ABSTRACT
The molluscicidal and piscicidal activity of extracts from the leaves, berries and bark of the tree Apodytes dimidiata were evaluated experimentally. The leaves were highly toxic to both Bulinus africanus and Biomphalaria pfeifferi, the intermediate host snails of Schistosoma spp. B. pfeifferi profusely exuded mucus which appeared to render some protection against the toxic substance(s) of the plant but did not prevent their eventual demise. The LC10 after one-hour exposures of fish (Oreochromis mossambicus) was within molluscicidal levels.
Subject(s)
Biomphalaria , Bulinus , Disease Vectors , Fishes , Plant Extracts , Animals , Dose-Response Relationship, Drug , South AfricaABSTRACT
The D3-trishomocubyl system was prepared from tertiary pentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecan-8-ols 5 in one step by using a modified Ritter reaction yielding only one of the possible two geometrical isomers of 4-amino-3-alkyl (or aryl)-D3-trishomocubane (8). Promising antagonism of reserpine-induced catalepsy was exhibited by these compounds which compared favorable with that of amantadine. Weak to mild anticholinergic properties were observed during the reduction of oxotremorine induced tremor and salivation procedure. Acute toxicities similar to that of amantadine were observed for some of these compounds. D3-Trishomocubyl-4-amines appeared as a promising new class of anti-Parkinson agents.
Subject(s)
Antiparkinson Agents/chemical synthesis , Bridged-Ring Compounds/chemical synthesis , Animals , Antiparkinson Agents/therapeutic use , Antiparkinson Agents/toxicity , Bridged-Ring Compounds/therapeutic use , Bridged-Ring Compounds/toxicity , Catalepsy/drug therapy , Chemical Phenomena , Chemistry , Male , Mice , Stereoisomerism , Structure-Activity RelationshipABSTRACT
A new pentacyclic triterpene [1] with anti-inflammatory activity was isolated from the roots of Commiphora merkeri. The structure was established on the basis of spectral data and conversion to its triacetate.
Subject(s)
Analgesics/isolation & purification , Anti-Inflammatory Agents/isolation & purification , Heterocyclic Compounds/pharmacology , Plants, Medicinal/analysis , Triterpenes/pharmacology , Heterocyclic Compounds/isolation & purification , Magnetic Resonance Spectroscopy , Molecular Structure , Steroids , Triterpenes/isolation & purificationSubject(s)
Antihypertensive Agents , Chromones/pharmacology , Plants, Medicinal/analysis , Animals , Chromones/toxicity , Rats , South AfricaABSTRACT
Chemical modification of the naturally occurring phlorophenone antimicrobial agent caespitin is described. These modifications include variations in the phenone side chain, substitution with prenyl, allyl, and benzyl in the 4-position of the phlorophenone nucleus, and ring cyclizations via etherification to give furan and chroman compounds. Several of these derivatives show enhanced in vitro potency over caespitin. Studies on the development of microbial resistance against these compounds show that no or very little resistance developed after several passes of these compounds in representative microbial strains.
