Bloodroot
B
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.
Species (Family)
Sanguinaria canadensis L. (Papaveraceae)
Synonym(s)
Red Indian Paint, Red Root, Sanguinaria, S. australis Greene, S. canadensis var. rotundifolia (Greene) Fedde, S. dilleniana Greene, Tetterwort
Part(s) Used
Rhizome
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).
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)
Figure 1 Selected constituents of bloodroot. |
Figure 2 Bloodroot (Sanguinaria canadensis). |
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Figure 3 Bloodroot – dried drug substance (rhizome).
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) (2–8 mL for emetic dose) three times daily.(G7)
Pharmacological Actions
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)
Bloodroot |
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Side-Effects, Toxicity
None documented for bloodroot. Much has been documented |
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concerning the potential toxicity of the alkaloid constituents in |
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bloodroot, in particular of sanguinarine. |
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Conclusions reached in the 1960s over the carcinogenic |
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potential of sanguinarine have more recently been disproved.(6) |
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In addition, negative mutagenic activity has been observed in the |
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Ames test (microbial, with and without activation).(6) |
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Sanguinarine is poorly absorbed from the gastrointestinal tract. |
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This is reflected in stated acute oral LD50 values (rat) of 1.7 g/kg |
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(sanguinarine) and 1.4 g/kg (sanguinaria extract), compared with |
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an acute intravenous LD50 (rat) value of 28.7 mg/kg (sanguinar- |
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ine).(1) Symptoms of diarrhoea, ataxia and reduced activity were |
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observed in animals receiving high oral doses of sanguinarine.(5) |
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The acute dermal toxicity (LD50) of sanguinarine is stated to be |
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greater than 200 mg/kg in rabbits.(1) The first experimental study |
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of sanguinarine toxicity (1876) reported prostration and severe |
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respiratory distress as the most marked signs of oral toxicity.(1) |
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However, in more recent short-term toxicity studies no toxic signs |
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were observed in the fetuses of rats following maternal |
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administration of 5–30 mg/kg/day of sanguinarine. (1) |
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The reproductive and developmental toxicity potential of an S. |
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canadensis extract has been evaluated in rats and rabbits.(6) |
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Developmental toxicity (increase in postimplantation loss, slight |
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decrease in fetal and pup body weights) was only evident at |
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maternally toxic doses. No effect was reported on reproductive |
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capabilities, on parturition or on lactation. It was concluded that |
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oral ingestion of sanguinaria extract has no selective effect on |
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fertility, reproduction, or on fetal or neonatal development.(6) |
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Hepatotoxicity has been documented in rats following a single |
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intraperitoneal administration (10 mg/kg) |
of sanguinarine.(5) |
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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)
Contra-indications, Warnings
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.
Preparations
Proprietary multi-ingredient preparations
Australia: Lexat. Canada: Mielocol; Viadent; Wampole Bronchial Cough Syrup. Italy: Dentosan Carie & Alito.
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Bloodroot |
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References |
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benzophenanthridine alkaloids from Chelidonium majus. Planta Med |
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1981; 43: 161–165. |
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Becci PJ et al. Short-term toxicity studies of sanguinarine and of two |
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Schwartz HG. Safety profile of sanguinarine and sanguinaria extract. |
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alkaloid extracts of Sanguinaria canadensis. J Toxicol Environ Health |
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Compend Cont Educ Dent Suppl 1986; 7: S212–S217. |
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1987; 20: 199–208. |
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Dalvi RR. Sanguinarine: its potential as a liver toxic alkaloid present |
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Godowski KC. Antimicrobial action of sanguinarine. J Clin Dent |
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in the seeds of Argemone mexicana. Experientia 1985; 41: 77–78. |
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1989; 1: 96–101. |
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Keller KA. Reproductive and developmental toxicological evaluation |
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Lenfield J et al. Antiinflammatory activity of quaternary |
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of Sanguinaria extract. J Clin Dent 1989; 1: 59–66. |
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Blue Flag
Summary and Pharmaceutical Comment
Little is known about the phytochemical, pharmacological or toxicological properties of blue flag and its constituents, although related species are known to be toxic. In view of these factors, the use of blue flag is not recommended.
Species (Family)
Iris versicolor L.
Synonym(s)
Iris caroliniana Watson, Iris virginica L.
Part(s) Used
Rhizome
Pharmacopoeial and Other Monographs
BHC 1992(G6)
BHP 1996(G9)
Martindale 35th edition(G85)
Legal Category (Licensed Products)
GSL(G37)
Constituents
The following is compiled from several sources, including General References G22, G40, G48 and G64.
Acids Isophthalic acid 0.002%, salicylic acid, lauric acid, stearic acid, palmitic acid and 1-triacontanol.
Volatile oils 0.025%. Furfural.
Other constituents Iridin, b-sitosterol, iriversical(1) and tannin.
Food Use
Blue flag is not used in foods.
Herbal Use
Blue flag is stated to possess cholagogue, laxative, diuretic, dermatological, anti-inflammatory and antiemetic properties. It has been used for skin diseases, biliousness with constipation and liver dysfunction, and specifically for cutaneous eruptions.(G7, G64)
Figure 1 Selected constituents of blue flag.
B
Dosage
Dosages for oral administration (adults) for traditional uses recommended in older standard herbal and pharmaceutical reference texts are given below.
Dried rhizome 0.6–2.0 g as a decoction three times daily.(G6, G7,
G10)
Liquid extract 1–2 mL (1 : 1 in 45% alcohol) three times
daily.(G6, G7, G10)
Pharmacological Actions
None documented.
Side-effects, Toxicity
It has been stated that the fresh root of blue flag can cause nausea and vomiting.(G42) Therefore, dosage recommendations relate to small doses of dried root.
Furfural, a volatile oil constituent, is known to be irritant to mucous membranes causing lachrymation, inflammation of the
Figure 2 Blue flag (Iris versicolor).
Figure 3 Blue flag – dried drug substance (rhizome).
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88 Blue Flag
eyes, irritation of the throat, and headache.(G48) Whether these irritant properties are attributable to the volatile oil of blue flag has not been established. Acute oral toxicity (rat, LD50) for
Bfurfural has been documented as 127 mg/kg body weight.(G48) Iridin has been reported to be poisonous in both humans and livestock.(G22) However, it is unclear whether this substance is the same iridin documented as a constituent of blue flag.
Contra-indications, Warnings
In view of the possible irritant nature of the volatile oil, blue flag may not be suitable for internal use.
Drug interactions None documented.
Pregnancy and lactation The safety of blue flag has not been established. In view of this, together with the documented irritant
properties of some of the constituents, blue flag should not be taken during pregnancy.
Preparations
Proprietary multi-ingredient preparations
UK: Catarrh Mixture; HRI Clear Complexion; Napiers Skin Tablets; Skin Eruptions Mixture.
References
1Krick W et al. Isolation and structural determination of a new methylated triterpenoid from rhizomes of Iris versicolor L. Z Naturforsch 1983; 38: 689–692.