Therapeutic effects and mechanism of ferulic acid and icariin in mammary gland hyperplasia model rats via regulation of the ERK pathway.

Background: Ferulic acid (FA) and icariin (ICA), as the active compounds derived from and , respectively, have been shown to promote blood circulation, regulate menstruation, exhibit anti-inflammatory effects, and modulate estrogen levels. The aim of this study was to elucidate the possible mechanism of FA, ICA, and FA-ICA on estrogen-induced mammary gland hyperplasia (MGH) in rats.

Methods: Hematoxylin and eosin (HE) staining was performed to record the pathological changes in breast tissue, and enzyme-linked immunosorbent assay (ELISA) was utilized to determine the serum levels of luteinizing hormone (LH), PRL (prolactin), testosterone (T), estradiol (E2), follicular stimulating hormone (FSH), and progesterone (P).

Comparison of the efficacy and safety of intensive-dose and standard-dose statin treatment for stroke prevention: A meta-analysis.

Background: Previous study indicated that high-dose statin treatment might increase the risk of hemorrhagic stroke and adverse reactions. We aim to compare the efficacy and safety of intensive-dose and standard-dose statin treatment for preventing stroke in high-risk patients.

Methods: A thorough search was performed of multiple databases for publications from 1990 to June 2015.

Cytotoxic nor-dammarane triterpenes from Viburnum hainanense Merr. et Chun.

Five new nor-dammarane triterpenes, 12β-O-acetyl-17β-hydoxy-3,15-dioxo-20,21,22,23,24,25,26,27-octanordammanran (1), 12β-hydoxy-17β-methoxy-3,15-dioxo-20,21,22,23,24,25,26,27-octanordammanran (2), 12β-O-acetyl-3,15-dioxo-17-en-20,21,22,23,24,25,26,27-octanordammanran (3), 12β-hydoxy-15α-O-acetyl-3-oxo-17-en-20,21,22,23,24,25,26,27-octanordammanran (4) and 3β-hydoxy-17-oxo-12-en-20,21,22,23,24,25,26,27-octanordammanran (5), were obtained from the ethanol extract of the whole plants of Viburnum hainanense Merr. et Chun. Structural elucidation of all the compounds was performed by spectral methods such as 1D and 2D NMR, IR, UV, and HRESIMS.

Quantification of Niacin and Its Metabolite Nicotinuric Acid in Human Plasma by LC-MS/MS: Application to a Clinical Trial of a Fixed Dose Combination Tablet of Niacin Extended-Release/Simvastatin (500 mg/10 mg) in Healthy Chinese Volunteers.

Our paper aimed to develop rapid, sensitive, and specific LC-MS/MS method for the quantification of niacin (NA) and its metabolite nicotinuric acid (NUA) in human plasma. Following protein precipitation with acetonitrile, the NA, NUA, and internal standard (5-fluorouracil) were separated on a Zorbax 300SB-C8 column (250 mm × 4.6 mm, 5 μm) with a mobile phase consisting of methanol-2 mM ammonium acetate (3 : 97, v/v) at a flow rate of 1 mL/min (split 1 : 1).

Estrogen receptor α enhances the transcriptional activity of ETS-1 and promotes the proliferation, migration and invasion of neuroblastoma cell in a ligand dependent manner.

Background: It is well known that estrogen receptor α (ERα) participates in the pathogenic progress of breast cancer, hepatocellular carcinoma and head and neck squamous cell carcinoma. In neuroblastoma cells and related cancer clinical specimens, moreover, the ectopic expression of ERα has been identified. However, the detailed function of ERα in the proliferation of neuroblastoma cell is yet unclear.

Antinociceptive activity of astragaloside IV in the animal model of chronic constriction injury.

To investigate the applicability of astragaloside IV (AG) for the treatment of refractory neuropathic pain, we systemically evaluated the antinociceptive activity of AG in the animal model of chronic constriction injury. We studied behaviors, electrophysiology, and biochemistry from day 2 to day 23 after the surgery. We found that when administered intraperitoneally at the dose of 60 mg/kg, AG caused significant inhibition of allodynia and hyperalgesia induced by mechanic and thermal stimuli as well as downregulation of the expressions of a series of proteins involved in mediating neuropathic pain in the dorsal root ganglia, such as P2X purinoceptor 3, glial cell-derived neurotrophic factor, glial cell-derived neurotrophic factor family receptor α1, and transient receptor potential cation channel subtypes A1 and V1.

Simultaneous determination of calycosin-7-O-β-d-glucoside, calycosin, formononetin, astragaloside IV and schisandrin in rat plasma by LC-MS/MS: application to a pharmacokinetic study after oral administration of Shenqi Wuwei chewable tablets.

A rapid, sensitive and reliable high-performance liquid chromatography-mass spectrometry (LC-MS/MS) method was developed and validated for simultaneous quantification of the five main bioactive components, calycosin, calycosin-7-O-β-d-glucoside, formononetin, astragaloside IV and schisandrin in rat plasma after oral administration of Shenqi Wuwei chewable tablets. Plasma samples were extracted using solid-phase extraction separated on a CEC18 column and detected by MS with an electrospray ionization interface in multiple-reaction monitoring mode. Calibration curves offered linear ranges of two orders of magnitude with r > 0.

Evaluation of the wound-healing activity and anti-inflammatory activity of aqueous extracts from Acorus calamus L.

