[Therapeutic effect and mechanism of Mailuo Shutong Pills on posterior limb swelling caused by femur fracture in rats based on intestinal flora and intestinal metabolism].

This study aimed to investigate the protective effect and underlying mechanism of Mailuo Shutong Pills(MLST) on posterior limb swelling caused by femur fracture in rats. The rats were randomly divided into a sham operation group, a model group, a low-dose MLST group(1.8 g·kg~(-1)·d~(-1)), a high-dose MLST group(3.6 g·kg~(-1)·d~(-1)), and a positive drug group(60 mg·kg~(-1)·d~(-1) Maizhiling Tablets). The femur in the sham operation group was exposed and the wound was sutured, while the other four groups underwent mechanical damage to cause femur fracture. The rats were treated with corresponding drugs by gavage 7 days before modeling and 5 days after modeling, while those in the sham operation group and the model group were given an equivalent dose of distilled water by gavage. Hematoxylin-eosin(HE) staining was used to detect the pathological injury of the posterior limb muscle tissues in rats, and the degree of hind limb swelling was measured. The enzyme-linked immunosorbent assay(ELISA) kit was used to detect the expression levels of interleukin-6(IL-6), interleukin-1ß(IL-1ß), and tumor necrosis factor-α(TNF-α) in the serum of rats in each group. The activity of superoxide dismutase(SOD), malondialdehyde(MDA), catalase(CAT), and glutathione peroxidase(GSH-Px) in rat serum was also measured. Western blot was used to detect the protein expression levels of heme oxygenase 1(HO-1), NAD(P)H quinone oxidoreductase 1(NQO1), and nuclear transcription factor E2-related factor 2(Nrf2) in rat posterior limb muscle tissues. The changes in the intestinal flora and intestinal metabolites in rats were detected by 16S rDNA sequencing and ultra-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS), respectively, to explore the underlying mechanism of MLST in treating posterior limb swelling caused by femur fracture in rats. Compared with the model group, MLST significantly improved the degree of posterior limb swelling in rats, reduced the levels of serum inflammatory factors, and alleviated oxidative stress injury. The HE staining results showed that the inflammatory infiltration in the posterior limb muscle tissues of rats in the MLST groups was significantly improved. Western blot results showed that MLST significantly increased the protein expression of HO-1, NQO1, and Nrf2 in rat posterior limb muscle tissues compared with the model group. The 16S rDNA sequencing results showed that MLST improved the disorder of intestinal flora in rats after femur fracture. The UPLC-MS/MS results showed that MLST significantly affected the bile acid biosynthesis and metabolism pathway in the intestine after femur fracture, and the Spearman analysis confirmed that the metabolite deoxycholic acid involved in bile acid biosynthesis was positively correlated with the abundance of Turicibacter. The metabolite cholic acid was positively correlated with the abundance of Papilibacter, Staphylococcus, and Intestinimonas. The metabolite lithocholic acid was positively correlated with Papilibacter and Intestinimonas. The above results indicated that MLST could protect against the posterior limb swelling caused by femur fracture in rats. This protective effect may be achieved by improving the pathological injury of the posterior limb muscle, reducing the expression levels of inflammatory and oxidative stress-related factors in serum, reducing the oxidative injury of the posterior limb muscle, improving intestinal flora, and balancing the biosynthesis of bile acids in the intestine.

Quality markers of Baizhu dispensing granules based on multi-component qualitative and quantitative analysis combined with network pharmacology and chemometric analysis.

