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.

Effects of Different Geographical Aspects and Ontogenetic Variability on Total Hypericin Content of Hypericum triquetrifolium Turra. and Hypericum scabrum L.

The present study was conducted to determine the total hypericin contents of Hypericum triquetrifolium Turra.and Hypericum scabrum L.species which are naturally distributed in the flora of Siirt province,Turkey.Hypericin contents of Hypericum species grown in different geographical aspects(North,South,East,and West),and it was measured at different harvest times(full bloom-ing and post blooming period).In the current study,it has been determined that total hypericin content varies considerably according to aspects,plant developmental stages(ontogenetic variance),and species.According to species x aspect interaction,the highest total hypericin content was recorded from the west aspect(3.13 mg/g)in Hypericum triquetrifolium,while,the lowest hypericin content was also obtained from the west aspect(1.22 mg/g)in Hypericum scabrum.When the highest total hypericin content was analyzed according to aspect x species x harvest time interaction,the highest total hypericin content was produced from Hypericum triquetrifolium at the harvest of west aspect with 5.28 mg/g,while the minimum amount of hypericin was obtained from the same aspect in Hypericum scabrum with 0.50 mg/g.In species x harvest time interaction,the highest total hypericin content was obtained from the full bloom(3.10 mg/g)harvest in Hypericum triquetrifolium,while the lowest hypericin was obtained from the full bloom(1.26 mg/g)harvest in Hypericum scabrum.The data suggest that the aver-age total hypericin content was 2.26 mg/g in Hypericum triquetrifolium and 1.28 mg/g in Hypericum scabrum.

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.

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.

长柱金丝桃(Hypericum ascyron L.)分泌结构的研究

对长柱金丝桃各类器官进行了整体透明和解剖学研究,确定合理的采收部位和采摘时间。结果表明,植株富含分泌囊和分泌小管道两种分泌结构;叶片中分泌囊(道)的发育属于裂生型;地上部分泌结构分布较多,尤以叶片中数量最多、分布密度最大;确定植物的最佳采收时期是每年8～9月的花果期、最佳采收部位是地上部。此研究结果为此药用植物合理的采收部位和采收时间的确定提供解剖学依据,同时为其他植物分泌囊(道)发育规律的研究提供理论依据。

Hypercohones A-C,acylphloroglucinol derivatives with homo-adamantane cores from Hypericum cohaerens

Three new homo-adamantanyl type natural products were derived from polyprenylated polycyclic acylphloroglucinol.Hypercohones A-C(1-3),along with five other known hypercohones(4-8),were isolated from the aerial parts of Hypericum cohaerens.The structures of 1-3 were elucidated on the basis of comprehensive spectroscopic analysis.The inhibitory activities of these isolates against five human cancer cell lines in vitro were tested.

Hypercohones D–G,New Polycyclic Polyprenylated Acylphloroglucinol Type Natural Products from Hypericum cohaerens

Four new polycyclic polyprenylated acylphloroglucinol type metabolites,hypercohones D–G(1–4),along with four known analogues(5–8),were isolated from the aerial parts of Hypericum cohaerens.The structures of these isolates were elucidated by extensive spectroscopic methods.The inhibitory activities of these isolates against five human cancer cell lines in vitro were also tested.

Carascynol A,a hybrid of caryophyllane-type terpenoid and a C6 unit degraded by polyprenylated acylphloroglucinols from Hypericum ascyron

Carascynol A,an unprecedented 4/9/8 ring system hybrid with a peroxide bridge,was characterized from Hyperi-cum ascyron.The architecture contains a caryophyllane-type moiety and a C_(6) unit derived from polyprenylated acylphloroglucinols.Its structure and absolute configuration were determined by comprehensive spectroscopic and X-ray diffraction data.Biologically,compound 1 inhibited cell proliferation in LoVo,SW480,and HCT116 cell lines(IC_(50)=12.30-24.57μM).

Dearomatized Isoprenylated Acylphloroglucinol Derivatives with Potential Antitumor Activities from Hypericum henryi

A series of dearomatized isoprenylated acylphloroglucinols derivatives,hyperhenols A-E(1-5),as well as seven known analogues(6-12),were characterized from Hypericum henryi.Their structures were determined by combination of NMR,ECD spectroscopy,and X-ray difraction analysis.Compounds 1 and 6-8 were tested to exhibit potential antitumor properties,of which 6 and 7 inhibited cell growth through inducing apoptosis and cell cycle arrest.In addition,these compounds could induce autophagy and PINK1/Parkin-mediated mitophagy in cancer cell lines,as well as suppress lung cancer A549 cells metastasis in vitro.

