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AGATHOSMA BETULINA HERBA - PlantZAfrica

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<strong>AGATHOSMA</strong> <strong>BETULINA</strong> <strong>HERBA</strong><br />

Definition<br />

Agathosma Betulina Herba consists of the<br />

fresh or dried leaves and smaller stalks of<br />

Agathosma betulina (Berg.) Pillans<br />

(Rutaceae).<br />

Synonyms<br />

Barosma betulina Bartl. and Wendl. f.<br />

Hartogia betulina Berg.<br />

Vernacular names<br />

Figure 1a: Live plant<br />

boegoe, bergboegoe (A), buchu (San);<br />

round leaf buchu<br />

Description<br />

Macroscopical 1, 2<br />

Evergreen, multi-stemmed, perennial<br />

resprouting woody shrub to 1m in height,<br />

with glabrous yellow to red-brown stems;<br />

leaves alternate to opposite, 14-25 × 6-<br />

14mm, broadly elliptic to nearly round<br />

(average length:breadth ratio 1.95), with<br />

rounded and recurved apex; glabrous with<br />

prominent main and subsidiary veins on<br />

abaxial surface; gland dotted on underside;<br />

margin serrate with an oil gland at the base<br />

of each serration; flowers (June-Nov)<br />

axillary, usually solitary, up to 20mm in<br />

diameter, white to pale purple-pink, borne on<br />

slender stalks ±7mm long.<br />

Figure 1b: Dried leaf<br />

Figure 2: line drawing<br />

1 Pillans, N. (1950). A revision of the genus<br />

Agathosma (Rutaceae). Journal of South African<br />

Botany 16: 55-117.<br />

2 Spreeth, A.D. (1976). ʼn Hersiening van die<br />

Agathosma-species van kommersiële belang (A<br />

revision of the commercially important<br />

Agathosma species). Journal of South African<br />

Botany 42(2): 109-119.


Microscopical 3<br />

Crude drug<br />

Collected as required or available in the<br />

marketplace as bundles of leafy twigs with<br />

light yellow-green, highly aromatic foliage;<br />

texture soft when fresh, leathery when dry;<br />

occasional flowers may be present. BPC<br />

quality buchu leaf is freely available in<br />

pharmacies in South Africa and<br />

unstandardised leaf in supermarkets.<br />

Geographical distribution<br />

Sandy mountain slopes of the Western<br />

Cape Province, in the Calvinia, Cedarberg,<br />

Tulbagh, Ceres and Piketberg districts, at<br />

altitudes of 300-700m above sea level.<br />

Figure 3: microscopical features<br />

1. Cells of the upper leaf epidermis<br />

2. Cells of the lower leaf epidermis with<br />

anomocytic stomata<br />

3. Cells of upper leaf epidermis in sectional view<br />

showing unicellular warty clothing hair<br />

4. Cells of lower leaf epidermis with clothing hair<br />

5. Cells of upper leaf epidermis (sectional view)<br />

containing sphaerocrystalline masses of<br />

diosmin<br />

6. Cells of the petiole<br />

7. Cells of the mesophyll containing cluster<br />

crystals (rosette aggregates) of calcium<br />

oxalate<br />

Characteristic features are: the polygonal<br />

cells of the upper leaf epidermis with slightly<br />

thickened walls, some containing<br />

sphaerocrystalline pale yellow masses of<br />

diosmin; the smaller thin-walled polygonal<br />

cells of the lower leaf epidermis; the<br />

numerous anomocytic stomata of the lower<br />

leaf surface only; occasional unicellular<br />

warty covering trichomes of leaf and petiole,<br />

each up to 300µ in length; the cells of the<br />

leaf mesophyll containing calcium oxalate<br />

cluster crystals, each up to 80µ in diameter;<br />

the spherical schizo-lysigenous oil glands of<br />

the mesophyll containing oil droplets<br />

staining red with Soudan IV solution; the<br />

fibres accompanying the leaf midrib and<br />

main veins.<br />

Figure 4: distribution map<br />

Quality standards<br />

Identity tests<br />

Thin layer chromatography on silica gel<br />

using as solvent a mixture of toluene:diethyl<br />

ether:1.75M acetic acid (1:1:1). Reference<br />

compound cineole (0, 1% in chloroform).<br />

Method according to Appendix 2a.<br />

Note The methods used for thin layer<br />

chromatography and HPLC gave poor<br />

results for this species. Further work is<br />

required.<br />

HPLC on C 18 column, method according to<br />

Appendix 2b.<br />

Water-soluble extractive value: not less than<br />

14% 3<br />

Volatile oil content: not less than 1.3% 3; not<br />

less than 1.8% 4<br />

3 British Herbal Medicine Association (1996).<br />

Buchu. pp. 46-47 in: British Herbal<br />

Pharmacopoeia, Biddles Ltd., King’s Lynn.<br />

4 British Pharmaceutical Codex (1963).<br />

Pharmaceutical Society of Great Britain, Lund<br />

Humphries, London.


