Identification Of Phenyl Alanine Ammonia Lyase Gene Involved In The Synthesis Of Anacardic Acid In Anacardium Occidentale L.

Anacardic acids, a class of medicinally and industrially important phenolic compounds is found in a variety of dicotyledonous families chiefly in Cashew (Anacardium occidentale L). Phenylalanine ammonia-lyase (PAL) shows a dominant role in the biosynthesis of poly phenolic compounds, which are involved in the defense mechanism in harsh environments related to various stimuli. The current study was conducted to find out the presence of anacardic acid in ethyl acetate extract of young leaves of cashew using high performance thin layer chromatography (HPTLC) method and the presence of phenyl alanine ammonia lyase gene also plays a role in the biosynthesis of anacardic acid in young leaves was also confirmed by cDNA synthesis from a cellular mRNA template connected to the polymerase chain reaction (PCR).

Antiplasmodial evaluation of Anacardium occidentale and alkyl-phenols

Abstract The ethanol crude extract from cashew (Anacardium occidentale L. Anacardiaceae) displayed significant antiplasmodial activity (IC50 0.577 µg/ml). Liquid chromatography-high resolution Mass spectrometry analysis was performed to identify the main compounds existing in the ethanol extract. The occurrence of anacardic acids, cardols, and 2-methylcardols derivatives was confirmed in the extract. The IC50 obtained, when the main isolated compounds were evaluated in Plasmodium falciparum D6 strain, ranged from 5.39 µM to >100 µM. Tested here for the first time, the data showed that cardol triene 1 (IC50 = 5.69 µM) and 2-methylcardol triene 4 (IC50 = 5.39 µM) demonstrated good antimalarial activity. In conclusion, Anacardium occidentale nuts presented relevant biological potential, and further studies should be considered.

Antifungal potential of cashew nut shell liquid in the control of plant pathogens / Potencial antifúngico do líquido da castanha de caju no controle de fitopatógenos

Extracted from the fruit of Anacardium occidentale L., Cashew Nut Shell Liquid (CNSL) is a phenolic lipid that has potential biological use. Conventional pesticides are increasingly being replaced by natural products because of the impact that their mismanagement can have on human health and the environment. The objective of this work was to evaluate the fungicidal potential effect of CNSL on the fungi Colletotrichum gloesporioides and Lasiodiplodia theobromae, in particular its use in reducing negative impacts on fruit production. Chemical and physical tests were conducted to determine features of the sample, such as pH, electrical conductivity and solubility, and to measure its anacardic acid content. In vitro and in vivo tests were also conducted to evaluate the inhibition of mycelial growth on papaya fruit, the identification of volatile components and the inhibition of spore production. CNSL had the highest fungicidal potential for both fungi in vitro at a concentration of 320 µg mL-1, and the same concentration was also maximal for sporulation inhibition in both fungi. In the in vivo tests the protective effect of CNSL was higher for C. gloesporioides fungus, whereas its curative effect was higher for L. theobromae. It was found that the substance with fungicidal potential was non-volatile and that the presence of the pathogens altered the chemical properties of the fruit.

O Líquido da Castanha de Caju é um lipídio fenólico extraído do fruto da Anacardium occidentale L. que demonstra ter potencial de uso biológico. A substituição dos agrotóxicos convencionais por produtos naturais vem aumentando devido aos impactos que o mau manejo pode acarretar a saudade humana e ao meio ambiente. Este trabalho objetivou avaliar o potencial fungicida deste produto frente aos fungos Colletotrichum gloesporioides e Lasiodiplodia theobromae por sua importância nos impactos negativos na produção frutífera. Foram realizados testes químicos e físicos para determinar o padrão da amostra como: pH, condutividade elétrica, solubilidade e determinação do teor de ácido anacárdico na amostra. Para os ensaios biológicos foram realizados testes de inibição do crescimento micelial in vitro e em in vivo em frutos de mamões, determinação de compostos voláteis e inibição da produção de esporos. O LCC apresentou maior potencial fungicida no teste in vitro na concentração de 320 µg mL-1 para ambos os fungos, nesta mesma concentração ocorreu a maior inibição da esporulação tanto para o C. gloesporioides quanto para o L. theobromae. No teste realizado in vivo ocorreu maior inibição para o fungo C. gloesporioides no tratamento protetor e para o fungo L. theobromae o tratamento curativo foi mais eficaz. Constatou-se que a substância com potencial fungicida não é volátil e a presença do patógeno altera os padrões químicos do fruto.

