Medicinal plants commonly used in the Newly Independent

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Defi nition

Folium cum Flore Crataegi consists of the dried fl ower-bearing branches 

of Crataegus monogyna Jacq. (Lindm), C. laevigata (Poir.) DC, their hy-

brids or, more rarely, other Crataegus species (Rosaceae).



Crataegus monogyna Jacq. (Lindm): C. apiifolia Medik. non Michx., C. 

Oxyacantha L. ssp. monogyna Lev., Mespilus elegans Poir., M. monogyna 

All., M. Monogyna Ehrh. (3).

Crataegus laevigata (Poir.) DC: C. oxyacantha L., C. oxyacantha L. 

ssp. Polygala Lev., C. oxyacanthoides Thuill, Mespilus oxyacantha (Gartn.) 

Crantz. (134).

Selected vernacular names

Aubeline, aubepine, biancospino, calabrice, calavrice, eenarijlige meidorn, 

eenstijlige meidorn, eingriffeliger Weissdorn, Einkern-Weissdorn, épine 

blanche, espinero, espino blanco, espino majuelo, galagonya virágzó ágvég, 

hagdorn, hagedorn, harthorne, haw, hawthorn, hedge thorn, majuelo, may, 

May thorn, Mehlbeerbaum, Mehldorn, seiyosanzashi, shanzha, sorkh valik, 

spina, Stumpf gelappter Weissdorn, Weissdorn, whitethorn, za bur, zu’rurr 

el awdiyah, zweigriffeliger Weissdorn, Zweikern-Weissdorn (135–8).

Geographical distribution

Common to the temperate areas of the northern hemisphere, including 

eastern areas of North America, parts of South America, east Asia and 

Europe (910).



Adopted from the volume 2 of WHO monographs on selected medicinal plants.


  Fructus Crataegi is included in the European pharmacopoeia (1) and in the pharmacopoeia of the 

People’s Republic of China (2). However, clinical and pharmacological data for this plant part are 

insuffi cient to justify monographing at this time.

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Crataegus monogyna: a thorny shrub; leaves bright green with 3 or 5 acute 

lobes, deeper and further apart than those of C. laevigata. Flowers, 

grouped into branchy corymbs, have 5 triangular sepals, 5 white petals, 

and an androecium of 15–20 stamens inserted on the edge of a monocar-

pellate, brownish-green receptacle; fl oral peduncles and sepals pubescent, 

stamen with black anthers and 1 style (19).

Crataegus laevigata: a thorny shrub; twigs glabrescent, brown; leaves 

bright green, obovate, with 3, 5 or 7 shallow, obtuse lobes. Flowers, 

grouped into branchy corymbs, have 5 triangular sepals, 5 white petals, 

and an androecium of 15–20 stamens inserted on the edge of a bi- or tri-

carpellate receptacle; fl oral peduncles and sepals glabrous, stamens with 

red anthers and 2–3 styles; fruits deep red, globose or ellipsoid (911).

Plant material of interest: dried leaf with fl ower

General appearance

Crataegus monogyna: leaves bright green with 3 or 5 acute lobes, deeper 

and further apart than those of C. laevigata, with secondary venation 

curved outwards. Flowers, grouped into branchy corymbs, have 5 trian-

gular sepals, 5 white petals, and an androecium of 15–20 stamens inserted 

on the edge of a monocarpellate, brownish-green receptacle; fl oral pe-

duncles and sepals pubescent, anthers black with 1 style; sepals lanceolate, 

acuminate, falling over the ovary after fl owering (19).

Crataegus laevigata: leaves bright green with 3, 5 or 7 shallow, obtuse, 

converging lobes, with secondary venation curved inward. Flowers, 

grouped into branchy corymbs, have 5 triangular sepals, 5 white petals, 

and an androecium of 15–20 stamens inserted on the edge of a bi- or tri-

carpellate receptacle; fl oral peduncles and sepals glabrous, stamens with 

red anthers and 2–3 styles.

Organoleptic properties

Odour: characteristic, faint; taste: slightly bitter-sweet, astringent (1215).

