A phytochemical investigation of the roots of Euphorbia fischeriana led to the isolation of four tigliane-type diterpenoid glucosides (1-2, 4, and 5) and two daphnane-type diterpenoid glucosides (3 and 6). Compounds 1-3 represent previously undescribed structures. Their chemical structures were fully elucidated through comprehensive spectroscopic analyses, including HRESIMS, IR and NMR experiments. A plausible biosynthetic pathway for 1-6 is also proposed. In bioactivity tests, compounds 2, 4, and 5 exhibited notable inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophages, suggesting their potential anti-inflammatory activity.
{"title":"Tigliane and daphnane diterpenoid glucosides from the roots of Euphorbia fischeriana: Isolation, structural elucidation, and anti-inflammatory activity.","authors":"Jia Zhang, Xian-Feng Yue, Meng-Ya Wang, Jia-Lu Du, Yi-Lin Chen, Li-Wei Ma, Jie-Kun Xu","doi":"10.1016/j.fitote.2026.107177","DOIUrl":"https://doi.org/10.1016/j.fitote.2026.107177","url":null,"abstract":"<p><p>A phytochemical investigation of the roots of Euphorbia fischeriana led to the isolation of four tigliane-type diterpenoid glucosides (1-2, 4, and 5) and two daphnane-type diterpenoid glucosides (3 and 6). Compounds 1-3 represent previously undescribed structures. Their chemical structures were fully elucidated through comprehensive spectroscopic analyses, including HRESIMS, IR and NMR experiments. A plausible biosynthetic pathway for 1-6 is also proposed. In bioactivity tests, compounds 2, 4, and 5 exhibited notable inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophages, suggesting their potential anti-inflammatory activity.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"107177"},"PeriodicalIF":2.6,"publicationDate":"2026-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147456619","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Colorectal cancer (CRC) is the third leading cause of cancer-related mortality worldwide, representing a serious threat to human life and health. There is an urgent need to develop novel therapeutic agents. Longan (Dimocarpus longan Lour.), a plant typical used for both medicinal and food purposes, has been shown in modern pharmacological studies to possess significant anti-CRC activity in its seeds and flowers. However, the active components in longan leaves and their potential anti-CRC effects remain unexplored. In this study, the ethanol extract of longan leaves (ELL) was separated and purified using ODS column chromatography and preparative HPLC. The major constituents of ELL were identified through a combination of hydrolytic monosaccharide analysis, high-resolution mass spectrometry, nuclear magnetic resonance spectroscopy, and HPLC comparison with standards. Subsequently, an integrative approach incorporating network pharmacology, molecular docking, molecular dynamics (MD) simulations, along with experimental validations-including CCK-8, apoptosis, wound healing assay, transwell assay, and Western blotting-was employed to investigate the mechanism underlying the inhibitory effect of ELL on CRC. Seven flavonoid glycosides were identified from longan leaves with five compounds reported for the first time. ELL significantly suppressed proliferation and migration, and induced apoptosis in CRC cells. Network pharmacology, molecular docking, and MD simulations suggested that the primary active compounds in ELL contributing to its anti-CRC activity are afzelin, quercitrin, and trifolin, with AKT1 as the key target. Western blot analysis confirmed that ELL markedly downregulated AKT1 protein expression. These findings indicate that ELL may serve as a potential therapeutic agent for colorectal cancer.
