Article

Eleutherococcus senticosus as a crude medicine: Review of biological and pharmacological effects

Authors:
To read the full-text of this research, you can request a copy directly from the authors.

Abstract

Eleutherococcus senticosus (Rupr. et Maxim.) Harms (Acanthopanax senticosus, Araliaceae, ES, thereafter), also called Siberian ginseng, Ciwujia in Chinese, and Gasiogalpi in Korea, is distributed in the southeastern Russia, northeast China, Korea, and Japan. The woody medicinal plant has been known since ancient times for its curative properties, and particularly the cortical roots and stem tissues of ES have been utilized for the treatment of various ailments such as cancer, diabetes, cardiovascular diseases, hepatitis, spleen and liver complaints. Due to its giant therapeutic efficacy, more and more investigations have been carried out on the isolation and analysis of active compounds of ES, and their in vitro and in vivo pharmacological activities and even clinical effects in humans. This review, therefore, provides a comprehensive review of the pharmacologically relevant compounds of ES characterized so far and of the studies supporting its use as a medicinal plant. Particular attention has been given to anti-inflammatory, anti-oxidative, anti-carcinogenic, anti-fatigue, anti-diabetes, hypolipide, immunoprotection and immunoregulation, and antimicrobial and antiviral activities. This work presented here would help more detailed pharmacological cognition and further understanding of natural components of this medicinal plant species.

No full-text available

Request Full-text Paper PDF

To read the full-text of this research,
you can request a copy directly from the authors.

... The 1994 DSHEA (Dietary Supplement Health and Education Act) regulation allows a direct commercialization of ES as a supplement for consumption in the United States without the regulation of the FDA (Food and Drug Administration) [11]. ...
... The extracts from different parts of ES have been considered good for health [21]. The ES antioxidant effect is related to improvements in the treatment of diabetes, cancer and inflammatory state, in addition to their immunoregulatory and immunomodulatory property, and antimicrobial and antiviral activity [11]. ...
... The study by Rhie and Won (2004) [22] demonstrated the potent effect on body weight gain of mice treated with ES, which was significantly reduced, besides demonstrating a significant reduction in the plasmatic cholesterol concentration. One hypothesis for this important effect in reducing weight could be explained by the action of ES on glucose and insulin metabolism [20], besides the effect of lower concentrations of corticosterone in rats [11,23]. ...
Article
Full-text available
Ginseng is one of the most popular herbal sup-plements in the world. It is a plant widely used in folk and traditional medicines for cardiovascular, immune, nervous and endocrine systems, and according to the researchers, it has the ability to increase the non-specific resistance state, which characterizes it as an adaptogenic substance. There are different species of ginseng, such as the American, Chinese, Korean and Japanese ginseng; the Korean species (Panax ginseng) is being used for thousands of years as a tonic, prophylactic and "restorative" agent, with power-ful antioxidant properties. For a long time, its use was empirical, because people used to beli-eve that it was a panacea that promoted longe-vity, with beneficial effects for the treatment of physical fatigues. Nowadays, the active compo-nents of Eleutherococcus senticosus are well described, however, there are no data on the quantity of a certain class of these secondary compounds produced in each species. Although the Eleutherococcus senticosus extract may con-tain several substances, including vitamins, mi-nerals, cellulose, and ethanol, the substances responsible for inducing various physiological responses are the eleutherosides (in the root) and ciwujianosides (in the leaf). As Eleutheroco-ccus senticosus receives great attention by show-ing that its active components can provide protec-tion against oxidative stress, among other bene-fits, contributing to health and the prevention and treatment of diseases, such as diabetes, can-cer, cardiovascular disease and inflammation. The purpose of this article is to describe the main, adverse and toxicological effects of Eleuthero-coccus senticosus recently related in the litera-ture.
... Abbreviations 2 4-D 2, 4-Dichlorophenoxy acetic acid C 2 H 4 Ethylene CO 2 Carbon dioxide DW Dry weight FW Fresh weight GA 3 Gibberellic acid MJ Methyl jasmonate MS medium Murashige and Skoog medium O 2 Oxygen vvm Air volume per medium volume per minute ...
... 4-D 2, 4-Dichlorophenoxy acetic acid C 2 H 4 Ethylene CO 2 Carbon dioxide DW Dry weight FW Fresh weight GA 3 Gibberellic acid MJ Methyl jasmonate MS medium Murashige and Skoog medium O 2 Oxygen vvm Air volume per medium volume per minute ...
... 4-D 2, 4-Dichlorophenoxy acetic acid C 2 H 4 Ethylene CO 2 Carbon dioxide DW Dry weight FW Fresh weight GA 3 Gibberellic acid MJ Methyl jasmonate MS medium Murashige and Skoog medium O 2 Oxygen vvm Air volume per medium volume per minute ...
Article
Eleutherococcus senticosus (Rupr. & Maxim.) Maxim (Acanthopanax senticosus), popularly known as 'Siberian ginseng', is a woody medicinal plant which is used in traditional medicine as an adaptogen. It is marketed throughout the world as a health supplement. The major active ingredients are lignan glycosides called eleutherosides. Efforts have been made recently to produce bioactive compounds from suspension cultures of somatic embryos. Bioreactor cultures have been established for the production of embryogenic biomass and bioactive compounds. In this review, we have presented bioreactor scale production of bioactive compounds and explained various bioprocess strategies for the production of eleutheroside B, E, E1 and chlorogenic acid. © 2014 Springer Science+Business Media Dordrecht. All rights reserved.
... The active components of Scutellariae Radix are flavonoids; the three major flavonoids are baicalin and its aglycone baicalein, and wogonin. Eleutherococci Senticosi Cortex, also called 'Siberian Ginseng', has been reported to possess anti-oxidant, anti-diabetic, anti-fatigue, immunomodulating and anti-cancer effects 7) . It is rich in eleutherosides, especially eleutheroside B and E, compounds that are responsible for its diverse pharmacological activities 8) . ...
... Cortex have a long history of use in stroke prevention and therapy 9) and have been intensively studied as neuroprotective agents in a variety of experimental brain injury models 7,8,10) . Previously, our group found that Scutellariae Radix and Eleutherococci Senticosi ...
Article
Full-text available
Objectives : HT070 is a mixture of herbal extracts from root of Scutellaria baicalensis and stem bark of Eleutherococcus senticosus , which have long been used for stroke therapy in traditional Korean Medicine. The purpose of this study was to investigate the neuroprotective effects of HT070 on global cerebral ischemia and its potential mechanisms.Methods : Transient global cerebral ischemia was produced by 10 min of four-vessel occlusion (4-VO) in male Wistar rats. HT070 was administered orally at a dosage of 200 mg/kg twice at 0 and 90 min after reperfusion. Hippocampal neuronal damage was measured 7 days after reperfusion. To explore the potential mechanisms, we used hydrogen peroxide (H2O2)-induced rat pheochromocytoma (PC12) cells as an in vitro model. PC12 cells were pretreated with HT070 for 1 h and then exposed to 100 ?M H2O2 for 6 h in the presence of HT070. Cell viability was measured by MTT assay and the mRNA expression of Bax, Bcl-2, iNOS and COX-2 were measured by quantitative RT-PCR.Results : Oral administration of HT070 at a dose of 200 mg/kg significantly reduced neuronal death in the hippocampal CA1 region by 13.4% as compared to the vehicle-treated group. HT070 increased cell viability, reversed the down-regulated Bcl-2 mRNA level, and suppressed the up-regulated mRNA expressions of Bax, iNOS, and COX-2 in H2O2-treated PC12 cells.Conclusions : HT070 protects against delayed neuronal death after global cerebral ischemia and its neuroprotection properties might be attributed to the inhibition of mitochondrial apoptosis and ROS-generating enzymes.
... & Maxim.) Harms (Yan-Lin et al., 2011;Jia et al., 2020) amongst other traditions including Western Herbal Medicine, and is thought to restore vigor, improve general health, restore memory, promote appetite and increase longevity (European Medicines Agency, 2016). ES was first established as a medicinal plant officially in the Union of Soviet Socialist Republics (USSR) in 1962. ...
Article
Ethnopharmacological relevance Eleutherococcus senticosus (Rupr. et Maxim.) Maxim (ES) (syn. Acanthopanax senticosus (Rupr. & Maxim.) Harms) is a medicinal plant used in traditional medicine of Russian Far East and East Asia and known as an adaptogen – a category of herbal medicinal products which have non-specific inter-system anti-stress effects throughout the human body. ES was first established as a medicinal plant officially in the pharmacopeia of the Union of Soviet Socialist Republics (USSR) in 1962, and is currently recommended by the European Medicines Agency (EMA) to be prescribed to treat symptoms of asthenia such as fatigue and weakness. Aim of the review During the time of the USSR, a distinct research directive was undertaken on ES to examine substances which improve stamina and endurance, with over 1000 studies published. Due to security measures within the former USSR these papers were not accessible to the public and were never translated into English. This is the first study to make findings of the USSR studies on ES available to the international research and scientific community. Methods This study was an archival retrieval. References for studies were sought from printed journal and conference preceding’s publications, then located within library catalogues of three libraries in St Petersburg Russia. Eligibility criteria included human clinical trials examining the efficacy of ES in any condition, published in the Russian language in the Soviet Union. Results A total of 46 studies published between 1962 and 1986 in the USSR were sourced. Of the retrieved articles, 29 were reported as placebo-controlled trials, 11 were reported as controlled trials and six studies did not report the study design. Trends in studies were those reporting on healthy volunteers (n=21) at a dose of 2 ml extract/day (n=14) examining outcomes such as physical and mental stamina under varying conditions, normal work conditions, high temperatures and high altitudes, incidence or prophylaxis of colds and influenza (n=5), effects on color perception and vision (n=2), work capacity (n=1), cognitive effects (n=1), prophylaxis of hearing loss (n=3), effects on blood cell counts (n=2) and sensitivity to UV radiation (n=1). Conclusions ES appears to exhibit benefits for cognitive function and physical and mental endurance and its effect as a respiratory system infection prophylaxis treatment are promising. This study is the first to publish the findings of clinical trials on ES from the USSR, which supports the traditional use and offers a valuable contribution to the body of evidence on medicinal uses of ES when the data is applied within the context of its limitations.
