[A new sesquiterpene lactone from biological transformation of Hericium erinaceus and Artemisiae Annuae Herba].

This study aimed to investigate the chemical constituents from the biological transformation of Hericium erinaceus and Artemisiae Annuae Herba(HQ biological transformation). The chemical constituents of ethyl acetate fraction of 75% ethanol extract in HQ biological transformation were separated and purified by silica gel and Sephadex LH-20 gel column chromatographies together with semi-preparative high performance liquid chromatography(HPLC). Their structures were identified by physicochemical properties, spectroscopic analysis, as well as comparisons with the data reported in literature. Nine compounds were isolated and identified as 2α-hydroxydeoxyartemisinin(1), 6ß-hydroxy-stigmast-4,22-dien-3-one(2), 3ß,5α-dihydroxy-ergosta-7,22-dien-6-one(3), friedelin(4), dankasterone(5), ergosterol endoperoxide(6), 3ß-hydroxy-5,9-epoxy-(22E,24R)-ergosta-7,22-dien-6-one(7), 3α,5α,9α-trihydroxy-(22E,24R)-ergosta-7,22-dien-6-one(8), and stigmast-3-one(9). Compound 1 was a new sesquiterpene lactone named 2α-hydroxy-deoxyartemisinin. The activity against Helicobacter pylori(Hp) of compounds 1-9 in vitro was determined by Kirby-Bauer disk diffusion method. The screening results showed compounds 1, 2 and 5 had certain anti-Hp activity.

Long-term efficacy and safety of hypoxia-inducible factor prolyl hydroxylase inhibitors in anaemia of chronic kidney disease: A meta-analysis including 13,146 patients.

WHAT IS KNOWN AND OBJECTIVE: Previous studies based on small-sample clinical data proved that short-term use of hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors increased haemoglobin levels in anaemic patients with chronic kidney disease (CKD). However, these studies reached conflicting conclusions on iron parameters and adverse event profiles. Our meta-analysis aimed to evaluate the long-term efficacy and safety of HIF-PHD inhibitors in renal anaemia. METHODS: Randomized controlled trials comparing treatment with HIF-PHD inhibitors versus placebo or erythropoiesis-stimulating agents (ESAs) were thoroughly searched in the PubMed, Embase, Cochrane Library and international clinical trial registries. Meta-analysis was performed on main outcomes with random effects models. RESULTS AND DISCUSSION: A total of 30 studies comprising 13,146 patients were included. The HIF-PHD inhibitors used included roxadustat, daprodustat, vadadustat, molidustat, desidustat and enarodustat. HIF-PHD inhibitors significantly increased haemoglobin levels in comparison with placebo [weighted mean difference (WMD) 1.53, 95% confidence interval (CI) 1.39 to 1.67] or ESAs (WMD 0.13, 95% CI 0.03 to 0.22). Hepcidin, ferritin and serum iron levels were decreased, while total iron binding capacity and transferrin levels were increased in the HIF-PHD inhibitor group versus those in placebo or ESAs group. Additionally, HIF-PHD inhibitors medication was associated with cholesterol-lowering effects. As for safety, the risk of serious adverse events in the HIF-PHD inhibitor group was increased in comparison with placebo group [risk ratio (RR) 1.07, 95% CI 1.01 to 1.13], but comparable to the ESAs group (RR 1.02, 95% CI 0.94 to 1.10). Compared with placebo, the agents increased the risk of diarrhoea (1.21, 1.00 to 1.47), nausea (1.46, 1.09 to 1.97), oedema peripheral (1.32, 1.01 to 1.59), hyperkalemia (1.27, 1.05 to 1.54) and hypertension (1.34, 1.02 to 1.76). Compared with ESAs, the drugs increased the risk of vomiting (1.30, 1.02 to 1.65), headache (1.27, 1.05 to 1.53) and thrombosis events (1.31, 1.05 to 1.63). WHAT IS NEW AND CONCLUSION: HIF-PHD inhibitors treatment effectively increased haemoglobin levels and promoted iron utilization in anaemic patients with CKD, and they were well tolerated for long-term use. In order to avoid unfavourable effects of excessive iron consumption, it was appropriate to administer HIF-PHD inhibitors in combination with iron supplements for long-term treatment.

Alkaloids and phenylpropanoid from Rhizomes of Arundo donax L.

