Pharmacokinetics and tissue distribution of monotropein and deacetyl asperulosidic acid after oral administration of extracts from Morinda officinalis root in rats.

BACKGROUND: Iridoid glycosides (IGs), including monotropein (MON) and deacetyl asperulosidic acid (DA) as the main ingredients, are the major chemical components in Morinda officinalis How. (MO) root, possessing various pharmacological properties including anti-osteoporosis, anti-inflammation and anti-rheumatism activities.The aim of the present study was to further elucidate the pharmacological actions of MO by investigating the pharmacokinetics and tissue distribution of IGs in MO. METHODS: An ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS) method was developed and validated for simultaneous determination of MON and DA levels in plasma and various tissues of Wistar rats. MON, DA and acetaminophen (ACE) as the internal standard (IS) were extracted from rat plasma and tissue samples by direct deproteinization with methanol. The rats were administered orally at 1650 mg/kg MO and 25, 50 and 100 mg/kg MO iridoid glycosides (MOIGs) or intravenously at MOIG 25 mg/kg for pharmacokinetic study of MON and DA. In addition, 100 mg/kg MOIG was administered orally for tissue distribution study of MON and DA. Non-compartmental pharmacokinetic profiles were constructed. Tissue distributions were calculated according to the validated methods. RESULTS: Significant differences in the pharmacokinetic parameters were observed in male and female rats. The AUC0-t, Cmax and bioavailability of MON and DA in female rats were higher than those in male rats. MON and DA mainly distributed in the intestine and stomach after oral administration, and noteworthily high concentrations of MON and DA were detected in the rat hypothalamus. CONCLUSION: The results of the present study may shed new lights on the biological behavior of MOIGs in vivo, help explain their pharmacological actions, and provide experimental clues for rational clinical use of these IGs extracted from the MO root.

Lack of efficacy of nebulized magnesium sulfate in treating adult asthma: A meta-analysis of randomized controlled trials.

BACKGROUND: Nebulized magnesium sulfate (MgSO4) has been used to treat asthma, but the efficacy remains controversial. We aimed to comprehensively review the efficacy of nebulized MgSO4 in treating adult patients with asthma. METHODS: PubMed, Embase, and Cochrane Library were searched for relevant studies published up to July 18, 2016. Randomized controlled trials (RCTs) were included if adult patients with acute or stable asthma had been treated with nebulized MgSO4 compared with placebo or another bronchodilator. Standardized mean differences (SMDs), relative risks (RRs) and 95% confidence intervals (CIs) were calculated. Outcomes included pulmonary function, hospital admission and adverse events. RESULTS: A total of 1386 patients from sixteen trials (1240 acute asthma patients and 146 stable asthma patients) were subjected to meta-analysis. Compared to placebo as normal saline, whether using in acute or stable adult asthma, nebulized MgSO4 did not significantly improve the respiratory function: SMD 0.39 (95% CI -0.03-0.82, P = 0.07), and 1.48 (95% CI -0.14-3.11, P = 0.07), respectively. Furthermore, nebulized MgSO4 did not reduce hospital admission in adult patients with acute asthma (RR, 0.72; 95% CI, 0.52-1.00; P = 0.05), although it was not associated with increased adverse events (RR 1.15; 95% CI, 0.88-1.52; P = 0.31). CONCLUSIONS: Evidence to date suggests that nebulized MgSO4 has no role in the management of adult patients with acute or stable asthma.

Quality evaluation of the leaves of Magnolia officinalis var. biloba using high-performance liquid chromatography fingerprint analysis of phenolic compounds.

The high-performance liquid chromatography fingerprint method is a simple and reliable technique to evaluate the quality of leaves of Magnolia officinalis Rehd.et Wils. var. biloba Rehd.et Wils. We used the following bioactive phenolic constituents as reference compounds: rutin, afzelin, hyperoside, isoquercitrin, quercetin-3-O-α-l-rhamnoside, honokiol and magnolol. The conditions of an Agilent 1200 HPLC were: YMC-Pack-ODS-AQ column (250 × 4.6 mm id S-5 µm, 12 nm), mobile phase acetonitrile and 0.2% phosphoric acid in a gradient elute mode, flow rate 1.0 mL/min, detection wavelength 280 nm and column temperature 30°C. The analytical method was validated in terms of linearity, stability, repeatability, precision and recovery tests. While performing fingerprint analysis, we identified 11 peaks as characteristic peaks and assessed the similarities of 17 samples collected from different geological regions of China. The peak areas were used to evaluate the variation in the chemical composition of the tested samples. For this purpose, we performed hierarchical cluster analysis of the peak areas. Our results indicate that simultaneous determination of multiple ingredients could be done through chromatographic fingerprint analysis. Therefore, this high-performance liquid chromatography fingerprint method was readily utilized to evaluate the quality of leaves of M. officinalis var.biloba, which are used in several traditional herbal preparations.

