Pub Date : 2025-04-23DOI: 10.1016/j.fitote.2025.106566
Yun Wang , Xin-Yu Li , Sheng-Li Wu , Pianchou Gongpan , Yi Yang , Mei Huang , Da-Hong Li , Chang-An Geng
Thirteen diarylheptanoids, including four undescribed ones (1–4), were isolated from the leaves of Amomum tsao-ko. Compounds 1 and 2 are two unusual diarylheptanoid-phenylpropanoid hybrids. Several of the isolates were tested for their biological activity in promoting GLP-1 secretion and inhibiting multiple type 2 diabetes-related enzymes. 2-Hydroxymusaitinerin A (1) demonstrated broad inhibitory activity against GPa, PTP1B and α-glucosidase with inhibition rates of 99.0 %, 59.4 % and 55.9 %, respectively at 200 μM. Platyphyllone (12) is a mixed-type inhibitor of α-glucosidase (IC50 = 25.8 μM), inhibiting the enzyme through both non-competitive and anti-competitive modes, as shown by enzyme kinetic study. Fluorescence quenching test confirmed that compound 12 directly interacted with α-glucosidase, forming a basal complex via a single binding site. Molecular docking predicted hydrogen-bonding interactions between OH-4′′, OH-5 and 3‑carbonyl groups of 12 and α-glucosidase. This study highlights that the leaves of Amomum tsao-ko are a rich source of diarylheptanoids with multi-enzyme inhibitory effects.
{"title":"Antidiabetic diarylheptanoids from the leaves of Amomum tsao-ko and their inhibition mechanism against α-glucosidase","authors":"Yun Wang , Xin-Yu Li , Sheng-Li Wu , Pianchou Gongpan , Yi Yang , Mei Huang , Da-Hong Li , Chang-An Geng","doi":"10.1016/j.fitote.2025.106566","DOIUrl":"10.1016/j.fitote.2025.106566","url":null,"abstract":"<div><div>Thirteen diarylheptanoids, including four undescribed ones (<strong>1–4</strong>), were isolated from the leaves of <em>Amomum tsao-ko</em>. Compounds <strong>1</strong> and <strong>2</strong> are two unusual diarylheptanoid-phenylpropanoid hybrids. Several of the isolates were tested for their biological activity in promoting GLP-1 secretion and inhibiting multiple type 2 diabetes-related enzymes. 2-Hydroxymusaitinerin A (<strong>1</strong>) demonstrated broad inhibitory activity against GPa, PTP1B and <em>α</em>-glucosidase with inhibition rates of 99.0 %, 59.4 % and 55.9 %, respectively at 200 μM. Platyphyllone (<strong>12</strong>) is a mixed-type inhibitor of <em>α</em>-glucosidase (IC<sub>50</sub> = 25.8 μM), inhibiting the enzyme through both non-competitive and anti-competitive modes, as shown by enzyme kinetic study. Fluorescence quenching test confirmed that compound <strong>12</strong> directly interacted with <em>α</em>-glucosidase, forming a basal complex via a single binding site. Molecular docking predicted hydrogen-bonding interactions between OH-4′′, OH-5 and 3‑carbonyl groups of <strong>12</strong> and <em>α</em>-glucosidase. This study highlights that the leaves of <em>Amomum tsao-ko</em> are a rich source of diarylheptanoids with multi-enzyme inhibitory effects.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106566"},"PeriodicalIF":2.5,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143874780","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 : 2025-04-23DOI: 10.1016/j.fitote.2025.106568
Nurdan Yazici , Kübra Kolci , Rengin Reis , Hasan Kırmızıbekmez , Gülin Renda
Trachystemon orientalis D.Don is a perennial species belonging to the family Boraginaceae. It is predominantly distributed in the northern parts of Türkiye. The stems, roots, and aerial parts of the species are consumed as food and traditionally used in the treatment of various types of cancer. The aim of this study was to evaluate the cytoprotective effects of its extracts and metabolites against cigarette smoke extract (CSE)-induced toxicity on BEAS-2B cells. For the study, T. orientalis roots (A) and aerial parts (B) were extracted separately using 80 % methanol. B exhibited a higher cytoprotective effect than A on the BEAS-2B cell line for 24 h. Therefore, B was partitioned against n-hexane (B1) and n-butanol (B2) to yield sub-extracts. B2 exhibited the lowest cytotoxicity profile among the tested concentrations (0.1–1 mg/mL). Chromatographic separation on B2 led to the isolation of rosmarinic acid (1), kaempferol 3-O-glucoside (astragalin) (2), and kaempferol 7-O-glucoside (3). Notably, compound 2 was isolated for the first time from the genus Trachystemon, while compound 3 was obtained for the first time from the family Boraginaceae. The extract B2 (0.1 mg/mL), and isolated compounds 1 (50 μM), 2 (12.5 μM), and 3 (25 μM) exhibited statistically significant cytoprotective activity against CSE-induced cytotoxicity on human bronchial epithelia in the MTT assay. It is anticipated that these findings will provide valuable insights into the development of plant-based adjuvant therapies for respiratory diseases, with a particular focus on secondary metabolites that are responsible for cytoprotective activity.
