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  • 1
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    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-04-05
    Description: Many macro and micro species, from terrestrial and aquatic environments, produce structurally unique compounds and, in many countries, still are the primary sources of medicines. In fact, secondary metabolites are an important source of chemotherapeutic agents but are also lead compounds for synthetic modification and the optimization of biological activity. Therefore, the exploitation of secondary metabolites, or their inspired synthetic compounds, offers excellent opportunities for the pharmaceutical industry. This Medicines Special Issue focuses on the great potential of secondary metabolites for therapeutic application. The Special Issue contains 16 articles reporting relevant experimental results, and an overview of bioactive secondary metabolites, their biological effects, and new methodologies that improve and accelerate the process of obtained lead compounds with regard to new drug development. We would like to thank all 83 authors, from all over the world, for their valuable contributions to this Special Issue.
    Keywords: QD1-999 ; Q1-390 ; antitumor ; triterpenoids ; seaweeds ; diterpenes ; Boswellia ; antioxidant activity ; antiplasmodial ; Maytenus chiapensis ; phenolic derivatives ; secondary metabolites ; medicinal applications ; Malus x domestica ; pectin ; cytotoxic activity ; xanthine oxidase ; phytochemistry ; antioxidant ; Scabiosa ; sugars ; sargaquinoic acid ; pentacyclic triterpenoids ; analysis ; antimicrobial and anticancer activity ; iridoids ; Tuscany ; GC-MS ; (-)-rabdosiin ; kratom ; plant defense ; cembranoids ; tingenone ; deoxypodophyllotoxin ; anticancer ; pristimerin ; inflammation ; boswellic acids ; plants ; anti-inflammatory ; legalization ; Mitragyna speciosa ; Ocimum sanctum ; cordycepin ; cytotoxic ; medicine ; Artemisia species ; antimicrobial activity ; lignans ; Artemisia vachanica ; Cordyceps militaris ; frankincense ; ancient varieties ; sargahydroquinoic acid ; Tajikistan ; antiSMASH ; ABTS ; polyphenols ; therapeutics ; infectious diseases ; antibacterial ; nutraceutics ; total phenolics ; LC-MS/MS ; innate immunity ; HPLC-PAD ; sarganaphthoquinoic acid ; biosynthetic gene clusters ; DPPH ; EGCG ; cneorubenoids ; PPAR-? ; bowel diseases ; amentoflavone ; molecular docking ; sargachromenoic acid ; cannabinoids ; flavonoids ; essential oils ; TCM ; HPLC-PDA ; ascorbic acid ; antioxidants ; Lamiaceae ; nanoemulsion ; malaria ; therapeutic uses ; quinonemethide triterpenoids ; artemisinin ; natural products ; biological activities ; FRAP ; toxicology ; defensins ; Celastraceae ; cannabis ; vector control ; Juniperus ; analytical determination ; thema EDItEUR::P Mathematics and Science::PN Chemistry
    Language: English
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  • 2
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    Publication Date: 2019-07-30
    Description: Knowledge about folk medicines is limited to elder community members of remote communities, like Sete Cidades in the Azores. The Azores, 1300 km west of Portugal, are nine volcanic islands, totalling 2330 km2 of land dispersed by 173,200 km2 in the North Atlantic Ocean. The present study aims to scientifically document the uses of plant species for medicinal purposes, in the Sete Cidades. Twenty-eight community members from 40 to 84 years of age, of whom half were 55 to 64 years old, were interviewed. Twenty-nine taxa were reported as being used for medicinal purposes, ten of which have not been previously reported for ethnomedicinal use in Portugal, with a first record of the use of Morella faya. Leaves were the most used plant part (55%), and decoction the most common preparation mode. The five reported taxa with both the highest use value (0.71–0.25) and relative frequency of citation (0.14–0.11) were Clinopodium menthifolium subsp. ascendens, Aloysia citriodora, Mentha x piperita, Citrus limon and Rosmarinus officinalis. The traditional uses of some of the reported plants are supported by scientific studies, confirming their ethnomedicinal value and the need to preserve local knowledge of folk medicine practices.
