Four new clerodane diterpenes, casearinols A and B (1 and 2) and casearinones A and B (3 and 4), were isolated from the leaves of Casearia guianensis. These immunomodulatory compounds have been structurally elucidated primarily on the basis of 2D NMR analysis and spectral data comparison with known compounds. These compounds inhibited the binding of T-cell leukocyte function antigen 1 to intercellular adhesion molecule 1.

Cytokinin analysis by immunoaffinity chromatography (IAC), high-performance liquid chromatography (HPLC) and radioimmunoassay (RIA) or enzyme-linked immunosorption assay (ELISA) has been used to study two separate topics: the role of tRNA in bacterial cytokinin biosynthesis and the changes in cytokinin concentration which occur during cereal grain development. Transfer RNA isopentenylation in the gall-forming plant pathogen Agrobacterium tumefaciens is encoded by the chromosomal miaA locus. Mutation of miaA reduces tRNA isopentenylation significantly and preliminary data suggest that turnover of isopentenylated tRNA is responsible for low level secretion of free N6-isopentenyladenine (iP) by the bacteria. However, the major route of cytokinin biosynthesis by gall-forming plant patho- genic bacteria is not via tRNA turnover but by direct biosynthesis mediated by dimethylallylpyro- phosphate: 5'-AMP transferase (DMAPP :AMP transferase) encoded by such genes as ipt, tzs (from A, tumefaciens) or ptz (from Pseudomonas savastanoi). Analysis of cytokinin levels in developing wheat and rice grains in the period immediately following pollination showed large transient increases in zeatin (Z) and zeatin riboside (ZR) which coincided with the period of maximum endosperm cell division reported by others. Detailed analyses of maize kernels, where development can be staged readily, showed that Z and ZR concentrations peaked 9 days after pollination (DAP). During the period 8-10 DAP, cytokinin oxidase underwent a significant increase in specific activity, indicating that cytokinin catabolism was enhanced as endosperm cell division ended.

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A new trichothecene, harzianum A [1], was isolated from the soil-borne fungus Trichoderma harzianum. The structure of 1 was determined by extensive spectral analyses including the nmr techniques of PS-COSY, HMQC, HMBC, and NOESY. Harzianum A [1] contains a (Z,E,E)-2,4,6-octatriendioic acid esterified on the 4 beta hydroxyl group of trichodermol and is structurally related to the trichoverroids. Harzianum A [1] showed no cytotoxicity against baby hamster kidney cells, no activity against Gram-negative and Gram-positive bacteria, but modest antifungal activity at 100 micrograms/ml.

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Previous investigations have shown the feasibility of increasing pod number on legumes by the application of 6-benzylaminopurine (BA) directly to the raceme. These investiptions were designed to determine what reproductive parameter was affected by cytokinin application, and if these applications were overcoming a deficiency in root-produced cytokinins during late flowering. Five individual main stem racemes on greenhouse grown soybeans (Glycine max L. Menf.) were treated with 2 millimolar BA. A single application of BA when pods appeared at 25 to 50% of the proximal floral positions resulted in a 58% increase in pod set due primarily to a 33% reduction in floral abscission. Applications of BA at later intervals also resulted in significant reductions in total abscission. When three applications of BA were imposed on the upper five nodes of field grown soybeans, total pod number and seed weight were significantly increased in this section of the canopy by 27 and 18%, respectively. Throughout the flowering period, root pressure exudate was sampled for the subsequent separation and quantification of zeatin, dihydrozeatin, zeatin riboside, dihydrozeatin riboside, and isopentenyladenine. Total cytokinin flux peaked from 0 to 9 days after flowering began, and then dropped to one-half of this level by 15 days postanthesis. The probability that a flower would initiate a pod was directly related to the concentration of total cytokinins present in the exudate when the flower opened.Yield in soybean is determined by the number of seeds per unit area, and the average weight per seed. The number of seeds per unit area is determined by the number of flowers which initiate pods that attain maturity. Soybeans produce an abundance of flowers, but shed a rather large proportion of them before the seeds begin to fill. Estimates vary, but investigators have shown that the abscission of flowers and small pods ranges from 32 to 82% of the total flowers produced (29,30

Leukotriene B(4) (LTB(4)) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA(4) hydrolase is the rate-limiting step for LTB(4) production, this enzyme represents an attractive pharmacological target for the suppression of LTB(4) production. From an in-house screening program, SC-22716 (1, 1-[2-(4-phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA(4) hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA(4) hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.