Pyroligneous extracts with therapeutic action: A technological prospect

Abstract The Pyroligneous extract is a product from the combustion of plant biomass with applications in the fields of health, industrial chemistry, and agriculture. The discovery of new molecules with therapeutic potential and of natural origin continues to be one of the great challenges for research centres around the world. The following work aims to analyze, through a technological prospection, the use of pyroligneous extracts for therapeutic purposes. To carry out the study, searches were carried out in documents deposited in Brazil, Europe, and the United States and searched on platforms specialized in patents. The number of inventions using pyroligneous extract with therapeutic applications is still quite small, however, innovations have been observed for the treatment of diseases of great clinical relevance such as cancer and hypertension. The systematic mapping of innovations is of great importance for the development of new technologies.

Technological Prospecting: Mapping Patents on L-asparaginases from Extremophilic Microorganisms.

BACKGROUND: L-asparaginase (L-ASNase, L-asparagine amidohydrolase, E.C.3.5.1.1) is an enzyme with wide therapeutic applicability. Currently, the commercialized L-ASNase comes from mesophilic organisms, presenting low specificity to the substrate and limitations regarding thermostability and active pH range. Such factors prevent the maximum performance of the enzyme in different applications. Therefore, extremophilic organisms may represent important candidates for obtaining amidohydrolases with particular characteristics desired by the biotechnological market. OBJECTIVES: The present study aims to carry out a technological prospecting of patents related to the L-asparaginases derived from extremophilic organisms, contributing to pave the way for further rational investigation and application of such enzymes. METHODS: This patent literature review used six patents databases: The LENS, WIPO, EPO, USPTO, Patent Inspiration, and INPI. RESULTS: It was analyzed 2860 patents, and 14 were selected according to combinations of descriptors and study criteria. Approximately 57.14% of the patents refer to enzymes obtained from archaea, especially from the speciesPyrococcus yayanosii (35.71% of the totality). CONCLUSION: The present prospective study has singular relevance since there are no recent patent reviews for L-asparaginases, especially produced by extremophilic microorganisms. Although such enzymes have well-defined applications, corroborated by the patents compiled in this review, the most recent studies allude to new uses, such as the treatment of infections. The characterization of the catalytic profiles allows us to infer that there are potential sources still unexplored. Hence, the search for new L-ASNases with different characteristics will continue to grow in the coming years and, possibly, ramifications of the technological routes will be witnessed.

Citrus limon (L.) Burm f. Essential Oil Has Anxiolytic and Sedative Properties by Modulating GABAA-Receptors

Abstract The high prevalence of anxiety disorders associated with pharmacotherapy side effects have motivated the search for new pharmacological agents. Species from Citrus genus, such as Citrus limon (sicilian lemon), have been used in folk medicine as a potential therapy to minimize emotional disorders. In order to searching for new effective treatments with fewer side effects, the present study evaluated the anxiolytic mechanism of action and the hypnotic-sedative activity from the Citrus limon fruit's peels essential oil (CLEO). Adults male Swiss mice were submitted to barbiturate-induced sleep test; elevated plus-maze (EPM) and light-dark box (LDB) (evaluation of the mechanism of action); rotarod; and catalepsy tests. CLEO oral treatment decreased latency and increased the sleep total time; moreover it induced in animals an increased the number of entries and percentage of time spent into open arms of the EPM; an increased the number of transitions and the percentage of time into light compartment in the LDB; which were only antagonized by flumazenil pretreatment, with no injury at motor function. Thus, results suggest that CLEO treatment induced an anxiolytic behavior suggestively modulated by the benzodiazepine binding site of the GABAA receptor or by an increase of GABAergic neurotransmission, without cause impairment in the motor coordination.

Melatonin receptor 1B -1193T>C polymorphism is associated with diurnal preference and sleep habits.

BACKGROUND: Melatonin modulates the master circadian clock through the activation of G-protein-coupled receptors MT1 and MT2. It is presumed, therefore, that genetic variations in melatonin receptors can affect both sleep and circadian phase. We investigated whether the -1193T > C (rs4753426) polymorphism in the promoter of MT2 receptor gene (MTNR1B) is associated with diurnal preference and sleep habits. This polymorphism was previously associated with sunshine duration, suggesting a role in circadian entrainment. METHODS: A total of 814 subjects who completed the Morningness-Eveningness and the Munich Chronotype questionnaires were genotyped for the selected polymorphism. Linear and multinomial regression were performed to test the interaction between gene variants and diurnal preference/sleep habits. RESULTS: The -1193C variant was associated with the extreme morningness phenotype in a codominant model (C/C vs. T/T), recessive model (C/C + C/T vs. T/T) and alleles (C vs. T). A negative correlation was found between -1193C alleles and social jetlag scores. The frequency of -1193T allele was higher in the group that stay in bed more than 8 h/night compared to the group that stay in bed less than 8 h/night on weekends. CONCLUSION: To the best of our knowledge, these data provide the first insights into the role of MTNR1B gene in the regulation of sleep, biological rhythms, and entrainment in humans.

