• Title/Summary/Keyword: Anti-platelet activity

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Antithrombotic Activity of Hermetia illucens (Black Soldier Fly) (동애등에의 항혈전 활성)

  • Pyo, Su-Jin;Won, Jun;Kang, Deok-Gyeong;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.30 no.4
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    • pp.386-393
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    • 2020
  • Insect industry has been focused as production of food, animal feed, pollinator and for environmental remediation. Hermetia illicens, called as black soldier fly (BSF) is famous as nutritive feed. In this study, to evaluate the antithrombotic activities of BSF, the larvae (instar 2~6), pupae, residue after adult emergence [RAAE] and adult of Hermetia illicens [black soldier fly, BSF] were collected and their ethanol extracts were prepared. Growth of BSF larvae was very rapid and the weight of larvae was increased to 25-folds during 10 days cultivation. The ethanol extraction ratios showed from 1.0% (pupae) to 18.5%(adults). The highest total polyphenol, total flavonoid, and total sugar contents were observed in RAEE (17.2 mg/g), pupae (3.4 mg/g), and instar 6 (37.6 mg/g), suggesting that metabolic changes occur during the life cycle of the BSF. Anti-coagulation assay showed that extracts of RAEE, instar 6 and pupa of BSF significantly inhibited thrombin, prothrombin, and blood coagulation factors. Furthermore, the extracts of RAEE, instar 3 and adult of BSF showed a strong platelet aggregation inhibitory activity. Our results suggest that pupae and RAEE of BSF have potential as antithrombotic agents. This is the first study to provide evidence of the antithrombotic activity of the BSF and bioactivity alterations during its life cycle.

Neuronal injury in AIDS dementia: Potential treatment with NMDA open-channel blockers and nitric oxide-related species

  • Lipton, Stuart A.
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.19-29
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    • 1996
  • The neurological manifestations of AIDS include dementia, encountered even in the absence of opportunistic superinfection or malignancy. The AIDS Dementia Complex appears to be associated with several neuropathological abnormalities, including astrogliosis and neuronal injury or loss. How can HIV-1 result in neuronal damage if neurons themselves are only rarely, if ever, infected by the vitus\ulcorner In vitro experiments from several different laboratiories have lent support to the existence of HIV- and immune-related toxins. In one recently defined pathway to neuronal injury, HIV-infected macrophages/microglia as well as macrophages activated by HIV-1 envelope protein gp120 appear to secrete excitants/neurotoxins. These substances may include arachidonic acid, platelet-activating factor, free radicals (NO - and O$_2$), glutamate, quinolinate, cysteine, cytokines (TNF-${\alpha}$, IL1-B, IL-6), and as yet unidentified factors emanating from stimulated macrophages and possibly reactive astrocytes. A final common pathway for newonal suscepubility appears to be operative, similar to that observed in stroke, trauma, epilepsy, and several neurodegenerative diseases, including Huntington's disease, Parkinson's disease, and amyotrophic lateral sclerosis. This mechanism involves excessive activation of N-methyl-D-aspartate (NMDA) receptor-operated channels, with resultant excessive influx of Ca$\^$2+/ leading to neuronal damage, and thus offers hope for future pharmacological intervention. This chapter reviews two clinically-tolerated NMDA antagonists, memantine and nitroglycerin; (ⅰ) Memantine is an open-channel blocker of the NMDA-associated ion channel and a close congener of the anti-viral and anti-parkinsonian drug amantadine. Memantine blocks the effects of escalating levels of excitotoxins to a greater degree than lower (piysiological) levels of these excitatory amino acids, thus sparing to some extent normal neuronal function. (ⅱ) Niuoglycerin acts at a redox modulatory site of the NMDA receptor/complex to downregulate its activity. The neuroprotective action of nitroglycerin at this site is mediated by n chemical species related to nitric oxide, but in a higher oxidation state, resulting in transfer of an NO group to a critical cysteine on the NMDA receptor. Because of the clinical safety of these drugs, they have the potential for trials in humans. As the structural basis for redox modulation is further elucidated, it may become possible to design even better redox reactive reagents of chinical value. To this end, redox modulatory sites of NMDA receptors have begun to be characterized at a molecular level using site-directed mutagenesis of recombinant subunits (NMDAR1, NMDAR2A-D). Two types of redox modulation can be distinguished. The first type gives rise to a persistent change in the functional activity of the receptor, and we have identified two cysteine residues on the NMDARI subunit (#744 and #798) that are responsible for this action. A second site, presumably also a cysteine(s) because <1 mM N-ethylmaleimide can block its effect in native neurons, underlies the other, more transient redox action. It appears to be at this, as yet unidentified, site on the NMDA receptor that the NO group acts, at least in recombinant receptors.

