Homoisoflavonoids from Caesalpinia spp.: A Closer Look at Chemical and Biological Aspects

Homoisoflavonoids are rare compounds distributed within a few families of plants including species from Fabaceae. The genus Caesalpinia, the main focus of this chapter, is a prolific source of these unique natural products. Homoisoflavonoids from Caesalpinia spp. are associated to ethnopharmacological uses for diverse purposes. In this sense, the following chapter sheds light on the occurrence, biosynthesis, isolation, synthesis, and structural analysis of these compounds from species of the genus Caesalpinia and their biological potential

Design and synthesis of new benzophenone derivatives with in vivo anti-inflammatory activity through dual inhibition of edema and neutrophil recruitment.

A series of novel benzophenone derivatives containing a thiazole heterocyclic nucleus were designed by molecular hybridization. Molecular docking studies have demonstrated the inhibitory potential of the designed compounds against cyclooxygenase (COX) isoenzymes. These compounds were synthesized, characterized, and evaluated for their anti-inflammatory properties by the croton oil-induced ear edema assay to examine their effect on both prostaglandin (PG) production and neutrophils recruitment. The thiazole derivatives displayed a potent effect in terms of reducing ear edema. The analysis suggested that the presence of 4-phenyl-2-hydrazinothiazole and the absence of C40 -OCH3 on the benzophenone derivative structure are strongly related to the inhibition of PG production. In addition, the derivatives 2e, 3a and 3c concomitantly inhibit PG production and neutrophil recruitment, which may be a mechanism of action better than of common NSAIDs due to their inability to inhibit the neutrophil recruitment. Thus, these compounds can be considered as potential lead compounds toward the development of new anti-inflammatory drugs with an innovating mechanism of actio

An Insight Into the Intraspecific Variation of Biosynthetic Gene Clusters Between Strains of Burkholderia thailandensis

The present study aimed to investigate the intraspecific variation of biosynthetic gene clusters (BGCs) in different strains of Burkholderia thailandensis in order to guide natural products (NPs) discovery process. Species from the genus Burkholderia are emerging as promising species due to their biosynthetic potential. Through genome-mining strategies, it was able to identify that B. thailandensis strains present major genome variation between chromosomes I and II and the standard. The positioning of BGCs also differs when comparing each chromosome. Classical pathways as well as terpene and bacteriocins were commonly identified to all of them and BGCs related to the production of nonribosomal peptides and polyketides compounds are often noticed. In addition, hybrids BGCs were identified as using large amount of replicon information. Among all species studied, the strain MSMB121 showed greater potential for biosynthesizing novel natural products and after phylogenetic analysis, the likelihood of recognizing sites of novelties was assigned

Measurement of vapor-liquid-equilibrium data and caloric data for the system ch3oh-hcl

The volatile oils from leaves of five Brazilian specimens of Swietenia macrophylla King (Meliaceae) collected in three different Amazon Rainforest Conservation Areas in the States of Mato Grosso, Pará, and Rondônia were extracted and analyzed by GC and GC/MS. The oils showed to be composed by terpenoids, majority hydrocarbon sesquiterpenes, being germacrene D (20.5-46.8%) and bicyclogermacrene (8.3-11.1%) the main components. Besides these derivatives, only α-cubebene, β-caryophyllene, β-gurjunene and γ-cadinene were detected in all of the analyzed samples. This analysis indicated a great diversity of constituents in the oils obtained from specimens collected in these regions, which could be associated to the different susceptibility in the attack of H. grandella in S. macrophylla cultures

Anti‐inflammatory activity of Lauraceae plant species and prediction models based on their metabolomics profiling data

The Lauraceae is a botanical family known for its anti‐inflammatory potential. However, several species have not yet been studied. Thus, this work aimed to screen the anti‐inflammatory activity of this plant family and to build statistical prediction models. The methodology was based on the statistical analysis of high‐resolution liquid chromatography coupled with mass spectrometry data and the ex vivo anti‐inflammatory activity of plant extracts. The ex vivo results demonstrated significant anti‐inflammatory activity for several of these plants for the first time. The sample data were applied to build anti‐inflammatory activity prediction models, including the partial least square acquired, artificial neural network, and stochastic gradient descent, which showed adequate fitting and predictive performance. Key anti‐inflammatory markers, such as aporphine and benzylisoquinoline alkaloids were annotated with confidence level 2. Additionally, the validated prediction models proved to be useful for predicting active extracts using metabolomics data and studying their most bioactive metabolites