{"title":"From computational prediction to in vitro experimental validation: Identifying active compounds in longan leaves and their anti-colorectal cancer mechanisms.","authors":"Jinrui Wei, Yuxin Xie, Jianfeng Qin, Yina Ouyang, Haifeng Qin, Dongxing Zhou, Huizhen Wang, Mingming Wei, Lichuan Wu","doi":"10.1016/j.fitote.2026.107178","DOIUrl":"10.1016/j.fitote.2026.107178","url":null,"abstract":"<p><p>Colorectal cancer (CRC) is the third leading cause of cancer-related mortality worldwide, representing a serious threat to human life and health. There is an urgent need to develop novel therapeutic agents. Longan (Dimocarpus longan Lour.), a plant typical used for both medicinal and food purposes, has been shown in modern pharmacological studies to possess significant anti-CRC activity in its seeds and flowers. However, the active components in longan leaves and their potential anti-CRC effects remain unexplored. In this study, the ethanol extract of longan leaves (ELL) was separated and purified using ODS column chromatography and preparative HPLC. The major constituents of ELL were identified through a combination of hydrolytic monosaccharide analysis, high-resolution mass spectrometry, nuclear magnetic resonance spectroscopy, and HPLC comparison with standards. Subsequently, an integrative approach incorporating network pharmacology, molecular docking, molecular dynamics (MD) simulations, along with experimental validations-including CCK-8, apoptosis, wound healing assay, transwell assay, and Western blotting-was employed to investigate the mechanism underlying the inhibitory effect of ELL on CRC. Seven flavonoid glycosides were identified from longan leaves with five compounds reported for the first time. ELL significantly suppressed proliferation and migration, and induced apoptosis in CRC cells. Network pharmacology, molecular docking, and MD simulations suggested that the primary active compounds in ELL contributing to its anti-CRC activity are afzelin, quercitrin, and trifolin, with AKT1 as the key target. Western blot analysis confirmed that ELL markedly downregulated AKT1 protein expression. These findings indicate that ELL may serve as a potential therapeutic agent for colorectal cancer.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"107178"},"PeriodicalIF":2.6,"publicationDate":"2026-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147456580","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-03-04DOI: 10.1016/j.fitote.2026.107151
Shang Jia, Huasong Bai, Tong Liu, Hengyan Wang, Ye Yue, Zhanzhong Wang
{"title":"Corrigendum to 'Insight into the effect and mechanisms of ginsenosides and perilla seed extracts on hepatocellular bioactivities: Hypolipidemic, hypoglycemic, and antioxidant properties' [Fitoterapia 187 (2025) 106932].","authors":"Shang Jia, Huasong Bai, Tong Liu, Hengyan Wang, Ye Yue, Zhanzhong Wang","doi":"10.1016/j.fitote.2026.107151","DOIUrl":"https://doi.org/10.1016/j.fitote.2026.107151","url":null,"abstract":"","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"107151"},"PeriodicalIF":2.6,"publicationDate":"2026-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147364582","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Baliospermum effusum Pax et Hoffm., a shrub known as “Baodongdian” in Dai folk medicine, has been traditionally employed for treating traumatic injuries, rheumatism, and jaundice. The present study investigated the acute toxicity, anti-inflammatory and antinociceptive properties, and phytochemical constituents of the 95 % ethanolic extract of B. effusum (EEBe). The toxicity assessment revealed that EEBe (2000 mg/kg) induced no adverse effects in behavior, mortality, body/organ weights, histopathology, or biochemical parameters over 14 d. Pharmacological assays on EEBe (150, 300, and 600 mg/kg) revealed that it effectively inhibited carrageenan-induced paw edema (n = 10), xylene-stimulated ear edema (n = 8), and acetic acid-triggered writhes (n = 8), while showing no significant antinociceptive activity in the hot-plate test (n = 8). ELISA (n = 8) showed that EEBe modulated serum IL-1β, IL-6, and IL-10 levels, while qRT-PCR (n = 5) demonstrated the downregulation of IL-1β and IL-6 mRNA expression. Furthermore, eight compounds including 4-hydroxy-2,3-dimethyl-2-nonen-4-olide (1), 22-dehydroclerosterol (2), β-sitosterol (3), vanillin (4), 1-linolenoylglycerol (5), 1-O-stearoyl-glycerol (6), bis(2,3-dihydroxypropyl)nonanedioate (7), and (3S,5S)-diverniciaoid A (8) were isolated from EEBe, with compounds 5 and 7 suppressing NO production in LPS-induced RAW 264.7 macrophages. These data revealed that EEBe was non-toxic at 2000 mg/kg and exhibited anti-inflammatory and antinociceptive properties, and that 5 and 7, reported for the first time from this species, showed anti-inflammatory activity in vitro, collectively supporting the folk use of B. effusum for inflammatory and pain-related disorders. To our knowledge, this is the first report on the in vivo pharmacological activities and toxicity of B. effusum.
