- 1. Pancreatic lipase inhibitory activity of cassiamin A, a bianthraquinone from Cassia siamea.
In continuation towards the discovery of potential antiobesity lead(s) from natural products, we have screened n-hexane, dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH) extracts of 33 Indian medicinal plants (200 extracts) for in vitro pancreatic lipase inhibitory activity. Of the screened extracts, the EtOAc extract of Cassia siamea roots showed 74.3 +/- 1.4% enzyme inhibition at 250 microg/mL concentration. Bioassay guided fractionation of the active extract afforded 6 known compounds viz. chrysophanol (1), physcion (2), emodin (3), cassiamin A (4), friedelin (5) and cycloart-25-en-3beta,24-diol (6). These compounds were further evaluated for pancreatic lipase inhibitory activity. Cassiamin A (4), a bianthraquinone, was found to be most active with an IC50 value of 41.8 +/- 1.2 microM and compounds 2 and 5 were found to be moderate enzyme inhibitors. Results indicate the antiobesity potential of C. siamea through pancreatic lipase inhibition....(more)
Kumar D, et al. Nat Prod Commun 2013 Feb;8(2):195-8.
Related Products: Frangula Emodin
- 2. Antimycobacterial effect of extract and its components from Rheum rhaponticum.
The global threat of tuberculosis demands the search for alternative antimycobacterial drugs. The present study examined roots and petioles from Rheum rhaponticum for antimycobacterial activity. Crude methanol extracts and eight phenolic compounds isolated by preparative column chromatography were tested against Mycobacterium tuberculosis H37Ra and M. bovis using the broth dilution method. The extract from roots and its components, such as rhaponticin, deoxyrhaponticin, resveratrol, barbaloin, aloe-emodin, and chrysophanol were found to have antimycobacterial activity against both microorganisms. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration of all the investigated samples ranged from 32 to 512 microg/mL. The anthracene derivatives were the most active; their MICs were 32, 64, and 64 microg/mL (M. tuberculosis H37Ra) and 128, 64, and 64 microg/mL (M. bovis), respectively. The microorganisms were resistant to stimulation with extract from petioles, as were quercetin and rutin. The results showed that anthracene and stilbene derivatives play a prominent role in the antimycobacterial properties of R. rhaponticum....(more)
Smolarz HD, et al. J AOAC Int 2013 Jan-Feb;96(1):155-60.
Related Products: Frangula Emodin
- 3. Stilbene glucoside inhibits the glucuronidation of emodin in rats through the down-regulation of UDP-glucuronosyltransferases 1A8: Application to a drug-drug interaction study in Radix Polygoni Multiflori.
ETHNOPHARMACOLOGICAL RELEVANCE:
The integrated effects of herbal medicines were the outcome of all of the inherent components. Currently, few studies have focused on the multicomponent interactions in an herbal medicine to elucidate its pharmacological and/or toxicological effects. In this study, an attempt was made to investigate the interaction between stilbene glucosides and the anthraquinones contained in Radix Polygoni Multiflori (RPM) and to explore the interaction's mechanism from the perspective of UDP-glucuronosyltransferase (UGT) regulation.
MATERIALS AND METHODS:
The extract of RPM was separated into a stilbene glucoside fraction and a emodin fraction. A rapid high-performance liquid chromatography-mass spectrometry method was developed and validated to disclose the influence of stilbene glucoside on the pharmacokinetics of emodin in rats. Drug and Statistics 2.0 was used for the estimation of the pharmacokinetic parameters. Gene expression analysis in liver and intestinal tissues was performed by a semi-quantitative reverse transcription-polymerase chain reaction (RT-PCR) method.
RESULTS:
The analytical method appeared to be suitable for the analysis of emodin with desirable linearity, accuracy, precision and stability, and the total analysis time was less than 2min on a short column. Glucuronide of emodin, which is the major metabolite of emodin, was determined after β-glucuronidase hydrolysis. As the in vivo pharmacokinetic studies had indicated, the AUC, Cmax and T1/2 of emodin were increased after the stilbene glucoside treatment, and the glucuronidation of emodin was significantly inhibited. The mRNA levels from UGT1A8 and UGT1A2 were decreased by stilbene glucoside treatment. In contrast, the expression of UGT1A1, UGT1A6 and UGT1A9 mRNA was increased in the liver following treatment.
CONCLUSIONS:
The influence of stilbene glucoside on the pharmacokinetics of emodin may be attributed to the inhibition of UGT1A8 mRNA expression. Thus, it is important to extend this research to deepen our understanding of the pharmacological and/or toxicological effects of RPM.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved....(more)
Ma J, et al. J Ethnopharmacol 2013 May 20;147(2):335-40.
Related Products: Frangula Emodin
- 4. Isolation and characterization of two flavonoids, engeletin and astilbin, from the leaves of Engelhardia roxburghiana and their potential anti-inflammatory properties.
Engeletin, a flavonoid compound, was isolated from the leaves of Engelhardia roxburghiana for the first time, along with astilbin, another flavonoid. The chemical structures of engeletin and astilbin were confirmed by (1)H and (13)C nuclear magnetic resonance (NMR) and mass spectrometry (MS) spectra, and their anti-inflammatory activities were studied in lipopolysaccharide (LPS)-stimulated mouse J774A.1 macrophage cells. LPS induced the inflammatory state in macrophage cells and increased mRNA expressions of pro-inflammatory cytokines. Engeletin and astilbin exhibited remarkable inhibitory effects on interleukin (IL)-1β and IL-6 mRNA expression. Significant inhibition of LPS-mediated mRNA expressions were also seen in LPS binding toll-like receptor (TLR)-4, pro-inflammatory cytokine tumor necrosis factor (TNF)-α, IL-10, chemoattractant monocyte chemotactic protein (MCP)-1, and cyclooxygenase (COX)-2 genes. The reduced expression of these cytokines may alleviate immune response and reduce inflammatory activation, indicating that engeletin and astilbin may serve as potential anti-inflammatory agents....(more)
Huang H, et al. J Agric Food Chem 2011 May 11;59(9):4562-9.
Related Products: Engelhardia Leaf Extract
- 5. [Effect of epimedium extract on osteoprotegerin and RANKL mRNA expressions in glucocorticoid-induced femoral head necrosis in rats].
OBJECTIVE:
To investigate the effect of glucocorticoid on the expression levels of osteoprotegerin (OPG) and receptor activator of nuclear factor kappa B ligand (RANKL) mRNAs in rat femoral head and the antagonistic effect of Epimedium, and explore the mechanism of Epimedium in preventing glucocorticoid-induced femoral head necrosis.
