LYSIONOTIN Usage And Synthesis

Description

Chinese stone Chlorophytum is the whole herb of Lysionotus pauciflorus Maxim, which belongs to Gesneriaceae. Stone Chlorophytum is a small evergreen shrub, which is born in wet places of rock slope and clings to the stone or a tree. Cutting stone Chlorophytum in summer and autumn season when leafiness, removing impu rities, and drying. Stone Chlorophytum is more in Jiangsu, Zhejiang, Anhui, Jiangxi, Hunan, Hubei, Shaanxi, Sichuan, Yunnan, Guizhou, and Guangxi.
Stone Chlorophytum has a long medical history in Yunnan, Guizhou, and south of Qinling region. The function was described in various previous dynasty medicine classics. Stone Chlorophytum tastes bitter, is flat, and goes into the lung, liver, and kidney meridians. It has been recorded in herbal formula that stone Chlorophytum could eliminate sputum and poison, promote digestion, nourish blood, and cure rheumatism, emphysema, dizziness, and various kinds of deficiency. In the classifi cation of herbs, it was recorded that stone Chlorophytum could cure hematemesis, blood vomiting, pain of waist and knee, and contusions. It has been described incommon folk medicinal herbs that stone Chlorophytum could clear the lung to relieve cough, cool blood, and hemostasis .

Physical properties

Appearance: yellow needle crystal or light yellow powder, odorless, and tasteless. Solubility: slightly soluble in chloroform and in methanol, ethanol, or ethyl acetate, very slightly soluble in ether, insoluble in water, and soluble in 5% sodium carbon ate solution, potassium hydroxide, or sodium hydroxide solution. Melting point: 197–199 °C

History

Stone Chlorophytum is the folk antituberculous herb, the fat-soluble component separated from which is lysionotin. China’s scientists for the first time found that lysionotin is the effective component of the antituberculosis in stone Chlorophytum. Xu Yin et al., who worked in Shanghai Institute of Materia Medica, Chinese Academy of Sciences, found that lysionotin is 5,7-dihydroxy 4′,6′,8-trimethoxy flavonoids by structure identification, which is the known compound nevadensin
Farkas et al. used a 14-step synthesis to demonstrate the structure of nevadensin with complex reaction steps. The synthesis route was simpler, which was designed by Tang Cheng-fang in Shanghai Institute of Materia Medica, Chinese Academy of Sciences, and the total yield was ten times higher .
oluble, clinical use of injection caused pain to the patients. In order to overcome the above shortcomings, methylamine glucoside salt of nevadensin was synthesized for intramuscular injection. The effect is significant without causing pain. In order to explore its structure-activity relationship, seven chemical analogues were designed and synthesized with good activity in antibacterial test of Mycobacterium tuberculo sis, which include 6,8-dichloro-4′-methoxyflavone, 6,7-dimethyl-4′-methoxyflavone, 6,7-dichloro-4′-methoxyflavone, dimethoxy-3′, 4′-dimethoxyflavone, 6,7-dichloro-3′, 4′-dimethoxyflavone, 6-chloro-4′-methoxyflavone, and 4-dichloro 6-(4-methoxybenzoyloxy) acetophenone (Fig. 3)

Definition

ChEBI: Nevadensin is a trimethoxyflavone that is flavone substituted by methoxy groups at positions 6, 8 and 4' and hydroxy groups at positions 5 and 7 respectively. It has a role as a plant metabolite. It is a trimethoxyflavone and a dihydroxyflavone. It is functionally related to a flavone. It is a conjugate acid of a nevadensin-7-olate.

Indications

It can make expectoration easy, relieve a cough, soften hard lumps, and dispel nodes. It is used clinically for bronchitis, lymph node tuberculosis, chill cold, etc

Pharmacology

Anti-Mycobacterium tuberculosis, Anti-inflammatory Effect
Nevadensin 200 μg/ml in vitro has obvious anti-Mycobacterium tuberculosis effect; in vivo test also has a protective effect. The treatment for lymph node is sig nificant . Nevadensin has significant inhibitory effect on the experimental arthri tis caused by serotonin, formaldehyde, and kaolin. It also has an inhibitory effect on the cotton ball granuloma. Furthermore, the anti-inflammatory effect does not depend on the presence of adrenal cortex
Antihypertensive Effect
The main role of nevadensin in the central nervous system causes blood pressure reduction, which also has an impact on the peripheral nervous system. Lateral ventricle injection of nevadensin could reduce arterial blood pressure, and the effect of lowering systolic blood pressure was stronger than that of reducing diastolic blood pressure. The mechanism might be that the action of nevadensin on α-adrenergic receptor is stronger than that of the central β-adrenergic receptor.
Scavenging Free Radicals
Phenolic hydroxyl group of nevadensin is the main active group that scavenges free radicals (OH).

Clinical Use

Nevadensin has been used for the adjuvant therapy of cervical lymph node tuberculosis, tuberculosis, bone tuberculosis, and bronchitis treatment. Adverse reactions were mainly nausea, vomiting, diarrhea and abdominal discomfort, etc

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