Investigation of the pharmaceutical and pharmacological equivalence of different Hawthorn extracts

Seven Hawthorn extracts were tested in isolated guinea pig aorta rings. The effect on noradrenaline- (10 microM) induced contraction was investigated. The extracts were prepared using ethanol (40 to 70% v/v), methanol (40 to 70% v/v), and water as the extraction solvents. The aqueous-alcoholic extracts displayed similar spectra of constituents. They were characterised by similar procyanidin, flavonoid, total vitexin and total phenols content and by similar TLC fingerprint chromatograms. The aqueous extract, however, showed a different fingerprint and a noticeably lower concentration of procyanidins, flavonoids and total phenols but a similar total vitexin content. All 7 extracts had a relaxant effect on the aorta precontracted by noradrenaline and led to relaxations to 44 until 29% of the initial values. The EC50 values of the aqueous-alcoholic extracts varied between 4.16 and 9.8 mg/l. The aqueous extract produced a similarly strong maximal relaxation as the other extracts, but the EC50, at 22.39 mg/l, was markedly higher. The results show that Hawthorn extracts with comparable quality profiles were obtained by using aqueous-alcoholic extraction solvents (40 to 70% ethanol or methanol). The extracts exerted comparable pharmacological effects. When using water as the extraction solvent, both, the spectrum of constituents and the pharmacological effect, deviated remarkably. It is thus possible to obtain bioequivalent extracts with comparable effect profiles by using 40 to 70% ethanol or methanol as the extraction solvent.     

超声法提取山里红叶总黄酮及其抗氧化活性研究

采用超声辅助提取法从山里红叶中提取总黄酮。通过Box Behnken实验设计(BBD)结合响应面法(RSM)来优化超声提取的条件。影响山里红叶总黄酮提取效率的4个主要变量为液固比,温度,乙醇浓度和时间,得到的最佳值分别为15,40℃,40%,32 min。在此条件下,总黄酮的产率为15.50 mg·g^-1。体外抗氧化实验表明,山里红叶提取物的DPPH自由基清除能力为0.69 mg·mL^-1(以IC₅₀值表示) ,与传统的浸渍提取和热回流提取方法相比,超声提取的方法具有更好的抗氧化活性。实验结果表明超声提取法适用于提取山里红叶中的总黄酮,并且其提取物具有较好的抗氧化活性。     

Effect of irradiance on shoot development in vitro

The growth of Disanthus cercidifolius and Rhododendron cultivars, and to a lesser extent Crataegus oxyacantha cv. Paul's Scarlet, was modified by altering either the spectral quality or the level of irradiance received by shoot cultures; which were otherwise maintained under uniform medium and plant growth regulator (PGR) conditions in vitro. When the spectrum of Philips colour 84 (white) fluorescent lamps was modified by coloured cellulose acetate filters, red light promoted shoot extension and axillary branching, whereas blue light inhibited shoot growth and reduced leaf chlorophyll content in the sensitive cultivar R. cv. Dopey. By using single or multiple layers of neutral density filters, or moving cultures nearer to the light source, irradiance from white light was varied. All cultures grew well at low levels of irradiance (c. 11 µmol m^–2 s^–1), but the growth and leaf chlorophyll content of cultures of Disanthus and Rhododendron cultivars were suppressed by increasing irradiance. In three related Rhododendron cultivars, increased irradiance promoted the development of adventitious shoots. Crataegus shoots were tolerant of a wide range of irradiances and only shoot extension was inhibited at the highest level tested; leaf chlorophyll content was unaffected. These results are discussed in terms of the differential perception of light relative to the natural habitats of these plants, and of the possible direct effect of irradiance upon PGRs in the culture system.     

Baseline severity but not gender modulates quantified Crataegus extract effects in early heart failure - A pooled analysis of clinical trials

Objective

The efficacy of quantified Crataegus extract in chronic heart failure (CHF) has been assessed in numerous clinical studies. The present pooled analysis evaluates the impact of baseline severity and gender on objective and patient-reported endpoints and associations between both types of outcomes in patients with early CHF.

Methods

Available data from 687 individual patients treated with quantified Crataegus extract or placebo in ten studies were pooled. Treatment effects on physiologic outcome parameters and on symptoms were analysed for their association with baseline severity and gender. Changes in symptom scores were investigated with respect to their relation to physiologic outcome parameters. Results were compared with observations in a 3-year cohort study.

