grindeliae robustae herba medicinal revaluation
TRANSCRIPT
GRINDELIAE ROBUSTAE HERBA MEDICINAL REVALUATION by Rulph Holt Cheney, S c D .
Projessor of Biology, Brooklyn College; Brooklyn College of Phurmucy ; nnd Honorary Associute, Brooklyn Botanic Gulden
The genus GRINDELZA I), a shrub of the Composite family, has served in the United States as a source of therapeutic agents since the attention of the Jesuit Fathers, in their Mission Stations along the coast of California, was called to its utilization by the Indian natives before the conquest of the country by white men. It was introduced into the general practice of Medicine in that area in 1875. To-day, it is still employed by local populations. During the last century the medical profession prescribed it both externally in dermatitis conditions; and, internally for disfunctions of an asthmatic nature. In 1880, it was introduced into the U.S. Pharmacopoeia and was prescribed in America and Europe. It continued to be an official drug in this listing until 1926. In that year, it was introduced as an official drug in the U.S. National Formulary and was so recognized through the U.S.N.F. ed. 10 (1955) but was deleted in ed. 11 (1960). This discontinuance of its official standing in American medicine, after a century of recognition, makes it imperative to determine promptly, with the advantages of modern research methods, the true merits and accurate potentialities of this drug for the specific and general conditions for which it has been employed. Otherwise, a drug of benefit to human welfare may be overlooked. At present, Grzndelza extracts are obtained from air-dried buds; flowering heads, and leaves of this shrub are used primarily and regularly only as a self-treatment medicine by rural populations. Currently, advances in the knowledge of the chemistry of this genus, and the individual physiologic effects of several of the principles involved, justify a revaluation of its medicinal value. The persistent belief in the efficacy of the teas and tinctures prepared from various species of Grindelin causes the writer to suggest that the constituents should be re-studied with the modern research facilities in pharmacology; and, be
iven a re-investigation by physicians to determine the true praLtica1 value g y patient testing under controlled conditions of experimentation There are 35 species of Grindelia, all of which are perennial shrubs and are indigenous to North and South America. One of tlle species most commonly used for medicinal purposes, is Grindeliu CamPorum 2 , Greene 3 ) , formerly referred to botanically as G. robustu 4, Nuttall Thus the drug is still known in pharmaceutical commerce as Grindeli& robzLst& Herbu or simply as Grindelin (U.S.P. X, 1955). This species grows mostly on the plains of western North America, especially in California and in Mexico. In both areas
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Griizdelia robusta Nutt., flowering tops are used to prepare a tea for internal consumption as an alterative and externally as a wash for poison oak (Rhus diz)evsiloba Torrey & Gray) and as a remedy for poison ivy (Rhus toxico- detzdrou L) . The leaf tea is reported enthusiastically, by Indians, Spanish- Mexicans, and rural white populations of California, to be helpful in alleviating the discomfort of inflammatory arthritis. The leaves of the shrubs are broad, coarsely-toothed, and possess a clasping base. The flowers grow in solitary yellow heads with discs of the same colour. The distinctive feature of the genus Girzdelia is the limb of the calyx which is composed of 2 to 8 rigid, narrow awns. Some species of this shrub sometimes reach a height of one meter. A stickv, milk-white exudation (turning brown when dry) appears on the reflexed parts of the involucres early in the growth of the plant. It is also found abundantly later in the leaves. Grindelia robustn Nutt. and several other species are known by the common names of Gum Plant, Gum Weed, Rosin Weed, and less commonly as Tar Weed, Wild Sunflower; and, in the Spanish language in Mexico as Grindella. The crude drug, as it appears on the market, consists of the dried leaves and flowering tops collected during, or just prior to, the height of the flowering season which in most areas is in June although in Montana it is August. The actual gathering period depends upon the time when the flowering tops and leaves are covered with the resinous exudate. The commercial drug, Grindelin, has a balsamic odour, and an aromatic, bitter and resinous taste. By chemical analysis, this material contains a mixture of amorphous resins - sometimes as much as 2 1 % - which are freely soluble in alcohol and ether; an oleoresin; and acid-gum; saponin; tannin (1.5 %) ; robustic acid; levulose; a wax; an alkaloid grindeline; and a glucoside. Such a diversification in chemical composition gives it considerable potentiality as a source of chemo- therapeutic agents. More is known about the glucoside, grindelol, than about the alkaloid, grindeline. Grindelol composition has been reported by Power and Rogerson as C2:;H::s0, (c-72.97 %; H-10.12 %) possessing a molecular weight 378.53 and a melting point 256-7". Later, Power and Salway revised the formula to C:;,;H5,j0,j and state that it is a phytosterol glucoside and is isomeric with Anonol which according to Callan and Tutin is a phytosterol obtained from the fruit of the tropical Sour Sap, Anofza nzwicata L The crvstals melt at 257" and are insoluble in water but soluble in pyridine, C5H5N. Further chemical studies should be made. The chief medicinal use has been externally for burns and poison ivy; and, internally for asthma and bronchitis. The average dose of the aqueous extract is 0.2 to 0.6 gms ( 3 to 10 grains) ; or, of the fluid extract 1 to 4 ml. (15 to 60 minims). In addition to the home-brewed teas and tinctures by rural popul-
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ations, the following preparations have been employed in some local American and European therapy : 1. Extractum Grindeliz fluidum .............................................................................. 2 grams.