... In the extract of Siberian ginseng, saponins, lignans, triterpenoid, coumarins, and flavones. Phenolic compounds such as eleutheroside E and syringin have been reported to have a variety of medicinal anti-leishmania, anti-gout, antihyperglycemic, anti-hepatitis, immunostimulatory, effects concerning antibacterial, anticancer, anti-inflammatory, haemostatic, hypocholesterolemic effects and antioxidant activity [2][3][4]. ...
Article
Full-text available
Objective: This study was examined to in vitro antioxidant activity and Total Phenol and Flavonoids content analysis of methanolic root extract of Eleutherococcus senticosus (Siberian ginseng). Methods: 1,1-dephenyl-2-picryl-hydrazyl free radical scavenging and FRAP assay propose that antioxidant activity of methanol root extract because of reducing capacity of the antioxidant against oxidative effects of reactive oxygen species. Results: Scavenging activity of Siberian ginseng root RC50 value was shown 713.42±11.55 µg/ml and reducing power 0.13±0.01 mmol/g was investigated. In addition, total phenol 12.6±1.13 mg GAE/g DW and total flavonoids 9.8±0.20 mg QE/g DW were recorded. Conclusion: Although all tests were performed in vitro assay, these results recommend that Siberian ginseng root may be a good source of antioxidant ingrediant.
... Magazine, Volume 13, Issue 50, April-June, 2017 Eleutherococcus senticosus (Araliaceae) P6919/Roots Glycans: Eleutherans A, B, C, D, E, F, and G, eleutheroside C Lignans and their glycosides: sesamine, eleutheroside D Triterpene saponins: eleutheroside I, K, L, and M Sinapaldehyde glucoside, coniferaldehyde glucoside, coniferin, 1,5-di-O-caffeoylquinic acid, 3' ,5'-O-dicaffeoylquinic acid, 4' ,5'-O-dicaffeoylquinic acid eleutheroside E2, isomaltol 3-O-αglucopyranoside. [62] Lonicera confusa (Caprifoliaceae) P6880/ Wood Flavonoids: Rutin, quercetin, luteolin-7-O-β-D-galactoside, lonicerin, tricin, tricin-7-O-β-Dglucopyranoside, chrysoeirol-7-O-neohesperidoside, and tricin-7-O-neohesperidoside. ...
Article
Background: Herbal medicine is widely used all over the world for treating various health disorders. It is employed either alone or in combination with synthetic drugs or plants to be more effective. Objective: The assessment of the effect of both water and methanol extracts of 57 widely used plants from Traditional Chinese Medicine (TCM) against the main phase I metabolizing enzyme CYP3A4 in vitro for the first time. Materials and methods: The inhibition of cytochrome P450 activity was evaluated using a luminescence assay. The principal component analysis (PCA) was used to correlate the inhibitory activity with the main secondary metabolites present in the plant extracts. Molecular modeling studies on CYP3A4 (PDB ID 4NY4) were carried out with 38 major compounds present in the most active plant extracts to validate the observed inhibitory effect. Results: Aqueous extracts of Acacia catechu, Andrographis paniculata, Arctium lappa, Areca catechu, Bupleurum marginatum, Chrysanthemum indicum, Dysosma versipellis, and Spatholobus suberectus inhibited CYP3A4 is more than 85% (at a dose of 100 μg/mL). The corresponding methanol extracts of A. catechu, A. paniculata, A. catechu, Mahonia bealei, and Sanguisorba officinalis inhibited the enzyme by more than 50%. Molecular modeling studies revealed that two polyphenols, namely hesperidin and rutin, revealed the highest fitting scores in the active sites of the CYP3A4 with binding energies equal to -74.09 and -71.34 kcal/mol, respectively. Conclusion: These results provide evidence that many TCM plants can inhibit CYP3A4, which might cause a potential interference with the metabolism of other concomitantly administered herbs or drugs. Summary: In this study, the inhibitory activity of the aqueous and methanol extracts of 57 widely used plants from Traditional Chinese Medicine (TCM) against the main phase I metabolizing enzyme CYP3A4 was tested in vitro for the first time.Aqueous extracts of Acacia catechu, Andrographis paniculata, Arctium lappa, Areca catechu, Bupleurum marginatum, Dysosma versipellis, and Spatholobus suberectus inhibited CYP3A4 by more than 85% (at a dose of 100 μg/mL).The activity could be attributed to the presence of polyphenolics as revealed from the multivariate chemometric analysis and molecular modeling study.These results provide evidence that many TCM plants can inhibit CYP3A4, which might cause a potential interference with the metabolism of other concomitantly administered herbs or drugs. Abbreviation used: CHARMm: Chemistry at HARvard Macromolecular Mechanics, CYP: Cytochrome P450, DMSO: Dimethyl Sulfoxide, PCA: Principal Component Analysis, PDB: Protein Data Bank, TCM: Traditional Chinese Medicine.
... While ginsenosides (triterpenoid saponins of the plant) are con- sidered as the main bioactive ingredients of the Panax species, the active compounds in Siberian ginseng are eleutherosides which are believed to be potent compounds [4,5]. ...
Article
Ginseng has gained fame as one of the most popular herbs originating from Eastern countries. Among different species which are known as ginseng, Panax ginseng C. A. Mey. (Korean or Asian ginseng) is the most frequently used one. Ginsenosides have been proposed to account for most of the biological activities of ginseng. The widely appreciated health-promoting effect of ginseng pertains to the beneficial effects of this plant against immune, cardiovascular and sexual diseases and cancer. In addition, there are some new aspects of the pharmacological activity of this plant which justify its use in dermatologic diseases. In dermatology, ginseng has been investigated mechanistically for its therapeutic effects in photoaging, wound and injury, skin cancer, dermatitis, hair loss, alopecia and cold hypersensitivity. Here, we reviewed experimental and clinical studies exploring the therapeutic efficacy of ginseng and ginsenosides in the field of dermatology.
... It is considered to be an adaptogen and is chiefly exploited for strengthening the spleen and kidney. 10,11 Eleutherosides, the major bioactive compounds found in E. senticosus, are phenylpropanoids, lignin glycosides that occur abundantly in the roots and stems. 12 E. senticosus has been proven to possess anticancer, 13 antioxidant, and antimicrobial activities. ...
Article
Full-text available
Pharmacologically active stem of the oriental herbal adaptogen, Siberian ginseng, was employed for the ecofriendly synthesis of Siberian ginseng silver nanoparticles (Sg-AgNPs) and Siberian ginseng gold nanoparticles (Sg-AuNPs). First, for metabolic characterization of the sample, liquid chromatography-tandem mass spectrometry analysis (indicated the presence of eleutherosides A and E), total phenol content, and total reducing sugar were analyzed. Second, the water extract of the sample mediated the biological synthesis of both Sg-AgNPs and Sg-AuNPs that were crystalline face-centered cubical structures with a Z-average hydrodynamic diameter of 126 and 189 nm, respectively. Moreover, Fourier transform infrared analysis indicated that proteins and aromatic hydrocarbons play a key role in the formation and stabilization of Sg-AgNPs, whereas phenolic compounds accounted for the synthesis and stability of Sg-AuNPs. 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H tetrazolium bromide (MTT) assay determined that Sg-AgNPs conferred strong cytotoxicity against MCF7 (human breast cancer cell line) and was only slightly toxic to HaCaT (human keratinocyte cell line) at 10 µg·mL-1. However, Sg-AuNPs did not display cytotoxic effects against both of the cell lines. The disc diffusion assay indicated a dose-dependent increase in the zone of inhibition of Staphylococcus aureus (ATCC 6538), Bacillus anthracis (NCTC 10340), Vibrio parahaemolyticus (ATCC 33844), and Escherichia coli (BL21) treated with Sg-AgNPs, whereas Sg-AuNPs did not show inhibitory activity. In addition, the 2,2-diphenyl-1-picrylhydrazyl assay demonstrated that both Sg-AgNPs and Sg-AuNPs possess strong antioxidant activity. To the best of our knowledge, this is the first report unraveling the potential of Eleutherococcus senticosus for silver and gold nanoparticle synthesis along with its biological applications, which in turn would promote widespread usage of the endemic Siberian ginseng.
... +82 43 271 0413. E-mail: taekyung7708[at] effects concerning antibacterial, anticancer, anti-inflammatory, antioxidant, haemostatic, immunostimulatory, and hypocholesterolemic effects ( Huang et al., 2011;Lee and Shin, 2002;Sun et al., 2011). In addition, the seed's essential oil showed significant antioxidant activity and antimicrobial activity ( Bajpai et al., 2013aBajpai et al., , 2013b), indicating that Siberian ginseng has potential as a crude drug and a dietary health supplement. ...
