BLOODROOT (Sanguinaria canadensis L. (Papaveraceae))

HERBAL

MEDICINAL

PLANT

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BLOODROOT !

Sanguinaria canadensis L. (Papaveraceae)

By

RETTODWIKART THENU

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BLOODROOT !

(bluhd’rewt)

SUMMARY AND PHARMACEUTICAL COMMENT

Bloodroot is characterised by isoquinoline alkaloid constituents (benzophenanthridine-type), predominantly sanguinarine. A wide range of pharmacological activities has been documented for this class of compounds including antimicrobial, anti-inflammatory, antihistaminic, cardiotonic and antiplaque. Other benzophenanthridine alkaloids have been associated with cytotoxic activities. However, recent interest over the potential use of bloodroot in oral hygiene has stimulated considerable research into both sanguinarine and bloodroot extracts. Results have indicated that products such as oral rinses and toothpastes containing either sanguinaria extracts or sanguinarine may be of value in dental hygiene.

SCIENTIFIC NAME

Sanguinaria canadensis L. (Papaveraceae)

OTHER COMMON NAMES

Coon root, Indian paint, paucon, pauson, red puccoon, redroot, sweet slumber, tetterwort

ORIGIN

Bloodroot is a perennial found in Canada and the southern region of the United States.

PHARMACOPOEIAL AND OTHER MONOGRAPHS

BHP 1983(G7)

Martindale 35th edition(G85)

LEGAL CATEGORY (LICENSED PRODUCTS)

Bloodroot is not included in the GSL.(G37)

CONSTITUENTS

The following is compiled from several sources, including General References G22 and G41.

Alkaloids Isoquinoline type. 3.0–7.0%.(1) Sanguinarine (approx. 1%), sanguidimerine, chelerythrine, protopine; others include oxysanguinarine, a- and b-allocryptopine, sanguilutine, dihydrosanguilutine, berberine, coptisine and homochelidonine.

Other constituents Resin, starch, organic acids (citric, malic). Alkaloid content of other plant parts recorded as 0.08% (leaf), 1.8% (root).

USES

Bloodroot has been used for its expectorant, antimicrobial, antiinfl ammatory, antiplaque (dental—topically), and antifungal properties. It has also been used topically for the treatment of skin, ear, and nose cancer and for nasal polyps.

FOOD USE

Bloodroot is listed by the Council of Europe as a natural source of food flavouring (category N3). This category indicates that bloodroot can be added to foodstuffs in the traditionally accepted manner, although there is insufficient information available for an adequate assessment of potential toxicity.(G16)

HERBAL USE

Bloodroot is stated to act as an expectorant, spasmolytic, emetic, cathartic, antiseptic, cardioactive, topical irritant and escharotic (scab-producing). Traditionally it is indicated for bronchitis (subacute or chronic), asthma, croup, laryngitis, pharyngitis, deficient capillary circulation, nasal polyps (as a snuff), and specifically for asthma and bronchitis with feeble peripheral circulation.(G7)

ACTIONS

The use of bloodroot is considered to be obsolete because of its toxicity. However, its various actions account for its continued use. The isoquinolone alkaloids sanguinarine and chelerythrine possess antimicrobial and antimycobacterial actions. Sanguinarine is a hypotensive dental antiplaque and CNS depressant.

Analgesic Action

The analgesic action of bloodroot occurs via mechanisms similar to those of opioids, with paralysis of the nerve endings leading to lessened pain.

Antiplaque Action

The antiplaque action of bloodroot is well documented in the literature. Some toothpaste and mouthwash manufacturers include bloodroot as an ingredient to help limit oral plaque. The alkaloid sanguinarine is effective against various oral bacteria (Dzink et al, 1985; Godowski, 1989). This action appears to be due to an alkaloid present in the herb.

Topical Action

Bloodroot has been found to corrode and destroy topical cancers and topical fungal infections (Phelan et al, 1963). In cancers of the nose and ears, bloodroot has been shown to destroy these lesions.

Other Actions

Methanol extracts of the rhizomes of bloodroot were analyzed. Two isoquinoline alkaloids were identifi ed in the active fraction. Sanguinarine and chelerythrine inhibited the growth of bacterium (Mahady, 2003).  

