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SSRN 2025年

作者： Chen, Ting-Yu Chang, Chi-Yuan Wen, Ting-Chun Xu, Li Lin, Yu-Han Peng, Cheng-Liang Yeh, Yi-Qi Chen, Chueh-Hsuan Chuang, Kuo-Hsiang Wu, Si-Han Graduate Institute of Pharmacognosy Taipei Medical University Taipei11031 Taiwan Graduate Institute of Nanomedicine and Medical Engineering Taipei Medical University Taipei11031 Taiwan Department of Isotope Application National Atomic Research Institute Taoyuan Taiwan National Synchrotron Radiation Research Center Hsinchu Science Park Hsinchu30076 Taiwan Research Center for Applied Science Academia Sinica Taiwan PhD Program in Clinical Drug Development of Chinese Herbal Medicine Taipei Medical University Taipei Taiwan International Ph.D. Program in Biomedical Engineering College of Biomedical Engineering Taipei Medical University Taipei11031 Taiwan

The immunogenicity of polyethylene glycol (PEG) remains a critical challenge in nanomedicine, as pre-existing anti-PEG antibodies can compromise therapeutic efficacy through accelerated blood clearance (ABC) and life-threatening hypersensitivity. Here, we address this challenge by engineering the PEG architecture, creating short-chain dense brush PEGylation (PEG500) on rigid mesoporous silica nanoparticles (MSNs). Unlike conventional PEG2000-liposomes, MSN-PEG500 evades antibodies via three synergistic mechanisms: (1) short-chain PEG500 reduces epitope accessibility, (2) high grafting density (4.43 chains/nm2, according to TGA) forms an dense steric shield, and (3) the rigid silica surface prevents PEG burial. ELISA studies demonstrated that, at equivalent nanoparticle concentrations, MSN-PEG500 exhibits a 26-fold reduction in anti-PEG IgG (6.3) binding and a 1000-fold reduction in anti-PEG IgM (AGP3) binding compared to Lipodox (PEG2000), both of which target the PEG backbone. Furthermore, radiolabeled MSN-PEG500 achieved prolonged circulation and 25% tumor accumulation (ID/g) at 24 hours. In strongly immunized mice, doxorubicin-loaded MSN-PEG500 preserved therapeutic efficacy and 100% survival, whereas Lipodox induced fatal hypersensitivity. Mechanistic investigations revealed that complement activation drives PEG2000 immunotoxicity, and pretreatment with the C3 inhibitor compstatin effectively mitigated temperature drops from 10°C to 2°C in immunized hosts. By demonstrating that nanoscale control of polymer conformation dictates immunological fate, this work provides a clinically translatable blueprint for developing immune-evasive nanomedicines. © 2025, The Authors. All rights reserved.

关键词： Silica nanoparticles

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Discovery of Novel Zoanthamine-Type Alkaloids Derived from Cultured Zoanthus Kuroshio with Prominent Therapeutic Potential Against Osteoporosis

SSRN

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SSRN 2025年

作者： Pham, Ngoc-Thac Peng, Bo-Rong Le, Huong-Giang Chen, Yun-Shiuan Huynh, Thanh Hao Chen, Lo-Yun Nguyen, Le Anh Tuan Nguyen, Dang T. Su, Jui-Hsin El-Shazly, Mohamed Lee, Mei-Hsien Lai, Kuei-Hung PhD Program in Clinical Drug Development of Herbal Medicine College of Pharmacy Taipei Medical University Taipei110301 Taiwan Graduate Institute of Pharmacognosy College of Pharmacy Taipei Medical University Taipei110301 Taiwan Graduate Institute of Healthy Industry Technology Research Center for Chinese Herbal Medicine College of Human Ecology Chang Gung University of Science and Technology Taoyuan333324 Taiwan Faculty of Pharmacy Lac Hong University Dongnai Bien Hoa Viet Nam Faculty of Applied Sciences Ton Duc Thang University Ho Chi Minh City Viet Nam National Museum of Marine Biology and Aquarium Pingtung944401 Taiwan Department of Marine Biotechnology and Resources National Sun Yat-sen University Kaohsiung804201 Taiwan Department of Pharmacognosy Faculty of Pharmacy Ain-Shams University Organization of African Unity Street Abassia Cairo11566 Egypt Center for Reproductive Medicine and Sciences Taipei Medical University Hospital Taipei110301 Taiwan Traditional Herbal Medicine Research Center Taipei Medical University Hospital Taipei110301 Taiwan

