Molecular hybridization: A useful tool in the design of new drug prototypes

Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hyrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can results in compounds presenting modified selectivity profile, different and/or dual modes of action and reduced undesired side effects. So, in this described several example of different strategies for drug design, discovery and pharmacomodulation focused on new innovative hybrid compounds presenting analgesic, anti-inflammatory, platelet anti-aggregating, anti-infections, anticancer, cardio- and neuroactive properties.

Anthracycline-induced cardiotoxicity

The anthracyclines constitute a group of drugs widely used for the treatment of a variety of human tumors. However, the development of irreversible cardiotoxicity has limited their use. Anthracycline-induced cardiotoxicity can persist for years with no clinical symptoms. However, its prognosis becomes poor after the development of overt heart failure, possibly even worse than ischemic or idiopathic dilated cardiomyopathies. Due to the successful action of anthracyclines as chemotherapic agents, several strategies have been tried to prevent/ attenuate their side effects. Although anthracycline-induced injury appears to be multifactorial, a common denominator among most of the proposed mechanisms is cellular damage mediated by reactive oxygen species. However, it remains controversial as to whether antioxidants can prevent such side effects given that different mechanisms may be involved in acute versus chronic toxicity. The present review applies a multisided approach to the critical evaluation of various hypotheses proposed over the last decade on the role of oxidative stress in cardiotoxicity induced by doxorubicin, the most used anthracycline agent. The clinical diagnosis and treatment is also discussed. © 2008 Bentham Science Publishers Ltd.

Dietary α-tocopheryl acetate on fillet quality of tilapia

This work compared the effects of dietary α-tocopheryl acetate on storage life of tilapia fillets. Three experimental diets containing increasing a-tocopherol levels (zero, 100, and 200 mg kg-1) were used. The fish, with a mean initial weight of 184.23 ± 1.68 g, were fed diets for 63 days. After that period, they were slaughtered, filleted, and the fillets were grounded to accelerate lipid oxidation. Fish growth, survival, fillet yield, chemical composition and lipid oxidation of tilapia ground fillets were evaluated 0, 30 and 60 days after frozen storage. The results demonstrated that there was no significant difference between treatments for performance, and also, tocopherol did not influence the chemical composition values of fillets. Increased tocopherol levels in the feeds promoted a reduction in ground fillets lipid oxidation values.

Eugenia dysenterica DC: Actividad antioxidante, Perfil de ácidos grasos y determinación de tocoferoles

This work aimed to characterize the proximate composition, antioxidant activity and fatty acids profile and tocopherol composition of the oil from Eugenia dysenterica DC seeds. To obtain the extract, the dehydrated and triturated seeds were extracted with ethyl alcohol for 30 minutes, at a proportion of 1:3 of seeds:ethyl alcohol, under continuous agitation at room temperature. Afterwards, the mixture was filtered and the supernatant was dehydrated at 40°C in order to determine by direct weighing the dry matter yield of the extract. The cagaita seeds showed to be an important source of total carbohydrates, had relevant antioxidant activity and a high content of total phenolic compounds. In comparison to other oils and fats, cagaita seeds oil do not constitutes a good source of tocopherols.

Proximate composition of guariroba (Syagrus oleracea), jerivá (Syagrus romanzoffiana) and macaúba (Acrocomia aculeata) palm fruits

This study aimed to characterize the pulp and kernel of guariroba (Syagrus oleracea), jerivá (Syagrus romanzoffiana) and macaúba (Acrocomia aculeata) palm fruits, through their proximate composition, carotenoids contents and tocopherol composition. The three kernels showed to be composed mainly of lipids and proteins, as the three pulps, of carbohydrate and fiber. In the kernels the levels of lipids ranged from 45.17 to 56.37% and proteins from 15.46 to 28.61%. In the pulps the total fiber content ranged from 20.26 to 26.98%. The pulps also presented a significant amount of ash, which represents a significant mineral content, especially in the guariroba (5.16%). Moreover, the pulp oils showed higher carotenoids and tocopherol contents. The jerivá pulp oil contained carotenoid and tocopherol on average 1219 μg/g and 323.50. mg/kg, respectively. The consumption of the whole fruit, pulp, and kernel supplies important quantities of many necessary nutrients for human diet, including vitamins A and E. © 2011 Elsevier Ltd.

ANTIOXIDANT ACTIVITY OF ROSEMARY EXTRACT IN SOYBEAN OIL UNDER THERMOXIDATION

This study examined the antioxidant activity of lyophilized rosemary extract added to soybean oil, subjected to thermoxidation conditions and also its synergistic effect with the synthetic antioxidant tertiary butylhydroquinone (TBHQ). Soybean oil samples with no antioxidant added (SO), 3,000mg/kg rosemary extract (RE), 50mg/kg TBHQ (TBHQ), and a mixture of those two antioxidants (RE+TBHQ) were heated to 180C for 20h. After 0, 10 and 20h, the oxidative stability, total polar compounds, tocopherol content and fatty acid profile were determined. The addition of rosemary extract increased oxidative stability and resulted in a lower formation of total polar compounds and a higher retention of tocopherols. The RE treatment showed the highest amount of polyunsaturated fatty acids after 20h. There was not any synergy between TBHQ and rosemary extract in preventing oxidation of soybean oil. Rosemary extract showed a higher antioxidant potential when compared with TBHQ. PRACTICAL APPLICATIONS: Antioxidants are important ingredients in food processing because they have the capacity to protect foods, containing oils and fats, from damage caused by free radicals and reactive oxygen species. Synthetic antioxidants are widely used in the food industry; however, their utilization has been questioned because of toxicity. Therefore, there is a growing interest in the use of natural antioxidants to reduce or replace the synthetic antioxidants. Several species are used in cooking, medicine and by the pharmaceutical industry, standing out the rosemary. Being rich in compounds with high antioxidant activity, the rosemary extract can be used to replace synthetic antioxidants used in vegetable oils. © 2012 Wiley Periodicals, Inc.

