FitoterapiaPub Date : 2024-10-23DOI: 10.1016/j.fitote.2024.106269
{"title":"Two new abietane diterpenoids from Caryopteris trichosphaera","authors":"","doi":"10.1016/j.fitote.2024.106269","DOIUrl":"10.1016/j.fitote.2024.106269","url":null,"abstract":"<div><div>Two new abietane diterpenoids, cartrisine A (<strong>1</strong>) and cartrisine B (<strong>2</strong>) were isolated from <em>Caryopteris trichosphaera</em>. Their structures were elucidated based on HR-ESI-MS and NMR spectral data. Compound <strong>2</strong> exhibited moderate antibacterial bioactivity against MRSA and VRE, and showed a strong synergistic effect with market antibiotics against MRSA and VRE.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497678","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}
FitoterapiaPub Date : 2024-10-23DOI: 10.1016/j.fitote.2024.106276
{"title":"A novel normonoterpene glycoside and a new benzophenone derivative from Hypericum cerastioides and their in vitro cytotoxic activities","authors":"","doi":"10.1016/j.fitote.2024.106276","DOIUrl":"10.1016/j.fitote.2024.106276","url":null,"abstract":"<div><div>Phytochemical investigations on the aerial parts of <em>Hypericum cerastioides</em> led to the isolation and identification of a novel normonoterpene (<strong>1</strong>) and a previously undescribed benzophenone glycoside (<strong>3</strong>) along with eleven known secondary metabolites (<strong>2</strong>, <strong>4</strong>–<strong>13</strong>). Their structures were deduced based on extensive 1D and 2D NMR analyses as well as HRESIMS. Compound <strong>1</strong> is a rare type of normonoterpene derivative with eight carbon atoms. The chemotaxonomic significance of the isolates was also discussed. Compounds were evaluated for their <em>in vitro</em> cytotoxic activities against SW480, A375, DU145 and MCF7 cancer cell lines using doxorubicin as a reference drug. Compounds <strong>1</strong> and <strong>7</strong> demonstrated weak cytotoxicity.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497672","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}
FitoterapiaPub Date : 2024-10-23DOI: 10.1016/j.fitote.2024.106262
{"title":"Talarmalnoids A–F: Fusicoccane diterpenoids from an arthropod-derived endophytic fungus Talaromyces malicola","authors":"","doi":"10.1016/j.fitote.2024.106262","DOIUrl":"10.1016/j.fitote.2024.106262","url":null,"abstract":"<div><div>The metabolites from the endophytic fungus <em>Talaromyces malicola</em> hosted in the gastrointestinal tract of the arthropods <em>Armadillidium vulgare</em> were investigated, and six undescribed fusicoccane diterpenoids, talarmalnoids A–F (<strong>1</strong>–<strong>6</strong>), along with three known analogs were isolated. Talarmalnoid C (<strong>3</strong>) was an unprecedented fusicoccane diterpenoid with two sugar units, i.e., 6-<em>O</em>-methyl-<em>α</em>-<span>d</span>-glucose and <em>α</em>-<span>d</span>-glucose. Talarmalnoids D and E (<strong>4</strong> and <strong>5</strong>) were fusicoccane-type diterpenoids with unusual seven-membered rings attached at the C-3′ and C-4′ positions. Their structures and absolute configurations were identified by NMR, HRESIMS analyses, X-ray single crystal diffraction, GC–MS, ECD analyses, <sup>13</sup>C NMR calculations, and DP4+ probability analyses. Bioassay results showed that talarmalnoid B (<strong>2</strong>) exhibited significant inhibitory activities against the LPS-inducted production of NO in RAW 264.7 cells, with IC<sub>50</sub> value of 0.83 μM.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497676","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}
FitoterapiaPub Date : 2024-10-22DOI: 10.1016/j.fitote.2024.106272
