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Biological Research on Plant Bioactive Compounds

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: 25 August 2025 | Viewed by 5701

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Special Issue Editors

Dr. Adriana Trifan

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Guest Editor

Department of Pharmacognosy-Phytotherapy, Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy Iasi, 700115 Iasi, Romania
Interests: pharmacognosy; phytochemistry; high-resolution mass spectrometry; gas chromatography; antimicrobials; anticancer; anti-inflammatory
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Dr. Simon Vlad Luca

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Biothermodynamics, TUM School of Life Sciences, Technical University of Munich, 85354 Freising, Germany
Interests: Natural products; medicinal plants; phytochemistry; metabolite profiling; high-resolution mass spectrometry; downstream processing; liquid–liquid chromatography; centrifugal partition chromatography; countercurrent chromatography; anti-inflammatory; anticancer
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue on plant bioactive compounds aims to provide an extensive overview of their potential applications in treating and managing a wide range of human diseases. Plant bioactive compounds, which encompass primary and specialized metabolites, are small molecules naturally produced by various plants. These compounds are notable for their significant biological properties, making them highly useful in medical applications. There is a growing interest in pharmaceuticals and bioactive compounds derived from natural products due to their significant health benefits.

This Special Issue seeks to influence the future research trajectory of important natural products and their related bioactive compounds by featuring high-quality, cutting-edge research and molecular insights from research groups worldwide.

The scope of this Special Issue includes, but is not limited to, the following:

Natural products;
Medicinal chemistry;
Pharmacology;
Other related research fields.

We invite original research articles and review articles that cover the molecular aspects of these topics. We look forward to your valuable contributions and to advancing the field of natural bioactive compounds.

Dr. Adriana Trifan
Dr. Simon Luca
Guest Editors

Manuscript Submission Information

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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

plant bioactive compounds
extraction and analysis of plant bioactive compounds
bioactivity and pharmacokinetics of plant compounds
natural products and modern diseases
plant bioactive compounds and by-products
discovery and development of natural plant drugs

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Published Papers (7 papers)

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Research

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18 pages, 3761 KiB

Open AccessArticle

Effects of Bioconverted Guava Leaf (Psidium guajava L.) Extract on Skeletal Muscle Damage by Regulation of Ubiquitin–Proteasome System and Apoptosis in Type 2 Diabetic Mice

by Heaji Lee, Bo-Gyu Jun, Su-Hyun Kim, Choong Hwan Lee and Yunsook Lim

Int. J. Mol. Sci. 2025, 26(8), 3877; https://doi.org/10.3390/ijms26083877 - 19 Apr 2025

Viewed by 120

Abstract

Skeletal muscle atrophy is one of the serious complications of diabetes, which increases the risk of frailty, falls, and mortality. However, interventions for muscle atrophy are limited, and research is needed regarding the treatment of muscle wasting. Recently, the bioconversion of natural products by lactic acid bacteria has been highlighted as a possibility to improve the bioavailability of active ingredients. This process also produces metabolites, which are key signaling mediators for a variety of physiological functions. This study investigated the effect of bioconverted guava leaf (Psidium guajava L., GL) by Lactobacillus plantarum on hyperglycemia-induced skeletal muscle atrophy in type 2 diabetes mellites (T2DM) mice. Diabetes was induced by a high-fat diet with a two-time streptozotocin (STZ) injection (60 mg/kg BW) in male C57BL/6J mice. After diabetes was induced (a fasting blood glucose level (FBG) ≥ 300 mg/dL), the mice were administered with GL (100 mg/kg/day) or bioconverted GL (FGL) (50 mg/kg/day) by oral gavage for 14 weeks. FGL contains different substances such as hydroxyl-isocaproic acid and hydroxyl-isovaleric acid compared to GLE itself, which have potential to prevent muscle degradation in T2DM mice. GL and FGL supplementation reduced the FBG level in T2DM mice. In addition, GL and FGL supplementation enhanced muscle strength, the skeletal muscle cross-sectional area, and ameliorated ubiquitin–proteasome system (UPS)-related pathways in T2DM mice. On the other hand, GLE supplementation ameliorated glucose tolerance demonstrated by oral glucose tolerance test and enhanced insulin signaling pathway. In addition, only FGL supplementation attenuated skeletal muscle inflammation and apoptosis with an improved mammalian target of the rapamycin (mTOR)-autophagy-related pathway. Although administered at a half dose of GLE, FGL demonstrated greater efficacy in regulating the expression of these molecular markers. The result suggests that even GL itself has anti-diabetic effects, and the functionality would be enhanced by the bioconversion of GL with L. Plantarum, which has an additive or/and a synergistic effect. Taken together, FGL could be used as a potential nutraceutical to attenuate muscle degradation by the inhibition of inflammation, the UPS, and the apoptosis pathway. Full article

