Pub Date : 2025-12-25DOI: 10.1016/j.fitote.2025.107066
Nilofar , Gunes Ak , Enver Saka , Gokhan Zengin , Cziaky Zoltan , Josef Jeko , Annalisa Chiavaroli , Simonetta Cristina Di Simone , Mariachiara Gabriele , Maria Loreta Libero , Giustino Orlando , Luigi Menghini , Claudio Ferrante , Jasmina Glamočlija , Mladen Rajaković , Evren Yildiztugay , Meng-Yao Li
Since ancient times, plants have been used as a valuable source for treating serious diseases. Three different plants, namely Aubrieta pinardii, Johrenia dichotoma, and Malabaila dasyantha were used and extracted using the extraction solvents ethyl acetate (EA), methanol (MeOH), and water. Antioxidant activity was determined using several in vitro assays. Subsequently, the enzyme inhibition activities of the extracts were evaluated against cholinesterases (AChE and BChE), tyrosinase, amylase, and glucosidase. The antibacterial and antifungal effects of the extracts were assessed. Methanol extracts of A. pinardii, J. dichotoma, and M. dasyantha yielded the highest total flavonoids (TFC) compared to EA and water extracts. The analysis using HPLC-ESI-Q-TOF-MS identified various classes of phytochemicals within the species examined. Aubrieta pinardii extracts were abundant in glucosinolates, whereas J. dichotoma and M. dasyantha extracts were characterized by the presence of coumarins and furanocoumarins. The EA extracts exhibited greater inhibition of microorganism growth compared with MeOH and water extracts. Notably, J. dichotoma showed similar or superior antifungal activity against A. niger (MIC/MFC 0.25/0.50 mg/mL) and M. dasyantha demonstrated comparable efficacy against T. viride (MIC/MFC 0.50/1.00 mg/mL) and P. verrucosum var. cyclopium (MIC/MFC 0.125/0.25 mg/mL) when benchmarked against the reference drug ketoconazole. These results provide valuable information about A. pinardii, J. dichotoma, and M. dasyantha chemical profiles and underline the importance of selecting appropriate solvents for the extraction of metabolites from plant matrix for potential applications in the treatment of various diseases.
自古以来,植物就被用作治疗严重疾病的宝贵资源。采用三种不同的植物,即红毛赤杨(Aubrieta pinardii)、二叉菊(Johrenia dichotoma)和马拉贝拉(Malabaila dasyantha),分别用乙酸乙酯(EA)、甲醇(MeOH)和水进行提取。采用几种体外测定法测定其抗氧化活性。随后,研究了提取物对胆碱酯酶(AChE和BChE)、酪氨酸酶、淀粉酶和葡萄糖苷酶的抑制活性。评价了各提取物的抗菌和抗真菌作用。与EA和水提取物相比,pinardii, J. dichotoma和M. dasyantha甲醇提取物的总黄酮(TFC)含量最高。HPLC-ESI-Q-TOF-MS分析鉴定出不同种类的植物化学物质。红毛紫苏提取物中硫苷含量较高,而双花紫苏和大花紫苏提取物中主要含有香豆素和呋喃香豆素。与MeOH和水提取物相比,EA提取物对微生物生长的抑制作用更大。值得注意的是,当与对照药物酮康唑作对照时,J. dichotoma对黑曲霉(MIC/MFC 0.25/0.50 mg/mL)和M. dasyantha对T. viride (MIC/MFC 0.50/1.00 mg/mL)和P. verrucosum var. cyclopium (MIC/MFC 0.125/0.25 mg/mL)表现出相似或更好的抗真菌活性。这些结果为pinardii, J. dichotoma和M. dasyantha的化学特征提供了有价值的信息,并强调了选择合适的溶剂从植物基质中提取代谢物的重要性,以潜在地应用于治疗各种疾病。
{"title":"Multi-faceted bioactivity of three unexplored Turkish plants: A comparative phytochemical and pharmacological profiling","authors":"Nilofar , Gunes Ak , Enver Saka , Gokhan Zengin , Cziaky Zoltan , Josef Jeko , Annalisa Chiavaroli , Simonetta Cristina Di Simone , Mariachiara Gabriele , Maria Loreta Libero , Giustino Orlando , Luigi Menghini , Claudio Ferrante , Jasmina Glamočlija , Mladen Rajaković , Evren Yildiztugay , Meng-Yao Li","doi":"10.1016/j.fitote.2025.107066","DOIUrl":"10.1016/j.fitote.2025.107066","url":null,"abstract":"<div><div>Since ancient times, plants have been used as a valuable source for treating serious diseases. Three different plants, namely <em>Aubrieta