Chemosensitizing Effect of Cernumidine Extracted from Solanum cernuum on Bladder Cancer Cells in Vitro.

Cernumidine (CER) is a guanidinic alkaloid isolated from Solanum cernuum leaves. In this work, we investigated the cytotoxicity, chemosensitizing effect of cernumidine to cisplatin (cDDP) and the possible mechanism of action of the combination on bladder cancer cells. Cernumidine showed cytotoxicity and could sensitize bladder cancer cells to cisplatin. The combination of CER+cDDP inhibited cell migration on T24 cells. CER+cDDP down-regulated MMP-2/9 and p-ERK1/2, while it increased EGFR activity corroborating the observed cell migration inhibition. Down-regulation of Bcl-2 and up-regulation pro-apoptotic Bax and further depletion of the mitochondrial membrane potential (ΔΨm) indicates that mitochondria play a central role in the combination treatment inducing the mitochondrial signaling pathway of apoptosis in T24 cells. Our data showed that the alkaloid cernumidine is worthy of further studies as a chemosensitizing agent to be used in complementary chemotherapy.

A new alkaloid and flavonoids isolated from Solanum cernuum leaves by high-performance countercurrent chromatography.

Solanum cernuum is a medicinal plant widely distributed in south-east regions of Brazil and popularly used to treat several disorders. Despite their utilisation as a medicine, few studies on its chemical composition are reported. An efficient separation method for the ethyl acetate fraction was developed by high-performance countercurrent chromatography using n-butanol/chloroform/methanol/water (3:7:3:4, v/v/v/v) as the solvent system, affording five compounds (1-5) in one-step separation. A new cyclic guanidine alkaloid named cernidine (5) was obtained, besides four glycosylated flavonoids: afzelin (1), astragalin (2), kaempferol 3-O-α[apiofuranosyl-(1 â†’ 2)]-α-rhamnopyranoside (3) and kaempferol 3-O-α[apiofuranosyl-(1→2)]-ß-galactopyranoside (4). A further purification step afforded a mixture of trans- and cis-tiliroside (6-7). Countercurrent chromatography proved itself as a powerful tool for the isolation of similar compounds since compounds 1-2 and 3-4 possess little structural differences.

Protective effects of Solanum cernuum extract against chromosomal and genomic damage induced by methyl methanesulfonate in Swiss mice.

Solanum cernuum Vell is a Brazilian shrub or small tree, restricted to Southeast states of the country. The leaves are commercialized as "panacéia" and indicated for the treatment of urinary disorders, gonorrhea, scabies, skin diseases and as desobstruent, diuretic and antiarrhythmic. The hydroalcholic extract is active in the treatment of gastric ulcer. The aim of this study was to evaluate the genotoxic and antigenotoxic potential of S. cernuum hydroalcoholic extract (SC) in Swiss mice by micronucleus and comet assays. The animals were treated by gavage with the doses of 500, 1000 and 2000mg/kg body weight (b.w.). For antigenotoxicity assessment, the doses of 15, 30, 60, 120 and 240mg/kg b.w SC were administered simultaneously with the mutagen methyl methanesulfonate (MMS, 40mg/kg b.w., i.p.). The results showed that the SC was not genotoxic in both micronucleus and comet assays. On the other hand, the treatment with the lowest dose of SC (15mg/kg b.w.) plus MMS showed a statistically significant reduction in the frequency of micronuclei compared to treatment only with MMS. For the comet assay, significant reduction in extensions of DNA damage was observed in all treatments with SC combined with MMS in comparison with only MMS. The antigenotoxic activity observed for the SC may be due to the antioxidant potential of the compounds present in the extract such as guanidine alkaloids and flavonoids.

Gastroprotective activity of the hydroethanolic extract and isolated compounds from the leaves of Solanum cernuum Vell.