Soursop (Annona muricata L.) and sugar apple (Annona squamosa L.): Antioxidant activity, fatty acids profile and determination of tocopherols

Purpose: This study aims to analyze the soursop and sugar apple seeds as to its composition, to evaluate the antioxidant potential of seeds extract and characterize the oil extracted from them, regarding the fatty acids profile and content of tocopherols. Design/methodology/approach: To obtain the extracts, dried and crushed seeds were extracted with ethanol for 30 minutes, at a ratio of 1:3 (m/m, seed: ethyl alcohol) under continuous stirring at room temperature. Then, the mixture was filtered and the supernatants subjected to rotoevaporator at 40°C aiming to determine, by direct weighing, the yields of dry extracts. Findings: According to the results, the soursop and sugar apple seeds constituted significant sources of lipids, proteins and carbohydrates and can therefore be used in food and feed, and offer relevant antioxidant activity of phenolic compounds. The oil seeds are a good source of unsaturated fatty acids, especially oleic and linoleic acids and they have significant amounts of total tocopherol. Research limitations/implications: Implications are the identification of bioactive compounds extracted from seeds of tropical and subtropical fruits, and to prevent certain types of diseases. Practical implications: The information presented might be directly used for developing of functional foods such as fruits. Originality/value: The article tries to identify new source of compounds extracted from fruits. © Emerald Group Publishing Limited.

Chemical composition and antioxidant activity of dried powder formulations of Agaricus blazei and Lentinus edodes

Several mushroom species have been pointed out as sources of antioxidant compounds, in addition to their important nutritional value. Agaricus blazei and Lentinus edodes are among the most studied species all over the world, but those studies focused on their fruiting bodies instead of other presentations, such as powdered preparations, used as supplements. In the present work the chemical composition (nutrients and bioactive compounds) and antioxidant activity (free radical scavenging activity, reducing power and lipid peroxidation inhibition) of dried powder formulations of the mentioned mushroom species (APF and LPF, respectively) were evaluated. Powder formulations of both species revealed the presence of essential nutrients, such as proteins, carbohydrates and unsaturated fatty acids. Furthermore, they present a low fat content (<2 g/100 g) and can be used in low-calorie diets, just like the mushrooms fruiting bodies. APF showed higher antioxidant activity and higher content of tocopherols and phenolic compounds (124 and 770 μg/100 g, respectively) than LPF (32 and 690 μg/100 g). Both formulations could be used as antioxidant sources to prevent diseases related to oxidative stress. © 2012 Elsevier Ltd. All rights reserved.

Physicochemical and bioactive properties of Hymenaea courbaril L. pulp and seed lipid fraction

This study aimed to assess the nutritional composition of the fruit and the physicochemical and bioactive properties of jatoba (Hymenaea courbaril L.) pulp and seed oils. The lipid content of both fractions was below 6%. There was a significant presence of minerals, especially, sodium, potassium and phosphorus. The main macronutrient in pulp and seed was crude fiber, and considerable amounts of Vitamin C, 51.87 and 121.45. mg/100. g respectively, were found. The physicochemical properties demonstrated the good quality of the oils. The oxidative stability index was influenced by the composition of fatty acids reaching a value of 45.97. h for the jatoba pulp oil. The most abundant bioactive compounds were α-tocopherol (886.37 and 993.63. mg/kg) and β-sitosterol (61.83 and 91.09. mg/kg) for pulp and seed oils, respectively. Among the unsaturated fatty acids in the pulp, the oleic (46.09%) and linolenic acid (14.54%) stood out. The pulp and seed oils can be considered a valuable source for new industrial, cosmetic and pharmaceutical products. © 2013 Elsevier B.V.

Fatty acids and some antioxidant compounds of Psidium guajava seed oil

Physico-chemical characteristics, fatty acid and tocopherol compositions, total phenolic content and antioxidant activity of crude oil extracted from guava (Psidium guajava var. pomifera) seeds were investigated. Oil yield from the seeds was 14.0%. Data obtained for the analytical indexes compared well with those of others edible oils. The oil showed high levels of unsaturated fatty acids (88.1%), mainly linoleic acid (78.4%). The tocopherol and total phenolic contents in the oil amounted to 29.2 and 92.3 mg/100 g, respectively. The guava seed oil exhibited a great DPPH · scavenging activity showing EC₅₀ of 12.9 g oil/g [DPPH · ] -1 and antiradical efficiency of 7.9×10 -2 . Therefore, the potential utilization of the guava seed oil as a raw material of food, chemical and pharmaceutical industries appears to be favourable and provides the use of a renewable resource, adding value to agricultural products.

Efeito do tocoferol no desempenho e na estabilidade lipidica da tilápia nilotica (Oreochromis niloticus)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Influência da adição in vivo de vitamina E e de métodos de abate nos atributos de qualidade de filés de tilápia

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Análise vibracional do α-tocoferol

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Ação antioxidante de alfa-tocoferol e extrato de alecrim em óleo de soja submetido à termoxidação

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

Caracterização dos frutos e dos óleos extraídos da polpa e amêndoa de guariroba (Syagrus oleracea), Jerivá (Syagrus romanzoffiana) e macaúba (Acromia aculeata)

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