OBJECTIVE: To evaluate the efficacy and safety of Shexiang Tongxin Dropping Pill (STDP) in treating stable angina patients with phlegm-heat and blood-stasis syndrome by exercise duration and metabolic equivalents. METHODS: This multicenter, randomized, double-blind, placebo-controlled clinical trial enrolled stable angina patients with phlegm-heat and blood-stasis syndrome from 22 hospitals. They were randomized 1:1 to STDP (35 mg/pill, 6 pills per day) or placebo for 56 days. The primary outcome was the exercise duration and metabolic equivalents (METs) assessed by the standard Bruce exercise treadmill test after 56 days of treatment. The secondary outcomes included the total angina symptom score, Chinese medicine (CM) symptom scores, Seattle Angina Questionnaire (SAQ) scores, changes in ST-T on electrocardiogram and adverse events (AEs). RESULTS: This trial enrolled 309 patients, including 155 and 154 in the STDP and placebo groups, respectively. STDP significantly prolonged exercise duration with an increase of 51.0 s, compared to a decrease of 12.0 s with placebo (change rate: -11.1% vs. 3.2%, P<0.01). The increase in METs was significantly greater in the STDP group than in the placebo group (change: -0.4 vs. 0.0, change rate: -5.0% vs. 0.0%, P<0.01). The improvement of total angina symptom scores (25.0% vs. 0.0%), CM symptom scores (38.7% vs. 11.8%), reduction of nitroglycerin consumption (100.0% vs. 11.3%), and all domains of SAQ, were significantly greater with STDP than placebo (all P<0.01). The changes in Q-T intervals at 28 and 56 days from baseline were similar between the two groups (both P>0.05). Twenty-five participants (16.3%) with STDP and 16 (10.5%) with placebo experienced AEs (P=0.131), with no serious AEs observed. CONCLUSION STDP could improve exercise tolerance in patients with stable angina and phlegm-heat and blood stasis syndrome, with a favorable safety profile. (Registration No. ChiCTR-IPR-15006020).
Humans ; Double-Blind Method ; Drugs, Chinese Herbal/adverse effects* ; Male ; Female ; Middle Aged ; Angina, Stable/physiopathology* ; Aged ; Syndrome ; Treatment Outcome ; Placebos ; Tablets

AIM To study the chemical constituents from the root tubers of Stephania kwangsiensis H.S.Lo and their tyrosinase inhibition and insecticidal activities.METHODS The 70％ ethanol extract from root tubers of S.kwangsiensis was isolated and purified by Sephadex LH-20,MCI,ODS,semi-prepative HPLC and HSCCC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The tyrosinase inhibitory activities were determined by using levodopa as substrate,and the insecticidal activities were evaluated by the control effect of Diaphorina citri.RESULTS Twelve compounds were isolated and identified as tetrahydropalmatine ( 1 ),dehydrocrebanine ( 2 ),crebanine ( 3 ),stephanine ( 4 ),liriodenine ( 5 ),piperumbellactam A ( 6 ),sinoacutine ( 7 ),(+)-salutaridine N-oxide ( 8 ),bisnorargemonine ( 9 ),(+)-corytuberine (10),sebiferine (11) and palmatrubine (12).The IC50 values of compounds 5-7 to tyrosinase were (0.1702±0.0101),(0.7663±0.0331) and (0.5193±0.0075) mg/mL,respectively.The control effects of compounds 2-5,7,8,10-12 against D.citri ranged from ( 19.33±0.57 )％ to ( 77.15±0.45 )％.CONCLUSION Compounds 2,5,6,and 8-12 are isolated from this plant for the first time,6 and 9 are first obtained from genus Stephania.Compounds 5-7 displayed significant tyrosinase inhibition activities.Compounds 7,8 and 10 show strong insecticidal activities.

AIM To study the chemical constituents from the root tubers of Stephania kwangsiensis H.S.Lo and their tyrosinase inhibition and insecticidal activities.METHODS The 70％ ethanol extract from root tubers of S.kwangsiensis was isolated and purified by Sephadex LH-20,MCI,ODS,semi-prepative HPLC and HSCCC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The tyrosinase inhibitory activities were determined by using levodopa as substrate,and the insecticidal activities were evaluated by the control effect of Diaphorina citri.RESULTS Twelve compounds were isolated and identified as tetrahydropalmatine ( 1 ),dehydrocrebanine ( 2 ),crebanine ( 3 ),stephanine ( 4 ),liriodenine ( 5 ),piperumbellactam A ( 6 ),sinoacutine ( 7 ),(+)-salutaridine N-oxide ( 8 ),bisnorargemonine ( 9 ),(+)-corytuberine (10),sebiferine (11) and palmatrubine (12).The IC50 values of compounds 5-7 to tyrosinase were (0.1702±0.0101),(0.7663±0.0331) and (0.5193±0.0075) mg/mL,respectively.The control effects of compounds 2-5,7,8,10-12 against D.citri ranged from ( 19.33±0.57 )％ to ( 77.15±0.45 )％.CONCLUSION Compounds 2,5,6,and 8-12 are isolated from this plant for the first time,6 and 9 are first obtained from genus Stephania.Compounds 5-7 displayed significant tyrosinase inhibition activities.Compounds 7,8 and 10 show strong insecticidal activities.

