Preparation of a ε-caprolactonic diterpenoid derivate by unexpected oxidative cleavage/lactonization of 2-oxoaustroeupatol

From aerial parts of Austroeupatorium inulifolium was isolated the ent-nor-furano triol labdane austroeupatol 1.The compound 1 was treated with IBX showing an unexpected selectivity at the potentially oxidizable sites of the sub-strate yielding the 2-oxoaustroeupatol(2)and 2,19-dioxoaustroeupatol(3).The treatment of 2 with sodium periodate yields a heterocyclic derivative(ε-caprolactone derivate 4)formed by oxidative cleavage and unexpected intramo-lecular attack of the hydroxymethylene(C-19)oxygen to the ketonic carbon(C-2).A plausible mechanistic pathway for the obtention of compound 4 is proposed.

A stereoselective formal synthesis of (±)-Prelog-Djerassi lactonic acid

During the course of our program in the synthesis of natural products by retroDiels-Alder reaction using a rigid molecule tricyclo-[5.2.1.0]-deca-4,8-dien-3-one（1） as the starting material, it was observed that aldol condensation of compound （2）

Britanin–a beacon of hope against gastrointestinal tumors?

Britanin is a bioactive sesquiterpene lactone known for its potent anti-inflammatory and anti-oxidant properties.It also exhibits significant anti-tumor activity,suppressing tumor growth in vitro and in vivo.The current body of research on Britanin includes thirty papers predominantly related to neoplasms,the majority of which are gastrointestinal tumors that have not been summarized before.To drive academic debate,the present paper reviews the available research on Britanin in gastrointestinal tumors.It also outlines novel research directions using data not directly concerned with the digestive system,but which could be adopted in future gastrointestinal research.Britanin was found to counteract liver,colorectal,pancreatic,and gastric tumors,by regulating proliferation,apoptosis,autophagy,immune response,migration,and angiogenesis.As confirmed in pancreatic,gastric,and liver cancer,its most commonly noted molecular effects include nuclear factor kappa B and B-cell lymphoma 2 downregulation,as well as Bcl-2-associated X protein upregulation.Moreover,it has been found to induce the Akt kinase and Forkhead box O1 axis,activate the AMP-activated protein kinase pathway,elevate interleukin-2 and peroxisome proliferator-activated receptor-γlevels,reduce interleukin-10,as well as downregulate matrix metalloproteinase-9,Twist family bHLH transcription factor 1,and cyclooxygenase-2.It also inhibits Myc–HIF1αinteraction and programmed death ligand 1 transcription by interrupting the Ras/RAF/MEK/ERK pathway and mTOR/P70S6K/4EBP1 signaling.Future research should aim to unravel the link between Britanin and acetylcholinesterase,mast cells,osteolysis,and ischemia,as compelling data have been provided by studies outside the gastrointestinal context.Since the cytotoxicity of Britanin on noncancerous cells is significantly lower than that on tumor cells,while still being effective against the latter,further in-depth studies with the use of animal models are merited.The compound exhibits pleiotropic biological activity and offers considerable promise as an anti-cancer agent,which may address the current paucity of treatment options and high mortality rate among patients with gastrointestinal tumors.

Study on Induction of Microcystis aeruginosa Cell Apoptosis by Signal Molecule N-acetyl-homoserine Lactones(AHLs)

[Objective]The relationship between signal molecule N-acety-homoserine lactones（AHLs） and Microcystis aeruginosa cell apoptosis was studied.[Method]With M.aeruginosa as the test materials treated by 5 μmol/L N-acety-homoserine lactones（AHLs）,the morphology of cell apoptosis was observed through staining with DAPI.[Result]Microcystis aeruginosa cell apoptosis was induced by signal molecule N-acetyhomoserine lactones（AHLs） with the concentration of 1 μmol/L to inhibit the growth and proliferation of Microcystis aeruginosa.[Conclusion] The results provided the important scientific basis and new management ideas for the treatment of water bloom of Microcystis aeruginosa.

High Performance Liquid Chromatography-Electrospray Ionization-Mass Spectrometric Analysis of Bilobalide and Ginkgolides in Ginkgo biloba L. Leaves

The ginkgo terpenoids including bilobalide and ginkgolides are the main pharmaceutical components in the leaves or extracts of Ginkgo biloba L. In this paper, the analysis of bilobalide and ginkgolides in leaves of Ginkgo biloba L. by high performance liquid chromatography (HPLC)-electrospray ionization (ESI)-mass spectrometry (MS) was carried out. The separation was performed on Inertsil ODS3 column with methanol-water (36:64) as mobile phase, with 1 mL·min -1 of flow rate at 35℃. Then the mass spectrum analysis was conducted by ZMD micromass electrospray ionization (ESI)-mass spectrometer (MS). The HPLC total ion chromatogram and selected ion chromatogram (with 325, 407, 423, 439 of m/z) of the sample and ESI-/MS mass spectra of the peaks in the chromatograms were obtained. So bilobalide, ginkgolide A, B, C and J in Ginkgo biloba L. leaves were identified. The method is easy and rapid, with a good accuracy.

