Brief Introduction

Synonyms--- Cascara Buckthorn, Cascara, Cascara Sagrada, Rhamni Purshianae cortex and Rhamnus, Bearberry, and in the Chinook Jargon, Chittam or Chitticum; syn. Frangula purshiana, Rhamnus purshianus

Cascaroside A

Chemical Name: (10S)-1-hydroxy-3-(hydroxymethyl)-10-[(2S,3R,4S,5S,6R)-3,4,5- trihydroxy-6-(hydroxymethyl)oxan-2-yl]-8-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-10H-anthracen-9-one
CAS No.: 53823-08-8

Molecular Formula: C₂₇H₃₂O₁₄

Mol. Wt.:

Molecular Structure:

Carscara, Rhamnus purshiana(Cascara Buckthorn, Cascara, Cascara Sagrada, Rhamni Purshianae cortex and Rhamnus, Bearberry, and in the Chinook Jargon, Chittam or Chitticum; syn. Frangula purshiana, Rhamnus purshianus) is a species of buckthorn native to western North America from southern British Columbia south to central California, and inland to western Montana. It is the largest species of buckthorn, occasionally growing up to 15 m tall, though more commonly a large shrub or small tree 5–10 m tall, with a trunk 20–50 cm in diameter. The bark is brownish to silver-grey with light splotching. The leaves are deciduous, alternate, clustered near the ends of twigs; they are oval, 5–15 cm long and 2–5 cm broad with a 0.6–2 cm petiole, dark shiny green on top, fuzzy and paler green below. The flowers are tiny, 4–5 mm diameter, with five greenish yellow petals; the flowering season is brief, disappearing by early summer. The fruit is a berry 6–10 mm diameter, bright red at first, quickly maturing deep purple or black, and containing three seeds.

The dried, aged bark of this tree has been used continually for at least 1,000 years by both native and immigrant Americans as a laxative natural medicine, commercially called "Cascara Sagrada", but old timers call it "chitticum bark". The laxative action is due to the Cascara glycosides (cascarosides A, B, C & D).

Cascara Sagradameans "sacred bark" in Spanish. The much more pertinent name chitticum means "shit come" in Chinook Jargon; chittam comes from the Chinook Jargon phrase chittam stick = "laxative tree" which is similarly from the English word "shit".

The bark is harvested mostly from wild trees; over-harvesting in the middle 1900s eliminated mature trees near many settled areas. Once stripped from the tree, the bark is aged for about 1 year to make its effect milder. Fresh cut, dried bark causes vomiting and violent diarrhea.

Long used as a laxative by Native American groups of the northwest Pacific coast, chitticum bark or Cascara Sagrada was accepted in medical practice in the United States in 1877, and by 1890 had replaced the berries of the European Buckthorn (R. catharticus) as a commonly used laxative. It was the principal ingredient in many commercial, over-the-counter laxatives in North American pharmacies until 9 May 2002, when the U.S. Food and Drug Administration issued a final rule banning the use of aloe and cascara sagrada as laxative ingredients in over-the-counter drug products. Use of Cascara Sagrada has been associated with abdominal pain and diarrhea and is potentially carcinogenic.

Cascara bark is now listed as a laxative in the pharmacopoeias of over 17 different countries around the world. The bark is primarily used for constipation and for conditions that require a softened stool such as hemorrhoids, anal fissures, and after rectal-anal surgery. The bark of a related Eurasian species, Rhamnus frangula, is used likewise for the same purposes. The bark is taken from the stem and branches in the spring but must be stored for at least a year or, alternatively, heat treated before using to allow anthrones in the fresh bark to oxidize, otherwise preparations will cause stomach upset. Cascara bark acts as a mild laxative that works by preventing electrolytes and water from being absorbed in the large intestine; the excess liquid softens the stool and promotes bowel contractions. Both the German and British Pharmacopoeias recommend Cascara bark for constipation and for all disorders in which defecation with a soft stool is desired, e.g. anal fissures, hemorrhoids and after rectal operations. The active glycosides are hydrolyzed in the gut into their aglycones at least in part by the action of bacterial enzymes; by influencing the water and electrolyte transport in the colon, these aglycones are responsible for the laxative action. Emodin at different concentrations has many therapeutic benefits including: anti-inflammatory at 15mg/kg; antiseptic; antispasmodic; antiulcer, cathartic; vasorelaxant and viricidal. Anthraquinones are also cytotoxic and stimulate cellular regeneration, detoxification and cleansing. Chronic use of anthraquinones-type laxatives, however, often causes pseudomelanosis coli and should be avoided.