{"title":"Cytoprotective Effect of Trachystemon orientalis against cigarette smoke extract- Induced toxicity on human bronchial epithelial cells","authors":"Nurdan Yazici , Kübra Kolci , Rengin Reis , Hasan Kırmızıbekmez , Gülin Renda","doi":"10.1016/j.fitote.2025.106568","DOIUrl":"10.1016/j.fitote.2025.106568","url":null,"abstract":"<div><div><em>Trachystemon orientalis</em> D.Don is a perennial species belonging to the family Boraginaceae. It is predominantly distributed in the northern parts of Türkiye. The stems, roots, and aerial parts of the species are consumed as food and traditionally used in the treatment of various types of cancer. The aim of this study was to evaluate the cytoprotective effects of its extracts and metabolites against cigarette smoke extract (CSE)-induced toxicity on BEAS-2B cells. For the study, <em>T. orientalis</em> roots (<strong>A</strong>) and aerial parts (<strong>B</strong>) were extracted separately using 80 % methanol. <strong>B</strong> exhibited a higher cytoprotective effect than <strong>A</strong> on the BEAS-2B cell line for 24 h. Therefore, <strong>B</strong> was partitioned against <em>n</em>-hexane (<strong>B1</strong>) and <em>n</em>-butanol (<strong>B2</strong>) to yield sub-extracts. <strong>B2</strong> exhibited the lowest cytotoxicity profile among the tested concentrations (0.1–1 mg/mL). Chromatographic separation on <strong>B2</strong> led to the isolation of rosmarinic acid (<strong>1</strong>), kaempferol 3-<em>O</em>-glucoside (astragalin) (<strong>2</strong>), and kaempferol 7-<em>O</em>-glucoside (<strong>3</strong>). Notably, compound <strong>2</strong> was isolated for the first time from the genus <em>Trachystemon</em>, while compound <strong>3</strong> was obtained for the first time from the family Boraginaceae. The extract <strong>B2</strong> (0.1 mg/mL), and isolated compounds <strong>1</strong> (50 μM), <strong>2</strong> (12.5 μM), and <strong>3</strong> (25 μM) exhibited statistically significant cytoprotective activity against CSE-induced cytotoxicity on human bronchial epithelia in the MTT assay. It is anticipated that these findings will provide valuable insights into the development of plant-based adjuvant therapies for respiratory diseases, with a particular focus on secondary metabolites that are responsible for cytoprotective activity.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106568"},"PeriodicalIF":2.5,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143874673","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 : 2025-04-21DOI: 10.1016/j.fitote.2025.106549
Anna Paizanni Guillén , Elihú Bautista , Jesús Morales-Jiménez , David Douterlungne
Aristolochia is a pantropical genus with important pharmacological properties. Despite making up 75 % of the global Aristolochia, the species from the Americas have received comparatively little research attention. Here, we exhaustively review the ethnopharmacology and phytochemistry of Aristolochia species from the Americas, based upon 238 literature references and specimen vouchers of 28 Americas herbaria. The resulting database encompasses 919 records on 95 Aristolochia species with 129 documented traditional medicinal uses. South America and Mexico displayed the highest prevalence of traditional medicinal uses at the regional and national levels, respectively. The most recurrent medicinal uses included treatments against poisonous animals (17.6 %), gastrointestinal diseases (15.1 %), and gynecological diseases (9.89 %). American Aristolochia species produce secondary metabolites such as lignans, diterpenes, sesquiterpenes, isoquinoline and protopine type alkaloids, aristolactams, and aristolochic acids that have been shown to have substantial therapeutic potential. These compounds exhibit various properties, such as neurotrophic effects, inhibition of myotoxicity, anticholinergic and antihistaminic activities, relaxation of the tracheal muscle, as well as antibacterial, antifungal, antiprotozoal activity and, antispasmodic effects. However, in vivo and toxicity tests remain scarce. For example, less than 5 % of the publications focus on isolating aristolochic acids, known for their association with nephropathy and urothelial cancer. We found no instances of hazardous or fatal incidents resulting from traditional uses, despite their known toxicity. This is likely because traditional healers are aware of the hazards and dosage quantities. Finally, we identified crucial future directions for Aristolochia studies based on promising bioprospecting studies; relatively understudied infrageneric groups; poorly known traditional uses, and species-specific chemical compounds without further studies.
