1.Anti-inflammatory Constituents from Artemisia iwayomogi Kitamura: A Bioassay-guided Fractionation Study
Ngoc Khanh VU ; Thi Thanh LE ; Trong Trieu TRAN ; Manh Tuan HA ; Jeong Ah KIM ; Byung Sun MIN
Natural Product Sciences 2025;31(1):43-48
Bioassay-guided fractionation of the methanolic extract of Artemisia iwayomogi Kitamura led to the isolation of 12 known compounds (1‒12). Notably, this study marks the first report of 3-epimeridinol (1) being isolated and structurally characterized from a natural source. Additionally, compounds 3, 4, and 7 were isolated from the Asteraceae family for the first time. The structural elucidation of the isolated compound was achieved through analysis of 1D, 2D NMR, and MS data. Upon evaluation of their inhibitory effects against lipopolysaccharideinduced nitric oxide production, compound 12 demonstrated significant inhibitory activity with greater potency than the reference compound quercetin. These results established A. iwayomogi as a promising source of antiinflammatory agents.
2.Cytotoxic Compounds Obtained through Cell Viability Screening of Fungal Extracts, Isolated from Urban Soil Samples I
Natural Product Sciences 2025;31(1):32-42
Soil microorganisms have been reported to interact with plants, playing key roles such as providingnutrients essential for plant growth and protecting them from plant pathogens. Additionally, various bioactive molecules from soil significantly contribute to controlling diseases threatening human such as cancer and infectious diseases. Considering the crucial roles and potential of these soil microorganisms, the Natural Products Drug Discovery research group (NPDD) at Duksung Women’s University collected soil samples from various environments, isolated fungi from the soil, and aimed to discover bioactive compounds. In this process, 96 fungal strains were cultured on small scale to generate their ethyl acetate extracts, which were subsequently screened for cell viability using MDA-MB-231 triple-negative breast cancer cells. Among them, a subset of 17 with over 60% inhibitory activity were selected as top-performing strains, and other 13 strains with below 60% were chosen for large-scale fermentation candidates by HR-ESI-MS dereplication process to discover new bioactive molecules.Chemical investigation of a part of these large-scale fermentation candidates led to the isolation of 13 major metabolites (1–13), and all isolates were evaluated for their cytotoxicity against MDA-MB-231 cells. As a result, strigaibol C (1), trichoguizaibol J (2), beauvericin (3), and sclerotioramine (13) showed strong inhibitory activities with IC50 values of 0.99, 0.68, 4.25, and 21.8 μM, respectively.
3.PTP1B Inhibitory Activity of Flavonoids from the Roots of Astragalus membranaceus Bunge
Thi Ly PHAM ; Manh Tuan HA ; Byung Sun MIN ; Jeong Ah KIM
Natural Product Sciences 2025;31(1):62-73
The roots of Astragalus membranaceus Bunge have long been used in herbal medicine for their diversebiological activities. Notably, its potential anti-diabetic properties have been extensively studied, highlighting promising therapeutic prospects. In this study, we conducted a comprehensive investigation focusing on flavonoid components from the roots of A. membranaceus and their PTP1B inhibitory activity. As a result, we isolated a total of 24 flavonoids, among which formonentin (1), pratensein (3), and vesticarpan (19) emerged as the most potent inhibitors against PTP1B with IC50 value of 10.9 ± 1.09 μM, 10.0 ± 1.71 μM, and 10.3 ± 1.31 μM, respectively.Additionally, through the enzyme kinetic analysis, the inhibition mode of compound 19 was determined as a competitive inhibitor, with Ki value of 7.6 ± 1.17 μM. Furthermore, the molecular docking simulation elucidated the binding mechanism of compound 19 with PTP1B, mainly through van der Waals forces and hydrogen bonds.This study highlights the PTP1B inhibitory potential of the flavonoid constituents derived from the roots of A. membranaceus. Moreover, discovering vesticarpan (19) as a novel PTP1B inhibitor provides a significant foundation for further investigations to develop innovative therapeutic strategies for diabetes treatment.
