Pub Date : 2025-01-12DOI: 10.1016/j.fitote.2025.106392
Yi-Fan Xia, Jin-Hui Zheng, Yan-Song Li, Ping Yu, Zhe Liu, Jie Zhou, Lei Fang
Two undescribed oxazole-containing diterpenoids (1-2) and a new diterpenoid (3) were isolated from the roots of Salvia miltiorrhiza. Their structures were elucidated by extensive HRESIMS and NMR spectroscopic analysis, and the absolute configurations of 1 and 3 were confirmed by comparison of the calculated and experimental electronic circular dichroism (ECD) spectra. Compound 1 represents the first example of an abietane diterpenoid with a benzo[d]oxazole unit fused in the ring B of the abietane skeleton. The cytotoxicity of 1-3 was evaluated against four human tumor cell lines (A549, MCF-7, HepG2, and PC-3), and 1-2 showed weak cytotoxic activities.
{"title":"Three new diterpenes from the roots of Salvia miltiorrhiza and their cytotoxicity.","authors":"Yi-Fan Xia, Jin-Hui Zheng, Yan-Song Li, Ping Yu, Zhe Liu, Jie Zhou, Lei Fang","doi":"10.1016/j.fitote.2025.106392","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106392","url":null,"abstract":"<p><p>Two undescribed oxazole-containing diterpenoids (1-2) and a new diterpenoid (3) were isolated from the roots of Salvia miltiorrhiza. Their structures were elucidated by extensive HRESIMS and NMR spectroscopic analysis, and the absolute configurations of 1 and 3 were confirmed by comparison of the calculated and experimental electronic circular dichroism (ECD) spectra. Compound 1 represents the first example of an abietane diterpenoid with a benzo[d]oxazole unit fused in the ring B of the abietane skeleton. The cytotoxicity of 1-3 was evaluated against four human tumor cell lines (A549, MCF-7, HepG2, and PC-3), and 1-2 showed weak cytotoxic activities.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106392"},"PeriodicalIF":2.5,"publicationDate":"2025-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142983159","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 : 2025-01-11DOI: 10.1016/j.fitote.2025.106390
Dong Liu, Yaling He, Xinmiao Zhang, Ziyang Ye, Ming Ye
LEP-1a, a new polysaccharide fraction isolated and purified from Lachnum YM40, has a molecular weight of 24.29 kDa. LEP-1a's chemical composition investigation showed that mannose, galactose, and glucose made up the majority of its cosmetics. The methylation, nuclear magnetic resonance, and Fourier transform infrared investigations demonstrated that the (1 → 2)-β-D-Galp, (1 → 2,6)-α-D-Manp, glycosidic connections of LEP-1a were comprised of 1→)-α-D-Manp, (1 → 4)-α-D-Galp, (1 → 6)-α-D-Manp, (1 → 2)-β-D-Glcp, (1 → 4)-β-D-Glcp, (1 → 2)-α-D-Manp, and (1 → 3, 6)-β-D-Manp. LEP-1a has a linear microscopic morphology, as demonstrated by atomic force microscopy, scanning electron microscopy, and rheological property investigation. Moreover, the polysaccharide LEP-1a displayed bile acid- and cholesterol-binding capacities and inhibitory activity on lipase.