Marine invertebrates are well-established as prolific sources of secondary metabolites, renowned for their remarkable chemical diversity and extensive spectrum of biological activities. Among these, Zoanthus Kuroshio (ZK) has gained significant attention due to its abundant chemical constituents, particularly alkaloids, which exhibit promising bioactivities against osteoporosis. To investigate its therapeutic potential, the extracts of cultured ZK exhibited significant anti-osteoporotic activity in vitro with MG-63 cells, leading to the integration of Global Natural Products Social Molecular Networking (GNPS) to identify fractions containing the highest amounts of alkaloids. Subsequent isolation efforts resulted in the discovery of five novel zoanthamine-type alkaloids: norzoabenzaldehyde (1), norzoazepanol (2), 11-keto-3-acetoxynorzoanthamine (3), 11-hydroxynorzoanthamide B (4), and 11-hydroxyzoanthamide B (5), alongside four previously identified compounds, including norzoanthaminone (6), 3-acetoxynorzoanthamine (7), 3-acetoxyzoanthamine (8), and 3-hydroxynorzoanthamine (9). Structural elucidation of compounds 1, 3, 4, and 5 was achieved using comprehensive spectroscopic analyses, whereas compound 2 required advanced techniques, including time-dependent density functional theory nuclear magnetic resonance (TDDFT-NMR) calculations and comparative analysis of theoretical and experimental electronic circular dichroism (ECD) data, to ascertain its absolute configuration. Bioassays evaluating alkaline phosphatase activity and mineralization demonstrated that compound 9 exhibited significant activity, with an IC50 value of 20 µM. The mechanism by which this compound operates was elucidated through network pharmacology, molecular docking and dynamics simulations, further confirming the stability of interactions between compound 9 and key protein targets, thereby emphasizing its potential as a promising lead compound for osteoporosis therapeutics. © 2025, The Authors. All

关键词： Spectroscopic analysis

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Comparative metabolomics of acetylcholinesterase and α-glucosidase inhibitors in pericarp of Garcinia mangostana L

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Botanical studies 2025年第1期66卷 13页

作者： Yun-Han Wang Ta-Wei Liu Sui-Wen Hsiao Man-Hsiu Chu Tzong-Huei Lee Su-Jung Hsu Shih Yin Chen Ching-Kuo Lee Ph.D. Program in Clinical Drug Development of Herbal Medicine Taipei Medical University 250 Wu Xin Street Taipei 110 Taiwan. School of Pharmacy Taipei Medical University 250 Wu Xin Street Taipei 110 Taiwan. Ph.D. Program in Drug Discovery and Development Industry Taipei Medical University 250 Wu Xin Street Taipei 11031 Taiwan. Institute of Fisheries Science National Taiwan University Taipei City Taiwan. School of Pharmacy Taipei Medical University 250 Wu Xin Street Taipei 110 Taiwan. juliahsu@ntu.edu.tw. Institute of Fisheries Science National Taiwan University Taipei City Taiwan. juliahsu@ntu.edu.tw. Xantho Biotechnology Co. Ltd. Rm ER15 17F.-1 No. 3 Yuanqu St. Nangang Dist. Taipei City 11503 Taiwan (R.O.C.). Ph.D. Program in Clinical Drug Development of Herbal Medicine Taipei Medical University 250 Wu Xin Street Taipei 110 Taiwan. cklee@tmu.edu.tw. School of Pharmacy Taipei Medical University 250 Wu Xin Street Taipei 110 Taiwan. cklee@tmu.edu.tw. Ph.D. Program in Drug Discovery and Development Industry Taipei Medical University 250 Wu Xin Street Taipei 11031 Taiwan. cklee@tmu.edu.tw. Graduate Institute of Pharmacognosy Taipei Medical University 250 Wu Xin Street Taipei 11031 Taiwan. cklee@tmu.edu.tw. School of Food Safety Taipei Medical University 250 Wu Xin Street Taipei 11031 Taiwan. cklee@tmu.edu.tw. Department of Chemistry Chung Yuan Christian University 200 Zhongbei Road Zhongli District Taoyuan 32023 Taiwan. cklee@tmu.edu.tw.