METHODS:
Forty-eight adult SD rats were randomized into glucocorticoid group, Epimedium group and control group. In the former two groups, the rats received intramuscular injection of 12.5 mg prednisolone twice a week, and in Epimedium group, additional 1 ml/100 g aqueous Epimedium extract (equivalent to 0.1 g/ml of the crude drug) was administered intragastrically once daily. The control group received only intramuscular saline injection. After 4 weeks of treatment, osteonecrosis of the left femoral head was detected by HE staining, and the right femoral head was sampled for detection of OPG and RANKL mRNA expressions using real-time quantitative PCR.
RESULTS:
In glucocorticoid, Epimedium and control groups, the mortality rate of the rats was 12.5% (2/16), 6.25% (1/16), 0 (0/16), and femoral head necrosis occurred at a rate of 71.43% (10/14), 26.67% (4/15), and 0 (0/16), respectively. In glucocorticoid group, the expression level of OPG mRNA was significantly lower, RANKL expression significantly higher, and OPG/RANKL ratio significantly lower than those in Epimedium and control groups (P<0.05). OPG, RANKL and their ratios showed no significant differences between Epimedium group and the control group.
CONCLUSION:
Epimedium can prevent glucocorticoid-induced femoral head necrosis probably by antagonizing glucocorticiod-induced abnormal expressions of OPG and RANKL mRNA....(more)
Wang JZ, et al. Nan Fang Yi Ke Da Xue Xue Bao 2011 Oct;31(10):1714-7. Chinese.
Related Products: Epimedium Extract
- 6. Pharmacokinetics of prenylflavonoids and correlations with the dynamics of estrogen action in sera following ingestion of a standardized Epimedium extract.
To explore pharmacokinetic properties of prenylflavonoids from the Traditional Chinese Medicinal plant Epimedium, three doses of a standardized extract (100, 300 and 600 mg/kg body weight), were administered to ovariectomized rats and serial blood samples were obtained. Serum concentrations of the Epimedium prenylflavonoids icariin, icariside I, icariside II, icaritin and desmethylicaritin were determined by LC-MS/MS. Aliquots of sera were also applied to human cell lines that permanently express ERalpha and ERbeta proteins for the ex vivo measurement of estrogenic activity. All five prenylflavonoids exhibit non-linear dose-dependent increases in the area under concentration versus time curves. Two distinct pharmacokinetic patterns were evident, an early phase wherein icariin and icariside II reached t(max) 0.5-1 h, and a late phase wherein icariside I, icaritin and desmethylicaritin peaked at t(max) 8h. Total concentrations of icaritin and desmethylicaritin reached C(max) approximately 2 microM and approximately 0.25 microM respectively. Estrogenic activity in Epimedium-treated rat sera lagged by several hours compared to animals treated with control drug estradiol benzoate, corresponding to the appearance of bioactive metabolites desmethylicaritin, icaritin and icariside I. Following glucuronidase/sulphatase treatment, prolonged estrogenic activity at higher Epimedium doses (300 and 600 mg/kg of body weight) was evident, and correlated with the persistence of micromolar levels of icaritin at the 48-72 h sampling period. The depot effect resulted in time-concentration bioactivity profiles at the three Epimedium doses (area under curve 374, 543, and 771pME2 h(-1)) that exceeded that observed for estradiol benzoate (148pME2 h(-1)). Our study correlated the pharmacokinetics of prenylflavonoids with the dynamics of their estrogenic effects and reveals the potential estrogenicity of this Epimedium extract. This study may aid the development of prenylflavonoids as drugs for menopause and other conditions requiring estrogenic action....(more)
Wong SP, et al. J Pharm Biomed Anal 2009 Sep 8;50(2):216-23.
Related Products: Epimedium Extract
- 7. [Research on quality of Epimedium extract in market].
OBJECTIVE:
To review the quality of Epimedium extract in the market.
METHOD:
The contents of icariin, epimedin C, sagittatoside B and total flavonoids in Epimedium extracts sold in the market were assayed by the methods of HPLC and UV respectively. HPLC fingerprintings were obtained at the same time.
RESULT:
The contents of icariin in most of the extracts are closely similar with the ones labeled by the companies. 3 type chromatograms were classified in all the HPLC fingerprintings, and were corresponded with their raw materials. The contents of epimedin C, sagittatoside B and total flavonoids were different in the samples with the same content of icariin.
CONCLUSION:
We can primarily confirm the origin of raw materials by comparing the HPLC fingerprinting of extracts with the ones of materials. The difference of extracts quality mainly comes from the difference of materials. So we suggest that Epimedium extract product should be labeled the origin of materials, and assayed with more compound contents, to ensure the quality stabilization....(more)
Peng YD, et al. Zhongguo Zhong Yao Za Zhi 2007 Sep;32(18):1858-61. Chinese.
Related Products: Epimedium Extract
- 8. Use of escin as a perforating agent on the IonWorks quattro automated electrophysiology platform.
The automated electrophysiology platform IonWorks has facilitated the medium-throughput study of ion channel biology and pharmacology. Electrical and chemical access to the cell is by perforated patch, afforded by amphotericin. Permeation of the amphotericin pore is limited to monovalent cations. We describe here the use of the saponin escin as an alternative perforating agent. With respect to the number and robustness of seals formed across a variety of cell and ion channel types, the performance of escin is equal to that of amphotericin. Escin also permits the permeation of larger molecules through its pore. These include nucleotides, important intracellular modulators of ion channel activity that can be used to prevent ion channel rundown of, for instance, Ca(V)1.2. Furthermore, pharmacologic agents such as QX314 can also permeate and be used for mechanistic studies. Escin, in combination with IonWorks, increases the scope of ion channel screening and can facilitate the assay of previously difficult-to-assay targets....(more)
Morton MJ, et al. J Biomol Screen 2013 Jan;18(1):128-34.
Related Products: Escin
- 9. Interaction between titanium and cadmium in various guinea pig organs.
Titanium (Ti) is used in many fields, while cadmium (Cd) is known to cause the itai-itai disease. In the present study, possible interactions between titanium and cadmium were investigated. Aorta, taenia coli, and liver were removed from male guinea pigs. Muscle tension was measured using intact aorta and taenia coli and using β-escin-permeabilized taenia coli in a physiological salt solution and a hyperpotassium solution containing Cd and/or Ti. Cellular Cd contents were determined using all tissues after washout with EDTA solution. Cadmium-induced relaxation in the hyperpotassium solution recovered significantly (P < 0.01) following Ti treatment in taenia coli, but not in the aorta. In β-escin-permeabilized taenia coli, the percentage recoveries after Cd treatment and after Ti plus Cd treatment were 67.3 ± 8.7 % (n = 4) and 87.7 ± 3.8 % (n = 4), respectively, compared with Ca-induced control contraction. Cellular Cd contents in taenia coli decreased significantly following treatment with Ti 10(-4) M. Although similar results were obtained using the aorta and the liver, there were no significant differences between the control and Ti 10(-5) M. High concentrations of Ti may reduce cellular Cd content....(more)
Takano T, et al. Biol Trace Elem Res 2013 Feb;151(2):209-16.
