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Hawthorn - A Health Food

Authors:

Abstract

The genus of Crataegus (hawthorn) is cultivated in many parts of the world, and regarded as medicinal plant in many countries. Hawthorn fruit is commonly used to cure scurvy, constipation and digestive disorders, Hawthorn flowers and leaves are often used against mild cardiac disorders. Modern studies found extracts of Hawthorn fruits, flowers and leaves possess a wide range of pharmacological properties, the pharmacological properties of Hawthorn are mostly related to the involved phenolic compounds including flavonoids. In this article, the active chemical properties and medicinal value of Hawthorn are reviewed.
Hawthorn—A Health Food
HAN Junyan
1,a
, TAN Dehong
2,b
, LIU Guangchun
1,c
1.
College of Biological and Environmental Engineering, Shenyang University, Shenyang,
China.110044
2.
College of Food, Shenyang Agricultural University, Shenyang, China.110866
a
Hanjunyan@yahoo.cn,
b
tandehongsy@126.com,
c
liugc@yahoo.cn (corresponding author)
Key words: crataegus; hawthorn; flavonoid; Shanzha; caridiac
Abstract: The genus of Crataegus (hawthorn) is cultivated in many parts of the world. and regarded
as medicinal plant in many countries. Hawthorn fruit is commonly used to cure scurvy, constipation
and digestive disorders, Hawthorn flowers and leaves are often used against mild cardiac disorders.
Modern studies found extracts of Hawthorn fruits, flowers and leaves possess a wide range of
pharmacological properties, the pharmacological properties of Hawthorn are mostly related to the
involved phenolic compounds including flavonoids. In this article, the active chemical properties
and medicinal value of Hawthorn are reviewed.
Introduction
The genus of Crataegus (hawthorn) belongs to the rosaceae family, comprising approximately 280
species, is cultivated in many parts of the world. Hawthorn is regarded as medicinal plant in many
countries[1]. Modern studies found extracts of Hawthorn fruits, flowers and leaves possess a wide
range of pharmacological properties, the pharmacological properties of Hawthorn are mostly related
to the involved phenolic compounds including flavonoids[2].
In this article, the active chemical properties, medicinal value and safety issue of Hawthorn are
reviewed.
Chemical properties
General chemical properties and composition of Hawthorn fruit Özcan et al.[3]
established chemical properties and minerals content of hawthorn fruits (Crataegus spp.). The
energy, protein, cellulose, oil, ash, acidity and water-soluble extract values of hawthorn fruits are
34.02 kcal/g, 2.48%, 4.67%, 0.87%, 2.28%, 1.98% and 32.31%, respectively. The minerals of Ca, K,
Mg, Na and P, are 3046.37 ppm, 13,531.96 ppm, 1502.55 ppm, 312.18 ppm and 1477.88 ppm,
respectively.
Functional compounds of hawthorn The dominant functional components in hawthorn
fruits, leaves and flowers are phenolics, including flavonoids (e.g. hyperoside, isoquercitrin,
quercitin), proanthocyanins (e.g. epicatechin) and phenolic acid (e.g. chlorogenic acid) [4].
Medicinal value of Hawthorn
Antioxidant effects The antioxidant effects and the active constituents of hawthorn have
been widely studied, which are closely related with other pharmacological properties of Hawthorn.
[5]. Polyphenols scavenge free radicals collaborating with other antioxidants and metals [6], which
possess the ideal chemical structure for scavenging free radicals. The highest radical scavenging
activity is exhibited by compounds that have an ortho 30, 40 - dihydroxy structure at ring B (e.g.
catechin, quercetin) or hydroxyl groups in position meta, e.g. 5, 7 - dihydroxy at ring A (e.g.
kaempferol, apigenin), as well as those that have a double bond between the C2 and C3 and the C3 -
hydroxyl group at ring C. The activity is also influenced by the flavonoid particle glycosylation [7].
Applied Mechanics and Materials Vol. 140 (2012) pp 350-354
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Medicinal effects on cardiovascular system Hawthorn was first documented as a treatment
for various cardiovascular disorders in Europe in the late 1800s [8], now, hawthorn products have
become popular herbal supplements for cardiomedicinal purpose, including cardiovascular
protection, endothelium-dependent vasorelaxation, improvement of coronary circulation, and
hypolipidemic effects, etc, are used for improving cardiac function, arrhythmia cholesterolemia and
hypertension [9].