{"title":"Phytochemical constituents and toxicological, anti-inflammatory, and antinociceptive assessment of Baliospermum effusum Pax et Hoffm.","authors":"Qing-Ying Hong, Zu-Hui Wang, Yi-Hang Ba, Yi-Huan Li, De-Xin Li, Hong-Ping He, Rui Yang, Hua-Yi Jiang","doi":"10.1016/j.fitote.2025.107078","DOIUrl":"10.1016/j.fitote.2025.107078","url":null,"abstract":"<div><div><em>Baliospermum effusum</em> Pax et Hoffm., a shrub known as “Baodongdian” in Dai folk medicine, has been traditionally employed for treating traumatic injuries, rheumatism, and jaundice. The present study investigated the acute toxicity, anti-inflammatory and antinociceptive properties, and phytochemical constituents of the 95 % ethanolic extract of <em>B</em>. <em>effusum</em> (EEBe). The toxicity assessment revealed that EEBe (2000 mg/kg) induced no adverse effects in behavior, mortality, body/organ weights, histopathology, or biochemical parameters over 14 d. Pharmacological assays on EEBe (150, 300, and 600 mg/kg) revealed that it effectively inhibited carrageenan-induced paw edema (<em>n</em> = 10), xylene-stimulated ear edema (<em>n</em> = 8), and acetic acid-triggered writhes (<em>n</em> = 8), while showing no significant antinociceptive activity in the hot-plate test (<em>n</em> = 8). ELISA (<em>n</em> = 8) showed that EEBe modulated serum IL-1<em>β</em>, IL-6, and IL-10 levels, while qRT-PCR (<em>n</em> = 5) demonstrated the downregulation of IL-1<em>β</em> and IL-6 mRNA expression. Furthermore, eight compounds including 4-hydroxy-2,3-dimethyl-2-nonen-4-olide (<strong>1</strong>), 22-dehydroclerosterol (<strong>2</strong>), <em>β</em>-sitosterol (<strong>3</strong>), vanillin (<strong>4</strong>), 1-linolenoylglycerol (<strong>5</strong>), 1-<em>O</em>-stearoyl-glycerol (<strong>6</strong>), bis(2,3-dihydroxypropyl)nonanedioate (<strong>7</strong>), and (3<em>S</em>,5<em>S</em>)-diverniciaoid A (<strong>8</strong>) were isolated from EEBe, with compounds <strong>5</strong> and <strong>7</strong> suppressing NO production in LPS-induced RAW 264.7 macrophages. These data revealed that EEBe was non-toxic at 2000 mg/kg and exhibited anti-inflammatory and antinociceptive properties, and that <strong>5</strong> and <strong>7</strong>, reported for the first time from this species, showed anti-inflammatory activity in vitro, collectively supporting the folk use of <em>B</em>. <em>effusum</em> for inflammatory and pain-related disorders. To our knowledge, this is the first report on the in vivo pharmacological activities and toxicity of <em>B</em>. <em>effusum</em>.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107078"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145892275","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-03-01Epub Date: 2025-12-26DOI: 10.1016/j.fitote.2025.107044
Qiya Zhang , Meiqin Wang , Li Jiang , Yang Wang , Yuan Lu , Xue Ma , Yongjun Li
This study investigated the chemical composition of Hypericum patulum and its plasma metabolites in rats using ultra-high-performance liquid chromatography coupled to a Q-Exactive Plus Orbitrap mass spectrometer (UPLC-Q Exactive Plus Orbitrap MS). A total of 162 compounds were identified in the plant extract of H. patulum, encompassing 50 flavonoids, 32 organic acids, 26 xanthones, 12 polycyclic polyprenylated acylphloroglucinols (PPAPs), 10 amino acids, 8 coumarins, 5 alkaloids, 3 sugars, 2 terpenoids, 3 aldehydes, and 11 others. Analysis of rat plasma revealed 48 compounds, consisting of 20 prototypes (predominantly xanthones, organic acids, and flavonoids) and 28 metabolites generated via glucuronidation, methylation, and sulfation. In LPS-induced RAW 264.7 macrophages, H. patulum extract significantly inhibited NO release and suppressed the expression of pro-inflammatory mediators, including IL-6, TNF-α, COX-2, iNOS, and IL-1β. In vivo, quercetin and shikimic acid attenuated xylene-induced ear edema and inflammatory infiltration in mice, and also lowered serum levels of the pro-inflammatory cytokines TNF-α, IL-6, and IL-1β. Antibacterial testing revealed that shikimic acid demonstrated activity against a panel of pathogens, with minimum inhibitory concentration (MIC) of 13.00, 6.50, and 20.08 mg/mL against Staphylococcus aureus, Escherichia coli, and β-hemolytic Streptococcus, respectively. Vanillic acid showed MICs of 6.50 mg/mL against S. aureus and 3.25 mg/mL against E. coli, whereas quercetin inhibited S. aureus at a concentration of 3.25 mg/mL. These findings characterize the pharmacologically active components of H. patulum, thereby validating its traditional use and laying a foundation for future investigations into its therapeutic mechanisms.
