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Effect of Ilex hainanensis Merr. On HFD-induced nonalcoholic fatty liver disease and rebalance of gut microbiota and bile acids metabolism in mice Ilex hainanensis Merr.对高密度脂蛋白胆固醇诱导的非酒精性脂肪肝以及小鼠肠道微生物群和胆汁酸代谢的再平衡的影响
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-12 DOI: 10.1016/j.fitote.2024.106186
{"title":"Effect of Ilex hainanensis Merr. On HFD-induced nonalcoholic fatty liver disease and rebalance of gut microbiota and bile acids metabolism in mice","authors":"","doi":"10.1016/j.fitote.2024.106186","DOIUrl":"10.1016/j.fitote.2024.106186","url":null,"abstract":"<div><p>Nonalcoholic fatty liver disease (NAFLD) is a clinicopathological syndrome characterized by excessive intracellular fat deposition in the hepatocytes, and the development is exacerbated by gut microbiota and bile acids metabolism disorders. <em>Ilex hainanensis</em> Merr. is a traditional medicine of the Zhuang nationality, historically esteemed for its efficacy in lowering blood pressure and lipid levels. This study aimed to investigate the pharmacodynamic effects in NAFLD mice and impacts on gut microbiota and bile acids (BAs) metabolism of <em>I. hainanensis</em> extract (IHA). 16 compounds were identified from IHA by HPLC-DAD-MS analysis. IHA significantly reduced body weight indexs, alanine transaminase (ALT) and aspartate transaminase (AST) activities, improved dyslipidemia and insulin resistance (IR), and effectively ameliorated hepatic steatosis in HFD-induced NAFLD mice. IHA also altered gut microbiota composition, particularly enhancing the abundance of bacteria involved in BAs metabolism, as well as augmented BAs synthesis in the liver and increased fecal excretion. In conclusion, our findings suggest that IHA holds promise in improving NAFLD conditions and modulating gut microbiota and BAs metabolism. These insights contribute to a deeper understanding of the mechanisms underlying IHA-mediated alleviation of lipid accumulation in NAFLD.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141982058","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}
引用次数: 0
[1–7-NαC]-Crocaorb A1 and A2, orbitides from the latex of Croton campanulatus [1-7-NαC]-Crocaorb A1 和 A2,从巴豆乳汁中提取的眶苷。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-12 DOI: 10.1016/j.fitote.2024.106183
{"title":"[1–7-NαC]-Crocaorb A1 and A2, orbitides from the latex of Croton campanulatus","authors":"","doi":"10.1016/j.fitote.2024.106183","DOIUrl":"10.1016/j.fitote.2024.106183","url":null,"abstract":"<div><p>Two new heptapeptides, [1–7-NαC]-crocaorbs A1 (<strong>1</strong>) and A2 (<strong>2</strong>), were isolated from the latex of <em>Croton campanulatus</em>. Their structures were determined using NMR spectroscopic techniques, ESI-HRMS data, Marfey's method, and further refined using molecular dynamics with simulated annealing (MD/SA). Molecular dynamics calculations of peptides <strong>1</strong> and <strong>2</strong> demonstrated greater stability in simulations using a biological solvent compared to those using DMSO. Compound <strong>1</strong>, the most abundant peptide in latex, was assessed for NO production, antiplasmodial and cytotoxicity activities. The peptide significantly increased nitric oxide (NO) production at concentrations of 40, 20 or 10 μM (17.932 ± 1.1, 18.270 ± 0.9, 18.499 ± 0.7, respectively). Its antiplasmodial activity exhibited limited efficacy, with only 5% inhibition of <em>Plasmodium falciparum</em> 3D7 growth at a concentration of 50 μM. Also, it exhibited no cytotoxic effects in the J774A.1 murine macrophages cell line. This study represents the first report of a phytochemical investigation of the species <em>C. campanulatus</em>, which showed orbitides with distinctive sequences in contrast to other peptides described for the genus <em>Croton</em> and contributes to the study of structural diversity within this particular class of compounds.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141982057","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}
引用次数: 0
