Bioactive Compounds From Plants and Their Therapeutic Applications in Lifestyle-Related Diseases

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (25 April 2025) | Viewed by 14064

Special Issue Editors


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Guest Editor
Department of Natural Products Chemistry, Daiichi University of Pharmacy, Fukuoka, Japan
Interests: obesity; diabetes; traditional medicines; metabolism
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Pharmacognosy with the Medicinal Plant Garden, Medical University of Lublin, Lublin, Poland
Interests: terpenoids, essential oils and volatile extracts; chromatographic techniques; isolation; bryophytes natural product chemistry; bioactivity-guided isolation of compounds from medicinal; aromatic, and spore-forming plants; chemosystematics of liverworts based on their terpenoid, aromatic, and phenolic constituents
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear colleagues,

Plants are a source of a wide range of compounds that are ingredients in many pharmaceutical agents. However, while there are many scientific reports regarding the identification of new compounds, their pharmacological activity has not been fully investigated. For this reason, accompanied by the fact that medicinal plants are still an interesting subject of scientific work, the search for new biologically active compounds and studies on new applications of already known natural compounds, especially in lifestyle-related diseases, are interesting and necessary.

This Special Issue, titled “Bioactive Compounds from Plants and their Therapeutic Applications in Lifestyle-related Diseases”, aims to collect both original articles and comprehensive reviews related to the research aimed at elucidating the pharmacological actions of plant-derived compounds using methods-based on cell lines and laboratory animals, as well as clinical trials. Submitted manuscripts should focus on the wide range of diseases related to lifestyle, such as obesity, diabetes, atherosclerosis, hepatic steatosis, dementia, and mental health disorders. Papers reporting medicinal properties with new molecular mechanisms will be appreciated. Authors are encouraged to submit their research based on single components as well as mixtures, upon comprehensive chemical characterization.

We believe that the papers collected within this Special Issue will contribute to the treatment and prevention of lifestyle-related diseases, which may help save many patients.

We are looking forward to your contribution.

Dr. Syota Kagawa
Dr. Agnieszka Ludwiczuk
Guest Editors

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Keywords

  • natural compounds
  • lifestyle-related diseases
  • pharmacology
  • molecular mechanisms
  • clinical applications

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Related Special Issue

Published Papers (6 papers)

