The Effects of Acupressure on Improving Health and Reducing Cost for Patients Undergoing Thoracoscopic Surgery.

OBJECTIVES: This study aimed to assess the effectiveness of practicing acupressure on the Shenmen and Neiguan acupoints with a view to reduce anxiety and improve the comfort and physical health of patients undergoing thoracoscopic surgery. METHODS: A total of 100 hospitalized patients undergoing thoracoscopic surgery were assigned randomly into the experimental (n = 49) and control groups (n = 51). Subjects in the experimental group received routine care plus acupressure on the Shenmen and Neiguan acupoints, while those in the control group received regular routine care. The data were collected using demographic information, physical and surgical data, the Visual Analog Scale (VAS)-A, the State-Trait Anxiety Inventory Y Form (STAI-Y1), and Shortened General Comfort Questionnaire scores. The linear mixed model was used to examine the influences of acupressure on VAS-A and STAI-Y1 scores at different time points before and after the surgery to observe group-by-time interactions. RESULTS: The mean age of the subjects was 60.97 years. All subjects had mild-to-moderate anxiety after surgery and showed a statistically significant decline in regression coefficients on the first and second days after the intervention (ß = -11.61, p = 0.002; ß = -18.71, p < 0.001). Similarly, for STAI-YI scores, the data showed a significant difference in the pre-test and post-test interactions between the two groups (ß = 4.72, p = 0.031). Conversely, acupressure did not have a statistically significant difference on comfort (F = 2.953, p = 0.057). Compared with the control subjects, the experimental subjects used less morphine and developed side effects less frequently (p < 0.01). They were also able to get out of bed after surgery 163.79 min earlier (p < 0.05). CONCLUSIONS: Acupressure is a simple and easy-to-practice treatment. Acupressure on the Shenmen and Neiguan acupoints reduces anxiety and improves recovery in patients after undergoing thoracoscopic surgery.

The effectiveness of acupressure for managing postoperative pain in patients with thoracoscopic surgery: A randomized control trial.

PURPOSE: More than 86% patients experience moderate to severe pain after thoracoscopic surgery. A combination of diverse nonpharmacological pain relief methods is a developing trend for pain management. The purpose of this study was to explore the effect of acupressure in reducing pain after thoracoscopic surgery. DESIGN: A Randomized controlled study with purpose sampling was used for this study. Patients who underwent thoracoscopic surgery at a medical center in central Taiwan were enrolled. Study data was collected from September 2020 to April 2021 after the approval of the institutional review board. A total of 100 participants were randomized into two groups (49 and 51 in the experimental and control groups, respectively). METHODS: Participants in the experimental group received acupressure at the Neiguan (PC6) and Shenmen (HT7) acupoints thrice a day for 2 days, whereas those in the control group received routine treatment and did not receive acupressure. The measurement included questionnaires for the collection of general information, physiological information, and disease rating scale. The Visual Analogue Scale-Pain (VAS-P) was used to measure the severity of pain. SPSS statistical software was used for data analysis. Independent sample t-test and chi-squared test were used for descriptive statistics, and paired t-test and linear mixed model were used to examine the effect of acupressure in alleviating pain. FINDINGS: After acupressure intervention, the pain score of the experimental group was lower than that of the control group, and this difference was significant ß = 17.76, p < 0.001 on day 1 after intervention; ß = 19.80, p < 0.001 on day 2 after intervention. The postoperative pain score in the experimental group on day 2 after intervention was significantly lower than that in the control group (t = 2.039, p = 0.044). After the subjects received acupressure, pain index significantly decreased after considering the interaction between time and group (p < 0.001). Regardless of the type of surgery, there were significant differences in pain index when the interaction between time and group was considered (p < 0.001). CONCLUSIONS: This study provided an experimental basis that acupressure can help in pain management in patients after thoracoscopic surgery, and the pain relief results become more significant as the duration of intervention increases. CLINICAL RELEVANCE: Acupressure is effective in relieving postoperative pain in any type of thoracoscopic surgery. Nurses can use acupressure to help control pain in patients after thoracoscopic surgery.

