药用金钮扣属植物研究综述

植物药在人类的医学实践中已有上千年的应用历史,特别是在亚洲的一些国家,植物药用资源被认为是一种可以随时取用的宝贵的医疗保健资源。印度拥有众多种类的药用植物,然而,其中很大一部分传统药用植物并没有被开发使用或未被现代医学科学研究证明其功效。因此,目前很有必要开发传统药用植物并使其最大限度地造福人类。本篇综述总结报道了一种很有潜力的药用植物即金钮扣属植物。过去几年中,很多从这类植物中提取的新化合物及其功效已经得到证实,因此本文旨在总结最新的有关金钮扣属植物的植物化学及民族药物学应用、药理学作用及物种保护方法的科学研究报道。     

LC–MS profiling of N-alkylamides in Spilanthes acmella extract and the transmucosal behaviour of its main bio-active spilanthol

N-Alkylamides are a promising group of naturally occurring bio-actives, with evidence for immune stimulating properties, which find applications i.a. in buccal preparations. In Spilanthes extracts, these properties are mainly ascribed to the most abundant N-isobutylamide, spilanthol. Yet, other N-alkylamides present in these extracts may contribute to this effect, as well as to its potential toxicity and physiologic interactions. Therefore, N-alkylamide profiling of an ethanolic Spilanthes extract was performed using a gradient reversed phase high performance liquid chromatography/electrospray ionization ion trap mass spectrometry (HPLC/ESI-MS) method on an embedded polar column. MS¹ and MS² fragmentation data were used for identification purposes. Moreover, the transmucosal behaviour of spilanthol, formulated in this ethanolic extract and in two commercially available oral gels, was evaluated using porcine buccal mucosa in a Franz diffusion cell experimental set-up. A high-throughput HPLC-UV method was used for the quantification of spilanthol in the receptor phase. Fundamental permeation characteristics of spilanthol in a solvent-independent way (100% aqueous dose solution) were obtained using different propylene glycol/water ratios.     

Effects of herbal products and their constituents on human cytochrome P4502E1 activity

Ethanolic extracts from fresh Echinacea purpurea and Spilanthes acmella and dried Hydrastis canadensis were examined with regard to their ability to inhibit cytochrome P450_2E1 mediated oxidation of p-nitrophenol in vitro. In addition, individual constituents of these extracts, including alkylamides from E. purpurea and S. acmella, caffeic acid derivatives from E. purpurea, and several of the major alkaloids from H. canadensis, were tested for inhibition using the same assay. H. canadensis (goldenseal) was a strong inhibitor of the P450_2E1, and the inhibition appeared to be related to the presence of the alkaloids berberine, hydrastine and canadine in the extract. These compounds inhibited 2E1 with K_I values ranging from 2.8 μM for hydrastine to 18 μM for berberine. The alkylamides present in E. purpurea and S. acmella also showed significant inhibition at concentrations as low as 25 μM, whereas the caffeic acid derivatives had no effect. Commercial green tea preparations, along with four of the individual tea catechins, were also examined and were found to have no effect on the activity of P450_2E1.     

金钮扣不同提取物止咳化痰作用研究

目的:研究金钮扣不同提取物的止咳、化痰作用。方法:金钮扣用95%乙醇回流提取得到醇提取物,加水溶解后依次用石油醚、氯仿、乙酸乙酯、正丁醇萃取,浓缩得相应的萃取物和水相溶解部位。采用豚鼠枸橼酸引咳法、小鼠气管酚红法,观察金钮扣不同提取物的止咳、化痰作用。结果:金钮扣醇提取物组、乙酸乙酯组、正丁醇组和空白对照组的咳嗽潜伏期分别为133.5、138.4、137.1、87.8s,咳嗽次数分别为7、8、8和16次,酚红分泌量分别为1.031、1.014、1.262、0.656μg;醇提取物组、乙酸乙酯组和正丁醇组的咳嗽潜伏期延长、咳嗽次数减少、酚红分泌量增加,与空白对照组比较均具有显著性差异(P<0.01或P<0.05)。石油醚组、氯仿组和水溶部分组的咳嗽潜伏期、咳嗽次数及酚红分泌量,与空白对照组比较均无显著性差异。结论:金钮扣醇提取物止咳和化痰作用的有效成分主要集中在乙酸乙酯和正丁醇萃取部位。     

Antihepatotoxic Activity of Spilanthes ciliata

Abstract

The ethanol extract of the whole plant of Spilanthes ciliata was screened for its hepatoprotective effects in Wistar rats. A significant hepatoprotective effect was obtained against paracetamol-induced hepatic damage as evident from decreased levels of serum enzymes and an almost normal histological architecture of the liver, following treatment with the plant extract prior to paracetamol overdose-induced liver damage. The extract was also effective in increasing the choleretic activity of anaesthetized normal rats. The extract shortened hexobarbitone-induced sleeping time in mice, which was increased by carbon tetrachloride (CCl₄) treatment, besides showing significant antilipid peroxidant effects in vitro.     

金纽扣的显微结构研究

对金纽扣的显微结构进行了研究。结果表明，金纽扣的显微结构鉴别特征为：根部次生构造不发达，皮层裂隙较多，维管束辐射型，根横切面观细胞壁普遍较厚；茎中内皮层凯氏点明显，髓部大，中央破裂呈空洞状，周围有若干裂隙；粉末中可见花粉粒，球型，有刺状雕纹。     

Skin penetration enhancing properties of the plant N-alkylamide spilanthol

Ethnopharmacological relevance

Plants are often used for skin diseases in different ethnopharmacological systems. Local and systemic effects of topically applied compounds can be significantly increased by plant constituents having skin penetration enhancers.

