ベルベリン 化学特性,用途語,生産方法
解説
[C20H18NO4]＋(336.37)．ウンベラチンともいう．ヒロハヘビノボラズBerberis vulgaris，オウレンCoptis japonicaの根，キハダPhellodendron amurenseの樹皮，そのほか種々の植物に広く見いだされるアルカロイド．
六水和物として結晶し，黄色の針状晶．融点145 ℃．水溶性である．ベルベリンは第四級塩基型(a)とプソイド塩基型(b)との平衡で存在し，種々の反応がこの互変異性で説明される．塩生薬である黄蘗 (おうばく) ，黄連の主成分。苦みを有し，胃の運動を促進し，唾液や胃液の分泌を亢進させる作用があるので，苦味健胃剤や整腸剤として使用される。ほかに腸管運動抑制，血圧下降，抗貧血作用，ブドウ球菌や赤痢菌の発育阻止作用がある。森北出版「化学辞典（第2版）
用途
用於含量測定/鑑定/藥理實驗等。
説明
Coptis chinensis was widely used in China as a folk medicine by Shennong around
3000 BC. Coptis chinensis was firstly described in the ancient Chinese medical
book The Divine Farmer’s Herb-Root Classic. Coptis chinensis was used to treat
intestinal bacterial infections and antipyretic analgesic for thousands of years ago
Coptis chinensis also called zhilian, chuanlian, weilian, jizhualian, shanglian,
and xuanlian in Chinese history. Coptis chinensis was accepted by most physicians,
and the Chinese pharmacopoeia also uses Coptis chinensis as its official name .
Coptis chinensis mainly grows in Anhui, Hunan, Sichuan, and Yunnan and has been
cultivated in Sichuan since the Ming dynasty, which has a long history of cultivation. Other species of Coptis chinensis from different places were used as medicine.
However, commodity circulation of wild Rhizoma coptidis has not been formed .
Coptis chinensis is national three level protection plants at present and majorly produced in Shizhu of Chongqing, West Hubei, Shanxi, and Gansu.
Berberine is a quaternary ammonium salt from the protoberberine group of isoquinoline alkaloids. It is found in some plants such as huanglian 黄连 (Rhizoma
coptidis), huangbo黄柏 (Phellodendri Chinensis Cortex), sankezhen三颗针
(Berberidis Radix), and so on.
The components of Coptis chinensis which have antibacterial and antiinflammatory effects are original alkaloid berberine class, including berberine, coptisine, palmatine, epiberberine, columbamine, jatrorrhizine, worenine, and
magnoflorine, with berberine having the highest content (5–8%).
化学的特性
White to yellow crystals. Iinsoluble in water; soluble in ether, alcohol. Salts of berberine are berberine bisulfate, berberine sulfate, and berberine hydrochloride. All three are yellow crystals, slightly soluble in water.
物理的性質
Appearance: Berberine is odorless and yellow crystalline powder. Solubility:
Berberine is soluble in hot water, slightly soluble in water or ethanol and in chloroform, and insoluble in ether. Melting point: Melting point of berberine is about
204–206?°C.?Berberine is heat labile.
来歴
Berberine is often used in the form of quaternary ammonium alkali. The solubility of berberine in water is lower, for example, berberine hydrochloride is 1:500, and berberine sulfate is 1:30. In 1926, berberine was first separated from bark of Zanthoxylum clava. Modern pharmacology study showed that berberine has defined structure and is a monomer of traditional Chinese medicine. Berberine can be obtained from many sources and is used in clinics, with reliable pharmacological effects and various and unique mechanisms.
At present, berberine can be synthesized by industrial biosynthesis. A series of derivatives can also be synthesized by structure modification, and the pharmacological activities of these derivatives have been tested.
使用
Antiseptic drug.Treat intestinal infection caused from dysentery bacillus and E.coil
世界保健機関（WHO）
Berberine, an alkaloid contained in many plants including
Berberis species, remains available in many tropical countries. Both traditional
herbal remedies and tablet formulations containing this substance have been used
in the treatment of gastrointestinal disease, and injectable preparations have been
claimed to be of value in the treatment of cutaneous leishmaniasis. The action
taken in Singapore relates to reports of jaundice, haemolytic anaemia and
kernicterus with brain damage in infants with G6PD deficiency who were exposed
either in utero or post-natally. Preparations for topical application are also
available in some countries. These have not been associated with reports of
systemic toxicity.
危険性
Toxic via ingestion, inhalation, skin absorption.
薬理学
Berberine hydrochloride has extensive pharmacological effects, such as antibacterial, antiviral, anti-inflammatory, analgesic, anticancer, hyperglycemic, antilipidemic, antihypertension, anti-arrhythmic, anti-heart failure, and so on. Experimental study and clinical reports demonstrate that berberine has therapeutic effect on the endocrine system, circulatory system, nervous system, digestive system, and respiratory system and other diseases.
The clinical indication of berberine is intestinal bacterial infectious diarrhea, which is confirmed by years of clinical application. Berberine hydrochloride exerts effect on intestinal infection, eye conjunctivitis, and suppurative otitis media induced by Shigella dysenteriae, Escherichia coli, and Staphylococcus aureus and ameliorates gastritis and combined gastric and duodenal ulcers. Berberine hydrochloride also has curative effect on acute lung injury, pneumonia, and other respiratory diseases; peptic ulcer, colitis, and other digestive system diseases; pregnancy, urinary, and reproductive system infections; and other urinary tract and reproductive system diseases.
臨床応用
Rhizoma coptidis, as the digestive tract disease medication, has a history of more
than 3000?years in China and India. Berberine, as a cathartic nonprescription drug,
is mainly used in the treatment of intestinal infection clinically. Clinical research
showed that berberine has hypoglycemic effect and has very good prevention and
treatment for diabetic patients with complications such as hypertension, hyperlipidemia, thrombosis, and inflammation
There are few oral side effects of berberine hydrochloride, accidentally appears
nausea, vomiting, rash, and fever, which can disappear after withdrawal of drug. In
patients with hemolytic anemia and lack of glucose-6-phosphate dehydrogenase, it
was forbidden to be used. Berberine if used intravenously is toxic, but is only suitable for oral drug delivery .
安全性プロファイル
An alkaloid poison by ingestionand subcutaneous routes. In humans, toxic doses lowerthe body temperature, increase peristalsis, and cause deathby central paralysis. Mutation data reported. Should carry apoison label. Should never be ingested without t
純化方法
Berberine crystallises from pet ether or ether as yellow needles or from H2O. [Beilstein 27 II 567, 27 III/IV 6539.]
ベルベリン 上流と下流の製品情報
原材料
準備製品