在识别卡诺索尔类似物中的功能组方面取得了进展,以解决它们在骨肌功能中的有效性
A Berger1, J Sarniguet2, G Hugon3
1PhyMedExp, Montpellier University, CNRS, INSERM, Montpellier 34090, France; MMDN, Montpellier University, EPHE, INSERM, Montpellier, France.
概括
迷香二二醇和其天然类似物在保护骨肌肉免受衰老和疾病的保护方面表现有前途. 特定的结构特征,如基团,对于它们的肌肉保护和抗氧化作用至关重要.
科学领域:
- 自然产品化学 自然产品化学
- 骨肌肉生理学 骨肌肉生理学
- 分子生物学分子生物学
背景情况:
- 骨肌损失 (缩) 与衰老,疾病和不活动有关.
- 卡诺索尔是一种迷香衍生的二烯,显示出对抗肌肉缩的潜力.
- 了解卡诺索尔的结构-活性关系是优化其治疗潜力的关键.
研究的目的:
- 调查卡诺索尔及其衍生物的结构-活性关系.
- 评估它们在减少氧化损伤和增强骨肌肉健康方面的有效性.
- 为了确定负责carnosol肌肉保护作用的关键结构特征.
主要方法:
- 合成和评估天然和合成的卡诺索尔类似物 (罗斯曼醇,伊斯诺斯曼醇,二甲基卡诺索尔,二甲基利索斯曼醇).
- 试验室检测:小鼠和人类骨肌细胞的氧化损伤 (脂质过氧化,H2AX酸化).
- 在体外测试:肌管缩和人类骨肌细胞中的MuRF1 (E3无酸酶) 抑制.
- 在体内测试:斑马鱼幼虫用于运动和肌肉纤维分析.
主要成果:
- 炭醇,罗斯曼醇和异醇对抗氧化损伤表现出类似的抗氧化活性.
- 肉醇和异醇促进了肌管缩,并抑制了MuRF1,与罗斯曼醇不同.
- 甲基化衍生物 (二甲基卡诺索尔,二甲基利索斯曼醇) 缺乏抗氧化和增肥作用.
- 炭醇和异醇改善了斑马鱼的运动和肌肉特征;甲氧化类似物没有.
- 在C-11/C-12和20,7-乳部分保存的基团对肉醇的肌肉保护作用至关重要.
结论:
- 肉醇的特定结构元素,特别是C-11/C-12的基组,对于其抗氧化和肌肉保护功能至关重要.
- 炭醇和异醇显示出缓解骨肌肉损失的显著潜力.
- 对肉醇衍生物的进一步研究可能会导致针对肌肉消耗条件的新型治疗策略.
相关概念视频
Classification of Skeletal Muscle Relaxants
2.7K
Skeletal muscle relaxants are a group of drugs that can reduce muscle stiffness and induce temporary paralysis to relieve pain. These agents can act centrally to reduce muscle tone or spasms in painful conditions such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), or spinal injuries; they are called antispasmodics or spasmolytics.
Peripherally acting skeletal muscle relaxants interfere with the neurotransmission at the neuromuscular end plate to induce paralysis during...
Peripherally acting skeletal muscle relaxants interfere with the neurotransmission at the neuromuscular end plate to induce paralysis during...
2.7K
Overview of Advanced Functional Groups
25.6K
Functional groups are groups of atoms with specific chemical properties that occur within organic molecules and are sometimes denoted as “R”. Functional groups can “functionalize” a compound by enabling it to adopt different physical and chemical properties.
Types of Advanced Functional Groups
The table below summarizes some of the major functional groups in organic chemistry.
25.6K
Classification of Skeletal Muscle Fibers
56.9K
Skeletal muscles continuously produce ATP to provide the energy that enables muscle contractions. Skeletal muscle fibers can be categorized into three types based on differences in their contraction speed and how they produce ATP, as well as physical differences related to these factors. Most human muscles contain all three muscle fiber types, albeit in varying proportions.
Slow-Twitch Muscle Fibers
Slow oxidative, muscle fibers appear red due to large numbers of capillaries and high levels of...
Slow-Twitch Muscle Fibers
Slow oxidative, muscle fibers appear red due to large numbers of capillaries and high levels of...
56.9K
Skeletal Muscle Relaxants: Therapeutic Uses
617
Skeletal muscle relaxants are used to relax muscle tone and alleviate painful muscle contractions. However, the choice of skeletal muscle relaxants depends on the duration of the surgical procedure in order to minimize potential side effects. Skeletal muscle relaxants like neuromuscular blocking agents [NMBAs] are commonly employed as adjuvants alongside general anesthetics in clinical settings. NMBAs are also used to maintain controlled ventilation during surgery of the larynx or pharynx...
617
Overview of Functional Groups
13.3K
Functional groups are a group of atoms with characteristic properties, which when linked to the carbon skeleton of a molecule, alter the properties of that molecule. For example, certain functional groups will make a molecule hydrophilic, whereas others will make them hydrophobic. These functional groups are an indispensable part of organic chemistry and important components of biological molecules, such as carbohydrates, proteins, lipids, and nucleic acids. Each functional group is a unique...
13.3K
Introduction to Functional Groups
28.8K
Functional groups are group of atoms with specific chemical properties that occur within organic molecules and sometimes denoted as “R”. Functional groups are found along the carbon backbone of macromolecules can form chains or rings of carbon atoms. Functional groups can “functionalize” a compound by enabling it to adopt different physical and chemical properties.
Types of common functional groups
The table below summarizes some of the major functional...
28.8K


