Pub Date : 2025-12-09DOI: 10.1016/j.fitote.2025.107035
Yuan Gao , Jia-Hui Wang , Ming-Qian Han , Rong Huang , Shao-Hua Wu
Three racemic pairs of new dimeric phthalides, (±)-phomophthalides A-C ((±)-1–3), together with eight known compounds (4–11), were obtained from the culture broth of the endophytic fungus Phomopsis sp. YM 355364 isolated from the medicinal plant Aconitum carmichaeli. The chemical structures of the new compounds were established by extensive NMR spectroscopic and HRESI-MS analysis and DP4+ calculations. The new compounds were tested for their antimicrobial activities by broth microdilution method. Compound 1 showed moderate inhibitory activity toward three pathogenic fungal strains Fusarium solani, Candida albicans, and Botrytis cinerea with MIC values of 16, 32, and 32 μg/mL, respectively. Compound 2 exhibited antifungal activity against B. cinerea and C. albicans with MIC values of 16 and 32 μg/mL, respectively.
从药用植物乌头内生真菌Phomopsis sp. YM 355364的培养液中分离得到3对新的二聚体苯酞（±）-phomophthalides A-C（±）-1-3)和8个已知化合物（4-11）。通过NMR、HRESI-MS分析和DP4+计算确定了新化合物的化学结构。用微量肉汤稀释法测定了新化合物的抑菌活性。化合物1对茄灰镰刀菌、白色念珠菌和灰霉病菌具有中等抑制活性，MIC值分别为16、32和32 μg/mL。化合物2对灰绿芽孢杆菌和白色念珠菌的MIC值分别为16和32 μg/mL。
{"title":"Dimeric Phthalides from an endophytic fungus Phomopsis sp. of Aconitum carmichaeli","authors":"Yuan Gao , Jia-Hui Wang , Ming-Qian Han , Rong Huang , Shao-Hua Wu","doi":"10.1016/j.fitote.2025.107035","DOIUrl":"10.1016/j.fitote.2025.107035","url":null,"abstract":"<div><div>Three racemic pairs of new dimeric phthalides, (±)-phomophthalides A-C ((±)-<strong>1–3</strong>), together with eight known compounds (<strong>4–11</strong>), were obtained from the culture broth of the endophytic fungus <em>Phomopsis</em> sp. YM 355364 isolated from the medicinal plant <em>Aconitum carmichaeli</em>. The chemical structures of the new compounds were established by extensive NMR spectroscopic and HRESI-MS analysis and DP4+ calculations. The new compounds were tested for their antimicrobial activities by broth microdilution method. Compound <strong>1</strong> showed moderate inhibitory activity toward three pathogenic fungal strains <em>Fusarium solani</em>, <em>Candida albicans</em>, and <em>Botrytis cinerea</em> with MIC values of 16, 32, and 32 μg/mL, respectively. Compound <strong>2</strong> exhibited antifungal activity against <em>B. cinerea</em> and <em>C. albicans</em> with MIC values of 16 and 32 μg/mL, respectively.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107035"},"PeriodicalIF":2.6,"publicationDate":"2025-12-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145741789","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 : 2025-12-09DOI: 10.1016/j.fitote.2025.107034
Chunhong Liu , Zheng Yan , Xueqiang Chen , Sanchita Mandal , Ushasi Das , Sudarshan Singh , Opeyemi Joshua Olatunji
Stilbenoids are naturally existing phenolic chemicals that have a stilbene backbone structure and are found in a variety of plant species. Plants produce these antimicrobial substances, known as phytoalexins, in reaction to stresses such as disease or ultraviolet light. The structure, variety, isomer form, and biosynthesis of stilbenoids are important characteristics. In addition to their anti-inflammatory and anti-diabetic qualities, they also exhibit antibacterial activity, cardioprotective and neuroprotective benefits, and the ability to prevent and treat cancer. The most researched stilbenoid is resveratrol, although related substances such as piceatannol, gnetol, and pterostilbene also have notable bioactivity. In vitro, in vivo, and a few human clinical investigations have all been done on stilbenoids. Although preclinical models show promising results, further clinical data is required to validate their good benefits in people. To completely grasp their therapeutic potential, more investigation is required. This article explores naturally occurring stilbenoids and their therapeutic properties, including preclinical and clinical research, patents, and emerging research. It highlights their abundance, structural traits, bioavailability, safety, and effectiveness. This article also focus on polymeric carriers, such as nanoparticles, micelles, hydrogels, and dendrimers, improve the stability, bioavailability, and therapeutic efficacy of stilbenoids, polyphenolic compounds with multifaceted therapeutic applicationssuch as antioxidant, anti-inflammatory, anti-aging, cardioprotective, anti-diabetes, neurodegeneration, anti-obesity, anticancer, and antimicrobial properties.
