1.Low hygroscopic spray-dried powders with trans-glycosylated food additives enhance the solubility and oral bioavailability of ipriflavone.
Fujimori M1, Kadota K1, Kato K2, Seto Y2, Onoue S2, Sato H1, Ueda H3, Tozuka Y4. Food Chem. 2016 Jan 1;190:1050-5. doi: 10.1016/j.foodchem.2015.06.081. Epub 2015 Jun 23.
The improvement in the solubility and dissolution rate may promote a superior absorption property towards the human body. The spray-dried powders (SDPs) of ipriflavone, which was used as a model hydrophobic flavone, with trans-glycosylated rutin (Rutin-G) showed the highest solubilizing effect of ipriflavone among three types of trans-glycosylated food additives. The SDPs of ipriflavone with Rutin-G have both a significant higher dissolution rate and solubility enhancement of ipriflavone. This spray-dried formulation of ipriflavone with Rutin-G exhibited a low hygroscopicity as a critical factor in product preservation. In addition, an improvement in the oral absorption of ipriflavone was achieved by means of preparing composite particles of ipriflavone/Rutin-G via spray drying, indicating a 4.3-fold increase in the area under the plasma concentration-time curve compared with that of untreated ipriflavone. These phenomena could be applicable to food ingredients involving hydrophobic flavones for producing healthy food with a high quality.
2.Chinese herbal medicines for treating osteoporosis.
Liu Y1, Liu JP, Xia Y. Cochrane Database Syst Rev. 2014 Mar 6;3:CD005467. doi: 10.1002/14651858.CD005467.pub2.
BACKGROUND: Chinese herbal medicines have been used for a long time to treat osteoporosis. The evidence of their benefits and harms needs to be systematically reviewed.
3.Inhibitory effects of isoflavonoids on rat prostate testosterone 5α-reductase.
Bae M1, Woo M, Kusuma IW, Arung ET, Yang CH, Kim YU. J Acupunct Meridian Stud. 2012 Dec;5(6):319-22. doi: 10.1016/j.jams.2012.07.022. Epub 2012 Aug 9.
Testosterone 5α-reductase inhibitors represent important therapeutic drugs for use against androgen-dependent diseases such as benign prostatic hyperplasia, male pattern baldness, and acne. We have searched for inhibitors of rat prostate testosterone 5α-reductase in the cultured broths of many kinds of soil bacteria, and have found that cultured soybean-casein digest broths of certain bacterial strains have a potent inhibitory effect on the enzyme. We tested 10 selected isoflavonoids, including isoflavones and O-methylated isoflavones, for inhibitory effects on rat prostate testosterone 5α-reductase to determine the important structural elements for inhibition of the enzyme. Genistein, biochanin A, equol, and 3',4',7-trihydroxyisoflavone showed considerably higher inhibitory effects whereas daidzein, formononetin, glycitein, prunetin, ipriflavone, and 4',7-dimethoxyisoflavone showed lower inhibitory effects. The IC(50) values of genistein, biochanin A, equol, 3',4',7-trihydroxyisoflavone, and riboflavin, a positive control, for rat prostate testosterone 5α-reductase were 710 μm, 140 μm, 370 μm, 690 μm, and 17 μm, respectively.
4.Beneficial Effects of a Flavonoid Fraction of Herba Epimedii on Bone Metabolism in Ovariectomized Rats.
Zhao BJ1, Wang J2, Song J2, Wang CF2, Gu JF2, Yuan JR2, Zhang L2, Jiang J2, Feng L2, Jia XB2. Planta Med. 2016 Mar;82(4):322-9. doi: 10.1055/s-0035-1558294. Epub 2016 Jan 29.
A flavonoid fraction of Herba Epimedii, including eight flavonoid glycoside compounds, epimedoside A, ikarisoside F, baohuoside II, sagittatoside A, sagittatoside B, 7-O-rhamnosyl icariside II, 2″-O-rhamnosyl icariside II, and baohuoside I, was isolated and prepared from the leaves of Herba Epimedii. This study was conducted to assess the potential effect of the flavonoid fraction of Herba Epimedii on osteoporosis in ovariectomized rats. Rats received repeated administration of a vehicle (ovariectomized), the flavonoid fraction of Herba Epimedii (7.5, 15, 30 mg/kg/d), and ipriflavone (200 mg/kg/d) once a day for 8 weeks, beginning 4 weeks after ovariectomization. Then, the bone turnover markers, bone biomechanical properties, trabecular architecture, and related protein expressions were evaluated by biochemical assay kits, mechanical testing, microcomputed tomography, immunohistochemical evaluation, and Western blot analysis. Treatment with the flavonoid fraction of Herba Epimedii (15, 30 mg/kg/d) and ipriflavone (200 mg/kg/d) significantly increased bone strength while dramatically inhibiting the serum alkaline phosphatase and tartrate-resistant acid phosphatase levels in ovariectomized rats.