BACKGROUND:Mangosteen (Garcinia mangostana L.) pericarp extract has demonstrated potential against Alzheimer's disease (AD) and diabetes mellitus (DM). This study introduces a rapid dereplication and comparative approach to identify and characterize acetylcholinesterase (AChE) and α-glucosidase inhibitors in mangosteen pericarp. Using protein-subtraction, MS profiling, and computational modeling is effective for screening, identifying, and analyzing enzyme-inhibiting compounds from plant sources, and quantitative analysis of the main components has been performed. RESULTS:The Mangosteen pericarp extract observed significant inhibitory activity against α-glucosidase and AChE, with IC50 values of 31.02 and 70.56 µg/mL, respectively. By comparing profiles of protein-subtracted extracts with non-treated extracts, eight potential inhibitors for each enzyme were identified: 8-desoxygartanin, gartanin, 3-isomangostin, β-mangostin, 9-hydroxycalabaxanthone, γ-mangostin, α-mangostin, and garcinone E. The α-mangostin was the most abundant, comprising 39.589% of the extract. Molecular docking revealed these inhibitors target the peripheral anionic site of AChE and the active site of α-glucosidase, forming key hydrogen bonds and pi-pi stacking interactions. CONCLUSION:This study emphasizes mangosteen pericarp as a promising natural source of these inhibitors, with potential for use in developing nutraceuticals and pharmaceuticals. The study validated a systems biology approach by applying dereplication and comparative UPLC-ESI-MS/MS metabolomics profiling to identify target-binding molecules in both protein-treated and untreated plant extracts. Further confirmation was obtained through molecular docking predictions, mechanism analysis, and compound quantification assays.

关键词： Acetylcholinesterase Comparative metabolomics Dereplication Mangosteen (Garciniaman gostana L) α-glucosidase

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Exploring the wound-healing potential and seasonal chemical variability of the Formosan Callery pear Pyrus calleryana: implications for therapeutic applications

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Pharmaceutical Biology 2024年第1期62卷 621-633页

作者： Peng, Bo-Rong Tang, Xin-Yun Chen, Yun-Shiuan Lai, Kuei-Hung Lee, Mei-Hsien Graduate Institute of Pharmacognosy College of Pharmacy Taipei Medical University PhD Program in Clinical Drug Development of Herbal Medicine College of Pharmacy Taipei Medical University Center for Reproductive Medicine and Sciences Taipei Medical University Hospital

