Cascara
Scientific Name(s): Rhamnus pushiana DC. Family: Rhamnaceae
Common Name(s): Buckthorn , cascara sagrada , chittem bark , sacred bark
Clinical Overview
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Uses of Cascara
Cascara extracts are used in laxatives.
Cascara Dosing
Typical doses of cascara are 1 g of bark, 1 mL of fluid extract, or 300 mg of dried extract. A systematic review has been published on the use of cascara and other laxatives. 1
Contraindications
Cascara is contraindicated in ileus of any origin.
Pregnancy/Lactation
Documented adverse effects (emmenagogue and abortifacient effects). Avoid use. 2 , 3 , 4
Cascara Interactions
None well documented.
Cascara Adverse Reactions
Extended use may cause chronic diarrhea and attendant ills.
Toxicology
When used for short periods of time at appropriate doses, cascara appears to have no toxicities.
Botany
The official cascara sagrada is the dried bark of Rhamnus pushiana collected from small to medium-sized wild deciduous trees. They usually range from 20 to 40 feet high and possess thin, elliptic to ovate-oblong, acutely pointed leaves. The greenish flowers are arranged in umbellate cymes and the fruit is purplish-black and broadly obovoid (8 mm long). The commercial bark is flattened or transversely curved, longitudinally ridged with a brownish to red-brown color. It has gray or white lichen patches and occasional moss attachments. Cascara trees are found in North America in California, Oregon, Washington, Idaho, Montana and as far north as Southeast British Columbia. 5 , 6 A synonym is Frangula purshiana (D.C.) A. Gray ex J.C. Cooper.
History
The American cascara is a folkloric medicine of relatively recent origin, having been introduced as a tree bark laxative by early Mexican and Spanish priests of California (probably Rhamnus californica ). R. purshiana itself was not described officially until 1805 and the bark was not brought into regular medicinal use until 1877. The European counterpart (European buckthorn, Rhamnus frangula ) was described much earlier by the Anglo-Saxons. In fact, the berries were official in the 1650 London Pharmacopoeia. 7
Chemistry
The active laxative principles of cascara include at least 6% to 9% anthracene derivatives which exist as normal O-glycosides and C-glycosides. The four primary glycosides or cascaroside A, B, C and D, contain both O- and C-glycosidin linkages. Chemically these are designated as the C-10 isomers of the 8-O-β-D-glucopyranosides of aloin and chrysophanol. The probable breakdown products of the C-glycosides are the two aloins: Barbaloin which is derived from aloe-emodin anthrone and chrysaloin which is derived from chrysophanol anthrone. Other glycosides isolated include a number of O-glycosides derived from emodin, emodin oxanthrone, aloe-emodin and chrysophanol. A number of dianthrones are also present including emodin, aloe-emodin, chrysophanol and the heterodianthrones, palmidin A, B and C. Compounds found in the free state include aloe-emodin, emodin and chrysophanol.
The free anthraquinones are likely formed in the leaves and stored in the bark largely as C-glycosides. The older bark contains the most C-glycosides. Although not commercially viable, R. purshiana cell suspension cultures produce anthracene derivatives. 6 , 7
Cascara juice also contains other non-laxative compounds eg, rhamnol (cinchol, cupreol, quebrachol); linoleic, myristic and syringic-acids; resins, fat, starch and glucose; malic and tannic acid. The dried seeds contain 7% to 25% protein, 13% to 57% oil and 1% to 2% ash. 8 The presence in the bark of bitter substance and methylhydrocotoin is disputed. 9
A variety of extraction methods have been examined for cascara. Boiling water prevents the losses and changes to the compound that occur in cold water extraction. 10 Active fractions of anthraquinone glucosides have been isolated from R. pushiana and R. frangula by high pressure liquid chromatography. 11 Hydrophilic anthraquinone glycosides have been separated from lesser hydrophilic anthraquinone aglycones by XAD-2 column chromatography. 12 The quantitative analysis of anthraquinones and anthranol in 16 species of Rhamnus from South and East Anatolia have been examined. 13 Likewise, a new naphthalene compound, nakahalene and known anthraquinones, including physcion and frangulin B, have been isolated from Rhamnus species. 14
Cascara Uses and Pharmacology
LaxativeAnimal data
Research reveals no animal data regarding the use of cascara as a laxative.
Clinical dataAs in other laxatives (aloe, senna, etc.), the anthraglycosides are responsible for the cathartic properties in cascara. Cascarosides A and B are the major active principles which act on the large intestine to induce peristalsis and evacuation. 6 More specifically, the anthraglycosides produce an active secretion of water and electrolytes within the lumen of the small intestine and inhibit the absorption of these from the large intestine. This causes an increase in the volume of the bowel contents and strengthens the dilatation pressure in the intestine to stimulate peristalsis. They exert this action with a minimum of side effects. 9 In general, the cascarosides are more active than their hydrolyzed by-products. 6 Furthermore, these cascarosides possess a sweet and more pleasant taste than the aloins and hence should be extracted separately, if possible. 7 Cascara is largely used in the form of a liquid extract or elixir or as tablets made from a standardized dry extract. 6
The daily dose ranges from 20 to 160 mg of the cascara derivatives for the treatment of constipation. 9 The average dose range of total hydroxyanthracene derivatives is 20 to 70 mg daily. 15 The laxative action is seen within 6 to 8 hours after administration. Basically, cascara can be used in most conditions where easy defecation with a soft stool is desired (eg, constipation, hemorrhoids, anal fissures and post rectal-anal surgery). It is contraindicated in ileus of any origin and during pregnancy and lactation. 9
No major side effects are known; however, chronic use or abuse (eg, for weight loss) can result in electrolyte loss, especially potassium. Chronic use can also lead to pigmentation of the intestinal mucosa (melanosis coli).
