Exploring a novel class tryptophan hydroxylase 1 inhibitor derived from Sambucus williamsii Hance for the osteoporosis treatment

Objective:Gut-derived serotonin strongly inhibits bone formation by inhibiting osteoblast proliferation.Our previous study demonstrated that the lignan-rich fraction prepared from Sambucus willimasii Hance,a folk herbal medicine used to treat bone fractures and joint diseases in China,exerted bone-protective effects,and its actions were modulated by suppressing the synthesis of gut-derived serotonin via the inhibition of intestinal tryptophan hydroxylase 1(TPH-1).However,there is no direct evidence for the action of lignans on TPH-1.This study aimed to verify the direct action of lignans on the TPH-1 and its influence on serotonin synthesis and bone properties.Methods:Molecular docking and surface plasmon resonance were performed to determine the affinities of lignans to TPH-1.The cell viability and the protein activity and expression of TPH-1 were measured in RBL2H3 cells.The serum serotonin level and bone mineral density upon lignan treatment in ovariectomized mice were determined.Result:The lignans showed high binding scores and binding affinities to TPH-1,inhibited the activity and protein expression of TPH-1,suppressed the serum serotonin levels in ovariectomized mice as well as promoted bone mineral density.Conclusion:This is the first study to report that lignans are novel TPH-1 inhibitors and that these lignans could be potential agents for the management of serotonin-related diseases,including osteoporosis.

Antioxidant,Hypoglycemic and Hypolipidemic Activities of Sambucus williamsii Seed Oil

[Objectives] To explore the antioxidant activity of Sambucus williamsii seed oil. [Methods]DPPH scavenging method and Prussian blue method( total reducing power) were used. S. williamsii seed oil has antioxidant activity. In the DPPH scavenging free radical experiment,S. williamsii oil showed the ability to scavenge free radicals,and its scavenging ability had linear relationship with oil concentration( R =0. 999 6). Besides,the IC_(50) value of S. williamsii seed oil scavenging DPPH free radicals was 61. 30 ± 0. 88 mg/mL. In the total reducing power measurement experiment,the S. williamsii seed oil has a reducing ability,and its reducing ability is proportional to the oil concentration,and has the concentration dependence. Through studying the inhibitory effect of S. williamsii seed oil on α-glucosidase,the hypoglycemic activity of S. williamsii seed oil was determined. The ability of samples to inhibit α-glucosidase was judged through measuring the absorbance at 400 nm of the reaction system. [Results]In the concentration range of 1. 56-25. 00 mg/mL,the S. williamsii seed oil can effectively inhibit α-glucosidase,and the inhibition rate was 62. 66%-85. 22%. The animal in vivo experiment was used to determine the hypolipidemic activity of the S. williamsii seed oil. First,a high fat modelwas established,S. williamsii seed oil was given through intragastric administration. Then,total cholesterol( TC),triglyceride( TG),high-density lipoprotein cholesterol( HDL-C),and low density lipoprotein cholesterol( LDL-C) were measured. Through comparison of high,medium and low dose groups of S. williamsii seed oil with the high fat modelcontrol group,it was found that the TC,TG,LDL-C levels were significantly decreased( P < 0. 01) and the HDL-C levels were significantly increased( P < 0. 05),indicating that S. williamsii seed oil can effectively reduce the levels of TC,TG,LDL-C in the serum of hyperlipidemic mice,and effectively inhibit the decrease of HDL-C level,thus S. williamsii seed oil can reduce blood lipids in mice,namely,has hypolipidemic effects. In addition,the greater the dose of S. williamsii seed oil,the more obvious the effect of blood lipid levels in mice,indicating that the hypolipidemic effect of S. williamsii seed oil was dose dependent. [Conclusions] S. williamsii seed oil has reducing ability,and there is a significant dose-effect relationship in the concentration range of 2-10 mg/mL. As natural plant oil,S. williamsii seed oil has the advantages of good stability,small toxic and side effects,and strong effect,and has high value of developing new antioxidants.

