Department of Biotechnological and Applied Clinical Sciences, University of L'Aquila, L'Aquila, Italy.
European Center for Brain Research/Santa Lucia Foundation IRCCS, Rome, Italy.
Methods Mol Biol. 2023;2576:1-8. doi: 10.1007/978-1-0716-2728-0_1.
Endocannabinoids (eCBs) are endogenous lipids able to bind to cannabinoid receptors, the primary molecular targets of the cannabis (Cannabis sativa) active principle Δ-tetrahydrocannabinol. During the last 20 years, several N-acylethanolamines and acylesters have been shown to act as eCBs, and a complex array of receptors, metabolic enzymes, and transporters (that altogether form the so-called "eCB system") has been shown to finely tune their manifold biological activities. It appears now urgent to develop methods and protocols that allow to assay in a specific and quantitative manner the distinct components of the eCB system and that can properly localize them within the cell. A brief overview of eCBs and of the proteins that bind, transport, and metabolize these lipids is presented here, in orderto put in a better perspective, the relevance of methodologies that help to disclose molecular details of eCB signaling in health and disease. Proper methodological approaches form also the basis for a more rationale and effective drug design and therapeutic strategy to combat human disorders.
内源性大麻素 (eCBs) 是能够与大麻素受体结合的内源性脂质，大麻素受体是大麻（Cannabis sativa）活性成分 Δ-四氢大麻酚的主要分子靶标。在过去的 20 年中，已经证明了几种 N-酰基乙醇胺和酰基酯作为 eCBs 的作用，并且已经证明了一组复杂的受体、代谢酶和转运蛋白（共同构成所谓的“eCB 系统”）可以精细地调节它们多方面的生物学活性。现在似乎迫切需要开发方法和协议，以特定和定量的方式检测 eCB 系统的不同成分，并在细胞内对其进行适当定位。本文简要概述了 eCBs 以及结合、运输和代谢这些脂质的蛋白质，以便更好地了解有助于揭示健康和疾病中 eCB 信号分子细节的方法的相关性。适当的方法学方法也是制定更合理和有效的药物设计和治疗策略以对抗人类疾病的基础。
