首页期刊导航|Fitoterapia
期刊信息/Journal information
Fitoterapia
Inverni della Beffa SpA
Fitoterapia

Inverni della Beffa SpA

0367-326X

Fitoterapia/Journal FitoterapiaSCIISTP
正式出版
收录年代

    Synthesis, biological evaluation and mechanism studies of C-3 substituted nitrogenous heterocyclic 23-Hydroxybetulinic acid derivatives as anticancer agents

    Zhou, HaipinZhu, HuajianZha, YuxinXu, Jinyi...
    12页
    查看更多>>摘要：A series of novel nitrogenous heterocycle substituted 23-Hydroxybetulinic acid (23-HBA) derivatives with amide linkages at the C-3 position were designed, synthesized and evaluated for their antitumor activities. The biological screening results showed that most of the derivatives exhibited more potent antiproliferative activities than 23-HBA. In particular compound 11-9 exhibited the most potent activities with IC50 values ranging from 1.96 mu M to 6.20 mu M against five cancer cell lines (B16, HepG2, A2780, MCF-7 and A549). The preliminary mechanism study showed that compound 11-9 caused cell cycle arrest at G1 phase, induced cell apoptosis and depolarized mitochondria of B16 cells in a dose dependent manner. Moreover, western blot analysis indicated that compound 11-9 down-regulated the expression of anti-apoptotic protein Bcl-2, up-regulated the expression of pro-apoptotic protein Bad, and activated cytochrome C and caspase 3 to cause cell apoptosis. In summary, 11-9 may serve as a promising lead for the development of new natural product-based antitumor agents and deserve further investigation.
      原文链接:
    • NSTL
    • Elsevier

    Stilbenes from the leaves of Cajanus cajan and their in vitro anti-inflammatory activities

    Tan, Ling-XuanXia, Tian-QiHe, Qi-FangTang, Wei...
    9页
    查看更多>>摘要：Eighteen stilbenes (1-18), including six previously undescribed ones (1-6), with diverse modification patterns were isolated from the leaves of edible and medicinal plant Cajanus cajan. Among the new isolates, compounds 1-3 were initially obtained as three racemic mixtures, which were further resolved into three pairs of optically pure enantiomers, respectively, by chiral HPLC. Besides, compounds 8, 10, 11, and 18 were obtained from C. cajan for the first time. The chemical structures and absolute configurations of the new stilbenes were elucidated unambiguously on the basis of extensive spectroscopic analyses, single crystal X-ray crystallographic study, and quantum chemical electronic circular dichmism (ECD) calculations. In addition, the in vitro antiinflammatory activities of all isolated stilbenes were evaluated. Compounds 2, 9, 10, 11, and 14 exerted moderate suppression of nitric oxide (NO) secretion in lipopolysaccharide (LPS)-induced RAW264.7 cells without exhibiting substantial cytotoxicity.
      原文链接:
    • NSTL
    • Elsevier

    Diverse dihydroagarofuran sesquiterpene derivatives from the stem and branch of Tripterygium wilfordii

    Hu, Ya-LinXu, Tian-QiYin, Wen-JingCheng, Huai-Yu...
    8页
    查看更多>>摘要：Ten new dihydroagarofuran sesquiterpene polyol esters, tripterdines A-J (1-10) were isolated from the stem and branch of Tripterygium wilfordii. The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses, including UV, IR, HRESIMS, NMR, and CD exciton chirality method. The structures of compounds 1, 3, and 6 were confirmed by X-ray crystallographic analyses. The anti-inflammatory and cytotoxic activities were assessed for all the compounds (1-10). Compounds 3, 5 and 10 exhibited potent anti-inflammatory activities with the secretion level of TNF-alpha ranging from 43.86% to 51.27%, and the IL-6 ranging from 32.44% to 50.64%. In addition, compounds 1, 3, 7 and 9 showed weak cytotoxicities against three human tumor cell lines (Huh7, MCF-7 and HCT-116).
      原文链接:
    • NSTL
    • Elsevier

    Synthesis and biological evaluation of scutellarein derivatives as neuroprotective agents via activating Nrf2/HO-1 pathway

