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The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition)

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A special issue of Nutrients (ISSN 2072-6643). This special issue belongs to the section "Nutritional Epidemiology".

Deadline for manuscript submissions: 25 April 2025 | Viewed by 11114

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Prof. Dr. Jacqueline Isaura Alvarez-Leite

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Departamento de Bioquímica e Imunologia, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil
Interests: obesity; inflammation; immunity; bioactive compounds; nutrition; apolipoproteins
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Special Issue Information

Dear Colleagues,

Bioactive compounds are being studied to better understand their effects on health and disease. These compounds are found in several foods, such as beverages (wine, cedar, juices), vegetable oils, spices (curcuma, pepper, etc.), teas and infusions. Through the results of in vitro or in vivo studies, some of these compounds have already showed several potentially beneficial effects on human health and in the prevention of disease. Plant bioactive compounds are of great interest in this area due to the range of compound varieties and actions, such as thermogenesis, inflammation, metabolism and endocrine factors.

More research is needed to explore their use in improving physical performance; the aging process; or preventing or helping treat diseases such as obesity, CVD, diabetes mellitus tumors and inflammatory processes in general.

In this context, we invite you to submit your research work or experience to the Special Issue “The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition)”. Clinical, experimental and in vitro studies, as well as reviews on the effects of bioactive compounds in obesity and its comorbidities, are welcome.

Prof. Dr. Jacqueline Isaura Alvarez-Leite
Guest Editor

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Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Nutrients is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

bioactive compounds
obesity
diabetes
tumors
inflammatory
cardiovascular disease
plants
immunity
diet
nutrition

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Published Papers (8 papers)

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20 pages, 879 KiB

Open AccessArticle

Preliminary Data on the Senolytic Effects of Agrimonia pilosa Ledeb. Extract Containing Agrimols for Immunosenescence in Middle-Aged Humans: A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Comparison Study

by Yoshiki Shimizu, Shieri Shimodan, Mariko Hayashida, Misato Yazaki, Tsuyoshi Sakurada, Tomomichi Watanabe, Yuri Ishii, Yoshie Hirose, Jiro Saito and Sachiyuki Teramoto

Nutrients 2025, 17(4), 667; https://doi.org/10.3390/nu17040667 - 13 Feb 2025

Viewed by 1200

Abstract

Objectives: To assess the effects of agrimol-containing Agrimonia pilosa Ledeb. extract (APE) for senescent immune cell removal in middle-aged Japanese adults with immunosenescence. Design and Setting: A randomized, double-blind, placebo-controlled, parallel-group study was conducted in Japan between June 2023 and April 2024. Participants: 110 individuals aged 40–59, selected based on CD8+ T cells with highly-expressing-senescence-associated-β-galactosidase (SA-βGal). Intervention: Participants were randomly assigned to receive 50 mg APE containing 0.2 mg of agrimols or a placebo for eight consecutive weeks. Measurements: The primary endpoint was the change in the proportion of CD8+ T cells with high SA-βGal expression at 8 weeks of intake from the baseline. The secondary endpoints included the proportion of CD4+ T cells with high SA-βGal expression, CD4+ and CD8+ T cell subsets, and the ratio of various immune cells. Results: Of the 635 subjects screened, 110 with immunosenescence were included in this study. In total, 55 participants in the placebo group and 53 in the APE group completed the intervention. There were no statistically significant changes in either the primary or secondary endpoints due to APE intake. In the male population, the proportion of CD8+ T cells with high SA-βGal expression was reduced by APE intake (p = 0.044). Furthermore, the proportion of naïve CD8+ T cells increased and the number of effector memory CD8+ T cells decreased with the consumption of APE. Conclusions: APE was suggested to reduce senescent immune cells, indicating its potential as a candidate senolytic agent for humans; however, the results of this study are preliminary data, and further research on APE is needed (clinical trial registration: UMIN000051574). Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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18 pages, 6248 KiB

Open AccessArticle

The Effect of Flavonoids and Topiramate on Glucose Carbon Metabolism in a HepG2 Steatosis Cell Culture Model: A Stable Isotope Study

by Li Ma, Qing-Yi Lu, Shu Lim, Guang Han, Laszlo G. Boros, Mina Desai and Jennifer K. Yee

