[Is there a difference in the pharmacodynamic effect of total Rauwolfia alkaloids & reserpine? Experimental note].
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The oxidation products of three Rauwolfia alkaloids having yohimbane skeleton, namely, reserpine, rescinnamine and ajmalicine have been characterised by chromatographic and spectroscopic techniques. The Rf values of the oxidation products (3, 4-dehydro derivatives) in several solvent systems and the spectral data on UV, IR, NMR and fluorescence characteristics have been determined to confirm the structure of these compounds.
A simple, sensitive and economically viable spectrophotometric method for the determination of some Rauwolfia alkaloids (ajmaline, ajmalicine, reserpine and yohimbine-HCl) has been developed. The method involves the oxidation of Rauwolfia alkaloids by iron(III) and subsequent complexation of iron(II) with 1,10-phenanthroline, forming a red-colored complex having the maximum absorbance at 510 nm. The method is applied to the determination of reserpine in tablets of pharmaceutical formulations. The common excipients do not interfere with the proposed method. A statistical comparison of these results with those of a reported method shows good agreement and indicates no significant difference in the precision.
Experiments were performed to explore the influence of two rauwolfia alkaloid derivatives, rescinnamine and syrosingopine, on noradrenaline at the sympathetic nerve-endings by delineating the localization of noradrenaline in the walls of femoral artery and abdominal aorta of rats treated with these agents compared to reserpine, using the fluorescence histochemical technique. Noradrenaline-containing nerve fibers emitting an intense yellowish-green fluorescence were demonstrated circumjacent internally to the adventitial smooth muscle layer of the femoral artery in both normal rats and spontaneously hypertensive rats (SHR). In both normal rats and SHR, treatment with rescinnamine or syrosingopine in an oral dose of 5 mg/kg caused essentially the same degree of depletion of the noradrenaline fluorescence localized subjacent to the adventitial smooth musculature of the femoral artery, as did that with 5 mg/kg of reserpine. The noradrenaline fluorescence vanished completely following treatment of rats with 15 mg/kg of rescinnamine or 30 mg/kg of syrosingopine. Noradrenaline-containing nerve fibers showing yellowish-green fluorescence were observed distributed subjacent to the entire internal circumference of the adventitial smooth muscle layer of the abdominal aorta in both the normal rats and SHR. In response to oral administration of rescinnamine or syrosingopine in a dose of 5 mg/kg, both normal and SHR rats showed a diminution of the noradrenaline fluorescence in the region of adventitial smooth musculature of abdominal aorta equivalent to that evoked by 5 mg/kg of reserpine. Treatment with 15 mg/kg of rescinnamine or 30 mg/kg of syrosingopine resulted in a complete disappearance of noradrenaline fluorescence in that region.(ABSTRACT TRUNCATED AT 250 WORDS)
The effect of three rauwolfia-alkaloids and two semi-synthetic derivatives on the catecholamine content of the hearts of guinea pigs was examined. The substances were: ajamaline, N-methyl-ajamaline, N-n-propylajmaline, rescinnamine and reserpine. The presence of catecholamines in isolated atria was tested with tyramine (10(-5) g/ml). Rescinnamine and reserpine depleted the hearts of catecholamines, ajmaline and its derivatives did not.
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In a case-control study of 1881 women with breast cancer and 1523 controls with benign conditions, 65 cases (3.5%) and 64 controls (4.2%) reported having used a drug that contained rauwolfia, giving a rate ratio estimate of 0.8 (95% confidence interval, 0.5-1.1). Use that ended more than a year previously was negatively associated with breast cancer (rate ratio, 0.5; 95% confidence interval, 0.2-0.9). The risk of breast cancer did not vary significantly according to duration of use. Nor did it vary within strata of varying base-line risk, such as age at first pregnancy. The data suggest that rauwolfia alkaloids do not increase the risk of breast cancer.
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