Papers by M. Gómez-Serranillos
Discovery and Development of Anti-Breast Cancer Agents from Natural Products, 2021
Abstract Worldwide, breast cancer is the second most common cancer after lung cancer and it is th... more Abstract Worldwide, breast cancer is the second most common cancer after lung cancer and it is the first most incident and prevalent cancer in women. Plant-derived natural products have historically been in drug discovery process as a source of chemotherapeutic agents against different kinds of cancers, including breast cancer. More than half of the anticancer drugs used in clinical uses have presently a natural origin. In this context, vinca alkaloids (vinblastine and vincristine), isolated from the Madagascar periwinkle plant Catharanthus roseus G. Don. (Apocynaceae), were the first natural products with potent antitumor properties for clinical use. Their main mechanism of action is related to their ability to interfere with the mitotic spindle apparatus and thus to trigger cellular arrest in metaphase during mitosis and consequently to cause apoptosis and tumor cell death. On the basis of the pharmacological interest of vinca alkaloids as anticancer agents, there have been developed semisynthetic analogs, including vinorelbine (5′-nor-vinca-alkaloid, modified on the catharanthine ring) and vinflunine (a bis-fluorinated vinorelbine derivative). Since the discovery of vinca alkaloids, both natural and synthetic origin, numerous clinical trials have been carried out to-date to evaluate the efficacy of these compounds against breast cancer. These anticancer agents are commonly used in combination chemotherapy regimens as well as a therapeutic option if other chemotherapy agents fail. The current chapter covers the historical outcome of vinca alkaloids, from the discovery of compounds of natural origin (vinblastine and vincristine) to the synthesis of analogs with anticancer activity (vinorelbine and vinflunine), together with a comprehensive review of the newest preclinical and clinical investigations on these compounds against breast cancer.
Planta Medica, 2021
Depsidones are some of the most abundant secondary metabolites produced by lichens. These compoun... more Depsidones are some of the most abundant secondary metabolites produced by lichens. These compounds have aroused great pharmacological interest due to their activities as antioxidants, antimicrobial, and cytotoxic agents. Hence, this paper aims to provide up-to-date knowledge including an overview of the potential biological interest of lichen depsidones. So far, the most studied depsidones are fumarprotocetraric acid, lobaric acid, norstictic acid, physodic acid, salazinic acid, and stictic acid. Their pharmacological activities have been mainly investigated in in vitro studies and, to a lesser extent, in in vivo studies. No clinical trials have been performed yet. Depsidones are promising cytotoxic agents that act against different cell lines of animal and human origin. Moreover, these compounds have shown antimicrobial activity against both Gram-positive and Gram-negative bacteria and fungi, mainly Candida spp. Furthermore, depsidones have antioxidant properties as revealed in ox...
The quality management means the search of the continuous improvement in the activities and proce... more The quality management means the search of the continuous improvement in the activities and processes, with the aim of reaching the full satisfaction of the needs and requirements of our costumers. That is why we have to take management decisions that must be based in objective data and facts. We wanted to know if the application of a Quality Management System in the Community Pharmacy means a significant improvement in the processes related to the management of the pharmacies, the pharmaceutical care given to the costumers / patients, and their satisfaction level. The results of sixteen different processes indicators, obtained from several community pharmacies (1 to 7 depending on the indicator) that have established a Quality Management System according to the ISO 9001 Norm, were normalized. The time trend of every indicator was adjusted to a straight line, and we analysed, with the F test if the slope was different of 0, considering it significant if p<0.05. The improvement pe...
Current Topics in Medicinal Chemistry, 2021
Lichens are a symbiotic association between a fungus (mycobiont) and a green algae/- cyanobacteri... more Lichens are a symbiotic association between a fungus (mycobiont) and a green algae/- cyanobacterium (photobiont). Lichens are a source of secondary metabolites, most of them being exclusively for these species, among which dibenzofurans are found. Dibenzofurans are a small group (over 35 different identified compounds), being usnic acid the most studied. In the last 10 years, there has been a growing interest in the pharmacological activity of dibenzofurans. In this work, dibenzofurans isolated from lichens (alectosarmentin, condidymic acid, didymic acid, isousnic acid, isostrepsilic acid, usimines A-C and usnic acid) were reviewed, most of which showed antibacterial, antifungal, and cytotoxic activities. These findings provide future guidance for research on pharmacological activity of dibenzofurans.