Nutrients 2025, 17(3), 564; https://doi.org/10.3390/nu17030564 - 31 Jan 2025

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Abstract

Background: Insufficient treatment options are available for metabolic dysfunction-associated steatotic liver disease (MASLD). Flavonoids and topiramate have been studied for weight loss but need investigation into their effects on liver metabolism. This study’s aim was to examine the effects of flavonoids or topiramate on glucose metabolic carbon flux in a cell culture model of steatosis. Methods: Steatosis was induced in HepG2 cells through exposure to oleic acid (OA, 0.5 mml/L) conjugated to bovine serum albumin (2:1). Additionally, 50% U¹³C-glucose was supplied in the medium as a stable isotope tracer. Cells were treated with DMSO, 10 μM of naringenin, morin, silibinin, or topiramate (44 μM) for 72 h. A non-steatotic, untreated HepG2 cell control was included. Cell extracts were analyzed by gas chromatography/mass spectrometry and mass isotopomer distribution analysis for glycogen synthesis, de novo fatty acid synthesis, tricarboxylic acid (TCA) cycle activity, and ribose synthesis. Groups were compared by ANOVA with Tukey’s pair-wise testing. Results: Compared to untreated HepG2 controls, OA-exposed steatotic cells exhibited increased lipid accumulation by ORO staining (1.6-fold), enhanced palmitate de novo synthesis, reduced pyruvate carboxylase/pyruvate dehydrogenase (PC/PDH) ratio, and reduced ribose synthesis. Treatment with topiramate or silibinin ameliorated the lipid accumulation (1.3-fold) and mitigated enhancement of de novo synthesis. Morin-treated cells exhibited enhanced de novo synthesis but suppressed ribose synthesis. Conclusions: Potential mechanisms of reduced lipid accumulation by topiramate and silibinin may include suppression of palmitate de novo synthesis and a relative decrease in carbon flux through the PDH pathway. Further studies are needed on potential utility in MASLD based on their specific metabolic effects. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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23 pages, 4328 KiB

Open AccessArticle

Herbal Extracts Mixed with Essential Oils: A Network Approach for Gastric and Intestinal Motility Disorders

by Roberta Budriesi, Ivan Corazza, Simone Roncioni, Roberta Scanferlato, Dalila De Luca, Carla Marzetti, Roberto Gotti, Nicola Rizzardi, Christian Bergamini, Matteo Micucci, Davide Roncarati and Laura Beatrice Mattioli

Nutrients 2024, 16(24), 4357; https://doi.org/10.3390/nu16244357 - 17 Dec 2024

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Abstract

Background: Three herbal extracts (Asparagus racemosus Willd., Tabebuia avellanedae Lorentz, and Glycyrrhiza glabra L.) were mixed with three essential oils (Foeniculum vulgare Mill., Mentha piperita L., and Pimpinella anisum L.) to formulate a product (HEMEO) whose active compounds include saponins and steroids in Asparagus racemosus, known for their anti-inflammatory properties; glycyrrhizin and flavonoids in Glycyrrhiza glabra, which exhibit gastroprotective and antispasmodic effects; menthol in Mentha piperita, contributing with antispasmodic and antimicrobial properties; and anethole and polyphenols in Pimpinella anisum, which modulate intestinal motility and offer antimicrobial activity. Objective: HEMEO was formulated for applications in intestinal motility disorders. Methods: HEMEO was evaluated for spontaneous and induced motility effects in isolated guinea pig ileum, colon, and stomach. Ex vivo experiments were conducted using LabChart software v7.0, and the product’s antibacterial action against Helicobacter pylori and its antioxidant effects were assessed through disc diffusion and FRAP assays. The presence of the volatile compounds in the formulation was confirmed by GC-MS analysis; the TPC of HEMEO, determined using the Folin–Ciocalteu method, was 9.925 ± 0.42 mg GAE/g. Conclusions: HEMEO showed a phenolic content correlated with its antioxidant potential and in addition inhibited H. pylori growth and demonstrated notable antioxidant properties, suggesting its role as a supportive agent in digestive processes and in managing motility disorders. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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14 pages, 1619 KiB

Open AccessArticle

Capsaicin Improves Systemic Inflammation, Atherosclerosis, and Macrophage-Derived Foam Cells by Stimulating PPAR Gamma and TRPV1 Receptors

by Danielle Lima Ávila, Weslley Fernandes-Braga, Janayne Luihan Silva, Elandia Aparecida Santos, Gianne Campos, Paola Caroline Lacerda Leocádio, Luciano Santos Aggum Capettini, Edenil Costa Aguilar and Jacqueline Isaura Alvarez-Leite