{"title":"New chalcone derivatives containing morpholine-thiadiazole: Design, synthesis and evaluation of against tobacco mosaic virus","authors":"","doi":"10.1016/j.fitote.2024.106272","DOIUrl":"10.1016/j.fitote.2024.106272","url":null,"abstract":"<div><div>Twenty chalcone derivatives containing morpholine-thiadiazole were designed and synthesized from the natural product chalcone. The bioactivity test results indicate that some compounds exhibit good antiviral activity against tobacco mosaic virus (TMV). In particular, the EC<sub>50</sub> values for the curative and protective activity of <strong>S14</strong> against TMV were 91.8 and 130.6 <em>μ</em>g/mL, which was better than that of the antiviral agent ningnanmycin (NNM, 237.8, 220.6 <em>μ</em>g/mL). The results of preliminary mechanism study indicated that <strong>S14</strong> had strong binding capacity and affinity to tobacco mosaic virus coat protein (TMV-CP). In the chlorophyll content assay, the chlorophyll content of tobacco leaves increased significantly after the action of <strong>S14,</strong> so that it can enhance the photosynthetic capacity of plants. In addition, the results of malondialdehyde (MDA) content assay also indicated that <strong>S14</strong> could improve the disease resistance of tobacco.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497681","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}
FitoterapiaPub Date : 2024-10-22DOI: 10.1016/j.fitote.2024.106268
Guan-Ke Liu, Bing-Yang Zhang, Zheng Niu, Jia-Qi Chen, Chun-Yu Fan, Xin-Yue Deng, Fan-Qing Ye, Shi-Jie Cao, Ning Kang, Tie Yao, Feng Qiu
{"title":"Triterpenoids from the rhizomes and roots of Gentiana scabra Bge. And their cytotoxic activities.","authors":"Guan-Ke Liu, Bing-Yang Zhang, Zheng Niu, Jia-Qi Chen, Chun-Yu Fan, Xin-Yue Deng, Fan-Qing Ye, Shi-Jie Cao, Ning Kang, Tie Yao, Feng Qiu","doi":"10.1016/j.fitote.2024.106268","DOIUrl":"https://doi.org/10.1016/j.fitote.2024.106268","url":null,"abstract":"<p><p>Phytochemical investigation on the rhizomes and roots of Gentiana scabra (Gentianaceae) led to the isolation of five new triterpenoids (1-5), together with seven known ones (6-12). The structures and absolute configurations of the new compounds were elucidated by spectroscopic data interpretation, ECD calculation and X-ray crystallographic analysis. Noticeably, compound 4 was an uncommon 3,4-seco-pentacyclic triterpenoid in natural products. The in vitro cytotoxic activities of all isolates against human cancer cell lines (HepG2, Hep3B, HCT116, and U87) were measured using MTT assay. Among them, compounds 2-9, 11, and 12 exhibited anti-proliferative effects against these tumor cell lines.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497677","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}
FitoterapiaPub Date : 2024-10-21DOI: 10.1016/j.fitote.2024.106270
{"title":"The medicinal plant Peucedanum japonicum Thunberg: A review of traditional use, phytochemistry, and pharmacology","authors":"","doi":"10.1016/j.fitote.2024.106270","DOIUrl":"10.1016/j.fitote.2024.106270","url":null,"abstract":"<div><div><em>Peucedanum japonicum</em> (the family Umbelliferae) is a perennial herbaceous plant with various crucial traditional values for coughs, colds, headaches, and inflammatory responses. For drug developments, the current research aims to offer an overview of the previous results in the three main aspects of traditional use, phytochemistry, pharmacological values, and molecular mechanisms regarding this medicinal species. By chromatographic analysis and separation, more than 120 isolated compounds have been obtained. Khellactone-type coumarins and phenolic compounds are the primary phytochemical classes with some coumarins, such as calipteryxin, praerutorin A, and pteryxin, being the main metabolites. Pharmacological activities of <em>P. japonicum</em> constituents included anticancer, antioxidative, antimicrobial, antiviral, antiplatelet, and tyrosine inhibitory activities, especially anti-inflammation and anti-obesity. It is worth mentioning that the obtained constituents joined to protect the neurons, bone, and urine systems, and exerted vasorelaxant. In general, the underlying mechanism of anti-inflammatory action can be explained by mitogen-activated protein kinase/nuclear factor-kappa B (MAPK/NF-κB) signaling pathway, whereas anti-obesity activity is deduced from regulating lipid metabolism-related genes. It also noted that pteryxin is the most active compound, but the clinical studies and synthesis of new derivatives containing enhanced medicinal values have been still limited, which should be improved.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497682","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}