Proceedings of 6th International Electronic Conference on Medicinal Chemistry, 2020
Proceedings of 6th International Electronic Conference on Medicinal Chemistry, 2020
Proceedings of 6th International Electronic Conference on Medicinal Chemistry, 2020
Food Reviews International, 2020
This systematic review shows the effectiveness of Matricaria chamomilla for improving health. Ori... more This systematic review shows the effectiveness of Matricaria chamomilla for improving health. Original papers and case reports published during 2014–2018 in PubMed, Science Direct and Scopus were i...
Molecules, 2020
Aloe vera has been traditionally used to treat skin injuries (burns, cuts, insect bites, and ecze... more Aloe vera has been traditionally used to treat skin injuries (burns, cuts, insect bites, and eczemas) and digestive problems because its anti-inflammatory, antimicrobial, and wound healing properties. Research on this medicinal plant has been aimed at validating traditional uses and deepening the mechanism of action, identifying the compounds responsible for these activities. The most investigated active compounds are aloe-emodin, aloin, aloesin, emodin, and acemannan. Likewise, new actions have been investigated for Aloe vera and its active compounds. This review provides an overview of current pharmacological studies (in vitro, in vivo, and clinical trials), written in English during the last six years (2014–2019). In particular, new pharmacological data research has shown that most studies refer to anti-cancer action, skin and digestive protective activity, and antimicrobial properties. Most recent works are in vitro and in vivo. Clinical trials have been conducted just with Aloe...
Proceedings of 5th International Electronic Conference on Medicinal Chemistry, 2019
This study reports for first time the antioxidant capacity and cholinesterase inhibitory activity... more This study reports for first time the antioxidant capacity and cholinesterase inhibitory activity of the methanol extract of the lichen Vulpicida pinastri (Scop.) J.E. Mattsson & M.J. Lai and its chemical composition. This lichen specie with a greenish yellow foliose thallus was collected in Puerto Alto del Peñon, Zamora (Spain). Antioxidant capacity was assessed by in vitro tests (DPPH, ORAC and FRAP), total phenolic content by Folin-Ciocalteu method, cholinesterase inhibitory activity by Ellman's colorimetric method and chemical composition by HPLC-UV method. The results showed that the values for antioxidant capacity were IC50 283.7 ± 31.7 g/ml for DPPH, 1.5 ± 0.1 mol TE/mg dry extract for ORAC and 25.4 ± 2.3 mol of Fe2+ eq/g sample for FRAP. Moreover, total phenolic content had a value of 48, 9 ±4.8 g GA/mg. Furthermore, IC50 values were 0.19 ± 0.003 mg/mL for acetylcholinesterase inhibitory activity and 0.89 ± 0.018 mg/mL for butyrylcholinesterase inhibitory activity. Finally, the analysis of chemical composition revealed that the major secondary metabolites were vulpinic acid (9.3 ± 0.8), pinastric acid (41.9 ± 1.07) and usnic acid (36.5 ± 3.62). In conclusion, Vulpicida pinastri is a promising agent to further study for the prevention and treatment of Alzheimer's disease based on its antioxidant and cholinesterase inhibitory activities.
Proceedings of 5th International Electronic Conference on Medicinal Chemistry, 2019
Proceedings of 5th International Electronic Conference on Medicinal Chemistry, 2019
Consumption of medicinal plants for central nervous system (CNS) disorders among university stude... more Consumption of medicinal plants for central nervous system (CNS) disorders among university students in the Community of Madrid 2
Phytochemistry, 2019
Parmelia Acharius is one of the most representative genera within Parmeliaceae family which is th... more Parmelia Acharius is one of the most representative genera within Parmeliaceae family which is the largest and the most widespread family of lichen-forming fungi. Parmelia lichens present a medium to large foliose thallus and they are distributed from the Artic to the Antartic continents, being more concentrated in temperate regions. According to its current description, the genus encompasses up to 41 different species and it is phylogenetically located within the Parmelioid clade (the largest group in the family). Interestingly, some of its species are among the most common epiphytic lichens in Europe such as Parmelia sulcata Taylor and Parmelia saxatilis (L.) Ach. The present work aims at providing a complete overview of the existing knowledge on the genus, from general concepts such as taxonomy and phylogeny, to their ecological relevance and biological interest for pharmaceutical uses. As reported, Parmelia lichens arise as valuable tools for biomonitoring environmental pollution due to their capacity to bioaccumulate metal elements and its response to acid rain. Moreover, they produce a wide array of specialized products/metabolites including depsides, depsidones, triterpenes and dibenzofurans, which have been suggested to exert promising pharmacological activities, mainly antimicrobial, antioxidant and cytotoxic activities. Herein, we discuss past and recent data regarding to the phytochemical characterization of more than 15 species. Even though the knowledge is still scarce in comparsion to other groups of organisms such as higher plants and other non-lichenized fungi. Reviewed works suggest that Parmelia lichens are worthy of further research for determining their actual possibilities as sources of bioactive compounds with potential therapeutic applications.
