The antinociceptive and anti-alpha-glucosidase effects of glucosides from Hemiphragma heterophyllum Wall.

Hemiphragma heterophyllum Wall. is commonly used in traditional Yi herbal medicine for treating bellyache and toothache. In the current study, an unreported monoterpene glucoside, (S)-thymoquinol O-(6-O-oleuropeoyl)-ß-d-glucopyranoside (1), together with 11 known glucosides were obtained from the whole herb of H. heterophyllum. Their structures were determined based on a detailed analysis of spectroscopic data and acid hydrolysis and methanolysis reactions. Bioassay results showed that compounds 1 and 10 at 40 mg/kg exhibited significant antinociceptive activity in the acetic acid-induced writhing model, with inhibitions of 59.80% and 64.07%, respectively. Moreover, five of the isolates showed moderate anti-α-glucosidase activities with IC50 values ranging from 5.67 to 46.16 µM.

Triterpenoid saponins from Psammosilene tunicoides and their antinociceptive activities.

Herein, five undescribed oleanane-type triterpenoid saponins, namely, psammosaponins A-E, along with nine known compounds, were isolated from the roots of Psammosilene tunicoides. Moreover, part of the ethanolic extract of P. tunicoides was acid-hydrolyzed and three aglycones were isolated from the resulting hydrolysate. The structures of all compounds were established through extensive analysis involving 1D and 2D NMR experiments, HRESIMS measurements, chemical derivatization, and comparison of spectroscopic data with the values reported in the literature. In all, 10 of the isolated saponins and the three aglycones were evaluated in the acetic acid-induced writhing model for their antinociceptive activity. At a dose of 40 mg/kg, these compounds exhibited significant inhibitory effects on the mouse writhing response, with inhibitions ranging from 31.9% to 79.3%. In addition, the structure-activity relationships of the isolates were discussed. Among the isolates, quillaic acid 3-O-glucuronide and 16α-hydroxygypsogenic acid showed better antinociceptive activity with inhibitions of 79.3% and 73.7%, respectively. Both isolates also exhibited antinociceptive activities in hot plate and formalin tests on mice. Their antinociceptive mechanism was explored in lipopolysaccharide-stimulated RAW 264.7 cells. These isolates could significantly inhibit the production of nitric oxide and interleukin-6 and downregulate the expression levels of inducible NO synthase, COX-1, and COX-2.

The combined analgesic, sedative, and anti-gastric cancer mechanisms of Tinospora sagittata var. yunnanensis (S. Y. Hu) H. S. Lo based on integrated ethnopharmacological data.

ETHNOPHARMACOLOGY RELEVANCE: As a Yi medicine for eliminating wind to relieve pain, Tinospora sagittata var. yunnanensis (S. Y. Hu) H. S. Lo (TSY) is widely used to treat sore throat, stomach pain, bone and muscle injuries, and tumors; however, the material basis and mechanism of action remain unclear. AIM OF THE STUDY: This study aims to investigate the potential active compounds of TSY and related pharmacological mechanisms against gastric cancer using a multitarget strategy. MATERIALS AND METHODS: The main chemical components of TSY were collected through a literature review and database searches. The components were further screened for ADMET properties, and their targets were predicted using network pharmacology (admetSAR) and substructure-drug-target network-based inference (SDTNBI) approaches in silico. The pharmacological mechanism of action of TSY extract for pain relief, sedation, and anti-gastric cancer activities were identified via in vivo and in vitro biochemical analyses. RESULTS: Here, 28 chemical components were identified, 7 active compounds were selected, and 75 targets of TSY extract were predicted. A compound-target-disease network topological approach revealed that the predicted targets are highly related to the digestive system and nervous system. Network pharmacology results suggested that the anti-gastric cancer activity of TSY was highly correlated with its analgesic and sedative targets and MAPK. In vivo experiments confirmed that TSY extract not only reduced the number of voluntary activities in the mouse model but also exhibited a synergistic effect on sodium pentobarbital-induced sleep, reduced the number of mice exhibiting writhing responses to acetic acid, and increased the hot plate pain threshold of mice. Thus, TSY extract exhibits good analgesic and sedative effects. The TSY extract inhibited HGC-27 cell proliferation and induced apoptosis by regulating apoptotic proteins (BAX, BCL-2 and BCL-XL) in vitro. CONCLUSIONS: TSY exhibits combined analgesic, sedative, and anti-gastric cancer activities.

