The genus Erythrina L.: A review on its alkaloids, preclinical, and clinical studies.

Erythrina L. genus (Fabaceae) comprises about 115 species, and it has been extensively studied, mainly because of its alkaloids, which have pharmacological properties. References demonstrated that Erythrina spp. have a potential to act in the central nervous system, presenting anxiolytic and anticonvulsant properties already established. Phytochemical investigations confirmed the presence of tetracyclic alkaloids as the major compounds. However, other alkaloid classes have also been reported, including dimeric and trimeric substances, coupled through direct polymerization or two erythrinine units via an acetyl glucose. The present review covers the relevant literature from 1990 until 2017 and outlines the current data on chemical composition and preclinical and clinical studies on Erythrina species. Additionally, the quite striking analogy in the biosynthetic route of erythrin, morphinans, and Amaryllidaceae family alkaloids was also discussed.

pH-dependent cytotoxic effects of extracts of the marine sponge Polymastia janeirensis on cancer cell lines.

The purpose of this work was to study the cytotoxic effects of marine sponge Polymastia janeirensis, which has been observed in the field to release an orange substance that is toxic to fish. The result showed that aqueous extract (pH 7.0) was highly cytotoxic to glioma (U87) and neuroblastoma (SHSY5Y) cancer cell lines (IC50 < 1.0 µg/mL). In addition, this extract showed potent antioxidant and procoagulant (decreased the clotting time by 1.7-fold) activities. Interestingly, the cytotoxic effects were pH-dependent since the viability of the cancer cells was not affected with the extract (pH 5.5). The close similarity between the aqueous extract (pH 7.0) and the orange liquid that is released by the sponge indicates that this potential chemical defence of P. janeirensis deserves further investigation.

Sphingosines Derived from Marine Sponge as Potential Multi-Target Drug Related to Disorders in Cancer Development.

Haliclona tubifera, marine sponge species abundant in Brazilian coastline, presents only a few papers published in the literature. Recently, we have reported the isolation of two modified C18 sphingoid bases: (2R,3R,6R,7Z)-2-aminooctadec-7-ene-1,3, 6-triol and and (2R,3R,6R)-2-aminooctadec-1,3,6-triol. In order to continue our research, in this work aimed at the biological investigation of fractions that led to the isolation of these compounds. We evaluated the cytotoxic effect of marine sponge H. tubifera fractions in glioma (U87) and neuroblastoma (SH-SY5Y) human cell lines. In addition, considering the link between cancer, imbalance of reactive oxygen species and coagulation disorders, we also investigated the in vitro effects on blood coagulation and their redox properties. We showed that the ethyl acetate (EtOAc) fraction, rich in sphingoid bases, had important cytotoxic effects in both cancer cell lines with an IC50 < 15 µg/mL and also can inhibit the production of peroxyl radicals. Interestingly, this fraction increased the recalcification time of human blood, showing anticoagulant properties. The present study indicates the sphingosines fraction as a promising source of chemical prototypes, especially multifunctional drugs in cancer therapy.

Cytotoxic effects on tumour cell lines of fatty acids from the marine sponge Scopalina ruetzleri.

OBJECTIVES: Marine sponges are among the most promising sources of chemically diversified fatty acids (FAs). In addition, several studies have shown the effect of polyunsaturated FAs on cancer therapy. This research carried out a biological and chemical evaluation of the sponge Scopalina ruetzleri collected on the South Brazilian coastline. METHODS: Bioassay-guided fractionation of S. ruetzleri was performed in human glioma (U87) and neuroblastoma (SH-SY5Y) cell lines, and the in-vitro effects on free radicals were evaluated. KEY FINDINGS: The ethyl acetate fraction of S. ruetzleri showed promising cytotoxic effects in cancer cell lines, with IC50 < 20 µg/ml. Fingerprint (1) H Nuclear Magnetic Resonance (NMR) analysis showed that this fraction is mainly constituted of FAs. Through FA methyl ester analysis, it was possible to identify 32 FAs. In addition, some minor unusual FAs for the marine biosphere were identified. The results of conjugated dienes method showed that FAs fraction, at concentrations above 50 µg/ml, has a pro-oxidant effect, indicating that lipid peroxidation may be partially responsible for the mechanism of cytotoxicity on cancer cells. CONCLUSION: This work also contributes to studies that focus on the application of FAs on cancer therapy as a new adjuvant to radio or chemotherapy, or as a chemotherapeutic agent.

Chemical analysis, antioxidant, antichemotactic and monoamine oxidase inhibition effects of some pteridophytes from Brazil.

