A new elemane-type sesquiterpenoid glycoside from Curcuma phaeocaulis / 药学学报

To study the chemical constituents and their biological activities in the rhizomes of Curcuma phaeocaulis, silica gel column chromatography, reverse medium pressure liquid chromatography, preparative thin layer chromatography, and semi-preparative high performance liquid chromatography were used for isolation and purification and modern spectroscopic methods were used to determine the structure of the isolated compound. Moreover, the effect of the compound on the proliferation of HUVECs was determined by the MTT assay. A new elemane-type sesquiterpenoid glycoside was isolated from the n-butanol soluble fraction of 95% ethanolic extract of the rhizomes of Curcuma phaeocaulis. Its structure was identified as (1Z)-2-hydroxy-curzerenone 2-O-β-D-glucoside. It showed no inhibitory effect on the proliferation of HUVECs.

NOX4/Src regulates ANP secretion through activating ERK1/2 and Akt/GATA4 signaling in beating rat hypoxic atria

Nicotinamide adenine dinucleotide phosphate oxidases (NOXs) are the major enzymatic source of reactive oxygen species (ROS). NOX2 and NOX4 are expressed in the heart but its role in hypoxia-induced atrial natriuretic peptide (ANP) secretion is unclear. This study investigated the effect of NOX on ANP secretion induced by hypoxia in isolated beating rat atria. The results showed that hypoxia significantly upregulated NOX4 but not NOX2 expression, which was completely abolished by endothelin-1 (ET-1) type A and B receptor antagonists BQ123 (0.3 µM) and BQ788 (0.3 µM). ET-1-upregulated NOX4 expression was also blocked by antagonists of secreted phospholipase A2 (sPLA2; varespladib, 5.0 µM) and cytosolic PLA2 (cPLA2; CAY10650, 120.0 nM), and ET-1-induced cPLA2 expression was inhibited by varespladib under normoxia. Moreover, hypoxia-increased ANP secretion was evidently attenuated by the NOX4 antagonist GLX351322 (35.0 µM) and inhibitor of ROS N-Acetyl-D-cysteine (NAC, 15.0 mM), and hypoxia-increased production of ROS was blocked by GLX351322. In addition, hypoxia markedly upregulated Src expression, which was blocked by ET receptors, NOX4, and ROS antagonists. ET-1-increased Src expression was also inhibited by NAC under normoxia. Furthermore, hypoxiaactivated extracellular signal-regulated kinase 1/2 (ERK1/2) and protein kinase B (Akt) were completely abolished by Src inhibitor 1 (1.0 µM), and hypoxia-increased GATA4 was inhibited by the ERK1/2 and Akt antagonists PD98059 (10.0 µM) and LY294002 (10.0 µM), respectively. However, hypoxia-induced ANP secretion was substantially inhibited by Src inhibitor. These results indicate that NOX4/Src modulated by ET-1 regulates ANP secretion by activating ERK1/2 and Akt/GATA4 signaling in isolated beating rat hypoxic atria.

Clinical study on improving the strength and activity of lumbar spine with Qiang Jin exercises / 中国骨伤

OBJECTIVE@#To observe the effect of Qiang Jin exercises on the muscle strength and activity of lumbar spine in patients with lumbar disc herniation.@*METHODS@#From March 2016 to September 2017, at the Department of Orthopaedics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, a total of 110 subjects were enrolled, and 98 eligible subjects were screened. The subjects were randomized by stratified randomization and divided into experimental group and control group, 49 cases in each group, 25 males and 24 females in the experimental group, 25 males and 24 females in the control group. The experimental group exercised with Qiang Jin exercises, one time each morning and evening, each time10 sets were made;the control group used classic rehabilitation training, training twice a week, and three months was a course of treatment. After 12 weeks of training, the muscle strength and activity of the lumbar spine were evaluated and compared with the muscle strength and activity of the lumbar spine before training.@*RESULTS@#The experimental group and the control group had different muscle strength and activity of the lumbar spine before and after treatment (@*CONCLUSION@#Qiang Jin exercises can effectively improve the muscle strength and activity of the lumbar spine and improve the daily living ability of patients.