    Electronic ISSN: 2223-7747
    Topics: Biology
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  • 4
    Publication Date: 2020-03-26
    Description: Recently there is a great social expectation that scientists should produce more sustainable and environmentally friendly chemical processes. Within this necessity, biocatalysis presents many attractive features because reactions are often performed in water, under mild conditions, the catalyst is biodegradable and can be obtained from renewable raw materials. In this work, we propose a simple, rapid and low-cost method for the preparation and application of an enzymatic extract from turnip root. The protocol described includes (1) the preparation of the enzymatic extract, (2) the procedure for the assessment of the more favorable working parameters (temperature, pH) and (3) the methodology for the application of the extract as the catalyst for biotransformation reactions. We anticipate that the protocol in this research will provide a simple way for obtaining an enzymatic extract which can operate efficiently under mild conditions and can effectively catalyze the biotransformation of simple phenols.
    Electronic ISSN: 2409-9279
    Topics: Biology , Medicine
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  • 5
    Publication Date: 2019-12-20
    Description: Macroalgae are increasingly viewed as a source of secondary metabolites with great potential for the development of new drugs. In this development, in vitro studies are only the first step in a long process, while in vivo studies and clinical trials are the most revealing stages of the true potential and limitations that a given metabolite may have as a new drug. This literature review aims to give a critical overview of the secondary metabolites that reveal the most interesting results in these two steps. Phlorotannins show great pharmaceutical potential in in vivo models and, among the several examples, the anti-dyslipidemia activity of dieckol must be highlighted because it was more effective than lovastatin in an in vivo model. The IRLIIVLMPILMA tridecapeptide that exhibits an in vivo level of activity similar to the hypotensive clinical drug captopril should still be stressed, as well as griffithsin which showed such stunning results over a variety of animal models and which will probably move onto clinical trials soon. Regarding clinical trials, studies with pure algal metabolites are scarce, limited to those carried out with kahalalide F and fucoxanthin. The majority of clinical trials currently aim to ascertain the effect of algae consumption, as extracts or fractions, on obesity and diabetes.
    Electronic ISSN: 1660-3397
    Topics: Chemistry and Pharmacology
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  • 6
    Publication Date: 2020-06-10
    Description: Nature represents an amazing source of inspiration since it produces a great diversity of natural compounds selected by evolution, which exhibit multiple biological activities and applications. A large and very active research field is dedicated to identifying biosynthesized compounds, to improve/develop new methodologies to produce/reuse natural compounds and to assess their potential for pharmaceutical, cosmetic and food industries, among others, and also to understand their mechanism of action. Here, the main results presented in each work are highlighted. The applications suggested are mostly related to pharmacological uses and involve mainly pure natural compounds and essential oils. These works are significant contributions and reinforce the dynamic field of natural products applications.
    Electronic ISSN: 2076-3417
    Topics: Natural Sciences in General
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  • 7
    Publication Date: 2020-04-25
    Description: Sesquiterpene lactones, a vast range of terpenoids isolated from Asteraceae species, exhibit a broad spectrum of biological effects and several of them are already commercially available, such as artemisinin. Here the most recent and impactful results of in vivo, preclinical and clinical studies involving a selection of ten sesquiterpene lactones (alantolactone, arglabin, costunolide, cynaropicrin, helenalin, inuviscolide, lactucin, parthenolide, thapsigargin and tomentosin) are presented and discussed, along with some of their derivatives. In the authors’ opinion, these compounds have been neglected compared to others, although they could be of great use in developing important new pharmaceutical products. The selected sesquiterpenes show promising anticancer and anti-inflammatory effects, acting on various targets. Moreover, they exhibit antifungal, anxiolytic, analgesic, and antitrypanosomal activities. Several studies discussed here clearly show the potential that some of them have in combination therapy, as sensitizing agents to facilitate and enhance the action of drugs in clinical use. The derivatives show greater pharmacological value since they have better pharmacokinetics, stability, potency, and/or selectivity. All these natural terpenoids and their derivatives exhibit properties that invite further research by the scientific community.
