L The whole plant is used to stupefy fish, and the leaves and latex are used in Ghana and Liberia for the treatment of rickets, diarrhoea and skin lesions (Githens, 1949; Oliver, 1960).
C Reichstein and co-workers isolated in 1954 a series of digitalis heterosides from the fresh wood of this species and identified several aglycones including strophanthidin, strophanthidol and nigrescigenin. Later they also isolated, inter alia, 6-dehydroxy-strophanthidin, strophanthigenin and convallotoxin (Mauli and Tamm, 1957; Patel and Rowson, 1964; Berthold et al., 1965).
Calocin, a pregnane glycoside has been reported in this species by Sravasta et al. (1982).
The barks of the related Periploca graeca and of P. aphylla (not found in West Africa) yield the glycosides periplocin and periplocymarin of the digitalin group (Paris and Moyse, 1971, p. 97).
P In the USSR periplocin and periplocymarin are used as cardiotonics and diuretics and are said to be better suited for slow intravenous injection than strophanthin (in the Russian Pharmacopoeia the active dose is stated as 0.02-0.05 mg) (see also Martindale, 1969).
Cryptostegia grandiflora (Roxb.) R.Br. ex. Lindley (Fig. 2.3) PERIPLOCACEAE
L The latex of this widely cultivated ornamental shrub has been used as a source of rubber, and has been considered to be oncolytic (Chopra et al., 1956; Paris and Moyse, 1971).
C In earlier investigations leaves and stems were found to contain two cardenolides, cryptograndoside A and B, which are glycosides of oleandrogenin with sarmentose and glucose, respectively, and thus are similar to hongheloside A (Aebi and Reichstein, 1950; Mcllroy, 1950; Abisch and Reichstein, 1962b). In 1972 five cardenolides were isolated and identified as oleandrogenin, gitoxigenin, rhodexin B, 16-propionylgitoxigenin and a new natural product, 16-anhydrotoxigenin (Dos-kotch et al., 1972).
P An alcoholic extract of the above-ground portion of the plant had been found to have an inhibitory action against the cell culture (KB) of human carcinoma of the nasopharynx (Abbot et al., 1966). In a further study at the Cancer Chemotherapy National Service Centre (CCNSC), systematic fractionation showed that mainly oleandrogenin, gitoxigenin and rhodexin B were significantly active (Abbot et al.,
Fig. 2.3. Cryptostegia grandiflora (Roxb.) R. Br. ex. Lindley. («) Flower
Fig. 2.3. Cryptostegia grandiflora (Roxb.) R. Br. ex. Lindley. («) Flower
1967). A parallel appears to exist between cytotoxicity towards KB cells, a heart action and inhibition of the ATPase-mediated active transport of K+ and Na+ (Kupchan et al., 1967; Doskotch et al., 1972).
Swallow wort, wild ipecacuanha L The roots of this West Indian species, widely cultivated in West Africa as an ornamental shrub, are used in the West Indies and in India, in decoction or pulverised, as an expectorant and emetic. They have similar effects to Ipecacuanha roots but are more strongly purgative. The roots of an indigenous related species, Pachycarpus lineolatus (Decne.) Bullock syn. (A. lineolata (Decne.) Schltr.), are
Fig. 2.4. Calotropis procera (Ait.) Ait.
Fig. 2.4. Calotropis procera (Ait.) Ait.
given in northern Nigeria in decoction with native soda for intestinal troubles. In East Africa the roots are used to stimulate digestion (Dalziel, 1937). C The roots of both Asclepias spp. contain cardenolides of which the most important aglycones are uzarigenin, corotoxigenin, and coroglaucigenin, but asclepogenin, curassavogenin and ascurogenin have also been reported as well as the cardenolides asclepin (in the Indian plants) and calotroposide which are both also found in Calotropis (Tschesche et al., 1958; Patel and Rowson, 1964; Singh and Rastogi, 1969; Patnaik and Dhawan, 1971; Hocking, 1976). The leaves contain polyphenols (quercetin and kaempferol) (Bate-Smith, 1962). P The alcoholic extract of the plant and asclepin have a digitoxin-like cardiotonic action and the total extract is used as a diuretic, expectorant and emetic (Paris and Moyse, 1971, p. 98).
Calotroposide shows an inhibiting action on malignant tumors (Kupchan et al., 1964; Bezanger-Beauquesne and Pinkas, 1971).