ETHNOPHARMACOLOGICAL RELEVANCE: The dispensing granules of traditional Chinese medicines (TCMs) is an innovative form of medicinal material for TCMs decoction, which is gradually recognized in the clinic due to being suitable for production on a large scale and convenient to take for patients. However, the quality control of TCMs dispensing granules is being challenged, because they contain too many unrevealed hydrophilic components. AIM OF THE STUDY: Here, the dispensing granules produced from the rhizome of Atractylodes macrocephala (Baizhu dispensing granules), were explored as a case to explore the quality markers correlated to the clinical efficacy of TCMs dispensing granules by a comprehensive strategy of integrating chemical profiling, network pharmacology, and chemometric analysis. MATERIALS AND METHODS: First, the chemical profiling of Baizhu dispensing granules was characterized by using ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS). Subsequently, the potential active components responsible for the efficacy of Baizhu dispensing granules were screened via network pharmacology, and the ultra-performance liquid chromatography coupled with photodiode array detector (UPLC-PDA) method was developed for quantitative analysis of the potential active components in 26 batches of Baizhu dispensing granules. Finally, the quality markers of Baizhu dispensing granules were deciphered based on content variations of potential active components and chemometric analysis. RESULTS: A total of 69 components were identified from Baizhu dispensing granules. Network pharmacology analysis further revealed that eight of them including five caffeoylquinic acids (31, 32, 36, 42, 44) and three sesquiterpenoids (63, 67, 76) were intimately connected to the core targets of dyspepsia, enteritis, gastritis and immunity. The contents of eight components differed greatly among 26 batches of Baizhu dispensing granules. Chlorogenic acid (31), cryptochlorogenic acid (32) and atractylenolide III (63) have higher concentrations and make great contributions to distinguish different batches of the Baizhu dispensing granules based on principal component analysis (PCA) and orthogonal partial least squares-discriminate analysis (OPLS-DA), and could be used as the quality markers of Baizhu dispensing granules. CONCLUSIONS: Our study defined the quality markers of Baizhu dispensing granules, which will benefit further investigation on the quality evaluation of TCMs dispensing granules containing Baizhu. The strategy used in this study will be helpful for discovering the quality markers of other TCMs dispensing granules.

Meta-analysis of clinical trials focusing on hypertonic dextrose prolotherapy (HDP) for knee osteoarthritis.

Hypertonic dextrose prolotherapy (HDP) is an injection of a concentrated dextrose solution for the purpose of local treatment of musculoskeletal pain and possible enhancement of repair mechanisms. This systematic review and meta-analysis examines the clinical utility of HDP injection for treatment of knee osteoarthritis (OA). Randomized controlled trials (RCTs) utilizing HDP to treat knee OA were retrieved from MEDLINE, EMBASE, and Cochrane Library (CENTRAL). Identification and inclusion of RCTs utilizing intra-articular and extra-articular administration of HDP vs administration of other injectate or physical therapy as control for knee OA were included. Primary clinical outcomes were changes in knee WOMAC, pain and function score. Secondary outcomes were adverse events related to HDP. For continuous outcomes with same or different measurements, we calculated, respectively the weighted mean difference (WMD) or the standardized mean difference (SMD), respectively. Results were pooled using DerSimonian and Laird random effect models across the included studies and heterogeneity between studies was estimated using the I2 index. Five studies comprising a total of 319 treated patients met inclusion criteria and were included in the final analysis. At a mean of 22.8 weeks follow-up, HDP treatment significantly improved total WOMAC score (WMD = 13.77, 95% CI: 6.75-20.78; p < 0.001; I2 = 90%), pain (SMD = 1.33, 95% CI: 0.49-2.17; p < 0.001; I2 = 91%) and knee function (SMD = 1.30, 95% CI: 0.45-2.14; p < 0.001; I2 = 91%) compared with control group. There were no severe adverse events related to dextrose injection reported in all the included studies. HDP is a promising treatment for knee OA with a reasonable safety profile. Further research in mechanism of HDP activity and long-term follow-up study will be needed for exploring this novel therapy modality.

Design, synthesis and biological evaluation of novel evodiamine and rutaecarpine derivatives against phytopathogenic fungi.

