Research Update:Horse chestnut and aescin

  seminal trace...Horse chestnut Aescin.Horse Chestnut Extract.CAS.NO.090045-79-7.Aescin,Escin.beta-Escin.20.0%UV.CAS.NO:6805-41-0.M.F.:C55 H86O24.Extract of horse chestnut; Aesculus hippocastanum extract;Aesculus glabra,ext......

 


   Phytochemical info of Horse chestnut:

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 Definition:Horse chestnut extract are majorly composed of
 Chemical information disclosed as following table:


  Research Update:Horse chestnut and aescin

  Studying of technological properties of horse-chestnut leaves.:Georgian Med News. 2006 Dec;(141):79-81.Goletiani K, Bashura A, Polovko N, Bashura A, Tsagareishvili G. National pharmaceutical university of Kharkov, cathedra of cosmetology and aromatology; Kutateladze Institute of Pharmacochemistry of Academy of Science of Georgia.

 In order to prepare the new remedy - the tincture of leafs of horse-chestnut, we studied technological parameters of the vegetal material. With the purpose of definition of optimal conditions of extraction of operating substance from vegetative raw materials, calculation of norm of raw material charge and extractive by development technological regulations, and also for management for process of extracting have been studied some technological properties of horse-chestnut. In the course of experimental works, there were specified relative density, bulk weight and volume weight; porosity, free volume of a layer of a raw material, rate of water absorption. The results of studies are used in development of technology of tincture of horse-chestnut leaves.

  Flavonol Oligosaccharides from the Seeds of Aesculus hippocastanum.:Planta Med. 1999 Oct;65(7):636-42.Hubner G, Wray V, Nahrstedt A.1 Institute of Pharmaceutical Biology and Phytochemistry, Westf. Wilhelms-Universitat Munster, Germany.

 Nine flavonol oligosides of quercetin and kaempferol with glucose, xylose, and rhamnose as sugars were isolated from the seeds of AESCULUS HIPPOCASTANUM L. (Hippocastanaceae). Five of them are new compounds (2 trisaccharides, 1 bisdesmoside, a nicotinic and a indolinone hydroxyacetic acid ester of the bisdesmoside). Their structures were elucidated mainly using ( 1)H- and (13)C-NMR techniques.

  A horse chestnut extract, which induces contraction forces in fibroblasts, is a potent anti-aging ingredient.:J Cosmet Sci. 2006 Sep-Oct;57(5):369-76.

 Contraction forces generated by non-muscle cells, such as fibroblasts, play important roles in determining cell morphology, vasoconstriction, and/or wound healing. We have searched among various plant extracts for ingredients that generate cell contraction forces using fibroblast-populated collagen gels. Using that model, we found that an extract of horse chestnuts (Aesculus hippocastanum) is able to generate such contraction forces in fibroblasts. The involvement of stress fiber formation in that response is suggested by the inhibition of such force generation by cytochalasin D and rhodamine phalloidin stain. Clinical testing of the extract was carried out using 40 healthy female volunteers. A gel formulation that included 3% of the extract was applied topically to the skin around the eye three times daily for nine weeks. The efficacy of the extract to diminish wrinkles was evaluated by visual scoring based on photo scales. After six weeks, significant decreases in the wrinkle scores at the corners of the eye or in the lower eyelid skin were observed compared with controls. After nine weeks, similar results were obtained. Taken together, our results suggest that an extract of horse chestnuts can generate contraction forces in fibroblasts and is a potent anti-aging ingredient.

  A review of the microcirculation in skin in patients with chronic venous insufficiency: the problem and the evidence available for therapeutic options..:Int J Low Extrem Wounds. 2006 Sep;5(3):169-80.Wollina U, Abdel-Naser MB, Mani R. Department of Dermatology, Hospital Dresden-Friedrichstadt, Academic Teaching Hospital of the Technical University of Dresden, Germany. wollina-uw@khdf.de.

 Impairment of the cutaneous microcirculation is a major predisposing factor in inflammation and ulceration in patients with chronic venous insufficiency (CVI). Increase of capillary filtration rate predisposes to the formation of edema. Local lymphedema is a complication of CVI, often underdiagnosed. This review is focused on CVI but excludes the complication of ulceration. Treatment of microcirculatory dysfunction can be done by pharmacologic intervention or compression therapy or using a combination of both. This review is focused on drugs that have been evaluated by randomized prospective controlled trials. The following compounds are discussed: horse chestnut seed extracts, flavonoids, red vine leaves extracts, total triterpenic fraction of Centella asiatica (L), prociadins, calcium dobesilate, and pentoxifylline. The microcirculatory effects of compression therapy using bandages or stockings are also reviewed. The major microcirculatory effects that have been shown are the reduction of capillary filtration rate and improvements in levels of transcutaneous partial pressures of oxygen and carbon dioxide (TcPO(2) and TcPCO(2)). Available data suggest that a combination of pharmacologic and compression therapy may have some additive effects.