{"title":"Characterization, physicochemical properties, antioxidant activity and hypolipidemic activities of a polysaccharides from Lachnum YM40.","authors":"Dong Liu, Yaling He, Xinmiao Zhang, Ziyang Ye, Ming Ye","doi":"10.1016/j.fitote.2025.106390","DOIUrl":"10.1016/j.fitote.2025.106390","url":null,"abstract":"<p><p>LEP-1a, a new polysaccharide fraction isolated and purified from Lachnum YM40, has a molecular weight of 24.29 kDa. LEP-1a's chemical composition investigation showed that mannose, galactose, and glucose made up the majority of its cosmetics. The methylation, nuclear magnetic resonance, and Fourier transform infrared investigations demonstrated that the (1 → 2)-β-D-Galp, (1 → 2,6)-α-D-Manp, glycosidic connections of LEP-1a were comprised of 1→)-α-D-Manp, (1 → 4)-α-D-Galp, (1 → 6)-α-D-Manp, (1 → 2)-β-D-Glcp, (1 → 4)-β-D-Glcp, (1 → 2)-α-D-Manp, and (1 → 3, 6)-β-D-Manp. LEP-1a has a linear microscopic morphology, as demonstrated by atomic force microscopy, scanning electron microscopy, and rheological property investigation. Moreover, the polysaccharide LEP-1a displayed bile acid- and cholesterol-binding capacities and inhibitory activity on lipase.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106390"},"PeriodicalIF":2.5,"publicationDate":"2025-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142978046","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 : 2025-01-11DOI: 10.1016/j.fitote.2025.106389
Guo-Sen He, Ji-Kai Xia, Qi-Hu Li, Yan Zheng, Chun-Ru Shi, Run Li, Quan Hong, Xiang-Mei Chen
Background: Specnuezhenide (SPN) is a bioactive iridoid terpenoid compound mainly found in Ligustri Lucidi Fructus (LLF), that has a broad spectrum of pharmacological effects, including anti-neoplastic, hepatoprotective, anti-aging, anti-inflammatory, immune-modulatory properties.
Purpose: The present review provides a comprehensive summary of natural medicinal plants, traditional Chinese medicine compounds containing SPN, and their corresponding pharmacological mechanisms.
Methods: Using several globally recognized databases such as Web of Science, Google Scholar, PubMed, ScienceDirect, Wiley, ACS, Springer, and CNKI until December 2024, A comprehensive literature search and analysis was carried out with the keywords "Specnuezhenide", " Pharmacology ", "Pharmacokinetics" and " Chinese herbal compound".
Results: The results indicated that SPN is present in a diverse range of plants, including LLF, Osmanthus fragrans seeds and Naked barley. SPN plays an anti-inflammatory role by regulating the NF-κB and MAPK signaling pathways, down-regulating the expression of TNF-α, IL-1β, IL-6 and other cytokines. Furthermore, many Chinese herbal compounds have been found to contain SPN, such as treatment of spleen and kidney deficiency of compound Shenhua tablet, treatment of liver-kidney Yin deficiency of Er Zhi Wan, treatment of pulmonray abscess of Qidongning and treatment of stagnation of QI due to depression of the liver of Shuganzhi Tablet. SPN is primarily distributed in the stomach, intestine, and liver. However, due to its limited absorption in the gastrointestinal tract and low blood concentration, its bioavailability is significantly reduced.
Conclusions: Thereby, SPN holds immense potential in the prevention and treatment of liver, lung and kidney complications. This review intends to provide a novel insight for further development of SPN, hoping to reveal the potential of SPN and necessity of further studies in this field.
