Anti-tumor mechanism of sesquiterpenoids from Cryptoporus volvatus based on molecular docking / 南方医科大学学报

OBJECTIVE@#To identify the target genes mediating anti-tumor effect of sesquiterpenoids from Cryptoporus volvatus and explore the possible mechanism using molecular docking and molecular dynamics simulation.@*METHODS@#Based on the chemical structure of sesquiterpenes from C. volvatus, we explored the online reverse target finding websites PharmMapper, SEA, Target Hunter and related literature for preliminary prediction of possible anti-tumor targets. Discovery Studio 4.0 (Libdock function) and Maestro 12.3 were used to connect sesquiterpenes with the possible targets, and the potential targets were selected according to the scores. The interaction between the sesquiterpenes and the targets were analyzed using 2D interaction diagram, and the influence of different sesquiterpene skeletons on their activity was inferred based on their activity measurements in experiment. Kinetic simulation was performed for front-end protein sequence (1UNQ) of the Akt (protein kinase B) and for the complex formed by 1UNQ and compound 4 (which had the best cytotoxic activity in vitro) in its optimal conformation, and the root mean square deviation (RMSD) value and root mean square float (RMSF) value of the complex and 1UNQ were measured to evaluate the stability of the binding of compound 4 to the target.@*RESULTS@#The sesquiterpenes showed optimal binding with 1UNQ. Analysis of 2D interaction diagram suggested that the hydrogen bonding and electrostatic force were the most important forces mediating the interaction between the sesquiterpenes and 1UNQ. Analysis of the optimal 3D conformation showed that for different sesquiterpenes, a slight change of the molecular framework produced a steric hindrance effect and caused changes in their bioactivity. Kinetic simulation showed that the complex formed by compound 4 and1UNQ had a lower RMSD than the target pure protein sequence, indicating that compound 4 could stably bind to 1UNQ. The anti-tumor effect of the sesquiterpenoids from C. volvatus was associated with their ability to cause Lys-144 acetylation, which blocks Akt binding to the downstream PIP3 and thus affects the proliferation of tumor cells.@*CONCLUSION@#1UNQ is the target of sesquiterpenoids from C. volvatus, which affects the proliferation of tumor cells by acetylating Lys-14.

Early diagnosis and treatment of chronic active Epstein-Barr virus hepatitis / 中国实用内科杂志

Non-hepatotropic viruses such as Epstein-Barr virus(EBV) has high infection rate in the population with biological characteristics of infective-latent-activation. EBV-related diseases including infectious mononucleosis(IM), chronic active EBV infection(CAEBV), EBV-related tumors and other diseases are complex and diverse, and all these can lead to varying degrees of liver damage.CAEBV can induce hepatitis(chronic active Epstein-Barr virus hepatitis, CAEBVH) or even liver failure. The prognosis of the disease is poor and the mortality rate is high. Early identification, diagnosis, and multidisciplinary collaborative treatment of CAEBVH are key to improving the prognosis of patients. This article will review the diagnosis and treatment progress of CAEBVH, and provide references for clinicians to diagnose and treat CAEBVH.

Glycolipids from Polygala sibirica var. megalopha and their in vitro inhibitory activity on xanthine oxidase / 中草药