{"title":"Aristolochia species (Aristolochiaceae) from the Americas, a review of their traditional medicinal uses, phytochemistry, and pharmacological properties","authors":"Anna Paizanni Guillén , Elihú Bautista , Jesús Morales-Jiménez , David Douterlungne","doi":"10.1016/j.fitote.2025.106549","DOIUrl":"10.1016/j.fitote.2025.106549","url":null,"abstract":"<div><div><em>Aristolochia</em> is a pantropical genus with important pharmacological properties. Despite making up 75 % of the global <em>Aristolochia</em>, the species from the Americas have received comparatively little research attention. Here, we exhaustively review the ethnopharmacology and phytochemistry of <em>Aristolochia</em> species from the Americas, based upon 238 literature references and specimen vouchers of 28 Americas herbaria. The resulting database encompasses 919 records on 95 <em>Aristolochia</em> species with 129 documented traditional medicinal uses. South America and Mexico displayed the highest prevalence of traditional medicinal uses at the regional and national levels, respectively. The most recurrent medicinal uses included treatments against poisonous animals (17.6 %), gastrointestinal diseases (15.1 %), and gynecological diseases (9.89 %). American Aristolochia species produce secondary metabolites such as lignans, diterpenes, sesquiterpenes, isoquinoline and protopine type alkaloids, aristolactams, and aristolochic acids that have been shown to have substantial therapeutic potential. These compounds exhibit various properties, such as neurotrophic effects, inhibition of myotoxicity, anticholinergic and antihistaminic activities, relaxation of the tracheal muscle, as well as antibacterial, antifungal, antiprotozoal activity and, antispasmodic effects. However, <em>in vivo</em> and toxicity tests remain scarce. For example, less than 5 % of the publications focus on isolating aristolochic acids, known for their association with nephropathy and urothelial cancer. We found no instances of hazardous or fatal incidents resulting from traditional uses, despite their known toxicity. This is likely because traditional healers are aware of the hazards and dosage quantities. Finally, we identified crucial future directions for <em>Aristolochia</em> studies based on promising bioprospecting studies; relatively understudied infrageneric groups; poorly known traditional uses, and species-specific chemical compounds without further studies.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106549"},"PeriodicalIF":2.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143874781","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 : 2025-04-21DOI: 10.1016/j.fitote.2025.106553
Chengfeng Gao , Man Zhu , Yang Xu , Yali Wang , Dejuan Sun , Hua Li , Lixia Chen
Research on the aerial parts of Aconitum gymnandrum Maxim. led to identifying three undescribed diterpenoid alkaloids gymnaconitines H-J (1–3), along with eleven known analogues (4–14). Based on 1D/2D NMR and HRESIMS, the structures of these compounds were successfully determined. Additionally, the inhibitory effects of all compounds on NO production were evaluated in lipopolysaccharide-induced RAW264.7 cells. It is noteworthy that compounds 1, 3 and 6 demonstrated significant inhibitory effects, showing IC50 values of 10.36 ± 1.02 μM, 12.87 ± 1.11 μM, and 19.67 ± 1.29 μM, respectively. Using target screening and molecular docking technology, it is hypothesized that compound 1 may play an anti-inflammatory role by combining with Flamin-B.
