Research into Bioactive Natural Compounds: New Molecules, Bioinspired Syntheses, Biotechnological Methods and Bioassays—Celebrating the Pioneering Work of Prof. Alejandro Fernandez Barrero

Dear Colleagues,

In 2020, Professor Alejandro F. Barrero retired after devoting more than 45 years to teaching and research activities. During these years. Prof. Barrero focused his efforts on the field of natural products chemistry, including the isolation, structural elucidation, chemical synthesis, and pharmacology of compounds derived from natural sources. Prof. Barrero’s team discovered more than two hundred new natural molecules and, in parallel, a number of biomimetic syntheses of natural products, employing new protocols based on both radical and cationic chemistry. Furthermore, he pioneered the use of innovative natural compounds as starting materials, thus favoring isolation methodologies. He also performed biosynthetic studies of terpenes using genetically modified fungi. Honoring the work of Prof. Barrero, this Special Issue is dedicated to the study of the chemistry of natural products.

Historically, natural products and their structural analogues have played a significant role in many fields that contribute to human welfare, including human and veterinary medicine, agriculture, and the food and the cosmetic industries.

The research into natural products is currently an efficient and safe approach to worldwide problems. In particular, there is a need for improved agricultural practices and strategies to address population explosion and climate change in tandem with stricter regulations for insecticide use. Similarly, the demand for new drugs including new antibiotics is enormous; according to the WHO, one of the greatest threats that we face as a global community is antibiotic resistance, which is revitalizing interest in the use of natural products as drug leads.

In parallel to these needs, the development of improved analytical tools, genome mining, and advances in microbial culturing are creating new opportunities for natural product-based bioactive compound discovery.

Finally, the fact that many of these natural products can be obtained from renewable sources may enable the study of their potential contributions to the circular economy.

This Special Issue aims to perform an overall survey of the research into bioactive natural compounds, including the description of new naturally occurring molecules, as well as the synthesis of these bioactive compounds, including biomimetic synthesis, microbial culturing production and the preparation of new active derivatives. Studies carried out to test the bioactivity of these natural compounds will also be considered. This subject fits the scope of this journal, particularly in the area of “Natural and Bio-inspired Molecules”

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following areas:

• Processes used for the extraction-fractioning of bioactive natural terpenoids and new natural products;
• Biotechnology: the study of biosynthetic routes and production of bioactive natural products from fungi and bacteria, known as biotransformation;
• Synthesis of bioactive natural products using bioinspired synthetic approaches and the use of natural synthons and bioconversions;
• Search for pharmacologically active natural products, biopesticides, etc.

We look forward to receiving your contributions.

Dr. José Francisco Quílez del Moral
Dr. Azucena González Coloma
Guest Editors

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• natural products
• bioactivity
• organic synthesis
• biotecnnology
• structural elucidation

Title: Bovistols E and F, new Terpenoids Isolated from Psathyrella microrhiza CF-117891
Authors: Fernando Reyes et al.
Affiliation: Fundación MEDINA, Avda del Conocimiento 34, 18016, Armilla, Granada, Spain
Abstract: Bioactivity-based purification of the acetone extract of a culture of the fungus Psathyrella microrhiza CF-117891 led to the isolation of the newbis-sesquiterpenes bovistols E and F (1 and 2) together with the anti-plasmodial macrolide coriolide (3). The structures of the compounds were determined by a combination of (+)-ESI-TOF mass spectrometry and NMR spectroscopy. Of the three compounds isolated, coriolide displayed previously unreported moderate anti-Plasmodiun falciparum 3 D7 activity, with an EC50 value 17.8 µM, whereas the new bovistols did not show any biological activity in their pure forms against this parasite nor against Tripanosoma cruzi Tulahuen parasites. This work further demonstrates that fungal extracts can be a rich source of new chemistry for possible future applications.

Title: Terpenes with Cyclic Anhydride Scaffolds: Occurrence, Biosynthesis and Bioactivity
Authors: Jose Francisco Quilez del Moral
Affiliation: Department of Organic Chemistry, University of Granada, 18071 Granada, Spain

Title: New dimethoxyaryl-sesquiterpene derivatives with cytotoxic activity against MCF-7 breast cancer cells: From the synthesis, topoisomerase I/II inhibition to studies on the mechanism of cell death
Authors: Prof M Cuellar
Affiliation: Universidad de Valparaíso, Chile

Title: Molecular Diversity from longipinenes of Santolina viscosa Lag trough acid catalysis
Authors: Prof Dorado
Affiliation: University of Almeria, Spain