Unveiling the hidden potential: Above-ground parts of Paris yunnanensis Franch. Is promise as an anti-acne therapeutic beyond traditional medicinal sites 揭开隐藏潜力的面纱:云南帕里斯(Paris yunnanensis Franch.作为一种抗痤疮疗法,它的前景超出了传统的药用范围。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-10 DOI: 10.1016/j.fitote.2024.106179
{"title":"Unveiling the hidden potential: Above-ground parts of Paris yunnanensis Franch. Is promise as an anti-acne therapeutic beyond traditional medicinal sites","authors":"","doi":"10.1016/j.fitote.2024.106179","DOIUrl":"10.1016/j.fitote.2024.106179","url":null,"abstract":"<div><p>The dried rhizomes of <em>Paris yunnanensis</em> Franch<em>.</em> have been extensively utilized in traditional Chinese medicine as hemostatic, antitumor, and antimicrobial agents. An examination of classical texts and renowned Chinese medical formulations showcased its efficacy in acne treatment. Presently, there is a significant scarcity of <em>Paris</em> resources. Consider directing attention towards the non-medicinal parts of <em>Paris</em> to mitigate the strain on medicinal resources within this realm. To address these resource limitations, this study investigated the bioactivity and pharmacodynamics of the above-ground parts of <em>Paris</em> (AGPP). A synergistic approach integrating network pharmacology, molecular docking (in silico validation), and animal experimentation (in vivo validation) was employed to elucidate the potential mechanisms underlying the efficacy of AGPP against acne vulgaris in this study. The active constituents in AGPP extracts were identified via UHPLC-Q-Orbitrap HRMS analysis, with their targets extracted for network pharmacological analysis. KEGG pathway analysis unveiled potential therapeutic mechanisms, validated through molecular docking and rat auricular acne model experiments. Comprehensive chemical characterization revealed fifty constituents, including steroidal saponins, flavonoids, amino acids, organic acids, phytohormones, phenolic acids, and alkaloids. Diosgenin, Quercetin, Kaempferol, Ecdysone, and α-linolenic acid were identified as main constituents with acne-treating potential. Core targets included SRC, MAPK3, and MAPK1, with key signaling pathways implicated. Histologically, AGPP mitigated acne-induced follicular dilatation and inflammation, inhibiting inflammatory cytokine production (IL-6, IL-1β, TNF-α). This study offers insight into AGPP's mechanism for acne treatment, laying groundwork for Paris development and drug discovery.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141916485","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}
引用次数: 0
Effect of ultrasonic and conventional extraction on bioactive components, glucosinolate content and antidiabetic activity of Crambe tataria 超声波萃取和传统萃取对蝙蝠葛生物活性成分、葡萄糖苷酸含量和抗糖尿病活性的影响
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106177
{"title":"Effect of ultrasonic and conventional extraction on bioactive components, glucosinolate content and antidiabetic activity of Crambe tataria","authors":"","doi":"10.1016/j.fitote.2024.106177","DOIUrl":"10.1016/j.fitote.2024.106177","url":null,"abstract":"<div><p>This study was conducted to determine and compare the phenolic compounds, glucosinolate contents and antidiabetic effects of the extracts obtained by ultrasonic and conventional extraction method of the leaves and flowers of the <em>Crambe tataria</em>. The highest antioxidant activity (12.95 mg/mL IC<sub>50</sub> value) and total phenolic content (1313.57 mg GAE/100 g fw) were detected in the ultrasonic flower extract. In total flavonoid results, extracts obtained from the flower part of <em>C. tataria</em> had higher values than that of extracts obtained from the leaf part. The most abundant phenolic component in the flower extract was catechin. The highest catechin content in all samples was detected in the ultrasonic flower extract with a value of 374.37 mg/kg. Rutin was the dominant phenolic component in the leaf extract. Rutin values were 654.38 mg/kg and 757.30 mg/kg for conventional and ultrasonic extraction, respectively. In glucosinolate analysis, the highest glucoraphanin content was obtained in flower samples and by conventional extraction method (3466.84 mg/kg). The highest contents of sinigrin (689.97 mg/kg), glucotropaeolin (420.89 mg/kg), glucoerucin (357.27 mg/kg), glucoraphasatin (181.11 mg/kg) and gluconasturtin (66.07 mg/kg) were detected in ultrasonic flower extracts. The highest α-amylase and α-glucosidase enzyme inhibition effects belonged to the ultrasonic flower extract with values of 3.70 mg/mL and 4.89 mg/mL, respectively. As a result, this study determined for the first time that ultrasonic extraction of <em>C. tataria</em> flowers has much higher bioactive components and antidiabetic effects, revealing the potential use of this plant in the fields of medicine, pharmacology and chemistry.