{"title":"Diterpenoid alkaloids from Aconitum gymnandrum Maxim. and their anti-inflammatory activity","authors":"Chengfeng Gao , Man Zhu , Yang Xu , Yali Wang , Dejuan Sun , Hua Li , Lixia Chen","doi":"10.1016/j.fitote.2025.106553","DOIUrl":"10.1016/j.fitote.2025.106553","url":null,"abstract":"<div><div>Research on the aerial parts of <em>Aconitum gymnandrum</em> Maxim. led to identifying three undescribed diterpenoid alkaloids gymnaconitines H-J (<strong>1</strong>–<strong>3</strong>), along with eleven known analogues (<strong>4</strong>–<strong>14</strong>). Based on 1D/2D NMR and HRESIMS, the structures of these compounds were successfully determined. Additionally, the inhibitory effects of all compounds on NO production were evaluated in lipopolysaccharide-induced RAW264.7 cells. It is noteworthy that compounds <strong>1</strong>, <strong>3</strong> and <strong>6</strong> demonstrated significant inhibitory effects, showing IC<sub>50</sub> values of 10.36 ± 1.02 μM, 12.87 ± 1.11 μM, and 19.67 ± 1.29 μM, respectively. Using target screening and molecular docking technology, it is hypothesized that compound <strong>1</strong> may play an anti-inflammatory role by combining with Flamin-B.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106553"},"PeriodicalIF":2.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143863714","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 : 2025-04-19DOI: 10.1016/j.fitote.2025.106557
Ammara Hakeem , Mohammad Saleem , Rukhsana Anwar , Muhammad Asif , Taha Muhammad , Sherif S. Ebada , Nawal M. Al Musayeib , Mohamed L. Ashour
Traditionally, people use the decoction of Fernandoa adenophylla leaves to treat diabetes mellitus. This study investigated the antidiabetic activity of F. adenophylla methanol extract (Fa.Me) in streptozotocin (STZ)-induced diabetes rats, with metformin as a positive control. We analysed several relevant biomarkers and antioxidant enzymes using ELISA assays and assessed gene expression (PEPCK, G6-PDH, PFKFB1, GS, GK, and GLUT-4) using qRT-PCR. The obtained results revealed an upregulation of G6-PDH (PPS pathway), PFKFB1 (glycolysis), GS (glycogenesis), and GLUT-4 (glucose transporter), while the PEPCK (gluconeogenesis) gene was downregulated. Besides, the antidiabetic biomarkers showed elevated adiponectin, SOD, and glutathione levels; however, amylase level decreased in the treatment groups. We observed a dose-dependent reduction in HbA1c, insulin, and random blood glucose in the metformin and Fa.Me groups. Histopathological analysis of animals' liver and pancreas showed an intact structure of hepatocytes in extract groups, while atrophic changes in the pancreas were observed in the diseased group. By modulating the oxidative stress and glucose metabolism-control genes, F. adenophylla demonstrated significant antidiabetic properties and held potential for further clinical exploration.
{"title":"Molecular events responsible for hypoglycaemic attributes of Fernandoa adenophylla extract in streptozotocin-induced diabetes","authors":"Ammara Hakeem , Mohammad Saleem , Rukhsana Anwar , Muhammad Asif , Taha Muhammad , Sherif S. Ebada , Nawal M. Al Musayeib , Mohamed L. Ashour","doi":"10.1016/j.fitote.2025.106557","DOIUrl":"10.1016/j.fitote.2025.106557","url":null,"abstract":"<div><div>Traditionally, people use the decoction of <em>Fernandoa adenophylla</em> leaves to treat diabetes mellitus. This study investigated the antidiabetic activity of <em>F. adenophylla</em> methanol extract (Fa.Me) in streptozotocin (STZ)-induced diabetes rats, with metformin as a positive control. We analysed several relevant biomarkers and antioxidant enzymes using ELISA assays and assessed gene expression (PEPCK, G6-PDH, PFKFB1, GS, GK, and GLUT-4) using qRT-PCR. The obtained results revealed an upregulation of G6-PDH (PPS pathway), PFKFB1 (glycolysis), GS (glycogenesis), and GLUT-4 (glucose transporter), while the PEPCK (gluconeogenesis) gene was downregulated. Besides, the antidiabetic biomarkers showed elevated adiponectin, SOD, and glutathione levels; however, amylase level decreased in the treatment groups. We observed a dose-dependent reduction in HbA1c, insulin, and random blood glucose in the metformin and Fa.Me groups. Histopathological analysis of animals' liver and pancreas showed an intact structure of hepatocytes in extract groups, while atrophic changes in the pancreas were observed in the diseased group. By modulating the oxidative stress and glucose metabolism-control genes, <em>F. adenophylla</em> demonstrated significant antidiabetic properties and held potential for further clinical exploration.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106557"},"PeriodicalIF":2.5,"publicationDate":"2025-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143869377","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 : 2025-04-19DOI: 10.1016/j.fitote.2025.106556