Microscopic characteristics

Leaf dorsoventral; cells of upper epidermis polygonal, straight-walled 

with striated cuticle, those of lower epidermis more sinuous; anomocytic 

stomata on lower epidermis only; covering trichomes on both epidermis-

es but more numerous on the lower, which are long, tapering, unicellular or 

very occasionally uniseriate with 2 cells, walls moderately thickened; 

cluster crystals or groups of small prismatic crystals of calcium oxalate in 

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Folium cum Flore Crataegi

the cells along the veins. Epidermis of fl oral pedicel and receptacle con-

tain abundant covering trichomes similar to those on the leaf, but longer 

and more undulating; calyx with numerous anomocytic stomata on the 

outer epidermis, inner epidermis with a striated cuticle; epidermal cells of 

corolla distinctly papillose; fi brous layer of anther with characteristic 

thickenings; pollen grains spherical to elliptical, up to 45 µm in diameter, 

with 3 germinal pores and faintly granular exine. Epidermal cells of stem 

have thickened anticlinal outer walls; cortex parenchymatous with pris-

matic and cluster crystals of calcium oxalate; dense groups of small, tight-

ly packed pericyclic fi bres with much thickened and lignifi ed walls; xylem 

completely lignifi ed, composed of scattered vessels, thick-walled fi bres 

and parenchyma separated by distinct medullary rays containing brown-

coloured matter; larger vessels with bordered pits, smaller elements with 

annular or spiral thickening; central pith parenchymatous and lignifi ed, 

cells with moderately thickened walls and numerous pits (1215).

Powdered plant material

Yellowish-green. Unicellular covering trichomes, usually with a thick 

wall and wide lumen, almost straight or slightly curved, pitted at the base; 

fragments of leaf epidermis with cells which have sinuous to polygonal 

anticlinal walls and large anomocytic stomata surrounded by 4–7 subsid-

iary cells; parenchymatous cells of mesophyll containing cluster crystals 

of calcium oxalate, usually 10–20 µm in diameter; cells associated with 

veins contain groups of small prismatic crystals. Petal fragments showing 

rounded polygonal epidermal cells, strongly papillose, thick walls with 

clearly visible wavy striations in the cuticle; anther fragments showing 

endothecium with an arched and regularly thickened margin. Stem frag-

ments containing collenchymatous cells, bordered, pitted vessels and 

groups of lignifi ed sclerenchymatous fi bres with narrow lumina. Numer-

ous spherical to elliptical or triangular pollen grains up to 45 µm in diam-

eter, with 3 germinal pores and a faintly granular exine (1).

General identity tests

Macroscopic and microscopic examinations, thin-layer chromatography 

(17), and microchemical test for the presence of procyanidins (7).

Purity tests


Tests for specifi c microorganisms and microbial contamination limits are 

as described in the WHO guidelines on quality control methods for me-

dicinal plants (16).

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Foreign organic matter

Not more than 8% lignifi ed branches with a diameter greater than 2.5 mm 

(1) and not more than 2% other foreign matter (115).

Total ash

Not more than 10% (1).

Loss on drying

Not more than 10% (1).

Pesticide residues

The recommended maximum limit of aldrin and dieldrin is not more than 

0.05 mg/kg (17). For other pesticides, see the European pharmacopoeia 

(17), and the WHO guidelines on quality control methods for medicinal 

plants (16) and pesticide residues (18).

Other purity tests

Chemical, acid-insoluble ash, sulfated ash, water-soluble extractive and 

alcohol-soluble extractive tests to be established in accordance with na-

tional requirements.

Heavy metals

For maximum limits and analysis of heavy metals, consult the WHO 

guidelines on quality control methods for medicinal plants (16).

Radioactive residues

Where applicable, consult the WHO guidelines on quality control meth-

ods for medicinal plants (16) for the analysis of radioactive isotopes.

Chemical assays

Contains not less than 1.5% of fl avonoids, calculated as hyperoside (1), 

and not less than 0.6% of fl avone C-glycosides, calculated as vitexin (14), 

determined by spectrophotometry at 410 and 336 nm, respectively (1). A 

high-performance liquid chromatography method is also available (19).

Major chemical constituents

The major constituents are fl avonoids (rutin, hyperoside, vitexin, vitex-

in-2´´ rhamnoside, acetylvitexin-2´´ rhamnoside) and related proanthocy-

anidins (1920). In the infl orescence, fl avonol glycosides, mainly in the 

form of hyperoside, spiraeoside and rutin, are present. The primary fl avo-

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Folium cum Flore Crataegi

noid derivatives in the leaves are epi-catechin (epi-catechol) and/or cate-

chin (catechol), and the related procyanidins formed during condensation 

of 2–8 monomeric units of the above catechins (1922), together with 

oligomeric procyanidins (23). The presence of simple phenolic acids (e.g. 

chlorogenic and caffeic acids) has also been reported. Of the non-pheno-

lic constituents, pentacyclic triterpenes (e.g. ursolic and oleanolic acids) 

and the 2-

α-hydroxy derivative of oleanolic acid, known as crataegolic 

acid, are among the characteristic components (4). The structures of the 

characteristic constituents are presented below.


