A new nitrosyl ruthenium complex: Synthesis, chemical characterization, in vitro and in vivo antitumor activities and probable mechanism of action

This study describes the synthesis of a new ruthenium nitrosyl complex with the formula [RuCl(2)NO(BPA)] [BPA = (2-hydroxybenzyl)(2-methylpyridyl)amine ion], which was synthesized and characterized by spectroscopy, cyclic voltammetry, X-ray crystallography, and theoretical calculation data. The biological studies of this complex included in vitro cytotoxic assays, which revealed its activity against two different tumor cell lines (HeLa and Tm5), with efficacy comparable to that of cisplatin, a metal-based drug that is administered in clinical treatment. The in vivo studies showed that [RuCl2NO(BPA)] is effective in reducing tumor mass. Also, our results suggest that the mechanism of action of [RuCl(2)NO(BPA)] includes binding to DNA, causing fragmentation of this biological molecule, which leads to apoptosis. (C) 2011 Elsevier Masson SAS. All rights reserved.

Poly(epsilon-caprolactone)nanocapsules as carrier systems for herbicides: Physico-chemical characterization and genotoxicity evaluation

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Computational analysis and physico-chemical characterization of an inclusion compound between praziquantel and methyl-beta-cyclodextrin for use as an alternative in the treatment of schistosomiasis

Schistosomiasis is still an endemic disease in many regions, with 250 million people infected with Schistosoma and about 500,000 deaths per year. Praziquantel (PZQ) is the drug of choice for schistosomiasis treatment, however it is classified as Class II in the Biopharmaceutics Classification System, as its low solubility hinders its performance in biological systems. The use of cyclodextrins is a useful tool to increase the solubility and bioavailability of drugs. The aim of this work was to prepare an inclusion compound of PZQ and methyl-beta-cyclodextrin (MeCD), perform its physico-chemical characterization, and explore its in vitro cytotoxicity. SEM showed a change of the morphological characteristics of PZQ:MeCD crystals, and IR data supported this finding, with changes after interaction with MeCD including effects on the C-H of the aromatic ring, observed at 758 cm(-1). Differential scanning calorimetry measurements revealed that complexation occurred in a 1:1 molar ratio, as evidenced by the lack of a PZQ transition temperature after inclusion into the MeCD cavity. In solution, the PZQ UV spectrum profile in the presence of MeCD was comparable to the PZQ spectrum in a hydrophobic solvent. Phase solubility diagrams showed that there was a 5.5-fold increase in PZQ solubility, and were indicative of a type A(L) isotherm, that was used to determine an association constant (K(a)) of 140.8 M(-1). No cytotoxicity of the PZQ:MeCD inclusion compound was observed in tests using 3T3 cells. The results suggest that the association of PZQ with MeCD could be a good alternative for the treatment of schistosomiasis.

Physical and chemical characterization of yellow mangosteen fruits

O trabalho teve como objetivo a caracterização físico-química de frutos de mangostão amarelo (Garcinia xanthochymus Hook). Seis amostras de 25 frutos cada foram colhidas em plantas de mangostão amarelo do Banco Ativo de Germoplasma da Universidade Estadual Paulista e caracterizadas pela avaliação de diâmetro e altura, peso, percentagem e número de sementes por fruto, percentagem de casca, percentagem de polpa, sólidos solúveis (SS), acidez titulável (AT), vitamina C e relação SS/AT. O mangostão amarelo tem boas qualidades tecnológicas e é uma fonte intermediária de vitamina C com conteúdo médio de 120,33 mg/100g de fruta fresca.

Thermal study and physico-chemical characterization of some functional properties of guava seeds protein isolate (Psidium guajava)

The guava seed protein isolate ( PI) was obtained from the protein precipitation belonging to the class of the gluteline (Ip 4.5). The conditions for the preparation of the PI were determined by both the solubility curve and simultaneous thermogravimetry-differential thermal analysis (TG-DTA): pH 11.5, absence of NaCl and whiteners and T=( 25 +/- 3) degrees C. Under these conditions a yield of 77.0 +/- 0.4%, protein content of 94.2 +/- 0.3, ashes 0.50 +/- 0.05% and thermal stability, T= 200 degrees C, were obtained. The TG-DTA curves and the PI emulsification capacity study showed the presence of hydrophobic microdomains at pH 11.5 and 3.0 suggesting a random coil protein conformation and, to pH 10.0, an open protein conformation. The capacity of emulsification (CE), in the absence of NaCl, was verified for: 1 - pH 3.0 and 8.5, using the IP extracted at pH 10.0 and 11.5, CE >= 343 +/- 5 g of emulsified oil/g of protein; 2 - pH 6.60 just for the PI obtained at pH 11.5, CE >= 140 +/- 8 g of emulsified oil/g of protein.

