マトリン

外観

白色～ほとんど白色粉末～結晶

解説

マトリン，α形は融点77 ℃．β形は融点87 ℃．[α]_D"＋38°(エタノール)．γ形は沸点223°(0.8 kPa)．d₄²⁰"1.088．δ形は融点84 ℃．[α]_D"＋41°(水)．水，ベンゼン，クロロホルム，エーテルに可溶．臭化水素酸塩は融点272～275 ℃．総アルカロイドを水酸化カリウムで加水分解すると，マトリン酸カリウムC15H25N2O2K(融点239 ℃)として容易に精製できる．これを2％ 塩酸と処理すると，マトリン塩酸塩となり，アルカリ処理でマトリンを再生する．中枢抑制，抗原虫作用，末梢血管収縮などの薬効が報告されているが，毒性が強いので多量には用いられない．

森北出版「化学辞典（第2版）

用途

マトリン(Matrine)は、クララ属の植物に含まれるアルカロイドである。抗がん作用、オピオイド受容体のκ-受容体やµ-受容体へのアゴニスト等、様々な薬理作用を持つ。
マトリンは、in vitroでもin vivoでも強い抗腫瘍作用を示す。マトリンの抗腫瘍作用は、細胞増殖の阻害とアポトーシスの誘導によるものと考えられている。またマトリンは、中国の伝統的な薬草であるクララの成分でもある。
マトリンや関連化合物のオキシマトリンは、イエシロアリに対する摂食阻害の効果がある。

製造

マトリン，ソホカルピジンともいう．マメ科マトリグサSophora angustifoliaの根(漢薬の苦参)および同属の植物より得られるアルカロイド．ルピンアルカロイドに属し，ルパニンの構造異性体である．精製方法の違いにより，次の4種類の多形が存在し，これらは相互転換できる．

説明

Matrine is an alkaloid isolated from the traditional Chinese medicine Sophora flavescens Aiton. The extraction process involves the use of organic solvents on dry roots, plants, and fruits of kushen 苦参 (Sophora flavescens Ait). Matrine is also present in S. alopecuroides L. and S. subprostrata Chun et T. Chen.
Chinese medicine Radix Sophora flavescentis have dampness eliminating insecticide and diuretic effects. Sophora flavescens is used for heat dysentery, hemafecia, jaundice and anuria, red leukorrhea, vulva pruritus, eczema, wet sores, skin itching, scabies, ringworm, and trichomonas vaginitis. Sophora flavescens is recorded in the ancient Materia Medica. “Southern Yunnan Materia Medica” also recorded the effects of Saphora flavescens.
Sophora flavescens is a species of Sophora japonica and is distributed in temperate and subtropical regions. Sophora flavescens is widely distributed in China, mainly in the north of Hebei, the west of Henan, and southwest of Shandong, Anhui, Hubei, and Guizhou.

化学的特性

Matrine is a white crystal or powder in the form of needles, which can turn yellow with prolonged exposure to air. It is soluble in water, benzene, chloroform, and methanol, but only slightly soluble in petroleum ether. Matrine has a melting point of 76°C (α-matrine), 87°C (β-matrine), 223°C (γ-matrine), and 84°C (δ-matrine), and a specific optical rotation of +31 to +36°.

来歴

As early as the 1930s, the Soviet Union began to study Sophora flavescens, and the china research began in 1972. Sophora flavescens in the chemical composition are divided into two major categories of alkaloids and flavonoids. Global research efforts are currently concentrated on studying alkaloids. So far, there are 23 species of alkaloids isolated and identified in roots, stems, leaves, and flowers of Sophora flavescens. The main components of Sophora flavescens have obvious anti-cancer effects, and oxymatrine has anti-cancer and antiaging effects.

使用

(+)-Matrine is an alkaloid compound extracted from the roots of Sophora species which maintain anti-inflammatory, anti-cancer and a host of other positive pharmacological effects. Apoptotic agent.

適応症

In clinical settings, matrine injection was used for chronic active hepatitis, and suppository was used for trichomoniasis or Candida vaginitis and chronic cervicitis and can also be used for senile vaginitis and pelvic inflammatory disease.

定義

ChEBI: Matrine is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and μ-receptor agonist.

薬理学

Matrine has antiarrhythmic, anti-inflammatory, anti-fibrosis, and anti-tumor effects. It has significant effects of negative frequency and positive inotropic action, which can enhance myocardial contractility, slow down the heart rate, and extend the PR and QTC interval. Matrine can promote the expression of the bcl-2 gene and can improve the ratio of bcl-2/Bax to inhibit apoptosis of myocardial cell caused by myocardial ischemia reperfusion and then reduce myocardial deficiency caused by coronary atherosclerotic heart disease and myocardial infarction to achieve the role of antiarrhythmic. In addition, matrine can also play an anti-pulmonary fibrosis effect by inhibiting the proliferation of lung fibroblasts and the expression of pulmonary interstitial fibroblasts (FN).

臨床応用

Matrine has multiple pharmacological effects and can treat a variety of diseases in clinical setting. At present, the researches on matrine are mainly focused on antiliver injury and liver fibrosis and anti-tumor and anti-cardiovascular diseases. It was worthy of attention that matrine has other pharmacological activities, such as leukocyte-elevating effects and anti-virus effects, and these effects were necessary for further development and utilization. The pharmacological effects of matrine stayed in the experimental phase, and they need further development and research to promote the development of clinical practice. Improvements in the modern formulation of matrine can improve their clinical application.