Results

Physiologic outcome parameters maximal workload (MWL), left ventricular ejection fraction (LVEF) and pressure-heart rate product increase (PHRPI) at 50 W ergometric exercise improved more in active treatment than in placebo patients. Magnitude of improvement was independent from baseline for LVEF but increased for MWL and PHRPI with baseline severity. Improvement of typical symptoms like reduced exercise tolerance, exertional dyspnea, weakness, fatigue, and palpitations improved more with active treatment and in patients with more severe symptoms. A weak association between improvements in MWL, PRHP, and symptoms could be demonstrated. Gender differences in treatment effects could be explained by baseline differences. Results of the pooled analysis are in agreement with observations in the cohort study.

Conclusions

Crataegus extract treatment effects on physiologic outcomes and typical symptoms were modulated by baseline severity. Taking baseline differences into account, benefits were comparable in male and female patients with impaired exercise-tolerance in early chronic heart-failure.     

野山楂茎化学成分研究

采用硅胶、AB-8大孔树脂和凝胶柱层析方法对野山楂茎化学成分进行分离纯化,并根据理化性质和光谱数据分析鉴定得到9个化合物,分别是:棕榈酸(1)、硬脂酸(2)、β-谷甾醇(3)、槲皮素(4)、芦丁(5)、熊果酸(6),β-胡萝卜甙(7),柠檬酸(8)和儿茶素(9)。除化合物4外,其余均首次从野山楂中分离得到。     

Search for potential Angiotensin Converting Enzyme (ACE)-inhibitors from plants

MeOH extracts, fractions and pure substances from Musanga cecropioides, Cecropia species and Crataegus oxyacantha /C. monogyna were screened by using an in vitro bio-assay based on the inhibition of Angiotensin Converting Enzyme (ACE), as measured from the enzymatic cleavage of the chromophore-fluorophore-labelled substrate dansyltriglycine into dansylglycine and diglycine. Phenolic acids showed no significant ACE-inhibition whereas flavonoids and proanthocyanidins demonstrated inhibitory activity at 0.33 mg/ml using this test system.     

Monoterpene and lignan glycosides in the leaves of Crataegus pinnatifida

In the present phytochemical study on the leaves of Crataegus pinnatifida, a new monoterpene glycoside, (3S,5R,6R,7E,9R)-3,6-epoxy-7-megastigmen-5,9-diol-9-O-β-Dglucopyranoside(6) and a new sesquilignan glycoside, acernikol-4’’-O-β-D-glucopyranoside (15), together with thirteen known compounds were isolated.     

Food acceptance by a monophagous and an oligophagous insect in relation to seasonal changes in host plant suitability

Food acceptance by larvae of two lepidopteran species feeding on Rosaceae, viz. Yponomeuta evonymellus (monophagous) and Y. padellus (oligophagous), was compared. The influence of seasonal changes in plants as food for both insects was examined, in particular, the effects of nitrogen and sorbitol in leaves. In the laboratory, Y. evonymellus accepts Crataegus monogyna, a host plant of Y. padellus, and Y. padellus accepts Prunus padus, the host plant of Y. evonymellus. P. padus is the most suitable food plant for Y. evonymellus. No difference in food-quality for Y. padellus was found between C. monogyna and P. padus. The performance of both species on P. padus is less influenced by seasonal changes than on Crataegus. The suitability of Crataegus decreases during the season. This is probably caused by the decrease of its nitrogen content, and not by the decrease of sorbitol in the plant. The monophagous, Y. evonymellus, is more sensitive to seasonal changes in its food when fed with a non host plant than the oligophagous Y. padellus. In oviposition experiments both species have a preference for their normal host-plants.     

Latitudinal variation in the fruiting phenology of a bird-dispersed plant (shape Crataegus monogyna) in Western Europe

A number of fleshy-fruit-bearing plants of temperate regions are dispersed by migratory frugivorous birds. It has been suggested that the more southerly populations of such species should produce ripe fruits later than more northerly populations, to ensure that fruit is available when the birds arrive. I will call this the adaptive delay hypothesis. To test this hypothesis, I monitored fruiting phenology of Crataegus monogyna Jacq. at ten sites (in all of which fruit consumption is very largely by redwings, Turdus iliacus, and fieldfares, Turdus pilaris) between northern Spain (42° N) and northern Scotland (59° N). There was no negative correlation between latitude and date of fruit ripening (earliest recorded date on which ripe fruits had appeared, or earliest recorded date by which all fruits had ripened). My results thus argue against the adaptive delay hypothesis.     

云南山楂果化学成分的研究

从云南山楂的果实中分得10个化物,经光谱分析及化学反应分别鉴定为槲皮素(Ⅰ)、芦丁(Ⅱ)、牡荆素(Ⅲ)、金丝挑甙(Ⅳ)、胡萝卜甙(Ⅴ)、熊果酸(Ⅵ)、氯原酸(Ⅶ)、奎宁酸(Ⅷ)、β-谷甾醇(Ⅺ)及二十九烷醇(Ⅹ)。