Integrative Effects and Vagal Mechanisms of Transcutaneous Electrical Acustimulation on Gastroesophageal Motility in Patients With Gastroesophageal Reflux Disease.

INTRODUCTION: Impaired esophageal and gastric motilities are known to contribute to symptoms of gastroesophageal reflux disease (GERD). However, there is a lack of GERD therapy, targeting both gastric and esophageal functions. This study was designed to investigate the effects of transcutaneous electrical acustimulation (TEA) on symptoms of GERD and gastroesophageal functions and possible mechanisms in patients with GERD. METHODS: Thirty patients with GERD with ineffective esophageal motility were equally divided and randomized into a 4-week sham-TEA or 4-week TEA treatment. The GERD questionnaire (GerdQ), GERD health-related quality-of-life questionnaire, high-resolution esophageal manometry, a nutrient drink test, the electrogastrogram, and ECG were performed to assess the severity of reflux symptoms, low esophageal sphincter (LES) pressure, distal contractile integral (DCI), gastric accommodation, gastric slow waves (GSW), and autonomic functions, respectively. RESULTS: Compared with sham-TEA, the 4-week TEA treatment significantly decreased the GerdQ score (P = 0.011) and GERD health-related quality of life (P = 0.028) and improved nutrient drink-induced fullness (P < 0.001) and belching (P < 0.001) in patients with GERD. Although only acute TEA significantly enhanced LES pressure (P < 0.05), both acute and chronic TEA remarkedly increased DCI (P < 0.05) and reduced the incidence of ineffective esophageal contractions during wet swallows (P = 0.02). In addition, chronic TEA significantly increased gastric accommodation and the percentage of postprandial normal GSW compared with sham-TEA and baseline. Concurrently, TEA-enhanced vagal activity (P = 0.02) and the vagal activity positively correlated with LES pressure (r = 0.528; P = 0.003) and DCI (r = 0.522; P = 0.003). DISCUSSION: The TEA treatment performed in this study improves reflux-related symptoms, increases DCI, reduces the incidence of ineffective esophageal contractions during wet swallows, and improves gastric accommodation and slow waves. The improvement in GERD symptoms might be attributed to the integrative effects of TEA on these gastroesophageal functions mediated via the vagal mechanism.

Cell-based 3D bionic screening by mimicking the drug-receptor interaction environment in vivo.

Most small-molecule drugs influence cell behavior through their interaction with one or more cellular proteins. The efficacy is unanticipated in the later stages of drug development if small-molecule drugs are discovered in the absence of a biological context. Bionic screening is an in vivo drug-receptor interaction platform that can identify small molecules with recognized activity, improving the likelihood of drug efficacy in the clinic. Here, we report the design of an innovative cell-based bionic screening system using 3D microcarrier cultures to simulate in vivo conditions and facilitate small-molecule drug discovery. Through its combination with HPLC/MS, the method can comprehensively identify small-molecule lead compounds in arbitrarily complex systems in an unbiased manner. In particular, cell-covered microcarriers provide a high-density of cells for affinity performance assessments in the absence of appreciable cell damage and maintain immunogenicity, the 3D structure of which is similar to tissue morphology in vivo, thereby mimicking in vivo drug-receptor interactions. The method is scalable, easy to handle, and requires minimal optimization across a range of different cell lines to realize high-throughput drug screening for the corresponding diseases. This provides a valuable tool for lead compound discovery in more physiologically relevant systems and may address the lack of clinically available drugs.

Stepwise frontal analysis coupled with cell membrane chromatography for affinity screening and characterization analysis of bioactive constituent from the mature fruits of schisandra chinensis.