SUGARCANE BAGASSE PULPING and BLEACHING: THERMAL and CHEMICAL CHARACTERIZATION

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Mechanical, physical, and chemical characterization of Ti-35Nb-5Zr and Ti-35Nb-10Zr casting alloys

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Chemical characterization of a dye processing plant effluent - Identification of the mutagenic components

This work shows the chemical characterization of a dye processing plant effluent that was contributing to the mutagenicity previously detected in the Cristais river, São Paulo, Brazil, that had an impact on the quality of the related drinking water. The mutagenic dyes Disperse Blue 373, Disperse Orange 37 and Disperse Violet 93, components of a Black Dye Commercial Product (BDCP) frequently used by the facility, were detected by thin layer chromatography (TLC). The blue and orange dyes were quantified by high performance liquid chromatography (HPLC/DAD) in a raw and treated effluent samples and their contribution to the mutagenicity was calculated based on the potency of each dye for the Salmonella YG1041. In the presence of S9 the Disperse Blue 373 accounted for 2.3% of the mutagenic activity of the raw and 71.5% of the treated effluent. In the absence of S9 the Disperse Blue 373 accounted for 1.3% of the mutagenic activity of the raw and 1.5% of the treated effluent. For the Disperse Orange 37, in the presence of S9, it contributed for 0.5% of the mutagenicity of the raw and 6% of the treated effluent. In the absence of S9; 11.5% and 4.4% of the raw and treated effluent mutagenicity, respectively. The contribution of the Disperse Violet 93 was not evaluated because this compound could not be quantified by HPLC/DAD. Mutagenic and/or carcinogenic aromatic amines were also preliminary detected using gas chromatograph/mass spectrometry in both raw and treated and are probably accounting for part of the observed mutagenicity. The effluent treatment applied by the industry does not seem to remove completely the multagenic compounds. The Salmomella/microsome assay coupled with TLC analysis seems to be an important tool to monitor the efficiency of azo dye processing plant effluent treatments. (c) 2006 Elsevier B.V. All rights reserved.

Isolation and chemical characterization of PwTx-II: A novel alkaloid toxin from the venom of the spider Parawixia bistriata (Araneidae, Araneae)

Brazil has many species of spiders belonging to Araneidae family however, very little is known about the composition, chemical structure and mechanisms of action of the main venom components of these spiders. The main objective of this work was to isolate and to perform the chemical characterization of a novel beta-carboline toxin from the venom of the spider Parawixia bistriata, a typical species of the Brazilian 'cerrado'. The toxin was purified by RP-HPLC and structurally elucidated by using a combination of different spectroscopic techniques (UV, ESI-MS/MS and H-1 NMR), which permitted the assignment of the molecular structure of a novel spider venom toxin, identified as 1-4-guanidinobutoxy-6-hydroxy-1,2,3,4-tetrahydro-beta-carboline, and referred to here as PwTx-II. This compound is toxic to insects (LD50 = 12 +/- 3 eta g/mg honeybee), neurotoxic, convulsive and lethal to rats (LD50 = 9.75 mg/kg of male Wistar rat). (c) 2005 Elsevier Ltd. All rights reserved.

Poly(hydroxybutyrate-co-hydroxyvalerate) microspheres loaded with atrazine herbicide: screening of conditions for preparation, physico-chemical characterization, and in vitro release studies

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Alternatives for the Treatment of Schistosomiasis: Physico-Chemical Characterization of an Inclusion Complex Between Praziquantel and Hydroxypropyl-beta-Cyclodextrin

"Alternatives for the Treatment of Schistosomiasis: Physico-Chemical Characterization of an Inclusion Complex Between Praziquantel and Hydroxypropyl-beta-Cyclodextrin". Praziquantel (PZQ) is the drug of choice commonly used for the treatment of shistosomiasis. However, it has low aqueous solubility, which could limit its bioavailability in the body. To circumvent these features, an inclusion complex with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was prepared. Thus, the objective of this work was to prepare and characterize the PZQ/HP-beta-CD inclusion complex. Morphological, spectroscopic, and calorimetric analysis showed the first signs of the guest/host interaction. The complexation kinetic analysis was used to determine the kinetic constant and, besides that, it was possible to establish the time consumed to reach equilibrium. Using the solubility isotherm, it was observed that the interaction with HP-beta-CD increased 2.4 fold the aqueous solubility of plain PZQ. In vitro cytotoxicity tests, using fibroblast cells, evidenced no toxicity for these cells at the concentrations tested. These results demonstrated that there is a potential use of PZQ in formulations with HP-beta-CD.

