, are reported. Compounds 1a and 1c crystallized in the triclinic centrosymmetric space group P1¯, whereas compound 1b crystallized in the orthorhombic space group Pbca. The X-ray analysis reveals that structures 1a and 1b exhibits s-trans conformation, whereas structure 1c exists in s-cis conformation, concerning the olefinic double bonds. In addition, the results show that the position of the nitro substituent attached to the aromatic B-ring has a direct effect on the molecular coplanarity of these compounds. The Hirshfeld surface analysis suggests that the non-covalent π-π stacking interactions are the most important contributors for the crystal packing of 1a and 1b. In 1c, the crystal packing is mainly stabilized by weak intermolecular C―H···O interactions due to the planar nature of the molecule.