Intestinal antispasmodic effects of Helichrysum italicum (Roth) Don ssp. italicum and chemical identification of the active ingredients

Ethnopharmacological relevance

In the Mediterranean Area, the flowers of Helichrysum italicum ssp. italicum are a traditional remedy for the treatment of intestinal complaints and are used as herbal tea for curing digestive, stomachic and intestinal diseases. In order to find scientific evidence for the traditional utilization of this plant, the effect of an ethanolic extract of Helichrysum italicum was investigated by using in vivo and in vitro experimental models. Then, through bioassay-guided fractionation procedures, active component(s) were identified.

Material and methods

Contractility in vitro was evaluated by stimulating the isolated ileum, in an organ bath, with acetylcholine and barium chloride; motility in vivo was evaluated by measuring upper gastrointestinal transit, both in control mice and in mice with experimental intestinal inflammation induced by croton oil. Chromatographic separation techniques such as HPLC and silica gel columns have yielded the active principles of Helichrysum italicum.

Results

We found that the ethanolic extract of Helichrysum italicum ssp. italicum flowers elicited antispasmodic actions in the isolated mouse ileum and inhibited transit preferentially in the inflamed gut. A bioassay guided fractionation of the extract yielded the known compounds 12-acetoxytremetone (1) and 2,3-dihydro-2-[1-(hydroxymethyl)ethenyl]-5-benzofuranyl]-ethanone (2).

Conclusion

Present study supported the traditional use of Helichrysum italicum ssp. italicum flowers for intestinal complaints and through bioassay-guided fractionation procedures from the crude extract we showed that 12-acetoxytremetone (1) and 2,3-dihydro-2-[1-(hydroxymethyl)ethenyl]-5-benzofuranyl]-ethanone (2) acted in a synergistic way to produce an intestinal antispasmodic effect.     

Mycology,cultivation, traditional uses,phytochemistry and pharmacology of Wolfiporia cocos (Schwein.) Ryvarden et Gilb.: A review

Ethnopharmacological relevance

Wolfiporia cocos (Schwein.) Ryvarden et Gilb. has a long history as a Chinese traditional medicine with uses of inducing diuresis, excreting dampness, invigorating the spleen, and tranquilizing the mind. Recently, Wolfiporia cocos has received increasing interest, and phytochemical and pharmacological studies have validated the traditional uses of this species.

Aims of the review

To provide an up-to-date and comprehensive overview of the mycology, cultivation, traditional uses, chemical constituents and pharmacological activities aspects of Wolfiporia cocos in order to highlight its ethnopharmacological use and to explore its therapeutic potentials and to provide a basis for future research.

Materials and methods

The accessible literature, from 1980 to 2012, on Wolfiporia cocos written in English, Chinese, French, Korean, Spanish and Turkish were selected and analyzed.

Results

The phytochemical and modern pharmacological studies demonstrated that Wolfiporia cocos possess a wide spectrum of pharmacological activities, such as anti-tumor, anti-oxidant, anti-rejection, nematicidal, anti-hyperglycemic, antibacterial, anti-inflammatory and anti-hypertonic stress activities, which could be explained by the presence of various triterpenes and polysaccharides.

Conclusions

Modern phytochemical and pharmacological investigations showed that major active components separated from Wolfiporia cocos had anti-tumor, anti-oxidant, anti-rejection activities, and so on. Further investigations are needed to explore the relationship of the molecular mass, chain stiffness, and water solubility of polysaccharide from Wolfiporia cocos with the antitumor activities.     

Semen Astragali Complanati: An ethnopharmacological,phytochemical and pharmacological review

Ethnopharmacological relevance

Semen Astragali Complanati (SAC), the dried ripe seed of Flatstem Milkvetch (Astragalus complanatus Bunge) (Leguminosae), is commonly used in traditional Chinese medicine (TCM) for treating muscle, liver, kidney, blood, skin and reproductive system diseases.

Materials and methods

Relevant information about SAC was gathered via “Google Scholar”, “ISI Web of Knowledge”, “PubMed”, “ScienceDirect”, “Medline Plus”, “ACS”, “CNKI” and “Wiley Online Library” and from books in local libraries.

Results

The major contents of SAC include fatty acids, amino acids, polysaccharides, flavonoids, triterpene glycosides and trace elements. Previous scientific studies have reported that SAC exhibits a number of therapeutic effects on chronic diseases such as cardiovascular diseases, diabetes mellitus and cancers. It has been found that flavonoids are the main bioactive component in SAC. However most of the previous studies have shown the effects brought by the total flavonoid fraction extracted from SAC only; further studies are warranted for the biological effects produced by individual components. There are only a few studies on the toxicity of SAC and the overall results show that its toxicity is quite low or even non-existent.