Physical-chemical characterization of processing tomato fruit

Fruit of 28 tomato cultivars for industrial processing were characterized to identify cultivars with potential for in natura consumption. The experiment was carried out in Jaboticabal-SP, Brazil (21o15'22'' South, 48o18'58'' West, altitude 595 m), on a Haplorthox soil during June-December. The cultivars used in this study were: H 7155, Hypeel 108, Andino, U 573, H 9036, Ipa 6, H 9494, AG 33, Yuba, RPT 1294, AG 72, Peelmech, Curicó, Hypeel 45, RPT 1478, H 9492, H 9498, H 2710, Hitech 45, Halley, Botu 13, H 9553, U 646, NK 1570, AG 45, RPT 1095, RPT 1570 and PSX 37511. The experimental design was randomized blocks, replicated four times. Ten fruits per plot were analyzed, evaluating the following characteristics: shape (oblong or round); length and diameter (mm); external and internal coloration; presence of fissures; number of loci; pulp thickness (mm); soluble solids content (Brix) and total acidity. Only cultivars Hypeel 108, AG 72, NK 1570, RPT 1570 had oblong fruit. Cultivars which had pulp thicker than 5.5 mm, a characteristic which is directly related to fruit yield for industrial purposes were: Ipa 6, Andino, U 646, H 9553, RPT 1294 and Hypeel 108. Cultivars Ipa 6 and Andino also presented elevated values for length, diameter and pulp thickness, indicating them as quality material for industry or, alternatively, for in natura market. Among the cultivars which presented better values for acidity (higher or equal to 0.3 g citric acid 100 g-1) were RPT 1095, AG 45, H 9553 and Hypeel 45.

Physical and chemical characterization of dovyalis fruits

The objective of this work was to establish physical and chemical characterizations of dovyalis hybrid fruits (Dovyalis abyssinica and D. hebecarpa). Samples of 25 fruits were characterized by evaluation of length and width, weight, percentage and number of seeds per fruit, peel percentage, pulp percentage, total soluble solids (TSS), titratable acidity (TA), vitamin C and TSS/TA ratio. Dovyalis fruit has good physical quality for market with an average of 75% pulp. Vitamin C content averaged 120.3 mg/100 g of fresh fruit, characterizing dovyalis as a good source of vitamin C. © 2005 by The Haworth Press, Inc. All rights reserved.

Chemical characterization and acaricide potential of essential oil from aerial parts of Tagetes patula L. (Asteraceae) against engorged adult females of Rhipicephalus sanguineus (Latreille, 1806)

Rhipicephalus sanguineus, commonly known as the brown dog tick, is one of the most widely distributed species of tick. In dogs, it can cause anemia and provide the transmission of pathogenic microorganisms such as Babesia canis, Ehrlichia canis, Hepatozoon canis, Anaplasma platys, and Mycoplasma haemocanis. To man, it can transmit the intracellular parasites Rickettsia rickettsii and Rickettsia conorii, the causative agents of the Rocky Mountain spotted fever in the Americas and Mediterranean and spotted fever in Europe and North Africa. Its control is performed by applying synthetic formulations composed of pyrethroids; however, continued use of these products results in environmental damage and acquisition of resistance. Alternatively, studies with botanical insecticides have been increasingly recurrent. Therefore, this study aimed to test the efficacy of essential oil of Tagetes patula, a ruderal species widely described in the literature for its insecticidal properties, in engorged females of R. sanguineus by the adults immersion test (AIT) and impregnated paper disk test (IPDT). The essential oil used, through gas chromatography coupled to mass spectrometry, revealed the presence of 55 compounds, being the 4-vinyl guaiacol and gamma terpinene the majority ones. The AIT compared to the IPDT was more efficient in inhibiting oviposition of tick; however, the eggs laid by the females submitted to saturated atmosphere with essential oil, from IPDT, not hatched, interrupted their development cycle. Besides being a pioneer work, the results presented here contributes to new researches, aiming the incorporation of essential oil in an acaricide for use in the environment. © 2013 Springer-Verlag Berlin Heidelberg.