Nutrients 2024, 16(18), 3167; https://doi.org/10.3390/nu16183167 - 19 Sep 2024

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Abstract

Background: Capsaicin, a bioactive compound found in peppers, is recognized for its anti-inflammatory, antioxidant, and anti-lipidemic properties. This study aimed to evaluate the effects of capsaicin on atherosclerosis progression. Methods: Apolipoprotein E knockout mice and their C57BL/6 controls were utilized to assess blood lipid profile, inflammatory status, and atherosclerotic lesions. We also examined the influence of capsaicin on cholesterol influx and efflux, and the role of TRPV1 and PPARγ signaling pathways in bone marrow-derived macrophages. Results: Capsaicin treatment reduced weight gain, visceral adiposity, blood triglycerides, and total and non-HDL cholesterol. These improvements were associated with a reduction in atherosclerotic lesions in the aorta and carotid. Capsaicin also improved hepatic oxidative and inflammatory status. Systemic inflammation was also reduced, as indicated by reduced leukocyte rolling and adhesion on the mesenteric plexus. Capsaicin decreased foam cell formation by reducing cholesterol influx through scavenger receptor A and increasing cholesterol efflux via ATP-binding cassette transporter A1, an effect primarily linked to TRPV1 activation. Conclusions: These findings underscore the potential of capsaicin as a promising agent for atherosclerosis prevention, highlighting its comprehensive role in modulating lipid metabolism, foam cell formation, and inflammatory responses. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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16 pages, 3227 KiB

Open AccessArticle

Euglena gracilis Enhances Innate and Adaptive Immunity through Specific Expression of Dectin-1 in CP-Induced Immunosuppressed Mice

by Hwan Hee Lee, Ji-Yeon Seong, Hyojeung Kang and Hyosun Cho

Nutrients 2024, 16(18), 3158; https://doi.org/10.3390/nu16183158 - 18 Sep 2024

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Abstract

Background: Euglena gracilis (E. gracilis), a species of unicellular algae, can accumulate large amounts of β-1,3-glucan paramylon, a polysaccharide, in its cytoplasm and has recently attracted interest as a bioproduct due to its various health benefits. In this study, the immune-enhancing effect of E. gracilis powder (EP) was investigated in vitro and in vivo. Methods: In vitro, the production of NO and cytokines and the mechanism of the signaling pathway of β-1,3-glucan were identified in RAW264.7 cells. In vivo, cyclophosphamide-induced (CP-induced) immunosuppressed C57BL/6 female mice were orally administered with three different concentrations (100, 300, and 600 mg/kg) of EP daily. After 14 days, the organs and whole blood were collected from each animal for further study. Results: The weight loss of CP-treated mice was reversed by treatment with EP to levels comparable to those of control mice. In addition, the frequencies of NK1.1⁺, CD3⁺, CD4⁺, CD8⁺, and B220⁺ in immune cells isolated from the spleen were increased by EP treatment compared with water or RG. The secretion of TNF-α, IFN-γ, and IL-12 from splenocytes was also increased by EP treatment, as was the level of IgM in the serum of the mice. Finally, EP treatment specifically upregulated the expression of dectin-1 in the liver of CP-treated mice. Conclusions: E. gracilis could be a good candidate for a natural immune stimulator in the innate and adaptive response by secreting TNF-α, IFN-γ, and IL-12 through stimulating dectin-1 expression on the surface of immune cells. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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16 pages, 1946 KiB

Open AccessArticle

Botanical Bioflavonoid Composition from Scutellaria baicalensis- and Acacia catechu-Protected Mice against D-Galactose-Induced Immunosenescence, and Cyclophosphamide Induced Immune Suppression

by Mesfin Yimam, Teresa Horm, Alexandria O’Neal, Paola Chua, Ping Jiao, Mei Hong and Qi Jia

Nutrients 2024, 16(18), 3144; https://doi.org/10.3390/nu16183144 - 18 Sep 2024

Viewed by 1354

Abstract

Oxidative stress and chronic inflammation create a perpetual cycle in the elderly, where impaired immune function amplifies susceptibility to oxidative damage, and oxidative stress further weakens the immune response. This cycle is particularly detrimental to the respiratory system of the elderly, which is an easy target for constant exogenous harmful attacks during cold/flu season or under heavy air pollution. Herbal medicines that protect respiratory function are seen as safer alternatives to conventional therapies; however, there is limited availability of scientifically validated, safe, and effective natural supplements for these conditions. In this study, we evaluated a standardized bioflavonoid composition, UP446, that contains bioactives from the roots of Scutellaria baicalensis and the heartwoods of Acacia catechu as a natural and nutritional supplement for its antioxidative and immunoregulatory effects in oxidative stress-accelerated aging and chemically induced immune suppression mouse models. Immunosenescence was induced through the repeated subcutaneous inoculation of D-galactose (D-Gal) at a dose of 500 mg/kg/day in CD-1 mice. UP446 was administered orally at doses of 100 mg/kg and 200 mg/kg starting in the fifth week of immunosenescence induction. This study lasted a total of ten weeks. All mice received a quadrivalent influenza vaccine 2 weeks before termination. Whole blood, serum, spleen homogenate, and thymus tissues were processed for analysis. Cyclophosphamide (Cy)-induced immunosuppression was triggered by three consecutive injections of cyclophosphamide at 80 mg/kg/day, followed by the oral administration of UP446 for 18 days at doses of 100 mg/kg and 200 mg/kg. Blood was collected from each animal at necropsy, and serum was isolated for IgA and IgG ELISA analysis. UP446 was found to improve immune response, as evidenced by the stimulation of innate (NK cells) and adaptive immune responses (T cells and cytotoxic T cells), an increase in antioxidant capacity (glutathione peroxidase), the preservation of vital immune organs (the thymus), and a reduction in NFκB. UP446 also increased serum levels of IgA and IgG. The findings presented in this report demonstrate the antioxidative, anti-inflammatory, and immune-regulatory activities of UP446, suggesting its potential use in respiratory conditions involving immune stress due to aging, oxidative stress, and/or pathogenic challenges. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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12 pages, 2186 KiB

