バイカリン 化学特性,用途語,生産方法
外観
うすい黄色〜黄色, 結晶〜粉末
定義
本品は、次の化学式で表される有機化合物である。
溶解性
メタノールに極めて溶けにくく、水又はジエチルエーテルにほとんど溶けない。
用途
薬理研究用。
化粧品の成分用途
皮膚コンディショニング剤、酸化防止剤
説明
Baicalin is one of the main active ingredients obtained from the roots of huang qin
(Scutellaria baicalensis Georgi). The Pharmacopoeia of the People’s Republic of
China (2015) stipulates that the content of baicalin in radix scutellariae with dry
goods shall not be less than 9.0%. The medicinal radix scutellariae distribution in
China are now Yunnan radix scutellariae (S. amoena C.?H. Wright), sticky hairs
radix scutellariae (S. viscidula Bunge), Gansu radix scutellariae (S. rehderiana
Diels), Lijiang radix scutellariae (S. likiangensis Diels), Sichuan radix scutellariae
(S. hypericifolia Lev l.), radix scutellariae (S. tenax W.?W. Smith var. patentipilosa
G.? Y. Wu), etc., which contain a certain amount of baicalin. Radix scutellariae
medicinal has a long history in China. Listed as goods in Shen Nong’s Classic of
Materia Medica, it has been used clinically to treat diseases with symptoms such as
“heat jaundice, intestinal dysentery, edema, amenorrhea, malignant sore, and scleritis” for about 2000? years. Scutellaria is recorded in the Pharmacopoeia of the
People’s Republic of China to have the effects of “clear heat and wet, purging fire to
detoxify, stop bleeding and tocolysis.” It is one of the commonly used traditional
Chinese herbs, which is clinically used alone or with other Chinese medicine compatibility for the treatment of respiratory infections, acute dysentery, viral hepatitis,
allergic disease and gynecological disease, and so on.
化学的特性
Light yellow powder
物理的性質
Appearance: light yellow crystalline powder at room temperature. Solubility: insoluble in methanol, ethanol, and acetone; slightly soluble in chloroform and nitrobenzene; almost insoluble in water; soluble in hot acetic acid. Melting point:
202–205?°C.
来歴
The chemical research of the genus Scutellaria began in 1889. Baicalein (scutellarein) is the first flavonoid isolated from Vietnam radix scutellariae (S. altissima) in
1910. In 1922, Shibata Gui Tai and his collaborators isolated and obtained baicalin,
baicalein, wogonin, and benzoic acid from Scutellaria baicalensis.
Among the flavonoids in Scutellaria baicalensis, the content of baicalein is the
highest. Its official name is baikeli. Baicalin is formed by the combination of baicalein and one molecule of glucuronic acid. Both baicalein and baicalin exist in
Scutellaria baicalensis. Studies showed that baicalein could be transferred into
baicalin and other metabolites in the blood. However, baicalin by oral is hardly
absorbed. Baicalein can be absorbed and also rapidly converted into baicalin.
At present, there are a variety of mature extraction methods for obtaining baicalin
and baicalein from Scutellaria baicalensis. Due to the poor water solubility, oral
preparation of baicalin is mostly used in clinical practice. Research showed that
baicalin had a significant first pass effect, which led to its low bioavailability.
Baicalin-metal complexes formed by the combination of baicalin and metal ions
were found to enhance bioavailability and increase pharmacological activities.
In addition, the preparation of ester-type prednisone was easily hydrolyzed by esterase and could improve the lipid solubility of baicalin.
使用
Baicalin has been used in a study to examine its neuroprotective effect in chronically stressed rats.2
適応症
Baicalin is mainly used for the adjuvant therapy of acute and chronic hepatitis and
persistent hepatitis.
定義
ChEBI: The glycosyloxyflavone which is the 7-O-glucuronide of baicalein.
一般的な説明
Baicalin is a key flavonoid found in the roots of
Scutellaria baicalensis. It is known to have different biological activities, such as anti-oxidative, anti-inflammatory, antitumor and anti-apoptotic activities.
臨床応用
In clinical, baicalin is mainly used as the adjuvant therapy for acute and chronic
hepatitis and persistent hepatitis. Baicalin was shown to reduce the expression of
hepatitis B surface antigen, e antigen and the core antigen, and inhibited hepatitis B
virus DNA replication. Reduced serum alanine aminotransferase level was observed
in hepatitis patient treated with baicalin, and other liver function indexes were also
found to be improved. No adverse reactions about baicalin have been reported. In
addition, baicalin was reported to treat early diabetic nephropathy and alleviate the
symptoms of diabetic neuropathy
As one of the antimicrobial components of Scutellaria baicalensis, eye drops
containing 3% baicalin are used clinically in the treatment of trachoma, with the
similar curative effect as rifampicin.
Moreover, baicalein is used clinically for the treatment of enteritis and
dysentery.
酵素阻害剤
This baicalein glucuronide (FW = 446.36 g/mol; CAS 21967-41-9), also known as 5,6-dihydroxy-4-oxygen-2-phenyl-4H-1-benzopyran-7-b-D glucopyranose acid, is a flavone prodrug found in the Chinese medicinal herb Huang-chin (Scutellaria baicalensis) that is hydrolyzed to baicalein (See Baicalein). Baicalin is a slow, tight-binding inhibitor of Jack Bean urease, rapidly forming initial BA-urease complex (Ki = 3.9 × 10–3 M) that slowly isomerizes to the final complex (overall inhibition constant of Ki* = 0.15 × 10 μM. Inhibition can be reversed by dithiothreitol but not dilution of substrate. Baicalin also inhibits prolyl oligopeptidase, a cytosolic serine peptidase that hydrolyzes proline-containing peptides at the carboxy terminus of proline residues and is associated with schizophrenia, bipolar affective disorder, and related neuropsychiatric disorders. (See Pramiracetam)
バイカリン 上流と下流の製品情報
原材料
準備製品