Natural Product Communications, 2014
The aerial parts of Mentha longifolia L. are used as herbal remedies for curing different disease... more The aerial parts of Mentha longifolia L. are used as herbal remedies for curing different diseases through traditional Bedouin medicine. The antioxidant activity of the ethanolic extracts of M. longifolia was investigated measuring peroxyl radical-scavenging activity by ORAC assay, with Trolox (a water-soluble analogue of α-tocopherol) employed as reference compound. In addition, the total content of phenolic compounds estimated by the Folin-Ciocalteau method and the identification of the polyphenols using high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS) have been performed. Furthermore, the effect of these extracts on cell viability and intracellular ROS production was assayed using the U373-MG human astrocytoma cell line in a H2O2-induced oxidative stress model. Results showed that the major type of polyphenols found were benzoic acids, cinnamic acids, flavones and flavanones. The total phenolic content was 37.7 mg gallic acid/g sample and the ORAC v...
Inflammopharmacology, 2018
Cyanidin and chlorogenic acid are polyphenols from plant origin that are present in many common f... more Cyanidin and chlorogenic acid are polyphenols from plant origin that are present in many common fruits, particularly in berries. To corroborate the protective or detrimental effects of both compounds from a neuro-inflammatory perspective, in vitro experiments were carried out in human astrocytes (U-373). Astrocytes were pre-treated with a range of concentrations of either cyanidin, chlorogenic acid or a combined treatment for a period of 30 min, before exposure to Escherichia coli lipopolysaccharide (LPS) challenge for 23.5 h, after which cytotoxicity (propidium iodide exclusion assay), cytoprotective effects (XTT assay) and effects on functional capacity (secretion of pro-inflammatory cytokines IL-6 and MCP-1) were evaluated. No treatment resulted in cytotoxicity, but high dose (20 µg/mL) LPS significantly reduced mitochondrial reductive capacity (p < 0.001). This effect was prevented in a dose-dependent manner by both cyanidin and chlorogenic acid, as well as by the combination treatment. However, in the absence of LPS, IL-6 secretion was significantly increased in response to 2 µM of either cyanidin or chlorogenic acid (both p < 0.0001), as well as the combination treatment (p < 0.01). MCP-1 secretion followed a similar trend, but did not reach statistical significance. Although we acknowledge the requirement for in vivo investigations to validate our interpretations, current data highlight the potential risk for antioxidant toxicity that is linked to high dose supplementation with single compound antioxidants. Research focused at elucidating synergistic effects between different antioxidants is required to minimise risk of adverse effects.
Journal of Food and Drug Analysis, 2018
Eucalyptus globulus is employed as herbal tea and therapeutical purposes. In this work, it is inv... more Eucalyptus globulus is employed as herbal tea and therapeutical purposes. In this work, it is investigated for first time the neuroprotective activities, based on antioxidant properties, of varying polarity extracts (acetone, ethanol and methanol) from E. globulus leaves and elucidate their main bioactive constituents. Methanol and acetone extracts contained the highest phenolic compounds amount and chlorogenic acid was the major compound identified by UPLC-ESI-MS/MS. Moreover, the three tested extracts showed significant antioxidant properties, varying their potency depending on the in vitro technique used. Furthermore, E. globulus extracts were effective in ameliorating H 2 O 2-induced oxidative stress by increasing cell viability, GSH levels and antioxidant enzymes activity and, by decreasing ROS production and lipid peroxidation levels in SH-SY5Y cells. Taken together, E. globulus leaves extracts could be used as raw material for food and pharmaceutical supplements for their high content in antioxidant compounds with health benefits properties against oxidative stress.