A new bis-indole alkaloid, named arundaline (1), a new phenylpropanoid, named arundalcohol (2), and four known alkaloids, N-acetyltryptamine (3), trans-N-(p-coumaroyl)serotonin (4), trans-N-feruloylserotonin (5), and tuberosine B (6), were isolated from 70% aqueous ethanol extracts of the rhizomes of Arundo donax L. Their structures were elucidated by spectroscopic analysis and comparison of the data with literature values. Compounds 3-6 were isolated from the genus Arundo for the first time.

Inhibition of LPS-induced brain injury by NR2B antagonists through reducing assembly of NR2B-CaMKII-PSD95 signal module.

Background: Accumulating evidence suggests that inflammation is a contributor to the cause and progression of neurodegenerative disease, such as Alzheimer's disease (AD) and Parkinson disease (PD). However, the exact mechanisms of neuroinflammation are still unclear. Here, we discussed the potential mechanisms of lipopolysaccharide (LPS)-induced brain injury via NR2B antagonists (Ro25-6981) treatment in mice. Methods: Neuroinflammation was induced in mice by virtue of LPS (1 mg/kg) by intraperitoneal injection. Immunoprecipitation was performed to measure the assembly of NR2B-calmodulin dependent protein kinase II (CaMKII)-Postsynaptic density protein 95 (PSD95) signal module in the hippocampus and frontal cortex. Nissl's staining was employed to access neuron injury in the brain. Results: Data demonstrated that LPS could induce neuron damage, and promote the assembly of NR2B-CaMKII-PSD95 signal module and increase the expression of phosphorylated CaMKII and c-Jun N-terminal kinase (JNK) in the frontal cortex and hippocampus. However, NR2B antagonists could protect neuron injury against LPS-induced inflammation, inhibit the assembly of NR2B-CaMKII-PSD95 signal module and decrease the level of phosphorylated CaMKII and JNKs in mice. Conclusions: These findings indicated that the assembly of NR2B-CaMKII-PSD95 signal module is related to LPS-induced neuroinflammation, NR2B plays a key role in the assembly of NR2B-CaMKII-PSD95 signal module and NR2B antagonists could alleviate LPS-related inflammation through the reduced assembly of NR2B-CaMKII-PSD95 signal module in frontal cortex and hippocampus.

Protective effect and mechanisms of Weining granule on N-methyl-N'-nitro-N- nitrosoguanidine-induced gastric cancer in rats.

OBJECTIVE: To investigate the protective effect and molecular mechanisms of Weining granule on N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced gastric cancer in rats. METHODS: A total of sixty healthy male wistar rats were randomly divided into five groups, including control group (CG), gastric cancer model group (MG), low-dose Weining granule treated group (LWT), medium-dose Weining granule treated group (MWT), and high-dose Weining granule treated group (HWT). Except the control group, the other groups were treated with MNNG to establish a rat model of gastric cancer. Low-dose Weining granule treated group, medium-dose Weining granule treated group, and high-dose Weining granule treated group were fed 9.0, 18.0 and 36.0 g/kg Weining granule, respectively. Histopathologic and molecular biologic technology were adopted to determine the protective effect of Weining granule on MNNG-induced gastric cancer in rats. The pathological changes of gastrointestinal tissue were observed. Meanwhile, the differential expression of proliferation, apoptosis and angiogenesis markers were determined, including proliferating cell nuclear antigen (PCNA), pokemon, cyclin D1, B-cell lymphoma-2 (Bcl-2), caspase-3, phosphatase and tensin homolog (PTEN) and vascular endothelial growth factor (VEGF). RESULTS: After the MNNG treated, the pathological changes of stomach tissue were improved noticeably, including the intestinal metaplasia and atypic hyperplasia. The experiment was completed in 58 rats (96.67%). As compared with gastric cancer model group, the general states of rats were improved significantly after treated with different dose Weining granule. Moreover, treatment with different doses of Weining granule could inhibit the protein and mRNA expression of PCNA, pokemon, cyclin D1, Bcl-2, and VEGF, while increase caspase-3 and PTEN (P < 0.01). CONCLUSION: Weining granule could improve gastric cancer by suppressing cell proliferation, promoting tumor cell apoptosis, and inhibiting angiogenesis.

[A new sesquiterpene from Acorus calamus (â ¡)].

