Aminoalkaloids EPHEDRA Ephedra gerardiana, E. sinica, E. equisetina, E. distachya, E. intermedia, E. major Family: Ephedraceae (Gnetaceae) Synonyms: Ma Huang. Habitat: West Central China, Southern Siberia, Japan.

Characters E. sinica E. equisetina E. distachya Stems 30cm long, ashy greyish green in colour Internodes 3-6 cm long Very woody much branched 20-200 cm in length, ashy yellow green in colour Internodes 1-2.5cm 37cm long, woody Gennish yellow Internodes 2.5-6 cm long Leaves Subulate recurved apex lamina whitish and base reddish brown Apex shorter not recurved, Brownish purple in colour Leaf apex short acute often fissured at base

MICROSCOPY OF EPHEDRA STEM Epidermis STROMA Group of fibres at the apex of rib Pith Pericyclic fibres Xylem

Chemical constituents The plants typically contain 0.5–2.0% of alkaloids, according to species, and from 30–90% of the total alkaloids is (−)-ephedrine. Related structures, including the diastereoisomeric (+)-pseudoephedrine and the demethyl analogues (−)-norephedrine and (+)-norpseudoephedrine are also present. In E. intermedia, the proportion of pseudoephedrine exceeds that of ephedrine.

Medicinal uses/Therapeutic actions: antispasmodic properties, acts on the air passages and is of benefit in asthma and hay fever; it is also employed for rheumatism; a 5 to 10 per cent solution has mydriatic properties, prophylactically used for low blood pressure in influenza, pneumonia, Ephedrine- indirectly acting sympathomimetic amine with effects similar to noradrenaline Lack the phenolic groups of the catecholamines, it has only weak action on adrenoreceptors but it is able to displace noradrenaline from storage vesicles in the nerve terminals, which can then act on receptors. It is orally active and has a longer duration of action than noradrenaline. It also has bronchodilator activity, giving relief in asthma, plus a vasoconstrictor action on mucous membranes, making it an effective nasal decongestant. Pseudoephedrine is also widely used in compound cough and cold preparations and as a decongestant. The ephedrine and pseudoephedrine used medicinally are usually synthetic. One commercial synthesis of ephedrine involves a fermentation reaction on benzaldehyde using brewer’s yeast (Saccharomyces sp.), giving initially an alcohol, then reductive condensation with methylamine yields (−)-ephedrine with very high enantioselectivity. The herbal drug ephedra/Ma Huang is currently being traded as ‘herbal ecstasy’. Consumption gives CNS stimulation, but in high amounts can lead to hallucinations, paranoia, and psychosis.

ACONITE: Monkshood. Blue Rocket. Friar's Cap. Auld Wife's Huid. Terpenoid ACONITE: Monkshood. Blue Rocket. Friar's Cap. Auld Wife's Huid. Aconitum napellus (Ranunculaceae )

Dried Aconite root Upper extremity, when crowned with an undeveloped bud, enclosed by scaly leaves, is about 3/4 inch in diameter, tapering quickly downwards. It is dark brown in colour and marked with the scars of rootlets. The surface is usually longitudinally wrinkled, especially if it has been dried entire. breaks with a short fracture and should be whitish and starchy within.

Microscopy: A transverse section shows a thick bark, separated from the inner portion by a well-marked darker line, which often assumes a stellate appearance. Brown outer tissue cortex suberised cells protective tissue metaderm (brown tabular cells having no regular arrangement). Some cells of cortex are thick walled, pitted, lignified forming characteristic sclerids.

Phloem: Primary and secondary consisting phloem parenchyma and sieve tissue Xylem contains xylem vessels Cells of all parenchymatous tissue like xylem parenchyma and phloem parenchyma contains starch grains Ca oxalate absent . Aconite root as found in commerce is, however, often yellowish or brownish internally with the stellate markings not clearly shown, probably from having been collected too early. It should be lifted in the autumn of the second year.

CHEMICAL CONSTITUENTS: Aconite root -0.3 to 1 per cent alkaloidal matter- Aconitine - the only crystallizable alkaloid, is present to the extent of not more than 0.2 per cent, acrid and highly toxic - with the alkaloids Benzaconine (Picraconitine) and Aconine. The Aconitines are a group of highly toxic alkaloids derived from various species of Aconite, The Aconitines are divided into two groups: 1) Aconitines proper- Aconitine, Japaconitine, Indaconitine, 2) Pseudaconitines - Pseudaconitine and Bikhaconitine. The lethal dose for the guinea-pig being considered to be the most convenient and satisfactory standard. Tinctures vary enormously as to strength, some proving seven times as powerful as others.