Two new monoterpene esters from Illigera paviflora Dunn roots.

Two new monoterpene esters, illigerates H and I (1 and 2), and six known compounds actinodaphine (3), bulbocupnine (4), stephanine (5), hypserpanine B (6), betulinic acid (7) and gallic acid (8) were obtained from the root of Illigera paviflora Dunn. Their structures were elucidated by spectroscopic analysis. Anti-inflammatory and α-glucosidase inhibitory activity of some isolated compounds were assessed. Two monoterpenes 1 and 2 exhibited weak in vitro anti-inflammatory activity (IC50 64.5 ± 5.3 and 79.2 ± 7.5 µM) while compounds 3-6 showed inhibition of α-glucosidase with IC50 values ranged from 87.17 to 118.74 µM.

I-125 seeds brachytherapy with transcatheter arterial chemoembolization for subcapsular hepatocellular carcinoma.

BACKGROUND: I-125 seeds brachytherapy (ISB) has been used to improve the clinical effectiveness of transarterial chemoembolization (TACE) for hepatocellular carcinoma (HCC). We aim to appraise the safety and clinical efficacy of combined ISB and TACE for the treatment of subcapsular HCC. MATERIALS AND METHODS: A retrospective investigative study extending from January 2017 to December 2020, involved individuals suffering from subcapsular HCC, who were subjected to TACE treatment with or without ISB in our center. The clinical effectiveness was compared between 2 groups. RESULTS: Sixty-four patients, in total, with subcapsular HCC had to undergo TACE with (n = 32) or without (n = 32) ISB in our center. After CT-guided ISB, only 2 (6.3%) patients experienced a self-limited pneumothorax. Combined treatment resulted in a significantly higher complete response (56.3% vs. 18.8%, P = 0.002) and total response (90.7% vs. 59.4%, P = 0.004) rates than that of TACE alone. In comparison to the TACE alone group, the median progression-free survival was substantially longer in the combined treatment group (11 months vs. 5 months, P = 0.016). Further, 15 and 28 patients in combined and TACE alone groups respectively died within the follow-up. The median OS was comparable between combined and TACE alone groups (22 months vs. 18 months, P = 0.529). CONCLUSIONS: Combined TACE and ISB therapy is a safe treatment method for individuals suffering from subcapsular HCC. When compared, combined treatment had significantly enhanced clinical efficacy as a subcapsular HCC therapy, in comparison to TACE alone.

Secondary metabolites isolated from Agrimonia pilosa Ledeb.

A pilot study on the ethanol extracts of Agrimonia pilosa found to have anti-α-glucosidase and anti-inflammatory activities. Subsequent chemical study afforded a new phenylethyl isocoumarin glycoside (1) and eight known compounds (2-9). The structure of 1 was elucidated by comprehensive spectroscopic analysis and chemical transformations. All compounds showed modest α-glucosidase inhibitory activity (IC50 values ranging from 36.8 to 210.7 µM), which was lower than that of the positive control acarbose (IC50=301.9 µM). Those compounds except inactive compounds 3 and 6 showed weak anti-inflammatory activity.[Formula: see text].

Development of a model to predict recurrence after bronchial artery embolization for non-cancer related hemoptysis.

