Biocontrol evaluation of extracts and a major component, clusianone, from Clusia fluminensisPlanch. & Triana againstAedes aegypti

Studies evaluated the effects of hexanic extracts from the fruits and flowers ofClusia fluminensis and the main component of the flower extract, a purified benzophenone (clusianone), against Aedes aegypti. The treatment of larvae with the crude fruit or flower extracts from C. fluminensis did not affect the survival ofAe. aegypti (50 mg/L), however, the flower extracts significantly delayed development of Ae. aegypti. In contrast, the clusianone (50 mg/L) isolate from the flower extract, representing 54.85% of this sample composition, showed a highly significant inhibition of survival, killing 93.3% of the larvae and completely blocking development of Ae. aegypti. The results showed, for the first time, high activity of clusianone against Ae. aegypti that both killed and inhibited mosquito development. Therefore, clusianone has potential for development as a biopesticide for controlling insect vectors of tropical diseases. Future work will elucidate the mode of action of clusianone isolated from C. fluminensis.

Cytotoxic and Antiviral Activity of Extracts and Compounds Isolated from Clusia Fluminensis Planch. & Triana (Clusiaceae) / Atividade Citotóxica e Antiviral de Extratos e Compostos Isolados de Clusia Fluminensis Planch. & Triana (Clusiaceae)

The worldwide distribution of herpes simplex virus type 1 (HSV-1) allied to the emergence of resistant strains makes necessary and urgent the search and development of new substances capable of preventing and treating HSV-1 infections. Studies demonstrate synergy between genital herpes and human immunodeficiency virus type 1 (HIV-1), which represents a major concern for global public health. Objective: The objective of this study was to evaluate the activity of crude extracts and isolated substances from C. fluminensis in the in vitro replication of the HSV-1 virus and HIV-1-RT activity. Methods: This study evaluated the activity of extracts and isolated compounds from Clusia fluminensis Planch. & Triana against HSV-1 using Vero cells in culture and against HIV-1 using a recombinant reverse transcriptase enzyme (HIV -1 RT). The percentage of inhibition against HSV-1 was determined from viral lysis plaque reduction assay, and the anti-HIV-1-RT test was performed by a fluorimetric assay. It was also evaluated the cytotoxic activity of the samples using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide]. Results: The crude extracts showed high percentage of inhibition against HSV-1, reaching 81.4 to 100.0% inhibition in non-cytotoxic concentration (50 µg/mL). The isolated compounds, lanosterol and clusianone, demonstrated 100% inhibition in non-cytotoxic concentration (50 µg/mL). We also examined the effects of the extracts and isolates on the activity of the HIV-1-RT. Among the crude extracts, only the methanolic extract of leaves and methanolic extract of stems showed inhibitory activity against HIV-1-RT. Regarding the isolated compounds, lanosterol showed a moderate activity. Conclusion: Our data demonstrate that extracts and isolates compounds Clusia fluminensis Planch. & Triana have promising antiviral activity inhibiting HSV-1 replication and HIV-1 by inhibiting the anti-RT activity.

A distribuição mundial do vírus herpes simplex tipo 1 (HSV-1) aliada ao surgimento de cepas resistentes torna necessária e urgente a busca e o desenvolvimento de novas substâncias capazes de prevenir e tratar infecções HSV-1. Estudos demonstram sinergia entre herpes genital e vírus da imunodeficiência humana tipo 1 (HIV-1), o que representa uma grande preocupação para a saúde pública global. Objetivo: O objetivo deste estudo foi avaliar a atividade de extratos brutos e substâncias isoladas de Clusia fluminensis Planch. & Triana na replicação in vitro do vírus HSV-1 e na atividade anti HIV-1-RT. Métodos: Este estudo avaliou a atividade de extratos e substâncias isoladas de Clusia fluminensis Planch. & Triana contra o HSV-1 utilizando células Vero em cultura e contra o HIV-1 utilizando a enzima transcriptase reversa recombinante (HIV-1 RT). A porcentagem de inibição contra o HSV-1 foi determinada a partir do ensaio de redução de placas de lise viral, e o ensaio anti-HIV-1 RT foi realizado por um ensaio fluorimétrico. Também foi avaliada a atividade citotóxica das amostras utilizando MTT [brometo de 3- (4,5-dimetiltiazol-2-il) -2,5-difeniltetrazólio]. Resultados: Os extratos demonstraram elevada percentagem de inibição contra o HSV-1, atingindo 81,4 a 100,0% de inibição em concentração não citotóxica (50 µg/mL). Os compostos isolados, lanosterol e clusianona, demonstraram 100% de inibição em concentração não citotóxica (50 µg/mL). Examinamos também os efeitos dos extratos e isolados sobre a atividade anti-HIV-1 RT. Entre os extratos brutos, apenas o extrato metanólico das folhas e caules apresentaram atividade anti-HIV-1 RT. Em relação aos compostos isolados, lanosterol mostrou uma atividade moderada. Conclusão: Nossos dados demonstram que os extratos e compostos isolados de Clusia fluminensis Planch. & Triana possuem atividade antiviral promissora inibindo a replicação do HSV-1 e HIV-1 através da inibição da atividade anti-RT.