Article
This study was designed to examine the in vitro antioxidant and antimicrobial activities of essential oil and crude methanolic (MeOH) extract of Eleutherococcus senticosus (common name, Siberian ginseng) fruit and its partitioned fractions, including hexane, ethyl acetate (EtOAc), n-butanol (BuOH) and aqueous. 1,1-dephenyl-2-picryl-hydrazyl free radical scavenging and reducing power assay suggest that antioxidant activity of EtOAc and BuOH fractions is due to the reducing ability of the antioxidant against oxidative effects of reactive oxygen species. In addition, the essential oil of Siberian ginseng fruit showed remarkable antimicrobial activity against Kocuria rhizophila (MIC = 125 μg/ml), Micrococcus luteus (MIC = 500 μg/ml), and Escherichia coli (MIC = 63 μg/ml). The chemical compositions of the essential oil obtained by the simultaneous steam-distillation and extraction method were analyzed using GC-MS; trans-caryophyllene (21.7%), humulene (7.4%), bicyclogermacrene (6.0%), (+) spathulenol (4.5%), germacrene-D (3.2%), tau-muurolol (2.5%) and delta-cadinene (2.3%) were found as main constituents. Furthermore, HPLC analysis identified ursolic acid as one of the principal components in Siberian ginseng fruit extract. Although this study has been carried out by in vitro assay, these results suggest that Siberian ginseng fruit may be a good candidate as a source of antioxidant and antimicrobial ingredients.
... As the Eleutherococcus species have wide pharmacological properties, there is a need to carry out research towards anti-leukemic properties. The abundance and variety of chemical compounds give a large hope for new drugs [10,[12][13]. ...
Article
Full-text available
The Eleutherococcus species including 40 species native to Asia are medicinal plants widely used in traditional medicine. Some of these species are cultivated at the botanical gardens in Europe. On the basis on our earlier studies it was concluded that the extracts of analyzed species act as antioxidants, inhibitors of MMPs, and cytotoxic against Jurkat 45 leukemia cell line. In this study, the anti-leukemic potential of roots and leaves from six Eleutherococcus species cultivated in Poland was determined. The in vitro cytotoxic activity towards human promyelotic leukemia cell line HL60 using trypan blue assay was evaluated. The induction of apoptosis in stimulated leukemia cells was determined by AnnexinV method. Morphological changes in treated cells were observed by microscopic investigations. The results showed that ethanolic extracts from the roots and the leaves of E. senticosus, E. setchuensis, E. sessiliflorus, E.gracilistylus, E. henryi and E. divaricatus exhibit cytotoxic effect towards leukemic HL60 cells. The received IC50 values for roots ranged from 49- 208 μg/mL and for the leaves from 116-518 μg/mL. The ethanol extract from the roots of E. divaricatus showed the highest cytotoxic and proapoptotic effect on HL60 human lymphoid leukemia cell line.
... It has been reported that ES has several active constituents, including lignans (sesamine, eleutheroside E), glycans (eleutherans, eleutheroside D), triterpene saponins 2 Evidence-Based Complementary and Alternative Medicine (eleutheroside I, K, L, and M), steroid glycosides (eleutheroside A), hydroxycoumarins (isoflaxidin), phenylacrylic acid derivatives (syringin), and flavones [7]. ...
Article
Full-text available
Eleutheroside E (EE), a principal component of Eleutherococcus senticosus (ES), has anti-inflammatory and protective effects in ischemia heart. However, it is unknown whether it ameliorates insulin resistance and reduces hyperglycemia in diabetes. This study investigated the effect of EE-containing ES extracts, as well as EE, on hyperglycemia and insulin resistance in db/db mice. EE increased the insulin-provoked glucose uptake in C2C12 myotubes. Moreover, EE improved TNF- α -induced suppression of glucose uptake in 3T3-L1 adipocytes. Five-week-old db/db mice were fed a diet consisting of ES extract or EE for 5 weeks. Both were effective in improving serum lipid profiles and significantly decreased blood glucose and serum insulin levels. ES and EE supplementation effectively attenuated HOMA-IR. Glucose tolerance and insulin tolerance tests showed that EE increased insulin sensitivity. Immunohistochemical staining indicated that ES and EE protected pancreatic alpha and beta cells from diabetic damage. In addition, ES and EE improved hepatic glucose metabolism by upregulating glycolysis and downregulating gluconeogenesis in obese type 2 diabetic mice. These data suggest that EE mediates the hyperglycemic effects of ES by regulating insulin signaling and glucose utilization. The beneficial effects of EE may provide an effective and powerful strategy to alleviate diabetes.
Article
Eleutherococcus senticosus (Rupr. & Maxim.) Maxim., popularly known as ‘Siberian ginseng’, is an important medicinal plant. Pharmacologically active compounds of this plant are called eleutherosides and among them, eleutheroside B is the most prevalent. The E. senticosus has been reported to have many medicinal properties however; very few studies are reported to understand the medicinal properties of eleutheroside B. Consequently, in the present study various computational tools have been used to predict the drug-likeness, bioactivities, and pharmacokinetic properties of eleutheroside B. Besides, the inhibitory potential of eleutheroside B has been investigated against cyclooxygenase 2 (COX-2) enzyme. This study suggests that eleutheroside B is a drug-like compound with bioactivity score (-0.08 to 0.38), having satisfactory pharmacokinetic values. Metabolism and toxicities were further studied using FAME3, GLORY, pred-hERG and Endocrine Disruptome tools. No severe toxicities (Ames, hepatotoxicity, cardiotoxicity, skin sensitization) were predicted. Rat acute toxicity, ecotoxicity and cell line cytotoxicity were evaluated based on GUSAR and CLC-pred. The compound has been predicted as non-toxic (class 5), non-hERG inhibitor and less likely to cause adverse drug interactions. Molecular docking against COX-2 enzyme revealed strong hydrogen bonds (SER530, TYR355, LEU352, SER353, VAL349, TYR385, MET522) and hydrophobic interaction (LEU352) with eleutheroside B. The docking score (-6.97 kcal/mol) suggested that this molecule can be utilized as an anti-inflammatory agent as well as a potential anticancer drug in the future. Hence, this is a comprehensive integrated in silico approach to establish the anti-inflammatory mechanism of eleutheroside B in the background of its potential in future drug development. Communicated by Ramaswamy H. Sarma
Article
The purpose of this study was to investigate the effect of Acanthopanax senticosus extract (ASE) (ethanol: DW=1:1, v/v) on inhibition of type 2 diabetes using an OLETF rat model via regulation of HbA1c and AGEs levels. Supplementation with ASE 0.1% and 0.5% effectively lowered levels of glucose, insulin, oral glucose tolerance test, and Homa-insulin resistance, suggesting reduced insulin resistance. Blood levels of HbA1c and AGEs were significantly reduced in a dose-dependent manner. As oxidative stress plays a key role in accelerating production of HbA1c and AGEs, which worsen symptoms of type 2 diabetes, levels of malonaldehyde and pro-inflammatory cytokines were measured. Lipid peroxidation in both blood and liver tissues was significantly reduced, and induction of pro-inflammatory cytokines interleukin-β and tumor necrosis factor-α, which elevate production of HbA1c and AGEs, was inhibited (P<0.05). To evaluate the possible cellular events after AGEs receptor activation, genetic expression of protein kinase C (PKC)-δ and transforming growth factor (TGF)-β was measured by real-time polymerase chain reaction. Supplementation with both ASE 0.1% and 0.5% significantly inhibited mRNA expression of PKC-δ and TGF-β, indicating that ASE may have beneficial effects on preventing insulin-resistant cells or tissues from progressing to diabetic complications. Taken together, ASE has potential to improve type 2 diabetes by inhibiting insulin resistance and protein glycosylation, including production of HbA1c and AGEs. Anti-oxidative activities of ASE are a main requisite for reducing production of HbA1c and AGEs and are also related to regulation of the PKC signaling pathway, resulting in suppression of TGF-β, which increases synthesis of collagen, prostaglandin, and disease-related proteins. © 2016, Korean Society of Food Science and Nutrition. All rights reserved.
Article
Background: Metabolic syndrome is a major risk factor for a variety of obesity-related diseases. Recently, the effects of functional foods have been investigated on lipid metabolism as a means to reduce lipid content in the blood, liver, and adipose tissues associated with carnitine O-palmitoyl transferase (CPT) activity. Acanthopanax senticosus (Rupr. et Maxim) Harms (AS) is a medicinal herb possessing a wide spectra of functions including anti-oxidant, anti-inflammatory, and anti-fatigue actions. Despite much research being focused on the cortical roots of AS, little information is available regarding its leaves, which are also expected to promote human health, for example by improving abnormal lipid metabolism. Here, we explored whether AS leaves affect lipid metabolism in mice fed a high-fat diet. Results: The administration of AS to BALB/c mice fed a high-fat diet significantly decreased plasma triglycerides (TG). CPT activity in the liver of these mice was significantly enhanced by AS treatment. Conclusion: These findings indicate that AS leaves have potential to alleviate increase in plasma TG levels due to high-fat diet intake in mice, possibly by increasing mitochondrial fatty acid β-oxidation, especially via CPT activation. Consequently, daily intake of AS leaves could promote beneficial health effects including the prevention of metabolic syndrome.
Article
Although it has recently been reported that Acanthopanax senticosus has a protective effect against the development of metabolic disorders such as diabetes and hyperlipidemia, its underlying molecular mechanisms have remained to be elucidated. In this study, we observed that treatment of an extract of A. senticosus (ASE) reduced body weight and adiposity and improved glucose tolerance in high-fat diet (HFD)-induced obese mice. HFD-induced weight gain in white adipose tissues and liver was also significantly reduced in ASE-treated HFD-fed mice, which was found to be contributed by suppression of mRNA expression of genes involved in fatty-acid uptake and fat synthesis in white adipose tissue. ASE treatment also attenuated M1 macrophage activation, increased regulatory T (Treg) cell population, and modulated leptin/adiponectin profile that might alleviate chronic inflammation to protect against HFD-induced insulin resistance. Our findings suggest a therapeutic potential of ASE for prevention and treatment of type 2 diabetes without adverse effects such as weight gain and dyslipidemia.
