Pub Date : 2022-01-01DOI: 10.53519/analesranf.2022.88.01.03
Á. Cores Esperón, M. Villacampa
The small molecules development has dominated the design of new drugs until the rise of nucleic acid-based therapies, either by modifying a gene or by preventing it from being effectively transcribed. Taking advantage of this new approaches, the pharmacological intervention in therapeutic targets that are considered unmodifiable up to now with small molecules were allowed. However, these new approaches are not devoid of defects such as low bioavailability due to their stability and pharmacokinetic problems, in addition to being irreversible DNA modifications in many cases, with the subsequent risk of suffering chronic adverse effects. Alternatively, a series of chimeric heterobifunctional compounds, called PROTACs (Protein Targeting Chimeras), have emerged with force in recent years. These PROTACs are able to bring E3 ligases closer with proteins of interest in space to label them with ubiquitin. Finally, it was degraded by the proteasome. This approach enables the generation of different PROTACs structures by rational design and, also, allows the chemical structure modification to improve their stability and pharmacokinetic profile keeping their activity. This review aims to give a comprehensive approach of what PROTACs are, what E3 ligases recruit, relevant factors in PROTAC development, and other approaches similar to this but that use non-proteasomal degradation pathways.
{"title":"Protac: redirecting protein degradation systems to new substrates","authors":"Á. Cores Esperón, M. Villacampa","doi":"10.53519/analesranf.2022.88.01.03","DOIUrl":"https://doi.org/10.53519/analesranf.2022.88.01.03","url":null,"abstract":"The small molecules development has dominated the design of new drugs until the rise of nucleic acid-based therapies, either by modifying a gene or by preventing it from being effectively transcribed. Taking advantage of this new approaches, the pharmacological intervention in therapeutic targets that are considered unmodifiable up to now with small molecules were allowed. However, these new approaches are not devoid of defects such as low bioavailability due to their stability and pharmacokinetic problems, in addition to being irreversible DNA modifications in many cases, with the subsequent risk of suffering chronic adverse effects. Alternatively, a series of chimeric heterobifunctional compounds, called PROTACs (Protein Targeting Chimeras), have emerged with force in recent years. These PROTACs are able to bring E3 ligases closer with proteins of interest in space to label them with ubiquitin. Finally, it was degraded by the proteasome. This approach enables the generation of different PROTACs structures by rational design and, also, allows the chemical structure modification to improve their stability and pharmacokinetic profile keeping their activity. This review aims to give a comprehensive approach of what PROTACs are, what E3 ligases recruit, relevant factors in PROTAC development, and other approaches similar to this but that use non-proteasomal degradation pathways.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71087754","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-12-31DOI: 10.53519/analesranf.2021.87.04.00
Carmen Avendaño López
El Dr. Vicente Larraga, del Centro de Investigaciones Biológicas “Margarita Salas” (CIB-CSIC), recibió el pasado 1 de diciembre el IX Premio FEI al Investigador Innovador del Año 2021 compartido con los Dres. Mariano Esteban y Luis Enjuanes, del Centro Nacional de Biotecnología (CNB-CSIC). Este premio reconoce el esfuerzo de estos tres Profesores de Investigación y de sus grupos de trabajo en la búsqueda de una vacuna española frente al SAR-CoV-2 (COVID-19). ¡Enhorabuena a todos ellos!