{"title":"Specnuezhenide: Comprehensive review of pharmacology, pharmacokinetics and ethnomedicinal uses.","authors":"Guo-Sen He, Ji-Kai Xia, Qi-Hu Li, Yan Zheng, Chun-Ru Shi, Run Li, Quan Hong, Xiang-Mei Chen","doi":"10.1016/j.fitote.2025.106389","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106389","url":null,"abstract":"<p><strong>Background: </strong>Specnuezhenide (SPN) is a bioactive iridoid terpenoid compound mainly found in Ligustri Lucidi Fructus (LLF), that has a broad spectrum of pharmacological effects, including anti-neoplastic, hepatoprotective, anti-aging, anti-inflammatory, immune-modulatory properties.</p><p><strong>Purpose: </strong>The present review provides a comprehensive summary of natural medicinal plants, traditional Chinese medicine compounds containing SPN, and their corresponding pharmacological mechanisms.</p><p><strong>Methods: </strong>Using several globally recognized databases such as Web of Science, Google Scholar, PubMed, ScienceDirect, Wiley, ACS, Springer, and CNKI until December 2024, A comprehensive literature search and analysis was carried out with the keywords \"Specnuezhenide\", \" Pharmacology \", \"Pharmacokinetics\" and \" Chinese herbal compound\".</p><p><strong>Results: </strong>The results indicated that SPN is present in a diverse range of plants, including LLF, Osmanthus fragrans seeds and Naked barley. SPN plays an anti-inflammatory role by regulating the NF-κB and MAPK signaling pathways, down-regulating the expression of TNF-α, IL-1β, IL-6 and other cytokines. Furthermore, many Chinese herbal compounds have been found to contain SPN, such as treatment of spleen and kidney deficiency of compound Shenhua tablet, treatment of liver-kidney Yin deficiency of Er Zhi Wan, treatment of pulmonray abscess of Qidongning and treatment of stagnation of QI due to depression of the liver of Shuganzhi Tablet. SPN is primarily distributed in the stomach, intestine, and liver. However, due to its limited absorption in the gastrointestinal tract and low blood concentration, its bioavailability is significantly reduced.</p><p><strong>Conclusions: </strong>Thereby, SPN holds immense potential in the prevention and treatment of liver, lung and kidney complications. This review intends to provide a novel insight for further development of SPN, hoping to reveal the potential of SPN and necessity of further studies in this field.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106389"},"PeriodicalIF":2.5,"publicationDate":"2025-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142978079","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}
Background: Ginseng-Schisandra chinensis (GSC) decoction has shown good efficacy in the treatment of asthma, but its t mechanism in the treatment of asthma is still not fully understood.
Purpose: This study aims to elucidate the therapeutic mechanism of GSC for AS by identifying the active components of GSC.
Methods: The chemical composition of GSC was analyzed using UHPLC-MS/MS. The network pharmacology method combined with TCMSP and GeneCards database was used to identify potential targets and enriched pathways related to AS treatment. Use AutoDock for molecular docking to evaluate the binding affinity of active ingredients to core targets. Finally, the LPS-induced A549 cell inflammation model was used to evaluate the effect of GSC on the release of inflammatory cytokines.
Results: The main components in GSC, including ginsenosides (Rf, Rd, Rg2, Ro, Rg5, Rh1) and lignans (schisandrin A, B, schisandrol A, B, schisandrin ester A) were identified. Network analysis revealed 139 intersection targets and highlighted STAT3, TNF, EGFR, IL1B, and AKT1 as key targets, with the PI3K/AKT signaling pathway as the main pathway. Experimental results showed that GSC significantly reduced the levels of IL-1β, IL-6 and TNF-α in LPS-induced A549 cells (p < 0.01), indicating its powerful anti-inflammatory effect.
Conclusion: GSC plays a role in treating asthma by targeting STAT3, TNF, IL-1β and AKT1, regulating the PI3K/AKT signaling pathway and inhibiting the release of inflammatory cytokines. These findings provide a basis for the clinical application of GSC.
