贯叶金丝桃(Hypericum perforatum)种子灌浆与发芽特性研究

贯叶金丝桃(Hypericum perforatum)是抗抑郁中药的基原植物,以有性繁殖为主,种子微小。为了揭示贯叶金丝桃种子发育规律,明确种子适宜采收期,以甘肃礼县栽培的2年生贯叶金丝桃为研究对象,于开花后第5天开始,每隔3 d测定种子粒重变化动态,并拟合Logistic曲线方程,最后测定各时期采收种子的发芽指标。结果表明:贯叶金丝桃种子灌浆持续期44 d,籽粒干质量变化符合Logistic生长曲线:开花后第5~11天为渐增期,第11~32天为快增期,第32~44天进入稳增期后略有下降。在灌浆过程中,种子鲜质量呈先升高后下降的动态变化趋势,在花后第32天达到最大值0.2697 g;灌浆速率和脱水速率呈波动趋势,种子干质量与平均灌浆速率、灌浆持续期呈极显著正相关,与含水量呈极显著负相关。种子发芽率和发芽指数在开花后44天达到最大,发芽势在开花后41天达到最大,发芽率、发芽势和发芽指数均与灌浆持续期呈极显著正相关,与含水量呈极显著负相关。以上说明甘肃礼县贯叶金丝桃繁种时以开花后44天左右(8月9日前后)为种子采收适宜期,过早采收和延迟采收均影响种子发芽质量。

In Vitro and in Silico Insights on the Biological Activities, Phenolic Compounds Composition of Hypericum perforatum L. Hairy Root Cultures

Three Hypericum perforatum hairy root lines(HR B,HR F and HR H)along with non-transformed roots were analyzed for phenolic compounds composition and in vitro enzyme inhibitory properties.In silico molecular modeling was performed to predict the interactions of the most representative phenolic compounds in HR clones with enzymes related to depression,neurodegeneration and diabetes.Chromatographic analyses revealed that HR clones represent an efficient source of quinic acid and hydroxybenzoic acids,epicatechin and procyanidin derivatives,quercetin and kaempferol glycosides,as well numerous xanthones.In vitro antidepressant activity of HR extracts through monoamine oxidase A(MAO-A)inhibition was attributed to the production of oxygenated and prenylated xanthones.The neuroprotective potential of HR extracts was related to the accumulation of quercetin 6-C-glucoside,epicatechin,procyanidins andγ-mangostin isomers as potential inhibitors of acetylcholinesterase(AChE)and butyrylcholinesterase(BChE).Vanillic acid and prenylated xanthones in HR clones as promising inhibitors of tyrosinase additionally contributed to the neuroprotective activity.Five preeminent xanthones in HR(γ-mangostin,mangiferin,garcinone C,garcinone E and 1,3,7-trihydroxy-6-metoxy-8-prenyl xanthone)along with the flavonol quercetin 6-C-glucoside effectively inhibitedα-amylase andα-glucosidase indicating the antidiabetic properties of HR extracts.Transgenic roots of H.perforatum can be exploited for the preparation of novel phytoproducts with multi-biological activities.

Influence of Hypericum perforatum Extract on Piglet Infected with Porcine Respiratory and Reproductive Syndrome Virus

To study the influence of Hypericum perforatum extract （HPE） on piglets infected with porcine respiratory and reproductive syndrome virus （PRRSV）, enzyme-labeled immunosorbent assay （ELISA） and cytopathic effect （CPE） were used to determine in vitro whether HPE could induce swine pulmonary alveolar macrophages （PAMs） to secrete IFN-γ, and whether PRRSV titers in PAMs were affected by the levels of HPE-induced IFN-γ. HPE （200 mg·kg-1） was administrated by oral gavage to piglets infected with the PRRSV in vivo to observe whether HPE affected the viremia, lung viral titers, and weight gain of piglets infected with PRRSV. The results showed that HPE was capable of inducing PAMs to produce IFN-γ in a dose dependent manner and HPE pretreatment was capable of significantly reducing PRRSV viral titers in PAMs （P〈 0.01）. Administration of HPE to the PRRSV-infected animals significantly （P〈 0.05） reduced viremia over time as compared with the PRRSV-infected animals. But there was not significant decrease in lung viral titers at day 21 post-infection between the HPE- treated animals and the PRRSV-infected control piglets. There were no significant differences in weight gain over time among the HPE-treatment animals, the normal control, and the HPE control animals. The PRRSV-infected animals caused significant （P〈 0.01） growth retardation as compared with the HPE controls and the normal piglets. It suggested that HPE might be an effective novel therapeutic approach to diminish the PRRSV-induced disease in swine.

