MEDICINAL CHEMISTRY AND NATURAL PRODUCTS

Our research in the scope of the natural products has been a powerful tool for combating several diseases like cancer and other pathological disorder, having contributed to get and to understand all the mechanism involved onto the formation of anticancer and anti-infective drugs as well as on Central Nervous System (CNS). Thus, "oxoisoaporphines" (7H-dibenzo[de,h]quinolin-7-one) are a small group of isoquinoline alkaloids that have shown an important chemical characteristic as antidepressive pro-drugs. In this sense, these alkaloids that bearing a nitrogen atom and a carbonyl group at C-1 and C-7 respectively, they have demostrated with several chemical structures, either total or partially hydrogenated, a high and selective ability to the inhibition of the isoform A of the human monoamine oxidase (h-MAO-A) in nanomolar range, according to the IC50 value. This unusual pharmacological property does not reported in the current bibliography due to that this type of pharmacological behaviour only had been found in certain amphetamine derivatives.

On the other hand, similar chemical structres called "perimidinones" (7H-benzo[e]perimidin-7-one) in the last decades, have been used as paintings. However, our research group has found that this alkaloid and its derivatives have an interesting reactivity in the photochemical activity on the production of singlet oxygen, a pioneer in the treatment of cancer with photodynamic therapy. Due to the excellent results in the scope of the pharmacology and using molecular docking in order to see the different chemical interactions between the alkaloid and receptor, these molecules could give us an alternative against depression and anxiety like oxoisoaporphine derivatives with low cytotoxicity and good bioavailabllity if these compounds were few soluble in aqueous solution. Thus, the next chemical structures of "oxoisoaporphines" and "perimidinones" are shown as follows:   

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SUPRAMOLECULAR CHEMISTRY-DRUG DELIVERY SYSTEM

The supramolecular chemistry of cyclodextrins (CDs) has been widely used in pharmaceutical formulations of drugs to increase their water solubility (e.g. itraconazole) and stability (e.g.PGE1), to mask odor (garlic oil) and flavor, to perform a drug release control (loteprednol) and to favor their absorption (e.g. piroxicam). In most cases such formulations are based on unmodified CDs mixed with the corresponding drug. When a large increase in water solubility is desired sometimes dimethyl- or hydroxypropyl-β-CD is used.

In our first studies related with β-CD derivatives with some aromatic compounds as naphtho-quinolinones and coumarins, the experimental data shown an excellent incorporation of both type of compounds, with a regioselectivity of enter and incorporation constant (Ks) highest expected. However, this first step is the beginning to apply it to supramolecular systems with chromophore, which can be detected by UV-light when the guest-compound is incorporated inside CD. On the other hand, the use of chitosan as natural drug delivery system and synthetic polymer as PCL (poly-e-caprolactone) are the carriers used in medicine to afford nanocapsules, which can deliver the active drug in a controlled way in the organism, minimizing the concentration of the active product and affordinbg a therapeutic effect during a long time.

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RECENT ARTICLES

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NEWS FOR THE WORLD

01/06/2021 - We have published an article about Emodin with potential antineoplastic effects in Cancers (MDPI, IF = 6.12). More details, see: https://www.mdpi.com/2072-6694/13/11/2733

 

26/05/2021 - Prof. Sobarzo-Sánchez was appointed within the Editorial Board Member as Academic Editor for Oxidative Medicine and Cellular Longevity (Hindawi).

 

13/05/2021 - We have published two new collaborations in the scope of fungal pathogens and about COVID-19 treatment in Molecules. Further information, see: https://www.mdpi.com/1420-3049/26/10/2933#cite;

https://www.mdpi.com/1420-3049/26/10/2917#cite

 

05/04/2021 - Prof. Sobarzo-Sánchez has been assigned as Co-Editor for Current Medicinal Chemistry (Bentham Science) in the scope of Medicinal Chemistry and Pharmacology of Natural Products. Thanks a lot for this kind appointment. 

01/03/2021 - We have published, in collaboration with INPST members, an interesting article about Natural Products and their applications in Nature Reviews Drug Discovery. Please, check it now here.