pinardii</em>, <em>Johrenia dichotoma</em>, and <em>Malabaila dasyantha</em> were used and extracted using the extraction solvents ethyl acetate (EA), methanol (MeOH), and water. Antioxidant activity was determined using several in vitro assays. Subsequently, the enzyme inhibition activities of the extracts were evaluated against cholinesterases (AChE and BChE), tyrosinase, amylase, and glucosidase. The antibacterial and antifungal effects of the extracts were assessed. Methanol extracts of <em>A</em>. <em>pinardii</em>, <em>J</em>. <em>dichotoma</em>, and <em>M</em>. <em>dasyantha</em> yielded the highest total flavonoids (TFC) compared to EA and water extracts. The analysis using HPLC-ESI-Q-TOF-MS identified various classes of phytochemicals within the species examined. <em>Aubrieta pinardii</em> extracts were abundant in glucosinolates, whereas <em>J. dichotoma</em> and <em>M. dasyantha</em> extracts were characterized by the presence of coumarins and furanocoumarins. The EA extracts exhibited greater inhibition of microorganism growth compared with MeOH and water extracts. Notably, <em>J. dichotoma</em> showed similar or superior antifungal activity against <em>A. niger</em> (MIC/MFC 0.25/0.50 mg/mL) and <em>M. dasyantha</em> demonstrated comparable efficacy against <em>T. viride</em> (MIC/MFC 0.50/1.00 mg/mL) and <em>P. verrucosum</em> var. <em>cyclopium</em> (MIC/MFC 0.125/0.25 mg/mL) when benchmarked against the reference drug ketoconazole. These results provide valuable information about <em>A</em>. <em>pinardii</em>, <em>J</em>. <em>dichotoma</em>, and <em>M</em>. <em>dasyantha</em> chemical profiles and underline the importance of selecting appropriate solvents for the extraction of metabolites from plant matrix for potential applications in the treatment of various diseases.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107066"},"PeriodicalIF":2.6,"publicationDate":"2025-12-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145846318","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 : 2025-12-25DOI: 10.1016/j.fitote.2025.107069
Jing Wang , Xue Zhang , Lu Chen , Jun Du , Xiaohong Wu , Liang Chen , Yingchun Wu , YiMing Li
Rubus chingii Hu, a food material with medicinal value, has been used to treat urinary system diseases, such as prostatitis, benign prostate hyperplasia (BPH) and lower urinary tract symptoms (LUTS). However, there is no research on the efficacy and mechanism of compounds of R. chingii. in treating BPH. In this study, 10 previously unreported ent-pimarane-type (rubuschinoside A–B, 1–2), ent-isopimarane-type (rubuschinoside CD, 3–4) and ent-labdane-type (goshonoside J16–21, 5–10) diterpene glycosides were isolated from the dried fruits of R. chingii. Their structures were elucidated and confirmed using high-resolution electrospray ionization mass spectrometry (HRESIMS), nuclear magnetic resonance spectroscopy (NMR), single crystal X-ray diffraction and electron capture detector (ECD). All compounds were tested for their apoptosis-inducing activity in BPH cells, and compounds 1, 3, 4 and 8 exhibited significant pro-apoptotic effects. Further apoptosis mechanistic studies on compound 8 revealed that it could increase the expression of Fas, FADD, caspase 3 and caspase 8 mRNA expression levels at 50 μM. Collectively, this study suggested that diterpenoid glycosides from R. Chingii may induce apoptosis in hyperplastic prostate cells through activation of the Fas/caspase-8 signaling cascade.