Hepatoprotective effect of ganoderma triterpenoids against oxidative damage induced by tert-butyl hydroperoxide in human hepatic HepG2 cells.

CONTEXT: Ganoderma triterpenoids (GTs) have been recognised as an important bioactive ingredient in Ganoderma Lucidum (Leyss. ex Fr.) Karst. (Polyporaceae), widely used for treating and preventing chronic hepatopathy of various etiologies. OBJECTIVE: The objective of this study is to better understand the hepatoprotective effect of GTs and to enhance their use in food supplement pharmaceutical and medical industries. MATERIALS AND METHODS: HepG2 cells were pretreated in the presence or absence of GTs (50, 100 and 200 µg/ml) for 4 h, then exposed with 60 µmol/L of t-BHP for an additional 4 h. The cell viability was evaluated by MTT method. ALT, AST and LDH production in culture medium and intracellular MDA, GSH and SOD levels were determined. Moreover, the total triterpenoid content and chemical constituents in GTs were detected by ultraviolet spectrophotometry and HPLC/Q-TOF-MS, respectively. RESULTS: GTs (50, 100 and 200 µg/ml) significantly increased the relative cell viability by 4.66, 7.78 and 13.46%, respectively, and reduced the level of ALT by 11.44%, 33.41% and 51.24%, AST by 10.05%, 15.63% and 33.64%, and LDH by 16.03%, 23.4% and 24.07% in culture medium, respectively. GTs could also remarkably decrease the level of MDA and increase the content of GSH and SOD in HepG2 cells. Furthermore, the total triterpenoid content in GTs was 438 mg GAAEs/g GTs. And 16 triterpenoids in GTs were identified or tentatively characterised. DISCUSSION AND CONCLUSION: Our results showed that GTs had potent cytoprotective effect against oxidative damage induced by t-BHP in HepG2 cells, thus suggesting their potential use as liver protectant.

Quantitative and chemical fingerprint analysis for the quality evaluation of Receptaculum Nelumbinis by RP-HPLC coupled with hierarchical clustering analysis.

A simple and reliable method of high-performance liquid chromatography with photodiode array detection (HPLC-DAD) was developed to evaluate the quality of Receptaculum Nelumbinis (dried receptacle of Nelumbo nucifera) through establishing chromatographic fingerprint and simultaneous determination of five flavonol glycosides, including hyperoside, isoquercitrin, quercetin-3-O-ß-d-glucuronide, isorhamnetin-3-O-ß-d-galactoside and syringetin-3-O-ß-d-glucoside. In quantitative analysis, the five components showed good regression (R > 0.9998) within linear ranges, and their recoveries were in the range of 98.31%-100.32%. In the chromatographic fingerprint, twelve peaks were selected as the characteristic peaks to assess the similarities of different samples collected from different origins in China according to the State Food and Drug Administration (SFDA) requirements. Furthermore, hierarchical cluster analysis (HCA) was also applied to evaluate the variation of chemical components among different sources of Receptaculum Nelumbinis in China. This study indicated that the combination of quantitative and chromatographic fingerprint analysis can be readily utilized as a quality control method for Receptaculum Nelumbinis and its related traditional Chinese medicinal preparations.

Influence of slope angle on deposit morphology and propagation of laboratory landslides.