BACKGROUND: Relapse after effective bronchial arterial embolization (BAE) for controlling hemoptysis is not uncommon. Studies reported diverse predictors of recurrence. However, a model to assess the probability of recurrence in non-cancer related hemoptysis patients after BAE has not been reported. This study was to develop a model to predict recurrence after BAE for non-cancer related hemoptysis. METHODS: The study cohort included 487 patients who underwent BAE for non-cancer-related hemoptysis between January 2015 and December 2019. We derived the model's variables from univariate and multivariate Cox regression analyses. The model presented as a nomogram scaled by the proportional regression coefficient of each predictor. Model performance was assessed with respect to discrimination and calibration. RESULTS: One-month and 1-, 2-, 3- and 5-year recurrence-free rates were 94.5%, 88.0%, 81.4%, 76.2% and 73.8%, respectively. Risk factors for recurrence were underlying lung diseases and the presence of systemic arterial-pulmonary circulation shunts. This risk prediction model with two risk factors provided good discrimination (area under curve, 0.69; 95% confidence interval, 0.62-0.76), and lower prediction error (integrated Brier score, 0.143). CONCLUSION: The proposed model based on routinely available clinical and imaging features demonstrates good performance for predicting recurrence of non-cancer-related hemoptysis after BAE. The model may assist clinicians in identifying higher-risk patients to improve the long-term efficacy of BAE.

Insertion of I-125 seed-loaded stent for inoperable hilar cholangiocarcinoma.

INTRODUCTION: Stent insertion is the most frequently used option to treat malignant biliary obstruction (MBO) patients. Hilar cholangiocarcinoma (HCCA) is the most common disease that causes hilar MBO. AIM: To assess the clinical efficacy and long-term outcomes of I-125 seed-loaded stent (ISS) insertion for HCCA patients. MATERIAL AND METHODS: Consecutive patients with HCCA underwent either normal stent (NS) or ISS insertion between January 2017 and December 2019. The baseline and treatment data of these two groups were compared. RESULTS: During the period, a total of 93 patients with inoperable HCCA were divided into either NS (n = 48) or ISS (n = 45) insertion groups at our centre. Technical success rates of the NS and ISS insertion were 91.7% and 95.6%, respectively (p = 0.733). Clinical success rates were 93.2% and 100% in the NS and ISS groups, respectively (p = 0.24). Stent dysfunction was observed in 11 and 8 patients in the NS and ISS groups, respectively (p = 0.47). The median stent patency was 143 days and 208 days in the NS and ISS groups, respectively (p < 0.001). All patients died in the follow-up period, with median survival duration of 178 days and 220 days in the NS and ISS groups, respectively (p < 0.001). ISS insertion was the only predictor of longer patency (p = 0.002) and survival (p = 0.01). CONCLUSIONS: ISS insertion might achieve longer patency and overall survival in patients with inoperable HCCA as compared with NS insertion.

A Nomogram to Predict Recurrence After Bronchial Artery Embolization for Hemoptysis Due to Bronchiectasis.

OBJECTIVE: To develop and validate a nomogram for predicting recurrent hemoptysis after successful bronchial arterial embolization (BAE) in patients with bronchiectasis. MATERIALS AND METHODS: From January 2015 to December 2019, a total of 251 patients were enrolled in this study. A nomogram was developed with the predictors of recurrent events, which were identified by univariate and multivariate Cox regression analyses. We evaluated nomogram discrimination by area under the receiver operating characteristic curve, calibration by the calibration curve, and clinical usefulness potential by decision curve analysis. RESULTS: The one-month, 1-year, 2-year, 3-year, and 5-year cumulative recurrence-free rates of patients were 98.4%, 90.5%, 82.8%, 77.7%, and 74.4%, respectively. Three predictive factors, namely sex, lung destruction, and systemic arterial-pulmonary circulation shunts, were applied to develop the nomogram. The model maintained good discrimination (area under the curve, 0.72; 95% confidence interval, 0.62-0.81), low prediction error (integrated Brier score, 0.129), and certain net benefits in terms of clinical usefulness. CONCLUSIONS: The proposed nomogram showed favorable predictive efficacy for hemoptysis recurrence after BAE in patients with bronchiectasis. Improved long-term outcomes are expected with close follow-up, a healthy lifestyle, and pulmonary rehabilitation for patients at risk of recurrence according to the model.

A stent with radioactive seed strand insertion for inoperable malignant biliary obstruction: A meta-analysis.