16-Hydroxytriptolide" An Active Compound from Tripterygium wilfordii

From the dried roots and leaves of Tripterygium wilfordii^(1.2),a new diter- penoid triepoxide,16-hydroxytriptolide was isolated,and its structure and stereochemistry elucidated as 16-(S)-hydroxy-triptolide on the basis of spectral data(IR, MS, UV,~1HNMR,^(13)CNMR,2d-NMR,Selective Long-range DEPT)and x-ray crystallographic analysis.This compound showed definite antiinflammatory action,strong immunosuppressive and antifertile activities.In addition,a known compound,triptolide was also isolated and all the spectral signals of^1 HNMR and ^(13)CNMR were assigned.

生物降解织物与农业

论述现今在业上使用最多的塑膜对农业环境的影响;开发生物降解织物的现实意义;简介几种生物降解纤维(甲壳素纤维、Lyocell纤维,Lacton纤维等)及织物的制造方法;并叙述了生物降解织物在农业上的主要功能及应用。

Three Novel Eremophilanolides from Ligularia virgaurea spp.oligocephala

From the alcoholic extract of the whole plant of Ligularia virgaurea spp. oligocephala,three novel eremophilane sesquiterpene lactones, 6α, 10α-dihydroxy-1-oxoeremophila- 7(11),8(9)-dien-8, 12-olide, 6β, 10α-dihydroxy-1-oxoeremophila-7 (11), 8 (9)-dien-8, 12-olide and10α-diydroxy-1-oxoeremophila-7(11), 8 (9)-dien-8, 12 olide were isolated. Their structure s wereelucidated by various, spectroscopic methods including intensive 2D NMR techniques (COSY,HMQC, HMBC and ~1H-~1H NOESY) and HR-MS.

Sesquiterpene Lactones from Elephantopus scaber

A new germacranolide sesquiterpene lactone, isoscabertopin, was isolated from Elephantopus scaber together with the known scabertopin. Their structures were determined by spectroscopic methods.

A new cassane diterpenoid lactone from the seed of Caesalpinia minax

A new cassane diterpenoid lactone was isolated from the seed of Caesalpinia minax. On the basis of spectral evidences, its structure was established as 12α-methoxyl, 5α, 14β-dihydroxy-1α, 6α, 7β-triacetoxycass-13（15）-en-16, 12-olide.

A New Sesquiterpene Lactone from Ainsliaea bonatii

A new sesquiterpene lactone, Ainsliaolide A, was isolated from Ainsliaea bonatii. Thestructure was determined on the basis of spectral data.

A New Sesquiterpene from the Roots of Lindera strychnifolia

A new sesquiterpene lactone, strychnilactone (1), together with five known sesquiterpenoids, linderane (2), lindenenol (3), linderalactone (4), hydroxylindestenolide (5), pseudoneolinderane (6) have been isolated from the extracts of Supercritical Fluid Extraction of Lindera strychnifolia. The structure of the new compound was elucidated by means of spectroscopic analysis. And the relative configuration of 1 was assigned on the basis of NOE analysis.

Eupatoranolide, a New Sesquiterpene Lactone from Eupatorium adenophorum

A new sesquiterpene lactone eupatoranolide was isolated from the flowers of Eupatorium adenophorum, its structure was elucidated as 2 beta-acetoxy-(7 alpha, 9 beta H)-3.6(11)-cadinadien-12(7)-olide by spectral analysis.

Two New Sequiterpenoids from Helicteres angustifolia

A new sesquiterpenoid lactone, 3,6,9-trimethyl-pyrano[2,3,4-de]chromen-2-one (1) and a novel sesquiterpenoid quinone, 6-[2-(5-acetyl-2,7-dimethyl-8-oxo-bicyclo[4.2.0]octa-1,3,5- trien-7-yl)-2-oxo-ethyl]-3,9-dimethylnaphtho[1,8-bc]pyran-7,8-dione (2) together with a known perezone (3) were isolated from the roots of Helicteres angustifolia. The structures were elucidated as mainly on the basis of 1D and 2D NMR spectroscopic data.

Genome-wide identification of WRKY gene family and expression analysis under abiotic stresses in Andrographis paniculata

Andrographis paniculata(A.paniculata)is a Chinese herbal medicine that clears away heat,reduces inflammation,protects the liver,and promotes choleretics.The WRKYs of A.paniculata are still not well characterized,although many WRKYs have been identified in various plant species.In the present study,59 A.paniculata WRKY(ApWRKY)genes were identified and renamed on the basis of their respective chromosome distribution.These ApWRKYs were divided into three groups via phylogenetic analysis according to their WRKY domains and combined with WRKY of Arabidopsis.The 59 identified ApWRKY transcription factors were nonuniformity distributed on 23 chromosomes of A.paniculata.From the structural analysis of the conserved motifs,different ApWRKYs structures showed different biological functions,and the ApWRKY transcription factor had certain species-specificity in the evolutionary process.The expression patterns of the 41 ApWRKYs were examined through quantitative real-time PCR(qRT-PCR)in various tissues and under abiotic stresses(salt).The results showed that most of the ApWRKY had different reactions to salt treatment.In addition,the content of the four main secondary metabolites in A.paniculata leaves was determined under salt stress.The results show that under a low concentration of salt treatment,the synthesis of andrographolide can be improved.