{"title":"Novel diterpenoid glycosides from Rubus chingii Hu induce apoptosis in BPH-1 cells through fas/caspase-8 pathway activation","authors":"Jing Wang , Xue Zhang , Lu Chen , Jun Du , Xiaohong Wu , Liang Chen , Yingchun Wu , YiMing Li","doi":"10.1016/j.fitote.2025.107069","DOIUrl":"10.1016/j.fitote.2025.107069","url":null,"abstract":"<div><div><em>Rubus chingii</em> Hu, a food material with medicinal value, has been used to treat urinary system diseases, such as prostatitis, benign prostate hyperplasia (BPH) and lower urinary tract symptoms (LUTS). However, there is no research on the efficacy and mechanism of compounds of <em>R. chingii</em>. in treating BPH. In this study, 10 previously unreported <em>ent</em>-pimarane-type (rubuschinoside A–B, <strong>1</strong>–<strong>2</strong>), <em>ent</em>-isopimarane-type (rubuschinoside C<img>D, <strong>3</strong>–<strong>4</strong>) an<em>d ent-</em>labdane<em>-</em>type (goshonoside J16–21, <strong>5</strong>–<strong>10</strong>) diterpene glycosides were isolated from the dried fruits of <em>R. chingii</em>. Their structures were elucidated and confirmed using high-resolution electrospray ionization mass spectrometry (HRESIMS), nuclear magnetic resonance spectroscopy (NMR), single crystal X-ray diffraction and electron capture detector (ECD). All compounds were tested for their apoptosis-inducing activity in BPH cells, and compounds <strong>1</strong>, <strong>3</strong>, <strong>4</strong> and <strong>8</strong> exhibited significant pro-apoptotic effects. Further apoptosis mechanistic studies on compound <strong>8</strong> revealed that it could increase the expression of Fas, FADD, caspase 3 and caspase 8 mRNA expression levels at 50 μM. Collectively, this study suggested that diterpenoid glycosides from <em>R. Chingii</em> may induce apoptosis in hyperplastic prostate cells through activation of the Fas/caspase-8 signaling cascade.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107069"},"PeriodicalIF":2.6,"publicationDate":"2025-12-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145838638","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 : 2025-12-25DOI: 10.1016/j.fitote.2025.107072
Xiaoli Li , Zejun Liu , Qiuyi Jing , Hong Pan , Fuguo Shi
Monotropein, an iridoid glycoside, is the principal bioactive constituent with the highest amount isolated from Morindae officinalis radix, which has been reported to have potent pharmacological properties. Monotropein contains a hemiacetal structure. The hemiacetal may be converted into a reactive dialdehyde intermediate and covalently bind to the primary amine. Therefore, we speculated that the metabolites of monotropein with hemiacetal can generate dialdehyde intermediates, a class of highly reactive metabolites that enable covalent modification of proteins. This study characterized the metabolic profiling of monotropein, especially the unstable dialdehyde intermediates, using UPLC-Q/Orbitrap MS. A total of eighteen stable metabolites were characterized in monotropein-treated rats. The main metabolic pathways were dehydration, deglycosylation, and decarboxylation. It is noteworthy that six unstable dialdehyde intermediates of monotropein were characterized for the first time. They were the hemiacetal ring-opening products of M4 (monotropein aglycone), M5 (decarboxylated aglycone), M6 (methylated aglycone), M7 (dehydrated aglycone), M8 (hydrogenated aglycone), and M9 (dehydroxymethyl aglycone). The dialdehyde intermediates were identified by their stable dihydropyridine conjugates with amino acids. Five dialdehyde intermediates enabled covalent modification of proteins in the intestine. In conclusion, eighteen stable metabolites and six reactive dialdehyde intermediates were characterized in this study, which contributes to understanding the pharmacological effects of monotropein.
{"title":"Formation of series reactive dialdehyde intermediates by metabolism of monotropein","authors":"Xiaoli Li , Zejun Liu , Qiuyi Jing , Hong Pan , Fuguo Shi","doi":"10.1016/j.fitote.2025.107072","DOIUrl":"10.1016/j.fitote.2025.107072","url":null,"abstract":"<div><div>Monotropein, an iridoid glycoside, is the principal bioactive constituent with the highest amount isolated from <em>Morindae officinalis</em> radix, which has been reported to have potent pharmacological properties. Monotropein contains a hemiacetal structure. The hemiacetal may be converted into a reactive dialdehyde intermediate and covalently bind to the primary amine. Therefore, we speculated that the metabolites of monotropein with hemiacetal can generate dialdehyde intermediates, a class of highly reactive metabolites that enable covalent modification of proteins. This study characterized the metabolic profiling of monotropein, especially the unstable dialdehyde intermediates, using UPLC-Q/Orbitrap MS. A total of eighteen stable metabolites were characterized in monotropein-treated rats. The main metabolic pathways