Because the freshly prepared cascara product contains anthrones, it can lead to severe vomiting and intestinal cramping. Therefore, the bark should be stored for at least a year before use or processed by heating in air to eliminate the presence of anthrones.
Other usesRecent studies have shown that aloe-emodin has antileukemic activity against the P-388 lymphocytic leukemia in mice, 6 that Rhamnus anthraquinones can act as sunscreens in cosmetics, 16 that cascarosides are not readily metabolized in animal model gut microflora, 17 that a Formosan Rhamnus species contains physcion and frangulin B which exhibited a high activity against human hepatoma PLC/PRF/5 and KB cell lines, 14 that R. purshiana extracts are capable of inactivating herpes simplex virus, 18 that anthranoids are transformed to their corresponding glucuronide and sulfate derivatives and appear in the urine and bile, 19 and that a mixture of Curcuma amara and R. purshiana roots have choleretic and serum cholesterol lowering effects in rats. 20
Dosage
Typical doses of cascara are 1 g of bark, 1 mL of fluidextract, or 300 mg of dried extract. A systematic review has been published on the use of cascara and other laxatives. 1
Pregnancy/Lactation
Documented adverse effects (emmenagogue and abortifacient effects). Avoid use. 2 , 3 , 4
Interactions
No direct interactions are known with cascara except where chronic use leads to a potassium deficiency which can potentiate the effects of cardiotonic glycosides (eg, digitalis). The anthraquinone glycosides should not be used for long periods of time because they can cause the above problems or lead to laxative dependence. 9
Adverse Reactions
Extended or habitual use of cascara is to be avoided because it can cause chronic diarrhea and weakness, due to excessive potassium loss. Chronic use can cause melanin pigmentation of the mucous membranes of the colon. 8 , 9 Emodin can produce dermatitis. 8
Toxicology
When used for short periods of time at appropriate doses, cascara appears to have no toxicities.
Bibliography
1. Petticrew M, Watt I, Sheldon T. Systematic review of the effectiveness of laxatives in the elderly. Health Technol Assess . 1997;1:i-iv, 1-52.2. Brinker FJ. Herb Contraindications and Drug Interactions . 2nd ed. Sandy, OR: Eclectic Medical Publications; 1998.
3. Newall CA, Anderson LA, Phillipson JD, eds. Herbal Medicines: A Guide for Health-Care Professionals . London: Pharmaceutical Press; 1996.
4. Ernst E. Herbal medicinal products during pregnancy: are they safe? BJOG . 2002;109:227-235.
5. Osol A, Farrar GE, eds. The Dispensatory of the United States of America , 25th ed. Philadelphia: JB Lippincott, 1955.
6. Leung AY. Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics . New York: J Wiley Interscience, 1980.
7. Evans WC. Trease and Evans' Pharmacognosy , 13th ed. New York: Bailliere Tindall, 1989.
8. Duke JA. Handbook of Medicinal Herbs . Boca Raton, FL: CRC Press, 1985.
9. Bisset NG, ed. Herbal Drugs and Phytopharmaceuticals . Stuttgart: Medpharm Scientific Publishers, 1994.
10. Fairbairn JW, Simic S. New dry extract of cascara ( Rhamnus pushiana DC bark). J Pharm Pharmacol . 1970;22:778.
11. Terracciano M, et al. Analysis of the principle constituents in extracts of cascara and frangula by high pressure liquid chromatography. Boll Chim Farm . 1977;116:402.
12. Denee R, Huizing HJ. Purification and separation of anthracene derivatives on the polystyrene divinylbenzene copolymer. J Nat Prod . 1981;44:257.
13. Coskun M. Quantitative determination of anthraderivatives in Rhamnus species growing in South and East Anatolia (Turkey). Part 2. Int J Crude Drug Res . 1989;27:167.
14. Wei BL, et al. Nakahalene and cytotoxic principles of Formosan Rhamnus species. J Nat Prod . 1992;55:967.
15. Reynolds JEF, ed. Martindale: The Extra Pharmacopoeia , 31st ed. London: Royal Pharmaceutical Society, 1996.
16. Bader S, et al. Natural hydroxyanthracenic polyglycosides as sunscreens. Cosmetics and Toiletries . 1981;96:67.
17. Dreessen M, Lemli J. Studies in the field of drugs containing anthraquinone derivatives. Part 36. Metabolism of cascarosides by intestinal bacteria. Pharm Acta Helv . 1988;63(9–10):287.
18. Sydiskis RJ, et al. Inactivation of enveloped viruses by anthraquinones extracted from plants. Antimicrob Agents Chemother . 1991;35(12):2463.
19. de Witte P, Lemli L. The metabolism of anthranoid laxatives. [Review] Hepato Gastroenterology . 1990;37(6):601.
20. Beynen AC. Lowering of serum cholesterol by Temoe Lawak Singer, a Curcuma mixture. Artery . 1987;14(4):190.
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