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141912281","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}
引用次数: 0
Triterpenoid saponins from the roots of Panax notoginseng with protective effects against APAP-induced liver injury 三七根中的三萜类皂甙对 APAP 引起的肝损伤具有保护作用
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106159
{"title":"Triterpenoid saponins from the roots of Panax notoginseng with protective effects against APAP-induced liver injury","authors":"","doi":"10.1016/j.fitote.2024.106159","DOIUrl":"10.1016/j.fitote.2024.106159","url":null,"abstract":"<div><p>Five previously undescribed protopanaxatriol-type saponins, notoginsenosides Ta-Te (<strong>1</strong>–<strong>5</strong>), together with eighteen known triterpenoid saponins (<strong>6</strong>–<strong>23</strong>) were isolated from the roots of <em>Panax notoginseng</em>. The structures of new compounds were determined by HRESIMS and NMR spectroscopic analyses and chemical methods. Compounds <strong>1</strong> and <strong>2</strong> were the first examples of ginsenosides featuring a 6-deoxy-<em>β</em>-<span>d</span>-glucose moiety from <em>Panax</em> species. Compounds <strong>1</strong>–<strong>4</strong>, <strong>7</strong>, <strong>10</strong>, <strong>12</strong>, <strong>21</strong>–<strong>22</strong> showed protective effects on L02 cells against the injury of acetaminophen (APAP). Among them, notoginsenoside R1 (<strong>12</strong>), ginsenoside Rg1 (<strong>21</strong>), and ginsenoside Re (<strong>22</strong>) were the most potent ones, with cell viabilities &gt;80%. Moreover, compounds <strong>12</strong> and <strong>22</strong> remarkably alleviated APAP-induced liver injury in mice. These saponins are potential hepatoprotective agents.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141912284","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}
引用次数: 0
Targeted discovery of clerodane diterpenoids from Tinospora sinensis as immunomodulatory agents 从天竺葵中发现可作为免疫调节剂的蛤蜊烷二萜类化合物。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106174
{"title":"Targeted discovery of clerodane diterpenoids from Tinospora sinensis as immunomodulatory agents","authors":"","doi":"10.1016/j.fitote.2024.106174","DOIUrl":"10.1016/j.fitote.2024.106174","url":null,"abstract":"<div><p>Under the guidance of MS/MS-based molecular networking, five new clerodane diterpenoid glucosides, tinosinesides R-V (<strong>1</strong>–<strong>5</strong>), along with 15 known diterpenoids (<strong>6–20</strong>), were isolated from the stems of <em>Tinospora sinensis</em>. Compound <strong>1</strong> represents the first example of diterpenoid bearing a thio sugar and compound <strong>5</strong> is the first 18,19-dinor-clerodane with <em>cis</em>-fused A/B ring. The structures of the new compounds were elucidated by spectroscopic means, and their absolute configurations were established on the basis of time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculation and chemical methods. Selected compounds were evaluated for their immunomodulatory effect and several compounds could enhance the proliferation of B lymphocytes. Preliminary mechanistic studies disclosed that <strong>3</strong> could promote B cell generation and inhibit B cell differentiation.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141912283","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}
引用次数: 0
Antiproliferative metabolites against glioma cells from the marine-associated actinomycete Streptomyces sp. ZZ735 海洋放线菌链霉菌 ZZ735 对胶质瘤细胞的抗增殖代谢物。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106176