Objective: To investigate the glycolipids from Polygala sibirica var. megalopha and their structure-activity relationship of xanthine oxidase (XO) inhibitory activity. Methods: The 75% EtOH extract of P. sibirica var. megalopha was chromatographied with D101 macroporous resins column by water, 35% EtOH, 65% EtOH, and 95% EtOH, successively. Compared to other elution parts, the 65% EtOH elution part exhibited stronger XO inhibition. Further bioassay-guided separation led to the isolation of four known glycolipids, which demonstrated potent XO inhibition. Results: Four compounds were identified to be tenuifoliside A (1), 3,6'-disinapoyl sucrose (2), 3'-E-3,4,5-trimethoxycinnamoyl-6-benzoyl sucrose (3), and 3'-E-3,4,5-trimethoxycinnamoyl-4-benzoyl sucrose (4) through spectroscopic data analysis. All compounds were obtained from this plant for the first time. This enzyme inhibition was dose dependent and the IC50 values of compounds 1, 3, and 4 were 9.5, 10.2, and 7.7 μmol/L, respectively. Among them, compound 2 had significantly higher XO inhibitory activity than that of the control allopurinol (IC50=11.2 μmol/L). It was speculated that the styryl side chain linking with sugar base played an important role on the XO inhibitory activity. Conclusion: Glycolipides as a novel series of XO inhibitors, may be developed into a promising remedy for human gout.

Efficacy observation on electroacupuncture in the treatment of oculomotor impairment caused by ophthalmic nerve injury / 中国针灸

<p><b>OBJECTIVE</b>To observe the difference in the clinical efficacy on oculomotor impairment between electroacupuncture and acupuncture and explore the best therapeutic method in the treatment of this disease.</p><p><b>METHODS</b>Sixty cases of oculomotor impairment were randomized into an electroacupuncture group and an acupuncture group, 30 cases in each one. In the electroacupuncture group, the points were selected on extraocular muscles, the internal needling technique in the eye was used in combination of electroacupuncture therapy. In the acupuncture group, the points and needling technique were same as the electroacupuncture group, but without electric stimulation applied. The treatment was given 5 times a week, 15 treatments made one session. After 3 sessions of treatment, the clinical efficacy, palpebral fissure size, pupil size, oculomotor range and the recovery in diplopia were compared before and after treatment in the two groups.</p><p><b>RESULTS</b>In the electroacupuncture group, the palpebral fissure size was (9.79+/-2.65)mm and the eyeball shifting distance was (18.12+/-1. 30)mm, which were hig-her than (8.23+/-2.74)mm and (16.71+/-1. 44)mm respectively in the acupuncture group. In the electroacupuncture group, the pupil diameter was (0. 44 +/-0. 42)mm, which was less than (0. 72 +/- 0. 53)mm in the acupuncture group, indicating the significant difference (all P<0. 05). The cured rate was 63. 33% (19/30) and the total effective rate was 93.33% (28/30) in the electroacupuncture group, which was better than 36.67% (11/30) and 83. 333 (25/30) in the acupuncture group separately, indicating the significant difference (all P<0. 05).</p><p><b>CONCLUSION</b>Electroacupuncture presents the obvious advantages in the treatment of oculomotor impairment, characterized as quick and high effect, short duration of treatment and remarkable improvements in clinical symptoms, there are important significance for the improvement of survival quality of patients.</p>

Effect of long-term monotherapy of atypical antipsychotics on the levels of body mass index, leptin concentration and insulin resistance in patients with schizophrenia / 中国药学杂志

OBJECTIVE: To compare the effects of clozapine, olanzapine and resperidone on the levels of body mass index (BMI), leptin, fasting insulin concentration(FINS) and insulin resistance(IR) in inpatients with schizophrenia; to investigate the relationship between BMI, leptin, FINS and IR in subjects. METHODS: Seventy-four Chinese inpatients with schizophrenia, treated with monotherapy of clozapine (n=27), risperidone (n=19) and olanzapine (n=13) for at least one year or unmedicated (n=15), were recruited; Levels of BMI, leptin, FINS and were measured, homeostasis model assessment of insulin resistance(HOMA-IR) were performed. RESULTS: Significant difference in the mean levels of BMI was the found between four groups (P<0.05). In post hoc test, it was seen that clozapine and olanzapine-treated patients had higher levels of BMI than those in risperidone and control group; there was a significant difference in the level of leptin (P<0.05), which was the highest in clozapine-treated patients; in the comparison of the mean values of FINS and HOMA-IR levels between four groups, there was no statistically significant difference. There was a positive correlation between BMI and leptin leves, FINs, and HOMA-IR (p<0.05). CONCLUSION: Treatment with clozapine, olanzapine and risperidone is associated with abnormal glucose and lipid metabolism in inpatients with schizophrenia. The positive correlation between BMI and serum leptin, fasting serum insulin levels, HOMA-IR suggests that the increase of serum leptin and fasting serum insulin levels would be an important trait of metabolic syndrome related to monotherapy of treatment with clozapine, olanzapine and risperidone in inpatients with schizophrenia.