In vitro Anti-Hepatitis B Virus Effect of Hypericum perforatum L.

The anti-hepatitis B virus(HBV)effects and its mechanisms of the ethanol extracts of Hypericum perforatum L.(EHP)in vitro were explored.HepG2 2.2.15 cells,a stable HBV-producing cell line,were cultured as the model system to observe the anti-HBV effect.The viral antigens of cellular secretion,HBsAg and HBeAg,were determined by enzyme linked immunosorbent assay(ELISA).The quantity of HBV-DNA released in the supernatant was assayed by real-time PCR.In order to understand the mechanisms of the suppression of H...

An extract of Hypericum perforatum induces wound healing through inhibitions of Ca^(2+) mobilizations,mitochondrial oxidative stress and cell death in epithelial cells:Involvement of TRPM2 channels

The wound is induced by several mechanical and metabolic factors.In the etiology of the wound recovery,excessive oxidative stress,calcium ion(Ca^(2+))influx,and apoptosis have important roles.Ca^(2+)-permeable TRPM2 channel is activated by oxidative stress.Protective roles of Hypericum perforatum extract(HP)on the mechanical nerve injury-induced apoptosis and oxidative toxicity through regulation of TRPM2 in the experimental animals were recently reported.The potential protective roles in HP treatment were evaluated on the TRPM2-mediated cellular oxidative toxicity in the renal epithelium(MPK)cells.The cells were divided into three groups as control,wound,and wound+HP treatment(75μM for 72 h).Wound diameters were more importantly decreased in the wound+HP group than in the wound group.In addition,the results of laser confocal microscopy analyses indicated protective roles of HP and TRPM2 antagonists(N-(p-Amylcinnamoyl)anthranilic acid and 2-aminoethyl diphenylborinate)against the wound-induced increase of Ca^(2+) influx and mitochondrial ROS production.The wound-induced increase of early(annexin V-FITC)apoptosis and late(propidium iodide)apoptosis were also decreased in the cells by the HP treatment.In conclusion,HP treatment acted protective effects against wound-mediated oxidative cell toxicity and apoptosis through TRPM2 inhibition.These effects may be attributed to their potent antioxidant effect.

Antihyperglycemic effect of Hypericum perforatum ethyl acetate extract on streptozotocin-induced diabetic rats

Objective:To evaluate the antihyperglycemic activity of ethyl acetate extract of Hypericum perforatum(H.perforatum)in streptozotocin(STZ)-induced diabetic rats.Methods:Acute toxicity and oral glucose tolerance lest were performed in normal rats.Male albino rats were rendered diabetic by ST/(40 mg/kg,intraperitoneally).H.perforatum ethyl acetate extract was orally administered to diabetic rats at SO,100 and 200 mg/kg doses for 15 days to determine the antihyperglycemic activity.Biochemical parameters were determined at the end of the treatment.Results:H.perforatum ethyl acetate extract showed dose dependant fall in fasting blood glucose(FBG).After 30 min of extract administration,FBG was reduced significantly when compared with normal rats.H.perforatum ethyl acetate extract produced significant reduction in plasma glucose level,serum total cholesterol,triglycerides,glucose-6-phosphatase levels.Tissue glycogen content,HDL-cholesterol,glucose-6-phosphate dehydrogenase were significantly increased compared with diabetic control.No death or lethal effect was observed in the toxic study.Conclusions:The results demonstrate that H.perforatum ethyl acetate extract possesses potent antihyperglycemic activity in STZ induced diabetic rats.