{"title":"Antiproliferative metabolites against glioma cells from the marine-associated actinomycete Streptomyces sp. ZZ735","authors":"","doi":"10.1016/j.fitote.2024.106176","DOIUrl":"10.1016/j.fitote.2024.106176","url":null,"abstract":"<div><p>Metabolites produced by the genus <em>Streptomyces</em> are the most important resource for discovering bioactive compounds. In this study, chemical investigation on the metabolites produced by the marine-derived <em>Streptomyces</em> sp. ZZ735 in rice solid medium led to the isolation of eighteen compounds (<strong>1</strong>–<strong>18</strong>). Chemical structures of the isolated compounds were determined based on their HRESIMS data and the extensive NMR spectral analyses. Streptonaphthothiazines A (<strong>1</strong>), B (<strong>2</strong>), 2-(2-hydroxy-2-methylpropanoylamino)-benzoic acid (<strong>7</strong>), and streptomycinoic acids A (<strong>17</strong>), B (<strong>18</strong>) are characterized as five previously undescribed compounds. The structural backbones of streptonaphthothiazines A (<strong>1</strong>), B (<strong>2</strong>) and streptomycinoic acids A (<strong>17</strong>), B (<strong>18</strong>) are found from a natural resource for the first time. It is also the first report of 2-(2-methylpropanoylamino)-benzoic acid (<strong>3</strong>), 2-(2-methylpropanoylamino)-benzamide (<strong>4</strong>), methyl 2-(3-hydroxypropanoylamino)-benzoate (<strong>5</strong>), 2-propionylaminobenzamide (<strong>6</strong>), and (2<em>E</em>)-3-(3-hydroxy-4,5-dimethoxyphenyl)-2-propenoic acid (<strong>15</strong>) as natural products. Streptonaphthothiazines A (<strong>1</strong>), B (<strong>2</strong>) and streptomycinoic acids A (<strong>17</strong>), B (<strong>18</strong>) have antiproliferative activity against human glioma U87MG or U251 cells with IC<sub>50</sub> values ranging from 31.8 to 37.9 μM.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141912280","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}
引用次数: 0
Gentiana decoction inhibits liver fibrosis and the activation of hepatic stellate cells via upregulating the expression of Parkin 龙胆草煎剂通过上调 Parkin 的表达,抑制肝纤维化和肝星状细胞的活化。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-07 DOI: 10.1016/j.fitote.2024.106170
{"title":"Gentiana decoction inhibits liver fibrosis and the activation of hepatic stellate cells via upregulating the expression of Parkin","authors":"","doi":"10.1016/j.fitote.2024.106170","DOIUrl":"10.1016/j.fitote.2024.106170","url":null,"abstract":"<div><p>Liver fibrosis is a wound-healing process. It can be induced by various chronic liver diseases. Liver fibrosis is characterized by the activation of hepatic stellate cells (HSCs), a key event. However, no effective treatment strategies to cure or alleviate liver fibrosis-induced pathologic changes have yet been developed. Traditional Chinese medicine (TCM) exhibits a good anti-fibrosis action, with few side effects. Gentiana decoction, a TCM also called Longdan Xiegan Tang (LXT), is used for purging the liver in clinical settings. However, the role of LXT in preventing liver fibrosis and the underlying regulatory mechanism have not yet been investigated. This study demonstrates that LXT treatment can protect the liver from the injuries resulting from CCl<sub>4</sub>-induced liver fibrosis in mice and suppress the activation of HSCs. The mice in the LXT group exhibit litter collagen I and HSC activation marker α-smooth muscle actin (α-SMA) expression. Transcriptome sequencing of the mouse liver tissue reveals that the level of Parkin, a mitophagy marker, decreased in CCl<sub>4</sub>-induced liver fibrosis. Further study shows that the injection of Parkin-overexpression adeno-associated virus (Parkin–AAV) via the tail vein can reduce CCl<sub>4</sub>-induced liver fibrogenesis in mice. We conducted a mechanistic study also, which suggests that LXT treatment suppresses the activation of HSCs by upregulating the expression of Parkin. Hence, it can be suggested that LXT inhibits liver fibrosis by activating the Parkin signaling pathway.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141912282","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}