R X 

hyperoside H  Gal 

spiraeoside Glc H 

rutin H 



vitexin R = H 

vitexin 2

"-rhamnoside R = Rha 

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6-deoxy- -



6)-  -






R    R 


ca t ec h i n   (ca t ec h o l )    



epi - ca t ec h i n   ( epi - ca t ec h o l )    H   OH 















-rhamnopyranosyl = 6-

deoxy- -





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Folium cum Flore Crataegi

Medicinal uses

Uses supported by clinical data

Treatment of chronic congestive heart failure stage II, as defi ned by the 

New York Heart Association (24–34).

Uses described in pharmacopoeias and in traditional systems

of medicine

Support of cardiac and circulatory functions (35).

Uses described in folk medicine, not supported by experimental

or clinical data

As an antispasmodic agent in the treatment of asthma, diarrhoea, gall 

bladder disease and uterine contractions, and as a sedative for the treat-

ment of insomnia (5).


Experimental pharmacology

Inotropic effects

Positive inotropic effects of Folium cum Flore Crataegi and its constitu-

ents have been demonstrated both in vitro and in vivo. These effects are 




α α






α α 








pr o c y a n i d i n    2 







R )   - 

R )   - 

R )   - 

S)   - 

R )    


R )   - 

R )   - 

R )  - 

R )   - 

R )    


R )   - 

R ) 

- ( 

S)   - 

S)   - 



R )   - 

R )   - 

S)    α- ( R)   - 


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generally attributed to the fl avonoid and procyanidin constituents of the 

leaves with fl owers (3,  3638). A hydroalcoholic extract of the fl owers 

with leaves, fl avonoid and procyanidin fractions of the extract, and iso-

lated constituents (e.g. biogenic amines, crataegolic acid, epi-catechin, hy-

peroside, luteolin 7-glucoside, rutin and vitexin) all have positive inotro-

pic effects, and prolong the refractory period in cardiac myocytes, 

isolated papillary muscles and isolated guinea-pig hearts (3648). In iso-

lated guinea-pig hearts perfused at constant pressure, 3 µg/ml of a stan-

dardized extract increased the contractility of the heart by 9.5% (40). In 

isolated, electrically stimulated strips of failing human left ventricular 

myocardium, a standardized extract (18.75% oligomeric procyanidins) 

increased the force of contraction at concentrations higher than 10 µg/ml; 

a 100 µg/ml extract improved the force–frequency relationship (39). A 

standardized extract of the leaves and fl owers increased the contractility 

of myocardial cells by 153%, at a concentration of 120 µg/ml (44). An 

aqueous extract of the leaves with fl owers, two proanthocyanidin frac-

tions and two fl avonoid fractions of the extract dilated coronary blood 

vessels, and had positive inotropic effects on isolated guinea-pig hearts 

(extract or fraction: 0.05 mg/ml) (41).

Chronotropic effects

Intragastric administration of a macerate or fl uidextract of the shoots, 

fl owers or leaves to rats (12.5–25.0 mg/kg body weight) signifi cantly in-

hibited arrhythmias induced by aconitine, calcium chloride or chloro-

form/epinephrine (< 0.05) (4950). The extracts also reduced blood pres-

sure in rats at the same dosage (49,  50). Aconitine-induced arrythmias 

were also inhibited after intravenous administration of a 95% ethanol ex-

tract of the bark and leaves (50 mg/kg body weight) to rabbits (51). Intra-

venous administration of a fl avonoid-enriched extract of the leaves and 

fl owers to rabbits (20 mg/kg body weight) or rats (2 mg/kg body weight) 

inhibited barium chloride-induced arrhythmias (5253). Intravenous ad-

ministration of a standardized extract (containing 18.75% oligomeric pro-

cyanidins) to anaesthetized dogs (7.5–30.0 mg/kg body weight) increased 

maximum left ventricular contraction velocity by 16.8–31.1% (54).

An aqueous extract improved cardiac performance during reperfusion, 

reduced lactate levels and accelerated energy metabolism in reperfused 

ischaemic rat heart. No increase in coronary blood fl ow was observed 

(55). Intragastric administration of single doses of a standardized extract 

(containing 18.75% oligomeric procyanidins) of the leaves with fl owers 

(100 mg/kg body weight) or an oligomeric procyanidin-enriched fraction 

(20 mg/kg body weight) daily to rats protected against perfusion-induced 

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Folium cum Flore Crataegi

arrhythmias, hypotensive crisis and mortality (56,  57). The oligomeric 

procyanidin-enriched fraction did not decrease the reperfusion-induced 

elevation of creatine kinase plasma levels (57). Administration of pow-

dered leaves and fl owers to rats (2% of diet) reduced the release of lactate 

dehydrogenase after perfusion-induced heart ischaemia (58).