Landslide deposits often exhibit surface features, such as transverse ridges and X-shaped conjugate troughs, whose physical formation origins are not well understood. To study the deposit morphology, laboratory studies typically focus on the simplest landslide geometry: an inclined plane accelerating the sliding mass immediately followed by its deceleration on a horizontal plane. However, existing experiments have been conducted only for a limited range of the slope angle θ. Here, we study the effect of θ on the kinematics and deposit morphology of laboratory landslides along a low-friction base, measured using an advanced 3D scanner. At low θ (30°-35°), we find transverse ridges formed by overthrusting on the landslide deposits. At moderate θ (40°-55°), conjugate troughs form. A Mohr-Coulomb failure model predicts the angle enclosed by the X-shaped troughs as 90° - φ, with φ the internal friction angle, in agreement with our experiments and a natural landslide. This supports the speculation that conjugate troughs form due to failure associated with a triaxial shear stress. At high θ (60°-85°), a double-upheaval morphology forms because the rear of the sliding mass impacts the front during the transition from the slope to the horizontal plane. The overall surface area of the landslides increases during their downslope motion and then decreases during their runout.

Anoectochiluszhongshanensis (Orchidaceae), a new species from Guangxi, China.

A new species of Anoectochilus (Orchidaceae) from Guangxi, China, A.zhongshanensis, is described here, which was identified based on phylogenetic studies adopting combined plastid markers (rbcL-matK-trnL-F), morphological observation and chemical analysis. Molecular phylogenetic results support the systematic status of A.zhongshanensis as a new species in Anoectochilus genus. Morphologically, this new species is similar to A.zhejiangensis and A.malipoensis, but differs by its characteristic labellum and column, including the hastate or scalpel-shaped lobes of epichile, forward curved and pinnately divided cristate lobes at both sides of the mesochile and inverted triangle column wings. Furthermore, HPLC-ELSD analysis of these three species revealed the interesting chemotaxonomic difference that the principle and characteristic lactone glycoside in this new species was kinsenoside, rather than its diastereoisomer, goodyeroside A, a major glycoside in A.zhejiangensis and A.malipoensis.

Antioxidant activities of extract and fractions from receptaculum nelumbinis and related flavonol glycosides.

The antioxidant activities of ethanolic crude extract (ECE) and its four different solvent sub-fractions (namely, petroleum ether fraction (PEF), ethyl acetate fraction (EAF), n-butanol fraction (BF) and the aqueous fraction (AF) from the receptacles of Nelumbo nucifera Gaertn. (Receptaculum Nelumbinis) were investigated using two in vitro antioxidant assays. BF showed the highest total phenolic content (607.6 mg/g gallic acid equivalents), total flavonoid content (862.7 mg/g rutin equivalents) and total proanthocyanidin content (331.0 mg/g catechin equivalents), accompanied with the highest antioxidant activity compared to other fractions through 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical scavenging assays. Five flavonol glycosides, namely hyperoside (1), isoquercitrin (2), quercetin-3-O-ß-d-glucuronide (3), isorhamnetin-3-O-ß-d-galactoside (4) and syringetin-3-O-ß-d-glucoside (5) were isolated from the Receptaculum Nelumbinis. Compounds 2-5 were isolated for the first time from the Receptaculum Nelumbinis. The five isolated flavone glycosides, particularly compounds 1-3, demonstrated significant DPPH and ABTS radical scavenging activity, with IC(50) values of 8.9 ± 0.2, 5.2 ± 0.2, 7.5 ± 0.1 for DPPH and 114.2 ± 1.7, 112.8 ± 0.8, 172.5 ± 0.7 µg/mL for ABTS, respectively. These results suggest that Receptaculum Nelumbinis has strong antioxidant potential and may be potentially used as a safe and inexpensive bioactive source of natural antioxidants.

Corrigendum to "Quantitative determination of multi-class bioactive constituents for quality assessment of ten Anoectochilus, four Goodyera and one Ludisia species in China" [Chinese Herbal Medicines 12 (2020) 430-439].

[This corrects the article DOI: 10.1016/j.chmed.2020.07.002.].

Effects of volatile components and ethanolic extract from Eclipta prostrata on proliferation and differentiation of primary osteoblasts.

