In vivo antimalarial activity of synthetic hepcidin against Plasmodium berghei in mice / 中国天然药物

The present study was designed to investigate the antimalarial activity of synthetic hepcidin and its effect on cytokine secretion in mice infected with Plasmodium berghei. The mice were infected with P. berghei intravenously and treated with hepcidin according to 4-day suppression test and Rane's test. The serum levels of interleukins (IL-1β, IL-2, IL-6, IL-10, IL-12p70, and IL-17A), tumor necrosis factor-α (TNF-α), and interferon-γ (IFN-γ) in the experimental mice were determined using a cytometric bead array (CBA) kit. The survival rate of the infected mice was also registered. Additionally, the serum iron, alanine transaminase (ALT), aspartate transaminase (AST), and total bilirubin (BIL) were detected to evaluate liver functions. Hepcidin exerted direct anti-malarial function in vivo and increased survival rate in a dose-dependent manner. In addition, the secretion of T helper cell type 1 (Th1), Th2, and Th17 cytokines, TNF-α, and IFN-γ were inhibited by hepcidin. In conclusion, our results demonstrated that synthetic hepcidin exerts in vivo antimalarial activity and possesses anti-inflammatory function, which provides a basis for future design of new derivatives with ideal anti-malarial activity.

Phenolic acids isolated from the fungus Schizophyllum commune exert analgesic activity by inhibiting voltage-gated sodium channels / 中国天然药物

The present study was designed to search for compounds with analgesic activity from the Schizophyllum commune (SC), which is widely consumed as edible and medicinal mushroom world. Thin layer chromatography (TLC), tosilica gel column chromatography, sephadex LH 20, and reverse-phase high performance liquid chromatography (RP-HPLC) were used to isolate and purify compounds from SC. Structural analysis of the isolated compounds was based on nuclear magnetic resonance (NMR). The effects of these compounds on voltage-gated sodium (NaV) channels were evaluated using patch clamp. The analgesic activity of these compounds was tested in two types of mouse pain models induced by noxious chemicals. Five phenolic acids identified from SC extracts in the present study included vanillic acid, m-hydroxybenzoic acid, o-hydroxybenzeneacetic acid, 3-hydroxy-5-methybenzoic acid, and p-hydroxybenzoic acid. They inhibited the activity of both tetrodotoxin-resistant (TTX-r) and tetrodotoxin-sensitive (TTX-s) NaV channels. All the compounds showed low selectivity on NaV channel subtypes. After intraperitoneal injection, three compounds of these compounds exerted analgesic activity in mice. In conclusion, phenolic acids identified in SC demonstrated analgesic activity, facilitating the mechanistic studies of SC in the treatment of neurasthenia.

Identification and characterization of a novel neuropeptide (neuropeptide Y-HS) from leech salivary gland of Haemadipsa sylvestris / 中国天然药物

The present study was designed to identify immunomodulatory components from the leech salivary gland of Haemadipsa sylvestris. The Sephadex G-50, Resource(TM) S column chromatography and reverse-phase high performance liquid chromatography (RP-HPLC) were used to isolate and purify the salivary gland extracts (SGE). Structural analysis of isolated compounds was based on Edman degradation and matrix assisted laser desorption ionization time-of-flight mass spectrometer (MALDI-TOF-MS). The cDNA encoding the precursor of the compound was cloned from the cDNA library of the salivary gland of H. sylvestris. The levels of inflammatory mediators, including tumor necrosis factor-α (TNF-α), interferon γ (IFN-γ), interleukin-6 (IL-6), and monocyte chemotactic protein-1 (MCP-1) were assayed using an enzyme-linked immunosorbent assay (ELISA). The effects on cell proliferation and cell viability were observed using MTT assay. A novel neuropeptide Y (Neuropeptide Y-HS) from the leech salivary gland of H. sylvestris was purified and characterized. It was composed of 36 amino acid residues and the amino acid sequence was determined to be FLEPPERPAVFTSVEQMKSYIKALNDYYLLLGRPRF-NH2, containing an amidated C-terminus. It showed significant inhibitory effects on the production of inflammatory cytokines including TNF-α, IFN-γ, IL-6, and MCP-1. Neuropeptide Y was identified from leeches for the first time. The presence of neuropeptide Y-HS in leech salivary gland may help get blood meal from hosts and inhibit inflammation.

Determination of cinnamic acid, cinnama ldehyde, paeonol, alisol B 23-acetate, atractylodes lancea and atractylodin in Yeming granules by RP-HPLC / 中国药学杂志

OBJECTIVE: To develop a RP-HPLC method for determination of cinnamic acid, cinnama ldehyde, paeonol, alisol B 23 acetate, atractylodes lancea, and atractylodin in Yeming granules. METHODS: The determination was performed on an Eclipse XDB-C18column (4.6 mm × 250 mm, 5 μm) at 30°C with a flow rate of 1.0 mL · min-1. The mobile phase was 0.3% phosphate-acetonitrile at gradient elution. The detection wavelength was set at 240 nm. RESULTS: The linear regression equations for cinnamic acid, cinnama ldehyde, paeonol, alisolB 23 acetate, atractylodes lancea, and atractylodin were ρ=-0.0055A + 0.0083 (r=0.9996), ρ=0.0255, 4+0.1336 (r=0.9999), ρ=0.0408 A +0.664 3 (r=0.999), ρ=0.003 3 4+0.0171(r=0.999 9), ρ=0.0163 A + 0.1075 (r=0.999 8), ρ=0.0229A + 0.0884 (r=0.9999), respectively. Good linearity was obtained over the ranges of 0.3096-2.322, 10.24-76.8, 37.36-280.2, 0.5128-3.846, 1.612-12.09 and 10.26-76.95 μg · mL-1, respectively. The recoveries were 100.1%, 99.8%, 100.7%, 99.3%, 100.4% and 100.5%, respectively. CONCLUSION: The method is simple and suitable to control the quality of Yeming granules. Copyright 2012 by the Chinese Pharmaceutical Association.