{"title":"Pharmacological insights on multifaceted therapeutic applications of stilbenoids: A comprehensive updates","authors":"Chunhong Liu , Zheng Yan , Xueqiang Chen , Sanchita Mandal , Ushasi Das , Sudarshan Singh , Opeyemi Joshua Olatunji","doi":"10.1016/j.fitote.2025.107034","DOIUrl":"10.1016/j.fitote.2025.107034","url":null,"abstract":"<div><div>Stilbenoids are naturally existing phenolic chemicals that have a stilbene backbone structure and are found in a variety of plant species. Plants produce these antimicrobial substances, known as phytoalexins, in reaction to stresses such as disease or ultraviolet light. The structure, variety, isomer form, and biosynthesis of stilbenoids are important characteristics. In addition to their anti-inflammatory and anti-diabetic qualities, they also exhibit antibacterial activity, cardioprotective and neuroprotective benefits, and the ability to prevent and treat cancer. The most researched stilbenoid is resveratrol, although related substances such as piceatannol, gnetol, and pterostilbene also have notable bioactivity. <em>In vitro</em>, <em>in vivo</em>, and a few human clinical investigations have all been done on stilbenoids. Although preclinical models show promising results, further clinical data is required to validate their good benefits in people. To completely grasp their therapeutic potential, more investigation is required. This article explores naturally occurring stilbenoids and their therapeutic properties, including preclinical and clinical research, patents, and emerging research. It highlights their abundance, structural traits, bioavailability, safety, and effectiveness. This article also focus on polymeric carriers, such as nanoparticles, micelles, hydrogels, and dendrimers, improve the stability, bioavailability, and therapeutic efficacy of stilbenoids, polyphenolic compounds with multifaceted therapeutic applicationssuch as antioxidant, anti-inflammatory, anti-aging, cardioprotective, anti-diabetes, neurodegeneration, anti-obesity, anticancer, and antimicrobial properties.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107034"},"PeriodicalIF":2.6,"publicationDate":"2025-12-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145741775","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 : 2025-12-08DOI: 10.1016/j.fitote.2025.107030
Chenglin Chi, Xiaoli Yang, Can Li, Zongchao Li, Shufang Yang, Yuan Du, Weizhen Huang, Rongxia Liu
The Tetradium ruticarpum (E)–Zingiber officinale Roscoe (Z) herb pair is a well-known herbal formulation with multiple beneficial cardiovascular pharmacological activities. Therefore, E and Z are potentially natural products for Atherosclerosis (AS). However, it is not clear whether E and Z work synergistically in the treatment of AS and which of their components is responsible. This study was to determine the synergistic effect of E and Z in the treatment of AS, to identify the active ingredient combination (AIC) that exerts the action of the original formula and to determine its molecular mechanism. First, the combined effects of E and Z were assessed in an ApoE−/− mouse model and then confirmed in vascular smooth muscle cells (VSMCs) by the combination index (CI). In addition, the AIC of E-Z was evaluated by cascade analysis and its efficacy was confirmed in vitro and in vivo. The results showed that both E, Z and E-Z had anti-AS effects in ApoE−/− mice, with E-Z having the most significant effect. Moreover, the CI method demonstrated that E, Z could synergistically inhibit the proliferation of VSMCs. In addition, the AICs obtained by the cascade analysis strategy effectively inhibited VSMCs proliferation in vitro and significantly reduced the formation of neoplastic endothelium in mice in vivo. This inhibitory effect was associated with the reduction of ROS levels and activation of the Nrf2/HO-1 signaling pathway in VSMCs. This study provides an effective method for characterizing herbal combinations, exploring their active ingredients, and promoting efficacy-based herbal quality control.
