Pharmacokinetic study of exogenously administered ß-endorphin using a rapid radioreceptor assay in rats

A rapid radioreceptor assay for measuring ß-endorphin (ß-EP) in unextracted serum has been developed. The method is based upon the inhibition by ß-EP of ³H-naloxone binding to the specific receptors on rat brain membranes, prepared in a stable form of pellets. Effect of serum on the assay was minimized by adding pooled serum to the equal dilution of total serum in the assay mixture. Pharmacokinetic analysis of pharmacologically active ß-EP equivalents (ß-EP eq.) in rats was performed using this method. The serum disappearance of ß-EP eq. after iv administration followed a biexponential decline and pharmacokinetic parameters were calculated by a two-compartment open model. The half-lives of α-phase and ß-phase were 2.6 ± 0.5 min and 6.2 ± 1.6 hr (mean ± SE; n=6), respectively. The volume of the central compartment (V₁) and that of steady-state (Vd_ss) were 67 ± 16 and 480 ± 75 ml/kg (mean ± SE; n=6), respectively. The total body serum clearance (CL_tot) was 2.1 ± 0.9 ml/min/kg (mean ± SE; n=6). The serum disappearance curve of ß-EP eq. obtained in the present study was similar to that previously reported by Houghten et al. (Proc. Natl. Acad. Sci. U.S.A. $\text{77}$, 4588–4591 (1980)), in which the disapperance of total radioactivity of tritiated ß-EP in rats was examined.     

Pollen morphology of Solanurn L. section Solanum

J. M. EDMONDS, 1984. Pollen morphology of Solanum L. section Solnnum . The pollen morphology of both dried and fresh, fixed material was examined using SEM. The work confirmed thc spheroidal to sub-prolate shape, the tricolporate nature and the granular surface sculpturing, typical of Solanurn pollen, but failed to demonstrate the occurrence of exine patterns which could bc of practical taxonomic use is differentiating the species belonging to the section Solanurn . Quantification of the exine sculpturing, by means of granule density counts, indicated a possible relationship between this feature and the morpho-genetic diversity of certain species.     

Metabolism of indole-3-acetic acid and indole-3-methanol in wheat leaf segments

Indole-3-methanol is a product of indole-3-acetic acid metabolism in wheat leaves ( Triticum compactum Host., cv. Little Club). It leads either to the production of the corresponding aldehyde and carboxylic acid, to the production of a polar glucoside which releases indole-3-methanol on β-glucosidase treatment, or to an unidentified apolar product on mild alkaline hydrolysis in aqueous methanol. With reference to a published pathway of indole-3-acetic acid degradation, the results provide evidence for a prominent role of indole-3-methanol and also for the occurrence of co-oxidation processes in wheat leaves involving indole-3-acetic acid and phenolic cosubstrates.     

Activation and alteration of plant and fungal polyphenoloxidase isoenzymes in sodium dodecylsulfate electrophoresis

Electrophoretic analysis of polyphenoloxidase isoenzymes from a variety of angiosperms and from mushroom revealed that the enzymes remain active in the presence of 0.1 % sodium dodecylsulfate. Electrophoresis in the presence of sodium dodecylsulfate allows the detection of latent enzyme forms of polyphenoloxidase, and can also convert slower migrating enzyme forms to faster migrating forms. Electrophoresis in the absence of sodium dodecylsulfate followed by incubation in the presence of sodium dodecylsulfate can also be used to detect latent forms of polyphenoloxidase. Together, these approaches provide a method for screening latent enzymes and give some insight into the mechanism of activation by sodium dodecylsulfate.     

Further glaucolides from south african Vernonia species

The investigation of three South African Vernonia species afforded minute amounts of five new glaucolides, two monoepoxides and three diepoxides. The structures were elucidated by ¹H NMR spectroscopy. The roots of Vernonia sutherlandii contain, in addition to vernonataloide, bergamotene and santalene, minute amounts of the corresponding acetoxy derivatives.     

An intramolecular linkage involving isodityrosine in extensin

We isolated isodityrosine, a diphenyl ether linked amino acid, from cell wall hydrolysates and from two tryptic peptides of extensin. Determination of the molecular weights, net charges and composition of the peptides indicated that isodityrosine (IDT) can form a short intramolecular linkage in sequences consisting of:

     

Triterpenes from Periandra dulcis roots

Three oleanane triterpenes were isolated from the roots of Periandra dulcis,and identified as 3β-hydroxy-25-al-olean-18-en-30-oic acid (periandric acid I), 3β-hydroxy-25-al-olean-12-en-30-oic acid (periandric acid II) and 3-oxo-25-hydroxy-olean-12-en-30-oic acid. The former two compounds (periandric acids I and II) were identical with the aglycones obtained by hydrolysis of periandrin I and II, respectively and the latter one was a new triterpene.     

Purification and properties of indole 2,3-dioxygenase from maize leaves

An indole 2,3-dioxygenase was purified ca 38-fold from maize leaves. The enzyme had an MW of about 98000, an optimum pH of 5.0 and the energy of activation was 9.1 kcal/mol. The K_max for indole was 1.4 × 10^?4 M. The enzyme was inhibited by diethyldithiocarbamate, salicylaldoxime and sodium dithionite. The inhibition by diethyldithiocarbamate was specifically reversed by Cu²⁺. The dialysed enzyme was stimulated by Cu²⁺. Four atoms of oxygen were utilized in the disappearance of 1 mole of indole. Inhibition of the enzyme by -SH compounds and -SH group inhibitors, and their partial removal by Cu²⁺ only, suggested the involvement of -SH groups in binding of Cu²⁺ at the catalytic site.     

Germacranolides from Schkuhria anthemoidea

The isolation of eucannabinolide and three new sesquiterpene lactones from Schkuhria anthemoidea is reported. The structures and stereochemistries of the new compounds were established by chemical and spectroscopic means. The structure of santhemoidin B was confirmed by X-ray crystallography.     

Condensed tannins: co-occurrence of procyanidins,prodelphinidins and profisetinidins in the heartwood of Acacia baileyana

The flavonoids and condensed tannins of the heartwood of Acacia baileyana var. purpurea are described. In conformity with other Acacia species, the hydroxylation pattern of the flavonoids is of the resorcinol type but, in sharp contrast, the tannins are heterogeneous consisting of a mixture of the resorcinol and phtoroglucinol series. Dimeric proanthocyanidins of the phloroglucinol type were absent and this exception to the general observation that they invariably co-occur with the polymers may be explained by the relative nucleophilicity of the aromatic A-rings.