Hydrolysis products of aconitum alkaloids base Acid Hypaconitine Hypaconine Acetic acid and benzoic acid Jesaconitine aconine Acetic acid and anisic acid Pseudoaconitine Pseudoaconine Acetic acid and veraric acid Lycaconitine Lycaconine Lycotannic acid (N-succnylanthranillic acid)

Medicinal actions/Uses: Anodyne, diuretic and diaphoretic. Externally it relieves the pain of neuralgia, pleurisy and aneurism.. Poisoning from, and Antidotes: The symptoms of poisoning are tingling and numbness of tongue and mouth and a sensation of ants crawling over the body, nausea and vomiting with epigastric pain, laboured breathing, pulse irregular and weak, skin cold and clammy, features bloodless, giddiness, staggering, mind remains clear. A stomach tube or emetic should be used at once, 20 minims of Tincture of Digitalis given if available, stimulants should be given and if not retained diluted brandy injected per rectum, artificial respiration and friction, patient to be kept lying down.

Other Varieties: Japanese Aconite syn. Aconitum Chinense =A. uncinatum, var. Faponicum = A. volubile It has conical or top-shaped, gradually tapering tuberous roots, 1 to 2 inches long, 1/3 to 1 inch in thickness at the top, externally covered with a brown, closely adhering skin internally white. Dried roots do not contain much alkaloid, if steeped when fresh in a mixture of common salt, vinegar and water. The poisonous alkaloid present is called Japaconitine, to distinguish it from the official Aconitine and the Pseudaconitine of A. laciniatum. Japaconitine is similar in constituents and properties with the Aconitine of A. Napellus. Indian Aconite root or Nepal Aconite A. laciniatum (Staph.). It is also called Bikh or Bish, and is collected in Nepal. It is much larger than the English variety, being a conical, not suddenly tapering root, 2 to 4 inches long and an inch or more at the top, of a lighter brown than the official variety, the rootlet scars much fewer than the official root. Internally it is hard and almost resinous, the taste intensely acrid and is much shriveiled longitudinally. This root yields a very active alkaloid, Pseudoaconitine, and resembles it in many of its properties to Aconitine ; it is about twice as active as Aconitine. Indian Aconite root was formerly attributed to A. ferox (Wall). Their large size and less tapering character -distinguish these from the official drug.

Other varieties of Aconite are A. chasmanthum (Staph Other varieties of Aconite are A. chasmanthum (Staph.), known in India as Mohri, which contains Indaconitine, and A. spicatum, another Indian species containing Bikhaconitine, resembling Pseudaconitine. Russian Aconite, A. orientale, grows abundantly in the Crimea and Bessarabia. It has a small, compact, greyish-black root with a transverse section similar to that of A. Napellus. Taste: hot and acrid. When treated by a process which gave 0.0526 per cent of crystalline Aconitine from a sample of powdered root of A. Napellus, the dried root of A. orientale yielded 2.207 per cent of total alkaloids, which were, however, amorphous. The total alkaloid has not yet been investigated further. Atis root A. heterophyllum (Wall), -in Western temperate Himalayas. This species does not contain Aconitine and is said to be non-poisonous. Chief constituent: intensely bitter alkaloid - Atisine - possessing tonic and antiperiodic principles. A. palmatum, of Indian origin, yields a similar alkaloid, Palmatisine. Chinese aconite: A. carmichaelli, A. cusnezofii, A. brachypodum The province of Szechwen in West China grows large quantities of medicinal plants, among them A. Wilsoni, A. Fischeri, and A. Hemsleyan,

CINCHONA

Cinchona succirubra provides what is called ‘red’ bark (alkaloid content 5–7%), C. ledgeriana gives ‘brown’ bark (alkaloid content 5–14%), and C. calisaya ‘yellow’ bark with an alkaloid content of 4–7%. Selected hybrids can yield up to 17% total alkaloids. Bark is stripped from trees which are about 8–12 years old, the trees being totally uprooted by tractor for the process. A considerable number of alkaloids have been characterized in cinchona bark, four of which account for some 30–60% of the alkaloid content.

HYDRASTIS

The chief constituents of Hydrastis rhizome are the alkaloids Berberine (3.5 to 4 per cent.), which constitutes the yellow colouring matter of the drug, Hydrastine (2 to 4 per cent.), a peculiar crystallizable substance and a third alkaloid, Actions and uses: The action is tonic, laxative, alterative and detergent. It is a valuable remedy in the disordered conditions of the digestion and has a special action on the mucous membrane, making it of value as a local remedy in various forms of catarrh. In chronic inflammation of the colon and rectum, injections of Hydrastine are often of great service, and it has been used in haemorrhoids with excellent results, the alkaloid Hydrastine having an astringent action.