{"title":"The Tetradium ruticarpum–Zingiber officinale Roscoe herb pair inhibits atherogenic events: A study of the synergistic effects and active ingredient combination of a two-herb formula","authors":"Chenglin Chi, Xiaoli Yang, Can Li, Zongchao Li, Shufang Yang, Yuan Du, Weizhen Huang, Rongxia Liu","doi":"10.1016/j.fitote.2025.107030","DOIUrl":"10.1016/j.fitote.2025.107030","url":null,"abstract":"<div><div>The <em>Tetradium ruticarpum</em> (E)–<em>Zingiber officinale Roscoe</em> (Z) herb pair is a well-known herbal formulation with multiple beneficial cardiovascular pharmacological activities. Therefore, E and Z are potentially natural products for Atherosclerosis (AS). However, it is not clear whether E and Z work synergistically in the treatment of AS and which of their components is responsible. This study was to determine the synergistic effect of E and Z in the treatment of AS, to identify the active ingredient combination (AIC) that exerts the action of the original formula and to determine its molecular mechanism. First, the combined effects of E and Z were assessed in an ApoE<sup>−/−</sup> mouse model and then confirmed in vascular smooth muscle cells (VSMCs) by the combination index (CI). In addition, the AIC of <em>E</em>-Z was evaluated by cascade analysis and its efficacy was confirmed in vitro and in vivo. The results showed that both E, Z and <em>E</em>-Z had anti-AS effects in ApoE<sup>−/−</sup> mice, with E-Z having the most significant effect. Moreover, the CI method demonstrated that E, Z could synergistically inhibit the proliferation of VSMCs. In addition, the AICs obtained by the cascade analysis strategy effectively inhibited VSMCs proliferation in vitro and significantly reduced the formation of neoplastic endothelium in mice in vivo. This inhibitory effect was associated with the reduction of ROS levels and activation of the Nrf2/HO-1 signaling pathway in VSMCs. This study provides an effective method for characterizing herbal combinations, exploring their active ingredients, and promoting efficacy-based herbal quality control.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107030"},"PeriodicalIF":2.6,"publicationDate":"2025-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145721972","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 : 2025-12-08DOI: 10.1016/j.fitote.2025.107031
Lucas Silva Tironi , Johan Mateo Rios Marin , Omar Cabezas Gómez , Antonio Gilberto Ferreira , Jan Schripsema , Jaine Honorata Hortolan Luiz
Endophytic fungi are well known for producing a wide variety of specialized metabolites, often characterized by complex and diverse chemical structures. In this study, the differential 1H NMR technique was used as an innovative tool for dereplication and for supporting compound identification in complex mixtures, complemented by similarity calculations developed to evaluate the similarity of the chemical profiles of the extracts obtained over consecutive cultivation days of Lasiodiplodia sp. One-dimensional (1D) and two-dimensional (2D) NMR analyses of the POLd-14 extract and MLd-1 to MLd-3 subfractions led to the identification of known compounds: 3-carboxy-2-methylene-4-heptanolide (1) and decumbic acid (2) in POLd-14; indole-3-carboxylic acid (3) in MLd-1 and MLd-3; 4-hydroxybenzoic acid (4) and 4-hydroxymellein (5) in MLd-1; and 4-hydroxyphenylacetamide (6) in MLd-2. Differential 1H NMR enabled the unequivocal identification of compounds (1) and (2). These results contribute to bioprospecting and to a better understanding of the metabolite diversity of Lasiodiplodia sp. under varying culture conditions, including diferences in carbon and nitrogen sources, cultivation periods, and extraction methods. The study also underscore the potential of Lasiodiplodia sp. endophyte as an alternative source of bioactive metabolites with pharmacological relevance, which can be cultivated under different conditions guiding the production of different specialized metabolites.
{"title":"Bioprospecting and exploration of the chemical profile of Lasiodiplodia sp. extracts: Evaluation of specialized metabolites by similarity calculations, and dereplication with differential 1H NMR","authors":"Lucas Silva Tironi , Johan Mateo Rios Marin , Omar Cabezas Gómez , Antonio Gilberto Ferreira , Jan Schripsema , Jaine Honorata Hortolan Luiz","doi":"10.1016/j.fitote.2025.107031","DOIUrl":"10.1016/j.fitote.2025.107031","url":null,"abstract":"<div><div>Endophytic fungi are well known for producing a wide variety of specialized metabolites, often characterized by complex and diverse chemical structures. In this study, the differential <sup>1</sup>H NMR technique was used as an innovative tool for dereplication and for supporting compound identification in complex mixtures, complemented by similarity calculations developed to evaluate the similarity of the chemical profiles of the extracts obtained over consecutive cultivation days of <em>Lasiodiplodia</em> sp. One-dimensional (1D) and two-dimensional (2D) NMR analyses of the POLd-14 extract