RESUMEN
This study presents the metabolic profiling of potato powders obtained through various processing procedures and commercially available potato powders. The metabolic fingerprinting was conducted using 1H NMR-based metabolomics coupled with machine learning projections. The results indicate hot air-dried potatoes have higher fumarate, glucose, malate, asparagine, choline, gamma aminobutyric acid (GABA), alanine, lactate, threonine, and fatty acids. In comparison, steam-cooked potatoes have higher levels of phenylalanine, sucrose, proline, citrate, glutamate, and valine. Moreover, the contents of metabolites in processed potatoes in this study were higher than those found in commercial potato powders, regardless of the drying or cooking methods used. The results indicate that a new processing technique may be developed to improve the nutritional value of potatoes.
Asunto(s)
Solanum tuberosum , Solanum tuberosum/química , Polvos , Quimiometría , Espectroscopía de Resonancia Magnética/métodos , Glucosa , Metabolómica/métodosRESUMEN
Allobetulin is structurally similar tobetulinic acid, inducing the apoptosis of cancer cells with low toxicity. However, both of them exhibited weak antiproliferation against several tumor cell lines. Therefore, the new series of allobetulon/allobetulin-nucleoside conjugates 9a-10i were designed and synthesized for potency improvement. Compounds 9b, 9e, 10a, and 10d showed promising antiproliferative activity toward six tested cell lines, compared to zidovudine, cisplatin, and oxaliplatin based on their antitumor activity results. Among them, compound 10d exhibited much more potent antiproliferative activity against SMMC-7721, HepG2, MNK-45, SW620, and A549 human cancer cell lines than cisplatin and oxaliplatin. In the preliminary study for the mechanism of action, compound 10d induced cell apoptosis and autophagy in SMMC cells, resulting in antiproliferation and G0/G1 cell cycle arrest by regulating protein expression levels of Bax, Bcl-2, and LC3. Consequently, the nucleoside-conjugated allobetulin (10d) evidenced that nucleoside substitution was a viable strategy to improve allobetulin/allobetulon's antitumor activity based on our present study.
Asunto(s)
Antineoplásicos , Cisplatino , Antineoplásicos/farmacología , Apoptosis , Línea Celular Tumoral , Proliferación Celular , Cisplatino/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Nucleósidos/farmacología , Oxaliplatino/farmacología , Relación Estructura-ActividadRESUMEN
Fifteen betulonic/betulinic acid conjugated with nucleoside derivatives were synthesized to enhance antitumor potency and water solubility. Among these, the methylated betulonic acid-azidothymidine compound (8c) exhibited a broad-spectrum of antitumor activity against three tested tumor cell lines, including SMMC-7721 (IC50 = 5.02 µM), KYSE-150 (IC50 = 5.68 µM), and SW620 (IC50 = 4.61 µM) and along with lower toxicity (TC50 > 100 µM) estimated by zebrafish embryos assay. Compared to betulinic acid (<0.05 µg/mL), compound 8c showed approximately 40-fold higher water solubility (1.98 µg/mL). In SMMC-7721 cells, compound 8c induced autophagy and apoptosis as its concentration increased. Transcriptomic sequencing analysis was used to understand the potential impacts of the underlying mechanism of 8c on SMMC-7721 cells. Transcriptomic studies indicated that compound 8c could activate autophagy by inhibiting the PI3K/AKT pathway in SMMC-7721 cells. Furthermore, in the xenograft mice study, compound 8c significantly slowed down the tumor growth, as potent as paclitaxel treated group. In conclusion, methylated betulonic acid-azidothymidine compound (8c) not only increases water solubility, but also enhances the potency against hepatocellular carcinoma cells by inducing autophagy and apoptosis, and suppressing the PI3K/Akt/mTOR signaling pathway.
Asunto(s)
Antineoplásicos , Carcinoma Hepatocelular , Proliferación Celular , Neoplasias Hepáticas , Nucleósidos , Triterpenos , Humanos , Carcinoma Hepatocelular/tratamiento farmacológico , Carcinoma Hepatocelular/patología , Triterpenos/farmacología , Triterpenos/química , Triterpenos/síntesis química , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/síntesis química , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Hepáticas/patología , Animales , Ratones , Relación Estructura-Actividad , Proliferación Celular/efectos de los fármacos , Nucleósidos/farmacología , Nucleósidos/química , Nucleósidos/síntesis química , Pez Cebra , Ensayos de Selección de Medicamentos Antitumorales , Estructura Molecular , Apoptosis/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Transcriptoma/efectos de los fármacos , Línea Celular Tumoral , Ratones DesnudosRESUMEN
We developed a quantitative proton nuclear magnetic resonance (qNMR) with global spectral deconvolution (GSD) method to determine the gamma-aminobutyric acid content in Chinese yam with the proton signal at δH 2.30. Trimethylsilyl-2,2,3,3-tetradeuteropropionic acid sodium salt was set as the internal standard. The method was validated and showed admissible stability, repeatability, and precision. Compared to the traditional high-performance liquid chromatography method, this method did not involve tedious pre-treatment and expensive standard. Compared to ordinary qNMR, GSD algorithm could effectively remove the effect of noise, baseline distortions and signal overlapping. Overall, qNMR with GSD method is a rapid, simple and reliable method to quantitatively determine functional metabolites even overlapped with other compounds in herbs or foods.
Asunto(s)
Dioscorea , Espectroscopía de Protones por Resonancia Magnética , Protones , Espectroscopía de Resonancia Magnética/métodos , Cromatografía Líquida de Alta Presión/métodosRESUMEN
This study aimed to discover a simple, rapid, effective, inexpensive, and natural method to enhance the GABA content in edible rhizomes. To achieve this aim, edible rhizome samples were treated with different processing methods. Drying with hot air increased the GABA content in Chinese yam (CY) eight-fold compared with untreated CY. Drying with sunshine or hot air increased it 13- and 28-fold in taro root, respectively. These processing methods also produced an apparent increase in the GABA contents in other edible rhizome, such as lotus rhizomes, potatoes, and sweet potatoes. However, lyophilization did not affect the GABA content. Further, HPLC data showed that while GABA levels increased, glutamate levels decreased, indicating that GABA is produced by the catalytic action of glutamate decarboxylase on glutamate under drought conditions. Drying with hot air or sunshine to enhance the GABA content was not indicated in the literature.
Asunto(s)
Dioscorea , Rizoma , Desecación , Glutamato Descarboxilasa , Ácido gamma-AminobutíricoRESUMEN
This paper studies the degradation mechanism, the reaction kinetics and the toxicity of photolysis products of naproxen in waters under UV irradiation (120 W mercury lamp) by quenching experiments of reactive oxygen species (ROS), oxygen concentration experiment and toxicity evaluation using Vibrio fischeri bacteria. The results demonstrated that NPX could be degraded effectively by UV irradiation and the photolysis pathways was the sum of the degradation by direct photolysis and self-sensitization via ROS, and the contribution rates of self-sensitized photodegradation were 0.1%, 80.2%, 35.7% via *OH, (1)O2, O2*-, respectively. The effect of oxygen concentration illustrated that dissolved oxygen had an inhibitory effect on the direct photodegradation of NPX, and the higher the oxygen content, the more obvious the inhibitory effect. The toxicity evaluation illustrated the formation of some intermediate products that were more toxic than NPX during the photodegradation of NPX. The process of NPX degradation in all cases could be fitted by the pseudo first-order kinetics model.