Chemical variability between different organs of the medicinal plant Casearia sylvestris

The phytochemical profile of essential oils and extracts from Casearia sylvestris leaves, flowers and fruits have been investigated here. Leaf and flower extracts were prepared by sonication and analyzed by thin-layer chromatography and high-performance liquid chromatography. The phenolic content was determined by ultraviolet spectrophotometry. Leaves, flowers, and fruits essential oils were extracted by hydrodistillation. The highest extracts yields were 20.3 % (leaves) and 23.4 % (flowers) with ethanol 70 %. Essential oil extraction yields were 0.3 % (leaves) and 0.1 % (flowers and fruits). Bicyclogermacrene was the major component in all essential oil. Thin-layer chromatography suggests a chemical profile similar for leaves and flowers. The leaves and flowers phenolic content were similar (14.0 and 15.0 %, respectively). Chromatography analyses indicated the predominance of casearin clerodane diterpenes in leaves (λmax 232-235), whereas in flowers, diterpenes with a different standard diene in side-chain C13(16) and C14 (λmax 223-229). The different phytochemical profile of C. sylvestris flowers as compared to the leaves could be explored by the search for new bioactive components. This is the first report on the fruit and flower C. sylvestris essential oil composition. These data could be used as quality control of herbal medicine derived from C. sylvestris leaves.(AU)

Salvinorin A preserves cerebral pial artery autoregulation after forebrain ischemia via the PI3K/AKT/cGMP pathway

This study aimed to investigate the protective effect of salvinorin A on the cerebral pial artery after forebrain ischemia and explore related mechanisms. Thirty Sprague-Dawley rats received forebrain ischemia for 10 min. The dilation responses of the cerebral pial artery to hypercapnia and hypotension were assessed in rats before and 1 h after ischemia. The ischemia reperfusion (IR) control group received DMSO (1 µL/kg) immediately after ischemia. Two different doses of salvinorin A (10 and 20 µg/kg) were administered following the onset of reperfusion. The 5th, 6th, and 7th groups received salvinorin A (20 µg/kg) and LY294002 (10 µM), L-NAME (10 μM), or norbinaltorphimine (norBIN, 1 μM) after ischemia. The levels of cGMP in the cerebrospinal fluid (CSF) were also measured. The phosphorylation of AKT (p-AKT) was measured in the cerebral cortex by western blot at 24 h post-ischemia. Cell necrosis and apoptosis were examined by hematoxylin-eosin staining (HE) and TUNEL staining, respectively. The motor function of the rats was evaluated at 1, 2, and 5 days post-ischemia. The dilation responses of the cerebral pial artery were significantly impaired after ischemia and were preserved by salvinorin A treatment. In addition, salvinorin A significantly increased the levels of cGMP and p-AKT, suppressed cell necrosis and apoptosis of the cerebral cortex and improved the motor function of the rats. These effects were abolished by LY294002, L-NAME, and norBIN. Salvinorin A preserved cerebral pial artery autoregulation in response to hypercapnia and hypotension via the PI3K/AKT/cGMP pathway.

Aspectos toxicológicos da planta medicinal Casearia sylvestris Swartz: revisão de literatura / Toxicology of the medicinal plant Casearia sylvestris Swartz: a literature review

In the West, the consumption of medicinal plants is increasing strongly, and up to 40% of the population use medicinal plants and phytotherapic preparations regularly, in the belief that they are innocuous and/or safe. However, in most cases there is no scientific proof of their pharmacological and toxicological properties. The aim of this study was to carry out a bibliographical review of the toxicological properties of Casearia sylvestris Swartz and collect data providing a basis for its rational use. Some studies validate classical therapeutic indications of C. sylvestris, such as to treat diarrhea and snakebites, justifying its empirical use. Nevertheless, there are few reports about its toxicological properties and these present only limited findings, describing results as 50% lethal dose (LD50) and the acute toxicity of its constituents. Currently, research is insufficient to ensure safety of popular preparations based on C. sylvestris. Therefore, it is necessary to make a fuller assessment of its deleterious profile, especially with respect to the toxic potential of its constituents, as well as its capacity to harm target organs and organic systems...