Evodiamine and rutaecarpine are two alkaloids isolated from traditional Chinese herbal medicine Evodia rutaecarpa, which have been reported to have various biological activities in past decades. To explore the potential applications for evodiamine and rutaecarpine alkaloids and their derivatives, various kinds of evodiamine and rutaecarpine derivatives were designed and synthesized. Their antifungal profile against six phytopathogenic fungi Rhizoctonia solani, Botrytis cinerea, Fusarium graminearum, Fusarium oxysporum, Sclerotinia sclerotiorum, and Magnaporthe oryzae were evaluated for the first time. Furthermore, a series of modified imidazole derivatives of rutaecarpine were synthesized to investigate the structure-activity relationship. The results of antifungal activities in vitro showed that imidazole derivative of rutaecarpine A1 exhibited broad-spectrum inhibitory activities against R. solani, B. cinerea, F. oxysporum, S. sclerotiorum, M. oryzae and F. graminearum with EC50 values of 1.97, 5.97, 12.72, 2.87 and 16.58 µg/mL, respectively. Preliminary mechanistic studies showed that compound A1 might cause mycelial abnormalities of S. sclerotiorum, mitochondrial distortion and swelling, and inhibition of sclerotia formation and germination. Moreover, the curative effects of compound A1 were 94.7%, 81.5%, 80.8%, 65.0% at 400, 200, 100, 50 µg/mL in vivo experiments, which was far more effective than the positive control azoxystrobin. Significantly, no phytotoxicity of compound A1 on oilseed rape leaves was observed obviously even at a high concentration of 400 µg/mL. Therefore, compound A1 is expected to be a novel leading structure for the development of new antifungal agents.

New phenylpropanoids from the fruits of Xanthium sibiricum and their anti-inflammatory activity.

Seven new phenylpropanoids, including two pairs of enantiomers of 8-O-4'-type neolignans, named (±)-xanthiifructins A-B (1a/1b-2a/2b), a pair of simple phenylpropanoid derivatives (±)-xanthiifructins C (3a/3b), and a racemic phenylpropanoid derivative xanthiifructin D (4), together with four known analogues (5-8) were isolated from the fruits of Xanthium sibiricum. Racemic xanthiifructins A-C were separated on chiral HPLC columns. Their structures were elucidated by comprehensive spectroscopic data analysis and comparison with the literatures. The anti-inflammatory and cytotoxic activities were evaluated for all isolates. Among them, (-)-xanthiifructin C (3b) exhibited potent inhibitory effect against nitric oxide production in lipopolysaccharide-activated RAW 264.7 mouse macrophage cells with an IC50 value of 9.94 ± 0.57 µM. All compounds obviously were inactive for three human tumor cell lines (MCF-7, HepG2, and A549) with IC50 values much more than 10 µM.

One pair of new enantiomeric trinorsesquiterpenes from the aerial parts of Justicia gendarussa.

A pair of new enantiomeric trinorsesquiterpenes, (+)-genpenterpene A (1a) and (-)-genpenterpene A (1b), together with seven known compounds (2-8), were isolated from the aerial parts of Justicia gendarussa Burm.f.. All of these known compounds were isolated from this plant for the first time. Racemic genpenterpene A was separated by chiral HPLC column. Their chemical structures were elucidated based on extensive spectroscopic analysis, single crystal X-ray diffraction, and ECD calculations. (+)-genpenterpene A (1a) exhibited potent inhibitory effect against nitric oxide production in lipopolysaccharide-activated RAW 264.7 mouse macrophage cells with an IC50 value of 9.54 ± 1.02 µM.

New compounds from the aerial parts of Justicia gendarussa Burm.f. and their antioxidant and anti-inflammatory activities.

Three new compounds (1-3), together with six known compounds (4-9), were isolated from the ethyl acetate fraction of ethanol extract of the aerial parts of Justicia gendarussa Burm.f. All of these known compounds were isolated from the plant for the first time. Their structures including absolute configurations were elucidated on the basis of HR-ESI-MS, NMR spectroscopic analyses, single crystal X-ray diffraction and comparison with the literatures. Compounds 1-9 were tested for their antioxidant and anti-inflammatory activities. Compounds 5 and 8 showed the antioxidant activities with IC50 values of 28.61 ± 1.56 and 22.55 ± 1.38 µM, respectively. Compounds 2 and 3 showed anti-inflammatory activity in LPS-induced RAW 264.7 macrophages with the IC50 values of 20.95 ± 1.11 and 16.50 ± 1.04 µM, respectively.

Lyciyunin, a new dimer of feruloyltyramine and five bioactive tyramines from the root of Lycium yunnanense Kuang.

