RESUMEN
Curcuma wenyujin, as one of the eight Daodi-herbs in Zhejiang province, is widely used. It has the effects of eliminating stasis and dissipating mass, moving Qi and activating blood, and clearing heart and relieving depression. Modern studies have shown that it has anti-tumor, anti-inflammatory, anti-oxidation, anti-thrombus and liver-protecting effects and mainly contains sesquiterpenoids, monoterpenoids, diterpenoids, and curcumins. This paper reviews the research progress in the chemical constituents and pharmacological effects of C. wenyujin in the last decade, discusses the modern clinical applications combined with the traditional efficacy, and predicts its quality markers(Q-markers) from plant consanguinity, medicinal properties, efficacy, processing and measurability of chemical components based on the theory of Q-markers, so as to provide a reference for the establishment of a scientific quality evaluation system and the research and application of this herb in the future.
Asunto(s)
Curcuma , Antiinflamatorios , Curcuma/química , HígadoRESUMEN
Paclitaxel is highly effective at killing many malignant tumors; however, the development of drug resistance is common in clinical applications. The issue of overcoming paclitaxel resistance is a difficult challenge at present. In this study, we developed nano drugs to treat paclitaxel-resistant lung adenocarcinoma. We selected cabazitaxel and ß-elemene, which have fewer issues with drug resistance, and successfully prepared cabazitaxel liposome, ß-elemene liposome and cabazitaxel-ß-elemene complex liposome with good flexibility. The encapsulation efficiencies of cabazitaxel and ß-elemene in these liposomes were detected by precipitation microfiltration and microfiltration centrifugation methods, respectively. Their encapsulation efficiencies were all above 95%. The release rates were detected by a dialysis method. The release profiles of cabazitaxel and ß-elemene in these liposomes conformed to the Weibull equation. The release of cabazitaxel and ß-elemene in the complex liposome were almost synchronous. The pharmacodynamics study showed that cabazitaxel flexible liposome and ß-elemene flexible liposome were relatively good at overcoming paclitaxel resistance on paclitaxel-resistant lung adenocarcinoma. As the flexible complex liposome, the dosage of cabazitaxel could be reduced to 25% that of the cabazitaxel injection while retaining a similar therapeutic effect. It showed that ß-elemene can replace some of the cabazitaxel, allowing the dosage of cabazitaxel to be reduced, thereby reducing the drug toxicity.
Asunto(s)
Resistencia a Antineoplásicos , Liposomas , Sesquiterpenos/administración & dosificación , Sesquiterpenos/farmacocinética , Taxoides/administración & dosificación , Taxoides/farmacocinética , Adenocarcinoma del Pulmón/tratamiento farmacológico , Adenocarcinoma del Pulmón/patología , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/química , Antineoplásicos/farmacocinética , Protocolos de Quimioterapia Combinada Antineoplásica , Línea Celular Tumoral , Modelos Animales de Enfermedad , Humanos , Liposomas/química , Ratones , Estructura Molecular , Paclitaxel/farmacología , Tamaño de la Partícula , Sesquiterpenos/química , Taxoides/química , Carga Tumoral/efectos de los fármacos , Ensayos Antitumor por Modelo de XenoinjertoRESUMEN
The chemical compositions of Anemone raddeana Rhizome, a kind of traditional Chinese medicine, were reviewed, along with its bioactivity and pharmacological properties and method improvements of extracting and detecting triterpenoid saponins. A. raddeana Rhizome is used to treat neuralgia and rheumatism, and is rich in triterpenoid saponins, most of which are pentacyclic, with oleanane as the nucleus. So far, 37 triterpenoid saponins have been determined from the herb. Its reported bioactivity and pharmacological properties have been described as anticancerous, antimicrobial, anti-inflammatory, analgesic, antipyretic, anticonvulsive, antihistaminic, and sedative. It has also been used for the induction of the humoral immune response and treatment of liver fibrosis in chronic hepatitis. However, the herb also has hemolytic effects and can be toxic, which limits its clinical application. Further studies are needed on the pharmaceutical functions, mechanisms, and immunological responses to contribute to the herb's clinical applications.
Asunto(s)
Anemone/química , Extractos Vegetales/farmacología , Animales , Humanos , Fitoquímicos/química , Fitoquímicos/farmacología , Extractos Vegetales/química , Rizoma/químicaRESUMEN
OBJECTIVE: To study the fingerprint of Zedoary Turmeric Oil (ZTO) as the bulk drug of Kingkong Elemene for making it safe, effective, stable, and controllable. METHODS: Fingerprints were detected by gas chromatography. ß-elemene peak was regarded as reference peak (S). The relative peak area of each common peak and the relative retention time were calculated. With a total of modes for reference, the fingerprints of 10 batches of Kingkong ZTO were detected, and their similarity was calculated by traditional Chinese medicine (TCM) fingerprint similarity calculation software. RESULTS: The determination method was stable and reliable. Totally 19 common characteristic peaks of Kingkong ZTO was found. The fingerprint similarity of these batches of Kingkong ZTO were not lower than 0.96. CONCLUSIONS: Gas chromatography for detecting the fingerprint of Kingkong ZTO was reliable and repeatable. The established fingerprint of Kingkong ZTO could guarantee the quality stability and safety of different product batches.