Abortifacient (f; CEB; DEM); Alterative (f; CRC); Analgesic (f; DEM; APA); Anesthetic (1; CRC); Antibacterial (1; APA); Anticholinesterase (1; HH3); Antiedemic (1; HH3); Antiemetic (f; DEM); Antiinflammatory (1; APA; HH3); Antiplaque (1; PHR; PH2); Antipyretic (f; CRC); Antiseptic (1; APA; CAN; PHR; PH2); Antispasmodic (f; CAN); Antitumor (1; APA; COX; FNF); Aphrodisiac (f; CRC); Arteriosedative (f; CRC); Bradycardic (f; CRC); Cardioactive (f; CAN; DEM; HH3); Cholagogue (1; FEL); COX-2-Inhibitor (1; COX; FNF); Decongestant (f; APA); Depurative (f; DEM); Diaphoretic (f; CEB; CRC); Diuretic (f; CEB; CRC); Emetic (1; APA; CAN; PHR; PH2); Emmenagogue (f; CRC); Escharotic (1; CAN; HOX); Expectorant (f; APA; CAN; HH3; PHR); Laxative (f; CAN; CRC); Narcotic (1; CRC; PHR); Paralytic (1; PHR); Positive Inotropic (1; HH3); Rubefacient (f; CRC); Secretagogue (1; FEL); Sedative (f; CRC); Spasmogenic (1; PHR); Sternutator (f; CRC); Stimulant (f; CRC); Tonic (f; CRC; DEM); Vermifuge (f; CRC; DEM).

Activities documented for bloodroot are principally attributable to the isoquinoline alkaloid constituents, in particular sanguinarine. Interest has focused on the use of sanguinarine in dental hygiene products. Unless otherwise stated, the following actions refer to sanguinarine.

IN VITRO AND ANIMAL STUDIES

Considerable antimicrobial activity has been documented against both Gram-positive and Gram-negative bacteria, Candida and dermatophytes (fungi), and Trichomonas (protozoa).(2) In addition, anti-inflammatory activity has been described against carrageenan-induced rat paw oedema.(3) Prolongation of the ventricular refractory period has been attributed to an inhibition of NaþKþ ATPase.(4, 5) However, a single intravenous injection of sanguinarine to anaesthetised dogs reportedly exerted no effect on cardiovascular parameters monitored.(4) In vitro inhibition of bone resorption and collagenase has been documented.(2)

CLINICAL STUDIES

Many studies have investigated the efficacy of bloodroot extracts in oral hygiene.(2) Preparations containing bloodroot extracts, such as oral rinses and toothpastes, have been reported to significantly lower plaque, gingival and bleeding indices.(2) Alteration of the oral microbial flora, or development of resistant microbial strains has not been observed with the use of bloodroot extracts.(2)

Figure 1.  Bloodroot (Sanguinaria canadensis) Flower (1a) and Root (1b).

PRODUCT AVAILABILITY

Extract, tincture

Plant Part Used: Rhizome

DOSAGES

DOSAGE 

·         Adult PO extract: 0.06-0.3 ml tid (1:1 in 60% alcohol)

·         Adult PO tincture: 0.3-2 ml tid

·         Adult PO rhizome: 60-500 mg tid (Jellin et al, 2008)

DOSAGE

Dosages for oral administration (adults) for traditional uses recommended in older standard herbal reference texts are given

below.

·         Rhizome  0.06–0.5 g (1–2 g for emetic dose) three times daily.(G7)

·         Liquid extract  0.06–0.3 mL (1 : 1 in 60% alcohol) (1–2 mL for emetic dose) three times daily.(G7)

·         Tincture  0.3–2 mL (1 : 5 in 60% alcohol) (2–8mL for emetic dose) three times daily.(G7).

DOSAGE

0.06–0.5 (–2 g for emesis) g rhizome 3 x/day (CAN); 0.06–0.3 ml (–2 ml for emesis) liquid extract (1:1 in 60% alcohol) 3 x/day (CAN); 0.3–2 ml (–8 ml for emesis) tincture (1:5 in 60% alcohol) 3 x/day (CAN); 0.5 g powdered root (PNC); 0.5–1.5 ml liquid root extract (PNC); 2–8 ml root tincture (PNC); 0.3–0.5 g solid root extract (PNC).