Lyciyunin, a new dimer of feruloyltyramine (1), together with five known tyramines (2-6), was isolated from the water-soluble fraction of an EtOH extract of the root of L. yunnanense. Based on HR-TOF-MS, NMR spectral data and quantum chemistry ECD calculations, the structure of this new compound was determined, including its absolute configuration. Compounds (1-6) were tested for their antioxidant activity using in vitro DPPH radical scavenging assay, and 1-6 showed the moderate antioxidant activities with IC50 values of 12.44 ± 0.39, 21.29 ± 0.75, 24.44 ± 1.63, 21.15 ± 0.66, 21.15 ± 0.66 and 45.15 ± 0.56 µM, respectively. Compounds (5-6) showed anti-inflammatory activity in LPS-induced RAW 264.7 macrophages with the IC50 values of 43.95 ± 6.11 and 33.50 ± 2.04 µM, respectively.

Versatile electrochemical biosensor based on bi-enzyme cascade biocatalysis spatially regulated by DNA architecture.

The regulation of biocatalytic cascades in microenvironments for high performance and extended applications is still challenging. Herein, we develop a rolling circle amplification (RCA)-based one-pot method to prepare the micron-sized DNA flowers (DFs), which achieve the co-encapsulation and spatial regulation of bi-enzyme molecules, glucose oxidase (GOx) and horseradish peroxidase (HRP). In this system, GOx and HRP are integrated into the DFs simultaneously during RCA with the bridging of magnesium between enzyme residues and phosphate backbones on DFs. The cascade of GOx/HRP is regulated with the formation of highly ordered and hydrogen-bonded water environment in the cavity of DFs, resulting in an enhanced cascade catalytic efficiency compared with that in homogeneous solution. Moreover, the high density of DNA scaffold ensures the encapsulation of GOx/HRP with high efficiency. Accordingly, a glucose electrochemical biosensor with amplified signal response is fabricated using the as-prepared GOx/HRP DFs as biosensing interface, realizing sensitive detection of glucose. Further, through designing the complementary sequence of aptamer into the programmable circular template of RCA, the bi-enzyme co-encapsulated DFs are versatilely applied to sensitive and selective detection of cancerous exosomes and thrombin in "signal-on" and "signal-off" modes, respectively, which are further applied to the analysis of complex biological samples successfully. Overall, the encapsulation of multi-enzyme with DFs proposes a promising strategy to regulate the microenvironment of biocatalytic cascades, which hold great potential in biotechnology, bioanalysis and disease diagnosis.

Effects and mechanism of Chinese medicine Jiawei Yupingfeng in a mouse model of allergic rhinitis / 中西医结合学报

OBJECTIVE@#Chinese medicine has the potential to modulate allergic rhinitis (AR). There have been studies investigating the treatment efficacy of Yupingfeng San, alone or in combination with other ingredients, in AR, though few have studied the potential mechanisms of these drugs. In the present study, we measured the effects of Jiawei Yupingfeng (JWYPF), a traditional Chinese medicine formula, on mice with ovalbumin-induced AR and explored its underlying mechanism of action.@*METHODS@#Forty BALB/c mice were randomly divided into normal control, allergy control and two treatment groups of ten mice each. In the normal control group, mice were sensitized and challenged with saline. The mice in the allergy control and treatment groups were sensitized and challenged with ovalbumin and aluminum hydroxide gel. The treatments of JWYPF and Nasonex were administered intranasally in the AR mice for one week. Several signs of allergic inflammation, such as nasal eosinophils and inflammatory cytokines, were measured to determine the underlying mechanisms.@*RESULTS@#Mice in the JWYPF and Nasonex groups had significantly lower AR symptom scores than those in the allergy control group (the mean differences between JWYPF and the allergy control, and Nasonex and the allergy control were -2.00 ± 0.35 and -2.40 ± 0.32). After treatment with JWYPF and Nasonex, the levels of ovalbumin-specific IgE and histamine were significantly reduced, as were the levels of interlukin-4 and transforming growth factor-β, while interferon-γ levels were increased (all P < 0.0001, vs. allergy control). These two treatments also significantly inhibited eosinophil and mast cell infiltration into the nasal cavity but were not statistically different from one-another.@*CONCLUSION@#JWYPF has a potential therapeutic effect on AR via adjusting the rebalance of T helper 1 and T helper 2.

[Chemical constituents from Xanthii Fructus].