采用超高效液相色谱- Q-Exactive Plus Orbitrap质谱联用技术（UPLC-Q Exactive Plus Orbitrap MS）对大鼠血药金丝桃及其血浆代谢物的化学成分进行了研究。共鉴定出162种化合物，包括50种黄酮类化合物、32种有机酸、26种山酮类化合物、12种多环聚丙烯酰化酰基间苯三酚（PPAPs）、10种氨基酸、8种香豆素、5种生物碱、3种糖、2种萜类化合物、3种醛类化合物和11种其他化合物。对大鼠血浆的分析发现了48种化合物，包括20种原型化合物（主要是山酮类、有机酸和类黄酮）和28种通过葡萄糖醛酸化、甲基化和磺化产生的代谢物。在lps诱导的RAW 264.7巨噬细胞中，育兔草提取物显著抑制NO释放，抑制IL-6、TNF-α、COX-2、iNOS和IL-1β等促炎介质的表达。在体内，槲皮素和莽草酸可减轻二甲苯诱导的小鼠耳部水肿和炎症浸润，并降低血清中促炎细胞因子TNF-α、IL-6和IL-1β的水平。抑菌试验表明，莽草酸对多种病原菌均有抑制作用，对金黄色葡萄球菌、大肠杆菌和β-溶血性链球菌的最低抑制浓度（MIC）分别为13.00、6.50和20.08 mg/mL。香草酸对金黄色葡萄球菌的mic为6.50 mg/mL，对大肠杆菌的mic为3.25 mg/mL，槲皮素对金黄色葡萄球菌的mic为3.25 mg/mL。这些发现表征了黄菌的药理活性成分，从而验证了其传统用途，并为进一步研究其治疗机制奠定了基础。
{"title":"Study on chemical composition, plasma-absorbed components, and anti-inflammatory and antibacterial activity of Hypericum patulum","authors":"Qiya Zhang , Meiqin Wang , Li Jiang , Yang Wang , Yuan Lu , Xue Ma , Yongjun Li","doi":"10.1016/j.fitote.2025.107044","DOIUrl":"10.1016/j.fitote.2025.107044","url":null,"abstract":"<div><div>This study investigated the chemical composition of <em>Hypericum patulum</em> and its plasma metabolites in rats using ultra-high-performance liquid chromatography coupled to a Q-Exactive Plus Orbitrap mass spectrometer (UPLC-Q Exactive Plus Orbitrap MS). A total of 162 compounds were identified in the plant extract of <em>H. patulum</em>, encompassing 50 flavonoids, 32 organic acids, 26 xanthones, 12 polycyclic polyprenylated acylphloroglucinols (PPAPs), 10 amino acids, 8 coumarins, 5 alkaloids, 3 sugars, 2 terpenoids, 3 aldehydes, and 11 others. Analysis of rat plasma revealed 48 compounds, consisting of 20 prototypes (predominantly xanthones, organic acids, and flavonoids) and 28 metabolites generated via glucuronidation, methylation, and sulfation. In LPS-induced RAW 264.7 macrophages, <em>H. patulum</em> extract significantly inhibited NO release and suppressed the expression of pro-inflammatory mediators, including IL-6, TNF-<em>α</em>, COX-2, iNOS, and IL-1<em>β</em>. In vivo, quercetin and shikimic acid attenuated xylene-induced ear edema and inflammatory infiltration in mice, and also lowered serum levels of the pro-inflammatory cytokines TNF-<em>α</em>, IL-6, and IL-1<em>β</em>. Antibacterial testing revealed that shikimic acid demonstrated activity against a panel of pathogens, with minimum inhibitory concentration (MIC) of 13.00, 6.50, and 20.08 mg/mL against <em>Staphylococcus aureus</em>, <em>Escherichia coli</em>, and <em>β-hemolytic Streptococcus</em>, respectively. Vanillic acid showed MICs of 6.50 mg/mL against <em>S. aureus</em> and 3.25 mg/mL against <em>E. coli</em>, whereas quercetin inhibited <em>S. aureus</em> at a concentration of 3.25 mg/mL. These findings characterize the pharmacologically active components of <em>H. patulum</em>, thereby validating its traditional use and laying a foundation for future investigations into its therapeutic mechanisms.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107044"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145849585","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-03-01Epub Date: 2025-12-27DOI: 10.1016/j.fitote.2025.107077
Karolina Matejczuk , Piotr M. Kuś , Piotr Szweda
Bee bread (BB), a fermented bee product rich in bioactive compounds, such as aminoacids and peptides, vitamins and polyphenols, has garnered attention for its potential health benefits, particularly high antioxidant potential. However, its role in protecting genetic material from damage (antigenotoxic and antimutagenic activity) remains largely unexplored. This study provides the first comprehensive evaluation of both antigenotoxic and antimutagenic activities of Polish bee bread extracts in human HEK293 cells, integrating functional assays with advanced chemical profiling.
Twenty Polish BB samples were analyzed for antioxidant activity using DPPH Radical Scavenging Assay and Cellular Antioxidant Activity assays, revealing significant radical scavenging and intracellular ROS reduction capacities. UHPLC-DAD-QqTOF-MS profiling identified 71 compounds, predominantly flavonoids and phenolamides, known for their cytoprotective roles.
Importantly, comet assay results demonstrated that BB extracts significantly reduced methyl methanesulfonate (MMS)-induced DNA strand breaks, while cytokinesis-block micronucleus assay confirmed up to 91 % reduction in mutagenicity without intrinsic genotoxicity. Unlike previous studies that focused primarily on antioxidant activity, our work establishes bee bread as a natural chemoprotective agent against DNA damage and chromosomal instability, highlighting its potential in disease prevention. These findings expand the current understanding of bee bread bioactivity and position it as a promising candidate for functional food and nutraceutical applications.
