Objective To study the mechanism of enhanced HaCaT cellular uptake of tetrahydropalmatine (THP) by asarum essential oil (AEO) and sinapine thiocyanate (SPT) in Sanfu Patch. Methods Effect of SPT, AEO, and THP on cell viability of HaCaT were determined by MTT. HaCaT cellular uptake of THP and the enhancing effects of AEO and SPT on THP uptake were visualized with confocal laser scanning microscope (CLSM) based on the green autofluorescence of THP, and the THP uptake content by HaCaT was further determined with HPLC. Moreover, HaCaT cells were labeled with diphenylhexatriene (DPH). After the labeled cells were treated with AEO, SPT, and THP, respectively, the cellular membrane fluidity was determined with fluorescence polarization technology. Results THP fluorescence intensity within HaCaT cells was significantly increased when THP was co-delivered with AEO or SPT respectively, and the THP content with each group within the cells was also significantly higher than that of THP delivered alone. In addition, AEO was superior to SPT in enhancing THP uptake by HaCaT cells. The fluorescence polarization and membrane micro-viscosity of HaCaT cells were significantly decreased after AEO treatment, which indicated that membrane fluidity was increased by the treatment with AEO. However, SPT or THP did not present the character of increasing the membrane fluidity.Conclusion HaCaT cellular uptake of THP can be enhanced by AEO and SPT of Sanfu Patch, in which AEO enhances the cellular uptake of THP through increasing the cellular membrane fluidity, while the mechanism of SPT in enhancing THP cellular uptake remains further clarification.

Objective:To study the effect of electroacupuncture (EA) at the Pericardium Meridian on the heart function of volunteers with acute hypoxia, and to provide scientific evidence for the acupoints selection along the affected meridian in acupuncture-moxibustion therapy. Methods:Based on a self-control design, eighteen healthy volunteers were recruited in the study. Points from the Pericardium Meridian [Neiguan (PC 6), Ximen (PC 4), Quze (PC 3) and Tianquan (PC 2)], non-Pericardium Meridian point [Shousanli (LI 10)], non-meridian and non-acupoint points [1.0-1.5 cm lateral to Neiguan (PC 6) and Ximen (PC 4), respectively on both sides], and a blank control (only inhaling low-oxygen gas without EA stimulation) were selected to observe, once every week, 10 sessions in total, and only 1 acupoint was observed once. The volunteers inhaled low-oxygen gas mixture (10.8% O2 and 89.2% N2) for 30 min to imitate acute hypoxia. EA was conducted when the gas mixture was inhaled for 10 min and then lasted for 20 min; meanwhile, hemodynamic indexes such as cardiac output (CO), cardiac index (CI), systemic vascular resistance (SVR), systemic vascular resistance index (SVRI), left cardiac work (LCW), left cardiac work index (LCWI) and heart rate (HR) were recorded on a hemodynamic monitor. Results:EA at the acupoints of Pericardium Meridian significantly down-regulated the increased CO/CI, LCW/LCWI, and HR (P<0.05), and significantly up-regulated the decreased SVR/SVRI in hypoxia (P<0.05); EA at other meridian acupoints or at non-meridian and non-acupoint points didn't produce such effects. Conclusion: EA at the Pericardium Meridian can obviously improve the cardiac hyper-activation caused by acute hypoxia in healthy volunteers.

Objective To evaluate the effect of exogenous hydrogen sulfide (H2 S) on myocardial damage induced by renal ischemia-reperfusion (I/R) in rats.Methods Thirty pathogen-free male Wistar rats,weighing 250-300 g,were randomized into 3 groups (n =10 each) using a random number table:sham operation group (S group); myocardial damage induced by renal I/R group (I/R group); NaHS group.Renal I/R was induced by occlusion of the left kidney for 120 min followed by 60 min reperfusion in anesthetized rats.In NaHS group,NaHS 100 μg/kg was injected intraperitoneally at 20 min before reperfusion.At the end of reperfusion,the rats were sacrificed and the hearts were obtained for determination of malondialdehyde (MDA) content and glutathione peroxidase (GSH-Px) activity in myocardial tissues and for microscopic examination.Results Compared with S group,MDA content was significantly increased,and GSH-Px activity was decreased in I/R and NaHS groups.Compared with I/R group,MDA content was significantly decreased,and GSH-Px activity was increased in NaHS group.The pathological changes of myocardium were significantly attenuated in NaHS group as compared with I/R group.Conclusion Exogenous H2 S can alleviate myocardial damage induced by renal I/R in rats.

Lipids of Thamnidium elegans,Mortierella ramanninace,Rhizopus arrhizus,Pythium irregulare and Rhodotorulla aurantiaca were extracted by Soxhlet extraction,supercritical-CO 2 fluid extraction,acid-heating extraction and organic solvent extraction,respectively.Four extraction methods were evaluated on sample treatment,minimum sample quantity,requirements of apparatus,ability of treating sample and content of lipid.The components of fatty acids were analysed by gas chromatography.Soxhlet extraction can acquired maximum lipid content,but it took the most time.Supercritical-CO 2 fluid extraction and acid-heating extraction has a same lipid content which was lower than that of Soxhlet extraction.Acid-heating extraction was the most handy,and its ability to treat sample in a hour was the most powerful.Organic solvent extraction was less efficient.Acid-heating extraction was a simple and efficient method of fungi lipid extraction fitting to breed mutant strains that highly producting lipid and polyunsaturated fatty acids.