were dehydration, deglycosylation, and decarboxylation. It is noteworthy that six unstable dialdehyde intermediates of monotropein were characterized for the first time. They were the hemiacetal ring-opening products of M4 (monotropein aglycone), M5 (decarboxylated aglycone), M6 (methylated aglycone), M7 (dehydrated aglycone), M8 (hydrogenated aglycone), and M9 (dehydroxymethyl aglycone). The dialdehyde intermediates were identified by their stable dihydropyridine conjugates with amino acids. Five dialdehyde intermediates enabled covalent modification of proteins in the intestine. In conclusion, eighteen stable metabolites and six reactive dialdehyde intermediates were characterized in this study, which contributes to understanding the pharmacological effects of monotropein.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107072"},"PeriodicalIF":2.6,"publicationDate":"2025-12-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145838640","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 : 2025-12-24DOI: 10.1016/j.fitote.2025.107065
Huan Yan , Yong-Sheng Zhou , Long-Gao Xiao , Wei Ni , Yupeng Geng , Hai-Yang Liu
The phytochemical reinvestigation on the whole plants of Chloranthus holostegius led to the isolation of five undescribed sesquiterpenes (named chloranholosins U-Y, 1–5), including two lindenane-type sesquiterpenes, two acorane-type sesquiterpenes, and one elemane-type sesquiterpene, together with 30 known compounds. Their structures and absolute configurations were elucidated by a comprehensive method including the spectroscopic data, and electronic circular dichroism (ECD) calculations. Chloranholosin U (1) was elucidated as a rare lindenane–dinormonotepenoid hybrid with an oxa-difuranofurone moiety. Furthermore, all new isolates and 18 known compounds were evaluated for their inhibitory activity against LPS-induced nitric oxide (NO) production in RAW 264.7 macrophage cells, while their cytotoxic activities were also assessed against five human tumor cell lines. Though these compounds did not show inhibitory activity for NO production, compounds 16, 34, and 35 displayed moderate cytotoxicity. Compound 16 showed cytotoxicity against HL-60, HepG2, MDA-MB-231, and SW480 (IC50 10.98–36.48 μM), compounds 34 and 35 were active on HL-60 (IC50 18.98 and 14.89 μM), and 34 also inhibited A549 (IC50 24.32 μM).
{"title":"Terpenoids from the whole plants of Chloranthus holostegius","authors":"Huan Yan , Yong-Sheng Zhou , Long-Gao Xiao , Wei Ni , Yupeng Geng , Hai-Yang Liu","doi":"10.1016/j.fitote.2025.107065","DOIUrl":"10.1016/j.fitote.2025.107065","url":null,"abstract":"<div><div>The phytochemical reinvestigation on the whole plants of <em>Chloranthus holostegius</em> led to the isolation of five undescribed sesquiterpenes (named chloranholosins U-Y, <strong>1</strong>–<strong>5</strong>), including two lindenane-type sesquiterpenes, two acorane-type sesquiterpenes, and one elemane-type sesquiterpene, together with 30 known compounds. Their structures and absolute configurations were elucidated by a comprehensive method including the spectroscopic data, and electronic circular dichroism (ECD) calculations. Chloranholosin U (<strong>1</strong>) was elucidated as a rare lindenane–dinormonotepenoid hybrid with an oxa-difuranofurone moiety. Furthermore, all new isolates and 18 known compounds were evaluated for their inhibitory activity against LPS-induced nitric oxide (NO) production in RAW 264.7 macrophage cells, while their cytotoxic activities were also assessed against five human tumor cell lines. Though these compounds did not show inhibitory activity for NO production, compounds <strong>16</strong>, <strong>34</strong>, and <strong>35</strong> displayed moderate cytotoxicity. Compound <strong>16</strong> showed cytotoxicity against HL-60, HepG2, MDA-MB-231, and SW480 (IC<sub>50</sub> 10.98–36.48 μM), compounds <strong>34</strong> and <strong>35</strong> were active on HL-60 (IC<sub>50</sub> 18.98 and 14.89 μM), and <strong>34</strong> also inhibited A549 (IC<sub>50</sub> 24.32 μM).</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107065"},"PeriodicalIF":2.6,"publicationDate":"2025-12-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145838639","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}
Five previously undescribed triterpenoids (1–5), and four triterpenoids (6–9) which had been synthesized previously but had not been isolated from a natural source, along with twenty-three known triterpenoids (10−32) were isolated from the methanol extract of dammar resin of Vatica mangachapoi. HRESIMS, NMR, UV, and ECD spectroscopy were employed to determine the structures of these triterpenoids. Compounds 2, 6, 22, and 29 significantly reduced LPS-induced TNF-α levels in RAW264.7 cells, while compounds 3, 13, 16, and 17 reduced IL-6 levels at a concentration of 10 μM. These results suggest that these compounds exhibit potential anti-inflammatory activity.