and MLd-1 to MLd-3 subfractions led to the identification of known compounds: 3-carboxy-2-methylene-4-heptanolide (<strong>1</strong>) and decumbic acid (<strong>2</strong>) in POLd-14; indole-3-carboxylic acid (<strong>3</strong>) in MLd-1 and MLd-3; 4-hydroxybenzoic acid (<strong>4</strong>) and 4-hydroxymellein (<strong>5</strong>) in MLd-1; and 4-hydroxyphenylacetamide (<strong>6</strong>) in MLd-2. Differential <sup>1</sup>H NMR enabled the unequivocal identification of compounds (<strong>1</strong>) and (<strong>2</strong>). These results contribute to bioprospecting and to a better understanding of the metabolite diversity of <em>Lasiodiplodia</em> sp. under varying culture conditions, including diferences in carbon and nitrogen sources, cultivation periods, and extraction methods. The study also underscore the potential of <em>Lasiodiplodia</em> sp. endophyte as an alternative source of bioactive metabolites with pharmacological relevance, which can be cultivated under different conditions guiding the production of different specialized metabolites.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107031"},"PeriodicalIF":2.6,"publicationDate":"2025-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145721895","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 : 2025-12-08DOI: 10.1016/j.fitote.2025.107025
Sandeep Palakkil Mavilavalappil , Shabeer Ali Hassan Muhammed , Sandhya Mohan , M. Divya Lakshmanan , Toine F. Bovee , K. Sreejith
We could successfully reverse the polycystic ovary syndrome (PCOS) in a rat model using an anti-androgenic compound extracted from Embelia tsjeriam–cottam, which exhibited spectral characteristics consistent with Embelin. The identity of the anti-androgenic fraction was confirmed as Embelin using FT-IR, UV spectrophotometry, and UPLC-MS/MS analyses. The anti-androgenic activity of the extracted Embelin was evaluated using the Yeast RIKILT Androgen Assay and compared against (i) 5α-dihydrotestosterone (5α-DHT), (ii) a commercially sourced Embelin standard, and (iii) flutamide, a known androgen receptor antagonist. In silico molecular docking studies further revealed that Embelin exerts its anti-androgenic effects by competitively binding to the ligand-binding domain of the androgen receptor (AR), with interaction energy values comparable to those of 5α-DHT and hydroxyflutamide. The embelin fraction (up to 100 μl) and in combination with 5α-DHT, was non-toxic and promoted normal cell proliferation in vitro. Further, the extract also efficiently scavenged the 5α-DHT-induced Reactive Oxygen Species generation and downregulated the 5α-DHT-induced androgen receptor (AR) expression significantly in the in vitro system. A PCOS rat model was successfully established through 5α-DHT induction. Embelin treatment effectively reversed several hallmark features of PCOS, including ovarian dysfunction (e.g., hypo-progesteronemia, follicular cysts, and estrous cycle irregularities) as well as metabolic disturbances such as insulin resistance, weight gain, dyslipidaemia, and adipocyte hypertrophy. In conclusion, this is the first study to demonstrate the therapeutic potential of Embelin in ameliorating PCOS-related ovarian and metabolic dysfunctions.
{"title":"Anti-androgenic compound Embelin ameliorates polycystic ovary syndrome by reversing the ovarian dysfunction and associated metabolic irregularities in 5α-DHT-induced PCOS rats","authors":"Sandeep Palakkil Mavilavalappil , Shabeer Ali Hassan Muhammed , Sandhya Mohan , M. Divya Lakshmanan , Toine F. Bovee , K. Sreejith","doi":"10.1016/j.fitote.2025.107025","DOIUrl":"10.1016/j.fitote.2025.107025","url":null,"abstract":"<div><div>We could successfully reverse the polycystic ovary syndrome (PCOS) in a rat model using an anti-androgenic compound extracted from <em>Embelia tsjeriam–cottam</em>, which exhibited spectral characteristics consistent with Embelin. The identity of the anti-androgenic fraction was confirmed as Embelin using FT-IR, UV spectrophotometry, and UPLC-MS/MS analyses. The anti-androgenic activity of the extracted Embelin was evaluated using the Yeast RIKILT Androgen Assay and compared against (i) 5α-dihydrotestosterone (5α-DHT), (ii) a commercially sourced Embelin standard, and (iii) flutamide, a known androgen receptor antagonist. <em>In silico</em> molecular docking studies further revealed that Embelin exerts its anti-androgenic effects by competitively binding to the ligand-binding domain of the androgen receptor (AR), with interaction energy values comparable to those of 5α-DHT and hydroxyflutamide. The embelin fraction (up to 100 μl) and in combination with 5α-DHT, was non-toxic and promoted normal cell proliferation <em>in vitro</em>. Further, the extract also efficiently scavenged the 5α-DHT-induced Reactive Oxygen Species generation and downregulated the 5α-DHT-induced androgen receptor (AR) expression significantly in the <em>in vitro</em> system. A PCOS rat model was successfully established through 5α-DHT induction. Embelin treatment effectively reversed several hallmark features of PCOS, including ovarian dysfunction (<em>e.g.</em>, hypo-progesteronemia, follicular cysts, and estrous cycle irregularities) as well as metabolic disturbances such as insulin resistance, weight gain, dyslipidaemia, and adipocyte hypertrophy. In conclusion, this is the first study to demonstrate the therapeutic potential of Embelin in ameliorating PCOS-related ovarian and metabolic dysfunctions.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107025"},"PeriodicalIF":2.6,"publicationDate":"2025-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145721898","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 : 2025-12-08DOI: 10.1016/j.fitote.2025.107027