Calotropis procera (Ait.) Ait. (Fig. 2.4) ASCLEPIADACEAE
Mudar, apple of Sodom, swallow wort L Local healers use the acid latex of this plant as a rubefacient and to extract guinea worms (Dracunculus medinensis). Others use the dried rootbark in soup to treat colic and as a stomachic, and the burnt root is made up as an ointment for skin eruptions, foul ulcers, etc. (Dalziel, 1937). C The very toxic latex contains a cardiac heteroside, calotroposide, with an aglycone identical to ouabain, and seven other heteroside alkaloids; calotropin, calactin, calotoxin, uscharin, uscharidin, voruscharin and proceroside. Apart from calactin and proceroside these all have the same genin (calotropa H genin) (Hesse and Ludwig, 1960;Crout etal., 1963,1964). Besides the heterosides the latex is reported to contain amyrin, traces of glutathione and a proteolytic enzyme, 'calotropain'. P The aqueous and alcoholic extracts of the roots initially produce a slight depression, followed by a stimulation, of the rate and force of myocardial contractions in isolated frog and rabbit hearts (0.2 ml/kg). They also produce marked vasoconstriction in frog and rat and a persistent rise in blood pressure in the dog, which cannot be altered by any sympathetic drug (Derasari and Shah, 1965; Indian Council of Medical Research, 1976). In the cat the cardiotonic actions of calotroposide, calotoxoside and uscharin are 83%, 76% and 58%, respectively, of the action of ouabain (Chen etal., 1942). The cardioactive effect was confirmed by Patel and Rowson (1964).
The enzyme calotropain is said to be more active than papain, bromelin or ficin (Atal and Sethi, 1962); it also has an anthelmintic action (Garg et al., 1963).
Pergularia daemia (Forsk.) Chiov. syn. (P. external. E.Br., Daemia externa R.Br., Asclepias daemia Forsk.) ASCLEPIADACEAE
L Locally, anthelmintic properties are attributed to the leaves of the plant. The latex or a poultice of the leaves is also applied to boils and abscesses, and the plant is said to have emmenagogic action. In Ghana a soup made with the leaves is given to women immediately after childbirth (Dalziel, 1937). C The stems of the plant contain uzarigenin, coroglaucigenin and calactin (India), whilst in the seeds calactin, calotropin and eight further cardenolides are found. The plant also contains a bitter resin called pergularin, which is structurally near to tomentogenin from Marsdenia tomentosa (Mittal et al., 1962). Patel and Rowson (1964) established that in the Nigerian species only the seeds have cardiotonic action; the leaves, roots and stems do not (Rowson, 1965; Paris and Moyse, 1971). P The plant has a physiological action on the uterus similar to that of pituitrin but mainly limited to the upper part of the uterus and its use as a pituitrin substitute in delivery has been suggested (Dutta and Gosh, 1947). This action is not inhibited by progesterone. A general stimulating effect on involuntary muscles and an increase of the arterial blood pressure has also been observed (Gupta et al., 1950; Unesco, 1960).
Xysmalobium heudelotianum Decne. ASCLEPIADACEAE
L The tuber of this plant is used as a bitter tonic and is eaten by the Hausas (Northern
Nigeria) as a remedy for stomach troubles (Dalziel, 1937). C The tubers contain, like those of the East African X. undulatum R.Br., uzarosides (uzarin is a monoglycoside of uzarigenin, an isomer of digitoxigenin) and glycosides of xysmalogenin and of 17a-uzarigenin (Kuritzkes et al., 1963; Paris and Moyse, 1971, p. 97).
Glucosides of pregnane derivatives were reported in the roots ofX. undulatum (L.) Ait. by Tschesche and Snatzke in 1960 (Paris and Moyse, 1971, p. 96). P The uzarosides of X. heudelotianum have a weak cardiotonic action. They are mainly used as antispasmodics and antidiarrhoeal agents and in dysmenorrhoea (Paris and Moyse, 1971, p. 97).
Plants belonging to other botanical families. Cardenolides related to those found in the above-mentioned Apocynaceae and Asclepiadaceae are also occasionally found in members of other botanic families.
L The bark provides a fibre (jute) and the mucilagenous leaves are used in food and as a vegetable. In indigenous medicine in India the seeds are used as a purgative and the leaves as a tonic and diuretic (Chopra etal., 1956; Oliver, 1960). C From the seeds, 11-15% of a fixed oil and several steroid heterosides could be isolated (Chakrabasti and Senn, 1954). The corresponding aglycones, at first named corchorin, corchorogenin, corchsularin and olitorigenin, were later identified as strophanthidin (Senn et al., 1957). The main heterosides are corchoroside, olitoroside and helveticoside. The latter can be hydrolysed to give one molecule of strophanthidin and one molecule of D-digitoxose. Olitoroside is strophanthidin-/?-D-boivinopyranoside-3/3-D-glucopyranoside (Chakrabasti and Senn, 1954; Senn et al., 1957; Schmersal, 1969). P Strophanthidin has an action comparable to that of ouabain. The corresponding corchorosides A and B were found to contain lethal doses of 0.0768 and 0.1413 mg/ kg, respectively, which thus makes corchoroside A one of the most potent heart poisons (Frérejacque and Durgeat, 1954). Pharmacological and clinical trials have been carried out by Russian research workers. In pharmacological tests on rabbits with experimental myocarditis and myocardiosclerosis, and in dogs with acute coronary insufficiency a therapeutic effect was obtained with doses of 0.05 units/kg (one cat unit = 14 ju,g/kg) (Kiteava, 1966).
