Bioassays

Objectives

(i) To acquire the concept of bioactivity and of bioactivity assays in the search for new drugs. (ii) Being able to describe and discuss the main bioactivity assays used in the modern search for compounds with pharmacological potential. (iii) To be able to interpret and criticize results of bioassays carried out in the practical lab component and in the scientific literature. (iv) To design bioassays for specific objectives of research. (v) To communicate scientific results.

Program

1. Bioassays – concept. Using bioassays in the search for new drugs. Synthetic molecules vs Natural Products. In vitro and in vivo assays – ethics, efficiency and costs. Bioassay-guided fractionation. Dose / effect and its quantification: EC50, IC50, LD50.

2. Antimicrobial, antitumour, antioxidant, anticholinesterasic, anti-inflammatory activities. Mechanisms of action.

3. XXIst century: High Throughput Screening. Multi-arrays. Natural Products databases. QSAR (Quantitative Structure/Activity Relationship) studies. In silico bioassays.

4. Introduction to the lab activity: (i) the protocol; (ii) calculating EC50 or IC50 from the results; (iii) rules for the report elaboration.

5. In the Lab: Determination of a biological activity (DPPH, anticholinesterasic or other) in 96-well microplates using serial dilution and spectrophotometric quantification.

Teaching Methodologies

The curricular unit will be use b-learning, combining presential activities, both in the lab and in the lecture room, with asynchronous activities supported by the Moodle platform available in the Azores University. Student’s participation is encouraged by the application of Problem-Based Learning (PBL) methodology and by the practical application of bioassays in the lab. For evaluation, the students will write a scientific paper concerning the bioactivity carried out in the lab. Some papers will be available to the students in Moodle platform, but they will be encouraged to search for bibliography in PubMed and other databases.

Bibliography

Barreto, M.C., Simões, N. (eds.) Determination of Biological Activities. A Laboratory Manual. Universidade dos Açores, Ponta Delgada, 2012. ISBN 978-972-8612-82-5.

Koehn, F.E., Carter, G.T. 2005. Nature Reviews 4, 206.

Eloff, J.N. 2004. Phytomedicine 11, 370.

Zhang, A.; Sun, H.; Wang, X. 2013. Eur. J. Med. Chem. 63, 570.

Blunt, J. W.; Copp, B. R.; Keyzers, R. A.; Munro, M. H. G.; Prinsep, M. R. 2013. Nat. Prod. Rep., 30, 237.

Cragg, G. M.; Newman, D. J. 2013. Biochim. Biophys. Acta, 1830, 3670. 7.

Other papers, available in Moodle platform