  Beta-escin inhibits colonic aberrant crypt foci formation in rats and regulates the cell cycle growth by inducing p21(waf1/cip1) in colon cancer cells.:Mol Cancer Ther. 2006 Jun;5(6):1459-66.Patlolla JM, Raju J, Swamy MV, Rao CV. Department of Medicine, OU Cancer Institute, University of Oklahoma Health Sciences Center, 975 Northeast 10th Street, Oklahoma City, OK 73104, USA.

 Extracts of Aesculus hippocastanum (horse chestnut) seed have been used in the treatment of chronic venous insufficiency, edema, and hemorrhoids. Most of the beneficial effects of horse chestnut are attributed to its principal component beta-escin or aescin. Recent studies suggest that beta-escin may possess anti-inflammatory, anti-hyaluronidase, and anti-histamine properties. We have evaluated the chemopreventive efficacy of dietary beta-escin on azoxymethane-induced colonic aberrant crypt foci (ACF). In addition, we analyzed the cell growth inhibitory effects and the induction of apoptosis in HT-29 human colon cancer cell line. To evaluate the inhibitory properties of beta-escin on colonic ACF, 7-week-old male F344 rats were fed experimental diets containing 0%, 0.025%, or 0.05% beta-escin. After 1 week, the rats received s.c. injections of azoxymethane (15 mg/kg body weight, once weekly for 2 weeks) or an equal volume of normal saline (vehicle). Rats were continued on respective experimental diets and sacrificed 8 weeks after the azoxymethane treatment. Colons were evaluated histopathologically for ACF. Administration of dietary 0.025% and 0.05% beta-escin significantly suppressed total colonic ACF formation up to approximately 40% (P < 0.001) and approximately 50% (P < 0.0001), respectively, when compared with control diet group. Importantly, rats fed beta-escin showed dose-dependent inhibition (approximately 49% to 65%, P < 0.0001) of foci containing four or more aberrant crypts. To understand the growth inhibitory effects, HT-29 human colon carcinoma cell lines were treated with various concentrations of beta-escin and analyzed by flow cytometry for apoptosis and cell cycle progression. Beta-escin treatment in HT-29 cells induced growth arrest at the G1-S phase, which was associated with the induction of the cyclin-dependent kinase inhibitor p21(WAF1/CIP1), and this correlated with reduced phosphorylation of retinoblastoma protein. Results also indicate that beta-escin inhibited growth of colon cancer cells with either wild-type or mutant p53. This novel feature of beta-escin, a triterpene saponin, may be a useful candidate agent for colon cancer chemoprevention and treatment.


  Treatment of patients with venous insufficiency with fresh plant horse chestnut seed extract: a review of 5 clinical studies.:Adv Ther. 2006 Jan-Feb;23(1):179-90.Suter A, Bommer S, Rechner J.Medical Department, Bioforce AG, Roggwil, Switzerland.

 Extracts from the seed of the horse chestnut (Aesculus hippocastanum L.) have traditionally been used to treat patients with chronic venous insufficiency and to alleviate its associated symptoms, including lower leg swelling. The efficacy of preparations that contain horse chestnut seed extract (HCSE) is believed to be due largely to an inhibitory effect on the catalytic breakdown of capillary wall proteoglycans. Aesculaforce is a fresh plant HCSE that is available as an oral tincture, as tablets (20 mg or 50 mg), and as topical gel. Four clinical trials in patients with chronic venous insufficiency and 1 study in patients with varicose veins demonstrated the effectiveness of these preparations through the objective measure of reduction in lower leg edema and the subjective alleviation of leg pain, heaviness, and itching. Safe, well tolerated, and acceptable to patients, the fresh plant HCSE preparation Aesculaforce offers a real alternative in the treatment of patients with mild to moderate venous insufficiency.