Related Products: Escin
- 10. Escin inhibits type I allergic dermatitis in a novel porcine model.
Background: Current standard medications for the treatment of allergic inflammation consist primarily of glucocorticoids and anti-histamines, but adverse side effects or insufficient responsiveness by patient subpopulations illustrate the need for safe and novel alternatives. Thus, there is a demand to develop a porcine model that is able to mimic mast cell-mediated type I hypersensitivity. Previously, we found that escin, a pharmacologically active mix of triterpene saponins from horse chestnut extracts, exerts anti-allergic effects in murine models and merits further investigation as an anti-allergic therapeutic. Methods: We developed a new porcine model of allergic dermatitis based on a clinical prick test protocol. Histamine clearly provoked erythema and swelling at the prick site, whereas the mast cell-degranulating compound 48/80 even more pronounced caused wheal and flare reactions known from the human prick response. This model was used to test the anti-allergic efficacy of orally applied escin. Results: Oral pretreatment of animals with escin strongly inhibited the allergic skin response induced by compound 48/80 in a dose-dependent manner. Additional in vitro data from murine mast cells indicate an engagement of the glucocorticoid receptor pathway upon treatment with escin. Conclusions: This model provides a valuable and easy-to-set-up tool for preclinical studies of mast cell-inhibiting compounds. The successful implementation of this model supports the development of oral escin applications as a novel anti-allergic therapy....(more)
Sipos W, et al. Int Arch Allergy Immunol 2013;161(1):44-52.
Related Products: Escin
- 11. A novel GABAergic action mediated by functional coupling between GABAB-like receptor and two different high-conductance K+ channels in cricket Kenyon cells.
The γ-aminobutyric acid type B (GABAB) receptor has been shown to attenuate high-voltage-activated Ca(2+) currents and enhance voltage-dependent or inwardly rectifying K(+) currents in a variety of neurons. In this study, we report a novel coupling of GABAB-like receptor with two different high-conductance K(+) channels, Na(+)-activated K(+) (KNa) channel and Ca(2+)-activated K(+) (KCa) channel, in Kenyon cells isolated from the mushroom body of the cricket brain. Single-channel activities of KNa and KCa channels in response to bath applications of GABA and the GABAB-specific agonist SKF97541 were recorded with the cell-attached patch configuration. The open probability (Po) of both KNa and KCa channels was found to be increased by bath application of GABA, and this increase in Po was antagonized by coapplication of the GABAB antagonist CGP54626, suggesting that GABAB-like receptors mediate these actions. Similarly, GABAB-specific agonist SKF97541 increased the Po of both KNa and KCa channels. Perforated-patch recordings using β-escin further revealed that SKF97541 increased the amplitude of the outward currents elicited by step depolarizations. Under current-clamp conditions, SKF97541 decreased the firing frequency of spontaneous action potential (AP) and changed the AP waveform. The amplitude and duration of AP were decreased, whereas the afterhyperpolarization of AP was increased. Resting membrane potential, however, was not significantly altered by SKF97541. Taken together, these results suggest that GABAB-like receptor is functionally coupled with both KNa and KCa channels and this coupling mechanism may serve to prevent AP formation and limit excitatory synaptic input....(more)
Nakamura A, et al. J Neurophysiol 2013 Apr;109(7):1735-45.
Related Products: Escin
- 12. A Rapid Method for Total Β-Escin Analysis in Dry, Hydroalcoholic and Hydroglycolic Extracts of Aesculus hippocastanum L. by Capillary Zone Electrophoresis.
INTRODUCTION:
Seeds of Aesculus hippocastanum L. are used in European phytotherapy to treat inflammatory and vascular problems, and also to help in the regulation of the microcirculation. Thus, the quality control of herbal medicines using this species is important.
OBJECTIVE:
To develop and to optimise a capillary zone electrophoresis method to determine total β-escin in different extracts of A. hippocastanum L.
METHODS:
The optimal condition found through chemometric approach was: 25 mmol/L of bicarbonate-carbonate buffer, pH 10.3; +20 kV of voltage; 20°C of cartridge temperature; direct ultraviolet detection at 226 nm; 13 mbar injection for 5 s and analysis time within 6 min.
RESULTS:
Repeatability, coefficient of variation (CV; %) = 3.19, 3.07 and 1.89 (n = 12), and intermediate precision, CV (%) = 3.05, 3.53 and 2.99 (n = 24) for dry, hydroalcoholic and hydroglycolic extracts, respectively were achieved. The accuracy was evaluated through recovery tests in concentration levels of 100, 150 and 200 g/L, ranging from 98.17 to 104.68%. The proposed method exhibited linearity (r = 0.9983) in the concentration range from 101.4 to 907.2 g/L and limits of detection and quantification equal to 11.63 and 38.76 g/L respectively.
CONCLUSION:
A fast and reliable methodology for determination of total β-escin was successfully validated and applied on extracts of A. hippocastanum L. demonstrating its usefulness to quality control of medicines containing this plant species. Copyright © 2013 John Wiley & Sons, Ltd.
Copyright © 2013 John Wiley & Sons, Ltd....(more)
Dutra LS, et al. Phytochem Anal 2013 Mar 19.
Related Products: Escin
- 13. Synergistic protective effects of escin and low?dose glucocorticoids on blood?retinal barrier breakdown in a rat model of retinal ischemia.
Escin, a natural mixture of triterpenoid saponins isolated from the seed of the horse chestnut (Aesculus hippocastanum), has been demonstrated to possess glucocorticoid (GC)like antiedematous and antiinammatory effects. The aim of the present study was to investigate whether escin exhibits synergistic protective effects on bloodretinal barrier (BRB) breakdown when combined with GCs in a rat model of retinal ischemia. Low concentrations of escin and triamcinolone acetonide (TA) alone did not affect BRB permeability. However, when administered together, lowdose escin and TA significantly reduced BRB permeability following ischemia. Furthermore, lowdose escin and TA alone did not affect the expression of occludin in the ischemic retina; however, when administered together, they significantly increased occludin expression in the ganglion cell layer of the ischemic retina. This indicates that escin and GCs have synergistic protective effects on BRB breakdown and the molecular mechanisms may be correlated with the upregulation of occludin. Therefore, the administration of escin may allow a reduction in the dose of GCs for the treatment of macular edema. The combination of escin with GCs is potentially a beneficial treatment method for BRB breakdown and warrants further investigation....(more)
Zhang F, et al. Mol Med Rep 2013 May;7(5):1511-5.
Related Products: Escin
- 14. Preparation, purification and regioselective functionalization of protoescigenin-the main aglycone of escin complex.