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The Effects of Yunjogyosim-tang on Stress and Sleep-related Substance of Rats Induced by Chronic Mild Stress (Chronic Mild Stress 유발 흰쥐에서 윤조교심탕(潤燥交心湯)이 스트레스 및 수면 관련 호르몬에 미치는 영향)

  • Kim, Ha-na;Kim, Kyeong-ok
    • Journal of Oriental Neuropsychiatry
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    • v.28 no.1
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    • pp.25-38
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    • 2017
  • Objectives: The study aims were to evaluate the Anti-stress and Sleep-inductive effects of Yunjogyosim-tang (YJGS) in rats induced by Chronic Mild Stress (CMS). Methods: 25 healthy Rats were randomly divided into 5 groups; Normal, CMS (Control), YJGS 50, YJGS 100, and YJGS 200. All rats except the normal group were exposed to random stress conditions like water deprivation, empty bottles, forced runs on the treadmill, etc. according to the timetable of CSM for 3 weeks. After a week starting the experiment, Rats in YJGS 50, YJGS 100, and YJGS 200 groups were fed orally once a day for 2 weeks. Blood samples were taken afterward from each rat for analysis of Complete blood count, AST, ALT, and glucose levels. Corticosterone, serotonin, and melatonin were measured by ELISA kit. BDNF and $TNF-{\alpha}$ were measured by RT-PCT. Results: 1. Corticosterone levels were lower in YJGS 50, and YJGS 200 groups compared to the control group. 2. Serotonin levels were lower in the YJGS 100 and YJGS 200 groups compared to the control group. 3. Melatonin levels were higher in the YJGS 50 group compared to the control group. 4. Activity levels were higher in the BDNF, and YJGS 50 groups compared to the control group. 5. In the Activity of $TNF-{\alpha}$, YJGS 50 group showed a significant decrease compared to the control group. 6. In the Glucose content, YJGS 50, YJGS 100, and YJGS 200 groups showed a significant decrease compared to the control group. 7. When analyzing leukocytes, monocytes were found to be increased in YJGS 100 and YJGS 200 groups compared to the control group. 8. When analyzing red blood cells, more changes occurred to erythrocytes and thrombocytes in the YJGS 50 and YJGS 200 groups than in the control group. Hemoglobin was significantly increased in the YJGS 100 group and platelet levels were significantly increased in all experimental groups compared with the control group. Conclusions: These results suggest that Yunjogyosim-tang has anti-stress and sleep-inductive effects on rats induced by CMS.

The Activation of Stress-induced Heat Shock Protein 27 and the Relationship of Physical Therapy (스트레스-유도 열충격단백질 27(Heat Shock Protein 27)의 활성과 물리치료의 상관성)

  • Kim, Mi-Sun;Lee, Sung-Ho;Kim, Il-Hyun;Hwang, Byong-Yong;Kim, Jung-Hwan
    • The Journal of Korean Physical Therapy
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    • v.20 no.1
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    • pp.57-65
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    • 2008
  • Purpose: Heat shock proteins (HSPs) are a group of proteins that are activated when cells are exposed to a variety of environmental stresses, such as infection, inflammation, exposure to toxins, starvation, hypoxia, brain injury, or water deprivation. The activation of HSPs by environmental stress plays a key role in signal transduction, including cytoprotection, molecular chaperone, anti-apoptotic effect, and anti-aging effects. However, the precise mechanism for the action of small HSPs, such as HSP27 and mitogen-activated protein kinases (MAPKs: extracellular-regulated protein kinase 1/2 (ERK1/2), p38MAPK, stress-activated protein kinase/c-Jun N-terminal kinase (SAPK/JNK), is not completely understood, particularly in application of cell stimulators including platelet-derived growth factor (PDGF), angiotensin II (AngII), tumor necrosis factor $\alpha$ (TNF$\alpha$), and $H_2O_2$. This study examined the relationship between stimulators-induced enzymatic activity of HSP27 and MAPKs from rat smooth and skeletal muscles. Methods: 2-dimensional electrophoresis (2DE) and matrix assisted laser desorption ionizationtime-of-flight/time-of-flight (MALDI-TOF/TOF) analysis were used to identify HSP27 from the intact vascular smooth and skeletal muscles. Three isoforms of HSP27 were detected on silver-stained gels of the whole protein extracts from the rat aortic smooth and skeletal muscle strips. Results: The expression of PDGF, AngII, TNF$\alpha$, and $H_2O_2$-induced activation of HSP27, p38MAPK, ERK1/2, and SAPK/JNK was higher in the smooth muscle cells than the control. SB203580 (30${\mu}$M), a p38MAPK inhibitor, increased the level of HSP27 phosphorylation induced by stimulators in smooth muscle cells. Furthermore, the age-related and starvation-induced activation of HSP27 was higher in skeletal muscle cells (L6 myoblast cell lines) and muscle strips than the control. Conclusion: These results suggest, in part, that the activity of HSP27 and MAPKs affect stressors, such as PDGF, AngII, TNF$\alpha$, $H_2O_2$, and starvation in rat smooth and skeletal muscles. However, more systemic research will be needed into physical therapy, including thermotherapy, electrotherapy, radiotherapy and others.