Stems: not more than 5% 3, 4<br />

Total ash: not more than 5% 3, 4<br />

Purity tests<br />

Assay<br />

None available. Assay methods for buchu oil<br />

have been published. 5-7<br />

Major chemical constituents<br />

Apart from the common flavonoids rutin and<br />

diosmin, the foliage of A. betulina contains<br />

1.5-2.5% 3, 4 of an essential oil of which the<br />

main constituents are<br />

menthone/isomenthone (29.83-60.0%), (ψ)-<br />

diosphenol/diosphenol (9.46-40.88%),<br />

limonene (11.6-17.0%),<br />

pulegone/isopulegone (7.0-34.1%) and both<br />

cis- and trans-8-mercapto-p-menthane-3-<br />

ones (±3%) 5, 6,<br />

7 . The latter are said to<br />

contribute most to the characteristic odour of<br />

the oil, reminiscent of blackcurrants (see d<br />

below).<br />

Figure 7: chemical constituents<br />

Dosage forms<br />

In traditional practice, A. betulina is most<br />

commonly taken orally in the form of an<br />

aqueous infusion, sometimes sweetened<br />

with brown sugar, or as a tincture in brandy.<br />

Other dosage forms include a vinegar<br />

infusion, for external application as an<br />

GR1, 11 and 21-<br />

antiseptic wash or embrocation.<br />

24<br />

5 Kaiser, R., Lamparsky, D. and Schudel, P.<br />

(1975). Analysis of buchu leaf oil. Journal of<br />

Agricultural and Food Chemistry 23(5): 943-<br />

950.<br />

6<br />

Blommaert, K.L.J. and Bartel, E. (1976).<br />

Chemotaxonomic aapects of the buchu series<br />

Agathosma betulina Pillans and A. crenulata<br />

Pillans from local plantings. Journal of South<br />

African Botany 42(2): 121-126.<br />

7 Posthumus, M.A. van Beek, T.A., Collins, N.F.<br />

and Graven, E.H. (1996). Chemical composition<br />

of the essential oils of Agathosma betulina, A.<br />

crenulata and an A. betulina × crenulata hybrid<br />

(Buchu). Journal of Essential Oil Research 8:<br />

223-228.<br />

Buchu was introduced into Britain in 1790<br />

and in 1821 included in the British<br />

Pharmacopoeia (BP); later also in the British<br />

Pharmaceutical Codex (BPC). It remained<br />

an official remedy until 1963; dosage forms<br />

included a concentrated infusion (BPC<br />

1954) and a tincture (BPC 1949). Various<br />

mixtures were listed in formularies current at<br />

the time e.g. Mistura Buchu et Hyoscyamus<br />

(British National Formulary 1939) and<br />

Compound Buchu Mixture (Chelsea Hospital<br />

for Women).<br />

In Europe, a number of patent remedies<br />

containing buchu e.g. teas, dragees and<br />

drops are available for self medication GR8 .<br />

Medicinal uses


Buchu, originally a highly prized San and<br />

Khoi-khoi traditional remedy, has remained<br />

one of the most popular herbal medicines in<br />

South Africa. Its traditional use<br />

encompasses the treatment of kidney and<br />

urinary tract infections, colds, stomach<br />

ailments, rheumatism, gout and fever.<br />

Externally it is applied as an antiseptic wash<br />

to infected wounds and as a compress to<br />

GR1, 11<br />

relieve swelling, bruising and sprains<br />

and 19-24 . Combinations of buchu with wilde<br />

als (Artemisia afra) or wilde knoffel<br />

(Tulbaghia spp.) are commonly taken for<br />

colds and influenza or as a general tonic.<br />

Buchu was described in the BP and BPC as<br />

a weak diuretic and urinary tract antiseptic<br />

for the treatment of urethritis, cystitis and<br />

prostatitis. These are its recommended uses<br />

in Europe at the present time 8, 9 GR 6, 7, 8,<br />

and<br />

10.<br />

Pharmacology/bioactivity<br />

In vitro tests of both aqueous/alcoholic<br />

extracts and of volatile oil demonstrated little<br />

antimicrobial activity against common<br />

urinary tract pathogens GR7 . A more recent<br />

study showed the essential oil (10µl/well) to<br />

possess weak antimicrobial activity against<br />

Escherichia coli, Staphylococcus aureus and<br />

Saccharomyces cerevisiae but none against<br />

Enterococcus hirae and Pseudomonas<br />

aeruginosa 10 . In the same study, initial<br />