Progress of treatment on oculomotor paralysis with electroacupuncture / 中国针灸

Collecting information from the database of China National Knowledge Information (CNKI) and VIP database of Chinese Journals, an overall analysis and review on treatment of oculomotor paralysis with electroacupuncture in recently years are made in the paper. The electroacupuncture, which can provide constant stimulation and reinforce the effect of acupuncture, is the major therapy to treat oculomotor paralysis. However, the best stimulate threshold of electroacupuncture on oculorotary muscles has not been reported yet. The parameters of electroacupuncture adopted in clinic are not standardized, which lead to unfavorable therapeutic effect as well as unclear mechanism of treatment. Therefore, it is suggested that the study should focus on enhancing the research level and broadening researcher's mind to explore the best parameter for the electroacupuncture stimulation on the oculorotary muscles, to make clear the mechanism of treatment and to search for valuable observation indicators in the future.

Experimental study on electroacupuncture for strengthening gastrointestinal motility in the rat with acute pancreatitis / 中国针灸

<p><b>OBJECTIVE</b>To explore the mechanism of EA in treatment of acute pancreatitis.</p><p><b>METHODS</b>Twenty-four healthy male Wistar rats were randomly divided into 3 groups, a control group, a model group and an EA group. In the model group, rat acute pancreatitis model was prearpared by intraperitoneal injection of Caerulein, and in the EA group, EA was given at "Zusanli" (ST 36) and "Tianshu" (ST 25) of the model rat. The gastric emptying rate, small intestinal impelling ratio, myeloperoxidase activity in the pancreas tissue, pathological score of the pancreas and serum amylase were detected.</p><p><b>RESULTS</b>Compared with the control group, both the gastric emptying rate and the intestinal impelling ratio significantly decreased in the model group (P<0.05), and they significantly increased in the EA group compared with the model group (P<0.05). Myeloperoxidase activity in the pancreas tissue, pathological score of the pancreas and serum amylase activity significantly decreased in the EA group as compared with the model group (P<0.05).</p><p><b>CONCLUSION</b>EA can significantly improve the disturbance of gastrointestinal motility induced by acute pancreatitis and relieve pathological damage of pancreas.</p>

Observation on therapeutic effect of eye-needling combined with medication for treatment of ophthalmoplegia / 中国针灸

<p><b>OBJECTIVE</b>To observe the therapeutic effect of eye-needling combined with medication for treatment of ophthalmoplegia and explore the possible mechanism.</p><p><b>METHODS</b>One hundred and twenty cases were randomly divided into a treatment group and a control group. According to etiological factors, the control group were treated with medication and the treatment group with the medication plus eye-acupuncture at main point ocular muscles. Changes of the rima oculi, the range of ocular movement and the dialopia angle after treatment were recorded and statistically analyzed in the two groups.</p><p><b>RESULTS</b>The total effective rate was 93.4% and the cured rate was 54.1% in the treatment group, and 74.6% and 18.6% in the control group, with significant difference between the two groups (P < 0. 01).</p><p><b>CONCLUSION</b>Eye-needling combined with medication has an obvious therapeutic effect which is better than simple medication for ophthalmoplegia.</p>