Cell membrane chromatography (CMC) is effective and widely used in drug screening, especially for the analysis of complex matrixes. However, it is time-consuming and costly given that cells or animals are employed for activity confirmation, which leads to a large amount of waste being produced if the result is negative. Stepwise frontal analysis is employed to saturate the affinity stationary phase, by using a series of low- to high-concentration solutions which resultantly form a staircase pattern. In doing so, the waste of samples, caused by the balancing process, can be avoided. In this study, stepwise frontal analysis coupled with a CMC system was performed for screening and characterizing the affinity of an active compound from wuweizi. Schizandrin A was screened and identified by α1A AR /CMC coupled with UHPLC-MS/MS. By comparing the values obtained with those related to the equilibrium dissociation constant (Kd) calculated by zonal elution, the accuracy of the stepwise frontal analysis was verified. Subsequently, the type of affinity force between Schizandrin A and α1A AR was studied by thermodynamic parameters. Moreover, schizandrin A showed an antagonistic effect on phenylephrine-induced contractions, which relax prostate muscle strips in a non-competitive antagonism manner. It has already suggested that the active compound, schizandrin A, could be used as a lead compound for the treatment of benign prostate hyperplasia (BPH) and should be further studied. Thus, the findings of this study are significant given that they could result in an online screening and affinity analysis method being utilized for the discovery of medicinal compounds as well as clarify the interaction characteristics between a drug and a receptor.

miR-541 potentiates the response of human hepatocellular carcinoma to sorafenib treatment by inhibiting autophagy.

OBJECTIVE: Autophagy participates in the progression of hepatocellular carcinoma (HCC) and the resistance of HCC cells to sorafenib. We investigated the feasibility of sensitising HCC cells to sorafenib by modulating miR-541-initiated microRNA-autophagy axis. DESIGN: Gain- and loss-of-function assays were performed to evaluate the effects of miR-541 on the malignant properties and autophagy of human HCC cells. Autophagy was quantified by western blotting of LC3, transmission electron microscopy analyses and confocal microscopy scanning of mRFP-GFP-LC3 reporter construct. Luciferase reporter assays were conducted to confirm the targets of miR-541. HCC xenograft tumours were established to analyse the role of miR-541 in sorafenib-induced lethality. RESULTS: The expression of miR-541 was downregulated in human HCC tissues and was associated with malignant clinicopathologic phenotypes, recurrence and survival of patients with HCC. miR-541 inhibited the growth, metastasis and autophagy of HCC cells both in vitro and in vivo. Prediction software and luciferase reporter assays identified autophagy-related gene 2A (ATG2A) and Ras-related protein Rab-1B (RAB1B) as the direct targets of miR-541. Consistent with the effects of the miR-541 mimic, inhibition of ATG2A or RAB1B suppressed the malignant phenotypes and autophagy of HCC cells. Furthermore, siATG2A and siRAB1B partially reversed the enhancement of the malignant properties and autophagy in HCC cells mediated by the miR-541 inhibitor. More interestingly, higher miR-541 expression predicted a better response to sorafenib treatment, and the combination of miR-541 and sorafenib further suppressed the growth of HCC cells in vivo compared with the single treatment. CONCLUSIONS: Dysregulation of miR-541-ATG2A/RAB1B axis plays a critical role in patients' responses to sorafenib treatment. Manipulation of this axis might benefit survival of patients with HCC, especially in the context of the highly pursued strategies to eliminate drug resistance.

Ameliorating Effects and Autonomic Mechanisms of Transcutaneous Electrical Acustimulation in Patients With Gastroesophageal Reflux Disease.

