Multiple stimulus-response berberine plus baicalin micelles with particle size-charge-release triple variable properties for breast cancer therapy.

OBJECTIVE: The aim was to develop a nanoscale drug delivery system with enzyme responsive and acid sensitive particle size and intelligent degradation aiming to research the inhibitory effect on breast cancer. SIGNIFICANCE: The delivery system addressed the problems of tissue targeting, cellular internalization, and slow drug release at the target site, which could improve the efficiency of drug delivery and provide a feasible therapeutic approach for breast cancer. METHODS: The acid sensitive functional material DSPE-PEG2000-dyn-PEG-R9 was synthesized by Michael addition reaction. Then, the berberine plus baicalin intelligent micelles were prepared by thin-film hydration. Subsequently, we characterized the physical and chemical properties of berberine plus baicalin intelligent micelles, evaluated its anti-tumor effects in vivo and in vitro. RESULTS: The target molecule was successfully synthesized, and the intelligent micelles showed excellent chemical and physical properties, delayed drug release and high encapsulation efficiency. In vitro and in vivo experiments also confirmed that the intelligent micelles could effectively target tumor sites, penetrate tumor tissues, enrich in tumor cells, inhibit tumor cell proliferation, inhibit tumor cell invasion and migration, and induce tumor cell apoptosis. CONCLUSION: Berberine plus baicalin intelligent micelles have excellent anti-tumor effects and no toxicity to normal tissues, which provides a new potential drug delivery strategy for the treatment of breast cancer.

Sesquiterpene lactone dimers from the fruit of Carpesium abrotanoides L.

Seven undescribed sesquiterpene lactone dimers (SLDs) (carpeabrodilactones A-G), one known SLD, and six known sesquiterpenes were isolated from the fruit of Carpesium abrotanoides L. Carpeabrodilactone A was a dimeric carabrane featuring a rare C-13-C-13' linkage. Carpeabrodilactones B and C are the first two SLDs to be described possessing a carabranolide unit and a guaianolide unit connected by an O-ether linkage. The structures of the SLDs were assigned based on HRESIMS, NMR analysis, 13C NMR calculation, ECD calculation, and modified Mosher's method. Four SLDs showed potent cytotoxicity against K562 and/or A549 cells, with IC50 values below 10 µM, but none inhibited protein tyrosine phosphatases at 40 µM, including PTP1B, SHP1, CD45, and TCPTP.

One-step synthesis of a carbon dot-based fluorescent probe for colorimetric and ratiometric sensing of tetracycline.

Carbon dots (CDs) with blue fluorescence were synthesized using indole-3-butyric acid and l-tryptophan using a one-step hydrothermal method. The CDs were further employed as a fluorescent sensor with high selectivity for colorimetric and ratiometric detection of tetracycline (TC) in water. The limit of detection (LOD) was found to be 0.33 µM for TC with R2 = 0.98387. Besides, the CDs could be applied in practical water samples and showed good recovery.

Two Trinuclear CuII Complexes: Effect of Phosphonate Ligand on the Magnetic Property and Electrocatalytic Reactivity for Water Oxidation.

Two trinuclear copper phosphonate complexes, [Cu3 (pda)3 (tBuPO3 )]⋅2(Et3 NH) (1) and [Cu3 (pda)3 (PhPO3 )]⋅2(Et3 NH) (2), have been synthesized and investigated by a combination of X-ray crystallography, PXRD, magneto- and electrochemistry, EPR, in situ UV-vis spectroelectrochemistry and DLS. The two complexes feature almost identical crystal structures, the anions of which are both supported by pda2- and tBuPO3 2- /PhPO3 2- groups, bridging three five-coordinated CuII atoms to form a crown-like structure. This is the first time that trinuclear copper phosphonate complexes have been isolated and characterized. Magnetic susceptibility measurements reveal that complexes 1 and 2 both display overall ferromagnetic characters, but with different exchange interactions between the metal ions within the two clusters. The electrocatalytic activity for water oxidation of the two complexes was preliminarily investigated, which reveals that both of the two complexes can carry out electrocatalytic water oxidation in a neutral system owing to the introduction of phosphonate ligands into the complexes, with a TOF of about 0.82 s-1 (1) and 0.58 s-1 (2), respectively. We propose that the presence of phosphonate ligands may affect the magnetic property and catalytic activity of the complexes.