  Using horsechestnut seed extract in the treatment of venous leg ulcers: a cost-benefit analysis.:Ostomy Wound Manage. 2006 Apr;52(4):68-70, 72-4, 76-8.Leach MJ, Pincombe J, Foster G. School of Health Sciences, University of South Australia, North Terrace Adelaide, South Australia 5000. Matthew.Leach@unisa.edu.au

 Venous leg ulcers affect approximately 0.6% of the western population, consuming millions of healthcare dollars every year. To determine whether an alternative venous ulcer treatment using horsechestnut seed extract-- Aesculus hippocastanum-- and conventional therapy involving dressings and compression was more cost-effective than using conventional therapy alone, a 12-week cost-benefit analysis of horsechestnut seed extract therapy was conducted. The study, using data from a 12-week prospective, randomized, placebo-controlled trial conducted in South Australia in 2002-2004, involved 54 patients with venous ulceration who received treatment through a large South Australian district nursing service. Taking into account the cost of horsechestnut seed extract, dressing materials, travel, staff salaries, and infrastructure for each patient, horsechestnut seed extract therapy combined with conventional therapy was found to be more cost-effective than conventional therapy alone with an average savings of AUD 95 in organizational costs and AUD 10 in dressing materials per patient. This study confirms that dressing change frequency has a significant impact on the total cost of wound care and suggests that district nursing service operation efficiency may be enhanced through the use of horsechestnut seed extract as a result of less frequent nursing visits. Further study of this treatment modality is warranted.

  Clinical efficacy of horsechestnut seed extract in the treatment of venous ulceration.:J Wound Care. 2006 Apr;15(4):159-67.Leach MJ, Pincombe J, Foster G. School of Health Sciences, University of South Australia, North Terrace Adelaide. Matthew.Leach@unisa.edu.au

 OBJECTIVE: To evaluate the clinical efficacy of orally administered horsechestnut seed extract in the treatment of venous leg ulcers. METHOD: In a prospective triple-blind randomised placebo-controlled trial, 54 patients with venous leg ulcers from a large South Australian community nursing service were randomly allocated to receive horsechestnut seed extract (n=27) or placebo (n=27) for 12 weeks. Ulcers were assessed at weeks 0, 4, 8 and 12 utilising a wound assessment tool and the Alfred/Medseed Wound Imaging System. RESULTS: The difference between groups in the number of healed leg ulcers and change in wound surface area, depth, volume, pain and exudate was not statistically significant. However, horsechestnut seed extract did have a significant effect on the percentage of wound slough over time (RM-ANOVA F=2.76, p=0.045) and on the number of dressing changes at week 12 (t=-2.71, p=0.009). CONCLUSION: Even though horsechestnut seed extract is likely to attenuate the pathogenesis of venous insufficiency and, in turn, facilitate venous ulcer healing, the current study did not statistically support such a claim. However, taking into account the small sample and insufficient power of the trial, and the significant improvement in wound slough and visit frequency, it appears that it may be useful in the management of venous leg ulcers.

  Synthesis of 3-O-(beta-D-xylopyranosyl-(1-->2)-beta-D-glucopyranosyl)-3'-O-(beta-D-glucopyranosyl)tamarixetin, the putative structure of aescuflavoside A from the seeds of Aesculus chinensis.:Carbohydr Res. 2006 Jun 12;341(8):1047-51. Epub 2006 Apr 3.

 3-O-(beta-D-xylopyranosyl-(1-->2)-beta-D-glucopyranosyl)-3'-O-(beta-D-glucopyranosyl)tamarixetin, the putative flavonal glycoside named aescuflavoside A, isolated from the seeds of Aesculus chinensis, is synthesized via regioselective glycosylation of 7-O-benzyltamarixetin with glycosyl bromides under phase-transfer-catalyzed conditions.

  Butcher's Broom, in the treatment of venous insufficiency.:Pol Merkur Lekarski. 2005 Aug;19(110):234-6.Bylka W, Kornobis J. Katedra i Zaklad Farmakognozji Akademii Medycznej, Poznaniu.

 Numerous extracts of the plants, natural compounds and their derivatives, acting on the venous system, including horse-chestnut seed extracts aescin, rutin, troxerutin, diosmin and hesperidine. They have a long tradition in herbal medicine for their venotonic and anti-oedematous properties. This review is concerning Rusci aculeati rhizoma, which recently taken in Poland on the symptoms of chronic venous insufficiency and hemorrhoids.


