scholarly journals R-(-)-Gossypol Acetic Acid

2020 ◽  
Author(s):  
Biomolecules ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 1667
Author(s):  
Jian-Hong Lin ◽  
Kun-Ta Yang ◽  
Pei-Ching Ting ◽  
Yu-Po Luo ◽  
Ding-Jyun Lin ◽  
...  

Myocardial ischemia/reperfusion (I/R) injury has been associated with ferroptosis, which is characterized by an iron-dependent accumulation of lipid peroxide to lethal levels. Gossypol acetic acid (GAA), a natural product taken from the seeds of cotton plants, prevents oxidative stress. However, the effects of GAA on myocardial I/R-induced ferroptosis remain unclear. This study investigated the ability of GAA to attenuate I/R-induced ferroptosis in cardiomyocytes along with the underlying mechanisms in a well-established rat model of myocardial I/R and isolated neonatal rat cardiomyocytes. H9c2 cells and cardiomyocytes were treated with the ferroptosis inducers erastin, RSL3, and Fe-SP. GAA could protect H9c2 cells against ferroptotic cell death caused by these ferroptosis inducers by decreasing the production of malondialdehyde and reactive oxygen species, chelating iron content, and downregulating mRNA levels of Ptgs2. GAA could prevent oxygen-glucose deprivation/reperfusion-induced cell death and lipid peroxidation in the cardiomyocytes. Moreover, GAA significantly attenuated myocardial infarct size, reduced lipid peroxidation, decreased the mRNA levels of the ferroptosis markers Ptgs2 and Acsl4, decreased the protein levels of ACSL4 and NRF2, and increased the protein levels of GPX4 in I/R-induced ex vivo rat hearts. Thus, GAA may play a cytoprotectant role in ferroptosis-induced cardiomyocyte death and myocardial I/R-induced ferroptotic cell death.


2017 ◽  
Vol 8 (4) ◽  
pp. 533 ◽  
Author(s):  
Ghulam Abbas ◽  
Ahmed Suliman Al-Harrasi ◽  
Hidayat Hussain ◽  
Samina Abdul Sattar ◽  
M. Iqbal Choudhary

<p>This study was performed to identify new inhibitors of protein glycation <em>in vitro</em>. Protein glycation is one of the major causes of late diabetic complications. In this study, terpenoids and alkaloids, isolated from different medicinal plants, along with their derivatives, were evaluated for their antiglycation activity <em>in vitro,</em> while MTT assay on mouse fibroblast 3T3 cells was used to assess their potential cytotoxicity. Among the tested compounds, gossypol (2,2′-<em>bis</em>-(formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene) (<strong>1</strong>), isolated from<em> Gossypium herbaceum, </em>and its derivatives,<em> </em>gossypol acetic acid (<strong>2</strong>), gossypolidene- 4-aminoantipyrine (<strong>4</strong>), and gazolidone (<strong>6</strong>), showed a potent antiglycation activity (IC<sub>50</sub> &lt; 16 <em>µ</em>M), while gossypolidene-4-aminoantipyrine (<strong>5</strong>) showed a significant antiglycation activity with IC<sub>50 </sub>value 82.934±2.924<em> µ</em>M, in BSA-fluorescence assay. Alkaloid, noscapine (3S)-6,7-Dimethoxy-3-[(5R)-4-methoxy-6-methyl-5,6,7,8-tetrahy-dro-1,3-dioxolo[4,5-g]isoquinolin-5-yl] isobenzofuran-1(3<em>H</em>)-one (<strong>7</strong>), isolated from <em>Papaver somniferum, N</em>-nitrosoaphyllinic acid (<strong>9</strong>), a derivative of alkaloid aphylline<em>, </em>and 2<em>H</em>-quinolizine, octahydro salt (<strong>11</strong>), a salt of alkaloid lupinine, exhibited significant inhibition activity with<em> </em>IC<sub>50 </sub>values 152.662±5.432, 393.758 ±4.001 µM and 110.203±4.816µM, respectively. Similarly, compounds<strong> </strong>gossypolidene thiocarbamide (<strong>3</strong>), deoxypeganine hydrochloride (<strong>8</strong>)<strong>, </strong>lupinine (<strong>10</strong>) and cytisine (<strong>12</strong>) showed moderate inhibition with IC<sub>50</sub> values of 401.865 ±18.450, 863.322 ±6.415, 712.176±7.745, and 728.462±2.331<em> </em>µM, respectively. The results were compared with the standard antiglycation agent, rutin (<strong>13</strong>) (IC<sub>50 </sub>=98.012±2.030 µM).</p>Cellular cytotoxicity assay showed only gossypol acetic acid (<strong>2</strong>) and gossypolidene thiocarbamide (<strong>3</strong>) as somewhat toxic to 3T3 (mouse fibroblast) cells with IC<sub>50 </sub>values<em> </em>2.07 ±0.61 and 5.00 ±1.89 µM, respectively. Cycloheximide was used as a standard in this assay with IC<sub>50</sub> value 0.3 ± 0.089 μM


1960 ◽  
Vol 43 (2) ◽  
pp. 329-331
Author(s):  
Carroll L Hoffpauir ◽  
James A Harris ◽  
J P Hughes

Reproduction ◽  
1989 ◽  
Vol 85 (1) ◽  
pp. 73-78 ◽  
Author(s):  
J. Mohan ◽  
J. N. Panda ◽  
U. S. Singh ◽  
R. P. Moudgal

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