Tran Hong Quang , Pham Thi Cham , Tran Thi Hong Hanh , Dang Viet Anh , Nguyen Hoang Nam , Nguyen Quoc Vuong , Nguyen Thi Thanh Ngan
Polygala paniculata L. has been reported to exhibit diverse therapeutic effects, including neuroprotective, gastroprotective, antinociceptive, antidepressant, vasorelaxant, and hypotensive effects, as well as traditional uses in treating stomachache, rheumatic pain, rhinitis, and chronic bronchitis. Using multiple chromatographic techniques, 10 oligosaccharide esters were isolated from the whole plants of P. paniculata, comprising seven new compounds, polypanicoses A-G (1–7), one new natural product, 3′-O-benzoylsucrose (8), and two known ones, senegose F (9) and tenuifoliside A (10). Their structures were elucidated through comprehensive spectroscopic methods, including NMR and HRESI mass spectra. Compounds 1–6, 8, and 9 inhibited nitric oxide (NO) overproduction in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages, with IC50 values ranging from 44.6 ± 1.0 to 99.6 ± 8.3 μM. Molecular docking simulations suggested that 1 and 4 inhibit NO overproduction by binding to the active site of iNOS, thereby modulates the protein's activity. Both 1 and 4 further attenuated iNOS expression, suggesting that their NO inhibitory activity is associated with down-regulation of iNOS expression.
{"title":"Oligosaccharide esters from Polygala paniculata with their NO inhibitory activity","authors":"Tran Hong Quang , Pham Thi Cham , Tran Thi Hong Hanh , Dang Viet Anh , Nguyen Hoang Nam , Nguyen Quoc Vuong , Nguyen Thi Thanh Ngan","doi":"10.1016/j.fitote.2025.107027","DOIUrl":"10.1016/j.fitote.2025.107027","url":null,"abstract":"<div><div><em>Polygala paniculata</em> L. has been reported to exhibit diverse therapeutic effects, including neuroprotective, gastroprotective, antinociceptive, antidepressant, vasorelaxant, and hypotensive effects, as well as traditional uses in treating stomachache, rheumatic pain, rhinitis, and chronic bronchitis. Using multiple chromatographic techniques, 10 oligosaccharide esters were isolated from the whole plants of <em>P. paniculata</em>, comprising seven new compounds, polypanicoses A<strong>-</strong>G (<strong>1–7</strong>), one new natural product, 3′-<em>O</em>-benzoylsucrose (<strong>8</strong>), and two known ones, senegose F (<strong>9</strong>) and tenuifoliside A (<strong>10</strong>). Their structures were elucidated through comprehensive spectroscopic methods, including NMR and HRESI mass spectra. Compounds <strong>1–6</strong>, <strong>8</strong>, and <strong>9</strong> inhibited nitric oxide (NO) overproduction in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages, with IC<sub>50</sub> values ranging from 44.6 ± 1.0 to 99.6 ± 8.3 μM. Molecular docking simulations suggested that <strong>1</strong> and <strong>4</strong> inhibit NO overproduction by binding to the active site of iNOS, thereby modulates the protein's activity. Both <strong>1</strong> and <strong>4</strong> further attenuated iNOS expression, suggesting that their NO inhibitory activity is associated with down-regulation of iNOS expression.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107027"},"PeriodicalIF":2.6,"publicationDate":"2025-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145721978","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}
Calystegia japonica Choisy (Convolvulaceae) is a perennial herbaceous vine widely distributed throughout southeastern and eastern Asia. In traditional Chinese medicine, the whole parts of C. japonica have been used for their diuretic and tonic properties. In this study, four new resin glycosides, designated calyjaponins I (1)–IV (4), were isolated from the aerial parts of C. japonica. Their structures were elucidated on the basis of spectroscopic data and chemical analyses. All compounds possessed new glycosidic acid moieties and were identified as hexaglycosides featuring intramolecular cyclic ester (jalapin-type) structures, in which the sugar moieties were partially acylated with organic acids, including (E)-2-methylbut-2-enoic and 2R-methyl-3R-hydroxybutyric acids. Compounds 1–4 were further evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and for cytotoxicity against HL-60 human promyelocytic leukemia cells. All tested compounds exhibited both anti-HSV-1 and cytotoxic activities.
