Pub Date : 2024-10-23DOI: 10.1016/j.fitote.2024.106269
Two new abietane diterpenoids, cartrisine A (1) and cartrisine B (2) were isolated from Caryopteris trichosphaera. Their structures were elucidated based on HR-ESI-MS and NMR spectral data. Compound 2 exhibited moderate antibacterial bioactivity against MRSA and VRE, and showed a strong synergistic effect with market antibiotics against MRSA and VRE.
{"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}
Pub Date : 2024-10-23DOI: 10.1016/j.fitote.2024.106276
Phytochemical investigations on the aerial parts of Hypericum cerastioides led to the isolation and identification of a novel normonoterpene (1) and a previously undescribed benzophenone glycoside (3) along with eleven known secondary metabolites (2, 4–13). Their structures were deduced based on extensive 1D and 2D NMR analyses as well as HRESIMS. Compound 1 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 in vitro cytotoxic activities against SW480, A375, DU145 and MCF7 cancer cell lines using doxorubicin as a reference drug. Compounds 1 and 7 demonstrated weak cytotoxicity.
{"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}
Pub Date : 2024-10-23DOI: 10.1016/j.fitote.2024.106262
The metabolites from the endophytic fungus Talaromyces malicola hosted in the gastrointestinal tract of the arthropods Armadillidium vulgare were investigated, and six undescribed fusicoccane diterpenoids, talarmalnoids A–F (1–6), along with three known analogs were isolated. Talarmalnoid C (3) was an unprecedented fusicoccane diterpenoid with two sugar units, i.e., 6-O-methyl-α-d-glucose and α-d-glucose. Talarmalnoids D and E (4 and 5) 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, 13C NMR calculations, and DP4+ probability analyses. Bioassay results showed that talarmalnoid B (2) exhibited significant inhibitory activities against the LPS-inducted production of NO in RAW 264.7 cells, with IC50 value of 0.83 μM.
研究人员对寄生在节肢动物犰狳胃肠道中的内生真菌 Talaromyces malicola 的代谢物进行了调查，并分离出了六种未曾描述过的 fusicoccane 二萜，即 Talarmalnoids A-F（1-6），以及三种已知的类似物。Talarmalnoids C（3）是一种前所未有的含有两个糖单位（即 6-O-甲基-α-d-葡萄糖和α-d-葡萄糖）的草杉烷二萜类化合物。Talarmalnoids D 和 E（4 和 5）是在 C-3' 和 C-4' 位置上连接有不寻常的七元环的 fusicoccane 型二萜类化合物。通过核磁共振、HRESIMS 分析、X 射线单晶衍射、气相色谱-质谱、ECD 分析、13C 核磁共振计算和 DP4+ 概率分析，确定了它们的结构和绝对构型。生物测定结果表明，talarmalnoid B (2) 对 RAW 264.7 细胞在 LPS 诱导下产生的 NO 具有显著的抑制活性，IC50 值为 0.83 μM。
{"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}
Pub Date : 2024-10-22DOI: 10.1016/j.fitote.2024.106272
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 EC50 values for the curative and protective activity of S14 against TMV were 91.8 and 130.6 μg/mL, which was better than that of the antiviral agent ningnanmycin (NNM, 237.8, 220.6 μg/mL). The results of preliminary mechanism study indicated that S14 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 S14, so that it can enhance the photosynthetic capacity of plants. In addition, the results of malondialdehyde (MDA) content assay also indicated that S14 could improve the disease resistance of tobacco.
{"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}
Pub 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
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.
{"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}
Pub Date : 2024-10-21DOI: 10.1016/j.fitote.2024.106270
Peucedanum japonicum (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 P. japonicum 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.
Peucedanum japonicum（伞形科）是一种多年生草本植物，具有治疗咳嗽、感冒、头痛和炎症反应的各种重要传统价值。为了开发药物，目前的研究旨在从传统用途、植物化学、药理价值和分子机制三个主要方面概述有关该药用植物的以往成果。通过色谱分析和分离，共分离出 120 多种化合物。主要的植物化学成分为黄柏酮类香豆素和酚类化合物，其中一些香豆素类化合物，如萼片香豆素、praerutorin A 和 pteryxin 是主要的代谢产物。日本鸦胆子成分的药理活性包括抗癌、抗氧化、抗菌、抗病毒、抗血小板和酪氨酸抑制活性，尤其是抗炎和抗肥胖活性。值得一提的是，所获得的成分还能保护神经元、骨骼和尿液系统，并起到舒张血管的作用。一般来说，抗炎作用的基本机制可通过丝裂原活化蛋白激酶/核因子-卡巴B（MAPK/NF-κB）信号通路来解释，而抗肥胖活性则可通过调节脂质代谢相关基因来推导。研究还指出，翼苷是活性最高的化合物，但临床研究和合成药用价值更高的新衍生物仍然有限，有待改进。
{"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}
Pub Date : 2024-10-20DOI: 10.1016/j.fitote.2024.106265
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.
{"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}
Pub Date : 2024-10-20DOI: 10.1016/j.fitote.2024.106266
Three new neoclerodane diterpenoids (1–3), two new steroids (4–5), one new monoterpene (6), one new derivative of benzaldehyde (7) and one new iridoid glycoside (8), along with 19 known phenolic compounds, were isolated from Clerodendrum trichotomum. 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 α-glucosidase inhibitory and the peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist activities, and the results showed that three phenylethanoid glycosides, verbascoside (9), leucosceptoside a (10), and isoacteoside (13), and two flavonoids, apigenin (22) and luteolin (26) showed potent inhibitory effects against α-glucosidase, with IC50 values in the range from 15 to 700 μM. In addition, four flavonoids apigenin 7-O-β-D-glucuronide (19), apigenin (22), luteolin (26), and quercetin (27) exhibited significant PPAR-γ agonistic activities with EC50 values in the range 2.3–24.9 μM.
{"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}
Pub Date : 2024-10-18DOI: 10.1016/j.fitote.2024.106264
Six new prenylated flavonoids, named visconaeas A-F (1–6), and eleven known isopentenyl flavonoids (7–17) were isolated from Dodonaea viscosa (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 4 showed low cytotoxicity and strong anti-Zika virus potential with EC50 16.34 μM.
{"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}
Pub Date : 2024-10-18DOI: 10.1016/j.fitote.2024.106267
Background
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.
Aim
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).
Materials and methods
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.
Results
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.
Conclusion
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.
{"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}
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