[Research progress on chemical constituents and pharmacological effects of Glechomae Herba and prediction of its Q-markers].

Glechomae Herba, the dried aerial part of Glechoma longituba(Labiatae), has the effects of promoting urination, draining dampness, and relieving stranguria. It has received wide attention in recent years owing to the satisfactory efficacy on lithiasis. Amid the in-depth chemical and pharmacological research, it has been found that Glechomae Herba has antibacterial, anti-inflammatory, antioxidant, antithrombotic, hepatoprotective, cholagogic, antitumor, hypoglycemic, and lipid-lowering effects. The main chemical constituents are volatile oils, flavonoids, terpenoids, phenylpropanoids, and organic acids. This paper summarized the chemical constituents and pharmacological effects of Glechomae Herba. Based on genetic relationship of plants, the characteristics, efficacy, and pharmacokinetics of the chemical constituents, and the potential of these constituents as quality markers(Q-markers), it was summed up that ursolic acid, caffeic acid, rosmarinic acid, luteolin-7-O-diglucuronide, apigenin, apigenin-7-O-diglucuronide, apigetrin, and glechone can be the candidate Q-markers of Glechomae Herba.

Pentacyclic triterpenoids from spikes of Prunella vulgaris L. with thyroid tumour cell cytostatic bioactivities.

Five new triterpenoids, including four ursane types (1-4) and one oleanane type (5), together with 15 known ursane types pentacyclic triterpenoids (6-20) were isolated from the fruit spikes of Prunella vulgaris L., a traditional Chinese herbal medicine. Their structures were elucidated based on IR, HR-ESI-MS, and NMR spectroscopic data. The SW579 cell line was used to evaluate anti-thyroid cancer activities of (1-20). The results indicated that (7-9), (16), and (19) exhibited apparent inhibitory activity with IC50 values of 25.73-71.41 µM (cisplatin as positive control, IC50 14.49 ± 0.97 µM). Network pharmacology and molecular docking were also used for the prediction of the synergistic actions and the underlying mechanisms. Accordingly, four potential targets have been characterized.

New chlorophenolic glycoside from Curculigo orchioides and their activities on 5α-reductase.

Two new chlorophenolic glucosides curculigines P (1) and Q (2), together with seven known compounds (3-9), were isolated from the dried rhizomes of Curculigo orchioides. Their structures were determined by spectroscopic methods including 1 D, 2 D NMR and MS. All the isolated compounds were evaluated on 5α-reductase activity by a HaCaT-based bioassay. Compounds 1-9 showed varying degrees of inhibiting activity against 5α-reductase, while compound 1 indicated the most potent inhibitory effect.[Formula: see text].

Hypoxia-inducible factor-prolyl hydroxylase inhibitor ameliorates myopathy in a mouse model of chronic kidney disease.

Muscle wasting and diminished physical performance contribute to the morbidity and mortality of chronic kidney disease (CKD), for which no curative therapy exists. Accumulating evidence indicates that impaired angiogenesis occurs in the muscles of CKD models. Therefore, proangiogenesis therapy is considered a potentially effective strategy for limiting CKD-associated myopathy. Hypoxia-inducible factor (HIF)-prolyl hydroxylase inhibitor (HIF-PHI) stabilizes HIF and enhances muscle angiogenesis during acute ischemia; however, little evidence was available from CKD models. Here, we assessed whether pharmacological activation of HIF by MK-8617 (MK), a novel orally active HIF-PHI, improves CKD-associated myopathy. Mice were divided into sham or CKD groups, and CKD mice were subdivided into CKD + vehicle or MK treatment groups (1.5, 5, or 12.5 mg/kg for 12 wk). In CKD mice, skeletal muscle mass, mitochondrial amount, and exercise capacity decreased compared with sham mice. Compared with the CKD + vehicle group, low (1.5 mg/kg) and medium (5 mg/kg) doses of MK, but not the high dose (12.5 mg/kg), significantly restored these changes and was accompanied by incremental increases in HIF-1α. Furthermore, increased capillary density and area were observed in a MK dose-dependent manner, which is likely related to an improved VEGF response in the skeletal muscle of CKD mice. In addition, macrophage and proinflammatory cytokines, including monocyte chemoattractant protein 1, TNF-α, and IL-6, significantly increased in the high-dose MK group. These results indicate that HIF-PHI provides a potential therapeutic strategy to improve CKD-associated myopathy.

LINGO-1 antibody ameliorates myelin impairment and spatial memory deficits in the early stage of 5XFAD mice.