Dipal M. Gandhi , Kriti H. Sharma , Aakash Kumar S , Jigar N. Shah , Snehal S. Patel
A new, precise, and reproducible HPTLC method was developed and validated for the estimation of andrographolide (AG), gallic acid (GA), and kutkin (KT2) in an ayurvedic formulation, HEPASAVE Syrup. The quantification of the three biomarkers was performed on TLC aluminum plates pre-coated with silica gel 60F254 as stationary phase. Linear ascending development was carried out in a Camag twin trough glass chamber saturated with toluene: ethyl acetate: formic acid: methanol (3:3:0.8:0.4, v/v/v/v) at room temperature (25 ± 2 °C). Camag TLC scanner III was used for simultaneous spectro-densitometric scanning and analysis in absorbance mode at 254 nm. The system was found to give compact spots for AG, GA, and KT2 with the respective Rf values of 0.74, 0.66, and 0.21. The data for calibration plots showed a good linear relationship for AG with r2 = 0.995, GA with r2 = 0.993, and KT2 with r2 = 0.992 in the concentration range of 200 ng to 800 ng, 80 ng to 320 ng and 2000 ng to 6000 ng, respectively to the peak area. The amount of AG, GA, and KT2 in the formulation was quantified and found to be 1.27 %w/v, 1.15 %w/v, and 0.014 %w/v, respectively. Statistical analysis of the data showed that the method is reproducible for the quantification of AG, GA, and KT2, simultaneously in HEPASAVE Syrup. It also significantly reduced the levels of SGPT, SGOT, and ALP in animals.
{"title":"Simultaneous estimation of bioactive markers using validated HPTLC method and assessment of hepatoprotective effect of HEPASAVE: An Ayurvedic formulation","authors":"Dipal M. Gandhi , Kriti H. Sharma , Aakash Kumar S , Jigar N. Shah , Snehal S. Patel","doi":"10.1016/j.fitote.2025.106556","DOIUrl":"10.1016/j.fitote.2025.106556","url":null,"abstract":"<div><div>A new, precise, and reproducible HPTLC method was developed and validated for the estimation of andrographolide (AG), gallic acid (GA), and kutkin (KT2) in an ayurvedic formulation, HEPASAVE Syrup. The quantification of the three biomarkers was performed on TLC aluminum plates pre-coated with silica gel 60F<sub>254</sub> as stationary phase. Linear ascending development was carried out in a Camag twin trough glass chamber saturated with toluene: ethyl acetate: formic acid: methanol (3:3:0.8:0.4, <em>v</em>/v/<em>v</em>/v) at room temperature (25 ± 2 °C). Camag TLC scanner III was used for simultaneous spectro-densitometric scanning and analysis in absorbance mode at 254 nm. The system was found to give compact spots for AG, GA, and KT2 with the respective R<sub>f</sub> values of 0.74, 0.66, and 0.21. The data for calibration plots showed a good linear relationship for AG with r<sup>2</sup> = 0.995, GA with r<sup>2</sup> = 0.993, and KT2 with r<sup>2</sup> = 0.992 in the concentration range of 200 ng to 800 ng, 80 ng to 320 ng and 2000 ng to 6000 ng, respectively to the peak area. The amount of AG, GA, and KT2 in the formulation was quantified and found to be 1.27 %<em>w</em>/<em>v</em>, 1.15 %w/v, and 0.014 %w/v, respectively. Statistical analysis of the data showed that the method is reproducible for the quantification of AG, GA, and KT2, simultaneously in HEPASAVE Syrup. It also significantly reduced the levels of SGPT, SGOT, and ALP in animals.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106556"},"PeriodicalIF":2.5,"publicationDate":"2025-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143869379","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 : 2025-04-19DOI: 10.1016/j.fitote.2025.106560
Xiaoliang Zhao , Qingsong Zhou , He Mou , Li Ma , Yanmei Liu , Kaili Qi , Cunjin Wang , Jing Zhang , Ji Zhang , Weijie Zhang