{"title":"Network pharmacology prediction and molecular docking-based strategy to explore the potential mechanism of Ginseng-Schisandra Chinensis decoction against asthma.","authors":"Ting Zhou, Qingqing Li, Kaiyue Zhang, Meng Zhang, Hui Li, Wei Wu","doi":"10.1016/j.fitote.2025.106388","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106388","url":null,"abstract":"<p><strong>Background: </strong>Ginseng-Schisandra chinensis (GSC) decoction has shown good efficacy in the treatment of asthma, but its t mechanism in the treatment of asthma is still not fully understood.</p><p><strong>Purpose: </strong>This study aims to elucidate the therapeutic mechanism of GSC for AS by identifying the active components of GSC.</p><p><strong>Methods: </strong>The chemical composition of GSC was analyzed using UHPLC-MS/MS. The network pharmacology method combined with TCMSP and GeneCards database was used to identify potential targets and enriched pathways related to AS treatment. Use AutoDock for molecular docking to evaluate the binding affinity of active ingredients to core targets. Finally, the LPS-induced A549 cell inflammation model was used to evaluate the effect of GSC on the release of inflammatory cytokines.</p><p><strong>Results: </strong>The main components in GSC, including ginsenosides (Rf, Rd, Rg2, Ro, Rg5, Rh1) and lignans (schisandrin A, B, schisandrol A, B, schisandrin ester A) were identified. Network analysis revealed 139 intersection targets and highlighted STAT3, TNF, EGFR, IL1B, and AKT1 as key targets, with the PI3K/AKT signaling pathway as the main pathway. Experimental results showed that GSC significantly reduced the levels of IL-1β, IL-6 and TNF-α in LPS-induced A549 cells (p < 0.01), indicating its powerful anti-inflammatory effect.</p><p><strong>Conclusion: </strong>GSC plays a role in treating asthma by targeting STAT3, TNF, IL-1β and AKT1, regulating the PI3K/AKT signaling pathway and inhibiting the release of inflammatory cytokines. These findings provide a basis for the clinical application of GSC.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106388"},"PeriodicalIF":2.5,"publicationDate":"2025-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142970296","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 : 2025-01-07DOI: 10.1016/j.fitote.2025.106387
Yan-Yan Luo, Jin-Bu Xu, Shuai Huang, Xian-Li Zhou
The phytochemistry study of Aconitum bulbilliferum Hand.-Mazz. is firstly reported. Two C20-diterpenoid alkaloids, named bulbilliferines A and B (1 and 2), three C19-diterpenoid alkaloids, bulbillifedines A-C (3-5), and twenty known compounds (6-25) were isolated from the roots of A. bulbilliferum. The structures of these compounds were determined by the comprehensive spectroscopic analyses (HRESIMS, IR, 1D and 2D NMR). Among them, bulbilliferine A (1) is a denudatine-type diterpenoid alkaloid bearing a 16, 17-epoxy group. At a nontoxic dose of 10 mg/kg, 14-O-anisoylchasmanine (14) hydrochloride and austroconitine B (17) hydrochloride respectively exhibited the excellent analgesic effects with 83.6 % and 83.1 % inhibitions against acetic acid-induced writhing of mice.
{"title":"Diterpenoid alkaloids from the roots of Aconitum bulbilliferum.","authors":"Yan-Yan Luo, Jin-Bu Xu, Shuai Huang, Xian-Li Zhou","doi":"10.1016/j.fitote.2025.106387","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106387","url":null,"abstract":"<p><p>The phytochemistry study of Aconitum bulbilliferum Hand.-Mazz. is firstly reported. Two C<sub>20</sub>-diterpenoid alkaloids, named bulbilliferines A and B (1 and 2), three C<sub>19</sub>-diterpenoid alkaloids, bulbillifedines A-C (3-5), and twenty known compounds (6-25) were isolated from the roots of A. bulbilliferum. The structures of these compounds were determined by the comprehensive spectroscopic analyses (HRESIMS, IR, 1D and 2D NMR). Among them, bulbilliferine A (1) is a denudatine-type diterpenoid alkaloid bearing a 16, 17-epoxy group. At a nontoxic dose of 10 mg/kg, 14-O-anisoylchasmanine (14) hydrochloride and austroconitine B (17) hydrochloride respectively exhibited the excellent analgesic effects with 83.6 % and 83.1 % inhibitions against acetic acid-induced writhing of mice.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106387"},"PeriodicalIF":2.5,"publicationDate":"2025-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946841","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}
Maintaining lipid homeostasis is important for intestinal and body health. Litchi flower essential oil (LFEO), mainly containing 9,12-Octadecadienoic acid (Z,Z)-, α-Curcumene, Gamma.-Sitosterol, α-linolenic acid, β-Bisabolene and n-Hexadecanoic acid, has been demonstrated significant anti-obesity activity. However, it remains uncertain whether LFEO could ameliorate intestinal damage associated with lipid metabolism disorders. The aim of this study was to investigate the protective effect of LFEO against intestinal injury caused by lipid disturbance in Caenorhabditis elegans. Firstly, LFEO significantly ameliorated the lipid disturbance induced by Pseudomonas aeruginosa and maintained lipid homeostasis. Secondly, LFEO maintained intestinal health by attenuating mitochondrial damage. After LFEO treatment, the intestinal width of worms was reduced by 24.82 % (on day 5) and 23.81 % (on day 7), respectively, while the intestinal breakage rate was only 15.33 %. In terms of capacity metabolism, LFEO significantly protected the neuronal structure, improved pharyngeal function, and maintained energy intake in lipid-disordered worms. The results of this study indicated that LFEO effectively reduced the intestinal damage and maintained intestinal health in lipid disorder nematodes. It made a new understanding for LFEO to reduce intestinal damage caused by lipid disorders, and provided a reference for the large-scale production of LFEO to promote the development of litchi circular economy.