Anti-Influenza A Virus Effect of Hypericum perforatum L. Extract

To study the antiviral effect of Hypericum perforatum L. extract (HPE) on influenza A virus (IAV) (H1N1) in vitro and in vivo. Cytopathic effect (CPE) and neutral red (NR) dye uptake were used to examine the antiviral effect of HPE on Madin Darby Canine Kidney (MDCK) cells which were infected with IAV in vitro. HPE was effective against influenza A virus (IAV) in vitro, with a 50% effective concentration (EC50) of 40 μg/mL. The mean 50% cytotoxic concentration (CC50) in the MDCK used in these experiments was 1.5 mg/mL. Ribavirin was run in parallel with EC50 values of 5.0 μg/mL; the mean CC50 for ribavirin was 520 μg/mL. Oral gavage administrations of HPE or ribavirin to mice infected with the IAV were highly effective in preventing death, slowing the decline of arterial oxygen saturation, inhibiting lung consolidation and reducing lung virus titers. The minimum effective dose of HPE in these studies was 31.25 mg/kg/day, which was administered twice daily for 5 d beginning 4 h prior to virus exposure. Below a dosage of 2000 mg/kg/day, almost all treated mice survived, which suggests that HPE is of low toxicity. Ribavirin’s minimum effective dose was 40 mg/kg/day with the LD50 determined to be 200 mg/kg/day. Delay of the initiation of either HPE or ribavirin therapy, using approximately 1/3 LD50 dose each time, could still be protective as late as 48 h after exposure to the IAV. While both agents appeared to have similar efficacy against IAV infections, HPE was considered to be less toxic and may warrant further evaluation as a possible therapy for influenza.

Effect of the Extract from Hypericum perforatum on Highly Pathogenic Avian Influenza Virus(HPAIV)

[Objective] The aim was to study the effects of the extract from Hypericum perforatum on highly pathogenic Avian Influenza Virus(HPAIV)in vivo.[Method] Chickens infected with H5N1 virus were treated with the extract from H.perforatum for 4 d.The virus was then detected by hemoagglutination(HA)test and reverse transcription polymerase chain reaction(RT-PCR).[Result] No H5N1 virus could be detected at the 7th d when the chickens were treated with 0.2 or 0.1 g/(kg·d)of the extract from H.perforatum.However,the virus could be detected in other chickens without the extract from HPE treatment.[Conclusion] The extract from H.perforatum might be a potential drug candidate to control infection of H5N1 subtype AIV in chickens.

Pleomorphic hepatocellular carcinoma following consumption of hypericum perforatum in alcoholic cirrhosis

Hepatocellular carcinoma(HCC)often develops in patients with underlying liver disease,yet HCC with syncytial giant cells(SGCs)is extremely rare.Herein,we report a 55-year-old man with a 6-year history of alcoholic cirrhosis who during his regular checkup presented with marked elevation of alpha-fetoprotein.Clinical examination and imaging analyses revealed a tumor-like lesion in segment 4 of the liver,which was removed by limited wedge resection.Histological analysis by hematoxylin and eosin staining indicated pleomorphic and atypical nodules,with some SGCs,embedded within the boundaries of the neoplastic lesion.The adjacent liver parenchyma showed microvesicular steatosis,pericellular fibrosis,and moderate hemosiderin accumulation(grade 2,as determined by Prussian blue iron stain)in hepatocytes and Kupffer cells but no copper accumulation(as determined by orcein stain).Immunohistochemical analysis showed hepatocyte antigen-positive staining for the neoplastic cells and SGCs.The diagnosis was made for cirrhosis-related HCC with SGCs.The previous reports of pleomorphic HCC have featured osteoclast-like(i.e.,mesenchymal type)giant cells,making this case of epithelial type giant cells very rare.The patient’s 6-month history of hypericum perforatum/St John’s wort self-medication may have prompted the cirrhosis or HCC progression or the unusual SGC manifestation.