  Horse Chestnut Extract Induces Contraction Force Generation in Fibroblasts through Activation of Rho/Rho Kinase.:

 Contraction forces generated by non-muscle cells such as fibroblasts play important roles in determining cell morphology, vasoconstriction, and/or wound healing. However, few factors that induce cell contraction forces are known, such as lysophosphatidic acid and thrombin. Our study analyzed various plant extracts for ingredients that induce generation of cell contraction forces in fibroblasts populating collagen gels. We found that an extract of Horse chestnut (Aesculus hippocastanum) is able to induce such contraction forces in fibroblasts. The involvement of actin polymerization and stress fiber formation in the force generation was suggested by inhibition of this effect by cytochalasin D and by Rhodamine phalloidin. Rho kinase inhibitors (Y27632 and HA1077) and a Rho inhibitor (exoenzyme C3) significantly inhibited the force generation induced by the Horse chestnut extract. H7, which inhibits Rho kinase as well as other protein kinases, also significantly inhibited induction of force generation. However, inhibitors of other protein kinases such as myosin light chain kinase (ML-9), protein kinase C (Calphostin), protein kinase A (KT5720), and tyrosine kinase (Genistein, Herbimycin A) had no effect on force generation induced by Horse chestnut extract. These results suggest that the Horse chestnut extract induces generation of contraction forces in fibroblasts through stress fiber formation followed by activation of Rho protein and Rho kinase but not myosin light chain kinase or other protein kinases.

  Treatment of patients with venous insufficiency with fresh plant horse chestnut seed extract: a review of 5 clinical studies.:

 Extracts from the seed of the horse chestnut (Aesculus hippocastanum L.) have traditionally been used to treat patients with chronic venous insufficiency and to alleviate its associated symptoms, including lower leg swelling. The efficacy of preparations that contain horse chestnut seed extract (HCSE) is believed to be due largely to an inhibitory effect on the catalytic breakdown of capillary wall proteoglycans. Aesculaforce is a fresh plant HCSE that is available as an oral tincture, as tablets (20 mg or 50 mg), and as topical gel. Four clinical trials in patients with chronic venous insufficiency and 1 study in patients with varicose veins demonstrated the effectiveness of these preparations through the objective measure of reduction in lower leg edema and the subjective alleviation of leg pain, heaviness, and itching. Safe, well tolerated, and acceptable to patients, the fresh plant HCSE preparation Aesculaforce offers a real alternative in the treatment of patients with mild to moderate venous insufficiency.
 

  Using horsechestnut seed extract in the treatment of venous leg ulcers: a cost-benefit analysis.:

 Venous leg ulcers affect approximately 0.6% of the western population, consuming millions of healthcare dollars every year. To determine whether an alternative venous ulcer treatment using horsechestnut seed extract-- Aesculus hippocastanum-- and conventional therapy involving dressings and compression was more cost-effective than using conventional therapy alone, a 12-week cost-benefit analysis of horsechestnut seed extract therapy was conducted. The study, using data from a 12-week prospective, randomized, placebo-controlled trial conducted in South Australia in 2002-2004, involved 54 patients with venous ulceration who received treatment through a large South Australian district nursing service. Taking into account the cost of horsechestnut seed extract, dressing materials, travel, staff salaries, and infrastructure for each patient, horsechestnut seed extract therapy combined with conventional therapy was found to be more cost-effective than conventional therapy alone with an average savings of AUD 95 in organizational costs and AUD 10 in dressing materials per patient. This study confirms that dressing change frequency has a significant impact on the total cost of wound care and suggests that district nursing service operation efficiency may be enhanced through the use of horsechestnut seed extract as a result of less frequent nursing visits. Further study of this treatment modality is warranted.

  Clinical efficacy of horsechestnut seed extract in the treatment of venous ulceration.:

 Objective: To evaluate the clinical efficacy of orally administered horsechestnut seed extract in the treatment of venous leg ulcers. Method: In a prospective triple-blind randomised placebo-controlled trial, 54 patients with venous leg ulcers from a large South Australian community nursing service were randomly allocated to receive horsechestnut seed extract (n=27) or placebo (n=27) for 12 weeks. Ulcers were assessed at weeks 0, 4, 8 and 12 utilising a wound assessment tool and the Alfred/Medseed Wound Imaging System. Results: The difference between groups in the number of healed leg ulcers and change in wound surface area, depth, volume, pain and exudate was not statistically significant. However, horsechestnut seed extract did have a significant effect on the percentage of wound slough over time (RM-ANOVA F=2.76, p=0.045) and on the number of dressing changes at week 12 (t=-2.71, p=0.009). CONCLUSION: Even though horsechestnut seed extract is likely to attenuate the pathogenesis of venous insufficiency and, in turn, facilitate venous ulcer healing, the current study did not statistically support such a claim. However, taking into account the small sample and insufficient power of the trial, and the significant improvement in wound slough and visit frequency, it appears that it may be useful in the management of venous leg ulcers.