Current Topics in Medicinal Chemistry, 2018
Background: Candida albicans is an opportunistic yeast that causes more than 90% of all vulvovagi... more Background: Candida albicans is an opportunistic yeast that causes more than 90% of all vulvovaginal infections. Because of being inherently resistant to antifungals drugs such as azole derivatives, the search for anti-Candida albicans agents with new pharmacological targets is considered as the main therapeutic strategy to prevent and treat these types of infections. In this context, products of natural origin are a promising source of compounds with antifungal activity. Objective: The current review analyzes clinical evidence on the effectiveness of natural products in the vulvovaginal Candida albicans infections. Method: A literature review in the electronic databases PubMed, Google Scholar, Cochrane Library Plus, Web of Science, Latin American and Caribbean Literature on Health Sciences (Lilacs) and Scientific Electronic Library Online (SciELO) using the search terms “Natural Products”, “Phytotherapy”, “Vulvovaginal Candidiasis” and “Clinical Trials” together with the Boolean te...
Neuroprotective Natural Products, 2017
Pharmaceutical Biology, 2016
Context: Crataegus monogyna Jacq L. (Lind.) (Rosaceae) is used in folk medicine as a sedative, ae... more Context: Crataegus monogyna Jacq L. (Lind.) (Rosaceae) is used in folk medicine as a sedative, aerial parts being rich in polyphenols with antioxidant ability. Objectives: To study the variation in polyphenolic composition and antioxidant ability of spontaneous samples of C. monogyna in order to assess the relationship among these variables. Materials and methods: Aerial parts of C. monogyna were collected from nine different locations in central Spain and extracted with methanol after drying. Total polyphenols were determined by the Folin-Ciocalteu method using gallic acid (GA) as standard. Sixteen polyphenolic compounds (11 flavonoids and 5 phenolic acids) were identified and quantified by reversed-phase HPLC in one single analysis. The antioxidant ability was evaluated by the oxygen radical absorbance capacity (ORAC) and the free radical scavenging activity (DPPH) methods. Linear correlation analysis was used to explore the relationships between the studied variables. Results: Total polyphenol content ranged between 117.729 ± 0.011 and 204.286 ± 0.015 mg GAE/g extract, depending on the geographic origin. No relationship was found between total polyphenols and antioxidant ability by the ORAC or DPPH methods. Chromatographic analysis yielded lower amounts of polyphenols (23.3-143.26 mg/kg), as only flavonoids and phenolic acids were quantified. All the samples exhibited antioxidant activity between 1.32 ± 0.08 and 2.76 ± 0.007 lmol Trolox equivalents/mg and IC 50 from 0.82 ± 0.10 to 3.76 ± 0.67 lg/mL. Conclusion: A statistically significant relationship between flavonoids and phenolic acids content and the antioxidant potential obtained by the ORAC method for C. monogyna samples was proven.
Pharmaceutical Biology, 2015
Pharmacological interest of lichens lies in their capacity to produce bioactive secondary metabol... more Pharmacological interest of lichens lies in their capacity to produce bioactive secondary metabolites, being most of them phenolic compounds with reactive hydroxyl groups that confer antioxidant potential through various mechanisms. Increasing incidence and impact of oxidative stress-related diseases (i.e., neurodegenerative disorders) has encouraged the search of new pharmacological strategies to face them. Lichens appear to be a promising source of phenolic compounds in the discovery of natural products exerting antioxidant activity. The present review thoroughly discusses the available knowledge on antioxidant properties of lichens, including both in vitro and in vivo studies and the parameters assessed so far on lichen constituents. Literature survey was performed by using as main databases PubMed, Google Scholar, Scopus, Science Direct, and Recent Literature on Lichens. We reviewed 98 highlighted research articles without date restriction. Current report collects data related to antioxidant activities of more than 75 lichen species (from 18 botanical families) and 65 isolated metabolites. Much information comes from in vitro investigations, such as chemical assays evaluating radical scavenging properties, lipid peroxidation inhibition, and reducing power of lichen species and compounds; similarly, research on cellular substrates and animal models generally measures antioxidant enzymes levels and other antioxidant markers, such as glutathione levels or tissue peroxidation. Since consistent evidence demonstrated the contribution of oxidative stress on the development and progression of several human diseases, reviewed data suggest that some lichen compounds are worthy of further investigation and better understanding of their antioxidant and neuroprotective potentials.
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Papers by M. Gómez-Serranillos