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Research

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23 pages, 1563 KiB  
Article
Bioactive Compounds, Antioxidant, Cytotoxic, and Genotoxic Investigation of the Standardized Liquid Extract from Eugenia involucrata DC. Leaves
by Monatha Nayara Guimarães Teófilo, Leonardo Gomes Costa, Jamira Dias Rocha, Fernando Gomes Barbosa, Anielly Monteiro de Melo, Grazzielle Guimarães de Matos, Cristiane Maria Ascari Morgado, Amanda Silva Fernandes, Lucas Barbosa Ribeiro de Carvalho, Clayson Moura Gomes, Milton Adriano Pelli de Oliveira, Joelma Abadia Marciano de Paula, Elisa Flávia Luiz Cardoso Bailão and Leonardo Luiz Borges
Pharmaceuticals 2025, 18(5), 764; https://doi.org/10.3390/ph18050764 - 21 May 2025
Viewed by 401
Abstract
Background: Eugenia involucrata DC., a Cerrado native plant, is recognized for its medicinal properties. However, its bioactive compounds remain inadequately explored. Objectives: This study investigated bioactive compounds from a standardized liquid extract from E. involucrata leaves that can act with antioxidant, [...] Read more.
Background: Eugenia involucrata DC., a Cerrado native plant, is recognized for its medicinal properties. However, its bioactive compounds remain inadequately explored. Objectives: This study investigated bioactive compounds from a standardized liquid extract from E. involucrata leaves that can act with antioxidant, cytogenotoxic, cytoprotective, and genoprotective effects. Methods: The phenolic compounds in the standardized liquid extract from E. involucrata leaves were screened by HPLC-DAD. The capture of the free radicals DPPH, ABTS+, and the metal reduction power FRAP determined the antioxidant potential. Cytotoxicity was evaluated in RAW 264.7 macrophages (MTT assay), and (anti)cytotoxic and (anti)genotoxic effects were assessed in human lymphocytes using the Trypan blue exclusion method and comet assay, respectively. Results: The extracts present key phenolic compounds, such as ellagic acid, myricitrin, and epicatechin gallate. The standardized extract demonstrated antioxidant capacity, evidenced by its ability to reduce iron and scavenge free radicals. The liquid extract from E. involucrata leaves exhibited cytotoxic effects on RAW 264.7 macrophages at higher concentrations, while demonstrating (anti)cytotoxic activity on human lymphocytes from all tested concentrations. The highest concentration tested of the standardized liquid extract from E. involucrata leaves (250 µg/mL) showed genotoxicity against human lymphocytes compared to the negative control. In contrast, the lowest concentration (62.5 µg/mL) exhibited an antigenotoxic effect on human lymphocytes, reducing the genotoxicity of doxorubicin by approximately 27%. Conclusions: The bioactive compounds in the standardized liquid extract from E. involucrata leaves exhibited antioxidant and antigenotoxic properties, suggesting potential value for nutraceutical and pharmaceutical applications, particularly those related to oxidative stress associated withaging and disease progression. Full article
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29 pages, 12098 KiB  
Article
Mechanistic Advances in the Therapeutic Application of Bixin for Lung Inflammation In Vitro and In Vivo
by Alexsandro Tavares Figueiredo-Junior, Bruno Clemente Brandão Marques, Douglas Galdino dos Santos, Wesley Leandro Gouveia, Raysa Magali Pillpe Meza, Luzineide Wanderley Tinoco, Lídia Moreira Lima, Samuel Santos Valenca and Manuella Lanzetti
Pharmaceuticals 2025, 18(4), 530; https://doi.org/10.3390/ph18040530 - 5 Apr 2025
Viewed by 509
Abstract
Background: Nrf2 plays a key role in regulating the antioxidant response against oxidative stress. Therefore, it is imperative to examine the advantages of Nrf2 activation by new small molecules capable of inhibiting the Nrf2-Keap1 protein interaction that do not present electrophilic sites, since [...] Read more.
Background: Nrf2 plays a key role in regulating the antioxidant response against oxidative stress. Therefore, it is imperative to examine the advantages of Nrf2 activation by new small molecules capable of inhibiting the Nrf2-Keap1 protein interaction that do not present electrophilic sites, since electrophilic compounds have intrinsic toxicity. The bixin pigment has been used as a form of treatment and prevention of several pathological conditions in animal models since it was described as an Nrf2 activator without electrophilic sites. This study aims to synthetize a soluble derivate KBx (potassium bixinate) and evaluate its ability to activate Nrf2/ARE in a model of exposure to cigarette smoke extract (CSE; in vitro) and intranasal LPS administration (in vivo). Methods: In the in vivo study, C57BL/6 mice were pretreated with 200 mg/kg of KBx (gavage) during 5 consecutive days and then challenged with 60 µg of LPS i.n. for 16 h. Bronchoalveolar lavage was collected to examine cytokines dosage. In the in vitro study, RAW 264.7 macrophages were exposed to CSE and post-treated with KBx to evaluate their ability to revert the redox imbalance caused by the stressor. Results: KBx was characterized using mass spectrometry (433.1778 m/z). KC levels were increased in the LPS group (p = 0.021), and KBx inhibited this (p = 0.001). IL-10 levels were decreased (p = 0.055) in the LPS group that was prevented when pretreated with KBx (p = 0.037). The in vitro study showed KBx to be a more potent derivate of bixin through its ability to intercept ROS formation with three-fold more potency, and it showed an anti-inflammatory propriety by reducing the nuclear translocation of p65 (p < 0.001). Conclusions: In conclusion, these data suggest that KBx was able to activate the Nrf2/ARE pathway and intercept ROS formation induced by CSE and LPS in both in vivo and in vitro studies. Full article