In clinical trials favourable results have been obtained in cases of chronic cardiac insufficiency both with the corchorosides and with olitoroside by several Soviet authors. The clinical condition and electrocardiogram of the patients were improved (increase in amplitude of T-wave) (Turova, 1962; Umarova etal., 1968).
Urginea indica (Roxb.) Kunth. syn. (Scilla indica Roxb.) LILIACEAE
L In South Africa U. altissima is known to be fatal to stock (Watt and Breyer-Brandwijk, 1962) and this probably also applies to U. indica. In northern Nigeria the scorched and dried bulbs are included in a liniment for rheumatic knees and sometimes the crushed bulbs are applied to bruises and aches (Dalziel, 1937). C From the bulbs of these species and from the Mediterranean U. maritima Bak. a crystalline glycoside, scillaren A, and a mixture of amorphous glycosides, scillaren B, have been extracted (Chopra et al., 1938, p. 251). The genin of scillaren A is scillaridin. The glycosides are chemically related to the digitalis and strophanthus glycosides. They are steroid heterosides of the bufanolid type (with a hexagonal lactonic cycle) (Seshadri and Subramanian, 1950). P The bulbs are official in the British Pharmaceutical Codex (1949) and US National Formulary. Scillaren, unlike digitalis, does not accumulate, but is bound more to the myocardium than is strophanthin. Scillaren A acts quickly but is rapidly hydrolyzed in the blood. Squill is mainly a diuretic which acts by increasing the renal circulation, but excessive doses may cause irritation and obstruction of the kidneys. Average doses in heart insufficiency are 6 mg/24 h with maintenance doses of 2 mg/24 h (Paris and Moyse, 1967, p. 50). The glycosides have the advantage of being useful in the treatment of conditions refractory to, or no longer responsive to, digitalis and strophanthus therapy (Darwish, 1980).
Urginea extracts have also been found to have antiprotozoal, hypoglycaemic (Bapat etal., 1970) and oncolytic actions (Dhar et al., 1968).
Mansonia altissima (Chev.) Chev. var. altissima STERCULIACEAE
L The bark of this tree has been used in the Ivory Coast as an arrow poison and in West African local medicine for the treatment of leprosy and as an aphrodisiac (Oliver, 1960).
C It contains mansonin which is a 2,3-di-(0-methyl)-6-deoxy-/3-D-glucopyranoside of strophanthidin. Strophothevoside is the corresponding 3-0-methyl-6-deoxy-/3-glucopyranoside. Besides mansonin, minute quantities of as many as 30 other cardenolides have been traced in the seeds by paper chromatography. They are all derived from three genins: strophanthidin, nigrescigenin and an undetermined genin (Algeier et al., 1967). P An amorphous fraction of mansonin was found to have a cardiotonic activity comparable to that of strophanthin G. Unfortunately, the yield of active substance is small and variable (Terrioux, 1952).
Antiaris africana Engl. syn. (A. kerstingii Engl., A. toxicaría (Rumph. ex Pers.) Lesch. var. africana) MORACEAE
L The tree is called 'bark cloth tree' as in Ashanti (Ghana) a strong white cloth is made from the bark. In the Ivory Coast the bark has been used as a purgative and in the treatment of leprosy (Dalziel, 1937).
C Seven heterosides of the digitalis type are reported in the latex including a- and /3-antiarin. On hydrolysis they produce antiarigenin and antiarose, and antiarigenin and L-rhamnose respectively. The seeds contain eveñomoside, antioside and several other glycosides and aglycones (Bisset, 1962; Wehrli et al., 1962; Mühlrad et al., 1965).
P The West African Antiaris appears to be less toxic than the Asiatic A. toxicaría (Pers.) Lesch. The dried latex of the Asian species (water-soluble extract) is a violent heart poison, causing fibrillation and a drastic fall in the blood pressure. In smaller doses it appears to be a stimulant for the heart and circulation (Chopra et al., 1938; Patel and Rowson, 1964).
Schwenkia americana L. syn. (S. hirta Wright, S. guineensis Schum. & Thonn.)
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