Context: Pyrus calleryana Decne (Rosaceae), renowned for its therapeutic properties, is known to moisturize the lungs (removing dryness;relieving cough), clear heat (acting as an antipyretic;febrifuge) and aid in detoxification (relieving pyogenic inflammation;eliminating toxins). However, scientific evidence supporting its efficacy in wound healing is lacking. Objective: This study investigated *** samples collected over a year to explore metabolite variations and their impact on skin wound-healing activities. Materials and methods: P. calleryana (PC) twigs and leaves were collected from the Matsu Islands, Taiwan, spanning 2018–2020. Extracts were prepared using 95% ethanol or water, and we assessed the chemical composition, total phenolic/triterpenoid contents and antioxidant properties. Metabolites were analysed via LC–MS/MS and molecular networking. Wound healing potential was evaluated on WS-1 cells through MTT and migration assays, and gene expression analyses, with tests including control (DMSO), compounds 1 (3′-hydroxylbenzyl-4-hydroxybenzoate-4′-O-β-glucopyranoside) and 2 (vanilloylcalleryanin) (100 µM), and a positive control (ascorbic acid, 100 µM) for 24 h. Results: Significant variations in extract compositions were observed based on the solvent used, with distinct metabolomic profiles in extracts collected during different months. Notably, compounds 1 and 2 showed no cytotoxic effects on human dermal fibroblast cells and significantly accelerated wound closure at 100 μM. A gene expression analysis indicated upregulation of wound healing-associated genes, including MMP-1 (matrix metalloproteinase-1) and COL1A1 (collagen, type 1, alpha 1). Conclusions: This study reports the first evidence of PC compounds aiding wound healing. Utilizing Global Natural Products Social Molecular Networking (GNPS) and principal component analysis (PCA) approaches, we unveiled metabolomic profiles, suggesting the potential to expedite wound-healing. © 2024 The Autho

关键词： COL1A1 GNPS LC-MS/MS MMP-1

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Ascophyllum nodosum and Fucus vesiculosus ameliorate restenosis via improving inflammation and regulating the PTEN/PI3K/AKT signaling pathway

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Food Science and Human Wellness 2024年第3期13卷 1711-1728页

作者： Crystal Ngofi Zumbi Chun-Hsu Pan Hui-Yu Huang Chieh-Hsi Wu Program in Clinical Drug Development from Herbal Medicine College of PharmacyTaipei Medical UniversityTaipei 11031China Program in Drug Discovery and Development Industry College of PharmacyTaipei Medical UniversityTaipei 11031China School of Pharmacy Taipei Medical UniversityTaipei 11031China Graduate Institute of Metabolism and Obesity Sciences Taipei Medical UniversityTaipei 11031China

Restenosis is a common complication following coronary *** traditional use of seaweeds for health benefits has increasingly been explored,however few studies exist reporting its protective effects on the development of restenosis and gut *** aim of this study was to investigate the potential of seaweed extracts(SE) of Ascophyllum nodosum and Fucus vesiculosus in inhibiting intimal hyperplasia in a rat model of restenosis and its underlying mechanisms in macrophages and vascular smooth muscle cells(vSMCs).16S rRNA sequencing was done to investigate the regulatory effect of SE on the gut microbiome of injured *** indicated by the results,SE significantly inhibited the progression of intimal hyperplasia in vivo,attenuated inflammation in macrophages and could inhibit the proliferation,dedifferentiation and migration of *** was observed through immunoblotting assays that treatment with SE significantly upregulated PTEN expression in macrophages and inhibited the upregulation of PI3K and AKT expression in ***,according to the 16S rRNA gene sequencing analysis,supplementation with SE modulated gut microbiota composition in injured *** conclusion,SE could ameliorate intimal hyperplasia by inhibiting inflammation and vSMCs proliferation through the regulation of the PTEN/PI3K/AKT pathway and modulating the gut microbiome.

关键词： Ascophyllum nodosum Fucus vesiculosus PTEN/PI3K/AKT Restenosis Macrophage Vascular smooth muscle cells Gut microbiota

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MiR-22 as a metabolic silencer and liver tumor suppressor

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Liver Research 2020年第2期4卷 74-80页

作者： Lijun Wang Yu-Shiuan Wang Eko Mugiyanto Wei-Chiao Chang Yu-Jui Yvonne Wan Department of Pathology and Laboratory Medicine University of California DavisSacramentoCA The College of Life Science Yangtze UniversityJingzhouHubei PhD Program in Clinical Drug Development of Chinese Herbal Medicine College of PharmacyTaipei Medical UniversityTaipei Department of Clinical Pharmacy School of PharmacyTaipei Medical UniversityTaipei

