Absorption and Metabolic Behavior of Hesperidin (Rutinosylated Hesperetin) after Single Oral Administration to Sprague-Dawley Rats.

We investigated the absorption and metabolic behavior of hesperidin (hesperetin-7-O-rutinoside) in the blood system of Sprague-Dawley rats by liquid chromatography- and matrix-assisted laser desorption ionization mass spectrometries (LC-MS and MALDI-MS). After a single oral administration of hesperidin (10 mg/kg), which was expected to be absorbed in its degraded hesperetin form, we detected intact hesperidin in the portal vein blood (tmax, 2 h) for the first time. We successfully detected glucuronized hesperidin in the circulating bloodstream, while intact hesperidin had disappeared. Further MS analyses revealed that homoeriodictyol and eriodictyol conjugates were detected in both portal and circulating blood systems. This indicated that hesperidin and/or hesperetin are susceptible to methylation and demethylation during the intestinal membrane transport process. Sulfated and glucuronized metabolites were also detected in both blood systems. In conclusion, hesperidin can enter into the circulating bloodstream in its conjugated forms, together with the conjugated forms of hesperetin, homoeriodictyol, and/or eriodictyol.

Naturally Occurring Hair Growth Peptide: Water-Soluble Chicken Egg Yolk Peptides Stimulate Hair Growth Through Induction of Vascular Endothelial Growth Factor Production.

Alopecia is divided into two categories: androgenic alopecia and nonandrogenic alopecia. An androgen-dependent abnormality of biological functions causes alopecia in males, but the role of androgens is not yet elucidated in female pattern hair loss (FPHL). Modulation of androgenic activity is not effective in certain kinds of androgenic alopecia in females, as well as in cases of nonandrogenic alopecia in males and females. The hair growth drug, minoxidil, stimulates vascular endothelial growth factor (VEGF) production as well as vascularization and hair growth in females. Yet, because minoxidil has side effects with long-term use, a safe alternative hair growth agent is needed. Whereas hair develops after birth in mammalian species, hair mostly grows in a precocial bird, in the chicken, between hatching days 14 and 15. Therefore, we hypothesized that the chicken egg contains a key hair growth factor. In this study, we demonstrated that water-soluble peptides derived from the egg yolk stimulate VEGF production and human hair follicle dermal papilla cell growth. We also found that these peptides enhance murine hair growth and improve hair growth in FPHL. Finally, we characterized that water-soluble egg yolk peptides induce VEGF expression through insulin growth factor-1 receptor activation-induced hypoxia-inducible factor-1α transcription pathway. We have given the name "hair growth peptide (HGP)" to this water-soluble egg yolk peptide.

N-acetyl glucosamine and proteoglycan containing supplement improves the locomotor functions of subjects with knee pain.

The aim of this study was to investigate the effect of N-acetyl glucosamine and proteoglycan-containing supplement (NGPS) on knee pain and locomotor functions in middle-aged and elderly persons with knee pain. An open trial was conducted on 19 subjects suffering from knee pain. The subjects, aged (55.6 ± 6.9) years, were given the NGPS tablets, which they must take 3 times per day, that contain 526.5 mg of N-acetyl glucosamine (GlcNAc) and 33.6 mg of proteoglycan for 12 weeks. Subjective pain was evaluated using the Visual Analog Scale (VAS), while the function of the knee with regard to daily operation was evaluated using the Japanese Knee Osteoarthritis Score (JKOM). Walking, stair-climbing and swelling were evaluated using the Japanese Orthopedic Association Score (JOA). These items were evaluated at a baseline, and after 4, 8, and 12 weeks of NGPS treatment. The VAS scores at 8 (p = 0.004) and 12 (p < 0.001) weeks were significantly lower than that at the baseline. The JKOM total score was significantly lower at 8 and 12 weeks (p = 0.001) than that at the baseline. The JOA score in the more painful side of the leg was significantly higher at 12 weeks (p = 0.002) than that at the baseline. The present study reveals that intake of NGPS is effective for relieving knee pain and improving knee function when walking or climbing stairs, swelling and bending or stretching.

Synthesis and Characterization of a New Hydroquinone Derivative: Disodium p-Phenylene Diisostearyl Diphosphate.

A novel amphiphilic hydroquinone derivative having a C18 alkyl chain phosphate attached to the hydroquinone (HQ) moiety was chemically synthesized. The thermal stability, distribution between organic and aqueous phases, and in vitro skin permeability were evaluated. This HQ derivative was identified as disodium p-phenylene diisostearyl diphosphate (HQ-2P2IS) by UV, infrared, mass, and nuclear magnetic resonance spectroscopies. Product HQ-2P2IS was obtained in good yield (56%), and it exhibited satisfactory stability in neutral solution, comparable to that of HQ. Its skin permeability was also higher than that of HQ. HQ-2P2IS is susceptible to enzymatic hydrolysis by tissue phosphatase, which releases HQ in the skin tissues. Thus, these characteristics indicate that the novel hydroquinone derivative presented herein, i.e., HQ-2P2IS, may serve as an effective pro-hydroquinone for skin care applications.