smooth muscle spasmogenic activity<br />

(guinea pig ileum), followed by spasmolysis,<br />

was demonstrated for the essential oil<br />

(concentration range 4×10 -6 to 8 ×10 -5 v/v in<br />

methanol). Spasmolytic action was dose<br />

related, with an IC50 of 8×10 -6 .<br />

In an in vitro assay, aqueous leaf extracts<br />

showed no antiviral activity (cell culture)<br />

against Herpes Virus Type 2, Influenza Virus<br />

8 Pharmacopée Française, Xe édition (1983). See<br />

also Bulletin Officiel No. 90/22 bis: Buchu,<br />

feuille<br />

9 German Kommission E monograph (published<br />

1/2/1990): Barosmae folium (Buccoblätter)<br />

10 Lis-Balchin, M. and Simpson, S.H. (2001).<br />

Buchu (Agathosma betulina and A. crenulata,<br />

Rutaceae) essential oils: their pharmacological<br />

action on guinea pig ileum and antimicrobial<br />

activity on micro-organisms. Journal of<br />

Pharmacy and Pharmacology 53(4):579-582.<br />

A2 (Manheim 57), Poliovirus II or Vaccinia<br />

Virus 11 . In this study no cytotoxic activity<br />

aginst HeLa cells was shown. Antimutagenic<br />

activity of an aqueous leaf infusion was<br />

assessed in vitro (Salmonella typhimurum<br />

TA 98 and TA 100) against ethyl<br />

methanesulphonate- and amino anthraceneinduced<br />

mutagenicity, but no activity could<br />

be demonstrated 12 . In vivo anti-inflammatory<br />

activity has been demonstrated for diosmin<br />

(isolated from the overground parts of the<br />

plant), which reduced carrageenan-induced<br />

rat paw oedema at a dose of 600mg/kg body<br />

weight. Other animal studies appear to be<br />

lacking.<br />

Contraindications<br />

Owing to the variable composition of buchu<br />

essential oil, particularly in respect of<br />

pulegone levels (see 9.0 above), the use of<br />

buchu preparations during pregnancy and<br />

lactation is contraindicated.<br />

Adverse reactions<br />

Traditional practitioners report gastrointestinal<br />

irritation as a possible side effect<br />

of oral use. Buchu preparations should<br />

therefore be used with caution by patients<br />

suffering from kidney infections,<br />

haemorrhoids or irritable bowel syndrome.<br />

See also GR 6-8.<br />

Precautions<br />

Prolonged or excessive use of this herb is<br />

not advisable.<br />

Dosage<br />

Dried leaf: 1-2 g (± 1-2 teaspoonsful<br />

powdered leaf) by infusion, three times daily.<br />

An infusion may be prepared by adding<br />

600ml of boiling water to 30g of powdered<br />

11 May, G. and Willuhn, G. (1978). Antiviral<br />

activity of aqueous extracts from medicinal<br />

plants in tissue cultures. Arzneimittel-Forschung.<br />

28(1): 1-7.<br />

12 Badria, F. A. (1994). Is man helpless against<br />

cancer? An environmental approach:<br />

antimutagenic agents from Egyptian food and<br />

medicinal preparations. Cancer Letters 84 (1): 1-<br />

5.


drug and allowing to stand in a covered<br />

vessel for 30 minutes. The resultant infusion<br />

is strained and stored in the refrigerator; to<br />

be taken in 30-60ml (2-4 tablespoonsful)<br />

doses, three times daily, diluted with plenty<br />

of water.<br />

Concentrated Buchu Infusion BPC 1954<br />

(1:2.5 prepared by percolation with 25%<br />

ethanol): 4-8ml<br />

Liquid extract (1:1 in 90% ethanol ): 0.3-1.2<br />

ml<br />

Buchu Tincture BPC 1949 (1:5 prepared<br />

by percolation in 60% ethanol): 2-4ml<br />

Food use<br />

Buchu oil has been approved in the USA as<br />

a food flavouring agent, at concentrations of<br />

up to about 0.002% (15.4 ppm). The oil is<br />

also listed by the Council of Europe as a<br />

natural source of food flavouring (category<br />

N3) GR17<br />

Copyright in this monograph resides with the authors, the South<br />

African National Biodiversity Institute, the South African Medical<br />

Research Council and the University of the Western Cape. It may<br />

not be reproduced in whole or in part without the written consent of<br />

the copyright holders.

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