Alchornea glandulosaEthyl Acetate Fraction Exhibits Antiangiogenic Activity: Preliminary Findings fromIn VitroAssays Using Human Umbilical Vein Endothelial Cells

Abstract

Alchornea glandulosa has traditionally been used in Brazilian folk medicine for the treatment of immuneinflammatory diseases and as an antiulcer agent to heal gastric ulcer and gastritis. Angiogenesis is a complex multistep process that consists of proliferation, migration, and anastomosis of endothelial cells and has a major role in the development of pathologic conditions, such as inflammatory diseases. To investigate a possible link between the anti-inflammatory activities and antiangiogenic effects of A. glandulosa ethyl acetate fraction (AGF), this study examined which features of the angiogenic process could be disturbed by this fraction. The antiangiogenic activity of AGF was determined in vitro by using human umbilical vein endothelial cells (HUVEC), and cell viability, proliferation, apoptosis, invasion, and capillary-like structures formation were addressed. To elucidate the mechanism of action, nuclear factor jB (NFjB), a transcription factor implicated in these processes, was also evaluated in HUVEC incubated with AGF. A significant decrease in proliferation, a relevant increase in apoptosis, and a strong reduction in invasion capacity (as assessed by bromodeoxyuridine, terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick-end labeling, and double-chamber assays, respectively) were observed. AGF also led to a drastic reduction in the number of capillary-like structures formed when HUVEC were cultured on growth factor-reduced Matrigel-coated plates. In addition, incubation of HUVEC with AGF resulted in reduced NFjB activity. These findings emphasize the antiangiogenic potential of AGF and support its therapeutic use for disorders that involve excessive angiogenesis, such as chronic inflammation and tumor growth.

Alchornedine, a New Anti-Trypanosomal Guanidine Alkaloid from Alchornea glandulosa

“…(Euphorbiaceae), commonly known as "tapiá", "tamanqueiro", or "amor-seco", has been used in traditional medicine to treat inflammatory disorders [4]. Chemically, previous studies reported the occurrence of terpenoids, flavonoids, tannins, and diisopentenil/triisopentenil guanidine alkaloids in A. glandulosa, several of which displayed important biological activities such as anti-inflammatory, anti-tumoral, and antiangiogenic [5][6][7][8]. As part of our continuous research to find new antiparasitic compounds from Brazilian flora [9], this work investigated the anti-trypanosomal activity of the MeOH extract from the leaves of A. glandulosa, which afforded one new guanidine alkaloid, alchornedine (1), as a bioactive compound as well as two other inactive guanidine alkaloids, pteroginine (2) and pteroginidine (3).…”

“…3. Despite the occurrence of several guanidine alkaloids in A. glandulosa [5][6][7][8], the bioactivity-guided fractionation of the active MeOH extract from leaves afforded alchornedine (1), which displayed anti-trypanosomal activity. Considering the dose-response curves, alchornedine (1) killed almost 100 % of the parasites at the highest tested concentration.…”

Decyl Gallate as a Possible Inhibitor of N-Glycosylation Process in Paracoccidioides lutzii

“…Chemical studies of ethanolic extract obtained from the leaves of Alchornea glandulosa identified the presence of phenolic compounds, such as gallic acid, which has a range of biological activities, including anti-inflammatory and antifungal activity (10)(11)(12)(13). Structurally, modifications were made in this molecule by the addition of variably sized carbon chains, resulting in the formation of alkyl gallates.…”