{"title":"Litchi flower essential oil (LFEO) restores intestinal health in lipid disorder Caenorhabditis elegans.","authors":"Danxian Luo, Jingrui Luo, Yun Chen, Ruina Xu, Yong Cao, Zuanxian Su, Yunjiao Chen","doi":"10.1016/j.fitote.2025.106386","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106386","url":null,"abstract":"<p><p>Maintaining lipid homeostasis is important for intestinal and body health. Litchi flower essential oil (LFEO), mainly containing 9,12-Octadecadienoic acid (Z,Z)-, α-Curcumene, Gamma.-Sitosterol, α-linolenic acid, β-Bisabolene and n-Hexadecanoic acid, has been demonstrated significant anti-obesity activity. However, it remains uncertain whether LFEO could ameliorate intestinal damage associated with lipid metabolism disorders. The aim of this study was to investigate the protective effect of LFEO against intestinal injury caused by lipid disturbance in Caenorhabditis elegans. Firstly, LFEO significantly ameliorated the lipid disturbance induced by Pseudomonas aeruginosa and maintained lipid homeostasis. Secondly, LFEO maintained intestinal health by attenuating mitochondrial damage. After LFEO treatment, the intestinal width of worms was reduced by 24.82 % (on day 5) and 23.81 % (on day 7), respectively, while the intestinal breakage rate was only 15.33 %. In terms of capacity metabolism, LFEO significantly protected the neuronal structure, improved pharyngeal function, and maintained energy intake in lipid-disordered worms. The results of this study indicated that LFEO effectively reduced the intestinal damage and maintained intestinal health in lipid disorder nematodes. It made a new understanding for LFEO to reduce intestinal damage caused by lipid disorders, and provided a reference for the large-scale production of LFEO to promote the development of litchi circular economy.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106386"},"PeriodicalIF":2.5,"publicationDate":"2025-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946849","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}
Two new tropolone-bearing sesquiterpenoids (1-2), two new dolabrane-type diterpenoids (3-4) along with eight known compounds as ionone-type sesquiterpenoid (5), oleanane triterpenoid (6), vanillin and its derivative (7-8), neolignan (9), two lignans (10-11), flavanonol glycoside (12) were isolated from whole plants of Croton lauioides Radcl.-Sm. & Govaerts. The structures of all isolated compounds were elucidated by extensive spectral data including 1D, 2D NMR, HR-ESI-MS, and by comparing their NMR data with those of previously reported compounds. The experimental and calculated electronic circular dichroism data were used to determine their absolute configurations. All new compounds (1-4) were evaluated for their anti-inflammatory activity on LPS-induced RAW264.7 macrophages, and cytotoxicity against five human cancer cell lines (HepG2, A-549, MDA-MB-231, HL-60, and SW-480). Compound 2 showed signicant inhibitory activity against NO production with an IC50 value of 16.41 ± 0.48 μM, better than that of L-NMMA (positive control, IC50 = 42.83 ± 0.80 μM), while compound 1 exhibited comparable anti-inflammatory activity with IC50 value of 47.50 ± 0.46 μM. Furthermore, compound 1 was also found to display selective cytotoxicity against human cancer cell line HepG2 with an inhibition rate of 79.09 % at 40.0 μM.