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Evaluation of in-vitro Antithrombosis Activity of Lees of Korean Traditional Wine (전통주 주박의 항혈전 활성 평가)

  • Kim, Mi-Sun;Lee, Ye-Seul;Kim, Jong Sik;Shin, Woo-Chang;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.24 no.8
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    • pp.865-872
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    • 2014
  • In this study, ethanol and hot water extracts of lees from Korean traditional wine (J-B, J-S, J-Y, J-H, and J-W) were prepared, and their effects on blood coagulation, platelet aggregation, and hemolysis of human red blood cells (hRBCs) were investigated to develop functional food ingredients from lees. The pH and brix of the lees ranged from 3.90 to 4.29 and 5.0 to $27.0^{\circ}$, respectively, and there was a huge difference in the water and ethanol content among the lees. The nuruk and additives used affected the color and physicochemical properties of lees. The J-W takju made from only rice and traditional nuruk, which has $13^{\circ}$ brix and 1.8% of alcohol, has potential as functional food ingredient. With regard to the extraction yields of lees, higher yields were obtained from J-H, which contains different medicinal plants, in ethanol, followed by J-W, J-B, J-S, and J-Y. Higher extraction yields of lees were obtained from J-S in hot water, followed by J-B, J-W, J-H, and J-Y, respectively. The ethanol extract of J-H and the hot water extract of J-Y had the highest contents of total polyphenol and total flavonoids among the lees extracts. The 10 lees extracts did not show hemolysis activity against hRBCs up to 5 mg/ml. In an anticoagulation activity assay, the ethanol extracts of three yakju lees (J-B, J-S, and J-Y) and the hot water extract of J-W inhibited thrombin activity, whereas the hot water extract of J-B, J-S, and J-H inhibited blood coagulation factors. In an antiplatelet aggregation activity assay, only the J-W takju lees showed significant inhibition activity. Our results suggest that lees from traditional wine had high potential as a novel antithrombosis agent.

Evaluation of the Useful Bioactivities of Spent Mushroom Substrate of Shiitake (표고버섯 수확 후 배지의 유용 생리활성 평가)

  • Sung, Hwa-Jung;Pyo, Su-Jin;Park, Jong-Yi;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.29 no.2
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    • pp.164-172
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    • 2019
  • In Korea, shiitake mushroom, Lentinula edodes, is cultivated on artificial medium containing oak sawdust and wheat bran. The annual production of spent mushroom substrate (SMS) of shiitake, a byproduct of the mushroom industry, is estimated to reach over 50,000 tons per year. This study aimed to improve the use of SMS as a novel bioresource. Hot water extracts of SMS after the first and third harvest were prepared and their bioactivities evaluated. Hot water extracts of uninoculated medium and shiitake were used as controls. Extracts of SMS showed higher radical scavenging of DPPH anions, ABTS cations, nitrites, and a higher reducing power than those of shiitake or medium extracts. After the first and third harvests at 0.5 mg/disc, SMS extracts showed no antibacterial or antifungal activities against the pathogenic and food-spoilage bacteria and fungi. However, they showed good inhibitory activities against ${\alpha}$-glucosidase at 0.5 mg/ml. In addition, SMS extracts had strong anti-coagulation activities via their inhibition of thrombin, prothrombin, and blood coagulation factors without platelet aggregation activity. Our results suggested SMS should no longer be perceived as a useless byproduct but should be understood as a novel bioresource, the extracts of which could be developed as antioxidant, antidiabetic, and antithrombosis agents.