4.Cognitive Enhancing Effects of Androst-16-ene-3,6-diol Isolated from Lysimachia christinae on Scopolamine-Induced Impaired Memory Function
Natural Product Sciences 2025;31(1):55-61
The ability of androst-16-ene-3,6-diol, a compound derived from Lysimachia christinae, to enhancecognitive function was assessed in mice with scopolamine-induced amnesia. through behavioral and biochemical studies. The Morris water maze test demonstrated significant improvements in spatial learning and memory, with treated mice showing reduced escape latency, shorter path lengths, and enhanced swimming trajectories compared to scopolamine-treated controls. In the passive avoidance test, androst-16-ene-3,6-diol effectively restored retention memory, getting about 65% of the performance detected in control mice group. Biochemical analysis revealed that androst-16-ene-3,6-diol notably diminished acetylcholinesterase activity in the cortex and hippocampus, critical regions for learning and memory. These effects were comparable to those of donepezil, a standard acetylcholinesterase inhibitor used as a positive control (1 mg/kg orally). The findings indicate that androst-16-ene-3,6-diol exerts robust cognitive-enhancing effects by mitigating scopolamine-induced cholinergic deficits through acetylcholinesterase inhibition. This highlights its potential as a promising therapeutic candidate for memory impairment and neurodegenerative disorders.
5.Therapeutic Potential of Methanol Extract of Euonymus alatus in HT22 Cells Through Neuroprotective Mechanisms
Natural Product Sciences 2025;31(1):49-54
Oxidative stress, a key factor in the progression of brain diseases, induces apoptosis through multiplepathways. This study investigates the protective effects of Euonymus elatus, a traditional Korean remedy for conditions such as atherosclerosis, dysmenorrhea, and pain, on neuronal cells under oxidative stress. Excess glutamate was used to model oxidative stress, resulting in elevated reactive oxygen species (ROS), increased intracellular calcium (Ca²⁺), reduced mitochondrial membrane potential, and decreased activity of glutathionerelated enzymes, including glutathione reductase (GR) and glutathione peroxidase (GPx). Experimental results revealed that E. elatus extract provided significant cytoprotective effects. The extracts improved cell viability in MTT assays, reduced ROS and Ca²⁺ levels, restored mitochondrial membrane potential, and enhanced the activity of GR and GPx. These findings highlight the potential of E. elatus as a therapeutic candidate for mitigating oxidative stress and treating neurodegenerative disorders, such as Alzheimer’s disease.
6.15-Methylhexadecanoic Acid and Other Chemical Constituents from Calliandra calothyrsus (Meisn) (Fabaceae) with Their Antibacterial Activities
Armel Cyrille TENKEU ; Florence Déclaire MABOU ; Andreea Veronica Dediu BOTEZATU ; Jean-de-Dieu TAMOKOU ; Germaine Matsuete TAKONGMO ; Sophie TOMASI ; Laurence VOUTQUENNE-NAZABADIOKO ; Rodica Mihaela DINICA ; Apollinaire TSOPMO ; David NGNOKAM
Natural Product Sciences 2025;31(1):24-31
A chemical study of the methanol extract from the leaves of Calliandra calothyrsus led to the isolation of nine compounds including, 15-methylhexadecanoic acid (1), isolated for the first time from this plant, kaempferol (2), quercetin-3-O-α-L-rhamnopyranoside (3), kaempferol-3-O-α-L-rhamnopyranoside (4), quercetin-3-O-β-D-galactopyranoside (hyperin) (5), polifoliosid (6), D-pinitol (7), quercetin (8), rhamnetin-3-O-β-D-xylopyranoside (9). New derivatives, namely tributyronitrilequercetin-3-O-α-L-rhamnopyranoside (10), tetrabutyronitrilequercetin-3-O--L-rhamnopyranoside (11) were obtained upon alkylation of compound 3 with 4-bromobutyronitrile.Structures of isolated compounds and semi-synthetic derivatives were assigned by 1D and 2D NMR analysis and mass spectrometry. The extracts and the isolated compounds were evaluated for their antibacterial activities. The EtOAc extract was highly active against Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus.For pure compounds, the best MIC (8 µg/mL) was obtained with quercetin-3-O-β-D-galactopyranoside (5) against Enterococcus faecalis and quercetin (8) against Pseudomonas aeruginosa. The alkylation of compound 3enhanced its antimicrobial activities by up to 4-fold depending on the species.