{"title":"Reflections on the IX FEI Award for Innovative Researcher of the Year 2021. Difficulties of the development of new medicines in academic researc","authors":"Carmen Avendaño López","doi":"10.53519/analesranf.2021.87.04.00","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.04.00","url":null,"abstract":"El Dr. Vicente Larraga, del Centro de Investigaciones Biológicas “Margarita Salas” (CIB-CSIC), recibió el pasado 1 de diciembre el IX Premio FEI al Investigador Innovador del Año 2021 compartido con los Dres. Mariano Esteban y Luis Enjuanes, del Centro Nacional de Biotecnología (CNB-CSIC). Este premio reconoce el esfuerzo de estos tres Profesores de Investigación y de sus grupos de trabajo en la búsqueda de una vacuna española frente al SAR-CoV-2 (COVID-19). ¡Enhorabuena a todos ellos!","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46029823","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-12-31DOI: 10.53519/analesranf.2022.88.05.25
F. Sánchez-Muniz, A. Macho-González, S. Bastida, A. Garcimartín, A. Bocanegra, A. Canales, Meritxel Nus, Miguel Vázquez-Velasco, L. González-Torres, Rocío Redondo Castillejo, Marina Hernández Martín, María Elvira Muñoz López-Oliva, J. A. Santos, Paloma Celada, M. González-Muñoz, Adriana R Schultz Moreira, J. Benedí
At present, it is considered that the consumption of meat and meat products is excessive and predisposes towards the most prevalent pathologies. Therefore, obtaining meat products with a “healthier” composition and even containing bioactive ingredients that make them functional, acquires relevance in health. General aspects about concept, obtaining methods and current significance in health of functional foods are given. The design of a functional meat product makes it possible to modify the nutritional composition of conventional meat products and ensure a longer shelf life and oxidative stability, as well as helping consumers to improve one or more bodily functions and/or to decrease the risk of suffering degenerative diseases. The publications on functional meat from the AFUSAN group and from other researchers related to the incorporation of whole foods such as nuts or algae into meat matrices, as well as different ingredients for which there is scientific evidence on their role. in health: glucomannans, spirulina, hydroxytyrosol, chia oil, silicon, designer triglycerides enriched in ω-3 polyunsaturated fatty acids, polyphenols from carob pulp. Studies have been conducted in humans with high cardiovascular risk (e.g. overweight/obesity, dyslipidemia, hypertension, tobacco use) and in murine models (Wistar or Zucker fa/fa rats) in which hypercholesterolemia, fatty liver, obesity, or Type 2 Diabetes Mellitus was induced. Although each functional ingredient seems to induce specific changes, it can be pointed out that in many cases these functional foods, compared to conventional ones, are capable of exerting pleiotropic effects in murine models, improving the lipoprotein profile, reducing, among other aspects, oxidative stress and inflammation. In humans, relevant results on lipemia, thrombogenesis and oxidative stress should be highlighted. The use of a carob extract as a functional ingredient of restructured meat exerts multiple effects in models of Type 2 Diabetes at different stages of the disease, particularly in liver and colon, improving in this last organ, the antioxidant status, the integrity of the intestinal barrier and the microbiota plurality. These results suggest the benefits of consuming meat and conventional meat preparations for functional products, which ensure the supply of some nutrients via the meat matrix and eliminate those that imply health risks. The work ends by proposing future lines of action within the framework of a plural, functional and precision diet. Keywords: functional meats; meat shelf life; oxidative modifications functional effects; human; experimental models; obesity; non-alcohlic fatty liver disease; type 2 Diabetes
{"title":"Healthy and functional meat products. Scientific evidence of the AFUSAN group","authors":"F. Sánchez-Muniz, A. Macho-González, S. Bastida, A. Garcimartín, A. Bocanegra, A. Canales, Meritxel Nus, Miguel Vázquez-Velasco, L. González-Torres, Rocío Redondo Castillejo, Marina Hernández Martín, María Elvira Muñoz López-Oliva, J. A. Santos, Paloma Celada, M. González-Muñoz, Adriana R Schultz Moreira, J. Benedí","doi":"10.53519/analesranf.2022.88.05.25","DOIUrl":"https://doi.org/10.53519/analesranf.2022.88.05.25","url":null,"abstract":"At present, it is considered that the consumption of meat and meat products is excessive and predisposes towards the most prevalent pathologies. Therefore, obtaining meat products with a “healthier” composition and even containing bioactive ingredients that make them functional, acquires relevance in health. General aspects about concept, obtaining methods and current significance in health of functional foods are given. The design of a functional meat product makes it possible to modify the nutritional composition of conventional meat products and ensure a longer shelf life and oxidative stability, as well as helping consumers to improve one or more bodily functions and/or