ABSTRACT
As part of a continuing effort aimed at the development of efficacious antihistaminic and bronchodilator agents for the treatment of asthma and related respiratory diseases, a series of novel trisubstituted deoxyvasicine derivatives was designed and synthesized. Bronchodilatory activity of pure samples of ligands 17a-d, and DL-8-chlorovasicine hydrochloride is investigated and compared with isoprenaline and aminophylline. These studies confirm the activity of ligands 17a-d and the potentiating effect of 17c on aminophylline.
Subject(s)
Alkaloids/chemical synthesis , Alkaloids/pharmacology , Bronchial Spasm/prevention & control , Bronchodilator Agents/pharmacology , Quinazolines , Alkaloids/chemistry , Aminophylline/pharmacology , Animals , Drug Evaluation, Preclinical , Guinea Pigs , In Vitro Techniques , Isoproterenol/pharmacology , Structure-Activity Relationship , Trachea/drug effectsABSTRACT
Two new carbazole alkaloids, designated as clausenol and clausenine, were isolated from an alcoholic extract of the stem bark of Clausena anisata. Their structures were established as 1-hydroxy-6-methoxy-3-methylcarbazole and 1,6-dimethoxy-3-methyl carbazole, respectively, from physical and chemical evidence and synthesis. Clausenol was found to be active against Gram-positive and Gram-negative bacteria and fungi.
Subject(s)
Anti-Bacterial Agents/chemistry , Carbazoles/chemistry , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Plants, Medicinal , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Carbazoles/isolation & purification , Carbazoles/pharmacology , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Molecular Structure , Plant Stems , Spectrophotometry, InfraredSubject(s)
Anesthetics, Inhalation/adverse effects , Cerebral Ventricle Neoplasms/surgery , Nitrous Oxide/adverse effects , Pneumocephalus , Postoperative Complications , Adult , Cranial Fossa, Posterior , Female , Humans , Pneumocephalus/diagnostic imaging , Pneumocephalus/etiology , Pneumocephalus/therapy , Posture , Tomography, X-Ray ComputedABSTRACT
A new carbazole alkaloid designated as clausenal was isolated from the leaves of Clausena heptaphylla and its structure established as 1,8-dimethoxy-3-formylcarbazole from physical, chemical and synthetic evidence. The alkaloid was found to be active against both Gram-positive and Gram-negative bacteria, and fungi.
Subject(s)
Alkaloids/chemistry , Alkaloids/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Bacteria/drug effects , Carbazoles/chemistry , Carbazoles/pharmacology , Fungi/drug effects , Alkaloids/isolation & purification , Anti-Bacterial Agents , Carbazoles/isolation & purification , Microbial Sensitivity Tests , Plant LeavesABSTRACT
Preliminary phytochemical investigation of the leaves of Synclisia scabrida indicated the presence of two alkaloids in the water extracts and five alkaloids in the ethanol extracts. The alkaloidal fraction obtained from the cold ethanol extract furnished on column-chromatography, a homogeneous amorphous solid which has been designated as alkaloid C. Alkaloid C showed positive test for alkaloids. The UV and IR spectra and colour reactions of alkaloid C indicated that the compound may be a phenolic bisbenzylisoquinoline alkaloid. All the extracts delayed the onset and shortened the duration of apomorphine-induced stereotyped behaviour in chicks. In addition, 40 mg kg-1 i.p. of the ethanolic extract induced catalepsy in rats. The cold water extract (CWE) synchronized the EEG of the hyperstriatum, optic tectum and the reticular formation while the EMG activity was slightly enhanced. The hot ethanol alkaloidal extract (HEE) inhibited the growth of Pseudomonas aeruginosa and Staphylococcus aureus. The minimum inhibitory concentration of HEE on Pseudomonas aeruginosa strains I and II were 5 and 2.5 micrograms/ml while for Staphylococcus aureus strains I and II were 5 and 10 micrograms/ml, respectively. Up to 1 g kg-1 i.p. of the extract failed to induce any lethal effect in chicks and rats. These effects of the leaf extracts of Synclisia scabrida Miers support some of the local uses of the plant by traditional medical practitioners.