BACKGROUND/AIM: Gastric dysmotility is one of pathophysiologies of gastroesophageal reflux disease (GERD). The aim of this study was to investigate the effects of transcutaneous electrical acustimulation (TEA) on gastric accommodation and gastric slow waves, and evaluate possible mechanisms in patients with GERD. METHODS: Thirty patients were studied in two randomized sessions of sham-TEA and TEA with the measurements of esophageal high-resolution manometry (HRM), gastric accommodation assessed by a nutrient-drinking test, electrogastrogram (EGG), electrocardiogram (ECG), and postprandial dyspeptic symptoms. RESULTS: Compared with sham-TEA, TEA improved nutrient drinking-induced fullness (42.0 ± 3.3 vs. 31.0 ± 3.5, P = 0.003) at 10 min after the drink, and belching right after the drink (22.0 ± 4.6 vs. 11.7 ± 3.1, P = 0.012) and at 10 min (16.0 ± 3.8 vs. 3.0 ± 1.5, P = 0.002) after the drink. TEA also improved gastric accommodation (954 ± 37 mL vs. 857 ± 47 mL, P = 0.001) and normalized maximal drink-induced impairment in gastric slow waves. Concurrently, TEA enhanced vagal activity assessed from spectral analysis of heart rate variability in the postprandial state (0.42 ± 0.03 vs. 0.49 ± 0.04, P = 0.039). The vagal activity was positively correlated with the percentage of normal slow waves (r = 0.528; P = 0.003) and negatively correlated with the regurgitation score (r = -0.408, P = 0.025). CONCLUSIONS: Acute TEA increases gastric accommodation, improves gastric slow waves, and reduces postprandial fullness and belching, possibly mediated via the vagal mechanisms.

Tai Chi can prevent cardiovascular disease and improve cardiopulmonary function of adults with obesity aged 50 years and older: A long-term follow-up study.

To research the possible role of Tai Chi in preventing cardiovascular disease and improving cardiopulmonary function in adults with obesity aged 50 years and older.Between 2007 and 2012, 120 adults with obesity, aged 50 years and older, were divided into a Tai Chi group and a control group, with 60 participants in each group. The 2 groups were evaluated for weight, waist circumference, hip circumference, blood pressure (BP), body mass index, and incidence of chronic disease during follow-up monitoring.Two- and 6-year follow-up showed that the average BP in the Tai Chi group along with either the systolic or diastolic pressure decreased significantly compared to those in the control group (P < .001). Waist and hip circumference, weight, and body mass index in the Tai Chi group were significantly reduced compared to those in the control group (P < .001). The cardiopulmonary function of the control group and the Tai Chi group changed, with the cardiac index significantly higher in the Tai Chi group than in the control group (P < .05). The Tai Chi group had significantly higher levels of lung function, including vital capacity, maximal oxygen uptake, and total expiratory time, than the control group. The total incidence of complications and mortality in the Tai Chi group were much lower than those in the control group (P < .001). The incidence of cardiovascular and cerebrovascular disease in the Tai Chi group (16.67%) was lower than that in the control group (38.33%).Tai Chi is not only a suitable exercise for elderly people with obesity, but it can also help to regulate BP, improve heart and lung function in these individuals, as well as reduce the incidence of cardiovascular disease and other chronic diseases, helping to improve their quality of life.

Structural Characterization and Antioxidant Activity of Polysaccharides from Athyrium multidentatum (Doll.) Ching in d-Galactose-Induced Aging Mice via PI3K/AKT Pathway.

The purpose of this study was to characterize the polysaccharides from Athyrium multidentatum (Doll.) Ching (AMC) rhizome and explore the protective mechanism against d-galactose-induced oxidative stress in aging mice. METHODS: A series of experiments, including molecular weight, monosaccharide composition, Fourier transform infrared (FT-IR) spectroscopy, and 1H nuclear magnetic resonance (1H NMR) spectroscopy were carried out to characterize AMC polysaccharides. The mechanism was investigated exploring d-galactose-induced aging mouse model. Quantitative real-time reverse transcription polymerase chain reaction (RT-qPCR) and western blotting assays were performed to assess the gene and protein expression in liver. KEY FINDINGS: Our results showed that AMC polysaccharides were mainly composed of mannose (Man), rhamnose (Rha), glucuronic acid (Glc A), glucose (Glc), galactose (Gal), arabinose (Ara), and fucose (Fuc) in a molar ratio of 0.077:0.088:0.09:1:0.375:0.354:0.04 with a molecular weight of 33203 Da (Mw). AMC polysaccharides strikingly reversed d-galactose-induced changes in mice, including upregulated phosphatidylinositol 3-kinase (PI3K), Akt, nuclear factor-erythroid 2-related factor 2 (Nrf2), forkhead box O3a (FOXO3a), and hemeoxygenase-1 (HO-1) mRNA expression, raised Bcl-2/Bax ratio, downregulated caspase-3 mRNA expression, enhanced Akt, phosphorylation of Akt (p-Akt), Nrf2 and HO-1 protein expression, decreased caspase-3, and Bax protein expression. CONCLUSION: AMC polysaccharides attenuated d-galactose-induced oxidative stress and cell apoptosis by activating the PI3K/AKT pathway, which might in part contributed to their anti-aging activity.

