These results may provide evidence that oral administration of Gen exerts beneficial anti-inflammatory effects in a rodent model of TNBS-induced chronic colitis. While the sample size of this study was small, it nevertheless might encourage the realization of larger blinded randomized controlled studies for the proof of concept.

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Background and purpose: Studies with oestrogen receptora (ERa)-and ERb-selective compounds have already shown that the effects of 17b-estradiol (E 2 ) on body weight, movement drive and bone-protection are mediated via ERa. This study was based on the hypothesis that activation of ERb may antagonize ERa-mediated effects and designed to investigate potential effects of ERa/ERb heterodimers. Experimental approach: Ovariectomized (OVX) female Wistar rats were treated with combinations of the ERa-specific agonist 16a-LE2 (ALPHA; 1 and 10 mg kg À1 d À1 ), the ERb-specific agonist 8b-VE2 (BETA; 100 mg kg À1 d À1 ), the phytoestrogen, genistein (10 mg kg À1 d À1 ) and with the anti-oestrogen compound, ICI 182,780 (3 mg kg À1 d À1 ) for three weeks. The combined effects of the substances on body weight increase, tibial bone mineral density (BMD) and the influence on running wheel activity (RWA) were investigated. Key results: OVX-induced body weight increase was reduced by co-administration of genistein and BETA. Co-application of BETA or genistein with ALPHA had no effect on ALPHA-mediated bone-protection. The RWA of OVX animals was significantly reduced by treatment with genistein but stimulated by application of ALPHA. The stimulatory effect of ALPHA on RWA could be antagonized by co-treatment with the pure antioestrogen ICI 182,780 but also by co-administration of genistein or BETA. Conclusions and implications:Our results indicate that activation of ERb may modulate ERa-mediated physiological effects in vivo. The observation that substances with selective affinity for ERb are able to antagonize distinct physiological functions, like RWA, may be of great relevance to the pharmaceutical use of such drugs.

Reduced estrogen levels occurring during menopause in woman are accompanied by a variety of disorders, e. g., hot flushes, depressions, osteoporosis, increase of body weight, and reduced movement drive. In this study we investigated the combined effects of physical activity, estradiol substitution, and a phytoestrogen-rich diet on bone mineral density, increase of body weight, and movement drive in an animal model. Ovariectomized (OVX) female Wistar rats were either fed an isoflavone-rich diet (IRD) or substituted with 17beta-estradiol (E2) for 3 months. Sham-operated rats (Sham) and vehicle-treated OVX animals served as controls. One half of the animals had the opportunity of voluntary wheel running. OVX rats displayed an eight times lower movement activity than Sham animals. E2 treatment, but not IRD, significantly increased the movement activity of OVX rats. During 3 months the lowest increase of body weight was observed in Sham animals, the highest rate in OVX animals. Along with running activity E2 treatment, but not IRD, also lowered the increase of body weight significantly compared to OVX animals. Bone mineral density (BMD) in the trabecular area of the tibia was strongly reduced in OVX rats compared to Sham animals. In contrast to IRD, E2 substitution resulted in a protection of BMD in this area compared to OVX animals. Our data demonstrate that body weight, movement drive, and BMD are positively influenced by E2. The steroid estrogen acts in the trabecular area of the tibia in a bone-protective manner, increases movement drive and antagonizes the increase of body weight. All these effects could not be observed in animals fed an isoflavone-rich diet.

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