[Biomechanical analysis of the correlation between sacral tilt displacement and L5S1 disc degeneration].

OBJECTIVE: To biomechanical analysis of the correlation between sacral tilt displacement and L5-S1 disc degeneration. METHODS: From July 2011 to July 2013, 81 patients with lumbar disc herniation and sacroiliac joint disorder including 45 males and 36 females with an average age of (45.39±1.30) years ranging from 18 to 65 years old were selected. The course of the disease ranged from 1 to 144 months with an average of (12.64±2.19) months. All patients were taken lumbar spine lateral X-ray films, the lumbar curvature angle, L4-L5 or L5-S1 intervertebral gap distance between points, and the lumbosacral angle was measured and correlated analyzed. RESULTS: The lumbar curvature of female patients with L5S1DH were significantly larger than male patients [(22.18±8.62)° vs (16.17±4.97)°, P<0.05]. Lumbar curvature and lumbosacral angle showed a positive correlation in LDH (R=0.48, P<0.01,y=7.25+0.38x, P<0.01); Male patients with L4-5DH were more obvious (R=0.55, P<0.05, y=5.80+0.43x, P<0.01); Female patients with L5S1DH were particularly evident(R=0.74, P<0.01,y=0.91x-5.30, P<0.01). The lumbosacral angle and L4-5 intervertebral gap was a positive correlation in L4-5DH(R=0.27, P<0.05); While L5-S1 intervertebral gap and lumbosacral angle were not correlated(P>0.05) in L5S1DH. CONCLUSIONS: The sacral tilt displacement and L5-S1 disc degeneration were closely related to provide a new understanding philosophy and therapeutic approach for clinical treatment of intractable lumbar L5S1DH.

[Biomechanical analysis on the correlation between iliac rotation displacement and L(4,5) disc degeneration].

OBJECTIVE: To study the biomechanical relationship between iliac rotation displacement and L(4,5) disc degeneration, and to provide clinical evidences for the prevention and treatment of L(4,5) disc degeneration and herniation. METHODS: From March 2012 to February 2014,68 patients with lumbar disc herniation combined with sacroiliac joint disorders were selected. Among them, 42 patients with L(4,5) disc herniation combined with sacroiliac joint disorders included 22 males and 20 females, ranging in age from 19 to 63 years old, with an average of (51.78 +/- 20.18) years old, and the duration of the disease ranged from 1 to 126 months with an average of (11.18 +/- 9.23) months. Twenty-six patients with L5S1 disc herniation combined with sacroiliac joint disorders included 11 males and 15 females, ranging in age from18 to 65 years old with an average of (45.53 +/- 27.23) years old, and the duration of the disease ranged from 0.5 to 103 months with an average of (11.99 +/- 12.56) months. Sixty-eight anteroposterior lumbar radiographs, 68 lateral lumbar radiographs,and 68 pelvic plain films were taken. The degree of lumbar scoliosis, pelvic tilt,and disc thickness were measured. The correlation between pelvic tilt and lumbar scoliosis ,lumbar scoliosis and disc thickness were studied by using linear and regression methods. The hiomechanical analysis was performed. RESULTS: There was a positive correlation between pelvic tilt and lumbar scoliosis in patients with L(4,5) disk herniation (R=0.49, P=0.00). There was a causal relationship and good linear proportional relationship (Y=3.05+1.07X, P=0.00) in the two variables. There was a negative correlation between lumbar scoliosis and intervertebral space in male patients with L (4,5) disk herniation (R = -0.50, P=0.01). There was a causal relationship and good linear proportional relationship in the two variables (Y=13.09-0.27X, P=0.02). But there was a positive correlation between lumbar scoliosis and intervertebral space in male patients with L5S1 disk herniation (R=0.46, P=0.04). CONCLUSION: Iliac rotational displacement are closely related with L(4,5) disc degeneration and herniation in biomechanics. A new concepts and therapeutic approach is provided for clinical treatment of chronic and refractory herniation of L(4,5) disc in patients

[Expression analysis of green fluorescent protein in tissues and organs in α-1,3 galactosyltransferase knockout pigs].

