A new crinane-type alkaloid, 6-epihydroxypowelline (1), together with six known alkaloids, lycorine (2), 2-O-acetyllycorine (3), deacetylbowdensine (4), 1-epideacetylbowdensine (5), 8-demethyl-3-oxomaritidine (6), and (-)-marithamine (7) were isolated from the whole parts of the Crinum latifolium L. in Vietnam. The structure identification of all compounds was determined by 1D, 2D-NMR as well as HR-ESI-MS spectroscopic techniques. The absolute configuration of these compounds was established by the ECD data. In addition, in vitro inhibition of acetylcholinesterase (AChE) activities was assessed for all isolated alkaloids. All alkaloids had AChE inhibitory effects, with IC50 values ranging from 32.65 ± 2.72 to 212.76 ± 8.30 µM and compound 3 displayed the strongest inhibition of AChE, with IC50 values of 32.65 ± 2.72 µM (in comparison to the reference drug, galanthamine, which had an IC50 of 2.40 ± 0.45 µM).

A new crinane-type alkaloid, 6-epihydroxypowelline (1), together with six known alkaloids, lycorine (2), 2-O-acetyllycorine (3), deacetylbowdensine (4), 1-epideacetylbowdensine (5), 8-demethyl-3-oxomaritidine (6), and (-)-marithamine (7) were isolated from the whole parts of the Crinum latifolium L. in Vietnam. The structure identification of all compounds was determined by 1D, 2D-NMR as well as HR-ESI-MS spectroscopic techniques. The absolute configuration of these compounds was established by the ECD data. In addition, in vitro inhibition of acetylcholinesterase (AChE) activities was assessed for all isolated alkaloids. All alkaloids had AChE inhibitory effects, with IC50 values ranging from 32.65 ± 2.72 to 212.76 ± 8.30 µM and compound 3 displayed the strongest inhibition of AChE, with IC50 values of 32.65 ± 2.72 µM (in comparison to the reference drug, galanthamine, which had an IC50 of 2.40 ± 0.45 µM).

A new crinane-type alkaloid, 6-epihydroxypowelline (1), together with six known alkaloids, lycorine (2), 2-O-acetyllycorine (3), deacetylbowdensine (4), 1-epideacetylbowdensine (5), 8-demethyl-3-oxomaritidine (6), and (-)-marithamine (7) were isolated from the whole parts of the Crinum latifolium L. in Vietnam. The structure identification of all compounds was determined by 1D, 2D-NMR as well as HR-ESI-MS spectroscopic techniques. The absolute configuration of these compounds was established by the ECD data. In addition, in vitro inhibition of acetylcholinesterase (AChE) activities was assessed for all isolated alkaloids. All alkaloids had AChE inhibitory effects, with IC50 values ranging from 32.65 ± 2.72 to 212.76 ± 8.30 µM and compound 3 displayed the strongest inhibition of AChE, with IC50 values of 32.65 ± 2.72 µM (in comparison to the reference drug, galanthamine, which had an IC50 of 2.40 ± 0.45 µM).

A new crinane-type alkaloid, 6-epihydroxypowelline (1), together with six known alkaloids, lycorine (2), 2-O-acetyllycorine (3), deacetylbowdensine (4), 1-epideacetylbowdensine (5), 8-demethyl-3-oxomaritidine (6), and (-)-marithamine (7) were isolated from the whole parts of the Crinum latifolium L. in Vietnam. The structure identification of all compounds was determined by 1D, 2D-NMR as well as HR-ESI-MS spectroscopic techniques. The absolute configuration of these compounds was established by the ECD data. In addition, in vitro inhibition of acetylcholinesterase (AChE) activities was assessed for all isolated alkaloids. All alkaloids had AChE inhibitory effects, with IC50 values ranging from 32.65 ± 2.72 to 212.76 ± 8.30 µM and compound 3 displayed the strongest inhibition of AChE, with IC50 values of 32.65 ± 2.72 µM (in comparison to the reference drug, galanthamine, which had an IC50 of 2.40 ± 0.45 µM).