A two-step chemical process for controlled degradation of escin, affording a mixture of olean-12-ene sapogenins, was elaborated and scaled up. The main component of the mixture-protoescigenin-was isolated and purified, in the form of its corresponding monohydrate, without resource to chromatographic methods. This material was further converted into the high purity 3,24;16,22-di-O,O-isopropylidene derivative in a validated large scale laboratory process....(more)
Gruza MM, et al. Molecules 2013 Apr 15;18(4):4389-402.
Related Products: Escin
- 15. 3',4'-Dihydroxyflavonol reduces vascular contraction through Ca²? desensitization in permeabilized rat mesenteric artery.
3',4'-Dihydroxyflavonol (DiOHF) exerts endothelium-independent relaxation in rat aortic rings. In this study, we hypothesized that DiOHF reduces vascular contraction through Ca² desensitization in permeabilized third-order branches of rat mesenteric arteries. The third-order branches of rat mesenteric arteries were permeabilized with β-escin and subjected to tension measurement. Cumulative addition of phenylephrine (0.3-30 μM) produced concentration-dependent vascular contraction of endothelium-intact and endothelium-denuded arterial rings, which were inhibited by pretreatment with DiOHF (10, 30, or 100 μM). In addition, DiOHF dose-dependently decreased vascular contractions induced by 3.0 μM phenylephrine. β-Escin-permeabilized third-order branches of mesenteric arteries were contracted with Ca², NaF, or guanosine-5'-(γ-thio)triphosphate (GTPγS) 30 min after pretreatment with DiOHF or vehicle. Pretreatment with DiOHF for 30 min inhibited vascular contraction induced by cumulative additions of Ca² (pCa 9.0-6.0) or NaF (4.0-16.0 mM) in permeabilized arterial rings. Cumulative addition of DiOHF also reduced vascular contraction induced by Ca²-controlled solution of pCa 6.0, 16.0 mM NaF, or 100 μM GTPγS in permeabilized arterial rings. DiOHF inhibited the increase in vascular tension provoked by calyculin A, even though it did not affect vascular tension already produced by calyculin A. DiOHF accelerated the relaxation induced by rapidly lowering Ca². DiOHF reduced vascular contraction through Ca² desensitization in permeabilized third-order branches of rat mesenteric arteries. These results suggest that DiOHF may have a therapeutic potential in the treatment of cardiovascular diseases....(more)
Kim HY, et al. Naunyn Schmiedebergs Arch Pharmacol 2012 Feb;385(2):191-202.
Related Products: Escin
- 16. The antinociceptive effect of intrathecal escin in the rat formalin test.
This study investigated the antinociceptive effect of intrathecal escin and examined its effect on the formalin-induced activation of c-Fos and phosphorylated p38 mitogen-activated protein kinase (p-p38 MAPK) in the rat spinal cord. Rats were chronically implanted with lumbar intrathecal catheters, and the ability of intrathecal escin to alter nociceptive behaviours in the rat formalin test was examined. The expression of c-Fos and p-p38 MAPK in the dorsal horn of the spinal cord was detected in the control and escin (40μg) groups using immunohistochemical techniques. Intrathecal escin produced a dose-dependent reduction in formalin-evoked flinching behaviour in rats during the second phase; however, no effect was observed in the first phase. In addition, immunohistochemical experiments showed that the expression of c-Fos and p-p38 MAPK in the spinal cord dorsal horn increased after an injection of formalin into the paw. Interestingly, the 40μg dose of intrathecal escin, which was the larger of the two doses that blocked formalin-induced hyperalgaesia, attenuated the formalin-induced increases in c-Fos and p-p38 MAPK in the dorsal horn of the spinal cord. The decrease in pain-related behaviours and c-Fos expression indicated that escin produced antinociceptive effects in the rat formalin test. Although the specific mechanisms of these effects were not investigated, the reduction in p-p38 MAPK in the dorsal horn of the spinal cord may be involved....(more)
Li Q, et al. Eur J Pharmacol 2012 Jan 15;674(2-3):234-8.
Related Products: Escin
- 17. Comparative pharmacokinetics and bioavailability of escin Ia and isoescin Ia after administration of escin and of pure escin Ia and isoescin Ia in rat.
ETHNOPHARMACOLOGICAL RELEVANCE:
Escin Ia and isoescin Ia have been traditionally used clinically as the chief active ingredients of escin, a major triterpene saponin isolated from horse chestnut (Aesculus hippocastanum) seeds for the treatment of chronic venous insufficiency, hemorrhoids, inflammation and edema.
AIM OF THE STUDY:
To establish a sensitive LC-MS/MS method and investigate the pharmacokinetic properties of escin Ia and isoescin Ia in rats and the pharmacokinetics difference of sodium escinate with pure escin Ia and isoescin Ia. The absolute bioavailability of escin Ia and isoescin Ia and the bidirectional interconversion of them in vivo were also scarcely reported.
MATERIALS AND METHODS:
Wister rats were administrated an intravenous (i.v.) dose (1.7 mg/kg) of sodium escinate (corresponding to 0.5mg/kg of escin Ia and 0.5mg/kg of isoescin Ia, respectively) and an i.v. dose (0.5mg/kg) or oral dose (4mg/kg) of pure escin Ia or isoescin Ia, respectively. At different time points, the concentrations of escin Ia and isoescin Ia in rat plasma were determined by LC-MS/MS method. Main pharmacokinetic parameters including t(1/2), MRT, CL, V(d), AUC and F were estimated by non-compartmental analysis using the TopFit 2.0 software package (Thomae GmbH, Germany) and statistical analysis was performed using the Student's t-test with P<0.05 as the level of significance.
RESULTS:
After administration of sodium escinate, the t(1/2) and MRT values for both escin Ia and isoescin Ia were larger than corresponding values for the compounds given alone. Absorption of escin Ia and isoescin Ia was very low with F values both <0.25%. Escin Ia and isoescin Ia were found to form the other isomer in vivo with the conversion of escin Ia to isoescin Ia being much extensive than from isoescin Ia to escin Ia.
CONCLUSION:
Comparison of the pharmacokinetics of escin Ia and isoescin Ia given alone and together in rat suggest that administration of herbal preparations of escin for clinical use may provide longer duration of action than administration of single isomers. The interconversion of escin Ia and isoescin Ia when given alone indicates that administration of one isomer leads to exposure to the other.
Copyright © 2011 Elsevier Ireland Ltd. All rights reserved....(more)
Wu XJ, et al. J Ethnopharmacol 2012 Jan 6;139(1):201-6.
Related Products: Escin
- 18. Protective effect of esculetin on hyperglycemia-mediated oxidative damage in the hepatic and renal tissues of experimental diabetic rats.