The healing effects of herbal preparations from Sambucus ebulus and Urtica dioica in full-thickness wound models

Objective:To investigate the healing effects of two herbal preparations.Methods:For this purpose,106 wistar rats were divided into 9 groups including a control,eucerine,phenytoin,Urtica dioica(U.dioica)(2%),U.dioica(5%),Sambucus ebulus(S.ebulus)(2%),S.ebulus(5%),combination(2%),and combination(5%)groups.The control group remained untreated,the eucerin and phenytoin groups were considered as the negative and positive controls respectively,and the remaining groups received different concentrations of the ointments.Full thickness wounds were made.The healing process of the wounds was investigated on day 7,14 and 21 of the experiment.Several factors including the number of fibroblasts,new vessel formation(angiogenesis),thickness of the granulomatous tissues(GT),and the overlying epithelium were analyzed.Results:Among the studied groups,all of the treatment groups were significantly different from the control,eucerin,and phenytoin groups in a positive manner with regard to all studied factors(P 0.05).However,the best results were observed with the S.ebulus(2%) and the combination 2% groups(P 0.05).Conclusions:Topical ointments prepared from the extracts of U.dioica and S.ebulus and their combination possess strong wound healing properties.It is postulated that a synergistic effect may exist between the two extracts since the combination 2% showed better results than the sole extracts.

Biological Characteristics of Root Rot Pathogen on Sambucus chinensis

Effects of different media,pH values,temperatures,carbon and nitrogen sources on mycelial growth and sporulation of root rot pathogen on Sambucus chinensis was determined in the paper.The results showed that root rot pathogen on S.chinensis was identified as Fusariumsp.The mycelial growth and sporulation of Fusariumsp.in PSA medium was the best;the optimal temperature for mycelial growth and sporulation was from 25℃ to 30℃ and the optimal temperature was 28℃;the suitable pH values for mycelial growth and sporulation was from 5 to 7,and the optimum pH value was 6;the absence or presence of carbon sources had significant effect on growth of Fusariumsp.;sucrose was the best carbon source utilized in mycelial growth,while lactose was the worst; KNO3 was the best nitrogen source utilized in mycelial growth,while（NH4） 2 SO4 was the worst one.

接骨木叶粗多糖提取工艺研究

以水为溶剂提取接骨木(Sambucus williamsii)叶粗多糖,利用苯酚-硫酸比色法测定粗多糖的含量,设计单因素试验考察提取温度、提取时间、料水质量比、乙醇浓度、提取次数以及提取液pH对多糖提取率的影响,并应用正交试验优化提取工艺。结果表明,优化的提取工艺为提取温度75℃、提取时间3 h、料水质量比1∶30、乙醇体积分数80%,此条件下接骨木叶粗多糖的提取率为15.52%。

接骨木和贵州金丝桃生理生态特性与喀斯特环境适生性比较

依据贵州省石漠化现状和植物对喀斯特环境条件的影响,筛选喀斯特生态修复适生植物,通过Li-6400便携式光合测定系统分别测定了接骨木(Sambucus williamsii Hance)、贵州金丝桃(Hypericum kouytcheouense Levl.)2种药用植物的叶片光合作用日变化特征,并结合植物叶片的叶绿素含量、碳酸酐酶(Carbonic anhydrase,CA)活性、稳定碳同位素δ13C变化范围比较了2种植物在喀斯特生境下的适生能力。结果表明,接骨木对于喀斯特石漠化环境有着更好的适生性。

A mimetic peptide of α2,6-sialyllactose promotes neuritogenesis

Oxidative stress contributes to the pathogenesis of neurodegenerative diseases.With the aim to find reagents that reduce oxidative stress,a phage display library was screened for peptides mimicking a2,6-sialyllactose(6'-SL),which is known to beneficially influence neural functions.Using Sambucus nigra lectin,which specifically binds to 6'-SL,we screened a phage display library and found a peptide comprising identical sequences of 12 amino acids.Mimetic peptide,reverse peptide and scrambled peptide were tested for inhibition of 6'-SL binding to the lectin.Indeed,lectin binding to 6'-SL was inhibited by the most frequently identified mimetic peptide,but not by the reverse or scrambled peptides,showing that this peptide mimics 6'-SL.Functionally,mimetic peptide,but not the reverse or scrambled peptides,increased viability and expression of neural cell adhesion molecule L1 in SK-N-SH human neuroblastoma cells,and promoted survival and neurite outgrowth of cultured mouse cerebellar granule neurons challenged by H_20_2-induced oxidative stress.The combined results indicate that the 6'-SL mimetic peptide promotes neuronal survival and neuritogenesis,thus raising hopes for the treatment of neurodegenerative diseases.This study was approved by the Medical Ethics Committee of Shantou University Medical College,China(approval No.SUMC 2014-004)on February 20,2014.