INDICATIONS

Adenopathy (1; CRC; FNF); Alcoholism (f; CRC); Alzheimer’s (1; COX; FNF; HH3); Anemia (f; CRC; FEL); Aphonia (f; CRC); Arthrosis (1; APA; COX; CRC); Asthma (f; CAN; CRC; FEL; HH3); Bacteria (1; APA); Bleeding (f; DEM); Blepharosis (f; CRC); Bronchosis (1; CAN; CRC; HH3); Burn (f; CRC; DEM); Cancer (1; APA; COX; HOX); Cancer, breast (1; CRC; JLH); Cancer, ear (1; CRC; JLH); Cancer, nose (1; CRC; JLH); Cancer, skin (1; COX; CRC; JLH); Cancer, uterus (1; CRC; JLH); Candida (f; HH3); Cardiopathy (f; DEM); Catarrh (f; CRC; DEM; FEL); Chest Ache (f; CRC); Childbirth (f; CRC); Chlorosis (f; FEL); Cold (f; APA; CRC; DEM); Congestion (f; APA); Constipation (f; CRC; DEM); Cough (f; APA; CRC; DEM); Cramp (f; CAN; DEM); Croup (1; CAN; CRC; DEM; FEL); Deafness (f; CRC); Dermatosis (f; FEL); Debility (f; DEM; FEL); Diarrhea (f; DEM); Diphtheria (f; CRC); Divination (f; CRC); Duodenosis (f; FEL); Dysentery (1; CRC; FEL; FNF); Dysmenorrhea (f; CRC; DEM; HH3); Dyspepsia (f; CRC; DEM; FEL); Ear (f; CRC); Eczema (f; CRC; FEL); Enterosis (f; DEM); Escherichia (1; HH3); Fever (f; APA; CEB; CRC); Fits (f; DEM); Flu (f; CRC); Flush (f; CRC); Frigidity (f; CRC); Fungus (f; CEB; FEL); Gall (f; DEM); Gas (f; DEM); Gastrosis (f; CRC; FEL); Gleet (f; CRC); Gingivosis (1; APA; PH2); Glossosis (f; CRC); Gonorrhea (f; DEM); Gout (f; CRC); Halitosis (1; APA); Headache (f; CEB; CRC; FEL); Head Cold (f; CEB; DEM); Hemoptysis (f; CRC; DEM); Hemorrhoid (f; CRC; DEM); Hepatosis (f; CRC; DEM); Hysteria (f; FEL); Impotence (f; FEL); Infection (f; HH3); Inflammation (1; APA;

FEL; HH3); Insomnia (f; CRC); Keratosis (f; CRC); Laryngosis (f; CRC; FEL; HH3); Melanoma (1; HOX); Migraine (f; CRC); Mucososis (f; FEL); Mycosis (1; APA; FEL); Nervousness (f; CRC); Neuralgia (f; CRC); Ophthalmia (f; CRC); Pain (1; CRC; DEM; APA); Periodontosis (1; FNF; JAD); Pertussis (f; CEB; CRC; FEL); Pharyngosis (1; CAN; CRC; FNF; HH3); Phthisis (f; FEL); Plaque (1; CRC); Pneumonia (f; CRC; FEL); Polyp (1; CAN; CEB; DEM; HOX); Pulmonosis (f; CEB; DEM); Quinsy (f; CRC); Respirosis (f; CRC); Rheumatism (f; APA; CRC; DEM); Rhinosis (f; CRC; HH3); Ringworm (f; FEL); Salmonella (1; HH3); Scarlatina (f; CRC; FEL); Scrofula (f; FEL); Sore (f; DEM); Sore Throat (1; APA; CRC; FEL); Spermatorrhea (f; FEL); Staphylococcus (1; HH3); Stomachache (f; DEM); Streptococcus (1; HH3); Swelling (1; HH3); Syncope (f; DEM); Syphilis (f; CRC; DEM; FEL); Tinnitus (f; CRC); Toothache (1; CRC); Tracheosis (f; FEL); Tuberculosis (1; CEB; CRC; DEM); Tumor (1; APA; COX; CRC; FNF); Typhoid (f; CRC); Ulcer (f; DEM); Vaginosis (1; CRC; FNF); VD (f; CRC); Vomiting (f; DEM); Water Retention (f; CEB; CRC); Whitlow (f; CRC); Worm (f; CRC; DEM); Wound (f; DEM); Yeast (1; HH3).

CONTRAINDICATIONS/ WARNINGS

CLASS 2B/2D HERB.

Bloodroot should not be used during pregnancy and breastfeeding, and it should not be given to children. Bloodroot should not be used to treat deep wounds. The FDA classifi es this herb as unsafe; therefore this herb should be used only under the supervision of a qualifi ed herbalist. Handling the fresh root without gloves can cause skin irritation.

Drug interactions None documented. However, the potential for preparations of bloodroot to interact with other medicines administered concurrently, particularly those with similar or opposing effects, should be considered.

Pregnancy and lactation There is limited evidence from animal studies that bloodroot is non-toxic during pregnancy (see above). However, in view of its pharmacologically active constituents and lack of clinical data on safety, use of bloodroot during pregnancy and lactation should be avoided.

