Naxagolide

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Ma'arif Burhan - One of the best experts on this subject based on the ideXlab platform.

  • In silico analysis of phytochemical compounds in Ethyl Acetate fraction of Semanggi (Marsilea crenata Presl.) leaves as neuroprotective agent
    2020
    Co-Authors: Agil Mangestuti, Laswati Hening, Kuncoro Hadi, Ma'arif Burhan
    Abstract:

    Objective: Phytoestrogen is a group of compounds that can replace the estrogen function in the body. One of its roles was as neuroprotective with anti-neuroinflammatory mechanism, by inhibiting classical pathway activation of microglia cell. Marsilea crenata Presl. is a plant that suspected to contain phytoestrogens. The aim of this research was to determine the metabolite profile of ethyl acetate fraction of M. crenata using UPLC-QToF-MS/MS, and prediction the anti-neuroinflammatory activity of compounds with molecular docking. Methods: The 100 ppm of 96% ethanol extract in DCM and methanol were injected 5 µl each into the UPLC-QToF-MS/MS, and then analyzed by Masslynx 4.1 software to determine the compounds. The compounds from metabolite profiling then prepared with SwissADME webtool and Avogadro 1.90.0 software, molecular docking was done using Autodock Vina and Biovia Discovery Studio Visualizer. Results: The result of metabolite profiling shows a total 128 compounds in both DCM and methanol. The molecular docking results showed that the seven compounds were predicted to be phytoestrogen compounds, there are 7 compounds that are predicted to have activities similar to 17ß-estradiol, they are 11-Aminoundecanoic acid, dopamantine, Naxagolide, 1,1'-(Decylimino)di(2-propanol), 3-(Hexadecylamino)-1,2-propanediol, 2-Chloro-4-(1H-imidazol-1-yl)-6-(1-piperidinyl)-1,3,5-triazine, and Jasmolone. Conclusion: The compounds of ethyl acetate fraction from M. crenata were predicted have similar activities to 17ß-estradiol to be phytoestrogen compounds, which have potential as anti-neuroinflammatory

Agil Mangestuti - One of the best experts on this subject based on the ideXlab platform.

  • In silico analysis of phytochemical compounds in Ethyl Acetate fraction of Semanggi (Marsilea crenata Presl.) leaves as neuroprotective agent
    2020
    Co-Authors: Agil Mangestuti, Laswati Hening, Kuncoro Hadi, Ma'arif Burhan
    Abstract:

    Objective: Phytoestrogen is a group of compounds that can replace the estrogen function in the body. One of its roles was as neuroprotective with anti-neuroinflammatory mechanism, by inhibiting classical pathway activation of microglia cell. Marsilea crenata Presl. is a plant that suspected to contain phytoestrogens. The aim of this research was to determine the metabolite profile of ethyl acetate fraction of M. crenata using UPLC-QToF-MS/MS, and prediction the anti-neuroinflammatory activity of compounds with molecular docking. Methods: The 100 ppm of 96% ethanol extract in DCM and methanol were injected 5 µl each into the UPLC-QToF-MS/MS, and then analyzed by Masslynx 4.1 software to determine the compounds. The compounds from metabolite profiling then prepared with SwissADME webtool and Avogadro 1.90.0 software, molecular docking was done using Autodock Vina and Biovia Discovery Studio Visualizer. Results: The result of metabolite profiling shows a total 128 compounds in both DCM and methanol. The molecular docking results showed that the seven compounds were predicted to be phytoestrogen compounds, there are 7 compounds that are predicted to have activities similar to 17ß-estradiol, they are 11-Aminoundecanoic acid, dopamantine, Naxagolide, 1,1'-(Decylimino)di(2-propanol), 3-(Hexadecylamino)-1,2-propanediol, 2-Chloro-4-(1H-imidazol-1-yl)-6-(1-piperidinyl)-1,3,5-triazine, and Jasmolone. Conclusion: The compounds of ethyl acetate fraction from M. crenata were predicted have similar activities to 17ß-estradiol to be phytoestrogen compounds, which have potential as anti-neuroinflammatory

Laswati Hening - One of the best experts on this subject based on the ideXlab platform.

  • In silico analysis of phytochemical compounds in Ethyl Acetate fraction of Semanggi (Marsilea crenata Presl.) leaves as neuroprotective agent
    2020
    Co-Authors: Agil Mangestuti, Laswati Hening, Kuncoro Hadi, Ma'arif Burhan
    Abstract:

