3β-[(3-O-メチル-2,6-ジデオキシ-α-L-arabino-ヘキソピラノシル)オキシ]-11α,14-ジヒドロキシ-5β-カルダ-20(22)-エノリド

3β-[(3-O-メチル-2,6-ジデオキシ-α-L-arabino-ヘキソピラノシル)オキシ]-11α,14-ジヒドロキシ-5β-カルダ-20(22)-エノリド 化学特性,用途語,生産方法

• 説明

  Divasidum is a cardiac glycoside compound found in the seeds of Apocynaceae plant Strophanthus divaricatus. Strophanthus divaricatus is also known as Gelsemium elegans and Morinda umbellata L. This plant was recorded in Flora of China . “Bencaoqiuyuan” suggested that it can be used for treating itching and tinea capitis. “Lu Chuan Materia Medica” and “Lingnan herbal medicine” also suggest that it is useful for treating sore, congestion, malignant ulcers, and bruises. It grows in Guizhou, Yunnan, Guangxi, Guangdong, and Fujian provinces in China. It is also distributed in Vietnam and Laos. Divasidum, decogenin, sarmentogenin, sarmutogenin, bipindogenin, and other types of cardiac glycosides are found in the roots, stems, leaves, and other parts of Strophanthus divaricatus. In China, divasidum has been developed into injection for the treatment of heart failure.

• 物理的性質

  Appearance: small white crystalline powder, odorless, bitter taste. Solubility: soluble in water, chloroform, or ether.

• 来歴

  A white amorphous saponin was first extracted from the seeds of Strophanthus divari_x005fcatus in 1940, and the content is 1.8%. Strophanthiline A, B, and C were then identified. Its effect is about two-thirds of that of strophanthin K.?Then, divaricoside (content 0.46%) and caudoside (content 0.19%) were identified in 1953 and 1954 .

• 適応症

  This product is included in the Pharmacopoeia of the People’s Republic of China (1963). Divasidum injection can treat congestive heart failure and myocardial infarction.

• 薬理学

  The cardiotonic action of divasidum is similar to strophanthidin . The positive inotropic action of strophanthidin at the high concentration is achieved by inhibiting Na+-K+-ATPase activity. Divasidum increases the calcium ion concentration in ventricular myocytes, and this effect is dependent on the T-type calcium channels, L-type calcium channels, and Na+-Ca2+ exchange . Another study shows that divasidum has a diuretic effect and sedative effect, and it is similar to strophanthin K . Studies have also shown that the diuretic mechanism of divasidum is the direct effect of the cardiac glycoside on the kidney, so that water and chlorine reabsorption in the renal tubules decreased, while the nitrogen excretion increased. In addition, similar as strophanthin K, divasidum is able to excite uterine smooth muscle. Six new cardiac glycosides that were isolated from the ethanol extract of Strophanthus divaricatus (Roupellina boivinii) grown in Africa inhibit the proliferation of human ovarian cancer cell line A2780 . One study in cats suggested that oral administration of divasidum did not induce drug accumulation after 5?days.

• 臨床応用

  It was observed that among the 22 patients with congestive heart failure, divasidum treatment displayed good therapeutic effect in 14 patients. In another report, divasidum treatment of congestive heart failure in 58 cases, 39 cases have good results. However, fast injection induces side effects . The current clinical application of the divasidum preparation is divasidum injection, which is a mixture of divasidum and divostroside.

3β-[(3-O-メチル-2,6-ジデオキシ-α-L-arabino-ヘキソピラノシル)オキシ]-11α,14-ジヒドロキシ-5β-カルダ-20(22)-エノリド 生産企業

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