OBJECTIVE: To investigate whether miR-372-5p regulates PI3K/AKT/CXCL12 signaling pathway by targeting PTEN to promote metastasis of colorectal cancer cells. METHODS: We detected the differential expression of miR-372-5p using RT-qRCR in colorectal cancer and adjacent tissues, colorectal cancer cells and normal intestinal epithelial cells. Bioinformatic analysis and double luciferase assay were performed for verification of the targeting relationship between miR-372-5p and PTEN. Western blotting was used to assess the effects of transfection with miR-372-5p inhibitor and miR-372-5p mimics alone, co-transfection with miR-372-5p inhibitor and si-PTEN, and co-transfection with miR-372-5p mimics and PI3K inhibitor on the expressions of PTEN and CXCL12 and the activation of PI3K/AKT signal pathway; Transwell assay and scratch assay were used to examine the changes in the migration ability of the transfected cells, the cells co-transfected with miR-372-5p mimics and si-CXCL12, and the cells treated with conditioned medium from HCT116 cells transfected with miR-372-5p mimics. RESULTS: The expression of miR-372-5p was significantly higher in colorectal cancer tissues than in adjacent tissues, and higher in HCT116 and SW620 cells than in NCM460 cells (P < 0.01). Double luciferase assay confirmed that PTEN was a potential target gene of miR-372-5p (P < 0.05). Transfection of HCT116 cells with miR-372-5p mimics obviously decreased PTEN protein expression, increase CXCL12 expression and the phosphorylation level of AKT, and lowered the cell migration ability, while transfection with miR-372-5p inhibitor produced the opposite effects (P < 0.05); si-PTEN obviously neutralized the effect of miR-372-5p inhibitor (P < 0.01). PI3K inhibitor significantly decreased CXCL12 expression and inhibited the cell migration (P < 0.05), and this effect was mitigated by miR-372-5p mimics (P < 0.01). Treatment with the conditioned medium from HCT116 cells transfected with miR-372-5p mimics significantly enhanced the migration ability of NCM460 cells, and this effect was suppressed by transfection with si-CXCL12 (P < 0.01). CONCLUSION MiR-372-5p activates PI3K/AKT signaling pathway by targeting PTEN and up-regulates CXCL12 expression to promoting metastasis of colorectal cancer cells.
Chemokine CXCL12/metabolism* ; Colorectal Neoplasms/pathology* ; Culture Media, Conditioned ; Humans ; MicroRNAs/metabolism* ; Neoplasm Metastasis ; PTEN Phosphohydrolase/metabolism* ; Phosphatidylinositol 3-Kinases/metabolism* ; Proto-Oncogene Proteins c-akt/metabolism* ; Signal Transduction

OBJECTIVE: To study the clinical characteristics of the patients with tiny lumbar disc herniation and severe symptoms(tLDHSS) and the therapeutic effects of percutaneous endoscopic lumbar discectomy(PELD). METHODS: From January 2014 to February 2019, 34 patients with tLDHSS were reviewed retrospectively, including 20 males and 14 females, aged from 31 to 73 (48.8±10.1) years, with a follow up duration ranged from 8 to 48 (21.8±10.3) months. The clinical manifestations, imaging and surgical data were analyzed. The visual analogue scale (VAS) and Oswestry Disability Index (ODI) scores were analyzed before operation, 1 month after operation and at the latest follow-up. The preoperative and postoperativescores were compared. At the latest follow up, the Macnab system was used to evaluate the effects of the operation. RESULTS: The main symptom of 34 cases was severe radiation pain on one side of lower limbs. The duration of preoperative symptoms ranged from 0.33 to 84 months. The disc herniation was found in 7 cases of L and 27 cases of LS. According to the MSU division of lumbar disc herniation, 31 cases were located in area B. In all cases, it was confirmed that the protruding nucleus compressed the nerve root, and in 26 cases, the nerve root was obviously inflamed. The operation time ranged from 30 to 80 min, with a mean time of (43.5±9.5) min. The preoperative VAS score was 8.1±1.3 and ODI score was 31.8±6.7. And the VAS score was 1.1± 0.3, 0.7±0.4 on the first month after operation and the latest follow up, respectively. The ODI score was 5.3±2.1 and 0 to 10 (with a median score of 2) on the first month after operation and the latest follow-up respectively. The postoperative VAS and ODI scores were improved compared with preoperative scores.At the latest follow up, 28 cases got an excellent result and 6 cases good according to Macnab evaluation system. During the follow-up period, only one patient had recurrent disc herniation. CONCLUSION The main symptom of patients with tLDHSS is severe radiation pain on one side of lower limb. It manifests as sudden onset and shorter course of disease. Severe local inflammation was induced by local compression of the protruding nucleus pulposus on the nerve root out of the dura. For this kind of patients, thin layer CT scan has an important diagnostic value. In the treatment of this kind of patients, the symptoms are relieved rapidly, the curative effect is definite and the recurrence rate is low.
Adult ; Aged ; Diskectomy, Percutaneous ; Endoscopy ; Female ; Humans ; Intervertebral Disc Displacement ; Lower Extremity ; Lumbar Vertebrae ; Male ; Middle Aged ; Pain ; Retrospective Studies ; Treatment Outcome