BACKGROUND: Ferns are a group of plants that have been little explored from a chemical and biological perspective but that have interesting potential, occurring in various parts of the world. OBJECTIVE: This work investigates the chemical profile and the biological effects of ferns from Brazil. MATERIALS AND METHODS: Analyses were performed using rapid performance liquid chromatography (RP-LC) with a diode array detector (DAD). Extracts were tested for their in vitro antioxidant activity, by the total reactive antioxidant potential method and for their antichemotactic potential, by the Boyden chamber method. Cytotoxic effects were assessed by lactate dehydrogenase levels, while the monoamine oxidase (MAO) assay was carried out using a fluorescence-based method. RESULTS: Different chemical compositions were found for the studied ferns, such as Asplenium gastonis, in which hesperidin was identified in its extract, while A. serra showed the presence of xanthone mangiferin. The most samples with highest antioxidant activity were the Asplenium serra, Lastreopsis amplissima and Cyathea dichromatolepis extracts, at 10 µg/mL. High antichemotactic activity was found for A. serra (94.06%) and Didymochlaena truncatula (93.41%), at 10 µg/mL. The extracts showed no cytotoxicity at the highest concentration. Against MAO-A, D. truncatula (82.61%), Alsophila setosa (82.21%), Cyathea phalerata (74.07%) and C. delgadii (70.32%) were the most active extracts (100 µg/mL). CONCLUSION: The hypothesis was considered that phenolics and triterpenes are responsible for these pronounced activities.

Morphoanatomical identification and physicochemical parameters of the drug Erythrina verna Vell. trunk bark / Identificación morfoanatómica y parámetros físico-químicos de la cortezadel leño de Erythrina verna Vell

“Mulungu” (Erythrina verna Vell., Fabaceae.) is an arboreal specie native to southeastern Brazil, used for medicinal purposes. This plant is characterized by the presence of alkaloids that have demonstrated anxiolytic activity. Due to this activity, this plant is listed by the Brazilian National Program of Medicinal Plants and Herbal Medicines. However, bibliographic information is lacking regarding this species. This study aims to describe E. verna barks, macro and microscopically, as well as some physicochemical parameters for the quality control of its raw material. In addition, the chromatographic profile of its alkaloid fraction and optimization of extraction methods for crude extract production has also been performed.

“Mulungu” (Erythrina verna Vell., Fabaceae.) es una especie arborea nativa del sudeste de Brasil, utilizada con fines medicinales. Esta planta se caracteriza por la presencia de alcaloides que han demostrado actividad ansiolítica. Debido a esta actividad, esta planta se encuentra en la lista del Programa Nacional Brasileño de las Plantas Medicinales y Medicinas Herbarias. Sin embargo, la información bibliográfica es escasa con respecto a esta especie. Este estudio tiene como objetivo describir E. Verna corteza, macro y microscópicamente, así como algunos parámetros físico-químicos para el control de la calidad de la materia prima fresca. Además, el perfil cromatográfico de la fracción alcaloidica y la optimización de métodos de extracción para la producción de extracto crudo también fue realizada.

Biological activities of ACL-I and physicochemical properties of ACL-II, lectins isolated from the marine sponge Axinella corrugata.

Lectin II from the marine sponge Axinella corrugata (ACL-II) was purified by affinity chromatography on rabbit erythrocytic stroma incorporated into a polyacrylamide gel, followed by gel filtration on Ultrogel AcA 44 column. Purified ACL-II is a lectin with an Mr of 80 kDa and 78 kDa, estimated by SDS-PAGE and by FPLC on Superose 12 HR column, respectively. ACL-II mainly agglutinates native rabbit erythrocytes and this hemagglutinating activity is independent of Ca(2+), Mg(2+) and Mn(2+), but is inhibited by d-galactose, chitin and N-acetyl derivatives, with the exception of GalNAc. ACL-II is stable for up to 65 °C for 30 min, with a better stability at a pH range of 2 to 6. In contrast, ACL-I displays a strong mitogenic and cytotoxic effect.

ACL-I, a lectin from the marine sponge Axinella corrugata: isolation, characterization and chemotactic activity.

The lectin from the marine sponge Axinella corrugata (ACL-I) was purified by affinity chromatography on rabbit erythrocytic stroma incorporated into a polyacrylamide gel followed by gel filtration on Ultrogel AcA 44 column. Purified ACL-I is a hexameric glycoprotein with a Mr of 82.3 kDa estimated by SDS-PAGE and 78.5 kDa by FPLC on Superose 12 HR column. The pI of lectin is 6.3 and ACL-I is constituted of 13.9 kDa similar subunits some of them linked by disulphide bridges. This lectin agglutinates native rabbit, goat and dog erythrocytes and in less extent human erythrocytes. The hemagglutinating activity is independent of Ca(2+), Mg(2+) and Mn(2+), but it is strongly inhibited by carbohydrates containing N-acetyl groups. ACL-I is stable up to 70 degrees C for 30 min, with optimum pH between 7 and 8, and it is also resistant to enzymatic proteolysis in vitro. In the presence of reducing or denaturant agents, the lectin activity decreases. ACL-I displays chemotactic effect on rat neutrophil in vitro which is inhibited by N-acetyl-d-glucosamine.