Three polysaccharides, namely SHC, SFH, and SFA, were extracted from Sophora sophora under various conditions. A single-factor experimental design was employed to investigate the influence of reaction solvent, sulfating reagent ratio, reaction time, and temperature on the yield of sulfated products, the degree of sulfate group substitution, and their inhibitory effects on HepG2 cell proliferation. Three sulfated derivatives, SHCS, SFHS, and SFAS, were synthesized and confirmed through Fourier Transform Infrared Spectroscopy, Ultraviolet Spectroscopy, and Nuclear Magnetic Resonance Spectroscopy. Among these, SFHS exhibited the highest degree of substitution (DS) at 1.22, followed by SFAS at 0.97 and SFCS at 0.56. In vitro analyses revealed that sulfated modification significantly enhanced free radical scavenging activity, tumor cell growth inhibition, and immune response enhancement. Specifically, SFHS exhibited scavenging activities against DPPH, hydroxyl, and superoxide anion free radicals with rates of 69.8 % ± 6.1 %, 50.4 % ± 4.2 %, and 58.5 % ± 5.1 %, respectively, at 5 mg/mL. Furthermore, it inhibited the proliferation of HepG2 cells by 51.9 % ± 5.6 % at 400 μg/mL and HeLa cells by 43.7 % ± 1.8 % at 800 μg/mL. At 800 μg/mL, SFHS treatment resulted in a phagocytosis rate of neutral red by RAW264.7 macrophages, which was 246.6 % ± 13.9 % relative to the control group, while nitric oxide production was measured at 237.6 % ± 6.2 %. These results suggest that sulfation can enhance the biological functions of polysaccharides derived from S. flavescens, indicating potential applications in functional foods and pharmaceuticals.
{"title":"Sulfated modification of polysaccharides from Sophora flavescens: Impact on antioxidant, antitumor, and immunomodulatory activities","authors":"Xiaoliang Zhao , Qingsong Zhou , He Mou , Li Ma , Yanmei Liu , Kaili Qi , Cunjin Wang , Jing Zhang , Ji Zhang , Weijie Zhang","doi":"10.1016/j.fitote.2025.106560","DOIUrl":"10.1016/j.fitote.2025.106560","url":null,"abstract":"<div><div>Three polysaccharides, namely SHC, SFH, and SFA, were extracted from <em>Sophora sophora</em> under various conditions. A single-factor experimental design was employed to investigate the influence of reaction solvent, sulfating reagent ratio, reaction time, and temperature on the yield of sulfated products, the degree of sulfate group substitution, and their inhibitory effects on HepG2 cell proliferation. Three sulfated derivatives, SHCS, SFHS, and SFAS, were synthesized and confirmed through Fourier Transform Infrared Spectroscopy, Ultraviolet Spectroscopy, and Nuclear Magnetic Resonance Spectroscopy. Among these, SFHS exhibited the highest degree of substitution (DS) at 1.22, followed by SFAS at 0.97 and SFCS at 0.56. <em>In vitro</em> analyses revealed that sulfated modification significantly enhanced free radical scavenging activity, tumor cell growth inhibition, and immune response enhancement. Specifically, SFHS exhibited scavenging activities against DPPH, hydroxyl, and superoxide anion free radicals with rates of 69.8 % ± 6.1 %, 50.4 % ± 4.2 %, and 58.5 % ± 5.1 %, respectively, at 5 mg/mL. Furthermore, it inhibited the proliferation of HepG2 cells by 51.9 % ± 5.6 % at 400 μg/mL and HeLa cells by 43.7 % ± 1.8 % at 800 μg/mL. At 800 μg/mL, SFHS treatment resulted in a phagocytosis rate of neutral red by RAW264.7 macrophages, which was 246.6 % ± 13.9 % relative to the control group, while nitric oxide production was measured at 237.6 % ± 6.2 %. These results suggest that sulfation can enhance the biological functions of polysaccharides derived from <em>S. flavescens</em>, indicating potential applications in functional foods and pharmaceuticals.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106560"},"PeriodicalIF":2.5,"publicationDate":"2025-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143851952","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 : 2025-04-19DOI: 10.1016/j.fitote.2025.106559
Wen-xiang Xu , Zhen-yun Liu , Qing-yue Bu , Peng Jiang , Yi-qiang Zhang , Yu-meng Luo , Wei Guan , Xiao-chi Ma , Meng-meng Li , Qing-shan Chen , Li-li Zhang , Hai-xue Kuang , Bing-you Yang , Yan Liu
Eight new triterpenoid saponins, named huangqiyesaponin IV to XI (1–8), along with three previously identified compounds (9–11), were isolated from the 70 % ethanol solution of the leaves of Astragalus membranaceus (Fisch.) Bunge. These compounds were isolated through various column chromatography techniques, including those using silica gel, ODS, and preparative liquid chromatography. Their structures were elucidated based on comprehensive spectral analyses, including 1D and 2D-NMR, HRESIMS, and IR, as well as comparisons with existing literature. Additionally, HT22 cells stimulated with D-galactose were employed to assess the neuroprotective potential of all isolated compounds. The findings revealed that compounds 3 and 7–9 demonstrated notable neuroprotective effects.