Recent enhancement of the immunity in AIDS and other immunocompromised patients by hyperforin an antibiotic from <i>Hypericum perforatum</i>L. (<i>in vitro</i>model) part I

Today, Hypericum perforatum L. is probably one of the best-characterized medicinal plants, and hyperforin is its best-characterized constituent. Extracts from H. perforatum are widely used as antidepressants;however, less attention has been given to other properties of hyperforin, such as antitumor, fungicidal, antiviral and antibacterial action, or its possible use as a substance with immunomodulation properties. The present study summarizes results that describe the influence of hyperforin as an immunomodulation agent on phagocytosis and the breakdown of Escherichia coli by human polymorphonuclear neutrophils (PMNs). Hyperforin at 1 - 100 μg/mL concentrations was found to have a major influence on phagocytosis and the breakdown of E. coli by PMNs in vitro. A 100 μg/mL solution of hyperforin increased the uptake of non-opsonized E. coli almost 50-fold, and the uptake of IgG-opsonized E. coli more than threefold;on the other hand, the uptake of serum-opsonized bacteria was reduced to approximately 60% of that of the control. Hyperforin seems to bind to both PMNs and E. coli and acts like an opsonin. The elimination of remnants of IgG-opsonized E. coli from the PMNs was stimulated by hyperforin, while the elimination of remnants from non-op-so nized and serum-opsonized material was unaffected by the drug. Hyperforin exhibited clear immunomodulation ability as a phagocytosisstimulating agent. Hyperforin is probably inactive against human immunodeficiency virus (HIV) and most Gram-negative bacteria. However, it can protect acquired immunodeficiency syndrome (AIDS) patients and other immunocompromised patients by its antibacterial activity against Gram-positive bacteria and by enhancement of phagocytosis of Gram-positive and Gram-negative bacteria;some Gram-negative bacteria, such as Neisseria, are sensitive to hyperforin. Hyperforin has the ability to penetrate the blood-brain barrier (BBB) and blood-testis barrier (BTB) and is a valuable antibacterial agent against meningitis and gonorrhea. These properties of hyperforin are important for an antibiotic with immunomodulation activity in the struggle against the growing mortality in AIDS patients as a result of opportunistic bacteria, as recently shown by Bekondi et al. (2006, Int. J. Infect. Dis. 10, 387-395). It could also help to combat primary and opportunistic pathogens associated with meningitis in adults' relation to HIV serostatus.

Pseudohypericin and Hyperforin in Hypericum perforatum from Northern Turkey:Variation among Populations,Plant Parts and Phenological Stages

Hypericum perforatum is a perennial medicinal plant known as ＂St. John＇s wort＂ in Western Europe and has been used in the treatment of several diseases for centuries. In the present study, morphologic, phenologic and population variability in pseudohypericin and hyperforin concentrations among H. perforatum populations from Northern Turkey was investigated for the first time. The aerial parts of H. perforatum plants representing a total of 30 individuals were collected at full flowering from 10 sites of Northern Turkey to search the regional variation in the secondary metabolite concentrations. For morphologic and phenologic sampling, plants from one site were gathered in five phenological stages： vegetative, floral budding, full flowering, fresh fruiting and mature fruiting. The plant materials were air-dried at room temperature and subsequently assayed for chemical concentrations by high performance liquid chromatography. Secondary metabolite concentrations ranged from traces to 2.94mg/g dry weight （DW） for pseudohypericin and traces -6.29mg/g DW for hyperforin. The differences in the secondary metabolite concentrations among populations of H. perforatum were found to be significant. The populations varied greatly in hyperforin concentrations, whereas they produced a similar amount of pseudohypericin. Concentrations of both secondary metabolites in all tissues increased with advancing of plant development and higher accumulation levels were reached at flowering. Among different tissues, full opened flowers were found to be superior to stems, leaves and the other reproductive parts with regard to pseudohypericin and hyperforin accumulations. The present findings might be useful to optimize the processing methodology of wild-harvested plant material and obtain increased concentrations of these secondary metabolites.