Eclipta prostrata, an aromatic plant, is known in Chinese herbal medicine for the treatment of various kidney diseases. In the present study, the volatile components were isolated from the aerial parts of this plant by hydrodistillation and analysed by GC-MS. A total of 55 compounds, which were the major part (91.7%) of the volatiles, were identified by matching mass spectra with a mass spectrum library (NIST 05.L). The main components were as follows: heptadecane (14.78%), 6,10,14-trimethyl-2-pentadecanone (12.80%), n-hexadecanoic acid (8.98%), pentadecane (8.68%), eudesma-4(14),11-diene (5.86%), phytol (3.77%), octadec-9-enoic acid (3.35%), 1,2-benzenedicarboxylic acid diisooctyl ester (2.74%), (Z,Z)-9,12-octadecadienoic acid (2.36%), (Z)-7,11-dimethyl-3-methylene-1,6,10-dodecatriene (2.08%) and (Z,Z,Z)-1,5,9,9-tetramethyl-1,4,7-cycloundecatriene (2.07%). The effects of volatile components and ethanolic extract from the aerial parts of this plant on the proliferation and differentiation of primary osteoblasts were evaluated by the MTT method and measuring the activity of alkaline phosphatase (ALP activity). Both volatile components and ethanolic extract (1 microg/mL to 100 microg/mL) significantly (p < 0.01) stimulated the proliferation and increased the ALP activity of primary osteoblasts. These results propose that E. prostrata can play an important role in osteoblastic bone formation, and may possibly lead to the development of bone-forming drugs.

[Design, synthesis of quinolinone acid-containing compounds with anti-HIV integrase activity].

A series of novel quinolinone acid-containing compounds were designed and synthesized. Their structures were confirmed with 1H NMR and MS. The target compounds were tested for anti-HIV-1 integrase activities in vitro with enzyme linked immunosorbent assay (ELISA). The result showed that D-2, D-4 and D-7 have anti-integrase activity with IC50 < 100 micromol L(-1).

Quantitative determination of multi-class bioactive constituents for quality assessment of ten Anoectochilus, four Goodyera and one Ludisia species in China.

Objective: To establish multi-class bioactive constituents' determination of ten Anoectochilus, four Goodyera and one Ludisia species, and provide reference for the improvement of their quality control. Methods: HPLC-ELSD and phenol-sulphuric acid methods were used for the quantitative determination of lactone glycosides (kinsenoside and its diastereoisomer, goodyeroside A) and polysaccharides, respectively, while an efficient iHPLC-MS/MS method was established for rapid determination of other minor constituents in ten Anoectochilus species and five related species. Results: The contents of kinsenoside, goodyeroside A, polysaccharides and flavonoids varied notably almost in all tested samples, including both wild plants and tissue cultures. In particular, kinsenoside was the major lactone glycoside in A. roxburghii, A. formosanus, A. xingrenensis, A. nandanensis, A. brevilabris and A. burmannicus, whereas goodyeroside A was the predominant constituent in A. lylei, A. longilobus, A. elatus, A. zhejiangensis, G. schlechtendaliana, G. biflora, G. yangmeishanensi, G. repens and Ludisia discolor. Conclusion: Our present study suggested that A. lylei, A. longilobus, A. elatus, A. zhejiangensis, Ludisia discolor and Goodyera species cannot be used as alternatives for A. roxburghii, and goodyeroside A may be reasonably used as a diagnostic marker for distinguishing A. roxburghii from A. lylei, A. longilobus, A. elatus and A. zhejiangensis, Goodyera and Ludisia species. The established method thus could be potentially used for the quality evaluation and control of Anoectochilus and some related species.

Inhibitory effects of morinda officinalis extract on bone loss in ovariectomized rats.

The present study was undertaken to investigate the protective effects of ethanol extract from the root of Morinda Officinalis (RMO) on ovariectomy-induced bone loss. Administration of RMO extract increased trabecular bone mineral content and bone mineral density of tibia, improved the levels of phosphorus (P), calcium (Ca) and OPG, decreased the levels of DPD/Cr, TRAP, ACTH and corticosterone, but did not reverse the levels of ALP, TNF-alpha and IL-6 in serum of ovariectomized rats. These findings demonstrated that RMO extract reduced bone loss in ovariectomized rats, probably via the inhibition of bone resorption, but was not involved with bone formation. Anthraquinones and polysaccharides from Morinda officinals could be responsible for their antiosteoporotic activity, and the action mechanism of these constituents needs to be further studied. Therefore, RMO has the potential to develop a clinically useful antiosteoporotic agent.

Antiosteoporotic activity of anthraquinones from Morinda officinalis on osteoblasts and osteoclasts.