FitoterapiaPub Date : 2024-10-20DOI: 10.1016/j.fitote.2024.106265
{"title":"A strategic review of STAT3 signaling inhibition by phytochemicals for cancer prevention and treatment: Advances and insights","authors":"","doi":"10.1016/j.fitote.2024.106265","DOIUrl":"10.1016/j.fitote.2024.106265","url":null,"abstract":"<div><div>Cancer remains a significant global health concern. The dysregulation of signaling networks in tumor cells greatly affects their functions. This review intends to explore phytochemicals possessing potent anticancer properties that specifically target the STAT3 signaling pathway, elucidating strategies and emphasizing their potential as promising candidates for cancer therapy. The review comprehensively examines various STAT3 inhibitors designed to disrupt the signaling cascade, including those targeting upstream activation, SH2 domain phosphorylation, DNA binding domain (DBD), N-terminal domain (NTD), nuclear translocation, and enhancing endogenous STAT3 negative regulators. A literature review was conducted to identify phytochemicals with anticancer activity targeting the STAT3 signaling pathway. Popular research databases such as Google Scholar, PubMed, Science Direct, Scopus, Web of Science, and ResearchGate were searched from the years 1989 - 2023 based on the keywords “Cancer”, “STAT3”, “Phytochemicals”, “Phytochemicals targeting STAT3 signaling”, “upstream activation of STAT3”, “SH2 domain of STAT3”, “DBD of STAT3”, “NTD of STAT3, “endogenous negative regulators of STAT3”, or “nuclear translocation of STAT3”, and their combinations. A total of 264 relevant studies were selected and analyzed based on the mechanisms of action and the efficacy of the phytocompounds. The majority of the discussed phytochemicals primarily focus on inhibiting upstream activation of STAT3. Additionally, flavonoid and terpenoid compounds exhibit multifaceted effects by targeting one or more checkpoints within the STAT3 pathway. Analysis reveals that phytochemicals targeting upstream activation predominantly belong to the classes of flavonoids and terpenoids, which hold significant promise as effective anticancer therapeutics. Future research in this field can be directed towards exploring and developing these scrutinized classes of phytochemicals to achieve desired therapeutic outcomes in cancer treatment.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497673","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}
FitoterapiaPub Date : 2024-10-20DOI: 10.1016/j.fitote.2024.106266
{"title":"Bioactive constituents from Clerodendrum trichotomum and their α-glucosidase inhibitory and PPAR-γ agonist activities","authors":"","doi":"10.1016/j.fitote.2024.106266","DOIUrl":"10.1016/j.fitote.2024.106266","url":null,"abstract":"<div><div>Three new neoclerodane diterpenoids (<strong>1–3</strong>), two new steroids (<strong>4–5</strong>), one new monoterpene (<strong>6</strong>), one new derivative of benzaldehyde (<strong>7</strong>) and one new iridoid glycoside (<strong>8</strong>), along with 19 known phenolic compounds, were isolated from <em>Clerodendrum trichotomum</em>. Their structures were established by a combination of detailed spectroscopic analyses (1D and 2D NMR) and high resolution electrospray ionization mass spectroscopy (HRESIMS). The isolated compounds were screened on <em>α</em>-glucosidase inhibitory and the peroxisome proliferator-activated receptor gamma (PPAR-<em>γ</em>) agonist activities, and the results showed that three phenylethanoid