Effects of light intensity and LED spectrum on the medicinal component accumulation of hydroponic Hypericum perforatum L.under controlled environments

Medicinal components of Hypericum perforatum L.plants varies widely due to fluctuations in growth environment and biotic and abiotic contamination during cultivation management.The quality of extracts or preparations is difficult to control because of the unstable raw materials.The aim of this study is to enhance the yield and medicinal component contents of H.perforatum by optimizing lighting factors under controlled environment.H.perforatum plants were hydroponically cultivated for 30 d under 3 levels of photosynthetic photon flux density(PPFD)with 200,300,and 400μmol/(m^(2)·s)using white LEDs(R:B ratio is the ratio of red light to blue light,R:B ratio of 0.9 and 1.8)and white plus red LED(R:B ratio of 2.7).The results showed that PPFD and LED spectrum had significant effects on the growth and accumulation of medicinal components of H.perforatum.Biomass accumulation of stem,leaf,and root increased linearly with the increase of PPFD under each LED spectrum.Fresh weights and dry weights of stem,leaf,and root were significantly higher under a PPFD of 400μmol/(m^(2)·s)with R:B ratio of 0.9 than those of 200μmol/(m^(2)·s),respectively.The relative growth rate and net photosynthetic rate showed linear relationships with PPFD under the same LED spectrum.Total hypericin content,total hyperforin content,and energy yield of hypericin increased with increasing PPFD.Total hypericin content and energy yield of hypericin of P400-L0.9 were 78%and 89%more than those of P400-L2.7,respectively.Total hyperforin content and energy yield of hyperforin of P400-L0.9 and P400-L2.7 were no significant differences.Based on energy efficiency,an R:B ratio of 0.9 of white LEDs with a PPFD of 400μmol/(m^(2)·s)was beneficial to improve medicinal component contents of hydroponic H.perforatum in plant factory with LED lighting.

Signal interaction between nitric oxide and hydrogen peroxide in heat shock-induced hypericin production of Hypericum perforatum suspension cells

Heat shock(HS, 40℃, 10 min) induces hypericin production, nitric oxide(NO) generation, and hydrogen peroxide(H2O2) accumulation of Hypericum perforatum suspension cells.Catalase(CAT) and NO spe-cific scavenger 2-4-carboxyphenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide(cPTIO) suppress not only the HS-induced H2O2 generation and NO burst, but also the HS-triggered hypericin produc-tion.Hypericin contents of the cells treated with both NO and H2O2 are significantly higher than those of the cells treated with NO alone, although H2O2 per se has no effects on hypericin production of the cells, which suggests the synergistic action between H2O2 and NO on hypericin production.NO treatment enhances H2O2 levels of H.perforatum cells, while external application of H2O2 induces NO generation of cells.Thus, the results reveal a mutually amplifying action between H2O2 and NO in H.perforatum cells.CAT treatment inhibits both HS-induced H2O2 accumulation and NO generation, while cPTIO can also suppress H2O2 levels of the heat shocked cells.The results imply that H2O2 and NO may enhance each other's levels by their mutually amplifying action in the heat shocked cells.Membrane NAD(P)H oxidase inhibitor diphenylene iodonium(DPI) and nitric oxide synthase(NOS) inhibitor S,S′-1,3-phenylene-bis(1,2-ethanediyl)-bis-isothiourea(PBITU) not only inhibit the mutually amplifying action between H2O2 and NO but also abolish the synergistic effects of H2O2 and NO on hypericin production, showing that the synergism of H2O2 and NO on secondary metabolite biosynthesis might be dependent on their mutual amplification.Taken together, data of the present work demonstrate that both H2O2 and NO are essential for HS-induced hypericin production of H.perforatum suspension cells.Furthermore, the results reveal a special interaction between the two signal molecules in mediating HS-triggered secondary metabolite biosynthesis of the cells.