Bioactivity-guided fractionation led to the successful isolation of antiosteoporotic components, i.e. physicion (1), rubiadin-1-methyl ether (2), 2-hydroxy-1-methoxy- anthraquinone (3), 1,2-dihydroxy-3-methylanthraquinone (4), 1,3,8-trihydroxy-2-methoxy- anthraquinone (5), 2-hydroxymethyl-3-hydroxyanthraquinone (6), 2-methoxyanthraquinone (7) and scopoletin (8) from an ethanolic extract of the roots of Morinda officinalis. Compounds 4-8 are isolated for the first time from M. officinalis. Among them, compounds 2 and 3 promoted osteoblast proliferation, while compounds 4, 5 increased osteoblast ALP activity. All of the isolated compounds inhibited osteoclast TRAP activity and bone resorption, and the inhibitory effects on osteoclastic bone resorption of compounds 1 and 5 were stronger than that of other compounds. Taken together, antiosteoporotic activity of M. officinalis and its anthraquinones suggest therapeutic potential against osteoporosis.

Berberine inhibits adipocyte differentiation, proliferation and adiposity through down-regulating galectin-3.

This study is designed to investigate the effects of berberine (BBR) on galectin-3 (Gal-3) and the relationships to its suppressive activities on adipocyte differentiation, proliferation and adiposity. Our results showed that BBR greatly suppressed the differentiation and proliferation of mouse primary preadipocytes isolated from epididymal white adipose tissue (eWAT), during which the expression level of Gal-3 was down-regulated significantly. Overexpression of Gal-3 totally abolished the suppressive activities of BBR on Gal-3 expression, preadipocyte differentiation and proliferation. BBR reduced Gal-3 promoter activity, destabilized its mRNA and inhibited firefly luciferase activity of a recombinant plasmid containing the Gal-3 3' untranslated region (UTR). Furthermore, BBR up-regulated microRNA (miRNA) let-7d expression and the suppressive activity on Gal-3 3'UTR was abolished by point mutation on the let-7d binding site. In mice fed a high-fat diet (HFD), BBR up-regulated let-7d and down-regulated Gal-3 expression in eWAT; it also suppressed adipocyte differentiation and proliferation and reduced adiposity greatly. In summary, our study proves that BBR inhibits the differentiation and proliferation of adipocytes through down-regulating Gal-3, which is closely associated with its anti-obesity effect. Our results may support the future clinical application of BBR for the treatment of obesity or related diseases.

Expression of soluble triggering receptor expression on myeloid cells-1 in pleural effusion.

BACKGROUND: Triggering receptors expressed on myeloid cells (TREM) proteins are a family of cell surface receptors expressed broadly by cells of the myeloid lineage. The aim of this study was to investigate the clinical significance of soluble TREM-1 (sTREM-1) in pleural effusions, and to determine the effects of pneumonia on pleural sTREM-1 concentrations. METHODS: Pleural fluid was collected from 109 patients who presented to the respiratory institute (35 with malignant pleural effusion, 31 with tuberculous pleural effusion, 21 with bacterial pleural effusion, and 22 with transudate). The concentrations of sTREM-1, tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta) were determined in effusion and serum samples by enzyme linked immunosorbent assay (ELISA). RESULTS: The concentrations of sTREM-1 in bacterial pleural effusion were significantly higher than those in malignant, tuberculous, and transudative groups (all P < 0.001). An sTREM-1 cutoff value of 768.1 ng/L had a sensitivity of 86% and a specificity of 93%. Pleural sTREM-1 levels were positively correlated with levels of TNF-alpha and IL-1beta. Patients with complicating bacterial pneumonia did not have elevated concentration of sTREM-1 in pleural effusion when compared with patients without pneumonia. CONCLUSIONS: Determination of pleural sTREM-1 may improve the ability of clinicians to differentiate pleural effusion patients of bacterial origin from those with other etiologies. The occurrence of bacterial pneumonia did not affect pleural sTREM-1 concentrations.

Spatial-temporal dynamics of carbon emissions and carbon sinks in economically developed areas of China: a case study of Guangdong Province.