AIMS: Multiple evidence has indicated that myelin injury is common in Alzheimer's disease (AD). However, whether myelin injury is an early event in AD and the relationship between it and cognitive function is still elusive. METHODS: Spatial memory of 5XFAD mice was determined by Morris water maze at 1 and 3 months old. Meanwhile, the deposition of Aß, the expression of myelin basic protein (MBP), LINGO-1, NgR, and myelin ultrastructure in many memory-associated brain regions were detected in one-month-old and three-month-old mice (before and after LINGO-1 antibody administration) using immunostaining, Western blot (WB), and transmission electron microscopy (TEM), respectively. RESULTS: No abnormal Aß deposition was found in one-month-old 5XFAD mice. However, spatial memory deficits were proved in accordance with an obvious demyelination in memory-associated brain regions in one-month-old mice and both deteriorated with age. Administration of LINGO-1 antibody could obviously restore the myelin impairments in CA1 and DG region and partially ameliorate spatial memory deficits. CONCLUSIONS: Our results demonstrated that myelin injury was an early event in 5XFAD mice even prior to emergence of deposition of Aß. Intervention with the LINGO-1 antibody could attenuate impaired spatial memory deficits by remyelination, which suggested that myelin injury was involved in spatial memory deficits and remyelination may be a potential therapeutic strategy in early stage of AD or mild cognitive impairments.

The Effect of Apolipoprotein E ε4 (APOE ε4) on Visuospatial Working Memory in Healthy Elderly and Amnestic Mild Cognitive Impairment Patients: An Event-Related Potentials Study.

Background: Apolipoprotein E (APOE) ε4 is the only established risk gene for late-onset, sporadic Alzheimer's disease (AD). Previous studies have provided inconsistent evidence for the effect of APOE ε4 status on the visuospatial working memory (VSWM). Objective: The aim was to investigate the effect of APOE ε4 on VSWM with an event-related potential (ERP) study in healthy controls (HC) and amnestic mild cognitive impairment (aMCI) patients. Methods: The study recorded 39 aMCI patients (27 APOE ε4 non-carriers and 12 APOE ε4 carriers) and their 43 matched controls (25 APOE ε4 non-carriers and 18 APOE ε4 carriers) with an 64-channel electroencephalogram. Participants performed an N-back task, a VSWM paradigm that manipulated the number of items to be stored in memory. Results: The present study detected reduced accuracy and delayed mean correct response time (RT) in aMCI patients compared to HC. P300, a positive component that peaks between 300 and 500 ms, was elicited by the VSWM task. In addition, aMCI patients showed decreased P300 amplitude at the central-parietal (CP1, CPz, and CP2) and parietal (P1, Pz, and P2) electrodes in 0- and 1-back task compared to HC. In both HC and aMCI patients, APOE ε4 carriers showed reduced P300 amplitude with respect to non-carriers, whereas no significant differences in accuracy or RT were detected between APOE ε4 carriers and non-carriers. Additionally, standardized low-resolution brain electromagnetic tomography analysis (s-LORETA) showed enhanced brain activation in the right parahippocampal gyrus (PHG) during P300 time range in APOE ε4 carriers with respect to non-carriers in aMCI patients. Conclusion: It demonstrated that P300 amplitude could predict VSWM deficits in aMCI patients and contribute to early detection of VSWM deficits in APOE ε4 carriers.

Spatial learning and memory impairments are associated with increased neuronal activity in 5XFAD mouse as measured by manganese-enhanced magnetic resonance imaging.

Dysfunction of neuronal activity is a major and early contributor to cognitive impairment in Alzheimer's disease (AD). To investigate neuronal activity alterations at early stage of AD, we encompassed behavioral testing and in vivo manganese-enhanced magnetic resonance imaging (MEMRI) in 5XFAD mice at early ages (1-, 2-, 3- and 5-month). The 5XFAD model over-express human amyloid precursor protein (APP) and presenilin 1 (PS1) harboring five familial AD mutations, which have a high APP expression correlating with a high burden and an accelerated accumulation of the 42 amino acid species of amyloid-ß. In the Morris water maze, 5XFAD mice showed longer escape latency and poorer memory retention. In the MEMRI, 5XFAD mice showed increased signal intensity in the brain regions involved in spatial cognition, including the entorhinal cortex, the hippocampus, the retrosplenial cortex and the caudate putamen. Of note, the observed alterations in spatial cognition were associated with increased MEMRI signal intensity. These findings indicate that aberrant increased basal neuronal activity may contribute to the spatial cognitive function impairment at early stage of AD, and may further suggest the potential use of MEMRI to predict cognitive impairments. Early intervention that targets aberrant neuronal activity may be crucial to prevent cognitive impairment.

Seventeen steroids from the pith of Tetrapanax papyriferus.

Two new steroidal ketones (1, 2), together with 10 known steroids (3-12) and five known steroidal saponins (13-17), have been obtained from the pitch of Tetrapanax papyrierus. The structures of 1 and 2 were elucidated as 3ß-hydroxystigmast-8, 22-diene-7,11-dione and 3ß-hydroxystigmast-8-ene-7,11-dione by IR, HR-ESI-MS, 1D and 2D NMR techniques. Except for 4, 14, 15, 16, 13 compounds reported in this paper were isolated from Tetrapanax papyriferus for the first time.

[Forensic analysis of LCN DNA using sample concentration methods followed by miniSTR genotyping].