    Han, TongZhang, ShuangWei, RenyueJia, Guiyan...
    9页
    查看更多>>摘要：Oxidative stress has been considered as the main factor of neurodegenerative diseases. Activation of the Nrf2/ HO-1 pathway, as one of the most crucial endogenous protection systems, was regarded as an effective strategy to against oxidative injury. Here, a series of phosphate esters or phosphonates of scutellarein derivatives were designed, synthesized and evaluated on SH-SY5Y cell lines to examine neuroprotective effects against H2O2 induced damage. Among them, compound 16d exhibited more potent cytoprotective effect than the lead compound scutellarin. Preliminary mechanism studies showed that compound 16d could prevent H2O2 induced neuronal apoptosis, significantly decrease ROS generation, elevate SOD and reduce MDA levels in a dosedependent manner in SH-SY5Y cell lines. Furthermore, western blot assay disclosed that compound 16d could activate Nrf2, and increase the expression of its downstream genes HO-1 in a concentration-dependent manner, thus displaying potent neuroprotective activity. Overall, these findings demonstrated that compound 16d, as a promising neuroprotective agent, deserved further development.
      原文链接:
    • NSTL
    • Elsevier

    Flavanols from Tetrapleura tetraptera with cytotoxic activities

    Ayoolu, Oguntimehin SamuelOgbole, Omonike OluyemisiAjaiyeoba, Edith OriabureNchiozem-Ngnitedem, Vaderament-A...
    6页
    查看更多>>摘要：Tetrapleura tetraptera is a medicinal plant used in East and West Africa to treat inflammation and related diseases. From the stem bark of the plant, three previously undescribed flavan-3-ol derivatives named (2R,3S)-3,3 ',5 ',7-tetrahydroxy-4 '-methoxyflavane (1), (2R,3S)-3 ',5 ',7-trihydroxy-4 '-methoxyflavane-3-O-beta-D-glucopyranoside (2), and (2R,3S,4S)-3,3 ',4,5 ',7-pentahydroxy-4 '-methoxyflavane (3) were isolated with three known analogues. The structural elucidation of the compounds was performed based on NMR spectroscopy and HRMS data analyses. The absolute configurations around the stereogenic carbons were determined using Circular Dichroism (ECD) and density functional theory (DFT) calculations. The cytotoxicity of the isolated compounds was tested using resazurin reduction assay. Compound 1 was moderately active against both recalcitrant leukemia cell lines with IC50 values of 21.90 mu M towards CCRF-CEM and 50.80 towards CEM/ADR5000. Similar level of activity was observed for compound 3 against CCRF-CEM cell line, IC50 = 35.50 mu M. All the tested compounds were not cytotoxic compared with the standard drug, doxorubicin, with IC50 values of 0.0075 against CCRF-CEM and 24.30 mu M against CEM/ADR5000.
      原文链接:
    • NSTL
    • Elsevier

    A pair of novel phenylethanol glycosides from Cistanche tubulosa (Schenk) Wight

    Xiong, Wei-LinSun, YuMa, Tian-ChengZhang, Xiao-Ying...
    8页
    查看更多>>摘要：A pair of differential epimers with opposite C-7 configurations, crenatosides A and B (1 and 2), and 10 known phenylethanoid glycosides (PhGs) (3-12) were obtained from the succulent stem of Cistanche tubulosa. The structures were elucidated based on extensive spectral data (UV, IR, 1D and 2D NMR, HR-ESIMS), which are first reported natural products with unique glycoside structures. After acid hydrolysis, the configuration of the sugar was determined by comparing it with the normative sugar by HPLC. The absolute configurations of both compounds were determined by ECD spectrum analysis. All the obtained compounds were examined for their inhibitory effect on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in mouse microglial cells (BV-2 cells), and compounds 1 and 2 showed potent inhibition on NO production with IC50 values of 5.62 mu M and 6.30 mu M, respectively.
      原文链接:
    • NSTL
    • Elsevier

    Local effects of natural alkylamides from Acmella oleracea and synthetic isobutylalkyl amide on neuropathic and postoperative pain models in mice

    Dallazen, Jorge Luizda Luz, Bruna BarbosaMaria-Ferreira, DanieleNascimento, Adamara Machado...
    10页
    查看更多>>摘要：Neuropathic and postoperative pain are clinical conditions that impair the patient's quality of life. The current pharmacotherapy of both painful states is ineffective and accompanied by several side effects. In order to develop new therapeutics targets, the secondary metabolites of plants have been extensively studied. Acmella oleracea ("jambu") is a native plant from the Amazon region and rich in alkylamides, bioactive compounds responsible for inducing anesthetic and chemesthetic sensations. We previously demonstrated that the intraplantar administration of an hexanic fraction (HF) rich in alkylamides from jambu and the synthetic isobutylalkyl amide (IBA) at 0.1 mu g/20 mu L can promote antinociceptive and anti-inflammatory effects. Thus, this study aimed to evaluate the local effect of HF and IBA (0.1 mu g/20 mu L) on neuropathic (partial sciatic nerve ligation, PSNL) and postoperative pain (plantar incision surgery, PIS) models in mice. Seven days after the PSNL, the mechanical (von Frey test) and cold (acetone-evoked evaporative cooling) allodynia, and digital gait parameters were analyzed. The intraplantar HF and IBA treatments attenuated the mechanical and cold allodynia as well as the static (max. Contact and print area) and dynamic (stand duration) parameters of digital gait analyses. On the day after PIS, the mechanical allodynia, heat hyperalgesia (hot plate, 52 +/- 0.1 degrees C), and spontaneous nociception scores were evaluated. Topical treatment with HF reduced the mechanical allodynia, heat hyperalgesia, and spontaneous nociception scores. In contrast, IBA treatment only partially reduced the mechanical allodynia. In summary, the local treatment with HF was effective on both neuropathic and postoperative pain, as opposed to IBA, which only had an effect on neuropathic pain.
      原文链接:
    • NSTL
    • Elsevier