PURPOSE: The purpose of the study was to assess the relative clinical effectiveness of stent insertion with or without radioactive seed strand (RSS) insertion in patients suffering from malignant biliary obstruction (MBO). METHODS AND MATERIALS: Relevant articles published as of November 2020 in the Embase, PubMed, and Cochrane Library databases were identified and analyzed. Primary study endpoints for this meta-analysis were stent dysfunction, stent patency, and overall survival (OS), whereas secondary endpoints were rates of clinical success and complications. RevMan v5.3 was used to perform all meta-analyses. RESULTS: In total, there were nine studies incorporating 643 patients (280 and 363 who underwent stent insertion with and without RSS, respectively). No differences were observed between these groups with respect to pooled rates of clinical success (p = 0.25), stent dysfunction (p = 0.47), cholangitis (p = 0.97), cholecystitis (p = 0.95), or pancreatitis (p = 0.66). However, stent patency duration (p < 0.00001) and patients' OS (p < 0.00001) were significantly increased in patients in the stent + RSS group. No heterogeneity was detected for any of these endpoints, nor did funnel plots yield any publication bias. A subgroup analysis of patients with hilar MBO similarly exhibited stent + RSS insertion to be associated with longer stent patency and OS as compared with stent insertion alone. CONCLUSIONS: These findings showed that relative to stent insertion, stent + RSS insertion is associated with longer OS and stent patency in patients with inoperable MBO.

Noroleanane-type triterpenoids from Dolichos trilobus L. and their anti-α-glucosidase activities.

Falcatane A (1) and B (2), 4-oxo-3,24-dinor-2,4-secooleanane- and 3-oxo-24- noroleanane-type triterpenoids, together with seven known triterpenoids involving 2-hydroxy-3-oxo-24-noroleana-1,4,12-trien-28-oic acid (3) and oleanolic acid (4), were separated from the ethyl acetate roots extract of Dolichos trilobus using the column chromatography of silica gel, MCI gel, and Sephadex LH-20. The compounds were determined by analysis of IR, NMR spectroscopic data and mass spectrometry. In the bioassay, all isolates showed varying degree of the α-glucosidase inhibitory activity except compound 2.

Anti-inflammatory monoterpene esters from the stems of Illigera aromatica.

Two new monoterpene esters illigerates F and G (1 and 2) together with 5 know compounds illigerate A (3), illigerate C (4), actinodaphnine (5), N-methylactinodaphnine(6) and N-methyllaurotetanine(7) were isolated from Illigera aromatica S. Z. Huang et S. L. Mo. Their structures were identified by extensive NMR data and by comparing with the known compounds. The anti-inflammatory activity of four monoterpenes (1 - 4) was evaluated by inhibiting nitric oxide (NO) production in lipopolysaccharide-activated murine macrophage RAW 264.7 cells and four monoterpenoids exhibited inhibitory effect with IC50 values of 71.5 ± 7.3, 74.7 ± 5.6, 48.0 ± 7.4 and 65.1 ± 3.7 µM, respectively.

Correlation between left behind expericences with depressive and anxiety symptoms of left behind middle school stutents / 中国学校卫生

Objective@#To explore the relationship between left behind experiences due to work migration of parents with depressive and anxiety symptoms among left behind middle school stutents, to provide a theoretical basis for the government to formulate intervention policies for mental health of left behind children.@*Methods@#The stratified random cluster sampling method was used to investigate 2 160 children in Poyang and Guangfeng Counties of Shangrao City, Jiangxi Province from April to June, 2019. Finally, 776 left behind children aged 13 to 18 were selected. The Generalized Anxiety Disorder (GAD-7) and Patient Health Questionnaire (PHQ-9) were used to evaluate the depression and anxiety symptoms. Family characteristics and lifestyle behaviors of left behind children were investigated by questionnaire.@*Results@#In terms of gender, the detection rates of both depressive symptoms and anxiety symptoms were higher in girls than in boys. In terms of age, the detection rates of depressive symptoms (43.2%) and anxiety symptoms (39.9%) in left behind children in high school (16-18 years old) were higher than those in middle school (13-15 years old)( 27.3 % and 33.0%). The detection rate of depressive among left behind children significantly differet in sexual, gender ( χ 2= 10.48 , 21.08); the detection rate of anxiety symptoms among left behind children significantly different in sexual, maternal occupation, and paternal educational background ( χ 2=8.66, 5.30, 8.35) ( P <0.05).@*Conclusion@#Parent child separation is associated with depressive symptoms in left behind middle school stutents. Mental health of children in middle school stutents is of great significance to the prevention of depression and anxiety symptoms in left behind children.

