Digestion and absorption of Siraitia grosvenori triterpenoids in the rat.

When administered to rats, mogroside V (a pentaglucose-conjugated mogroside), the main sweetening component of Siraitia grosvenori, was mostly degraded by digestive enzymes and intestinal microflora, and was excreted in the feces as mogrol (aglycone) and its mono- and diglucosides. However, trace amounts of mogrol and its monoglucoside were found in the portal blood as sulfates and/or glucuronide conjugates.

Triterpene glycosides of Siraitia grosvenori inhibit rat intestinal maltase and suppress the rise in blood glucose level after a single oral administration of maltose in rats.

The effect of the crude extract from Siraitia grosvenori Swingle (SG-ex) on the postprandial rise in blood glucose level was investigated. The increase in plasma glucose level in response to the oral administration of maltose was significantly suppressed in rats when SG-ex was given orally 3 min before the maltose administration. There was, however, no effect when glucose was administered instead, suggesting that the antihyperglycemic effect of SG-ex is elicited by inhibition of maltase in the small intestinal epithelium. In vitro, SG-ex inhibited rat small intestinal maltase. Similar effects were also observed both in vivo and in vitro when the concentrate of the sweet elements (triterpene glycosides) prepared from SG-ex was used. Furthermore, the main sweet element of SG-ex, mogroside V, and some minor elements such as mogroside IV, siamenoside I, and mogroside III also exhibited maltase inhibitory effect with IC50 values of 14, 12, 10, and 1.6 mM, respectively. These results suggest that SG-ex exerts anti-hyperglycemic effects in rats by inhibiting maltase activity and that these effects are at least partially exerted by its sweet elements, triterpene glycosides.

Anticarcinogenic activity of natural sweeteners, cucurbitane glycosides, from Momordica grosvenori.

To search for cancer chemopreventive agents from natural resources, many phytochemicals and food additives have been screened. Consequently, two natural sweeteners, mogroside V and 11-oxo-mogroside V isolated from the fruits of Momordica grosvenori, exhibited strong inhibitory effect on the primary screening test indicated by the induction of Epstein-Barr virus early antigen (EBV-EA) by a tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA). These sweet glycosides, having cucurbitane triterpenoid aglycon, exhibited the significant inhibitory effects on the two-stage carcinogenesis test of mouse skin tumors induced by peroxynitrite (ONOO-) as an initiator and TPA as a promoter. Further, 11-oxo-mogroside V also exhibited the remarkable inhibitory effect on two-stage carcinogenesis test of mouse skin tumor induced by 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter.

Natural synergism of acid and lactone type mixed sophorolipids in interfacial activities and cytotoxicities.

Sophorolipids (SLs) naturally produced from Candida bombicola are a mixture of lactonic (SL-lactone) and acidic (SL-acid) sophorosides of 17-L-hydroxydecanoic acid with an SL-lactone:SL-acid ratio of 72:28. SLs are biodegradable low-foaming surfactants with high detergency and hardness-tolerance properties. To analyze the effect of the SL-lactone:SL-acid ratio on these properties, SL-LXs containing X% SL-lactone, in which X varied from 0 to 100, were prepared and their interfacial activities and cytotoxicities examined. The minimum surface tension values for all SLs examined were comparable. The critical micelle concentration (CMC) was 680 mg/L for SL-L0 and 62-110 mg/L for the other SLs. Interestingly, natural SL (SL-L72) had the lowest surface tension and CMC among all of the SLs examined. The foaming ability and stability of the SLs were dependent on the SL-L content. SL-L0 and L17 had higher foaming values than the other SLs examined in 0-ppm hardness water. These values greatly reduced and became constant when the SL-L content increased over 55%. The detergencies of all of the SLs examined were comparable, except for those of SL-L0 and SL-L100, which were slightly lower than those of the other SLs. These results suggest that natural synergism between SLs creates a better balance for many interfacial activities. The cytotoxicity of SL-L72 was higher than that of SL-L0, but was comparable to that of surfactin, which is commercially available for cosmetic use. The low cytotoxicities and high interfacial properties of SLs increase their usefulness as biocompatible surface active agents for many applications.

