A New Sesquiterpene from Celastrus Angulatus

One new sesquiterpene polyol eater named angulatin C was isolated from the root bark of Celastrus angulatus along with a known compound, angulatin B. Their structures were elucidated on the basis of spectral analysis.

A Novel Sesquiterpene Polyol Ester from Celastrus Angulatus and its Antitumor Activities

A new sesquiterpene polyol ester was isolated from the leaves of Celastrus angulatus. Its structure was determined as 1 (beta), 2 (beta), 9 (a) -triacetoxy-8 (a) -((a) -hydroxyl-isobutyryloxy)-15-benzoyloxy-4 (a) -hydroxy-dihydroagarofuran by means of NMR, MS and IR spectral analysis. Preliminary biological study on antitumor activity revealed that this compound showed strong nonselective cytotoxicity against four of the NCI panel cell lines.

A NEW ALKALOID FROM CELASTRUS ANGULATUS

A new β-dihydroagarofuran alkaloid Ⅰ was isolated from Celastrus angulatus.The structure was established on the basis of 1D and 2D NMR analysis,and x-ray diffraction.

AN IHSECTICIDAL SESQUITERPENE FROM CELASTRUS ANGULATUS

An insecticidal sesquiterpene polyol ester,angulatin A,was isolated from the root bark of Celastrus angulatus.Its structure was established as 1α,2α-diacetoxy-8β,15-diisobutyryloxy-9α- benzoyloxy-4β,6β-dihydroxydihyclro-β-agarofuran by spectroscopic methods.

INVESTIGATION OF CHEMICAL CONSTITUENT FROM CELASTRUS ANGULATUS

Three new β-dihydroagarofuran sesquiterpene polyol esters,one alkaloid and two non-alkaloids,were isolated from the MeOH extract of seed oil of Celastrus angulatus. Their structures were elucidated on the basis of UV,IR,mass,NOE difference,~1H-NMR,^(13)C- NMR and ~1H-^(13)C long-range correlation spectroscopy.

Erratum to "Celastrus paniculatus oil ameliorates synaptic plasticity in a rat model of attention deficit hyperactivity disorder"

In the article“Celastrus paniculatus oil ameliorates synaptic plasticity in a rat model of attention deficit hyperactivity disorder”published on pages 105-114,Issue 3,Volume 11 of Asian Pacific Journal of Tropical Biomedicine,Figure 5 was incorrectly published.

外来入侵杂草刺果瓜(Sicyos angulatus L.)严重危害玉米

刺果瓜（Sic yos angulatus L.）为葫芦科野胡瓜属一年生攀援草本植物,生长扩展速度快,种子量大、繁殖力极强.该杂草原产于美国,我国仅在台湾和大连地区发生.2013年本研究调查发现,刺果瓜于2002年在宣化区屈家庄首次发生,目前已导致张家口地区约400 hm2玉米受害,造成减产50％～80％.刺果瓜的生长、入侵、传播途径和防控技术等尚不清楚,急需进行深入研究.

大连地区外来植物——刺果瓜(Sicyos angulatus L.)对大连生态的影响及防治对策

刺果瓜原产美国,因其具有攀援生长、迅速成景的绿化效果,曾经被广泛栽种用作藩篱植物,但它强烈的侵占能力又使人感到恐惧,为此,许多国家已将它认作有害杂草,以限制它的蔓延.本文报道刺果瓜对大连生态的影响,提出防治对策.

Celastrus paniculatus oil ameliorates synaptic plasticity in a rat model of attention deficit hyperactivity disorder