This study was carried out to investigate the chemical constituents from Xanthii Fructus(the fruits of Xanthium sibiricum). The compounds were separated and purified by silica gel column chromatography, Sephadex LH-20 and ODS chromatography and semi-preparative HPLC. Base on HR-ESI-MS, NMR and other spectral data, their structures were identified. The anti-inflammatory activity of the isolated compounds was evaluated by lipopolysaccharide(LPS)-induced macrophage RAW264.7 as a screening model. A total of twenty-one compounds were isolated from the EtOAc fraction of 95% ethanol extract and identified as uracil(1), thymine(2), uridine(3), indole-3-carbaldehyde(4), indole-3-carboxylic acid(5), 2'-O-methyluridine(6), guanosine(7), 2,4(1H,3H)-quinazolinedione(8), 3-hydroxy-3-(2-hydroxyethyl)indolin-2-one(9), nicotinamide(10), N-acetyl-L-phenylalaninol(11), heliolactam(12), terresoxazine(13), caudatin(14), qingyangshengenin(15), caudatin-3-O-ß-D-oleandropyranosyl-(1→4)-ß-D-cymaropyranosyl-(1→4)-ß-D-cymaropyranoside(16), caudatin-3-O-ß-D-cymaropyranosyl-(1→4)-ß-D-oleandropyranosyl-(1→4)-ß-D-cymaropyranosyl-(1→4)-ß-D-cymaropyranoside(17), caudatin-3-O-α-L-cymaropyranosyl-(1→4)-ß-D-cymaropyranosyl-(1→4)-ß-D-cymaropyranosyl-(1→4)-α-L-cymaropyranosyl-(1→4)-ß-D-oleandropyranosyl-(1→4)-ß-D-cymaropyranoside(18), qinyangshengenin-3-O-ß-D-oleandropyranosyl-(1→4)-ß-D-oleandropyranosyl-(1→4)-ß-D-cymaropyranoside(19), qinyangshengenin-3-O-ß-D-oleandropyranosyl-(1→4)-ß-D-cymaropyranosyl-(1→4)-ß-D-digitoxopyranoside(20), rostratamine-3-O-ß-D-oleandropyranosyl-(1→4)-ß-D-cymaropyranosyl-(1→4)-ß-D-cymaropyranoside(21). Compounds 5-21 are obtained from genus Xanthium for the first time. Compounds 12 and 13 indirectly exhibited anti-inflammatory activity by suppressing LPS-induced NO production in RAW264.7 cells with IC_(50) values of(15.45±0.56) and(20.14±0.78) µmol·L~(-1), respectively.

Bioactive sulfur-containing compounds from Xanthium sibiricum, including a revision of the structure of xanthiazinone.

Seven previously undescribed sulfur-containing compounds, (+)- and (-)-xanthiazinone A, (+)- and (-)-xanthiazinone B, (+)- and (-)-xanthiazinone C and xanthiazinone D, and four known thiazinedione derivatives, together with three thiophene derivatives were isolated from the fruits of Xanthium sibiricum. Racemic xanthiazinones A-C were separated by chiral HPLC columns. Their chemical structures were elucidated based on extensive spectroscopic analyses, ECD calculations, and single crystal X-ray diffractions. The X-ray crystallographic analyses for xanthiazinones A-C represent the first example described for the structure elucidation of the thiazinedione with the five-membered lactone ring attached via an oxygen atom. Accordingly, the previously proposed structure for xanthiazinone was revised. The anti-inflammatory and cytotoxic activities were evaluated for all the isolated compounds. (+)-xanthiazinone B and 2-hydroxy-xanthiazone exhibited potent inhibitory effects against nitric oxide production in lipopolysaccharide-activated RAW 264.7 mouse macrophage cells with IC50 values of 8.75 and 10.90 µM, respectively. All compounds obviously were inactive for three human tumor cell lines (HepG2, MCF-7, and A549) with IC50 values more than 10 µM.