{"title":"Two new sesquiterpenoids and two new diterpenoids from Croton lauioides with anti-inflammatory and cytotoxic activities.","authors":"Jia-Xin Hu, Qian Liang, Li-Lin Xiao, Rong-Lin Jia, Xiao-Min Su, Li-Ping Liu, Xiahong He, Wen-Hui Xu","doi":"10.1016/j.fitote.2025.106384","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106384","url":null,"abstract":"<p><p>Two new tropolone-bearing sesquiterpenoids (1-2), two new dolabrane-type diterpenoids (3-4) along with eight known compounds as ionone-type sesquiterpenoid (5), oleanane triterpenoid (6), vanillin and its derivative (7-8), neolignan (9), two lignans (10-11), flavanonol glycoside (12) were isolated from whole plants of Croton lauioides Radcl.-Sm. & Govaerts. The structures of all isolated compounds were elucidated by extensive spectral data including 1D, 2D NMR, HR-ESI-MS, and by comparing their NMR data with those of previously reported compounds. The experimental and calculated electronic circular dichroism data were used to determine their absolute configurations. All new compounds (1-4) were evaluated for their anti-inflammatory activity on LPS-induced RAW264.7 macrophages, and cytotoxicity against five human cancer cell lines (HepG2, A-549, MDA-MB-231, HL-60, and SW-480). Compound 2 showed signicant inhibitory activity against NO production with an IC<sub>50</sub> value of 16.41 ± 0.48 μM, better than that of L-NMMA (positive control, IC<sub>50</sub> = 42.83 ± 0.80 μM), while compound 1 exhibited comparable anti-inflammatory activity with IC<sub>50</sub> value of 47.50 ± 0.46 μM. Furthermore, compound 1 was also found to display selective cytotoxicity against human cancer cell line HepG2 with an inhibition rate of 79.09 % at 40.0 μM.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"181 ","pages":"106384"},"PeriodicalIF":2.5,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946896","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 : 2025-01-06DOI: 10.1016/j.fitote.2025.106379
Xiaolan Liu, Zhikun Zang, Rong Ji, Zhibin Wang
Aralia Linn. Plants (ALPs) is a member of the Araliaceae family, a genus of more than thirty species, some plants of Aralia Linn are commonly used as herbal medicines. ALPs is commonly utilized for relieving the symptoms of neurasthenia, rheumatoid arthritis, etc. The principal extraction approaches of polysaccharides of ALPs (AEP) encompass water extraction, ultrasonic-assisted, compound enzyme and microwave-assisted. Various extraction approaches and extraction conditions will affect the extraction rate and purity of the AEP. AEP is mainly composed of arabinose (Ara), galactose (Gal), rhamnose (Rha), xylose (Xyl) and so on with different proportions of monosaccharides. AEP is one of the principal active components of ALPs, which has a variety of biological activities. Studies have shown that activities of AEP are anti-tumor, cardioprotective, hepatoprotective, anti-radiation, and hypoglycemic. One of the anti-tumor mechanisms of AEP is mitochondrial apoptosis pathway, and its regulatory process is described in detail. This review mainly summarizes the researches on extraction, separation, structural characterization and pharmacological activities of some AEP both the latest local and international in recent years. It lays a foundation for clinical safety application and the broadening of the application scope.