{"title":"Bee bread as a natural shield against genetic damage: Investigation of antigenotoxic and antimutagenic potential","authors":"Karolina Matejczuk , Piotr M. Kuś , Piotr Szweda","doi":"10.1016/j.fitote.2025.107077","DOIUrl":"10.1016/j.fitote.2025.107077","url":null,"abstract":"<div><div>Bee bread (BB), a fermented bee product rich in bioactive compounds, such as aminoacids and peptides, vitamins and polyphenols, has garnered attention for its potential health benefits, particularly high antioxidant potential. However, its role in protecting genetic material from damage (antigenotoxic and antimutagenic activity) remains largely unexplored. This study provides the first comprehensive evaluation of both antigenotoxic and antimutagenic activities of Polish bee bread extracts in human HEK293 cells, integrating functional assays with advanced chemical profiling.</div><div>Twenty Polish BB samples were analyzed for antioxidant activity using DPPH Radical Scavenging Assay and Cellular Antioxidant Activity assays, revealing significant radical scavenging and intracellular ROS reduction capacities. UHPLC-DAD-QqTOF-MS profiling identified 71 compounds, predominantly flavonoids and phenolamides, known for their cytoprotective roles.</div><div>Importantly, comet assay results demonstrated that BB extracts significantly reduced methyl methanesulfonate (MMS)-induced DNA strand breaks, while cytokinesis-block micronucleus assay confirmed up to 91 % reduction in mutagenicity without intrinsic genotoxicity. Unlike previous studies that focused primarily on antioxidant activity, our work establishes bee bread as a natural chemoprotective agent against DNA damage and chromosomal instability, highlighting its potential in disease prevention. These findings expand the current understanding of bee bread bioactivity and position it as a promising candidate for functional food and nutraceutical applications.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107077"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145855107","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-03-01Epub Date: 2025-12-22DOI: 10.1016/j.fitote.2025.107051
Ke Xu , Xiao-Bin Li , Yu-Liang Xu , Fei Xie , Hong-Xiang Lou
Inclusion of the histone deacetylase (HDAC) inhibitor suberoylanilide hydroxamic acid (SAHA) into the culture medium of the endolichenic fungus Phialocephala fortinii resulted in the separation of three new perylenequinones phialocephalarins E-G (1–3) and enhanced the production of the known compounds phialocephalarins A-B (4–5). A comprehensive spectral analysis combined with electron circular dichroism (ECD) data has elucidated their structures. Phialocephalarin E (1) displayed anti-inflammatory activity with the maximum inhibition rate of 57.3 % ± 7.3 % (50 μM). Further molecular docking experiment revealed the affinity degree of compound 1 to the prostaglandin E2 receptor 4 (EP4R) and the molecular dynamics (MD) simulation results showed compound 1-EP4R complex had relatively good binding stability.
{"title":"Anti-inflammatory perylenequinones from the endolichenic fungus Phialocephala fortinii triggered by a histone deacetylase inhibitor","authors":"Ke Xu , Xiao-Bin Li , Yu-Liang Xu , Fei Xie , Hong-Xiang Lou","doi":"10.1016/j.fitote.2025.107051","DOIUrl":"10.1016/j.fitote.2025.107051","url":null,"abstract":"<div><div>Inclusion of the histone deacetylase (HDAC) inhibitor suberoylanilide hydroxamic acid (SAHA) into the culture medium of the endolichenic fungus <em>Phialocephala fortinii</em> resulted in the separation of three new perylenequinones phialocephalarins <em>E</em>-G (<strong>1</strong>–<strong>3</strong>) and enhanced the production of the known compounds phialocephalarins A-B (<strong>4</strong>–<strong>5)</strong>. A comprehensive spectral analysis combined with electron circular dichroism (ECD) data has elucidated their structures. Phialocephalarin E (<strong>1</strong>) displayed anti-inflammatory activity with the maximum inhibition rate of 57.3 % ± 7.3 % (50 μM). Further molecular docking experiment revealed the affinity degree of compound <strong>1</strong> to the prostaglandin E2 receptor 4 (EP4R) and the molecular dynamics (MD) simulation results showed compound <strong>1</strong>-EP4R complex had relatively good binding stability.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107051"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827027","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-03-01Epub Date: 2026-01-02DOI: 10.1016/j.fitote.2025.107079
Zhongyou Yang , Jiankun Hong , Wuling Liu , Kunlin Yu , Anling Hu , Yi Kuang , Eldad Zacksenhaus , Xiao Xiao , Jingrui Song , Lei Huang , Chunlin Wang , Yanmei Li , Yaacov Ben-David