Background: Glioma is the most common primary malignant tumor in the central nervous system. Because of the resistance of glioma to chemoradiotherapy and its aggressive growth, the survival rate of patients with glioma has not improved. This study aimed to disclose the effect of retinol dehydrogenase 10 (RDH10) on the migration and invasion of glioma cells, and to explore the potential mechanism. Methods: Reverse transcription-polymerase chain reaction (RT-PCR) was used to determine the expression levels of RDH10 in healthy glial cells and glioma cells. Human glioma cell strains, U87 and U251, were infected with negative control or RDH10-interfering lentiviruses. RT-PCR and Western blotting were performed to determine the knockdown efficiency. Scratch and transwell assays were used to assess cell migration and invasion after RDH10 knockdown. Finally, changes in transforming growth factor-β (TGF-β)/SMAD signaling pathway-related expression were examined by Western blotting. Differences between groups were analyzed by one-way analysis of variance. Results: RDH10 was highly expressed in glioma cells. Compared with the control group, RDH10 knockdown significantly reduced RDH10 messenger RNA and protein expression levels in U87 and U251 glioma cells (U87: 1.00 ± 0.08 vs. 0.22 ± 0.02, t= 16.55, P < 0.001; U251: 1.00 ± 0.17 vs. 0.39 ± 0.01, t= 6.30, P < 0.001). The scratch assay indicated that compared with the control group, RDH10 knockdown significantly inhibited the migration of glioma cells (U87: 1.00% ± 0.04% vs. 2.00% ± 0.25%, t= 6.08, P < 0.01; U251: 1.00% ± 0.11% vs. 2.48% ± 0.31%, t= 5.79, P < 0.01). Furthermore, RDH10 knockdown significantly inhibited the invasive capacity of glioma cells (U87: 97.30 ± 7.01 vs. 13.70 ± 0.58, t = 20.36, P < 0.001; U251: 96.20 ± 7.10 vs. 18.30 ± 2.08, t = 18.51, P < 0.001). Finally, Western blotting demonstrated that compared with the control group, downregulation of RDH10 significantly inhibited TGF-β expression, phosphorylated SMAD2, and phosphorylated SMAD3 (TGF-β: 1.00 ± 0.10 vs. 0.53 ± 0.06, t= 7.05, P < 0.01; phosphorylated SMAD2: 1.00 ± 0.20 vs. 0.42 ± 0.17, t= 4.01, P < 0.01; phosphorylated SMAD3: 1.00 ± 0.18 vs. 0.41 ± 0.12, t= 4.12, P < 0.01). Conclusion RDH10 knockdown might inhibit metastasis of glioma cells via the TGF-β/SMAD signaling pathway.

OBJECTIVETo analyze the complications of lumbar intervertebral disc herniation treated with percutaneous endoscopic lumbar discectomy(PELD), and discuss how to avoid these complications.

METHODSThe data of 132 patients with lumbar intervertebral disc herniation underwent PELD from October 2013 and June 2015 were retrospectively analyzed, including 85 males and 47 females with an average age of 42.9 years old. There were 6 cases of L₃,₄, 68 of L₄,₅ and 58 of L₅S₁. The incidences of intraoperative and postoperative complications were analyzed.

RESULTSThere was spinal dura mater injury in 1 patient, but no cerebrospinal fluid leakage and nerve function deficit was found, the muscle strength did not decrease postoperatively and the incision healed well. Two patients converted to open surgery ultimately because of stenosis of the intervertebral foramen and adhesion between nucleus pulposus and spinal dura mater; two patients complicated with early recurrence(in 3 months);nucleus pulposus residue developed in 3 patients; all of them were treated by open surgery and got satisfactory results. One patient with heart disease history complicated with supraventricular tachycardia after surgery and 2 patients with the increased cerebrospinal fluid pressure during surgery.