卷花科（Calystegia japonica Choisy）是一种多年生草本藤本植物，广泛分布于东南亚和东亚。在传统中医，全部分的日本菊已被用于其利尿和滋补性质。本研究从粳稻的地上部分分离到4个新的树脂苷，命名为calyjaponins I (1)-IV(4)。根据光谱数据和化学分析对其结构进行了鉴定。所有化合物都含有新的糖苷酸片段，并被鉴定为具有分子内环酯（jalapin-type）结构的六糖苷，其中糖部分与有机酸(E)-2-甲基丁-2-烯酸和2r -甲基- 3r -羟基丁酸)部分酰化。化合物1-4对1型单纯疱疹病毒（HSV-1）的抗病毒活性和对HL-60人早幼粒细胞白血病细胞的细胞毒性进行了进一步评价。所有化合物均表现出抗hsv -1和细胞毒活性。
{"title":"Four new resin glycosides, calyjaponins I–IV, from the aerial parts of Calystegia japonica","authors":"Masateru Ono , Nozomi Shimada , Nanami Ogura , Hirotaka Nishikawa , Shin Yasuda , Hiroyuki Miyashita , Kazumi Yokomizo , Ryota Tsuchihashi , Masafumi Okawa","doi":"10.1016/j.fitote.2025.107009","DOIUrl":"10.1016/j.fitote.2025.107009","url":null,"abstract":"<div><div><em>Calystegia japonica</em> Choisy (Convolvulaceae) is a perennial herbaceous vine widely distributed throughout southeastern and eastern Asia. In traditional Chinese medicine, the whole parts of <em>C. japonica</em> have been used for their diuretic and tonic properties. In this study, four new resin glycosides, designated calyjaponins I (<strong>1</strong>)–IV (<strong>4</strong>), were isolated from the aerial parts of <em>C. japonica</em>. Their structures were elucidated on the basis of spectroscopic data and chemical analyses. All compounds possessed new glycosidic acid moieties and were identified as hexaglycosides featuring intramolecular cyclic ester (jalapin-type) structures, in which the sugar moieties were partially acylated with organic acids, including (<em>E</em>)-2-methylbut-2-enoic and 2<em>R</em>-methyl-3<em>R</em>-hydroxybutyric acids. Compounds <strong>1</strong>–<strong>4</strong> were further evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and for cytotoxicity against HL-60 human promyelocytic leukemia cells. All tested compounds exhibited both anti-HSV-1 and cytotoxic activities.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107009"},"PeriodicalIF":2.6,"publicationDate":"2025-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145713865","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 : 2025-12-07DOI: 10.1016/j.fitote.2025.107022
Trang Thi Minh Nguyen , Eun-Ji Yi , Xiangji Jin , Qiwen Zheng , Se-Jig Park , Gyeong-Seon Yi , Su-Jin Yang , Tae-Hoo Yi
Acne vulgaris is a prevalent inflammatory skin disorder influenced by sebaceous gland activity, hormonal regulation, and microbial proliferation. Dietary factors, including sweetening agents, may modulate acne pathophysiology, affecting sebum production, inflammatory responses, and the skin microbiome. This systematic review summarizes the effects of nutritive and non-nutritive sweeteners on acne-related markers, with a focus on Cutibacterium acnes activity and associated inflammatory pathways. Non-nutritive sweeteners such as mannitol and xylitol show potential in regulating acne pathogenesis and exhibiting antibacterial activity against C. acnes. Strategic combinations of sweeteners with bioactive compounds, such as mannitol with bakuchiol or Ginkgo biloba extract, and xylitol with propanediol and caprylic acid, further enhance anti-inflammatory and antimicrobial effects, offering a multifaceted approach to acne management. For nutritive sweeteners, experimental evidence suggests that glucose may enhance C. acnes biofilm susceptibility when combined with certain antibiotics. These findings emphasize the importance of careful selection and formulation of sweetening agents in dermatological interventions. Incorporating sweeteners, alone or in combination with bioactive compounds, could complement conventional acne therapies, reduce microbial proliferation, modulate inflammatory pathways, and support overall skin health. This review provides a scientific basis for dietary recommendations and the development of adjunctive acne treatments, highlighting sweetening agents as emerging functional modulators of acne pathogenesis.