New Constituents from Hypericum Japonicum

Two new glycosides 1,5-dihydroxyxathanone-6-o-beta-D-glucoside and flavanonol-taxifolin-3, 7-o-alpha-L-dirhamnoside. were isolated from the aerial parts of Hypericum japonicum Thunb, ex Murray, The chemical structures were determined by spectroscopic methods and chemical evidences

Effect of Hypericum perforatum L. compared with metronidazole in bacterial vaginosis:a double-blind randomized trial

Objective:To compare effect of Hypericum perforatum(H.perforatum) vaginal gel with metronidazole on bacterial vaginosis(BV) in terms of initial response to treatment and preventing recurrence(primary outcomes) and also patient complaints(secondary outcomes).Methods:In this double-blind,double dummy trial,married women aged 18-49 with BV were randomized into two groups and administered 5 g of 3%H.perforatum and placebo of metronidazole(n=82),or 5 g of 0.75%metronidazole and placebo of H.peiforatum(n=80)vaginally for 5 d.Amsel criteria were used for diagnosis and assessing cure and recurrence of BV.The comparisons was done using Chi-square,Fisher's exact and logistic regression.Results:At 10-12 d.cure rate was 82%in the H.perforatum and 85%in metronidazole group(risk ratio 0.9.95%confidence interval 0.6 to 1.3).Among the cured women,recurrence rate was 9%in the H.perforatum and 13%in the metronidazole group at the 30-35 d visit(risk ratio 0.8,95%confidence interval 0.4 to 1.3),There was no statistically significant difference between the groups regarding any patient complaints,except itching which was less in H.perforatum group(5%vs.16%,P=0.018 at the first and 13%vs.43%,P<0.001 at the second follow-up).No significant adverse event was reported at any groups.Conclusions:H.peiforatum could be a good option for treatment of BV.However,further studies arc needed for its public use.

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...

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.

New Prenylated flavonol from Hypericum japonicum

One new prenylated flavonol, 7,8-(2'',2'' -dimethylpyrano)-5,3',4'-trihydroxy-3-methoxyflavone was isolated from Hypericum japonicum. The chemical structure was determined by spectroscopic methods.

Pollen Morphology and Pollen Fertility Estimation of Three Medicinal Plant Species of <i>Hypericum</i>L. from Kaghan Valley, Northern Pakistan

Pollen morphology & pollen fertility estimation of three medicinal species belonging to genus Hypericum L. from flora of Kaghan valley, Northern Pakistan was investigated by light and scanning electron microscopy for the first time. The species are Hypericum elodeoides Choisy in, Hypericum oblongifolium Choisy, and Hypericum perforatum L. Pollen morphological characteristics with considerable variation are provided for these taxa. Among the studied taxa, the pollen grains were 3-4 colporate type and the largest pollen size was found in H. oblongifolium in polar view 23.0 μm and in equatorial view was 25.35 μm. The smallest pollen was of H. elodeoides in polar view which was 19.91 μm and in equatorial view was observed 12.53 μm in H. perforatum. The shape of the all pollen grain was circular to semi-angular in polar view, however in equatorial view the shape of the grains was oblate-spheroidal, in H. elodeoides, and H. oblongifolium while prolate in H. perforatum. Exine sculpturing was observed by scanning electron microscopy which showed foveolate sculpturing in H. elodeoides, reticulate in H. oblongifolium and scabrate in H. perforatum. Pollen fertility estimation ranged from 82.66% to 90.90% which shows that flora of selected species is well established.

Diverse Polyphenols from Hypericum faberi

Six new polyphenols with diferent isoprenylated xanthones,isoprenylated acylphloroglucinols,and chromone architectures,hyperfaberols A-F(1-6),were isolated from the whole plants of Hypericum faberi along with seven other related known compounds.In which hyperfaberols A/B(1/2)and 12-13 were isoprenylated xanthones,hyperfaberols C-E(3-5)and 8-11 were seven isoprenylated acylphloroglucinol derivatives,while 6-7 were two chromones.Their structures were elucidated by comprehensive analysis of their spectroscopic data as well as detailed comparison with the literature data.Compounds 1 and 11 showed cytotoxities against the human esophageal cancer cell line(ECA-109)and the pancreatic tumor cell line(PANC-1)in vitro,respectively.

Adipogenesis Inhibitory Activity of Hypersampsone P from Hypericum subsessile

Adamantane polycyclic polyprenylated acylphloroglucinols(PPAPs)with caged architecture,a special class of hybrid natural products,is specifically rich in the plant family Guttiferae,especially Hypericum or Garcinia genus.Hypersampsone P is one of Adamantane PPAPs compounds extracted from Hypericum subsessile.Here we have chosen,screened ten PPAPs and identified one of them showed an activity in inhibiting of adipocytes differentiation.Particularly,the compound,hypersamp-sone P,blunted the adipocyte differentiation dose-dependently.Moreover,hypersampsone P down-regulated the expressions of several key regulators for adipogenesis,including PPARγand FABP4.The treatment of cells at the early stage of adipo-genesis by hypersampsone P induced the greatest blunting of adipocyte differentiation and the effect might be involved in the LKB1-AMPK signaling pathway.