A new quaiane-tgpe sesquiterpene was isolated from the 95% ethanol extract of the rhizomes of Acorus calamus by silica gel and sephadex LH-20 column chromatographic methods. Structure and absolute configuration of the sesquiterpene were elucidated by spectroscopic data and X-ray crystallographic analysis, and named as 1R,5R,7S-guaiane-4R,10R-diol-6-one.

Chinese herb extract improves liver steatosis by promoting the expression of high molecular weight adiponectin in NAFLD rats.

High molecular weight (HMW) adiponectin (APN) is closely correlated with the development of fatty liver and is modulated by the Akt/forkhead box protein O1 (FOXO1) pathway through disulfide­bond A oxidoreductase­like protein (DsbA­L). The Chinese herb extract, QSHX, is used to treat liver diseases. The present study investigated the effects of QSHX on non­alcoholic fatty liver disease (NAFLD) and its underlying mechanism. A rat model of NAFLD was established by feeding of a high­fat and high­sugar diet for 20 weeks. From week 13, the rats were administered with QSHX, or saline as a control, for 8 weeks. The liver function, blood fat and plasma APN were measured using a radioimmunoassay. The hepatic tissue score was measured following staining for pathology. The expression and activities of Akt, FOXO1, DsbA­L and HMW APN in the adipose tissue and primary adipocytes of the rats were measured using western blot analysis. It was found that QSHX significantly decreased the body weight, liver index, and serum levels of aspartate aminotransferase, alanine aminotransferase and triglyceride; and increased the serum level of APN in the NAFLD rats. Following 8 weeks of treatment with QSHX, the hepatic steatosis in the liver tissue improved and the score of hepatic steatosis was significantly decreased. The results of the western blot analysis indicated that QSHX promoted the expression of DsbA­L and HMW APN, and reduced the expression levels of phosphorylated FOXO1 and FOXO1 in adipose tissue and primary adipocytes. It was concluded that QSHX reduced hepatic steatosis by promoting the expression of HMW APN and DsbA­L, which may have been induced by inhibiting the activation and expression of FOXO1 in adipocytes.

New Acorane-Type Sesquiterpene from Acorus calamus L.

A new sesquiterpene, named neo-acorane A (1), and two known ones, acoric acid (2) and calamusin D (3), were isolated from a 95% ethanol extract of the rhizome parts of Acorus calamus L. Their structures were elucidated by spectroscopic methods, and the absolute configurations were determined by single-crystal X-ray diffraction analysis. Compounds 1 and 2 are nonisoprenoid sesquiterpenoids, likely biosynthesized from an acorane-type sesquiterpene by oxidative fission of the six- or five-membered ring. Moreover, compounds 1 (10 µM), 2 (5 µM and 10 µM) and 3 (10 µM) showed cell proliferation activity on the SK-N-BE (2) cell line.

[Sesquiterpenoids of Acori Calami Rhizoma].

To study the chemical constituents and antimicrobial activity of Acori Calami Rhizoma. Components were isolated through various chromatographic methods and identified by spectroscopic data. The agar dilution method was adopted to analyze antimicrobial activity of the compounds in vitro.Eleven sesquiterpenoids were isolated, and indentified as 4ß,6ß-dihydroxy-1α,5ß(H)-guai-9-ene(1),4ß,6ß-dihydroxy-1α,5ß(H)-guai-10(14)-ene(2), teuclatriol(3), isocalamendiol(4), calamendiol(5), calamusin H(6), oxyphyllenodiols A(7), oplodiol(8), ananosmin(9), epishyobunone(10), and bullatantriol(11). Compound 9 was isolated from genus Acorus for the first time. Compounds 3, 7-9, and 11 had significantly antimicrobial activity. There were good sterilizing effects that the MBC of compound 9 to the four tested strains were 20.00 mg•L⁻¹, and compound 11 to Pseudomonas aeruginosa was 12.50 mg•L⁻¹.

[Determination of five pyrethroid pesticides residues in Anoectochilus roxburghii by cloud point extraction-back extraction and GC-MS].