    Recent advances in natural phthalides: Distribution, chemistry, and biological activities

    Meng, FanchengWang, YiboWei, XiaodongZeng, Yanping...
    20页
    查看更多>>摘要：Phthalides, an important class of bioactive natural products, are widely distributed in plants, fungi, lichens, and liverworts. Amon them, n-butylphthalide, a phthalide monomer, has been approved to cure ischemic stroke. Owing to their good bioactivities in anti-microbial, anti-inflammatory, anti-tumor, anti-diabetic, and other aspects, a large number of researches have been conducted on phthalides from nature materials. In recent years, hundreds of novel natural phthalides were obtained. This review provides profiles of the advances in the distribution, chemistry, and biological activities of natural phthalides in 2016-2022.
      原文链接:
    • NSTL
    • Elsevier

    Naphthoquinones from Catalpa bungei "Jinsi" as potent antiproliferation agents inducing DNA damage

    Liu, ShanZou, QunCai, XiaorongGuo, Zhiyong...
    7页
    查看更多>>摘要：Structure-guided isolation of a CH2Cl2-soluble fraction of the heartwood of Catalpa bungei "Jinsi" provided two new naphthoquinones, 9-hydroxy-4-oxo-alpha-lapachone (1) and 6-hydroxy-4-oxo-alpha-lapachone (2), together with three undescribed ones (3-5) and six known ones (6-11). The structures were elucidated on the basis of spectroscopic methods including electronic circular dichroism calculation. The antiproliferative effects of these isolates were evaluated in human breast adenocarcinoma cells MCF7. (4R)-4,9-dihydroxy-alpha-lapachone (5) and (4S)-4,9-dihydroxy-alpha-lapachone (6) exhibited the significant activities with IC50 values of 2.19 and 2.41 mu M, respectively. The structure-activity relationship of 1-11 in the antiproliferative assay was then discussed. The most potent 5 and 6 were found to induce cell arrest in G1 phage through DNA damage. The findings provided some valuable insights for the discovery and structural modification of alpha-lapachone as antiproliferative lead compounds against human breast adenocarcinoma cells.
      原文链接:
    • NSTL
    • Elsevier

    Two new neolignans and an indole alkaloid from the stems of Nauclea officinalis and their biological activities

    Wang, GuanghouHou, LijuanWang, YueLiu, Huan...
    8页
    查看更多>>摘要：A pair of new diastereoisomers neolignans (1-2) and a new alkaloid (7) were isolated from the stems of Nauclea officinalis: naucleaoxyneolignoside A (1), naucleaoxyneolignoside B (2), (2S,3S)-javaniside (7), together with nine known compounds, 2S-3,3-di-(4-hydroxy-3-methoxyphenye-propane-1,2-diol (3), threo-1,2-bis-(4-hydroxy-3-methoxyphenyl)-propane-1,3-diol (4), nauclefine (5), angustidine (6), naucleoxoside A (8), naucleoxoside B (9), angustoline (10), (3S,19R)-3,14-dihydroangustoline (11), and (3S,19R)-3,14-dihydroangustoline (12).The structures of 1, 2 and 7 were elucidated by extensive spectroscopic methods and the known compounds were identified by comparison of their data with those reported in the literature. The absolution configurations of 1, 2, 7,11 and 12 were confirmed by the quantum chemical CD calculation method. Compounds 1-9 showed weak to moderate inhibitory activity on nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro with IC50 values comparable to that of dexamethasone. In addition, compounds 1-9 were evaluated for the antibacterial and cytotoxic effects, and the results revealed that these compounds showed no anti-bacterial activity, and compounds 3-6 showed modest cytotoxic activity.
      原文链接:
    • NSTL
    • Elsevier