Article
In this study, we investigated the anti-adipogenic effects of Eleutherococcus senticosus and its active compounds in vitro to examine new functions. We first analyzed the active compounds in E. senticosus growing in Korea using HPLC and found that the concentration of eleutheroside B and E was higher in stems and roots than in other plant parts. There were no significant (p<0.05) differences in eleutheroside concentration between plant ages. Anti-adipogenic effects of E. senticosus on lipid accumulation in 3T3-L1 cells were examined. Extracts of stems and roots more effectively inhibited lipid accumulation in 3T3-L1 cells than extracts of other plant parts. Eleutheroside E was responsible for the pharmacological anti-adipogenic effects via regulation of the mTOR pathway. This is the first report of an anti-adipogenic effect of E. senticosus and the active compound eleutheroside E.
Article
Full-text available
Acanthopanax senticosus (Rupr. et Maxim) Harms (Araliaceae), also called Siberian Ginseng, Eleutherococcus senticosus, and Ciwujia in Chinese, is a widely used traditional Chinese herb that could invigorate qi, strengthen the spleen, and nourish kidney in the theory of Traditional Chinese Medicine. With high medicinal value, Acanthopanax senticosus (AS, thereafter) is popularly used as an "adaptogen" like Panax ginseng. In recent decades, a great number of chemical, pharmacological, and clinical studies on AS have been carried out worldwide. Several kinds of chemical compounds have been reported, including triterpenoid saponins, lignans, coumarins, and flavones, among which, phenolic compounds such as syringin and eleutheroside E, were considered to be the most active components. Considerable pharmacological experiments both in vitro and in vivo have persuasively demonstrated that AS possessed anti-stress, antiulcer, anti-irradiation, anticancer, anti-inflammatory and hepatoprotective activities, etc. The present review is an up-to-date and comprehensive analysis of the botany, chemistry, pharmacology, toxicity and clinical trials of AS.
Article
Full-text available
An ethanol extract derived from the roots of Eleutherococcus senticosus was found to influence markedly the cytokine synthesis of activated whole blood cultures of ten healthy volunteers. Whereas the synthesis of Rantes was increased over a wide range of concentrations, the release of IL-4, IL-5 and IL-12 was significantly inhibited. An inhibition at higher concentrations, switching to a stimulation at lower doses of the extract was seen with G-CSF, IL-6 and IL-13. From these particular immuno-pharmacological effects of Eleutherococcus senticosus we suggest this herbal preparation possesses immuno-modulatory potency, rather than just being immuno-suppressive or -stimulating.
Article
Full-text available
Double blind, randomized, placebo controlled pilot study of ImmunoGuard--a standardized fixed combination of Andrographis paniculata Nees., Eleutherococcus senticosus Maxim., Schizandra chinensis Bail., and Glycyrrhiza glabra L. special extracts standardized for the content of Andrographolide (4 mg/tablet), Eleuteroside E, Schisandrins and Glycyrrhizin, was carried out in two parallel groups of patients. The study was conducted in 24 (3-15 years of both genders) patients with Familial Mediterranean Fever (FMF), 14 were treated with tablets of series A (verum) and 10 patients received series B product (placebo). The study medication was taken three times of four tablets daily for 1 month. Daily dose of the andrographolide--48 mg. The primary outcome measures in physician's evaluation were related to duration, frequency and severity of attacks in FMF patients (attacks characteristics score). The patient's self-evaluation was based mainly on symptoms--abdominal, chest pains, temperature, arthritis, myalgia, erysipelas-like erythema. All of 3 features (duration, frequency, severity of attacks) showed significant improvement in the verum group as compared with the placebo. In both clinical and self evaluation the severity of attacks was found to show the most significant improvement in the verum group. Both the clinical and laboratory results of the present phase II (pilot) clinical study suggest that ImmunoGuard is a safe and efficacious herbal drug for the management of patients with FMF.
Article
Full-text available
The aim of this study was to determine whether sesamin, a component from Acanthopanax senticosus HARMS (ASH) pharmacologically offers protection against Parkinson's disease (PD) and its related depressive behavior in rats administered rotenone. We also examined how sesamin affected the rotenone-induced loss of tyrosine hydroxylase (TH) or glial cell line-derived neurotrophic factor (GDNF)-positive neurons in the midbrain of rats. Rats were orally administered sesamin (3, 30 mg/kg) once a day for 2 weeks before an intraperitoneal injection of rotenone (2.5 mg/kg). The pole test and catalepsy test were used to evaluate the effects of sesamin administration on bradykinesia and depressive behaviors in the PD model of rats given rotenone for 5 weeks. Those effects were compared with the ASH administrated group (250 mg/kg). Treatment with sesamin for seven weeks resulted in prophylactic effects on rotenone-induced parkinsonian bradykinesia and catalepsy, and the effects were equivalent to ASH effects. Immunohistochemistical analysis using TH or GDNF antibody showed that sesamin provided cytoprotective effects against rotenone-induced loss of DA cells. The results suggest that it may be possible to use the ASH and sesamin for the prevention of nigral degenerative disorders, e.g., PD with depression, caused by exposure to pesticide or environmental neurotoxins in general.
Article
In this study, we investigated the therapeutic effects of a novel formulation of low-dose calcium and vitamin D3, blended with Rehmannia glutinosa Libosch and Eleutherococcus senticosus Max (RE+), in postmenopausal women. The controls were given either a placebo or high dose calcium and vitamin D3 (Ca+D). Bone mineral density (BMD) in the L2-3 lumber spines and femur regions was assessed, and serum osteocalcin, bone-specific alkaline phosphatase (BALP), and cross-linked N-telopeptide of type I collagen (NTx) were used as markers of osteoblast and osteoclast activity. Furthermore, all variables were measured before and after 6 and 12 months of treatment. The osteocalcin level was higher in the RE+ group, and BALP was almost the same in all groups. Serum NTx was significantly decreased in the RE+ group after 12 months (p<0.05). The NTx in the Ca+D and placebo groups showed no significant change. The decrease of femur BMD was further demonstrated in the placebo group, but significantly increased in the RE+ group after 6 and 12 months of treatment (p<0.05). There were significant differences in the percent changes of femur BMD between the placebo and RE+ groups (p<0.01) and Ca+D and RE+ groups (p<0.05). The decrease of spine BMD in the placebo group was inhibited both in the Ca+D and RE+ groups, however, there was significant difference only between the placebo and RE+ groups (p<0.05). These findings suggest that continuous oral therapy of the RE+ formulation reduces rapidly decreasing bone mineral density in postmenopausal women more effectively than high doses of calcium and vitamin D3 alone by inhibiting osteoclastic activity. Therefore, it seems that the RE+ has its own antiosteoporotic effects. We suggest larger clinical studies to determine the most efficacious dosage and benefits of this novel treatment.
Article
Liquid-chromatography coupled with electrospray-ion trap mass spectrometry was applied to the analysis of the eleutherosides B and E in the Eleutherococcus senticosus cortexes. The optimum ESI/MS results were obtained in the positive ion mode using extracted ion chromatogram targeting Na-adduct molecular ion of each compound. This method allowed rapid and simple gradient separation of underivatized eleutherosides B and E without pre-purification steps at very low concentration.
Article
The chemical composition of the volatile constituents from the leaves, stems, and roots of Acanthopanax senticosus growing wild in Mt. Deok-Yu was determined by GC and GC/MS spectrometric analysis with the aid of NBS, Wiley Library and RI indice searches. The major constituents identified were δ-elemene (23.14%), β-elemene (5.59%), γ-cadinene (5.43%), and α-bergamotene (28.54%) in the leaves, α-pinene (11.50%), δ-elemene (17.62%), α-bergamotene (27.21%), and bicycloheptane derivative (6.38%) in the stems, and α-pinene (21.90%), and (+)-aromadendrene (3.77%) in the roots.
Article
In the article the authors demonstrated that phytoadaptogens (Panax ginseng, Eleutherococcus senticosus, Rhodiola rosea) take part in protecting brain neurons from various injuries. Ability of phytoadaptogens to have influence on neurodegenerative mechanisms at Parkinson's disease is discussed. Phytoadaptogens should be proposed for study or use as therapeutic modulators in neurodegenerative disorders including Parkinson's disease.
Article
In the present study, we investigated the component analysis, measurements of antioxidant activities and antimicrobial activities from fruit of Acanthopanax senticosus HARMS in order to detect the biological activities and develop novel functional resources. Different solvents extraction ratios were different according to different solvent extraction of Acanthopanax senticosus HARMS. Composition analysis were highly composed of carbohydrate as 72.33%. The minerals of different organs were highly composed of potasium as 5951.3 mg/100 g. The monosaccharides are composed of the arabinose, xylose, mannose, galactose, glucose. Antioxidant activity was measured in water extracts: 57.3 μg/ml, ethanol extracts: 630.1 μg/ml, methanol extracts: 248.5 μg/ml, 75% ethanol extracts: 198.97 μg/ml, 75% methanol extracts: 96.77 μg/ml, chloroform extracts: 1194.83 μg/ml at IC 50 value. The antimicrobial activities were observed in extracts from Acanthopanax senticosus HARMS against gram negative bacteria and gram positive bacteria.
Article
Siberian ginseng ([SG]; Eleutherococcus senticosus) is a commonly used herbal preparation. The objective of this study was to assess in normal volunteers (n = 12) the influence of a standardized SG extract on the activity of cytochrome P450 CYP2D6 and 3A4. Probe substrates dextromethorphan (CYP2D6 activity) and alprazolam (CYP3A4 activity) were administered orally at baseline and again following treatment with SG (1 × 485 mg twice daily) for 14 days. Urinary concentrations of dextromethorphan and dextorphan were quantified, and dextromethorphan metabolic ratios (DMRs) were determined at baseline and after SG treatment. Likewise, plasma samples were collected (0–60 h) for alprazolam pharmacokinetics at baseline and after SG treatment to assess effects on CYP3A4 activity. Validated high performance liquid chromatography methods were used to quantify all compounds and relevant metabolites. There were no statistically significant differences between pre- and post-SG treatment DMRs indicating a lack of effect on CYP2D6 (P > 0.05). For alprazolam there also were no significant differences in the pharmacokinetic parameters determined by noncompartmental modeling (Cmax, Tmax, area under the curve, half-life of elimination) indicating that SG does not significantly induce or inhibit CYP3A4 (P > 0.05). Our results indicate that standardized extracts of SG at generally recommended doses for over-the-counter use are unlikely to alter the disposition of coadministered medications primarily dependent on the CYP2D6 or CYP3A4 pathways for elimination.
