Applicability of eucalyptus wood waste extracts for the histological staining of connective tissue.

Biological staining of tissue is a crucial procedure in histotechnology. Rudimentary methods for section preparation have often used stains from natural products, although use of synthetic dyes has become the contemporary standard. Artificial dyes increase the operating costs of a laboratory as well as increase the environmental and personnel risks during manufacturing and usage. These considerations have stimulated research to find alternative natural stains from the wide diversity of plant species. The present study investigated the effect of Eucalyptus sp. (Myrtaceae) wood waste extract on histological staining of animal tissues, using a series of pigment concentrations, pH conditions, and temperatures. Eucalyptus wooden slivers were dried, milled, and 1 g, 2 g, and 4 g of the fine powder was subjected to 50% ethanol extraction for 2 days. Staining tests were then performed on formalin fixed paraffin embedded (FFPE) sections. Increasing acetic acid concentrations (1%, 2% and 4%) were added to the extracts and compared to an acid-free extract. Staining was performed at both ambient room temperature (RT) and 60°C. Connective tissue acidophilic components were well-contrasted and a hematoxylin counterstain demonstrated distinct structural differences between matrix and cell nuclei. Therefore, the present findings demonstrate the potential utility of the eucalyptus wood extracts application as a natural stain alternative for routine histology.

Bioceramic cement in the filling of bone defects in rats.

PURPOSE: To evaluate PBS®MCIMMO cement in the filling of bone defects. METHODS: Thirty-six adult male Wistar rats were divided into three groups of twelve individuals each (group 1, group 2 and group 3). In all groups, a bone failure in the femur was induced, 2.0 mm wide and 7.0 mm deep. In group 1, the PBS®MCIMMO cement was applied to the bone defect produced and a titanium implant (CONNECTION®) 1.5 mm thick and 6 mm long was installed. In group 2, only the PBS® CIMMO cement was installed. In group 3, only bone failure was performed. Kruskal Wallis tests were performed to compare the mean area among the three groups. RESULTS: In all comparisons, significance was observed for group 2 (p = 0.0014-0.0026). CONCLUSION: The PBS®CIMMO cement induced bone neoformation, and integration between the newly formed bone, cement, and implant was observed.

Bioceramic cement in the filling of bone defects in rats

Abstract Purpose To evaluate PBS®MCIMMO cement in the filling of bone defects. Methods Thirty-six adult male Wistar rats were divided into three groups of twelve individuals each (group 1, group 2 and group 3). In all groups, a bone failure in the femur was induced, 2.0 mm wide and 7.0 mm deep. In group 1, the PBS®MCIMMO cement was applied to the bone defect produced and a titanium implant (CONNECTION®) 1.5 mm thick and 6 mm long was installed. In group 2, only the PBS® CIMMO cement was installed. In group 3, only bone failure was performed. Kruskal Wallis tests were performed to compare the mean area among the three groups. Results In all comparisons, significance was observed for group 2 (p = 0.0014-0.0026). Conclusion The PBS®CIMMO cement induced bone neoformation, and integration between the newly formed bone, cement, and implant was observed.

Synthetic resveratrol-curcumin hybrid derivative inhibits mitosis progression in estrogen positive MCF-7 breast cancer cells.

Curcumin (1) and resveratrol (2) are bioactive natural compounds that display wide pharmacological properties, including antitumor activity. However, their clinical application has been limited due to their low solubility and bioavailability. Nevertheless, independent studies have considered these compounds as interesting prototypes for developing new chemical structures useful for anticancer therapy. Here in, we report the synthesis of novel curcumin-like hydrazide analogues (3a and 3b), and a series of curcumin-resveratrol hybrid compounds (4a-f), and the evaluation of their cytotoxic potential on three tumor cell lines MCF-7 (breast), A549 (lung), and HepG2 (liver). Cell viability was significantly reduced in all tested cell lines when compounds 4c-4e were used. The IC50 values for these compounds on MCF-7 cells were lower than those for curcumin, resveratrol, or curcumin combined with resveratrol. We evidenced that 4c promoted a drastic increase of G2/M population. The accumulation of cells in mitosis onset in treated cultures was due to, at least in part, the ability of 4c to modulate nuclear kinase proteins, which orchestrate important events in mitosis progression. We have also observed significant reduction of the relative RNAm abundance of CCNB1, PLK1, AURKA, AURKB in samples treated with 4c, with concomitant increase of CDKN1A (p21). Thus, compound 4c is a promising multi-target antitumor agent that should be considered for further in vivo studies.

Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates.

A new series of sixteen multifunctional N-benzyl-piperidine-aryl-acylhydrazones hybrid derivatives was synthesized and evaluated for multi-target activities related to Alzheimer's disease (AD). The molecular hybridization approach was based on the combination, in a single molecule, of the pharmacophoric N-benzyl-piperidine subunit of donepezil, the substituted hydroxy-piperidine fragment of the AChE inhibitor LASSBio-767, and an acylhydrazone linker, a privileged structure present in a number of synthetic aryl- and aryl-acylhydrazone derivatives with significant AChE and anti-inflammatory activities. Among them, compounds 4c, 4d, 4g and 4j presented the best AChE inhibitory activities, but only compounds 4c and 4g exhibited concurrent anti-inflammatory activity in vitro and in vivo, against amyloid beta oligomer (AßO) induced neuroinflammation. Compound 4c also showed the best in vitro and in vivo neuroprotective effects against AßO-induced neurodegeneration. In addition, compound 4c showed a similar binding mode to donepezil in both acetylated and free forms of AChE enzyme in molecular docking studies and did not show relevant toxic effects on in vitro and in vivo assays, with good predicted ADME parameters in silico. Overall, all these results highlighted compound 4c as a promising and innovative multi-target drug prototype candidate for AD treatment.

Alkaloids derived from flowers of Senna spectabilis, (-)-cassine and (-)-spectaline, have antiproliferative activity on HepG2 cells for inducing cell cycle arrest in G1/S transition through ERK inactivation and downregulation of cyclin D1 expression.

Cancer is one of the most critical problems of public health in the world and one of the main challenges for medicine in this century. Unfortunately, most patients are diagnosed at advanced stage, when the treatment options are palliative. Consequently, the search for novel therapeutic options is imperative. In the context, the plants represent an important source for discovering of novel compounds with pharmacological potential including antineoplastic agents. Herein, we aimed to investigate in vitro antiproliferative and cytotoxic potentials of an alkaloid mixture derived from Senna spectabilis, (−)-cassine (1) and (−)-spectaline (2). These alkaloids reduced cell viability in a concentration-dependent manner of six tumor cell lines. From initial screening, HepG2 cells were selected for further investigations. We show that alkaloids 1/2 have an important antiproliferative activity on HepG2 cells due to their ability in inducing cell cycle arrest in G1/S transition. This effect was associated to ERK inactivation and down-regulation of cyclin D1 expression. In addition, we evidenced a disruption of the microfilaments and microtubules in a consequence of the treatment. Taken together, the data showed by the first time that alkaloids 1/2 strongly inhibit cell proliferation of hepatocellular carcinoma cells. Therefore, they represent promise antitumor compounds against liver cancer and should be considered for further anticancer in vivo studies.