ABSTRACT
A dose-ranging pharmacokinetic study of buflomedil was carried out in eight subjects to determine the pharmacokinetic parameters of the drug after oral and intravenous administration. Based on AUC infinity analyses, the pharmacokinetics of buflomedil were found to be linear within the dose ranges studied (50 to 200 mg for i. v. injection and 150 to 450 mg for oral administration). In the oral study, the mean biological half-life of the drug was 2.97 h, while after intravenous dose it was 3.25 h. The apparent volume of distribution after the pseudodistribution equilibrium (Fd beta) and volume of distribution at the steady state (Vdss) were 1.43 +/- 0.24 l/kg and 1.32 +/- 0.26 l/kg, respectively. The mean urinary recovery of intact drug and the metabolite, paradesmethyl buflomedil, after intravenous dosing, were 23.6% and 18.7%, respectively, while after oral dosing, they were 18% and 14.8%, respectively. On the average, 72% of the dose was observed into the systemic circulation after oral administration. This level of bioavailability was attributed to the hepatic first-pass effect.
Subject(s)
Butyrophenones/metabolism , Pyrrolidines/metabolism , Vasodilator Agents/metabolism , Administration, Oral , Adult , Butyrophenones/administration & dosage , Humans , Injections, Intravenous , Kinetics , Male , Pyrrolidines/administration & dosage , Vasodilator Agents/administration & dosageABSTRACT
Aqueous extracts of Pteryxia terebinthina var. terebinthina were shown to possess antiarrhythmic activity. A novel furanocoumarin, pterybinthinone, the known coumarins pteryxin and umbelliferone, and sucrose were isolated from this plant. Attempts to re-isolate a structurally undefined, defibrillatory substance by means of a published protocol were unsuccessful.
Subject(s)
Anti-Arrhythmia Agents/isolation & purification , Plants/analysis , Aconitum/antagonists & inhibitors , Animals , Arrhythmias, Cardiac/chemically induced , Arrhythmias, Cardiac/drug therapy , Cats , Coumarins/isolation & purification , Coumarins/pharmacology , In Vitro Techniques , Ouabain/antagonists & inhibitors , Plant Extracts/pharmacology , Rabbits , Rats , Umbelliferones/isolation & purification , Umbelliferones/pharmacologyABSTRACT
A phytochemical investigation of the leaves and twigs of Helietta parvifolia (Rutaceae) resulted in the isolation of heliparvifoline, a new furoquinoline alkaloid, in addition to the known bases flindersiamine and isoflindersiamine.
Subject(s)
Alkaloids/isolation & purification , Hydroxyquinolines/isolation & purification , Plants/analysis , Quinolines/isolation & purification , Alkaloids/therapeutic use , Animals , Antineoplastic Agents/therapeutic use , Chemical Phenomena , Chemistry , Chromatography, Thin Layer , Hydroxyquinolines/therapeutic use , Leukemia, Experimental/drug therapy , Mice , Neoplasms, Experimental/drug therapy , Quinolines/therapeutic useABSTRACT
From the turpentine broom, Thamnosma montana, four alkaloids and three coumarins were isolated and characterized. Skimmianine (5), N-methyl-acridone (4) and 5-(3'-methyl-2',3'-dihydroxybutanyl)-8-methoxypsoralen (1) were obtained previously from T. montana. Robustine (2) is reported from a Thamnosma species for the first time and acridone (6), thamnosmonin (9), and thamontanin (14) are reported from a natural source for the first time. Evidence for the structures of the new isolates is presented.
Subject(s)
Alkaloids/analysis , Coumarins/analysis , Plants, Medicinal/analysis , Alkaloids/therapeutic use , Carcinoma/drug therapy , Cell Line , Chemical Phenomena , Chemistry , Leukemia, Lymphoid/drug therapy , Methoxsalen/analysis , Mouth Neoplasms/drug therapy , Neoplasms, Experimental/drug therapyABSTRACT
Herbadine, a novel dihydroindole alkaloid, was isolated from the arterial parts of Vinca libanotica Zucc. (Apocynaceae). The physical and spectral data (UV, IR, NMR, and mass spectroscopy) indicated the alkaloid to be a derivative of aimaline. Comparative high-resolution NMR studies with quebrachidine and high-resolution mass spectral studies established the structure of the alkaloid to be 2-epi-3-hydroxyquebrachidine. Herbadine was previously isolated from another species by Russian workers and a structure was postulated. The current paper gives evidence for a corrected structure of herbadine.