to decrease the risk of suffering degenerative diseases. The publications on functional meat from the AFUSAN group and from other researchers related to the incorporation of whole foods such as nuts or algae into meat matrices, as well as different ingredients for which there is scientific evidence on their role. in health: glucomannans, spirulina, hydroxytyrosol, chia oil, silicon, designer triglycerides enriched in ω-3 polyunsaturated fatty acids, polyphenols from carob pulp. Studies have been conducted in humans with high cardiovascular risk (e.g. overweight/obesity, dyslipidemia, hypertension, tobacco use) and in murine models (Wistar or Zucker fa/fa rats) in which hypercholesterolemia, fatty liver, obesity, or Type 2 Diabetes Mellitus was induced. Although each functional ingredient seems to induce specific changes, it can be pointed out that in many cases these functional foods, compared to conventional ones, are capable of exerting pleiotropic effects in murine models, improving the lipoprotein profile, reducing, among other aspects, oxidative stress and inflammation. In humans, relevant results on lipemia, thrombogenesis and oxidative stress should be highlighted. The use of a carob extract as a functional ingredient of restructured meat exerts multiple effects in models of Type 2 Diabetes at different stages of the disease, particularly in liver and colon, improving in this last organ, the antioxidant status, the integrity of the intestinal barrier and the microbiota plurality. These results suggest the benefits of consuming meat and conventional meat preparations for functional products, which ensure the supply of some nutrients via the meat matrix and eliminate those that imply health risks. The work ends by proposing future lines of action within the framework of a plural, functional and precision diet.\u0000\u0000Keywords: functional meats; meat shelf life; oxidative modifications functional effects; human; experimental models; obesity; non-alcohlic fatty liver disease; type 2 Diabetes","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45433873","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.53519/analesranf.2021.87.02.06
F. Minero, Luis Bravo Díaz
It is a bibliographic work that aims to obtain a “Pharmaceutical Look” at the work of García Márquez. It relates medicinal or associated plants, some medicinal and pharmaceutical aspects, with literary works that appear in a representative sample of the author’s novels, including One Hundred Years of Solitude and Love in the Times of Cholera. These novels take place in imaginary or real places in Colombia in the 19th century and the first half of the 20th. Plant remedies and to a lesser extent chemical and animal remedies have been found. For each of them, observations and interpretations medical, social and histórical, have been made that value the pharmacy and medicinal plants, which the author has used as resources to build the novels, regardless of whether they have a scientific basis or not. For this they are accompanied by textual literary texts. In conclusion, we highlight the masterful way in which García uses these resources and we recommend their reading or re-reading, also taking into account that at the same time it can be done from a pharmaceutical point of view.
{"title":"PHARMACY AND MEDICINAL PLANTS IN THE LITERATURE: CASE OF GARCÍA MÁRQUEZ","authors":"F. Minero, Luis Bravo Díaz","doi":"10.53519/analesranf.2021.87.02.06","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.02.06","url":null,"abstract":"It is a bibliographic work that aims to obtain a “Pharmaceutical Look” at the work of García Márquez. It relates medicinal or associated plants, some medicinal and pharmaceutical aspects, with literary works that appear in a representative sample of the author’s novels, including One Hundred Years of Solitude and Love in the Times of Cholera. These novels take place in imaginary or real places in Colombia in the 19th century and the first half of the 20th. Plant remedies and to a lesser extent chemical and animal remedies have been found. For each of them, observations and interpretations medical, social and histórical, have been made that value the pharmacy and medicinal plants, which the author has used as resources to build the novels, regardless of whether they have a scientific basis or not. For this they are accompanied by textual literary texts. In conclusion, we highlight the masterful way in which García uses these resources and we recommend their reading or re-reading, also taking into account that at the same time it can be done from a pharmaceutical point of view.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71086091","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.53519/analesranf.2021.87.01.06
Teresa Gil Alegre
I try to bring the pharmacy office closer from its legislation to its professional practice, focusing on less known points such as pharmaceutical care and quality of life, the psychiatric profile that accompanies non-adherence to medical therapy. I would like to draw the conclusion that I have managed to interest so that the mission of the pharmacists and pharmacy technicians who are part of them is known.
