RESUMEN
Background: Chemotherapy drugs can cause drug resistance and other problems when treating lung cancer, which leads to treatment failure. Ursolic acid (UA) is used in formulations based on traditional Chinese medicine. UA has excellent anti-tumor effects, but they are limited by solubility and non-specificity to tumor cells. Objectives: To overcome these issues, we created a novel hyaluronic acid (HA)-targeted liposome system for delivering UA (HA-Lipo/UA) to explore the targeting and anti-tumor effects of UA. Methods: We constructed the HA-Lipo/UA delivery system by the thin film hydration method. The uptake and localization of UA were detected by flow cytometry and microscope. Cell proliferation of A549 cells was detected by MTT assays. Apoptosis and reactive oxygen species (ROS) expression of A549 cells were also evaluated after being treated with HA-Lipo/UA. Western blot analysis evaluated the anti-tumor mechanism of HA-Lipo/UA. Results: HA-Lipo/UA exhibited favorable targeting of the cluster of differentiation (CD)44-overexpressing A549 cells. HA-Lipo/UA exhibited significant inhibition of the proliferation of A549 cells and induced their apoptosis compared with the corresponding monotherapies. HA-Lipo/UA induced overexpression of reactive oxygen species and upregulated expression of p53 and apoptosis-related protein in the transforming growth factor-ß signaling (ARTS) pathway, which induced cytochrome-c release, activation of caspase-3, and promoted mitochondrial apoptosis in A549 cells. Conclusions: Taken together, these data suggested that HA-Lipo/UA could be used to target tumor cells.
RESUMEN
Litsea pungens is a plant with medicinal and edible properties, where the fruits are edible and the leaves have medicinal properties. However, there is limited research on the chemical and pharmacological activities of the plant. In this study, essential oils were extracted by steam distillation and their antioxidant and antibacterial activities were further evaluated. Gas chromatography-mass spectrometry (GC-MS) was used to identify the chemical components of L. pungens fresh fruit essential oil (FREO) and L. pungens fresh flower essential oil (FLEO), rapeseed oil (RO) and commercial Litsea oil (CEO). The results showed that 12 chemical components were identified in FREO. Twelve chemical components were identified from FLEO, four chemical components were identified from CEO, and thirteen chemical components were identified from RO. Except for RO, the other three oils were mainly composed of terpenes, among which limonene is the main chemical component. In terms of antioxidant activity, FREO, FLEO, CEO and RO have antioxidant capacity, mainly reflected in the scavenging DPPH free radicals and the iron ion chelating ability, and the antioxidant activity shows a certain dose effect, but the antioxidant activity of FLEO is the weakest among the four oils. Meanwhile, under the stress of hydrogen peroxide, CEO demonstrated a significant antioxidant protective effect on cells. It is worth mentioning that compared with the positive control, the FREO exhibited a better antibacterial rate. When the concentration of essential oil is 20 mg/mL, the bacteriostatic rate can reach 100%. Therefore, it could be a promising candidate among medicinal and edible plants.