Acute erythroid leukemia (AEL), a rare form of acute myeloid leukemia (AML), is defined as type M6 under the FAB classification, and characterized by inhibition of terminal differentiation and rapid expansion of erythroid progenitors. Despite its poor prognosis, AEL responds well to chemotherapy. Yet, the frequent emergence of resistant clones is a major concern, necessitating the development of alternative therapeutic strategies to treat this rare disease. Yuxingcao formula (YXCF), which consists of 5 herbs, is used in Traditional Chinese Medicine to treat various diseases including cancer, although the underlying mechanisms are not fully understood. Herein, we shown that in an animal model of erythroleukemia induced by Friend virus, YXCF treatment strongly inhibits leukemia progression accompanied by induction of erythroid differentiation, apoptosis and cell cycle arrest. UPLC-MS/MS and network pharmacology analyses of YXCF identified 89 compounds, 20 of which are known to have anti-cancer activity. Molecular docking identified AKT1 as a potential target of one of these compounds, baicalein. In docking and CETSA analyses, baicalein binds AKT leading to inhibition of its phosphorylation and its target mTOR. Baicalein significantly inhibited proliferation of leukemic cells in culture associated with induction of apoptosis and cell cycle arrest as well as suppression of erythroleukemogenesis in vivo. YXCF is also inhibits the FLI1 oncogene, known to play a critical role in erythroleukemia, likely through kaempferol, another YXCF compound. Understanding the role of other components of YXCF may eventually enable the development of a combination drug therapy with optimal anti-leukemia activity for the treatment of AEL.
{"title":"Yuxingcao formula suppresses acute erythroleukemia through inhibition of AKT1 and FLI1","authors":"Zhongyou Yang , Jiankun Hong , Wuling Liu , Kunlin Yu , Anling Hu , Yi Kuang , Eldad Zacksenhaus , Xiao Xiao , Jingrui Song , Lei Huang , Chunlin Wang , Yanmei Li , Yaacov Ben-David","doi":"10.1016/j.fitote.2025.107079","DOIUrl":"10.1016/j.fitote.2025.107079","url":null,"abstract":"<div><div>Acute erythroid leukemia (AEL), a rare form of acute myeloid leukemia (AML), is defined as type M6 under the FAB classification, and characterized by inhibition of terminal differentiation and rapid expansion of erythroid progenitors. Despite its poor prognosis, AEL responds well to chemotherapy. Yet, the frequent emergence of resistant clones is a major concern, necessitating the development of alternative therapeutic strategies to treat this rare disease. Yuxingcao formula (YXCF), which consists of 5 herbs, is used in Traditional Chinese Medicine to treat various diseases including cancer, although the underlying mechanisms are not fully understood. Herein, we shown that in an animal model of erythroleukemia induced by Friend virus, YXCF treatment strongly inhibits leukemia progression accompanied by induction of erythroid differentiation, apoptosis and cell cycle arrest. UPLC-MS/MS and network pharmacology analyses of YXCF identified 89 compounds, 20 of which are known to have anti-cancer activity. Molecular docking identified AKT1 as a potential target of one of these compounds, baicalein. In docking and CETSA analyses, baicalein binds AKT leading to inhibition of its phosphorylation and its target mTOR. Baicalein significantly inhibited proliferation of leukemic cells in culture associated with induction of apoptosis and cell cycle arrest as well as suppression of erythroleukemogenesis in vivo. YXCF is also inhibits the FLI1 oncogene, known to play a critical role in erythroleukemia, likely through kaempferol, another YXCF compound. Understanding the role of other components of YXCF may eventually enable the development of a combination drug therapy with optimal anti-leukemia activity for the treatment of AEL.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107079"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145899731","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-03-01Epub Date: 2026-01-19DOI: 10.1016/j.fitote.2026.107102
Xiaojing Wei , Binjing Zhao , Xinyi Jiang , Lunli Lan , Rui Wang , Yuanyuan Li
Vladimiria souliei(Franch.)Ling is used as medicine with dried roots, which is a perennial herb in Asteraceae family. It has been generally applied as traditional Chinese medicine with relieving abdominal swelling or pain, and treatment of digestive system disease. However, the pharmacological mechanism of alleviating gastric ulcer (GU) for this herb were still unknown. UPLC-Q-TOF/MS was performed to analyze the main components of Vladimiria souliei extract (VSE). Based on the results of histopathological observation, cytokines assay, and immunohistochemistry staining, the therapeutic effect of VSE on ethanol-induced GU was appraised. Meanwhile, the CCK-8, LDH assay and crystal violet staining were assessed to evaluate the appropriate concentration of VSE in vitro. In GES-1 cells induced by ethanol, the cell viability, ROS and cell membrane damage assay were detected after the interference of VSE. Then, several pivotal proteins relating to necroptosis in GES-1 were evaluated through immunofluorescence staining to illustrate the further pharma-cological mechanisms. As a result, VSE significantly restrained the expansion of ulcer area, reduced the pepsin activity, restored the levels of SOD, decreased the levels of MDA, ROS, TNF-α, IL-1β, IL-6, and IL-18, ultimately ameliorated the gastric mucosa injury. Further analysis exhibited that VSE significantly inhibited the cellular necroptosis by down-regulating the levels of RIP1, RIP3 and MLKL. Conclusions: This research clarified that the VSE could improve gastric mucosal injury through inhibition of RIP1-RIP3-MLKL necrosome activation, which might provide scientific evidences on the application of Vladimiria souliei as a ethnic herb to ameliorate GU.