CONCLUSIONSPELD have a steep learning curve, and the technology is a safe and effective method in treating lumbar disc herniation, but the beginners must have enough open surgery experience, and to grasp indications strictly.

The purpose of this study was to investigate the effects of repetitive transcranial magnetic stimulation (rTMS) on patients with sleep bruxism (SB). Twelve patients with SB were included in an open, single-intervention pilot study. rTMS at 1 Hz and an intensity of 80% of the active motor threshold was applied to the ‘hot spot’ of the masseter muscle representation at the primary motor cortex bilaterally for 20 min per side each day for 5 consecutive days. The jaw-closing muscle electromyographic (EMG) activity during sleep was recorded with a portable EMG recorder at baseline, during rTMS treatment and at follow-up for 5 days. In addition, patients scored their jaw-closing muscle soreness on a 0–10 numerical rating scale (NRS). Data were analysed with analysis of variance. The intensity of the EMG activity was suppressed during and after rTMS compared to the baseline (P 5 0.04; P 5 0.02, respectively). The NRS score of soreness decreased significantly during and after rTMS compared with baseline (P,0.01). These findings indicated a significant inhibition of jaw-closing muscle activity during sleep along with a decrease of muscle soreness. This pilot study raises the possibility of therapeutic benefits from rTMS in patients with bruxism and calls for further and more controlled studies.

OBJECTIVETo explore the correlation among prevertebral hyperintensity (PVH), sagittal canal diameter on MRI and neurologic function of patients after cervical vertebral hyperextension injury without fracture and dislocation.

METHODSThe clinical data of 100 patients with cervical vertebral hyperextension injury without fracture and dislocation were retrospectively analyzed from September 2010 to December 2013. The patients were divided into PVH group and non-PVH group according to the presence of PVH on T2-weighted magnetic resonance imaging. There were 39 patients in PVH group, including 31 males and 8 females, aged from 21 to 83 years old with an average of (58.10 ± 14.78) years; and the other 69 patients in non-PVH group, including 49 males and 12 females, aged from 32 to 77 years old with an average of (55.05 ± 10.36) years. The sagittal disc level canal diameters of subaxial cervical spine were measured on mid-sagittal magnetic resonance imaging. The age, sex, cause of injury, and the segments of spinal stenosis were recorded. American Spinal Injury Association (ASIA) impairment scale and motor score were used to evaluate the neurological status.

RESULTSThe ASIA motor score of the group with PVH was 52.56 ± 31.97 while the ASIA motor score was 67.70 ± 22.83 in non-PVH group (P = 0.013). More patients with intramedullary hyperintensity signal on MRI were observed in the PVH group than in non-PVH group (P = 0.006). There was a significant positive correlation between ASIA motor score and sagittal disc level canal diameter of injury segment (P = 0.003). The neurological status was worse in patients with multi-level sagittal canal diameters below 8 mm.

CONCLUSIONThe PVH and the disc-level canal sagittal diameter of the injury segment are associated with neurological status. The patients with multi-level sagittal canal stenosis are vulnerable to severe cervical spinal cord injury.

Adult ; Aged ; Aged, 80 and over ; Cervical Vertebrae ; injuries ; Female ; Humans ; Magnetic Resonance Imaging ; Male ; Middle Aged ; Retrospective Studies ; Spinal Canal ; pathology ; Spinal Cord Injuries ; pathology ; physiopathology

OBJECTIVETo explore the usefulness of a head-space gas chromatography in the determination of residual solvents including methanol,ethanol,ethyl ether,and petroleum ether in muscone in artificial musk.

METHODSThe head-space gas chromatography was performed on HP-5(30 m×0.53 mm,5 Μm)capillary column with a hydrogen flame ionization detector. The carrier gas was nitrogen and the solvent was dimethyl sulfoxide. The injector temperature and the detector temperature were controlled at 180 ℃ and 250 ℃,respectively. The containers of head-space injector were preheated at 80 ℃ for 15 minutes. The column temperature was programmed raised,which achieved baseline separation of the components.

RESULTSThe results showed a good linear relationship for methanol,ethanol,ethyl ether,and petroleum ether(60-90 ℃)in the range of each consistency; and the limit of detection was 0.8,1.0,0.1,and 0.3 Μg/ml,respectively. The precision and average recoveries were satisfactory.

CONCLUSIONThe head-space gas chromatography is simple,rapid,and precise technique for measuring residual solvents in muscone.

Chromatography, Gas ; Cycloparaffins ; chemistry ; Drug Contamination ; Drugs, Chinese Herbal ; chemistry ; Ethanol ; analysis ; Solvents ; analysis