Improving cardiac function
Preclinical studies A number of experimental studies performed on whole animals, show
extracts of hawthorn can increase cardiac contractility, increase cardiac blood flow and decrease
blood pressure[10]. Studies conducted on isolated cardiac muscle or vascular tissue demonstrate
positive inotropic effects, mild chronotropic effects, increased cardiac flux from improved ejection
volume, and vasorelaxation[11].
The mechanism of action was assumed previously to include an increase in force of contraction of
the heart and a vasorelaxant effect, particularly on coronary vessels [12]. The later studies showed
the strengthening of the heart contraction in isolated perfused hearts was only evident to a relatively
small extent, while the increase in coronary flow was more noticeable. Hawthorn extracts also
possessed a relatively strong relaxant effect on the vascular smooth muscle (aorta), implying
Hawthorn can decrease the preload for the heart [13].
Clinical studies Hawthorn leave and flower extracts were shown to reduce the incidence of
sudden cardiac death in certain patients [14] and be effective in treating chronic heart failure [15].
Several double-blind clinical studies of patients diagnosed with Chronic Heart Failure (CHF) have
shown beneficial effects of hawthorn. Clinical trials with New York Heart Association (NYHA)
stage-II or -III CHF demonstrated that Hawthorn extracts (WS 1442 and Crataegutt novo 450)
effectively improved cardiac performance, including decreased ankle edema, improved ejection
fraction, mildly reduce blood pressure[16]. In a study, hawthorn was found to be as effective as
captopril in improving exercise tolerance. Based on ergometric performance parameters, the
minimum effective daily dose of hawthorn extract is 300 mg. In most trials, the maximum benefit
was seen after 6 to 8 weeks of therapy[17].
Compared to digitalis, hawthorn has a wider therapeutic range, lower risk in case of toxicity, has
less of an arrhythmogenic potential, is safer to use in renal impairment, and can be safely used with
diuretics and laxatives[18].
Antiarrhythmic effect
The cardiovascular effects described for hawthorn extract is some what like that of
phosphodiesterase-3 (PDE3) inhibitors, which demonstrate various pharmacological properties
including cardiomedicinal, vasodilating, anti-inflammatory and antioxidant, and have been
identified as potential therapeutic agents in cardiovascular disease[19]. However, Hawthorn extracts
show unique chronotropic effects that it appears to be antiarrhythmic but capable of inducing
rhythmicity in quiescent cardiomyocytes, suggesting Hawthorn extracts may contain unique PDE3
inhibitors without arrhythmogenic potential [20].
Hypocholesterolemic and atheroscleroprotective effect
Hawthorn possesses the benefits of hypocholesterolemic and atheroscleroprotective activity.
Consumption of hawthorn can alter cholesterol metabolism of the liver, increases hepatic LDL
receptor activity [21], and reduce blood lipid and cholesterol levels [22]. In addition, the abundant
amount of antioxidants contained in hawthorn can protect LDL from oxidation, slow down the
development of atherosclerosis [23].
Hawthorn improves serum lipid metabolism with increased LDL and decreased HDL. Kwok et
al.[24] investigated the hypocholesterolemic and atheroscleroprotective potentials of dietary
consumption of hawthorn in high-cholesterol diet (HCD) rats, the results showed an increased
plasma total cholesterol and LDL-cholesterol with a decreased HDL-cholesterol in HCD-fed rats for
4 weeks. Hawthorn markedly suppressed the elevated total cholesterol and LDL-lipoprotein levels
plus an increased HDL cholesterol level. Hawthorn also prevented the development of fatty liver,
and elevated oxidative stress (estimated by the decreased levels of anti-oxidant enzymes) associated
Applied Mechanics and Materials Vol. 140 351
with HCD. In additionally, Hawthorn improved the blunted relaxation of isolated aortas induced by
acetylcholine of HCD-fed rats. The results indicate benefits of Hawthorn on lipid metabolism and
blood vessels.