{"title":"PHARMACY OFFICE. PHARMACEUTICAL CARE. PERSONALIZED DOSING SERVICE","authors":"Teresa Gil Alegre","doi":"10.53519/analesranf.2021.87.01.06","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.01.06","url":null,"abstract":"I try to bring the pharmacy office closer from its legislation to its professional practice, focusing on less known points such as pharmaceutical care and quality of life, the psychiatric profile that accompanies non-adherence to medical therapy. I would like to draw the conclusion that I have managed to interest so that the mission of the pharmacists and pharmacy technicians who are part of them is known.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71086229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.53519/analesranf.2021.87.02.03
Albino García Sacristán
In 1921, Otto Loewi published an experimental study that gave rise to the birth of the chemical theory of nerve transmission, according to which, the nerve current causes, at the end of nerve fibers, the release of a chemical substance called a neurotransmitter. For his discoveries related to the chemical neurotransmission of nerve impulses, Loewi received the Nobel Prize in Physiology or Medicine in 1936.
{"title":"OTTO LOEWI: ONE HUNDRED YEARS OF CONFIRMATION OF CHEMICAL NEUROTRANSMISSION","authors":"Albino García Sacristán","doi":"10.53519/analesranf.2021.87.02.03","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.02.03","url":null,"abstract":"In 1921, Otto Loewi published an experimental study that gave rise to the birth of the chemical theory of nerve transmission, according to which, the nerve current causes, at the end of nerve fibers, the release of a chemical substance called a neurotransmitter. For his discoveries related to the chemical neurotransmission of nerve impulses, Loewi received the Nobel Prize in Physiology or Medicine in 1936.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71086378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.53519/analesranf.2021.87.02.09
J. García
Squalene is a hydrocarbon intermediary involved in the biosynthesis of phytosterols and terpenes in plants and of cholesterol in animals. Its discovery backs to 1916. Recent research on biological effects has shown this compound to display antioxidant, anti-inflammatory and anti-atherosclerotic properties. When animals accumulate in the liver, this fatty liver does not influence their longevity, but influences both gene expression networks and post-transcriptional protein levels. Combination of squalene with other biological compounds is an open aspect to develop functional food to control oxidative stress and aging in human and veterinary medicine. Its current use in cosmetics or as vaccine adjuvant makes of it a coveted molecule. Traditionally, sharps have been its source. However, the impact of their capture for this purpose is unsustainable and the search for new sources is highly required. The quest for those in order to reach the demand poses new technological challenges.
{"title":"SQUALENE, A VIBRANT MOLECULE DESPITE ITS ONE-HUNDRED-FIVE-YEAR OLD DISCOVERY","authors":"J. García","doi":"10.53519/analesranf.2021.87.02.09","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.02.09","url":null,"abstract":"Squalene is a hydrocarbon intermediary involved in the biosynthesis of phytosterols and terpenes in plants and of cholesterol in animals. Its discovery backs to 1916. Recent research on biological effects has shown this compound to display antioxidant, anti-inflammatory and anti-atherosclerotic properties. When animals accumulate in the liver, this fatty liver does not influence their longevity, but influences both gene expression networks and post-transcriptional protein levels. Combination of squalene with other biological compounds is an open aspect to develop functional food to control oxidative stress and aging in human and veterinary medicine. Its current use in cosmetics or as vaccine adjuvant makes of it a coveted molecule. Traditionally, sharps have been its source. However, the impact of their capture for this purpose is unsustainable and the search for new sources is highly required. The quest for those in order to reach the demand poses new technological challenges.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71086902","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.53519/analesranf.2021.87.03.07
R. Rodríguez Nozal
Max Weber (1864-1920), in his classic Die protestantische Ethik und der Geist des Kapitalismus, tried to justify the unequal industrial development of the different European countries based on the religious division of the continent as result of the Lutheran Reformation; According to their approach, the establishment of Protestantism in the north and centre and Catholicism in the south became the northern areas prosperous and the southern areas depressed, encouraging a tendency in the Protestant countries towards factory work, in opposition to the Catholic preference for craftsmanship. As far as the pharmaceutical industry was concerned, this approach led to two different models: the Central European model, Protestant-inspired, and the Mediterranean model, established in mainly Catholic countries such as Spain. The pharmaceutical industry was the driving force behind the new therapeutics that emerged during the 19th century, and it did so by acting on the two fundamental components of the drug: composition and presentation; while the Central European and Anglo-Saxon countries were inclined to promote the composition, the Mediterranean pharmaceutical industry channelled its efforts towards the final consumer product, the “pharmaceutical speciality”. Taking this framework into account, our intention is to offer a general overview of the Spanish pharmaceutical industry prior to the Transition, based on a series of stages ranging from the emergence of drugstore pharmacies in the mid-19th century to the establishment of pharmaceutical laboratories during Franco’s regime, including the classification of what we know as industrial medicines (“secret remedies”, “specific” and “pharmaceutical specialities”), their legal recognition (Stamp Act and health registration), their raw materials and main pharmaceutical forms.