Effect on coronary blood fl ow

Intragastric administration of an oligomeric procyanidin fraction of a 

standardized leaf and fl ower extract to dogs at a dose of 12–70 mg/kg 

body weight, three times daily for 60 days, increased myocardial blood 

fl ow (5960). Intravenous injection of an aqueous or 95% ethanol extract 

of the fl owers increased coronary blood fl ow and cardiac output, and de-

creased peripheral resistance in both dogs and guinea-pigs (6163). Ad-

ministration of a fl avonoid-enriched extract to cats and rabbits increased 

coronary blood fl ow by 48% and 163%, respectively, and reduced pitui-

trin-induced coronary insuffi ciency in rabbits (52). Intravenous adminis-

tration of a leaf with fl ower extract to cats (10 mg/kg body weight) or 

rabbits (20 mg/kg body weight) dilated coronary blood vessels, and im-

proved coronary blood fl ow (53).

Effect on action potential

A leaf preparation (10 mg/l) prolonged the duration of the action poten-

tial and delayed the recovery of V


 in isolated guinea-pig papillary mus-

cle (42). The electrophysiological correlation between the increase in the 

contraction amplitude of isolated canine papillary muscles, and vasodila-

tion in isolated human coronary arteries, was measured after application 

of an extract of the leaves with fl owers. The cardiac action potential sig-

nifi cantly increased in duration and overshoot, and maximal depolariza-

tion (< 0.001). Hyperpolarization of the resting membrane of normal 

and arteriosclerotic vascular smooth muscle cells of the human coronary 

artery was observed after treatment with fl avonoids isolated from the ex-

tract (0.1 and 100 µmol/l). The isometric wall tension decreased in both 

normal and arteriosclerotic vessels. The increase of peak-to-plateau repo-

larization in cardiac action potential and hyperpolarization of vascular 

smooth muscle suggest that the extract acts as a potassium channel agonist 


Antihypertensive effects

In various animal models, a decrease in peripheral vascular resistance and 

hypertension occurred after treatment with leaf and/or fl ower extracts (50

5466–69). Intravenous administration of a standardized fl uidextract of the 

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leaves with fl owers (equivalent to 6 mg of procyanidins/kg body weight) 

to anaesthetized normotensive dogs decreased norepinephrine-induced el-

evation of blood pressure. The extract (equivalent to 0.03 mg procyani-

dins/ml) also had 

β-blocking activity and inhibited epinephrine-induced 

tachycardia in isolated frog hearts (69). Hyperoside, isolated from an ex-

tract of the leaves and fl owers, administered either intravenously at a dose 

of 1 mg/kg body weight or by infusion at 0.1 mg/kg body weight/min for 

30 min, decreased blood pressure in anaesthetized dogs (68). Intravenous 

administration of an aqueous extract of the leaves (average dose 31 mg/kg 

body weight) decreased the systolic, diastolic and mean blood pressure in 

normotensive anaesthetized rats (66). Acute or chronic intragastric admin-

istration of a fl uidextract or a glycerol/ethanol extract reduced arterial 

blood pressure in normotensive rats and in rats with desoxycorticosterone 

acetate-induced hypertension (50). Intragastric administration of a stan-

dardized extract (300 mg/kg body weight daily) decreased blood pressure 

by 9 mm Hg (1.20 kPa) (67). Intravenous administration of a standardized 

extract (containing 18.75% oligomeric procyanidins) to anaesthetized rats 

(30 mg/kg body weight) or dogs (15 mg/kg body weight) decreased total 

peripheral resistance and arterial blood pressure (54).

Anti-infl ammatory effects

Both free radical production and lipid peroxidation are involved in vari-

ous pathological processes, including cardiac ischaemia. As determined 

by in vitro studies, Folium cum Flore Crataegi has free radical scavenging 

and antioxidant activities. A standardized extract (containing 18.75% 

oligomeric procyanidins) and an oligomeric procyanidin-fraction of the 

extract inhibited lipid peroxidation (IC


 0.48 µg/ml (extract), 0.3 µg/ml 

(fraction)), and the activity of human neutrophil elastase (IC


 4.75 µg/ml 

(extract), 0.84 µg/ml (fraction)) (56). A 70% methanol extract of the fl ow-

er buds inhibited lipid peroxidation in rat liver microsomes (IC


 23 µg/l) 

(7071). Both phenolic and fl avonoid-enriched fractions of extracts of the 

leaves and fl owers had antioxidant activity in vitro (7072).

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