Striatisporolide A, a butenolide metabolite from Athyrium multidentatum (Doll.) Ching, as a potential antibacterial agent.

The present study aimed to investigate the antibacterial activity of striatisporolide A (SA) against Escherichia coli (E. coli) and the underlying mechanism. Antibacterial activity was evaluated according to the inhibitory rate and zone of inhibition. The antibacterial mechanism was investigated by analyzing alkaline phosphatase (AKP) activity and ATP leakage, protein expression, cell morphology and intracellular alterations in E. coli. The results demonstrated that SA exerted bacteriostatic effects on E. coli in vitro. AKP activity and ATP leakage analysis revealed that SA damaged the cell wall and cell membrane of E. coli. SDS­PAGE analysis indicated that SA notably altered the level of 10 and 35 kDa proteins. Scanning electron microscopy and transmission electron microscopy analyses revealed marked alterations in the morphology and ultrastructure of E. coli following treatment with SA. The mechanism underlying the antimicrobial effects of SA against E. coli may be attributed to its actions of disrupting the cell membrane and cell wall and regulation of protein level. The findings of the present study provide novel insight into the antimicrobial activity of SA as a potential natural antibacterial agent.

The Evaluation of Proanthocyanidins/Chitosan/Lecithin Microspheres as Sustained Drug Delivery System.

Proanthocyanidin (PC) has attracted wide attention on cosmetics and pharmaceutical due to its antioxidant, anticancer, antimicrobial, antiangiogenic, and anti-inflammatory activities. However, PC applications are limited because of its sensitivity to thermal treatment, light, and oxidation and the poor absorption in the gastrointestinal tract. Thus, a novel dosage form of PC needs to be designed to improve its stability and bioavailability for drug delivery. The objective of this study is to fabricate proanthocyanidins/chitosan/lecithin (PC/CTS/LEC) microspheres and investigate various characteristics. In the current study, PC/CTS/LEC microspheres were prepared by spray-drying technology. The yield (61.68%), encapsulation efficiency (68.19%), and drug loading capacity (17.05%) were found in the results. The scanning electron microscope demonstrated that the microspheres were spherical in shape with wrinkled surfaces. DSC study displayed that the microspheres stability was greatly improved when comparing with bare PC. The in vitro release study showed that the 76.92% of PC was released from microspheres within 48 h. The moisture contents of microspheres ranged from 8% to 13%. The swelling rate and tapped density of microspheres were elevated with increasing the concentration of chitosan in the formulations. The moisture uptake of microspheres was saturated at 40°C/RH75% within 12 h. Our results indicated that the stability of PC/CTS/LEC microspheres was enhanced, and it is a promising carrier for sustained drug delivery system.

Hot Compress with Chinese Herbal Salt Packets Reducing PICC Catheter Complications: A Randomized Controlled Trial.