In folklore medicine, Acorus calamus has been used as a wound-healing agent for thousands of years; however, there have been few scientific reports on this activity so far. Now, we explored deeply the wound-healing effect of aqueous extracts from the fresh roots and rhizomes of A. calamus in vivo, as well as anti-inflammatory activity in vitro, so as to provide scientific evidence for the traditional application.

The application of an LC-MS/MS method in a pharmacokinetic study for the determination of the concentration of nifekalant in human plasma.

In the present study, a simple, rapid, and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of the concentration of Nifekalant in human plasma was developed and validated. The analyte and the internal standard were extracted from human plasma using dichloromethane and analyzed using an ultra-fast liquid chromatographer (UFLC) coupled to an electrospray ionization (ESI) tandem mass spectrometer in the positive mode. The chromatographic analysis was performed isocratically on an Inertsil ODS-SP column (150mm×4.

3-(4-Meth-oxy-phen-yl)-6,7-dihydro-1H-furo[3,4-c]pyran-4(3H)-one.

In the title compound, C14H14O4, the dihedral angle between the hydro-furan and benzene rings is 88.41 (15)°. The hydro-pyran ring adopts an envelope conformation, with the O-bound methyl-ene C atom as the flap.

Antibacterial, antifungal and cytotoxic isoquinoline alkaloids from Litsea cubeba.

Five novel isoquinoline alkaloids (+)-N-(methoxylcarbonyl)-N-nordicentrin (1), (+)-N-(methoxylcarbonyl)-N-norpredicentrine (2), (+)-N-(methoxylcarbonyl)-N-norbulbodione (3), and (+)-N-(methoxylcarbonyl)-N-norisocorydione (4), and (+)-8-methoxyisolaurenine-N- oxide (5) were isolated, together with one known compound, (+)-N-(methoxylcarbonyl)- N-norglaucine (6), from a 70% EtOH extract of the barks of Litsea cubeba. Structural elucidation of all the compounds were performed by spectral methods such as 1D- and 2D-NMR, IR, UV, and HRESIMS. Alkaloids 1, 2 and 6 showed antimicrobial activity against the bacterium S.

The influence of omeprazole on platelet inhibition of clopidogrel in various CYP2C19 mutant alleles.

Currently, concerns of clopidogrel and proton pump inhibitors (especially omeprazole) interaction are raised, because they are both metabolized by CYP2C19. What is more, omeprazole can also inhibit the activity of CYP2C19. The study was to compare the influence of omeprazole on platelet inhibition of clopidogrel in various CYP2C19 mutant alleles.

The analgesic activity and possible mechanisms of deacetyl asperulosidic acid methyl ester from Ji shi teng in mice.

Deacetyl Asperulosidic Acid Methyl Ester (DAAME) from Ji shi teng was evaluated on analgesic activity in mice using chemical and thermal models of nociception. Given intraperitoneally, DAAME, at doses of 40 and 80 mg/kg, produced significant inhibitions on chemical nociception induced by intraperitoneal acetic acid, subplantar formalin/capsaicin injections and on thermal nociception in the tail-flick test and in the hot plate test. In the open-field test and the rotarod test, DAAME couldn't impair the motor performance, indicating that the observed antinociception was unlikely due to motor abnormality.

Design and evaluation of self-emulsifying drug delivery systems of Rhizoma corydalis decumbentis extracts.

To improve the dissolution and oral absorption of Rhizoma corydalis decumbentis extracts (RCDE), a famous traditional Chinese herbal medicine which contains poorly water-soluble active components, self-emulsifying drug-delivery systems (SEDDS) were designed and evaluated in vitro and in vivo for the first time. Six formulations were prepared, and pseudoternary phase diagrams were constructed to identify the efficient self-emulsication region through the modified visual test. The optimized formulation consisted of 45% Solutol, 40% ethyl oleate, and 15% Transcutol P.

Analgesic activity of the aqueous fraction from the ethanolic extract of Chrysanthemum indicum in mice.

The aqueous fraction (AF) of an ethanolic extract from Chrysanthemum indicum was evaluated for analgesic activity in mice using chemical and thermal models of nociception. Given orally, AF at doses of 300 and 600 mg/kg produced significant inhibitions on chemical nociception induced by intraperitoneal acetic acid, subplantar formalin/capsaicin injections and on thermal nociception in the tail-flick test and in the hot plate test. In the pentobarbital sodium-induced sleeping time test and the open-field test, AF neither significantly enhanced the pentobarbital sodium-induced sleeping time nor impaired the motor performance, indicating that the observed analgesic activity was unlikely due to sedation or motor abnormality.

Mechanisms involved in the antinociception of petroleum ether fraction from the EtOH extract of Chrysanthemum indicum in mice.

The petroleum ether fraction (PEF) from the EtOH extract of flowers and buds of Chrysanthemum indicum was evaluated on antinociception in mice using chemical and thermal models of nociception. PEF administered orally at doses of 188 and 376 mg/kg produced significant inhibitions on chemical nociception induced by intraperitoneal acetic acid, subplantar formalin or capsaicin injections and on thermal nociception in the tail-flick test and the hot plate test. In the pentobarbital sodium-induced sleep time test and the open-field test, PEF neither enhanced the pentobarbital sodium-induced sleep time nor impaired the motor performance, indicating that the observed antinociception was unrelated to sedation or motor abnormality.

Antitumor activity of two gelsemine metabolites in rat liver microsomes.

Gelsemine is one of the major alkaloids from Gelsemium elegans Benth., which has been used as an antitumor remedy in clinic. In this paper, metabolism of gelsemine has been investigated in vitro in phenobarbital-treated rat liver microsomes.