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Fitoterapia
Inverni della Beffa SpA
Fitoterapia

Inverni della Beffa SpA

0367-326X

Fitoterapia/Journal FitoterapiaSCIISTP
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    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

    A new ent-clerodane diterpene from Detarium microcarpum Guill. & Perr. and its protective potential for osteoporosis

    Irshad, RimshaKabbashi, Ahmed Saeed AliSalawu, Kayode MuritalaUr-Rehman, Aziz...
    8页
    查看更多>>摘要：A new clerodane diterpene, named 6 alpha-hydroxy-3,13E-clerodien-15-oic acid (1), together with a known clerodane diterpene (2), four known labdane diterpenes (3-6), a triterpenoid (7), a known steroid (8), and two benzenoid compounds (9 and 10) were isolated from Detarium microcarpum Guill. & Perr. The structures of all obtained compounds were determined by chemical properties and spectroscopic evidence, accompanied by comparisons with data in the literature. Electronic circular dichroism (ECD) was performed for compounds 1-4 to confirm the absolute configuration. Compounds 1-3 and 8-10 were evaluated for the protective effect on osteoblasts. Compound 1 was observed to increase the proliferation of dexamethasone (DEX)-treated MC3T3-E1 cells significantly at 1 mu M, which was comparable with the positive control geniposide at 10 mu M. The results were further confirmed by flow cytometry analysis. In addition, compound 1 increased the level of alkaline phosphatase (ALP) and mineralization in osteoblasts inhibited by DEX. Moreover, Compound 9 (vanillic acid) showed a pronounced inhibition (IC50 6.5 +/- 0.6 mu M) on reactive oxygen species (ROS) production, and 10 (4-O-methyl gallic acid) showed a good inhibition with IC50 as 103.3 +/- 2.2 mu M, compared with the standard drug ibuprofen (IC50 54.2 +/- 9.2 mu M). Besides, compounds 1-3 and 8-10 were non-cytotoxic against MCF 7, NCI H460, Hela, and BJ cell lines.
      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

    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

    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