Characterization of Alcohol-Absorption Inhibitors from Chinese Traditional Medicines with Anti-Alcoholic Activity

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Alcoholism, which is a major health problem in the world, causes as much trouble physiologically as it dose socially. Excessive consumption of ethanol is known to affect profoundly nearly every organ in the body. In order to relieve ethanol toxicity in acute alcohol in ingestion, a couple of methods using an accelerator of ethanol metabolism and the sequestering of acetaldehyde have hitherto been reported. In addition, dehydrogenase inhibitors such as cyanamide and disulfiram have been used clinically for chronic alcoholics. It is known that dehydrogenase inhibitors force alcoholics to quit drinking based on the fear of unpleasant reaction elicited after ethanol intake, but these drugs are also reported to show many strong side effects.On the other hand, many Chinese traditional medicines have been known to have preventive and therapeutic effects for ethanol intoxication, but their active components have not been identified so far. In the course of our screening to find anti-alcoholic … More active principles contained in traditional medicines, several natural medicines were found to contain inhibitors of ethanol absorption. By monitoring the inhibitory effect on ethanol absorption in the rat, we have characterized new active triterpene oligoglycosides from Aralia elata (elatosides), Aesculus hippocastanum, A.turbinata (escins), Camellia japonica (camelliasaponins), Polygala senega var.latifolia (E,Z-senegasaponins, Z-senegins), Sapindus mukurossi (sapindosides), Kochia scoparia (kochianosides, scoparianosides), and Beta vulgaris (betavulgarosides). Furthermore, by examination of the structure requirement for the activity, it has been found that the active saponins can be classified into the following three types of structure : 1) Oleanen-28-oic acid 3-O-monodesmosides such as elatosides, sapindosides, kochianosides, scoparianosides, and betavulgarosides, 2) Acylated polyhydroxyoleanene 3-O-monodesmosides such as escine and camelliasaponins, and 3) Oleanene acylated bisdesmosides such as senegasaponins and senegins. Less