ETHNOPHARMACOLOGICAL RELEVANCE: Solanum cernuum Vell. (Solanaceae) is a Brazilian medicinal plant, traditionally known as "panaceia". Its folk name is probably due to its wide range of applications in traditional medicine including the treatment of ulcers. AIM OF THE STUDY: To evaluate the gastroprotective activities of the hydroethanolic extract (ESC) of S. cernuum and its major isolated compounds using in vivo gastric ulcer models. MATERIAL AND METHODS: The ESC extract was obtained by maceration followed by percolation of the dried and powdered leaves of S. cernuum in ethanol:water (7:3). The major compounds in the extract were isolated by applying various preparative chromatographic techniques. The gastroprotective activity was evaluated in mice using different gastric ulcer-induced models. The anti-Helicobacter pylori activity was performed using the agar-well diffusion and broth microdilution methods. RESULTS: The ESC extract showed gastroprotective effects in the assay of acute gastric ulcer-induced by HCl/EtOH, nonsteroidal anti-inflammatory drug, and acetic acid-induced chronic ulcer protocols. The results also demonstrated that the gastroprotection induced by ESC extract is related to the activity of nitric oxide and endogenous sulfhydryls, which are important gastroprotective factors. The ESC extract and the alkaloid cernumidine did not show activity against H. pylori in the concentrations tested. CONCLUSIONS: The present study showed that the crude extract of S. cernuum possessed gastroprotective activity which corroborating the traditional use of this plant for the treatment of gastric ulcers. The isolated flavonoids, quercitrin and afzelin as well as the phenylpropanoid, isoferulic acid are suggested to be the compounds responsible for the gastroprotective activity of S. cernuum extract.

Morphological, anatomical, macro and micromolecular markers for Solanum cernuum identification

The plants consumed as remedy by the population may have imprecise taxonomical identification. If these plants are used for the production of phytomedicines such misidentification may affect the quality of the product. Hereby, we describe markers for identification of the entire plant or grounded plant material or the crude extract of Solanum cernuum Vell. (Solanaceae). Specimens from four localities were collected, analyzed and compared. Morphological characters were used to identify the plant when it is not grounded or extracted. However, when the plant material is grounded, the set of trichomes may be used as anatomical marker. The region ITS1, 5.8S and ITS2 of the nuclear ribosomal DNA was cloned and sequenced. The sequence, with length of about 600 base pairs, being 48.1 percent AT , was deposited in GenBank under the accession number DQ837371. Once this sequence is specific to S. cernuum, it was used as marker for this species. For the crude extract, chromatographic profiles of the leaves extracts were obtained by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Two flavonoids were isolated and identified as quercitrin and afzelin. So, this study presents morphological, anatomical, macro and micromolecular markers to identify S. cernuum.

Plantas consumidas como remédio nem sempre são identificadas taxonomicamente de maneira correta. Se estas plantas forem utilizadas para obtenção de uma droga vegetal ou um fitoterápico, tal erro pode afetar a qualidade do produto final. Neste trabalho são descritos marcadores para a identificação de Solanum cernuum Vell. (Solanaceae), esteja a planta íntegra, triturada ou como extrato bruto. Indivíduos de quatro localidades de Minas Gerais foram coletados, analisados e comparados. Os caracteres morfológicos foram utilizados para a planta íntegra. Para a planta triturada, o conjunto dos tricomas foi utilizado como marcador anatômico. Um marcador macromolecular também foi determinado. Para tal a região ITS1, 5.8S e ITS2 do DNAr foi clonada e seqüenciada. A seqüência, com cerca de 600 pares de bases dos quais 48,1 por cento são AT, foi depositada no GenBank sob o número de acesso DQ837371. Por ser uma seqüência específica para S. cernuum, ela pode ser usada como marcador desta espécie. Para o extrato bruto foram determinados perfis cromatográficos de extratos das folhas por cromatografia em camada delgada e por cromatografia líquida de alta eficiência. Dois flavonóides foram isolados e identificados como quercitrina e afzelina. Assim, neste trabalho foram determinados marcadores morfológicos, anatômicos, macro e micromoleculares para identificar S. cernuum.

Morphology of the Phytophagous bug Platyscytus decempunctatus (Carvalho) (Heteroptera: Miridae)

Platyscytus decempunctatus Carvalho is a small mirid living throughout its life cicle plant Solanum cernuum Vell. (Solanaceae). The internal morphology of P. decempunctatus was studied and found that the female has a telotrophic ovary with three ovarioles in the right ovary and five in the left one. In the male reproductive trait there is a well developed tubular accessory gland. The phytophagous feeding habitat of P. decempunctatus was confirmed by the observations of chlorophyll pigments in the gut of all dissected specimens. The tubular salivary glands and the Malpighian tubules were also discussed.

Platyscytus decempunctatus Carvalho é um mirídeo de pequeno porte que vive durante seu ciclo de vida em plantas de Solanum cernuum Vell. (Solanaceae). A morfologia interna de P. decempunctatus foi estudada revelando que fêmeas possuem ovário do tipo telotrófico com três ovaríolos no ovário direito e cinco no esquerdo. Nas estruturas reprodutivas dos machos existe uma glândula acessória tubular bem desenvolvida. A fitofagia de P. decempunctatus foi confirmada devido a observações de pigmentos de clorofila no intestino de todos os espécimes dissecados. As glândulas salivares em formato tubular e os túbulos de Malpighi também foram discutidos.