{"title":"Vladimiria souliei alleviated ethanol induced gastric ulcer through inhibition of RIP1-RIP3-MLKL necrosome activation","authors":"Xiaojing Wei , Binjing Zhao , Xinyi Jiang , Lunli Lan , Rui Wang , Yuanyuan Li","doi":"10.1016/j.fitote.2026.107102","DOIUrl":"10.1016/j.fitote.2026.107102","url":null,"abstract":"<div><div><em>Vladimiria souliei(Franch.)Ling</em> is used as medicine with dried roots, which is a perennial herb in Asteraceae family. It has been generally applied as traditional Chinese medicine with relieving abdominal swelling or pain, and treatment of digestive system disease. However, the pharmacological mechanism of alleviating gastric ulcer (GU) for this herb were still unknown. UPLC-Q-TOF/MS was performed to analyze the main components of <em>Vladimiria souliei</em> extract (VSE). Based on the results of histopathological observation, cytokines assay, and immunohistochemistry staining, the therapeutic effect of VSE on ethanol-induced GU was appraised. Meanwhile, the CCK-8, LDH assay and crystal violet staining were assessed to evaluate the appropriate concentration of VSE <em>in vitro.</em> In GES-1 cells induced by ethanol, the cell viability, ROS and cell membrane damage assay were detected after the interference of VSE. Then, several pivotal proteins relating to necroptosis in GES-1 were evaluated through immunofluorescence staining to illustrate the further pharma-cological mechanisms. As a result, VSE significantly restrained the expansion of ulcer area, reduced the pepsin activity, restored the levels of SOD, decreased the levels of MDA, ROS, TNF-α, IL-1β, IL-6, and IL-18, ultimately ameliorated the gastric mucosa injury. Further analysis exhibited that VSE significantly inhibited the cellular necroptosis by down-regulating the levels of RIP1, RIP3 and MLKL. Conclusions: This research clarified that the VSE could improve gastric mucosal injury through inhibition of RIP1-RIP3-MLKL necrosome activation, which might provide scientific evidences on the application of <em>Vladimiria souliei</em> as a ethnic herb to ameliorate GU.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107102"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146017933","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-03-01Epub Date: 2026-02-02DOI: 10.1016/j.fitote.2026.107120
Putri Cahaya Situmorang , Helen Helen , Syafruddin Ilyas , Pandu Surya Pangestu , Syahputra Wibowo , Kaniwa Berliani , Alexander Patera Nugraha , Khatarina Meldawati Pasaribu
The increasing use of herbal electronic cigarettes raises concerns regarding their biological impact beyond conventional nicotine delivery. Although marketed as “natural” alternatives, their phytochemical vapors interact with molecular pathways that may influence respiratory health. This review summarizes current evidence on the molecular crosstalk between herbal phytochemicals and microRNAs (miRNAs) in the context of electronic cigarette vapor exposure, emphasizing their roles in oxidative stress, inflammation, and tissue remodelling. Literature was systematically examined to evaluate in vitro, in vivo, and bioinformatics findings on phytochemicals commonly incorporated in herbal e-liquids. Key molecular pathways (NF-κB, Nrf2/HO-1, MAPK, PI3K/Akt/mTOR, and TGF-β/Smad) and miRNA regulators were analyzed to elucidate mechanisms of lung injury and protection. The search strategy involved PubMed, Web of Science, and Scopus databases, using the keywords “herbal e-liquid,” “phytochemicals,” “lung injury,” “miRNA,” and “molecular pathway.” Evidence indicates that bioactive phytochemicals such as quercetin, linalool, and EGCG can modulate the expression of miRNAs (e.g., miR-21, miR-146a, miR-155, miR-210), thereby regulating inflammatory and oxidative responses. Crosstalk between these phytochemicals and miRNAs contributes to dual effects: mitigating reactive oxygen species and cytokine overproduction, while in some cases promoting pro-inflammatory or fibrotic signalling under chronic exposure. This bidirectional modulation highlights the complex balance between potential therapeutic benefits and risks of herbal vapor inhalation. Herbal electronic cigarettes cannot be considered risk-free. Their phytochemicals engage in intricate interactions with miRNA networks and molecular pathways that may influence respiratory health. Understanding this molecular crosstalk is essential for evaluating safety, guiding regulatory strategies, and identifying therapeutic prospects of phytochemical-based inhalation systems.