{"title":"Anti-inflammatory triterpenoids from dammar resin of Vatica mangachapoi","authors":"Rui-Jie Feng , De-Li Chen , Jian-He Wei , Hui Meng , Yun Yang","doi":"10.1016/j.fitote.2025.107056","DOIUrl":"10.1016/j.fitote.2025.107056","url":null,"abstract":"<div><div>Five previously undescribed triterpenoids (<strong>1</strong>–<strong>5</strong>), and four triterpenoids (<strong>6</strong>–<strong>9</strong>) which had been synthesized previously but had not been isolated from a natural source, along with twenty-three known triterpenoids (<strong>10</strong>−<strong>32</strong>) were isolated from the methanol extract of dammar resin of <em>Vatica mangachapoi</em>. HRESIMS, NMR, UV, and ECD spectroscopy were employed to determine the structures of these triterpenoids. Compounds <strong>2</strong>, <strong>6</strong>, <strong>22,</strong> and <strong>29</strong> significantly reduced LPS-induced TNF-α levels in RAW264.7 cells, while compounds <strong>3</strong>, <strong>13</strong>, <strong>16,</strong> and <strong>17</strong> reduced IL-6 levels at a concentration of 10 μM. These results suggest that these compounds exhibit potential anti-inflammatory activity.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107056"},"PeriodicalIF":2.6,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145833349","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 : 2025-12-23DOI: 10.1016/j.fitote.2025.107041
Aline Aparecida Macedo Marques , Karyne Garcia Tafarelo Moreno , Luciane Barbosa Pessoa , Luana Ale Bertoncello Pael , Katiana Simões Kittelson , Ariany Carvalho dos Santos , Gabriela Pereira da Silva , Bianca Viana Silva , Maria Luiza Fidelis da Silva , Luana Bonifácio Sanches , Denise Brentan da Silva , Arquimedes Gasparotto Junior
The therapeutic management of hypertension involves both pharmacological and non-pharmacological interventions. However, control remains inadequate despite effective treatments, often due to poor adherence. In this context, herbal medicines offer a complementary approach to conventional therapy. Citrullus lanatus (watermelon) seeds, frequently discarded as agricultural byproducts, represent a promising source of bioactive compounds. This study evaluated the cardiorenal properties of three extracts obtained from dried C. lanatus seeds, including an ethanol-soluble fraction from an aqueous extract (ESCL), a hydroethanolic extract, and an aqueous extract obtained by turbolysis. These extracts were chemically characterized using liquid chromatography coupled with diode array detection and mass spectrometry. Diuretic and hypotensive activities were assessed in vivo in normotensive female Wistar rats, while vasodilatory mechanisms were investigated ex vivo in isolated mesenteric vascular beds. Among the preparations screened, only the ESCL fraction displayed significant cardiorenal activity, reducing blood pressure and peripheral vascular resistance. Mechanistic investigation revealed that this vascular response is mediated via the nitric oxide/soluble guanylate cyclase/cyclic guanosine monophosphate signaling cascade. These findings highlight the pharmacological potential of ESCL as a candidate for the development of novel hypotensive agents.
{"title":"Involvement of the NO-sGC/cGMP signaling pathway in the vasodilator and hypotensive effects of the ethanol-soluble fraction from Citrullus lanatus (Thunb.) Matsum. & Nakai seeds in rats","authors":"Aline Aparecida Macedo Marques , Karyne Garcia Tafarelo Moreno , Luciane Barbosa Pessoa , Luana Ale Bertoncello Pael , Katiana Simões Kittelson , Ariany Carvalho dos Santos , Gabriela Pereira da Silva , Bianca Viana Silva , Maria Luiza Fidelis da Silva , Luana Bonifácio Sanches , Denise Brentan da Silva , Arquimedes Gasparotto Junior","doi":"10.1016/j.fitote.2025.107041","DOIUrl":"10.1016/j.fitote.2025.107041","url":null,"abstract":"<div><div>The therapeutic management of hypertension involves both pharmacological and non-pharmacological interventions. However, control remains inadequate despite effective treatments, often due to poor adherence. In this context, herbal medicines offer a complementary approach to conventional therapy. <em>Citrullus lanatus</em> (watermelon) seeds, frequently discarded as agricultural byproducts, represent a promising source of bioactive compounds. This study evaluated the cardiorenal properties of three extracts obtained from dried <em>C. lanatus</em> seeds, including an ethanol-soluble fraction from an aqueous extract (ESCL), a hydroethanolic extract, and an aqueous extract obtained by turbolysis. These extracts were chemically characterized using liquid chromatography coupled with diode array detection and mass spectrometry. Diuretic and hypotensive activities were assessed in vivo in normotensive female Wistar rats, while vasodilatory mechanisms were investigated ex vivo in isolated mesenteric vascular beds. Among the preparations screened, only the ESCL fraction displayed significant cardiorenal activity, reducing blood pressure and peripheral vascular resistance. Mechanistic investigation revealed that this vascular response is mediated via the nitric oxide/soluble guanylate cyclase/cyclic guanosine monophosphate signaling cascade. These findings highlight the pharmacological potential of ESCL as a candidate for the development of novel hypotensive agents.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107041"},"PeriodicalIF":2.6,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145833318","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 : 2025-12-23DOI: 10.1016/j.fitote.2025.107043
Bin Liu , Yang Xu , Lingxiao Ren , Xiaofen Liu , Lixia Chen , Hua Li
The seeds of Dimocarpus longan Lour. are rich in bioactive compounds, notably polyphenols, flavonoids, and sesquiterpenoids, which have demonstrated antioxidant, antitumor, and antifungal activities. Phytochemical investigation of the seeds led to the isolation of thirteen compounds (1−13), comprising six previously undescribed structures (1–6) and seven known analogues (7–13). The structures of the new compounds were elucidated through comprehensive spectroscopic analysis, including 1D/2D NMR, HR-ESI-MS, UV, ECD, and optical rotation. All isolated compounds were evaluated for their protective effects against hydrogen peroxide-induced oxidative stress in BV-2 microglial cells. Among them, compounds 2, 3, 7, 11, and 12 exhibited significant antioxidant activity. These findings underscore the potential of Dimocarpus longan seeds as a valuable source of bioactive agents for medicinal and functional food applications.
