Oral pectin/oligochitosan microspheres for colon-specific controlled release of quercetin to treat inflammatory bowel disease.

Inflammatory bowel disease (IBD) is a chronic, life quality-reducing disease with no cures available yet. To develop an effective medication suitable for long-term use is an urgent but unmet need. Quercetin (QT) is a natural dietary flavonoid with good safety and multifaceted pharmacological activities against inflammation. However, orally administrated quercetin yields unproductive outcomes for IBD treatment because of its poor solubility and extensive metabolism in the gastrointestinal tract. In this work, a colon-targeted QT delivery system (termed COS-CaP-QT) was developed, of which the pectin (PEC)/Ca2+ microspheres were prepared and then crosslinked by oligochitosan (COS). The drug release profile of COS-CaP-QT was pH-dependent and colon microenvironment-responsive, and COS-CaP-QT showed preferential distribution in the colon. The mechanism study showed that QT triggered the Notch pathway to regulate the proliferation of T helper 2 (Th2) cells and group 3 innate lymphoid cells (ILC3s) and the inflammatory microenvironment was remodeled. The in vivo therapeutic results revealed that COS-CaP-QT could relieve the colitis symptoms and maintain the colon length and intestinal barrier integrity.

[Research progress of continuous manufacturing and process knowledge system of traditional Chinese medicine].

In the past few years, continuous manufacturing(CM) has been put forward by the FDA. Pharmaceutical enterprises are encouraged to promote the implementation of CM, which has become a hot research direction of pharmaceutical technology. In February 2019, the FDA issued a draft guideline for the implementation of CM, which greatly promoted the development of CM and provided reference for continuous manufacturing of traditional Chinese medicine(TCM). The production process of TCM is a complex system. With the innovation of production equipment and the promotion of automation and informatization of TCM production, the exis-ting policies, regulations and traditional production control capacity are difficult to meet the market demand for high-quality TCM pro-ducts. In this paper, we reviewed the new technologies and methods of quality control in accordance with the characteristics of TCM production by referring to modern manufacturing technology, information technology and quality control technology. Based on the "QbD" theory and "PAT" technology, process knowledge system(PKS), an advanced control strategy, was proposed to provide a reference for the implementation of CM in TCM production.

Antiproliferative and Antimetastatic Effects of Praeruptorin C on Human Non-Small Cell Lung Cancer Through Inactivating ERK/CTSD Signalling Pathways.

Praeruptorin C (PC) reportedly has beneficial effects in terms of antiinflammation, antihypertension, and antiplatelet aggregation, and it potentially has anticancer activity. However, the effect of PC on human non-small cell lung cancer (NSCLC) is largely unknown. Compared with the effects of praeruptorin A and praeruptorin B, we observed that PC significantly suppressed cell proliferation, colony formation, wound closure, and migration and invasion of NSCLC cells. It induced cell cycle arrest in the G0/G1 phase, downregulated cyclin D1 protein, and upregulated p21 protein. PC also significantly reduced the expression of cathepsin D (CTSD). In addition, the phosphorylation/activation of the ERK1/2 signalling pathway was significantly suppressed in PC-treated NSCLC cells. Cotreatment with PC and U0126 synergistically inhibited CTSD expression, cell migration, and cell invasion, which suggests that the ERK1/2 signalling pathway is involved in the downregulation of CTSD expression and invasion activity of NSCLC cells by PC. These findings are the first to demonstrate the inhibitory effects of PC in NSCLC progression. Therefore, PC may represent a novel strategy for treating NSCLC.

A polysaccharide from the alkaline extract of Glycyrrhiza inflata induces apoptosis of human oral cancer SCC-25 cells via mitochondrial pathway.