{"title":"Historical development of the pharmaceutical industry in Spain prior to Transition","authors":"R. Rodríguez Nozal","doi":"10.53519/analesranf.2021.87.03.07","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.03.07","url":null,"abstract":"Max Weber (1864-1920), in his classic Die protestantische Ethik und der Geist des Kapitalismus, tried to justify the unequal industrial development of the different European countries based on the religious division of the continent as result of the Lutheran Reformation; According to their approach, the establishment of Protestantism in the north and centre and Catholicism in the south became the northern areas prosperous and the southern areas depressed, encouraging a tendency in the Protestant countries towards factory work, in opposition to the Catholic preference for craftsmanship. As far as the pharmaceutical industry was concerned, this approach led to two different models: the Central European model, Protestant-inspired, and the Mediterranean model, established in mainly Catholic countries such as Spain. The pharmaceutical industry was the driving force behind the new therapeutics that emerged during the 19th century, and it did so by acting on the two fundamental components of the drug: composition and presentation; while the Central European and Anglo-Saxon countries were inclined to promote the composition, the Mediterranean pharmaceutical industry channelled its efforts towards the final consumer product, the “pharmaceutical speciality”. Taking this framework into account, our intention is to offer a general overview of the Spanish pharmaceutical industry prior to the Transition, based on a series of stages ranging from the emergence of drugstore pharmacies in the mid-19th century to the establishment of pharmaceutical laboratories during Franco’s regime, including the classification of what we know as industrial medicines (“secret remedies”, “specific” and “pharmaceutical specialities”), their legal recognition (Stamp Act and health registration), their raw materials and main pharmaceutical forms.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71087314","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.53519/analesranf.2021.87.04.06
P. Esbrit Argüelles
Osteoporosis, the most prevalent pathology affecting the skeleton, currently represents a challenge for Western societies. Bone mass loss with age, mainly but not exclusively related to estrogen deficiency, increases fracture risk. Fracture repair is frequently impaired due to metabolic alterations and/or the extention of bone damage. Thus, strategies like use of osteogenic factors that help regenerate damaged bone tissue are highly needed. In this regard, systemic administration of parathormone (PTH) represents the first anabolic treatment in osteoporosis by predominantly increasing bone formation over bone resorption during bone remodeling. Recently, there is a pharmacological alternative to PTH based on a peptide analogue derived from the N-terminal sequence of PTH-related protein (PTHrP) (named abaloparatide). This peptide exhibits great affinity for PTH type 1 receptor, and presents pharmacokinetic advantages (decreasing the risk of hipercalcemia), compared to PTH in the treatment of osteoporosis. N-terminal peptides of both PTH and PTHrP promote the formation of fracture callus and bone healing in animal models of bone injury. In addition, osteostatin peptide derived from the C-terminal tail of PTHrP -unrelated to PTH- displays osteogenic features in vitro and in vivo in osteoporosis models. In recent years, osteostatin loading into various types of implants (including mesoporous bioceramics based on SiO and Zn-doped bioglasses) improves the capacity of the biomaterial to increase bone regeneration. Current data support the notion that PTHrP-derived peptides are a promising strategy for bone tissue engineering applications.