Chemical constituents from Xanthii Fructus / 中国中药杂志

This study was carried out to investigate the chemical constituents from Xanthii Fructus(the fruits of Xanthium sibiricum). The compounds were separated and purified by silica gel column chromatography, Sephadex LH-20 and ODS chromatography and semi-preparative HPLC. Base on HR-ESI-MS, NMR and other spectral data, their structures were identified. The anti-inflammatory activity of the isolated compounds was evaluated by lipopolysaccharide(LPS)-induced macrophage RAW264.7 as a screening model. A total of twenty-one compounds were isolated from the EtOAc fraction of 95% ethanol extract and identified as uracil(1), thymine(2), uridine(3), indole-3-carbaldehyde(4), indole-3-carboxylic acid(5), 2'-O-methyluridine(6), guanosine(7), 2,4(1H,3H)-quinazolinedione(8), 3-hydroxy-3-(2-hydroxyethyl)indolin-2-one(9), nicotinamide(10), N-acetyl-L-phenylalaninol(11), heliolactam(12), terresoxazine(13), caudatin(14), qingyangshengenin(15), caudatin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside(16), caudatin-3-O-β-D-cymaropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside(17), caudatin-3-O-α-L-cymaropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-α-L-cymaropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranoside(18), qinyangshengenin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranoside(19), qinyangshengenin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-digitoxopyranoside(20), rostratamine-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside(21). Compounds 5-21 are obtained from genus Xanthium for the first time. Compounds 12 and 13 indirectly exhibited anti-inflammatory activity by suppressing LPS-induced NO production in RAW264.7 cells with IC_(50) values of(15.45±0.56) and(20.14±0.78) μmol·L~(-1), respectively.

[oil microbial biomass and enzyme activities among different artificial forests in Ziwuling, Northwest China.] / å­åˆå²­äººå·¥æž—åœŸå£¤å¾®ç”Ÿç‰©ç”Ÿç‰©é‡åŠé ¶æ´»æ€§.

Decades of ecological restoration on the Loess Plateau has achieved significant on-site benefits to reduce soil erosion and improve soil quality, with remarkable off-site effects of reducing sediment delivery to Yellow River. However, regional forest community succession is still far from being adequately developed. The Ziwuling forest region and its highly developed forest community, as an advanced eco-zone, can lend practical experience to other regions on the Loess Plateau and help to identify the most suitable tree species for a better regional restoration in the future. With the aim to systematically understand the potential effects of typical local tree species to soil properties, three typical and well-established artificial forests in the Ziwuling region, Robinia pseudoacacia, Pinus tabuliformis and Platycladus orientalis were investigated in this study, with the climax community Quercus wutaishanica as a reference. All the four forest type had comparable stand age (25 years). Soil samples from 0-20 cm layers were collected from those four plantations. The soil microbial biomass (carbon and nitrogen), soil enzyme (invertase, urease and alkaline phosphatase) activities and their correlations were measured and analyzed. The results showed that: 1) soil invertase activity ranged from 16.94 to 64.49 mg·g-1·24 h-1, the soil urease activity from 0.15 to 0.26 mg·g-1·24 h-1, and the alkaline phosphatase activity from 0.65 to 1.23 mg·g-1·24 h-1. The activities of those three enzymes were significantly higher in the P. orientalis soil that in the R. pseudoacacia and P. tabuliformis soils. The geometric average values in the P. orientalis soil were even greater than that in the Q. wutaishanica soil. 2) The soil microbial biomass carbon and nitrogen varied from 247.37 to 529.84 mg·kg-1 and 41.48 to 77.91 mg·kg-1, respectively. Both of them were significantly greater in the P. orientalis soil than that in the R. pseudoacacia and P. tabu-liformis soils. Even though the soil microbial biomass carbon in the P. orientalis soil remained lower than that in the Q. wutaishanica soil, its soil microbial biomass nitrogen was greater than in the Q. wutaishanica soil. 3) The dissolved organic carbon and nitrogen in the P. tabuliformis soil were much greater than that in other species, even greater than their own soil microbial biomass carbon and nitrogen. Such a result indicated that dissolved organic matter might play a more important role in providing plant available nutrients than microbial biomass in the P. tabuliformis soil. 4) The microbial biomass carbon and nitrogen were significantly positively correlated with the total organic carbon and the total nitrogen, particularly for the R. pseudoacacia and P. tabuliformis soils. There were significantly positive relationships between the soil invertase activity, urease activity and alkaline phosphatase activity, and their soil organic carbon, total nitrogen and total phosphorus contents. 5) Based on the results of principal component analysis, we concluded that the artificial forests types had obvious effects on soil microbial carbon and nitrogen, soil organic carbon, total nitrogen, the ratio of carbon to phosphorus, the ratio of nitrogen to phosphorus and urease activity. Overall, our findings suggested that P. orientalis is better than R. pseudoacacia and P. tabuliformis in term of improving soil properties in the south forest zone on the Chinese Loess Plateau.

