Terpenes reduced the pro-inflammatory cytokines TNF-α and IL-1α and increased the production of IL-10. In addition, the terpenes, especially guaiene (53.3 ± 2.4%) and m-cymene (38.1 ± 0.6%), significantly inhibited NO production in a macrophage cell culture-based assay, whereas no effect was observed in the scavenging activity of this radical. L-carveol and m-cymene significantly inhibited O production with reductions of approximately 68.6 ± 2.2% and 48.2 ± 4.2%, respectively, at a concentration of 10 μM. Moreover, these terpenes were verified to suppress NF-κB activity. The results indicate that these terpenes have therapeutic potential and may be used to suppress inflammatory diseases or as a leading compounds.
Background:
Amaryllidaceae plants are known to be a great source of alkaloids, which are considered
an extensive group of compounds encompassing a wide range of biological activities. The remarkable
cytotoxic activities observed in most of the Amaryllidaceae alkaloids derivatives have prompt the chemical and
biological investigations in unexplored species from Brazil.
Objective:
To evaluate the cytotoxic and genotoxic properties of alkaloids of Griffinia gardneriana and Habranthus
itaobinus bulbs and study the role of caspase-3 as a molecular apoptosis mediator.
Methods:
Methanolic crude extracts of Griffinia gardneriana and Habranthus itaobinus bulbs were submitted to
acid-base extraction to obtain alkaloid-enriched fractions. The obtained fractions were fractionated using chromatographic
techniques leading to isolation and identification of some alkaloids accomplished via HPLC and
1H-NMR, respectively. Molecular docking studies assessed the amount of free binding energy between the isolated
alkaloids with the caspase-3 protein and also calculated the theoretical value of Ki. Studies have also been
developed to evaluate in vitro cytotoxicity and genotoxicity in such alkaloids and apoptosis activation via the
caspase pathway using both tumor and normal cell lines.
Results:
Seven alkaloids were isolated and identified. Among these, 11-hydroxyvittatine and 2-α-7-
dimethoxyhomolycorine were not cytotoxic, whereas tazettine, trisphaeridine, and sanguinine only showed
activity against the fibroblast lineage. Lycorine and pretazettine were 10 to 30 folds more cytotoxic than the
other alkaloids, including cancerous lines, and were genotoxic and capable of promoting apoptosis via the
caspase-3 pathway. This result supports data obtained in docking studies wherein these two compounds exhibited
the highest free energy values.
Conclusion:
The cytotoxicity assay revealed that, among the seven alkaloids isolated, only lycorine and pretazettine
were active against different cell lines, exhibiting concentration- and time-dependent cytotoxic actions
alongside genotoxic action and the ability to induce apoptosis by caspase-3, a result consistent with those obtained
in docking studies.
Vegetable oils have been used for a plethora of health benefits by their incorporation in foods, cosmetics, and pharmaceutical products, especially those intended for skin care. This study aimed to investigate the cutaneous benefits of a vegetable oil blend (VOB) formulation and its fatty acid composition. The anti-inflammatory activity was studied in macrophages of RAW 264.7 cells by investigating the release of nitric oxide (NO), superoxide anion generation (O
2
-
), tumor necrosis factor-alpha (TNF-α), and interleukin 6 (IL-6). ABTS cation radical scavenging capacity assay, ferric reducing antioxidant potential (FRAP), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and NO free radical scavenging assays were used to evaluate the antioxidant activity. VOB was tested for its ability to stimulate fibroblast proliferation and migration using the scratch assay, and antibacterial activity by the microdilution test. The fatty acid profile of a freshly prepared VOB formulation was determined by gas chromatography before and after accelerated stability testing. Chemical composition of VOB revealed the presence of oleic acid (C18:1n-9; 63.3%), linoleic acid (C18:2n-6; 4.7%), and linolenic acid (C18:3n-6; 5.1%) as major mono- and polyunsaturated fatty acids. No changes in the organoleptic characteristics and fatty acid composition were observed after the accelerated stability test. VOB 100 µg/mL reduced the healing time by increasing the total number of cells in the wounded area by 43.0±5.1% compared to the negative control group. VOB also suppressed the pro-inflammatory TNF-α and IL-6 cytokines, and NO and O
2
-
production in lipopolysaccharide-stimulated macrophage cells. In conclusion, the VOB formulation contributed to the improvement of current therapeutic strategies for cutaneous applications in skin care.
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