In the present study, we isolated and characterized a homogenous polysaccharide (GIAP1) from the alkaline extract of the roots of Glycyrrhiza inflata. The anti-tumor activity of GIAP1 toward human oral cancer SCC-25 cells and the underlying mechanisms were also examined in vitro. GIAP1 dose-dependently inhibited the proliferation of SCC-25 cells via inducing apoptosis. Moreover, GIAP1 downregulated Bax/Bcl-2 ratio, disrupted the mitochondrial membrane potential (MMP), and caused the release of cytochrome c to cytosol. Besides, GIAP1 triggered activation of capase-3 and caspase-9, as well as the degradation of poly (ADP-ribose) polymerase (PARP). In addition, the caspase-3 or caspase-9 inhibitor significantly inhibited GIAP1-induced apoptosis in SCC-25 cells. Collectively, we can conclude that the GIAP1 induces apoptosis in SCC-25 cells via a mitochondrial pathway.

A fast referenceless PRFS-based MR thermometry by phase finite difference.

Proton resonance frequency shift-based MR thermometry is a promising temperature monitoring approach for thermotherapy but its accuracy is vulnerable to inter-scan motion. Model-based referenceless thermometry has been proposed to address this problem but phase unwrapping is usually needed before the model fitting process. In this paper, a referenceless MR thermometry method using phase finite difference that avoids the time consuming phase unwrapping procedure is proposed. Unlike the previously proposed phase gradient technique, the use of finite difference in the new method reduces the fitting error resulting from the ringing artifacts associated with phase discontinuity in the calculation of the phase gradient image. The new method takes into account the values at the perimeter of the region of interest because of their direct relevance to the extrapolated baseline phase of the region of interest (where temperature increase takes place). In simulation study, in vivo and ex vivo experiments, the new method has a root-mean-square temperature error of 0.35 °C, 1.02 °C and 1.73 °C compared to 0.83 °C, 2.81 °C, and 3.76 °C from the phase gradient method, respectively. The method also demonstrated a slightly higher, albeit small, temperature accuracy than the original referenceless MR thermometry method. The proposed method is computationally efficient (~0.1 s per image), making it very suitable for the real time temperature monitoring.

[Effects of Nourishing yin clearing heat ([Chinese characters: see text]) Chinese herbal medicine on vascular endothelial growth factor the epiphyseal cartilage of growth retardation].

OBJECTIVE: To observe the effects of Nourishing yin clearing heat ([Chinese characters: see text]) Chinese herbal medicine on vascular endothelial growth factor (VEGF) in growth retardation induced by Decamethasone and observe its mechanisms. METHODS: Thirty one-month-old New Zealand white rabbits were randomly divided into normal group, dexamethasone-treated group and Nourishing yin clearing heat ([Chinese characters: see text]) Chinese herbal medicine-treated group. The rabbits in dexamethasone group and Nourishing yin clearing heat ([Chinese characters: see text]) Chinese herbal medicine-treated group received dexamethasone (5 mg/kg x d). The rabbits were sacrificed at the 6th and 12th week after administration, and then rabbit tibia articular was removed. (1) Using TUNEL stain to detect apoptotic index. (2) Using immunohistochemical stain to detect the positive index of the expression of vascular endothelial growth factor (VEGF) in the epiphyseal cartilage of growth. (3) Using fluorescent quantitative PCR to detect the expression intensity of VEGF mRNA in each group. RESULTS: At the 6th and 12th week after administration, there were significant difference in apoptotic index and cell proliferation index between dexamethasone group and normal group (P<0.01, dexamethasone group more than normal group). Immunohistochemical stain and fluorescent quantitative PCR indicated that the expression of VEGF and VEGF mRNA in dexamethasone group was significantly decreased as compared with that in normal group (P<0.01), and also obviously lower than Chinese herbal medicine-treated group (P<0.01). CONCLUSION: VEGF has 2. an important role during the growth retardation induced by Dexamethasone. Nourishing yin clearing heat ([Chinese characters: see text]) Chinese herbal medicine can reduce the growth retardation induced by Dexamethasone through increasing the VEGF expression in growth plate chondrocytes and then increase angiogenesis.