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In this study, we report on the isolation, purification, and anti-inflammatory evaluation of compounds from the plant species Ageratina pichinchensis. Using open-column chromatography, 11 known compounds were purified, which chemical structures were elucidated by nuclear magnetic resonance techniques (1D and 2D). All compounds were evaluated in an in vitro model of RAW 264.7 mouse macrophage cells, measuring the nitric oxide inhibition to determine the anti-inflammatory effect. The compound betuletol 3-O-β-glucoside (11) inhibited nitric oxide with a half-maximal inhibitory concentration (IC50) of 75.08 ± 3.07% at 75 µM; additionally, it inhibited the secretion of interleukin 6 (IL-6) and activation of the nuclear factor (NF-kβ). These results suggest that the anti-inflammatory effect attributed to A. pichinchensis species is promoted by compound 11, which could be considered a potential anti-inflammatory agent by suppressing the expression of NF-kβ target genes, such as those involved in the proinflammatory pathway and inducible nitric oxide synthase (iNOS). [ABSTRACT FROM AUTHOR]

Multidrug resistance (MDR) has become a major obstacle in the treatment of cancer, and is associated with mechanisms such as increased drug outflow, reduction of apoptosis, and/or altered drug metabolism. These problems can be mitigated by the coadministration of agents known as chemosensitizers, as they can reverse resistance to anticancer drugs and eventually resensitize cancer cells. We explore the chemosensitizing effect of Achillin, a guaianolide-type sesquiterpene lactone isolated from the Mexican medicinal plant Artemisia ludovisiana, to reverse MDR in Hep3B/PTX cells of hepatocellular carcinoma, which present resistance to paclitaxel (PTX). Achillin showed an important effect as chemosensitizer; indeed, the cytotoxic effect of PTX (25 nM) was enhanced, and the induction of G2/M phase cell cycle arrest and apoptosis were potentiated when combining with Achillin (100 μM). In addition, we observed that Achillin decreases P-gp levels and increases the intracellular retention of doxorubicin in Hep3B/PTX cells; in addition, homology structural modeling and molecular docking calculations predicted that Achillin interacts in two regions (M-site and R-site) of transporter drug efflux P-glycoprotein (P-gp). Our results suggest that the chemosensitizer effect demonstrated for Achillin could be associated with P-gp modulation. This work also provides useful information for the development of new therapeutic agents from guaianolide-type sesquiterpene lactones like Achillin. [ABSTRACT FROM AUTHOR]

Acmella radicans (Asteraceae) is a plant native to America. Despite it having medicinal attributes, studies on its phytochemical properties are scarce, and biotechnological studies do not exist for this species. In this study, we established an adventitious root culture from A. radicans internodal segments in shake flasks with indole-3-butyric acid (IBA), and then elicited it with jasmonic acid (JA) and salicylic acid (SA). The total phenolic content and antioxidant activity were evaluated, and a comparison was made using in vitro plantlets and wild plants. Internodal segments with 0.1 mg/L IBA showed 100% root induction and exhibited better growth after transfer to shake flasks with MS liquid culture medium. JA had a significant effect on biomass increase compared to unelicited roots, mainly with 50 µM JA (28%), while SA did not show significant results. Root elicited with 100 µM (SA and JA) showed a 0.34- and 3.9-fold increase, respectively, in total phenolic content (TPC) compared to the control. The antioxidant activity was also significant, and a lower half-maximal inhibitory concentration (IC 50 ) was observed as the AJ concentration increased. Roots elicited with AJ (100 µM) exhibited high antioxidant activity with DPPH (IC 50 = 9.4 µg/mL) and ABTS (IC 50 = 3.3 µg/mL) assays; these values were close to those for vitamin C (IC 50 = 2.0 µg/mL). The TPC and antioxidant activity of in vitro plants and root cultured in shake flasks showed the lowest values in most cases; even the root cultures without elicitation were better than those of a wild plant. In this study, we demonstrated that A. radicans root culture is capable of producing secondary metabolites, while its production and antioxidant activity can be enhanced using jasmonic acid.