ルチン三水和物 化学特性,用途語,生産方法
定義
本品は、次の化学式で表されるフラボノイドである。
解説
ルチン毛細血管の抵抗力を高め、透過性の亢進(こうしん)を抑制する作用を示す代表的化合物である。毛細血管が弱くてもろいためにおこる出血性の病気の治療や予防に血管補強剤や止血剤として用いられ、また高血圧や脳出血、心悸(しんき)亢進や狭心症などにも用いられることがある。アメリカのFDA（食品医薬品局Food and Drug Administration）では無効とされているが、日本では血管壁に存在するヒアルロン酸を溶かしてその透過性を高めるヒアルロニダーゼの反応を阻止するとして、臨床的に用いられることがある。
小学館 日本大百科全書(ニッポニカ)
化粧品の成分用途
ヘアコンディショニング剤、皮膚コンディショニング剤、酸化防止剤
効能
血管保護薬
使用する
ルチン通常1日150～200ミリグラムを3回に分服する。ヒトに対して常用量では毒性はない。
説明
Rutin is widely found in nature and is almost contained in all of the Rutaceae and
Sectaceae plants, especially abundant in Rutaceae, Rutaceae, Epacridaceae of leguminous,
buckwheat of Polygonaceae, Eulali of Hypericum, Berchemia polyphylla
var. leioclada of Tetranychidae, and wild wutong leaves of thistle, which are also
used as raw materials in rutin extraction. In addition, it also exists in the Ilex pubescens
of Aquifoliaceae, Forsythia of Oleaceae, pagoda tree pod of Leguminosae,
tobacco, jujube, apricots, flavedo, tomatoes, and other plants.
At present, rutin in China mainly extracted from the Sophora japonica Linn of
leguminous, which is listed in top grade of Shen Nong’s Classic Materia Medica. In
addition, tartary buckwheat, which is rich in rutin and flavonoids, is native to India
and now produced in China’s northwest, southwest, north, south, and other places.
化学的特性
Pale-Yellow Crystalline Solid
物理的性質
Appearance: light yellow or yellow-green needle crystal or crystalline powder,
tastes slightly bitter, usually contains three crystal water, melting point at 176–
178 °C. Solubility: Rutin is soluble in methanol, pyridine, alkaline solution, and
boiling water and hardly soluble in cold water, chloroform, carbon disulfide, ether,
benzene, and petroleum ether.
来歴
In the mid-1930s, Hungarian scientist Szent Gyorgy firstly separated the flavonoid
mixture. After the German pharmacy firstly made it into ranosine in 1942, the concept
of vitamin P has been established worldwide. Further study proved that rutin
was the most important flavonoids of vitamin P. These compounds were certified to
have effects on many diseases in medical.
Recently, the research of rutin mainly focuses on the extraction process improvement,
pharmacological effects, and pharmacodynamics research, aiming at improvement
of its bioavailability through the development of different dosage forms. As
for the extraction process, new extraction and purification methods have been developed
since the original alkali extraction acid precipitation method. These methods
greatly improve its extraction efficiency and reduce cost, including hot water precipitation,
hot water extraction with macroporous resin adsorbing purification,
ultrasonic radiation, hot water extraction with alcohol precipitation, cold alkali percolation
extraction with acid precipitation, continuous reflux extraction, ethanol
extraction, supercritical CO2 extraction, and enzymatic hydrolysis .
In recent years, advanced rutin dosage forms, such as rutin cyclodextrin saturation,
HPMC controlled release tablets, solid dispersion tablets, coprecipitate, and
rutin effervescent particles, greatly improve the rutin dissolution rate and its
bioavailability.
使用
Found in many plants, especially the buckwheat plant. Identity with Ilixanthin. Capillary protectant. Rutin is colored brown by tobacco enzyme under experimental conditions.
定義
ChEBI: A rutinoside that is quercetin with the hydroxy group at position C-3 substituted with glucose and rhamnose sugar groups.
薬理学
As a flavonoid substance, rutin has a significant protective effect on the cardiovascular
system, including the endothelium-dependent vasodilation through
NO-guanylate cyclase pathway, antagonization on platelet-activating factor (PAF),
inhibition on subsequent reactions induced by PAF binding to its specific membrane
receptor, and protection of myocardial cells .
Rutin also has good free radical scavenging effects. Studies showed that rutin
and its derivatives had a strong free radical scavenging effect, of which rutin possessed
the strongest antioxidant activity. Rutin removed superoxide anion and
hydroxyl radicals, exerted a strong anti-lipid peroxidation, protected mitochondria,
and enhanced the activity of superoxide dismutase (SOD).
臨床応用
Rutin is mainly used for the adjuvant treatment of hypertension and treatment for
the prevention of other bleedings due to lack of rutin, such as cerebral hemorrhage,
retinal hemorrhage, purpura, acute hemorrhagic nephritis, chronic bronchitis, and
abnormal blood osmolality, restoration of capillary elastic embolism, and also for
the prevention and treatment of diabetes and hyperlipidemia . Troxerutin, the
most important active ingredient in hydroxy rutin, is used in the treatment of varicose
veins/venous disorders, hemorrhoids, lymphedema, and postoperative edema,
treatment of thrombosis and cerebrovascular disease, and also in the treatment of
diabetes and liver disease. Since rutin has a mild effect with low cost and less
adverse reactions, especially its remarkable effect on acute cerebral infarction, it is
of great worth on promotion and application of rutin .
副作用
Rutin is usually well tolerated. And since rutin is mostly derived from fruits and vegetables, it has mostly no adverse effects when taken orally, and rutin supplements may be safe when taken in doses of up to 600 mg per day for up to 12 weeks. Side effects may include headache or stomach upset.
純化方法
The vitamin crystallises from MeOH or water/EtOH, dry it in air, then dry it further for several hours at 110o or in high vacuum at 120o. It forms yellow crystals from EtOH/Me2CO/H2O (2:1:1). It has also been purified by passing (0.5g) through a Kieselgel column (30 x 5cm) with EtOAc/MeOH/H2O (100:20:15), and after 750mL have passed through, the yellow fraction of 250mL gives the glycoside (0.3g) on evaporation. [H.rhammer et al. Chem Ber 101 1183 1968, Marini-Bettòlo Gazz Chim Ital 80 631 1950, Beilstein 18/5 V 519.]
ルチン三水和物 上流と下流の製品情報
原材料
準備製品