(This article belongs to the Special Issue Biological Research on Plant Bioactive Compounds)

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17 pages, 3736 KiB

Open AccessArticle

Molecular Mechanism of Vine Tea Dihydromyricetin Extract on Alleviating Glucolipid Metabolism Disorder in db/db Mice: Based on Liver RNA-Seq and TLR4/MyD88/NF-κB Pathway

by Xixin Zhou, Xin Liu, Yuhang Yi, Shiyun Chen, Yi Zhang, Wei Fan, Chenghao Lv and Si Qin

Int. J. Mol. Sci. 2025, 26(5), 2169; https://doi.org/10.3390/ijms26052169 - 28 Feb 2025

Viewed by 481

Abstract

The primary active compound in vine tea is dihydromyricetin (DMY), which has a longstanding history as a dietary supplement and traditional ethnic medicine. However, the precise molecular mechanism by which vine tea dihydromyricetin extract (VDMY) regulates glucolipid metabolic disorder remains unclear. In this study, we first assessed the effect of VDMY on various physiological parameters in db/db mice, followed by RNA sequencing (RNA-seq) to identify key signaling pathways affected by VDMY in liver tissues. We also examined the impact of VDMY on the liver’s TLR4/MyD88/NF-κB and FOXO1 pathways using Western blotting. Our results showed that VDMY significantly reduced fasting blood glucose (FBG), total cholesterol (TC), triglycerides (TGs), and low-density lipoprotein cholesterol (LDL-C), while increasing high-density lipoprotein cholesterol (HDL-C) levels. Additionally, VDMY enhanced the liver’s antioxidant capacity by upregulating superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH), while lowering malondialdehyde (MDA), alanine aminotransferase (ALT), and aspartate aminotransferase (AST), thus alleviating liver damage. RNA-seq analysis further revealed that VDMY influenced multiple biological processes, including transcription, glycolysis, gluconeogenesis, and redox reactions, suggesting that its effects may be mediated through the TLR4/MyD88/NF-κB and FOXO1 pathways. Additionally, Western blot analysis revealed that VDMY effectively downregulated the expressions of TLR4, MyD88, NF-κB, and FOXO1 proteins in the liver of db/db mice, indicating that VDMY could target these pathways to intervene glucolipid metabolism dysfunction. Full article

(This article belongs to the Special Issue Biological Research on Plant Bioactive Compounds)

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16 pages, 2917 KiB

Open AccessArticle

Vicenin-2 Hinders Pro-Inflammatory Response via Targeting the CaMKKβ-AMPK-SIRT1 Axis in Lipopolysaccharide-Stressed THP-1 Cells

by Alessandro Maugeri, Caterina Russo, Giuseppe Tancredi Patanè, Martina Farina, Antonio Rapisarda, Mariorosario Masullo and Michele Navarra

Int. J. Mol. Sci. 2025, 26(5), 2077; https://doi.org/10.3390/ijms26052077 - 27 Feb 2025

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Abstract

Plant secondary metabolites are known to be valuable agents to hamper inflammation owing to their multiple mechanisms of action. This study investigates the molecular mechanisms underlying the anti-inflammatory effects of vicenin-2 in lipopolysaccharide (LPS)-stressed THP-1 cells. After ascertaining the safety of vicenin-2 in our in vitro model, we assessed the anti-inflammatory potential of this flavonoid. Indeed, it counteracted the increase of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 levels, as well as the overexpression of both inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 caused by the exposure of THP-1 cells to LPS. Acknowledged the role of SIRT1 in the inflammatory process, we focused our attention on this enzyme. Our results showed that LPS dramatically decreased the expression of SIRT1, whereas vicenin-2 restored the levels of this enzyme to those of unexposed cells. These effects were also observed in terms of acetylated p53, a SIRT1 substrate. Notably, we observed that vicenin-2 did not act as a direct activator of SIRT1. Therefore, we investigated the potential involvement of AMP-activated protein kinase (AMPK), an upstream activator of SIRT1. Of note, by blocking AMPK by dorsomorphin, the protective effects of vicenin-2 on SIRT1 expression and activity were lost, suggesting the engagement of this kinase. Consequently, the blockage of AMPK caused a downstream loss of the anti-inflammatory effect of vicenin-2, which was no longer able to decrease both the activation of nuclear factor (NF)-κB and the production of cytokines induced by LPS. Finally, docking simulation suggested that vicenin-2 might act as an activator of Ca²⁺/calmodulin-dependent protein kinase kinase β (CaMKKβ), one of the regulators of AMPK. Overall, our results suggest that the anti-inflammatory effects of vicenin-2 may be due to the interaction with the CaMKKβ-AMPK-SIRT1 axis. Full article