  Synthesis of 3-O-(beta-D-xylopyranosyl-(1-->2)-beta-D-glucopyranosyl)-3'-O-(beta-D-glucopyranosyl)tamarixetin, the putative structure of aescuflavoside A from the seeds of Aesculus chinensis.:

 3-O-(beta-D-xylopyranosyl-(1-->2)-beta-D-glucopyranosyl)-3'-O-(beta-D-glucopyranosyl)tamarixetin, the putative flavonal glycoside named aescuflavoside A, isolated from the seeds of Aesculus chinensis, is synthesized via regioselective glycosylation of 7-O-benzyltamarixetin with glycosyl bromides under phase-transfer-catalyzed conditions.


  Antiinflammatory triterpenoid saponins from the seeds of Aesculus chinensis.:

 Phytochemical study of the ethanol extract of the seeds of Aesculus chinensis led to the isolation of a new triterpenoid saponin (6), together with five known triterpenoid saponins (1-5). The structure of the new compound was elucidated on the basis of spectral data to be 21,28-di-O-acetylprotoaescigenin-3-O-[beta-D-glucopyranosyl(1-2)][beta-D-glucopyranosyl(1-4)]-beta-D-glucopyranosiduronic acid (aesculiside A, 6). The antiinflammatory activities of the four main saponins (1-4) were compared with those of total saponin extracts, and single saponins showed more potent activity than total saponin extracts in mice.

  An open study to assess the safety and efficacy of Aesculus hippocastanum tablets (Aesculaforce 50mg) in the treatment of chronic venous insufficiency.:

 An open study was carried out to assess, primarily, the safety and tolerability of Aesculus hippocastanum in the treatment of CVI. Patients underwent 8 consecutive weeks of treatment and were asked to take one 50 mg Aesculus hippocastanum tablet, twice daily. In total, 91 adverse events were reported, of which only 4 were rated as probably related to the study drug. Patients judged the tolerability of the study medication in the majority of the cases at visits 2 and 3 (90 and 95%, respectively) to be "good" or "fairly good." Only 2 patients rated tolerability as poor at visit 3. For each of the symptoms investigated the difference in the median value between baseline and visit 3 was found to be statistically significant and both the ankle and lower leg circumference decreased. The PPG measurements were rejected after analysis since validation measurements carried out after the trial showed that the PPG technique had an internal error of around 30%. Nevertheless, the majority of patients rated efficacy to be "very good" or "good," with only 10 patients reporting no effect by the end of the study. The results of this study indicate that Aesculaforce 50 mg tablets are a safe, well-tolerated and efficacious treatment for Widmer stage I and II CVI.

  Horse chestnut:a multidisciplinary clinical review.:

 Horse chestnut seed extract (HCSE) is widely used in Europe for the management of chronic venous insufficiency (CVI). Although traditionally recommended for a variety of medical conditions, CVI is the only indication for which there is strong supportive scientific evidence. Review of the literature reveals 14 randomized controlled trials, of which seven are methodologically of high quality, albeit limited by small sample sizes and short durations. These studies support the superiority of HCSE over placebo, and suggest equivalence to compression stockings and to oral oxerutins. In the future, a longer and adequately powered randomized trial is warranted to compare HCSE to standard of care, and to further assess safety and long-term efficacy. There are no data to suggest that horse chestnut flower, raw seed, branch bark, or leaf are effective for any indication, and it is recommended that these products not be used, as they are known to be toxic when ingested.

  Horse chestnut seed extract for chronic venous insufficiency.:

