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PubMed2006

Synthesis of compounds with antiproliferative activity as analogues of prenylated natural products existing in Brazilian propolis.

This work describes the syntheses and antitumoral properties of five prenyl compounds from which antiproliferative activities were predicted by using the TOPS-MODE approach, a computational method for drug design. The syntheses of 2-(3-methylbut-2-enyloxy)acetophenone (2), 2-hydroxy-5-(3-methylbut-2-enyl)acetophenone (3), 2-hydroxy-3-(1,1-dimethylallyl)acetophenone (4), and 5-(3-methylbut-2-enyl)-2-(3-methylbut-2-enyloxy)acetophenone (5) were realized by O-prenylation of phenolic compounds with prenyl bromide and by Claisen rearrangement, respectively. Reaction of 2-hydroxy-5-(3-methylbut-2-enyl)acetophenone 3 under Vilsmeier-Haack conditions with phosphoryl chloride and N,N-dimethylformamide yielded 6-(3-methylbut-2-enyl)chromone-3-carbaldehyde (6). The compounds were tested for their cytotoxicity toward a diverse panel of cultured human tumor cell lines. Compound 3 showed significant selective cytotoxic activity (IC(50) < 9 microg/ml).

Acetophenones↗
PubMed2006

Role of caffeic acid phenethyl ester, an active component of propolis, against NAOH-induced esophageal burns in rats.

OBJECTIVES: This study was evaluated to investigate the efficacy of caffeic acid phenethyl ester (CAPE), which is a natural honeybee product exhibits a spectrum of biological activities including anti-microbial, anti-inflammatory, antioxidant and anti-tumoral actions, on the prevention of stricture development after esophageal caustic injuries in the rat. METHODS: Thirty healthy male Wistar albino rats were utilized in this study. The rats were randomly allotted into one of three experimental groups: group A (sham) animals were uninjured. Caustic esophageal burn was created by applying 1 ml 37.5% NaOH to the distal esophagus. Group B rats were injured but untreated. Group C rats were injured and received CAPE (10 micromol/kg/day i.p. for 28 days). Efficacy of the treatment was assessed by measuring the esophageal transit time, stenosis index, histopathologic damage score and biochemically by determining tissue hydroxyproline content, lipid peroxidation and antioxidant enzyme activities. RESULTS: The esophageal transit time, the stenosis index, histopathologic damage score and the hydroxyproline level were significantly increased in the untreated group compared with the sham and CAPE-treated groups. Treatment with CAPE decreased tissue hydroxyproline levels, histological damage, and the stenosis index, but except the esophageal transit time. Caustic esophageal burn also increased the lipid peroxidation and decreased the antioxidant enzyme activities in the untreated group. CAPE treatments decreased the elevated lipid peroxidation and also increased the reduced antioxidant enzyme activities. In corrosive esophageal burn group with no treatment, the most consistent findings were degenerative changes and increased in submucosal collagen content, and the luminal narrowing. CAPE treatment protected esophagus. Nevertheless, there was the slight increase in submucosal collagen. CONCLUSIONS: It is concluded that CAPE has a preventive effect on the stricture development after esophageal caustic injuries in the rat.

Animals↗
PubMedDate not supplied

[Early results in the treatment of Legg-Calvé-Perthes disease using intra-articular injections of aqueous propolis extract].

Authors presented results in conservative treatment of 54 cases of hip joint with aseptic necrosis of thigh bone. In 22 hips, excluding the typical conservative treatment, EEP injections were given. However, in the remaining 32, different forms of relieve were used. The obtained results in the first group (A) confirm the purpose of enrichment in conservative treatment by adapting intra- articular injections of EEP especially in advanced stages of necrosis (III-IV period of illness) and also in those whose parents did not express their consent on surgery in the early stage of the illness.

Child↗