Article
Eleven triterpenoid saponins were isolated from the leaves of a Chinese folk medicine, Acanthopanax senticosus (RUPR. et MAXIM) HARMS. Of these compounds, three were identified as known saponins. The structures of eight new saponins named ciwujianosides B (1), C1, (2), C2 (3), C3, (4), C4 (5), D1, (6), D2 (7), and E (8) were elucidated to be as follows : (1), 3-O-α-rhamnopyranosyl-(1→2)-β-arabinopyranosyl-30-norolean-12, 20(29)-dien-28-oic acid 28-O-α-rhamnopyranosyl-(1→4)-β-glucopyranosyl-(1→6)-β-glucopyranosyl ester; (2), 3-O-α-arabinopyranosyl-30-norolean-12, 20(29)-dien-28-oic acid 28-O-α-rhamnopyranosyl-(1→4)-β-glucopyranosyl-(1→6)-β-glucopyranosyl ester; (3), 3-O-α-rhamnopyanosyl-(1→2)-α-arabinopyranosyl-30-norolean-12, 20(29)-dien-28-oic acid 28-O-α-rhamnopyranosyl-(1→4)-6-O-acetyl-β-glucopyranosyl-(1→6)-β-glucopyranosyl ester; (4), 3-β-arabinopyranosyl oleanolic acid 28-O-α-rhamnopyranosyl-(1→4)-β-glucopyranosyl(1→6)-β-glucopyranosyl ester; (5), 3-O-α-rhamnopyranosyl-(1→2)-α-arabinopyranosyl oleanolic acid 28-O-α-rhamnopyranosyl-(1→4)-6-O-acetyl-β-glucopyranosyl-(1→6)-β-glucopyranosyl ester; (6), 3-O-α-arabinopyranosyl oleanolic acid 28-O-α-rhamnopyranosyl-(1→4)-6-O-acetyl-β-glucopyranosyl(1→6)-β-glucopyranosyl ester; (7), 3-O-α-arabinopyranosyl-30-norolean-12, 20(29)-dien-28-oic acid 28-O-α-rhamnopyranosyl-(1→4)-6-O-acetyl-β-glucopyranosyl-(1→6)-β-glucopyranosyl ester; (8), 3-O-α-rhamnopyranosyl-(1→2)-α-arabinopyranosyl-30-norolean-12, 20-(29)-dien-28-oic acid.
Article
An investigation of Eleutherococcus senticosus roots, using centrifugal partition chromatography as a key intermediate separation step, has led to the straightforward isolation of eight constituents. Four of these, sinapaldehyde glucoside, coniferaldehyde glucoside, coniferin and 1,5-di-O-caffeoylquinic acid, have been described for the first time in this plant. The quantitative analysis of different E. senticosus samples has been performed by high performance liquid chromatography using eleutherosides B and E as external standards.
Article
The number of studies devoted to the scientific evaluation of phytotherapy is rapidly increasing since Western patients seem more oriented towards so-called ‘alternative medicine’. Bearing such arguments in mind we decided to address attention to Eleutherococcus senticosus, a root of the Ginseng family known for thousands of years in China as a remedy for psychological distress. Forty-five paid, healthy volunteers (20 males, 25 females) were recruited. Entry criteria were: good health, age 18–30 years, student and a Symptoms Rating Test score <10. At screening evaluation subjects were randomized to receive orally either placebo (Pl group) or Eleutherococcus senticosus (Es group) for 30 days, in a double-blind design. Subjects were submitted to a stressful cognitive task, the Stroop Colour–Word test (Stroop CW), both before and after treatment. Stroop CW increased heart rate (HR) and systolic BP in every subject. In females there was a greater response than in males in terms of both systolic and diastolic BP. For both genders, the HR response to Stroop CW was reduced by Es treatment while no changes were found after Pl. In females, systolic BP was also reduced in Es group while it remained unchanged in Pl group. This study demonstrated that treatment with Eleutherococcus senticosus is able to reduce cardiovascular responses to stress in healthy young volunteers, while placebo was ineffective. Eleutherococcus senticosus is confirmed to be helpful for stress adaptation. Copyright © 2002 John Wiley & Sons, Ltd.
Article
The extract of the stem bark of Acanthopanax senticosus Harms (ASH) is known to have healing and protective effects on stress-induced disturbance of mental status. We have analysed whether a single or chronic (2 week) administration of ASH can affect concentrations of noradrenaline (NA), dopamine (DA) and their metabolites in the normal rat brain. A single p.o. administration of ASH elevated the NA and DA levels in the whole brain of rats in a dose-dependent manner. A single or 2 week administration of ASH (500 mg/kg) showed a marked increase in the DA level only in the striatum. However, NA levels were increased by a single dose of ASH in a wide range of brain regions such as the cortex, hypothalamus, striatum, hippocampus, substantia nigra and pons. When administered for 2 weeks no increase in NA levels was seen in these brain regions, except for an increase in the frontal cortex and anterior hypothalamus. The present results suggest that ASH may act by regulating NA and DA levels in specific brain regions related to stress response and Parkinson's disease.
Article
The root of Acanthopanax senticosus (also called Eleutherococcus senticosus or Siberian ginseng) has been used extensively in China, Russia and Japan as an adaptogen to fight against stress and fatigue. The present study was designed to ascertain the anti-fatigue property of Acanthopanax senticosus by load-weighted swimming test, sleep deprivation test, also to isolate and characterize the active constituents. Animals were orally administered with the extract of Acanthopanax senticosus. The anti-fatigue effects of the four fractions with different polarities from the 80% ethanol extract, and the different eluates collected from D101 macroporous resin chromatography and eleutheroside E, were examined based on the weight-loaded swimming capacity (physical fatigue) and the change of biochemical parameters in ICR mice. Moreover, the active fraction was later submitted to sleep-deprived mice (mental fatigue). The results shown that the n-butanol fraction significant extends the swimming time of mice to exhaustion. Furthermore, the 60% ethanol-water eluate, more purified eleutherosides (including eleutheroside E, E(2) and derivatives), were the exactly active constituents. Two compounds were isolated, which were identified as eleutheroside E, E(2). The eleutherosides possess the potent abilities to alleviate fatigue both in physical and mental fatigue. Eleutheroside E may be responsible for the pharmacological effect of anti-fatigue. Furthermore, the possible mechanisms were reduced the level of TG by increasing fat utilization, delayed the accumulation of blood urea nitrogen (BUN), and increased the LDH to reduce the accumulation of lactic acid in muscle and then protect the muscle tissue.
Article
Cadmium (Cd) is an important industrial pollutant, even though its mechanism of toxicity has not been completely clarified. Cd(2+) is toxic to a wide range of organs and tissues. Liver and kidneys are the primary target organs of cadmium toxicity. Cd(2+) induces apoptosis and causes necrotic cell death in certain pathophysiological situations. Eleutherococcus senticosus (Rupr. et Maxim.) Maxim. has many beneficial features. It supports the organism's stress response, immune system, and endocrine system, including the adrenal glands, spleen, and thymus gland. The aim of our study was to investigate the effects of the Eleutherococcus senticosus (ES) liquid extract on the accumulation of Cd(2+) in liver and on the mitotic and apoptotic activity of liver cells after chronic intoxication by Cd(2+). Experiments were carried out on white laboratory mice. Laboratory mice were given to drink solutions of different Cd(2+) and ES concentrations for 8 weeks. Cd(2+) concentration in mouse liver was detected using atomic absorption spectroscopy. Mitotic and apoptotic activity of liver cells was expressed as an estimated number of mitotic and apoptotic cells in randomly selected reference areas in a histological slide. ES combined with CdCl(2) leads to a significant decrease of cadmium concentration in the blood and liver of experimental mice. ES decreased the cadmium-induced mitotic and apoptotic activity of liver cells.
Article
Syringin is an active principle purified from the rhizome and root parts of Eleutherococcus senticosus (Araliaceae). The present study is designed to clarify the role of sympathetic activation in the insulinotropic effect of syringin. Plasma glucose lowering effect accompanying with the increase of plasma insulin and C-peptide were obtained in pentobarbital anesthetized Wistar rats 60min after an intravenous (i.v.) injection of syringin (100 microg/kg). However, neither the plasma glucose lowering action, nor the raised plasma levels of insulin and C-peptide can be obtained in conscious rats received same syringin treatment. Otherwise, the insulin-releasing and plasma glucose lowering actions of syringin (100 microg/kg, i.v.) were appeared in conscious rats under chemical sympathectomy using an intraperitoneal injection of guanethidine. In addition, plasma glucose lowering action of syringin (100 microg/kg, i.v.) was observed in conscious rats with alpha1-adrenoceptor blockade by prazosin. The stimulatory actions of syringin on the secretion of plasma insulin and C-peptide were also obtained in prazosin-treated conscious rats. The obtained results suggest that insulinotropic effect of syringin on the plasma glucose regulation is impaired in conscious rats with a regular sympathetic tone; decrease of sympathetic tone as observed in anesthetized animal might be helpful in the therapeutic benefit of syringin.
Article
In rat peritoneal mast cells induced by anti-immunoglobulin E, ciwujianosides D1 (1) and C1 (2) from Acanthopanax senticosus (ciwujia) strongly inhibited histamine release in a concentration-dependent manner. The inhibitory effect of 1 was approximately 6800 times stronger than that of disodium cromoglycate.
