Scales of Prochilodus magdalenae, a Colombian endemic fish species, were used to obtain chitosan for application as an antibacterial agent integrated into starch-based films. Analysis of its composition during the demineralization and deproteinization process indicated that minerals and protein were both removed successfully. At this point, mild conditions for the deacetylation process were employed, namely, 2, 4, and 6 wt.% NaOH at room temperature for 16 h. Chitosan processed under 2 wt.% NaOH had low molecular weight, with the lowest value of 107.18 ± 24.99 kDa, which was closely related to its antibacterial activity. Finally, this chitosan was integrated into a banana starch-based film, and its antibacterial activity was assayed in Escherichia coli and Staphylococcus aureus cultures, with positive results in the former culture, especially due to the low-molecular-weight characteristic of chitosan.
Bio-guided fractionation performed on the leaves-derived ethanol extract of Esenbeckia alata (Rutaceae), a plant used in traditional medicine, led to the isolation of two alkaloids, kokusaginine 1 and flindersiamine 2, as main cytotoxic agents. Primary ethanolic extract and raw fractions exhibited cell inhibition against five cancer cell lines at different levels (25–97% inhibition at 50 µg/mL) as well as isolated alkaloids 1–2 (30–90% inhibition at 20 µM). Although alkaloid 2 generally was the most active compound, both alkaloids showed a selective effect on K562, a human chronic myelogenous leukemia cell line. The E1-like ubiquitin-activating enzymes (e.g., UBA5) have been recently described as important targets for future treatment of cancer progression, such as leukemia, among others. Therefore, as a rationale to the observed cytotoxic selectivity, an in-silico evaluation by molecular docking and molecular dynamics was also explored. Compounds 1–2 exhibited good performance on the interaction within the active site of UBA5.
Plant materials (i.e., leaves, fruits, and seeds) from 40 trees of Azadirachta indica A. Juss. were collected from six different locations across the Colombian Caribbean coast. Eighty-four ethanolic extracts were prepared and the total limonoid contents (TLiC) and the antifungal activity against Fusarium oxysporum conidia were measured. Their chemical profiles were also recorded via liquid chromatography-electrospray ionization interface-mass spectrometry (LC-ESI-MS) analysis and the top-ranked features were then annotated after supervised multivariate statistics. Inter-location chemical variability within sample set was assessed by sparse partial least squares discriminant analysis (sPLS-DA) and the chemical profiles and biological activity datasets were integrated through single-Y orthogonal partial least squares (OPLS) to identify antifungal bioactives in test extracts. The TLiC and antifungal activity (IC50 values) of the A. indica-derived extracts were found to be ranging from 4.5 to 48.5 mg limonin equivalent per g dry extract and 0.08–44.8 μg/mL, respectively. The presence/abundance of particular limonoids between collected samples influenced the variability among locations. In addition, the integration of chemical and antifungal activity datasets showed five features as markers probably contributing to the bioactivity, annotated as compounds with an azadirone-like moiety. To validate the information provided by the single-Y OPLS model, a high performance liquid chromatography (HPLC)-based microfractionation was then carried out on an active extract. The combined plot of chromatographic profile and microfraction bioactivity also evidenced five signals possessing the highest antifungal activity. The most active limonoid was identified as nimonol 1. Hence, this untargeted metabolite profiling was considered as a convenient tool for identifying metabolites as inter-location markers as well as antifungals against Fusarium oxysporum.
Two undescribed 4′-O-methylkaempferol-[3″,4″-di-p-coumaroyl]-α-l-rhamnopyranosides, caerulines
A and B (1–2), along with three known 4′-O-methylkaempferol diacylrhamnosides isomers (3–5) were isolated from an ethanol extract of the leaves of Persea caerulea, a native plant growing on the Colombian
Caribbean coast. The chemical structures of 1 and 2 were elucidated by spectroscopic methods. The effect of
compounds 1–5 against four pathogenic microorganisms
[i.e., methicillin-resistant Staphylococcus aureus (MRSA), Acinetobacter baumannii, Candida albicans, and Aspergillus
fumigatus] was tested in vitro. The
compounds exhibited no activity against these pathogens except MRSA
(MIC 12–48 μg/mL). Caeruline B (2) was found
to be the most active compound with a modest anti-MRSA activity (MIC
= 12 μg/mL).
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