Context: Quassinoids are biologically active secondary metabolites found exclusively in the Simaroubaceae family of plants. These compounds generally present important biological properties, including cytotoxic and antitumor properties.Objective: In the present study, the cytotoxic effects of neosergeolide, a quassinoid isolated from Picrolemma sprucei Hook. f., were evaluated in human promyelocytic leukemia cells (HL-60).Materials and methods: Cytotoxicity and antiproliferative effects were evaluated by the MTT assay, May-Grunwald-Giemsa’s staining, BrdU incorporation test, and flow cytometry procedures. The comet assay and micronuclei analysis were applied to determine the genotoxic and mutagenic potential of neosergeolide.Results: After 24 h exposure, neosergeolide strongly inhibited cancer cell proliferation (IC50 0.1 µM), and its activity seemed to be selective to tumor cells because it had no antiproliferative effect on human peripheral blood mononuclear cells (PBMC) at tested concentrations. Apopto...

https://www.tandfonline.com/doi/pdf/10.3109/13880209.2012.654921

Involvement of intrinsic mitochondrial pathway in neosergeolide-induced apoptosis of human HL-60 leukemia cells: The role of mitochondrial permeability transition pore and DNA damage

The total syntheses of (±)-botryosphaeridione, (±)-pleodendione, (±)-hoaensieremodione, 4-epi-periconianone B, and their analogues have been accomplished for the first time. All the synthesized target compounds were screened in neural anti-inflammatory assays using LPS induced microglia cells (N9). Among them, compounds 1 and 21 were identified as potential lead compounds for further profiling.

/pdf/total-syntheses-and-biological-evaluation-of-5a96sx5tyy.pdf

Total Syntheses and Biological Evaluation of (±)-Botryosphaeridione, (±)-Pleodendione, 4-epi-Periconianone B, and Analogues

Several chiral amines bearing a heterocyclic moiety such as pyrrolidine, piperazine or tetrazole were prepared from L-phenylalanine. The enantioselectivity of the intramolecular asymmetric aldol reaction mediated by a combination of the synthetic chiral amine and a Bronsted acid to construct an enedione containing a seven-membered ring was examined in detail. A remarkable increase of enantioselectivity depending on the amount of Bronsted acid was observed.

A new chiral synthesis of a bicyclic enedione containing a seven-membered ring mediated by a combination of chiral amine and bronsted acid

........................................................................................................................................... i RESUMO .............................................................................................................................................. iii ACKNOWLEDGMENTS .................................................................................................................... v LIST OF PUBLICATIONS................................................................................................................ vii ABBREVIATIONS AND SYMBOLS ................................................................................................ ix GENERAL INDEX ............................................................................................................................ xiii INDEX OF FIGURES........................................................................................................................ xvi INDEX OF SCHEMES .................................................................................................................... xviii INDEX OF TABLES.......................................................................................................................... xix CHAPTER 1 ..............................................................................................................................

/pdf/search-for-bioactive-compounds-from-medicinal-plants-used-as-1yv8zd90hm.pdf

Search for bioactive compounds from medicinal plants used as antimalarials : the study of Momordica balsamina L.

(+)-(S) and (-)-(R)-5-methyl-Wieland-Miescher ketone (+)-1 and (-)-1, are important synthons in the diastereo and enantioselective syntheses of biological and/or pharmacological interesting compounds. A key step in these syntheses is the chemoselective C(1)O acetalization to (+)-5 and (-)-5, respectively. Various procedures for this transformation have been described in the literature. Among them, the classical procedure based on the use of 1,2-ethanediol and TsOH in refluxing benzene in the presence of a Dean-Stark apparatus. Within our work on bioactive natural products, it occurred to us to observe the partial racemization of (+)-5 in the course of the acetalization of (+)-1 by means of the latter methodology. Aiming to investigate this drawback, which, to our best knowledge, has no precedents in the literature, we acetalized with 1,2-ethanediol and TsOH in refluxing benzene and in the presence of a Dean-Stark apparatus under various experimental conditions, enantiomerically pure (+)-1. It was found that the extent of racemization depends on the TsOH/(+)-1 and 1,2-ethanediol/(+)-1 ratios. Mechanism hypotheses for this partial and unexpected racemization are provided.

https://www.mdpi.com/1422-0067/20/24/6147/pdf

Unexpected Racemization in the Course of the Acetalization of (+)-(S)-5-Methyl-Wieland–Miescher Ketone with 1,2-Ethanediol and TsOH under Classical Experimental Conditions

Bruceantin (1), a classical quassinoid with the highest reported antimalarial activity among the quassinoids examined thus far, was selected as a natural product lead for the design of a series of A/B-ring analogs. A viable strategy for the synthesis of the series was developed. The functionalized A-ring and the C-15 ester moiety in bruceantin are incorporated in all designed compounds. The preliminary bioassay results will be discussed in detail.

Synthesis of A/B-ring partial analogs of bruceantin as potential antimalarial agents.

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Synthesis of A/B-ring partial analogs of bruceantin as potential antimalarial agents.