Network pharmacology exploration reveals endothelial inflammation as a common mechanism for stroke and coronary artery disease treatment of Danhong injection.

Although Danhong injection (DHI) is the most widely prescribed Chinese medicine for both stroke and coronary artery disease (CAD), its underlying common molecular mechanisms remain unclear. An integrated network pharmacology and experimental verification approach was used to decipher common pharmacological mechanisms of DHI on stroke and CAD treatment. A compound-target-disease & function-pathway network was constructed and analyzed, indicating that 37 ingredients derived from DH (Salvia miltiorrhiza Bge., Flos Carthami tinctorii and DHI) modulated 68 common targets shared by stroke and CAD. In-depth network analysis results of the top diseases, functions, pathways and upstream regulators implied that a common underlying mechanism linking DHI's role in stroke and CAD treatment was inflammatory response in the process of atherosclerosis. Experimentally, DHI exerted comprehensive anti-inflammatory effects on LPS, ox-LDL or cholesterol crystal-induced NF-κB, c-jun and p38 activation, as well as IL-1ß, TNF-α, and IL-10 secretion in vascular endothelial cells. Ten of 14 predicted ingredients were verified to have significant anti-inflammatory activities on LPS-induced endothelial inflammation. DHI exerts pharmacological efficacies on both stroke and CAD through multi-ingredient, multi-target, multi-function and multi-pathway mode. Anti-endothelial inflammation therapy serves as a common underlying mechanism. This study provides a new understanding of DHI in clinical application on cardiovascular and cerebrovascular diseases.

Biomimetically inspired asymmetric total synthesis of (+)-19-dehydroxyl arisandilactone A.

Complex natural products are a proven and rich source of disease-modulating drugs and of efficient tools for the study of chemical biology and drug discovery. The architectures of complex natural products are generally considered to represent significant barriers to efficient chemical synthesis. Here we describe a concise and efficient asymmetric synthesis of 19-dehydroxyl arisandilactone A-which belongs to a family of architecturally unique, highly oxygenated nortriterpenoids isolated from the medicinal plant Schisandra arisanensis. This synthesis takes place by means of a homo-Michael reaction, a tandem retro-Michael/Michael reaction, and Cu-catalysed intramolecular cyclopropanation as key steps. The proposed mechanisms for the homo-Michael and tandem retro-Michael/Michael reactions are supported by density functional theory (DFT) calculation. The developed chemistry may find application for the synthesis of its other family members of Schisandraceae nortriterpenoids.

Bidirectional regulation of angiogenesis by phytoestrogens through estrogen receptor-mediated signaling networks.

Sex hormone estrogen is one of the most active intrinsic angiogenesis regulators; its therapeutic use has been limited due to its carcinogenic potential. Plant-derived phytoestrogens are attractive alternatives, but reports on their angiogenic activities often lack in-depth analysis and sometimes are controversial. Herein, we report a data-mining study with the existing literature, using IPA system to classify and characterize phytoestrogens based on their angiogenic properties and pharmacological consequences. We found that pro-angiogenic phytoestrogens functioned predominantly as cardiovascular protectors whereas anti-angiogenic phytoestrogens played a role in cancer prevention and therapy. This bidirectional regulation were shown to be target-selective and, for the most part, estrogen-receptor-dependent. The transactivation properties of ERα and ERß by phytoestrogens were examined in the context of angiogenesis-related gene transcription. ERα and ERß were shown to signal in opposite ways when complexed with the phytoestrogen for bidirectional regulation of angiogenesis. With ERα, phytoestrogen activated or inhibited transcription of some angiogenesis-related genes, resulting in the promotion of angiogenesis, whereas, with ERß, phytoestrogen regulated transcription of angiogenesis-related genes, resulting in inhibition of angiogenesis. Therefore, the selectivity of phytoestrogen to ERα and ERß may be critical in the balance of pro- or anti-angiogenesis process.