{"title":"Extraction, purification, structural characterization, and biological activity of polysaccharides from Aralia: A review.","authors":"Xiaolan Liu, Zhikun Zang, Rong Ji, Zhibin Wang","doi":"10.1016/j.fitote.2025.106379","DOIUrl":"10.1016/j.fitote.2025.106379","url":null,"abstract":"<p><p>Aralia Linn. Plants (ALPs) is a member of the Araliaceae family, a genus of more than thirty species, some plants of Aralia Linn are commonly used as herbal medicines. ALPs is commonly utilized for relieving the symptoms of neurasthenia, rheumatoid arthritis, etc. The principal extraction approaches of polysaccharides of ALPs (AEP) encompass water extraction, ultrasonic-assisted, compound enzyme and microwave-assisted. Various extraction approaches and extraction conditions will affect the extraction rate and purity of the AEP. AEP is mainly composed of arabinose (Ara), galactose (Gal), rhamnose (Rha), xylose (Xyl) and so on with different proportions of monosaccharides. AEP is one of the principal active components of ALPs, which has a variety of biological activities. Studies have shown that activities of AEP are anti-tumor, cardioprotective, hepatoprotective, anti-radiation, and hypoglycemic. One of the anti-tumor mechanisms of AEP is mitochondrial apoptosis pathway, and its regulatory process is described in detail. This review mainly summarizes the researches on extraction, separation, structural characterization and pharmacological activities of some AEP both the latest local and international in recent years. It lays a foundation for clinical safety application and the broadening of the application scope.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106379"},"PeriodicalIF":2.5,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946844","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 : 2025-01-06DOI: 10.1016/j.fitote.2025.106382
Lu Cao, Jiaxuan Guo, Junfeng Tan, Yu Mu, Yi Jiang, Xueshi Huang, Li Han
Fifteen new aliphatic metabolites, 2-methylpyrimidin-4(3H)-ones (1,2), 2-methoxy-2-methyl-1,2-dihydro-3H-pyrrol-3-ones (4a/4b, 5a/5b), butyrolactones (6-9), and aliphatic metabolites (16-20) as well as known pyridin-2(1H)-one (3) and butyrolactone analogues (10-15) were obtained from the fermentation broth of Streptomyces antifungus isolated from the forest soil sample collected in Tengchong, China. Pyrimidin-4(3H)-one derivatives (1, 2) with an individual 2-methylpyrimidin-4(3H)-one skeleton is a kind of rarely reported compound and were firstly obtained from natural source. The structures of the new metabolites were elucidated by comprehensive spectroscopic analysis including data from experimental and calculated ECD spectra as well as Mosher's reagent derivative method. Compounds 1, 2, 18, and 19 exhibited optimal activity against Staphylococcus aureus with MIC values ranged from 12.5 to 50 μg/mL. Further investigation revealed that 1 effectively inhibited biofilm formation and destroyed the preformed biofilm of S. aureus through oxidative damage, thereby exerting antibacterial effect.
{"title":"Discovery of new aliphatic metabolites with antibacterial activities from a soil-derived Streptomyces antifungus.","authors":"Lu Cao, Jiaxuan Guo, Junfeng Tan, Yu Mu, Yi Jiang, Xueshi Huang, Li Han","doi":"10.1016/j.fitote.2025.106382","DOIUrl":"10.1016/j.fitote.2025.106382","url":null,"abstract":"<p><p>Fifteen new aliphatic metabolites, 2-methylpyrimidin-4(3H)-ones (1,2), 2-methoxy-2-methyl-1,2-dihydro-3H-pyrrol-3-ones (4a/4b, 5a/5b), butyrolactones (6-9), and aliphatic metabolites (16-20) as well as known pyridin-2(1H)-one (3) and butyrolactone analogues (10-15) were obtained from the fermentation broth of Streptomyces antifungus isolated from the forest soil sample collected in Tengchong, China. Pyrimidin-4(3H)-one derivatives (1, 2) with an individual 2-methylpyrimidin-4(3H)-one skeleton is a kind of rarely reported compound and were firstly obtained from natural source. The structures of the new metabolites were elucidated by comprehensive spectroscopic analysis including data from experimental and calculated ECD spectra as well as Mosher's reagent derivative method. Compounds 1, 2, 18, and 19 exhibited optimal activity against Staphylococcus aureus with MIC values ranged from 12.5 to 50 μg/mL. Further investigation revealed that 1 effectively inhibited biofilm formation and destroyed the preformed biofilm of S. aureus through oxidative damage, thereby exerting antibacterial effect.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106382"},"PeriodicalIF":2.5,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946830","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 : 2025-01-06DOI: 10.1016/j.fitote.2025.106377