Hypotensive effect
Hawthorn leaves, flowers and fruits are used to treat mild hypertension alone or in conjunction with
prescribed drugs. In a pilot study of mild hypertension, there were promising hypotensive responses
to 500 mg of hawthorn extract per day after 10 weeks. Walker et al. [25] investigated the effects of
hawthorn for hypertension in patients with type II diabetes. Results showed there was a significant
group difference in mean diastolic blood pressure reductions (P = 0.035): the hawthorn group
showed greater reductions (baseline: 85.6 mmHg, 95% confidence interval [CI] = 83.3 to 87.8;
outcome: 83.0 mmHg, 95% CI = 80.5 to 85.7) than the placebo group (baseline: 84.5 mmHg, 95%
CI = 82 to 87; outcome: 85.0 mmHg, 95% CI = 82.2 to 87.8). There was no group difference in
systolic blood pressure reduction from baseline (3.6 and 0.8 mmHg for hawthorn and placebo
groups, respectively; P = 0.329). In a double-blind, placebo-controlled clinical trial to determine the
effects of the C. curvisepala leaves and flowers extract for mild hypertension, results showed a
significant decrease in both systolic and diastolic blood pressure after 3 months (p < 0.05), and a
time-dependent antihypertensive effect [26].
The mechanism for hypotension of Hawthorn is regard to be related to the inhibition of Angiotensin
I - Converting Enzyme (ACE), which is considered to be a useful therapeutic approach in the
treatment of high blood pressure. Within the enzyme cascade of the renin-angiotensin system, ACE
removes histidyl-leucine from angiotensin I to form the octapeptide angiotensin II, which is one of
the most potent vasoconstrictors. Angiotensin II also stimulates the synthesis and release of
aldosterone which promotes sodium and water retention, resulting in increasing of blood
pressure[27]. Using an in vitro ACE-inhibition assay, Inokuchi et al. [28] found ACE-inhibitory
fractions in Hawthorn fruits. Lacaille-Dubois et al.[29] found flavonoids and proanthocyanidins
from the flowers and leaves of C. oxyacantha/ monogyna demonstrated inhibitory activity at 0.33
mg/ml, while phenolic acids showed no significant ACE-inhibition.
Conclusion
Based on the present review, we learn that hawthorn possesses medical value especially in
cardiovascular field. For further developing hawthorn to commercial products, more works still
need to be done, e.g. purifying the active constituents, clarifying the molecular mechanisms for its
medical action, etc. which may lead to a new era for utilization of hawthorn.
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... It is readily available in the wild in temperate areas of Eurasia and North America, with over 280 species listed. In traditional Chinese medicine, the fruit is used for its stimulating properties of digestion and gastric function and for the improvement of blood circulation [6][7][8][9][10][11][12]. In Europe and North America, flowering tops (leaves and flowers) are used for their astringent, antispasmodic, cardiotonic, diuretic, hypotensive, vasodilative, sedative, antiatherosclerotic, and antihyperlipidemic properties [6-9,12-23]. ...
... In fact, few articles have focused on the extraction modes in water [28][29][30]33,37,41,44,53,62,66,76,79,84,85,87,96] and none have addressed all of the parameters in a single study for the investigation of hawthorn extraction mode and hawthorn extract analysis. Crataegus extracts have been studied and are still currently studied in clinical trials, showing their effectiveness in treating mild heart failure without side effects [6][7][8][9]14,15,[17][18][19][20]22]. Other biological tests have been performed on animals to investigate the impact of hawthorn extracts on various illnesses including cancers [33,55], atherosclerosis [48,58,75], thrombosis [52,59], cataract [97], anxiety [45], heart diseases [13,68,72,75,95], stomach diseases [10], neurological diseases [29], liver diseases [48,67,72], or microbial diseases [10,43,50,73]. ...