Plasma Accumulations of Vitamin B6 from an Oral Dose in a New Reversible Model for Mouse Gut Injury and Regeneration

Chemically based rodent models are used to assess the positive effects promoted by foods and gut microbiota on gut health. Lectins with enzymatic activity, such as type 2 ribosome-inactivating proteins, might also prove useful for exploring these issues. Sub-lethal doses of the lectin nigrin from Sambucus nigra L. to mice promoted reversible derangement of gut epithelium by induction of apoptosis of transit amplifying cells of the small intestine crypts in a time-dependent course. The present work seeks to study vitamin B6 accumulation in plasma from an oral bolus in a mouse nigrin model. 24 h after sub-lethal nigrin b treatment, there was clear body weight reduction associated to a notable increase in Evan’s blue stain accumulation in excised small intestine, an increase in myeloperoxidase activity, and a near 50% reduction in plasma accumulation of vitamin B6. Histological analysis of small intestine sections of nigrin b-treated animals also revealed significant derangement of intestinal crypts. Seventy two hours after nigrin b treatment, stain uptake decreased and vitamin B6 accumulation was almost restored despite villi derangement. Large intestine crypts were scarcely or not at all affected. Eight days after nigrin b treatment, vitamin B6 uptake and intestinal crypt structure had fully recovered. The nigrin b mice model supports the view that, under these conditions, the carrier-mediated vitamin B6 uptake component of the small intestine crypts is probably the most active when the vitamin is administered orally as a bolus. The findings provide insights into the suitability of the present mice model for nutritional or drug absorption studies in conditions of partially altered or injured intestinal mucosa.

Wildfire associated with a deciduous broadleaved forest from the Neogene Baoshan Basin at the southeastern margin of the Tibetan Plateau

Wildfire bears a close relationship with vegetation as its fuel source.The southeastern margin of the Tibetan Plateau witnesses frequent wildfires among various types of vegetation,whereas such wide in-teractions between wildfire and vegetation remain poorly studied from geological times.In this study,we reported a local fire using sedimentary macroscopic charcoals from the latest Miocene to early Pliocene of the Baoshan Basin in this region,and then inferred the local vegetation at the time of the fire event based chiefly on the coexistent fruit and seed fossil assemblage.Our taxonomic results show that the charcoal assemblage is probably dominated by broadleaved plants and the fruit and seed fossil assemblage is apparently dominated by Salix(Salicaceae)followed by Sambucus(Adoxaceae),suggesting a deciduous broadleaved forest in which the fire likely occurred.Under a seasonally dry climate associated with the Asian monsoon,this type of vegetation might be prone to natural fire,because in the wet rainy season the plants grew well to accumulate biofuel and in the dry season abundant ground litter resulting from leaf decay would be desiccated to become highly flammable.Due to the fire-tolerant habit of Salix as the dominant plant,the forest might be in return adapted to the fire event or even more fires that potentially followed.All these may suggest a close relationship between the fire event and the reconstructed vegetation.Our finding documents a new type of wildfire—vegetation interaction,namely the interaction between wildfire and deciduous broadleaved forest,from the geological past at the southeastern margin of the Tibetan Plateau.It therefore sheds new light on the wildfire history coupling vegetation change in the region.

接骨木培育及应用研究进展

接骨木(Sambucus williamsii Hance.)为忍冬科接骨木属落叶灌木或小乔木,分布广泛,是药食兼有的经济作物,同时也是珍稀的野生木本油料植物,具有较高的营养价值和药理活性。综述了接骨木的繁育技术、化学成分和药理活性,并由此提出展望,希望为接骨木以后的研究奠定坚实的理论基础。

In Vitro Antifungal Activity of Some Traditional Persian Medicinal Plants on Pathogenic Fungi

Objective： To investigate the antifungal activities of the extracts and sub-fractions of Phlomis olivieri, Verbascum speciosum, Sambucus ebulus and Erigeron hyrcanicus, four Persian medicinal plants used in Iranian folk medicine. Methods： Evaluation of the antifungal activity was performed on the clinical isolates of pathogenic fungi including Aspergillus fumigatus, A. flavus, Trichophyton mentagrophytes, T. rubrum, 7. verrucosum, Microsporum canis, M. gypseum and Epidermophyton floccosum, and the yeast Candida albicans. The susceptibility tests were done by agar well diffusion method. The minimum inhibitory concentration （MIC） and minimum fungicidal concentration （MFC） of active extracts and sub-fractions were measured using method of National Committee for Clinical Laboratory Standards （NCCLS）. Results： Only P. olivieri sub-fractions were found to have fungicidal activity among the other investigated plants. The MIC and MFC was found to be high in petroleum ether, chloroform and ethyl acetate fractions （100 and 200 mg/mL） against the studied pathogenic fungi and the yeast Candida albicans. P. olivieri sub-fractions significantly inhibited the growth of all pathogenic fungi and the yeast studied. Conclusion： If the antifungal activity of P. olivieri is confirmed by in vivo studies and if the responsible compound （s） is isolated and identified, it could be a good remedy for mycotic infections.