With obesity rate consistently increasing,a strong relationship between obesity and fatty liver disease has been *** than 90%of bariatric surgery patients also have non-alcoholic fatty liver diseases(NAFLDs).NAFLD and non-alcoholic steatohepatitis(NASH),which are the hepatic manifesta-tions of metabolic syndrome,can lead to liver ***,there is no effective medicine that can be used to treat NASH or liver ***,it is critically important to understand the mechanism underlying the development of these *** evidence suggests that microRNA 22(miR-22)can be a diagnostic marker for liver diseases as well as a treatment *** review paper focuses on the roles of miR-22 in metabolism,steatosis,and liver *** search is limited based on the publications included in the PubMed database in the recent 10 years.

关键词： MicroRNA-22(miR-22) Cancer Liver Metabolism Steatosis Non-alcoholic steatohepatitis Hepatitis

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Flexible nanohybrid substrates utilizing gold nanocubes/nano mica platelets with 3D lightning-rod effect for highly efficient bacterial biosensors based on surface-enhanced Raman scattering

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Journal of Materials Chemistry B 2024年第13期12卷 3226-3239页

作者： Chen, Yan-Feng Lu, Ming-Chang Lee, Chia-Jung Chiu, Chih-Wei Department of Materials Science and Engineering National Taiwan University of Science and Technology Taipei10607 Taiwan Ph.D. Program in Clinical Drug Development of Herbal Medicine College of Pharmacy Taipei Medical University Taipei11031 Taiwan

In this study, gold nanocubes (AuNCs) were quickly synthesized using the seed-mediated growth method and reduced onto the surface of two-dimensional (2D) delaminated nano mica platelets (NMPs), enabling the development of AuNCs/NMPs nanohybrids with a 3D lightning-rod effect. First, the growth-solution amount can be changed to easily adjust the AuNCs average-particle size within a range of 30-70 nm. The use of the cationic surfactant cetyltrimethylammonium chloride as a protective agent allowed the surface of AuNCs and nanohybrids to be positively charged. Positively charged nanohybrid surfaces presented a good adsorption effect for detecting molecules with negative charges on the surface. Additionally, the NMP surfaces were rich in ionic charges and provided a large specific surface area for stabilizing the growth of AuNCs. Delaminated AuNCs/NMPs nanohybrids can generate a 3D hotspot effect through self-assembly to enhance the Raman signal. Surface-enhanced Raman scattering (SERS) is highly sensitive in detecting adenine biomolecules. Its limit of detection (LOD) and Raman enhancement factor reached 10−9 M and 3.6 × 108, respectively. Excellent reproducibility was obtained owing to the relatively regular arrangement of AuNC particles, and the relative standard deviation (RSD) was 10.7%. Finally, the surface of NMPs was modified by adding the hydrophilic poly(oxyethylene)-diamine (POE2000) and amphiphilic PIB-POE-PIB copolymer at different weight ratios. The adjustment of the surface hydrophilicity and hydrophobicity of AuNCs/NMPs nanohybrids led to better adsorption and selectivity for bacteria. AuNCs/POE/NMPs and AuNCs/PIB-POE-PIB/NMPs were further applied to the SERS detection of hydrophilic Staphylococcus aureus and hydrophobic Escherichia coli, respectively. The SERS-detection results suggest that the LOD of hydrophilic Staphylococcus aureus and hydrophobic Escherichia coli reached 92 CFU mL−1 and 1.6 × 102 CFU mL−1, respectively. The AuNCs/POE/NMPs and AuNCs/P

关键词： Substrates

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Integration proteomics analysis to identify AMPK as key target pathways of TCM formula for high fat diet induced obesity in mice

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Journal of Traditional and Complementary medicine 2025年