{"title":"Eight new triterpenoid saponins from the leaves of Astragalus membranaceus (Fisch.) Bunge and their neuroprotective effects","authors":"Wen-xiang Xu , Zhen-yun Liu , Qing-yue Bu , Peng Jiang , Yi-qiang Zhang , Yu-meng Luo , Wei Guan , Xiao-chi Ma , Meng-meng Li , Qing-shan Chen , Li-li Zhang , Hai-xue Kuang , Bing-you Yang , Yan Liu","doi":"10.1016/j.fitote.2025.106559","DOIUrl":"10.1016/j.fitote.2025.106559","url":null,"abstract":"<div><div>Eight new triterpenoid saponins, named huangqiyesaponin IV to XI (<strong>1</strong>–<strong>8</strong>), along with three previously identified compounds (<strong>9</strong>–<strong>11</strong>), were isolated from the 70 % ethanol solution of the leaves of <em>Astragalus membranaceus</em> (Fisch.) Bunge. These compounds were isolated through various column chromatography techniques, including those using silica gel, ODS, and preparative liquid chromatography. Their structures were elucidated based on comprehensive spectral analyses, including 1D and 2D-NMR, HRESIMS, and IR, as well as comparisons with existing literature. Additionally, HT22 cells stimulated with D-galactose were employed to assess the neuroprotective potential of all isolated compounds. The findings revealed that compounds <strong>3</strong> and <strong>7</strong>–<strong>9</strong> demonstrated notable neuroprotective effects.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106559"},"PeriodicalIF":2.5,"publicationDate":"2025-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143851951","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 : 2025-04-17DOI: 10.1016/j.fitote.2025.106550
Xue-Ying Xu , Qiong Jin , Jia-Mei Geng, Pei-Feng Zhu, Zhu-Ya Yang, Xin Duan, Lu Liu
Two undescribed furan derivatives elsholtzia ketone-9-O-β-glucopyranoside (1) and 8-hydroxy-elsholtzia ketone-9-O-β-glucopyranoside (2) along with ten known compounds (3−12), were isolated from Elsholtzia rugulosa Hemsl. Their structures were elucidated based on extensive analyses of spectroscopic data and quantum chemical calculations. Anti-inflammatory experiments showed that 1, 7, and 12 reduce the production of nitric oxide (NO) and the levels of tumor necrosis factor-alpha (TNF-α), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) induced by lipopolysaccharide (LPS) in RAW264.7 cells.