The pig is an ideal source to provide organs because its organ size and physiology are similar to humans. However, an acute rejection will ensue after pig-to-human xenotransplantation. The α-1,3 galactosyltransferase gene knockout (GTKO) pigs were generated in recent years, and could solve the problem of hyperacute rejection. But due to lack of reporting genes, the rejection status of cells and organs post pig-to-human xenotransplantation cannot be visualized. In this study, we introduced the enhanced green fluorescent protein (EGFP) gene driven by the CAG promoter into GTKO porcine ear fibroblasts. Then we produced transgenic pigs expressing the EGFP gene by nuclear transfer technology. Expression levels of EGFP in different tissues and organs of the cloned pig were investigated by Nightsea DFP-1 Fluorescent Protein Flashlight, fluorescence microscope and quantitative PCR assays. The results showed that the protein and transcript of EGFP were expressed in all tissues and organs of the GTKO pig, but the expression was weak in the liver and central nervous system. In conclusion, we have successfully produced the transgenic GTKO pigs expressing EGFP in all tested tissues and organs, which builds up a good basis to track transplanted cells or tissues.

[Epidemiology investigation and biomechanics analyses for the correlation between sacroiliac joint disorder and lumbar intervertebral disc degeneration].

OBJECTIVE: To study the correlation between lumber disc degeneration and sacroiliac joint disorder, in order to provides a new understanding concepts and therapeutic approach for the prevention and treatment of chronic intractable low back pain. METHODS: From August 2009 to October 2010,129 cases with lumbar disc herniation were studied with epidemiological methods. Among them, 61 patients with L4, disc herniation included 37 males and 24 females, ranging in aged from 20 to 75 years old, duration of the disease ranged from 1 to 144 months; The other 68 patients with L5S1 disc herniation included 32 males and 36 females,ranging in aged froml8 to 76 years old,duration of the disease ranged from 0.5 to 240 months. The clinical data, symptoms and signs,X-ray characteristics of lumbar spine and pelvis of the patients were investigated by epidemiological. The risk of lumbar disc herniation was calculated with case-control study; independent variables were screened with single factor analysis; the risk factors for lumbar disc herniation were determined with logistic regression analysis, and biomechanics analyses were taken. RESULTS: Among 129 patients with lumbar disc herniation, 88 cases associated with sacroiliac joint disorders, sacroiliac joint disorder was a risk factor of lumbar disc herniation (OR = 4.61, P = 0.00); 47 cases associated with sacroiliac joint disorders in 61 patients with L4,5 disc herniation, iliac crest uneven caused by iliac rotational displacement was a high risk factor of L4,5 disc herniation (OR = 11.27, P = 0.00); 41 cases associated with sacroiliac joint disorders in 68 patients with L5S1 disc herniation, lumbar sacral angle abnormalities caused by sacral tilt shift was a high risk factor L5S1 disc herniation (OR = 2.31, P = 0.03). CONCLUSION: Lumbar disc herniation and sacroiliac joint disorder are two of fallot, the two factors affect each other and there is a causal relationship. They are common exists in low back pain.

[X-ray characteristics of sacroiliac joint disorders and its clinical significance].

OBJECTIVE: To study the X-ray characteristics of sacroiliac joint disorders and its clinical significance,so as to provide clinical diagnosis basis for Tuina treatment of sacroiliac joint disorder. METHODS: From July 2009 to March 2011,104 patients with sacroiliac joint disorder were reviewed,including 64 males and 40 females,ranging in age from 18 to 81 years, with an average of (45.39 +/- 1.30) years. The duration of the disease ranged from 1 to 144 months,with an average of (12.64 +/- 2.19) months. One hundred and four pelvic plain films and 97 lumbar spine lateral films of the patients with sacroiliac joint disorder were taken. On the lateral X-ray of lumbar,the sacral horizontal angles (lumbosacral angle) were measured; and on the X-ray of pelvis,the vertical distance of two side iliac crest (iliac crest difference), the distance from lateral border to medial margin of two hips (hip width),the clip angle between sacral spin connection and vertical axis were measured,and then the data were analyzed. RESULTS: The mean difference of iliac crest was (10.34+/-0.73) mm; the mean width difference of hip'was (6.73+/-1.01) mm; and the mean difference of the iliac crest was larger than that of mean difference of hip (P<0.01). The occurrence rate of inequal width of hip was higher(P<0.01). The mean abnormal lumbosacral angle was (7.29 +/- 1.86) degrees,and the mean angle of sacral crest tilting to left or right was (3.18 +/- 0.47) degrees; the mean abnormal lumbosacral angle was larger than that of angle of sacral crest tilting to left or right (P<0.01), and the occurrence rate of sacral crest tilting to left or right was higher