Open AccessArticle

Antihypertensive Effects of Lindera erythrocarpa Makino via NO/cGMP Pathway and Ca²⁺ and K⁺ Channels

by Sujin Shin, Junkyu Park, Ho-Young Choi, Youngmin Bu and Kyungjin Lee

Nutrients 2024, 16(17), 3003; https://doi.org/10.3390/nu16173003 - 5 Sep 2024

Viewed by 1477

Abstract

Studies have demonstrated the therapeutic effects of Lindera plants. This study was undertaken to reveal the antihypertensive properties of Lindera erythrocarpa leaf ethanolic extract (LEL). Aorta segments of Sprague–Dawley rats were used to study the vasodilatory effect of LEL, and the mechanisms involved were evaluated by treating specific inhibitors or activators that affect the contractility of blood vessels. Our results revealed that LEL promotes a vasorelaxant effect through the nitric oxide/cyclic guanosine 3′,5′-monophosphate pathway, blocking the Ca²⁺ channels, opening the K⁺ channels, and inhibiting the vasoconstrictive action of angiotensin II. In addition, the effects of LEL on blood pressure were investigated in spontaneously hypertensive rats by the tail-cuff method. LEL (300 or 1000 mg/kg) was orally administered to the rats, and 1000 mg/kg of LEL significantly lowered the blood pressure. Systolic blood pressure decreased by −20.06 ± 4.87%, and diastolic blood pressure also lowered by −30.58 ± 5.92% at 4 h in the 1000 mg/kg LEL group. Overall, our results suggest that LEL may be useful to treat hypertensive diseases, considering its vasorelaxing and hypotensive effects. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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9 pages, 1552 KiB

Open AccessBrief Report

Effect of Ficus pumila L. on Improving Insulin Secretory Capacity and Resistance in Elderly Patients Aged 80 Years Old or Older Who Develop Diabetes After COVID-19 Infection

by Kenji Gonda, Takeshi Hai, Kouichi Suzuki, Akihiko Ozaki, Takashi Shibusa, Seiichi Takenoshita, Yuko Maejima and Kenjyu Shimomura

Nutrients 2025, 17(2), 290; https://doi.org/10.3390/nu17020290 - 15 Jan 2025

Viewed by 1079

Abstract

(1) Background: It has been reported that people affected by COVID-19, an infectious disease caused by SARS-CoV-2, suffer from various diseases, after infection. One of the most serious problems is the increased risk of developing diabetes after COVID-19 infection. However, a treatment for post-COVID-19 infection diabetes has not yet been established. In this study, we investigated the effects of Ficus pumila L. extract, which has traditionally been used to reduce blood glucose levels in Okinawa, on patients who developed diabetes after COVID-19 infection. (2) Methods: In total, 128 rehabilitation patients aged 80 years old or older who developed diabetes after COVID-19 infection were included. The HOMA-β (Homeostatic model assessment of β-cell function) and HOMA-IR (Homeostatic model assessment of insulin resistance) were assessed to evaluate the glucose tolerance. (3) Results: The HOMA-β decreased and HOMA-IR increased in patients who developed after diabetes after COVID-19 infection. Subsequently, 59 patients were given Ficus pumila L. extract and their HOMA-β and HOMA-IR improved after ingestion. On the other hand, the control group of patients who did not consume Ficus pumila L. showed no improvement in both HOMA-β and HOMA-IR. (4) Conclusions: Ficus pumila L. extract, ingested by patients who developed diabetes after COVID-19 infection, stimulated insulin secretion capacity and improved insulin resistance. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Diseases (2nd Edition))

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