    Electronic ISSN: 2076-3417
    Topics: Natural Sciences in General
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  • 8
    Publication Date: 2020-08-23
    Description: Seaweed beach-casts are a seasonal phenomenon that regularly deposits tons of algae biomass on beaches, which are usually disposed of in landfills. The present work aimed to contribute to the valorization of this biomass by studying bioactivities that reveal its potential in the pharmaceutical and/or cosmeceutical industries. Methanol and ethanol extracts and fractions from 15 beach-casts biomass were tested for a range of bioactivities. Eight of the most active samples exhibit IC50 values between 11.38 µg/mL and 19.28 µg/mL and selectivity indexes higher than 3.8, against NCI-H1299 (lung cancer) and T47D (breast cancer). Concerning antiaging potential, all the extracts tested presented UV protection, with SPF values above 30, like the standard sunscreen. Regarding aging-related enzymes, 24 samples were tyrosinase inhibitors exhibiting IC50 values from 9.01 µg/mL to 200.09 µg/mL. Eight extracts inhibited collagenase (IC50 〈 248.76 µg/mL), two of them more actively than positive control EDTA (IC50 = 59.26 µg/mL). In addition to UV protection, the cumulative effect of antityrosinase and anticollagenase activities shown by the samples suggest that they may play a significant role in preventing skin photoaging. The results obtained demonstrate the high potential of beach-cast seaweed biomass as sources of cosmetic bioproducts with antiaging effects, and of selective cytotoxic metabolites.
    Electronic ISSN: 2076-3417
    Topics: Natural Sciences in General
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  • 9
    Publication Date: 2019-05-06
    Description: An imbalance in the production of reactive oxygen species in the body can cause an increase of oxidative stress that leads to oxidative damage to cells and tissues, which culminates in the development or aggravation of some chronic diseases, such as inflammation, diabetes mellitus, cancer, cardiovascular disease, and obesity. Secondary metabolites from Inula species can play an important role in the prevention and treatment of the oxidative stress-related diseases mentioned above. The databases Scopus, PubMed, and Web of Science and the combining terms Inula, antioxidant and secondary metabolites were used in the research for this review. More than 120 articles are reviewed, highlighting the most active compounds with special emphasis on the elucidation of their antioxidative-stress mechanism of action, which increases the knowledge about their potential in the fight against inflammation, cancer, neurodegeneration, and diabetes. Alantolactone is the most polyvalent compound, reporting interesting EC50 values for several bioactivities, while 1-O-acetylbritannilactone can be pointed out as a promising lead compound for the development of analogues with interesting properties. The Inula genus is a good bet as source of structurally diverse compounds with antioxidant activity that can act via different mechanisms to fight several oxidative stress-related human diseases, being useful for development of new drugs.
    Electronic ISSN: 2076-3921
    Topics: Chemistry and Pharmacology
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  • 10
    Publication Date: 2019-07-17
    Description: Chalcones and flavanones are isomeric structures and also classes of natural products, belonging to the flavonoid family. Moreover, their wide range of biological activities makes them key scaffolds for the synthesis of new and more efficient drugs. In this work, the synthesis of hydroxy and/or methoxychalcones was studied using less common bases, such as sodium hydride (NaH) and lithium bis(trimethylsilyl)amide (LiHMDS), in the aldol condensation. The results show that the use of NaH was more effective for the synthesis of 2′-hydroxychalcone derivatives, while LiHMDS led to the synthesis of polyhydroxylated chalcones in a one-pot process. During this study, it was also possible to establish the conditions that favor their isomerization into flavanones, allowing at the same time the synthesis of hydroxy and/or methoxyflavanones. The chalcones and flavanones obtained were evaluated to disclose their antioxidant, anticholinesterasic, antibacterial and antitumor activities. 2′,4′,4-Trihydroxychalcone was the most active compound in terms of antioxidant, anti-butyrylcholinesterase (IC50 26.55 ± 0.55 μg/mL, similar to control drug donepezil, IC50 28.94 ± 1.76 μg/mL) and antimicrobial activity. 4′,7-Dihydroxyflavanone presented dual inhibition, that is, the ability to inhibit both cholinesterases. 4′-Hydroxy-5,7-dimethoxyflavanone and 2′-hydroxy-4-methoxychalcone were the compounds with the best antitumor activity. The substitution pattern and the biological assay results allowed the establishment of some structure/activity relationships.
    Electronic ISSN: 2076-3417
    Topics: Natural Sciences in General
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