7.Prunus yedoensis Bark Water Extract Increases Hyaluronic Acid Synthesis and Skin Barrier-related Protein Levels
Natural Product Sciences 2025;31(1):13-23
Damage to barrier function due to a loss of moisture in the skin can lead to skin diseases, such as atopy and psoriasis. Hyaluronic acid (HA) has the ability to retain large amounts of moisture and thereby protects the skin against moisture loss. In addition, tight junctions prevent water loss and maintain barrier functions by restricting molecular movement through cell-to-cell connections. In this study, the effects of Prunus yedoensis bark water extract (PYBWE) on HA synthesis and tight junction protein expression in HaCaT cells were evaluated.In HaCaT cells, PYBWE had effects on the MAPKs, CREB, AKT, NF-κB, and CLDN-4 signaling pathways, at 25, 50, and 100 µg/mL concentrations increasing the amount of HA produced via HAS-2 and effectively improving skin barrier function.
8.Cytotoxicity against MDA-MB-231 Breast Cancer Cells of Fungal Metabolites of Trichoderma sp. Collected from Medicinal Herbal Garden
Natural Product Sciences 2025;31(1):6-12
Trichoderma sp. isolated from the herbal garden is one of the well-known soil fungi, and various metabolites produced by this genus, such as anthraquinones, azaphilones and peptaibols, have been reported to exhibit cytotoxicity against various cancer cells. A large-scale cultivation and a chemical investigation of Trichoderma sp. led to isolation and purification of 10 known compounds from its EtOAc extract. Their structures were elucidated by comparing 1D NMR ( 1H and 13C) and HRESIMS data with previously reported literature. The cytotoxicity of all isolated compounds was measured against MDA-MB-231 breast cancer cells, and koninginin E (10) showed significant inhibitory activity with an IC50 value of 7.3 µM.
9.Anti-pemphigus and Anti-atopic Potentials of Lycopi Herba Extract with MKK3 Inhibitory Activity in Human Keratinocyte HaCaT Cells
Natural Product Sciences 2025;31(1):1-5
Pemphigus is autoimmune blistering disease associated with autoantibodies (such as desmoglein 3 antibody) directed against the cell surface of keratinocytes, thereby loss of cell-cell adhesion of keratinocytes.The pathogenesis of pemphigus is currently thought to be mediated by direct inhibition via autoantibodies and subsequent signal transduction involving p38 mitogen activated protein kinase (MAPK) pathway. Several studies have reported both mitogen-activated protein kinase kinase 3 (MKK3) and MKK6 are required for full activation of p38, and we recently reported the activation of MKK3 in pemphigus skin tissue, but not MKK6, suggesting that MKK3 could be a potential therapeutic target for pemphigus vulgaris. Here, we found that AK23 IgG (desmoglein 3 antibody) induced the phosphorylation of MKK3 in human keratinocyte HaCaT cells, and treatment of MKK3-inhibiting Lycopi Herba extract (ELH) with MKK3 kinase IC50 , 12.25 μg/mL significantly inhibited AK23-induced fragmentation of HaCaT cell sheets in a dose-dependent manner without any cytotoxicity. Additionally, ELH exhibited anti-atopic activity. In conclusion, MKK3 could play an important role in blister formation in pemphigus, and the MKK3 inhibition by herbal extracts such as ELH could be a possible therapeutic strategy for treating patients with pemphigus as well as atopic dermatitis.
10.Anti-inflammatory Constituents from Artemisia iwayomogi Kitamura: A Bioassay-guided Fractionation Study
Ngoc Khanh VU ; Thi Thanh LE ; Trong Trieu TRAN ; Manh Tuan HA ; Jeong Ah KIM ; Byung Sun MIN
Natural Product Sciences 2025;31(1):43-48
Bioassay-guided fractionation of the methanolic extract of Artemisia iwayomogi Kitamura led to the isolation of 12 known compounds (1‒12). Notably, this study marks the first report of 3-epimeridinol (1) being isolated and structurally characterized from a natural source. Additionally, compounds 3, 4, and 7 were isolated from the Asteraceae family for the first time. The structural elucidation of the isolated compound was achieved through analysis of 1D, 2D NMR, and MS data. Upon evaluation of their inhibitory effects against lipopolysaccharideinduced nitric oxide production, compound 12 demonstrated significant inhibitory activity with greater potency than the reference compound quercetin. These results established A. iwayomogi as a promising source of antiinflammatory agents.

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