Natural products from plants and microorganisms traditionally have provided the pharmaceutical industry with one of the most important sources of “lead” compounds in the search for new drugs and medicines. The diversity of polyphenol structure is enormous. They are classified into several classes, the most important polyphenol in our food being phenolic acids and flavonoids, which include flavonol as one of subgroups. Flavonols are a group of plant secondary metabolites containing hydroxyl in 3rd position of chromone ring of a ‘6+3’ flavonoid ring structure. Several health beneficial activities have been attributed to these naturally occurring plant flavonols, including antioxidative, anticarcinogenic, vasoprotective, anti-inflammatory, neurodegenerative, antidiabetic, antiplatelet activities, among which antioxidative properties remain the main topic investigated in recent years. The main aim of this review is to put forward the pharmacological importance of major flavonols and newly found flavonol derivatives from the last 10 years and their related bioactivity as lead compounds. The bioactivity of these flavonoids depends on structure-activity relationship (SARs), the flavonols being one of the structurally active compounds. Most studies have demonstrated their occurrence and their absorption in humans, but the question remains as to which form is actually absorbed: aglycone, glycosidic or both. The major flavonols such as quercetin, kaempferol, myricetin, rutin, isorhamnetin, and galangin were found to exhibit anticancer activity. These flavonols also have positive effects on major diseases such as cardiovascular disease, type-2 diabetes, and Alzheimer’s disease. They are also found to have therapeutic value against osteoporosis, platelet aggregation, and antioxidant activity, the major action of prevention.

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黄酮醇和黄酮醇衍生物作为治疗分子的新属

传统上，植物和微生物的天然产物为制药业提供了寻找新药和新药的最重要“铅”化合物来源之一。多酚结构的多样性是巨大的。它们被分为几类，在我们的食物中最重要的多酚是酚酸和类黄酮，其中黄酮醇是其中的一类。黄酮醇是一组植物次生代谢产物，在“ 6 + 3”类黄酮环结构的色酮环的第3位含有羟基。这些天然存在的植物黄酮醇对健康有益，包括抗氧化，抗癌，血管保护，抗炎，神经退行性，抗糖尿病，抗血小板活性，其中抗氧化性能仍然是近年来研究的主要课题。这篇综述的主要目的是提出近十年来主要黄酮醇和新发现的黄酮醇衍生物的药理学重要性及其作为先导化合物的相关生物活性。这些类黄酮的生物活性取决于结构-活性关系（SAR），黄酮醇是结构活性化合物之一。大多数研究已经证明了它们的发生及其在人体中的吸收，但是仍然存在关于哪种形式真正被吸收的问题：糖苷配基，糖苷或两者兼而有之。发现主要的黄酮醇如槲皮素，山奈酚，杨梅素，芦丁，异鼠李素和高良姜精具有抗癌活性。这些黄酮醇还对诸如心血管疾病，2型糖尿病和阿尔茨海默氏病。还发现它们对预防骨质疏松症，血小板聚集和抗氧化活性具有治疗价值。