作者： Chen, Yu-Ju Ning, De-Shan Wang, Ching-Chiung Zhao, Hong-Wei Wang, Kun-Teng Lee, Ming-Chung Chiu, Wan Chun Yeh, Chiu-Li Jacinto Dela Vega, John Louie Lee, Chia-Jung Ph.D. Program in Clinical Drug Development of Herbal Medicine College of Pharmacy Taipei Medical University Taipei Taiwan Infinitus Company Ltd Guangdong Guangzhou China Graduate Institute of Pharmacognosy College of Pharmacy Taipei Medical University Taipei Taiwan School of Pharmacy Collage of Pharmacy Taipei Medical University Taipei Taiwan Traditional Herbal Medicine Research Center Taipei Medical University Hospital Taipei Taiwan Herbiotek Co. Ltd New Taipei City Taiwan School of Nutrition and Health Sciences College of Nutrition Taipei Medical University Taipei Taiwan Ph.D. Program in School of Pharmacy College of Pharmacy Taipei Medical University Taipei Taiwan

Background: Livsooth Authentic herbal Formula (LAH) is a novel Chinese herbal medicine that has been previously shown to prevent non-alcoholic fatty liver disease (NAFLD). However, its efficacy in treating obesity and its underlying mechanisms remain unclear. This study uniquely investigates the therapeutic effects of LAH on high-fat diet (HFD)-induced obese mice, focusing on its multi-targeted regulation of metabolic pathways. This research highlights the potential of a multi-component herbal formula in simultaneously activating the AMPK pathway, regulating lipid metabolism, and enhancing antioxidant defenses. By integrating network pharmacology predictions with proteomics analysis, in vivo, and in vitro experiments, this study provides a comprehensive understanding of LAH's mode of action. Materials and methods: Mice were fed a high-fat diet (HFD) for 8 weeks, followed by oral treatment with LAH at doses of 615 mg/kg and 2460 mg/kg for 10 weeks. Each treatment group consisted of 6 mice. Body weight, blood biochemistry, and antioxidant enzyme activities were measured. Network pharmacology and proteomics analyses were conducted to identify mechanisms, and in vitro studies validated molecular pathways. Results: This study utilized network pharmacology to investigate the therapeutic effects and mechanisms of LAH on obesity. Through relevant databases, 19 major chemical components and 605 potential targets were identified. KEGG pathway analysis identified the AMPK signaling pathway as a key target of LAH. Animal experiments showed that LAH reduced body weight by 16.55 % compared to HFD-induced mice. In addition to weight reduction, LAH significantly improved serum metabolic parameters. Glucose, triglyceride, and cholesterol levels were significantly reduced, and liver function improved, with ALT decreasing from 142.00 ± 32.63 U/L (HFD) to 63.57 ± 33.16 U/L (H-LAH), and AST from 147.20 ± 12.92 U/L (HFD) to 81.71 ± 31.31 U/L (H-LAH). It also enhanced liver antioxidant en

关键词： AMPK pathway Herb-based supplements Network pharmacology Obesity Proteomics analysis

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Application of bioactive molecular networking to identify corneal-cytoprotective compounds from Dialium cochinchinense Pierre. leaves

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Current Plant Biology 2025年 42卷

作者： Nguyen, Thi Tuyet Nhung Lin, Yu-Chi Nguyen, Le-Anh-Tuan Chao, Chih-Hua Vo, Thanh-Hoa Hsu, Su-Jung Tsai, Keng-Chang Lee, Ching-Kuo Cheng, Jing-Jy Ph.D. Program in Clinical Drug Development of Herbal Medicine College of Pharmacy Taipei Medical University Taipei 11031 Taiwan National Research Institute of Chinese Medicine Taipei 11221 Taiwan Faculty of Pharmacy Lac Hong University Dong Nai 810000 Viet Nam School of Pharmacy China Medical University Taichung 404328 Taiwan Chinese Medicine Research and Development Center China Medical University Hospital Taichung 404327 Taiwan University of Health Sciences Vietnam National University Ho Chi Minh City Ho Chi Minh City 700000 Viet Nam Center for Discovery and Development of Healthcare Product Vietnam National University Ho Chi Minh City Ho Chi Minh 700000 Viet Nam Institute of Fisheries Science National Taiwan University Taipei 106 Taiwan

