The reversible inhibition of calcineurin (CaN), which is the only Ca(2+)/calmodulin-dependent protein Ser/Thr phosphatase, is thought to be a key functional event for most cyclosporin A (CsA)- and tacrolimus (FK506)-mediated biological effects. In addition to CaN inhibition, however, CsA and FK506 have multiple biochemical effects because of their action in a gain-of-function model that require...

Aim: The present study investigates the anticancer activity of gossypol in combination with carboplatin in a mice model of ovarian cancer. Methods: In vitro, cytotoxic activity of gossypol (0-900 mg/ml) was assessed in ovarian cancer cell lines (NIHOVCAR3 and OVCAR8) and an epithelial cancer cell line (SHIN-3). According Chou-Talalay’s methods, the combination of i.p administered gossypol (20 o...

Conformations and inversion pathways leading to racemization of all the tautomers of gossypol, gossypolone, anhydrogossypol, and a diethylamine Schiff 's base of gossypol were investigated with MM3(2000). All forms have hindered rotation because of clashes between the methyl carbon atom and oxygen-containing moieties ortho to the bond linking the two naphthalene rings. Inversion energies genera...

Global cottonseed production can potentially provide the protein requirements for half a billion people per year; however, it is woefully underutilized because of the presence of toxic gossypol within seed glands. Therefore, elimination of gossypol from cottonseed has been a long-standing goal of geneticists. Attempts were made to meet this objective by developing so-called "glandless cotton" i...

Gossypol, the polyphenolic constituent isolated from cottonseeds, has been used as a male antifertility drug for a long time, and has been demonstrated to exhibit excellent anti-tumor activity towards multiple cancer types. The toxic effects of gossypol limit its clinical utilization, and enzyme inhibition is an important facet of this. In the present study, in vitro human liver microsomal incu...

After a feeding study comparing the growth response of rats fed a 10% protein diet of glandless cottonseed meal with the same meal to which gossypol had been bound showed the latter produced significantly lower weight gains, two experiments were conducted in which the diets were supplemented with single amino acids. The amino acids were either L-lysine, L-isoleucine, L-valine or L-threonine and...

Pima cotton production is increasing in the United States, but Pima cottonseed generally contains higher concentrations of the antinutritive pigment gossypol than conventional upland cottonseed. Heating promotes the reaction of gossypol with protein, reducing gossypol absorption and toxicity. The objective of this study was to assess the nutritional value for dairy cattle of Pima cottonseed cak...

In a program to identify new structural entities for the inhibition of the HIV-1 reverse transcriptase (RT) enzyme via database searching, a series of RT pharmacophores were developed. By utilising a novel filtering technique, the National Cancer Institute database of compounds was scanned producing 15 compounds to be screened for activity. A notable inclusion was a series of gossypol derivativ...

Gossypol is a naturally occurring compound in the cotton plant (Gossypium spp .) . Because gossypol has been recognized since the turn of the century to be toxic to animals, a limiting factor o f whole cottonseed and cottonseed meal as feed sources is their gossypol content (1) . Whole cottonseed and cottonseed meal are popular by-products of the cottonseed industry . Whole cottonseed is a good...

A study was made of the synthesis of oligomeric derivatives of gossypol with epichlorohydrin and allyl halides. The structure of the oligomeric derivatives of gossypol was confirmed by IR spectroscopic and elemental analysis. The antioxidative capacity of the oligomeric derivatives of gossypol in the inhibition of low-density polyethylene (LDPE) was investigated. Study of the antioxidative prop...