No Ocidente, o consumo de plantas medicinais vem aumentando substancialmente, onde cerca de 40% da população utiliza regularmente plantas medicinais e preparações fitoterápicas sob o rótulo de serem produtos inócuos ou seguros. Porém, na maioria das vezes, não há comprovação científica de suas propriedades farmacológicas e toxicológicas. O objetivo deste trabalho foi realizar um levantamento bibliográfico sobre as propriedades toxicológicas da Casearia sylvestris Swartz e coletar dados que fundamentem seu uso racional. Alguns estudos validam indicações terapêuticas clássicas da C. sylvestris como antidiarréico e no tratamento de ferimentos ofídicos, fundamentando seu uso empírico. Porém, poucos trabalhos relatam suas propriedades toxicológicas, havendo apenas abordagens limitadas em torno da Dose Letal 50% e da toxicidade aguda de seus constituintes. Até o presente momento, as pesquisas são insuficientes para garantir a segurança de preparações populares à base de C. sylvestris. Portanto, há necessidade de avaliar melhor seu perfil deletério, principalmente, no que diz respeito ao potencial tóxico de seus constituintes, assim como a sua capacidade lesiva sobre órgãos-alvos e sistemas orgânicos...

Identificação de diterpenos clerodânicos em diferentes órgãos de Casearia sylvestris Swartz / Identification of clerodane diterpenes in different organs of Casearia sylvestris Swartz

Casearia sylvestris Swartz (Salicaceae) é uma espécie vegetal arbórea ou arbustiva, disseminada pelo território brasileiro e bastante utilizada em nossa medicina popular. Diversos diterpenos clerodânicos bioativos típicos do gênero Casearia foram isolados desta espécie (ex. casearinas e casearvestrinas). O objetivo principal deste trabalho foi avaliar a presença de diterpenos clerodânicos em diferentes órgãos de C. sylvestris, utilizando técnicas analíticas cromatográficas e espectroscópicas. Os extratos dos diferentes órgãos foram analisados por cromatografia em camada delgada, cromatografia líquida de alta eficiência com detector de arranjo de diodos e ressonância magnética nuclear de 1H. Nas análises cromatográficas foram utilizados diterpenos clerodânicos isolados de C. sylvestris como padrões, incluindo rel-19S-acetóxi- 18R- butanoilóxi- 18,19- epóxi -6S -hidróxi -2R- (2-metilbutanoilóxi) -5S, 8R, 9R, 10S -cleroda-3,13(16),14-trieno, isolado do caule pela primeira vez. Foram obtidos perfis fitoquímicos dos órgãos avaliados. Os resultados indicaram a presença de diterpenos clerodânicos em toda planta, prevalecendo em maior número nas folhas. Além disso, os resultados também indicam que em caules, flores e raízes há predomínio de diterpenos clerodânicos com padrão diênico diferente daqueles obtidos de folhas de C. sylvestris.

Casearia sylvestris Swartz (Salicaceae) is a tree or shrub distributed widely in Brazil, where it is used in popular medicine. Several bioactive clerodane diterpenes typical of Casearia have been isolated from this species (e.g. casearins and casearvestrins). The main objective of this study was to identify clerodane diterpenes in various organs of C. sylvestris, using chromatographic and spectroscopic analytical techniques. The extracts of the different plant parts were analyzed by thin layer chromatography, high performance liquid chromatography with diode array detector and 1H nuclear magnetic resonance. In the chromatographic analysis, clerodane diterpenes isolated from C. sylvestris were used as standards, including rel-19Sacetóxi- 18R- butanoilóxi-18,19- epóxi -6S -hidróxi -2R- (2-metilbutanoilóxi) -5S, 8R, 9R, 10S -cleroda-3,13(16),14- triene, isolated for the first time from the stems. Phytochemical profiles of the organs were produced, which indicated the presence of clerodane diterpenes in all parts of the plant, notably in the leaves. The results also suggest that the main clerodane diterpenes in the stems, flowers and roots had conjugated double-bond patterns that differed from those found in the leaves.