{"title":"Effects of nutritive and non-nutritive sweeteners on acne vulgaris: A systematic review","authors":"Trang Thi Minh Nguyen , Eun-Ji Yi , Xiangji Jin , Qiwen Zheng , Se-Jig Park , Gyeong-Seon Yi , Su-Jin Yang , Tae-Hoo Yi","doi":"10.1016/j.fitote.2025.107022","DOIUrl":"10.1016/j.fitote.2025.107022","url":null,"abstract":"<div><div>Acne vulgaris is a prevalent inflammatory skin disorder influenced by sebaceous gland activity, hormonal regulation, and microbial proliferation. Dietary factors, including sweetening agents, may modulate acne pathophysiology, affecting sebum production, inflammatory responses, and the skin microbiome. This systematic review summarizes the effects of nutritive and non-nutritive sweeteners on acne-related markers, with a focus on <em>Cutibacterium acnes</em> activity and associated inflammatory pathways. Non-nutritive sweeteners such as mannitol and xylitol show potential in regulating acne pathogenesis and exhibiting antibacterial activity against <em>C. acnes</em>. Strategic combinations of sweeteners with bioactive compounds, such as mannitol with bakuchiol or <em>Ginkgo biloba</em> extract, and xylitol with propanediol and caprylic acid, further enhance anti-inflammatory and antimicrobial effects, offering a multifaceted approach to acne management. For nutritive sweeteners, experimental evidence suggests that glucose may enhance <em>C. acnes</em> biofilm susceptibility when combined with certain antibiotics. These findings emphasize the importance of careful selection and formulation of sweetening agents in dermatological interventions. Incorporating sweeteners, alone or in combination with bioactive compounds, could complement conventional acne therapies, reduce microbial proliferation, modulate inflammatory pathways, and support overall skin health. This review provides a scientific basis for dietary recommendations and the development of adjunctive acne treatments, highlighting sweetening agents as emerging functional modulators of acne pathogenesis.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107022"},"PeriodicalIF":2.6,"publicationDate":"2025-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145713834","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 : 2025-12-07DOI: 10.1016/j.fitote.2025.107026
Jianglong Li , Xueqian Wu , Zhenqiang Wang , Yifan Yang , Yuanyuan Wang , Ping Chen , Mei Zhang , Yuwei Bai , Yanbin Shi , Zhigang Yang
To investigate the blood-replenishing constituents from the roots of Angelica sinensis (Oliv.) Diels. The components were separated and purified by various chromatographic methods, and identified by physicochemical characterization and spectral data. The nitric oxide (NO) inhibition rate and mRNA expression of IL-6, IL-1β, TNF-α in LPS-induced RAW264.7 were detected by Griess method and RT-qPCR assays, respectively. The hemoglobin expression promotion rate in K562 cells was evaluated by benzidine staining method. Three new phthalide compounds (1–3), named as 7-(2-butyrylbenzoyl)senkyunolide I, 2-propyl-6,7-dioxolanesenkyunolide H, 6′,7′-dicarboxyl-wallichilide, were isolated from root of A. sinensis together with 45 known compounds (4–48). Among them, the IC50 values for NO inhibition of 7-(2-butyrylbenzoyl)senkyunolide I (1), 7-acetylsenkyunolide H (5), angeolide (25), ligustchuane B (33) and dibutyl phthalate (36) were 3.43 μM, 3.77 μM, 3.92 μM, 3.23 μM and 3.93 μM, respectively. Ferulic acid (28), 4,8-dihydroxyacetophenone (38) and vanillic acid (48) showed good hemoglobin-promoting effects, with the promotion rate of 40.6 %, 33.4 %, and 37.8 %, respectively. Thus, A. sinensis exhibited the blood-replenishing bioactivities through a synergistic effect with phthalide and ferulic acid derivatives.
{"title":"Phthalide compounds from the roots of Angelica sinensis and their blood-replenishing bioactivities","authors":"Jianglong Li , Xueqian Wu , Zhenqiang Wang , Yifan Yang , Yuanyuan Wang , Ping Chen , Mei Zhang , Yuwei Bai , Yanbin Shi , Zhigang Yang","doi":"10.1016/j.fitote.2025.107026","DOIUrl":"10.1016/j.fitote.2025.107026","url":null,"abstract":"<div><div>To investigate the blood-replenishing constituents from the roots of <em>Angelica sinensis</em> (Oliv.) Diels<em>.</em> The components were separated and purified by various chromatographic methods, and identified by physicochemical characterization and spectral data. The nitric oxide (NO) inhibition rate and mRNA expression of IL-6, IL-1β, TNF-α in LPS-induced RAW264.7 were detected by Griess method and RT-qPCR assays, respectively. The hemoglobin expression promotion rate in K562 cells was evaluated by benzidine staining method. Three new phthalide compounds (<strong>1</strong>–<strong>3</strong>), named as 7-(2-butyrylbenzoyl)senkyunolide I, 2-propyl-6,7-dioxolanesenkyunolide H, 6′,7′-dicarboxyl-wallichilide, were isolated from root of <em>A. sinensis</em> together with 45 known compounds (<strong>4</strong>–<strong>48</strong>). Among them, the IC<sub>50</sub> values for NO inhibition of 7-(2-butyrylbenzoyl)senkyunolide I (<strong>1</strong>), 7-acetylsenkyunolide H (<strong>5</strong>), angeolide (<strong>25</strong>), ligustchuane B (<strong>33</strong>) and dibutyl phthalate (<strong>36</strong>) were 3.43 μM, 3.77 μM, 3.92 μM, 3.23 μM and 3.93 μM, respectively. Ferulic acid (<strong>28</strong>), 4,8-dihydroxyacetophenone (<strong>38</strong>) and vanillic acid (<strong>48</strong>) showed good hemoglobin-promoting effects, with the promotion rate of 40.6 %, 33.4 %, and 37.8 %, respectively. Thus, <em>A. sinensis</em> exhibited the blood-replenishing bioactivities through a synergistic effect with phthalide and ferulic acid derivatives.