皮珀斯沙门诺酸,是来自Piper sarmentosum的新型胺类
Kexin Zhou1, Lizhu Han2, Wenlong Li1
1College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang 712046, China; School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou 310053, China.
Fitoterapia
|June 21, 2024
概括
这项研究从Piper sarmentosum中分离了六种新的胺类化合物,并测试了它们的生物活性. 化合物1,2和12显示神经炎症抑制,而1,2,7和11抑制了乙胆酶.
科学领域:
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- Piper sarmentosum是一种用于传统医学的植物.
- 胺基类化合物是一种具有多种生物活性的化合物.
研究的目的:
- 为了从Piper sarmentosum中分离和识别胺类化合物.
- 评估单独的化合物对细胞毒性,神经炎症抑制和乙胆酶抑制的作用.
主要方法:
- 对Piper sarmentosum的空中部件进行化学研究.
- 使用HRESIMS和1D/2DNMR进行结构阐明.
- 在体外检测细胞毒性,NO生产抑制和ACHE抑制.
主要成果:
- 确定了6种新的胺类化物 (pipersarmenoids A-F) 和8种已知的类似物.
- 化合物1,2和12显著抑制了氧化 (NO) 生产.
- 化合物1,2,7和11表现出中度的乙胆化酶 (AChE) 抑制活性.
结论:
- Piper sarmentosum 是一种具有潜在治疗应用的新型胺基类化合物的来源.
- 隔离的化合物显示出治疗神经炎症和阿尔茨海默病的前景.
相关概念视频
Physical Properties of Amines
3.1K
Amines with low molecular weight are usually gaseous at room temperature, while those with high molecular weight are liquid or solids in nature. Usually, low molecular weight amines have a rotten fish-like smell. Diamines typically have a pungent smell. For instance, cadaverine and putrescine, depicted in Figure 1, are two molecules responsible for decaying tissue.
3.1K
Amines: Introduction
4.3K
Amines are organic derivatives of ammonia. They are formed by replacing one or more ammonia protons with alkyl or aryl groups. Depending upon the number of organyl groups bonded to nitrogen, amines are classified as primary, secondary, or tertiary. Primary amines have one organyl group attached to the nitrogen atom, while secondary and tertiary amines have two and three organyl groups attached to the nitrogen atom, respectively.
4.3K
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
938
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...
938
Nomenclature of Aryl and Heterocyclic Amines
2.3K
The simplest aromatic amine is phenylamine, which contains an –NH2 functionality directly attached to an aromatic ring. The name aniline is designated for this skeleton. As shown in Figure 1, the common names of the functionalized anilines involve prefixes ortho-, meta-, and para- to indicate the substitution position. Different functionalized aniline derivatives also have notable trivial names.
2.3K
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
2.9K
Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
2.9K
Basicity of Heterocyclic Aromatic Amines
5.9K
Heterocyclic amines, where the N atom is a part of an alicyclic system, are similar in basicity to alkylamines. Interestingly, the heterocyclic amine having a nitrogen atom as part of an aromatic ring has much less basicity than its corresponding alicyclic counterpart. For this reason, as presented in Figure 1, piperidine (pKb = 2.8) is significantly more basic than pyridine (pKb = 8.8).
5.9K


