首页> 外国专利> PURE 3R-3'R STEREOISOMER OF ZEAXANTHIN FOR TREATING MACULAR DEGENERATION IN HUMANS

PURE 3R-3'R STEREOISOMER OF ZEAXANTHIN FOR TREATING MACULAR DEGENERATION IN HUMANS

机译:玉米黄质的纯3R-3'R立体异构体用于治疗人类黄斑变性

摘要

Methods and formulations are disclosed for makingand purifying the 3R-3'R stereoisomer of zeaxanthin as asole detectable isomer, in any desired quantity, for useas a drug or vitamin by humans. Zeaxanthin, a yellowishpigment which is naturally present in macular cells inthe center of the human retina, absorbs blue and near-ultraviolet light radiation, thereby protecting retinalcells against phototoxic damage. Zeaxanthin preparationswhich contain only the desired 3R-3'R stereoisomer can beproduced by a strain of Flavobacterium mul tivorum cells(ATCC accession number 55238). These cells (and othercells transformed with their zeaxanthin-producing genes)do not create any detectable quantities of the undesiredS-S or S-R isomers of zeaxanthin, and they do notsynthesize significant quantities of other carotenoidswhich might compete against zeaxanthin for alimentaryuptake after oral ingestion. After synthesis usingmicrobial fermentation, the zeaxanthin can beconcentrated to about 5 to 20% by simple and inexpensivesteps such as solvent extraction. It can also be purifiedto much higher levels by other methods, if desired. Thepure R-R isomer can be taken orally, either as atherapeutic drug by patients suffering from maculardegeneration, or as a vitamin or nutritional supplementby anyone who wants to reduce his or her risk ofsuffering from age-related macular degeneration, which iswidespread among people over the age of about 50 or 60.Extraction solvents, stabilizing agents, and convenientformulations for oral ingestion (such as mixed withvegetable oil and encapsulated, or used as a margarine orfood additive) are also disclosed.
机译:公开了用于制备的方法和制剂并纯化玉米黄质的3R-3'R立体异构体可以检测到的任何数量的唯一可检测异构体作为人类的药物或维生素。玉米黄质,微黄色黄斑细胞中天然存在的色素人类视网膜的中心,吸收蓝色且接近紫外线辐射,从而保护视网膜细胞抵抗光毒性损害。玉米黄质制剂仅含有所需3R-3'R立体异构体的化合物可以是多菌黄杆菌菌株产生的(ATCC登录号55238)。这些细胞(和其他用玉米黄质产生基因转化的细胞)不要创建任何可检测量的不希望的玉米黄质的S-S或S-R异构体合成大量其他类胡萝卜素可能与玉米黄质竞争营养口服后摄取。合成后使用微生物发酵后,玉米黄质可以通过简单而廉价的方法浓缩至约5%至20%溶剂萃取等步骤。也可以纯化如果需要,可以通过其他方法将其提高到更高的水平。的纯R-R异构体可以口服,形式为黄斑患者的治疗药物变性,或作为维生素或营养补品任何想要减少其风险的人患有与年龄有关的黄斑变性在50或60岁以上的人群中广泛传播。萃取溶剂,稳定剂,方便口服摄入剂型(例如与植物油并封装,或用作人造黄油或食品添加剂)。

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