This study analysed spatial-temporal dynamics of carbon emissions and carbon sinks in Guangdong Province, South China. The methodology was based on land use/land cover data interpreted from continuous high-resolution satellite images and energy consumption statistics, using carbon emission/sink factor method. The results indicated that: (1) From 2005 to 2013, different land use/land cover types in Guangdong experienced varying degrees of change in area, primarily the expansion of built-up land and shrinkage of forest land and grassland; (2) Total carbon emissions increased sharply, from 76.11 to 140.19 TgC yr-1 at the provincial level, with an average annual growth rate of 10.52%, while vegetation carbon sinks declined slightly, from 54.52 to 53.20 TgC yr-1. Both factors showed significant regional differences, with Pearl River Delta and North Guangdong contributing over 50% to provincial carbon emissions and carbon sinks, respectively; (3) Correlation analysis showed social-economic factors (GDP per capita and permanent resident population) have significant positive impacts on carbon emissions at the provincial and city levels; (4) The relationship between economic growth and carbon emission intensity suggests that carbon emission efficiency in Guangdong improves with economic growth. This study provides new insight for Guangdong to achieve carbon reduction goals and realize low-carbon development.

Antioxidant and Hepatoprotective Activities of Crude Polysaccharide Extracts from Lingzhi or Reishi Medicinal Mushroom, Ganoderma lucidum (Agaricomycetes), by Ultrasonic-Circulating Extraction.

We recently proposed, and successfully applied, a novel and efficient technique-ultrasonic-circulating extraction (UCE) integrating superfine pulverization-to extract and prepare antioxidant crude polysaccharides other natural active substances from Ganoderma lucidum. The aim of this study was to evaluate the antioxidant and hepatoprotective activities and active ingredients in the powder from UCE (UCEP) through comparison with powder from hot water extraction (HWEP). The DPPH radical, ABTS radical, superoxide anion, total antioxidant activity, and ferric-reducing antioxidant power assay results showed that the UCEP exhibited stronger (P < 0.01) in vitro antioxidant activity than the HWEP. The hepatoprotective activity of the extracts was evaluated against CCl4-induced oxidative damage in the liver. Measurements of reduced glutathione, superoxide dismutase, and malondialdehyde in rat liver; measurements of alanine transaminase, aspartate transaminase, and lactate dehydrogenase in rat blood; and Western blotting for antioxidant proteins of transforming growth factor-ß1, heme-oxygenase 1, and glutathione per-oxidase showed that the UCEP had antioxidant activity in vivo either similar to or slightly stronger than (P < 0.1) the HWEP. Further analysis of the active ingredients revealed that the UCEP and HWEP have similar mean yield and total triterpenoid content, but the former has significantly higher (P < 0.05) mean yield and total polysaccharide content than the latter. Our results suggest that the UCEP displays stronger antioxidant activities because of the larger amount of total polysaccharides; the UCEP may be able to be used as an antioxidant and liver protectant.

Serum tumor-associated autoantibodies as diagnostic biomarkers for lung cancer: A systematic review and meta-analysis.

OBJECTIVE: We performed a comprehensive review and meta-analysis to evaluate the diagnostic values of serum single and multiplex tumor-associated autoantibodies (TAAbs) in patients with lung cancer (LC). METHODS: We searched the MEDLINE and EMBASE databases for relevant studies investigating serum TAAbs for the diagnosis of LC. The primary outcomes included sensitivity, specificity and accuracy of the test. RESULTS: The systematic review and meta-analysis included 31 articles with single autoantibody and 39 with multiplex autoantibodies. Enzyme-linked immunosorbent assay (ELISA) was the most common detection method. For the diagnosis of patients with all stages and early-stage LC, different single or combinations of TAAbs demonstrated different diagnostic values. Although individual TAAbs showed low diagnostic sensitivity, the combination of multiplex autoantibodies offered relatively high sensitivity. For the meta-analysis of a same panel of autoantibodies in patients at all stages of LC, the pooled results of the panel of 6 TAAbs (p53, NY-ESO-1, CAGE, GBU4-5, Annexin 1 and SOX2) were: sensitivity 38% (95% CI 0.35-0.40), specificity 89% (95% CI 0.86-0.91), diagnostic accuracy 65.9% (range 62.5-81.8%), AUC 0.52 (0.48-0.57), while the summary estimates of 7 TAAbs (p53, CAGE, NY-ESO-1, GBU4-5, SOX2, MAGE A4 and Hu-D) were: sensitivity 47% (95% CI 0.34-0.60), specificity 90% (95% CI 0.89-0.92), diagnostic accuracy 78.4% (range 67.5-88.8%), AUC 0.90 (0.87-0.93). For the meta-analysis of the same panel of autoantibodies in patients at early-stage of LC, the sensitivities of both panels of 7 TAAbs and 6 TAAbs were 40% and 29.7%, while their specificities were 91% and 87%, respectively. CONCLUSIONS: Serum single or combinations of multiplex autoantibodies can be used as a tool for the diagnosis of LC patients at all stages or early-stage, but the combination of multiplex autoantibodies shows a higher detection capacity; the diagnostic value of the panel of 7 TAAbs is higher than the panel of 6 TAAbs, which may be used as potential biomarkers for the early detection of LC.