A method for residual determination of 5 pyrethroid pesticides in Anoectochilus roxburghii by cloud point extraction-back extraction-GC-MS was established. PEG 6000 was used as extraction agent and isooctane was used for back-extractant. The con- tent was calculated by external standard method. The linear range was from 15 to 2 000 µg x kg(-1) with the good correlation coefficients (0.955-0.999). The recoveries at spiked concentrations of 50-500 µg x kg(-1) ranged from 85.12% to 101.6%. The limit of detection and quantification of 5 pyrethroid pesticides were in the range of 0.63-3.10 µg x kg(-1) and 2.10-10.31 µg x kg(-1), respectively. The proposed method can be applied to the determination of pyrethroid pesticides residues in A. roxburghii.

Efficacy and safety of traditional Chinese medicine for the treatment of acquired immunodeficiency syndrome: a systematic review.

OBJECTIVE: To systematically review the efficacy and safety of Traditional Chinese Medicine (TCM) interventions, compared with control interventions (placebo or conventional Western medical therapy), in the treatment of acquired immunodeficiency syndrome (AIDS). METHODS: Electronic databases including PubMed, the Cochrane Library, China National Knowledge Infrastructure (CNKI), and Wanfang Data were searched to identify relevant randomized controlled trials (RCTs) published as of May 2012. Studies were selected according to the specified inclusion and exclusion criteria and then subjected to methodological quality assessment, data extraction, and meta-analysis according to the Cochrane Handbook for Systematic Reviews of Interventions. RESULTS: Twelve RCTs involving 881 patients with AIDS were included. Methodological quality assessment showed that two were high-quality, two were moderate-quality, and eight were low-quality. Meta-analysis showed that TCM interventions were associated with significantly reduced plasma viral load compared with placebo [odds ratio OR = 2.46, 95% confidence interval CI (1.02, 5.94); P = 0.04]. However, the reductions in plasma viral load significantly favored conventional Western medical therapy alone over integrated traditional Chinese and Western medical therapy [OR = 0.16, 95% CI (0.05, 0.55); P = 0.004]. Patients receiving TCM interventions had significantly higher CD4+ T lymphocyte counts compared with those on placebo [OR = 2.54, 95% CI (1.40, 4.60); P = 0.002]. In addition, TCM interventions were significantly more likely to have improved clinical symptoms [OR = 2.82, 95% CI (1.85, 4.31); P < 0.00001]. TCM interventions conferred a similar risk of adverse events (AEs) compared with control interventions [OR = 1.87, 95% CI (0.58, 6.01); P = 0.29]. CONCLUSION: Current evidence suggests that TCM interventions are significantly more effective than placebo in reducing plasma viral load and increasing CD4+ T lymphocyte count in patients with AIDS. When compared with conventional Western medical therapy, TCM interventions were significantly less effective in reducing plasma viral load, although they were associated with a higher percentage of patients with improved symptoms. Patients receiving TCM interventions did not seem to be at an increased risk of AEs.

[Biological characteristics of Fusarium oxysporum and inhibitory effects of five fungicides].

The mycelium growth and sporulation in different temperature, pH value and light conditions were detected by using the crossing and haemocytometer method. The toxicity of five fungicides to Fusarium oxysporum was tested by mycelia growth method, so as to provide the reference for prevention and control against F. oxysporum. The optimum temperature and pH value of F. oxysporum to grow and spore were 28 degrees C and 6-7. Alternating light and darkness promoted growth and sporulation of bacterial colony. As for five fungicides, the EC50 of tebuconazole was 10.02 mg x L(-1), 92.50 times as much as carbendazim. The EC50 of myclobutanil and Fuxing was 91.23, 96.68 mg x L(-1), respectively. Tebuconazole showed the most tremendous inhibitory effect and control efficiency on F. oxysporum.

Optimization of polysaccharides extraction from Tetrastigma hemsleyanum Diels et Gilg using response surface methodology.

A 15-run Box-Behnken design (BBD) was used to optimize the extraction conditions of polysaccharides from Tetrastigma hemsleyanum Diels et Gilg. Three factors such as extraction temperature (°C), extraction time (h), and ratio of water to raw material were investigated. The experimental data were fitted to a second-order polynomial equation using multiple regression analysis and also examined using the appropriate statistical methods. The adjusted coefficient of determination (R(Adj)(2)) for the model was 0.9754, and the probability value (P=0.001) demonstrated a high significance for the regression model. The optimum extraction conditions were found to be: optimized extraction temperature 83.3°C, extraction time 1.55 h and ratio of water to raw material 29.48. Under these conditions, the mean extraction yield of polysaccharides was 5.182 ± 0.093 %, which was in good agreement with the predicted model value.