Estudo de síntese e estabilidades química e enzimática de fármaco dirigido dendrimérico potencialmente ativo em doença de Chagas / Synthesis, chemical and enzymatic stability studies of targeted dendrimer potentially active in Chagas disease

A doença de Chagas representa um problema de saúde pública em muitos países e regiões. O tratamento consiste em fármacos tóxicos, com eficácia discutível, principalmente, na fase crônica da doença. Assim, faz-se necessário o planejamento de novos quimioterápicos, mais seguros e eficazes. Os dendrímeros são novas arquiteturas moleculares formadas por um foco central e ramificações partindo desse foco. Apresentam diversas aplicações biológicas como, por exemplo, atuar como transportadores de fármacos. Face ao exposto, o objetivo deste trabalho foi o estudo de condições para ligar o ácido anacárdico (AA) em derivado dendrimérico com potencial ação na doença de Chagas, o qual tem como foco central o ácido succínico (AS) e ramificações compostas por arginina (Arg) e lisina (Lys). Sabe-se que a cruzaína, uma cisteíno-protease do T. cruzi, catalisa a hidrólise de ligação peptídica entre lisina e arginina. A síntese dos compostos em fase sólida forneceu os derivados brutos: (1) pró-fármaco AA-K-R-NH2 e (2) G.05 AA-K(AS)-R-NH2, que foram purificados e caracterizados por Cromatografia Líquida de Alta Eficiência e espectrometria de massas. Os compostos purificados AA-K-R-NH2 e AA-K(AS)-R-NH2 apresentaram rendimentos de 34% e 47%, com pureza de 88% e 98%, respectivamente. Os resultados dos experimentos enzimáticos utilizando o AA-K-R-NH2 não foram conclusivos. Acredita-se que a baixa solubilidade e/ou baixa concentração podem ter contribuído para tal. Já na estabilidade química em pH 7,4 (que simula pH sanguíneo), pH 1,2 (que simula pH estomacal) e pH 8,5 (que simula pH intestinal), observou-se que o AA-K(AS)-R-NH2 foi estável durante as 24 h de ensaio. Estes últimos resultados são interessantes, pois espera-se que o pró-fármaco dendrimérico alcance o T. cruzi estruturalmente integro, sofrendo hidrólise e liberação do composto ativo no interior do parasita

Chagas disease is a public health problem in many countries and regions. The treatment consists of toxic drugs, with debatable efficacy, mainly, in the chronic phase of the disease. Thus, it is necessary to plan new chemotherapeutics, safer and more effective than those drugs. Dendrimers are new molecular architectures composed by a central focus and branching from that focus. They present several biological applications, such as acting as drug carriers. Thereby, the goal of this work was the study of conditions to bind anacardic acid (AA) in a dendrimeric derivative with potential action in Chagas disease, which was composed by a central focus of succinic acid (AS) and branches of arginine (Arg) and lysine (Lys). Cruzain, a T. cruzi cysteine protease, is known to catalyze the peptide-binding hydrolysis between lysine and arginine. Synthesis of the solid phase compounds provided the crude derivatives: (1) prodrug AA-KR-NH2 and (2) G.05 AA-K(AS)-R-NH2, which were purified and characterized by High Performance Liquid Chromatography (HPLC) and mass spectrometry. The purified AA-K-R-NH2 and AA-K(AS)-R-NH2 compounds showed yields of 34% and 47%, with purity of 88% and 98% respectively. The results of the enzymatic experiments using AA-K-R-NH2 were not conclusive. It is believed that the low solubility and/or low concentration may have contributed for this. On the chemical stability at pH 7.4 (which simulates blood pH), pH 1.2 (which simulates stomach pH) and pH 8.5 (which simulates intestinal pH), it was observed that AA-K(AS)R-NH2 was stable for 24 hours. These latter results are interesting because the dendrimeric prodrug is expected to reach structurally integral T. cruzi, undergoing hydrolysis and release of the active compound within the parasite