Materials and methods

In this study, we examined the proposed penetration enhancing properties of spilanthol, an N-alkylamide abundantly present in several Asteraceae plants like Spilanthes acmella L., on three model drugs (caffeine, testosterone and ibuprofen). Moreover, as plants are frequently contaminated with toxic environmental substances, the mutual influence on the transdermal behavior between spilanthol and six model mycotoxins (aflatoxin B1, ochratoxin A, fumonisin B1, citrinin, zearalenone, T-2 toxin) was investigated.

Results

Spilanthol exhibits component and concentration dependent penetration enhancing effects. No significant penetration enhancing effect for ibuprofen has been observed, but with increasing spilanthol concentration (from 0 up to 1 w/V%), the permeability of caffeine increased, resulting in an enhancing ratio (ER) of 4.60. For testosterone, a maximal penetration enhancing concentration of 0.5% spilanthol was found (ER=4.13). Next to its beneficial applicability to increase local as well as systemic pharmacological effects of dermally co-administrated drug, this N-alkylamide negatively influences human health risk if spilanthol containing formulations are polluted with mycotoxins: the presence of spilanthol (0.3 w/V%) induced a significant increase of permeability coefficient K_p of five investigated mycotoxins, with ER values ranging between 1.57 and 6.37. On the other hand, mycotoxins themselves do not significantly influence the transdermal behavior of spilanthol.

Conclusions

The existence of a significant mutual influence of compounds towards skin penetration should always be considered during the development or as part of the functional quality evaluation of topical products.     

Antiulcerogenic effect of Croton urucurana Baillon bark

Ethnopharmacological relevance

Elephantopus mollis, Spilanthes africana, Urena lobata, Momordica multiflora, Asystasia gangetica and Brillantaisia ovariensis are used in Cameroonian traditional medicine for the treatment of bone diseases and fracture repair. The aim of this study was to evaluate the effect of ethanolic extracts of six Cameroonian medicinal plants on bone regeneration following bone and marrow injury.

Materials and methods

Ethanol extract of Cameroonian medicinal plants were administered (each extract at 250, 500 and 750 mg/kg doses) orally to adult female Sprague–Dawley rats having a drill hole injury (0.8 mm) in the femur diaphysis. Vehicle (gum-acacia in distilled water) was given to the control group. After 12 days of treatment, animals were euthanized and femur bones collected. Confocal microscopy of fractured bone was performed to evaluate bone regeneration (calcein labeling). Only active plant extracts were used for further experiments. Thus, callus was analyzed by microcomputed tomography. Osteogenic effects of the extracts were evaluated by assessing mineralized nodules formation of bone marrow stromal cells and osteoblast recruitment at drill hole site by immunohistochemistry.

Results

Ethanolic extract of the leaves and twigs of Elephantopus mollis (EM) and whole plant of Spilanthes africana (SA) dose-dependently stimulated bone regeneration at the drill hole site. EM at 250 and 750 mg/kg doses and SA at 750 mg/kg dose significantly increased mineral deposition compared to controls. Both extracts at 500 and 750 mg/kg doses improved microarchitecture of the regenerating bone evident from increased bone volume fraction, trabecular thickness, trabecular number, and decreased trabecular separation and structure model index. EM and SA extracts increased the formation of mineralized nodules from the bone marrow stromal cells. In addition, EM and SA extracts increased osteoblast recruitment at the drill hole site evident from increased Runx-2 positive cells following their treatments compared to control.

Conclusion

Ethanolic extracts of EM and SA accelerate fracture repair in rats via stimulatory effects on osteoblast differentiation and mineralization, thereby justifying their traditional use.     

Preliminary studies on local anesthetic and antipyretic activities of Spilanthes acmella Murr. in experimental animal models

Objective:

Spilanthes acmella Murr. (Family: Compositae) is a herb that grows throughout the tropics. It is used in the treatment of rheumatism, fever, sore throat, and hemorrhoids. A tincture of the flowers is used to relieve toothache. The leaves and flowers produce numbness of the tongue when eaten as salad. The present study was undertaken to evaluate the local anesthetic and antipyretic activities of S. acmella in experimental animal models.

Materials and Methods:

Aqueous extract of S. acmella Murr. (SAM) was tested for local anesthetic action by (i) intracutaneous wheal in guinea pigs and (ii) plexus anesthesia in frogs. In both the models, 2% xylocaine was used as the standard drug. The anti-pyretic activity was determined by yeast-induced pyrexia in rats. Aspirin 300 mg/kg was used as the standard drug.

Result:

The test drug in concentrations of 10% and 20% produced 70.36% and 87.02% anesthesia respectively by the intracutaneous wheal compared to 97.22% anesthetic effect produced by 2% xylocaine (P<0.001). The mean onset of anesthesia with the test drug was 5.33±0.57 min compared to 2.75±0.31 min (P<0.001) for the standard drug in the plexus anesthesia model. In the anti-pyretic model, ASA in doses of 100, 200, and 400 mg produced dose-dependent reduction in mean temperature at various hours of observation.

Conclusion:

The present study shows that SAM has significant local anesthetic and antipyretic activities.     

Antiobesity properties of two African plants (Afromomum meleguetta and Spilanthes acmella) by pancreatic lipase inhibition

Ethanol extracts of seeds of Afromomum meleguetta and flower buds of Splilanthes acmella presented pancreatic lipase inhibitory activities in a concentration related manner under in vitro conditions. The two plants were extracted with 70% ethanol by sonication, fractionated on silica gel and tested at concentrations in the range 0.75-2.0 mg/mL. Lipase inhibitory activities of 90% and 40% were observed in A. meleguetta and S. acmella, respectively. The two plants have potentials as candidates for weight reduction and obesity control.