贯叶金丝桃二氯甲烷部位的化学成分研究

目的研究贯叶金丝桃Hypericum perforatum L.二氯甲烷部位的化学成分。方法贯叶金丝桃二氯甲烷部位采用硅胶、ODS、Sephadex LH-20、半制备HPLC等进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果从中分离得到11个化合物,分别鉴定为贯叶金丝桃降碳聚酮A(1)、α-芒柄花醇(2)、(3 R)-thunberginol(3)、2-geranyloxy-1-(2-methylpropanoyl)-phloroglucinol(4)、4,6-dihydroxy-2-O-(3″,7″-dimethyl-2″,6″-octadienyl)-1-(2′-methylbutanoyl)benzene(5)、norhyperpalum G(6)、garsubellin A(7)、garsubellin B(8)、(2″R/S)-kellerine C(9)、kobusone(10)、圣草酚(11)。结论化合物1为新化合物,化合物2~3为首次在藤黄科植物中分离得到,化合物4~10为首次从该植物中分离得到。

贯叶金丝桃提取物对急性缺氧大鼠肝肾损伤的改善作用

【目的】研究贯叶金丝桃提取物(Hypericum perforatum extract,HPE)对急性缺氧大鼠肝肾损伤的改善作用。【方法】通过小鼠常压密闭实验模型初步筛选HPE(20%乙醇提取物、70%乙醇提取物和95%乙醇提取物)的抗缺氧活性组分。进一步建立大鼠低压低氧肝、肾损伤模型:将80只健康大鼠随机分为8组,分别为常氧空白组(NG),缺氧模型组(HG),HPE低、中、高剂量组(HPE-L、HPE-M、HPE-H,100、200、400 mg/kg),金丝桃苷低、高剂量组(HYP-L、HYP-H,50、100 mg/kg)和醋酸地塞米松组(DXM,4 mg/kg)。观察HPE对急性缺氧大鼠肝、肾组织病理学变化的影响,并测定其中氧化应激指标和相关炎症因子的变化。【结果】与模型组比较,给予HPE干预后的大鼠肝、肾组织中丙二醛(MDA)和过氧化氢(H_(2)O_(2))含量下降(P<0.01,P<0.05),谷胱甘肽(GSH)含量增加(P<0.01,P<0.05),总超氧化物歧化酶(T-SOD)和过氧化氢酶(CAT)活力有所提高(P<0.01,P<0.05)。同时,大鼠肝、肾组织中炎症因子白细胞介素-1β(IL-1β)、白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)和血管内皮生长因子(VEGF)的释放均被抑制(P<0.01,P<0.05)。【结论】HPE对急性缺氧大鼠肝、肾损伤具有一定程度的改善作用。

贯叶金丝桃化学成分的分离与鉴定

目的研究藤黄科(Guttiferae)金丝桃属(Hypericum)贯叶金丝桃(Hypericum perforatum L.)的化学成分。方法采用正相硅胶色谱、反相ODS色谱、凝胶色谱及高效液相色谱等多种色谱方法对贯叶金丝桃体积分数95%乙醇提取物进行分离纯化。利用紫外、红外、核磁共振光谱,高分辨质谱及X-ray单晶衍射法对化合物的结构进行鉴定。结果从贯叶金丝桃中分离鉴定8个化合物,分别为perforxanthone A(1)、8-hydroxy-1,2,3-trimethoxyxanthone(2)、绵马酚D(3)、(S)-5-hydroxy-3,4-dimethyl-5-pentylfuran-2(5H)-one(4)、ent-4(15)-eudesmene-1β,6α-diol(5)、methyl-(E)-8-oxooctadec-9-enoate(6)、模绕酮酸(7)、白桦脂酸(8)。结论化合物1为新的氧杂蒽酮类化合物,化合物2-7为首次从该植物中分离得到。

贯叶连翘的历史沿革、化学成分及药理作用研究进展

贯叶连翘是我国传统中药之一,在宋代之前作为连翘中的“小翘”应用于临床,为今之“贯叶金丝桃”的带根全草,具有收敛止血,清热解毒,利湿等功效。主要含有黄酮类、间苯三酚类、萘骈二蒽酮类、挥发油类、酚酸类等化学成分。现代药理研究表明贯叶连翘具有抗抑郁、抗菌、抗肿瘤、保肝及抗纤维化等作用,其药理作用的机制较为复杂,部分机制还有待进一步深入研究。本文对贯叶连翘历史沿革、化学成分、质量控制及药理作用等方面进行文献整理并展开综述,以期为贯叶连翘的药用部位扩展及后续深入开发研究提供参考和依据。