Diabetes mellitus is the most common serious metabolic disorder and it is considered to be one of the five leading causes of death in the world. Hyperglycemia-mediated oxidative stress plays a crucial role in diabetic complications. Hence, this study was undertaken to evaluate the protective effect of esculetin on the plasma glucose, insulin levels, tissue antioxidant defense system and lipid peroxidative status in streptozotocin-induced diabetic rats. Diabetic rats exhibited increased blood glucose with significant decrease in plasma insulin levels. Extent of oxidative stress was assessed by the elevation in the levels of lipid peroxidation markers such as thiobarbituric acid reactive substances (TBARS), lipid hydroperoxides (HP) and conjugated dienes (CD); reduction in the enzymic antioxidant enzymes like superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione-S-transferase (GST); nonenzymic antioxidants Vitamin C, E and reduced glutathione (GSH) were observed in the liver and kidney tissues of diabetic control rats as compared to control rats. Oral supplementation of esculetin to diabetic rats for 45 days significantly brought back lipid peroxidation markers, enzymic and nonenzymic antioxidants to near normalcy. Moreover, the histological observations evidenced that esculetin effectively rescues the hepatocytes and kidney from hyperglycemia mediated oxidative damage without affecting its cellular function and structural integrity. These findings suggest that esculetin (40 mg/kg BW) treatment exerts a protective effect in diabetes by attenuating hyperglycemia-mediated oxidative stress and antioxidant competence in hepatic and renal tissues. Further, detailed studies are in progress to elucidate the molecular mechanism by which esculetin elicits its modulatory effects in insulin signaling pathway....(more)
Prabakaran D, et al. Biochimie 2013 Feb;95(2):366-73.
Related Products: Esculetin
- 19. Novel macrocyclic monoterpene glycosides from bioactive extract of Parkinsonia aculeata L.
Five novel macrocyclic monoterpene O-glycosides, parkinsenes A-E (1-5), and eleven known phenolic metabolites including three 3-O-glycosylflavonols (6-8), five C-glycosylflavones (9-13), p-hydroxybenzoic acid (14), esculetin (15), and diosmetin (16) were isolated from the leaves and small twigs of Parkinsonia aculeata L. (Fabaceae). Their structures were established by chemical and spectroscopic analyses (UV, ESI-MS, and 1D/2D NMR). The investigated 80 % aqueous methanol extract (AME) showed significant analgesic, antipyretic, anti-inflammatory, hepatoprotective, hypoglycemic, hypocholesterolemic, and antioxidant activities in a dose-dependent manner using two different doses 250 and 500 mg/kg b. wt....(more)
Marzouk MS, et al. Cell Biochem Biophys 2013 Apr;65(3):301-13.
Related Products: Esculetin
- 20. Neuroprotective effects of umbelliferone and esculetin in a mouse model of Parkinson's disease.
The production of reactive oxygen species and mitochondrial dysfunction in the brain are both associated with the progression of several neurodegenerative diseases, including Parkinson's disease. These characteristics are also observed when rodents are exposed to the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), a compound that causes nigrostriatal dopaminergic neurotoxicity and that has been used previously for assessing the effectiveness of neuroprotective agents. In this study, the neuroprotective effects of two coumarins, umbelliferone and esculetin, against MPTP-induced neurotoxicity were examined in C57BL/6J mice. The results show that dietary administration of umbelliferone and esculetin significantly attenuated MPTP-induced neurotoxicity in the substantia nigra pars compacta but not striatum, as measured by tyrosine hydroxylase staining. Both coumarins also prevented an MPTP-induced increase in nitrosative stress as measured by 3-nitrotyrosine immunoreactivity and also maintained glutathione levels in MPTP-exposed mice as well as in cell lines exposed to the metabolite 1-methyl-4-phenylpyridinium. Umbelliferone and esculetin also prevented MPTP-dependent caspase 3 activation, an indicator of apoptosis, but did not inhibit monoamine oxidase activity. This is the first time that the neuroprotective capabilities of these coumarins have been demonstrated, and the results indicate that umbelliferone and esculetin can protect against MPTP-induced neurotoxicity in the mouse. These compounds can cross the blood-brain barrier, so their effectiveness indicates that they have the potential to protect in neurodegenerative disease such as Parkinson's disease....(more)
Subramaniam SR, et al. J Neurosci Res 2013 Mar;91(3):453-61.
Related Products: Esculetin
- 21. Evaluation of percutaneous absorption of esculetin: effect of chemical enhancers.
Percutaneous transdermal absorption of esculetin (6,7-dihydroxycoumarin), an oxidative damage inhibitor, was evaluated by means of in vitro permeation studies in which vertical Franz-type diffusion cells and pig ear skin were employed. To determine the absorption of esculetin, we validated a simple, accurate, precise, and rapid HPLC-UV method. Additionally, the effects of several percutaneous enhancers were studied. Pretreatment of porcine skin was performed with ethanol (control vehicle), decenoic acid, oleic acid, R-(+)-limonene, and laurocapram (Azone®) (5% in ethanol, w/w, respectively). Pretreatment of skin with oleic acid or laurocapram led to statistically significant differences in the transdermal flux of esculetin with respect to controls. Of the two enhancers, laurocapram showed the greatest capacity to enhance the flux of esculetin across pig skin....(more)
del Rio Sancho S, et al. Planta Med 2013 Jan;79(2):131-6.
Related Products: Esculetin
- 22. Investigations of FT-IR, FT-Raman, FT-NMR spectra and quantum chemical computations of Esculetin molecule.
In this work, we report a combined experimental and theoretical study on molecular structure, vibrational spectra and electronic properties of Esculetin (ESC). The FT-IR, FT-Raman and FT-NMR spectra have been recorded and analyzed. The molecular geometry, harmonic vibrational frequencies, chemical shifts, HOMO, LUMO energies and molecular electrostatic potential map of ESC have been calculated by using Density Functional Theory (B3LYP) with 6-311G++(d,p), cc-pVDZ, cc-pVQZ and cc-pVTZ basis sets....(more)
Erdogdu Y. Spectrochim Acta A Mol Biomol Spectrosc 2013 Apr;106:25-33.
Related Products: Esculetin
- 23. Potent α-glucosidase and protein tyrosine phosphatase 1B inhibitors from Artemisia capillaris.
