4-Acetoxyscirpendiol of Paecilomyces tenuipes Inhibits Na⁺/D-Glucose Cotransporter Expressed in Xenopus laevis Oocytes

Abstract

Cordyceps, an entomopathogenic fungus, contains many health-promoting ingredients. Recent reports indicate that the consumption of cordyceps helps reduce blood-sugar content in diabetics. However, the mechanism underlying this reduction in circulatory sugar content is not fully understood. Methanolic extracts were prepared from the fruiting bodies of Paecilomyces tenuipes, and 4-beta acetoxyscirpendiol (4-ASD) was eventually isolated and purified. Na + /Glucose transporter-1 (SGLT-1) was expressed in Xenopus oocytes, and the effect of 4-ASD on SGLT-1 was analyzed utilizing a voltage clamp and by performing 2-deoxy-D-glucose (2-DOG) uptake studies. 4-ASD was shown to significantly inhibit SGLT-1 activity compared to the non-treated control in a dose-dependent manner. In the presence of the derivatives of 4-ASD (diacetoxyscirpenol or 15-acetoxyscirpendiol), SGLT-1 activity was greatly inhibited in an 4-ASD-like manner. Of these derivatives, 15-acetoxyscirepenol inhibited SGLT-1 as well as 4-ASD, whereas diacetoxyscirpenol was slightly less effective. Taken together, these results strongly indicate that 4-ASD in P. tenuipes may lower blood sugar levels in the circulatory system. We conclude that 4-ASD and its derivatives are effective SGLT-1 inhibitors.

Enhancement of IL-18 expression by <i>Paecilomyces tenuipes</i>

“…Besides cordycepin and polysaccharides (Yin et al 2007), a number of bioactive constituents have been reported from P. tenuipes. These include: tenuipesine A (Kikuchi et al 2004a), spirotenuipesine A and B (Kikuchi et al 2004b), paecilomycine A, B, and C (Kikuchi et al 2004c), 4b-acetoxyscirpene-3, 15-diol (Nam et al 2001;Oh et al 2001;Yoo et al 2005), ergosterol (Nam et al 2001), and beauvericin and its analogues (Nilanonta et al 2000(Nilanonta et al , 2002. Moreover, phthalic acid, stearic acid, di (2-ethylhexyl) phthalate, and cholesterol were also reported from this mushroom (Song et al 2007).…”

Enhancement of IL-18 expression by Paecilomyces tenuipes

“…Besides cordycepin and polysaccharides (Yin et al 2007), a number of bioactive constituents have been reported from P. tenuipes. These include: tenuipesine A (Kikuchi et al 2004a), spirotenuipesine A and B (Kikuchi et al 2004b), paecilomycine A, B, and C (Kikuchi et al 2004c), 4b-acetoxyscirpene-3, 15-diol (Nam et al 2001;Oh et al 2001;Yoo et al 2005), ergosterol (Nam et al 2001), and beauvericin and its analogues (Nilanonta et al 2000(Nilanonta et al , 2002. Moreover, phthalic acid, stearic acid, di (2-ethylhexyl) phthalate, and cholesterol were also reported from this mushroom (Song et al 2007).…”