glycosides, verbascoside (<strong>9</strong>), leucosceptoside a (<strong>10</strong>), and isoacteoside (<strong>13</strong>), and two flavonoids, apigenin (<strong>22</strong>) and luteolin (<strong>26</strong>) showed potent inhibitory effects against α-glucosidase, with IC<sub>50</sub> values in the range from 15 to 700 μM. In addition, four flavonoids apigenin 7<em>-O-β</em>-D-glucuronide (<strong>19</strong>), apigenin (<strong>22</strong>), luteolin (<strong>26</strong>), and quercetin (<strong>27</strong>) exhibited significant PPAR-<em>γ</em> agonistic activities with EC<sub>50</sub> values in the range 2.3–24.9 μM.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497680","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}
FitoterapiaPub Date : 2024-10-18DOI: 10.1016/j.fitote.2024.106264
{"title":"Six new prenylated flavonoids from Dodonaea viscosa with anti-Zika virus activity","authors":"","doi":"10.1016/j.fitote.2024.106264","DOIUrl":"10.1016/j.fitote.2024.106264","url":null,"abstract":"<div><div>Six new prenylated flavonoids, named visconaeas A-F (<strong>1–6</strong>), and eleven known isopentenyl flavonoids (<strong>7–17</strong>) were isolated from <em>Dodonaea viscosa</em> (L.) Jacq. The structures of the separated compounds were determined through comprehensive spectral analysis and quantum chemical calculations. These compounds were tested for their anti-Zika virus and cytotoxicity activities. The results indicated that compound <strong>4</strong> showed low cytotoxicity and strong anti-Zika virus potential with EC<sub>50</sub> 16.34 μM.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142461358","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}
FitoterapiaPub Date : 2024-10-18DOI: 10.1016/j.fitote.2024.106267
{"title":"Flavonoids from Camellia oleifera flower ameliorate type 2 diabetes mellitus by regulating the p53 pathway","authors":"","doi":"10.1016/j.fitote.2024.106267","DOIUrl":"10.1016/j.fitote.2024.106267","url":null,"abstract":"<div><h3>Background</h3><div>Camellia oleifera flower (COF) is rich in flavonoids and polyphenols, strongly preventing postprandial hyperglycemia and improving diabetes. However, research on the effective ingredients in COF extracts that have hypoglycemic effects is limited, and the mechanism by which COF extracts improve liver insulin resistance and glucose and lipid metabolism still needs to be clarified, requiring further investigation.</div></div><div><h3>Aim</h3><div>To systematically clarify the role of COF extracts in improving insulin resistance in diabetes mice and to explore their key targets and mechanisms in anti-type 2 diabetes (T2DM).</div></div><div><h3>Materials and methods</h3><div>Ultrafiltration combined with liquid chromatography-mass spectrometry (UPLC-Q-MS) was used to analyze α-glucosidase inhibitors in COF extracts qualitatively. Blood glucose, lipid, oxidative stress, and liver function indicators were detected in the db/db type 2 diabetes mouse model. Then, RNA-seq was used to identify differentially expressed mRNAs (DEGs) in the liver, screen for key genes and metabolic pathways, and validate the results' accuracy through qPCR experiments.</div></div><div><h3>Results</h3><div>17 α-glucosidase inhibitors were identified as flavonoids from COF. Through db/db type 2 diabetes mouse model, it was indicated that COF could significantly improve symptoms of hyperglycemia and hyperlipidemia, alleviate oxidative stress, and protect liver and pancreatic tissues by regulating key differential genes expressed, including Nek2, Cdk1, Ccnb1, and Ccnb2 via the p53 signaling pathway and ameliorate the insulin resistance effect.</div></div><div><h3>Conclusion</h3><div>This study demonstrated the anti-diabetic effect of COF, explored its potential hypoglycemic target, and provided data support for future T2DM prevention and drug treatment.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142461353","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}