(This article belongs to the Special Issue Biological Research on Plant Bioactive Compounds)

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18 pages, 3524 KiB

Open AccessArticle

Viability and Radiosensitivity of Human Tumor Cells from Breast and Colon Are Influenced by Hypericum perforatum Extract HP01

by Linda Rebecca Haake, Ahmed El Menuawy, Hannes Rennau, Frank Marthe, Urs Hähnel, Felix Bock, Guido Hildebrandt and Katrin Manda

Int. J. Mol. Sci. 2025, 26(2), 622; https://doi.org/10.3390/ijms26020622 - 13 Jan 2025

Viewed by 737

Abstract

To enhance the treatment of tumors that are resistant to radio- and chemotherapy while minimizing the side effects of radiochemotherapy, researchers are continuously seeking new active compounds for use in combination with radiotherapy. Therefore, the aim of our study was to examine the cytotoxic and radiosensitizing effects of an extract from St. John’s Wort (Hypericum perforatum), referred to as HP01, on human epithelial tumor cells in vitro. The growth of MCF-7 (breast carcinoma) and HT-29 (colon carcinoma) cells was examined under the influence of HP01. In combination with radiation, the effects of HP01 on cytotoxicity and long-term survival were assessed using a colony formation assay. The number of DNA double-strand breaks was analyzed using the γH2AX assay, while cell cycle distribution was examined via flow cytometry. A growth-inhibiting and cytotoxic effect was observed for both tumor cell lines starting at a concentration of 10 µg/mL HP01. Treatment with HP01 resulted in an inhibition of clonogenic survival of tumor cells after ionizing radiation (6 Gy). The number of DNA double-strand breaks (DSBs) in tumor cells increased with HP01 treatment, but the repair of radiation-induced DNA DSBs was not affected. Cell cycle analysis revealed that HP01, in addition to radiation, enhanced G2/M arrest in MCF-7 and HT-29 cells. Overall, HP01 not only showed a growth-inhibiting effect but also demonstrated a radiosensitizing effect on human tumor cells for the first time. We conclude that the HP01-induced G2/M accumulation of cells may be the main rationale for the drug-induced radiosensitivity. It is therefore a promising candidate for combined therapy in tumor diseases and warrants further investigation. Full article

(This article belongs to the Special Issue Biological Research on Plant Bioactive Compounds)

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17 pages, 3135 KiB

Open AccessArticle

Sulforaphane and Benzyl Isothiocyanate Suppress Cell Proliferation and Trigger Cell Cycle Arrest, Autophagy, and Apoptosis in Human AML Cell Line

by Anna Bertova, Szilvia Kontar, Martina Ksinanova, Alberto Yoldi Vergara, Zdena Sulova, Albert Breier and Denisa Imrichova

Int. J. Mol. Sci. 2024, 25(24), 13511; https://doi.org/10.3390/ijms252413511 - 17 Dec 2024

Cited by 1 | Viewed by 802

Abstract

Isothiocyanates (ITCs) are naturally occurring sulfur-containing compounds with diverse biological effects. This study investigated the effects of sulforaphane (SFN, an aliphatic ITC) and benzyl isothiocyanate (BITC, an aromatic ITC) on human acute myeloid leukemia SKM-1 cells, focusing on cell proliferation, cell death, and drug resistance. Both drug-sensitive SKM-1 cells and their drug-resistant SKM/VCR variant, which overexpresses the drug transporter P-glycoprotein, were used. SFN and BITC reduced cell viability in a dose-dependent manner, with BITC showing greater potency. IC50 values ranged from 7.0–8.0 µM for SFN and 4.0–5.0 µM for BITC in both cell types, with only slight differences between the variants. Both ITCs induced autophagy as evidenced by increased LC3-II production and caused a significant increase in the sub-G0/G1 cell population, especially with BITC. Apoptosis was more pronounced after BITC treatment, whereas SFN had a weaker effect. These results suggest that autophagy may act as a defense mechanism in response to ITC-induced apoptosis in human AML cells. Full article

