| Description: |
Negletein has anti-inflammatory and immunomodulatory activities via inhibition of TNF-α, iNOS and IL-1β, it also shows a comparable redox-active potential, and it (50 μM, 4 h) can activate Nrf2. Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells, it has anti- Alzheimer's disease activity, it inhibits the iron-dependent formation of ROS and also blocks the iron-induced oligomerization of amyloid beta 42 in vitro. Negletein has anti-hypoxia activity, it can significantly prolong the survival time of hypoxic mice.Negletein also shows significant antimicrobial activity.
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| Targets: |
TNF-α | NOS | IL Receptor | cAMP | Akt | ERK | Nrf2 | Antifection | ROS | NF-kB |
| In vitro: |
| Nat Prod Res. 2016 Sep;30(17):2002-6. | | Antimicrobial flavonoids isolated from Indian medicinal plant Scutellaria oblonga inhibit biofilms formed by common food pathogens.[Pubmed: 26508034 ] | Scutellaria oblonga Benth., a hitherto phytochemically unexplored Indian medicinal folklore plant was extracted with acetone and subjected to chromatography to yield nine flavonoids, for the first time from this plant.
METHODS AND RESULTS:
Antimicrobial assays were performed against 11 foodborne pathogens, and three molecules (Techtochrysin, Negletein and Quercitin-3-glucoside) depicted significant activity. These molecules were assessed for their rate of antibacterial action using time-kill curves which depicted complete inhibition of most of the bacteria within 12-16 h. The significant biofilm-reducing capability exhibited by these three molecules formed a significant finding of the current study. In most of the experiments, a 90-95% reduction in biofilms was observed.
CONCLUSIONS:
Thus, flavonoids as natural molecules from S. oblonga could be further researched to be used as potent antimicrobial and antibiofilm agents. | | Nat Prod Res. 2013;27(23):2227-30. | | Anti-inflammatory and immunomodulatory flavones from Actinocarya tibetica Benth.[Pubmed: 23768253] |
METHODS AND RESULTS:
Herein, we report the isolation and immunomodulatory activity of 11 phytoconstituents, viz. 7 flavonoids, 3 pentacyclic triterpenes and 1 phytosterol of an unexplored plant Actinocarya tibetica Benth.
Three flavones, 5-methoxy-6,7-methylenedioxyflavone (6), mosloflavone (7) and Negletein (8), showed promising anti-inflammatory activity via inhibition of TNF-α and IL-1β with IC50 values of 0.22, 0.71, 16.4 μM and 10.8, 7.8, 6.4 μM, respectively. These flavones also showed dose-dependent inhibition of TNF-α, IL-1β and iNOS levels in the supernatant of mouse macrophage cell line J774A. Molecular modelling studies revealed orientation and interactions of flavones 6-8 in the active site of TNF-α.
CONCLUSIONS:
These flavones can be used as a starting point to discover lead structures for treatment of inflammatory and immunomodulatory diseases. | | Arch Pharm Res. 2005 Dec;28(12):1345-9. | | Phenolic constituents with inhibitory activity against NFAT transcription from Desmos chinensis.[Pubmed: 16392667] |
METHODS AND RESULTS:
Six phenolic constituents, 2-methoxybenzyl benzoate (1), Negletein (2), 2',3'-dihydroxy-4',6'-dimethoxydihydrochalcone (3), 5,6-dihydroxy-7-methoxy-dihydroflavone (4), astilbin (5), and quercitrin (6) were isolated from the methanol extract of the dried leaves of Desmos chinensis. Their structures were elucidated from spectral and chemical data.
CONCLUSIONS:
Of these constituents, compounds 2 (IC50: 3.89 +/- 0.39 microM) and 3 (IC50: 9.77 +/- 0.26 microM) exhibited potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor, and compound 1 (IC50: 28.4 +/- 2.62 microM) exhibited moderate inhibitory activity. |
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| In vivo: |
| Zhong Yao Cai. 2015 Jan;38(1):89-92. | | Chemical Constituents with Anti-hypoxia Activity from Saussurea involucrata.[Pubmed: 26214875] | To investigate the chemical constituents with anti-hypoxia activity from Saussurea involucrata.
METHODS AND RESULTS:
The chemical constituents, isolated and purified by column chromatography from Saussurea involucrata, were identified by several spectroscopic methods. The anti-hypoxic activities of these compounds were examined using the normobaric hypoxic model of mice. Twelve compounds were isolated from petroleum ether extract of Saussurea involucrata and identified as n-octacosane (1), 1-undecanol (2), heptadecan-l-ol(3), heptacosan-1-ol(4), myristicin (5), apiol(6), β-sitosterol(7), lupeol(8), moslosooflavone (9), mosloflavone (10), Negletein(11), and 5, 6-dihydroxy-7, 8-dimethoxyflavone(12).
CONCLUSIONS:
All compounds except 7 and 8 are isolated from this plant for the first time. Compound 1, 5 and 8 - 12 can significantly prolong the survival time of hypoxic mice. |
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