Figure 2. Bloodroot – dried drug substance (rhizome).

SIDE EFFECTS/ADVERSE REACTIONS, TOXICITY

CNS: Headache, central nervous system depression, loss of consciousness

CV: Hypotension, shock, coma (excessive doses)

EENT: Glaucoma (high-doses)

GI: Nausea, vomiting, anorexia

INTEG: Contact dermatitis (topical)

None documented for bloodroot. Much has been documented concerning the potential toxicity of the alkaloid constituents in bloodroot, in particular of sanguinarine.

Conclusions reached in the 1960s over the carcinogenic potential of sanguinarine have more recently been disproved.(6) In addition, negative mutagenic activity has been observed in the Ames test (microbial, with and without activation).(6)

Sanguinarine is poorly absorbed from the gastrointestinal tract. This is reflected in stated acute oral LD50 values (rat) of 1.7 g/kg (sanguinarine) and 1.4 g/kg (sanguinaria extract), compared with an acute intravenous LD50 (rat) value of 28.7 mg/kg (sanguinarine).( 1) Symptoms of diarrhoea, ataxia and reduced activity were observed in animals receiving high oral doses of sanguinarine.(5) The acute dermal toxicity (LD50) of sanguinarine is stated to be greater than 200 mg/kg in rabbits.(1) The first experimental study of sanguinarine toxicity (1876) reported prostration and severe respiratory distress as the most marked signs of oral toxicity.(1) However, in more recent short-term toxicity studies no toxic signs were observed in the fetuses of rats following maternal administration of 5–30 mg/kg/day of sanguinarine. (1)

The reproductive and developmental toxicity potential of an S. canadensis extract has been evaluated in rats and rabbits.(6) Developmental toxicity (increase in postimplantation loss, slight decrease in fetal and pup body weights) was only evident at maternally toxic doses. No effect was reported on reproductive capabilities, on parturition or on lactation. It was concluded that oral ingestion of sanguinaria extract has no selective effect on fertility, reproduction, or on fetal or neonatal development.(6)

Hepatotoxicity has been documented in rats following a single intraperitoneal administration (10 mg/kg) of sanguinarine.(5) Toxicity was indicated by an increase in serum alanine aminotransferase and serum asparate aminotransferase activity, and by a significant reduction in microsomal cytochrome P450 and benzfetamine N-demethylase activities.(5) Macroscopic lesions were also observed but the authors stated that the two events could not be conclusively directly related.(5) No hepatotoxicity has been observed in short-term toxicity studies involving oral administration of sanguinarine.(1)

Animal studies have indicated sanguinarine to be non-irritant and to exhibit no allergenic or anaphylactic potential.(4) Human patch tests have shown sanguinarine to be non-irritant and nonsensitising.(4).

INTERACTIONS

Drug

Antihypertensives, ganglionic/peripheral adrenergic blockers: Bloodroot may increase the effects of these products.

CNS depressants: Bloodroot may increase the sedative effect of CNS depressants.

Corticosteroids: Bloodroot may increase potassium loss.

CLIENT CONSIDERATIONS

Assess

·         Assess the client’s cardiovascular status (blood pressure; pulse, including character) and level of consciousness. Hypotension, shock, and coma may occur with increased doses.

·         Determine the quantity of the herb ingested. 

Administer

·         Caution the client to take only carefully calculated doses of bloodroot. Higher doses can lead to coma.

·         Caution the client to not take orally the juice or powdered rhizome of bloodroot; may cause toxicity.

Teach Client/Family

·         Caution the client not to use bloodroot in children or those who are pregnant or breastfeeding until more research is available.

·         Caution the client to use bloodroot only under the direction of a competent herbalist. Bloodroot is considered unsafe by the FDA.

PREPARATIONS

PROPRIETARY MULTI-INGREDIENT PREPARATIONS

Australia: Lexat. Canada: Mielocol; Viadent; Wampole Bronchial Cough Syrup. Italy: Dentosan Carie & Alito.

REFERENCE 

Barnes, J., Anderson, LA, dan Phillipson, JD 2007.  Obat Herbal Edisi Ketiga. Pers Farmasi. Auckland dan London.

Duke, JA dengan Mary Jo Bogenschutz-Godwin, Judi duCellier, Peggy-Ann K. Duke. 2002.  Buku Pegangan Obat Herbal 2nd Ed . CRC Press LLC. AMERIKA SERIKAT.

Linda S-Roth. 2010.  Mosby's Handbook Of Herbal & Suplemen Alami, Edisi Keempat . Mosby Elsevier. AMERIKA SERIKAT.