 Background: Conservative therapy of chronic venous insufficiency (CVI) consists largely of compression treatment. However, this often causes discomfort and has been associated with poor compliance. Therefore, oral drug treatment is an attractive alternative. Objectives: To review the evidence from rigorous clinical trials assessing the efficacy and safety of oral horse chestnut seed extract (HCSE) versus placebo, or other treatments for CVI. SEARCH STRATEGY: Randomised controlled trials (RCTs) of HCSE for chronic venous insufficiency were sought through EMBASE (inception to December 2001), MEDLINE and AMED (from inception to February 2004), The Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library, Issue 1, 2004), the Specialised Trials Register of the Cochrane Peripheral Vascular Diseases Group (last searched February 2004), and Phytobase (from inception to January 2001, no longer operational). Manufacturers of HCSE preparations and experts on the subject were contacted for published and unpublished material. There were no restrictions on language. Selection Criteria: RCTs were included if they compared oral HCSE mono-preparations with placebo, or other treatments, in patients with CVI. Trials assessing HCSE as one of several active components in a combination preparation, or as a part of a combination treatment, were excluded. Data Collection and analysis: Two reviewers independently selected and assessed methodological quality of the studies using a standardised scoring system, and extracted data. Disagreements concerning evaluation of individual trials were resolved through discussion. Main Results: Overall, there appeared to be an improvement in CVI related signs and symptoms with HCSE compared with placebo. Leg pain was assessed in seven placebo-controlled trials. Six reported a significant reduction of leg pain in the HCSE groups compared with the placebo groups, while another reported a statistically significant improvement compared with baseline. One trial suggested a weighted mean difference (WMD) of 42.4 mm [95% confidence interval (CI) 34.9 to 49.9] measured on a 100 mm visual analogue scale. Leg volume was assessed in six placebo-controlled trials. Meta-analysis of five trials (n = 289) suggested a significant reduction in favour of HCSE compared with placebo (WMD 56.3 ml [95% CI 24.1 to 88.5]). One trial indicated that HCSE may be as effective as compression stockings at reducing leg volume. Adverse events were usually mild and infrequent. REVIEWERS' CONCLUSIONS: The evidence presented implies that HCSE is an efficacious and safe short-term treatment for CVI. However, several caveats exist and more rigorous RCTs are required to assess the efficacy of this treatment option.

  Antiviral flavonoids from the seeds of Aesculus chinensis.:

 A bioassay-guided fractionation of an ethanol extract of the seeds of Aesculus chinensis led to the isolation of two new flavanoids (1 and 2), along with eight known ones (3-10). The structures of the new compounds were elucidated by spectroscopic methods including 2D NMR. All compounds were tested for antiviral activity against respiratory syncytial virus (RSV), parainfluenza virus type 3 (PIV 3), and influenza virus type A (Flu A). Compounds 1, 2, and 6 showed significant antiviral activities against RSV with IC(50) values of 4.5, 6.7, and 4.1 microg/mL and selective index (SI) values of 15.8, 32, and 63.8, respectively. Compound 8 demonstrated significant antiviral activity against Flu A with an IC(50) of 24.5 microg/mL and a SI of 16.0, respectively.


  Bioavailability of beta-aescin from horse chestnut seed extract: comparative clinical studies of two Galenic formulations.:

 The bioavailability of beta-aescin--the main active constituent of horse chestnut seed extract--in a nonretarded test medication in comparison with that in a retarded reference formulation was evaluated in 2 randomized crossover clinical trials involving 18 healthy volunteers each. Serum concentration/time curves derived under steady-state conditions and pharmacokinetic parameters measured during both studies showed no significant difference between absorption rates for the retarded versus nonretarded preparation. In the first study, investigators found a test-to-reference ratio of 1.06 (90% confidence interval [CI] range: 99-113) for the area under the curve (AUC; the primary outcome measure). Absorption rates were diminished during the night compared with daytime rates for both study preparations. In the second study, using AUC and maximum concentration (Cmax) as the primary characteristics, investigators analyzed bioavailability based on the mean of 2 consecutive daytime periods and obtained estimates of 1.07 for AUC (90% CI range: 0.96-1.19) and 1.05 for Cmax (90% CI range: 0.90-1.21). Bioequivalence of the test and reference drug preparations was thus established according to the Note for Guidance on the Investigation of Bioavailability and Bioequivalence. Both treatments were equally well tolerated.

  Four new triterpene saponins from the seeds of Aesculus chinensis.:

 Two pairs of new geometrically isomeric triterpenoid saponins were isolated from the seeds of Aesculus chinensis and characterized as 28-acetyl-21-tigloylprotoaescigenin 3-O-[beta-D-xylopyranosyl (1 --> 2)] [beta-D-glucopyranosyl (1 --> 4)] [beta-D-glucopyranosiduronic acid (isoescin IIa, 1) and 28-acetyl-21-angeloylprotoaescigenin 3-O-[-beta-D-xylopyranosyl (1 --> 2)] [beta-D-glucopyranosyl (1 --> 4)] beta-D-glucopyranosiduronic acid (isoescin IIb, 2); 28-acetyl-21-tigloylbarringtogenol C 3-O-[beta-D-galactopyranosyl (1 --> 2)] [beta-D-glucopyranosyl (1 --> 4)] beta-D-glucopyranosiduronic acid (isoescin IIIa, 3) and 28-acetyl-21-angeloylbarringtogenol C 3-O-[beta-D-galactopyranosyl (1 --> 2)] [beta-D-glucopyranosyl (1 --> 4)] beta-D-glucopyranosiduronic acid (isoescin IIIb, 4). Their structures were established on the basis of spectroscopic and chemical evidence.