As a part of our ongoing effort to identify anti-diabetic constituents from natural sources, we examined the inhibitory activity of the methanol extracts of 12 species of the genus Artemisia, against α-glucosidase and protein tyrosine phosphatase 1B (PTP1B). The methanol extracts of different species exhibited promising α-glucosidase and PTP1B inhibitory activities. Since the methanol extract of Artemisia capillaris exhibited the highest α-glucosidase inhibitory activity together with significant PTP1B inhibitory activity, it was selected for further investigation. Repeated column chromatography based on bioactivity guided fractionation yielded 10 coumarins (esculetin, esculin, scopolin, isoscopolin, daphnetin, umbelliferone, 7-methoxy coumarin, scoparone, scopoletin, 6-methoxy artemicapin C), 8 flavonoids (hyperoside, quercetin, isorhamnetin, cirsilineol, arcapillin, isorhamnetin 3-robinobioside, linarin, isorhamnetin 3-glucoiside), 6 phenolic compounds (1,5-dicaffeoylquinic acid, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid methyl ester, 4,5-dicaffeoylquinic acid, 3-caffeoylquinic acid), and one chromone (capillarisin). Among these compounds, esculetin, scopoletin, quercetin, hyperoside, isorhamnetin, 3,5-dicaffeoylquinic acid methyl ester, 3,4-dicaffeoylquinic acid, and 1,5-dicaffeoylquinic acid exhibited potent α-glucosidase inhibitory activity when compared to the positive control acarbose. In addition, esculetin and 6-methoxy artemicapin C displayed PTP1B inhibitory activity. Interestingly, all isolated dicaffeoylquinic acids showed significant PTP1B inhibitory activity. Therefore, the results of the present study clearly demonstrate the potential of the A. capillaris extract to inhibit α-glucosidase and PTP1B. These inhibitory properties can be largely attributed to a combination of different chemical structures, including coumarins, flavonoids, and dicaffeoylquinic acids, which could be further explored to develop therapeutic or preventive agents for the treatment of diabetes....(more)
Nurul Islam M, et al. Arch Pharm Res 2013 Feb 24.
Related Products: Esculetin
- 24. Pro-inflammatory properties and neutrophil activation by Helicobacter pylori urease.
The gastric pathogen Helicobacter pylori produces large amounts of urease, whose enzyme activity enables the bacterium to survive in the stomach. We have previously shown that ureases display enzyme-independent effects in mammalian models, most through lipoxygenases-mediated pathways. Here, we evaluated potential pro-inflammatory properties of H. pylori urease (HPU). Mouse paw edema and activation of human neutrophils were tested using a purified, cell-free, recombinant HPU. rHPU induced paw edema with intense neutrophil infiltration. In vitro 100 nM rHPU was chemotactic to human neutrophils, inducing production of reactive oxygen species. rHPU-activated neutrophils showed increased lifespan, with inhibition of apoptosis accompanied by alterations of Bcl-XL and Bad contents. These effects of rHPU persisted in the absence of enzyme activity. rHPU-induced paw edema, neutrophil chemotaxis and apoptosis inhibition reverted in the presence of the lipoxygenase inhibitors esculetin or AA861. Neutrophils exposed to rHPU showed increased content of lipoxygenase(s) and no alteration of cyclooxygenase(s). Altogether, our data indicate that HPU, besides allowing the bacterial survival in the stomach, could play an important role in the pathogenesis of the gastrointestinal inflammatory disease caused by H. pylori....(more)
Uberti AF, et al. Toxicon 2013 Mar 1.
Related Products: Esculetin
- 25. Evaluation of anti-obesity effect of Aegle marmelos leaves.
The study was carried out to investigate the anti-obesity effects of Aegle marmelos leaves extracts and its phytochemical constituents in vitro and in vivo. The dichloromethane (DCM), ethyl acetate (EtOAc) and n-butanol extracts of A. marmelos leaves were studied for their lipolytic effect. Lipolysis was measured by determining the amount of glycerol released at 12h and 24h at 50μg/ml and 100μg/ml concentrations. Phytochemical investigation of the most active DCM extract yielded 14 compounds. The isolated compounds were evaluated for their lipolytic effects at 50μM and 100μM. The most active compounds, umbelliferone and esculetin were further screened for their antiobesity effects in vivo in the high fat diet (HFD) induced obese rat model. Umbelliferone and esculetin reduced body weight, total triglyceride (TG), total cholesterol (TC) and glucose level in their respective HFD groups. A. marmelos DCM extract and compounds isolated from it have the potential of counteracting the obesity by lipolysis in adipocytes....(more)
Karmase A, et al. Phytomedicine 2013 Apr 27.
Related Products: Esculetin
- 26. Different Expression Profiles of Bioactive Peptides in Pelophylax nigromaculatus from Distinct Regions.
Amphibian skin is an abundant repository of bioactive peptides, important components of the defensive system. The variability of the bioactive peptide repertoires of individual species remains unclear. In this study, dark-spotted frogs were collected from Kunming in Yunnan Province, China and Guiyang in Guizhou Province, China to determine whether the bioactive peptides in amphibian skin differ between the two regions. Eight antimicrobial peptides and an antioxidant peptide were identified by screening of cDNA library. Among the identified peptides, three antimicrobial peptides (pelophylaxin-2GY, temporin-1GY, and temporin-1KM) and an antioxidant peptide (antioxidin-PN) are reported here for the first time. Nigrocin-1, nigrocin-2, and pelophylaxin-2 were expressed by frogs in both regions. Pelophylaxin-2GY and temporin-1GY were found only in the frogs from Guiyang, whereas antioxidin-PN, esculetin-1, esculetin-2, and temporin-1KM were found only in those from Kunming. This difference was confirmed by allele-specific RT-PCR. The bioactive peptides expressed clearly varied between these populations of the same species....(more)
Song Y, et al. Biosci Biotechnol Biochem 2013 May 7.
Related Products: Esculetin
- 27. Drought stress has contrasting effects on antioxidant enzymes activity and phenylpropanoid biosynthesis in Fraxinus ornus leaves: an excess light stress affair?
The experiment was conducted using Fraxinus ornus plants grown outside under full sunlight irradiance, and supplied with 100% (well-watered, WW), 40% (mild drought, MD), or 20% (severe drought, SD) of the daily evapotranspiration demand, with the main objective of exploring the effect of excess light stress on the activity of antioxidant enzymes and phenylpropanoid biosynthesis. Net CO assimilation rate at saturating light and daily assimilated CO were significantly smaller in SD than in WW and MD plants. Xanthophyll-cycle pigments supported nonphotochemical quenching to a significantly greater extent in SD than in MD and WW leaves. As a consequence, the actual efficiency of PSII (Φ(PSII)) was smaller, while the excess excitation-energy in the photosynthetic apparatus was greater in SD than in WW or MD plants. The concentrations of violaxanthin-cycle pigments relative to total chlorophyll (Chl(tot)) exceeded 200 mmol mol¹ Chl(tot) in SD leaves at the end of the experiment. This leads to hypothesize for zeaxanthin a role not only as nonphotochemical quencher, but also as chloroplast antioxidant. Reductions in ascorbate peroxidase and catalase activities, as drought-stress progressed, were paralleled by greater accumulations of esculetin and quercetin 3-O-glycosides, both phenylpropanoids having effective capacity to scavenge HO. The drought-induced accumulation of esculetin and quercetin 3-O-glycosides in the vacuoles of mesophyll cells is consistent with their putative functions as reducing agents for HO in excess light-stressed leaves. Nonetheless, the concentration of HO and the lipid peroxidation were significantly greater in SD than in MD and WW leaves. It is speculated that vacuolar phenylpropanoids may constitute a secondary antioxidant system, even on a temporal basis, activated upon the depletion of primary antioxidant defences, and aimed at keeping whole-cell HO within a sub-lethal concentration range....(more)
Fini A, et al. J Plant Physiol 2012 Jul 1;169(10):929-39.