... Figure S7 gives the chemical structure of all the compounds identified. Cinnamtannin A2 [7] Vitexin 2-O-rhamnoside [8] Hyperoside [9] Isoquercetin [11] Apigenin -C-Hexoside [12] Grinded (1 mm) flowering tops Infusion Apigenin-C-hexoside R1 [40] Regarding the influence of the extraction mode on the UHPLC profiles, Figures 4 and 5 show that the profiles were very similar for infusion, maceration, US, and percolation modes with a majority (by decreasing order of peak area) of vitexin-2-O-rhamnoside (peak 8), chlorogenic acid (peak 3), hyperoside (peak 9), and isoquercetin (peak 11). The two remarkable differences concern the relative content in cyanidin (peak 1), which was significantly lower for the US mode; and a lower relative content in chlorogenic acid for the MW mode. ...
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Hawthorn (Crataegus) is used for its cardiotonic, hypotensive, vasodilative, sedative, antiatherosclerotic, and antihyperlipidemic properties. One of the main goals of this work was to find a well-defined optimized extraction protocol usable by each of us that would lead to repeatable, controlled, and quantified daily uptake of active components from hawthorn at a drinkable temperature (below 60 °C). A thorough investigation of the extraction mode in water (infusion, maceration, percolation, ultrasounds, microwaves) on the yield of extraction and the amount of phenolic compounds, flavonoids, and proanthocyanidin oligomers as well as on the Ultra High Performance Liquid Chromatography (UHPLC) profiles of the extracted compounds was carried out. High-resolution Fourier transform ion cyclotron resonance mass spectrometry was also implemented to discriminate the different samples and conditions of extraction. The quantitative and qualitative aspects of the extraction as well as the kinetics of extraction were studied, not only according to the part (flowers or leaves), the state (fresh or dried), and the granulometry of the dry plant, but also the stirring speed, the temperature, the extraction time, the volume of the container (cup, mug or bowl) and the use of infusion bags.
... In the framework of traditional medicine used in China, India and some European countries, the properties and effects on health of hawthorn extracts have been well documented. Hawthorn is generally used for its stimulating properties of digestion and gastric function and for the improvement of blood circulation [85,[145][146][147][177][178][179]. For example, dried fruits are often consumed fresh or processed into jams, jellies, soft drinks, candies and canned fruits, especially in Asia [155]. ...
... CA, BC and HAW), the extraction by infusion was found to be an efficient and the easiest way to extract the water-soluble components, in less than 2 min provided that the plant was grinded. It is worth noting that between the lowest extraction yield at 10 min (percolation Chapter III: Water-based extraction of bioactives principles from BA and CA 179 on raw BC, 7.4 %) and the highest value (MW on grinded BC, 33.1 %), a factor of ~4.5 was found on the extraction yield, demonstrating the importance of the protocol of extraction. ...
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... Notably, all five wild fruits have reasonable amount of potassium. The current study showed 77.2 mg/L for potassium in C. oxyacantha while Han et al., (2012) reported 13,531.9 ppm of potassium in C. oxyacantha. ...
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... CA, BC and HAW), the extraction by infusion was found to be an efficient and the easiest way to extract the water-soluble components, in less than 2 min provided that the plant was grinded. It is worth noting that between the lowest extraction yield at 10 min (percolation Chapter III: Water-based extraction of bioactives principles from BA and CA 179 on raw BC, 7.4 %) and the highest value (MW on grinded BC, 33.1 %), a factor of ~4.5 was found on the extraction yield, demonstrating the importance of the protocol of extraction. ...
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... HAW extracts demonstrated strong ACE inhibition (81-92%). HAW extracts have been described as an effective treatment of mild hypertension [64] and moderate heart failure [65][66][67][68][69][70][71]. The extracts of leaves and flowers (flowering tops) were shown to induce cardiovascular effects such as vasodilation and endothelial protection [64,72]. ...
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... Hawthorn has been investigated by evidence-based medicine for treating cardiac insufficiency such as congestive heart failure (CHF), irregular heartbeat (arrythmia), blood circulation problems (Tassel et.al. 2010), asthma, low blood pressure, high cholesterol, type 2 diabetes, muscle spasms, sedation (Han et al. 2011). The antioxidant activity of Crataegus preparations contributes significantly to its therapeutic profile (Gou et al. 2003). ...