Active Ingredients:      

Cascara bark contains: 8-10% of a complex mixture of anthraquinone glycosides of which 60-70% are cascarosides A, B, C, D, E, and F, 10-30% are aloins A and B with chrysaloins A and B and 10-20% are anthroquinone O-glycosides and free anthraquinones including: aloe-emodin, frangula emodin, iso-emodin, chrysophanol and physcion. The bark also contains resins, tannins and lipids. Cascarosides A and B are alooin O- and C-glycosides) and cascarosides C and D are deoxyaloin O- and C-glycosides. The bark also contains barbaloin and O-glycosides of emodin (e.g. frangulin), emosin oxanthrone and palmidin A, B, and C (also found in Rhubarb Root). The bark also contains linoleic acid, myristic acid and syringic acid.

The Casacara Bark Extract used in dietary supplements is derived from the bark of the stem and branches of the plantRhamnus purshianaL. (stored for at least one year).

Benefits

• Mild Laxative Effects

•Treating Annual Fissures

• Treating Constipation

• Treating Hemorrhoids

• Cellular Regeneration Effects

•Detoxifying Effects

•Cleaning Effects

•Pre and Post Operative Cleansing Effects

Mechanism

Referring to the above information.

Safety

Drug Interactions:       

In large dosages, the anthraquinones-type laxative compounds may increase the action of other laxatives and should not be taken at the same time. With chronic use/abuse, a potassium deficiency may develop that may potentiate the effects of cardiotonic glycosides.

Contraindications:      

Laxatives are contraindicated in the case of impacted bowel (serious bowel obstruction) or ileus of any origin (danger of intestinal rupture). Stimulant laxatives are also not recommended for the treatment of chronic constipation. Do not use during pregnancy and lactation, or if you have occlusion of the intestines, appendicitis, colitis or Crohn's disease.

Side Effects:

Cascara Bark should not be taken for long periods of time. Excessive use will result in loss of electrolytes, especially potassium, and may cause muscular weakness, constipation, and pigment deposits in the mucous membranes of the intestines (melanosis coli). A recent study suggested that pseudomelanosis coli is associated with an increased colorectal cancer risk.

Dosage

• SuggestedAmount:

The daily dosage with tea is 1-2g of cut or powdered aged bark yielding 20-30mg hydroxyanthracene derivates, calculated as cascaroside. To make a tea: Pour boiling water over 1-2 g of finely chopped Cascara bark, steep 10 minutes and then strain. 1 Teaspoon = 2.5 g. Average daily dose is 20-160 mg hydroxyanthracene derivatives. The bark takes about 6 to 8 hours to work after ingestion and should not be used for more than a few days at a time unless otherwise prescribed. Only aged drug should be used. Anthrones found in the fresh bark will irritate the stomach and may cause vomiting, colic, and bloody diarrhea.

•  Consult physicians for different condition specifics.

GNI’s Cascara Bark Extract Features and Benefits:

Cascara Bark Extract is one of GNI's most competitive products, with many advantages as list in the following, produced as our patent-pending process and know-how technology from Rhamnus purshianaL.bark.

•  Produced with pure water only

•  High purity: over 7%

•  NO solvent - residual free

•  Pesticide-free

•  Brown to yellow in appearance

•  High solubility in water

•  High anti-bacteria, and longer shelf life

Product Specifications:

8%, 20% Cascarosides HPLC,

4:1, 6:1