Objective:To explore the effect and mechanism of action of Celastrus paniculatus oil on the treatment of perinatal rats with attention deficit hyperactivity disorder.Methods:In the perinatal stage,the rats were either isolated or administered with lead acetate to establish an animal model of attention deficit hyperactivity disorder.Atomoxetine served as the reference standard.Animals’behaviours were assessed through Y-maze,novel object preference,fear conditioning and residentintruder aggression tests.Oxidative stress parameters,bioamine concentration(dopamine,noradrenaline and 5-hydroxytryptamine),nerve growth factor,interleukin-6,nuclear factor-κB,and tumour necrosis factor(TNF)-αwere estimated.Synaptophysin immunohistochemical assay was performed.Results:Celastrus paniculatus oil significantly improved behavioural parameters in Y maze,novel object preference,discrimination index,fear conditioning and resident intruder aggressive tests.The treatment groups showed a decrease in malondialdehyde level.Changes in the levels of dopamine,noradrenaline,and serotonin were restored by Celastrus paniculatus oil.Celastrus paniculatus oil increased nerve growth factor and decreased interleukin-6,nuclear factor-κB,and TNF-α.Synaptophysin immunoreactivity was also improved by Celastrus paniculatus oil with alleviated reactive gliosis,degeneration,and vascular proliferation.Conclusions:This research shows the therapeutic potential of Celastrus paniculatus oil for the treatment of attention deficit hyperactivity disorder.

The petroleum ether fraction of Celastrus paniculatus Willd. seeds demonstrates antiarthritic effect in adjuvant-induced arthritis in rats

Objective:Celastrus paniculatus(CP)Willd.is a plant indigenous to India with medicinal properties.It is used in the ayurvedic treatment of inflammatory ailments such as rheumatoid arthritis.The present study was designed to investigate the therapeutic efficacy of the petroleum ether fraction(PCP)obtained from CP seeds on adjuvant-induced arthritis in rats.Methods:Arthritis was induced in SpragueeDawley rats by immunization with Freund’s complete adjuvant(FCA).Arthritis severity was evaluated by arthritis score,paw volume,tibiotarsal joint thickness,body weight,dorsal flexion pain,motility test,stair climbing ability and index of thymus and spleen.Moreover,histopathology of knee joints supported by haematological analysis was used to assess the anti-arthritic action of PCP.The levels of superoxide dismutase(SOD),glutathione(GSH),catalase(CAT),nitric oxide(NO)and malondialdehyde(MDA)in liver were also assessed.Serum samples were collected for estimation of aspartate transaminase(AST),alanine transaminase(ALT)and alkaline phosphatase(ALP).In addition,cytokines such as tumour necrosis factor-alpha(TNF-a)and interleukin-6(IL-6)were estimated in plasma.Results:PCP significantly alleviated arthritic progression with regards to paw swelling,arthritic score,immune organ indices,hyperalgesic effect and body weight.This phenomenon was correlated with significant suppression of overproduction of inflammatory cytokines(TNFa and IL-6),oxidant stress markers(MDA and NO)and cellular enzyme(AST,ALT and ALP)levels versus arthritic rats without treatment.Moreover,PCP restored the decreased levels of SOD,CAT and GSH.Conclusion:Our results suggest that the anti-arthritic properties of PCP may be due to immunosuppressive effects,cytokine regulation,antioxidant effects and bone-protective activities.

Two New Sesquiterpenes from Celastrus Paniculatus.Subsp.Paniculatus

Two new beta-dihydroagarofuran sesquiterpene polyol esters were isolated from Celastrus paniculatus.subsp.paniculatus. Their Structures were deduced on the basis of spectral analyses including 2D NMR. CO2 supercritical fluid was used in separation.

A NEW SESQUITERPENE FROM CELASTRUS ROSTHONIANUS

A new sesquitcrpene was isolated from Celastrus rothornianus, its structure was clucidated mainly on the basis of spectral analysis.

Study on effect and mechanism of Celastrus Orbiculatus total terpenoids in regulating lipid metabolism