OBJECTIVE: To explore the preventive effect of applying hot compress with Chinese herbal salt packets (CHSP) to puncture vessels under aseptic conditions during peripherally inserted central catheter (PICC) on postoperative phlebitis. METHODS: A total of 720 hospitalized patients undergoing first PICC were assigned to treatment and control groups (360 cases each group) according to a random number table. The control group received conventional catheterization and nursing care. The treatment group was first given hot compress with CHSP (which consisted of honeysuckle 30 g, Semen brassicae 30 g, Salvia miltiorrhiza 30 g, Angelica dahurica 30 g, Semen raphani 30 g, Evodia rutaecarpa 30 g, and coarse salt 20 g) on the punctured vessel under aseptic conditions for 5-10 min before conventional catheterization. The main efficacy indices were the vessel diameters before and during catheterization and the success rate of a single catheter, and the secondary efficacy indiex was the incidence of superficial phlebitis within 1 week after catheterization. RESULTS: The vessel diameter during catheterization of the treatment group was remarkably increased compared with the control group [(7.96±0.42) mm vs. (4.39±0.54) mm, P<0.01]. The success rate of the single catheter of the treatment group was significantly higher than that of the control group [94.00% (329/350) vs. 73.72% (244/329), P<0.01]. The incidence of superficial phlebitis within 1 week after catheterization in the treatment group was lower than that in the control group (P=0.007). There was no adverse event with CHSP. CONCLUSION: Hot compress with CHSP during PICC is applicable as it can effectively improve the success rate of a single catheter and reduce the incidence of superficial phlebitis after catheterization (Trial registration No. ChiCTR-ONC-17010498).

Screening of bioactive components from traditional Chinese medicines using cell membrane chromatography coupled with mass spectrometry.

INTRODUCTION: Cell membrane chromatography (CMC), as a highly selective type of affinity chromatography, has been demonstrated as an effective method to screen bioactive components acting on specific receptor from a complicated biological system. OBJECTIVE: To review the recent research progress and the technical applications of these analytical methods using CMC combined with gas chromatography-mass spectrometry, (GC/MS) and liquid chromatography-mass spectrometry (LC/MS). METHODOLOGY: In this review, we briefly introduce the CMC offline GC/MS, CMC online GC/MS, CMC offline LC/MS, and CMC online LC/MS system. And the practical application of these technologies is also enumerated. Then the future of these technologies and research methods were discussed. RESULTS: Many bioactive components interacting with specific receptors have been screened and identified in traditional Chinese medicines. CONCLUSION: CMC technique has been combined with GC/MS and HPLC/MS and these combined systems have been successfully used to screen bioactive components acting on specific receptors from a complicated biological system.

Hot Compress with Chinese Herbal Salt Packets Reducing PICC Catheter Complications: A Randomized Controlled Trial / 中国结合医学杂志

<p><b>OBJECTIVE</b>To explore the preventive effect of applying hot compress with Chinese herbal salt packets (CHSP) to puncture vessels under aseptic conditions during peripherally inserted central catheter (PICC) on postoperative phlebitis.</p><p><b>METHODS</b>A total of 720 hospitalized patients undergoing first PICC were assigned to treatment and control groups (360 cases each group) according to a random number table. The control group received conventional catheterization and nursing care. The treatment group was first given hot compress with CHSP (which consisted of honeysuckle 30 g, Semen brassicae 30 g, Salvia miltiorrhiza 30 g, Angelica dahurica 30 g, Semen raphani 30 g, Evodia rutaecarpa 30 g, and coarse salt 20 g) on the punctured vessel under aseptic conditions for 5-10 min before conventional catheterization. The main efficacy indices were the vessel diameters before and during catheterization and the success rate of a single catheter, and the secondary efficacy indiex was the incidence of superficial phlebitis within 1 week after catheterization.</p><p><b>RESULTS</b>The vessel diameter during catheterization of the treatment group was remarkably increased compared with the control group [(7.96±0.42) mm vs. (4.39±0.54) mm, P<0.01]. The success rate of the single catheter of the treatment group was significantly higher than that of the control group [94.00% (329/350) vs. 73.72% (244/329), P<0.01]. The incidence of superficial phlebitis within 1 week after catheterization in the treatment group was lower than that in the control group (P=0.007). There was no adverse event with CHSP.</p><p><b>CONCLUSION</b>Hot compress with CHSP during PICC is applicable as it can effectively improve the success rate of a single catheter and reduce the incidence of superficial phlebitis after catheterization (Trial registration No. ChiCTR-ONC-17010498).</p>

Inhibitory Effect of Propolis on Platelet Aggregation In Vitro.