(This article belongs to the Special Issue Biological Research on Plant Bioactive Compounds)

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14 pages, 1419 KiB

Open AccessArticle

The Antioxidant, Antimicrobial, and Antitumor Proprieties of Flavonol-Rich Extracts from Allium ursinum (Wild Garlic) Leaves: A Comparison of Conventional Maceration and Ultrasound-Assisted Extraction Techniques

by Kinga Oravetz, Zorita Diaconeasa, Rahela Carpa, Elena Rakosy-Tican and Daniel Cruceriu

Int. J. Mol. Sci. 2024, 25(23), 12799; https://doi.org/10.3390/ijms252312799 - 28 Nov 2024

Viewed by 1060

Abstract

Despite the growing interest in using natural compounds for disease prevention and treatment, Allium ursinum (wild garlic), known for its therapeutic properties, has not been extensively studied for its chemical composition and biological activities. Therefore, this study aims to explore the in vitro antioxidant, antibacterial, and antitumor activities of A. ursinum extracts according to their functional phytochemical profile, while assessing whether ultrasound-assisted extraction (UAE) enhances bioactive properties in comparison to conventional maceration (CM). Both extracts were characterized by spectrophotometric methods and LC-ESI+-MS. The antioxidant activity was assessed via the CUPRAC and hydrogen peroxide scavenging assays, the antimicrobial properties via the disk-diffusion method against five pathogenic strains, and the antitumor activity via the MTT assay on four cancer cell lines. The major constituents of the methanolic extracts from leaves were kaempferol derivatives and alliin. The quercetin derivative rutin was also found. Maceration assisted using UAE yielded 20% more bioactive compounds in comparison to CM alone. Employing UAE in the extraction significantly increased antioxidant and antimicrobial proprieties, in line with its chemical composition. The antitumor cytotoxic activity was low to moderate, regardless of method, as explained by the absence of highly cytotoxic compounds. Wild garlic extracts possessed strong antioxidant and substantial antibacterial activities. Full article

(This article belongs to the Special Issue Biological Research on Plant Bioactive Compounds)

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Review

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34 pages, 4591 KiB

Open AccessReview

Phytochemicals Controlling Enterohemorrhagic Escherichia coli (EHEC) Virulence—Current Knowledge of Their Mechanisms of Action

by Patryk Strzelecki, Monika Karczewska, Agnieszka Szalewska-Pałasz and Dariusz Nowicki

Int. J. Mol. Sci. 2025, 26(1), 381; https://doi.org/10.3390/ijms26010381 - 4 Jan 2025

Viewed by 1252

Abstract

Enterohemorrhagic Escherichia coli (EHEC) is a common pathotype of E. coli that causes numerous outbreaks of foodborne illnesses. EHEC is a zoonotic pathogen that is transmitted from animals to humans. Ruminants, particularly cattle, are considered important reservoirs for virulent EHEC strains. Humans can become infected with EHEC through the consumption of contaminated food and water or through direct contact with infected animals or humans. E. coli O157:H7 is one of the most commonly reported causes of foodborne illnesses in developed countries. The formation of attaching and effacing (A/E) lesions on the intestinal epithelium, combined with Shiga toxin production, is a hallmark of EHEC infection and can lead to lethal hemolytic–uremic syndrome (HUS). For the phage-dependent regulation of Shiga toxin production, antibiotic treatment is contraindicated, as it may exacerbate toxin production, limiting therapeutic options to supportive care. In response to this challenge and the growing threat of antibiotic resistance, phytochemicals have emerged as promising antivirulence agents. These plant-derived compounds target bacterial virulence mechanisms without promoting resistance. Therefore, the aim of this study is to summarize the recent knowledge on the use of phytochemicals targeting EHEC. We focused on the molecular basis of their action, targeting the principal virulence determinants of EHEC. Full article

(This article belongs to the Special Issue Biological Research on Plant Bioactive Compounds)

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