{"title":"Antioxidant active ingredients from the seeds of Dimocarpus longan Lour","authors":"Bin Liu , Yang Xu , Lingxiao Ren , Xiaofen Liu , Lixia Chen , Hua Li","doi":"10.1016/j.fitote.2025.107043","DOIUrl":"10.1016/j.fitote.2025.107043","url":null,"abstract":"<div><div>The seeds of <em>Dimocarpus longan</em> Lour. are rich in bioactive compounds, notably polyphenols, flavonoids, and sesquiterpenoids, which have demonstrated antioxidant, antitumor, and antifungal activities. Phytochemical investigation of the seeds led to the isolation of thirteen compounds (<strong>1−13</strong>), comprising six previously undescribed structures (<strong>1–6</strong>) and seven known analogues (<strong>7–13</strong>). The structures of the new compounds were elucidated through comprehensive spectroscopic analysis, including 1D/2D NMR, HR-ESI-MS, UV, ECD, and optical rotation. All isolated compounds were evaluated for their protective effects against hydrogen peroxide-induced oxidative stress in BV-2 microglial cells. Among them, compounds <strong>2</strong>, <strong>3</strong>, <strong>7</strong>, <strong>11</strong>, and <strong>12</strong> exhibited significant antioxidant activity. These findings underscore the potential of <em>Dimocarpus longan</em> seeds as a valuable source of bioactive agents for medicinal and functional food applications.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107043"},"PeriodicalIF":2.6,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145833369","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 : 2025-12-23DOI: 10.1016/j.fitote.2025.107046
Yu-Ying Liu , Chan-Ting Lai , Salman Khan , Qian-Jing Zheng , Rong Zhang , Wei-Yi Wang , Bin Wu , Shan He , Li Yang , Ting-Ting Wang
One undescribed quinoline derivative, xylaminoquin A (1), one new p-aminobenzoic acid derivative, xylamidate B (2), and methyl 4-(butanoylamino)-3-hydroxybenzoate, reported for the first time as a natural product and named xylamidate C (3), together with known alkaloids and diketopiperazines, methyl 4-acetylamino-3-hydroxybenzoate (4), methyl 4-[(1-oxobutyl)amino]benzoate (5), pseurotin A (6), azaspirofuran A (7), cyclo(l-Tyr-l-Leu) (8), and cyclo-(l-Tyr-l-Val) (9) were isolated from Xylaria sp. NBUF245, a fungus associated with a Demosponge sp. collected from the marine mesophotic zone. Structurally, compound 1 is the first example of 3,7-dissubstitented quinoline derivative isolated from fungi. The structures of all compounds were elucidated by combined analysis of spectroscopic data and X-ray crystallography. Bioassay results showed that compound 5 effectively prevented prednisolone-induced bone loss in zebrafish at a concentration of 30 μM, suggesting potential osteoprotective activity.