Platelet hyperactivity plays an important role in arterial thrombosis and atherosclerosis. The present study was aimed to investigate the effects of different extracts of propolis and components of flavonoids on platelet aggregation. Platelet-rich plasma was prepared and incubated in vitro with different concentrations of the tested extracts and components of flavonoids. Platelets aggregation was induced by different agonists including adenosine diphosphate (ADP, 10 µM), thrombin receptor activator peptide (TRAP, 50 µM), and collagen (5 µg/mL). At 25 mg/L to 300 mg/mL, the water extract propolis (WEP) inhibited three agonists-induced platelet aggregations in a dose-dependent manner. The flavonoids isolated from the propolis also showed markedly inhibited platelet aggregation induced by collagen, ADP, and TRAP, respectively. The components including caffeic acid phenethyl ester (CAPE), galangin, apigenin, quercetin, kaempferol, ferulic acid, rutin, chrysin, pinostrobin, and pinocembrin and their abilities of inhibiting platelet aggregation were studied. It was concluded that propolis had an antiplatelet action in which flavonoids were mainly implicated.

Characterization the affinity of α1A adrenoreceptor by cell membrane chromatography with frontal analysis and stoichiometric displacement model.

As a bionic chromatographic method, cell membrane chromatography (CMC) has been used widely in screening active components in traditional Chinese medicine. Nevertheless, few studies have characterized the affinity between drug and receptor by CMC model. In this study, the alpha 1 adrenoreceptor (α1A AR) high expression CMC method, combined with frontal analysis and stoichiometric displacement model respectively, was established for characterizing the affinity of seven alkaloids binding to the α1A AR. The results indicate that the seven alkaloids have similar interaction strengths with tamsulosin hydrochloride (α1A AR antagonist) between them and α1A AR. In addition, electrostatic force is the main intermolecular forces between tamsulosin hydrochloride and seven alkaloids and α1A AR. The study provides a versatile approach for the characterization the affinity between drug and receptor by CMC model.

Cytoproliferative and Cytoprotective Effects of Striatisporolide A Isolated from Rhizomes of Athyrium multidentatum (Doell.) Ching on Human Umbilical Vein Endothelial Cells.

OBJECTIVES: The aim of this study was to investigate the proliferative and protective effects of striatisporolide A (SA) obtained from the rhizomes of Athyrium multidentatum (Doell.) Ching on human umbilical vein endothelial cells (HUVECs). METHODS: Cell viability was measured by the MTT method. Cell apoptosis was determined by flow cytometry. Intracellular ROS was measured by the 2,7-dichlorodihydrofluorescein diacetate (DCFH-DA) fluorescent probe. RESULTS: The viability rate in cells treated with 100 µM SA alone was increased to 128.72% ± 0.19% and showed a significant difference compared with the control group (p < 0.05). Meanwhile, SA augmented the cell viabilities in H2O2-treated HUVECs, and the cell viability was enhanced to 56.94% ± 0.13% (p < 0.01) when pre-incubated with 50 µM SA. The cell apoptosis rates were reduced to 2.17% ± 0.20% (p < 0.05) and 3.1% ± 0.34% (p < 0.01), respectively, after treatment with SA alone or SA/H2O2. SA inhibited the overproduction of reactive oxygen species (ROS) in HUVECs induced by H2O2 and the fluorescent intensity was abated to 9.47 ± 0.61 after pre-incubated with 100 µM SA. CONCLUSIONS: The biological activities of SA were explored for the first time. Our results stated that SA exhibited significant cytoproliferative and minor cytoprotective effects on HUVECs. We presume that the mechanisms of the proliferation and protection actions of SA involve interference with the generation of ROS and the cell apoptosis. These findings provide a new perspective on the biological potential of butenolides.

Cell membrane chromatography coupled with UHPLC-ESI-MS/MS method to screen target components from Peucedanum praeruptorum Dunn acting on α1A adrenergic receptor.