贯叶金丝桃对大鼠脑缺血再灌注损伤的保护作用及机制研究

目的探讨贯叶金丝桃对大鼠脑缺血再灌注损伤的保护作用及潜在机制。方法将雄性SD大鼠随机分为假手术组、模型组、阳性对照组(尼莫地平0.012g/kg)和贯叶金丝桃高、低剂量组(5.212、1.303g/kg),每组10只。除假手术组外其余各组大鼠均采用改良线栓法构建大鼠大脑左侧中动脉闭塞再灌注模型。各药物组大鼠于术后第2天开始灌胃相应药液,每天1次,连续7d。分别于药物干预前(造模后第1天)和末次给药后进行大鼠神经功能评分,以TTC染色法观察其末次给药后的脑梗死情况,以苏木精-伊红染色法和TUNEL染色法分别观察其脑皮层、海马组织的病理改变和神经细胞的凋亡情况,以Westernblot法和反转录聚合酶链式反应法分别检测其促红细胞生成素(EPO)、促红细胞生成素受体(EPOR)、Janus激酶2(JAK2)、信号转导及转录激活因子3(STAT3)、磷酸化STAT3(p-STAT3)蛋白和EPO、EPOR、JAK2、STAT3mRNA的表达情况。结果与假手术组比较,模型组大鼠药物干预前、末次给药后的神经功能评分和脑梗死比例均显著升高(P<0.01);脑皮层和海马组织神经细胞受损明显,凋亡的神经细胞明显增多,凋亡率显著升高(P<0.01);脑组织中EPO、EPOR蛋白及mRNA的表达水平均显著降低(P<0.01),JAK2、p-STAT3、STAT3蛋白和JAK2、STAT3mRNA的表达水平均显著升高(P<0.01)。与模型组比较,各药物组大鼠脑皮层和海马组织神经细胞受损及凋亡情况均有所改善,各定量指标大部分显著好转(P<0.05或P<0.01)。结论贯叶金丝桃对大鼠脑缺血再灌注损伤具有保护作用,其机制可能与调节EPO介导的JAK2/STAT3信号通路有关。

贯叶连翘的化学成分及降糖活性研究

目的:研究贯叶连翘Hypericum perforatum L.的化学成分及降糖活性。方法:运用硅胶柱色谱、ODS柱色谱、Sephadex LH-20葡聚糖凝胶柱色谱以及制备HPLC等多种方法对贯叶连翘地上部分95%乙醇提取物进行分离纯化,利用HR-ESI-MS、NMR等波谱技术对分离得到的化合物进行鉴定。通过体外α-葡萄糖苷酶活性抑制试验,测定化合物的降糖活性。结果:从贯叶连翘中分离得到14个化合物,分别鉴定为:北美芹素(1)、3′,4′-disenecioyl-cis-khellactone(2)、5,4′-二羟基-6,8-二甲基-7-甲氧基黄酮(3)、5,4′-二羟基-6-甲基-7-甲氧基黄酮(4)、5,7-二羟基-3-甲基色原酮(5)、5,7-二羟基-3-乙基色原酮(6)、2,4,6-三羟基苯甲酸乙酯(7)、香草醛(8)、7-hydroxy-5-methoxy-4,6-dimethylphthalidc(9)、α-生育醌(10)、豆甾醇(11)、乙酰-11-羰基-β-乳香酸(12)、阿魏酸二十六烷酯(13)、cosmosoic acid(14)。结论:其中,化合物1~4、10、12~14为首次从金丝桃属植物中分离得到,化合物5~7、9为首次从贯叶连翘中分离得到。化合物3和4表现出较好的α-葡萄糖苷酶抑制活性,其IC_(50)值分别为490.3和549.9μmol/L,与阳性药阿卡波糖效果(IC_(50)=500.1μmol/L)相当。