Asunto(s)
Curcuma/química , Aceites de Plantas/química , Sesquiterpenos/química , Cromatografía de Gases , Medicamentos Herbarios Chinos/químicaRESUMEN
Chitosan nanoparticles are good drug carriers because of their good biocompatibility and biodegradability, and can be readily modified. As a new drug delivery system, they have attracted increasing attention for their wide applications in, for example, loading protein drugs, gene drugs, and anticancer chemical drugs, and via various routes of administration including oral, nasal, intravenous, and ocular. This paper reviews published research on chitosan nanoparticles, including its preparation methods, characteristics, modification, in vivo metabolic processes, and applications.
Asunto(s)
Quitosano/administración & dosificación , Quitosano/química , Sistemas de Liberación de Medicamentos/métodos , Nanopartículas/administración & dosificación , Nanopartículas/química , Animales , HumanosRESUMEN
The production of a thermophilic 2-deoxyribose-5-phosphate aldolases (DERA) in Escherichia coli BL21 under continuous lactose induction strategy was investigated. The process was combined with the exponential feeding method, controlling the feeding rate to maintain the specific growth rate at 0.15 h(-1). The results indicate that the lactose concentration in the feed medium affected directly the expression of the target protein. The use of 50 g/L in the feed medium resulted in the biomass concentration of 39.3 g DCW/L, and an expression level of above 30%, and the maximum final DERA concentration of 16,200 U/L. Furthermore, the acetate concentration remained at a low level in the fed-batch phase, less than 0.5 g/L. In conclusion, combining glucose feeding with lactose induction is a more powerful way to achieve high cell density cultures and to efficiently produce the thermophilic DERA. The results also indicate the potential industrial utility in the scale production of other recombinant proteins.
Asunto(s)
Aldehído-Liasas/biosíntesis , Escherichia coli/genética , Lactosa , Proteínas Recombinantes/biosíntesis , Activación Transcripcional/efectos de los fármacos , Aldehído-Liasas/genética , Biomasa , Reactores Biológicos , Escherichia coli/enzimología , Fermentación , Glucosa/metabolismo , Calor , Microbiología Industrial , Lactosa/metabolismo , Lactosa/farmacología , Operón , Plásmidos , Proteínas Recombinantes/genética , Transformación BacterianaRESUMEN
Due to their small particle size and large and modifiable surface, nanoparticles have unique advantages compared with other drug carriers. As a research focus in recent years, polyethylene glycol-polylactic acid (PEG-PLA) block copolymer and its end-group derivative nanoparticles can enhance the drug loading of hydrophobic drugs, reduce the burst effect, avoid being engulfed by phagocytes, increase the circulation time of drugs in blood, and improve bioavailability. Additionally, due to their smaller particle size and modified surface, these nanoparticles can accumulate in inflammation or target locations to enhance drug efficacy and reduce toxicity. Recent advances in PEG-PLA block copolymer nanoparticles, including the synthesis of PEG-PLA and the preparation of PEG-PLA nanoparticles, were introduced in this study, in particular the drug release and modifiable characteristics of PEG-PLA nanoparticles and their application in pharmaceutical preparations.
Asunto(s)
Nanopartículas/administración & dosificación , Nanopartículas/química , Polietilenglicoles/administración & dosificación , Polietilenglicoles/química , Animales , Sistemas de Liberación de Medicamentos , HumanosRESUMEN
OBJECTIVE: To prepare tegafur magnetic long-circulating thermosensitive liposomes and study its pharmacokinetics and targeting properties in rats. METHODS: Tegafur magnetic long-circulating thermosensitive liposomes were prepared by reversed phase-ultrasound method and its concentration in various organs of rats were detected with high-performance liquid chromatography. RESULTS: The average size of tegafur magnetic long-circulating thermosensitive liposomes was about 126 nm, which showed strong ferromagnetism and superparamagnetism. Eight hours after administration in rats, the AUC value of tegafur magnetic long-circulating thermosensitive liposome in the liver was 17.4 times of that of the free drug, and 3.9 times of that of tegafur long-circulating liposome. The concentrations of the thermosensitive liposome in the serum and kidney were lower than those of the free drug, with a liver-targeting ratio reaching 73.9% and obviously prolonged half-life than the free drug. CONCLUSION: Tegafur complex liposome can obviously increase the drug concentration in the liver and decrease the nephrotoxicity of the drug in rats.
Asunto(s)
Sistemas de Liberación de Medicamentos , Liposomas/farmacocinética , Hígado/metabolismo , Magnetismo , Tegafur/farmacocinética , Animales , Femenino , Masculino , Nanopartículas , Distribución Aleatoria , Ratas , Ratas Wistar , Distribución TisularRESUMEN
OBJECTIVE: To prepare a stable water-based magnetic fluid. METHODS: A water-based magnetic fluid was prepared by addition of polyvinylpyrrolidone (PVP) as the coating agent for the magnetic particles. After preparation of Fe3O4 by co-precipitation method, PVP was added for its coating, followed by ultrasonic agitation and purification. RESULTS: The magnetic nanoparticles of homogeneously small size and water-based magnetic fluid were obtained, which had good dispersion in water with strong magnetism. CONCLUSION: PVP can be used as a surfactant to stabilize the magnetic fluid.