Steroids and flavonoids of Porcelia macrocarpa

Chaves, Mariana Helena; Roque, Nı́dia Franca; Ayres, Mariane Cruz Costa

doi:10.1590/s0103-50532004000400026

Cited by 19 publications

(5 citation statements)

References 11 publications

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“…The activity profile indicated that the inhibition was due to some flavonoid constituents. Preparative isolation afforded seven methoxylated flavonoids (9-15) which were identified as 3,7-O-dimethylherbacetin (9) [16], 3,3′,7-tri-Omethylgossypetin (10), 3,8-di-O-methylherbacetin (11) [17], 3,3′,4′-tri-O-methylmyricetin (12), 3,7,8-tri-O-methylherbacetin (13) [18], ternatin (14) [19], and 4′,7-di-O-methylquercetin (15, ombuin) [20] (l " Fig. 3 , and 14 all showed IC 50 s > 10 µM against both kinases.…”

Section: Resultsmentioning

confidence: 99%

Library-based Discovery of DYRK1A/CLK1 Inhibitors from Natural Product Extracts

et al. 2012

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The dual specificity tyrosine-phosphorylation-regulated kinase DYRK1A possesses diverse roles in neuronal development and adult brain physiology, and increased activity has been linked to neurodegenerative diseases. Very few inhibitors of this kinase have been reported up to now. Screening of a library of > 900 plant and fungal extracts afforded 25 extracts with IC₅₀s < 10 µg/mL against DYRK1A. To identify the active constituents, the extracts were submitted to a process integrating physicochemical data with biological information, referred to as HPLC-based activity profiling. Follow-up investigation of four extracts led to the targeted isolation of harmine (1, IC₅₀ 0.022 µM) from Peganum harmala, emodin (3, IC₅₀ 4.2 µM) from Cassia nigricans, kaempferol (4, IC₅₀ 0.91 µM) from Cuscuta chinensis, and 3,8-di-O-methylherbacetin (11, IC₅₀ 8.6 µM), 3,3',4'-tri-O-methylmyricetin (12, IC₅₀ 7.1 µM) and ombuin (15, IC₅₀ 1.7 µM) from Larrea tridentata as the active constituents. Active extracts and compounds were also tested on the closely related cdc2-like kinase CLK1. Finally, the selectivity profile of compounds was evaluated by including other members of the DYRKs and CLKs families. While the flavonoids and emodin did not show significant differences in the potency of their activities, harmine (1) was most active against DYRK1A, CLK1, and CLK4, and less potent against the other kinases, with selectivity ranging from 2- to 20-fold.

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Section: Resultsmentioning

confidence: 99%

Library-based Discovery of DYRK1A/CLK1 Inhibitors from Natural Product Extracts

et al. 2012

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“…A investigação de plantas na busca de metabólitos com ação anticâncer, conduziu à descoberta de substâncias com potencial antiestrogênico, que vêm sendo utilizadas para o tratamento do câncer de Figura 1 -Estruturas químicas de componentes naturais bioativos Figura 1 -Estruturas químicas de componentes naturais bioativos Figura 1 -Estruturas químicas de componentes naturais bioativos Figura 1 -Estruturas químicas de componentes naturais bioativos Figura 1 -Estruturas químicas de componentes naturais bioativos mama. Dentre todos os produtos naturais bioativos que apresentam atividade estrogênica, destacamse os esteróides, alcalóides, coumestanos e isoflavonóides (CHAVES et al, 2004;HARBONE, 1994;LAEKEMAN, 1986;PUPO et al, 2002;SAITO et al, 1993). Tomando-se como exemplo a classe dos flavonóides, ocorreu, há muitos anos atrás, um fato curioso com um rebanho de carneiros (da região oeste da Austrália) que se alimentava de um trevo conhecido cientificamente como Trifolium subterraneum.…”

Section: Produtos Naturais Bioativos Produtos Naturais Bioativos Prod...unclassified

Aspectos sobre Produtos Naturais na Descoberta de Novos Agentes Antitumorais e Antimutagênicos

et al. 2007

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O presente estudo traz um breve histórico sobre produtos naturais anticarcinogênicos, bem como aspectos relevantes de pesquisas quimiofarmacológicas onde agentes anticancerígenos são o alvo principal de investigações. Neste contexto, mostra uma abordagem geral sobre quimioterapia e mutagenicidade. Focaliza ainda, aspectos químicos e propriedades anticâncer e antimutagênica de uma das mais importantes plantas medicinais brasileiras da atualidade: Croton cajucara Benth, uma euforbiácea, muito utilizada na medicina popular da região Amazônica, de onde se isola a promissora substância trans-desidrocrotonina, cujo uso vem sendo difundido por todo o país, e que poderia representar uma substância a ser mais bem explorada como agente anticâncer. Sua incorporação em sistemas de liberação controlada também é abordada.

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“…Porcelia macrocarpa (Warming) R. E. Fries is a typical species from the Southeastern region from Brazil [5]. Previous chemical studies were carried out with this species and amides [6], alkaloids [7,8], flavonoids [9], steroids/terpenoids [9,10], and amino-acids [11] were isolated from its leaves and stems. Additionally, the occurrence of acetylene acetogenins in the seeds was also reported [12].…”

Section: Introductionmentioning

confidence: 99%

Antitrypanosomal Acetylene Fatty Acid Derivatives from the Seeds of Porcelia macrocarpa (Annonaceae)

et al. 2015

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Chagas' disease is caused by a parasitic protozoan and affects the poorest population in the world, causing high mortality and morbidity. As a result of the toxicity and long duration of current treatments, the discovery of novel and more efficacious drugs is crucial. In this work, the hexane extract from seeds of Porcelia macrocarpa R.E. Fries (Annonaceae) displayed in vitro antitrypanosomal activity against trypomastigote forms of T. cruzi by the colorimetric MTT assay (IC50 of 65.44 μg/mL). Using chromatographic fractionation over SiO2, this extract afforded a fraction composed by one active compound (IC50 of 10.70 µg/mL), which was chemically characterized as 12,14-octadecadiynoic acid (macrocarpic acid). Additionally, two new inactive acetylene compounds (α,α'-dimacro- OPEN ACCESSMolecules 2015, 20 8169 carpoyl-β-oleylglycerol and α-macrocarpoyl-α'-oleylglycerol) were also isolated from the hexane extract. The complete characterization of the isolated compounds was performed by analysis of NMR and MS data as well as preparation of derivatives.

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Steroids and flavonoids of Porcelia macrocarpa

Cited by 19 publications

References 11 publications

Library-based Discovery of DYRK1A/CLK1 Inhibitors from Natural Product Extracts

Library-based Discovery of DYRK1A/CLK1 Inhibitors from Natural Product Extracts

Aspectos sobre Produtos Naturais na Descoberta de Novos Agentes Antitumorais e Antimutagênicos

Antitrypanosomal Acetylene Fatty Acid Derivatives from the Seeds of Porcelia macrocarpa (Annonaceae)

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