    Objective: Phytoestrogen is a group of compounds that can replace the estrogen function in the body. One of its roles was as neuroprotective with anti-neuroinflammatory mechanism, by inhibiting classical pathway activation of microglia cell. Marsilea crenata Presl. is a plant that suspected to contain phytoestrogens. The aim of this research was to determine the metabolite profile of ethyl acetate fraction of M. crenata using UPLC-QToF-MS/MS, and prediction the anti-neuroinflammatory activity of compounds with molecular docking. Methods: The 100 ppm of 96% ethanol extract in DCM and methanol were injected 5 µl each into the UPLC-QToF-MS/MS, and then analyzed by Masslynx 4.1 software to determine the compounds. The compounds from metabolite profiling then prepared with SwissADME webtool and Avogadro 1.90.0 software, molecular docking was done using Autodock Vina and Biovia Discovery Studio Visualizer. Results: The result of metabolite profiling shows a total 128 compounds in both DCM and methanol. The molecular docking results showed that the seven compounds were predicted to be phytoestrogen compounds, there are 7 compounds that are predicted to have activities similar to 17ß-estradiol, they are 11-Aminoundecanoic acid, dopamantine, Naxagolide, 1,1'-(Decylimino)di(2-propanol), 3-(Hexadecylamino)-1,2-propanediol, 2-Chloro-4-(1H-imidazol-1-yl)-6-(1-piperidinyl)-1,3,5-triazine, and Jasmolone. Conclusion: The compounds of ethyl acetate fraction from M. crenata were predicted have similar activities to 17ß-estradiol to be phytoestrogen compounds, which have potential as anti-neuroinflammatory

Kuncoro Hadi - One of the best experts on this subject based on the ideXlab platform.

  • In silico analysis of phytochemical compounds in Ethyl Acetate fraction of Semanggi (Marsilea crenata Presl.) leaves as neuroprotective agent
    2020
    Co-Authors: Agil Mangestuti, Laswati Hening, Kuncoro Hadi, Ma'arif Burhan
    Abstract:

    Objective: Phytoestrogen is a group of compounds that can replace the estrogen function in the body. One of its roles was as neuroprotective with anti-neuroinflammatory mechanism, by inhibiting classical pathway activation of microglia cell. Marsilea crenata Presl. is a plant that suspected to contain phytoestrogens. The aim of this research was to determine the metabolite profile of ethyl acetate fraction of M. crenata using UPLC-QToF-MS/MS, and prediction the anti-neuroinflammatory activity of compounds with molecular docking. Methods: The 100 ppm of 96% ethanol extract in DCM and methanol were injected 5 µl each into the UPLC-QToF-MS/MS, and then analyzed by Masslynx 4.1 software to determine the compounds. The compounds from metabolite profiling then prepared with SwissADME webtool and Avogadro 1.90.0 software, molecular docking was done using Autodock Vina and Biovia Discovery Studio Visualizer. Results: The result of metabolite profiling shows a total 128 compounds in both DCM and methanol. The molecular docking results showed that the seven compounds were predicted to be phytoestrogen compounds, there are 7 compounds that are predicted to have activities similar to 17ß-estradiol, they are 11-Aminoundecanoic acid, dopamantine, Naxagolide, 1,1'-(Decylimino)di(2-propanol), 3-(Hexadecylamino)-1,2-propanediol, 2-Chloro-4-(1H-imidazol-1-yl)-6-(1-piperidinyl)-1,3,5-triazine, and Jasmolone. Conclusion: The compounds of ethyl acetate fraction from M. crenata were predicted have similar activities to 17ß-estradiol to be phytoestrogen compounds, which have potential as anti-neuroinflammatory

Seabrook G. R. - One of the best experts on this subject based on the ideXlab platform.

  • Comparison between the pharmacology of dopamine receptors mediating the inhibition of cell firing in rat brain slices through the substantia nigra pars compacta and ventral tegmental area.
    2024
    Co-Authors: Bowery B., Rothwell L. A., Seabrook G. R.
    Abstract:

    1. Electrophysiological recordings were made from presumed dopaminergic neurons in the substantia nigra pars compacta and ventral tegmental area of rat brain slices. The ability of selective dopamine receptor agonists to hyperpolarize neurones and inhibit cell firing, as well as the ability of dopamine receptor antagonists to block responses to quinpirole were compared. 2. Six dopamine receptor agonists were examined for their ability to hyperpolarize neurones within the substantia nigra pars compacta. Of these, the most potent ligand tested was Naxagolide with an EC50 value of 20 nM and estimated maximum of 10 mV. The rank order of agonist potency was Naxagolide > quinpirole > apomorphine > dopamine. 3. Quinpirole was more potent at inhibiting cell firing in the substantia nigra pars compacta (pIC50 = 7.65 +/ 0.06, n = 35) than in the ventral tegmental area (pIC50 = 7.24 +/- 0.06, n = 32; P < 0.01, Student's t test). 7-Hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OH-DPAT), a putative D3 selective agonist, had a comparable potency to quinpirole in both the ventral tegmental area (pIC50 = 7.39 +/- 0.26, n = 4), and substantia nigra pars compacta (pIC50 = 7.71 +/- 0.20; n = 4). 4. The inhibition of cell firing by quinpirole was antagonized by haloperidol, S(-)-sulpiride, clozapine, and ritanserin. S(-)-sulpiride and haloperidol had the highest estimated affinities in the substantia nigra, with pA2 values of 8.97 (slope = 0.85) and 8.20 (slope = 2.09) respectively.(ABSTRACT TRUNCATED AT 250 WORDS