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15 pages, 3100 KiB  
Article
Low-Dose Oral Ginger Improves Daily Symptom Scores in Asthma
by Charles W. Emala, Tarnjot K. Saroya, Yuqi Miao, Shuang Wang, Shengmin Sang and Emily A. DiMango
Pharmaceuticals 2024, 17(12), 1651; https://doi.org/10.3390/ph17121651 - 8 Dec 2024
Viewed by 4070
Abstract
Background/Objective: A significant number of individuals with asthma have poorly controlled daily symptoms and utilize dietary supplements such as ginger in a quest for improved symptom control; however, its effectiveness at improving the control of symptoms is unproven. We questioned whether low-dose oral [...] Read more.
Background/Objective: A significant number of individuals with asthma have poorly controlled daily symptoms and utilize dietary supplements such as ginger in a quest for improved symptom control; however, its effectiveness at improving the control of symptoms is unproven. We questioned whether low-dose oral ginger would improve subjective and objective measurements of asthma control in mild-to-moderate asthmatics. Methods: We performed a randomized, placebo-controlled, double-blinded study of a low dose (1 g twice daily) of a dietary supplement of ginger in 32 mild-to-moderate uncontrolled asthmatics over a 2-month trial period while maintaining daily conventional asthma therapies. The planned primary outcomes included an increased tolerance to inhaled methacholine and decreased concentrations of fractional excretion of exhaled nitric oxide (FeNO). Secondary planned outcomes included measurements of asthma control by the Asthma Control Test (ACT), a 2-week symptom recall test, and the Juniper mini Asthma Quality of Life Questionnaire (AQLQ), and blood eosinophils and asthma-associated cytokines. Results: Exhaled nitric oxide or blood eosinophils were not changed by oral ginger. However, three different measures of asthma symptom control were improved by the 28-day time point of oral ginger. Asthma-associated serum cytokines (IL-13 and IL-17A) were modulated by oral ginger. Conclusions: This is the first demonstration that a small daily dose of a dietary supplement of ginger may improve asthma symptoms and reduce inflammation in human asthmatics. These findings support the need for additional studies using larger doses of ginger in specific endotypes of asthmatics that may identify a novel therapeutic for asthma. Full article
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19 pages, 4182 KiB  
Article
Rutin-Activated Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Attenuates Corneal and Heart Damage in Mice
by Promise M. Emeka, Lorina I. Badger-Emeka, Krishnaraj Thirugnanasambantham and Abdulaziz S. Alatawi
Pharmaceuticals 2024, 17(11), 1523; https://doi.org/10.3390/ph17111523 - 12 Nov 2024
Viewed by 1326
Abstract
Background: Corneal degeneration is a form of progressive cell death caused by multiple factors, such as diabetic retinopathy. It is the most well-known neural degenerative disease caused by macular degeneration in the aged and those with retinitis pigmentosa. Myocardial infarction is becoming a [...] Read more.
Background: Corneal degeneration is a form of progressive cell death caused by multiple factors, such as diabetic retinopathy. It is the most well-known neural degenerative disease caused by macular degeneration in the aged and those with retinitis pigmentosa. Myocardial infarction is becoming a more common burden, causing cardiomyocyte degeneration, ischemia, and heart tissue death. This study examined the preventive effects of rutin on isoproterenol (ISO)-induced oxidative damage (that is, inflammation) on rabbit corneal epithelial cells and mouse heart injuries. Methods: These investigations involved a cytotoxicity test, biochemical analysis, qRT-PCR, Western blotting, and mouse cardiac histopathology. Results: The results showed that rutin enhanced ADH7 and ALDH1A1, retinoic acid signaling components in SIRC1 rabbit corneal cell lines. The production of NO by ocular epithelial cells was significantly reduced. It reduced cTnT and cTnI, CK-MB, and LDH contents in mouse cardiac tissue. The nuclear expressions of Nrf2, Sirt, and HO-1 were all increased by rutin. Docking studies revealed a good interaction between rutin and the Keap protein, enhancing Nrf2 nuclear activity. Conclusions: This showed that rutin can potentially enhance ADH7 and ALDH1A1 corneal signaling components, preventing corneal degeneration and mitigating ISO-induced myocardial infarction (MI) via Keap/Nrf2 expressions. Full article
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Review