Peucedanum praeruptorum Dunn (BaiHuaQianHu in Chinese) is a traditional Chinese medicine that has a long history of use in China. In this study, HEK 293 α1A adrenergic cell membrane chromatography was coupled with UHPLC-ESI-MS/MS and successfully used to identify active components from Peucedanum praeruptorum Dunn. Paeruptorin A, paeruptorin B, and paeruptorin C were identified with α1A adrenergic receptor activity. Pharmacological assays showed that tamsulosin hydrochloride, paeruptorin A, paeruptorin B, and paeruptorin C in concentrations of 1×10(-8) to 1×10(-4)mol/mL could relax prostate strips pre-contracted with adrenalin in a concentration dependent manner. Therefore, the HEK293 α1A cell membrane chromatography coupled UHPLC-ESI-MS/MS system may be a potentially useful drug discovery method for screening for medicinal herbal components with α1A adrenergic receptor inhibitory activity.

Fish oil improves lipid profile in juvenile rats with intrauterine growth retardation by altering the transcriptional expression of lipid-related hepatic genes.

OBJECTIVE: To determine whether maternal intrauterine undernutrition and post-weaning fish oil intake influence lipid profile in juvenile offspring, and explore the possible mechanisms at transcriptional levels. METHODS: After weaning, 32 control offspring and 24 intrauterine growth retardation (IUGR) offspring were randomly allocated to standard chow or fish oil diet. At 10 weeks, fasting plasma glucose, triglycerides, total cholesterol and expressions of related hepatic genes were examined. RESULTS: IUGR offspring without catch-up growth tended to develop hyperglycemia, dyslipidemia and hepatic steatosis. Down-regulation of CPT-1 and LDLR at transcriptional levels were found in IUGR offspring. Early short-term fish oil intervention reversed these unfavorable changes in juvenile rats with IUGR. The mechanisms might be mediated by decreased expression of ACC-1, increased expression of CPT-1, LDLR and ABCG5. CONCLUSION: These data suggest that IUGR offspring already present lipid abnormality in juvenile stage, and early short-term fish oil consumption is beneficial to prevent these unfavorable changes.

Combining Sprague-Dawley rat uterus cell membrane chromatography with HPLC/MS to screen active components from Leonurus artemisia.

CONTEXT: Leonurus artemisia (Lour.) S.Y.Hu (Lamiaceae) (YiMuCao in Chinese) is a traditional Chinese medicine. Leonurus artemisia has been shown to have many pharmacological effects such as increasing uterine contraction amplitude, and tension, but the active components are still unknown. OBJECTIVE: The objective of this study is to determine active components of L. Artemisia that are responsible for the biological activity using HPLC and cell membrane-based system. MATERIALS AND METHODS: The whole L. artemisia ethanol extract and its eight fractions were screened using Sprague-Dawley rat uterus cell membrane chromatography (CMC) combined with the HPLC/MS system. Oxytocin was used to investigate the activity of CMC column. The effect of active components screened from L. artemisia was studied by tension measurement of isolated rat uterine strips in vitro at a dose of 10(-7)-10(-4 )mol/L with oxytocin as a control. RESULTS: The acetone extract showed obvious activity when compared with the eight extracts of L. artemisia. From the acetone extract, in the negative ionization mode, the active compound was identified as genkwanin, with a molecular weight of 283. In vitro pharmacological experiments proved that genkwanin promoted uterine contractions at a dose from 10(-7) to 10(-4 )mol/L. The EC50 value was 4.86 ± 4.21 µmol/L for genkwanin and 4.30 ± 3.65 µmol/L for oxytocin on the contractile amplitude of uterine strips isolated from rats. DISCUSSION AND CONCLUSION: Genkwanin was identified as the active compound in L. artemisia by this method. In vitro pharmacological experiments proved that genkwanin promoted uterine contractions. Genkwanin may be used to uterine inertia and may have an effect on postpartum hemorrhage.