Objective To investigate the effect and mechanism of Celastrus Orbiculatus total terpenoids on lipid metabolism in hyperlipidemia mice.Methods ICR mice were selected as investigated subject.The hyperlipemia mice models were made with feeding high-fat forage and were randomly divided into six groups:the normal group,the model group,the positive control group(treated with simvastatin)and the three groups treated with Celastrus Orbiculatus total terpenoids with low,medium and high dosage,respectively.Each group included eight mice.The control group was fed normal forage,but other groups were fed high fat forage.All groups were allowed to drink water freely.Since the first day when the models were made,intragastric administration had been adopted.The normal group was fed normal forage without intragastric administration;the model group was received physiological saline 20 mL·kg-1·d-1 with intragastric administration;the positive control group received simvastatin 2.6 mg·kg-1·d-1 with intragastric administration;the three treated groups received Celastrus Orbiculatus total terpenoids 60 mg·kg-1·d-1,120 mg·kg-1·d-1,200 mg·kg-1·d-1 with intragastric administration respectively.Each group was weighed once a week.On the basis of establishing hyperlipidemia mice model,blood lipids,lipid metabolic enzyme,antioxidative capacity were investigated after 21 days feeding of high-fat forage.Results Compared with model group,TC and TG in mice treated with Celastrus Orbiculatus total terpenoids all reduced and HDL-C raised obviously(P<0.01).Celastrus orbiculatus total terpenoids was shown to decreased MDA content in both serum and liver,increased serum SOD activity and inhibited the activity of the cholesteryl ester transfer protein(CETP).Conclusions Celastrus Orbiculatus total terpenoids could remarkably modulate the lipid metabolic disorder in hyperlipidemia mice,and has a certain regulating function on lipoprotein,inferring that it could reduce the occur of atherosclerosis.The mechanism of regulating lipid metabolism might be related with decreasing the activity of CETP and increasing antioxidative capacity.

Study on Extraction Techniques of Celastrol from Celastrus orbiculatus Thunb.

[Objectives]This study was conducted to investigate the extraction technology of celastrol from Celastrus orbiculatus Thunb.[Methods]Solvent ultrasonic extraction was selected,and with the content of celastrol as the evaluation index,the effects of different solvents,extraction time,temperatures and material-to-liquid ratios on the extraction rate of celastrol were investigated by single factor and orthogonal experiments.[Results]The optimal extraction conditions were as follows:a solvent ratio of petroleum ether to ethyl acetate at 1∶1,a ratio of solvent to material at 10∶1(v/w),extraction time of 30 min,and an extraction temperature at 30℃.[Conclusions]This method has high extraction rate,and is simple and feasible.

南蛇藤总萜抑制中性粒细胞胞外诱捕网形成的作用与机制研究

为探索南蛇藤总萜(the total terpenoids of Celastrus orbiculatus Thunb.,TTC)对中性粒细胞胞外诱捕网(neutrophil extracellular traps,NETs)形成及其作用机制,通过分离与制备中性粒细胞,建立佛波酯(phorbol 12-myristate 13-acetate,PMA)诱导的NETs形成细胞模型。利用瑞氏-姬姆萨染色、扫描电镜与免疫荧光技术研究南蛇藤总萜对NETs形成及其生物学标志的影响,并利用Annexin V/PI试验研究南蛇藤总萜对中性粒细胞凋亡的影响。结果表明:南蛇藤总萜能剂量依赖性地抑制PMA诱导的NETs形成;南蛇藤总萜(80μg·mL^(-1))可阻断中性粒细胞弹性蛋白酶(neutrophil elastase,NE)的释放,并破坏NETs相关DNA-NE复合物的形成;南蛇藤总萜(80μg·mL^(-1))可显著抑制PMA诱导的瓜氨酸化组蛋白H3(citrullinated histone H3,CitH3)的表达水平;南蛇藤总萜可剂量依赖性地促进中性粒细胞凋亡。综上,南蛇藤总萜对中性粒细胞NETs的形成具有抑制作用,其机制可能与其直接诱导中性粒细胞凋亡有关。

