ABSTRACT
ObjectiveTo optimize the extraction and purification process of Gardeniae Fructus for industrial production， and to obtain the total iridoid and total crocin extracts. MethodOrthogonal test was used to optimize the water extraction process by taking contents of geniposide， genipin gentiobioside， gardenoside， crocin-1 and crocin-2 as indicators and the decocting time， decocting times and water amount as factors. The purification process was optimized by single factor test， and four different types of macroporous adsorption resins were screened. The process conditions such as resin type， maximum loading amount， water washing amount， ethanol concentration， ethanol dosage， and flow rate of sample loading were mainly investigated. In addition， the drying methods （vacuum drying and spray drying） of the extract were investigated， and a pilot scale-up verification test was carried out. ResultThe optimal water extraction process of Gardeniae Fructus was to add 15， 10 times the amount of water for decocting twice， 1 h each time. The optimal purification process was as follows：the water extract through SP825L macroporous resin column， the amount of crude drug-the amount of resin （1∶1.5）， the sample loading flow rate of 3 BV h-1， adding 2 BV of water to remove impurities， adding 4 BV of 30% ethanol to obtain the iridoid part， then adding 3 BV of 70% ethanol to obtain the crocin part， collecting the ethanol lotion， and drying at 70 ℃. Under these conditions， the extraction amount of total iridoids was 590.75 mg·g-1 with the transfer rate of 70.48%， and the yield of dry extract was 8.89%. The extraction amount of total crocins was 83.37 mg·g-1 with the transfer rate of 22.20%， and the dry extract yield was 2.60%. ConclusionThe optimized extraction and purification process is stable and feasible with high extraction rate of active components， which is suitable for the industrial extraction and purification of active parts of Gardeniae Fructus.
ABSTRACT
Zexietang is derived from Jingui Yaolue （《金匮要略》）， which is composed of Alismatis Rhizoma and Atractylodis Macrocephalae Rhizoma， and has the effect of inducing diuresis and invigorating the spleen to produce water. Compared with western medicine in the treatment of related diseases， Zexietang can not only improve the curative effect， but also reduce the occurrence of adverse reactions， so as to achieve long-term stable administration. The authors sorted out and analyzed the chemical composition， pharmacological effect and clinical application of Zexietang in recent years. It was found that the main active components of Zexietang were alismol A and B， 23-acetyl-alismol B and C， atractylenolides （atractylenolide Ⅰ， Ⅱ， Ⅲ） and polysaccharides. Pharmacological experiments showed that they had diuretic， hypolipidemic， anti-inflammatory and others. And it can be used in the treatment of hypertension， hyperlipidemia， vertigo， cerebral vascular insufficiency and other diseases combined with other Chinese materia medica， and the curative effect is obvious. By summarizing the research status of Zexietang in recent years， its active components and pharmacological mechanism can be further clarified， which provides the basis for the clinical application of Zexietang and guides the direction of its further research.
ABSTRACT
The small size， moderate drug loading， and targeting properties of nano-preparations make them can be excellent delivery tools for drugs， genes or proteins crossing the cell or blood-brain barrier （BBB）. Currently， facilitating drug crossing BBB with innovative nano-drug delivery systems is considered as a strategic approach for the prevention， diagnosis and treatment of central nervous system （CNS） diseases. However， with the deepening of the research， the adverse reactions and toxicity of nanocarriers have gradually attracted the attention of researchers. Based on this， this paper summarized the situation of BBB-penetrating targeted nano-preparations at home and abroad in recent years from the perspective of classification of types and properties of nanocarriers， and analyzed the advantages and disadvantages of each carrier. The results showed that nano-preparations with active ingredients of traditional Chinese medicine （TCM） as carriers have become a promising way of cancer treatment， but the complexity and diversity of TCM components limited its application to a certain extent. Further studies should be strengthened to lay a foundation for the application and development of TCM nano-preparations in the field of CNS diseases.