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The Balaton Ecomuseum, which is being continuously developed since 2017, will have a holistic approach, where the objectives of the ecomuseum embrace the whole cultural landscape of Lake Balaton as one unit with several thematic routes in one system and shall not be restricted to one particular subject area or a part of local heritage. One of these thematic routes is the recently developing Herbs and Spices Network, led by Zánka Herb Valley Visitor and Training Centre based on the collection, cultivation and processing of medicinal plants, herbs and spices. The place of herbs and spices in the diet needs to be considered in reviewing health benefits, including definitions of the food category and the way in which benefits might be viewed, and therefore researched. Here we describe the already established system of the Zánka Herb Valley Visitor and Training Centre, the potential of the Balaton Region in the development of herbal medicine illustrated by the scientific presentation of the 30 most collected herbs in the region and examples of other herbal centres, which are intended to become a part of the network. Herbal medicine, as an important part of the intangible cultural heritage, with hundreds of years old recipes for herbal concoctions has been known since ancient times before science related to modern medicine developed and continues to be used for generations until now. Furthermore, the medical effects of many agricultural crops should be better understood, such as the grapevine, which is being investigated for its medical compounds or the medicinal properties of other fruits and vegetables not sufficiently known to the general public. In this study we present a new system of the culture and interactive education of the collection, cultivation and use of medicinal plants, herbs and spices applying a learning by doing approach and a network embracing the whole area of the Balaton Ecomuseum.
... Hawthorn (Crataegus pinnatifida Bge.) belongs to rosaceae plants and is cultivated in many parts of China [1]. According to the previous literature, leaves and fruits are widely used as medicinal and food materials in china for their pharmaceutical value and nutritive value [2,3]. ...
... Hawthorn fruit has been used for a long time for their beneficial health effects, mainly consisting in curing scurvy, constipation and digestive disorders. Moreover, hawthorn flowers and leaves are often used against mild cardiac disorders [5]. In modern pharmacology, polyphenols, flavonoids and triterpenoid have been the most studied hawthorn health protective molecules. ...
... Hawthorn (Crataeguspinnatifida.) belongs to Rosaceaeplants and is cultivated in many areas of China [1]. According to literature, hawthorn leaves and fruits are widely used in China for their pharmaceutical and nutritive value [2]. ...
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The purpose of this work was to examine the relationship of the total polyphenol index (TPI) as measured spectrophotometrically and individual phenols as determined by HPLC to antioxidant activity in red wines made from two Vitis vinifera grape varieties grown in NW Spain (viz. Mencía and Brancellao) during bottled storage in the dark for 12 months. Antioxidant activity was determined by using various methods based on inhibition of the coupled oxidation of the β-carotene/linoleic acid mixture. Also, free radical scavenging activity was determined with 2,2-diphenyl-1-picrylhydrazyl (DPPH). Antioxidant activity as measured by DPPH after storage for 3 months was higher in Mencía wines than in Brancellao wines (4.5 ± 0.60 vs. 3.7 ± 0.30 mmol/L trolox equivalents). Beyond 3 months of storage, radical scavenging activity increased in both types of wine (from 4.5 ± 0.60 to 6.0 ± 0.80 mmol/L in Mencía wines and from 3.7 ± 0.30 to 4.7 ± 0.71 mmol/L trolox equivalents in Brancellao wines). The significant correlation found between antioxidant activity and TPI in all wines (r > 0.88) is indicative of the significance of condensation and polymerisation products to the total antioxidant activity of the wines. The relatively high correlation of total flavonols (r = 0.89) and acylated anthocyanins (r = 0.70) as measured by HPLC with to the overall antioxidant capacity suggests that these two polyphenol classes can substantially influence the antioxidant properties of these wines. The linoleic acid/β-carotene assay exposed a higher antioxidant capacity in Brancellao wines than in Mencía wines after 3 months of storage (6.0 ± 0.80 vs. 4.7 ± 0.70). Most of the studied wines lost an average 45% antioxidant activity during bottled storage. Antioxidant activity as measured with the linoleic acid/β-carotene assay was closely correlated with both hydroxycinnamic acids (r = 0.90) and flavanols (r = 0.71 and 0.61 for monomeric and polymeric forms, respectively).