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107026"},"PeriodicalIF":2.6,"publicationDate":"2025-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145713825","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 : 2025-12-06DOI: 10.1016/j.fitote.2025.107020
Zhichao Liu , Shixiang Chen , Huanjie Fu , Kuicheng Li , Hao Liu , Limin Qin , Lijuan Wang , Juan Jin , Luchang Yin , Jinhong Chen
Myocardial infarction (MI) is a multifactorial cardiovascular condition characterized by metabolic disturbances and inflammatory responses. QiShenYiQi dropping pills (QSYQ), a traditional Chinese medicine formula, have shown therapeutic potential through multi-component and multi-target mechanisms, yet their effects from the perspective of active compounds and metabolites remain underexplored. This study utilized phytochemical characterization, metabolomics, network pharmacology, molecular docking, and biological validation to investigate QSYQ's pharmacological mechanisms in MI treatment. Chemical constituents were identified via UHPLC-Q-Orbitrap HRMS, and plasma metabolites from MI rats were analyzed using UPLC–MS/MS. Network pharmacology and docking revealed 19 active components, 68 target proteins, and key pathways, including cAMP-Rap1 and PI3K-Akt, associated with QSYQ's effects. Experimental validation demonstrated that QSYQ significantly improved cardiac function, reduced myocardial fibrosis, and modulated key pathway proteins, including Cyclin D1. A two-week regimen proved more effective than one week. Enrichment analysis highlighted QSYQ's role in regulating cell proliferation and survival, supported by changes in 45 plasma metabolites. Molecular docking confirmed interactions between active components and targets, and biological validation reinforced the importance of cAMP-Rap1 and PI3K-Akt pathways. This study provides a systematic framework for understanding the therapeutic mechanisms of QSYQ, emphasizing its potential in addressing cardiac dysfunction and myocardial fibrosis in MI.
{"title":"QiShenYiQi dripping pills ameliorate post-myocardial infarction cardiac fibrosis via modulation of the cAMP/Rap1 and PI3K/Akt signaling pathways","authors":"Zhichao Liu , Shixiang Chen , Huanjie Fu , Kuicheng Li , Hao Liu , Limin Qin , Lijuan Wang , Juan Jin , Luchang Yin , Jinhong Chen","doi":"10.1016/j.fitote.2025.107020","DOIUrl":"10.1016/j.fitote.2025.107020","url":null,"abstract":"<div><div>Myocardial infarction (MI) is a multifactorial cardiovascular condition characterized by metabolic disturbances and inflammatory responses. QiShenYiQi dropping pills (QSYQ), a traditional Chinese medicine formula, have shown therapeutic potential through multi-component and multi-target mechanisms, yet their effects from the perspective of active compounds and metabolites remain underexplored. This study utilized phytochemical characterization, metabolomics, network pharmacology, molecular docking, and biological validation to investigate QSYQ's pharmacological mechanisms in MI treatment. Chemical constituents were identified via UHPLC-Q-Orbitrap HRMS, and plasma metabolites from MI rats were analyzed using UPLC–MS/MS. Network pharmacology and docking revealed 19 active components, 68 target proteins, and key pathways, including cAMP-Rap1 and PI3K-Akt, associated with QSYQ's effects. Experimental validation demonstrated that QSYQ significantly improved cardiac function, reduced myocardial fibrosis, and modulated key pathway proteins, including Cyclin D1. A two-week regimen proved more effective than one week. Enrichment analysis highlighted QSYQ's role in regulating cell proliferation and survival, supported by changes in 45 plasma metabolites. Molecular docking confirmed interactions between active components and targets, and biological validation reinforced the importance of cAMP-Rap1 and PI3K-Akt pathways. This study provides a systematic framework for understanding the therapeutic mechanisms of QSYQ, emphasizing its potential in addressing cardiac dysfunction and myocardial fibrosis in MI.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107020"},"PeriodicalIF":2.6,"publicationDate":"2025-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145707816","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}
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