無水ブルシン 化学特性,用途語,生産方法
外観
白色の結晶性粉末
成分
ブルシンは，フジウツギ科のマチン (馬銭)の種子からとれるアルカロイド。ストリキニンと同じ部分に含まれる。苦みがあり，ストリキニンと同じ神経毒だが，効力は 20分の1の弱さ。局所鎮痛剤に使用されたが，現在は使われない。
溶解性
熱水に可溶。冷水, エタノールに難溶。酢酸エチル, グリセリンに可溶、ベンゼンに微溶。エタノールおよびクロロホルムにやや溶けやすく、水に溶けにくい。
解説
2,3-dimethoxystrichnidin-10-one．C23H26N2O4(394.46)．ブルシンは，フジウツギ科マチンStrychnos nux-vomicaの成熟種子より得られる．ストリキノスアルカロイドの一つ．四水和物は融点105 ℃(無水物178 ℃)．[α]D"－119～127°(クロロホルム)．pK1 6.04，pK2 11.7．λmax 263，301 nm(log ε 4.09，3.93)．ストリキニーネよりも水，有機溶媒に溶けやすい．同様に，猛烈なけいれん毒であり，微量を神経興奮薬として用いる．また，しばしば酸類のラセミ分割に用いられる．LD50 1 mg/kg(ラット，経口)．森北出版「化学辞典（第2版）
用途
アミノ酸等の光学分割剤、TLCの分離能測定、硝酸塩の比色定量。
使用上の注意
やや風解しやすい。
説明
As a Chinese medicine, brucine was firstly recorded in Compendium of Materia
Medica. The Chinese name for brucine is “Maqian” because it looks like ancient
coins with horse icon, where “Ma” refers to “horse” and “qian” refers to “coins.”
This traditional Chinese herb has cold, bitter, and toxic properties. It can be used to
treat typhoid fever, throat pain, and lumps. Brucine is mainly extracted from the
traditional Chinese medicine “Maqian.” In 1819, Pelletier and Caventou firstly isolated the alkaline brucine from the seeds and bark of Strychnos nux-vomica
L.?Brucine is the dry and mature seeds of Loganiaceae Evergreen tree plants including Strychnos nux-vomica L. and Strychnos pierriana A.W. Hill.
化学的特性
White powder
物理的性質
Appearance: white crystalline powder; tastes very bitter. Solubility: slightly soluble
in water; soluble in ether, chloroform, ethanol, methanol, and other organic solvents
. Melting point: 175–178?°C. Specific optical rotation: ?118°.
使用
10,11-Dimethoxystrychnine can be used for antineoplastic, convulsant.
一般的な説明
A white crystalline solid. Combustible but may require some effort to ignite. Toxic by inhalation (vapor, dust, etc.) and ingestion.
空気と水の反応
Slightly soluble in water.
危険性
Poison by ingestion and inhalation.
健康ハザード
Chemical is toxic if inhaled, swallowed, or absorbed through skin. Inhalation produces intense bitter taste. Ingestion causes nausea, vomiting, restlessness, excitement, twitching, and (rarely) convulsions. Contact with dust irritates eyes.
火災危険
Special Hazards of Combustion Products: Toxic oxides of nitrogen may form in fires.
农业用途
Rodenticide: Used in the manufacture of other chemicals, in perfumes,
as a medication for animals, and as a poison for rodents
製品名
DOLCO MOUSE CEREAL®; PIED
PIPER MOUSE SEED® (Brucine)
薬理学
1. Analgesic effects: Brucine is reported to exert analgesic effects through both
central and peripheral pathways. Possible mechanisms of the analgesic effects
include blocking the voltage-gated sodium channel, inhibiting the synthesis of
PGE2, acting on the adrenergic receptor and the L-arginine-NO pathway. Brucine
(0.48?mg/kg) can significantly elevate the pain threshold in mice.
2. Anti-tumor effects: Studies have shown that brucine inhibits the cell proliferation in breast cancer, liver cancer, leukemia, and Ehrlich ascites tumors by inducing tumor cell apoptosis, inhibiting angiogenesis, reversing tumor multidrug
resistance, and regulating the expression of various cytokines. In addition, at the
dose of 320?μg/ml, the in?vitro hepatocarcinoma cell growth inhibition rate of
brucine is nearly 100%.
3. Anti-pathogen effects: In vitro study shows that 0.1% brucine can completely
inhibit the growth of Haemophilus influenzae, Streptococcus pneumoniae, and
alpha Streptococcus and Mlicrococcus catarrhalis. At the dose of 500?μg/ml, the
inhibitory rate of brucine on human immunodeficiency virus reverse transcriptase is above 30%.
4. Other pharmacological effects: Anti-inflammation, regulation of the immune
system, regulation of the cardiovascular system, antitussive, expectorant, and
antiasthenic and antibacterial effects.
臨床応用
The applications of brucine include reducing swelling; resolving mass; activating
meridians to stop pain; attenuating rheumatism, stubborn paralysis, and numbness
paralysis; alleviating bruises; etc. It has been used for nearly a thousand years and
achieved prominent clinical efficacy. In the clinical practice, brucine is used as a
compatibility prescription or compound medicine in treating rheumatism, rheumatoid arthritis, stroke hemiplegia, dementia, retinopathy, and orthopedic and other
surgical diseases.
Brucine is the main active ingredient in Strychnos and plays an important role in
treating diseases. However, brucine is also a toxic ingredient, which limits the scope
of its clinical application. Further studies of its pharmacological effects and toxicity
will improve its clinical application.
安全性プロファイル
A poison by
subcutaneous, intravenous, and
intraperitoneal routes. An alkaloid-like
strychnine, but one-sixth as toxic. When
heated to decomposition it emits toxic
fumes of Nx,. See also STRYCHNINE
純化方法
Crystallise brucine once from water or aqueous Me2CO (as the tetrahydrate), then suspend it in CHCl3 and shake with anhydrous Na2SO4 (to dehydrate the brucine, which then dissolves). Precipitate it by pouring the solution into a large bulk of dry pet ether (b 40-60o), filter and heat to 120o in a high vacuum [Turner J Chem Soc 842 1951]. The tetrahydrate crystallises from a mixture of EtOH and H2O as colourless elongated needles [Eeles Acta Cryst 6 809 1953, Beilstein 27 III/IV 7875.] VERY POISONOUS
無水ブルシン 上流と下流の製品情報
原材料
準備製品