A new ent-labdane diterpenoid lactone from Andrographis paniculata

A new ent-labdane diterpenoid lactone was isolated from Andrographis paniculata.Its structure was identified on the basis of spectral data including 2D NMR.

Fenugreek lactone attenuates palmitate-induced apoptosis and dysfunction in pancreatic β-cells

AIM: To investigate the effect of fenugreek lactone(FL) on palmitate(PA)-induced apoptosis and dysfunction in insulin secretion in pancreatic NIT-1 β-cells. METHODS: Cells were cultured in the presence or absence of FL and PA(0.25 mmol/L) for 48 h. Then, lipid droplets in NIT-1 cells were observed by oil red O staining, and the intracellular triglyceride content was measured by colorimetric assay. The insulin content in the supernatant was determined using an insulin radioimmunoassay. Oxidative stress-associated parameters, including total superoxide dismutase, glutathione peroxidase and catalase activity and malondialdehyde levels in the suspensions were also examined. The expression of upstream regulators of oxidative stress, such as protein kinase C-α(PKC-α), phospho-PKC-α and P47 phox, were determined by Western blot analysis and real-time PCR. In addition, apoptosis was evaluated in NIT-1 cells by flow cytometry assays and caspase-3 viability assays.RESULTS: Our results indicated that compared to the control group, PA induced an increase in lipid accumulation and apoptosis and a decrease in insulin secretion in NIT-1 cells. Oxidative stress in NIT-1 cells was activated after 48 h of exposure to PA. However, FL reversed the above changes. These effects were accompanied by the inhibition of PKC-α, phosphoPKC-α and P47 phox expression and the activation of caspase-3. CONCLUSION: FL attenuates PA-induced apoptosis and insulin secretion dysfunction in NIT-1 pancreatic β-cells. The mechanism for this action may be associated with improvements in levels of oxidative stress.

Synaptic and blood-brain barrier structural changes in a rat epilepsy model induced by coriaria lacton Replication experiment with animals

BACKGROUND： Structural and functional synaptic changes, as well as blood-brain barrier （BBB） changes, affect the micro-environment of nervous tissue and excitation, both of which play an important role in epilepsy. OBJECTIVE： To observe synaptic and BBB ultrastructural changes in the motor cortex of a rat epilepsy model induced by coriaria lacton, and to investigate the synaptic and BBB effects on the mechanism of epilepsy. DESIGN： A randomized controlled animal experiment. SETTING： Department of Histology and Embryology, Luzhou Medical College; and Electron Microscopy Laboratory, Luzhou Medical College. MATERIALS： Twenty healthy male Sprague Dawley rats, aged 8 weeks, were chosen for this study. The rats weighed （280 ± 50） g and were supplied by the Experimental Animal Center of Luzhou Medical College. Experimentation was performed in accordance with the ethical guidelines for the use and care of animals. The animals were randomly divided into a control group and an epilepsy group, with 10 rats in each group. METHODS： This study was performed at the Department of Histology and Embryology, and Electron Microscopy Laboratory, Luzhou Medical College between February and December 2006. According to the protocol, the epilepsy group was injected with 10 μ L/100 g coriaria lacton into the lateral ventricles to establish an epileptic model. The control group rats were not administered anything. Eight days after the model was established, all rats were anesthetized with ether. The motor cortex was removed and sectioned into ultrathin sections. Synaptic and BBB ultrastructural changes were observed by electron microscopy. MAIN OUTCOME MEASURES： （1）Structural changes of three different parts of the synapses, synaptic cleft width, postsynaptic density thickness, proportion of perforation synapses, curvature of synaptic interface, and length of active zones. （2）Capillary and BBB changes （endothelium, basement membrane, pericyte, and the astrocyte endfeet）. RESULTS： （1）Curvature of synaptic interface, length of active zones, thickness of postsynaptic density, and percentage of perforation synapses increased significantly. （2）There was significant edema in the endothelium, basement membrane, and the pericyte of the epilepsy group; the electron density of the basement membrane was reduced. CONCLUSION： （1） The coriaria lacton treatment altered synaptic ultrastructure, as well as BBB characteristics, in the epileptic rat model, and also improved synaptic transmission efficiency, as well as BBB permeability; （2）Synaptic and BBB ultrastructural changes might play an important role in the mechanism of epilepsy.

A new nor-sesquiterpene lactone from Ainsliaea fulvioides

A new nor-sesquiterpene lactone ainsliatone A （1） was isolated from the aerial parts of Ainsliaeafulvioides. Its structure was established by the basis of spectroscopic methods and single-crystal X-ray diffraction analysis.