南蛇藤提取物通过DJ-1/PTEN/FAK轴抑制非小细胞肺癌侵袭转移

目的研究南蛇藤提取物(Celastrus orbiculatus Thunb.Extract,COE)抑制非小细胞肺癌侵袭转移的具体机制。方法通过CCK-8法测定COE抑制H1299细胞的生物活性,并依此选取低毒浓度进行细胞侵袭转移的功能研究。使用伤口愈合实验和高内涵成像追踪细胞轨迹对细胞运动功能进行测定。通过Western bolt实验进行分子层面的研究,探究COE抑制肺癌侵袭转移的具体分子机制。实验的分组采用剂量梯度进行设置,分别为Control组(0.05%DMSO),COE组:20,40,80μg/mL。结果COE以剂量依赖的形式明显抑制了H1299的细胞活性。伤口愈合实验结果显示,COE显著抑制了H1299细胞的迁徙能力,统计分析显示差异有显著统计学意义。高内涵成像实时动态追踪细胞轨迹显示,80μg/mL浓度的COE显著抑制了H1299细胞的迁徙能力,表现在运动速度的降低和均方位移量的下降。Western bolt实验结果表明,COE通过DJ-1/PTEN/FAK轴抑制非小细胞侵袭转移。蛋白质印迹的归一化分析均具有统计学意义。结论南蛇藤提取物能在低细胞毒浓度下通过DJ-1/PTEN/FAK轴抑制非小细胞侵袭转移。

FOUR NEW ALKALOIDS FROM Celastrus angulatus

The roots of Celastrus angulatus Maxim. are used in folk medicine for antipycetic and anti-wandering arthritis purpose. It also has been used as insecticide. The seven alkaloids were isolated from the root-bark of this plant. They are

南蛇藤提取物对小鼠胃类器官生长及E-caherin表达的影响

目的探讨南蛇藤提取物(COE)对小鼠胃类器官生长及其胃上皮细胞E-cadherin表达的影响。方法将8周龄C57小鼠胃幽门部分离并培养成胃类器官。光镜下观察胃类器官形成的动态变化,HE染色观察胃上皮细胞间结构,免疫荧光染色观察胃上皮细胞的上皮钙黏蛋白E-cadherin表达。类器官传代到第3代后,用不同浓度的COE(0、5、10、20μg/ml)处理,收集类器官,计算其数量,测量其直径,噻唑蓝(MTT)比色法测其细胞活性,并用Western blot法检测COE处理后类器官中的E-cadherin表达。结果24~48 h形成囊样结构并出现中心结构为囊腺样的三维细胞团,72 h后逐渐出芽并形成胃类器官,提示类器官成功构建。类器官中的上皮细胞标志物E-cadherin表达,进一步证实类器官的形成。与对照组比较,COE组胃类器官数量与直径均增加、细胞活性增强(P<0.05),且E-cadherin的表达随着COE的剂量增加而逐渐增加(P<0.01)。结论小剂量的COE可促进E-cadherin的表达与类器官的生长形成,可能会影响胃黏膜损伤的修复。

南蛇藤提取物联合miR-451抑制胃癌细胞侵袭和迁移的机制研究

为探讨南蛇藤提取物联合miR-451抑制人胃癌AGS细胞侵袭和迁移的作用机制,用慢病毒转染技术构建稳定过表达miR-451的人胃癌AGS细胞,记作AGS/miR-451^(+)细胞。MTT试验检测不同浓度南蛇藤提取物(20、40、80、160或320μg·mL^(-1))对AGS/miR-451^(+)细胞增殖的影响。伤口愈合试验和Transwell试验观察南蛇藤提取物对细胞迁移的影响。qRT-PCR试验检测南蛇藤提取物处理后细胞内mTOR mRNA表达量的变化。Western blot试验分析南蛇藤提取物对上皮间质转化(epithelial-mesenchymal transformation, EMT)和PI3K/AKT/mTOR信号转导通路相关蛋白质表达的影响。结果表明:南蛇藤提取物处理24 h后明显抑制AGS/miR-451^(+)细胞的侵袭和迁移能力。细胞中E-Cadherin表达量增加,Vimentin和N-cadherin表达量降低。mTOR通路相关蛋白质,如mTOR、PI3K、AKT、4EBP1的总蛋白质表达水平和磷酸化蛋白质表达水平均显著降低。综上,南蛇藤提取物协同miR-451可抑制AGS/miR-451^(+)细胞的增殖、侵袭和迁移,其分子机制与PI3K/AKT/mTOR信号转导通路相关。