Extractum Glycvrrhizz (Syn. Liquiritiz) ............................................... 4 grams. Mucilage (aqueous gum constituents) up to 30 grams.
2. Extractum Grindeliz fluidum or tinct 10-20 drops or not more than 2 grams.
3. Powdered herb 2 grams 3 times daily. 4. Infusion 10 grams in 500 ml water within 24 hours. 5. For asthma in children, Decaux recommends tlie following potion to be
administered in teaspoonful doses during 48 hours: Extractum Grindeliz fluidum .............................................................................. 1 gram. Tinctura Lobeliz inflatz . . . . . . 2 grams. Alcoholic extract of Ane ...................................................... 2 grams. Syrup of Flores Aurantii .................................................................................. 40 grams. Aqua Tiliz officinalis 60 grams.
Obviouslv, a standardization of both the preparation and the dosage needs to be accomplished. The most commonly recommended preparation was the fluid extract. This galenical is made by percolating 100 parts of the powdered drug with 60 "/. alcohol until the material is exhausted, then removing the alcohol by distillation, dissolving the residue in 50 parts of distilled water containing 10 parts of sodium bicarbonate to neutralize the acid resin, adding sufficient water to the mixture to make 75 parts and finally diluting it with 90 "/. alcohol to make 100 parts by volume. If this preparation is intended to be used in warm climates, the proportion of alcohol should be increased to one-fourth bv weight of the finished product in order to inhibit fermentation. The fluid extract is prescribed in mixtures containing one-sixteenth their volume of mucilage of acacia to prevent the separation of resinous substances. The nauseous taste may be disguised with spirit of chloroform or fluid extract of licorice. Griizdelin fluid extract should always be kept in tight, light-resistant containers and exposure to direct sunlight or excessive heat should be avoided. The drug has expectorant and relaxing properties and is employed most advantageously in cases of asthma, hay fever, chronic bronchitis, stridulous laryngitis, whooping cough, pulmonary emphysema, and the cough accom- plishing pulmonary tuberculosis. It reduces the violence and frequency of paroxysms and is recommended in local areas for aged persons suffering from these diseases. Claims have been made for permanent control of these conditions, especially for asthmatic breathing, when given with regular frequency and in rather large doses. The action is tonic, stimulating expectorant, sedative antispasmodic, stomachic; and, because it is an effective diuretic: the drug
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is employed also with some success in kidney and bladder diseases including chronic cystitis and enlarged spleen. In addition to Grindelid robustu Nuttall, other species are the source of this medicinal material as their chemical composition varies primarily only in the proportion of the compounds. Grindelid hunzilis Hooker &: Arnott and G. cufzeifolia Nuttall are used as substitutes for G. robzista Nuttall. G. .rqz~ui~ro.ra G , (Pursh) 7 , Dunal is known as Curly-cup Gumweed in Western North America and on the Prairies from Saskatchewan to Mexico. This species possessing spatulate leaves, non-toothed achenes and only 3 or 3 pappus awns, grows along the relatively dry river banks in Illinois and Minnesota. This and some other species of the same genus are said to have a more powerful action on the spleen than any other Grirzdelia species. These species are used also in rheumatism and as a substitute for G. robzista Nuttall for its several purposes. All GriTzdelia species have a reputation as a remedy in the treatment of dermatitis caused by poison ivy (Xh2i.r toxicodendron L. j . During a three months trip of 12,000 miles throughout Western United States, the writer observed the natives of Indian Peublo villages and also the rural white population commonly employing the tea made from the buds and young flower-heads, especially of Grirzdelia cumifolia Nutt., as a wash for Rhzis poisoning. This tea was consumed orally for asthma and other bronchial disorders and pulmonary affections. The desirability of a revaluation of the chemotherapeutic actualities of Grindelin by properly qualified medical scientists seems to be clearlv indicated.
I ) Named for Prof. David Hieronymous Grindel, 1776-1836, Russian botanist. 2, from Greek campus = field; growing in fields or meadows. 3, L. E. Greene, a North American botanist 1842-1915. ") from Latin robur = strong, big, gigantic. ') Th. Nuttall, a North American botanist, 1786-1859. O ) from Greek eschara = rough, scurfy. ") Fr. Tr. Pursh, a German botanist in Canada, 1774-1820.
