| 摘要 |
<p>#CMT# #/CMT# 3-(3,4-Dihydroxy-phenyl)-1-[3-[2-(3,4-dihydroxy-phenyl)-3,5,7-trihydroxy-chroman-4-yl]-2,4,6-trihydroxy-5-(3,4,5-trihydroxy-6-hydroxymethyl-tetrahydro-pyran-2-yl)-phenyl]-propan-1-one (I) and its salt, derivative or ester, is new. #CMT# : #/CMT# Independent claims are included for: (1) a rooibos extract comprising at least 0.4 wt.% of (I); (2) the preparation of (I); and (3) a nourishment supplying agent comprising at least 100 mg/g of the rooibos extract. #CMT#ACTIVITY : #/CMT# Neuroprotective; Neuroleptic; Nootropic; Antiparkinsonian; Antidepressant; Analgesic; Antimicrobial. #CMT#MECHANISM OF ACTION : #/CMT# None given. #CMT#USE : #/CMT# (I) or a rooibos extract is useful: as a medicament or nourishment supplying agent; to treat neurological and psychiatric disorders of central nervous system, preferably dementia, Parkinson's disease, depression, Alzheimer's disease and pain (all claimed). (I) is useful in hair, skin or mouth care applications. (I) has antimicrobial activity. No biological data given. #CMT#ADVANTAGE : #/CMT# (I) exhibits high antioxidant activity and anti-irritative effect. (I) treats diseases without any side-effects. #CMT#BIOLOGY : #/CMT# Preferred Components: The rooibos extract is obtained by the unfermented rooibos. #CMT#FOOD : #/CMT# Preferred Components: The nourishment supplying agent contains at least 1 mg of (I). #CMT#ORGANIC CHEMISTRY : #/CMT# Preparation (Claimed): Preparation of (I) comprises drying and mincing unfermented rooibos raw material with an extracting agent, preferably methanol and/or water for a predetermined extraction time at up to 60[deg] C, filtering the extracts, drying the filtrate under reduced pressure and subsequently purifying the obtained mixture by three chromatographic separation steps using two Sephadex LH20-column and subsequently a lipophilic C18-high performance liquid chromatography-column. #CMT#ADMINISTRATION : #/CMT# Administration of (I) is peroral (40-800, preferably 300-600 mg), parenteral (preferably intravenous, subcutaneous and intramuscular) (3-60, preferably 10-30 mg) or rectal (40-80, preferably 60 mg). #CMT#EXAMPLE : #/CMT# Unfermented and minced leaves and/or branch tip of Aspalathus lineariswas mixed with methanol and water in a volume ratio of 50:50 at 60[deg] C for 1 hour under rotation. The liquid was extracted and the plant parts were filtered. The filtrate was concentrated and dried at 55[deg] C and 220 mbar. The remaining aqueous solution was diluted with water. The aqueous solution (3 l) was mixed with aqueous saturated n-butanol (1.5 l) and the butanol phase was concentrated under reduced pressure to obtain butanol extract. The butanol extract (approximately 50 g) was chromatographed over Sephadex LH20-column with 50 vol.% of methanol. Further, butanol extract (50 g) was dissolved in mobile phase (400 ml) and introduced into a separation column. The stationary phase was filtered and the eluate was dried to obtain methanol extract (approximately 0.5-1%). Methanol extract (approximately 4 g) was chromatographed using Sephadex LH20-column with methanol (80 vol.%). Further butanol extract (4 g) was dissolved in mobile phase (40 ml) and introduced into a separation column to obtain 3-(3,4-dihydroxy-phenyl)-1-(3-(2-(3,4-dihydroxy-phenyl)-3,5,7-trihydroxy-chroman-4-yl)-2,4,6-trihydroxy-5-(3,4,5-trihydroxy-6-hydroxymethyl-tetrahydro-pyran-2-yl)-phenyl)-propan-1-one.</p> |
