The dictyostatins are a promising class of potential anticancer drugs because they are powerful microtubule stabilizing agents, but the complexity of their chemical structures is a severe impediment to their further development. Based on both synthetic and medicinal chemistry analyses, 25,26-dihydro-16-desmethyldictyostatin and its C6 epimer were chosen as potentially potent yet accessible dictyostatin analogs, and three new syntheses were developed. A relatively classical synthesis involving vinyllithium addition and macrocyclization gave way to a newer and more practical approach based on esterification and ring-closing metathesis reaction. Finally, aspects of these two approaches were combined to provide a third new synthesis based on esterification and Nozaki-Hiyama-Kishi reaction. This was used to prepare the target dihydro analogs and the natural product. All of the syntheses are streamlined because of their high convergence. The work provided several new analogs of dictyostatin including a truncated macrolactone and a C10 E-alkene, which were 400-fold and 50-fold less active than (−)-dictyostatin. In contrast, the targeted 25,26-dihydro-16-desmethyldictyostatin analogs retained almost complete activity in preliminary biological assays.
This study has generated new knowledge about the biotechnological potential of T. delbrueckii (TD219) and S. cerevisiae (QA23) for improving the organoleptic properties of Chardonnay and Palomino wines.
Chickpea flour (CF)-based muffin formulations were made with CF alone and with added biopolymers [whey protein (WP), xanthan gum (XG) and inulin (INL)] to evaluate their suitability to be a wheat flour (WF) substitute in muffins. Structural characteristics of the batters and muffins were studied by means of rheometry, microscopy, physicochemical properties, and texture and sensory analysis. Partial replacement of CF with XG, alone (at 0.5 and 1%) or blended with either WP or INL, significantly increased the batter viscoelasticity as denser matrices developed; moreover, the muffins with XG added at 1% had similar hardness to wheat gluten muffins. The replacement of WF decreased the springiness, cohesiveness, chewiness, resilience and specific volume of the muffin. However, baked muffins with added XG also showed higher sensory sponginess and moisture associated with numerous air bubbles in the batter and were perceived to be easier to swallow and to have better general appearance.
The effects of five novel winemaking technologies on color were evaluated. Cold soak maceration (CSM), dry ice maceration (DIM), prefermentative juice runoff (PJR), delestage (D), and extended maceration (EM) were the process assayed on grapes from Tempranillo variety cultivated in a warm climate zone. Enological and color parameters were determined at stemmed-crushed, pressed, bottled and after 4 months aged in bottle. Significant differences were found in color intensity, percentage of red and blue, and hue at each step of the process and for every technique when compared to the control wine. However, differences tended to decrease with aging. Eleven anthocyanins (glucosides and acylated) were identified, and five quantified by HPLC. Also the anthocyanin distribution in free anthocyanin (% FA), copigmented anthocyanin (% CA) and polimerizated anthocyanin (% PA) were studied. Differences were found for total anhocyanin content, not in their relative abundance. Winemaking processes affected wine's main sensory attributes. DIM achieved a remarkably high valuation for aspect at bottle time, while EM obtained very positive remarks with regards to aroma and persistence at aging DIM and PJR seemed to be the most promising techniques, but after 4-months aging in bottle only EM wine showed a high anthocyanin content.
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