Conclusions

SAC is a valuable TCM herb with multiple pharmacological effects for treating some chronic diseases. More studies on SAC will help us to have a better understanding of its pharmacological mechanisms so as to provide more scientific evidence to explain its traditional uses, identify its therapeutic potential on other diseases and understand its possible harmful effects. Based on previous studies, it is easy to identify that antioxidant effect of SAC might play an important role on its pharmacological effects. Studying the effects of SAC on handling intracellular reactive oxygen species may be a potential direction to help understanding the molecular mechanisms of SAC on preventing and/or treating chronic diseases.     

Antispasmodic effects and composition of the essential oils from two South American chemotypes of Lippia alba

Ethopharmacology relevance

Lippia alba (Mill.) N. E. Brown (Verbenaceae) is an aromatic species used in Central and South America as eupeptic for indigestion. In Argentina, it is used by the “criollos” from the Chaco province. There are several chemotypes which differ in the chemical composition of the essential oils. Nowadays, it is experimentally cultivated in some countries of the region, including Argentina.

Aim of the study

To compare the chemical composition and pharmacology of the essential oils from two chemotypes: “citral” (CEO) and “linalool” (LEO), in isolated rat duodenum and ileum. Methods: Contractile concentration–response curves (CRC) of acetylcholine (ACh) and calcium in 40 mM K⁺-medium (Ca²⁺-CRC) were done in isolated intestine portions, in the absence and presence of CEO or LEO at different concentrations.

Results

Likewise verapamil, CEO and LEO induced a non-competitive inhibition of the ACh-CRC, with IC₅₀ of 7.0±0.3 mg CEO/mL and 37.2±4.2 mg LEO/mL. l-NAME, a NO-synthase blocker, increased the IC₅₀ of CEO to 26.1±8.7 mg CEO/mL. Likewise verapamil, CEO and LEO non-competitively inhibited the Ca²⁺-CRC, with IC₅₀ of 6.3±1.7 mg CEO/mL, 7.0±2.5 mg LEO/mL and 0.24±0.04 mg verapamil/mL (pIC₅₀: 6.28). CEO was proved to possess limonene, neral, geranial and (−)-carvone as the major components, while LEO was rich in linalool.

Conclusions

Results suggest that CEO has five times more potency than LEO to inhibit muscarinic contractions. The essential oils of both chemotypes interfered with the Ca²⁺-influx, but with an IC₅₀ about 28 times higher than that of verapamil. Moreover, CEO partially stimulated the NO production. These results show the medicinal usefulness of both Lippia alba chemotypes, thus validating its traditional use, potency and mechanism of action.     

Pharmacokinetics and tissue distribution of resveratrol,emodin and their metabolites after intake of Polygonum cuspidatum in rats

Ethnopharmacological relevance

The rhizome of Polygonum cuspidatum SIEB. et ZUCC. (Polygonaceae, PC), a widely used Chinese medicine, is commonly prescribed for the treatments of amenorrhea, arthralgia, jaundice, abscess, scald and bruises.

Aim of the study

PC contains various polyphenols including stilbenes, anthraquinones and flavonoids. This study investigated the pharmacokinetics and tissue distribution of emodin and resveratrol in PC.

Material and methods

Male Sprague-Dawley rats were orally administered PC (2 and 4 g/kg) and blood samples were withdrawn at the designed time points via cardiopuncture. Moreover, after 7-dose administrations of PC (4 g/kg), brain, liver, lung, kidney and heart were collected. The concentrations of resveratrol and emodin in the plasma and tissues were assayed by HPLC before and after hydrolysis with β-glucuronidase and sulfatase.

Results

The glucuronides/sulfates of emodin and resveratrol were exclusively present in the plasma. In liver, kidney, lung and heart, the glucuronides/sulfates of resveratrol were the major forms. For emodin, its glucuronides/sulfates were the major forms in kidney and lung, whereas considerable concentration of emodin free form was found in liver. Neither free forms nor conjugated metabolites of resveratrol and emodin were detected in brain.

Conclusion

The sulfates/glucuronides of resveratrol and emodin were the major forms in circulation and most assayed organs after oral intake of PC. However, the free form of emodin was predominant in liver.     

Central nervous system effects and chemical composition of two subspecies of Agastache mexicana; an ethnomedicine of Mexico

Ethnopharmacological relevance

Agastache mexicana subspecies mexicana (Amm) and xolocotziana (Amx) are used in Mexican traditional medicine to relief cultural affiliation syndromes known as “susto” or “espanto”, for “nervous” condition, and as a sleep aid. Despite its intensive use, neuropharmacological studies are scarce, and the chemical composition of the aqueous extracts has not been described. Aims of the study are: (1) To analyze the chemical composition of aqueous extracts from aerial parts of Amm and Amx. (2) To evaluate the anxiolytic-like, sedative, antidepressant-like effects. (3) Analyze the general toxic effects of different doses.

