Central nervous system and analgesic profiles of Lippia genus

Abstract Many people use medicinal plants to relieve disorders related to the central nervous system, such as depression, epilepsy, anxiety and pain, even though the effectiveness of most of them has not yet been proven through scientific studies. Plants of the Lippia genus, Verbenaceae, are widely used in ethnobotany as a food, for seasoning and in antiseptic remedies. They are also marketed and used for the treatment of different types of pain, including stomach ache, abdominal pain and headache, as well as being used as sedatives, anxiolytics and anticonvulsants. Despite their widespread use, there are no reviews on the central nervous system profile of plants of this genus. Therefore, the databases Medline-PubMed, Embase, Scopus and Web of Science were searched using the terms Lippia and biologic activity. Thirty-five papers were found. Eleven species of Lippia showed central nervous system activity, with leaves and the aerial parts of plants being the most commonly used, especially in aqueous and ethanol extracts or volatile oil. The species are composed mainly of terpenoids and phenylpropanoids, including polyketides, flavonoids and in less quantity some alkaloids. Although several species of Lippia present analgesic activity, most studies have not explored the mechanisms responsible for this effect, however, there is some evidence that volatile oils and constituents of the extracts may be responsible for the relief of some CNS disorders, but the effects on pain modulation seem to be the most exploited so far.

Natural products assessed in animal models for orofacial pain – a systematic review

ABSTRACT Orofacial pain is related to tissues of the head, face, neck and all the intraoral structures; it is rather debilitating to the patient and also difficult to treat. There are relatively few studies dedicated to the use of natural products to alleviate orofacial pain in preclinical experiment models (performed in experimental animals which provide support for clinical trials). Main objectives of the present systematic review summarize the studies on natural products assessed in animal models for orofacial pain seeking to give evidence to future development of new pharmaceutical products to manage the orofacial pain. Our review includes a thorough search of literature using the terms of orofacial pain, facial pain, medicinal plants and natural products. This search was performed using to retrieve English language articles in Medline-PubMed, Scopus and Web of Science. A total of eighteen studies were included in our survey for the inclusion criteria. Firstly, this review identified 210 citations from electronic search, after removal of duplicates and screening for relevant titles and abstracts, a total of eighteen articles were selected to the inclusion criteria established. Our findings suggest that natural products can be a promising or a trump tool for the development of new drugs to treat orofacial pain conditions, but the researchers that deal with experimental preclinical trials of new drugs (including natural products or synthetic drugs) for orofacial pain conditions urgently need to show translational evidence (with clinical approach) of these compounds.

ATIVIDADE ANTIMICROBIANA E EFEITO COMBINADO SOBRE DROGAS ANTIFÚNGICAS E ANTIBACTERIANAS DO FRUTO DE Morinda citrifolia L / Antimicrobial Activity and Combined Effects on Antifungal and Antibacterial Drugs the Fruit of Morinda citrifolia L / Actividad antimicrobiana y efecto combinado sobre medicamentos antifúngicos y antibacterianos del fruto de Morinda citrifolia L

O aparecimento de micro-organismos resistentes e a toxicidade associada aos fármacos antimicrobianos aumentam a necessidade de pesquisas por novos princípios ativos. Morinda citrifolia L., uma planta frutífera utilizada popularmente como antibacteriano e com diversos outros usos farmacológicos. Possui diversos metabólitos primários e secundários, principalmente flavonóides, triterpenóides e alcalóides. O presente trabalho visou testar o potencial antimicrobiano e modulador dos extratos do seu fruto. Os extratos do fruto foram testados quanto ao seu efeito antimicrobiano e em combinação com antibacterianos e antifúngicos contra microrganismos patógenos pelo método de microdiluição em caldo. Observou-se que as associações entre antibióticos e extratos mostraram resultados com relevância clínica diante dos testes com bactérias Pseudomonas aeruginosa e Escherichia coli.

The rising of the drug resistant microrganisms and the toxicity related with the antimicrobial drugs enhances the necessity about the search of new bioactive compounds. Morinda citrifolia L. is a fruit tree traditionally used as antibacterial and with several other pharmacological properties. This plant presents several phytocompounds as flavonoids, alkaloids and triterpenes. The objective of this work was assay the antimicrobial and modulatory potential of the fruit extract. The extract was assayed alone and associated with antibiotics and antifungals against pathogenic microrganisms using the microdilution assay. The results demonstrated that the association between extract and antimicrobial drugs resulted in a potentiation of the drug activity clinically relevant against Pseudomonas aeruginosa and Escherichia coli.