Anticancer and anti-angiogenic activities of extract from Actinidia eriantha Benth root.

ETHNOPHARMACOLOGICAL RELEVANCE: The roots of Actinidia eriantha Benth (AER) are commonly used traditional folk medicine for the treatment of gastric carcinoma, nasopharyngeal carcinoma, and breast carcinoma. Besides, the anti-proliferative and immunomodulatory effects of AER polysaccharides on tumor-bearing mice have been reported previously. AIM OF THE STUDY: This work was carried out to investigate the anticancer and anti-angiogenic activities of AER. MATERIALS AND METHODS: The growth inhibitory effects of ethanol extracts from the leaves (EEL), stems (EES) and roots (EER) of A. eriantha on human gastric carcinoma SGC7901 cells, human nasopharyngeal carcinoma CNE2 cells, human breast carcinoma MCF7 cells and human umbilical vein endothelial cells (HUVECs) were evaluated by MTT assay. The ethyl acetate fraction from EER (EA-EER) was further investigated for the anticancer activity against SGC7901 cells and the anti-angiogenic activity in HUVECs in vitro. The apoptosis in SGC7901 cells and HUVECs was confirmed by DAPI nuclear staining and flow cytometry analysis, the effect on cellular DNA fragmentation was detected in SGC7901 cells. And the cell cycle-arresting activity in HUVECs was determined by flow cytometry. Moreover, the inhibitory effect of EA-EER on cell migration in HUVECs was observed by both wound-healing and Transwell migration assays. RT-PCR and Western-blotting were performed to determine the mRNA and protein expression levels, respectively, including Bax, Bcl-2 and caspase-3 in SGC7901 cells, as well as VEGF-A and VEGFR-2 in HUVECs. Furthermore, the in vivo anti-angiogenic activity of EA-EER was evaluated by using chick embryo chorioallantoic membrane (CAM) assay. Ultimately, the chemical components in EA-EER were isolated and purified by repeated column chromatography followed by structure characterization using 1H and 13C nuclear magnetic resonance and mass spectroscopy. RESULTS: Compared with EEL and EES, EER displayed the strongest growth inhibitory effect on SGC7901 cells, CNE2 cells and HUVECs. Among the EER fractions, EA-EER exhibited the most potent growth inhibitory activity against SGC7901 cells, CNE2 cells and HUVECs. Moreover, EA-EER induced obvious apoptosis in SGC7901 and HUVECs, and significantly inhibited the proliferation of HUVECs via blockade of cell cycle G1 to S progression. Furthermore, EA-EER suppressed the expression of Bcl-2 and improved the expression Bax and caspase-3 in SGC7901 cells. EA-EER not only inhibited migration of HUVECs, but also down-regulated the expression of VEGF-A and VEGFR-2 in HUVECs. In vivo, EA-EER exposure reduced the formation of blood vessels in chick embryos. A bio-guided isolation of EA-EER led to the isolation of three compounds for the first time, namely (6R, 7E, 9S)-6, 9-hydroxy-megastigman-4, 7-dien-3-one-9-O-ß-D-glucopyranoside, Oleanolic acid-23-O-ß-D-glucopyranoside, 3ß, 23, 24-trihydroxyl-12-oleanen-28-oic acid. CONCLUSION: The present research demonstrated that the significant anticancer and anti-angiogenic effects of AER, providing the supportive evidence for its traditional use in the treatment for cancer. It was suggested that AER could be use as a potential source of cancer therapeutic drug.