Article
Intraperitoneal injection of an aqueous extract of the crude drug "shigoka" (Siberian ginseng), Eleutherococcus senticosus roots, remarkably diminished plasma-sugar level in mice. Fractionation of the extract by monitoring the activity yielded seven glycans, eleutherans A, B, C, D, E, F, and G, which exerted marked hypoglycemic effects in normal and alloxan-induced hyperglycemic mice.
Article
DISODIUM cromoglycate (INTAL) has been shown to be an effective inhibitor of experimental allergen-induced bronchoconstriction in asthmatics1,2. The compound is novel in that it specifically inhibits the allergic release of spasmogens in immediate hypersensitivity reactions in several animal systems3. A recent suggestion was that disodium cromoglycate does not inhibit the reagin antibody/antigen union per se but that it inhibits discharge of the mediators from mast cells4.
Article
Effects of saponin isolated from the leaves of Acanthopanax senticosus (ASS) on myocardial infarct size were studied in acute ischemic dogs. The results showed that ASS (in a dosage of 25.50 mg/kg, iv) could significantly reduce the sizes of acute myocardial infarcts and decline the serum CK and LDH activity at 6h after ligation of LAD. It could also decrease the serum FFA levels at 3h and 6h after LAD occlusion.
Article
The hypoglycemic effect of saponin isolated from the leaves of Acanthopanax senticosus (ASS) was studied. The results showed that ASS(100, 200 mg/kg, ip) could decrease various cases of experimental hyperglycemias induced by injection of adrenaline, glucose and alloxan, without affecting the levels of blood sugar in normal mice.
Article
The multiplicity of the drug-metabolizing cytochrome P450 system was discovered 20 years ago. During the past 10 years the complementary DNAs of the most important P450 enzymes have been cloned and sequenced, and much has been learned about their substrate specificities, selective inhibitors, and functional characteristics. Cytochrome P4501A2 (CYP1A2), CYP2C19, CYP2D6, and CYP3A4 are the most important P450s catalyzing the biotransformation of psychotropic drugs. Assessment of the activity of individual P450 enzymes makes it possible to forecast an appropriate initial dose in a patient. At present, this strategy can be recommended only for CYP2D6 before treatment with tricyclic antidepressants and certain neuroleptics. Important drug-drug interactions can be predicted if two substrates or a substrate and an inhibitor of a particular P450 are co-administered. Therapeutic drug monitoring is of invaluable help in discovering and handling this type of interaction.
Article
The adaptogen concept is examined from an historical, biological, chemical, pharmacological and medical perspective using a wide variety of primary and secondary literature. The definition of an adaptogen first proposed by Soviet scientists in the late 1950s, namely that an adaptogen is any substance that exerts effects on both sick and healthy individuals by 'correcting' any dysfunction(s) without producing unwanted side effects, was used as a point of departure. We attempted to identify critically what an adaptogen supposedly does and to determine whether the word embodies in and of itself any concept(s) acceptable to western conventional (allopathic) medicine. Special attention was paid to the reported pharmacological effects of the 'adaptogen-containing plant' Eleutherococcus senticosus (Rupr. & Maxim.) Maxim. (Araliaceae), referred to by some as 'Siberian ginseng', and to its secondary chemical composition. We conclude that so far as specific pharmacological activities are concerned there are a number of valid arguments for equating the action of so-called adaptogens with those of medicinal agents that have activities as anti-oxidants, and/or anti-cancerogenic, immunomodulatory and hypocholesteroletic as well as hypoglycemic and choleretic action. However, 'adaptogens' and 'anti-oxidants' etc. also show significant dissimilarities and these are discussed. Significantly, the classical definition of an adaptogen has much in common with views currently being invoked to describe and explain the 'placebo effect'. Nevertheless, the chemistry of the secondary compounds of Eleutherococcus isolated thus far and their pharmacological effects support our hypothesis that the reported beneficial effects of adaptogens derive from their capacity to exert protective and/or inhibitory action against free radicals. An inventory of the secondary substances contained in Eleutherococcus discloses a potential for a wide range of activities reported from work on cultured cell lines, small laboratory animals and human subjects. Much of the cited work (although not all) has been published in peer-reviewed journals. Six compounds show various levels of activity as anti-oxidants, four show anti-cancer action, three show hypocholesterolemic activity, two show immunostimulatory effects, one has choleretic activity and one has the ability to decrease/moderate insulin levels, one has activity as a radioprotectant, one shows anti-inflammatory and anti-pyretic activities and yet another has shown activity as an antibacterial agent. Some of the compounds show more than one pharmacological effect and some show similar effects although they belong to different chemical classes. Clearly, Eleutherococcus contains pharmacologically active compounds but one wishes that the term adaptogen could be dropped from the literature because it is vague and conveys no insights into the mechanism(s) of action. If a precise action can be attributed to it, then the exact term for said action should obviously be used; if not, we strongly urge that generalities be avoided. Also, comparison of Eleutherococcus with the more familiar Panax ginseng C.A. Meyer (Araliaceae), 'true ginseng' has underscored that they differ considerably chemically and pharmacologically and cannot be justifiably considered as mutually interchangeable. Accordingly, we recommend that the designation 'Siberian ginseng' be dropped and be replaced with 'Eleutherococcus'. In the case of both Eleutherococcus and true ginseng, problems inherent in herbal preparation use include inconsistencies not only in terms of indications for use, but in the nomenclature of constituent chemical compounds, standardization, dosage and product labeling. (ABSTRACT TRUNCATED)
Article
A mechanism of action for Panax ginseng (PG) and Eleutherococcus senticosus (ES) is proposed which explains how they could produce the paradoxical effect of sometimes increasing and sometimes decreasing the stress response. The mechanism suggests that this biphasic effect results from increased occupancy of positive and negative feedback stress hormone receptors by their natural ligands due to inhibition of specific enzymes which function to limit receptor occupancy. Specifically, it is suggested that PG inhibits 11-beta hydroxysteroid dehydrogenase one and ES inhibits catechol- O -methyl transferase, both of which reside in close proximity to stress hormone receptors and catalyse the degradation of stress hormones into inactive compounds. In addition, it is suggested that the increased energy said to result from PG and ES may be a consequence of their increasing the occupancy of stress hormone receptors which function to redistribute the body's energy reserves from regeneration to activity.
Article
A liquid extract from Eleutherococcus senticosus roots inhibited the productive replication of human rhinovirus (HRV), respiratory syncytial virus (RSV) and influenza A virus in cell cultures infected with these viruses, all of which belong to the RNA type viruses. Analysis of virus production after treatment of the infected cells using plaque-reduction assays showed a strong antiviral activity of the Eleutherococcus extract. In contrast, no effect was detected using the same protocol for cells infected with the DNA viruses, adenovirus (Adeno 5) or herpes simplex type 1 virus (HSV 1). Pre-treatment of cells did not inhibit either virus adsorption or virus replication. The results of the study demonstrate that the Eleutherococcus extract inhibited the replication of all RNA viruses studied so far. This antiviral activity remained stable under the conditions used for drug preparation and storage.
Article
A new lignan glycoside, named eleutheroside E(2) (1), has been isolated from the roots of Eleutherococcus senticosus (known as "Siberian ginseng"), along with isomaltol 3-O-alpha-D-glucopyranoside (2), eleutherosides B, E and E(1), and thymidine. The structure of 1 was established by spectral interpretations as episyringaresinol 4"-O-beta-D-glucopyranoside. Compound 2 is described here for the first time as a naturally occurring compound.
Article
A clinical trial was undertaken to investigate the effects of Eleutherococcus senticosus (ES) and Panax ginseng (PG) on competitive club-level endurance athletes engaged in their normal in-season training. Participants were matched for training stress and received a 33% ethanolic extract (8 mL/day) containing either ES, PG (equivalent to 4 g and 2 g/day of dried root, respectively), or a placebo. A pre-test and post-test were used to evaluate the effects of six weeks of supplementation on cortisol, testosterone, and testosterone to cortisol ratio (TCR) as well as circulating numbers of total T-cells, T-helper cells (CD4), T-suppressor cells (CD8), CD4 to CD8 ratio, natural killer cells, and B lymphocytes. None of the immune system variables changed significantly nor showed any clear trend from pre to post test in any of the treatment groups. No significant change in testosterone, cortisol or TCR was observed in the PG group. In the ES group, however, TCR decreased by 28.7% from 0.0464 to 0.0331 (P=0.03). The main contribution to this decrease appeared to be a non-significant (P= 0.07) 31% trend towards increased cortisol rather than a very small non-significant (P = 0.36) 7% decrease in the calculated mean for testosterone. This result suggested that contrary to initial expectation, ES increased rather than decreased hormonal indices of stress, which may be consistent with animal research suggesting a threshold of stress below which ES increases the stress response and above which ES decreases the stress response.
Article
We studied the effect of Acanthopanax senticosus stem (ACPS) on mast cell-dependent anaphylaxis. ACPS inhibited compound 48/80-induced systemic anaphylaxis at a dose of 1.0 g/kg by 50%. ACPS also inhibited passive cutaneous anaphylaxis reaction and histamine release from mast cells in a dose-dependent manner, respectively. Moreover, ACPS had an inhibitory effect on anti-dinitrophenyl IgE-induced tumor necrosis factor-alpha (TNF-alpha) production from mast cells. These results indicate that ACPS inhibits mast cell-mediated anaphylaxis in vivo and in vitro murine model.
