Identification of anti-cariogenic/low-glycemic activity factors from Lo Han Kuo

描述（由申请人提供）：虽然市面上有许多人工甜味剂，旨在为蔗糖/高果糖玉米糖浆提供零卡路里或低卡路里的人工替代品，但仍存在对普通人群或特定人群（例如苯酮尿症患者和糖尿病患者）潜在健康问题的担忧。此外，已作为非龋齿甜味剂销售的改性糖醇替代甜味剂，如山梨醇、木糖醇，以及最近作为低碳水化合物饮食甜味剂销售的甜味剂，已被观察到对某些个体有潜在的胃肠道紊乱。因此，鉴定新型甜味剂似乎仍有一个可行的市场，这些甜味剂可以：(1)一般人群使用；(2)具有抗龋齿能力；(3)血糖指数低，对健康的负面影响可以忽略；(4)增甜指数高，用量少；(5)具有在加热（即烘烤、烹调）、酸性条件（即碳酸饮料）、耐冷冻（即冰淇淋）下仍能保持其增甜能力的化学结构，可作为桌面增甜剂；(6)是天然的，对健康有很多好处。本提案描述了一种新的零卡路里高强度天然甜味剂，从中国罗汉果（Momordica grosvenori）中提取的罗汉果（LHK）提取物的研究。LHK提取物的甜度是蔗糖的300倍，最近在工业规模上得到了分离；然而，很少有重要的研究来阐明甜味剂的功能以及与潜在健康益处相关的生物学参数。综合我们的初步研究表明，枸杞提取物对口腔微生物具有抗菌活性，并具有体外低血糖作用。在这个I期计划中，将从LHK提取物中分离出生物活性成分并确定其化学结构。这些成分将评估其潜在的抗龋齿，抗牙周炎和胰岛素诱导特性。本提案是开发和记录的方法，将允许分离和表征的有效成分的LHK提取物。功能特性的纯化和筛选方法的发展代表了本STTR第一阶段的可交付成果。这一STTR的成功将确定一种具有治疗性口服和一般健康益处的有价值的甜味剂商业化的潜力。

DESCRIPTION (provided by applicant): While there exist numerous artificial sweeteners that are commercially available, designed to provide zero- or low-calorie artificial alternatives to sucrose/high fructose corn syrup, there remain concerns regarding potential health concerns in the general population or unique subsets of individuals (e.g. phenylketonurics and diabetics). Moreover, altered sugar alcohol substitute sweeteners, i.e. sorbitol, xylitol, that have been marketed as noncariogenic sweeteners, and more recently as sweeteners for low carbohydrate diets, have been observed to have the potential for gastrointestinal disturbances in some individuals. Thus, there appears to remain a viable market for the identification of novel sweetening agents that can be: (1) used by the general population; (2) demonstrate a anti-cariogenic capacity; (3) have a low glycemic index and negligible negative health effects; (4) has high sweetening index so low amounts can be used; (5) have a chemical structure that maintains its sweetening ability with heating (i.e. baking, cooking), acid conditions (i.e. carbonated drinks), withstand freezing (i.e. ice cream), and can be used as a tabletop sweetening agent; and (6) are natural with many health benefit. This proposal describes studies evaluating a novel zero-calorie high intensive natural sweetener, Lo Han Kuo (LHK) extract, derived from the Chinese Lo Han Kuo fruit (Momordica grosvenori). LHK extract is 300 times sweeter than sucrose and has recently been isolated on an industrial scale; however, little critical research has been conducted to elucidate the sweetening function coupled with biological parameters as related to potential health benefits. A composite of our preliminary studies provides evidence that LHK extract has antibacterial activity against oral microorganisms and has a low-glycemic capability in vitro. In this Phase I proposal, bioactive components will be isolated from LHK extract and their chemical structures determined. These components will be evaluated for their potential anti-caries, anti-periodontitis, and insulin-inductive properties. This proposal is to develop and document methods that will allow the active components of LHK extract to be isolated and characterized. The development of purification and screening methods for functional properties represents the deliverables for Phase I of this STTR. Success of this STTR will define the potential to commercialize a valuable sweetener with therapeutic oral and general health benefits.