isoemodin, and chrysophanol, also known as
chrysophanic acid), resins, tannins, and lipids,
among others (STAHL).1–6
Cascarosides account for 60–70% of the
total anthraglycosides (anthracene deriva-
tives) present; the remainder (10–20%) con-
sists mostly of anthraquinone-O-glucosides
(e.g., frangulaemodin- and aloe-emodin-
8-O-glucoside), aglycones of chrysophanol,
frangulaemodin, aloe-emodin, and physcion),
and small amounts of hetero- and isodian-
thrones (WICHTL). Cascarosides A and B are
O-glucosides of barbaloin, while cascarosides
C and D areO-glucosides of chrysaloin. Mild
acid hydrolysis of cascarosides yields aloins,
which, however, can be broken down to their
aglycones only bystrong oxidativehydrolysis.
PHARMACOLOGY AND BIOLOGICAL
ACTIVITIES
Cascarosides A and B are responsible for most
of the cathartic properties in cascara and act
on the large intestine by inducing increased
peristalsis (seesenna).7–9Cascarosides are
more active than their hydrolyzed products
(aloins and free anthraquinones).10–12
Laxatives can potentially interfere with
orally administered drugs taken at the same
time through a decrease in intestinal transit
time. Long-term use of anthranoid-containing
laxatives can result in potassium depletion; for
those taking cardiac glycosides potassium
deficiency may result in cardiac arrhythmias
(FUGH-BERMAN;WICHTL).
USES
Medicinal, Pharmaceutical, and Cosmetic.
Used extensively in laxative preparations; also
used in sunscreens.
Food. Only the bitterless extract is repor-
tedly used as a flavor component in foods,
including nonalcoholic beverages, frozen
dairy desserts, and candy and baked goods.
Average maximum use level is below 0.008%
(75 ppm).
Dietary Supplements/Health Foods. Crude
aged bark used in laxative and detoxicant teas;
extracts in herbal formulas (capsules, tablets,
drinks, etc.) for the laxative and alleged
detoxicant effects.
Traditional Medicine. Bark infusion used
by various North American Indian tribes as
a laxative and purgative; also taken for arthri-
tis and rheumatism, as a treatment for worms
in children, and used topically for sores
(MOERMAN); reportedly used in treatments of
cancer.^13
COMMERCIAL PREPARATIONS
Crude and fluid extract, aromatic fluid extract,
solid extract (bitter, bitterless, aromatic), pow-
der extract, granular extract, and cascaroside
concentrates; crude, aromatic fluid extract,
and bitter fluid and powder extracts are official
in U.S.P. Strengths of extracts (seeglossary)
are expressed in weight-to-weight ratios as
well as total cascaroside content.
Regulatory Status. Allowed as a natural fla-
voring substance at subtherapeutic levels
(§172.510). In 2002, the U.S. FDA. ruled that
in over-the-counter products cascara sagrada
is not GRAS and effective.^14 Bark subject of
a German therapeutic monograph; allowed
for short-term use in laxative formulations;
only sold in pharmacies (BLUMENTHAL 1;
WICHTL).
REFERENCES
See the General References forAPhA;BAILEY1;BARNES;BLUMENTHAL1;BRUNETON;DER MARDEROSIAN AND
BEUTLER;ESCOP1;FEMA;FUGH-BERMAN;KROCHMAL AND KROCHMAL;LUST;MARTINDALE;STAHL;WICHTL;
YOUNGKEN.
150 Cascara sagrada