A new crinane-type alkaloid, 6-epihydroxypowelline (1), together with six known alkaloids, lycorine (2), 2-O-acetyllycorine (3), deacetylbowdensine (4), 1-epideacetylbowdensine (5), 8-demethyl-3-oxomaritidine (6), and (-)-marithamine (7) were isolated from the whole parts of the Crinum latifolium L. in Vietnam. The structure identification of all compounds was determined by 1D, 2D-NMR as well as HR-ESI-MS spectroscopic techniques. The absolute configuration of these compounds was established by the ECD data. In addition, in vitro inhibition of acetylcholinesterase (AChE) activities was assessed for all isolated alkaloids. All alkaloids had AChE inhibitory effects, with IC50 values ranging from 32.65 ± 2.72 to 212.76 ± 8.30 µM and compound 3 displayed the strongest inhibition of AChE, with IC50 values of 32.65 ± 2.72 µM (in comparison to the reference drug, galanthamine, which had an IC50 of 2.40 ± 0.45 µM).

Adult ; Aged ; Aqueous Humor ; virology ; Female ; Humans ; Immunocompetence ; immunology ; Inflammation ; virology ; Male ; Middle Aged ; Retrospective Studies ; Young Adult

BACKGROUNDThe patients with early-onset epileptic encephalopathy (EOEE) suffer from neurodevelopmental delay. The aim of this study was to analyze the clinical manifestations and amplitude-integrated encephalogram (aEEG) characteristics of infants with EOEE with onset within the neonatal period, to make early diagnosis to improve the prognosis.

METHODSOne-hundred and twenty-eight patients with neonatal seizure were enrolled and followed up till 1 year old. Sixty-six neonates evolved into EOEE were as the EOEE group, the other 62 were as the non-EOEE (nEOEE) group. Then we compared the clinical and aEEG characteristics between the two groups to analyze the manifestations in neonates with EOEE.

RESULTSCompared to the nEOEE group, the incidence of daily seizure attacks, more than two types of convulsions, more than two antiepileptic drugs (AEDs) application, severely abnormal aEEG background, absence of cyclicity, and more than two seizures detection were significantly higher in the EOEE group (P < 0.05) (97% vs. 54.8%; 30.3% vs. 14.5%; 97.0% vs. 25.4%; 39.4% vs. 3.2%; 57.6% vs. 9.7%; and 56% vs. 3.2%, respectively). Severely abnormal background pattern (odds ratio [OR] = 0.081, 95% confidence interval [CI]: 0.009-0.729, P = 0.025) and more than two seizures detection by aEEG (OR = 0.158, 95% CI: 0.043-0.576, P = 0.005) were the independent risk factors for the evolvement into EOEE. The upper and lower margins of active sleep (AS) and quiet sleep (QS) were significantly higher in EOEE group than those of the control group (P < 0.05) (34.3 ± 13.6 vs. 21.3 ± 6.4; 9.9 ± 3.7 vs. 6.7 ± 2.2; 41.2 ± 15.1 vs. 30.4 ± 11.4; and 11.9 ± 4.4 vs. 9.4 ± 4.0; unit: μV, respectively). AS upper margin was demonstrated a higher diagnostic specificity and sensitivity for EOEE than another three parameters according to the receiver operating characteristic curves; the area under the curve was 0.827.

CONCLUSIONSThe clinical characteristics of the neonatal seizure which will evolve into EOEE were more than two AEDs application, high seizure frequency (daily attack), and more than two types of the seizure. Significant high voltage, severely abnormal background, absence of cyclicity, and more than two seizures detected on aEEG were the meaningful indicators to the prediction of EOEE.