NOX4/Src regulates ANP secretion through activating ERK1/2 and Akt/GATA4 signaling in beating rat hypoxic atria

Nicotinamide adenine dinucleotide phosphate oxidases (NOXs) are the major enzymatic source of reactive oxygen species (ROS). NOX2 and NOX4 are expressed in the heart but its role in hypoxia-induced atrial natriuretic peptide (ANP) secretion is unclear. This study investigated the effect of NOX on ANP secretion induced by hypoxia in isolated beating rat atria. The results showed that hypoxia significantly upregulated NOX4 but not NOX2 expression, which was completely abolished by endothelin-1 (ET-1) type A and B receptor antagonists BQ123 (0.3 µM) and BQ788 (0.3 µM). ET-1-upregulated NOX4 expression was also blocked by antagonists of secreted phospholipase A2 (sPLA2; varespladib, 5.0 µM) and cytosolic PLA2 (cPLA2; CAY10650, 120.0 nM), and ET-1-induced cPLA2 expression was inhibited by varespladib under normoxia. Moreover, hypoxia-increased ANP secretion was evidently attenuated by the NOX4 antagonist GLX351322 (35.0 µM) and inhibitor of ROS N-Acetyl-D-cysteine (NAC, 15.0 mM), and hypoxia-increased production of ROS was blocked by GLX351322. In addition, hypoxia markedly upregulated Src expression, which was blocked by ET receptors, NOX4, and ROS antagonists. ET-1-increased Src expression was also inhibited by NAC under normoxia. Furthermore, hypoxiaactivated extracellular signal-regulated kinase 1/2 (ERK1/2) and protein kinase B (Akt) were completely abolished by Src inhibitor 1 (1.0 µM), and hypoxia-increased GATA4 was inhibited by the ERK1/2 and Akt antagonists PD98059 (10.0 µM) and LY294002 (10.0 µM), respectively. However, hypoxia-induced ANP secretion was substantially inhibited by Src inhibitor. These results indicate that NOX4/Src modulated by ET-1 regulates ANP secretion by activating ERK1/2 and Akt/GATA4 signaling in isolated beating rat hypoxic atria.

Involvement of eIF2α in halofuginone-driven inhibition of TGF-β1-induced EMT

Halofuginone (HF) is an extract from the widely used traditional Chinese medicine (TCM) Dichroa febrifugathat facilitates the recovery of wounds and attenuates hepatic fibrosis. However, the role of HF in theepithelial-mesenchymal transition (EMT) of IPEC-J2 cells remains unclear. The current study explored theanti-EMT effect of HF in IPEC-J2 cells and illustrates its molecular mechanism. Transforming growth factorb1 (TGF-b1), as a recognized profibrogenic cytokine, decreased the level of the epithelial marker E-cadherinand increased the level of the mesenchymal markers, such as N-cadherin, fibronectin (FN), vimentin (Vim),and a-smooth muscle actin (a-SMA), in IPEC-J2 cells depending on the exposure time and dose. HF markedlyprevented the EMT induced by TGF-b1. Dissection of the mechanism revealed that HF inhibited IPEC-J2 cellEMT via modulating the phosphorylation of SMAD2/3 and the SMAD2/3-SMAD4 complexnuclear translocation. Furthermore, HF could promote the phosphorylation of eukaryotic translation initiationfactor-2a (eIF2a), which modulates the SMAD signaling pathway. These results suggested that HF inhibitsTGF-b1-induced EMT in IPEC-J2 cells through the eIF2a/SMAD signaling pathway. Our findings suggest thatHF can serve as a potential anti-EMT agent in intestinal fibrosis therapy.