Rg3-enriched Korean Red Ginseng extract inhibits blood-brain barrier disruption in an animal model of multiple sclerosis by modulating expression of NADPH oxidase 2 and 4

  • Lee, Min Jung;Choi, Jong Hee;Oh, Jinhee;Lee, Young Hyun;In, Jun-Gyo;Chang, Byung-Joon;Nah, Seung-Yeol;Cho, Ik-Hyun
    • Journal of Ginseng Research
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    • v.45 no.3
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    • pp.433-441
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    • 2021
  • Background: Multiple sclerosis (MS) and its animal model, the experimental autoimmune encephalomyelitis (EAE), are primarily characterized as dysfunction of the blood-brain barrier (BBB). Ginsenoside-Rg3-enriched Korean Red Ginseng extract (Rg3-KRGE) is known to exert neuroprotective, anti-inflammatory, and anti-oxidative effects on neurological disorders. However, effects of Rg3-KRGE in EAE remain unclear. Methods: Here, we investigated whether Rg3-KRGE may improve the symptoms and pathological features of myelin oligodendroglial glycoprotein (MOG)35-55 peptide - induced chronic EAE mice through improving the integrity of the BBB. Results: Rg3-KRGE decreased EAE score and spinal demyelination. Rg3-KRGE inhibited Evan's blue dye leakage in spinal cord, suppressed increases of adhesion molecule platelet endothelial cell adhesion molecule-1, extracellular matrix proteins fibronection, and matrix metallopeptidase-9, and prevented decreases of tight junction proteins zonula occludens-1, claudin-3, and claudin-5 in spinal cord following EAE induction. Rg3-KRGE repressed increases of proinflammatory transcripts cyclooxygenase-2, inducible nitric oxide synthase, interleukin (IL)-1 beta, IL-6, and tumor necrosis factor-alpha, but enhanced expression levels of anti-inflammatory transcripts arginase-1 and IL-10 in the spinal cord following EAE induction. Rg3-KRGE inhibited the expression of oxidative stress markers (MitoSOX and 4-hydroxynonenal), the enhancement of nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 (NOX2) and NOX4, and NADPH activity in the spinal cord of chronic EAE mice. Furthermore, apocynin, a NOX inhibitor, mimicked beneficial effects of Rg3-KRGE in chronic EAE mice. Conclusion: Our findings suggest that Rg3-KRGE might alleviate behavioral symptoms and pathological features of MS by improving BBB integrity through modulation of NOX2/4 expression.

Characterization of compounds and quantitative analysis of oleuropein in commercial olive leaf extracts (상업용 올리브 잎 추출물의 화합물 특성과 이들의 oleuropein 함량 비교분석)

  • Park, Mi Hyeon;Kim, Doo-Young;Arbianto, Alfan Danny;Kim, Jung-Hee;Lee, Seong Mi;Ryu, Hyung Won;Oh, Sei-Ryang
    • Journal of Applied Biological Chemistry
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    • v.64 no.2
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    • pp.113-119
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    • 2021
  • Olive (Olea europaea L.) leaves, a raw material for health functional foods and cosmetics have abundant polyphenols including oleuropein (major bioactive compound) with various biological activities: antioxidant, antibacterial, antiviral, anticancer activity, and inhibit platelet activation. Oleuropein has been reported as skin protectant, antioxidant, anti-ageing, anti-cancer, anti-inflammation, anti-atherogenic, anti-viral, and anti-microbial activity. Despite oleuropein is the important compound in olive leaves, there is still no quantitative approach to reveal oleuropein content in commercial products. Therefore, a validated method of analysis has to develop for oleuropein. In this study, the components and oleuropein content in 10 types of products were analyzed using a developed method with ultra-performance liquid chromatography to quadrupole time-of-flight mass spectrometry, charge of aerosol detector, and photodiode array. The total of 18 compounds including iridoids (1, 3, 4, 14, and 16-18), coumarin (2), phenylethanoids (5, 9, and 11), flavonoids (6-8, 10, 12, and 13), lignan (15), were tentatively identified in the leaves extract based high resolution mass spectrometry data, and the content of oleuropein in each product was almost identical between two detection methods. The oleuropein in three commercial product (A, G, H) was contained more over the suggested content, and it of five products (B, E, H, I, J) were analyzed within 5-10% error range. However, the two products (C, D) were found far lower than suggested contents. This study provides that analytical results of oleuropein could be a potential information for the quality control of leaf extract for a manufactured functional food.