  Aescin: pharmacology, pharmacokinetics and therapeutic profile.:

 Aescin, the major active principle from Aesculus hippocastanum (Hippocastanaceae) the horse chestnut tree, has shown satisfactory evidence for a clinically significant activity in chronic venous insufficiency (CVI), haemorrhoids and post-operative oedema. In one controlled trial aescin was shown to be as effective as compression therapy as an alternative to medical treatment for CVI. The therapeutic benefit is well supported by a number of experimental investigations in different animal models, indicative of clearcut anti-oedematous, anti-inflammatory and venotonic properties, mainly related to the molecular mechanism of the agent, allowing improved entry of ions into channels, thus raising venous tension in both in vitro and in vivo conditions. Other mechanisms, i.e. release of PGF(2) from veins, antagonism to 5-HT and histamine, reduced catabolism of tissue mucopolysaccharides, further underline the wide ranging mechanisms of the therapeutic activity of aescin. The excellent tolerability of aescin in the clinic indicates this treatment is of definite clinical benefit in patients with clinical conditions resulting in CVI, haemorrhoids or peripheral oedema formation.

  Bioactive saponins and glycosides. XIII. Horse chestnut. (3): Quantitative analysis of escins Ia, Ib, IIa, and IIb by means of high performance liquid chromatography:

 As a part of our studies on the characterization of bioactive saponin constituents of horse chestnut trees, a quantitative method using high performance liquid chromatography (HPLC) has been developed for four principle saponin constituents, such as escins Ia, Ib, IIa, and IIb, isolated from the seeds of European horse chestnut trees (Aesculus hippocastanum L., Hippocastanaceae). As an application of this HPLC method, we examined the contents and compositions of these escins in the seeds of horse chestnut trees (A. turbinata BLUME) and in several commercial materials named as "beta-escin". Additionally, the distribution of escins in the horse chestnut trees was examined, and escins were found to be contained only in the seeds.

  Bioactive saponins and glycosides. XII. Horse chestnut. (2): Structures of escins IIIb, IV, V, and VI and isoescins Ia, Ib, and V, acylated polyhydroxyoleanene triterpene oligoglycosides, from the seeds of horse chestnut tree (Aesculus hippocastanum L., Hippocastanaceae).:

 New acylated polyhydroxyoleanene triterpene oligoglycosides, escins IIIb, IV, V, and VI and isoescins Ia, Ib, and V, were isolated from the seeds of horse chestnut tree (Aesculus hippocastanum L.). Their structures were elucidated on the basis of chemical and physicochemical evidence.


  Bioactive saponins and glycosides. III. Horse chestnut. (1): The structures, inhibitory effects on ethanol absorption, and hypoglycemic activity of escins Ia, Ib, IIa, IIb, and IIIa from the seeds of Aesculus hippocastanum L.:

 Five bioactive triterpene oligoglycosides named escins, Ia, Ib, IIa, IIb, and IIIa were isolated from the seeds of horse chestnut tree, Aesculus hippocastanum L. (Hippocastanaceae). The chemical structures of escins Ia, Ib, IIa, IIb, and IIIa were determine on the basis of chemical and physicochemical evidence, which included selective cleavage of the glucuronide linkage using photochemical reaction and lead tetraacetate decarboxylation reaction. Escins Ia, Ib, IIa, and IIb were found to exhibit an ethanol absorption-inhibitory effect and hypoglycemic activity in the oral glucose tolerance test in rats. Some structure-activity relationships are reported.