La aparición de microorganismos resistentes y la toxicidad asociada a los antimicrobianos aumenta la necesidad de investigar nuevos principios activos. Morinda citrifolia L., es una planta fructífera utilizada popularmente como antibacteriano y con otros diversos usos farmacológicos. Posee diversos metabolitos primarios y secundarios, principalmente flavonoides, triterpenoides y alcaloides. Este estudio tuvo como objetivo ensayar la potencial actividad antimicrobiana y moduladora de los extractos obtenidos de su fruta. Los extractos de las frutas fueron testados tanto para determinar el efecto antimicrobiano como también utilizándolo en combinación con agentes antibacterianos y antifúngicos contra microorganismos patógenos, por el método de microdilución en caldo. Se observó que la asociación entre antibióticos y extractos dió resultados clínicamente significativos en pruebas con bacterias Pseudomonas aeruginosa y Escherichia coli.

Avaliação da atividade anti-Trypanosoma e anti-Leishmania de Mentha arvensis e Turnera ulmifolia / Evaluation of the anti-Trypanosoma and anti-Leishmania activity of Mentha arvensis and Turnera ulmifolia

Tripanosomiasis or “Chagas disease”, caused by Trypanosoma cruzi, affect 10 million people in Latin America. Today, the chemotherapy is the only specific treatment against this disease, being the most used drugs the nifurtimox and benznidazole. Leishmaniasis is a disease caused by parasites of the genus Leishmania, mainly founded in regions with forests, as the Amazonia. Recent reports about the Leishmaniasis indicate a deficit of therapeutical drugs available against this disease and reinforce the necessity of the discovering of new drugs. An interesting approach against these diseases is the use of natural products, as the extracts of plants as Mentha arvensis and Turnera ulmifolia. For the in vitro assays against T. cruzi and Leishmania, was used the clone CL-B5 and promastigote forms, respectively. The cytotoxic assay was performed using fibroblasts. Our results indicated that M. arvensis was active against all strains assayed, inhibiting 65 e 47 percent of the assayed strains (IC50 = 192.3 and 531.9 ug/mL respectively), representing an interesting and alternative source of natural products with anti-kinetoplastida activity.

Doença de Chagas, causada por Trypanosoma cruzi, afeta cerca de 10 milhões de pessoas nas Américas. Atualmente, a quimioterapia é o único tratamento específico disponível para esta doença, onde os medicamentos utilizados são nifurtimox e benzonidazol. Leishmaniose tegumentar Americana no Brasil é causada por uma variedade de espécies de Leishmania e uma grande diversidade destes parasitos pode ser encontrada na Região Amazônica. Revisões recentes na quimioterapia de leishmaniose enfatizam as deficiências dos agentes terapêuticos atualmente disponíveis e mostram a necessidade urgente de novos candidatos. Uma alternativa para substituir esses medicamentos são extratos naturais de Mentha arvensis e Turnera ulmifolia. Foram preparados extratos etanólicos das folhas de M. arvensis e T. ulmifolia. Para os testes in vitro de T. cruzi, foi utilizado o clone CL-B5 e para Leishmania brasiliensis foram utilizadas formas promastigotas. O ensaio de citotoxicidade foi realizado com linhagens de fibroblastos. Nossos resultados indicam que M. arvensis foi eficaz contra as cepas de parasitos testadas apresentando 65 e 47 por cento de inibição em uma concentração de 500 ug/mL (respectivamente, CE50 = 192.3 e 531.9 ug/mL), sendo considerada uma fonte alternativa de produtos naturais com atividade contra T. cruzi e L. brasiliensis.

Desenvolvimento do algoritmo de classificação hierárquica (Winclus) e aplicação à série de derivados indol-2-carboxilato / Development of a Hierarquical Classification Algorithm (Winclus) and its application to a indole-2-carboxylate series

A Classificação Hierárquica ou Cluster Analysis é um tipo de reconhecimento de padrões aplicável ao planejamento de fármacos. Nesse trabalho, apresenta-se um modelo de classificação aglomerativa, de forma a agrupar substituintes com base nas similaridades dos seus parâmetros físico-químicos. Uma vez agrupados, estuda-se a relação entre o modelo de classificação hierárquica e as respostas biológicas dos compostos, a partir da Relação Quantitativa Estrutura-Atividade (QSAR). O método é representado por um novo algoritmo, denominado Winclus, para o qual foi desenvolvido um programa destinado à sua aplicação. Neste trabalho, é abordo o desenvolvimento do software e a aplicação do mesmo à série...