Cansel Çelik, Özge Doğa İdiş, Yağmur Özhan, Dilruba Tirpanlar, Naz Unal, Burcin Gungor, Başak Aru, Enise Ece Gurdal, Wolfgang Sippl, Hande Sipahi, Hasan Kırmızıbekmez
As a result of anti-inflammatory activity-guided fractionation, 16 secondary metabolites from the underground parts of Valeriana phu L. were obtained, including five new ones belonging to iridoid (1, 2, and 5), phenylpropanoid (6) and neolignan (7) chemical classes. Their structures were elucidated by 1D and 2D NMR analyses as well as HRESIMS. The in vitro anti-inflammatory activities of the extract, fractions and isolates were evaluated through NO inhibition assay on LPS-induced RAW 264.7 cells. Compounds 1-3, 7-9, 11, 13, and 16 which significantly inhibited the nitrite release (IC50 14.94-94.81 μM) were also assessed for their reducing capacity on TNF-α, IL-1β, IL-6, PGE2 and COX-2 production. Compounds 3, 8, and 16 inhibited LPS induced iNOS expression levels in Western blotting. Molecular docking studies for the active compounds targeting iNOS, TNF-α and COX-2 were also carried out. Moreover, compounds with remarkable anti-inflammatory activities were tested for their potential cytotoxicity against breast (MCF-7 and MDA-MB-231), glioblastoma (U87 and A172), pancreas (MIA PaCa-2 and PANC-1), hepatocellular (Mahlavu and Hep3B) cancer cell lines by WST-8. Compounds, 7, 8, and 16 showed significant cytotoxicity against A172 and PANC-1 cell lines (IC50 18.3-21.8 μM) via causing cell cycle arrest, especially in the G2/M phase and triggering the apoptotic pathway.
{"title":"Isolation of anti-inflammatory and cytotoxic secondary metabolites from Valeriana phu and evaluation of their mechanisms of action.","authors":"Cansel Çelik, Özge Doğa İdiş, Yağmur Özhan, Dilruba Tirpanlar, Naz Unal, Burcin Gungor, Başak Aru, Enise Ece Gurdal, Wolfgang Sippl, Hande Sipahi, Hasan Kırmızıbekmez","doi":"10.1016/j.fitote.2025.106377","DOIUrl":"10.1016/j.fitote.2025.106377","url":null,"abstract":"<p><p>As a result of anti-inflammatory activity-guided fractionation, 16 secondary metabolites from the underground parts of Valeriana phu L. were obtained, including five new ones belonging to iridoid (1, 2, and 5), phenylpropanoid (6) and neolignan (7) chemical classes. Their structures were elucidated by 1D and 2D NMR analyses as well as HRESIMS. The in vitro anti-inflammatory activities of the extract, fractions and isolates were evaluated through NO inhibition assay on LPS-induced RAW 264.7 cells. Compounds 1-3, 7-9, 11, 13, and 16 which significantly inhibited the nitrite release (IC<sub>50</sub> 14.94-94.81 μM) were also assessed for their reducing capacity on TNF-α, IL-1β, IL-6, PGE2 and COX-2 production. Compounds 3, 8, and 16 inhibited LPS induced iNOS expression levels in Western blotting. Molecular docking studies for the active compounds targeting iNOS, TNF-α and COX-2 were also carried out. Moreover, compounds with remarkable anti-inflammatory activities were tested for their potential cytotoxicity against breast (MCF-7 and MDA-MB-231), glioblastoma (U87 and A172), pancreas (MIA PaCa-2 and PANC-1), hepatocellular (Mahlavu and Hep3B) cancer cell lines by WST-8. Compounds, 7, 8, and 16 showed significant cytotoxicity against A172 and PANC-1 cell lines (IC<sub>50</sub> 18.3-21.8 μM) via causing cell cycle arrest, especially in the G2/M phase and triggering the apoptotic pathway.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106377"},"PeriodicalIF":2.5,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946848","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}