{"title":"Use of peptides derived from parathyroid hormone-related protein for increasing bone formation and bone regeneration","authors":"P. Esbrit Argüelles","doi":"10.53519/analesranf.2021.87.04.06","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.04.06","url":null,"abstract":"Osteoporosis, the most prevalent pathology affecting the skeleton, currently represents a challenge for Western societies. Bone mass loss with age, mainly but not exclusively related to estrogen deficiency, increases fracture risk. Fracture repair is frequently impaired due to metabolic alterations and/or the extention of bone damage. Thus, strategies like use of osteogenic factors that help regenerate damaged bone tissue are highly needed. In this regard, systemic administration of parathormone (PTH) represents the first anabolic treatment in osteoporosis by predominantly increasing bone formation over bone resorption during bone remodeling. Recently, there is a pharmacological alternative to PTH based on a peptide analogue derived from the N-terminal sequence of PTH-related protein (PTHrP) (named abaloparatide). This peptide exhibits great affinity for PTH type 1 receptor, and presents pharmacokinetic advantages (decreasing the risk of hipercalcemia), compared to PTH in the treatment of osteoporosis. N-terminal peptides of both PTH and PTHrP promote the formation of fracture callus and bone healing in animal models of bone injury. In addition, osteostatin peptide derived from the C-terminal tail of PTHrP -unrelated to PTH- displays osteogenic features in vitro and in vivo in osteoporosis models. In recent years, osteostatin loading into various types of implants (including mesoporous bioceramics based on SiO and Zn-doped bioglasses) improves the capacity of the biomaterial to increase bone regeneration. Current data support the notion that PTHrP-derived peptides are a promising strategy for bone tissue engineering applications.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71087195","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.53519/analesranf.2021.87.03.10
Antonio Marcilla Díaz
Extracellular vesicles participate in intercellular communications, altogether with classic mechanisms like direct contact between cells and the secretion of mediators. They have attracted considerable interest since their discovery in reticulocytes in 1983. The term includes different types of vesicles that vary in size and origin, with exosomes, microvesicles and apoptotic bodies as the major ones. These structures are sorrounded by a lipid membrane, where various types of receptors are located, and can carry different cargo molecules, including sugars, proteins, nucleic acids and metabolites. They have been described in all kingdoms in nature (participating in both intercellular and inter-specific communications), in all types of biological fluids (as part of liquid biopsy). In fact, their presence in samples from both physiological and pathological processes has suggested them as excellent biomarkers. Their role in health and disease is being widely investigated. In this context, the study of extracellular vesicles produced by parasites, and specifically by helminths, constitutes a growing field of research, with great biomedical interest, mainly in the control of infections caused by them. In fact, these vesicles can be used to generate rapid and specific diagnosis systems, to produce new tools for vaccination, and to identify targets for new treatments. The ability of extracellular vesicles to modulate the immune response also opens new possibilities for their use against autoimmune diseases.
{"title":"Extracellular vesicles in the host-helminth communication: biomedical applications","authors":"Antonio Marcilla Díaz","doi":"10.53519/analesranf.2021.87.03.10","DOIUrl":"https://doi.org/10.53519/analesranf.2021.87.03.10","url":null,"abstract":"Extracellular vesicles participate in intercellular communications, altogether with classic mechanisms like direct contact between cells and the secretion of mediators. They have attracted considerable interest since their discovery in reticulocytes in 1983. The term includes different types of vesicles that vary in size and origin, with exosomes, microvesicles and apoptotic bodies as the major ones. These structures are sorrounded by a lipid membrane, where various types of receptors are located, and can carry different cargo molecules, including sugars, proteins, nucleic acids and metabolites. They have been described in all kingdoms in nature (participating in both intercellular and inter-specific communications), in all types of biological fluids (as part of liquid biopsy). In fact, their presence in samples from both physiological and pathological processes has suggested them as excellent biomarkers. Their role in health and disease is being widely investigated. In this context, the study of extracellular vesicles produced by parasites, and specifically by helminths, constitutes a growing field of research, with great biomedical interest, mainly in the control of infections caused by them. In fact, these vesicles can be used to generate rapid and specific diagnosis systems, to produce new tools for vaccination, and to identify targets for new treatments. The ability of extracellular vesicles to modulate the immune response also opens new possibilities for their use against autoimmune diseases.","PeriodicalId":50795,"journal":{"name":"Anales De La Real Academia Nacional De Farmacia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71087467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}