Aging is a complex physiological process that can be accelerated by chemical (high blood glucose levels) or physical (solar exposure) factors. It is accompanied by the accumulation of altered molecules in the human body. The accumulation of oxidatively modified and glycated proteins is associated with inflammation and the progression of chronic diseases (aging). The use of antiglycating agents is one of the recent approaches in the preventive strategy of aging and natural compounds seem to be promising candidates. Our study focused on the anti-aging effect of the flavonoid hesperetin, its glycoside hesperidin and its carbohydrate moieties rutinose and rhamnose on young and physiologically aged normal human dermal fibroblasts (NHDFs). The anti-aging activity of the test compounds was evaluated by measuring matrix metalloproteinases (MMPs) and inflammatory interleukins by ELISA. The modulation of elastase, hyaluronidase, and collagenase activity by the tested substances was evaluated spectrophotometrically by tube tests. Rutinose and rhamnose inhibited the activity of pure elastase, hyaluronidase, and collagenase. Hesperidin and hesperetin inhibited elastase and hyaluronidase activity. In skin aging models, MMP-1 and MMP-2 levels were reduced after application of all tested substances. Collagen I production was increased after the application of rhamnose and rutinose.

• MeSH
• hesperidin * farmakologie   MeSH
• hyaluronoglukosaminidasa MeSH
• kolagenasy metabolismus   MeSH
• lidé MeSH
• pankreatická elastasa MeSH
• rhamnosa * farmakologie   MeSH
• stárnutí kůže * účinky léků   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH

Triterpene bidesmosides are considered as highly cytotoxic saponins, usually less toxic against normal cells than monodesmosides, and less haemolytic. Biological activity of the betulin-type bidesmosides, rarely found in Nature, and seldom prepared due to serious synthetic problems, is poorly recognized. We report herein a protocol for the preparation of disubstituted lupane saponins (betulin bidesmosides) by treatment of their benzoates with potassium carbonate in dichloromethane / methanol solution. Cytotoxicity of all compounds was tested in vitro for a series of cancer cell lines, as well as normal human skin BJ fibroblasts. Presence of l-rhamnose moiety is crucial for cytotoxicity of betulin bidesmosides. On the other hand, l-arabinose fragment connected to lupane C-3 carbon atom significantly decreases activity. Presented results clearly show that betulin bidesmosides have significant clinical potential as anticancer agents.

• MeSH
• antitumorózní látky chemická syntéza   chemie   farmakologie   MeSH
• buněčné linie MeSH
• HeLa buňky MeSH
• lidé MeSH
• MFC-7 buňky MeSH
• nádory farmakoterapie   MeSH
• rhamnosa analogy a deriváty   chemická syntéza   farmakologie   MeSH
• triterpeny chemická syntéza   chemie   farmakologie   MeSH
• viabilita buněk účinky léků   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

The effect of unsubstituted deoxyhexoses, 2-deoxy-D-glucose (2-DG) and L-fucose, on tumor cells has been reported in several papers throughout the last decades. That of a similar deoxysugar, L-rhamnose, which is synthesized in bacteria and plants but not in animal cells, has until today not been explored. In the present study, we examined the effect of L-rhamnose on DNA and protein synthesis, growth and the potential induction of apoptosis of tumor cells in vitro. Using 2-DG for comparison, we studied the effect of L-rhamnose in concentrations up to 20 (32 resp.) mmol/l on the initial velocity of the incorporation of labeled precursors of DNA and proteins in short term cultures of both mouse Ehrlich ascites tumor (EAT) and human HL-60 cells in vitro, and further, on cell proliferation and apoptosis induction in HL-60 cells. Neither cytotoxic nor cytostatic effects of L-rhamnose were observed with the exception of slightly pronounced inhibition of DNA synthesis in EAT cells. From the lacking inhibition of the protein synthesis it can be considered that L-rhamnose does not interfere with energy metabolism, at least not in a similar manner as 2-DG.

• MeSH
• antitumorózní látky farmakologie   MeSH
• apoptóza účinky záření   MeSH
• buněčný cyklus účinky léků   MeSH
• deoxyglukosa farmakologie   MeSH
• experimentální nádory mléčných žláz metabolismus   patologie   MeSH
• HL-60 buňky MeSH
• lamin typ B metabolismus   účinky léků   MeSH
• lidé MeSH
• myši MeSH
• nádorové buňky kultivované účinky léků   MeSH
• proliferace buněk účinky léků   MeSH
• rhamnosa farmakologie   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• myši MeSH
• zvířata MeSH