Novel characteristics of sophorolipids, yeast glycolipid biosurfactants, as biodegradable low-foaming surfactants.

Sophorolipids (SLs) are a family of glycolipid type biosurfactants, which are largely produced by the non-pathogenic yeast, Candida bombicola. In order to investigate the possibility of SLs for industrial use, here we examined the interfacial activities, cytotoxicity and biodegradability of SLs, and compared these properties with those of two lipopeptide type biosurfactants (surfactin and arthrofactin), sodium laurate (soap, SP) and four kinds of chemically synthesized surfactants including two block-copolymer nonionic surfactants (BPs), polyoxyethylene lauryl ether (AE) and sodium dodecyl sulfate (SDS). It was indicated that SLs had extremely low-foaming properties and high detergency comparable with commercially available low-foaming BPs. These interfacial activities of SLs were maintained under 100 ppm water hardness. Cytotoxicity of SLs on human keratinocytes was the same as surfactin, which has already been commercialized as cosmetic material, but higher than BPs. Moreover, biodegradability of SLs using the OECD Guidelines for Testing of Chemicals (301C, Modified MITI Test) displayed that SLs can be classified as "readily" biodegradable chemicals, which are defined as chemicals that are degraded 60% within 28 days under specified test methods. We observed 61% degradation of SLs on the eighth day of cultivation. Our results indicate that SLs are low-foaming surfactants with high detergency, which also exhibit both low cytotoxicity and readily biodegradable properties.

Antidiabetic effect of long-term supplementation with Siraitia grosvenori on the spontaneously diabetic Goto-Kakizaki rat.

Siraitia grosvenori Swingle (SG) is a traditional Chinese fruit used as a folk medicine. Its extract (SG-ex) contains potent sweet elements with a sweetness several hundred times higher than table sugar. We investigated the antidiabetic effect of SG-ex in the type 2 diabetic Goto-Kakizaki (GK) rat. Diabetic 7-week-old GK rats were fed a diet supplemented with 0.4 % of the SG-ex for 13 weeks, and its antidiabetic effects were evaluated. SG-ex had no effect on food intake or body weight. In oral glucose tolerance tests (OGTT), SG-ex supplementation improved the insulin response at 15 min (control, 63 (sem 6) pm; SG-ex, 107 (sem 20) pm; P < 0.05) and reduced the plasma glucose level at 120 min after the glucose administration (control, 18.5 (sem 0.8) mm; SG-ex, 14.8 (sem 0.7) mm; P < 0.05). The total amount of insulin in whole pancreas taken from fasting rats was higher in the SG-ex-supplemented group, which may explain the greater capacity to secrete insulin during the OGTT. Thiobarbituric acid-reactive substances in both the liver and the plasma were lower in the SG-ex-supplemented group, suggesting that an absorbable component in SG-ex has an antioxidative effect on lipid peroxidation, thereby counteracting the oxidative stress caused by a diabetic state. Excreted urine volume and urinary albumin level for 24 h were both reduced in the SG-ex-supplemented group, suggesting the attenuation of kidney damage that is caused by diabetes. These data indicate that SG-ex supplementation may prevent complications and attenuate pathological conditions for type 2 diabetes, along with its sweet characteristics.

Effect of Lo Han Kuo (Siraitia grosvenori Swingle) on nasal rubbing and scratching behavior in ICR mice.

We studied the effect of Lo Han Kuo (Siraitia grosvenori Swingle) on histamine-induced nasal rubbing and compound 48/80-induced skin scratching behavior in ICR mice. An extract and glycoside (a complex of sweet components) of Lo Han Kuo were used in the study. Both the extract and glycoside caused no significant effect on nasal rubbing or scratching behavior, even at a dose of 1000 mg/kg when administered in a single dose. However, the effect of Lo Han Kuo became clear after repeated administration, and 300 and 1000 mg/kg of both extract and glycoside significantly inhibited nasal rubbing and skin scratching behavior after consecutive treatment for 4 weeks. Both the extract and glycoside inhibited the histamine release induced by compound 48/80 at concentrations of 300 and 1000 microg/ml. From these results, it is assumed that the inhibition of nasal rubbing and skin scratching behavior induced by Lo Han Kuo occurs through a mast cell-dependent mechanism.