{"title":"Quinoline and para-aminobenzoic acid derivatives with anti-osteoclastic activity from a marine mesophotic zone Demosponge sponge-associated fungus Xylaria sp. NBUF245","authors":"Yu-Ying Liu , Chan-Ting Lai , Salman Khan , Qian-Jing Zheng , Rong Zhang , Wei-Yi Wang , Bin Wu , Shan He , Li Yang , Ting-Ting Wang","doi":"10.1016/j.fitote.2025.107046","DOIUrl":"10.1016/j.fitote.2025.107046","url":null,"abstract":"<div><div>One undescribed quinoline derivative, xylaminoquin A (<strong>1</strong>), one new <em>p</em>-aminobenzoic acid derivative, xylamidate B (<strong>2</strong>), and methyl 4-(butanoylamino)-3-hydroxybenzoate, reported for the first time as a natural product and named xylamidate C (<strong>3</strong>), together with known alkaloids and diketopiperazines, methyl 4-acetylamino-3-hydroxybenzoate (<strong>4</strong>), methyl 4-[(1-oxobutyl)amino]benzoate (<strong>5</strong>), pseurotin A (<strong>6</strong>), azaspirofuran A (<strong>7</strong>), cyclo(<span>l</span>-Tyr-<span>l</span>-Leu) (<strong>8</strong>), and cyclo-(<span>l</span>-Tyr-<span>l</span>-Val) (<strong>9</strong>) were isolated from <em>Xylaria</em> sp. NBUF245, a fungus associated with a <em>Demosponge</em> sp. collected from the marine mesophotic zone. Structurally, compound <strong>1</strong> is the first example of 3,7-dissubstitented quinoline derivative isolated from fungi. The structures of all compounds were elucidated by combined analysis of spectroscopic data and X-ray crystallography. Bioassay results showed that compound <strong>5</strong> effectively prevented prednisolone-induced bone loss in zebrafish at a concentration of 30 μM, suggesting potential osteoprotective activity.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107046"},"PeriodicalIF":2.6,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145833376","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 : 2025-12-22DOI: 10.1016/j.fitote.2025.107051
Ke Xu , Xiao-Bin Li , Yu-Liang Xu , Fei Xie , Hong-Xiang Lou
Inclusion of the histone deacetylase (HDAC) inhibitor suberoylanilide hydroxamic acid (SAHA) into the culture medium of the endolichenic fungus Phialocephala fortinii resulted in the separation of three new perylenequinones phialocephalarins E-G (1–3) and enhanced the production of the known compounds phialocephalarins A-B (4–5). A comprehensive spectral analysis combined with electron circular dichroism (ECD) data has elucidated their structures. Phialocephalarin E (1) displayed anti-inflammatory activity with the maximum inhibition rate of 57.3 % ± 7.3 % (50 μM). Further molecular docking experiment revealed the affinity degree of compound 1 to the prostaglandin E2 receptor 4 (EP4R) and the molecular dynamics (MD) simulation results showed compound 1-EP4R complex had relatively good binding stability.
{"title":"Anti-inflammatory perylenequinones from the endolichenic fungus Phialocephala fortinii triggered by a histone deacetylase inhibitor","authors":"Ke Xu , Xiao-Bin Li , Yu-Liang Xu , Fei Xie , Hong-Xiang Lou","doi":"10.1016/j.fitote.2025.107051","DOIUrl":"10.1016/j.fitote.2025.107051","url":null,"abstract":"<div><div>Inclusion of the histone deacetylase (HDAC) inhibitor suberoylanilide hydroxamic acid (SAHA) into the culture medium of the endolichenic fungus <em>Phialocephala fortinii</em> resulted in the separation of three new perylenequinones phialocephalarins <em>E</em>-G (<strong>1</strong>–<strong>3</strong>) and enhanced the production of the known compounds phialocephalarins A-B (<strong>4</strong>–<strong>5)</strong>. A comprehensive spectral analysis combined with electron circular dichroism (ECD) data has elucidated their structures. Phialocephalarin E (<strong>1</strong>) displayed anti-inflammatory activity with the maximum inhibition rate of 57.3 % ± 7.3 % (50 μM). Further molecular docking experiment revealed the affinity degree of compound <strong>1</strong> to the prostaglandin E2 receptor 4 (EP4R) and the molecular dynamics (MD) simulation results showed compound <strong>1</strong>-EP4R complex had relatively good binding stability.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107051"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827027","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-22DOI: 10.1016/j.fitote.2025.107049
Zhiguo Mao , Xingyi Yang , Ying Liu , Yu Huan , Yixue Gao , Jinying Zhang , Xiangke Lin , Shuo Tian , Yagang Song , Mingsan Miao
Background
Prunella vulgaris L. is a traditional Chinese medicine known for its ability to disperse nodules and reduce swelling. However, research on the effect of the volatile oil from Prunella vulgaris L. on pulmonary nodulosis remains limited.
Aim of the study
To investigate whether essential oil from Prunella vulgaris L. (PVEO) improves pulmonary function in PS mice by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway.