Study on balance of process of alcohol precipitation of ganmaoling granules / 中国中药杂志

Ganmaoling granule is the first brand of domestic cold medicine sales, but its preparation method and process control parameters are relatively rough. Therefore it is urgent to upgrade the technologies of large varieties of traditional Chinese medicine (TCM). This paper focused on the balance between the remove of impurity and the retention of linarin during the process of alcohol precipitation of Ganmaoling granules. The effects of four factors on the process were investigated via single factor experiments. The results showed that the precipitating period, the initial ethanol concentration and the final ethanol concentration had a great effect on retention of linarin while the initial density of the extract has not. Similarly, the initial ethanol concentration, the final ethanol concentration and the initial extract density have a great effect on the yield of dry extract while the time of alcohol precipitation has not. The parameters of alcohol precipitation of Ganmaoling granules were optimized as 16 h of precipitating period, 95% ethanol as the initial reagent, 70% of the final ethanol concentration, and 1.10 of the initial extract density.

[Ecological stoichiometry characteristics of leaf-litter-soil in different plantations on the Loess Plateau, China]. / 黄土高原不同人工林叶片-凋落叶-土壤生态化学计量特征.

In order to research into the influence of Grain to Green Project in Ziwuling forest region, this paper took three typical plantations which were Robinia pseudoacacia plantation, Pinus tabuliformis plantation, and Platycladus orientalis plantation in the Ziwuling forest region of Shaanxi Province as research objects and analyzed the carbon, nitrogen and phosphorus contents of leaf, litter and soil among the three plantations. The results showed that the contents of C, N and P in the three plantations were in order of leaf > litter > soil, the contents of N and P in leaf of R. pseu-doacacia plantation were significantly higher than that of P. tabuliformis plantation and P. orientalis. Leaf N:P was 12.21, 5.36 and 6.09 in R. pseudoacacia plantation, P. tabuliformis plantation and P. orientalis plantation, respectively. It was indicated that the three species were all subject to N deficiency. C:N and C:P showed the trend of litter > leaf > soil, and N:P demonstrated the trend of leaf > litter > soil. There were highly significant positive relationships in C:N between leaf and litter in P. tabuliformis plantation. N and P in the leaf development process of R. pseu-doacacia plantation were proportionally absorbed, and proportionally remained in the litter after N and P resorption. R. pseudoacacia was the better plantation species than P. tabuliformis and P. orientalis in the south fo-rest zone on the Loess Plateau.

Bidirectional regulation of angiogenesis by phytoestrogens through estrogen receptor-mediated signaling networks / 中国天然药物

Sex hormone estrogen is one of the most active intrinsic angiogenesis regulators; its therapeutic use has been limited due to its carcinogenic potential. Plant-derived phytoestrogens are attractive alternatives, but reports on their angiogenic activities often lack in-depth analysis and sometimes are controversial. Herein, we report a data-mining study with the existing literature, using IPA system to classify and characterize phytoestrogens based on their angiogenic properties and pharmacological consequences. We found that pro-angiogenic phytoestrogens functioned predominantly as cardiovascular protectors whereas anti-angiogenic phytoestrogens played a role in cancer prevention and therapy. This bidirectional regulation were shown to be target-selective and, for the most part, estrogen-receptor-dependent. The transactivation properties of ERα and ERβ by phytoestrogens were examined in the context of angiogenesis-related gene transcription. ERα and ERβ were shown to signal in opposite ways when complexed with the phytoestrogen for bidirectional regulation of angiogenesis. With ERα, phytoestrogen activated or inhibited transcription of some angiogenesis-related genes, resulting in the promotion of angiogenesis, whereas, with ERβ, phytoestrogen regulated transcription of angiogenesis-related genes, resulting in inhibition of angiogenesis. Therefore, the selectivity of phytoestrogen to ERα and ERβ may be critical in the balance of pro- or anti-angiogenesis process.