Pentacyclic triterpenes as bioactive compounds isolated from Mauritia flexuosa L. f. acting against the Alzheimer's disease.

Alzheimer's disease is a significant concern due to its high prevalence and the limitations of current treatments. In our research, we investigated Mauritia flexuosa, a medicinal plant traditionally used for headaches, to identify active compounds with potential anti-Alzheimer's effects. Three pentacyclic triterpenes were isolated through column chromatography and characterised from the dichloromethane/methanol extract from Mauritia flexuosa (DCMEMf), with (3ß)-3-hydroxy-11-oxours-12-en-28-oic acid (3) showing the highest in vitro activity in the HMC3 and SVG p12 cell lines. Compound 3 inhibited the pharmacological targets NF-κB, PGE2, IDO1, and EGFR with IC50 values of 9.83, 3.86, 1.63 µM, and 49.57 nM, respectively, attributed to a hydroxyl group at the C-3 position of its structure. These findings suggest the potential of these compounds in treating neurological diseases, including headaches, and offer promising prospects for the development of new therapies against Alzheimer's.

Study of Pentacyclic Triterpenes from Lyophilised Aguaje: Anti-Inflammatory and Antioxidant Properties.

Mauritia flexuosa (M. flexuosa), commonly known as Aguaje or Moriche palm, is traditionally recognised in South America for its medicinal properties, particularly for its anti-inflammatory and antioxidant effects. However, the bioactive compounds responsible for these effects have not been thoroughly investigated. This study aims to isolate and characterise pentacyclic triterpenoid compounds from M. flexuosa and to evaluate their therapeutic potential. Using various chromatographic and spectroscopic techniques including Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS), three pentacyclic triterpenoid compounds were successfully isolated. Among them, compound 1 (3,11-dioxours-12-en-28-oic acid) exhibited notable bioactivity, significantly inhibiting the activation of Nuclear Factor kappa-light-chain-enhancer of activated B cells (NF-κB) (IC50 = 7.39-8.11 µM) and of Nitric Oxide (NO) (IC50 = 4.75-6.59 µM), both of which are key processes in inflammation. Additionally, compound 1 demonstrated potent antioxidant properties by activating the antioxidant enzyme Superoxide Dismutase (SOD) (EC50 = 1.87 µM) and the transcription factor Nuclear factor erythroid 2-related factor 2 (Nrf2) (EC50 = 243-547.59 nM), thus showing its potential in combating oxidative stress. This study is the first to isolate and characterise the three compounds from M. flexuosa, suggesting that compound 1 could be a promising candidate for the development of safer and more effective therapies for inflammatory and oxidative stress-related diseases.

Anti-Inflammatory, Antibacterial, Anti-Biofilm, and Anti-Quorum Sensing Activities of the Diterpenes Isolated from Clinopodium bolivianum.

This study reports for the first time the isolation of four diterpenoid compounds: 15-Hydroxy-12-oxo-abietic acid (1), 12α-hydroxyabietic acid (2), (-)-Jolkinolide E (3), and 15-Hydroxydehydroabietic acid (4) from Clinopodium bolivianum (C. bolivianum). The findings demonstrate that both the dichloromethane/methanol (DCMECB) extract of C. bolivianum and the isolated compounds exhibit significant anti-inflammatory (inhibition of NF-κB activation), antibacterial (primarily against Gram-positive bacteria), and anti-biofilm (primarily against Gram-negative bacteria) activities. Among the isolated diterpenes, compounds 3 and 4 showed notable anti-inflammatory effects, with IC50 values of 17.98 µM and 23.96 µM for compound 3, and 10.79 µM and 17.37 µM for compound 4, in the HBEC3-KT and MRC-5 cell lines. Regarding their antibacterial activity, compounds 3 and 4 were particularly effective, with MIC values of 0.53-1.09 µM and 2.06-4.06 µM, respectively, against the S. pneumoniae and S. aureus Gram-positive bacteria. Additionally, these compounds demonstrated significant anti-biofilm and anti-quorum sensing activities, especially against Gram-negative bacteria (H. influenzae and L. pneumophila). We also explain how compound 3 (BIC = 1.50-2.07 µM, Anti-QS = 0.31-0.64 µM) interferes with quorum sensing due to its structural homology with AHLs, while compound 4 (BIC = 4.65-7.15 µM, Anti-QS = 1.21-2.39 µM) destabilises bacterial membranes due to the presence and position of its hydroxyl groups. These results support the traditional use of C. bolivianum against respiratory infections caused by both Gram-positive and Gram-negative bacteria. Furthermore, given the increasing antibiotic resistance and biofilm formation by these bacteria, there is a pressing need for the development of new, more active compounds. In this context, compounds 3 and 4 isolated from C. bolivianum offer promising potential for the development of a library of new, more potent, and selective drugs.