A course-based undergraduate research experience to illustrate the early stages of the drug discovery process.

We have implemented at the University of Málaga (Spain) a new course-based undergraduate research experience (CURE) to involve undergraduate students of Science in a real-world scientific problem. Within the topic "Let's find acetylcholinesterase inhibitors as new drug candidates for the treatment of Alzheimer's", students have been engaged into the early stages of the drug discovery process. Working in groups of 4-5 persons, they have searched information in databases, proposed solutions to the driving question and designed protocols to carry them out in vitro and in silico. Overall, the implementation of this experience has been very satisfactory in terms of academic performance and students' perception. This article reports a session from the virtual international 2021 IUBMB/ASBMB workshop, "Teaching Science on Big Data".

El hipérico: una fuente de compuestos bioactivos con un amplio espectro de acción / Hypericum: a source of bioactive compounds with a wide range of action

El hipérico es una planta herbácea cuyos extractos han sido usados tradicionalmente para el tratamiento de muy diversas afecciones. Recientemente, se ha demostrado que los extractos de hipérico son efectivos para el tratamiento de la depresión leve a moderada. El hipérico es fuente de gran diversidad de compuestos bioactivos, siendo la hiperforina el principal causante de sus efectos antidepresivos. Otro compuesto característico del hipérico, la hipericina, es el más potente fotoactivador natural descrito. El renovado interés en el hipérico como fuente de compuestos con potencial aplicación farmacológica ha permitido caracterizar nuevos y prometedores efectos de la hiperforina y la hipericina, en particular como antitumorales y antiangiogénicos. Este trabajo revisa la etnobotánica del hipérico, con sus usos tradicionales y clínicos actuales, así como resume el estado actual del conocimiento acerca de los efectos biológicos de sus dos compuestos más característicos, la hipericina y la hiperforina

St. John’s wort is a herbaceous plant, which extracts have been traditionally used for the treatment of a high number of pathological conditions. Recently, it has been shown that St. John’s wort extracts are effective for the treatment of mild-tomoderate depression. St. John’s wort is a source of a great diversity of bioactive compounds, hyperforin being the main responsible for the described antidepressant effects. Another characteristic compound is hypericin, the most potent natural photoactivator described so far. The renewed interest for St. John’s wort as a source of compounds with potential pharmacological applications has allowed to characterize new and promising effects of hyperforin and hypericin, mainly as antitumoral and antiangiogenic compounds. This work reviews St. John’s wort ethnobotanics, along with its traditional and current clinical uses, as well as the current state-of-the-art of the biological effects of both hypericin and hyperforin

Anti-angiogenic effects of homocysteine on cultured endothelial cells.

High levels of homocysteine induce a sustained injury on arterial endothelial cells which accelerates the development of thrombosis and atherosclerosis. Some of the described effects of homocysteine on endothelial cells are features shared with an anti-angiogenic response. Therefore, we studied the effects of homocysteine on key steps of angiogenesis using bovine aorta endothelial cells as a model. Homocysteine decreased proliferation and induced differentiation. Furthermore, 5 mM homocysteine produced strong inhibitions of matrix metalloproteinase-2 and urokinase, two proteolytic activities that play a key role in extracellular matrix re-modeling, and decreased migration and invasion, other two key steps of angiogenesis. This study demonstrates that homocysteine can inhibit several steps of the angiogenic process.