Objective: To investigate the incidence and impact factors of adverse events (AE) in ultrasound-guided percutaneous microwave ablation (MWA) for treatment of colorectal liver metastases (CRLM). Methods: Clinical data of 427 CRLM patients who underwent ultrasound-guided percutaneous MWA were retrospectively analyzed. Totally 614 MWA sessions were performed and 1 334 lesions were ablated. The incidence and impact factors of AE were analyzed. Results: The overall incidence of AE was 4.89% (30/614), and no ablation-related death occurred. The risk factors affecting AE included number of insertions (OR=1.301, P=0.005), lesions at high-risk areas (OR=2.829, P=0.025), more than 5 lesions (OR=4.655, P=0.010), history of abdominal surgery (OR=7.716, P=0.047) and clonorchiasis (OR=17.683, P=0.005). Conclusion: The incidence of AE in ultrasound-guided percutaneous MWA for CRLM is low. The number of lesions and insertions, lesions at high-risk areas, history of abdominal surgery, and clonorchiasis are associated with the incidence of AE.

Objective： This study was designed to explore the relationship between clinicobiological acting and expression of p21 protein and estrogen receptor(ER) in colorectal cancer. Methods： The intensity of expression of p21 protein and ER for 206 patients with colorectal cancers were determined by labeled-streptokinase avidin-biotin(LSAB) assay. Results： The expression of p21 protein is negatively correlated with that of ER in colorectal cancer(r=-0.6613, P<0.01). The intensity of expression of p21 protein and ER in colorectal cancers were not related with the patients age, sexuality, tumor position, pathological type, histological type, Dukes stage etc.(r< 0.4,P>0.05). Both the expressions were related to the prognosis of colorectal cancer(P<0.01). Higher the intensity of expression of p21 protein worse the patients prognosis, and higher the intensity of expression of ER better the patient s prognosis. Conclusions： The abnormal expression of p21 protein is related to the dysbolism of estrogen in colorectal cancer. The detection of p21 protein and ER are helpful for diagnosis and prognostic evaluation for colorectal cancer.

Castleman disease is a rare and complicated disease. A case of Castleman disease (CD) in a 40-year-old woman on the neck was reported and literature review was made to understand the occurrence, clinical characteristics, diagnosis and differential diagnosis, treatment, and prognosis of Castleman disease. Because of the rarity of CD, its occurrence in the general population and the typical clinical manifestations are still lacked. There are two types of CD, namely localized CD and multicentric CD, both of them are not easy to be diagnosised. CT scans in preoperative is helpful for the clinical diagnosis, while histopathological examination and lymph node biopsy are beneficial for the early diagnosis. The treatment result is based on the histopathological examination and lymph node biopsy. The prognosis is different with the type of CD. For the localized CD, the prognosis is usually good, while for the multicentric CD is bad. Both of localized CD and multicentric CD have a certain reoccurrence rate.

Cyclodextrin can increase the solubility of poorly soluble drugs, but also decrease the permeability of poorly soluble drugs in inclusion complexes simultaneously, which partially or completely counteracts the contribution of improvement in solubility to the oral absorption of poorly soluble drugs. If a competing agent is added to the system to compete binding sites of cyclodextrins with drugs, drug permeability can be improved by increasing the concentration of free drugs in the inclusion complex system. In this paper, a rapid in vitro screening method for competing agents of cyclodextrin inclusion complex is proposed based on the principle that good drug permeability is in accord with good cell uptake. The equilibrium constants between drugs and hydroxypropyl-beta-cyclodextrin (HPCD) were determined by phase equilibrium solubility method. Cinnarizine (CN) with a high equilibrium constant was selected as a competing agent, coumarin 6 (C6) and 9-octadecyl berberine (BD) with smaller equilibrium constants were selected as model drugs. Both changes of solubility and uptake by Caco-2 and A549 cells of C6 and BD were investigated different concentrations of CN to the HPCD solution of C6 and BD. The results showed that the uptake of C6 and BD increased in a CN concentration-dependent manner, and the solubility of C6 and BD in HPCD solution decreased with the prolongation of equilibrium time. It might be due to increased free drug concentrations that resulted from the competition of CN for drug binding sites with HPCD. In our study, in vitro cell uptake method was firstly used to validate the ability of CN as a competing agent to increase drug permeability (cell uptake). This method can be used for preliminarily screening of competing agents for drug-cyclodextrin inclusion complexes.

BCS Ⅱ drugs are characterized by low solubility and high permeability. Improving their solubility is considered an important approach to improve its oral absorption. Recent strategies to increase the solubility of poorly-soluble drugs may unexpectedly result in greatly depressed permeability, ultimately leading to failure in improving oral absorption. Based on the mathematics of membrane permeability coefficient of a drug, the membrane/aqueous partition coefficient is dependent on the drug's solubility in the gastrointestinal milieu, suggesting a unique interplay between the solubility and permeability of the drug, and treating the one irrespectively of the other may be insufficient. When we focus on the increase of drug solubility and overlook the efficacy of drug permeability, the positive effect of increased solubility to drug oral absorption might be traded off by depressed permeability. To provide rational formulary designs, by optimizing excipients and evaluation, this review summarizes solubility- permeability interplay for different types of solubilizing techniques, such as cyclodextrin, surfactants-based vehicle, cosolvent, amorphous solid dispersions, other infectors such as P-gp transporters and new techniques for simultaneous evaluation of drug solubility and permeability.