Related Products: Esculetin
- 28. Plant bio-transformable HMG-CoA reductase gene loaded calcium phosphate nanoparticle: in vitro characterization and stability study.
Encapsulation of plasmid DNA in nanoparticle is expected to enhance the stability of DNA, reproducibility and frequency of the genetic transformation in plants. Here we report the formulation of HMG Co-A reductase gene loaded calcium phosphate nanoparticles (Cap nanoparticles) and their in-vitro, in-vivo characterization. The developed Cap nanoparticles were characterized by DSC, FT-IR, and XRD. Developed Cap nanoparticles were spherical in shape having the particle size and zeta potential in the range of 10.86±0.09nm to 33.42±0.18nm and -25.5±0.07mV to -31.7±0.07mV (for Cap-I to Cap-IV). DNA releasing in acidic media showed, initially slow release followed by fast release with a maximum release of Cap-I (95.77±1.39%) > Cap-II (87.32±2.07%) > Cap-III (76.54±2.01%) > Cap-IV (72.93±1.75%) over 60min. Cap nanoparticles were quite stable at storage condition of 40±0.5°C/75±5%RH, 25±0.5°C/60±RH, 4±0.5°C/ambient humidity and the integrity of pDNA encapsulated was confirmed by gel electrophoresis. Compared to wild type C. intybus, transformation efficiency and enhanced biosynthesis of esculin with the DNA nanoparticles in C. intybus were about 10% and 71%, respectively. Antioxidant activity capacity of the biotransformed plants was significantly higher than the normal plant due to high accumulation of esculin....(more)
Ohadi R MS, et al. Curr Drug Discov Technol 2013 Mar;10(1):25-34.
Related Products: Esculin
- 29. Streptococcus danieliae sp. nov., a novel bacterium isolated from the caecum of a mouse.
We report the characterization of one novel bacterium, strain ERD01G(T), isolated from the cecum of a TNF(deltaARE) mouse. The strain was found to belong to the genus Streptococcus based on phylogenetic analysis of partial 16S rRNA gene sequences. The bacterial species with standing name in nomenclature that was most closely related to our isolate was Streptococcus alactolyticus (97 %). The two bacteria were characterized by a DNA-DNA hybridization similarity value of 35 %, demonstrating that they belong to different species. The new isolate was negative for acetoin production, esculin hydrolysis, urease, α-galactosidase and β-glucosidase, was able to produce acid from starch and trehalose, grew as beta-hemolytic coccobacilli on blood agar, did not grow at >40 °C, did not survive heat treatment at 60 °C for 20 min and showed negative agglutination in Lancefield tests. On the basis of these characteristics, strain ERD01G(T) differed from the most closely related species S. alactolyticus, Streptococcus gordonii, Streptococcus intermedius and Streptococcus sanguinis. Thus, based on genotypic and phenotypic evidence, we propose that the isolate belongs to a novel bacterial taxon within the genus Streptococcus, for which the name Streptococcus danieliae is proposed. The type strain is ERD01G(T) (= DSM 22233(T) = CCUG 57647(T))....(more)
Clavel T, et al. Arch Microbiol 2013 Jan;195(1):43-9.
Related Products: Esculin
- 30. Chryseobacterium frigidisoli sp. nov., a psychrotolerant species of the family Flavobacteriaceae isolated from a glacier forefield of the Larsemann Hills, East Antarctica.
In the scope of diversity studies in glacier forefields on the Larsemann Hills, East Antarctica, a novel psychrotolerant, non-motile Gram-negative, shiny yellow, rod-shaped, aerobic bacterium PB4T was isolated from a soil sample. Strain PB4T produces indole from tryptophan and hydrolyses casein. It grows between 0°C and 25°C with an optimum growth temperature at 20°C. A wide range of substrates are used as sole carbon source and acid is produced from from esculin ferric citrate, D-cellobiose, D-maltose, D-lactose, D-saccharose, D-trehalose, D-melizitose, glycogen, amidon (starch) and gentibiose and weak from D-glucose, amygdalin, salicin and D-turanose. The major menaquinone is MK-6. Identified major fatty acids (>10%) are iso-C15:0 (13.0%) and iso-2OH-C15:0 (51.2%). G+C content is 33.7 mol%. For strain PB4T, highest 16S rRNA gene sequence similarity was found to the type strains of Chryseobacterium humi (97.0%) and Chryseobacterium marinum (96.5%). Considering phenotypic and genotypic characterisation, strain PB4T represents a novel species in the genus Chryseobacterium (Flavobacteriaceae), for which the name Chryseobacterium frigidisoli is proposed. The type strain is PB4T (LMG 27025)....(more)
Bajerski F, et al. Int J Syst Evol Microbiol 2013 Jan 4.
Related Products: Esculin
- 31. Potent α-glucosidase and protein tyrosine phosphatase 1B inhibitors from Artemisia capillaris.
As a part of our ongoing effort to identify anti-diabetic constituents from natural sources, we examined the inhibitory activity of the methanol extracts of 12 species of the genus Artemisia, against α-glucosidase and protein tyrosine phosphatase 1B (PTP1B). The methanol extracts of different species exhibited promising α-glucosidase and PTP1B inhibitory activities. Since the methanol extract of Artemisia capillaris exhibited the highest α-glucosidase inhibitory activity together with significant PTP1B inhibitory activity, it was selected for further investigation. Repeated column chromatography based on bioactivity guided fractionation yielded 10 coumarins (esculetin, esculin, scopolin, isoscopolin, daphnetin, umbelliferone, 7-methoxy coumarin, scoparone, scopoletin, 6-methoxy artemicapin C), 8 flavonoids (hyperoside, quercetin, isorhamnetin, cirsilineol, arcapillin, isorhamnetin 3-robinobioside, linarin, isorhamnetin 3-glucoiside), 6 phenolic compounds (1,5-dicaffeoylquinic acid, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid methyl ester, 4,5-dicaffeoylquinic acid, 3-caffeoylquinic acid), and one chromone (capillarisin). Among these compounds, esculetin, scopoletin, quercetin, hyperoside, isorhamnetin, 3,5-dicaffeoylquinic acid methyl ester, 3,4-dicaffeoylquinic acid, and 1,5-dicaffeoylquinic acid exhibited potent α-glucosidase inhibitory activity when compared to the positive control acarbose. In addition, esculetin and 6-methoxy artemicapin C displayed PTP1B inhibitory activity. Interestingly, all isolated dicaffeoylquinic acids showed significant PTP1B inhibitory activity. Therefore, the results of the present study clearly demonstrate the potential of the A. capillaris extract to inhibit α-glucosidase and PTP1B. These inhibitory properties can be largely attributed to a combination of different chemical structures, including coumarins, flavonoids, and dicaffeoylquinic acids, which could be further explored to develop therapeutic or preventive agents for the treatment of diabetes....(more)
Nurul Islam M, et al. Arch Pharm Res 2013 Feb 24.