OBJECTIVE: To optimize low copy number (LCN) DNA analysis methods for forensic STR genotyping. METHODS: Two groups of DNA sample, extracted using either Magnetic bead method or Chelex-100 methods, were previously amplified with a Identifiler PCR Amplification kit, but no genotype was detected. The DNA samples were concentrated using either a drying method or the Microcon-100 method, then amplified using an miniFiler PCR Amplification kit and genotyped. RESULTS: Among the 127 DNA samples, 47 samples, previously extracted using the Magnetic bead method, were genotyped with 36% success rate. Eighty samples, previously extracted using the Chelex-100 method, were genotyped with 30% success rate. CONCLUSION: The application of sample concentration methods and miniFiler kit can improve the success rate of LCN STR analysis.

[Evaluation of antioxidant activity of Radix Linderae and other two Chinese drugs using TLC-bioautography].

AIM: To evaluate the antioxidant capacity and quality of traditional Chinese medicines using TLC-bioautography. METHODS: Two chromatograms of each crude drug sample were obtained, after developing, by spraying with 1,1-diphenyl-2-picrylhydrazyl (DPPH) solution in ethanol and classical stained reagents, separately. The images sprayed with DPPH solution were captured under light after the plates were heated at 40 degrees C for 30 min, and scanned using video scan software to get peak areas of active compounds. RESULTS: Total peak areas of the spots on TLC were calculated to evaluate the antioxidant capacity of the tested crude drugs from different habitats and sources. The results indicated that Radix Linderae cultivated in Tiantai (Zhejiang province), Cortex Magnoliae Officinalis cultivated in Liangshan (Sichuan province), and Fructus Perillae acquired in Shanghai have the highest scavenging properties towards DPPH in their respective TLC-autographic assays. Norisoboldine, magnolol and honokiol, luteolin, apigenin and an unknown compound "U" proved to be the major antioxidant components in the corresponding crude drugs as they contribute the dominating peak areas to the total ones. CONCLUSION: TLC-bioautography can not only be used for screening of the components with antioxidant potency but also for the purpose of quality evaluation of traditional Chinese medicines at the same time, and the method proved to be selective, simple and reproducible.

[DNA genotyping of oral epithelial cells by laser capture microdissection].

OBJECTIVE: The STR genotypping of trace oral epithelial cells which are microdissected by laser capture microdissection system (LCM) is explored. METHODS: The oral epithelial cells are microdissected using a low-power infrared laser by VERITAS Microdissection Instrument. STR loci of Profiler Plus are detected by multiplex PCR procesures. RESULTS: DNA genotyping of 7-8 oral epithelial cells are succeeded, and DNA genotyping of 3-4 oral epithelial cells are failed. CONCLUSION: It is viable in genotyping of trace oral epithelial cells by Laser Capture Microdissection as a new technology of seperating single cell.

[PCR-based STR genotyping of sweat latent fingerprint samples involved in cases].

OBJECTIVE: To study the extracting and genotyping method of sweat latent fingerprint samples involved in cases. METHOD: Chlex 100 extraction method was used to extract DNA. STR loci were typed after PCR amplification by Profiler Plus kit. RESULTS: All the sweat latent fingerprint samples involved in cases obtained reliable results of STR genotyping. CONCLUSION: It is very important to find and extract sweat latent fingerprint samples properly for STR genotyping.

Simultaneous determination of six isoflavonoids in commercial Radix Astragali by HPLC-UV.

A HPLC-UV method for the quantification of six major isoflavonoids, calycosin 7-O-beta-D-glucoside (1), formononetin 7-O-beta-D-glucoside (2), (6alphaR, 11alphaR) 3-hydroxy-9,10-dimethoxypterocarpan-3-O-beta-D-glucoside (3), 7,2'-dihydroxy-3',4'-dimethoxyisoflavan-7-O-beta-D-glucoside (4), calycosin (5) and formononetin (6), in Radix Astragali (Huangqi) was developed and validated. The method was proven to be sensitive, specific, accurate and precise, as well as effective and easy.

[Determination of shionone in Radix Asteris by HPLC].

OBJECTIVE: To determine the content of shionone in Radix Aster from several different locations and markets. METHOD: The HPLC analysis was used to determine shionone directly, using Polaris C18 column and acetonitrile as the mobile phase with a flow rate of 1.0 mL.min-1, and the UV detection wavelength was 200 nm. RESULT AND CONCLUSION: The content of shionone was from 0.06% to 0.18%, depending on different locations and markets.

[Determination of calycosin-7-O-beta-D-glucopyranoside in radix astragali by HPLC].

OBJECTIVE: TO establish a RP-HPLC method for the determination of calycosin-7-O-beta-D-glucopyranoside in Radix Astragali, and to analyse the calycosin-7-O-beta-D-glucopyranoside content of ten samples of Radix Astragali, collected from different regions. METHOD: A Polaris C18(250 mm x 4.6 mm, 5 microns) column was used and a mixture of methanol-water (30:70) was used as the mobile phase at a flow rate of 1.0 mL.min-1. The column temperature was 25 degrees C and the UV detection wavelength was 254 nm. RESULT: The calibration curve was in good linearity over the range of 0.0106-2.12 micrograms with the regression equation Y = 3035. 97 X - 14.85(r = 0.9999). The average recovery was 95.8% (n = 5, RSD = 1.3%). CONCLUSION: The method is simple, quick, sensitive and reproducible. In all of the samples, the calycosin-7-O-beta-D-glucopyranoside contents differ markedly.