{"title":"Chemical constituents and anti-inflammatory investigation of Elsholtzia rugulosa Hemsl","authors":"Xue-Ying Xu , Qiong Jin , Jia-Mei Geng, Pei-Feng Zhu, Zhu-Ya Yang, Xin Duan, Lu Liu","doi":"10.1016/j.fitote.2025.106550","DOIUrl":"10.1016/j.fitote.2025.106550","url":null,"abstract":"<div><div>Two undescribed furan derivatives elsholtzia ketone-9-<em>O</em>-<em>β</em>-glucopyranoside (<strong>1</strong>) and 8-hydroxy-elsholtzia ketone-9-<em>O</em>-<em>β</em>-glucopyranoside (<strong>2</strong>) along with ten known compounds (<strong>3</strong>−<strong>12</strong>), were isolated from <em>Elsholtzia rugulosa</em> Hemsl. Their structures were elucidated based on extensive analyses of spectroscopic data and quantum chemical calculations. Anti-inflammatory experiments showed that <strong>1</strong>, <strong>7</strong>, and <strong>12</strong> reduce the production of nitric oxide (NO) and the levels of tumor necrosis factor-alpha (TNF-<em>α</em>), interleukin-1 beta (IL-1<em>β</em>), and interleukin-6 (IL-6) induced by lipopolysaccharide (LPS) in RAW264.7 cells.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106550"},"PeriodicalIF":2.5,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143845106","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 : 2025-04-17DOI: 10.1016/j.fitote.2025.106551
Mahmoud Nagaty Mahrous , Eman Zekry Attia , Mohamed S.A. Abdelkader , Deiaa E. Elsayed Abouzed , Sahar M. Gebril , Radwan Alnajjar , Ahmed A. Al-Karmalawy , Ashraf Nageeb Elsayed Hamed
Osteoarthritis (OA) is a serious health issue that lacks a totally effective treatment. In light of the critical need for alternative therapies to halt osteoarthritis and its progress, This study explores the potential of Lolium perenne as a treatment for osteoarthritis for the first time. The research evaluates the plant's protective effects against monosodium iodoacetate (MIA)-induced OA in rats. 24 rats were assigned into 4 groups, group I (sham control), group II (OA), group III (dichloromethane fraction (FrII) + OA), and group IV (ethyl acetate fraction (FrIII) + OA). For 21 days, the samples were given orally at a dose of 40 mg/kg. The obtained results indicated all treatment groups showed a significant decrease in the severity of articular cartilage degradation and in the concentration of Interleukin-1 beta (IL-1β) and Tumor necrosis factor alpha (TNF-α) cytokines compared to the OA-induced group Moreover, eight structurally varied metabolites were isolated and identified from the FrII and FrIII fractions derived from the methanol extract of the aerial part of L. perenne, which were linked with pro-inflammatory cytokines in the computational docking investigation. Interestingly, salcolin B (2b) and calquiquelignan E (4) isolated from FrII fraction, showed prevalent activity for the two tested receptors [salcolin B, IL-1β (−6.7354 kcal/mol) and calquiquelignan E, TNF-α (−6.2038 kcal/mol)] compared to the reference flurbiprofen drug. Finally, the frontier candidates against IL-1β and TNF-α receptors simulated at 100 ns and the MM-GBSA calculations confirming the docking results. These findings highlight L. perenne's potential as a natural therapeutic for OA.
{"title":"Chemical composition and anti-osteoarthritis potential of Lolium perenne L. assisted with computational studies","authors":"Mahmoud Nagaty Mahrous , Eman Zekry Attia , Mohamed S.A. Abdelkader , Deiaa E. Elsayed Abouzed , Sahar M. Gebril , Radwan Alnajjar , Ahmed A. Al-Karmalawy , Ashraf Nageeb Elsayed Hamed","doi":"10.1016/j.fitote.2025.106551","DOIUrl":"10.1016/j.fitote.2025.106551","url":null,"abstract":"<div><div>Osteoarthritis (OA) is a serious health issue that lacks a totally effective treatment. In light of the critical need for alternative therapies to halt osteoarthritis and its progress, This study explores the potential of <em>Lolium perenne</em> as a treatment for osteoarthritis for the first time. The research evaluates the plant's protective effects against monosodium iodoacetate (MIA)-induced OA in rats. 24 rats were assigned into 4 groups, group I (sham control), group II (OA), group III (dichloromethane fraction (FrII) + OA), and group IV (ethyl acetate fraction (FrIII) + OA). For 21 days, the samples were given orally at a dose of 40 mg/kg. The obtained results indicated all treatment groups showed a significant decrease in the severity of articular cartilage degradation and in the concentration of Interleukin-1 beta (IL-1β) and Tumor necrosis factor alpha (TNF-α) cytokines compared to the OA-induced group Moreover, eight structurally varied metabolites were isolated and identified from the FrII and FrIII fractions derived from the methanol extract of the aerial part of <em>L. perenne</em>, which were linked with pro-inflammatory cytokines in the computational docking investigation. Interestingly, salcolin B (<strong>2b</strong>) and calquiquelignan E (<strong>4</strong>) isolated from FrII fraction, showed prevalent activity for the two tested receptors [salcolin B, IL-1β (−6.7354 kcal/mol) and calquiquelignan E, TNF-α (−6.2038 kcal/mol)] compared to the reference flurbiprofen drug. Finally, the frontier candidates against IL-1β and TNF-α receptors simulated at 100 ns and the MM-GBSA calculations confirming the docking results. These findings highlight L. <em>perenne</em>'s potential as a natural therapeutic for OA.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106551"},"PeriodicalIF":2.5,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143874674","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