[Clinical study of safflower injection in treating and preventing the vascular crisis after free flap transplantation].

OBJECTIVE: To observe the clinical efficacy of Safflower Injection (Al) in treating and preventing the vascular crisis after free flap transplantation. METHODS: Sixty patients undergoing free flap transplantation were randomly assigned to the treatment group and control group according to the visiting sequence, thirty in each. Free flap transplantation was performed on all patients, and medication was given 0. 5 h before flap vascular anastomosis, 1-7 days after surgery. Twenty mL Al was intravenously dripped to patients in the treatment group after adding in 250 mL 5% glucose injection, while Dextran-40 was intravenously dripped to patients in the control group. The medication was conducted once per day. The hemorheology and four indices of blood coagulation [prothrombin time (PT), international normalized ratio (INR), activated partial thromboplastin time (APTT), fibrinogen (FIB)] were compared between the two groups before operation (TO), during operation (T1), 24 h after operation (T2), three days after operation (T3), and seven days after operation (T4). Meanwhile, flaps were observed and adverse reaction recorded. The clinical efficacy and safety were compared. RESULTS: Better result was obtained in the treatment group when compared their clinical efficacy (86. 67% vs 60. 00%, P<0.05). The whole blood high and low viscosity, plasma viscosity, red blood cell (RBC) volume, RBC aggregation index all decreased, and RBC deformed index increased in the two groups at T4, showing statistical difference when compared with those at T3 (P<0.05, P<0.01). There was no statistical significance in the four indices of blood coagulation when compared with any time point in the same group (P>0.05). There was no statistical significance in hemorheology and the four indices of blood coagulation between the two groups at the same time point (P>0.05). The adverse reaction rate in the treatment group was lower than that in the control group, showing statistical difference (13.33% vs 30.00%, P<0.05). CONCLUSIONS: AI could effectively prevent and treat the vascular crisis after free flap transplantation. It had less adverse reaction and good safety. It was better than Dextran-40. It was a safe and effective drug to prevent the vascular crisis.

[Heavy metals content and pollution risk assessment of cropland soils around a pesticide industrial park].

By the method of concentric circle distribution method, a total of 183 topsoil samples were collected from 30-km2 area around a pesticide industrial park in south Jiangsu Province, with the content and pollution index of soil Cd, Cr, Cu, Ni, Pb, Zn, Hg and As analyzed. The average contents of Hg, Cu, Cd, and Pb in the top soils were higher than those of the natural background values, and the contents of Hg and Cu were the highest. Taking the national standard II as the assessment criterion, the average pollution index values of Cd, Cr, Cu, Ni, Pb, Zn, and As in the top soils were all below 1, while those of the Hg and Cu were 1.59 and 1.05, respectively. In the southeast and northwest to the pesticide industrial park, soil heavy metals contamination was more serious, and, with the increasing distance to the park, the contents of soil Cd, Ni, Pb, Cr, As, Hg, Zn, and Cu increased first and then decreased to a stable level. The comprehensive pollution index of test metals indicated that the areas 200-1000 meter around the industrial park were of high risk in soil heavy metals contamination, while the areas 1000 meter beyond were safety. By using geostatistics and GIS, it was found that the pollution index of the eight heavy metals had significant spatial variability. Based on the principal component analysis and correlation analysis, it was speculated that the Zn, Ni, Cr, Pb, and As were mainly from soil parent materials, while the Hg, Cu, and Cd were mainly related to human activities.