Imaging study of lumbosacral multifidus muscle fat changes in patients with lumbar disc herniation / 中国骨伤

OBJECTIVE@#To compare the degeneration of lumbosacral multifidus muscle in patients with lumbar disc herniation.@*METHODS@#Magnetic Resonance Spectroscopy was performed on the multifidus muscle of 35 healthy volunteers and 35 patients with unilateral L lumbar disc herniation. There were 20 males and 15 females in each group, aged from 25 to 55 years old. In healthy volunteers, the mean age was (35.66±8.73) years old and the BMI was (21.85±1.94) kg/m; in the patients, the mean age was (36.09±7.70) years old, the BMI was (21.50±1.78) kg/m, the VAS score was (4.40±0.88) points, the course of disease was (11.2±7.14) months. The proportion of fat in the L lumbosacral multifidus muscle and the proportion of fat-suppressed cross-sectional area were observed by MRI, the differences of the observation indexes of the two groups were compared through data analysis.@*RESULTS@#In healthy volunteers, the proportion of fat on the left side of the multifidus muscle was (0.169± 0.035)%, the proportion of fat removal cross-sectional area on the left side of the multifidus muscle was (0.699±0.070)%, the proportion of fat on the right side of the multifidus muscle was (0.168±0.031)%, and the proportion of fat removal cross-sectional area on the right side of the multifidus muscle was (0.712±0.056)%, there was no significant difference between the two sides (>0.05). In patients, the proportion of fat on the healthy side of multifidus muscles was (0.173±0.021)%, the proportion of fat removal cross-sectional area on the healthy side of multifidus muscles was (0.695±0.054)%, the proportion of fat on the affected side of the multifidus muscle was (0.228±0.027)%, and the proportion of fat removal cross-sectional area on the affected side of the multifidus muscle was (0.629±0.048)%, the differences of the above indexes on both sides were statistically significant (0.05).@*CONCLUSION@#There is degeneration of lumbosacral multifidus muscle on the affected side of patients with unilateral L intervertebral disc herniation, featuring multifidus muscular atrophy and fat infiltration.

A comparative study on the surface electromyography of lumbosacral multifidus muscle in patients with lumbar disc herniation / 中国骨伤

OBJECTIVE@#To compare the degeneration of lumbosacral multifidus muscle in patients with lumbar disc herniation.@*METHODS@#Thirty-five healthy volunteers and 35 patients with unilateral L lumbar disc herniation from December 2015 to September 2017 were recruited. There were 20 males and 15 females in each group, aged from 25 to 55 years old. In healthy volunteers group, the mean age was (35.66±8.73) years old and the BMI was (21.85±1.94) kg /m. In patients with lumbar disc herniation, the mean age was (36.09±7.70) years old, the BMI was (21.50±1.78) kg /m, the VAS score was 4.40±0.88, the course of disease was (11.20±7.14) months. Surface electromyography analysis was performed on the multifidus muscle of the two groups. The average myoelectric amplitude of the multifidus muscle in the two groups were compared.@*RESULTS@#The average myoelectric amplitude of the multifidus muscle of healthy volunteers was (48.84±7.77) µV on the left and (49.13±7.86) µV on the right. There was no significant difference between the two sides (>0.05). The average myoelectric amplitude of multifidus muscle in patients with lumbar disc herniation was(48.82±8.14) µV on the healthy side and (42.81±7.00) µV on the affected side, and the difference was statistically significant between two sides(0.05). There was significant difference in the average myoelectric amplitude of multifidus muscle between the affected side of lumbar disc herniation and on the left of healthy volunteers, and also between the affected side of lumbar disc herniation and on the right of healthy volunteers(<0.05).@*CONCLUSION@#Patients with chronic lumbar disc herniation have an imbalance in myoelectric activity, and the muscle strength of the multifidus muscle on the affected side is significantly reduced.

Pharmacokinetics and safety of repirinast tablets in healthy Chinese subjects

ABSTRACT Repirinast is a new, synthetic, disodium cromoglycate-like antiallergic agent for oral administration in humans. This study evaluated the safety, tolerability and pharmacokinetics of repirinast tablets in healthy Chinese volunteers. This was a phase I, open-label, randomized, single- and multiple-dose study. Subjects were assigned to receive a single dose of repirinast tablet at either 150, 300, or 450 mg, or multiple doses of 150 mg twice daily for 5 days. Plasma samples were analyzed with LC-MS/MS. Pharmacokinetic parameters of active metabolite MY-1250 (deesterified repirinast) were calculated using non-compartmental analysis with WinNonlin software. Statistical analysis was performed using SPSS software. All adverse events (AEs) were mild and of limited duration. No serious adverse event (SAE), death or withdrawal from the study was observed. In the single-dose study, Cmax was reached at about 0.75 hour, and the mean t1/2 was approximately 16.21 hours. Area under curve (AUC) and Cmax increased with dose escalation, but dose proportionality was not observed over the range of 150 to 450 mg. In the multiple-dose study, the steady-state was reached within 3 days with no accumulation. Repirinast tablet was well tolerated in healthy Chinese subjects.