Methods
Network pharmacology was used to explore how PVEO might treat PS. GC–MS identified PVEO's chemical components. A PS mouse model was created using Propionibacterium acnes. ELISA measured inflammatory factors in the BALF and blood of these mice. Flow cytometry analyzed CD4+ T cell differentiation into TH1 and TH17 cells. Immunofluorescence assessed macrophage differentiation into M1 and M2 phenotypes and the expression of TLR4, MyD88, and NF-κB. PCR and WB were conducted to detect the expression of mRNAs and proteins related to the TLR4/MyD88/NF-κB pathway.
Results
Network pharmacology predictions indicated that the improvement of pulmonary function by PVEO in PS mice was associated with the TLR4/MyD88/NF-κB signaling pathway. PCR and western blot (WB) analyses demonstrated that PVEO inhibited the expression of relevant mRNAs and proteins within the TLR4/MyD88/NF-κB pathway. Immunofluorescence and flow cytometry assays suggested that PVEO suppressed the differentiation of M1 macrophages, TH1, and TH17 cells in lung tissues of PS mice.
Conclusion
PVEO exerts anti-PS effects by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway in macrophages.
背景:夏枯草(Prunella vulgaris L.)是一种以散瘤消肿著称的中药。然而,关于夏枯草挥发油对肺结节病的作用的研究还很有限。研究目的:探讨枯草精油(PVEO)是否通过抑制TLR4/MyD88/NF-κB通路介导的炎症,改善PS小鼠肺功能。方法:采用网络药理学方法探讨PVEO对PS的治疗作用,GC-MS鉴定PVEO的化学成分。采用痤疮丙酸杆菌建立小鼠PS模型。ELISA法测定这些小鼠的BALF和血液中的炎症因子。流式细胞术分析CD4+ T细胞向TH1和TH17细胞分化的情况。免疫荧光检测巨噬细胞向M1和M2表型分化及TLR4、MyD88和NF-κB的表达。采用PCR和WB检测TLR4/MyD88/NF-κB通路相关mrna和蛋白的表达情况。结果:网络药理学预测提示PVEO对PS小鼠肺功能的改善与TLR4/MyD88/NF-κB信号通路有关。PCR和western blot (WB)分析表明,PVEO抑制TLR4/MyD88/NF-κB通路相关mrna和蛋白的表达。免疫荧光和流式细胞术检测显示,PVEO可抑制PS小鼠肺组织中M1巨噬细胞、TH1和TH17细胞的分化。结论:PVEO通过抑制巨噬细胞TLR4/MyD88/NF-κB通路介导的炎症,发挥抗ps作用。
{"title":"Modulation of immune cell differentiation by Prunella vulgaris L. essential oil in pulmonary sarcoidosis treatment","authors":"Zhiguo Mao , Xingyi Yang , Ying Liu , Yu Huan , Yixue Gao , Jinying Zhang , Xiangke Lin , Shuo Tian , Yagang Song , Mingsan Miao","doi":"10.1016/j.fitote.2025.107049","DOIUrl":"10.1016/j.fitote.2025.107049","url":null,"abstract":"<div><h3>Background</h3><div><em>Prunella vulgaris</em> L. is a traditional Chinese medicine known for its ability to disperse nodules and reduce swelling. However, research on the effect of the volatile oil from <em>Prunella vulgaris</em> L. on pulmonary nodulosis remains limited.</div></div><div><h3>Aim of the study</h3><div>To investigate whether essential oil from <em>Prunella vulgaris</em> L. (PVEO) improves pulmonary function in PS mice by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway.</div></div><div><h3>Methods</h3><div>Network pharmacology was used to explore how PVEO might treat PS. GC–MS identified PVEO's chemical components. A PS mouse model was created using <em>Propionibacterium acnes</em>. ELISA measured inflammatory factors in the BALF and blood of these mice. Flow cytometry analyzed CD4<sup>+</sup> T cell differentiation into TH1 and TH17 cells. Immunofluorescence assessed macrophage differentiation into M1 and M2 phenotypes and the expression of TLR4, MyD88, and NF-κB. PCR and WB were conducted to detect the expression of mRNAs and proteins related to the TLR4/MyD88/NF-κB pathway.</div></div><div><h3>Results</h3><div>Network pharmacology predictions indicated that the improvement of pulmonary function by PVEO in PS mice was associated with the TLR4/MyD88/NF-κB signaling pathway. PCR and western blot (WB) analyses demonstrated that PVEO inhibited the expression of relevant mRNAs and proteins within the TLR4/MyD88/NF-κB pathway. Immunofluorescence and flow cytometry assays suggested that PVEO suppressed the differentiation of M1 macrophages, TH1, and TH17 cells in lung tissues of PS mice.</div></div><div><h3>Conclusion</h3><div>PVEO exerts anti-PS effects by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway in macrophages.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107049"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827020","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}