Related Products: Esculin
- 32. Description of Xenorhabdus khoisanae sp. nov., the symbiont of the entomopathogenic nematode Steinernema khoisanae.
Bacterial strain SF87, and additional strains SF80, SF362 and 106-C, isolated from the nematode Steinernema khoisanae, are non-bioluminescent Gram-negative bacteria that share many of the carbohydrate fermentation reactions recorded for the type strains of previously described Xenorhabdus spp. Based on the 16S rRNA gene sequence data, strain SF87 is 98% related to Xenorhabdus hominickii. Nucleotide sequences of strain SF87 obtained from the recA, dnaN, gltX, gyrB and infB genes showed 96 to 97% similarity with Xenorhabdus miraniensis. However, strain SF87 shares only 52.7% DNA homology with the type strain of X. miraniensis by DNA-DNA hybridization analysis, confirming that it belongs to a different species. Strains SF87, SF80, SF362 and 106-C are phenotypically similar to X. miraniensis and X. beddingii, except that they do not produce acid from esculin. Xenorhabdus khoisanae sp. nov. is proposed as a new species of the genus Xenorhabdus (type strain SF87<sup>T</sup>, DSM 25463<sup>T</sup>, ATCC BAA-2406<sup>T</sup>)....(more)
Ferreira T, et al. Int J Syst Evol Microbiol 2013 Mar 1.
Related Products: Esculin
- 33. A novel method for screening beta-glucosidase inhibitors.
BACKGROUND:
Few beta-glucosidase inhibitors have so far been reported from microorganisms due to the practical difficulties in performing the inhibition tests and subsequent interpretation of results. In an effort to investigate marine microbial extracts for β-glucosidase inhibitors, we developed a new protocol, using esculin as substrate in an agar plate based assay, to screen a large number of microbial extracts in a short span of time.
RESULTS:
With the new method, pale yellowish zones against the blackish brown background could be visually observed with more clarity in sample extracts where β-glucosidase inhibitor was present. The new method was compared with the closest existing method and established beyond doubt. This agar plate based procedure required about one hour for minimum 12 samples and the throughput increases with the size of the agar gel plate used.
CONCLUSIONS:
The new protocol was simple, rapid and effective in detecting beta-glucosidase inhibitors in microbial extracts....(more)
Pandey S, et al. BMC Microbiol 2013 Mar 8;13:55.
Related Products: Esculin
- 34. Spirostanol saponins and esculin from Rusci rhizoma reduce the thrombin-induced hyperpermeability of endothelial cells.
Rusci rhizoma extracts are traditionally used against chronic venous disorders (CVD). To determine the effect of its secondary plant metabolites on the endothelium, phenolic compounds and saponins from Butcher's broom were isolated from a methanolic extract, and their activity on the thrombin-induced hyperpermeability of human microvascular endothelial cells (HMEC-1) was investigated in vitro. In addition to the six known spirostanol saponins deglucoruscin (5), 22-O-methyl-deglucoruscoside (6), deglucoruscoside (7), ruscin (8), ruscogenin-1-O-(α-l-rhamnopyranosyl-(1→2)-β-d-galactopyranoside (9) and 1-O-sulpho-ruscogenin (10), three new spirostanol derivatives were isolated and identified: 3'-O-acetyl-4'-O-sulphodeglucoruscin (1), 4'-O-(2-hydroxy-3-methylpentanoyl)-deglucoruscin (2) and 4'-O-acetyl-deglucoruscin (3). Furthermore, the coumarin esculin (4), which is also prominently present in other medicinal plants used in the treatment of CVD, was isolated for the first time from Rusci rhizoma. Five of the isolated steroid derivatives (2, 5, 8, 9 and 10) and esculin (4) were tested for their ability to reduce the thrombin-induced hyperpermeability of endothelial cells in vitro, and the results were compared to those of the aglycone neoruscogenin (11). The latter compound showed a slight but concentration-dependent reduction in hyperpermeability to 71.8% at 100μM. The highest activities were observed for the spirostanol saponins 5 and 8 and for esculin (4) at 10μM, and these compounds resulted in a reduction of the thrombin-induced hyperpermeability to 41.9%, 42.6% and 53.3%, respectively. For 2, 5 and 8, the highest concentration tested (100μM) resulted in a drastic increase of the thrombin effect. The effect of esculin observed at a concentration of 10μM was diminished at 100μM. These in vitro data provide insight into the pharmacological mechanism by which the genuine spirostanol saponins and esculin can contribute to the efficacy of Butcher's broom against chronic venous disorders....(more)
Barbi? M, et al. Phytochemistry 2013 Jun;90:106-13.
Related Products: Esculin
- 35. Bartonella bovis isolated from a cow with endocarditis.
A 7-year-old pregnant Angus cow was found dead in the field. At necropsy, the aortic valve was expanded by moderate fibrous connective tissue and acidophilic coagulum containing multifocal marked bacteria, mineral, neutrophils, and red blood cells. Numerous tiny grayish, opaque bacterial colonies were detected on blood agar plates at 7 days after inoculation with a swab of the heart valve of the cow. The bacterium was a Gram-negative, very small coccobacillus that was catalase, oxidase, and urease negative, and did not change litmus milk, triple sugar iron agar, and sulfide-indole-motility medium. The bacterium was negative for esculin hydrolysis, phenylalanine deaminase, nitrate reduction, and gelatin hydrolysis. The isolate did not produce acid from glycerol, inulin, lactose, maltose, mannose, raffinose, salicin, sorbitol, sucrose, trehalose, glycogen, ribose, or starch. Polymerase chain reaction tests for the gltA, ssrA, ftsZ, ribC, rpoB, and 16S ribosomal RNA genes of Bartonella species were positive for the isolate. Amplicons were sequenced, and the gltA, ribC, ssrA, and 16S ribosomal RNA gene sequences were found to have 100% homology to the type strain of Bartonella bovis, whereas the fts and rpoB sequences showed 99.9% and 99.6% homology, respectively, to the type strain of Bartonella bovis. Diagnosticians should be aware of slow-growing microorganisms, and culture media should be incubated beyond the standard period to enhance the recovery of Bartonella species....(more)
Erol E, et al. J Vet Diagn Invest 2013 Mar;25(2):288-90.
Related Products: Esculin