Article
Liquid chromatography-electrospray time-of-flight mass spectrometry (HPLC-ESI/TOF/MS) and a novel NMR technique, developed to maximise the sensitivity obtained from the standard NMR spectrometer, have been applied to the identification of the phenolic constituents of Eleutherococcus senticosus. In addition, molecular modelling and dihedral bond angle calculations based on the vicinal 3JHH-coupling constants have been used in the unambiguous assignment of signals in the 1H-NMR spectra. 5'-O-Caffeoylquinic acid and three isomeric compounds, 1',5'-O-dicaffeoylquinic acid, 3',5'-O-dicaffeoylquinic acid and 4',5'-O-dicaffeoylquinic acid, have been isolated and identified from a sample. The isolation and structure determination of the latter two compounds are reported for the first time from this plant.
Article
The aim of the present work was an estimation of the influence of two plant pharmaceutical preparations containing an extract from the root of Eleutherococcus senticosus: Argoeleuter tablets and Immuplant tablets, on the humoral response of immunological system. Experiments were performed with female Balb/c mice six weeks old. In order to reveal the influence of taking preparations, containing an extract from Eleutherococcus senticosus on some elements of the immunological system, three ways of their administration have been compared: before illness, during illness and a combination of both. The obtained results allow formulating the following conclusions: - the pharmaceutical preparations, containing the extract from Eleutherococcus senticosus administered orally, influence on the increase of the level of immunoglobulins comprised in the mice's blood serum, - the pharmaceutical preparations act with different power, not fully dependent on the content of marker of the active substance - eleutheroside E, - dosage of the preparations containing the extract from Eleutherococcus senticosus should not be established basing only on the extract content, - best curative results, measured as the stimulation of humoral response of the organism were obtained when a given preparation was administered therapeutically, even though the combined administration - prophylactically with prolonged administration during illness also is correct.
Article
To analyse genetic relationships and intraspecific variation within Eleutherococcus senticosus, the polymerase chain reaction (PCR) was performed on total genomic DNAs of 10 Eleutherococcus collections. Ten primers were used for amplification, yielding 106 bands, of which 87 were polymorphic. The genetic diversity and genetic distance among 10 collections of Eleutherococcus species were used to describe the dendrogram showing the phylogenic relationship. The 10 collections were classified into two groups (groups I and II) at a similarity coefficient of 0.50. Group I included E. senticosus from Bukhaedo (Japan), E. sessliliflorus from Youngwal (Korea), E. seoulense and E. chiisanesis, while group II included several internal and Russian collections. The range of polymorphism was from 66.7 to 90.9% in the 87 amplified polymorphic DNA fragments. The similarity value of all collections ranged from 0.41 to 0.92, and the average genetic distance was 0.61. Thus, RAPD analysis was useful in determining genetic relatedness among collections and in identifying different genotypes of E. senticosus and other Eleutherococcus species. Also, the biological activity on DPPH radical scavenging, antilipid peroxidation in rat liver microsomes and cytotoxic sulforhodamine B (SRB) assay was evaluated using root extracts of E. senticosus, Odaesan, Korea. Ethyl acetate and n-butanol fractionation revealed strong antioxidant against scavenging on DPPH free radical and also ethyl acetate fractionation exhibited high antilipid peroxidative activities. In the cytotoxic effects were evaluated on seven human cancer cell lines, the values of 50% growth inhibition (GI(50)) were mostly below 30 microg/ml for crude extracts to be considered as significantly active.
Article
In the present study, liriodendrin isolated by activity-guided fractionation from the ethyl acetate (EtOAc) extracts of the stem bark of Acanthopanax senticosus, was evaluated for anti-inflammatory and antinociceptive activities. Liriodendrin (5, 10 mg/kg/day, p. o.) significantly inhibited the increase of vascular permeability induced by acetic acid in mice and reduced an acute paw edema induced by carrageenan in rats. When the analgesic activity was measured by the acetic acid-induced writhing test and hot plate test, liriodendrin showed a dose-dependent inhibition in animal models. In addition, syringaresinol, the hydrolysate of liriodendrin, more potently inhibited the LPS-induced production of NO, PGE 2 and TNF-alpha production of macrophages than liriodendrin. Consistent with these observations, the expression level of iNOS and COX-2 enzyme was decreased by syringaresinol in a concentration-dependent manner. These results suggest that the anti-inflammatory and antinociceptive effects of liriodendrin after oral administration were attributable to the in vivo transformation to syringaresinol, which may function as the active constituent.
Article
The antioxidant activities of Acanthopanax senticosus stems were evaluated in CCl4-intoxicated rats. The n-butanol fraction from the water extract of the stems, when pretreated orally at 200 mg/kg/day for 7 consecutive days in rats, was demonstrated to exhibit significant increases in antioxidant enzyme activities such as hepatic cytosolic superoxide dismutase, catalase and glutathione peroxidase by 30.31, 19.82 and 155%, respectively. The n-butanol fraction whereas showed a significant inhibition of serum GPT activity (65.79% inhibition) elevated with hepatic damage induced by CCl4-intoxication. Eleutheroside B, a lignan component, isolated from the n-butanol fraction was found to cause a moderate free radical scavenging effect on DPPH, its scavenging potency as indicated in IC50 value, being 58.5 microM. These results suggested that the stems of A. senticosus possess not only antioxidant but also hepatoprotective activities.
Article
Siberian ginseng (SG) has been widely and historically consumed as a health food product for the improvement of self well-being, but whether vascular relaxation may contribute to such a therapeutic health effect has not been studied. We therefore investigated the vasorelaxant effect of the aqueous extract of the roots of SG (Eleutherococcus senticosus Maxim) using several in vitro vascular rings prepared from dog carotid artery, rat aorta and rat mesenteric artery. SG extract (0.04-0.8 mg/ml) caused concentration-dependent relaxation in dog carotid arterial rings pre-contracted with 100 microM phenylephrine (PE), and the relaxation was primarily endothelium-dependent. Treatment with 100 microM L-NOARG (a nitric oxide synthase inhibitor) either prevented or totally reverted SG-induced relaxation, suggesting that the endothelium-dependent relaxation was mediated by NO. Similar endothelium-dependent vascular relaxant responses were also obtained with rat aortic and mesenteric arterial rings, except that it occurred over a relatively higher concentration range of SG (0.5-2.0 mg/ml). When tested in the presence of 300 microM L-NAME, the vasorelaxant effect of SG was inhibited totally in rat aorta but only partially in rat mesenteric artery. The relaxation to SG that was insensitive to L-NAME in rat mesenteric arterial rings was eliminated when the rings (both proximal and distal ends) were pre-treated with a combination of 300 microM L-NAME and 15 mM KCl indicating the involvement of endothelium-derived hyperpolarizing factor (EDHF). This vasorelaxant response of the SG extract was inhibited partially by atropine (1 microM), completely by TEA (5 mM), but not by indomethacin (1 microM) or propranolol (10 microM). SG up to 2 mg/ml had no effect on KCl-induced contraction in any of the vascular rings studied. When compared with carbachol-induced (CCh) relaxation, SG resembles CCh in that the sensitivity to L-NAME inhibition is dependent on vascular size, i.e. aorta >proximal end of mesenteric artery >distal end of mesenteric artery. However, SG exhibited different potencies to relaxation while CCh showed similar potency (EC(50) of about 0.2 microM) in all three vascular segments. In conclusion, we have demonstrated that the vascular effect of SG is endothelium-dependent and mediated by NO and/or EDHF depending on the vessel size. Other vasorelaxation pathways, such as inhibition of K(+)-channels and activation of muscarinic receptors, may also be involved.
Article
The cortex of Eleutherococcus senticosus (Rupr. & Maxim.) Maxim. has been used extensively in Russia, China, Korea and Japan as an adaptogen whose properties are the ability to increase as non-specific body resistance to stress and fatigue. Although it has been reported that Eleutherococcus senticosus has anti-fatigue and anti-stress actions, their actions are still unclear on the relationship between immune system, especially natural killer (NK) activity and endocrine system (corticosterone level). We compared the effects of the water extracts (A, B, C, D and E) of five Eleutherococcus senticosus cortex on the swimming time, NK activity and blood corticosterone level using forced swimming stressed mice. Among five kinds, C, D and E extracts significantly prolonged the swimming time. C and D extracts inhibited the reduction of NK activity and the corticosterone elevation induced by forced swimming. The contents of eleutheroside E, isoflaxidin and eleutherosides B plus E were in the order C > D > E > B > A and C > E > D > A > B extracts, respectively. Therefore, it is suggested that eleutheroside E may be contributed to the anti-fatigue action, the recovery of the reduction of NK activity and the inhibition of corticosterone elevation induced by swimming stress.
Article
An HPLC method based on several known methods for the determination of eleutherosides B and E was developed, optimised and validated in terms of linearity, precision (repeatability and intermediate precision on different days and at different concentration levels) and accuracy (recovery). The extraction procedure, the extraction solvent and the extraction yield were evaluated and optimised. A reversed-phase RP-18 column gradient eluted with a two-phase system consisting of phosphoric acid:water (0.5:99.5) and acetonitrile was used to evaluate the samples; detection was at 220 nm. Although eleutherosides B and E are commercially available, they are very costly, and therefore ferulic acid was chosen as external standard. The correction factors for the response of ferulic acid against both eleutherosides were determined and validated. This method, accepted by the European Pharmacopoeia Commission, will be included in the monograph on Eleutherococcus senticosus roots to assay the content of eleutherosides B and E.