Effects of irrigation volume on growth and quality of Lonicera japonica / 中国中药杂志

<p><b>OBJECTIVE</b>To study the effects of irrigation volume on the growth and quality of Lonicera japonica.</p><p><b>METHOD</b>Different volume of irrigation water was applied to the potted L. japonica before the first florescence of honeysuckle in order to keep the relative moisture content of the soil as 100%, 80%, 50%, 30%, and observe the growth and development of shoot and leaves, yield and quality of honeysuckle.</p><p><b>RESULT</b>As the of irrigation volume was reduced, the internodal elongation of shoot and the increase of the knot were restrained, and the yield of honeysuckle dropped. But the content of chlorogen acid in the buds treated by 80% irrigation volume was not affected, while that of the other treatment all decreased. The moisture contents of the leaves treated by 30% irrigation volume was significantly lower than that of the CK, while the specific leaf weight (SLW) increased significantly comparing to the CK. The content of chlorophyl in the leaves of 50% and 30% increased, while the ratio of chlorophyl A and B fell significantly. The content of dissoluble suger in the leaves of 80% and 50% irrigation volume was much higher than that in the CK. The results also showed that, the content of dissoluble protein in the leaves of 30% irrigation volume increased comparing with that in 50%, and the content of proline in leaveas of 30% irrigation volume increased significantly.</p><p><b>CONCLUSION</b>Using less irrigation volume (keeping 80% of relative moisture content of the soil) does not affect the quality of honeysuckle, but decreased dry weight of honeysuckle. It is necessary to take irrigation management during cultivation of honeysuckle.</p>

Effect of electroacupuncture on myoelectric activity of Jejunal limb After Roux-en-Y esophagojejunostomy / 中国针灸

<p><b>OBJECTIVE</b>To explore the effect of electroacupuncture on myoelectric activity of Jejunal limb after Roux-en-Y esophagojejunostomy.</p><p><b>METHODS</b>Fourteen health young pigs were randomly divided into 2 groups, an experimental group (total gastrectomy and Roux-en-Y esophagojejunostomy was carried out) and a control group (the abdominal cavity was closed after the electrode was placed), 7 pigs in each group. Electroacupunture was given at "Zusanli" (ST 36) in the experimental group. The changes of myoelectrogram of the jejunal limb was investigated.</p><p><b>RESULTS</b>Compared with the control group, the amplitude and the frequency of the slow wave, and the amplitude and incidence rate of the spike potential in the experimental group were changed significantly; the duration of migrating motor complex (MMC) phase III was (2.6 +/- 0.7) minutes in the experimental group, which was significantly shorter than (7.1 +/- 1.1) minutes in the control group. Electroacupuncture did not significantly influence the amplitude and the frequency of the slow wave, but could increased significantly the incidence rate and the amplitude of the spike potential; after electroacupuncture, the duration of MMC phase III was (5.7 +/- 0.9) minutes, which was significantly longer than (2.6 +/- 0.7) minutes before electroacupuncture.</p><p><b>CONCLUSION</b>Electroacupuncture at "Zusanli" (ST 36) can relieve the Roux-en-Y stasis syndrome through influencing myoelectric activity of the jejunum.</p>

Observation on therapeutic effect of electroacupuncture at points Baliao and Huiyang (BL 35) on retention of urine induced by spinal cord injury / 中国针灸

<p><b>OBJECTIVE</b>To explore a more effective therapy for retention of urine induced by spinal cord injury.</p><p><b>METHODS</b>Eighty-four cases were randomly divided into a treatment group of 46 cases and a control group of 38 cases. The treatment group were treated with electroacupuncture at Baliao and Huiyang (BL 35), and the control group with electroacupuncture at acupoints routinely selected.</p><p><b>RESULTS</b>The total effective rate and the cured rate were 82.6% and 43.5% in the treatment group and 63.2% and 23.7% in the control group respectively, with a very significant difference between the two groups (P < 0. 01).</p><p><b>CONCLUSION</b>Electroacupuncture at Baliao and Huiyang (BL 35) has obvious therapeutic effect on retention of urine induced by spinal cord injury.</p>