sesquiterpenes (aguerin B, cynaropicrin,
grosheimin), sesquiterpene glycosides (cynar-
ascolosides A, B, and C),^2 apigenin-7-rutino-
side, narirutin;^3 artichoke also contains up to
2%O-diphenolic derivatives such as caffeic
acid, 1-, 3-, 4-, and 5-caffeoylquinic acids, and
1,3-di-O-caffeoylquinic acid; flavonoids
(0.1–1.0%), including glycosides luteolin-
7-b-rutinoside (scolymoside), luteolin-7-b-
D-glucoside, and 4-b-D-glucoside; glycolic
and glyceric acids; taraxasterol,Y-taraxaster-
ol; inulin; guaianolides (cynaropicrin, 8-epi-
grosheimin); cynaratriol;4,5sugars; enzymes
(KARRER);6–12and a volatile oil consisting of
b-selinene and caryophyllene as its major
components, witha-cadrene, oct-1-en-3-one,
hex-1-en-3-one, decanal, non-trans-2-enal,
phenylacetaldehyde, and eugenol as the major
aromatic principles.13,14
Cynaropicrin, cynarin (1,3-dicaffeoylqui-
nic acid), 3-caffeoylquinic acid (chlorogenic
acid), and scolymoside are among various
active constituents identified so far.2,10,15,16
The maximum content of cynarin, the major
caffeoylquinic acid derivative in the artichoke
heads,^3 is obtained by aqueous ebullition of
the drug.^17
PHARMACOLOGY AND BIOLOGICAL
ACTIVITIES
Artichoke leaf extract has shown in vitro
antimicrobial^18 and antioxidant activities,
the latter attributed to caffeic acid, 1-caf-
feoylquinic acid, luteolin, apigenin-7-O-glu-
coside, luteolin-7-O-glucoside, luteolin-7-ru-
tinoside, cynarin, cynaroside, chlorogenic
acid, and narirutin.19,20Antioxidant activity
was also shown in the erythrocytes of rats fed
diets containing the edible portions of arti-
choke, and the effect was accompanied by a
decrease in plasma uric acid.^21 Anticlasto-
genic activity was shown in the in vivo
mouse bone marrow micronucleus assay
from the leaf homogenate or concentrate,^22
and topical administration of taraxastane-
type hydroxy triterpenes isolated from the
leaves (faradiol and taraxasterol) inhibited
the development of skin tumors in mice.^23
Although more than one study showed no
cholerectic activity from either cholorgenic
acid or cynarin in rats,16,24acute and repeat-
ed oral administration of an artichoke leaf
extract in rats produced increases in total bile
acid levels, however, without any effect on
cholesterol or phospholipid levels.^25 Sesqui-
terpene constituents of the leaves, notably
cynaropicrin, lowered serum triglyceride le-
vels in rats when administered orally follow-
ing olive oil.^2 Hepatoprotective activity has
been shown in both animal and in vitro
studies with artichoke extracts.^26
Placebo-controlled clinical trials of artichoke
leaf extracts have shown cholersterol-lowering
effects15,26–28and symptomatic improvement of
patients with functional dyspepsia.^29 Cynarin
has shown inconsistent hypolipidemic effects
in humans (MARTINDALE).30,31TOXICOLOGYSide effects from artichoke are mild or ab-
sent26–28,32and drug interactions are unknown
(BLUMENTHAL1). Allergic reactions to arti-
choke are rare, including allergic contact der-
matitis,^33 food allergy,^34 acute edema of the
tongue,^35 bronchial asthma, and allergic rhi-
nitis.^36 Potential allergens in artichoke are
sesquiterpene lactones, including cynaropi-
crin.37,38In rats, LD 50 of an extract containing
46% caffeoylquinic acids was 265 mg/kg i.p.
and by the oral route the LD 40 was 2000 mg/
kg. The LD 50 of a hydroalcoholic extract of
artichoke containing 19% caffeoylquinic
acids was 1000 mg/kg i.p.^39 Use is contra-
indicated in individuals with known allergies
to the Composite plant family, in bile duct
obstructions, and in gallstones (except under
medical advice) (BLUMENTHAL1).USESMedicinal, Pharmaceutical, and Cosmetic.
Artichoke leaf extracts have been widely used
in Europe for the treatment of digestive com-46 Artichoke