越来越多的草药电子烟的使用引起了人们对其生物影响的担忧，而不仅仅是传统的尼古丁输送。虽然作为“天然”替代品销售，但它们的植物化学蒸汽与可能影响呼吸健康的分子途径相互作用。本文综述了在电子烟蒸汽暴露的背景下，草药植物化学物质和microrna （mirna）之间的分子串扰的现有证据，强调了它们在氧化应激、炎症和组织重构中的作用。系统地检查了文献，以评估体外、体内和生物信息学的发现，这些发现通常包含在草药电子液体中。分析关键分子通路（NF-κB、Nrf2/HO-1、MAPK、PI3K/Akt/mTOR、TGF-β/Smad）和miRNA调节因子，阐明肺损伤机制及其保护作用。搜索策略涉及PubMed， Web of Science和Scopus数据库，使用关键词“草药电子液体”，“植物化学物质”，“肺损伤”，“miRNA”和“分子途径”。有证据表明，槲皮素、芳樟醇和EGCG等生物活性植物化学物质可以调节mirna（如miR-21、miR-146a、miR-155、miR-210）的表达，从而调节炎症和氧化反应。这些植物化学物质和mirna之间的串扰有助于双重作用：减轻活性氧和细胞因子的过量产生，同时在某些情况下促进慢性暴露下的促炎或纤维化信号传导。这种双向调节强调了草药蒸气吸入的潜在治疗益处和风险之间的复杂平衡。草药电子烟不能被认为是没有风险的。它们的植物化学物质与miRNA网络和可能影响呼吸健康的分子途径进行复杂的相互作用。了解这种分子串扰对于评估植物化学吸入系统的安全性、指导监管策略和确定治疗前景至关重要。
{"title":"Molecular crosstalk between herbal phytochemicals and microRNAs in electronic cigarette vapor: Implications for respiratory health","authors":"Putri Cahaya Situmorang , Helen Helen , Syafruddin Ilyas , Pandu Surya Pangestu , Syahputra Wibowo , Kaniwa Berliani , Alexander Patera Nugraha , Khatarina Meldawati Pasaribu","doi":"10.1016/j.fitote.2026.107120","DOIUrl":"10.1016/j.fitote.2026.107120","url":null,"abstract":"<div><div>The increasing use of herbal electronic cigarettes raises concerns regarding their biological impact beyond conventional nicotine delivery. Although marketed as “natural” alternatives, their phytochemical vapors interact with molecular pathways that may influence respiratory health. This review summarizes current evidence on the molecular crosstalk between herbal phytochemicals and microRNAs (miRNAs) in the context of electronic cigarette vapor exposure, emphasizing their roles in oxidative stress, inflammation, and tissue remodelling. Literature was systematically examined to evaluate in vitro, in vivo, and bioinformatics findings on phytochemicals commonly incorporated in herbal e-liquids. Key molecular pathways (NF-κB, Nrf2/HO-1, MAPK, PI3K/Akt/mTOR, and TGF-β/Smad) and miRNA regulators were analyzed to elucidate mechanisms of lung injury and protection. The search strategy involved PubMed, Web of Science, and Scopus databases, using the keywords “herbal e-liquid,” “phytochemicals,” “lung injury,” “miRNA,” and “molecular pathway.” Evidence indicates that bioactive phytochemicals such as quercetin, linalool, and EGCG can modulate the expression of miRNAs (e.g., miR-21, miR-146a, miR-155, miR-210), thereby regulating inflammatory and oxidative responses. Crosstalk between these phytochemicals and miRNAs contributes to dual effects: mitigating reactive oxygen species and cytokine overproduction, while in some cases promoting pro-inflammatory or fibrotic signalling under chronic exposure. This bidirectional modulation highlights the complex balance between potential therapeutic benefits and risks of herbal vapor inhalation. Herbal electronic cigarettes cannot be considered risk-free. Their phytochemicals engage in intricate interactions with miRNA networks and molecular pathways that may influence respiratory health. Understanding this molecular crosstalk is essential for evaluating safety, guiding regulatory strategies, and identifying therapeutic prospects of phytochemical-based inhalation systems.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107120"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146118311","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
扫码关注我们
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号