Article
The clinical efficacy of KanJang oral solution, a fixed combination of standardised extracts of Echinacea purpurea, Adhatoda vasica and Eleutherococcus senticosus, was compared with the combined extracts of Echinacea purpurea and Eleutherococcus senticosus alone (Echinacea mixture) in a controlled, double blind, randomized trial, and with Bromhexine (a standard treatment) in a controlled, open, randomized clinical trial on patients with non-complicated acute respiratory tract infections. Many of the parameters evaluated, such as severity of coughing, frequency of coughing, efficacy of mucus discharge in the respiratory tract, nasal congestion and a general feeling of sickness, showed significantly greater improvement in patients treated with KanJang compared with those receiving the standard treatment. However, no significant differences in the improvement of these symptoms (except in a reduced frequency of coughing) were observed between patients treated with the Echinacea mixture and those receiving the standard treatment. The only explanation is that the lack of extract of A. vasica in the Echinacea mixture reduces its efficacy compared with the complete KanJang oral solution even though direct double-blind comparison yielded no significant differences between these two groups of patients. The recovery time of patients being treated with KanJang or Echinacea mixture was 2 days shorter than that of patients receiving the standard treatment. None of the patients completing the study reported adverse reactions to the medication taken. The significance of the results obtained in this study is discussed with respect to the efficacy of KanJang in the treatment of acute respiratory infection and to the concept that multi-drug therapy offers higher efficacy compared with mono-drug treatment of such infections.
Article
A high performance liquid chromatography (HPLC) method was developed for the first time to quantify simultaneously the six major active ingredients in Acanthopanax senticosus (Rupr. et Maxim.) Harms, namely protocatechuic acid, syringin, chlorogenic acid, caffeic acid, liriodendrin and isofraxidin. The analysis was performed by a reverse phase gradient elution with an aqueous mobile phase (containing 0.05% phosphoric acid) modified by acetonitrile and diode-array multiple-wavelength UV detector (DAD). Six regression equations showed good linear relationships between the peak area of each marker and concentration. The recoveries of the markers listed above were 92.3%, 93.9%, 90.3%, 93.1%, 94.3% and 90.7%, respectively. The relative standard deviation of intra-day and inter-day were less than 2.7% and 3.1%, respectively. This method was validated for specificity, accuracy, precision and limits of quantification. Medicinal materials of ten commercial brands were analyzed and found to contain different amounts of the six bioactive markers. The method developed can be used for the quality control of Acanthopanax senticosus (Rupr. et Maxim.) Harms.
Article
The influence of a plant preparation AdMax (Nulab Inc., Clearwater, FL, USA) on immunity in ovarian cancer patients was studied. The preparation is a combination of dried ethanol/water extracts from roots of Leuzea carthamoides, Rhodiola rosea, Eleutherococcus senticosus and fruits of Schizandra chinensis. Twenty eight patients with stage III-IV epithelial ovarian cancer were treated once with 75 mg/m(2) cisplatin and 600 mg/m(2) cyclophosphamide. Peripheral blood was collected 4 weeks after the chemotherapy. Subclasses of T, B and NK lymphocytes were tested for in the blood samples: CD3, CD4, CD5, CD7, CD8, CD11B, CD16, CD20, CD25, CD38, CD45RA, CD50, CD71 and CD95. Immunoglobulin G, A and M concentrations were also determined. Changes were observed in the following T cell subclasses: CD3, CD4, CD5 and CD8. In patients who took AdMax (270 mg a day) for 4 weeks following the chemotherapy, the mean numbers of the four T cell subclasses were increased in comparison with the mean numbers of the T cell subclasses in patients who did not take AdMax. In patients who took AdMax, the mean amounts of IgG and IgM were also increased. The obtained results suggest that the combination of extracts from adaptogenic plants may boost the suppressed immunity in ovarian cancer patients who are subject to chemotherapy.
Article
The immunomodulatory properties of a diterpene lactone andrographolide and Kan Jang--a standardized fixed combination of Andrographis paniculata extract SHA-10 and Eleutherococcus senticosus extract SHE-3 were investigated. Their role on spontaneous and phytohemagglutinin (PHA)-induced proliferation of human peripheral blood lymphocytes (PBL) and on production of interferon-gamma (INF-gamma) and tumor necrosis factor-alpha (TNF-alpha) were determined in vitro. Proliferation of PBL induced by PHA was enhanced by co stimulation with andrographolide and Kan Jang. At the same time andrographolide and Kan Jang inhibit spontaneous proliferation of PBL in vitro. These preparations also have effect on the formation of INF-gamma, TNF-alpha and some immune activation markers such as neopterin (Neo), beta-2-microglobulin (beta2MG), and soluble receptor for interleukin-2 (sIL-2R or sCD25) in blood cells culture. Andrographolide and Kan Jang stimulate the INF-gamma, Neopterin and beta2MG formation, but do not have any significant effect on the production of INF-gamma and Neopterin in PHA stimulated blood cells. An opposite effect on these immune makers was observed in the PHA-stimulated blood cells: both andrographolide and Kan Jang increase the formation of TNF-alpha and beta2MG in cultivated whole blood cells. Thus, andrographolide and Kan Jang can have an in vitro effect on the activation and proliferation of immunocompetent cells as well on the production of key cytokines and immune activation markers. The results show an overall higher effect of the fixed combination as compared with the equivalent amount of the pure substance andrographolide. The data are consistent with results from clinical studies of Kan Jang and contributed to a better understanding of these results.
Article
Eleutherococcus senticosus (Araliaceae) is immunological modulator which has been successfully used for anti-inflammatory effectors on anti-rheumatic diseases in oriental medicine. Mitogen-activated protein kinases (MAPKs) and Akt modulate the transcription of many genes involved in the inflammatory process. In this study, we investigated the inhibitory effects of Eleutherococcus senticosus on the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharides (LPS)-activated macrophages. Finally, we studied the involvement of MAPKs and Akt signaling in the protective effect of Eleutherococcus senticosus in LPS-activated macrophages. Eleutherococcus senticosus significantly attenuated LPS-induced iNOS expression but not COX-2 expression. In using the standard inhibitors (MAPKs and Akt), our results show that Eleutherococcus senticosus downregulates inflammatory iNOS expression by blocking JNK and Akt activation.
Article
Increasing evidence suggests that aberrant activation of PI3K/Akt is involved in many human cancers, and that inhibition of the PI3K/Akt pathway might be a promising strategy for cancer treatment. Our investigation indicates that Rhabdastrellic acid-A, an isomalabaricane triterpenoid isolated from the sponge, Rhabdastrella globostellata, inhibits proliferation of HL-60 cells with an IC(50) value of 0.68mug/ml, and induces apoptosis. Rhabdastrellic acid-A also induces cleavage of the death substrate poly (ADP-ribose) polymerase (PARP) and caspase-3. Pretreatment of HL-60 cells with the caspase-3 specific inhibitor, DEVD-CHO, prevents Rhabdastrellic acid-A-induced DNA fragmentation and PARP cleavage. Activated PI3K and Akt significantly decreases after treatment with Rhabdastrellic acid-A in HL-60 cells. Expression levels of protein bcl-2, bax remain unchanged in response to Rhabdastrellic acid-A treatment in HL-60 cells. These results suggest that Rhabdastrellic acid-A inhibits PI3K/Akt pathway and induces caspase-3 dependent-apoptosis in HL-60 human leukemia cells.
Article
Eleutherococcus senticosus (Araliaceae ) is a very powerful adaptogenic agent. In the present study, the effects of syringin, an active principle of this herb, on plasma glucose levels in streptozotocin-induced diabetic rats (STZ-diabetic rats) were investigated. Thirty minutes after syringin was intravenously injected into fasting STZ-diabetic rats, plasma glucose levels dose-dependently decreased. In normal rats, syringin at the effective dose (1.0 mg/kg) significantly attenuated the increase in plasma glucose caused by an intravenous glucose challenge. Syringin dose-dependently (0.01 to 10.0 micromol/L) stimulated glucose uptake in soleus muscle isolated from STZ-diabetic rats. Syringin treatment of hepatocytes isolated from STZ-diabetic rats enhanced glycogen synthesis . The ability of syringin to enhance glucose utilization and lower plasma glucose level in rats suffering from insulin deficiency suggest that this chemical may be useful in the treatment of human diabetes.
Article
The present study is designed to screen the effect of syringin, an active principle purified from the rhizome and root parts of Eleutherococcus senticosus (Araliaceae), on the plasma glucose and investigate the possible mechanisms. Plasma glucose decreased in a dose-dependent manner 60 min after intravenous injection of syringin into fasting Wistar rats. In parallel to the decrease of plasma glucose, increases of plasma insulin level as well as the plasma C-peptide was also observed in rats receiving same treatment. Both the plasma glucose lowering action and the raised plasma levels of insulin and C-peptide induced by syringin were also inhibited by 4-diphenylacetoxy-N-methylpiperdine methiodide (4-DAMP), the antagonist of the muscarinic M3 receptors, but not affected by the ganglionic nicotinic antagonist, pentolinium or hexamethonium. Moreover, disruption of synaptic available acetylcholine (ACh) using an inhibitor of choline uptake, hemicholinium-3, or vesicular acetylcholine transport, vesamicol, abolished these actions of syringin. Also, physostigmine at concentration sufficient to inhibit acetylcholinesterase enhanced the actions of syringin. Mediation of ACh release from the nerve terminals to enhance insulin secretion by syringin can thus be considered. The results suggest that syringin has an ability to raise the release of ACh from nerve terminals, which in turn to stimulate muscarinic M3 receptors in pancreatic cells and augment the insulin release to result in plasma glucose lowering action.
Article
LC/ESI-MS n methods have been previously set up to detect the administration of (i) Harpagophytum and (ii) preparations containing a plant capable of anti-stress properties: Eleutherococcus senticosus. Harpagoside has been found to be the main indicator of Harpagophytum administration in the horse. These methods have been applied to a large number of horse urine samples of various origins. Regarding the detection of Harpagophytum administration, harpagoside, harpagide and 8-para-coumaroyl harpagide were detected together in only one sample out of 317. Eleutheroside E was found to be the main indicator of Eleutherococcus senticosus administration. It was detected in post-administration samples collected from two horses having received a feed supplement containing Eleutherococcus senticosus for several days. Out of the 382 samples tested, eleutheroside E was found in an unexpected large number of urine samples (39%) of various origins and its presence cannot be only due to the sole use of herbal dietary supplements.