Laxative Metabolites from the Leaves of Moringa oleifera.

Three new flavonoids, quercetin-3-O-6-[methyl-(S)-3-hydroxy-3-methylglutaroyl(1→6]-ß-d-glucopyranoside (1), kaempferol-3-O-[methyl-(S)-3-hydroxy-3-methylglutaroyl(1→6)]-ß-d-glucopyranoside (2), and quercetin-3-O-6-[(E)-4-methoxy-5-methylhexa-2,4-dienoatyl(1→6)]-ß-d-glucopyranoside (3), and two new alkaloids, 5-dehydroxymethyl-pyrrolemarumine 4″-O-α-l-rhamnopyranoside (4) and N1-methyl-N2-((4-O-α-l-rhamnopyranoside)benzyl) oxalamide (5), together with 45 known compounds (6-50) were isolated from the leaves of Moringa oleifera Lam. Among those compounds, 1-octacosanol (50), a straight-chain 28-carbon alcohol, exhibited good activity against diphenoxylate-induced constipation in mice, which is obtained as a laxative constituent from the plant for the first time. In order to have an accurate understanding of the content of compound 50, a quantification with gas chromatography-tandem mass spectrometry (GC-MS/MS) was carried out. The anti-inflammatory and α-glucosidase inhibitory activity of some compounds also was assessed.

Phenylpropanoid and Iridoid Glucosides from the Whole Plant of Hemiphragma heterophyllum and Their alpha-Glucosidase Inhibitory Activities.

Three phenylpropanoid glucosides (1:  - 3: ) and one iridoid glucoside (11: ), together with eleven known glucosides, were isolated from the ethanol extract of the whole plant of Hemiphragma heterophyllum. Their structures were elucidated by means of 1D and 2D NMR spectroscopy, HRMS, and chemical methods. All compounds except 11: and 13:  - 15: showed varying degrees of α-glucosidase inhibitory activity. Compounds 5, 9: , and 12: were marginally active in the bioassay, while compounds 1:  - 4: , 6:  - 8: , and 10: exhibited appreciable inhibitory activity with an IC50 value of 33.6 ~ 83.1 µM, which was much lower than that of the positive control acarbose (IC50 = 310.8 µM).

An updated meta-analysis of prostatic arterial embolization versus transurethral resection of the prostate in the treatment of benign prostatic hyperplasia.

OBJECTIVE: To investigate whether prostatic arterial embolization (PAE) could be recommended as a routine therapy for benign prostatic hyperplasia (BPH), we conducted an updated meta-analysis to assess the efficacy and safety of PAE compared with transurethral resection of the prostate (TURP). METHODS: Systematic literature retrieval by searching data from Web of science, Pubmed, Embase, Cochrane Library, ClinicalTrial.gov, CNKI, Wanfang and VIP databases was carried out to identify all related trials from the inception dates to June 2019. We also conducted subgroup analyses depending on the kind of study design, kind of PAE and kind of TURP. RESULTS: Nine studies comparing PAE with TURP involving a total of 860 BPH patients were selected. Postoperative reduced IPSS score (MD 2.50; 95% CI 0.78-4.21; P = 0.004), postoperative reduced QOL score (MD 0.40; 95% CI 0.09-0.71; P = 0.01), postoperative reduced PV (MD 8.59; 95% CI 4.74-12.44; P < 0.00001) and postoperative increased Qmax (MD 2.54; 95% CI 1.02-4.05; P = 0.001) were better in TURP than in PAE; however, PAE was associated with lower sexual dysfunction rate (OR 0.24; 95% CI 0.15-0.39; P < 0.00001) compared with TURP. Meanwhile, no significant difference in postoperative reduced PVR (MD 0.46; 95% CI - 2.08 to 3.00; P = 0.72) and complication (OR 0.57; 95% CI 0.21-1.55; P = 0.27) between PAE and TURP group was demonstrated. CONCLUSION: PAE was inferior to TURP in the improvement of postoperative IPSS, QOL, PV, Qmax and TURP still remained the gold standard. However, PAE may be a valuable alternative to TURP in the treatment of BPH patients who refuse surgery or with surgery contraindication.