Changes in the in vitro Antioxidant and Antithrombosis Activities of Salicornia europaea According to Harvest Time (수확시기에 따른 함초의 항산화 및 항혈전 활성의 변화)

  • Kim, Mi-Sun;Lee, Jung-Nam;Seong, Ha-Jung;Kim, Deuk Hoi;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.26 no.9
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    • pp.1033-1040
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    • 2016
  • In Korea, the aerial parts of the halophyte Salicornia europaea, known as hamcho, are used in salads in April–June and in oriental medicine in September–October In this study, with the aim of developing functional foods to aid blood circulation, hot water extract (HWE) and ethanol extract (EE) were prepared using hamcho harvested from the fields of Shinan, Jeonnam, Korea on 5th April (HWE-04, EE-04), 5th July (HWE-06, EE-06), 5th August (HWE-08, EE-08), 5th September (HWE-09, EE-09), and 5th October (HWE-10, EE-10), and their antioxidant and antithrombosis activities were evaluated. Among the HWEs, HWE-10 showed the highest concentration of total polyphenols and total flavonoids (22.4 and 17.6 mg/ml, respectively), and EE-09 had the highest concentration among the EEs (20.1 and 19.3 mg/ml, respectively). Among the HWEs and EEs, HWE-08 and EE-08 had the highest total sugar and reducing sugar content. In the antioxidation assay, HWE-10 and EE-09 showed strong reducing power, as well as DPPH, ABTS, and nitrite scavenging activities. The calculated RC50s of EE-09 against DPPH, ABTS, and nitrite were 578, 277, and 68.8 μg/ml, respectively. The antithrombosis activity assay revealed that HWE-04, HWE-06, EE-04, and EE-06 had anticoagulation activity against coagulation factors and that HWE-08, HWE-09, EE-08, and EE-09 expressed strong thrombin inhibitory activity, which was comparable to the antithrombosis activity of aspirin. In addition, EE-06 and HWE-08 exhibited strong aggregation inhibitory activities against human platelets. The results suggest that extract from hamcho harvested in particular periods and prepared using a defined solvent has strong potential as a novel food ingredient and an antioxidant and antithrombosis agent.

The Effect of Eisenia bicyclis Extracts on Antioxidant Activity and Serum Lipid Level in Ovariectomized Rats (대황 추출물의 in vitro 항산화 활성 및 난소를 절제한 흰쥐의 혈중 지질함량에 미치는 영향)

  • Park, Yong Soo;Kim, Mihyang
    • Journal of Life Science
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    • v.22 no.10
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    • pp.1407-1414
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    • 2012
  • Hormone replacement therapy (HRT) is an effective regimen that has been found to prevent these diseases in postmenopausal women. However, HRT is accompanied by an increased risk of unfavorable outcomes. This study was conducted to evaluate the effects of Eisenia Bicyclis extract on lipids in ovariectomized rats. Fifty 7-week-old female Sprague-Dawley rats were randomly assigned to four groups: sham-operated rats (SHAM), ovariectomized rats (OVX-CON), and ovariectomized rats that were treated with Eisenia bicyclis extracts. The extract-treated diets were fed to the rats for 6 weeks after operation. Antioxidant effects were measured by DPPH free radical scavenging activity. Antioxidant activity of the ethanol extract increased in a dose-dependent manner and was about 55.9% in a concentration of 100 ${\mu}g/ml$. We measured the total cholesterol content, triglyceride content, HDL-cholesterol content, LDL-cholesterol content, atherosclerotic index, cardiac risk factor in serum, and anti-platelet aggregation and blood rheology. The total cholesterol and triglyceride concentration in serum increased for the OVX-control group, but supplementation with the E. bicyclis extract caused these factors to decrease. Notably, the serum LDL-cholesterol concentration in the OVX-EB200 group was significantly lower than the OVX-CON group. In addition, the blood passage times in rats that received the E. bicyclis extract were more rapid than the times in the untreated group (OVX-CON). Microscopic evaluation revealed that whole blood passed more smoothly through the microchannels in rats in the E. bicyclis extract supplement groups. Our results clarified the effects of E. bicyclis extract on serum lipid content in ovariectomized rats, and consequently we expect positive effects from providing E. bicyclis extract to postmenopausal women with cardiovascular disease.