  Isolation of lectin from horse chestnut (Aesculus hippocastanum L.) seeds and study of its interaction with carbohydrates and glycoproteins:

 The lectin from horse chestnut seeds was obtained by affinity chromatography on a sorbent prepared from the egg white, 95 mg of lectin per 1 kg of fresh seeds being obtained. Molecular weight was determined by gel-filtration on tojopearl HW-55 and it composed 132 kDa. SDS-polyacrylamide gel electrophoresis revealed the presence of one component with molecular weight of 33 kDa. One band has been revealed by means of disc-electrophoresis in acidic (pH 4.5) and alkaline system (pH 8.9). Sugar was not detected in the lectin. Amino acid composition of the lectin has been determined. The lectin agglutinated horse erythrocytes in minimal concentration of 9.5 ngml, to the less extent rabbit (4.9 mkg/ml), rat (62 mkg/ml), human (73 mkg/ml), but did not agglutinate erythrocytes of a sheep and cow. Purified lectin did not interact with monosaccharides, but interacted with O-glycans.

  Steroidal constituents and anti-inflammatory activity of the horse chestnut (Aesculus hippocastanum L.) bark.:

 The content and the composition of sterols in the bark of the horse chestnut, Aesculus hippocastanum L., have been examined. Stigmasterol and alpha-spinasterol were, with the beta-sitosterol, the most abundant sterols. The petrol extract from bark shows anti-inflammatory activity.

  Isolation and characterization of esters of indole-3-acetic acid from the liquid endosperm of the horse chestnut (Aesculus species).:

 Esters of indole-3-acetic acid were extracted and purified from the liquid endosperm of immature fruits of various species of the horse chestnut (Aesculus parviflora, A. baumanni, A. pavia rubra, and A. pavia humulis). The liquid endosperm contained, at least 12 chromatographically distinct esters. One of these compounds was purified and characterized as an ester of indole-3-acetic acid and myo-inositol. A second compound was found to be an ester of indole-3-acetic acid and the disaccharide rutinose (glucosyl-rhamnose). A third compound was partially characterized as an ester of indole-3-acetic acid and a desoxyaminohexose.

  The mode of action of aescin and the release of prostaglandins.:

 The horse-chestnut saponin Aescin, an anti-exudative compound, induces contraction of isolated portal vein of rat and rabbit. This effect appears to be mediated by Prostaglandins of Falpha type. The ability of Aescin to stimulate generation and release of Prostaglandins has been demonstrated in isolated lung of the rat. Mass-fragmentographic analysis of the lung effluent indicate that when Aescin is perfused through this organ the release of PGF2alpha is increased. The capability of Aescin to generate Prostaglandins is discussed in connection with its anti-exudative activity.


  Escin in pharmaceutical oral dosage forms: quantitative densitometric HPTLC determination.:

 A practical and reliable method for the quantitative determination of escin in pharmaceuticals was developed. The TLC-densitometric determination was performed without using spray or dipping reagents in order to provide a more rapid and simple analytical procedure. Chromatographic separations were obtained on analytical HPTLC silica gel plates and the elution was made with 3.5:4.5:2 PropOH-ethyl acetate-water (v/v/v). Densitometric analysis was performed directly at 212 nm, corresponding to lambda max of escin obtained by in situ-scanning. A second degree polynomial regression relationship was found between the peak areas and the amounts of the escin standard deposited in the range 1.15-6.90 micrograms. The method is specific, accurate and reliable and was applied successfully to the quantitative determination of escin in commercial samples.

  The validity of radioimmunologic determination of bioavailability of beta-escin in horse chestnut extracts:

 The bioavailability under steady state conditions of a standard, slow-release horse chestnut seed extract (HCSE)-containing product was compared with that of an analogous, fast-release test preparation (Noricaven novo) in a prospective, randomised, double-blind study in a double cross-over design. The serum concentration of beta-escin (CAS 6805-41-0) was measured by radioimmunoassay. In addition, the biopharmaceutical properties of the HCSEs present in the products were investigated, the amount and composition of the active ingredient, escin, being analysed with a validated HPLC method. The pharmacokinetics of this study were compared with the corresponding data of a similar investigation carried out under analogous conditions concerning study design, analytical methods and reference preparation. Comparison of the similar studies revealed differences in characteristic pharmakokinetic values of beta-escin in terms of a shift of the concentration time curves as could be demonstrated for the reference product. The total amounts of escin in the two products investigated did not differ significantly. However, quantitative and qualitative differences were detected in the constituents of the two different extract preparations. It is concluded that the high specificity of the validated beta-escin radioimmunoassay leads to analytical imprecision due to the variable constituents of the extract preparations used. It is necessary to test whether this problem can be solved using an analytical approach, which is specific for each extract.


  Scientific References:

  1.Research Update:Horse chestnut and aescin