scholarly journals Two new α-Methoxy-γ-Pyrones From the Mangrove Sediment-Derived Streptomyces psammoticus SCSIO NS126

2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110414
Author(s):  
Kunlong Li ◽  
Mengdie Zhou ◽  
Ziqi Su ◽  
Xiliang Yang ◽  
Xuefeng Zhou ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Spectroscopic Analysis ◽  
Mangrove Sediment ◽  
Natural Sources ◽  
Fermentation Conditions ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Actinomycete Strain

Two new α-methoxy- γ-pyrone analogs, 2-methoxy-3-methyl-5,6-diethyl- γ-pyrone (2) and 2-methoxy-3,5-dimethyl-6-propyl- γ-pyrone (3), together with 2-methoxy-3,5-dimethyl-6-ethyl- γ-pyrone (1), firstly isolated from natural sources, were obtained from the EtOAc-solube extract of the mangrove sediment-derived actinomycete strain Streptomyces psammoticus SCSIO NS126, under the optimized fermentation conditions. Their structures were elucidated by detailed spectroscopic analysis and by comparison of their spectroscopic data with those reported in the literature. Those α-methoxy-γ-pyrones were evaluated for their acetylcholinesterase inhibitory activity; however, none of them exhibited obvious activity. Moreover, their biosynthetic relationship with piericidins was also discussed.

scholarly journals Cytotoxic Minor Piericidin Derivatives from the Actinomycete Strain Streptomyces psammoticus SCSIO NS126

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 428
Author(s):  
Kunlong Li ◽  
Ziqi Su ◽  
Yongli Gao ◽  
Xiuping Lin ◽  
Xiaoyan Pang ◽  
...  
Keyword(s):  
Renal Cell Carcinoma ◽  
Structural Diversity ◽  
Mangrove Sediment ◽  
Cytotoxic Activities ◽  
Spectroscopic Methods ◽  
Biosynthetic Pathways ◽  
Fermentation Conditions ◽  
Lead Compounds ◽  
Ic50 Values ◽  
Actinomycete Strain

The mangrove-sediment-derived actinomycete strain Streptomyces psammoticus SCSIO NS126 was found to have productive piericidin metabolites featuring anti-renal cell carcinoma activities. In this study, in order to explore more diverse piericidin derivatives, and therefore to discover superior anti-tumor lead compounds, the NS126 strain was further fermented at a 300-L scale under optimized fermentation conditions. As a result, eight new minor piericidin derivatives (piericidins L-R (1–7) and 11-demethyl-glucopiericidin A (8)) were obtained, along with glucopiericidin B (9). The new structures including absolute configurations were determined by spectroscopic methods coupled with experimental and calculated electronic circular dichroism. We also proposed plausible biosynthetic pathways for these unusual post-modified piericidins. Compounds 1 and 6 showed selective cytotoxic activities against OS-RC-2 cells, and 2–5 exhibited potent cytotoxicity against HL-60 cells, with IC50 values lower than 0.1 μM. The new piericidin glycoside 8 was cytotoxic against ACHN, HL-60 and K562, with IC50 values of 2.3, 1.3 and 5.5 μM, respectively. The ability to arrest the cell cycle and cell apoptosis effects induced by 1 and 6 in OS-RC-2 cells, 2 in HL-60 cells, and 8 in ACHN cells were then further investigated. This study enriched the structural diversity of piericidin derivatives and confirmed that piericidins deserve further investigations as promising anti-tumor agents.

scholarly journals CHEMICAL CONSTITUENTS AND ACETYLCHOLINESTERASE ACTIVITY FROM Polyalthia sumatrana (Miq.) Kurz

2022 ◽  
Vol 52 (1) ◽  
pp. 73-76
Author(s):  
Wan Mohd Nuzul Hakimi Wan Salleh ◽  
Natasa Mohd Shakri ◽  
Mohd Azlan Nafiah ◽  
Shamsul Khamis
Keyword(s):  
Cinnamic Acid ◽  
Vanillic Acid ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Chemical Constituents ◽  
Acetylcholinesterase Activity ◽  
Isolation And Identification ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Reported Data

This study was carried out to investigate the phytochemicals from Polyalthia sumatrana and their acetylcholinesterase inhibitory activity. Fractionation and purification of the leaves of P. sumatrana led to the isolation and identification of five alkaloids; boldine (1), norboldine (2), liriodenine (3), predicentrine (4), laurotetanine (5) together with β-sitosterol (6), β-sitostenone (7), vanillin (8), vanillic acid (9) and cinnamic acid (10). The structures of these compounds were obtained by analysis of their spectroscopic data, as well as the comparison with that of reported data. Acetylcholinesterase inhibitory activity revealed that all isolated alkaloids were found to inhibit AChE with percentage inhibition values ranged from 45.0 to 80.6%.

scholarly journals Chemical constituents and acetylcholinesterase inhibitory activity of Piper abbreviatum Opiz

2021 ◽  
Vol 34 (3) ◽  
pp. 625-632
Author(s):  
W. M. N. H. W. Salleh ◽  
M. A. Nafiah ◽  
K. H. Yen ◽  
H. Kassim ◽  
A. Tawang
Keyword(s):  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Chemical Constituents ◽  
Isolation And Identification ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Aerial Parts ◽  
The World ◽  
Chemotaxonomic Markers ◽  
Reported Data ◽  
Physiologically Active Compounds

Plants of the genus Piper have long been used as medicinal herbs. The chemistry of Piper species has been widely investigated and phytochemical investigations conducted in all parts of the world have led to the isolation of a number of physiologically active compounds. Thus, this study was carried out to investigate the phytochemicals from Piper abbreviatum and their acetylcholinesterase inhibitory activity, which has not been previously investigated. Fractionation and purification of the aerial parts of P. abbreviatum led to the isolation and identification of five methoxylated flavonoids, namely 5,7-dimethoxyflavone, 4ʹ,5,7-trimethoxyflavone, 3',4',5,7-tetramethoxyflavone, 5-hydroxy-7-methoxyflavone, 5-hydroxy-4ʹ,7-dimethoxyflavone, together with lupeol, lupenone, β-sitosterol, and β-sitostenone. The structures of these compounds were obtained by analysis of their spectroscopic data, as well as the comparison with that of reported data. Acetylcholinesterase inhibitory activity revealed that all isolated flavones were found to inhibit AChE with percentage inhibition values ranged from 24.2 to 58.2%. This is the first report on the isolation of methoxylated flavonoid from P. abbreviatum. The high variants of flavonoid compounds from this species may be used as chemotaxonomic markers for this Piper species.                     KEY WORDS: Piperaceae, Piper, Piper abbreviatum, Flavonoid, Acetylcholinesterase   Bull. Chem. Soc. Ethiop. 2020, 34(3), 625-632. DOI: https://dx.doi.org/10.4314/bcse.v34i3.17

Bromotyrosine alkaloids with acetylcholinesterase inhibitory activity from the Thai sponge Acanthodendrilla sp.

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
N Sirimangkalakitti ◽  
M Yokoya ◽  
K Changwichit ◽  
T Saesong ◽  
OJ Olatunji ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitory Activity

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

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