B I B L I O G R A P H Y :
Allport, N. L. - Chemistry and Pharmacy of vegetable drugs, London, 1943. Bertotto, F. - Flora Medicinal, Buenos Aires, 1949. Callan, T. and Tutin, F. - Pharm. Journ., vol. 87: 743-745, 1911.
Decaux, F. - Formulaire de PhytothCrapie, Paris, 1956. Erganzungsbuch zum Deutschen Arzneibuch (Erg. B. 6 ) , Stuttgart, 1953. Gathercoal, E. N. and Wirth, E. H. - Pharmacognosy, ed. 2, pages 630-632, 1947, USA. Konig, J. K. - Warcnlexikon, Braunschweig, 1920. Leyel, C. F. - Hearts-Ease, London, 1948. Leyel, C. F. - Compassionate Herbs, London, 1946. Lloyd, J. U. - Origin and History of Pharmacopcial vegetable drugs, Cincinnati, Ohio, U.S.A. 1929. Merck Index, ed. 6, Rahway, New Jersey, U.S.A. 1952. Nelson, A. - Medical Botany, Edinburgh, 1951. Potter's Cyclopaedia of botanical drugs and preparations, London, 1941.
Chemical examination of leaves of Anona muricatn L.
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Power, F. B. and Tutin, F. - The chemical examination of Grindelia. Par t 11, Proc. Amer. Pharmaccut.
Power, F. B. and Rogerson, H. - Chemical examination of Jalap. Journ. Amer. Chem. Soc., vol. 32:
Power, F. B. and Salway, A. H. - Identification of Ipuranol and some Allied Compounds as Phytostcrol
Stuhr, E. T. - Manual of Pacific Coast Drug Plants. Philadelphia, Pa., U.S.A., 1933. Steinmetz, E. F. - Codex Vegetabilis, Amsterdam, 1959. Steinmetz, E. F. - Drug Guide, Amsterdam, 1959. United States Pharmacopeia, ed. 9, 1916. United States National Formulary, ed. 10, 1955. Youngken, H. W. - Textbook of Pharmaceutical Botany, ed. 6, Phil., Pa., U.S.A., 1938. Youngken, H. W. - Textbook of Pharmacognosy, ed. 5, Philadelphia, Pa., U.S.A., 1943.
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U beys etziiizg GRINDELIAE ROBUSTAE HERBA - eine Rehabilitierung
Die Gattung GRZNDELZA I ) , ein Strauch aus der Familie der Korbblutler, ist in den Vereinigten Staaten von Nordamerika als Ausgangsmaterial fur medizinische Zubereitungen schon seit den Zeiten verwendet worden, als die Jesuiten auf ihren Stationen in Kalifornien sich fur diese Pflanze zu interessieren begannen. Sie folgten darin den indianischen Eingeborenen, die die Pflanze schon lange vor den ersten Einwanderern verwendeten. Die Pflanze wurde um 1875 in die allgemeine medizinische Praxis eingefuhrt. Heutzutage wird sie noch als Volksmedizin verwendet. Wahrend des vergangenen Jahr- hunderts verschrieb die medizinische Wissenschaft sie sowohl ausserlich gegen Hautkrankheiten als auch innerlich gegen asthmatische Beschwerden. 1880 wurde die Pflanze in die U.S. Pharmakopoe aufgenommen und in Amerika und Europa verschrieben; sie blieb offizinell bis 1926; in diesem Jahre wurde sie als anerkannte Droge in die U.S. National Formulary aufgenommen und blieb als solche anerkannt bis zur U.S.N.F. ed. 10 (1955), aber in der ed. 11 ( 1960) gestrichen. Die Streichung nach einem Jahrhundert offizineller An- erkennung in Amerika macht es notwendig mit modernen Untersuchungs- methoden den wahren Wert und die genauen Heilkrafte der Droge fur spezifische und allgemeine Zwecke, fur die sie verwendet wurde, festzustellen. Sonst konnte eine fur die Menschheit wertvolle Droge in Vergessenheit gera ten. Heutzutage werden Gritzdelin Extrakte aus luft-getrockneten Knospen her- gestellt ; Bluten und Blatter des Strauches werden vorwiegend und regelmassig nur als Hausmittel von der Landbevolkerung verwendet. Offenbar recht- fertigen die Fortschritte in der Kenntnis der Chemie dieser Gattung und der einzelnen physiologischen Wirkungen ihrer verschiedenen Bestandteile eine Rehabilitierung des medizinischen Wertes. Der beharrliche Glaube an der
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