The Antinociceptive Effect of the Leaves and Flowers Ethanolic Extracts of Tabebuia aurea (Silva Manso) Benth & Hook. F. ex S. Moore

ABSTRACT In view of the traditional use of Tabebuia aurea for treating pain and inflammation, the antinociceptive pharmacological potential of T. aurea ethanolic extracts (TAEE) was investigated through in vivo experimental models. First, the MTT assay was conducted to determine the potential cytotoxicity of the TAEEs. Afterwards, the acetic acid-induced writhing test and the formalin-, and glutamate-induced nociception tests were performed on Swiss adult mice treated with TAEEs (100 and 200 mg/kg doses, p.o.), or saline solution (control groups, 10mL/kg, p.o.), or standard drugs: dipyrone 40 mg/kg (p.o.), and morphine 5,7 mg/kg (i.p). In the MTT assay, none of the tested concentrations demonstrated signals of cytotoxicity. In the in vivo experimental models of acetic acid-induced writhing and glutamate-induced nociception, all TAEEs doses were able to statistically reduce the nociceptive response. However, the TAEEs did not show significant decrease in the amount of time that the animals spent licking the stimulated paw in the neurogenic phase of formalin-induced nociception test, differently of what was observed in the inflammatory phase. The results showed that T. aurea species induce an antinociceptive effect in rodents, which encourages the study of new drugs and contributes to the research on natural products.

Antibioticoprofilaxia em gestantes submetidas à cesariana / Antibiotic prophylaxis in parturients undergoing cesarean section

Objetivo: analisar o uso da antibioticoprofilaxia em gestantes submetidas à cesariana. Método: estudo transversal, realizado com 855 puérperas em maternidades. Os dados foram processados no programa EpiInfo, versão 3.2.2, e transportados para um banco de dados informatizados com a utilização do programa Microsoft Excel. Resultados: a prevalência de infecção puerperal encontrada foi de 6,8%, entretanto, verifica-se ainda que das 89,1% puérperas que fizeram uso de esquema profilático, apenas 6,1%desenvolveram infecção puerperal, prevalência menor que a encontrada entre as mulheres que não fizeram uso do esquema (13,0%) (p=0,012), demonstrando, assim, efetividade da antibioticoprofilaxia na prevenção de infecção puerperal. Conclusão: o uso da antibioticoprofilaxia reduz risco de infecção puerperal grave. A sua interrupção nas gestantes submetidas à cesariana pode aumentar as chances de morbidade grave e até mesmo de mortalidade materna.

Caracterização das mulheres que realizaram o aborto após gravidez indesejada / Characterization of women who carried out abortion after undesirable pregnancy

Objetivo: caracterizar o perfil das mulheres internadas em maternidades de referência após aborto de gravidez indesejada. Método: estudo transversal, de abordagem quantitativa, realizado com 855 puérperas em nove maternidades públicas. Os dados foram processados pelo programa Epi Info, versão 3.2.2, e transportados para um banco de dados do Microsoft Excel 2007. Resultados: com relação à saúde reprodutiva das puérperas pesquisadas, apenas 50,8% delas mencionaram a utilização de algum método contraceptivo, destacando-se os anticoncepcionais orais, com 47,4% de adesão; 73% nunca abortaram. Dentre as que abortaram, constatou-se que, em 75% delas, tal fato ocorreu uma única vez; 33,2% confirmaram ter sido induzido; e 66,8% relataram ser espontâneo. Conclusão: as mulheres que praticam o aborto são mulheres com fator socioeconômico baixo que ainda veem o aborto como forma de planejamento familiar recorrendo a essa prática quando se veem em uma situação em que a gravidez não é desejada.

3-Aminothiophene-2-acylhydrazones: non-toxic, analgesic and anti-inflammatory lead-candidates.

Different chemotypes are described as anti-inflammatory. Among them the N-acylhydrazones (NAH) are highlighted by their privileged structure nature, being present in several anti-inflammatory drug-candidates. In this paper a series of functionalized 3-aminothiophene-2-acylhydrazone derivatives 5a-i were designed, synthesized and bioassayed. These new derivatives showed great anti-inflammatory and analgesic potency and efficacy. Compounds 5a and 5d stand out in this respect, and were also active in CFA-induced arthritis in rats. After daily treatment for seven days with 5a and 5d (50 µmol/Kg), by oral administration, these compounds were not renal or hepatotoxic nor immunosuppressive. Compounds 5a and 5d also displayed good drug-scores and low risk toxicity calculated in silico using the program OSIRIS Property Explorer.