Objective: To observe the efficacy of ticagrelor for treating elderly acute coronary syndrome (ACS) patients with elective PCI and having low response to clopidogrel; to explore the bleeding risks induced by ticagrelor replacement. Methods: A total of 945 ACS patients ≥ 65 years treated in our hospital from 2014-01 to 2017-01 were enrolled. All patients received aspirin and clopidogrel dual antiplatelet therapy (DAPT), thrombelastography (TEG) was used to detect platelet inhibition rate when DAPT ≥ 5 days. Based on platelet inhibition rate, the patients were divided into 2 groups:Ticagrelor replacement group, n=293 patients with low response to clopidogrel and switched to ticagrelor treatment, when adjusted DAPT ≥ 5 days, platelet inhibition rate was rechecked to compare the changes; Clopidogrel group, the patients were continuously treated by the same medication, n=652. The patients were followed-up for 3 months, bleeding events were evaluated by TIMI criteria and compared between 2 groups. Risk factors of ticagrelor induced bleeding were assessed by multivariate Logistic regression analysis. Results: Platelet inhibition rates in Ticagrelor replacement group were (51.70±42.90) %, (48.99±41.85) % and (55.08±25.70) % at (5-7) d, (8-14) d and (15-90) d ticagrelor treatment, which were higher than previous clopidogrel treatment (14.50±24.15) %, all P<0.05. The incidences of severe bleeding events were similar between 2 groups, P=0.96. Multivariate Logistic regression analysis presented that female (OR=4.329, P=0.000), low body weight (OR=0.817, P=0.039) and elevated fasting blood glucose (OR=1.251, P=0.028) were the independent risk factors for bleeding complication in ticagrelor treated elderly ACS patients. Conclusion: Compared with clopidogrel, ticagrelor may faster and more effectively inhibit platelet aggregation without increasing severe bleeding; female, low body weight and elevated fasting blood glucose were the independent risk factors for bleeding complication in ticagrelor treated elderly ACS patients with elective PCI.

In vitro neuraminidase inhibition assays and ultrafiltration liquid chromatography with diodearray detector coupled to time of flight mass spectrometer (UPLC-DAD-TOF-MS) were combined to screen bioactive compounds inhibiting neuraminidase from Isatidis Radix. By comparing the compounds from Isatidis Radix before and after ultrafiltration, we found that arginine, goitrin and adenosinea can bind with neuraminidase, and the binding degree of the three compounds were (36.23 +/- 1.12)%, (32.54 +/- 1.02)% and (9.38 +/- 0.47)%, respectively. The IC50 of arginine and goitrin were (1.16 +/- 0.02), (1.20 +/- 0.02) g x L(-1), respectively. While the IC50 of adenosinea was higher than 500 g x L(-1). The results showed that arginine and goitrin might be the main compounds with antiviral activity of Isatidis Radix. This study may provide a useful method for the screening of bioactive compounds and quality control of Isatidis Radix.
Antiviral Agents ; analysis ; pharmacology ; Arginine ; analysis ; pharmacology ; Drug Evaluation, Preclinical ; Drugs, Chinese Herbal ; analysis ; pharmacology ; Isatis ; chemistry ; Mass Spectrometry ; Neuraminidase ; antagonists & inhibitors ; metabolism ; Orthomyxoviridae ; drug effects ; enzymology ; Oxazolidinones ; analysis ; pharmacology ; Plant Roots ; chemistry ; Ultrafiltration ; Viral Proteins ; antagonists & inhibitors ; metabolism

The study is to report the establishment of a method of screening the antitumor compounds based on the dynamic bio-response profile of cells to make up for the shortages of conventional end-point tests such as tedious operation and low sensitivity. Based on the principle of electric impedance of cells, the real-time cell electronic sensing (RT-CES) system was used to monitor the effect of epirubicin (EPI), cisplatinum (DDP) and carboplatin (CBP) on the growth of HepG2 cells, with the cell index (CI), half maximal inhibitory concentration (IC50) and detachment curve as evaluation indexes. Meanwhile, cell counting kit-8 (CCK-8) and microscopy were applied for verification. The results showed that CI curve could sensitively real-time profile the inhibitory effect of model drugs on HepG2 cells. The IC50 of EPI, DDP and CBP were 0.53 +/- 0.04, 9.79 +/- 0.26 and 597.00 +/- 3.79 microg x mL(-1), respectively. What's more, the significant differences of detachment curves of the three drugs indicated that their functional mechanisms might be different, this is consistent with the literature. The RT-CES system with non-invasive, label-free and real-time characteristics could be used to monitor the bio-response profile of the three drugs to HepG2 cells, allowing to qualitatively and quantitatively distinguish the antitumor activities of the three drugs, and could be a complementary method for the present screening of antitumor compounds.
Antineoplastic Agents ; pharmacology ; Biosensing Techniques ; methods ; Cell Count ; Cell Line, Tumor ; Cisplatin ; pharmacology ; Drug Screening Assays, Antitumor ; Electric Impedance ; Humans