Materials and methods

Anxiolytic-like and sedative effects were measured in the avoidance exploratory behavior, burying behavior and the hole-board tests. The antidepressant-like actions were studied in the forced swimming and tail suspension tests. Finally, general activity and motor coordination disturbances were evaluated in the open field, inverted screen and rota-rod tests. The acute toxicity of Amm and Amx was determined by calculating their LD₅₀ (mean lethal dose). The chemical analyses were performed employing chromatographic, photometric and HPLC–ESI-MS techniques.

Results

Low doses of Amm and Amx (0.1σ1.0 mg/kg) induced anxiolytic-like actions; while higher doses (over 10 mg/kg) induced sedation and reduced the locomotor activity, exerting a general inhibition in the central nervous system (CNS).

Conclusions

Results support the use of Amm and Amx in traditional medicine as tranquilizers and sleep inducers. Additionally, this paper contributes to the knowledge of the chemical composition of the aqueous extracts of these plants.     

Studien zum Lingshu als Beitrag zur Bewertung klinischer Akupunkturstudien: – Punktlokalisation,Stichtiefe, De Qi

Background

Clinical trials on acupuncture use a variety of control methods, such as sham acupuncture, minimal acupuncture, and placebo. Frequently, needle insertion on non-classical acupuncture points (“minimal acupuncture”) is employed for this purpose. The aim of such clinical trials is to evaluate specific effects of acupuncture. There is a controversial discussion regarding the appropriateness of comparing “true” acupuncture to “minimal acupuncture”.Minimal and verum acupuncture are distinguished by various criteria, such as “localisation”, “depth of needle insertion”, and “induction of de qi”.

Aim

This study is dedicated to the question of what information the Huang Di Neijing, specifically the Lingshu-compilation which extensively focuses on needling techniques, has to offer regarding the above mentioned criteria, and their importance for successful acupuncture. In relation to this, it will be discussed if the definition of “minimal acupuncture” as used in the German Acupuncture Trials, is feasible.

Methods

The entire original text of the Huang Di Neijing Lingshu was searched for information regarding “point localisation”, “insertion depth”, and “induction of “de qi”. The paragraphs in question were compiled and probed on statements regarding the efficacy of treatment. These subsequently were compared to the technique of “minimal acupuncture” as in the German Acupuncture Trials (ART, GERAC).

Results

The analysis of the Lingshu shows that neither a specific point localisation, nor a certain insertion depth or the induction of de qi are clearly and in all cases relevant for a successful therapy. Rather, the Lingshu offers specific indications for superficial needling. Sites of acupoint localisation aren't clearly defined and the induction of de qi is not understood as mandatory for a successful therapy.

Conclusion

The criteria distinguishing „verum acupuncture” from „minimal acupuncture” as practiced in many clinical trials don't correspond to the early practice of acupuncture as documented in the Lingshu. This can be a possible explanation for the good clinical results of minimal acupuncture in a number of clinical trials.However, for further discussions of this problem the developments and the clinical evolution present-day acupuncture has undergone since the ancient times have to be held in account.     

Evaluation of the wound healing potential of Wedelia trilobata (L.) leaves

Ethnopharmacological relevance

Wedelia trilobata (L.) Hitchc (Asteraceae) leaves are used in the treatment of wounds by traditional healers. Despite the use of this plant in wound healing, there is a scarcity of scientific data to support its therapeutic application.

Aim of the study

To investigate the wound healing potential of Wedelia trilobata (L.) leaves commonly employed by traditional healers and to clarify its traditional use in a scientific investigation.

Materials and methods

An ethanolic extract of Wedelia trilobata leaves was subjected to column chromatography. Hexane, ethyl acetate (WEA) and chloroform:methanol (50:50) (WCM) fractions were obtained. The fractions were tested using relevant in vitro wound healing assays. Antioxidant activity was measured by the DPPH assay. The fibroblast proliferation, oxidative stress using hydrogen peroxide, an in vitro scratch assay, and increasing collagen content was determined using fibroblast L929. Minimum inhibitory concentrations (MICs) were determined against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, and Pseudomonas aeruginosa.

Results

WEA (3 μg/mL) promoted fibroblast L929 survivability up to more than 90% before and more than 85% after hydrogen peroxide induced oxidative stress. WEA (3 μg/mL) induced a 70% migration rate in the in vitro scratch assay and the collagen content was increased to 261 μg/mL compared to the control (57.5 μg/mL). WCM exhibited a scavenging activity for DPPH with an IC₅₀ value of 179.5 μg/mL comparable to BHT (139.3 μg/mL). WEA was active against Gram positive bacteria Staphylococcus aureus, Staphylococcus epidermidis with MIC values of 62.5 and 31.25 μg/mL, respectively.

Conclusion

These scientific findings of wound healing activity supports the traditional claims for Wedelia trilobata (L.) leaves. The WEA displayed antibacterial and fibroblast stimulatory activities while WCM exhibited antioxidant to indicate its potential wound healing properties. However further studies to isolate the antibacterial, antioxidant and fibroblast stimulatory compounds that contribute to the wound healing properties of this plant are needed.