引用次数: 0
Limonin (LM) and its derivatives: Unveiling the neuroprotective and anti-inflammatory potential of LM and V-A-4 in the management of Alzheimer's disease and Parkinson's disease 柠檬素(LM)及其衍生物:揭示 LM 和 V-A-4 在治疗阿尔茨海默病和帕金森病中的神经保护和抗炎潜力。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-06 DOI: 10.1016/j.fitote.2024.106173
{"title":"Limonin (LM) and its derivatives: Unveiling the neuroprotective and anti-inflammatory potential of LM and V-A-4 in the management of Alzheimer's disease and Parkinson's disease","authors":"","doi":"10.1016/j.fitote.2024.106173","DOIUrl":"10.1016/j.fitote.2024.106173","url":null,"abstract":"<div><p>Neuroinflammation and neuronal apoptosis are central pathogenic consequences associated with Alzheimer's Disease (AD) and Parkinson's Disease (PD). Limonin (LM), a tetracyclic triterpenoid available in citrus fruits, has anti-tumor, antioxidant, anti-inflammatory, hepatoprotective, and neuroprotective actions. LM derivative, V-A-4 emerged as a potential neuroprotective drug due to their ability to target multiple molecular pathways intertwined with neuroinflammation and neuronal apoptosis. To date, the treatment of AD and PD is not successful even though the understanding of the mechanism of neuroinflammation and neuronal apoptosis is vast in the literature. Thus, there is an urgent need to identify novel neuroprotective drugs that could target the multiple molecular pathways associated with neuroinflammation and neuronal apoptosis. The various online databases (Google scholar, Pubmed, Scopus) were searched via keywords: limonin, limonin derivatives and neuroprotection. This review highlights the multifunctional nature of LM and derivatives in combating neuroinflammation and neuronal apoptosis by stimulating PI3K/AKT and downregulating TLR4/NF-κB critical pathways. By intervening in the secretion of NO and TNF-α from glial cells, V-A-4 attenuates the damaging cascade of neuroinflammation by suppressing IKK-α and IKK-β. Furthermore, V-A-4 demonstrates its versatility by suppressing the manifestation of miR-146a and miR-155, both intimately linked to neuroinflammation, this review summarized the activities of LM and its derivatives against AD and PD, with a special focus on V-A-4 as an effective neuroprotective drug. V-A-4's ability to stimulate PI3K/AKT signaling further underscores its neuroprotective effect in combating AD and PD. More in-vitro cell line studies are needed to develop V-A-4 as an upcoming neuroprotective compound.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141906310","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}
引用次数: 0
Design, synthesis and biological activity of α-nitrile substituted guaiazulene-based chalcone derivatives α-腈取代愈创木酚基查耳酮衍生物的设计、合成和生物活性。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2024-08-06 DOI: 10.1016/j.fitote.2024.106151
{"title":"Design, synthesis and biological activity of α-nitrile substituted guaiazulene-based chalcone derivatives","authors":"","doi":"10.1016/j.fitote.2024.106151","DOIUrl":"10.1016/j.fitote.2024.106151","url":null,"abstract":"<div><p>In present study, seventeen <em>α</em>-nitrile substituted guaiazulene-based chalcone derivatives including twelve new were designed, synthesized, and assayed for antiviral, cytotoxicity and signal pathway activities. All derivatives showed potential antiviral activity towards influenza virus or herpes simplex virus (HSV), <strong>7 g</strong> with the substitution of nitro group showed strong effects towards H1N1 virus at 30 μM with inhibitory rate of 66.0%, <strong>7o</strong> with thiophene exhibited potent anti HSV-1 activities with inhibitory rate of 65.8%. Moreover, several compounds exhibited inhibitory effects on tumor cells and hypoxia-inducible factor-1 (HIF1) signaling pathways. These results showed that <em>α</em>-nitrile substituted guaiazulene-based chalcones offered a promising framework for the further development of new highly efficient drugs.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141888886","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}
引用次数: 0
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