Dry eye disease (DED) requires innovative therapeutic strategies targeting inflammation and oxidative stress. In this study, we demonstrate for the first time that Dialium cochinchinense leaf extracts exhibited significant anti-inflammatory activities by inhibiting the nuclear transcription factor-κB (NF-κB) signaling pathway in macrophages. Additionally, these extracts showed notable antioxidant and cytoprotective capabilities, effectively mitigating oxidative stress-induced damage in corneal epithelial cells. We employed an advanced bioactive molecular networking strategy to prioritize and isolate key bioactive compounds, providing distinct advantages over traditional phytochemical screening methods. This approach led to the discovery of a new compound, 6S,9R-2′-O-sinapoyl-roseoside, and 11 known phenolic compounds. Notably, 10 of these compounds exhibited substantial corneal-cytoprotective effects in vitro. Network pharmacology analysis revealed 65 key shared targets between these compounds and DED, linked to PI3K/AKT and MAPK pathways critical for inflammation and cell survival. Subsequent molecular docking and molecular dynamics simulations confirmed stable and high-affinity binding interactions between the identified lead compounds and key protein targets implicated in DED. These findings demonstrate D. cochinchinense leaf extract and its bioactive constituents are promising natural candidates for DED, providing a scientific basis for further translational research and potential drug development. © 2025 The Authors

关键词： Bioactive molecular networking Cytoprotective effect Dialium cochinchinense Dry eye disease Molecular dynamics simulations Network pharmacology

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New ent-kaurene and germacrene derivatives from Mesona procumbens Hemseley and their biological activity

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Natural Product Research 2023年第13期37卷 2172-2180页

作者： Ganzon, Jerome G. Liaw, Chia-Ching Lin, Yu-Chi Lin, Zhi-Hu Wang, Chang-Hung Chen, Che-Yi Chuang, Kuo-Hsiang Kuo, Yao-Haur Division of Chinese Materia Medica Development National Research Institute of Chinese Medicine Taipei Taiwan Department of Biochemical Science and Technology National Chiayi University Chiayi Taiwan Ph.D. Program in Clinical Drug Development of Herbal Medicine Taipei Medical University Taipei Taiwan Graduate Institute of Pharmacognosy College of Pharmacy Taipei Medical University Taipei Taiwan Graduate Institute of Integrated Medicine College of Chinese Medicine China Medical University Taichung Taiwan Department of Research and Development Starsci Biotech Co. Ltd Taoyuan Taiwan

Mesona procumbens Hemseley is a well-known traditional herbal medicine used for heat-related ailments. In Taiwan, boiled extracts of M. procumbens are also used as desserts called grass jelly. In this study, the hexane extract from 75% EtOH of M. procumbens showed potent activities on inhibition of E. coli β-glucuronidase (eβG) and NO production and cytotoxicity against MCF-7 and HepG2 cancer cell lines. Furthermore, using various flash columns and HPLC chromatography on the bioactive layer led to the isolation of twelve compounds (1–12), including a new ent-kaurene, mesokaurol A (1), and a new germacrene derivative, mesogermapene A (2). Their structures were elucidated by extensive spectroscopic analyses, especially 2 D NMR and mass data. Biological assays showed that compound 9 (linolenic acid) had specific activity on inhibition of eβG (68.27%) at 100 µg/mL but was non-inhibitory to human β-glucuronidase. Compound 1 possessed significant cytotoxicity against MCF-7 (EC₅₀ = 9.76 µM) and HepG2 (EC₅₀ = 8.64 µM) cancer cell lines. © 2022 Informa UK Limited, trading as Taylor & Francis Group.

关键词： Anti-β-glucuronidase cytotoxicity germacrene Kaurane-type diterpene Mesona procumbens Hemseley

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