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25 pages, 6166 KiB  
Review
Evaluating the Anti-Osteoporotic Potential of Mediterranean Medicinal Plants: A Review of Current Evidence
by Alhareth Abdulraheem Al-Ajalein, Nurul ‘Izzah Ibrahim, Mh Busra Fauzi, Sabarul Afian Mokhtar, Isa Naina Mohamed, Ahmad Nazrun Shuid and Norazlina Mohamed
Pharmaceuticals 2024, 17(10), 1341; https://doi.org/10.3390/ph17101341 - 8 Oct 2024
Cited by 2 | Viewed by 2378
Abstract
Background: Bones are biological reservoirs for minerals and cells, offering protection to the other organs and contributing to the structural form of the body. Osteoporosis is a prevalent bone condition that significantly impacts people’s quality of life. Treatments utilizing natural products and medicinal [...] Read more.
Background: Bones are biological reservoirs for minerals and cells, offering protection to the other organs and contributing to the structural form of the body. Osteoporosis is a prevalent bone condition that significantly impacts people’s quality of life. Treatments utilizing natural products and medicinal plants have gained important attention in the management of osteoporosis and its associated implications, such as osteoporotic fractures. Even though thousands of plants grow in the Mediterranean region, the use of medicinal plants as an alternative therapy for osteoporosis is still limited. Methods: This article provides a comprehensive overview of seven Mediterranean medicinal plants that are used in osteoporosis and osteoporotic fractures in in vitro, in vivo, and clinical trials. The mechanism of action of the medicinal plants and their bioactive compounds against diseases are also briefly discussed. Results: The findings clearly indicate the ability of the seven medicinal plants (Ammi majus, Brassica oleracea, Ceratonia siliqua L., Foeniculum vulgare, Glycyrrhiza glabra, Salvia officinalis, and Silybum marianum) as anti-osteoporosis agents. Xanthotoxin, polyphenols, liquiritin, formononetin, silymarin, and silibinin/silybin were the main bioactive compounds that contributed to the action against osteoporosis and osteoporotic fractures. Conclusions: In this review, the Mediterranean medicinal plants prove their ability as an alternative agent for osteoporosis and osteoporotic fractures instead of conventional synthetic therapies. Thus, this can encourage researchers to delve deeper into this field and develop medicinal-plant-based drugs. Full article
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61 pages, 16027 KiB  
Review
High-Altitude Medicinal Plants as Promising Source of Phytochemical Antioxidants to Combat Lifestyle-Associated Oxidative Stress-Induced Disorders
by Mohammad Vikas Ashraf, Sajid Khan, Surya Misri, Kailash S. Gaira, Sandeep Rawat, Balwant Rawat, M. A. Hannan Khan, Ali Asghar Shah, Mohd Asgher and Shoeb Ahmad
Pharmaceuticals 2024, 17(8), 975; https://doi.org/10.3390/ph17080975 - 23 Jul 2024
Cited by 18 | Viewed by 3692
Abstract
Oxidative stress, driven by reactive oxygen, nitrogen, and sulphur species (ROS, RNS, RSS), poses a significant threat to cellular integrity and human health. Generated during mitochondrial respiration, inflammation, UV exposure and pollution, these species damage cells and contribute to pathologies like cardiovascular issues, [...] Read more.
Oxidative stress, driven by reactive oxygen, nitrogen, and sulphur species (ROS, RNS, RSS), poses a significant threat to cellular integrity and human health. Generated during mitochondrial respiration, inflammation, UV exposure and pollution, these species damage cells and contribute to pathologies like cardiovascular issues, neurodegeneration, cancer, and metabolic syndromes. Lifestyle factors exert a substantial influence on oxidative stress levels, with mitochondria emerging as pivotal players in ROS generation and cellular equilibrium. Phytochemicals, abundant in plants, such as carotenoids, ascorbic acid, tocopherols and polyphenols, offer diverse antioxidant mechanisms. They scavenge free radicals, chelate metal ions, and modulate cellular signalling pathways to mitigate oxidative damage. Furthermore, plants thriving in high-altitude regions are adapted to extreme conditions, and synthesize secondary metabolites, like flavonoids and phenolic compounds in bulk quantities, which act to form a robust antioxidant defence against oxidative stress, including UV radiation and temperature fluctuations. These plants are promising sources for drug development, offering innovative strategies by which to manage oxidative stress-related ailments and enhance human health. Understanding and harnessing the antioxidant potential of phytochemicals from high-altitude plants represent crucial steps in combating oxidative stress-induced disorders and promoting overall wellbeing. This study offers a comprehensive summary of the production and physio-pathological aspects of lifestyle-induced oxidative stress disorders and explores the potential of phytochemicals as promising antioxidants. Additionally, it presents an appraisal of high-altitude medicinal plants as significant sources of antioxidants, highlighting their potential for drug development and the creation of innovative antioxidant therapeutic approaches. Full article
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