Peroxisome proliferator-activated receptor γ is essential for secretion of ANP induced by prostaglandin D₂ in the beating rat atrium

Prostaglandin D₂ (PGD₂) may act against myocardial ischemia-reperfusion (I/R) injury and play an anti-inflammatory role in the heart. Although the effect of PGD₂ in regulation of ANP secretion of the atrium was reported, the mechanisms involved are not clearly identified. The aim of the present study was to investigate whether PGD₂ can regulate ANP secretion in the isolated perfused beating rat atrium, and its underlying mechanisms. PGD₂ (0.1 to 10 µM) significantly increased atrial ANP secretion concomitantly with positive inotropy in a dose-dependent manner. Effects of PGD₂ on atrial ANP secretion and mechanical dynamics were abolished by AH-6809 (1.0 µM) and AL-8810 (1.0 µM), PGD₂ and prostaglandin F2α (PGF2α) receptor antagonists, respectively. Moreover, PGD₂ clearly upregulated atrial peroxisome proliferator-activated receptor gamma (PPARγ) and the PGD₂ metabolite 15-deoxy-Δ12,14-PGJ₂ (15d-PGJ₂, 0.1 µM) dramatically increased atrial ANP secretion. Increased ANP secretions induced by PGD₂ and 15d-PGJ₂ were completely blocked by the PPARγ antagonist GW9662 (0.1 µM). PD98059 (10.0 µM) and LY294002 (1.0 µM), antagonists of mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) and phosphatidylinositol-3-kinase (PI3K)/protein kinase B (Akt) signaling, respectively, significantly attenuated the increase of atrial ANP secretion by PGD₂. These results indicated that PGD₂ stimulated atrial ANP secretion and promoted positive inotropy by activating PPARγ in beating rat atria. MAPK/ERK and PI3K/Akt signaling pathways were each partially involved in regulating PGD₂-induced atrial ANP secretion.

Current therapy status and research progress of cartilage defects of knees / 中国骨伤

To demonstrate the current strategies for treating cartilage defects of knees and the related research. Published papers about cartilage defects were searched and reviewed. The current strategies for the treatment were summarized. Based on the research of our study and others, the conclusion how to treat cartilage defects was made. The current ways for treating cartilage defects include micro-fractures, chondrocytes transplantation, mosaicplasty and tissue engineering; Research on functional magnetic resonance imaging in the early diagnosis of cartilage defects, cartilage degeneration is gradually increasing. There is still no effective treatment of cartilage defects and tissue engineering has brought new hopes for the treatment of cartilage defects , functional magnetic resonance imaging has some significance in early diagnosis of cartilage defects, cartilage degeneration.

Study thought of pharmaceutical preparations quality standards by dynamic quality control technology / 中国中药杂志

Pharmaceutical preparations, particularly as a "secret recipe" of traditional Chinese medicine in medical institutions, are the product of China's medical and health industry, and they are also an important means of competing of different medical institutions. Although pharmaceutical preparations have advantages and characteristics than institutes for drug and pharmaceutical companies, the quality standards of pharmaceutical preparations in medical institutions has not reached the desired level over the years. As we all know, the quality of pharmaceutical preparations is important to ensure the efficacy, especially under the environment of people pay more sttention on drug safety and effectiveness and contry increase emphasis on the stste of pharmaceutical preparations. In view of this, we will improve the grade, stability, and clinical efficacy of pharmaceutical preparations by the advanced equipment, testing instruments and the process dynamic quality control technology. Finally, we hope we can provide new ideas for the quality control of pharmaceutical preparations.