ABSTRACT
The paclitaxel-loaded and folic acid-modified poly(lactic-co-glycolic acid) nano-micelles(PTX@FA-PLGA-NMs) were prepared by the emulsion solvent evaporation method, and the parameters of paclitaxel-loaded nano-micelles were optimized with the particle size and PDI as evaluation indexes. The morphology of the nano-micelles was observed by transmission electron microscopy(TEM), and the stability, drug loading and encapsulation efficiency were systematically investigated. In vitro experiments were performed to study the cytotoxic effects of nano-micelles, apoptosis, and cellular uptake. Under the optimal parameters, the nano-micelles showed the particle size of(125.3±1.2) nm, the PDI of 0.086±0.026, the zeta potential of(-20.0±3.8) mV, the drug loading of 7.2%±0.75%, and the encapsulation efficiency of 50.7%±1.0%. The nano-micelles were in regular spherical shape as observed by TEM. The blank FA-PLGA-NMs exhibited almost no inhibitory effect on the proliferation and growth of tumor cells, while the drug-loaded nano-micelles and free PTX exhibited significant inhibitory effects. The IC_(50) of PTX@FA-PLGA-NMs and PTX was 0.56 μg·mL~(-1) and 0.66 μg·mL~(-1), respectively. The paclitaxel-loaded nano-micelles were potent in inhibiting cell migration as assessed by the scratch assay. PTX@FA-PLGA-NMs had good pro-apoptotic effect on cervical cancer HeLa cells and significantly promoted the uptake of HeLa cells. The results of in vitro experiments suggested that PTX@FA-PLGA-NMs could target and treat cervical cancer HeLa cells. Therefore, as nanodrug carriers, PTX@FA-PLGA-NMs with anti-cancer activity are a promising nano-system for improving the-rapeutic effects on tumors.
Subject(s)
Female , Humans , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Drug Carriers , Folic Acid , Glycolates , HeLa Cells , Micelles , Paclitaxel , Particle Size , Uterine Cervical Neoplasms/drug therapyABSTRACT
Objective To explore risk factors for healthcare-associated pneumonia (HAP) caused by carbapenemresistant Enterobacter cloacae (CREC) in patients in intensive care unit (ICU).Methods From July 2013 to June 2017, 64 patients with CREC-HAP in ICU of a hospital were collected as case group, and 64 patients with carbapenem-sensitive Enterobacter cloacae HAP (CSEC-HAP) were as control group, risk factors for the occurrence of CREC-HAP were analyzed retrospectively by 1∶1 matched case-control study.Results Univariate analysis showed that APACHE II score≥20, long length of ICU stay, use of ventilator, long length of ventilator use, use of carbapenems, long duration of antimicrobial use, and at least 2 kinds of antimicrobial agents combined use were associated with the occurrence of CREC-HAP (all P＜0.05).Multivariate logistic regression analysis showed that APACHE II score≥20, use of ventilator, long length of ventilator use, use of carbapenems, and long duration of antimicrobial use were independent risk factors for occurrence of CREC-HAP (all P＜0.05).Conclusion Risk factors for occurrence of CREC-HAP in ICU patients include the use of carbapenems, long length of ventilator use, long duration of antimicrobial use, and APACHE II score≥20.Effective preventive and control measures can be formulated and taken in view of the above risk factors.
ABSTRACT
<p><b>OBJECTIVE</b>To observe the effect of nitrotyrosine on renal expressions of nuclear factor-κB (NF-κB), monocyte chemoattractant protein-1 (MCP-1), and transforming growth factor-β1 (TGF-β1) in rats with diabetic nephropathy (DN).</p><p><b>METHODS</b>Rat DN models established by a single intraperitoneal injection of streptozotocin (STZ) were randomly allocated into model group, nitrotyrosine group and ebselen group, with untreated rats as the normal control group. The rats were given the corresponding drugs for 8 weeks, and after the last administration, the 24-h urinary protein level was measured and the kidneys of the rats were harvested for detecting the protein and mRNA expressions of NF-κB, MCP-1 and TGF-β1 with immunohistochemistry and RT-PCR, respectively. The pathological changes of the kidneys were assessed microscopically.</p><p><b>RESULTS</b>Compared with those in the model group, the 24-h urinary protein level and expressions of NF-κB, MCP-1 and TGF-β1 mRNA and protein in the renal tissues were significantly increased by nitrotyrosine treatment, which also caused worsened renal pathology, while treatment with ebselen significantly ameliorated these changes.</p><p><b>CONCLUSION</b>Nitrotyrosine can up-regulate the mRNA and protein expressions of NF-κB, MCP-1 and TGF-β1 and aggravate the inflammatory reaction in the renal tissue of DN rats to promote the progression of DN.</p>