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DOI: 10.1016/j.jff.2010.04.006 The hypocholesterolemic and atheroscleroprotective potentials of dietary consumption of hawthorn (dried fruit of Crataegus pinnatifida, Shan Zha) were investigated by monitoring plasma lipid profiles and aortic relaxation in Sprague–Dawley rats fed with either normal diet, high-cholesterol diet (HCD) or HCD supplemented with hawthorn powder (2%, w/w) (4 weeks). In HCD-fed rats, an increased plasma total cholesterol and LDL-cholesterol with a decreased HDL-cholesterol was observed, and consumption of hawthorn markedly suppressed the elevated total cholesterol and LDL-lipoprotein levels plus an increased HDL-cholesterol level. The blunted acetylcholine-induced, endothelium-dependent relaxation of isolated aortas of HCD-fed rats was improved by hawthorn. The development of fatty liver, an increased nitric oxide synthase (NOS) activity and an elevated oxidative stress (as estimated by the attenuated levels of anti-oxidant enzymes) associated with HCD were attenuated by hawthorn. Thus, the results demonstrated that hawthorn consumption provides overall beneficial effects on reversing HCD associated detrimental changes. Author name used in this publication: Mabel Yin-Chun Yau Author name used in this publication: Peter Hoi-Fu Yu
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Crataegus preparations have been used for centuries especially in Europe. To date, no proper data on their efficacy and safety as an add-on-treatment are available. Therefore a large morbidity/mortality trial was performed. To investigate the efficacy and safety of an add-on treatment with Crataegus extract WS 1442 in patients with congestive heart failure. In this randomised, double-blind, placebo-controlled multicenter study, adults with NYHA class II or III CHF and reduced left ventricular ejection fraction (LVEF< or =35%) were included and received 900 mg/day WS 1442 or placebo for 24 months. Primary endpoint was time until first cardiac event. 2681 patients (WS 1442: 1338; placebo: 1343) were randomised. Average time to first cardiac event was 620 days for WS 1442 and 606 days for placebo (event rates: 27.9% and 28.9%, hazard ratio (HR): 0.95, 95% CI [0.82;1.10]; p=0.476). The trend for cardiac mortality reduction with WS 1442 (9.7% at month 24; HR: 0.89 [0.73;1.09]) was not statistically significant (p=0.269). In the subgroup with LVEF> or =25%, WS 1442 reduced sudden cardiac death by 39.7% (HR 0.59 [0.37;0.94] at month 24; p=0.025). Adverse events were comparable in both groups. In this study, WS 1442 had no significant effect on the primary endpoint. WS 1442 was safe to use in patients receiving optimal medication for heart failure. In addition, the data may indicate that WS 1442 can potentially reduce the incidence of sudden cardiac death, at least in patients with less compromised left ventricular function.
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Hot 50% MeOH extracts of crude drugs considered to have a hypotensive effect were tested for inhibitory effects on hog kidney angiotensin converting enzyme. Of 65 samples tested, 14 showed reproducible inhibition in the preliminary screening. The extracts of 8 potent samples were fractionated by MCI gel and Sephadex LH-20 gel chromatographies to concentrate the inhibitors. The most potent fractions of Arecae Semen, Ephedrae Herba, Epimedii Herba, Polygoni avicularis Herba, Potentillae Herba and Rhei Rhizoma showed more than 90% inhibition at the concentration of 20μg/ml. Those of Moutan Cortex and Cinnamomi Cortex showed 86 and 78% inhibitions, respectively, at the same concentration. All of these fractions consisted of tannin-type compounds.
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Tincture of Crataegus (TCR), an alcoholic extract of the berries of Crataegus oxyacantha, when administered to rats fed a hyperlipidemic diet (HLD), could prevent the elevation in plasma lipid levels. A significant decrease in lipid deposits in liver and aorta was also observed. Analysis of the plasma lipoprotein profile showed that TCR produced remarkable reduction in the increased levels of cholesterol, triglycerides and phospholipids in the low density lipoprotein (LDL) and very low density lipoprotein (VLDL) fractions in hyperlipidemic rats. Histological examination showed severe fatty vacuolation and degeneration of liver of HLD fed rats. TCR administration had an ameliorating effect on these changes. Agarose gel electrophoretic pattern of plasma lipoproteins also indicated that the drug brought down the raised levels of the atherogenic beta-lipoproteins in hyperlipidemic rats.