来自Buxus sinica的结构多样化的化物及其细胞毒性
Liwu Lin1, Jiaxin Xu1, Lu Chai1
1State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, People's Republic of China; University of Chinese Academy of Sciences, Beijing, 100049, People's Republic of China; Yunnan Key Laboratory of Natural Medicinal Chemistry Chinese Academy of Sciences, Kunming, 650201, People's Republic of China.
Phytochemistry
|May 22, 2024
概括
研究人员从Buxus sinica中发现了41种Buxus类化合物,包括20种新化合物. 一些Buxus类化合物对人类卵巢癌细胞表现出显著的细胞毒性作用,其中一种化合物特别有效.
科学领域:
- 自然产品化学 自然产品化学
- 植物化学 植物化学
- 药用化学 医学化学
背景情况:
- 布克斯物种是已知的结构多样化的类化合物的来源.
- 了解Buxus sinica的化学成分可以导致发现新的生物活性化合物.
- 以前的研究已经确定了各种具有潜在药理活动的Buxus类化合物.
研究的目的:
- 对Buxus sinica树枝和树叶的甲醇提取物进行了广泛的植物化学研究.
- 为了隔离,识别和表征新的Buxus化物.
- 评估与人类瘤细胞系对抗分离化合物的细胞毒性活动.
主要方法:
- 对Buxus sinica甲醇提取物的植物化学分析.
- 使用色谱技术分离和净化类化合物.
- 使用综合光谱方法 (例如NMR,MS) 阐明结构.
- 对人类卵巢癌细胞系的细胞毒性测定 (ES2和A2780).
主要成果:
- 鉴定了41种Buxus类化合物,其中包括20种新化合物:循环素A-I和secobuxusinines A-K.
- 结构特征揭示了独特的特征,例如氧化CH3-18在cyclobuxusininesB和基组替代在secobuxusininesCE.
- 几种分离的化合物对ES2和A2780卵巢癌细胞系表现出显著的细胞毒性作用.
- 化合物36表现出强烈的细胞毒性,其IC50值为1.33μM (ES2) 和0.48μM (A2780).
结论:
- Buxus sinica是一种丰富的多样化和新的Buxus类化合物的来源.
- 这些类化合物的独特结构特征表明了专门的生物合成途径.
- 已识别的化合物,特别是化合物36,有潜力成为开发新的抗卵巢癌治疗方法的领导者.
更多相关视频
相关概念视频
Drugs that Destabilize Microtubules
2.0K
Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
2.0K
Antidotes
630
Antidotes are medicinal substances used to counteract the harmful effects of toxins or drugs in the body. They function in various ways, each uniquely designed to combat specific toxic compounds.
Specific antidotes operate by inhibiting the enzymes that control biochemical pathways, reducing the production of harmful metabolites.
An example of an antidote is atropine, which counteracts the detrimental effects of cholinesterase inhibitors. It achieves this by deactivating muscarinic receptors,...
Specific antidotes operate by inhibiting the enzymes that control biochemical pathways, reducing the production of harmful metabolites.
An example of an antidote is atropine, which counteracts the detrimental effects of cholinesterase inhibitors. It achieves this by deactivating muscarinic receptors,...
630
Depolarizing Blockers: Pharmocokinetics
319
Depolarizing blockers are administered through intravenous injection. Succinylcholine is the most common choice of depolarizing blockers in emergency clinical practices. Although they have a rapid onset, they readily diffuse away from the motor end plate into the extracellular fluid. They are metabolized by enzymes such as liver butyrylcholinesterase and plasma pseudocholinesterases. This produces a short duration of action, typically 5-10 minutes long, unlike nondepolarizing blockers, which...
319
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
947
Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
The direct-acting...
947