[A new guaiane-type sesquiterpenoid from Croton yunnanensis].

Five sesquiterpenoids were isolated from 90% ethanol extract of Croton yunnanensis by silica gel,Sephadex LH-20 column chromatography,as well as prep-HPLC methods. Based on MS,1 D and 2 D NMR spectral analyses,the structures of the five compounds were identified as 11-methoxyl alismol(1),6ß,7ß-epoxy-4α-hydroxyguaian-10-ene(orientalol C,2),multisalactone D(3),arvestonol(4),and 4,5-dihydroblumenol A(5). Compound 1 was a new guaiane-type sesquiterpenoid. Compounds 2-4 were isolated from the Croton genus for the first time,and compound 5 was obtained from this plant for the first time.

Three new diterpenoids from Aralia dumetorum.

Three new diterpenoids, dumetoranes A (1) and B (2), melanocane B (3), together with four known ones including melanocane A (4), ent-15S,16-dihydroxypimar-8(14)-en-19-oic acid (5), ent-pimara-8(14),15-diene-19-oic acid (6), and ent-pimara-8(14),15-diene-19-ol (7) were obtained from the ethanol extract of the roots of Aralia dumetorum. Their structure elucidation was achieved by the methods of spectroscopic HRMS, IR, NMR, and by comparison with literature. The cytotoxicities of compounds 1-3 and 5 were assayed by in vitro MTT methods.

α-Glucosidase Inhibitory and Anti-Inflammatory Coumestans from the Roots of Dolichos trilobus.

Four new coumestans dolichosins A - D (1: -4: ) were isolated from the roots of Dolichos trilobus, together with four known compounds: isosojagol (5: ), phaseol (6: ), psoralidin (7: ), and 4″,5″-dehydroisopsoralidin (8: ). Their structures were elucidated on the basis of spectroscopic data interpretation, mass spectrometric analyses, and the comparison with literature data of related compounds. The anti-inflammatory activity of these compounds (1: -8: ) was evaluated through the inhibition of nitric oxide production in lipopolysaccharide-activated murine macrophage RAW 264.7 cells, in which compounds 1: and 6: displayed moderate inhibitory activity and no cytotoxic effects. In a α-glucosidase inhibitory assay, compounds 1: and 5: -8: exhibited appreciable inhibition on α-glucosidase. Especially compounds 1, 7: , and 8: showed IC50 values lower than 20.0 µM.

Chemical constituents from the whole herb of Hemiphragma heterophyllum.

Phytochemical investigation on Hemiphragma heterophyllum led to the isolation of two new compounds, heterophyllumin A (1) and heterophylliol (3), along with nine known compounds, (‒)-sibiricumin A (2), iridolactone (4), jatamanin A (5), dihydrocatalpolgenin (6), 25-hydroperoxycycloart-23-en-3ß-ol (7), 24-methylenecycloartanol (8), (+)-pinoresinol (9), hexadec-(4Z)-enoic acid (10), and 9,12, 15-octadecatrienoic acid (11). Their structures were elucidated on the basis of detailed spectroscopic analyses and by comparison with literature data. Further, the structure of compound 3 was unambiguously confirmed by single-crystal X-ray analysis. Some of those compounds showed moderate activity in the α-glucosidase inhibition assay.